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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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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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 (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ625712A (en) 2009-11-27 2016-02-26 Genzyme Corp An amorphous and a crystalline form of genz 112638 hemitartrate as inhibitor of glucosylceramide synthase
KR20150002623A (ko) * 2012-03-30 2015-01-07 노파르티스 아게 신경모세포종, 유잉 육종 또는 횡문근육종의 치료에 사용하기 위한 화합물
CA2930359C (en) * 2013-12-06 2022-03-01 Novartis Ag Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor
CA2962714C (en) * 2014-10-03 2023-09-19 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
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
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
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

Family Cites Families (4)

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Publication number Priority date Publication date Assignee Title
UY29149A1 (es) * 2004-10-07 2006-05-31 Boehringer Ingelheim Int Tiazolil-dihidro-indazoles
EP2016075A1 (en) * 2006-05-03 2009-01-21 AstraZeneca AB Thiazole derivatives and their use as anti-tumour agents
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

Also Published As

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

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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