HRP20160077T1 - Imidazotriazini i imidazopiramidini kao inhibitori kinaze - Google Patents
Imidazotriazini i imidazopiramidini kao inhibitori kinaze Download PDFInfo
- Publication number
- HRP20160077T1 HRP20160077T1 HRP20160077TT HRP20160077T HRP20160077T1 HR P20160077 T1 HRP20160077 T1 HR P20160077T1 HR P20160077T T HRP20160077T T HR P20160077TT HR P20160077 T HRP20160077 T HR P20160077T HR P20160077 T1 HRP20160077 T1 HR P20160077T1
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- Croatia
- Prior art keywords
- alkyl
- nrc2rd2
- cr7r8
- haloalkyl
- independently selected
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- XZLIYCQRASOFQM-UHFFFAOYSA-N 5h-imidazo[4,5-d]triazine Chemical class N1=NC=C2NC=NC2=N1 XZLIYCQRASOFQM-UHFFFAOYSA-N 0.000 title 1
- 150000005237 imidazopyrimidines Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 56
- 125000001072 heteroaryl group Chemical group 0.000 claims 46
- 125000005843 halogen group Chemical group 0.000 claims 43
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 43
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 42
- 125000003118 aryl group Chemical group 0.000 claims 42
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 39
- 125000000753 cycloalkyl group Chemical group 0.000 claims 39
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 33
- 125000001424 substituent group Chemical group 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 20
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 16
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 16
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 16
- 125000005311 halosulfanyl group Chemical group 0.000 claims 15
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 14
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 10
- 101100310920 Caenorhabditis elegans sra-2 gene Proteins 0.000 claims 8
- 125000000732 arylene group Chemical group 0.000 claims 8
- 125000002993 cycloalkylene group Chemical group 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 6
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 6
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 6
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 6
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 6
- 125000006591 (C2-C6) alkynylene group Chemical group 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 230000002401 inhibitory effect Effects 0.000 claims 5
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 claims 4
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 claims 4
- 108091000080 Phosphotransferase Proteins 0.000 claims 4
- 210000004027 cell Anatomy 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000005549 heteroarylene group Chemical group 0.000 claims 4
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 4
- 102000020233 phosphotransferase Human genes 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- -1 C2-6 alknyl Chemical group 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 101100310926 Caenorhabditis elegans sra-3 gene Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 125000005083 alkoxyalkoxy group Chemical group 0.000 claims 2
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 150000005347 biaryls Chemical group 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000004966 cyanoalkyl group Chemical group 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000005349 heteroarylcycloalkyl group Chemical group 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- ZJCHPFBJPLGHNN-UHFFFAOYSA-N 2-fluoro-n-[1-(methoxymethyl)cyclopropyl]-4-[7-(1-quinolin-6-ylethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C=1C=C(C2=NN3C(C(C)C=4C=C5C=CC=NC5=CC=4)=CN=C3N=C2)C=C(F)C=1C(=O)NC1(COC)CC1 ZJCHPFBJPLGHNN-UHFFFAOYSA-N 0.000 claims 1
- CZGAGJHZXZVLIV-UHFFFAOYSA-N 2-fluoro-n-methyl-4-[7-(1-quinolin-6-ylethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1C1=NN2C(C(C)C=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 CZGAGJHZXZVLIV-UHFFFAOYSA-N 0.000 claims 1
- DJIOWWZVRZHPMS-UHFFFAOYSA-N 6-(4-fluorophenyl)-3-[(4-methoxyphenyl)methyl]imidazo[1,2-a]pyrimidine Chemical compound C1=CC(OC)=CC=C1CC1=CN=C2N1C=C(C=1C=CC(F)=CC=1)C=N2 DJIOWWZVRZHPMS-UHFFFAOYSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000009746 Adult T-Cell Leukemia-Lymphoma Diseases 0.000 claims 1
- 208000016683 Adult T-cell leukemia/lymphoma Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- PJXCVELEUHKAJM-UHFFFAOYSA-N C=1C=C2N=CC=CC2=CC=1C(C)C(N1N=2)=CN=C1N=CC=2C(C=C1F)=CC=C1C(=O)NC1CCC(O)CC1 Chemical compound C=1C=C2N=CC=CC2=CC=1C(C)C(N1N=2)=CN=C1N=CC=2C(C=C1F)=CC=C1C(=O)NC1CCC(O)CC1 PJXCVELEUHKAJM-UHFFFAOYSA-N 0.000 claims 1
- 101100310927 Caenorhabditis elegans sra-4 gene Proteins 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 101150009057 JAK2 gene Proteins 0.000 claims 1
- 101150069380 JAK3 gene Proteins 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000006644 Malignant Fibrous Histiocytoma Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 101100268648 Mus musculus Abl1 gene Proteins 0.000 claims 1
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000001894 Nasopharyngeal Neoplasms Diseases 0.000 claims 1
- 206010061306 Nasopharyngeal cancer Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma 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
- 108010051742 Platelet-Derived Growth Factor beta Receptor Proteins 0.000 claims 1
- 102000018967 Platelet-Derived Growth Factor beta Receptor Human genes 0.000 claims 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 claims 1
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 101150001535 SRC gene Proteins 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000015778 Undifferentiated pleomorphic sarcoma Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 201000006966 adult T-cell leukemia Diseases 0.000 claims 1
- 230000000172 allergic effect Effects 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 125000004980 cyclopropylene group Chemical group 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000008482 dysregulation Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 230000009033 hematopoietic malignancy Effects 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- UKWPIZOBFGTJOK-MLARANPPSA-N n-[(2r)-1-(dimethylamino)-3-methyl-1-oxobutan-2-yl]-4-[7-(1-quinolin-6-ylethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C1=CC(C(=O)N[C@H](C(C)C)C(=O)N(C)C)=CC=C1C1=NN2C(C(C)C=3C=C4C=CC=NC4=CC=3)=CN=C2N=C1 UKWPIZOBFGTJOK-MLARANPPSA-N 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- OWENJHPDJXCUQU-UHFFFAOYSA-N n-cyclopropyl-2-fluoro-4-[7-(1-quinolin-6-ylethyl)imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide Chemical compound C=1C=C2N=CC=CC2=CC=1C(C)C(N1N=2)=CN=C1N=CC=2C(C=C1F)=CC=C1C(=O)NC1CC1 OWENJHPDJXCUQU-UHFFFAOYSA-N 0.000 claims 1
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 230000008929 regeneration Effects 0.000 claims 1
- 238000011069 regeneration method Methods 0.000 claims 1
- 201000002793 renal fibrosis Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010042863 synovial sarcoma Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Classifications
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- 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
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon atoms
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- Health & Medical Sciences (AREA)
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- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
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- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
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- Immunology (AREA)
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- Urology & Nephrology (AREA)
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- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
- Gastroenterology & Hepatology (AREA)
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Claims (27)
1. Spoj formule l:
[image]
ili njegova farmaceutski prihvatljiva sol ili njegov prolijek, pri čemu:
A je N;
Cy1 je aril, heteroaril, cikloalkil, ili heterocikloalkil, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z;
Cy2je aril, heteroaril, cikloalkil, ili heterokicloalkil, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’;
L1 je (CR4R5)m;
L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t, (CR7R8)s-(heterocikloalkilen)-(CR7R8)t, (CR7R8)s-(heteroarilen)-(CR7R8)t, (CR7R8)sO(CR7R8)t, (CR7R8)sS(CR7R8)t, (CR7R8)sC(O)(CR7R8)t, (CR7R8)sC(O)NR9(CR7R8)t, (CR7R8)sC(O)O(CR7R8)t, (CR7R8)sOC(O)(CR7R8)t, (CR7R8)sOC(O)NR9(CR7R8)t, (CR7R8)sNR9(CR7R8)t, (CR7R8)sNR9C(O)NR9(CR7R8)t, (CR7R8)sS(O)(CR7R8)t, (CR7R8)sS(O)NR7(CR8R9)t, (CR7R8)sS(O)2(CR7R8)t, ili (CR7R8)sS(O)2NR9(CR7R8)t, pri čemu navedeni cikloalkilen, arilen, heterocikloalkilen, ili heteroarilen je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRe1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1;
R1 je H ili -W"-X"-Y"-Z";
R2 je H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORA, SRA, C(O)RB, C(O)NRCRD, C(O)ORA, OC(O)RB, OC(O)NRCRD, NRCRD, NRCC(O)RB, NRCC(O)NRCRD, NRCC(O)ORA, S(O)RB, S(O)NRCRD, S(O)2RB, NRCS(O)2RB, ili S(O)2NRCRD;
ili R2 i -L2-Cy2su povezani zajedno da bi formirali grupu formule:
[image]
pri čemu je prsten B spojeni arilni ili spojeni heteroarilni prsten, svaki opcionalno zamijenjen sa 1, 2, ili 3 -W’-X’-Y’-Z’;
R4 je H;
R5 je izabran od H, halo, OH, C1-6 alkil, i cikloalkil;
ili R4 i R5 zajedno sa C atomom na koji su vezani formiraju 3, 4, 5, 6, ili 7-člani cikloalkil;
R7 i R8 su nezavisno izabrani od H, halo, OH, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 haloalkil, CN, i NO2;
ili R7 i R8 zajedno sa C atomom za koji su povezani od 3, 4, 5, 6, ili 7-člana cikloalkilnog ili heterocikloalkilnog prstena, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od halo, OH, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 alkoksi, C1-6 haloalkil, CN, i NO2;
R9 je H, C1-6 alkil, C2-6 alkenil, ili C2-6 alkinil;
W, W’, i W" su nezavisno odsutni ili nezavisno odabrani od C1-6 alkilen, C2-6 alkenilen, C2-6 alkinilen, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh i NRhCONRi, pri čemu svaki od C1-6 alkilena, C2-6 alkenilena, i C2-6 alkinilena je opcionalno zamijenjen sa 1, 2 ili 3 supstituenta nezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, OH, C1-6 alkoksi, C1-6 haloalkoksi, amino, C1-6 alkilamino, i C2-8 dialkilamino;
X, X’, i X" su nezavisno odsutni ili nezavisno izabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, arilena, cikloalkilena, heteroarilena, i heterocikloalkilena, pri čemu svaki od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, arilena, cikloalkilena, heteroarilena, i heterocikloalkilena je opcionalno zamijenjen sa 1, 2 ili 3 supstituenta nezavisno izabranih od halo, CN, NO2, OH, C1-6 alkil, C1-6 haloalkil, C2-8 alkoksialkil, C1-6 alkoksi, C1-6 haloalkoksi, C2-8 alkoksialkoksi, cikloalkil, heterocikloalkil, C(O)ORj, C(O)NRhRi, amino. C1-6 alkilamino, i C2-8 dialkilamino;
Y, Y’, i Y" su nezavisno odsutni ili nezavisno izabrani od C1-6 alkilena, C2-6 alkenilena, C2-6 alkinilena, O, S, NRh, CO, COO, CONRh, SO, SO2, SONRh, i NRhCONRi, pri čemu svaki od C1-6 alkilena, C2-6 alkenilena, i C2-6 alkinilena je opcionalno zamijenjen sa 1, 2 ili 3 supstituenta nezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, OH, C1-6 alkoksi, C1-6 haloalkoksi, amino, C1-6 alkilamino, i C2-8 diaikilamino;
Z, Z’, i Z" su nezavisno izabrani od H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, SS(O)2NRc2Rd2, aril, cikloalkil, heteroaril, i heterocikloalkil, gdje navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil je opcionalno zamijenjen sa 1, 2, 3, 4 ili 5 supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2 , NRc2S(O)2Rb2, i S(O)2NRc2Rd2;
pri čemu dva susjedna -W-X-Y-Z, zajedno sa atomima sa kojima su povezani, opcionalno formiraju spojeni cikloalkilni prsten od 4-20 članova ili spojeni heterocikloalkilni prsten od 4-20 članova, svaki opcionalno zamijenjen sa 1, 2, ili 3, supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6haloalkil, halosulfanil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, Nrc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(=NRg)NRc3Rd3, NRc3C(=NR9)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, aril, cikloalkil, heteroaril, i heterocikloalkil;
pri čemu dva susjedna -W’-X’-Y’-Z’, zajedno sa atomima sa kojima su povezani, opcionalno formiraju spojeni cikloalkilni prsten od 4-20 članova ili spojeni heterocikloalkilni prsten od 4-20 članova, svaki opcionalno zamijenjen sa 1, 2, ili 3, supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3 , NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3,C(=NRg)NRc3Rd3, NRc3C(=NRg)NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, NRc3S(O)2Rb3, S(O)2NRc3Rd3, aril, cikloalkil, heteroaril, i heterocikloalkil;
Cy4 je nezavisno izabran od aril, cikloalkil, heteroaril, i heterocikloalkil, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 supstituenta nezavisno izabranih od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, Nrc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(=NRg)NRc4Rd4, NRc4C(=NRg)NRc4Rd4, P(Rf4)2, P(OR4)2, P(O)Re4Rf4, P(O)ORe4ORf4, S(O)Rb4, S(O)NRc4Rd4, S(O)2Rb4, NRc4S(O)2Rb4, i S(O)2NRc4Rd4;
RA je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril, ili heteroaril gdje navedeni C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril ili heteroaril je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, i C1-4 alkil ;
RB je H, C1-4 alkil, C2-4 alkenil, C2-4 alkinil, cikloalkil, heterocikloalkil, aril, ili heteroaril gdje navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, cikloalkil, heterocikloalkil, aril, ili heteroaril je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, i C1-4 alkil;
RC i RD su nezavisno izabrani od H, C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, gdje navedeni C1-4 alkil, C2-4 alkenil, ili C2-4 alkinil, je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, i C1-4 alkil;
ili RC i RD zajedno sa N atomom za koji su povezani u heterocikloalkilnu grupu od 4-, 5-, 6- ili 7- članova ili heteroarilnu grupu, svaku opcionalno zamijenjenih sa 1, 2, ili 3 supstituenta nezavisno odabranih od OH, CN, amino, halo, i C1-4 alkil;
Ra, Ra1, Ra2, Ra3, i Ra4 su nezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, i heterocikloalkilalkil, gdje navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Rb, Rb1, Rb2, Rb3, i Rb4 su nezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, i heterocikloalkilalkil, pri čemu navedeni C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alknil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Rc i Rd su nezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
ili Rc i Rd zajedno sa N atomom za koji su prikvačeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-člana ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Rc1 i Rd1 su nezavisno odabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocicloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
ili Rc1 i Rd1 zajedno sa N atomom sa kojim su spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Rc2 i Rd2 su nezavisno odabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, heterocikloalkilalkil, arilcikloalkil, arilheterocikloalkil, arilheteroaril, biaril, heteroarilcikloalkil, heteroarilheterocikloalkil, heteroarilaril, i biheteroaril, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil, heterocikloalkilalkil, arilcikloalkil, arilheterocikloalkil, arilheteroaril, biaril, heteroarilcikloalkil, heteroarilheterocikloalkil, heteroarilaril, i biheteroaril je svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, C1-6 haloalkoksi, hidroksialkil; cijanoalkil, aril, heteroaril, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkil, i alkoksialkoksi;
ili Rc2 i Rd2 zajedno sa N atomom za koji su spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrnim 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6alkil, C1-6alkoksi, C1-6haloalkil, C1-6 haloalkoksi, hidrohialkil, cianoalkil, aril, aril, heteroalkil, C(O)ORa4, C(O)Rb4, S(O)2Rb3,alkoksialkil, i alkoksialkoksi;
Rc3 i Rd3 su nezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
ili Rc3 i Rd3 zajedno sa N atomom za koji su spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-članova ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Rc4 i Rd4 su nezavisno izabrani od H, C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil, pri čemu navedeni C1-10 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, heteroaril, cikloalkil, heterocikloalkil, arilalkil, heteroarilalkil, cikloalkilalkil ili heterocikloalkilalkil je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
ili Rc4 i Rd4 zajedno sa N atomom za koji su spojeni formiraju heterocikloalkilnu grupu od 4-, 5-, 6- ili 7-člana ili heteroarilnu grupu, svaki opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od OH, CN, amino, halo, C1-6 alkil, C1-6 alkoksi, C1-6 haloalkil, i C1-6 haloalkoksi;
Re, Re1, Re2, i Re4 su nezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, (C1-6 alkoksi)-C1-6alkil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil, arilalkil, cikloalkilalkil, heteroarilalkil, i heterocikloalkilalkil;
Rf, Rf1, Rf2, i Rf4 su nezavisno izabrani od H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil;
Rg je H, CN, i NO2;
Rh i Ri su nezavisno izabrani od H i C1-6 alkil;
Rj je H, C1-6 alkil, C1-6 haloalkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, heterocikloalkil,
arilalkil, heteroarilalkil, cikloalkilalkil, ili heterocikloalkilalkil;
m je 1, ili 2;
r je 0, 1, 2, 3, 4, 5, ili 6;
s je 0, 1, 2, 3, ili 4; i
t je 0, 1, 2, 3, ili 4.
2. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy1 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; (b) Cy1 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; (c) Cy1 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z; ili (d) Cy1 je hinolinil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W-X-Y-Z, naročito hinolinil.
3. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy2 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (b) Cy2 je aril ili heteroaril, svaki opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’ pri čemu bar jedan od navedenih -W’-X’-Y’-Z’ je C(O)NRc2Rd2; (b) Cy2 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; ili (d) Cy2 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5-W’-X’-Y’-Z’.
4. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L1 je CH2 ili CH2CH2 ili cikloalkilen; ili pri čemu L1 je CH2 ili ciklopropilen.
5. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r.
6. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r i r je 0.
7. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva so, pri čemu L2je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, (CR7R8)s-(arilen)-(CR7R8)t,(CR7R8)s-(heterocikloalkilen)-(CR7R8)t, ili (CR7R8)s-(heteroarilen)-(CR7R8)t, gdje je navedeni cikloalkilen, arilen, heterocikloalkilen, ili heteroarilen opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od Cy4, halo, C1-6alkil, C2-6alkenil, C2-6alkinil, C1-6haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
8. Spoj prema patentnom zahtjev u 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je (CR7R8)r, (CR7R8)s-(cikloalkilen)-(CR7R8)t, ili (CR7R8)s-(arilen)-(CR7R8)t, gdje navedeni cikloalkilen ili arilen, je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabranih od Cy4, halo, C1-6alkil, C2-6alkenil, C2-6alkinil, C1-6haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2,P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, NRc1S(O)2Rb1, i S(O)2NRc1Rd1.
9. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva so, pri čemu L2 je (CR7R8)s-(cikloalkilen)-(CR7R8)t ili (CR7R8)s-(arilen)-(CR7R8)t, gdje navedeni cikloalkilen ili arilen, je opcionalno zamijenjen sa 1, 2, ili 3 supstituenta nezavisno izabrani od Cy4, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1,NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(=NRg)NRc1Rd1, NRc1C(=NRg)NRc1Rd1, P(Rf1)2, P(ORe1)2, P(O)Re1Rf1, P(O)ORe1ORf1, S(O)Rb1, S(O)NRc1Rd1, S(O)2 Rb1, NRc1S(O)2 Rb1, i S(O)2 NRc1Rd1.
10. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu L2 je cikloalkilen ili arilen; naročito gdje L2 je arilen.
11. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu (a) Cy2 je aril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (b) pri čemu Cy2 je heteroaril opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; (c) Cy2 je cikloalkil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’; ili (d) pri čemu Cy2 je heterocikloalkil opcionalno zamijenjen sa 1, 2, 3, 4, ili 5 -W’-X’-Y’-Z’.
12. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu R1 je H; ili pri čemu R2 je H; ili pri čemu R5 je H; ili pri čemu R7 je H; ili pri čemu R8 je H; ili pri čemu R9 je H.
13. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu -W-X-Y-Z je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril, i heterocikloalkil, pri čemu navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su opcionalno zamijenjeni sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabrani od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) Nrc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2OR12, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, i S(O)2NRc2Rd2 ; naročito pri čemu -W-X-Y-Z je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, Nrc2C(O)NRc2Rd2, Nrc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, ili S(O)2NRc2Rd2 ; naročito pri čemu -W-X-Y-Z je halo, C1-6alkil, C1-6 haloalkil, CN, NO2, N3, ili ORa2; naročito pri čemu -W-X-Y-Z je ORa2; naročito pri čemu -W-X-Y-Z je metoksi.
14. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, pri čemu -W'-X'-Y'-Z' je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg)NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, aril, cikloalkil, heteroaril, i heterocikloalkil, pri čemu navedeni C1-6 alkil, C2-6 alkenil, C2-6 alkinil, aril, cikloalkil, heteroaril, i heterocikloalkil su opcionalno zamijenjeni sa 1, 2, 3, 4 ili 5 supstituenata nezavisno izabrani od halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg) Nrc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, i S(O)2NRc2Rd2 ; naročito pri čemu -W'-X'-Y'-Z' je halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, halosulfanil, CN, NO2, N3, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, Nrc2C(O)Rb2, Nrc2C(O)NRc2Rd2, Nrc2C(O)ORa2, C(=NRg)NRc2Rd2, NRc2C(=NRg), NRc2Rd2, P(Rf2)2, P(ORe2)2, P(O)Re2Rf2, P(O)ORe2ORf2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, NRc2S(O)2Rb2, ili S(O)2NRc2Rd2; naročito pri čemu -W'-X'-Y'-Z' je halo, C1-6alkil, C1-6haloalkil, CN, NO2, N3, ORa2 ili C(O)Rc2RNd2 ; naročito pri čemu -W’-X’-Y’-Z’ je halo, C1-6 alkil, C1-6 haloalkil, CN, NO2, N3, ili ORa2, naročito pri čemu-W'-X'-Y'-Z' je halo ili C(O)NRc2Rd2.
15. Spoj prema pri čemu zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom IIa:
[image]
16. Spoj prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom formulu III:
[image]
17. Spoj prema patentnom zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, sa formulom VIII:
[image]
18. Spoj prema patentnom zahtjevu 1, izabrano od:
N-{(1R)-1-[(Dimetilamino)karbonyl]-2-metilpropil}-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2il]benzamid
2-Fluoro-N-(trans-4-hidroksicikloheksil)-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid;
2-Fluoro-N-metil-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid;
N-Ciklopropil-2-fluoro-4-[7-(1-hinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid;
2-Fluoro-N-[1-(metoksimetil)ciklopropil]-4-[7-(1-hiinolin-6-iletil)imidazo[1,2-b][1,2,4]triazin-2-il]benzamid, ili njegove farmaceutski prihvatljive soli.
19. Spoj, koji je 6-(4-Fluorofenil)-3-(4-metoksibenzil)imidazo[1,2-a]pirimidin ili njegova farmaceutski prihvatljiva sol.
20. Pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegovu farmaceutski prihvatljivu sol, i najmanje jedan farmaceutski prihvatljiv nosač.
21. Spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja aktivnosti receptora ili ne-receptorske tirozin kinaze uključujući kontakt navedene kinaze sa spojem.
22. Spoj prema patentnom zahtjevu 21, pri čemu kinaza pripada Met, PDGFR, HER, FLK, Src, Abl, ili JAK potfamilijama; naročito pri čemu je navedena kinaza c-Met, Ron, PDGFR beta, c-kit, EGFR, HER2, KDR, flt-3, Src, Abl, Jak1, Jak2, ili Jak3 kinaza; naročito pri čemu je navedena kinaza c-Met.
23. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja HGF/c-Met kinaze signalnog puta u ćeliji, uključujući kontakt navedene ćelije sa spojem.
24. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol, za upotrebu u metodi inhibiranja proliferativne aktivnosti ćelije koja obuhvata kontaktiranje navedene ćelije sa spojem prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegove farmaceutski prihvatljive soli.
25. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi inhibiranja rasta tumora kod pacijenta, ili za upotrebu u metodi inhibicije metastaze tumora kod pacijenta, uključujući davanje, navedenim pacijentima, terapijski efektivne količine spoja prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegove farmaceutski prihvatljive soli.
26. Spoj prema bilo kojem od patentnih zahtjeva od 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi liječenja bolesti kod pacijenta, naznačen time, da bolest povezana sa disregulacijom HGF/c-MET signalizirajućeg puta, uključujući administriranje, kod navedenog pacijenta, terapijski efektivne količine spoja; naročito pri čemu je navedena bolest karcinom, ateroskleroza, plućna fibroza, renalna fibroza, i regeneracija, bolest jetre, alergijski poremećaj, upalna bolest, autoimuni poremećaj, cerebrovaskularna bolest, kardiovaskularna bolest ili stanje povezano sa transplantacijom organa.
27. Spoj prema bilo kojem od patentnih zahtjeva 1 do 19, ili njegova farmaceutski prihvatljiva sol za upotrebu u metodi liječenja raka kod pacijenta koja obuhvaća primjenu kod navedenog pacijenta terapijski efektivne količine spoja; naročito pri čemu (a) navedeni rak je rak, muskuloskeletni sarkom, sarkom mekog tkiva, ili hematopoetski malignitet; (b) navedeni rak je rak mokraćnog mjehura, rak dojke, rak grlića materice, holangiokarcinom, kolorektalni rak, rak jednjaka, rak želuca, rak glave i vrata, rak bubrega, rak jetre, rak pluća, nazofaringealni rak, rak jajnika, rak gušterače, rak prostate, rak tiroidne žlijezde, osteosarkom, sinovijalni sarkom, rabdomiosarkom, MFH/fibrosarkom, lejomiosarkom, Kapošijev sarkom, multipli mijelom, limfom, leukemija T ćelija odraslih, akutna mijelogena leukemija, kronična mijeloidna leukemija, glioblastom, astrocitom, melanom, mezoteliom ili Vilmov tumor ili; (c) navedeni rak je karcinom pluća, rak jetre, rak želuca, glioblastom, rak dojke ili rak bubrega.
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| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| WO2009054984A1 (en) * | 2007-10-24 | 2009-04-30 | Merck & Co., Inc. | Heterocycle phenyl amide t-type calcium channel antagonists |
| UY31676A1 (es) | 2008-02-28 | 2009-09-30 | "derivados de 3-metil-imidiazo-[1,2-b]-piridazina" | |
| WO2009143211A2 (en) | 2008-05-21 | 2009-11-26 | Incyte Corporation | Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same |
| US20110269740A1 (en) * | 2008-07-02 | 2011-11-03 | Ambit Biosciences Corporation | Jak kinase modulating compounds and methods of use thereof |
| FR2933982A1 (fr) * | 2008-07-18 | 2010-01-22 | Sanofi Aventis | Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met |
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