CN103703004B - 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 - Google Patents
作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 Download PDFInfo
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- CN103703004B CN103703004B CN201180072418.8A CN201180072418A CN103703004B CN 103703004 B CN103703004 B CN 103703004B CN 201180072418 A CN201180072418 A CN 201180072418A CN 103703004 B CN103703004 B CN 103703004B
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- alkyl
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- hydrogen
- optionally substituted
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- 0 CCCC(C1)C(CC(C)(C)CCC)*C(CC(*)CC)*1C1C(C)(CC(C)=C)CC1 Chemical compound CCCC(C1)C(CC(C)(C)CCC)*C(CC(*)CC)*1C1C(C)(CC(C)=C)CC1 0.000 description 4
- MWIUPFYRAAIUMB-UHFFFAOYSA-N CC(C)(C(N(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O)=O)N Chemical compound CC(C)(C(N(Cc1c2c3c4cccc3[nH]1)CC2=NNC4=O)=O)N MWIUPFYRAAIUMB-UHFFFAOYSA-N 0.000 description 1
- UNRIMNNIMOSTHC-UHFFFAOYSA-N CC(C)(C)C(N(Cc1c2c(c3cc(F)c4)c4[nH]1)CC2=NNC3=O)=O Chemical compound CC(C)(C)C(N(Cc1c2c(c3cc(F)c4)c4[nH]1)CC2=NNC3=O)=O UNRIMNNIMOSTHC-UHFFFAOYSA-N 0.000 description 1
- HVLHCCLUCAZHED-UHFFFAOYSA-N CC(C)C(C)C(N(CC1N(C)N2)Cc([nH]c3ccc4)c1c3c4C2=O)=O Chemical compound CC(C)C(C)C(N(CC1N(C)N2)Cc([nH]c3ccc4)c1c3c4C2=O)=O HVLHCCLUCAZHED-UHFFFAOYSA-N 0.000 description 1
- YCKLPKOFOIMITK-UHFFFAOYSA-N CN(C)CC[n]1c2cccc(C(NN=C3C4)=O)c2c3c1CN4C(C1CC1)=O Chemical compound CN(C)CC[n]1c2cccc(C(NN=C3C4)=O)c2c3c1CN4C(C1CC1)=O YCKLPKOFOIMITK-UHFFFAOYSA-N 0.000 description 1
- DENYZIUJOTUUNY-MRXNPFEDSA-N C[C@@](CCC1)(c([nH]c2c3)c4c2c2cc3F)N1CC4=NNC2=O Chemical compound C[C@@](CCC1)(c([nH]c2c3)c4c2c2cc3F)N1CC4=NNC2=O DENYZIUJOTUUNY-MRXNPFEDSA-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)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (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)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610603192.4A CN106220635B (zh) | 2011-12-31 | 2011-12-31 | 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 |
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610603192.4A Division CN106220635B (zh) | 2011-12-31 | 2011-12-31 | 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103703004A CN103703004A (zh) | 2014-04-02 |
| CN103703004B true CN103703004B (zh) | 2016-06-29 |
Family
ID=48696280
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610603192.4A Active CN106220635B (zh) | 2011-12-31 | 2011-12-31 | 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 |
| CN201180072418.8A Active CN103703004B (zh) | 2011-12-31 | 2011-12-31 | 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610603192.4A Active CN106220635B (zh) | 2011-12-31 | 2011-12-31 | 作为parp抑制剂的稠合的四环或五环的二氢二氮杂*并咔唑酮 |
Country Status (29)
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011384858B2 (en) | 2011-12-31 | 2016-05-05 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors |
| DK2822656T3 (en) | 2012-03-07 | 2017-01-30 | Inst Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| CA2922469A1 (en) | 2013-09-11 | 2015-03-19 | Institute Of Cancer Research: Royal Cancer Hospital (The) | 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use |
| IL296835A (en) * | 2015-08-25 | 2022-11-01 | Beigene Ltd | Process for preparing parp inhibitor, crystalline forms, and uses thereof |
| AU2017242027B2 (en) | 2016-04-01 | 2020-10-08 | Recurium Ip Holdings, Llc | Estrogen receptor modulators |
| 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 |
| CN110392687B (zh) * | 2017-02-28 | 2022-08-02 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式及其用途 |
| 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 |
| CN112292133A (zh) * | 2018-06-01 | 2021-01-29 | 百济神州有限公司 | 在胃癌治疗中的parp抑制剂维持疗法 |
| CN113004279B (zh) * | 2019-05-10 | 2023-01-06 | 百济神州(苏州)生物科技有限公司 | 一种控制含parp抑制剂倍半水合物产物的含水量的方法 |
| CN113402502B (zh) * | 2019-05-16 | 2022-10-14 | 百济神州(苏州)生物科技有限公司 | 一种parp抑制剂中间体制备的物料组合体系 |
| MX2021014339A (es) * | 2019-05-31 | 2022-01-06 | Beigene Ltd | Preparacion de granulo inhibidor de parp y proceso de preparacion del mismo. |
| KR20220044528A (ko) | 2019-08-06 | 2022-04-08 | 리커리엄 아이피 홀딩스, 엘엘씨 | 돌연변이체를 치료하기 위한 에스트로겐 수용체 조절제 |
| WO2021046014A1 (en) | 2019-09-03 | 2021-03-11 | Teva Czech Industries S.R.O | Solid state forms of pamiparib and process for preparation thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002044183A2 (en) * | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| CN1759118A (zh) * | 2003-01-09 | 2006-04-12 | 美国辉瑞有限公司 | 作为激酶抑制剂的二氮杂䓬并吲哚衍生物 |
| WO2010017055A2 (en) * | 2008-08-06 | 2010-02-11 | Lead Therapeutics, Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE445326B (sv) | 1983-04-05 | 1986-06-16 | Malmstroem Anders E H | Sett och anordning for forhindrande av veggturbulens |
| US6799298B2 (en) | 1998-03-11 | 2004-09-28 | Overture Services, Inc. | Technique for locating an item of interest within a stored representation of data |
| RS50031B (sr) | 1999-01-11 | 2008-11-28 | Agouron Pharmaceuticals Inc., | Triciklični inhibitori poli(adp-riboza)polimeraza |
| US6423705B1 (en) | 2001-01-25 | 2002-07-23 | Pfizer Inc. | Combination therapy |
| US6906096B2 (en) | 2002-06-28 | 2005-06-14 | Irm Llc | 4,7-Disubstituted indoles and methods of making |
| WO2004105700A2 (en) | 2003-05-28 | 2004-12-09 | Guildford Pharmaceuticals, Inc. | Compounds, methods and pharmaceutical compositions for inhibiting parp |
| 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 |
| BRPI0709731A2 (pt) | 2006-04-04 | 2011-07-26 | Pfizer Prod Inc | terapia de combinaÇço de (2r,z)-2-amino-2-cicloexil-n-(5-(1-metil-1h-pirazol-4-il)-1- oxo-2,6-diidro-1h-[1,2]diazepino[4,5,6-cd]indol-8-il)acet amida |
| KR101641596B1 (ko) | 2007-11-15 | 2016-07-21 | 엠에스디 이탈리아 에스.알.엘. | Ｐａｒｐ 억제제로서의 피리다지논 유도체 |
| WO2011130661A1 (en) | 2010-04-16 | 2011-10-20 | Biomarin Pharmaceutical Inc. | Methods of using dihydropyridophthalazinone inhibitors of poly (adp-ribose)polymerase (parp) |
| AU2011384858B2 (en) | 2011-12-31 | 2016-05-05 | Beigene, Ltd. | Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as PARP inhibitors |
| BR112016005408B1 (pt) | 2013-09-13 | 2023-03-21 | Beigene Switzerland Gmbh | Anticorpos anti-pd1, f(ab) ou f(ab)2 e uso referido anticorpo para tratamento de cancer ou infecção viral |
| KR102130600B1 (ko) | 2014-07-03 | 2020-07-08 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
| US9637488B2 (en) | 2015-01-29 | 2017-05-02 | Fuqiang Ruan | Heterocyclic compounds as inhibitors of class I PI3KS |
| IL296835A (en) | 2015-08-25 | 2022-11-01 | 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 |
| CN110392687B (zh) | 2017-02-28 | 2022-08-02 | 百济神州(苏州)生物科技有限公司 | 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式及其用途 |
| US20200155567A1 (en) | 2017-07-17 | 2020-05-21 | Beigene, Ltd. | Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy |
-
2011
- 2011-12-31 AU AU2011384858A patent/AU2011384858B2/en not_active Ceased
- 2011-12-31 EA EA201491303A patent/EA027533B1/ru not_active IP Right Cessation
- 2011-12-31 NO NO11878508A patent/NO2797921T3/no unknown
- 2011-12-31 HU HUE11878508A patent/HUE035153T2/en unknown
- 2011-12-31 JP JP2014549295A patent/JP6034877B2/ja not_active Expired - Fee Related
- 2011-12-31 EP EP17183473.2A patent/EP3315500B1/en active Active
- 2011-12-31 ME MEP-2017-278A patent/ME02855B/me unknown
- 2011-12-31 BR BR112014012628A patent/BR112014012628B8/pt active IP Right Grant
- 2011-12-31 RS RS20171228A patent/RS56616B1/sr unknown
- 2011-12-31 WO PCT/CN2011/085148 patent/WO2013097225A1/en not_active Application Discontinuation
- 2011-12-31 EP EP11878508.8A patent/EP2797921B1/en active Active
- 2011-12-31 ES ES11878508.8T patent/ES2645814T3/es active Active
- 2011-12-31 HR HRP20171883TT patent/HRP20171883T1/hr unknown
- 2011-12-31 CA CA2856309A patent/CA2856309C/en active Active
- 2011-12-31 MX MX2014007840A patent/MX353578B/es active IP Right Grant
- 2011-12-31 CN CN201610603192.4A patent/CN106220635B/zh active Active
- 2011-12-31 CN CN201180072418.8A patent/CN103703004B/zh active Active
- 2011-12-31 NZ NZ624063A patent/NZ624063A/en not_active IP Right Cessation
- 2011-12-31 SI SI201131351T patent/SI2797921T1/en unknown
- 2011-12-31 KR KR1020147018104A patent/KR101716012B1/ko active Active
- 2011-12-31 LT LTEP11878508.8T patent/LT2797921T/lt unknown
- 2011-12-31 SG SG11201401726VA patent/SG11201401726VA/en unknown
- 2011-12-31 PL PL11878508T patent/PL2797921T3/pl unknown
- 2011-12-31 SM SM20170543T patent/SMT201700543T1/it unknown
- 2011-12-31 IN IN6169DEN2014 patent/IN2014DN06169A/en unknown
- 2011-12-31 US US14/369,374 patent/US9260440B2/en active Active
- 2011-12-31 DK DK11878508.8T patent/DK2797921T3/en active
- 2011-12-31 PT PT118785088T patent/PT2797921T/pt unknown
-
2014
- 2014-06-25 IL IL233365A patent/IL233365A/en active IP Right Grant
- 2014-07-28 ZA ZA2014/05560A patent/ZA201405560B/en unknown
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2016
- 2016-01-05 US US14/988,484 patent/US9617273B2/en not_active Expired - Fee Related
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2017
- 2017-04-05 US US15/479,958 patent/US10112952B2/en active Active
- 2017-11-16 CY CY20171101198T patent/CY1119804T1/el unknown
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2018
- 2018-09-19 US US16/135,512 patent/US10501467B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002044183A2 (en) * | 2000-12-01 | 2002-06-06 | Guilford Pharmaceuticals Inc. | Benzoazepine and benzodiazepine derivatives and their use as parp inhibitors |
| CN1759118A (zh) * | 2003-01-09 | 2006-04-12 | 美国辉瑞有限公司 | 作为激酶抑制剂的二氮杂䓬并吲哚衍生物 |
| WO2010017055A2 (en) * | 2008-08-06 | 2010-02-11 | Lead Therapeutics, Inc. | Dihydropyridophthalazinone inhibitors of poly(adp-ribose)polymerase (parp) |
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