KR20140033432A - (s)-피롤리딘-1,2-디카르복실산 2-아미드 1-(｛4-메틸-5-[2-(2,2,2-트리플루오로-1,1-디메틸-에틸)-피리딘-4-일]-티아졸-2-일｝-아미드)의 다형체 - Google Patents

(s)-피롤리딘-1,2-디카르복실산 2-아미드 1-(｛4-메틸-5-[2-(2,2,2-트리플루오로-1,1-디메틸-에틸)-피리딘-4-일]-티아졸-2-일｝-아미드)의 다형체 Download PDF

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Publication number
KR20140033432A
KR20140033432A KR1020137033590A KR20137033590A KR20140033432A KR 20140033432 A KR20140033432 A KR 20140033432A KR 1020137033590 A KR1020137033590 A KR 1020137033590A KR 20137033590 A KR20137033590 A KR 20137033590A KR 20140033432 A KR20140033432 A KR 20140033432A
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South Korea
Prior art keywords
cancer
compound
ray powder
powder diffraction
polymorph
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KR1020137033590A
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English (en)
Korean (ko)
Inventor
이자벨 실비 잘루
코르넬리우스 가우어
프랭크 스토바서
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노파르티스 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020137033590A 2011-06-21 2012-06-19 (s)-피롤리딘-1,2-디카르복실산 2-아미드 1-(｛4-메틸-5-[2-(2,2,2-트리플루오로-1,1-디메틸-에틸)-피리딘-4-일]-티아졸-2-일｝-아미드)의 다형체 Withdrawn KR20140033432A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161499222P 2011-06-21 2011-06-21
US61/499,222 2011-06-21
PCT/EP2012/061756 WO2012175522A1 (en) 2011-06-21 2012-06-19 Polymorphs of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide

Publications (1)

Publication Number Publication Date
KR20140033432A true KR20140033432A (ko) 2014-03-18

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KR1020137033590A Withdrawn KR20140033432A (ko) 2011-06-21 2012-06-19 (s)-피롤리딘-1,2-디카르복실산 2-아미드 1-(｛4-메틸-5-[2-(2,2,2-트리플루오로-1,1-디메틸-에틸)-피리딘-4-일]-티아졸-2-일｝-아미드)의 다형체

Country Status (11)

Country Link
US (1) US9006270B2 (enExample)
EP (1) EP2723733A1 (enExample)
JP (1) JP2014517049A (enExample)
KR (1) KR20140033432A (enExample)
CN (1) CN103619840B (enExample)
BR (1) BR112013032687A2 (enExample)
CA (1) CA2839621A1 (enExample)
IN (1) IN2014DN00145A (enExample)
MX (1) MX2013014887A (enExample)
RU (1) RU2014101626A (enExample)
WO (1) WO2012175522A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220045883A (ko) 2020-10-06 2022-04-13 엘지디스플레이 주식회사 전송 장치 및 표시 시스템

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY192644A (en) 2009-11-27 2022-08-29 Genzyme Corp An amorphous and a crystalline form of genz 112638 hemitartrate as inhibitor of glucosylceramide synthase
CN104244949A (zh) * 2012-03-30 2014-12-24 诺华股份有限公司 用于治疗神经母细胞瘤、尤文氏肉瘤或横纹肌肉瘤的化合物
DK3076969T3 (da) * 2013-12-06 2021-11-22 Novartis Ag Doseringsregime for en alfa-isoform-selektiv phosphatidylinositol-3-kinase-hæmmer
EP3200772B1 (en) * 2014-10-03 2022-08-03 Novartis AG Pharmaceutical compositions comprising alpelisib
EP3956330A4 (en) 2019-04-18 2023-01-18 The Johns Hopkins University SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A]PYRIDINE DERIVATIVES AND THEIR USE
CN112961090A (zh) * 2019-12-13 2021-06-15 武汉九州钰民医药科技有限公司 合成Alpelisib的关键中间体及其制备方法
CN110964005A (zh) * 2019-12-16 2020-04-07 武汉九州钰民医药科技有限公司 一种Alpelisib的制备工艺
CN111057051A (zh) * 2019-12-16 2020-04-24 武汉九州钰民医药科技有限公司 PI3K抑制剂Alpelisib的新合成方法
IL301817A (en) 2020-10-13 2023-06-01 Univ Johns Hopkins Modified 4-([4,2,1]triazolo[5,1-a]pyridin-6-yl)thiophene-2-carboxamide histories and their use
WO2022234408A1 (en) * 2021-05-03 2022-11-10 Novartis Ag Alpelisib formulation
CN116925023B (zh) * 2023-07-18 2025-11-21 江苏桐孚高新材料有限公司 2-全氟烷基-4h-吡喃-4-酮衍生物的改进合成方法

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UY29149A1 (es) * 2004-10-07 2006-05-31 Boehringer Ingelheim Int Tiazolil-dihidro-indazoles
JP2009535386A (ja) * 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ チアゾール誘導体および抗腫瘍剤としてのその使用
UA104147C2 (uk) * 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
AR082418A1 (es) * 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220045883A (ko) 2020-10-06 2022-04-13 엘지디스플레이 주식회사 전송 장치 및 표시 시스템

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Publication number Publication date
CA2839621A1 (en) 2012-12-27
US20140171470A1 (en) 2014-06-19
WO2012175522A1 (en) 2012-12-27
RU2014101626A (ru) 2015-07-27
JP2014517049A (ja) 2014-07-17
BR112013032687A2 (pt) 2016-08-30
MX2013014887A (es) 2014-02-17
CN103619840B (zh) 2016-01-20
AU2012274141A1 (en) 2013-12-12
US9006270B2 (en) 2015-04-14
EP2723733A1 (en) 2014-04-30
IN2014DN00145A (enExample) 2015-05-22
CN103619840A (zh) 2014-03-05
AU2012274141B2 (en) 2015-12-24

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PA0105 International application

Patent event date: 20131218

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid