ZA200504674B - Diazepinoindole derivatives as kinase inhibitors - Google Patents
Diazepinoindole derivatives as kinase inhibitors Download PDFInfo
- Publication number
- ZA200504674B ZA200504674B ZA200504674A ZA200504674A ZA200504674B ZA 200504674 B ZA200504674 B ZA 200504674B ZA 200504674 A ZA200504674 A ZA 200504674A ZA 200504674 A ZA200504674 A ZA 200504674A ZA 200504674 B ZA200504674 B ZA 200504674B
- Authority
- ZA
- South Africa
- Prior art keywords
- phenyl
- dihydro
- diazepino
- indol
- oxo
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title description 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 2
- BSYFXFLGOGQHFU-UHFFFAOYSA-N pyrrolo[2,3-g][1,2]benzodiazepine Chemical class N1=NC=CC=C2C3=NC=CC3=CC=C21 BSYFXFLGOGQHFU-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims description 172
- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000000623 heterocyclic group Chemical group 0.000 claims description 59
- 125000001424 substituent group Chemical group 0.000 claims description 59
- 125000001072 heteroaryl group Chemical group 0.000 claims description 55
- AHDDRJBFJBDEPW-DTWKUNHWSA-N trans-2-Phenylcyclopropanecarboxylic acid Chemical compound OC(=O)[C@@H]1C[C@H]1C1=CC=CC=C1 AHDDRJBFJBDEPW-DTWKUNHWSA-N 0.000 claims description 47
- 125000003118 aryl group Chemical group 0.000 claims description 45
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 45
- 150000003839 salts Chemical class 0.000 claims description 42
- 125000003342 alkenyl group Chemical group 0.000 claims description 27
- 125000000304 alkynyl group Chemical group 0.000 claims description 23
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 19
- 101150050673 CHK1 gene Proteins 0.000 claims description 18
- -1 2-phenyl-cyclopropanecarbonyl Chemical group 0.000 claims description 15
- DLFVBJFMPXGRIB-UHFFFAOYSA-N thioacetamide Natural products CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims description 12
- 102000001253 Protein Kinase Human genes 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 108060006633 protein kinase Proteins 0.000 claims description 10
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims description 8
- CRSYCFLQNTZJCV-UHFFFAOYSA-N 6-amino-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-9-one Chemical compound C1=2C=3C=NNC(=O)C1=CC(N)=CC=2NC=3C1=CC=CC=C1 CRSYCFLQNTZJCV-UHFFFAOYSA-N 0.000 claims description 7
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 7
- 239000002246 antineoplastic agent Substances 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
- 239000002253 acid Substances 0.000 claims description 5
- 229940034982 antineoplastic agent Drugs 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 3
- 230000005855 radiation Effects 0.000 claims description 3
- WUEPMEXUMQVEGN-UHFFFAOYSA-N 2,2,2-trifluoroacetic acid;2,2,2-trifluoro-n-[2-[2-[(2,2,2-trifluoroacetyl)amino]ethylamino]ethyl]acetamide Chemical compound OC(=O)C(F)(F)F.FC(F)(F)C(=O)NCCNCCNC(=O)C(F)(F)F WUEPMEXUMQVEGN-UHFFFAOYSA-N 0.000 claims description 2
- DQCWXAWRJUKYAS-UHFFFAOYSA-N 2-(2,3-dihydro-1H-inden-2-yl)-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)acetamide Chemical compound C1C2=CC=CC=C2CC1CC(=O)NC(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CC=C1 DQCWXAWRJUKYAS-UHFFFAOYSA-N 0.000 claims description 2
- CZLDSCXHCDKQFT-UHFFFAOYSA-N 2-fluoro-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)-3-(trifluoromethyl)benzamide Chemical compound C1=CC=C(C(F)(F)F)C(F)=C1C(=O)NC1=CC(NC(C=2C=CC=CC=2)=C2C=NNC3=O)=C2C3=C1 CZLDSCXHCDKQFT-UHFFFAOYSA-N 0.000 claims description 2
- MVBMKCBHWGCQSV-UHFFFAOYSA-N 9-oxo-2-phenyl-N-(2-phenylcyclopropyl)-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaene-6-carboxamide Chemical compound C=1C(=C23)NC(C=4C=CC=CC=4)=C3C=NNC(=O)C2=CC=1C(=O)NC1CC1C1=CC=CC=C1 MVBMKCBHWGCQSV-UHFFFAOYSA-N 0.000 claims description 2
- SKMKTYFTYJMUAV-UHFFFAOYSA-N N-[1-(4-fluorophenyl)ethyl]-9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaene-6-carboxamide Chemical compound C=1C=C(F)C=CC=1C(C)NC(=O)C(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CC=C1 SKMKTYFTYJMUAV-UHFFFAOYSA-N 0.000 claims description 2
- 125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims description 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims 10
- NALBLJLOBICXRH-UHFFFAOYSA-N dinitrogen monohydride Chemical compound N=[N] NALBLJLOBICXRH-UHFFFAOYSA-N 0.000 claims 5
- HCUARRIEZVDMPT-UHFFFAOYSA-N Indole-2-carboxylic acid Chemical compound C1=CC=C2NC(C(=O)O)=CC2=C1 HCUARRIEZVDMPT-UHFFFAOYSA-N 0.000 claims 4
- DPKSIAPPUDIZGD-JOCHJYFZSA-N (2R)-2-hydroxy-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)-2-phenylacetamide Chemical compound O=C([C@H](O)C=1C=CC=CC=1)NC(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CC=C1 DPKSIAPPUDIZGD-JOCHJYFZSA-N 0.000 claims 2
- NFXMJZRICBRUKE-UHFFFAOYSA-N 2-(3,4-dihydro-1H-isoquinolin-2-yl)-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)acetamide Chemical compound C1CC2=CC=CC=C2CN1CC(=O)NC(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CC=C1 NFXMJZRICBRUKE-UHFFFAOYSA-N 0.000 claims 2
- AHDDRJBFJBDEPW-UHFFFAOYSA-N 2-phenylcyclopropane-1-carboxylic acid Chemical compound OC(=O)C1CC1C1=CC=CC=C1 AHDDRJBFJBDEPW-UHFFFAOYSA-N 0.000 claims 2
- HXEACLLIILLPRG-RXMQYKEDSA-N D-pipecolic acid Chemical compound OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N benzene carboxamide Natural products NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 208000035269 cancer or benign tumor Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- DILRJUIACXKSQE-UHFFFAOYSA-N n',n'-dimethylethane-1,2-diamine Chemical compound CN(C)CCN DILRJUIACXKSQE-UHFFFAOYSA-N 0.000 claims 2
- SSOLNOMRVKKSON-UHFFFAOYSA-N proguanil Chemical compound CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C=C1 SSOLNOMRVKKSON-UHFFFAOYSA-N 0.000 claims 2
- VHMBMZURJCYWQL-QWHCGFSZSA-N (1R,2R)-N-(2-bromo-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)-2-phenylcyclopropane-1-carboxamide Chemical compound C1([C@@H]2C[C@H]2C(=O)NC=2C=C3NC(=C4C3=C(C(NN=C4)=O)C=2)Br)=CC=CC=C1 VHMBMZURJCYWQL-QWHCGFSZSA-N 0.000 claims 1
- VWJCDWQVWASWJL-ZWKOTPCHSA-N (1R,2R)-N-(9-oxo-2-pyridin-3-yl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)-2-phenylcyclopropane-1-carboxamide Chemical compound O=C([C@H]1[C@@H](C1)C=1C=CC=CC=1)NC(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CN=C1 VWJCDWQVWASWJL-ZWKOTPCHSA-N 0.000 claims 1
- SZTQDTNQGMICST-ZWKOTPCHSA-N (1R,2R)-N-[2-[3-(dimethylamino)propyl]-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]-2-phenylcyclopropane-1-carboxamide Chemical compound C1([C@@H]2C[C@H]2C(=O)NC=2C=C3NC(=C4C3=C(C(NN=C4)=O)C=2)CCCN(C)C)=CC=CC=C1 SZTQDTNQGMICST-ZWKOTPCHSA-N 0.000 claims 1
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- TWYJYUIFEPPLLC-ZMBIFBSDSA-N (2R)-2-amino-2-(4-hydroxyphenyl)-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)acetamide hydrochloride Chemical compound Cl.O=C([C@H](N)C=1C=CC(O)=CC=1)NC(C=C1C(=O)NN=CC=2C=31)=CC=3NC=2C1=CC=CC=C1 TWYJYUIFEPPLLC-ZMBIFBSDSA-N 0.000 claims 1
- AHRFABYUKRWAOZ-ZMBIFBSDSA-N (2R)-2-amino-2-cyclohexyl-N-(9-oxo-2-phenyl-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl)acetamide 2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1([C@@H](N)C(=O)NC=2C=C3C(=O)NN=CC4=C(C=5C=CC=CC=5)NC(=C34)C=2)CCCCC1 AHRFABYUKRWAOZ-ZMBIFBSDSA-N 0.000 claims 1
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- SOXNMWXZIMFNRZ-UHFFFAOYSA-N N-[2-[3-[(dimethylamino)methyl]phenyl]-9-oxo-3,10,11-triazatricyclo[6.4.1.04,13]trideca-1,4,6,8(13),11-pentaen-6-yl]-2-fluoro-3-(trifluoromethyl)benzamide Chemical compound CN(C)CC1=CC=CC(C2=C3C4=C(C(NN=C3)=O)C=C(NC(=O)C=3C(=C(C=CC=3)C(F)(F)F)F)C=C4N2)=C1 SOXNMWXZIMFNRZ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- 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
- C07D487/06—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D498/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (1)
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|---|---|---|---|
| US43939603P | 2003-01-09 | 2003-01-09 |
Publications (1)
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| ZA200504674B true ZA200504674B (en) | 2006-07-26 |
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| ZA200504674A ZA200504674B (en) | 2003-01-09 | 2005-06-08 | Diazepinoindole derivatives as kinase inhibitors |
Country Status (35)
| Country | Link |
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| EP (2) | EP1585749B1 (el) |
| JP (1) | JP3990718B2 (el) |
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| AT (1) | ATE404564T1 (el) |
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| BR (1) | BRPI0406701A (el) |
| CA (1) | CA2512683C (el) |
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| EC (1) | ECSP055911A (el) |
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| HK (1) | HK1086257A1 (el) |
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| IL (1) | IL169082A (el) |
| IS (1) | IS7884A (el) |
| MA (1) | MA27703A1 (el) |
| MX (1) | MXPA05007352A (el) |
| NO (1) | NO20053775L (el) |
| NZ (1) | NZ540638A (el) |
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| PT (1) | PT1585749E (el) |
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| SI (1) | SI1585749T1 (el) |
| TN (1) | TNSN05176A1 (el) |
| UA (1) | UA80733C2 (el) |
| WO (1) | WO2004063198A1 (el) |
| ZA (1) | ZA200504674B (el) |
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| EP1467730A4 (en) * | 2002-01-22 | 2010-03-10 | Univ California | Non-steroid ligands for the glucocorticoid receptor, compositions and uses thereof |
| AU2004203977B2 (en) * | 2003-01-09 | 2010-06-17 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
| AU2006215413B2 (en) * | 2005-02-18 | 2010-10-07 | Astrazeneca Ab | Method for determining responsiveness to CHK1 inhibitors |
| UA92164C2 (ru) | 2005-03-29 | 2010-10-11 | Айкос Корпорейшен | Соединения, пригодные для угнетения снк1 |
| GB0510390D0 (en) * | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| NZ565378A (en) | 2005-06-29 | 2011-03-31 | Threshold Pharmaceuticals Inc | Phosphoramidate alkylator prodrugs |
| AU2006279541A1 (en) | 2005-08-15 | 2007-02-22 | The Regents Of The University Of California | VEGF-activated FAS ligands |
| US8143052B2 (en) | 2005-08-25 | 2012-03-27 | Ube Industries, Ltd. | Process for preparing optically active (S or R)-α amino acid and (R or S)-α amino acid ester in one phase organic reaction medium |
| WO2007025303A2 (en) * | 2005-08-26 | 2007-03-01 | The Regents Of The University Of California | Non-steroidal antiandrogens |
| EP2004655A1 (en) * | 2006-04-04 | 2008-12-24 | Pfizer Products Incorporated | Polymorphic forms of (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-methyl-1h-pyrazol-4 l)-1-oxo-2,6-dihydro-1h-ý1,2¨diazepinoý4,5,6-cd¨indol-8-yl)acetamide |
| RU2409361C2 (ru) * | 2006-04-04 | 2011-01-20 | Пфайзер Продактс Инк. | КОМБИНИРОВАННАЯ ТЕРАПИЯ (2R,Z)-2-АМИНО-2-ЦИКЛОГЕКСИЛ-N-(5-(1-МЕТИЛ-1Н-ПИРАЗОЛ-4-ИЛ)-1-ОКСО-2,6-ДИГИДРО-1Н-[1,2]ДИАЗЕПИНО[4,5,6-cd]ИНДОЛ-8-ИЛ)АЦЕТАМИДОМ |
| JP2010510222A (ja) * | 2006-11-17 | 2010-04-02 | シェーリング コーポレイション | 増殖性障害に対する併用療法 |
| US8158656B2 (en) * | 2008-05-16 | 2012-04-17 | Shenzhen Chipscreen Biosciences Ltd. | 2-indolinone derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors |
| ES2378513T3 (es) * | 2008-08-06 | 2012-04-13 | Pfizer Inc. | Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1 |
| EP2346881A1 (en) * | 2008-10-10 | 2011-07-27 | Priaxon AG | Novel compounds which modulate kinase activity |
| US8314108B2 (en) | 2008-12-17 | 2012-11-20 | Eli Lilly And Company | 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile, pharmaceutically acceptable salts thereof, or solvate of salts |
| US8663210B2 (en) | 2009-05-13 | 2014-03-04 | Novian Health, Inc. | Methods and apparatus for performing interstitial laser therapy and interstitial brachytherapy |
| US8211901B2 (en) | 2009-05-22 | 2012-07-03 | Shenzhen Chipscreen Biosciences Ltd. | Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors |
| CN101906076B (zh) | 2009-06-04 | 2013-03-13 | 深圳微芯生物科技有限责任公司 | 作为蛋白激酶抑制剂和组蛋白去乙酰化酶抑制剂的萘酰胺衍生物、其制备方法及应用 |
| EP2705036B1 (en) | 2011-05-06 | 2015-08-12 | Zafgen Inc. | Tricyclic sulfonamide compounds and methods of making and using same |
| US9254299B2 (en) | 2011-12-22 | 2016-02-09 | Threshold Pharmaceuticals, Inc. | Administration of hypoxia activated prodrugs in combination with Chk1 inhibitors for treating cancer |
| KR101684039B1 (ko) | 2011-12-31 | 2016-12-07 | 베이진 엘티디 | Parp 저해제로서의 융합된 테트라 또는 펜타-사이클릭 피리도프탈라지논 |
| SG11201401726VA (en) | 2011-12-31 | 2014-10-30 | Beigene Ltd | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
| CN102746211B (zh) * | 2012-06-27 | 2015-05-27 | 上海泰坦化学有限公司 | 一种取代吲哚-3-甲醛类化合物的制备方法 |
| TWI633107B (zh) * | 2013-05-22 | 2018-08-21 | 開曼群島商百濟神州生物科技有限公司 | 作為ｐａｒｐ抑制劑的稠合四或五環二氫二氮呯并咔唑酮 |
| US9993460B2 (en) | 2013-07-26 | 2018-06-12 | Race Oncology Ltd. | Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof |
| WO2015069489A1 (en) | 2013-11-06 | 2015-05-14 | Merck Patent Gmbh | Predictive biomarker for hypoxia-activated prodrug therapy |
| JP6936007B2 (ja) | 2014-06-17 | 2021-09-15 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ｃｈｋ１阻害剤とａｔｒ阻害剤との組み合わせを使用してがんを処置する方法 |
| AU2016312011B2 (en) * | 2015-08-25 | 2021-02-04 | Beigene, Ltd. | Process for preparing Parp inhibitor, crystalline forms, and uses thereof |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| CN110087730B (zh) | 2016-09-27 | 2023-03-28 | 百济神州(苏州)生物科技有限公司 | 使用包含parp抑制剂的组合产品治疗癌症 |
| JP6541635B2 (ja) * | 2016-10-28 | 2019-07-10 | ベイジーン リミテッド | Ｐａｒｐ阻害剤としての縮合四環式または縮合五環式ジヒドロジアゼピノカルバゾロン |
| TW201840564A (zh) | 2017-02-28 | 2018-11-16 | 英屬開曼群島商百濟神州有限公司 | 稠合的四環或五環二氫二氮呯幷哢唑酮的鹽的結晶形式及其用途 |
| US11661581B2 (en) * | 2017-05-25 | 2023-05-30 | University Of Massachusetts | Use of CDK inhibitors to enhance growth and self-renewal of progenitor cells |
| CN111108105B (zh) * | 2017-09-22 | 2023-03-31 | 朱比兰特埃皮帕德有限公司 | 作为pad抑制剂的杂环化合物 |
| EP3461480A1 (en) | 2017-09-27 | 2019-04-03 | Onxeo | Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer |
| EP3914284A4 (en) * | 2019-01-25 | 2022-10-26 | Numedii, Inc. | METHOD FOR THE TREATMENT OF IDIOPATHIC PULMONARY FIBROSIS |
| CN114072410B (zh) * | 2019-08-01 | 2023-08-01 | 正大天晴药业集团股份有限公司 | 作为parp抑制剂吲哚并七元酰肟化合物 |
| JP7260718B2 (ja) | 2019-11-29 | 2023-04-18 | メッドシャイン ディスカバリー インコーポレイテッド | ジアザインドール誘導体及びそのＣｈｋ１阻害剤としての使用 |
| CA3184988A1 (en) * | 2020-07-13 | 2022-01-20 | Ahmed Mamai | Nicotinamide phosphoribosyltransferase (nampt) inhibitor-conjugates and uses thereof |
| CN115698019A (zh) * | 2020-07-31 | 2023-02-03 | 正大天晴药业集团股份有限公司 | 用作parp抑制剂的吲哚并七元酰肟类似物的结晶及其制备方法 |
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| GB9722320D0 (en) | 1997-10-22 | 1997-12-17 | Janssen Pharmaceutica Nv | Human cell cycle checkpoint proteins |
| US6383744B1 (en) | 1998-07-10 | 2002-05-07 | Incyte Genomics, Inc. | Human checkpoint kinase |
| WO2000016781A1 (en) | 1998-09-18 | 2000-03-30 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
| AU781711B2 (en) | 1999-01-11 | 2005-06-09 | Agouron Pharmaceuticals, Inc. | Tricyclic inhibitors of poly(ADP-ribose) polymerases |
| WO2001016306A2 (en) | 1999-08-27 | 2001-03-08 | Chiron Corporation | Chimeric antisense oligonucleotides and cell transfecting formulations thereof |
| ECSP003637A (es) | 1999-08-31 | 2002-03-25 | Agouron Pharma | Inhibidores triciclicos de poli (adp-ribosa) polimerasas |
| US6670167B1 (en) | 1999-11-01 | 2003-12-30 | Agouron Pharmaceuticals, Inc. | Catalytic domain of the human effector cell cycle checkpoint protein kinase materials and methods for identification of inhibitors thereof |
| US6881575B1 (en) | 1999-09-22 | 2005-04-19 | Canbas Co., Ltd. | Compositions and methods for inhibiting G2 cell cycle arrest and sensitizing cells to DNA damaging agents |
| US6211164B1 (en) | 2000-03-10 | 2001-04-03 | Abbott Laboratories | Antisense oligonucleotides of the human chk1 gene and uses thereof |
| MXPA03004832A (es) * | 2000-12-01 | 2004-05-04 | Guilford Pharm Inc | Compuestos y sus usos. |
| UA76977C2 (en) | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
| AU2004203977B2 (en) * | 2003-01-09 | 2010-06-17 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
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2004
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- 2004-01-05 AP AP2005003353A patent/AP2048A/xx active
- 2004-01-05 DK DK04700145T patent/DK1585749T3/da active
- 2004-01-05 WO PCT/IB2004/000026 patent/WO2004063198A1/en active IP Right Grant
- 2004-01-05 RS YUP-2005/0522A patent/RS20050522A/sr unknown
- 2004-01-05 GE GEAP20048886A patent/GEP20084367B/en unknown
- 2004-01-05 PL PL378372A patent/PL378372A1/pl not_active Application Discontinuation
- 2004-01-05 SI SI200430830T patent/SI1585749T1/sl unknown
- 2004-01-05 DE DE602004015724T patent/DE602004015724D1/de not_active Expired - Lifetime
- 2004-01-05 AT AT04700145T patent/ATE404564T1/de not_active IP Right Cessation
- 2004-01-05 JP JP2006500278A patent/JP3990718B2/ja not_active Expired - Fee Related
- 2004-01-05 KR KR1020057012806A patent/KR100697746B1/ko not_active IP Right Cessation
- 2004-01-05 EP EP04700145A patent/EP1585749B1/en not_active Expired - Lifetime
- 2004-01-05 OA OA1200500197A patent/OA13017A/en unknown
- 2004-01-05 EA EA200500893A patent/EA009337B1/ru not_active IP Right Cessation
- 2004-01-05 CA CA2512683A patent/CA2512683C/en not_active Expired - Fee Related
- 2004-01-05 EP EP08155745A patent/EP1947102A1/en not_active Withdrawn
- 2004-01-05 CN CN2004800063838A patent/CN1759118B/zh not_active Expired - Fee Related
- 2004-01-05 BR BR0406701-0A patent/BRPI0406701A/pt not_active IP Right Cessation
- 2004-01-05 ES ES04700145T patent/ES2309484T3/es not_active Expired - Lifetime
- 2004-01-05 MX MXPA05007352A patent/MXPA05007352A/es active IP Right Grant
- 2004-01-05 PT PT04700145T patent/PT1585749E/pt unknown
- 2004-01-05 NZ NZ540638A patent/NZ540638A/en unknown
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- 2004-05-01 UA UAA200506730A patent/UA80733C2/uk unknown
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- 2005-06-08 ZA ZA200504674A patent/ZA200504674B/en unknown
- 2005-06-09 IS IS7884A patent/IS7884A/is unknown
- 2005-07-07 HR HR20050624A patent/HRP20050624A2/hr not_active Application Discontinuation
- 2005-07-08 EC EC2005005911A patent/ECSP055911A/es unknown
- 2005-07-08 MA MA28375A patent/MA27703A1/fr unknown
- 2005-07-08 TN TNP2005000176A patent/TNSN05176A1/fr unknown
- 2005-07-08 CR CR7899A patent/CR7899A/es unknown
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2006
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