ME02202B - Jedinjenja pirolopirimidina kao inhibitori cdk4/6 - Google Patents
Jedinjenja pirolopirimidina kao inhibitori cdk4/6Info
- Publication number
- ME02202B ME02202B MEP-2015-157A MEP15715A ME02202B ME 02202 B ME02202 B ME 02202B ME P15715 A MEP15715 A ME P15715A ME 02202 B ME02202 B ME 02202B
- Authority
- ME
- Montenegro
- Prior art keywords
- pyridin
- pyrrolo
- ylamino
- diaza
- cyclopentyl
- Prior art date
Links
- 101100005789 Caenorhabditis elegans cdk-4 gene Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000004944 pyrrolopyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 20
- -1 dimethylamide 7-(4-tert-Butyl-phenyl)-2-[5-(3,8-diaza-bicyclo[3.2.1]octan-3-carbonyl)-pyridin-2-ylamino]-7H-pyrrolo[2 ,3-d]pyrimidine-6-carboxylic acids Chemical class 0.000 claims 15
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical compound CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 9
- 125000001424 substituent group Chemical group 0.000 claims 9
- 201000011510 cancer Diseases 0.000 claims 7
- QKIUAMUSENSFQQ-UHFFFAOYSA-N dimethylazanide Chemical compound C[N-]C QKIUAMUSENSFQQ-UHFFFAOYSA-N 0.000 claims 6
- 238000012552 review Methods 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 230000007170 pathology Effects 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 108700020796 Oncogene Proteins 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 210000003238 esophagus Anatomy 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- PUNCJUFFXSLLLA-LPHOPBHVSA-N 2-[[5-[(3ar,6as)-4-oxo-1,2,3,3a,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]pyridin-2-yl]amino]-7-cyclopentyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C([C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCC1 PUNCJUFFXSLLLA-LPHOPBHVSA-N 0.000 claims 1
- NGJPQECPPQEKSH-YLJYHZDGSA-N 2-[[5-[(3as,6ar)-2-methyl-4-oxo-3,3a,6,6a-tetrahydro-1h-pyrrolo[3,4-c]pyrrol-5-yl]pyridin-2-yl]amino]-7-cyclopentyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C([C@@H]4CN(C)C[C@@H]4C3)=O)N=C2N1C1CCCC1 NGJPQECPPQEKSH-YLJYHZDGSA-N 0.000 claims 1
- PUNCJUFFXSLLLA-VQIMIIECSA-N 2-[[5-[(3as,6ar)-4-oxo-1,2,3,3a,6,6a-hexahydropyrrolo[3,4-c]pyrrol-5-yl]pyridin-2-yl]amino]-7-cyclopentyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C([C@@H]4CNC[C@@H]4C3)=O)N=C2N1C1CCCC1 PUNCJUFFXSLLLA-VQIMIIECSA-N 0.000 claims 1
- BXALLQBVYDONPU-ICSRJNTNSA-N 2-[[5-[(3as,7ar)-6-oxo-2,3,3a,4,7,7a-hexahydro-1h-pyrrolo[3,4-c]pyridin-5-yl]pyridin-2-yl]amino]-7-cycloheptyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(C[C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCCCC1 BXALLQBVYDONPU-ICSRJNTNSA-N 0.000 claims 1
- PXFIUPLVBBAUKD-WMZOPIPTSA-N 2-[[5-[(3as,7ar)-6-oxo-2,3,3a,4,7,7a-hexahydro-1h-pyrrolo[3,4-c]pyridin-5-yl]pyridin-2-yl]amino]-7-cyclopentyl-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(C[C@H]4CNC[C@H]4C3)=O)N=C2N1C1CCCC1 PXFIUPLVBBAUKD-WMZOPIPTSA-N 0.000 claims 1
- JFBMZUGLNFOQBA-UHFFFAOYSA-N 7-cycloheptyl-2-[[5-(2,7-diazaspiro[3.5]nonane-7-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C(=O)N(CC1)CCC21CNC2 JFBMZUGLNFOQBA-UHFFFAOYSA-N 0.000 claims 1
- KSBSIXFKBIRVML-UHFFFAOYSA-N 7-cyclohexyl-n,n-dimethyl-2-[[5-(3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(CC4CCC(N4)C3)=O)N=C2N1C1CCCCC1 KSBSIXFKBIRVML-UHFFFAOYSA-N 0.000 claims 1
- HYLVNBXAOJUSTK-UHFFFAOYSA-N 7-cyclopentyl-2-[[5-(2,6-diazaspiro[3.3]heptane-2-carbonyl)pyridin-2-yl]amino]-n,n-dimethylpyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1=C2N(C3CCCC3)C(C(=O)N(C)C)=CC2=CN=C1NC(N=C1)=CC=C1C(=O)N(C1)CC21CNC2 HYLVNBXAOJUSTK-UHFFFAOYSA-N 0.000 claims 1
- BWRSHZDVVSAUGM-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(2'-oxospiro[8-azabicyclo[3.2.1]octane-3,4'-pyrrolidine]-1'-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(CC4(C3)CC3CCC(N3)C4)=O)N=C2N1C1CCCC1 BWRSHZDVVSAUGM-UHFFFAOYSA-N 0.000 claims 1
- YCUZSIPULIEBBG-UHFFFAOYSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-(3-oxo-1,4-diazabicyclo[3.2.2]nonan-4-yl)pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound CN(C)C(=O)C1=CC2=CN=C(NC=3N=CC(=CC=3)N3C(CN4CCC3CC4)=O)N=C2N1C1CCCC1 YCUZSIPULIEBBG-UHFFFAOYSA-N 0.000 claims 1
- OHOGKSHNJOSNJQ-BGYRXZFFSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(1r,5s)-3-oxa-7,9-diazabicyclo[3.3.1]nonane-9-carbonyl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound N1([C@]2([H])CNC[C@]1(COC2)[H])C(=O)C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 OHOGKSHNJOSNJQ-BGYRXZFFSA-N 0.000 claims 1
- FIMQVRFSGKERNW-PZJWPPBQSA-N 7-cyclopentyl-n,n-dimethyl-2-[[5-[(1s,6r)-9-methyl-3-oxo-4,9-diazabicyclo[4.2.1]nonan-4-yl]pyridin-2-yl]amino]pyrrolo[2,3-d]pyrimidine-6-carboxamide Chemical compound C([C@@]1(CC[C@](C2)(N1C)[H])[H])C(=O)N2C(C=N1)=CC=C1NC(N=C12)=NC=C1C=C(C(=O)N(C)C)N2C1CCCC1 FIMQVRFSGKERNW-PZJWPPBQSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 206010016935 Follicular thyroid cancer Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 206010023347 Keratoacanthoma Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 201000000582 Retinoblastoma Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 201000006083 Xeroderma Pigmentosum Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000001413 cellular effect Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 238000012512 characterization method Methods 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000002615 epidermis Anatomy 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 201000000497 familial melanoma Diseases 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 230000001900 immune effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- MGJXBDMLVWIYOQ-UHFFFAOYSA-N methylazanide Chemical compound [NH-]C MGJXBDMLVWIYOQ-UHFFFAOYSA-N 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 210000001331 nose Anatomy 0.000 claims 1
- TVMXDCGIABBOFY-UHFFFAOYSA-N octane Chemical compound CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000001696 purinergic effect Effects 0.000 claims 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- HKSQZEGSMBFHGC-UHFFFAOYSA-N pyrimidine-4-carboxamide Chemical compound NC(=O)C1=CC=NC=N1 HKSQZEGSMBFHGC-UHFFFAOYSA-N 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 238000001356 surgical procedure Methods 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 210000002105 tongue Anatomy 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Saccharide Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (25)
1. Jedinjenje prema formuli (I)naznačen time, što:R1 predstavlja C3-7alkil; C4-7 cikloalkil po slobodnom izboru supstituisan sa jednim ili više supstituenta koji su odabrani iz grupe koju čine C1-6alkil i OH; fenil po slobodnom izboru supstituisan jednim supstitutentom koji je odabran iz grupe koju čine C1-6 alkil, C(CH3)2CN, i OH; piperidinil po slobodnom izboru supstituisan sa jednom ciklopropil grupom ili C1-6 alkilom; tetrahidropiranil po slobodnom izboru supstituisan sa jednom ciklopropil grupom ili C1-6 alkilom; ili biciklo[2.2.1]heptanil;gde A predstavlja CH ili N;gde R11 predstavlja vodonik ili C1-4 alkil;gde L predstavlja vezu, C(O), ili S(O)2;gde R2Y može da bude izabran iz grupe koju čineV je NH ili CH2;X je O ili CH2;W je O ili NH;gde m i n svaki za sebe predstavljaju 1, 2, ili 3 pod uslovom da m i n nisu oba 3;gde je svaka R2Y po slobodnom izboru supstituisana sa jednim do četiri supstituenata od kojih je svaki nezavisno odabran iz grupe koju čine: C1-3 alkil po slobodnom izboru substituisan sa jednim ili dva supstituenta od kojih je svaki nezavisno odabran iz grupe koju čine hidroksi, NH2, i -S-C1-3alkil; CD3; halo; okso; C1-3 haloalkil; hidroksi; NH2; dimetilamino; benzil; -C(O)-C1-3alkil po slobodnom izboru supstituisan sa jednim ili dva supstituenta od kojih je svaki odabran iz grupe koju čine NH2’ -SCH3 i NHC(O)CH3; - S(O)2-C1-4 alkil; i pirolidinil-C(O)-;gde R4 predstavlja, vodonik, deuterijum, ili C(R5)(R6)(R7); igde R5, R6, R7, R8, R9 i R10 svaki za sebe nezavisno predstavljaju H ili deuterijum; ili njena farmaceutski prihvatljiva so.
2.Jedinjenje formule (I-B) prema patentnom zahtevu 1, naznačen time, što L predstavlja vezu ili C(O); gde R2Y može da bude izabran iz grupe koju čine V je NH ili CH2; X je O ili CH2; W je O ili NH; gde m i n svaki za sebe nezavisno mogu da budu 1, 2, ili 3 pod uslovom da m i n m i n nisu oba 3; gde je svaka R2Y po slobodnom izboru supstituisana sa jednim do četiri supstituenata od kojih je svaki odabran iz grupe koju čine: C1-3 alkil po slobodnom izboru substituisan sa jednim ili dva supstituenta od kojih je svaki nezavisno odabran iz grupe koju čine hidroksi, NH2, i -S-C1-3alkil; CD3; C1-3 haloalkil; hidroksi; NH2; dimetilamino; benzil; -C(O)-C1-3alkil po slobodnom izboru supstituisan sa jednim ili dva supstituenta od kojih je svaki odabran iz grupe koju čine NH2’ -SCH3 i NHC(O)CH3; - S(O)2-C1-4 alkil; i pirolidinil-C(O)-; ili njena farmaceutski prihvatljiva so.
3. Jedinjenje prema bilo kojem od predhodnih patentnih zahteva, naznačen time, što A predstavlja CH i R11 je vodonik; ili njena farmaceutski prihvatljiva so.
4. Jedinjenje prema bilo kojem od predhodnih patentnih zahteva, naznačen time, što R4 predstavlja C(R5)(R6)(R7) i R5, R6, R7, R8, R9 i R10 mogu da predstavljaju vodonik, ili njenu farmaceutski prihvatljivu so.
5. Jedinjenje prema bilo kojem od predhodnih patentnih zahteva, naznačen time, što R1 predstavlja C4-7 cikloalkil koji je po slobodnom izboru supstituisan jednom C1-6 alkil grupom, ili njena farmaceutski prihvatljiva so.
6. Jedinjenje prema bilo kojem od predhodnih patentnih zahteva, naznačen time, što je R2Y nesupstituisana ili njena farmaceutski prihvatljiva so.
7. Jedinjenje prema bilo kojem od patentnih zahteva 1-5 naznačen time, što R2Y predstavlja ili od kojih je bilo koja po slobodnom izboru supstituisana C1-3alkilom, ili njena farmaceutski prihvatljiva so.
8. Jedinjenje prema bilo kojem od patentnih zahteva 1-5 naznačen time, što R2Y predstavlja koja je po slobodnom izboru supstituisana C1-3 alkilom, ili njena farmaceutski prihvatljiva so.
9. Jedinjenje formule (I-C) u kojoj: R1 predstavlja ciklobutil, ciklopentil, cikloheksil, cikloheptil, gde je svaka od njih po slobodnom izboru supstituisana sa jednom metil,etil, ili OH; gde A predstavlja CH ili N; L može da predstavlja vezu, -C(O)-, ili S(O)2-; gde R2Y može da bude jedna iz grupe koju čine ili gde je svaka R2Y po slobodnom izboru supstituisana jednim ili dva supstituenta koji su nezavisno odabrani iz grupe koju čine halogen, metil, etil, ili okso; gde V predstavlja NH ili CH2; gde R4 predstavlja vodonik, deuterijum, ili C(R5)(R6)(R7); i R5, R6, R7, R8, R9 i R10 svaki za sebe nezavisno predstavljaju H ili deuterijum; ili njena ili njena farmaceutski prihvatljiva so.
10. Jedinjenje prema patentnom zahtevu 9, naznačen time, što A predstavlja CH; ili njena farmaceutski prihvatljiva so.
11. Jedinjenje prema patentnom zahtevu 10 naznačen time, što L predstavlja vezu ili -C(O)- i gde R4 predstavlja CH3; i R8, R9 i R10 mogu da budu H; ili njena farmaceutski prihvatljiva so.
12. Jedinjenje prema patentnom zahtevu 11 naznačen time, što R1 predstavlja ciklopentil; ili njena farmaceutski prihvatljiva so.
13. Jedinjenje prema patentnom zahtevu 1, naznačen time, što može biti odabrano iz grupe koju čine: 2-(5-(2,6-Diazaspiro[3.3]heptan-2-karbonil)piridin-2-ilamino)-7-ciklopentil-N,N-dimetil-7H-pirolo[2,3-d]pirimidin-6-karboksamid; dimetilamid 7-(4-terc-Butil-fenil)-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6- karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-((1R,6S)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6- karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Cikloheptil-2-[5-(2,5-diaza-biciklo[2.2.1]heptan-2-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-8-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; 2-(5-(2,7-diazaspiro[3.5]nonan-7-karbonil)piridin-2-ilamino)-7-cikloheptil-N,N-dimetil-7H-pirolo[2,3-d]pirimidin-6-karboksamid; dimetilamid 7-ciklopentil-2-[5-(8-metil-3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; metilamid 7-Ciklopentil-2-[5-((S,S)-2,5-diaza-biciklo[2.2.1]heptan-2-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-(3-terc-Butil-fenil)-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; 2-(5-((1R,5S)-3-oksa-7,9-diazabiciklo[3.3.1]nonan-9-karbonil)piridin-2-ilamino)-7-ciklopentil-N,N-dimetil-7H-pirolo[2,3-d]pirimidin-6-karboksamid; dimetilamid 7-[4-(Cijano-dimetil-metil)-fenil]-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-8-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-((1S,6R)-3,9-diaza-biciklo[4.2.1]nonan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-((1R,6S)-3,9-diaza-biciklo[4.2.1]nonan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(3,6-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; 7-ciklopentil-N,N-dimetil-2-(5-(5’-okso-8-azaspiro[biciklo[3.2.1]oktan-3,3’-pirolidin]-1’-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; dimetilamid 7-Ciklopentil-2[5-(1-okso-heksahidro-pirolo[1,2-a]pirazin-2-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; 7-ciklopentil-N,N-dimetil-2-(5-(2-okso-1-oksa-3,8-diazaspiro[4.5]dekan-3-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; dimetilamid 7-Ciklopentil-2-[5-((1S,6R)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 2-[5-(4-Okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7-fenil-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; i 7-cikloheksil-N,N-dimetil-2-(5-(4-okso-3,9-diazabiciklo[4.2.1]nonan-3-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; ili njena farmaceutski prihvatljiva so.
14. Jedinjenje prema patentnom zahtevu 1, naznačen time, što može biti odabrano iz grupe koju čine: dimetilamid 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline dimetilamid 7-Ciklopentil-2-[5-((S,S)-2,5-diaza-biciklo[2.2.1]heptan-2-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6- karboksilne kiseline dimetilamid 7-Ciklopentil-2-[5-((1R,6S)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline dimetilamid 7-Ciklopentil-2-[5-((1S,5S)-3,6-diaza-biciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklobutil-2-[5-((1S,6R)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline dimetilamid 7-Cikloheksil-2-[5-((1R,6S)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)- piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline dimetilamid 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-6-metil-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(3,8-diaza-biciklo[3.2.1]oktan-3-karbonil)-4-metil-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; dimetilamid 7-Ciklopentil-2-[5-(3,9-diaza-biciklo[3.3.1]nonan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; 7-ciklopentil-N,N-dimetil-2-(5-(3-okso-1,4-diazabiciklo[3.2.2]nonan-4-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-((1R,6S)-9-metil-4-okso-3,9-diazabiciklo[4.2.1]nonan -3-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-((3aS,6aR)-1-oksoheksahidropirolo[3,4-c]pirol-2(1H)-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-((3aR,6aS)-1-oksoheksahidropirolo[3,4-c]pirol-2(1H)-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-cikloheptil-N,N-dimetil-2-(5-(cis-6-oksotetrahidro-1H-pirolo[3,4-c]piridin-5(6H,7H,7aH)-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-(cis-6-oksotetrahidro-1H-pirolo[3,4-c]piridin-5(6H,7H,7aH)-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-((3aR,6aS)-5-metil-1-oksoheksahidropirolo[3,4-c]pirol-2(1H)-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-((1R,3r,5S)-2’-okso-8-azaspiro[biciklo[3.2.1]oktan-3,5’-oksazolidin]-3’-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-(2-okso-1-oksa-3,8-diazaspiro[4.6]undekan-3-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamid; 7-ciklopentil-N,N-dimetil-2-(5-(2-okso-1-oksa-3,7-diazaspiro[4.5]dekan-3-il)piridin-2-ilamino)-7H-pirolo[2,3-d]pirimidin-6-karboksamide; dimetilamid 7-Ciklopentil-2-[5-((S)-2-okso-1-oksa-3,7-diaza-spiro[4.5]dec-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; i dimetilamid 7-Ciklopentil-2-[5-((R)-2-okso-1-oksa-3,7-diaza-spiro[4.5]dec-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline; ili njena farmaceutski prihvatljiva so.
15. Jedinjenje prema patentnom zahtevu 1, naznačen time, što 7-ciklopentil-N,N-dimetil-2-(5-((1R,6S)-9-metil-4-okso-3,9-diazabiciklo[4.2.1]nonan-3-il)piridin-2-ilamino)-7H-pirolo[2,32,3-d]pirimidin-6-karboksamid ima sledeću formulu: ili njena farmaceutski prihvatljiva so.
16. Jedinjenje prema patentnom zahtevu 1, naznačen time, što dimetilamid 7-Ciklopentil-2-[5-(3,8-diazabiciklo[3.2.1]oktan-3-karbonil)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline ima sledeću formulu: ili njena farmaceutski prihvatljiva so.
17. Jedinjenje prema patentnom zahtevu 1, naznačen time, što dimetilamid 7-Ciklopentil-2-[5-((1R,6S)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline ima sledeću formulu ili njena farmaceutski prihvatljiva so.
18. Jedinjenje prema patentnom zahtevu 1, naznačen time, što metilamid 7-Ciklopentil-2-[5-((1R,6S)-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6-karboksilne kiseline ima sledeću formulu: ili njena farmaceutski prihvatljiva so.
19. Jedinjenje prema patentnom zahtevu 1, naznačen time, što metilamid 7-ciklopentil-2-[5-((1R,6S)-9-metil-4-okso-3,9-diaza-biciklo[4.2.1]non-3-il)-piridin-2-ilamino]-7H-pirolo[2,3-d]pirimidin-6- karboksilne kiseline ima sledeću formulu: ili njena farmaceutski prihvatljiva so.
20. Farmaceutska kompozicija koja obuhvata jedinjenje prema bilo kojem od predhodnih patentnih zahteva, ili njena farmaceutski prihvatljiva so, i farmaceutski prihvatljivi nosač ili ekscipijent.
21. Jedinjenje prema patentnom zahtevu 1 ili 9, za upotrebu u medicini.
22. .Jedinjenje prema patentnom zahtevu 1 ili 9, za upotrebu u lečenju raka.
23. Jedinjenje prema patentnom zahtevu 1 ili 9, za upotrebu u lečenju raka, naznačen time, što je odabrano iz grupe koju čine: mantle ćelijski limfom, multipli mijelom, rak dojke, ezofagealni kancer skvamoznih ćelija, liposarkom, T-ćelijski limfom, melanom, nesitnoćelijski rak pluća i rak pankreasa, folikularni karcinom štitaste žlezde, tumor mezenhimalnog porekla, fibrosarkom, rabdomiosarkom, tumor centralnog ili perifernog nervnog sistema, astrocitom, neuroblastom, gliom, švanom, melanom, seminom, teratokarcinom, osteosarkom, kseroderma pigmentozum, retinoblastom, keratoakatantom, i Kapošijev sarkom, karcinom bešike, dojke, debelog creva, bubrega, epidermis, jetre, pluća, ezofagusa (jednjaka), žučne kese, karcinom jajnika, pankreasa, stomaka, cerviksa, štitne žlezde, nosa, glave i jezika, prostate, i kože, leukemija, akutna limfocitna leukaemija, hronična limfocitna leukaemija, B-ćelijski limfom, difuzni krupnoćelijski B limfom, T-ćelijski limfom, Hodžkinov limfom, ne Hodžkinov limfom, limfom vlasastih ćelija, i Burkitov limfom, glioblastom multiforme, T ćelijski ALL, sarkomi i familijarni melanom.
24. Upotreba jedinjenja prema patentnom zahtevu 1 u proizvodnji leka za lečenje raka.
25. Jedinjenje formule (I) prema patentnom zahtevu 1, ili njena farmaceutski prihvatljiva so u kombinaciji sa jednim ili više drugih terapijskih sredstava za simultanu, odvojenu ili sekvencijalnu upotrebu u terapiji. EP 2 536 730 B1 REFERENCE KOJE SU NAVEDENE U OPISU Popis literature od strane podnosioca služi samo kao priručnik za čitaoca. Priručnik nije deo Evropske patent dokumentacije. Iako se posvećuje velika pažnja prevodu referenci, greške i propusti ne mogu biti izuzeti i EPO se odriče svake odgovornosti u tom smislu • WO 2007140222 A [0006] • WO 2009085185 A [0006] • WO 2008135232 A [0006] • US 20090203688 A [0006] • WO 2010020675 A [0134] [0267] [0274] • WO 2009067108 W [0260] • WO 2005097791 W [0279] • WO 2007040282 A [0303] • WO 2006137769 W [0362] • DE 102005030051 A1 [0638] [0650] [0670] Nepatentna literatura koja je navedena u opisu: • ORTEGA et al. Biochimica et Biophysica Acta-Reviews on Cancer, 2002, vol. 1602 (1), 73-87 [0002] [0003] [0004] • SHAPIRO. Journal of Clinical Oncology, 2006, vol. 24 (11), 1770-1783 [0002] [0003] • LUNDBERG et al. Molecular and Cellular Biology, 1998, vol. 18 (2), 753-761 [0002] • KAMB et al. Science, 1994, vol. 264 (5157), 436-440 [0002] [0004] • SHERR et al. Genes & Development, vol. 13 (12), 1501-1512 [0002] • AMIN et al. Archives of Pathology & Laboratory Medicine, 2003, vol. 127 (4), 424-431 [0003] • OUDAT et al. Modern Pathology, 2001, vol. 14 (1), 175A [0003] • BERGSAGEL et al. Immunological Reviews, 2003, vol. 194 (1), 96-104 [0003] • JIANG et al. Cancer Research, 1992, vol. 52 (10), 2980-2983 [0004] • AMOLD et al. Journal of Clinical Oncology, 2005 [0004] • SIRVENT et al. American Journal of Surgical Pathology, 2007, vol. 31 (10), 1476-1489 [0004] • BRAMBILLA et al. Journal of Pathology, 1999, vol. 188 (4), 351-360 [0004] • COWGILL et al. American Journal of Surgery, 2003, vol. 186 (3), 279-286 [0004] • GAZZERI et al. Oncogene, 1998, vol. 16 (4), 497-504 [0004] • DAILEY et al. Cytokine & Growth Factor Reviews, 2005, vol. 16 (2), 233-247 [0005] • ENGELMAN. Nature Reviews Cancer, 2009, vol. 9 (8), 550-562 [0005] • GARCIA-ECHEVERRIA. Purinergic Signalling, 2009, vol. 5 (1), 117-125 [0005] • GRAY-SCHOPFER et al. Cancer and Metastesis Reviews, 2005, vol. 24 (1), 165-183 [0005] • JOHN et al. Oncogene, 2009, vol. 28, S14-S23 [0005] • SHARMA et al. Nature Reviews Cancer, 2007, vol. 7 (3), 169-181 [0005] • MORIARTY K.J. et al. Bioorg Med Chem Lett, 2006, vol. 16, 5778-5783 [0006] • Remington’s Pharmaceutical Sciences. Mack Publishing Company, 1985 [0053] • STAHL; WERMUTH. Handbook of Pharmaceutical Salts: Properties, Selection, and Use. Wiley-VCH, 2002 [0053] • GREEN ; WUTTS. Protective Groups in Organic Synthesis [0114] • AMIN, H. M. ; MCDONNELL, T. J. ; MEDEIROS, L. J. ; RASSIDAKIS, G. Z. ; LEVENTAKI, V.; ; O’CONNOR, S. L. ; KEATING, M. J. ; LAI, R. Characterization of 4 mantle cell lymphoma cell lines – Establishment of an in vitro study model. Arch. Pathol. Lab. Med., 2003, vol. 127, 424-431 [0886]
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30624810P | 2010-02-19 | 2010-02-19 | |
| US201161429372P | 2011-01-03 | 2011-01-03 | |
| US201161429997P | 2011-01-05 | 2011-01-05 | |
| PCT/EP2011/052353 WO2011101409A1 (en) | 2010-02-19 | 2011-02-17 | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
| EP11707115.9A EP2536730B1 (en) | 2010-02-19 | 2011-02-17 | Pyrrolopyrimidine compounds as inhibitors of cdk4/6 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02202B true ME02202B (me) | 2016-02-20 |
Family
ID=44201966
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2015-157A ME02202B (me) | 2010-02-19 | 2011-02-17 | Jedinjenja pirolopirimidina kao inhibitori cdk4/6 |
Country Status (38)
| Country | Link |
|---|---|
| US (2) | US8957074B2 (me) |
| EP (1) | EP2536730B1 (me) |
| JP (1) | JP5788415B2 (me) |
| KR (1) | KR101812357B1 (me) |
| CN (1) | CN102918043B (me) |
| AR (1) | AR080198A1 (me) |
| AU (1) | AU2011217286B2 (me) |
| BR (1) | BR112012020922B1 (me) |
| CA (1) | CA2790637C (me) |
| CL (1) | CL2012002270A1 (me) |
| DK (1) | DK2536730T3 (me) |
| DO (1) | DOP2012000225A (me) |
| EA (1) | EA022355B1 (me) |
| EC (1) | ECSP12012111A (me) |
| ES (1) | ES2548532T3 (me) |
| GE (1) | GEP20146146B (me) |
| HN (1) | HN2012001744A (me) |
| HR (1) | HRP20151071T1 (me) |
| IL (1) | IL221520A (me) |
| MA (1) | MA34066B1 (me) |
| ME (1) | ME02202B (me) |
| MX (1) | MX2012009613A (me) |
| NI (1) | NI201200135A (me) |
| NZ (1) | NZ601754A (me) |
| PE (1) | PE20121815A1 (me) |
| PH (1) | PH12012501649A1 (me) |
| PL (1) | PL2536730T3 (me) |
| PT (1) | PT2536730E (me) |
| RS (1) | RS54263B1 (me) |
| SG (1) | SG183218A1 (me) |
| SI (1) | SI2536730T1 (me) |
| SM (1) | SMT201500265B (me) |
| TN (1) | TN2012000413A1 (me) |
| TW (1) | TWI503322B (me) |
| UA (1) | UA108369C2 (me) |
| UY (1) | UY33227A (me) |
| WO (1) | WO2011101409A1 (me) |
| ZA (1) | ZA201206079B (me) |
Families Citing this family (161)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL1879573T3 (pl) | 2005-05-10 | 2013-05-31 | Incyte Holdings Corp | Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania |
| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| PL2315756T3 (pl) | 2008-07-08 | 2015-02-27 | Incyte Holdings Corp | 1,2,5-oksadiazole jako inhibitory 2,3-dioksygenazy indoloaminy |
| ES2522346T3 (es) | 2008-08-22 | 2014-11-14 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de CDK |
| CN103002911B (zh) | 2008-09-26 | 2015-08-26 | 昂考梅德药品有限公司 | 卷曲蛋白结合药剂及其应用 |
| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Wnt拮抗劑及治療和篩選方法 |
| CA2794674A1 (en) | 2010-04-01 | 2011-10-06 | Oncomed Pharmaceuticals, Inc. | Frizzled-binding agents and uses thereof |
| WO2011130232A1 (en) * | 2010-04-13 | 2011-10-20 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor and an mtor inhibitor for treating cancer |
| US8691830B2 (en) | 2010-10-25 | 2014-04-08 | G1 Therapeutics, Inc. | CDK inhibitors |
| US8501768B2 (en) * | 2011-05-17 | 2013-08-06 | Hoffmann-La Roche Inc. | Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds |
| CN103635189B (zh) | 2011-07-01 | 2016-05-04 | 诺华股份有限公司 | 用于治疗癌症的含有cdk4/6抑制剂和pi3k抑制剂的联合治疗 |
| JP2015502958A (ja) * | 2011-12-09 | 2015-01-29 | オンコメッド ファーマシューティカルズ インコーポレイテッド | がんの処置のための併用療法 |
| AU2013239816B2 (en) | 2012-03-29 | 2017-08-24 | G1 Therapeutics, Inc. | Lactam kinase inhibitors |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| SMT202100451T1 (it) | 2012-07-11 | 2021-09-14 | Blueprint Medicines Corp | Inibitori del recettore di crescita dei fibroblasti |
| WO2014022830A2 (en) | 2012-08-03 | 2014-02-06 | Foundation Medicine, Inc. | Human papilloma virus as predictor of cancer prognosis |
| WO2014066328A1 (en) | 2012-10-23 | 2014-05-01 | Oncomed Pharmaceuticals, Inc. | Methods of treating neuroendocrine tumors using wnt pathway-binding agents |
| EA032649B1 (ru) | 2013-01-29 | 2019-06-28 | Аптиникс Инк. | Спиролактамные модуляторы nmda-рецептора и их применение |
| JP2016510411A (ja) | 2013-02-04 | 2016-04-07 | オンコメッド ファーマシューティカルズ インコーポレイテッド | Wnt経路インヒビターによる処置の方法およびモニタリング |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| TW201444849A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代的7-氮雜雙環類及其作為食慾激素受體調節劑之用途 |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| DK2968290T3 (da) | 2013-03-15 | 2019-11-25 | G1 Therapeutics Inc | Transient beskyttelse af normale celler under kemoterapi |
| HK1222766A1 (zh) | 2013-03-15 | 2017-07-14 | G1治疗公司 | 高效的抗赘生剂和抗增生剂 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| KR102529049B1 (ko) | 2013-08-14 | 2023-05-08 | 노파르티스 아게 | 암의 치료를 위한 조합 요법 |
| CA2928042C (en) | 2013-10-25 | 2022-05-10 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| SG10201900002QA (en) | 2014-01-24 | 2019-02-27 | Dana Farber Cancer Institue Inc | Antibody molecules to pd-1 and uses thereof |
| EP3099717B1 (en) | 2014-01-31 | 2019-03-27 | Novartis AG | Antibody molecules to tim-3 and uses thereof |
| US20150259420A1 (en) | 2014-03-14 | 2015-09-17 | Novartis Ag | Antibody molecules to lag-3 and uses thereof |
| US20150320754A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2015161285A1 (en) | 2014-04-17 | 2015-10-22 | G1 Therapeutics, Inc. | Tricyclic lactams for use in the protection of hematopoietic stem and progenitor cells against ionizing radiation |
| RU2671494C2 (ru) * | 2014-05-28 | 2018-11-01 | Шанхай Фокон Фармасьютикал Ко., Лтд | Некоторые ингибиторы протеинкиназы |
| CN105294737B (zh) * | 2014-07-26 | 2019-02-12 | 广东东阳光药业有限公司 | Cdk类小分子抑制剂的化合物及其用途 |
| AU2015314851B2 (en) * | 2014-09-11 | 2020-01-02 | Janssen Pharmaceutica Nv | Substituted 2-azabicycles and their use as orexin receptor modulators |
| WO2016040858A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
| TWI716362B (zh) | 2014-10-14 | 2021-01-21 | 瑞士商諾華公司 | 針對pd-l1之抗體分子及其用途 |
| CN105111201B (zh) * | 2014-10-16 | 2017-01-11 | 上海页岩科技有限公司 | 5-甲基-2-(吡啶-2-基氨基)-8H-吡啶并[2,3-d]嘧啶-7-酮化合物 |
| WO2016100882A1 (en) | 2014-12-19 | 2016-06-23 | Novartis Ag | Combination therapies |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| HK1248603A1 (zh) | 2015-03-10 | 2018-10-19 | Aduro Biotech, Inc. | 用於活化"干扰素基因的刺激剂"依懒性信号传导的组合物和方法 |
| US9969719B2 (en) * | 2015-03-11 | 2018-05-15 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Substituted 2-hydrogen-pyrazole derivative serving as anticancer drug |
| DK3317301T3 (da) | 2015-07-29 | 2021-06-28 | Immutep Sas | Kombinationsterapier omfattende antistofmolekyler mod lag-3 |
| US20180222982A1 (en) | 2015-07-29 | 2018-08-09 | Novartis Ag | Combination therapies comprising antibody molecules to pd-1 |
| EP3878465A1 (en) | 2015-07-29 | 2021-09-15 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
| EP3370768B9 (en) | 2015-11-03 | 2022-03-16 | Janssen Biotech, Inc. | Antibodies specifically binding pd-1 and their uses |
| CN106810536A (zh) | 2015-11-30 | 2017-06-09 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| JP7011596B2 (ja) * | 2015-12-02 | 2022-02-10 | アストライア セラピューティクス, エルエルシー | ピペリジニルノシセプチン受容体化合物 |
| US10112924B2 (en) | 2015-12-02 | 2018-10-30 | Astraea Therapeutics, Inc. | Piperdinyl nociceptin receptor compounds |
| WO2017106656A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
| WO2017161253A1 (en) | 2016-03-18 | 2017-09-21 | Tufts Medical Center | Compositions and methods for treating and preventing metabolic disorders |
| US10449195B2 (en) | 2016-03-29 | 2019-10-22 | Shenzhen Pharmacin Co., Ltd. | Pharmaceutical formulation of palbociclib and a preparation method thereof |
| US10835535B2 (en) * | 2016-05-07 | 2020-11-17 | Shanghai Fochon Pharmaceutical Co., Ltd. | Certain protein kinase inhibitors |
| WO2018005863A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Pyrimidine-based compounds for the treatment of cancer |
| EP3858835A1 (en) | 2016-07-01 | 2021-08-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018005533A1 (en) | 2016-07-01 | 2018-01-04 | G1 Therapeutics, Inc. | Antiproliferative pyrimidine-based compounds |
| WO2018009466A1 (en) | 2016-07-05 | 2018-01-11 | Aduro Biotech, Inc. | Locked nucleic acid cyclic dinucleotide compounds and uses thereof |
| SG10202101055VA (en) * | 2016-08-01 | 2021-03-30 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| MX385336B (es) | 2016-08-01 | 2025-03-18 | Aptinyx Inc | Moduladores del receptor nmda espiro-lactam y uso de los mismos. |
| JP2019527232A (ja) | 2016-08-01 | 2019-09-26 | アプティニックス インコーポレイテッド | スピロ−ラクタムnmda修飾因子及びこれを用いた方法 |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| CA3040815C (en) | 2016-10-20 | 2021-07-20 | Steven Martin Evans | Anti-proliferative agents for treating pah |
| WO2018081211A1 (en) * | 2016-10-26 | 2018-05-03 | Li George Y | Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide |
| AU2017359333B2 (en) | 2016-11-08 | 2024-03-21 | Dana-Farber Cancer Institute, Inc. | Compositions and methods of modulating anti-tumor immunity |
| EP3556758B1 (en) | 2016-12-16 | 2024-07-17 | Cstone Pharmaceuticals (Suzhou) Co., Ltd. | 1,2-dihydro-1,6-naphthyridin-2-one derivatives as cdk4/6 inhibitors |
| EP3565558B1 (en) | 2017-01-06 | 2023-12-06 | G1 Therapeutics, Inc. | Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer |
| UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
| CN108794452B (zh) | 2017-05-05 | 2021-05-28 | 上海时莱生物技术有限公司 | 具有激酶抑制活性的化合物、其制备方法和用途 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | Antibody molecules to cd73 and uses thereof |
| FI3645001T3 (fi) | 2017-06-29 | 2024-09-25 | G1 Therapeutics Inc | Git38:n morfisia muotoja ja niiden valmistusmenetelmiä |
| EP3728228A1 (en) | 2017-12-22 | 2020-10-28 | Ravenna Pharmaceuticals, Inc. | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
| MX2020007312A (es) | 2018-01-08 | 2021-01-08 | G1 Therapeutics Inc | Regimenes de dosificacion superior de g1t38. |
| US12398209B2 (en) | 2018-01-22 | 2025-08-26 | Janssen Biotech, Inc. | Methods of treating cancers with antagonistic anti-PD-1 antibodies |
| CN112204031B (zh) | 2018-01-31 | 2024-05-24 | 元羿生物科技(香港)有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| WO2019161224A1 (en) * | 2018-02-15 | 2019-08-22 | GiraFpharma LLC | Heterocyclic compounds as kinase inhibitors |
| BR122023024273A2 (pt) | 2018-02-27 | 2024-02-20 | Incyte Corporation | Compostos imidazopirimidinas e triazolopirimidinas, seus usos, método para inibir uma atividade de um receptor de adenosina e composição farmacêutica dos mesmos |
| WO2019178239A1 (en) * | 2018-03-13 | 2019-09-19 | Board Of Regents, The University Of Texas System | Methods for treatment of cancers with egfr activating mutations |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| WO2019222677A1 (en) | 2018-05-18 | 2019-11-21 | Incyte Corporation | Fused pyrimidine derivatives as a2a / a2b inhibitors |
| AR126019A1 (es) | 2018-05-30 | 2023-09-06 | Novartis Ag | Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación |
| GEP20237548B (en) | 2018-07-05 | 2023-10-10 | Incyte Corp | Fused pyrazine derivatives as a2a /a2b inhibitors |
| RS67557B1 (sr) | 2018-08-24 | 2026-01-30 | Pharmacosmos Holding As | Unapređena sinteza 1,4-diazaspiro[5.5]undekan-3-ona |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| CA3154278A1 (en) * | 2018-10-12 | 2020-04-16 | Corey Hopkins | Phosphodiesterase inhibitors |
| CN111100128B (zh) * | 2018-10-26 | 2022-09-06 | 广安凯特制药有限公司 | 一种瑞博西尼中间产品的合成方法及其中间体化合物 |
| EP3902805A4 (en) * | 2018-12-28 | 2023-03-01 | SPV Therapeutics Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| TWI829857B (zh) | 2019-01-29 | 2024-01-21 | 美商英塞特公司 | 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶 |
| US20200316064A1 (en) | 2019-02-15 | 2020-10-08 | Incyte Corporation | Cyclin-dependent kinase 2 biomarkers and uses thereof |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| WO2020180959A1 (en) | 2019-03-05 | 2020-09-10 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| MX2021013531A (es) | 2019-05-05 | 2022-02-11 | Qilu Regor Therapeutics Inc | Inhibidores de cdk. |
| TW202112767A (zh) | 2019-06-17 | 2021-04-01 | 美商佩特拉製藥公司 | 作為磷脂酸肌醇磷酸激酶抑制劑之胺基吡啶衍生物 |
| CN112094272A (zh) | 2019-06-18 | 2020-12-18 | 北京睿熙生物科技有限公司 | Cdk激酶抑制剂 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4007602A1 (en) | 2019-08-01 | 2022-06-08 | Incyte Corporation | A dosing regimen for an ido inhibitor |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| US20220348651A1 (en) | 2019-09-18 | 2022-11-03 | Novartis Ag | Entpd2 antibodies, combination therapies, and methods of using the antibodies and combination therapies |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為fgfr抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| CA3179692A1 (en) | 2020-04-16 | 2021-10-21 | Incyte Corporation | Fused tricyclic kras inhibitors |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| ES3048084T3 (en) | 2020-05-19 | 2025-12-09 | Pharmacosmos Holding As | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| US10988479B1 (en) | 2020-06-15 | 2021-04-27 | G1 Therapeutics, Inc. | Morphic forms of trilaciclib and methods of manufacture thereof |
| US11999752B2 (en) | 2020-08-28 | 2024-06-04 | Incyte Corporation | Vinyl imidazole compounds as inhibitors of KRAS |
| CN114306245A (zh) | 2020-09-29 | 2022-04-12 | 深圳市药欣生物科技有限公司 | 无定形固体分散体的药物组合物及其制备方法 |
| WO2022072783A1 (en) | 2020-10-02 | 2022-04-07 | Incyte Corporation | Bicyclic dione compounds as inhibitors of kras |
| CN112375081B (zh) * | 2020-11-23 | 2022-04-12 | 中国医学科学院医药生物技术研究所 | 具有抑制CDK4、6或9活性的吡咯[2,3-d]嘧啶衍生物及其制备方法和应用 |
| WO2022113003A1 (en) | 2020-11-27 | 2022-06-02 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022155941A1 (en) | 2021-01-25 | 2022-07-28 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors |
| WO2022206888A1 (en) | 2021-03-31 | 2022-10-06 | Qilu Regor Therapeutics Inc. | Cdk2 inhibitors and use thereof |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| MX2024000357A (es) | 2021-07-07 | 2024-02-12 | Incyte Corp | Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras). |
| US12600717B2 (en) | 2021-07-14 | 2026-04-14 | Incyte Corporation | Tricyclic compounds as inhibitors of KRAS |
| WO2023009438A1 (en) | 2021-07-26 | 2023-02-02 | Celcuity Inc. | 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (gedatolisib) and its combinations for use in the treatment of cancer |
| US12441742B2 (en) | 2021-08-31 | 2025-10-14 | Incyte Corporation | Naphthyridine compounds as inhibitors of KRAS |
| WO2023036252A1 (zh) * | 2021-09-08 | 2023-03-16 | 希格生科(深圳)有限公司 | 吡咯并嘧啶类或吡咯并吡啶类衍生物及其医药用途 |
| WO2023049697A1 (en) | 2021-09-21 | 2023-03-30 | Incyte Corporation | Hetero-tricyclic compounds as inhibitors of kras |
| CA3234375A1 (en) | 2021-10-01 | 2023-04-06 | Incyte Corporation | Pyrazoloquinoline kras inhibitors |
| WO2023064857A1 (en) | 2021-10-14 | 2023-04-20 | Incyte Corporation | Quinoline compounds as inhibitors of kras |
| WO2023091746A1 (en) | 2021-11-22 | 2023-05-25 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a kras inhibitor |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ck12抑制劑 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| CA3244187A1 (en) | 2021-12-22 | 2023-06-29 | Incyte Corporation | SALTS AND SOLID FORMS OF AN FGFR INHIBITOR AND THEIR METHODS OF PREPARATION |
| WO2023168686A1 (en) | 2022-03-11 | 2023-09-14 | Qilu Regor Therapeutics Inc. | Substituted cyclopentanes as cdk2 inhibitors |
| TW202341982A (zh) | 2021-12-24 | 2023-11-01 | 大陸商上海齊魯銳格醫藥研發有限公司 | Cdk2抑制劑及其用途 |
| EP4490151A1 (en) | 2022-03-07 | 2025-01-15 | Incyte Corporation | Solid forms, salts, and processes of preparation of a cdk2 inhibitor |
| EP4519267A4 (en) * | 2022-05-05 | 2026-02-25 | Beone Medicines I Gmbh | HETEROCYCLIC COMPOUNDS, THEIR COMPOSITIONS AND ASSOCIATED PROCESSING METHODS |
| AR129675A1 (es) | 2022-06-22 | 2024-09-18 | Incyte Corp | Inhibidores de cdk12 de aminas biciclicas |
| WO2024015731A1 (en) | 2022-07-11 | 2024-01-18 | Incyte Corporation | Fused tricyclic compounds as inhibitors of kras g12v mutants |
| WO2024026290A1 (en) * | 2022-07-25 | 2024-02-01 | Cayman Chemical Company Incorporated | NOVEL HETEROCYCLES AS sPLA2-X INHIBITORS |
| CA3263134A1 (en) * | 2022-07-29 | 2024-02-01 | Cedilla Therapeutics, Inc. | CDK2 INHIBITORS AND THEIR METHODS OF USE |
| WO2024220532A1 (en) | 2023-04-18 | 2024-10-24 | Incyte Corporation | Pyrrolidine kras inhibitors |
| GEAP202616866A (en) | 2023-04-18 | 2026-02-10 | Incyte Corp | 2-azabicyclo[2.2.1]heptane kras inhibitors |
| WO2024254245A1 (en) | 2023-06-09 | 2024-12-12 | Incyte Corporation | Bicyclic amines as cdk2 inhibitors |
| US20250163079A1 (en) | 2023-11-01 | 2025-05-22 | Incyte Corporation | Kras inhibitors |
| US20250195536A1 (en) | 2023-12-13 | 2025-06-19 | Incyte Corporation | Bicyclooctane kras inhibitors |
| US20260053814A1 (en) | 2024-08-21 | 2026-02-26 | Celcuity Inc. | Treatment regimens for gedatolisib in hormonally-driven disorders |
| WO2026060143A1 (en) | 2024-09-11 | 2026-03-19 | Incyte Corporation | Kras inhibitors |
| WO2026076207A1 (en) | 2024-10-04 | 2026-04-09 | Incyte Corporation | Tricyclic heteroaryl compounds as inhibitors of tyk2 and/or jak1 |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT72878B (en) | 1980-04-24 | 1983-03-29 | Merck & Co Inc | Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents |
| EP1485390B1 (en) | 2002-03-07 | 2008-10-08 | F. Hoffman-la Roche AG | Bicyclic pyridine and pyrimidine p38 kinase inhibitors |
| EP1590341B1 (en) | 2003-01-17 | 2009-06-17 | Warner-Lambert Company LLC | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| CN101723891A (zh) | 2003-02-10 | 2010-06-09 | 沃泰克斯药物股份有限公司 | 通过使n-芳基氨基甲酸酯与卤代杂芳基反应制备n-杂芳基-n-芳基胺的方法和类似方法 |
| US20050113379A1 (en) | 2003-09-05 | 2005-05-26 | Ping Ge | Heteroaryl fused pyridines, pyrazines and pyrimidines as CRF1 receptor ligands |
| US7749999B2 (en) | 2003-09-11 | 2010-07-06 | Itherx Pharmaceuticals, Inc. | Alpha-ketoamides and derivatives thereof |
| CA2546192C (en) | 2003-11-17 | 2010-04-06 | Pfizer Products Inc. | Pyrrolopyrimidine compounds useful in treatment of cancer |
| US7319102B1 (en) | 2003-12-09 | 2008-01-15 | The Procter & Gamble Company | Pyrrolo[2,3-d]pyrimidine cytokine inhibitors |
| PE20051089A1 (es) * | 2004-01-22 | 2006-01-25 | Novartis Ag | Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina |
| EP1713806B1 (en) | 2004-02-14 | 2013-05-08 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| JP2007526906A (ja) | 2004-03-05 | 2007-09-20 | 大正製薬株式会社 | ピロロピリミジン誘導体 |
| RS52545B (sr) | 2004-04-07 | 2013-04-30 | Novartis Ag | Inhibitori protein apoptoze (iap) |
| WO2005107760A1 (en) | 2004-04-30 | 2005-11-17 | Irm Llc | Compounds and compositions as inducers of keratinocyte differentiation |
| WO2006008545A2 (en) | 2004-07-22 | 2006-01-26 | Astex Therapeutics Limited | Thiazole and isothiazole derivatives as protein kinase inhibitors |
| US7906528B2 (en) | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| AU2005298637B8 (en) | 2004-10-29 | 2012-12-06 | Janssen Sciences Ireland Uc | HIV inhibiting bicyclic pyrimidine derivatives |
| US7521446B2 (en) | 2005-01-13 | 2009-04-21 | Signal Pharmaceuticals, Llc | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith |
| US7723340B2 (en) | 2005-01-13 | 2010-05-25 | Signal Pharmaceuticals, Llc | Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith |
| EP1846408B1 (en) | 2005-01-14 | 2013-03-20 | Janssen Pharmaceutica NV | 5-membered annelated heterocyclic pyrimidines as kinase inhibitors |
| WO2006091737A1 (en) | 2005-02-24 | 2006-08-31 | Kemia, Inc. | Modulators of gsk-3 activity |
| JP2006241089A (ja) | 2005-03-04 | 2006-09-14 | Astellas Pharma Inc | ピロロピリミジン誘導体またはその塩 |
| AR054391A1 (es) | 2005-06-20 | 2007-06-20 | Astrazeneca Ab | Procedimiento para la preparacion de 3,7- dihidroxi-1,5-diazaciclooctanos |
| DE102005030051A1 (de) | 2005-06-27 | 2006-12-28 | Grünenthal GmbH | Substituierte 1-Oxa-3,8-diazaspiro[4,5]-decan-2-on-Verbindungen und deren Verwendung zur Herstellung von Arzneimitteln |
| WO2007030438A2 (en) | 2005-09-06 | 2007-03-15 | Pharmacopeia, Inc. | Aminopurine derivatives for treating neurodegenerative diseases |
| GB0520164D0 (en) | 2005-10-04 | 2005-11-09 | Novartis Ag | Organic compounds |
| US8338607B2 (en) | 2005-10-06 | 2012-12-25 | Nippon Soda Co., Ltd. | Cyclic amine compounds and agents for pest control |
| WO2007058990A2 (en) | 2005-11-14 | 2007-05-24 | Kemia, Inc. | Therapy using cytokine inhibitors |
| WO2007075783A2 (en) | 2005-12-22 | 2007-07-05 | Wyeth | Substituted isoquinoline-1,3(2h,4h)-diones, 1-thioxo-1,4-dihydro-2h-isoquinoline-3-ones and 1,4-dihydro-3(2h)-isoquinolones and use thereof as kinase inhibitor |
| GB0526246D0 (en) | 2005-12-22 | 2006-02-01 | Novartis Ag | Organic compounds |
| CA2646429A1 (en) | 2006-03-09 | 2007-09-13 | Pharmacopeia, Inc. | 8-heteroarylpurine mnk2 inhibitors for treating metabolic disorders |
| CA2651072A1 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| TWI398252B (zh) * | 2006-05-26 | 2013-06-11 | 諾華公司 | 吡咯并嘧啶化合物及其用途 |
| WO2008135232A1 (en) | 2007-05-02 | 2008-11-13 | Riccardo Cortese | Use and compositions of purine derivatives for the treatment of proliferative disorders |
| WO2009049028A1 (en) | 2007-10-09 | 2009-04-16 | Targegen Inc. | Pyrrolopyrimidine compounds and their use as janus kinase modulators |
| KR20100108341A (ko) | 2007-11-20 | 2010-10-06 | 브리스톨-마이어스 스큅 컴퍼니 | 시클로프로필 융합된 인돌로벤즈아제핀 hcv ns5b 억제제 |
| BRPI0821209A2 (pt) | 2007-12-19 | 2019-09-24 | Amgen Inc | composto, composição farmacêutica, métodos de tratar câncer, para reduzir o tamanho de tumor, para tratar distúrbios, e para reduzir metástase em um tumor. |
| UY31631A1 (es) | 2008-02-06 | 2009-09-30 | Nuevos derivados de 7-fenil-7h-pirrolo-[2,3d]-pirimidin-2-il-amino, sales de los mismos, procesos para su preparacion, composiciones farmacéuticas que los comprenden y aplicaciones | |
| WO2009115084A2 (de) | 2008-03-20 | 2009-09-24 | Schebo Biotech Ag | Neue pyrrolopyrimidin-derivate und deren verwendungen |
| ES2522346T3 (es) | 2008-08-22 | 2014-11-14 | Novartis Ag | Compuestos de pirrolopirimidina como inhibidores de CDK |
| UY33226A (es) | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
| WO2011130232A1 (en) | 2010-04-13 | 2011-10-20 | Novartis Ag | Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor and an mtor inhibitor for treating cancer |
| AR083797A1 (es) | 2010-11-10 | 2013-03-20 | Novartis Ag | Succinato de dimetil-amida del acido 7-ciclopentil-2-(5-piperazin-1-il-piridin-2-il-amino)-7h-pirrolo-[2,3-d]pirimidin-6-carboxilico, proceso para prepararla, intermediarios de dicha sintesis y proceso de preparacion de los mismos |
-
2011
- 2011-02-15 UY UY33227A patent/UY33227A/es not_active Application Discontinuation
- 2011-02-17 PE PE2012001259A patent/PE20121815A1/es not_active Application Discontinuation
- 2011-02-17 BR BR112012020922-1A patent/BR112012020922B1/pt active IP Right Grant
- 2011-02-17 DK DK11707115.9T patent/DK2536730T3/en active
- 2011-02-17 MA MA35209A patent/MA34066B1/fr unknown
- 2011-02-17 WO PCT/EP2011/052353 patent/WO2011101409A1/en not_active Ceased
- 2011-02-17 EP EP11707115.9A patent/EP2536730B1/en active Active
- 2011-02-17 PL PL11707115T patent/PL2536730T3/pl unknown
- 2011-02-17 PT PT117071159T patent/PT2536730E/pt unknown
- 2011-02-17 UA UAA201209879A patent/UA108369C2/uk unknown
- 2011-02-17 SG SG2012058566A patent/SG183218A1/en unknown
- 2011-02-17 AU AU2011217286A patent/AU2011217286B2/en active Active
- 2011-02-17 US US13/579,359 patent/US8957074B2/en active Active
- 2011-02-17 CN CN201180021222.6A patent/CN102918043B/zh active Active
- 2011-02-17 EA EA201201161A patent/EA022355B1/ru not_active IP Right Cessation
- 2011-02-17 NZ NZ60175411A patent/NZ601754A/en not_active IP Right Cessation
- 2011-02-17 HR HRP20151071TT patent/HRP20151071T1/hr unknown
- 2011-02-17 MX MX2012009613A patent/MX2012009613A/es active IP Right Grant
- 2011-02-17 RS RS20150623A patent/RS54263B1/sr unknown
- 2011-02-17 KR KR1020127024329A patent/KR101812357B1/ko active Active
- 2011-02-17 SI SI201130591T patent/SI2536730T1/sl unknown
- 2011-02-17 AR ARP110100478 patent/AR080198A1/es unknown
- 2011-02-17 GE GEAP201112834A patent/GEP20146146B/en unknown
- 2011-02-17 CA CA2790637A patent/CA2790637C/en active Active
- 2011-02-17 ME MEP-2015-157A patent/ME02202B/me unknown
- 2011-02-17 JP JP2012553318A patent/JP5788415B2/ja active Active
- 2011-02-17 ES ES11707115.9T patent/ES2548532T3/es active Active
- 2011-02-17 PH PH1/2012/501649A patent/PH12012501649A1/en unknown
- 2011-02-18 TW TW100105536A patent/TWI503322B/zh not_active IP Right Cessation
-
2012
- 2012-08-14 ZA ZA2012/06079A patent/ZA201206079B/en unknown
- 2012-08-15 TN TNP2012000413A patent/TN2012000413A1/en unknown
- 2012-08-16 IL IL221520A patent/IL221520A/en not_active IP Right Cessation
- 2012-08-17 NI NI201200135A patent/NI201200135A/es unknown
- 2012-08-17 CL CL2012002270A patent/CL2012002270A1/es unknown
- 2012-08-17 DO DO2012000225A patent/DOP2012000225A/es unknown
- 2012-08-17 HN HN2012001744A patent/HN2012001744A/es unknown
- 2012-08-20 EC ECSP12012111 patent/ECSP12012111A/es unknown
-
2014
- 2014-12-12 US US14/568,410 patent/US9309252B2/en active Active
-
2015
- 2015-10-28 SM SM201500265T patent/SMT201500265B/it unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ME02202B (me) | Jedinjenja pirolopirimidina kao inhibitori cdk4/6 | |
| JP2013519707A5 (me) | ||
| JP6263269B2 (ja) | キナーゼ阻害剤及びその使用 | |
| US9828373B2 (en) | 2-amino-pyrido[2,3-D]pyrimidin-7(8H)-one derivatives as CDK inhibitors and uses thereof | |
| JP2024517693A (ja) | 2-アミノベンゾチアゾール化合物及びその使用方法 | |
| ES2531465T3 (es) | Derivados de pirimidinona, su preparación y su utilización farmacéutica | |
| JP2024532733A (ja) | 複素環式化合物及び使用方法 | |
| ME02635B (me) | Novi derivati pirola, postupak njihove priprave i farmaceutski pripravci koji ih sadrže | |
| BR112020022201A2 (pt) | análogos de rapamicina ligada a c40, c28, e c-32 como inibidores de mtor | |
| JP2017222709A5 (me) | ||
| JP2023549055A (ja) | 複素環式スピロ化合物及びその使用方法 | |
| JP2015511245A5 (me) | ||
| JP2019535664A5 (me) | ||
| JP2013500975A5 (me) | ||
| NZ610018A (en) | Aminoalcohol substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis | |
| MX2014008913A (es) | Nuevos derivados de indolizina, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen. | |
| JP2015508075A5 (me) | ||
| JP2012528828A5 (me) | ||
| JP2020527174A5 (me) | ||
| ME02922B (me) | Novi derivati indolizina, postupak njihove proizvodnje i farmaceutske kompozicije koje ih sadrže | |
| US12006320B2 (en) | Heterocyclic derivatives as PI3K inhibitors | |
| RU2014109748A (ru) | Морфолино-замещенные производные бициклических пиримидинмочевины или карбамата в качестве ингибиторов mtor | |
| AU2021373162A1 (en) | Pyrazolopyridazinone compound, and pharmaceutical composition and use thereof | |
| CN112867715A (zh) | 作为腺苷受体拮抗剂的5-氮杂吲唑衍生物 | |
| RU2023134860A (ru) | Ингибиторы мутации her2 |