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
CN2015088003 2015-08-25
CNPCT/CN2015/088003 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) CN112521390A (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 (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ624063A (en) 2011-12-31 2016-09-30 Beigene Ltd Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors
WO2017032289A1 (en) 2015-08-25 2017-03-02 Beigene, Ltd. Process for preparing parp inhibitor, crystalline forms, and uses thereof
CN110087730B (zh) * 2016-09-27 2023-03-28 百济神州(苏州)生物科技有限公司 使用包含parp抑制剂的组合产品治疗癌症
TW201840564A (zh) 2017-02-28 2018-11-16 英屬開曼群島商百濟神州有限公司 稠合的四環或五環二氫二氮呯幷哢唑酮的鹽的結晶形式及其用途
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
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
US20200155567A1 (en) * 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of cancers using a combination comprising parp inhibitors, temozolomide and/or radiation therapy
TWI826446B (zh) 2018-05-18 2023-12-21 瑞士商諾華公司 Tlr7/tlr8抑制劑之晶型
EP3801550A4 (en) * 2018-06-01 2022-02-16 BeiGene, Ltd. MAINTENANCE THERAPY OF A PARP INHIBITOR IN THE TREATMENT OF 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
CN111171002B (zh) * 2019-05-16 2021-04-06 百济神州(苏州)生物科技有限公司 一种parp抑制剂中间体的制备方法
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
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
MX2021014339A (es) 2019-05-31 2022-01-06 Beigene Ltd Preparacion de granulo inhibidor de parp y proceso de preparacion del mismo.
WO2021046014A1 (en) 2019-09-03 2021-03-11 Teva Czech Industries S.R.O Solid state forms of pamiparib and process for preparation thereof
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ｒａｓ抑制劑
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
WO2025255438A1 (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

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
EE05006B1 (et) 1999-01-11 2008-04-15 Agouron Pharmaceuticals, Inc. Polü(ADP-riboos)polümeraaside tritsüklilised inhibiitorid ja neid sisaldavad farmatseutilised kompositsioonid
US6887996B2 (en) * 2000-12-01 2005-05-03 Guilford Pharmaceuticals Inc. Compounds and their use
SI1585749T1 (sl) * 2003-01-09 2008-10-31 Pfizer Derivati diazepinoindola kot inhibitorji kinaze
ES2466565T3 (es) 2008-08-06 2014-06-10 Biomarin Pharmaceutical Inc. Inhibidores dihidropiridoftalazinona de poli(ADP-ribosa)polimerasa (PARP)
ES2927567T3 (es) 2013-09-13 2022-11-08 Beigene Switzerland Gmbh Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico
CN110156892B (zh) 2014-07-03 2023-05-16 百济神州有限公司 抗pd-l1抗体及其作为治疗剂及诊断剂的用途
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
WO2017032289A1 (en) 2015-08-25 2017-03-02 Beigene, Ltd. Process for preparing parp inhibitor, crystalline forms, and uses thereof
CN110087730B (zh) * 2016-09-27 2023-03-28 百济神州(苏州)生物科技有限公司 使用包含parp抑制剂的组合产品治疗癌症
TW201840564A (zh) * 2017-02-28 2018-11-16 英屬開曼群島商百濟神州有限公司 稠合的四環或五環二氫二氮呯幷哢唑酮的鹽的結晶形式及其用途
US20200155567A1 (en) * 2017-07-17 2020-05-21 Beigene, Ltd. Treatment of 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
ZA201800765B (en) 2019-10-30
IL296835A (en) 2022-11-01
IL257442B2 (en) 2023-03-01
NZ739876A (en) 2022-09-30
EP3341375A1 (en) 2018-07-04
US10457680B2 (en) 2019-10-29
EP3341375A4 (en) 2019-01-16
JP6940039B2 (ja) 2021-09-22
BR112018003634A8 (pt) 2023-01-17
AU2016312011A1 (en) 2018-03-08
CA2994895A1 (en) 2017-03-02
KR20180041748A (ko) 2018-04-24
BR112018003634A2 (en) 2018-11-21
AU2016312011B2 (en) 2021-02-04
EA037366B1 (ru) 2021-03-18
US20190177325A1 (en) 2019-06-13
IL257442B (en) 2022-11-01
WO2017032289A1 (en) 2017-03-02
CN112521390A (zh) 2021-03-19
MX2018002322A (es) 2018-04-11
TW201718586A (zh) 2017-06-01
JP2018528199A (ja) 2018-09-27
MX385450B (es) 2025-03-18
BR112018003634B1 (pt) 2023-11-21
CN107922425B (zh) 2021-06-01
CN107922425A (zh) 2018-04-17
IL257442A (en) 2018-04-30
EP3341375B1 (en) 2022-04-13
EA201890547A1 (ru) 2018-07-31

Similar Documents

Publication Publication Date Title
TWI736550B (zh) 製備ｐａｒｐ抑制劑、結晶形式的方法及其用途
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
CN113454081A (zh) 咪唑并吡啶基化合物及其用于治疗增生性疾病的用途
BR112015017963A2 (pt) composto de fenil amino pirimidina deuterado, método para preparar a composição farmacêutica, composição farmacêutica e uso do composto
JP2020524148A (ja) 置換５−シアノインドール化合物及びその使用
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
JP7776418B2 (ja) イソクエン酸デヒドロゲナーゼ（ｉｄｈ）阻害剤
TW202302535A (zh) 化合物
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
CN110283160A (zh) 一种pdgfr激酶抑制剂
HK40116388A (zh) 用作cdk7激酶抑制剂的化合物及其应用
HK40061853B (zh) 用作cdk7激酶抑制剂的化合物及其应用
WO2024008083A1 (zh) 用作cdk7激酶抑制剂的化合物及其应用
HK40089264A (zh) 用作cdk7激酶抑制剂的化合物及其应用
CN111978318A (zh) 咪唑并吡啶类mnk1/mnk2激酶抑制剂及其制备方法和应用
HK40058867B (zh) 咪唑幷吡啶基化合物及其用於治疗增生性疾病的用途
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