TWI736550B - 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 - Google Patents

製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 Download PDF

Info

Publication number
TWI736550B
TWI736550B TW105127160A TW105127160A TWI736550B TW I736550 B TWI736550 B TW I736550B TW 105127160 A TW105127160 A TW 105127160A TW 105127160 A TW105127160 A TW 105127160A TW I736550 B TWI736550 B TW I736550B
Authority
TW
Taiwan
Prior art keywords
compound
crystalline form
cancer
solvent
sesquihydrate
Prior art date
Application number
TW105127160A
Other languages
English (en)
Chinese (zh)
Other versions
TW201718586A (zh
Inventor
王鶴翔
昌友 周
任博
匡先照
Original Assignee
開曼群島商百濟神州有限公司
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=58099633&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI736550(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 開曼群島商百濟神州有限公司 filed Critical 開曼群島商百濟神州有限公司
Publication of TW201718586A publication Critical patent/TW201718586A/zh
Application granted granted Critical
Publication of TWI736550B publication Critical patent/TWI736550B/zh

Links

Images

Classifications

    • 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
    • C07D471/22—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 systems contains four or more hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
TW105127160A 2015-08-25 2016-08-24 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途 TWI736550B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/088003 2015-08-25
CN2015088003 2015-08-25

Publications (2)

Publication Number Publication Date
TW201718586A TW201718586A (zh) 2017-06-01
TWI736550B true TWI736550B (zh) 2021-08-21

Family

ID=58099633

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105127160A TWI736550B (zh) 2015-08-25 2016-08-24 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途

Country Status (15)

Country Link
US (1) US10457680B2 (enExample)
EP (1) EP3341375B1 (enExample)
JP (1) JP6940039B2 (enExample)
KR (1) KR20180041748A (enExample)
CN (2) CN107922425B (enExample)
AU (1) AU2016312011B2 (enExample)
BR (1) BR112018003634B1 (enExample)
CA (1) CA2994895A1 (enExample)
EA (1) EA037366B1 (enExample)
IL (2) IL296835A (enExample)
MX (1) MX385450B (enExample)
NZ (1) NZ739876A (enExample)
TW (1) TWI736550B (enExample)
WO (1) WO2017032289A1 (enExample)
ZA (1) ZA201800765B (enExample)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101716012B1 (ko) 2011-12-31 2017-03-13 베이진 엘티디 Parp 저해제로서의 융합된 테트라 또는 펜타-사이클릭 다이하이드로다이아제피노카르바졸론
AU2016312011B2 (en) 2015-08-25 2021-02-04 Beigene, Ltd. Process for preparing Parp inhibitor, crystalline forms, and uses thereof
US11202782B2 (en) 2016-09-27 2021-12-21 Beigene, Ltd. Treatment cancers using a combination comprising PARP inhibitors
CN110392687B (zh) * 2017-02-28 2022-08-02 百济神州(苏州)生物科技有限公司 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式及其用途
US12121518B2 (en) 2017-03-09 2024-10-22 The Board Of Supervisors Of Louisiana State Universi And Agricultural And Mechanical College PARP-1 and methods of use thereof
WO2018165615A1 (en) 2017-03-09 2018-09-13 The Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College Parp-1 and methods of use thereof
AU2018302999A1 (en) * 2017-07-17 2020-01-30 Beigene, Ltd. Treatment cancers using a combination comprising PARP inhibitors, temozolomide and/or radiation therapy
WO2019220390A1 (en) 2018-05-18 2019-11-21 Novartis Ag Crystalline forms of a tlr7/tlr8 inhibitor
WO2019228499A1 (en) * 2018-06-01 2019-12-05 Beigene, Ltd. Maintenance therapy of a parp inhibitor in treating gastric cancer
USD926356S1 (en) * 2019-03-14 2021-07-27 Tuanfang Liu Battery for electronic cigarette
CN113004279B (zh) * 2019-05-10 2023-01-06 百济神州(苏州)生物科技有限公司 一种控制含parp抑制剂倍半水合物产物的含水量的方法
CN113402502B (zh) * 2019-05-16 2022-10-14 百济神州(苏州)生物科技有限公司 一种parp抑制剂中间体制备的物料组合体系
CN111171001B (zh) * 2019-05-16 2022-04-29 百济神州(苏州)生物科技有限公司 一种parp抑制剂中间体的结晶方法
CA3141770A1 (en) 2019-05-31 2020-12-03 Beigene, Ltd. Parp inhibitor pellet preparation and preparation process therefor
CN112007011B (zh) * 2019-05-31 2024-07-23 百济神州(苏州)生物科技有限公司 一种parp抑制剂微丸胶囊及其制备工艺
WO2021046014A1 (en) 2019-09-03 2021-03-11 Teva Czech Industries S.R.O Solid state forms of pamiparib and process for preparation thereof
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013097225A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1140936B1 (en) 1999-01-11 2004-03-17 Agouron Pharmaceuticals, Inc. Tricyclic inhibitors of poly(adp-ribose) polymerases
US6887996B2 (en) * 2000-12-01 2005-05-03 Guilford Pharmaceuticals Inc. Compounds and their use
EA009337B1 (ru) * 2003-01-09 2007-12-28 Пфайзер Инк. Трициклические соединения, представляющие собой ингибиторы протеинкиназ, для увеличения эффективности противоопухолевых агентов и лучевой терапии
HUE035295T2 (en) 2008-08-06 2018-05-02 Medivation Technologies Inc Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
SMT202300039T1 (it) 2013-09-13 2023-03-17 Beigene Switzerland Gmbh Anticorpi anti-pd1 e loro uso come terapia e per diagnostica
TWI726608B (zh) 2014-07-03 2021-05-01 英屬開曼群島商百濟神州有限公司 抗pd-l1抗體及其作為治療及診斷之用途
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
AU2016312011B2 (en) 2015-08-25 2021-02-04 Beigene, Ltd. Process for preparing Parp inhibitor, crystalline forms, and uses thereof
US11202782B2 (en) * 2016-09-27 2021-12-21 Beigene, Ltd. Treatment cancers using a combination comprising PARP inhibitors
CN110392687B (zh) * 2017-02-28 2022-08-02 百济神州(苏州)生物科技有限公司 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式及其用途
AU2018302999A1 (en) * 2017-07-17 2020-01-30 Beigene, Ltd. Treatment cancers using a combination comprising PARP inhibitors, temozolomide and/or radiation therapy
CN113004279B (zh) * 2019-05-10 2023-01-06 百济神州(苏州)生物科技有限公司 一种控制含parp抑制剂倍半水合物产物的含水量的方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013097225A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors

Also Published As

Publication number Publication date
EA037366B1 (ru) 2021-03-18
EP3341375A4 (en) 2019-01-16
IL257442B2 (en) 2023-03-01
ZA201800765B (en) 2019-10-30
EP3341375A1 (en) 2018-07-04
AU2016312011A1 (en) 2018-03-08
EA201890547A1 (ru) 2018-07-31
IL257442A (en) 2018-04-30
BR112018003634A2 (en) 2018-11-21
CA2994895A1 (en) 2017-03-02
US10457680B2 (en) 2019-10-29
US20190177325A1 (en) 2019-06-13
TW201718586A (zh) 2017-06-01
AU2016312011B2 (en) 2021-02-04
CN107922425A (zh) 2018-04-17
CN112521390A (zh) 2021-03-19
MX385450B (es) 2025-03-18
WO2017032289A1 (en) 2017-03-02
NZ739876A (en) 2022-09-30
JP6940039B2 (ja) 2021-09-22
KR20180041748A (ko) 2018-04-24
CN107922425B (zh) 2021-06-01
IL257442B (en) 2022-11-01
EP3341375B1 (en) 2022-04-13
IL296835A (en) 2022-11-01
BR112018003634A8 (pt) 2023-01-17
BR112018003634B1 (pt) 2023-11-21
MX2018002322A (es) 2018-04-11
JP2018528199A (ja) 2018-09-27

Similar Documents

Publication Publication Date Title
JP6940039B2 (ja) Ｐａｒｐ阻害剤の製造方法、結晶型、及びその使用
CN107286077B (zh) 一种选择性的c-kit激酶抑制剂
TWI736531B (zh) B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途
WO2021190467A1 (zh) 含螺环的喹唑啉化合物
WO2022017533A1 (zh) 用作cdk7激酶抑制剂的化合物及其应用
JP2020524148A (ja) 置換５−シアノインドール化合物及びその使用
BR112015017963A2 (pt) composto de fenil amino pirimidina deuterado, método para preparar a composição farmacêutica, composição farmacêutica e uso do composto
CN115433187A (zh) 稠合的四环或五环二氢二氮杂䓬并咔唑酮的盐的结晶形式组合物及其用途
TWI815820B (zh) ２－（５－（４－（２－嗎啉乙氧基）苯基）吡啶－２－基）－ｎ－芐乙醯胺之固態形式
CN119173510A (zh) 一种羟基酰胺类衍生物及其应用
TW202302535A (zh) 化合物
JP7776418B2 (ja) イソクエン酸デヒドロゲナーゼ（ｉｄｈ）阻害剤
HK40040143A (en) Process for preparing parp inhibitor, crystalline forms, and uses thereof
TW202519531A (zh) 含丙烯酮類生物抑制劑的晶型及其製備方法和應用
EP4596553A1 (en) Salt of dioxane quinoline compound, crystal form thereof, preparation methods therefor and uses thereof
TW202606690A (zh) 吡啶并吡唑衍生物的晶型物、藥物組合物及其用途
HK40116388A (en) Compounds used as cdk7 kinase inhibitors and uses thereof
HK40061853B (en) Compound useful as cdk7 kinase inhibitor and use thereof
HK40089264A (en) Compound used as cdk7 kinase inhibitor and use thereof
WO2024008083A1 (zh) 用作cdk7激酶抑制剂的化合物及其应用
HK40058867B (en) Imidazopyridinyl compounds and use thereof for treatment of proliferative disorders
JP2008540449A (ja) （２ｅ，４ｓ）−４−［（ｎ−｛［（２ｒ）−１−イソプロピルピペリジン−２−イル］−カルボニル｝−３−メチル−ｌ−バリル）（メチル）アミノ］−２，５−ジメチルヘキサ−２−エン酸の非溶媒和およびホストゲスト溶媒和結晶フォーム、およびそれらの医薬的使用

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees