CN109843874B - 作为parp1、parp2和/或微管蛋白的抑制剂可用于治疗癌症的酞嗪衍生物 - Google Patents

作为parp1、parp2和/或微管蛋白的抑制剂可用于治疗癌症的酞嗪衍生物 Download PDF

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CN109843874B
CN109843874B CN201780051422.3A CN201780051422A CN109843874B CN 109843874 B CN109843874 B CN 109843874B CN 201780051422 A CN201780051422 A CN 201780051422A CN 109843874 B CN109843874 B CN 109843874B
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methyl
compound
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salt
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CN109843874A (zh
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乔鲍·J·佩托
戴维·M·雅布隆斯
特塞·曾
哈桑·莱姆贾巴尔-阿拉维
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Atlasmedx Inc
University of California San Diego UCSD
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Atlasmedx Inc
University of California San Diego UCSD
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201780051422.3A 2016-06-24 2017-06-23 作为parp1、parp2和/或微管蛋白的抑制剂可用于治疗癌症的酞嗪衍生物 Active CN109843874B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662354449P 2016-06-24 2016-06-24
US62/354,449 2016-06-24
US201662426095P 2016-11-23 2016-11-23
US62/426,095 2016-11-23
PCT/US2017/039119 WO2017223516A1 (en) 2016-06-24 2017-06-23 Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer

Publications (2)

Publication Number Publication Date
CN109843874A CN109843874A (zh) 2019-06-04
CN109843874B true CN109843874B (zh) 2022-05-27

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CN201780051422.3A Active CN109843874B (zh) 2016-06-24 2017-06-23 作为parp1、parp2和/或微管蛋白的抑制剂可用于治疗癌症的酞嗪衍生物

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US (3) US11072600B2 (enExample)
EP (1) EP3475272B1 (enExample)
JP (2) JP7033588B2 (enExample)
KR (1) KR102494294B1 (enExample)
CN (1) CN109843874B (enExample)
AU (1) AU2017280334C1 (enExample)
ES (1) ES2964531T3 (enExample)
HU (1) HUE066216T2 (enExample)
IL (1) IL263917B (enExample)
MX (2) MX387726B (enExample)
PL (1) PL3475272T3 (enExample)
PT (1) PT3475272T (enExample)
SG (1) SG11201811393WA (enExample)
WO (1) WO2017223516A1 (enExample)
ZA (2) ZA201808562B (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3298005B1 (en) 2015-05-21 2024-01-24 The Regents of The University of California Anti-cancer compounds
US11028055B2 (en) 2015-11-30 2021-06-08 Children's Medical Center Corporation Compounds for treating proliferative diseases
IL263917B (en) * 2016-06-24 2022-07-01 Univ California Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer
JP7372253B2 (ja) 2018-04-05 2023-10-31 ノビガ・リサーチ・エービー 癌の治療における使用のためのチューブリン重合阻害剤とポリ（ａｄｐ－リボース）ポリメラーゼ（ｐａｒｐ）阻害剤との新規組合せ
CN112574122B (zh) * 2019-09-27 2024-05-31 上海天慈国际药业有限公司 一种奥拉帕尼关键中间体的制备方法

Citations (4)

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WO2008114023A2 (en) * 2007-03-22 2008-09-25 Kudos Pharmaceuticals Limited Phthalazinone derivatives
CN101291928A (zh) * 2005-10-19 2008-10-22 库多斯药物有限公司 4-杂芳甲基取代的酞嗪酮衍生物
CN101981013A (zh) * 2008-03-27 2011-02-23 詹森药业有限公司 作为parp和微管蛋白聚合抑制剂的四氢菲啶酮和四氢环戊二烯并喹啉酮
CN104918917A (zh) * 2012-12-31 2015-09-16 卡迪拉保健有限公司 作为聚(adp-核糖)聚合酶-1的选择性抑制剂的取代的酞嗪-1(2h)-酮衍生物

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US3401171A (en) 1966-03-11 1968-09-10 Smithkline Corp 2-amidobenzimidazoles
SU1019810A1 (ru) 1981-07-28 1991-04-07 Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского Метиловый эфир 5(6)-[1-(2Н)-фталазинонил-4]-1Н-бензимидазолил-2-карбаминовой кислоты, обладающий антигельминтной активностью
SU1218649A1 (ru) 1984-09-19 1991-04-30 Институт медицинской паразитологии и тропической медицины им.Е.И.Марциновского Способ получени метилового эфира 5(6)-[1(2Н)-фталазинонил-4-]-1Н-бензимидазолил-2-карбаминовой кислоты формулы
EP1060166A1 (de) 1998-02-03 2000-12-20 Boehringer Ingelheim Pharma KG 5-gliedrige benzokondensierte heterocyclen als antithrombotika
US6677333B1 (en) 1999-01-26 2004-01-13 Ono Pharmaceutical Co., Ltd. 2H-phthalazin-1-one derivatives and drug containing its derivatives as active ingredient
DE19907813A1 (de) 1999-02-24 2000-08-31 Boehringer Ingelheim Pharma Substituierte bicyclische Heterocyclen, deren Herstellung und deren Verwendung als Arzneimittel
US7151102B2 (en) 2000-10-30 2006-12-19 Kudos Pharmaceuticals Limited Phthalazinone derivatives
GB2384776C (en) 2000-10-30 2006-02-03 Kudos Pharm Ltd Phthalazinone derivatives
AR042956A1 (es) 2003-01-31 2005-07-13 Vertex Pharma Inhibidores de girasa y usos de los mismos
KR101146806B1 (ko) 2003-03-12 2012-05-22 메이브릿지 리미티드 프탈라지논 유도체
CA2565200C (en) 2004-05-07 2013-12-24 Exelixis, Inc. Raf modulators and methods of use
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
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
CA2787297C (en) 2010-01-29 2018-09-04 Metanomics Gmbh Means and methods for diagnosing heart failure in a subject
CN102372706A (zh) 2010-08-09 2012-03-14 江苏恒瑞医药股份有限公司 酞嗪酮类衍生物、其制备方法及其在医药上的应用
TWI577693B (zh) 2011-05-31 2017-04-11 江蘇康緣藥業股份有限公司 聚（ａｄｐ-核糖）聚合酶之三環抑制劑
KR101546743B1 (ko) * 2012-01-16 2015-08-24 한국과학기술원 인돌 유도체 화합물, 이를 포함하는 Ａｂｌ 키나제 저해제 조성물 및 이상세포 성장 질환의 예방 및 치료용 약학 조성물
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
IL263917B (en) * 2016-06-24 2022-07-01 Univ California Phthalazine derivatives as inhibitors of parp1, parp2 and/or tubulin useful for the treatment of cancer

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101291928A (zh) * 2005-10-19 2008-10-22 库多斯药物有限公司 4-杂芳甲基取代的酞嗪酮衍生物
WO2008114023A2 (en) * 2007-03-22 2008-09-25 Kudos Pharmaceuticals Limited Phthalazinone derivatives
CN101981013A (zh) * 2008-03-27 2011-02-23 詹森药业有限公司 作为parp和微管蛋白聚合抑制剂的四氢菲啶酮和四氢环戊二烯并喹啉酮
CN104918917A (zh) * 2012-12-31 2015-09-16 卡迪拉保健有限公司 作为聚(adp-核糖)聚合酶-1的选择性抑制剂的取代的酞嗪-1(2h)-酮衍生物

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CA3029004A1 (en) 2017-12-28
MX2018015893A (es) 2019-08-01
ES2964531T3 (es) 2024-04-08
SG11201811393WA (en) 2019-01-30
US20190337928A1 (en) 2019-11-07
KR102494294B1 (ko) 2023-01-31
CN109843874A (zh) 2019-06-04
BR112018076821A2 (pt) 2019-04-02
IL263917A (en) 2019-02-28
AU2017280334A1 (en) 2019-01-17
JP2019522681A (ja) 2019-08-15
ZA202301066B (en) 2024-05-30
PL3475272T3 (pl) 2024-04-29
US20190352283A1 (en) 2019-11-21
KR20190033534A (ko) 2019-03-29
US11072600B2 (en) 2021-07-27
IL263917B (en) 2022-07-01
US10640493B2 (en) 2020-05-05
EP3475272B1 (en) 2023-09-13
US20220402894A1 (en) 2022-12-22
HUE066216T2 (hu) 2024-07-28
JP2022037004A (ja) 2022-03-08
US12145925B2 (en) 2024-11-19
AU2017280334C1 (en) 2022-10-20
AU2017280334B2 (en) 2021-07-29
MX2021013641A (es) 2022-01-06
EP3475272A1 (en) 2019-05-01
WO2017223516A1 (en) 2017-12-28
MX387726B (es) 2025-03-18
PT3475272T (pt) 2023-12-15
ZA201808562B (en) 2023-12-20
JP7033588B2 (ja) 2022-03-10

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