JP2002534523A5 - - Google Patents
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- JP2002534523A5 JP2002534523A5 JP2000593608A JP2000593608A JP2002534523A5 JP 2002534523 A5 JP2002534523 A5 JP 2002534523A5 JP 2000593608 A JP2000593608 A JP 2000593608A JP 2000593608 A JP2000593608 A JP 2000593608A JP 2002534523 A5 JP2002534523 A5 JP 2002534523A5
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- JP
- Japan
- Prior art keywords
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- pharmaceutically acceptable
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- acceptable salt
- aryl
- Prior art date
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- 150000003839 salts Chemical class 0.000 description 18
- 125000003118 aryl group Chemical group 0.000 description 16
- 239000002207 metabolite Substances 0.000 description 16
- 239000000651 prodrug Substances 0.000 description 16
- 229940002612 prodrug Drugs 0.000 description 16
- 239000012453 solvate Substances 0.000 description 16
- 125000003342 alkenyl group Chemical group 0.000 description 15
- 125000000217 alkyl group Chemical group 0.000 description 15
- 125000000304 alkynyl group Chemical group 0.000 description 15
- 150000001875 compounds Chemical class 0.000 description 15
- 102000004190 Enzymes Human genes 0.000 description 14
- 108090000790 Enzymes Proteins 0.000 description 14
- 125000000753 cycloalkyl group Chemical group 0.000 description 14
- 125000001072 heteroaryl group Chemical group 0.000 description 14
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 14
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 description 13
- 229910052736 halogen Inorganic materials 0.000 description 13
- 150000002367 halogens Chemical class 0.000 description 13
- 125000000547 substituted alkyl group Chemical group 0.000 description 12
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 description 11
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 description 11
- 230000002401 inhibitory effect Effects 0.000 description 8
- 0 *Cc(cc1)ccc1-c([n]c1ccc2)c(CN3)c1c2C3=O Chemical compound *Cc(cc1)ccc1-c([n]c1ccc2)c(CN3)c1c2C3=O 0.000 description 7
- 230000000694 effects Effects 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000012661 PARP inhibitor Substances 0.000 description 4
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 230000003013 cytotoxicity Effects 0.000 description 4
- 231100000135 cytotoxicity Toxicity 0.000 description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 125000001424 substituent group Chemical group 0.000 description 4
- 125000004093 cyano group Chemical group *C#N 0.000 description 3
- 102100037664 Poly [ADP-ribose] polymerase tankyrase-1 Human genes 0.000 description 2
- 102000012338 Poly(ADP-ribose) Polymerases Human genes 0.000 description 2
- 108010061844 Poly(ADP-ribose) Polymerases Proteins 0.000 description 2
- 108010017601 Tankyrases Proteins 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 230000001965 increasing effect Effects 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 2
- -1 nitro, amino Chemical group 0.000 description 2
- 229910052760 oxygen Inorganic materials 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 229910052717 sulfur Inorganic materials 0.000 description 2
- PKVZFELFJSNJPB-UHFFFAOYSA-N C#CCNC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O Chemical compound C#CCNC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O PKVZFELFJSNJPB-UHFFFAOYSA-N 0.000 description 1
- PELPWRMBLNFENG-NSCUHMNNSA-N C/C=C/c1cc([nH]c(Br)c2CCNC3=O)c2c3c1 Chemical compound C/C=C/c1cc([nH]c(Br)c2CCNC3=O)c2c3c1 PELPWRMBLNFENG-NSCUHMNNSA-N 0.000 description 1
- NWDFKLBRQRPNMY-UHFFFAOYSA-N C=C(CCCc1c(C(Nc2cc3ccccc3cc2)=O)[nH]2)c3c1c2ccc3 Chemical compound C=C(CCCc1c(C(Nc2cc3ccccc3cc2)=O)[nH]2)c3c1c2ccc3 NWDFKLBRQRPNMY-UHFFFAOYSA-N 0.000 description 1
- GTARMXPKNIBDGR-UHFFFAOYSA-N CC(C)NC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O Chemical compound CC(C)NC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O GTARMXPKNIBDGR-UHFFFAOYSA-N 0.000 description 1
- LHVVSOGORITFFH-UHFFFAOYSA-N CCCc1c(-c(cc2)ccc2S(C)=O)[nH]c2c1c(C(CC)=O)ccc2 Chemical compound CCCc1c(-c(cc2)ccc2S(C)=O)[nH]c2c1c(C(CC)=O)ccc2 LHVVSOGORITFFH-UHFFFAOYSA-N 0.000 description 1
- LYIUAHZNJYYRLK-UHFFFAOYSA-N CCCc1c(-c2ccc(CN3CCCC3)cc2)[nH]c2c1c(C(C=N)=O)cc(F)c2 Chemical compound CCCc1c(-c2ccc(CN3CCCC3)cc2)[nH]c2c1c(C(C=N)=O)cc(F)c2 LYIUAHZNJYYRLK-UHFFFAOYSA-N 0.000 description 1
- CVNBRRDKEKIBCA-UHFFFAOYSA-N CCCc1c(C(C(c2ccccc2)=N)=O)[nH]c2cccc(C(C)=O)c12 Chemical compound CCCc1c(C(C(c2ccccc2)=N)=O)[nH]c2cccc(C(C)=O)c12 CVNBRRDKEKIBCA-UHFFFAOYSA-N 0.000 description 1
- VBWVXWCLBKEBCB-UHFFFAOYSA-N CCCc1c(C(Nc(cc2)ccc2Cl)=O)[nH]c2cccc(C=O)c12 Chemical compound CCCc1c(C(Nc(cc2)ccc2Cl)=O)[nH]c2cccc(C=O)c12 VBWVXWCLBKEBCB-UHFFFAOYSA-N 0.000 description 1
- OZSBLJFTXFBONL-UHFFFAOYSA-N CNC(c1c(CCNC(C2CC=C3)=O)c2c3[nH]1)=O Chemical compound CNC(c1c(CCNC(C2CC=C3)=O)c2c3[nH]1)=O OZSBLJFTXFBONL-UHFFFAOYSA-N 0.000 description 1
- KKWMDDGYIRVOMY-UHFFFAOYSA-N CNCc1cccc(-c2c(CCNC(c3cc(F)c4)=O)c3c4[nH]2)c1 Chemical compound CNCc1cccc(-c2c(CCNC(c3cc(F)c4)=O)c3c4[nH]2)c1 KKWMDDGYIRVOMY-UHFFFAOYSA-N 0.000 description 1
- TVTOPSASQLZYEB-UHFFFAOYSA-N COc(ccc(Cl)c1)c1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1 Chemical compound COc(ccc(Cl)c1)c1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1 TVTOPSASQLZYEB-UHFFFAOYSA-N 0.000 description 1
- QMCBHIPGPJWTMX-UHFFFAOYSA-N CS(c(cc1)ccc1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1)(=O)=O Chemical compound CS(c(cc1)ccc1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1)(=O)=O QMCBHIPGPJWTMX-UHFFFAOYSA-N 0.000 description 1
- MRDWIBPBWIAABA-UHFFFAOYSA-N CSc(cc1)ccc1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1 Chemical compound CSc(cc1)ccc1-c1c(CCNC(c2ccc3)=O)c2c3[nH]1 MRDWIBPBWIAABA-UHFFFAOYSA-N 0.000 description 1
- SYGXSZZARIQGNS-UHFFFAOYSA-N C[n](cc1CN(C)C2=O)c3c1c2ccc3 Chemical compound C[n](cc1CN(C)C2=O)c3c1c2ccc3 SYGXSZZARIQGNS-UHFFFAOYSA-N 0.000 description 1
- VXHGKYBDQFTADR-UHFFFAOYSA-N C[n](cc1CNC2=O)c3c1c2ccc3 Chemical compound C[n](cc1CNC2=O)c3c1c2ccc3 VXHGKYBDQFTADR-UHFFFAOYSA-N 0.000 description 1
- UGQGSXIPHIMFTJ-UHFFFAOYSA-N Cc1cc(C(CCCc2c(-c3ccc(CNC)cc3)[nH]3)=O)c2c3c1 Chemical compound Cc1cc(C(CCCc2c(-c3ccc(CNC)cc3)[nH]3)=O)c2c3c1 UGQGSXIPHIMFTJ-UHFFFAOYSA-N 0.000 description 1
- VNUZUFYYLSIZFY-UHFFFAOYSA-N N=C(CC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O)C1CC1 Chemical compound N=C(CC(c([nH]c1ccc2)c(CCN3)c1c2C3=O)=O)C1CC1 VNUZUFYYLSIZFY-UHFFFAOYSA-N 0.000 description 1
- SMQBDMFORQBOIM-UHFFFAOYSA-N O=C(c1cccc([nH]2)c11)NCc1c2Br Chemical compound O=C(c1cccc([nH]2)c11)NCc1c2Br SMQBDMFORQBOIM-UHFFFAOYSA-N 0.000 description 1
- IHJPJQJALQHPFF-UHFFFAOYSA-N O=C1NCCc2c(-c3c(CCNC(c4ccc5)=O)c4c5[nH]3)[nH]c3c2c1ccc3 Chemical compound O=C1NCCc2c(-c3c(CCNC(c4ccc5)=O)c4c5[nH]3)[nH]c3c2c1ccc3 IHJPJQJALQHPFF-UHFFFAOYSA-N 0.000 description 1
- OADDPRZHUAMSOC-UHFFFAOYSA-N O=C1NCCc2c(-c3ccc(CCN4CCCC4)cc3)[nH]c3cccc1c23 Chemical compound O=C1NCCc2c(-c3ccc(CCN4CCCC4)cc3)[nH]c3cccc1c23 OADDPRZHUAMSOC-UHFFFAOYSA-N 0.000 description 1
- AMXUETXVQWSXKX-UHFFFAOYSA-N O=C1NCCc2c(-c3cccc(-c4ccccc4)c3)[nH]c3c2C1CC=C3 Chemical compound O=C1NCCc2c(-c3cccc(-c4ccccc4)c3)[nH]c3c2C1CC=C3 AMXUETXVQWSXKX-UHFFFAOYSA-N 0.000 description 1
- IYQQQOPMPOKHBL-UHFFFAOYSA-N O=C1NCc2c(-c3ccccc3)[nH]c3cccc1c23 Chemical compound O=C1NCc2c(-c3ccccc3)[nH]c3cccc1c23 IYQQQOPMPOKHBL-UHFFFAOYSA-N 0.000 description 1
- QXBNJYBFEBEQQQ-UHFFFAOYSA-N O=Cc(cc1)ccc1-c([nH]c1ccc2)c(CN3)c1c2C3=O Chemical compound O=Cc(cc1)ccc1-c([nH]c1ccc2)c(CN3)c1c2C3=O QXBNJYBFEBEQQQ-UHFFFAOYSA-N 0.000 description 1
- 125000002252 acyl group Chemical group 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11543199P | 1999-01-11 | 1999-01-11 | |
| US60/115,431 | 1999-01-11 | ||
| PCT/US2000/000411 WO2000042040A1 (en) | 1999-01-11 | 2000-01-10 | Tricyclic inhibitors of poly(adp-ribose) polymerases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2002534523A JP2002534523A (ja) | 2002-10-15 |
| JP2002534523A5 true JP2002534523A5 (cg-RX-API-DMAC10.html) | 2006-09-21 |
| JP4093448B2 JP4093448B2 (ja) | 2008-06-04 |
Family
ID=22361361
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2000593608A Expired - Lifetime JP4093448B2 (ja) | 1999-01-11 | 2000-01-10 | ポリ(adp−リボース)ポリメラーゼの三環系阻害剤 |
Country Status (39)
Families Citing this family (124)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6291425B1 (en) | 1999-09-01 | 2001-09-18 | Guilford Pharmaceuticals Inc. | Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage |
| WO2001023390A2 (de) * | 1999-09-28 | 2001-04-05 | Basf Aktiengesellschaft | Azepinoindol-derivate, deren herstellung und anwendung |
| US6589725B1 (en) | 1999-10-25 | 2003-07-08 | Rigel Pharmaceuticals, Inc. | Tankyrase H, compositions involved in the cell cycle and methods of use |
| US6531464B1 (en) | 1999-12-07 | 2003-03-11 | Inotek Pharmaceutical Corporation | Methods for the treatment of neurodegenerative disorders using substituted phenanthridinone derivatives |
| US6476048B1 (en) | 1999-12-07 | 2002-11-05 | Inotek Pharamaceuticals Corporation | Substituted phenanthridinones and methods of use thereof |
| CZ20023110A3 (cs) * | 2000-03-20 | 2003-02-12 | N-Gene Research Laboratories Inc. | Deriváty amidoximu propenkarboxylové kyseliny, způsob jejich přípravy a farmaceutické přípravky je obsahující |
| US6534651B2 (en) | 2000-04-06 | 2003-03-18 | Inotek Pharmaceuticals Corp. | 7-Substituted isoindolinone inhibitors of inflammation and reperfusion injury and methods of use thereof |
| ATE478664T1 (de) | 2000-12-01 | 2010-09-15 | Eisai Inc | Azaphenanthridone-derivate und deren verwendung als parp-inhibitoren |
| DE60218458T2 (de) | 2001-05-08 | 2007-11-15 | Kudos Pharmaceuticals Ltd. | Isochinolinon derivate als parp inhibitoren |
| AU2002331621B2 (en) | 2001-08-15 | 2008-06-05 | Icos Corporation | 2H-phthalazin-1-ones and methods for use thereof |
| US6956035B2 (en) | 2001-08-31 | 2005-10-18 | Inotek Pharmaceuticals Corporation | Isoquinoline derivatives and methods of use thereof |
| US20030096833A1 (en) | 2001-08-31 | 2003-05-22 | Jagtap Prakash G. | Substituted ideno[1,2-c]isoquinoline derivatives and methods of use thereof |
| WO2003051879A1 (en) * | 2001-12-14 | 2003-06-26 | Altana Pharma Ag | Known and novel 4,5-dihydro-imidazo[4,5,1-ij]quinolin-6-ones useful as poly(adp-ribose)polymerase inhibitors |
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| GB0317466D0 (en) * | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| NZ544989A (en) * | 2003-07-25 | 2009-10-30 | Cancer Rec Tech Ltd | Tricyclic PARP inhibitors |
| BRPI0417056A (pt) | 2003-12-01 | 2007-02-06 | Kudos Pharm Ltd | inibidores de reparo de dano no dna para tratamento de cáncer |
| MXPA06009701A (es) | 2004-02-26 | 2007-03-26 | Inotek Pharmaceuticals Corp | Derivados de isoquinolina y metodos de uso de los mismos. |
| GB0419072D0 (en) | 2004-08-26 | 2004-09-29 | Kudos Pharm Ltd | Phthalazinone derivatives |
| MX2007002461A (es) * | 2004-09-22 | 2008-03-13 | Pfizer | Formas polimorficas y amorfas de la sal fosfato de 8-fluoro-2-{4-[metilamino)metil]fenil}-1, 3, 4, 5-tetrahidro-6h-azepino [5, 4, 3-cd]indol-6-ona. |
| MX2007003314A (es) * | 2004-09-22 | 2007-08-06 | Pfizer | Combinaciones terapeuticas que comprenden inhibidor de poli(adp-ribosa)polimerasas. |
| MX2007003311A (es) * | 2004-09-22 | 2007-05-16 | Pfizer | Procedimiento para preparar inhibidores de poli (adp-ribosa) polimerasas. |
| CN101133061B (zh) * | 2004-09-22 | 2011-09-07 | 辉瑞有限公司 | 8-氟-2-{4-[(甲基氨基)甲基]苯基}-1,3,4,5-四氢-6H-氮杂卓并[5,4,3-cd]吲哚-6-酮的磷酸盐的多晶型物和非晶物 |
| EP1841771A4 (en) | 2005-01-19 | 2008-09-24 | Mgi Gp Inc | COMPOUNDS OF DIAZABENZO [DE] ANTHRACENE-3-ONE AND USE IN INHIBITION OF PARP |
| BRPI0606191A2 (pt) | 2005-02-25 | 2009-06-09 | Inotek Pharmaceuticals Corp | compostos de amino e carboxamido tetracìclicos e métodos do seu uso |
| US7402596B2 (en) | 2005-03-24 | 2008-07-22 | Renovis, Inc. | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof |
| DE102005022111A1 (de) * | 2005-05-12 | 2006-11-16 | Siemens Ag | Verfahren zum Datenaustausch |
| JPWO2006137510A1 (ja) | 2005-06-24 | 2009-01-22 | 小野薬品工業株式会社 | 脳血管障害時における出血低減剤 |
| ATE478863T1 (de) | 2005-07-14 | 2010-09-15 | Irm Llc | Heterotetracyclische verbindungen als tpo- mimetica |
| NZ587586A (en) | 2005-07-18 | 2012-04-27 | Bipar Sciences Inc | Treatment of cancer |
| WO2007025009A2 (en) | 2005-08-24 | 2007-03-01 | Inotek Pharmaceuticals Corporation | Indenoisoquinolinone analogs and methods of use thereof |
| GB0521373D0 (en) | 2005-10-20 | 2005-11-30 | Kudos Pharm Ltd | Pthalazinone derivatives |
| CN101370497B (zh) * | 2006-01-17 | 2010-11-17 | 雅培制药有限公司 | 包含parp抑制剂和细胞毒性剂的联合产品及用途 |
| TWI464148B (zh) | 2006-03-16 | 2014-12-11 | Evotec Us Inc | 作為p2x7調節劑之雙環雜芳基化合物與其用途 |
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| WO2008154129A1 (en) * | 2007-06-08 | 2008-12-18 | Bausch & Lomb Incorporated | Pharmaceutical compositions and method for treating, reducing, ameliorating, alleviating, or preventing dry eye |
| RU2010108008A (ru) | 2007-09-14 | 2011-10-20 | Астразенека Аб (Se) | Фталазиноновые производные |
| JP5439380B2 (ja) | 2007-10-03 | 2014-03-12 | エーザイ インク. | Parp阻害化合物、組成物及び使用方法 |
| CA2705537A1 (en) | 2007-11-12 | 2009-05-22 | Bipar Sciences, Inc. | Treatment of breast cancer with a parp inhibitor alone or in combination with anti-tumor agents |
| UY31603A1 (es) | 2008-01-23 | 2009-08-31 | Derivados de ftalazinona | |
| GB0804755D0 (en) | 2008-03-14 | 2008-04-16 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| RS55157B2 (sr) | 2008-10-07 | 2023-10-31 | Kudos Pharm Ltd | Farmaceutska formulacija 514 |
| WO2011058367A2 (en) | 2009-11-13 | 2011-05-19 | Astrazeneca Ab | Diagnostic test for predicting responsiveness to treatment with poly(adp-ribose) polymerase (parp) inhibitor |
| KR100986820B1 (ko) * | 2010-01-27 | 2010-10-12 | (주)에코베이스 | 막힘방지형 고효율 산기장치 및 이를 이용한 수질정화장치 |
| KR20120127495A (ko) | 2010-02-12 | 2012-11-21 | 화이자 인코포레이티드 | 8-플루오로-2-{4-[(메틸아미노)메틸]페닐}-1,3,4,5-테트라하이드로-6h-아제피노[5,4,3-cd]인돌-6-온의 염 및 다형체 |
| EP2646428B1 (en) | 2010-12-02 | 2016-06-01 | Shanghai De Novo Pharmatech Co Ltd. | Heterocyclic derivatives, preparation processes and medical uses thereof |
| CN103703004B (zh) | 2011-12-31 | 2016-06-29 | 百济神州有限公司 | 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 |
| MX2014008071A (es) | 2011-12-31 | 2015-07-06 | Beigene Ltd | Tetra o penta-piridoftalazinonas ciclicas fusionadas como inhibidores de poli(adenosin-difosfato-ribosa)polimerasas. |
| WO2014073447A1 (ja) | 2012-11-08 | 2014-05-15 | 日本化薬株式会社 | カンプトテシン類と抗癌効果増強剤の結合した高分子化合物及びその用途 |
| JP6407303B2 (ja) | 2014-01-05 | 2018-10-17 | ワシントン・ユニバーシティWashington University | ポリ(adp−リボース)ポリメラーゼ−1(parp−1)のための放射標識トレーサー、その方法および使用 |
| CN103772395B (zh) * | 2014-01-23 | 2016-05-11 | 中国药科大学 | 一类具有parp抑制活性的化合物、其制备方法及用途 |
| DK3157566T3 (da) | 2014-06-17 | 2019-07-22 | Vertex Pharma | Fremgangsmåde til behandling af cancer under anvendelse af en kombination chk1- og atr-inhibitorer |
| KR102803917B1 (ko) | 2014-08-22 | 2025-05-07 | 파르마& 슈바이츠 게엠베하 | 루카파립의 고 용량 강도 정제 |
| CN105607772B (zh) * | 2014-11-13 | 2020-11-03 | 现代自动车株式会社 | 触摸输入装置以及包括该装置的车辆 |
| TW201702218A (zh) | 2014-12-12 | 2017-01-16 | 美國杰克森實驗室 | 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法 |
| EP3265560B1 (en) | 2015-03-02 | 2021-12-08 | Sinai Health System | Homologous recombination factors |
| WO2017013237A1 (en) | 2015-07-23 | 2017-01-26 | Institut Curie | Use of a combination of dbait molecule and parp inhibitors to treat cancer |
| EA037366B1 (ru) | 2015-08-25 | 2021-03-18 | Бейджин, Лтд. | Способ получения ингибитора parp, кристаллические формы и их применения |
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