ME02048B - N-(4-((3-(2-AMINO-4-PIRlMIDlNIL)-2-PIRlDlNlL)OKSI)FENIL)-4-(4-METIL-2-THIENIL)- 1-FTALAZINAMIN ZA PRIMENU U TRETMANU KANCERA REZISTENTNOG NA ANTIMITOTIČKE AGENSE - Google Patents
N-(4-((3-(2-AMINO-4-PIRlMIDlNIL)-2-PIRlDlNlL)OKSI)FENIL)-4-(4-METIL-2-THIENIL)- 1-FTALAZINAMIN ZA PRIMENU U TRETMANU KANCERA REZISTENTNOG NA ANTIMITOTIČKE AGENSEInfo
- Publication number
- ME02048B ME02048B MEP-2015-10A MEP1015A ME02048B ME 02048 B ME02048 B ME 02048B ME P1015 A MEP1015 A ME P1015A ME 02048 B ME02048 B ME 02048B
- Authority
- ME
- Montenegro
- Prior art keywords
- cancer
- group
- compound according
- leukemia
- agent
- Prior art date
Links
- 239000003080 antimitotic agent Substances 0.000 title claims description 5
- IVUGFMLRJOCGAS-UHFFFAOYSA-N n-[4-[3-(2-aminopyrimidin-4-yl)pyridin-2-yl]oxyphenyl]-4-(4-methylthiophen-2-yl)phthalazin-1-amine Chemical compound CC1=CSC(C=2C3=CC=CC=C3C(NC=3C=CC(OC=4C(=CC=CN=4)C=4N=C(N)N=CC=4)=CC=3)=NN=2)=C1 IVUGFMLRJOCGAS-UHFFFAOYSA-N 0.000 title description 2
- 208000016691 refractory malignant neoplasm Diseases 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 claims 16
- 239000002246 antineoplastic agent Substances 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 8
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 6
- 229940127089 cytotoxic agent Drugs 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 4
- 206010005003 Bladder cancer Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 3
- 229930012538 Paclitaxel Natural products 0.000 claims 3
- 206010038389 Renal cancer Diseases 0.000 claims 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 3
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 229960003668 docetaxel Drugs 0.000 claims 3
- 229960004679 doxorubicin Drugs 0.000 claims 3
- 206010017758 gastric cancer Diseases 0.000 claims 3
- 201000010982 kidney cancer Diseases 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 201000007270 liver cancer Diseases 0.000 claims 3
- 208000014018 liver neoplasm Diseases 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
- 229960001592 paclitaxel Drugs 0.000 claims 3
- 201000011549 stomach cancer Diseases 0.000 claims 3
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 3
- 210000001685 thyroid gland Anatomy 0.000 claims 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
- 201000005112 urinary bladder cancer Diseases 0.000 claims 3
- MHFUWOIXNMZFIW-WNQIDUERSA-N (2s)-2-hydroxypropanoic acid;n-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide Chemical compound C[C@H](O)C(O)=O.C1CN(C)CCN1C1=CC(NC2=NNC(C)=C2)=NC(SC=2C=CC(NC(=O)C3CC3)=CC=2)=N1 MHFUWOIXNMZFIW-WNQIDUERSA-N 0.000 claims 2
- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims 2
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 claims 2
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 2
- GBJVVSCPOBPEIT-UHFFFAOYSA-N AZT-1152 Chemical group N=1C=NC2=CC(OCCCN(CC)CCOP(O)(O)=O)=CC=C2C=1NC(=NN1)C=C1CC(=O)NC1=CC=CC(F)=C1 GBJVVSCPOBPEIT-UHFFFAOYSA-N 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims 2
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims 2
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- XKFTZKGMDDZMJI-HSZRJFAPSA-N N-[5-[(2R)-2-methoxy-1-oxo-2-phenylethyl]-4,6-dihydro-1H-pyrrolo[3,4-c]pyrazol-3-yl]-4-(4-methyl-1-piperazinyl)benzamide Chemical compound O=C([C@H](OC)C=1C=CC=CC=1)N(CC=12)CC=1NN=C2NC(=O)C(C=C1)=CC=C1N1CCN(C)CC1 XKFTZKGMDDZMJI-HSZRJFAPSA-N 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 2
- 210000003679 cervix uteri Anatomy 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229960000975 daunorubicin Drugs 0.000 claims 2
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229960001904 epirubicin Drugs 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 208000019691 hematopoietic and lymphoid cell neoplasm Diseases 0.000 claims 2
- 229960000908 idarubicin Drugs 0.000 claims 2
- 210000001672 ovary Anatomy 0.000 claims 2
- 210000000496 pancreas Anatomy 0.000 claims 2
- 210000002307 prostate Anatomy 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 210000002784 stomach Anatomy 0.000 claims 2
- 229960004528 vincristine Drugs 0.000 claims 2
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 2
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 2
- 229960004355 vindesine Drugs 0.000 claims 2
- UGGWPQSBPIFKDZ-KOTLKJBCSA-N vindesine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(N)=O)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1N=C1[C]2C=CC=C1 UGGWPQSBPIFKDZ-KOTLKJBCSA-N 0.000 claims 2
- 229960002066 vinorelbine Drugs 0.000 claims 2
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims 2
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 1
- 206010003571 Astrocytoma Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000032612 Glial tumor 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
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
- 229940122803 Vinca alkaloid Drugs 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 1
- 210000000254 ciliated cell Anatomy 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 230000003325 follicular Effects 0.000 claims 1
- 210000000232 gallbladder Anatomy 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229960001156 mitoxantrone Drugs 0.000 claims 1
- KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims 1
- 208000007538 neurilemmoma Diseases 0.000 claims 1
- 238000011275 oncology therapy Methods 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
- 210000001428 peripheral nervous system Anatomy 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 206010039667 schwannoma Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 208000001608 teratocarcinoma Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 32
- 241000699660 Mus musculus Species 0.000 description 32
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K35/00—Medicinal preparations containing materials or reaction products thereof with undetermined constitution
- A61K35/02—Medicinal preparations containing materials or reaction products thereof with undetermined constitution from inanimate materials
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Description
LISTA SEKVENCI
[0108]
<110> Amgen Inc.
<120> Primena N-(4-((3-(2-amino-4-pirimidinil)-2-piridinil)oksi)fenil)-4-(4-metil-2-tienil)-1-ftalazinamin u terapiji kancera rezistentnih na antimitotički agens
<130> EP81180HV210pau
<140> 10 755 044.4 <141> 2010-09-09
<150> PCT/US2010 10/048247
<151> 2010-09-09
<150> 12/878,539 <151> 2011-09-09
<150> 61/241,527 <151> 2009-09-11
<160> 16
<170>Patent u verziji 3.5
<210> 1
<211> 32
<212> DNK
<213> Mus musculus (miš)
<400> 1
gcttgttact tattacagct agaggcatca tg 32
<210> 2
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 2
tcaaggattt ctccccctgc acgattc 27
<210> 3
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 3
tctcctcccc ctttctctct aaggatg 27
<210> 4
<211> 25
<212> DNK
<213> Mus musculus (miš)
<400> 4
acccgagtga atgacaggga ccatc 25
<210> 5
<211> 26
<212> DNK
<213> Mus musculus (miš)
<400> 5
aacagccatc cagagggttc aggaag 26
<210> 6
<211> 26
<212> DNK
<213> Mus musculus (miš)
<400> 6
ccacacaccc agtctgttct tcatcc 26
<210> 7
<211> 28
<212> DNK
<213> Mus musculus (miš)
<400> 7
aaggggagca ttggcatccc tgactttc 28
<210> 8
<211> 28
<212> DNK
<213> Mus musculus (miš)
<400> 8
gtatttgggg aaaatgctgg gctcagac 28
<210> 9
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 9
accaggcagt gacggtggca tcatatg 27
<210> 10
<211> 25
<212> DNK
<213> Mus musculus (miš)
<400> 10
tgacagccac aaacagagct cccac 25
<210> 11
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 11
ggtaagtgtt ccacctcaga cggaaattg 29
<210> 12
<211> 33
<212> DNK
<213> Mus musculus (miš)
<400> 12
cattaaactg ggtcattcct aactggtact cag 33
<210> 13
<211> 30
<212> DNK
<213> Mus musculus (miš)
<400> 13
ctcaatgaaa gctggggaag gagaatttcc 30
<210> 14
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 14
agaggcattg atagtggaaa cctcacatc 29
<210> 15
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 15
acagtgagac ttacagacgc atcctcaag 29
<210> 16
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 16
aggagagctc cctgaacaca cacaaag 27
LISTA SEKVENCI
[0109]
<110> Amgen Inc.
<120>Primena N-(4-((3-(2-amino-4-pirimidinil)-2-piridinil)oksi)fenil)-4-(4-metil-2-tienil)-1-ftalazinamina u terapiji kancera rezistentnih na antimitotički agens
<130> EP81180HV210pau
<140> 10 755 044.4 <141> 2010-09-09
<150> PCT/US2010/048247
<151> 2010-09-09
<150> 12/878,539 <151> 2011-09-09
<150> 61/241,527 <151> 2009-09-11
<160> 16
<170>Petent u verziji 3.5
<210> 1
<211> 32
<212> DNK
<213> Mus musculus (miš)
<400> 1
gcttgttact tattacagct agaggcatca tg 32
<210> 2
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 2
tcaaggattt ctccccctgc acgattc 27
<210> 3
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 3
tctcctcccc ctttctctct aaggatg 27
<210> 4
<211> 25
<212> DNK
<213> Mus musculus (miš)
<400> 4
acccgagtga atgacaggga ccatc 25
<210> 5
<211> 26
<212> DNK
<213> Mus musculus (miš)
<400> 5
aacagccatc cagagggttc aggaag 26
<210> 6
<211> 26
<212> DNK
<213> Mus musculus (miš)
<400> 6
ccacacaccc agtctgttct tcatcc 26
<210> 7
<211> 28
<212> DNK
<213> Mus musculus (miš)
<400> 7
aaggggagca ttggcatccc tgactttc 28
<210> 8
<211> 28
<212> DNK
<213> Mus musculus (miš)
<400> 8
gtatttgggg aaaatgctgg gctcagac 28
<210> 9
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 9
accaggcagt gacggtggca tcatatg 27
<210> 10
<211> 25
<212> DNK
<213> Mus musculus (miš)
<400> 10
tgacagccac aaacagagct cccac 25
<210> 11
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 11
ggtaagtgtt ccacctcaga cggaaattg 29
<210> 12
<211> 33
<212> DNK
<213> Mus musculus (miš)
<400> 12
cattaaactg ggtcattcct aactggtact cag 33
<210> 13
<211> 30
<212> DNK
<213> Mus musculus (miš)
<400> 13
ctcaatgaaa gctggggaag gagaatttcc 30
<210> 14
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 14
agaggcattg atagtggaaa cctcacatc 29
<210> 15
<211> 29
<212> DNK
<213> Mus musculus (miš)
<400> 15
acagtgagac ttacagacgc atcctcaag 29
<210> 16
<211> 27
<212> DNK
<213> Mus musculus (miš)
<400> 16
aggagagctc cctgaacaca cacaaag 27
Claims (14)
1. Jedinjenje N-(4-((3-(2-amino-4-pirimidinil)-2-piridinil)oksi)fenil)-4-(4-metil-2-tienil)-1-ftalazina-min ili njegova farmaceutski prihvatljiva so, za primenu u terapiji kancera u subjekta, naznačeno time što je kancer subjekta refraktaran na tretman nekim antikancerskim agensom.
2. Jedinjenje za primenu saglasno zahtevu 1, naznačeno time da je antikancerski agens neki hemoterapeutski agens.
3. Jedinjenje saglasno zahtevu 2, naznačeno time da je hemoterapeutski agens, agens izabran iz grupe se sastoji od antimitotičkog agensa i antraciklina.
4. Jedinjenje saglasno zahtevu 2, naznačeno time da je hemoterapeutski agens neki agens izabran iz grupe koja se sastoji od taksola, docetaksela, vinkristina, vindezina i vinorelbina, daunorubicina, doksorubicina, idarubicina, epirubicina i mitoksantrona.
5. Jedinjenje saglasno zahtevu 1, naznačeno time da je antikancerski agens AZD 1152, PHA-739358, MK-0457 ili njihova kombinacija.
6. Jedinjenje saglasno bilo kojem zahtevu 1-5, naznačeno time da je kancer jedan ili više (a) solidnih ili hematoloških tumora izabranih iz grupe koju sačinjavaju kancer mokraćne bešike, dojke, debelog creva, bubrega, jetre, pluća, nesitnoćelijski kancer pluća, jednjaka, žučne kese, jajnika, pankreasa, želuca, grlića materice, štitne žlezde, prostate i kože, (b) neki hematopoetski tumor limfoidne linije izabran između leukemije, akutne limfocitne leukemije, akutne limfoblastne leukemije, limfoma B ćelija, limfoma T ćelija, Hodžkinovog limfoma, ne-Hodžkinovog limfoma, limfoma trepljastih ćelija i Burketovog limfoma, (c) hematopoetski tumor mijeloidne linije, izabran iz grupe akutnih i hroničnih mijelogenih leukemija, mijelodisplaznog sindroma i promijelocitne leukemije (d) neki tumor mezenhimskog porekla izabran iz grupe fibrosarkoma i rabdomiosarkoma, (e) tumor centralnog i perifernog nervnog sistema izabran iz grupe astrocitoma, neuroblastoma, glioma i švanoma, ili (f) melanom, seminom, teratokarcinom, osteosarkom, ksenoderma pigmentosum, keratoktantom, kancer folikulskih ćelija štitne žlezde ili Kapošijev sarkom.
7. Jedinjenje saglasno bilo kojem od zahteva 1-5, naznačeno time što je jedan ili više solidnih tumora izabrano između kancera mokraćne bešike, dojke, debelog creva, bubrega, jetre, pluća, nesitnoćelijski kancer pluća, glave i vrata, jednjaka, želuca, jajnika, pankreasa, stomaka, grlića materice, štitne žlezde i prostate ili limfoma i leukemija.
8. Jedinjenje saglasno bilo kojem od zahteva 1-5, naznačeno time što je kancer, kancer prostate, kancer jajnika, kancer dojke, holangiokarcinom, akutna mijeloidna leukemija, hronična mijeloidna leukemija ili kombinacija nekih od ovih kancera.
9. Primena jedinjenja N-(4-(83-(2-amino-4-pirimidinil)-2-piridinil)oksi)fenil)-4-(4-metil-2-tienil)-1-ftalazinamin ili njegove farmaceutski prihvatljive soli za dobijanje medikamenta za terapiju kancera refraktarnog na tretman antikancerskim agensom.
10. Primena jedinjena saglasno zahtevu 9 za pripremu medikamenta za terapiju kancera izabranog iz grupe koja se sastoji od kancera mokraćne bešike, kancera dojke, kancera debelog creva, kancera bubrega, kancera jetre, kancera pluća, nesitnoćelijskog kancera pluća, kancera glave i vrata, kancera jednjaka, kancera želuca, kancera jajnika, kancera pankreasa, kancera stomaka, kancera grlića materice, kancera štitne žlezde, kancera prostate, limfoma, leukemije, multipnog mijeloma ili kombinacije ovih kancera, naznačeno time što je kancer refraktaran na terapiju antikancerskim agensom.
11. Primena jedinjenja saglasno zahtevu 9 u smanjenju veličine solidnih tumora u subjekta, naznačeno time što je tumor subjekta prethodno tretiran nekim hemoterapeutskim agensom izabranim iz grupe koju sačinjavaju paklitaksel, docetaksel, doksorubicin i vinka alkaloidi.
12. Primena jedinjenja saglasno zahtevu 9, naznačeno time što je antikancerski agens neki hemoterapeutski agens izabran iz grupe koju sačinjavaju antimitotički agens i antraciklin.
13. Primena jedinjenja saglasno zahtevu 9, naznačeno time što je antikancerski agens neki hemoterapeutski agens izabran iz grupe koja se sastoji od taksola, docetaksela, vinkristina, vinblastina, vindezina i vinorelbina, daunorubicina, doksorubicina, idarubicina, epirubicina i motoksantrona.
14. Primena jedinjenja saglasno zahtevu 9, naznačeno time što je antikancerski agens AZD 1152, PHA-739358, MK-0457 ili njihova kombinacija.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US24152709P | 2009-09-11 | 2009-09-11 | |
| PCT/US2010/048247 WO2011031842A1 (en) | 2009-09-11 | 2010-09-09 | N-4 ( - ( ( 3- ( 2 -amino-4 pyrimidinyl) -2 -pyridinyl) oxy) phenyl) -4- (4-methyl-2-thienyl) -1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer |
| EP10755044.4A EP2475368B1 (en) | 2009-09-11 | 2010-09-09 | N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridin yl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer |
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| ME02048B true ME02048B (me) | 2015-05-20 |
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| MEP-2015-10A ME02048B (me) | 2009-09-11 | 2010-09-09 | N-(4-((3-(2-AMINO-4-PIRlMIDlNIL)-2-PIRlDlNlL)OKSI)FENIL)-4-(4-METIL-2-THIENIL)- 1-FTALAZINAMIN ZA PRIMENU U TRETMANU KANCERA REZISTENTNOG NA ANTIMITOTIČKE AGENSE |
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| US8921367B2 (en) | 2012-05-31 | 2014-12-30 | Amgen Inc. | Use of AMG 900 for the treatment of cancer |
| CN103664737A (zh) * | 2012-09-25 | 2014-03-26 | 杨子娇 | 一类治疗房角狭窄的化合物及其用途 |
| KR101701235B1 (ko) | 2013-09-30 | 2017-02-03 | 한국원자력의학원 | Ｈｒｐ-3 억제제를 포함하는 방사선 또는 약물내성 암의 치료용 약학 조성물 |
| BR112016010564A2 (pt) | 2013-11-11 | 2017-10-10 | Amgen Inc | terapia de combinação incluindo um inibidor de mdm2 e um ou mais agentes farmaceuticamente ativos para tratamento de cânceres |
| WO2015084649A1 (en) | 2013-12-03 | 2015-06-11 | Amgen Inc. | Crystalline forms of n-(4-((3-(2-amino-4-pyrimidinyl) - 2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1 -phthalazinamine pharmaceutically acceptable salts and uses thereof |
| RU2713179C2 (ru) * | 2014-02-21 | 2020-02-04 | Фрост Биолоджик, Инк. | Антимитотические амиды для лечения рака и пролиферативных заболеваний |
| EP3443351A4 (en) * | 2016-04-15 | 2019-12-18 | Felicitex Therapeutics, Inc. | COMBINATIONS FOR THE TREATMENT OF NEOPLASIA BY TARGETING RESTING CELLS AND INHIBITORS OF MITOSIS |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| CA3098574A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| MX2020012204A (es) | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
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| US20060178318A1 (en) * | 2003-07-03 | 2006-08-10 | Shubha Anand | Use of aurora kinase inhibitors for reducing the resistance of cancer cells |
| CN101405282B (zh) * | 2006-01-23 | 2015-03-25 | 安姆根有限公司 | 极光激酶调节剂和使用方法 |
| DK1984353T3 (en) * | 2006-01-23 | 2016-03-14 | Amgen Inc | Aurorakinasemodulatorer and method of use |
| US7560551B2 (en) * | 2006-01-23 | 2009-07-14 | Amgen Inc. | Aurora kinase modulators and method of use |
| GB0609619D0 (en) * | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Combination |
| GB0609621D0 (en) * | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
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