CA2839621A1 - 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 - Google Patents

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 Download PDF

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Publication number
CA2839621A1
CA2839621A1 CA2839621A CA2839621A CA2839621A1 CA 2839621 A1 CA2839621 A1 CA 2839621A1 CA 2839621 A CA2839621 A CA 2839621A CA 2839621 A CA2839621 A CA 2839621A CA 2839621 A1 CA2839621 A1 CA 2839621A1
Authority
CA
Canada
Prior art keywords
compound
ray powder
powder diffraction
polymorph
diffraction pattern
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2839621A
Other languages
English (en)
French (fr)
Inventor
Isabelle Sylvie Gallou
Cornelius Gauer
Frank Stowasser
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CA2839621A1 publication Critical patent/CA2839621A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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)
CA2839621A 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 Abandoned CA2839621A1 (en)

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
CA2839621A1 true CA2839621A1 (en) 2012-12-27

Family

ID=46319784

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2839621A Abandoned CA2839621A1 (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

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)

Families Citing this family (12)

* 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
JP7649637B2 (ja) 2020-10-06 2025-03-21 エルジー ディスプレイ カンパニー リミテッド 伝送装置及び表示システム
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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
KR20140033432A (ko) 2014-03-18
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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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20180619