CN110650963B - Gdc-0077的多晶型物和固体形式及其制备方法 - Google Patents

Gdc-0077的多晶型物和固体形式及其制备方法 Download PDF

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Publication number
CN110650963B
CN110650963B CN201880028227.3A CN201880028227A CN110650963B CN 110650963 B CN110650963 B CN 110650963B CN 201880028227 A CN201880028227 A CN 201880028227A CN 110650963 B CN110650963 B CN 110650963B
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polymorph
crystalline
gdc
cancer
anhydrous
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Chinese (zh)
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CN110650963A (zh
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P·查克拉瓦蒂
韩翀
S·M·凯利
K·纳格普迪
S·萨维奇
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
CN201880028227.3A 2017-04-28 2018-04-26 Gdc-0077的多晶型物和固体形式及其制备方法 Active CN110650963B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762491812P 2017-04-28 2017-04-28
US62/491,812 2017-04-28
PCT/EP2018/060820 WO2018197653A1 (en) 2017-04-28 2018-04-26 Polymorphs and solid forms of (s)-2-((2-((s)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide, and methods of production

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CN110650963A CN110650963A (zh) 2020-01-03
CN110650963B true CN110650963B (zh) 2022-09-27

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US (4) US20180339997A1 (enExample)
EP (2) EP3615541B1 (enExample)
JP (2) JP6998969B2 (enExample)
KR (1) KR102342776B1 (enExample)
CN (1) CN110650963B (enExample)
AU (1) AU2018259089B2 (enExample)
CA (1) CA3048591A1 (enExample)
ES (1) ES3027566T3 (enExample)
IL (3) IL298518B2 (enExample)
MX (1) MX394540B (enExample)
PL (1) PL3615541T3 (enExample)
TW (1) TWI826373B (enExample)
WO (1) WO2018197653A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20211775A1 (es) 2015-07-02 2021-09-08 Hoffmann La Roche Compuestos de benzoxacepina oxazolidinona y metodos de uso
ES2953833T3 (es) 2016-12-15 2023-11-16 Hoffmann La Roche La invención se refiere a procedimientos de preparación de compuestos de benzoxacepina oxazolidinona e intermedios útiles
MX394540B (es) 2017-04-28 2025-03-21 Hoffmann La Roche Polimorfos y formas solidas de la (s)-2-((2-((s)-4-(difluorometil)-2-oxooxazolidin-3-il)-5,6-dihidrobenzo[f]imidazo[1,2-d] [1,4]oxazepin-9-il)amino)propanamida, y metodos de produccion.
CN112313202A (zh) * 2019-05-21 2021-02-02 江苏众强药业有限公司 曲前列尼尔钠盐新晶型及制备方法
MX2022000279A (es) * 2019-07-07 2022-02-03 Olema Pharmaceuticals Inc Regimenes de antagonistas del receptor de estrogeno.
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
KR20220119610A (ko) * 2019-11-25 2022-08-30 상하이 한서 바이오메디컬 컴퍼니 리미티드 3개의 융합된 고리 유도체-함유 염 또는 결정 형태 및 이의 약학 조성물
CN112830935B (zh) * 2019-11-25 2023-12-22 上海翰森生物医药科技有限公司 含三并环类衍生物自由碱的晶型及其药物组合物
TWI801730B (zh) * 2020-04-07 2023-05-11 神雲科技股份有限公司 具系統設定資料同步功能的伺服器
TW202440096A (zh) 2023-03-24 2024-10-16 美商亞文納營運公司 雌激素受體降解劑之給藥方案

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102762576A (zh) * 2009-09-28 2012-10-31 霍夫曼-拉罗奇有限公司 苯并氧杂氮杂*pi3k抑制剂化合物和使用方法
WO2017001645A1 (en) * 2015-07-02 2017-01-05 F. Hoffmann-La Roche Ag Benzoxazepin oxazolidinone compounds and methods of use
CN110088111A (zh) * 2016-12-15 2019-08-02 豪夫迈·罗氏有限公司 (S)-2-((2-((S)-4-(二氟甲基)-2-氧代噁唑烷-3-基)-5,6-二氢苯并[f]咪唑并[1,2-d][1,4]氧氮杂卓-9-基)氨基)丙酰胺的制备方法

Family Cites Families (6)

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US5846824A (en) 1994-02-07 1998-12-08 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
US6274327B1 (en) 1992-04-13 2001-08-14 Ludwig Institute For Cancer Research Polypeptides having kinase activity, their preparation and use
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
US9012464B2 (en) 2010-11-25 2015-04-21 Ratiopharm Gmbh Salts and polymorphic forms of Afatinib
MX356804B (es) 2013-12-16 2018-06-13 Hoffmann La Roche Polimorfos de 2-(4-(2-(1-isopropil-3-metil-1h-1,2,4-triazol-5-il)- 5,6-dihidrobenzo[f]imidazol[1,2-d][1,4]oxazepin-9-il)-1h-pirazol- 1-il)-2-metilpropanamida, metodos de produccion, y usos farmaceuticos de los mismos.
MX394540B (es) 2017-04-28 2025-03-21 Hoffmann La Roche Polimorfos y formas solidas de la (s)-2-((2-((s)-4-(difluorometil)-2-oxooxazolidin-3-il)-5,6-dihidrobenzo[f]imidazo[1,2-d] [1,4]oxazepin-9-il)amino)propanamida, y metodos de produccion.

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102762576A (zh) * 2009-09-28 2012-10-31 霍夫曼-拉罗奇有限公司 苯并氧杂氮杂*pi3k抑制剂化合物和使用方法
WO2017001645A1 (en) * 2015-07-02 2017-01-05 F. Hoffmann-La Roche Ag Benzoxazepin oxazolidinone compounds and methods of use
CN110088111A (zh) * 2016-12-15 2019-08-02 豪夫迈·罗氏有限公司 (S)-2-((2-((S)-4-(二氟甲基)-2-氧代噁唑烷-3-基)-5,6-二氢苯并[f]咪唑并[1,2-d][1,4]氧氮杂卓-9-基)氨基)丙酰胺的制备方法

Non-Patent Citations (1)

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Title
Crystalline Polymorphism of Organic Compounds;CAIRA ED-MONTCHAMP JEAN-LUC;《TOPICS IN CURRENT CHEMISTRY》;19980101;第198卷;第163-208页 *

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US12410189B2 (en) 2025-09-09
CN110650963A (zh) 2020-01-03
IL298518B2 (en) 2025-05-01
US20230167128A1 (en) 2023-06-01
JP6998969B2 (ja) 2022-02-10
WO2018197653A1 (en) 2018-11-01
US11028100B2 (en) 2021-06-08
AU2018259089A1 (en) 2019-07-04
KR102342776B1 (ko) 2021-12-23
AU2018259089A9 (en) 2019-10-10
CA3048591A1 (en) 2018-11-01
IL298518B1 (en) 2025-01-01
EP4534148A3 (en) 2025-05-21
IL267464A (en) 2019-08-29
BR112019013292A2 (pt) 2019-12-10
JP2021181446A (ja) 2021-11-25
WO2018197653A9 (en) 2019-09-19
US11591345B2 (en) 2023-02-28
JP2020517713A (ja) 2020-06-18
PL3615541T3 (pl) 2025-06-23
US20180339997A1 (en) 2018-11-29
ES3027566T3 (en) 2025-06-16
IL267464B2 (en) 2023-05-01
IL267464B1 (en) 2023-01-01
EP3615541B1 (en) 2025-03-19
EP4534148A2 (en) 2025-04-09
KR20190133724A (ko) 2019-12-03
IL298518A (en) 2023-01-01
IL317762A (en) 2025-02-01
EP3615541A1 (en) 2020-03-04
TW201843160A (zh) 2018-12-16
US20210094970A1 (en) 2021-04-01
MX2019012507A (es) 2019-12-19
US20200399286A1 (en) 2020-12-24
MX394540B (es) 2025-03-21
TWI826373B (zh) 2023-12-21
EP3615541C0 (en) 2025-03-19
AU2018259089B2 (en) 2022-05-12

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