JOP20210310A1 - أشكال الحالة الصلبة - Google Patents

أشكال الحالة الصلبة

Info

Publication number
JOP20210310A1
JOP20210310A1 JOP/2021/0310A JOP20210310A JOP20210310A1 JO P20210310 A1 JOP20210310 A1 JO P20210310A1 JO P20210310 A JOP20210310 A JO P20210310A JO P20210310 A1 JOP20210310 A1 JO P20210310A1
Authority
JO
Jordan
Prior art keywords
solid state
state forms
forms
fluoro
methyl
Prior art date
Application number
JOP/2021/0310A
Other languages
English (en)
Inventor
Patricia Lopez
Stephanie Azali
Prashant Agarwal
Albert Amegadzie
Mary Chaves
Darren Leonard Reid
Roman Shimanovich
Ron C Kelly
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of JOP20210310A1 publication Critical patent/JOP20210310A1/ar

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)

Abstract

يتعلق الاختراع الحالي بأشكال متبلورة وغير متبلورة من 6- فلورو-7-(2- فلورو-6- هيدروكسي فنيل) -1-(4- ميثيل-2-(2- بروبانيل) -3- بيريدينيل) -4-((2S) -2- ميثيل-4-(2- بروبينويل) -1- بيبرازنيل) بيريدو[3،2d-] بيريميدين-2(1H)- ون، بما في ذلك العديد من الأشكال اللامائية، أشكال الهيدرات وأشكال المذيبات، وأشكال الحالة الصلبة منها، التركيبات الصيدلانية، وطرق علاج مرض يتوسطه تثبيط KRAS G12C.
JOP/2021/0310A 2019-05-21 2020-05-20 أشكال الحالة الصلبة JOP20210310A1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962851044P 2019-05-21 2019-05-21
PCT/US2020/033831 WO2020236947A1 (en) 2019-05-21 2020-05-20 Solid state forms

Publications (1)

Publication Number Publication Date
JOP20210310A1 true JOP20210310A1 (ar) 2023-01-30

Family

ID=71083699

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2021/0310A JOP20210310A1 (ar) 2019-05-21 2020-05-20 أشكال الحالة الصلبة

Country Status (20)

Country Link
US (3) US11236091B2 (ar)
EP (1) EP3972973A1 (ar)
JP (3) JP7092935B2 (ar)
KR (1) KR20220011670A (ar)
CN (1) CN114144414A (ar)
AR (1) AR118978A1 (ar)
AU (1) AU2020280024A1 (ar)
BR (1) BR112021023277A2 (ar)
CA (2) CA3140392A1 (ar)
CL (2) CL2021003064A1 (ar)
CO (1) CO2021017366A2 (ar)
CR (1) CR20210665A (ar)
IL (1) IL288077A (ar)
JO (1) JOP20210310A1 (ar)
MX (1) MX2021014126A (ar)
PE (1) PE20220504A1 (ar)
SG (1) SG11202112855WA (ar)
TW (1) TW202110835A (ar)
UY (1) UY38710A (ar)
WO (1) WO2020236947A1 (ar)

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KR102592246B1 (ko) 2016-12-22 2023-10-23 암젠 인크 폐암, 췌장암 또는 대장암을 치료하기 위한 kras g12c 억제제로서의 벤즈이소티아졸, 이소티아졸로[3,4-b]피리딘, 퀴나졸린, 프탈라진, 피리도[2,3-d]피리다진 및 피리도[2,3-d]피리미딘 유도체
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
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AU2019262589B2 (en) 2018-05-04 2022-07-07 Amgen Inc. KRAS G12C inhibitors and methods of using the same
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ES2938987T3 (es) 2018-06-01 2023-04-18 Amgen Inc Inhibidores de KRAS G12c y métodos de uso de los mismos
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
JP2020090482A (ja) 2018-11-16 2020-06-11 アムジエン・インコーポレーテツド Kras g12c阻害剤化合物の重要な中間体の改良合成法
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3883565A1 (en) 2018-11-19 2021-09-29 Amgen Inc. Kras g12c inhibitors and methods of using the same
WO2020146613A1 (en) 2019-01-10 2020-07-16 Mirati Therapeutics, Inc. Kras g12c inhibitors
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
US11236091B2 (en) * 2019-05-21 2022-02-01 Amgen Inc. Solid state forms
MX2022002465A (es) 2019-08-29 2022-05-19 Mirati Therapeutics Inc Inhibidores de kras g12d.
WO2021061749A1 (en) 2019-09-24 2021-04-01 Mirati Therapeutics, Inc. Combination therapies
AU2020405170A1 (en) 2019-12-20 2022-06-30 Mirati Therapeutics, Inc. SOS1 inhibitors
US20230183235A1 (en) * 2020-05-20 2023-06-15 Teva Pharmaceuticals International Gmbh Solid state forms of amg-510 and process for preparation thereof
TW202229278A (zh) * 2020-11-26 2022-08-01 大陸商上海翰森生物醫藥科技有限公司 含氮雜環類衍生物的鹽、晶型及其製備方法和應用
TW202241442A (zh) 2021-01-08 2022-11-01 美商安進公司 Kras g12c抑制劑在治療癌症中之用途
JP2024510612A (ja) * 2021-03-17 2024-03-08 アムジエン・インコーポレーテツド ソトラシブ投与レジメン
WO2022246069A1 (en) * 2021-05-19 2022-11-24 Teva Pharmaceuticals International Gmbh Process for preparation of sotorasib and solid state form thereof
WO2022269008A1 (en) 2021-06-24 2022-12-29 Sandoz Ag Crystalline form of sotorasib
EP4227305A1 (en) 2022-02-10 2023-08-16 Sandoz AG Crystalline form of sotorasib
CN114605406B (zh) * 2021-09-18 2023-05-26 都创(上海)医药开发有限公司 Amg510化合物的晶型及其制备方法和用途
AU2022421224A1 (en) 2021-12-22 2024-06-20 The Regents Of The University Of California Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase
CN115368358A (zh) * 2022-09-01 2022-11-22 浙江九洲药业股份有限公司 一种Sotorasib新晶型及其制备方法与应用

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