KR101716012B1 - Parp 저해제로서의 융합된 테트라 또는 펜타-사이클릭 다이하이드로다이아제피노카르바졸론 - Google Patents
Parp 저해제로서의 융합된 테트라 또는 펜타-사이클릭 다이하이드로다이아제피노카르바졸론 Download PDFInfo
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- KR101716012B1 KR101716012B1 KR1020147018104A KR20147018104A KR101716012B1 KR 101716012 B1 KR101716012 B1 KR 101716012B1 KR 1020147018104 A KR1020147018104 A KR 1020147018104A KR 20147018104 A KR20147018104 A KR 20147018104A KR 101716012 B1 KR101716012 B1 KR 101716012B1
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- alkyl
- hydrogen
- compound
- cycloalkyl
- substituents
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- QXRPWODAKFREFD-SFHVURJKSA-N CC(C)(C)OC(N[C@@H](Cc1ccccc1)C(N(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O)=O)=O Chemical compound CC(C)(C)OC(N[C@@H](Cc1ccccc1)C(N(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O)=O)=O QXRPWODAKFREFD-SFHVURJKSA-N 0.000 description 1
- YADMFPWTDIQDHU-UHFFFAOYSA-N CC(C)(CC(c1c2[nH]c3cc(F)cc4c13)=NNC4=O)C2=O Chemical compound CC(C)(CC(c1c2[nH]c3cc(F)cc4c13)=NNC4=O)C2=O YADMFPWTDIQDHU-UHFFFAOYSA-N 0.000 description 1
- MHQFEYXRRZRKBA-UHFFFAOYSA-N CC(C)(Cc1c2c(c3cc(F)c4)c4[nH]1)CC2=NNC3=O Chemical compound CC(C)(Cc1c2c(c3cc(F)c4)c4[nH]1)CC2=NNC3=O MHQFEYXRRZRKBA-UHFFFAOYSA-N 0.000 description 1
- LNWPRZVIPZXIHL-UHFFFAOYSA-N CC(C)(Cc1c2c(c3ccc4)c4[n]1CCN1CCCCC1)CC2=NNC3=O Chemical compound CC(C)(Cc1c2c(c3ccc4)c4[n]1CCN1CCCCC1)CC2=NNC3=O LNWPRZVIPZXIHL-UHFFFAOYSA-N 0.000 description 1
- PNRLVHMYIPKIQD-UHFFFAOYSA-N CCN(CC)CC[n]1c2cccc3c2c2c1CCCC2=NNC3=O Chemical compound CCN(CC)CC[n]1c2cccc3c2c2c1CCCC2=NNC3=O PNRLVHMYIPKIQD-UHFFFAOYSA-N 0.000 description 1
- DAHUIBDZXNSUMD-UHFFFAOYSA-N CN(C)CCN(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O Chemical compound CN(C)CCN(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O DAHUIBDZXNSUMD-UHFFFAOYSA-N 0.000 description 1
- FQNVRHRLGXDLDH-UHFFFAOYSA-N CN(C)CC[n]1c2cc(F)cc(C(NN=C3C4)=O)c2c3c1CN4C(C1CC1)=O Chemical compound CN(C)CC[n]1c2cc(F)cc(C(NN=C3C4)=O)c2c3c1CN4C(C1CC1)=O FQNVRHRLGXDLDH-UHFFFAOYSA-N 0.000 description 1
- DENYZIUJOTUUNY-MRXNPFEDSA-N C[C@@](CCC1)(c2c3c(c4cc(F)c5)c5[nH]2)N1CC3=NNC4=O Chemical compound C[C@@](CCC1)(c2c3c(c4cc(F)c5)c5[nH]2)N1CC3=NNC4=O DENYZIUJOTUUNY-MRXNPFEDSA-N 0.000 description 1
- QRUNNSQWZBBFOG-OAHLLOKOSA-N C[C@@]1(c([nH]c2ccc3)cc2c3C(OC)=O)NCCC1 Chemical compound C[C@@]1(c([nH]c2ccc3)cc2c3C(OC)=O)NCCC1 QRUNNSQWZBBFOG-OAHLLOKOSA-N 0.000 description 1
- CKNPHWCEQJGVBL-UHFFFAOYSA-N C[n]1c2cccc(C(OC)=O)c2c2c1CCCC2=O Chemical compound C[n]1c2cccc(C(OC)=O)c2c2c1CCCC2=O CKNPHWCEQJGVBL-UHFFFAOYSA-N 0.000 description 1
- UFQXERGSNIOIJS-AWEZNQCLSA-N N[C@@H](Cc1ccccc1)C(N(Cc1c2c(c3ccc4)c4[nH]1)CC2=NNC3=O)=O Chemical compound N[C@@H](Cc1ccccc1)C(N(Cc1c2c(c3ccc4)c4[nH]1)CC2=NNC3=O)=O UFQXERGSNIOIJS-AWEZNQCLSA-N 0.000 description 1
- GDXWROWTQBURAK-UHFFFAOYSA-N O=C(c1ccccc1)ON(Cc([nH]c1c2)c3c1c1cc2F)CC3=NNC1=O Chemical compound O=C(c1ccccc1)ON(Cc([nH]c1c2)c3c1c1cc2F)CC3=NNC1=O GDXWROWTQBURAK-UHFFFAOYSA-N 0.000 description 1
- BMHYPRGJMZLOIG-UHFFFAOYSA-N O=C(c1ccccc1)ON(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O Chemical compound O=C(c1ccccc1)ON(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O BMHYPRGJMZLOIG-UHFFFAOYSA-N 0.000 description 1
- GGJVOTFHPYZESL-UHFFFAOYSA-N O=C1NN=C(CCC2)c3c2[nH]c2c3c1ccc2 Chemical compound O=C1NN=C(CCC2)c3c2[nH]c2c3c1ccc2 GGJVOTFHPYZESL-UHFFFAOYSA-N 0.000 description 1
- FLCHMGRFSJQORK-UHFFFAOYSA-N O=C1NN=C(CCCC2)c3c2[nH]c2cccc1c32 Chemical compound O=C1NN=C(CCCC2)c3c2[nH]c2cccc1c32 FLCHMGRFSJQORK-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2011/085148 WO2013097225A1 (en) | 2011-12-31 | 2011-12-31 | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20140107353A KR20140107353A (ko) | 2014-09-04 |
| KR101716012B1 true KR101716012B1 (ko) | 2017-03-13 |
Family
ID=48696280
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020147018104A Expired - Fee Related KR101716012B1 (ko) | 2011-12-31 | 2011-12-31 | Parp 저해제로서의 융합된 테트라 또는 펜타-사이클릭 다이하이드로다이아제피노카르바졸론 |
Country Status (29)
| Country | Link |
|---|---|
| US (4) | US9260440B2 (https=) |
| EP (2) | EP3315500B1 (https=) |
| JP (1) | JP6034877B2 (https=) |
| KR (1) | KR101716012B1 (https=) |
| CN (2) | CN103703004B (https=) |
| AU (1) | AU2011384858B2 (https=) |
| BR (1) | BR112014012628B8 (https=) |
| CA (1) | CA2856309C (https=) |
| CY (1) | CY1119804T1 (https=) |
| DK (1) | DK2797921T3 (https=) |
| EA (1) | EA027533B1 (https=) |
| ES (1) | ES2645814T3 (https=) |
| HR (1) | HRP20171883T1 (https=) |
| HU (1) | HUE035153T2 (https=) |
| IL (1) | IL233365A (https=) |
| IN (1) | IN2014DN06169A (https=) |
| LT (1) | LT2797921T (https=) |
| ME (1) | ME02855B (https=) |
| MX (1) | MX353578B (https=) |
| NO (1) | NO2797921T3 (https=) |
| NZ (1) | NZ624063A (https=) |
| PL (1) | PL2797921T3 (https=) |
| PT (1) | PT2797921T (https=) |
| RS (1) | RS56616B1 (https=) |
| SG (1) | SG11201401726VA (https=) |
| SI (1) | SI2797921T1 (https=) |
| SM (1) | SMT201700543T1 (https=) |
| WO (1) | WO2013097225A1 (https=) |
| ZA (1) | ZA201405560B (https=) |
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|---|---|---|---|---|
| IN2014DN06169A (https=) | 2011-12-31 | 2015-08-21 | Beigene Ltd | |
| CA2865511A1 (en) | 2012-03-07 | 2013-09-12 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| US9611223B2 (en) | 2013-09-11 | 2017-04-04 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| EP3341375B1 (en) * | 2015-08-25 | 2022-04-13 | BeiGene, Ltd. | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
| CN112745316A (zh) * | 2016-04-01 | 2021-05-04 | 里科瑞尔姆Ip控股有限责任公司 | 雌激素受体调节剂 |
| 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 |
| 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 |
| CN106883232B (zh) * | 2017-03-31 | 2019-01-22 | 苏州康润医药有限公司 | 一种氮杂非那烯-3-酮的衍生物及其制备方法与应用 |
| US20200155567A1 (en) * | 2017-07-17 | 2020-05-21 | Beigene, Ltd. | Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy |
| WO2019228499A1 (en) * | 2018-06-01 | 2019-12-05 | Beigene, Ltd. | Maintenance therapy of a parp inhibitor in treating gastric cancer |
| CN111171031B (zh) * | 2019-05-10 | 2021-04-09 | 百济神州(苏州)生物科技有限公司 | 一种含parp抑制剂倍半水合物产物的制备方法 |
| CN111171002B (zh) * | 2019-05-16 | 2021-04-06 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体的制备方法 |
| KR20220016028A (ko) * | 2019-05-31 | 2022-02-08 | 베이진 엘티디 | Parp 억제제 펠릿 제조 및 이의 제조방법 |
| CA3148221A1 (en) | 2019-08-06 | 2021-02-11 | Recurium Ip Holdings, Llc | Estrogen receptor modulators for treating mutants |
| WO2021046014A1 (en) | 2019-09-03 | 2021-03-11 | Teva Czech Industries S.R.O | Solid state forms of pamiparib and process for preparation thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025217307A1 (en) | 2024-04-09 | 2025-10-16 | Revolution Medicines, Inc. | Methods for predicting response to a ras(on) inhibitor and combination therapies |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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| WO2002044183A2 (en) | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| WO2004063198A1 (en) | 2003-01-09 | 2004-07-29 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
| WO2010017055A2 (en) | 2008-08-06 | 2010-02-11 | Lead Therapeutics, Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
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| SE445326B (sv) | 1983-04-05 | 1986-06-16 | Malmstroem Anders E H | Sett och anordning for forhindrande av veggturbulens |
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| CN101415417A (zh) | 2006-04-04 | 2009-04-22 | 辉瑞产品公司 | (2r,z)-2-氨基-2-环己基-n-(5-(1-甲基-1h-吡唑-4-基)-1-氧代-2,6-二氢-1h-[1,2]二氮杂卓并[4,5,6-cd]吲哚-8-基)乙酰胺的组合疗法 |
| WO2007113647A1 (en) | 2006-04-04 | 2007-10-11 | Pfizer Products Inc. | Polymorphic forms of (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-methyl-1h-pyrazol-4υl)-1-oxo-2,6-dihydro-1h-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide |
| ES2524787T3 (es) | 2007-11-15 | 2014-12-12 | Msd Italia S.R.L. | Derivados de piridazinona como inhibidores de PARP |
| WO2011130661A1 (en) | 2010-04-16 | 2011-10-20 | Biomarin Pharmaceutical Inc. | Methods of using dihydropyridophthalazinone inhibitors of poly (adp-ribose)polymerase (parp) |
| IN2014DN06169A (https=) | 2011-12-31 | 2015-08-21 | Beigene Ltd | |
| EA034666B1 (ru) | 2013-09-13 | 2020-03-04 | Бейджин Свитзерланд Гмбх | Антитело против pd-1 и его применение для лечения рака или вирусной инфекции и фрагмент антитела |
| TWI726608B (zh) | 2014-07-03 | 2021-05-01 | 英屬開曼群島商百濟神州有限公司 | 抗pd-l1抗體及其作為治療及診斷之用途 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| EP3341375B1 (en) | 2015-08-25 | 2022-04-13 | BeiGene, Ltd. | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
| 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 |
| 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 |
| US20200155567A1 (en) | 2017-07-17 | 2020-05-21 | Beigene, Ltd. | Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy |
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Patent Citations (3)
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| WO2002044183A2 (en) | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| WO2004063198A1 (en) | 2003-01-09 | 2004-07-29 | Pfizer Inc. | Diazepinoindole derivatives as kinase inhibitors |
| WO2010017055A2 (en) | 2008-08-06 | 2010-02-11 | Lead Therapeutics, Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
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