JP2003513015A5 - - Google Patents
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- Publication number
- JP2003513015A5 JP2003513015A5 JP2001519702A JP2001519702A JP2003513015A5 JP 2003513015 A5 JP2003513015 A5 JP 2003513015A5 JP 2001519702 A JP2001519702 A JP 2001519702A JP 2001519702 A JP2001519702 A JP 2001519702A JP 2003513015 A5 JP2003513015 A5 JP 2003513015A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- aryl
- heterocycloalkyl
- alkynyl
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000001072 heteroaryl group Chemical group 0.000 description 119
- 125000003118 aryl group Chemical group 0.000 description 117
- 125000000304 alkynyl group Chemical group 0.000 description 112
- 125000000753 cycloalkyl group Chemical group 0.000 description 112
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 112
- 125000003342 alkenyl group Chemical group 0.000 description 108
- 125000000547 substituted alkyl group Chemical group 0.000 description 104
- 0 C*(CC1)CCC1c(cc1)ccc1-c1nc2cccc3c2[n]1CCNC3=O Chemical compound C*(CC1)CCC1c(cc1)ccc1-c1nc2cccc3c2[n]1CCNC3=O 0.000 description 37
- 125000000217 alkyl group Chemical group 0.000 description 32
- 150000003839 salts Chemical class 0.000 description 31
- 229910052736 halogen Inorganic materials 0.000 description 24
- 150000002367 halogens Chemical class 0.000 description 24
- 239000002207 metabolite Substances 0.000 description 23
- 239000000651 prodrug Substances 0.000 description 23
- 229940002612 prodrug Drugs 0.000 description 23
- 239000012453 solvate Substances 0.000 description 23
- 229910052760 oxygen Inorganic materials 0.000 description 21
- 150000001875 compounds Chemical class 0.000 description 19
- 229910052717 sulfur Inorganic materials 0.000 description 18
- 102000004190 Enzymes Human genes 0.000 description 17
- 108090000790 Enzymes Proteins 0.000 description 17
- 229920000776 Poly(Adenosine diphosphate-ribose) polymerase Polymers 0.000 description 14
- 125000004093 cyano group Chemical group *C#N 0.000 description 14
- 101710179684 Poly [ADP-ribose] polymerase Proteins 0.000 description 12
- 102100023712 Poly [ADP-ribose] polymerase 1 Human genes 0.000 description 12
- 125000003277 amino group Chemical group 0.000 description 10
- 230000002401 inhibitory effect Effects 0.000 description 10
- 230000000694 effects Effects 0.000 description 9
- 238000000034 method Methods 0.000 description 8
- 125000003545 alkoxy group Chemical group 0.000 description 6
- 125000004104 aryloxy group Chemical group 0.000 description 4
- 238000003556 assay Methods 0.000 description 4
- 125000005553 heteroaryloxy group Chemical group 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 125000001424 substituent group Chemical group 0.000 description 4
- 125000005017 substituted alkenyl group Chemical group 0.000 description 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 3
- 230000003013 cytotoxicity Effects 0.000 description 3
- 231100000135 cytotoxicity Toxicity 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 3
- 239000001301 oxygen Substances 0.000 description 3
- ROELIXRBIXJIOG-UHFFFAOYSA-N O=C1NCCC(C2)C(c(cc3)ccc3-c3ccncc3)=Nc3c2c1ccc3 Chemical compound O=C1NCCC(C2)C(c(cc3)ccc3-c3ccncc3)=Nc3c2c1ccc3 ROELIXRBIXJIOG-UHFFFAOYSA-N 0.000 description 2
- 239000012661 PARP inhibitor Substances 0.000 description 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 description 2
- 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
- -1 hydroxy, nitro, amino Chemical group 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- BZXYEGGSSGOSIM-UHFFFAOYSA-N C=C(C1CC=C2)C=C(c3ccc[s]3)N(CCN3)C1=C2C3=O Chemical compound C=C(C1CC=C2)C=C(c3ccc[s]3)N(CCN3)C1=C2C3=O BZXYEGGSSGOSIM-UHFFFAOYSA-N 0.000 description 1
- GVTAOCLQEWVUAH-UHFFFAOYSA-N C=[F]c(cc1)ccc1C1=Cc2cccc3c2C1CCCCNC3=O Chemical compound C=[F]c(cc1)ccc1C1=Cc2cccc3c2C1CCCCNC3=O GVTAOCLQEWVUAH-UHFFFAOYSA-N 0.000 description 1
- SLSKEBAZNJLQAF-UHFFFAOYSA-N CC(/[O]=C(/CCC1)\CCC1c(cc1)ccc1-c1nc2cccc3c2[n]1CCNC3=O)=C Chemical compound CC(/[O]=C(/CCC1)\CCC1c(cc1)ccc1-c1nc2cccc3c2[n]1CCNC3=O)=C SLSKEBAZNJLQAF-UHFFFAOYSA-N 0.000 description 1
- ADSOSINJPNKUJK-UHFFFAOYSA-N CCCCc1ncccc1 Chemical compound CCCCc1ncccc1 ADSOSINJPNKUJK-UHFFFAOYSA-N 0.000 description 1
- XDCGESSCGGOREE-UHFFFAOYSA-N CN(CCCC1)C1c(cc1)ccc1C1=Nc2cccc3c2CCC1CCNC3=O Chemical compound CN(CCCC1)C1c(cc1)ccc1C1=Nc2cccc3c2CCC1CCNC3=O XDCGESSCGGOREE-UHFFFAOYSA-N 0.000 description 1
- FSBYWAPDIVFGHZ-INIZCTEOSA-N Cc(cc1)ccc1C1=Cc2cccc3c2[C@H]1CCCNC3=O Chemical compound Cc(cc1)ccc1C1=Cc2cccc3c2[C@H]1CCCNC3=O FSBYWAPDIVFGHZ-INIZCTEOSA-N 0.000 description 1
- XYJIKZQLRLLMNR-UHFFFAOYSA-N NCc(cc1)ccc1-c(c(CCNC1=O)c2)nc3c2c1cc(F)c3 Chemical compound NCc(cc1)ccc1-c(c(CCNC1=O)c2)nc3c2c1cc(F)c3 XYJIKZQLRLLMNR-UHFFFAOYSA-N 0.000 description 1
- GXNDKAHDTWOGOA-UHFFFAOYSA-N O=C(c1ccc2)NCCc3cc1c2nc3-c1ccc(C2NCCCC2)cc1 Chemical compound O=C(c1ccc2)NCCc3cc1c2nc3-c1ccc(C2NCCCC2)cc1 GXNDKAHDTWOGOA-UHFFFAOYSA-N 0.000 description 1
- MZHKZUQKRRERNT-UHFFFAOYSA-N O=C1NCCC2C(c(cc3)ccc3F)=Nc3c2c1ccc3 Chemical compound O=C1NCCC2C(c(cc3)ccc3F)=Nc3c2c1ccc3 MZHKZUQKRRERNT-UHFFFAOYSA-N 0.000 description 1
- WTRLEQBHPVZRBL-HNNXBMFYSA-N O=C1NCCC[C@@H]2c3c1cccc3C=C2c(cc1)ccc1F Chemical compound O=C1NCCC[C@@H]2c3c1cccc3C=C2c(cc1)ccc1F WTRLEQBHPVZRBL-HNNXBMFYSA-N 0.000 description 1
- FXVARHWMURCUDT-UHFFFAOYSA-N O=C1NCCN2C(c3cccc(CN4CCCC4)c3)=NC3=CC=CC1C23 Chemical compound O=C1NCCN2C(c3cccc(CN4CCCC4)c3)=NC3=CC=CC1C23 FXVARHWMURCUDT-UHFFFAOYSA-N 0.000 description 1
- ZHFXLZSZUBSOBW-UHFFFAOYSA-N O=C1NCC[n]2c(-c(cc3)ccc3F)nc3cc(F)cc1c23 Chemical compound O=C1NCC[n]2c(-c(cc3)ccc3F)nc3cc(F)cc1c23 ZHFXLZSZUBSOBW-UHFFFAOYSA-N 0.000 description 1
- XLFLIGQYRJBFHN-UHFFFAOYSA-N O=C1NCC[n]2c(-c(cc3)ccc3F)nc3cccc1c23 Chemical compound O=C1NCC[n]2c(-c(cc3)ccc3F)nc3cccc1c23 XLFLIGQYRJBFHN-UHFFFAOYSA-N 0.000 description 1
- QVDJUNLKWJHUPW-UHFFFAOYSA-N O=C1NCC[n]2c(-c3ccc(C4NCCCC4)cc3)nc3c2c1ccc3 Chemical compound O=C1NCC[n]2c(-c3ccc(C4NCCCC4)cc3)nc3c2c1ccc3 QVDJUNLKWJHUPW-UHFFFAOYSA-N 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15214299P | 1999-08-31 | 1999-08-31 | |
| US60/152,142 | 1999-08-31 | ||
| PCT/US2000/023882 WO2001016136A2 (en) | 1999-08-31 | 2000-08-31 | Tricyclic inhibitors of poly(adp-ribose) polymerases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003513015A JP2003513015A (ja) | 2003-04-08 |
| JP2003513015A5 true JP2003513015A5 (https=) | 2006-09-21 |
| JP4272375B2 JP4272375B2 (ja) | 2009-06-03 |
Family
ID=22541675
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001519702A Expired - Lifetime JP4272375B2 (ja) | 1999-08-31 | 2000-08-31 | ポリ（ａｄｐ−リボース）ポリメラーゼの三環系阻害剤 |
Country Status (48)
Families Citing this family (69)
| 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 |
| EP1183259A2 (de) * | 1999-09-28 | 2002-03-06 | Basf Aktiengesellschaft | Azepinoindol-derivate, deren herstellung und anwendung |
| DE19946289A1 (de) * | 1999-09-28 | 2001-03-29 | Basf Ag | Benzodiazepin-Derivate, deren Herstellung und Anwendung |
| DE10021468A1 (de) * | 2000-05-04 | 2001-11-08 | Basf Ag | Verwendung von PARP-Inhibitoren in kosmetischen Zubereitungen |
| US7151102B2 (en) | 2000-10-30 | 2006-12-19 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| FR2816942B1 (fr) * | 2000-11-23 | 2003-05-09 | Sanofi Synthelabo | Derives de benzimidazole, leur preparation et leur application en therapeutique |
| 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 |
| US7026311B2 (en) | 2002-01-10 | 2006-04-11 | Abbott Gmbh & Co., Kg | Dibenzodiazepine derivatives, their preparation and use |
| DE60335359D1 (de) | 2002-04-30 | 2011-01-27 | Kudos Pharm Ltd | Phthalazinonderivate |
| WO2003103666A2 (en) * | 2002-06-07 | 2003-12-18 | Altana Pharma Ag | Novel 4,5-dihydro-imidazo[4,5,1-ij]quinolin-6-ones |
| JP3990718B2 (ja) | 2003-01-09 | 2007-10-17 | ファイザー・インク | キナーゼ阻害剤としてのジアゼピノインドール誘導体 |
| GB0305681D0 (en) | 2003-03-12 | 2003-04-16 | Kudos Pharm Ltd | Phthalazinone derivatives |
| US7449464B2 (en) | 2003-03-12 | 2008-11-11 | Kudos Pharmaceuticals Limited | Phthalazinone derivatives |
| US7531530B2 (en) * | 2003-07-25 | 2009-05-12 | Cancer Research Technology Limited | Therapeutic compounds |
| GB0317466D0 (en) | 2003-07-25 | 2003-08-27 | Univ Sheffield | Use |
| WO2005035534A1 (ja) * | 2003-10-08 | 2005-04-21 | Ono Pharmaceutical Co., Ltd. | 複素ビシクロ環および複素トリシクロ環化合物およびその医薬 |
| PL2305221T3 (pl) * | 2003-12-01 | 2015-11-30 | Kudos Pharm Ltd | Inhibitory naprawy uszkodzeń DNA w leczeniu raka |
| 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 |
| US7820668B2 (en) * | 2005-01-19 | 2010-10-26 | Eisai Inc. | Diazabenzo[de]anthracen-3-one compounds and methods for inhibiting PARP |
| AR053902A1 (es) | 2005-06-14 | 2007-05-23 | Schering Corp | Inhibidores de aspartil proteasa heterociclicos macrociclicos |
| WO2006137510A1 (ja) | 2005-06-24 | 2006-12-28 | Ono Pharmaceutical Co., Ltd. | 脳血管障害時における出血低減剤 |
| ZA200800907B (en) * | 2005-07-18 | 2010-04-28 | Bipar Sciences Inc | Treatment of cancer |
| US20070032469A1 (en) * | 2005-08-05 | 2007-02-08 | Astrazeneca Ab | Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators |
| GB0521373D0 (en) | 2005-10-20 | 2005-11-30 | Kudos Pharm Ltd | Pthalazinone derivatives |
| JP2010504079A (ja) * | 2006-06-12 | 2010-02-12 | バイパー サイエンシズ，インコーポレイティド | Ｐａｒｐ阻害剤を用いる疾病の治療方法 |
| US20100279327A1 (en) * | 2006-06-12 | 2010-11-04 | Bipar Sciences, Inc. | Method of treating diseases with parp inhibitors |
| US20080262062A1 (en) * | 2006-11-20 | 2008-10-23 | Bipar Sciences, Inc. | Method of treating diseases with parp inhibitors |
| 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 |
| WO2008030883A2 (en) * | 2006-09-05 | 2008-03-13 | Bipar Sciences, Inc. | Treatment of cancer |
| UY30639A1 (es) | 2006-10-17 | 2008-05-31 | Kudos Pharm Ltd | Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones |
| AU2008258599B2 (en) | 2007-06-05 | 2013-06-13 | Nsab, Filial Af Neurosearch Sweden Ab, Sverige | Disubstituted phenylpyrrolidines as modulators of cortical catecholaminergic neurotransmission |
| 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. |
| EP2217244A4 (en) * | 2007-11-12 | 2011-08-31 | Bipar Sciences Inc | TREATMENT OF NUTRITIONAL CANCER AND EGG CANCER WITH A PARP INHIBITOR ALONE OR IN COMBINATION WITH ANTITUMOROUS MEDICINES |
| 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 |
| RU2010128107A (ru) * | 2007-12-07 | 2012-01-20 | Байпар Сайенсиз, Инк. (Us) | Лечение рака ингибиторами топоизомеразы в комбинации с ингибиторами parp |
| UY31603A1 (es) | 2008-01-23 | 2009-08-31 | Derivados de ftalazinona | |
| MX2010008572A (es) * | 2008-02-04 | 2010-11-30 | Bipar Sciences Inc | Metodos de diagnostico y tratamiento de enfermedades mediadas por poli(adp-ribosa) polimerasa. |
| GB0804755D0 (en) * | 2008-03-14 | 2008-04-16 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
| CA2737400C (en) | 2008-10-07 | 2016-11-22 | Astrazeneca Uk Limited | Pharmaceutical formulation 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 |
| WO2014037313A1 (de) * | 2012-09-05 | 2014-03-13 | Bayer Cropscience Ag | Verwendung substituierter benzodiazepinone und benzazepinone oder deren salze als wirkstoffe gegen abiotischen pflanzenstress |
| CA2935857C (en) * | 2014-01-05 | 2020-12-15 | Washington University | Radiolabeled tracers for poly (adp-ribose) polymerase-1 (parp-1), methods and uses therefor |
| 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 |
| GB201519573D0 (en) | 2015-11-05 | 2015-12-23 | King S College London | Combination |
| WO2018022851A1 (en) | 2016-07-28 | 2018-02-01 | Mitobridge, Inc. | Methods of treating acute kidney injury |
| RU2019114863A (ru) | 2016-11-02 | 2020-12-03 | Иммуноджен, Инк. | Комбинированное лечение конъюгатами антитело-лекарственное средство и ингибиторами parp |
| WO2018162439A1 (en) | 2017-03-08 | 2018-09-13 | Onxeo | New predictive biomarker for the sensitivity to a treatment of cancer with a dbait molecule |
| WO2018197461A1 (en) | 2017-04-28 | 2018-11-01 | Akribes Biomedical Gmbh | A parp inhibitor in combination with a glucocorticoid and/or ascorbic acid and/or a protein growth factor for the treatment of impaired wound healing |
| KR20200121800A (ko) | 2018-01-05 | 2020-10-26 | 싸이브렉사 1, 인크. | 산성 또는 저산소성 질환에 걸린 조직에 관련된 질환의 치료를 위한 화합물, 조성물 및 방법 |
| CA3092779A1 (en) | 2018-03-13 | 2019-09-19 | Onxeo | A dbait molecule against acquired resistance in the treatment of cancer |
| US11535633B2 (en) | 2018-06-28 | 2022-12-27 | Jiangsu Hengrui Medicine Co., Ltd. | Fused tricyclic heterocycle compounds and therapeutic uses thereof |
| AU2019326633B2 (en) * | 2018-08-24 | 2022-09-08 | Adlai Nortye Biopharma Co., Ltd. | High activity sting protein agonist |
| US20220056044A1 (en) * | 2018-12-14 | 2022-02-24 | Jiangsu Hengrui Medicine Co., Ltd. | Tricyclic compounds as sting agonists, and preparation methods and medicinal uses thereof |
| CN113365998B (zh) * | 2019-02-02 | 2023-04-14 | 正大天晴药业集团股份有限公司 | 用于parp抑制剂的吲哚并七元酰肟类似物 |
| CN111909157B (zh) * | 2019-05-07 | 2023-02-03 | 南京药石科技股份有限公司 | Ezh2抑制剂及其用途 |
| MX2022000449A (es) | 2019-07-10 | 2022-04-25 | Cybrexa 2 Inc | Conjugados peptídicos de citotoxinas como terapéuticos. |
| US11555019B2 (en) | 2019-07-10 | 2023-01-17 | Cybrexa 3, Inc. | Peptide conjugates of microtubule-targeting agents as therapeutics |
| GB201913030D0 (en) | 2019-09-10 | 2019-10-23 | Francis Crick Institute Ltd | Treatment of hr deficient cancer |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US20230234938A1 (en) | 2020-04-28 | 2023-07-27 | Rhizen Pharmaceuticals Ag | Novel compounds useful as poly(adp-ribose) polymerase (parp) inhibitors |
| WO2022090938A1 (en) | 2020-10-31 | 2022-05-05 | Rhizen Pharmaceuticals Ag | Phthalazinone derivatives useful as parp inhibitors |
| CN116940691A (zh) | 2021-01-08 | 2023-10-24 | 赛博克萨2公司 | 用于制备缀合物连接部分的方法 |
| WO2022155172A1 (en) | 2021-01-13 | 2022-07-21 | Cybrexa 3, Inc. | Peptide conjugates of therapeutics |
| CA3214298A1 (en) | 2021-04-08 | 2022-10-13 | Swaroop Kumar Venkata Satya VAKKALANKA | Inhibitors of poly(adp-ribose) polymerase |
| US20250154115A1 (en) * | 2022-02-11 | 2025-05-15 | The University Of North Carolina At Chapel Hill | Arylbenzoisoxazole compounds as ip6k and ipmk inhibitors and methods of use thereof |
| CN121398822A (zh) | 2023-06-21 | 2026-01-23 | 四方生物科学有限公司 | 用于在治疗hr功能正常的癌症的方法中的用途的包含脱氧胞苷衍生物和parp抑制剂的组合 |
| WO2025106920A1 (en) * | 2023-11-15 | 2025-05-22 | Yale University | Parp pet imaging agents and methods of using the same |
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2000
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