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 (https=) | 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 |
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| PL2305221T3 (pl) | 2003-12-01 | 2015-11-30 | Kudos Pharm Ltd | Inhibitory naprawy uszkodzeń DNA w leczeniu raka |
| US20050228007A1 (en) | 2004-02-26 | 2005-10-13 | Prakash Jagtap | Isoquinoline derivatives and methods of use thereof |
| GB0419072D0 (en) | 2004-08-26 | 2004-09-29 | Kudos Pharm Ltd | Phthalazinone derivatives |
| PT1794163E (pt) * | 2004-09-22 | 2010-03-01 | Pfizer | Método para a preparação de inibidores de poli(adpribose)- polimerases |
| MX2007003314A (es) * | 2004-09-22 | 2007-08-06 | Pfizer | Combinaciones terapeuticas que comprenden inhibidor de poli(adp-ribosa)polimerasas. |
| ATE551345T1 (de) | 2004-09-22 | 2012-04-15 | Pfizer | Polymorphe formen des phosphatsalzes von 8-fluor- 2-ä4-ä(methylamino)methylüphenylü-1,3,4,5- tetrahydro-6h-azepinoä5,4,3-cdüindol-6-on |
| 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 |
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| JP2008531562A (ja) | 2005-02-25 | 2008-08-14 | イノテック ファーマシューティカルズ コーポレイション | 四環アミノ化合物および四環カルボキサミド化合物およびこれらの使用法 |
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| MX2008000462A (es) | 2005-07-14 | 2008-03-10 | Irm Llc | Compuestos heterotetraciclicos como mimeticos de tpo. |
| ZA200800907B (en) | 2005-07-18 | 2010-04-28 | Bipar Sciences Inc | Treatment of cancer |
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| EP1976515A2 (en) * | 2006-01-17 | 2008-10-08 | Abbott Laboratories | Combination therapy with parp inhibitors |
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| CN101534836B (zh) | 2006-09-05 | 2011-09-28 | 彼帕科学公司 | Parp抑制剂在制备治疗肥胖症的药物中的用途 |
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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 |
| MX2010002749A (es) | 2007-09-14 | 2010-06-25 | Astrazeneca Ab | Derivados de ftalazinona. |
| ES2504690T3 (es) | 2007-10-03 | 2014-10-08 | Eisai Inc. | Compuestos inhibidores de PARP, composiciones y métodos de uso |
| US7732491B2 (en) | 2007-11-12 | 2010-06-08 | 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 | |
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| 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 |
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| JP5699223B2 (ja) | 2010-12-02 | 2015-04-08 | シャンハイ デュァ ノボ ファルマテック カンパニー リミテッド | 複素環誘導体、その合成法および医療用途 |
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| CA2935857C (en) | 2014-01-05 | 2020-12-15 | Washington University | Radiolabeled tracers for poly (adp-ribose) polymerase-1 (parp-1), methods and uses therefor |
| 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 |
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| 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 |
| AU2016296905B2 (en) | 2015-07-23 | 2018-07-05 | Centre National De La Recherche Scientifique | 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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| CN107286166B (zh) * | 2016-04-11 | 2020-03-31 | 上海勋和医药科技有限公司 | 取代1，3，4，5-四氢-6h-吡咯并[4，3，2-ef][2]苯并氮杂-6-酮衍生物 |
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