CN102372716A - 酞嗪酮类衍生物、其制备方法及其在医药上的应用 - Google Patents

酞嗪酮类衍生物、其制备方法及其在医药上的应用 Download PDF

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Publication number
CN102372716A
CN102372716A CN2010102483075A CN201010248307A CN102372716A CN 102372716 A CN102372716 A CN 102372716A CN 2010102483075 A CN2010102483075 A CN 2010102483075A CN 201010248307 A CN201010248307 A CN 201010248307A CN 102372716 A CN102372716 A CN 102372716A
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CN
China
Prior art keywords
pyrazine
methyl
general formula
alkyl
aryl
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.)
Pending
Application number
CN2010102483075A
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English (en)
Chinese (zh)
Inventor
邓炳初
李心
李相勤
陈阳
王斌
朱哲
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
Original Assignee
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Jiangsu Hengrui Medicine Co Ltd, Shanghai Hengrui Pharmaceutical Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Priority to CN2010102483075A priority Critical patent/CN102372716A/zh
Priority to EP11815986.2A priority patent/EP2604610B1/en
Priority to HK13101036.9A priority patent/HK1174030B/xx
Priority to PL11815986.2T priority patent/PL2604610T3/pl
Priority to PT118159862T priority patent/PT2604610T/pt
Priority to CA2806324A priority patent/CA2806324C/en
Priority to JP2013523468A priority patent/JP5808408B2/ja
Priority to PCT/CN2011/001223 priority patent/WO2012019427A1/zh
Priority to RU2013106754/04A priority patent/RU2564527C2/ru
Priority to US13/811,957 priority patent/US9273052B2/en
Priority to HUE11815986A priority patent/HUE029275T2/en
Priority to AU2011288876A priority patent/AU2011288876B2/en
Priority to KR1020137003185A priority patent/KR101829940B1/ko
Priority to ES11815986.2T priority patent/ES2582315T3/es
Priority to CN201180003990.9A priority patent/CN102686591B/zh
Priority to BR112013002220-5A priority patent/BR112013002220B1/pt
Priority to UAA201301524A priority patent/UA111161C2/uk
Publication of CN102372716A publication Critical patent/CN102372716A/zh
Priority to US15/016,986 priority patent/US9566277B2/en
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN2010102483075A 2010-08-09 2010-08-09 酞嗪酮类衍生物、其制备方法及其在医药上的应用 Pending CN102372716A (zh)

Priority Applications (18)

Application Number Priority Date Filing Date Title
CN2010102483075A CN102372716A (zh) 2010-08-09 2010-08-09 酞嗪酮类衍生物、其制备方法及其在医药上的应用
US13/811,957 US9273052B2 (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
HUE11815986A HUE029275T2 (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, method of preparation and therapeutic use
PL11815986.2T PL2604610T3 (pl) 2010-08-09 2011-07-26 Pochodna ketonu ftalazynonowego, sposób jej wytwarzania oraz jej farmaceutyczne zastosowanie
PT118159862T PT2604610T (pt) 2010-08-09 2011-07-26 Derivado cetona de ftalazinona, processo para a sua preparação e seu uso farmacêutico
CA2806324A CA2806324C (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
JP2013523468A JP5808408B2 (ja) 2010-08-09 2011-07-26 フタラジノンケトン誘導体、その製造法および医薬用途
PCT/CN2011/001223 WO2012019427A1 (zh) 2010-08-09 2011-07-26 酞嗪酮类衍生物、其制备方法及其在医药上的应用
RU2013106754/04A RU2564527C2 (ru) 2010-08-09 2011-07-26 Производное фталазинонкетона, способ его получения и его фармацевтическое применение
EP11815986.2A EP2604610B1 (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
HK13101036.9A HK1174030B (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
AU2011288876A AU2011288876B2 (en) 2010-08-09 2011-07-26 Phthalazinone ketone derivative, preparation method thereof, and pharmaceutical use thereof
KR1020137003185A KR101829940B1 (ko) 2010-08-09 2011-07-26 프탈라지논 케톤 유도체, 이의 제조방법, 및 이의 약학적 용도
ES11815986.2T ES2582315T3 (es) 2010-08-09 2011-07-26 Derivado de ftalazinona-cetona, método de preparación de la misma y uso farmacéutico de la misma
CN201180003990.9A CN102686591B (zh) 2010-08-09 2011-07-26 酞嗪酮类衍生物、其制备方法及其在医药上的应用
BR112013002220-5A BR112013002220B1 (pt) 2010-08-09 2011-07-26 Derivado de ftalazinona cetona, seus usos e seu método de preparação, e composição farmacêutica
UAA201301524A UA111161C2 (uk) 2010-08-09 2011-07-26 Похідна фталазинонкетону, спосіб її одержання та її фармацевтичне застосування
US15/016,986 US9566277B2 (en) 2010-08-09 2016-02-05 Methods of using phthalazinone ketone derivatives

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2010102483075A CN102372716A (zh) 2010-08-09 2010-08-09 酞嗪酮类衍生物、其制备方法及其在医药上的应用

Publications (1)

Publication Number Publication Date
CN102372716A true CN102372716A (zh) 2012-03-14

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Family Applications (2)

Application Number Title Priority Date Filing Date
CN2010102483075A Pending CN102372716A (zh) 2010-08-09 2010-08-09 酞嗪酮类衍生物、其制备方法及其在医药上的应用
CN201180003990.9A Active CN102686591B (zh) 2010-08-09 2011-07-26 酞嗪酮类衍生物、其制备方法及其在医药上的应用

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201180003990.9A Active CN102686591B (zh) 2010-08-09 2011-07-26 酞嗪酮类衍生物、其制备方法及其在医药上的应用

Country Status (15)

Country Link
US (2) US9273052B2 (enExample)
EP (1) EP2604610B1 (enExample)
JP (1) JP5808408B2 (enExample)
KR (1) KR101829940B1 (enExample)
CN (2) CN102372716A (enExample)
AU (1) AU2011288876B2 (enExample)
BR (1) BR112013002220B1 (enExample)
CA (1) CA2806324C (enExample)
ES (1) ES2582315T3 (enExample)
HU (1) HUE029275T2 (enExample)
PL (1) PL2604610T3 (enExample)
PT (1) PT2604610T (enExample)
RU (1) RU2564527C2 (enExample)
UA (1) UA111161C2 (enExample)
WO (1) WO2012019427A1 (enExample)

Cited By (12)

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Publication number Priority date Publication date Assignee Title
CN102702108A (zh) * 2012-06-27 2012-10-03 上海大学 1,2-二氢酞嗪类化合物及其合成方法
CN102863393A (zh) * 2012-09-26 2013-01-09 上海大学 1,2-二氢酞嗪类化合物及其合成方法
CN102898377A (zh) * 2012-02-14 2013-01-30 南京圣和药业有限公司 一类新型酞嗪酮衍生物及其用途
CN106749261A (zh) * 2015-11-23 2017-05-31 中国科学院上海药物研究所 一类取代三唑并哌嗪类parp抑制剂及其制备方法和用途
CN108778336A (zh) * 2016-12-01 2018-11-09 江苏恒瑞医药股份有限公司 一种vegfr抑制剂与parp抑制剂联合在制备治疗胃癌的药物中的用途
WO2019037753A1 (zh) * 2017-08-24 2019-02-28 江苏恒瑞医药股份有限公司 一种parp-1抑制剂的晶型及其制备方法
CN110840845A (zh) * 2018-11-16 2020-02-28 江苏恒瑞医药股份有限公司 一种包含parp抑制剂的药物组合物
CN111278830A (zh) * 2018-01-09 2020-06-12 江苏恒瑞医药股份有限公司 一种parp抑制剂及其中间体的制备方法
CN111732594A (zh) * 2020-08-18 2020-10-02 苏州富士莱医药股份有限公司 一种氟唑帕利的制备方法
WO2022247816A1 (zh) * 2021-05-24 2022-12-01 江苏恒瑞医药股份有限公司 含氮杂环类化合物、其制备方法及其在医药上的应用
RU2785677C1 (ru) * 2018-11-16 2022-12-12 Цзянсу Хэнжуй Медисин Ко., Лтд. Фармацевтическая композиция, содержащая ингибиторы parp
WO2024109871A1 (zh) * 2022-11-23 2024-05-30 江苏恒瑞医药股份有限公司 一种含氮杂环类化合物的可药用盐、晶型及制备方法

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WO2017101796A1 (zh) * 2015-12-16 2017-06-22 四川科伦博泰生物医药股份有限公司 酞嗪酮衍生物、其制备方法及用途
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
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PT3448859T (pt) 2017-03-20 2019-10-25 Forma Therapeutics Inc Composições de pirrolopirrole como ativadores de piruvato quinase (pkr).
CN110475779A (zh) 2017-04-12 2019-11-19 豪夫迈·罗氏有限公司 标记含醛靶分子的方法
BR112020010435A2 (pt) * 2017-12-06 2020-11-24 Jiangsu Hengrui Medicine Co., Ltd. uso de inibidor da parp no tratamento de câncer de ovário ou câncer de mama resistente à quimioterapia
AU2019212093B2 (en) 2018-01-26 2024-05-30 Recordati Industria Chimica E Farmaceutica S.P.A Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mGlu5 receptors
WO2019169156A1 (en) * 2018-02-28 2019-09-06 The Trustees Of The University Of Pennsylvania Low affinity poly(ad-ribose) polymerase 1 dependent cytotoxic agents
US20200407720A1 (en) 2018-03-13 2020-12-31 Onxeo A dbait molecule against acquired resistance in the treatment of cancer
BR112020019824A2 (pt) * 2018-03-29 2021-01-05 Board Of Regents, The University Of Texas System Composto de fórmula estrutural i ou um sal do mesmo, composição farmacêutica, método de inibição de cbp, método de inibição de p300, método de tratamento de uma doença mediada por cbp, método de tratamento de uma doença mediada por p300 e método para alcançar um efeito em um paciente
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
CN112584836A (zh) * 2018-10-22 2021-03-30 江苏恒瑞医药股份有限公司 一种ar拮抗剂联合parp抑制剂在制备治疗前列腺癌的药物中的用途
TW202110448A (zh) * 2019-05-28 2021-03-16 大陸商江蘇恆瑞醫藥股份有限公司 Ｐａｒｐ抑制劑聯合ｖｅｇｆｒ抑制劑用於治療卵巢癌或乳腺癌的用途
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
CN112870365A (zh) * 2019-11-29 2021-06-01 江苏恒瑞医药股份有限公司 Ezh2抑制剂和/或parp抑制剂与化疗药物联合在制备治疗肿瘤药物中的用途
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CA3176219A1 (en) 2020-04-21 2021-10-28 Kunhee LEE Crystalline forms of phthalazinone compound
JP7626783B2 (ja) 2020-04-21 2025-02-07 アイディーエンス カンパニー リミテッド フタラジノン誘導体及びその中間体を調製するプロセス
EP4221708A4 (en) 2020-10-02 2024-11-06 Board of Regents, The University of Texas System IMIDAZOPIPERAZINE INHIBITORS OF TRANSCRIPTION-ACTIVATING PROTEINS
AU2021355480B2 (en) 2020-10-02 2026-03-05 Board Of Regents, The University Of Texas System Imidazopiperazine inhibitors of transcription activating proteins
US12059419B2 (en) 2020-10-16 2024-08-13 Idience Co., Ltd. Pharmaceutical composition comprising phthalazinone derivatives
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
US20240317762A1 (en) * 2021-07-16 2024-09-26 Oregon Health & Science University Phthalazinone-based parp-1 inhibitors
CA3226796A1 (en) * 2021-07-29 2023-02-02 Xiaoxia Yan Novel parp7 inhibitor and use thereof
CN115650988B (zh) * 2022-10-27 2024-09-13 江苏恒瑞医药股份有限公司 一种parp抑制剂的制备方法
WO2024188265A1 (zh) * 2023-03-13 2024-09-19 江苏豪森药业集团有限公司 哌啶烯类化合物在制备治疗癌症的药物中的应用
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

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RU2785677C1 (ru) * 2018-11-16 2022-12-12 Цзянсу Хэнжуй Медисин Ко., Лтд. Фармацевтическая композиция, содержащая ингибиторы parp
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KR20210092771A (ko) * 2018-11-16 2021-07-26 지앙수 헨그루이 메디슨 컴퍼니 리미티드 Parp 억제제를 포함하는 약학 조성물
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US12318385B2 (en) 2018-11-16 2025-06-03 Jiangsu Hengrui Medicine Co., Ltd. Pharmaceutical composition comprising PARP inhibitors
WO2020098774A1 (zh) * 2018-11-16 2020-05-22 江苏恒瑞医药股份有限公司 一种包含parp抑制剂的药物组合物
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CN110840845A (zh) * 2018-11-16 2020-02-28 江苏恒瑞医药股份有限公司 一种包含parp抑制剂的药物组合物
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WO2022247816A1 (zh) * 2021-05-24 2022-12-01 江苏恒瑞医药股份有限公司 含氮杂环类化合物、其制备方法及其在医药上的应用
WO2024109871A1 (zh) * 2022-11-23 2024-05-30 江苏恒瑞医药股份有限公司 一种含氮杂环类化合物的可药用盐、晶型及制备方法

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