CN103228648A - (s)-2-氨基-3-(4-(2-氨基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧基)嘧啶-4-基)苯基)丙酸的晶体形式 - Google Patents

(s)-2-氨基-3-(4-(2-氨基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧基)嘧啶-4-基)苯基)丙酸的晶体形式 Download PDF

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Publication number
CN103228648A
CN103228648A CN2011800534249A CN201180053424A CN103228648A CN 103228648 A CN103228648 A CN 103228648A CN 2011800534249 A CN2011800534249 A CN 2011800534249A CN 201180053424 A CN201180053424 A CN 201180053424A CN 103228648 A CN103228648 A CN 103228648A
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China
Prior art keywords
amino
phenyl
crystalline compounds
chloro
pyrazol
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Pending
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CN2011800534249A
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Chinese (zh)
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李群
胡伟峰
杨小根
赵江琼
赵芒柱
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Lexicon Pharmaceuticals Inc
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Lexicon Genetics Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
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    • A—HUMAN NECESSITIES
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P9/12—Antihypertensives
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN2011800534249A 2010-11-05 2011-11-03 (s)-2-氨基-3-(4-(2-氨基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧基)嘧啶-4-基)苯基)丙酸的晶体形式 Pending CN103228648A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41042110P 2010-11-05 2010-11-05
US61/410,421 2010-11-05
PCT/US2011/059107 WO2012061576A1 (en) 2010-11-05 2011-11-03 Crystalline forms of ( s ) - 2 - amino - 3 - (4 - ( 2 - amino - 6 - ( (r) - 1 - (4 - ch loro-2- (3 -methyl- 1h- pyrazol- 1 -yl) phenyl) - 2, 2, 2 - trifluoroethoxy) pyrimidin- 4 - yl) phenyl) propanoic acid

Publications (1)

Publication Number Publication Date
CN103228648A true CN103228648A (zh) 2013-07-31

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CN2011800534249A Pending CN103228648A (zh) 2010-11-05 2011-11-03 (s)-2-氨基-3-(4-(2-氨基-6-((r)-1-(4-氯-2-(3-甲基-1h-吡唑-1-基)苯基)-2,2,2-三氟乙氧基)嘧啶-4-基)苯基)丙酸的晶体形式

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US (1) US8772483B2 (https=)
EP (1) EP2635569A1 (https=)
JP (1) JP2013541589A (https=)
KR (1) KR20130141572A (https=)
CN (1) CN103228648A (https=)
AR (1) AR083755A1 (https=)
AU (1) AU2011323302A1 (https=)
BR (1) BR112013011015A2 (https=)
CA (1) CA2816963A1 (https=)
MX (1) MX2013004921A (https=)
RU (1) RU2013125756A (https=)
SG (1) SG189535A1 (https=)
TW (1) TW201245183A (https=)
WO (1) WO2012061576A1 (https=)
ZA (1) ZA201303049B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109180650A (zh) * 2018-08-28 2019-01-11 湖南华腾制药有限公司 一种氘代色氨酸羟化酶抑制剂的晶型
CN113242736A (zh) * 2018-11-16 2021-08-10 阿尔塔万特科学公司 一种治疗肺动脉高压和相关性肺动脉高压的方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011063181A1 (en) * 2009-11-23 2011-05-26 Lexicon Pharmaceuticals, Inc. Methods and assays for the treatment of irritable bowel syndrome
US20120077831A1 (en) * 2009-11-23 2012-03-29 Philip Manton Brown Methods and assays for the treatment of irritable bowel syndrome
UA119247C2 (uk) 2013-09-06 2019-05-27 РОЙВЕНТ САЙЕНСИЗ ҐмбГ Спіроциклічні сполуки як інгібітори триптофангідроксилази
US9611201B2 (en) 2015-03-05 2017-04-04 Karos Pharmaceuticals, Inc. Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008073933A2 (en) * 2006-12-12 2008-06-19 Lexicon Pharmaceuticals, Inc. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7897763B2 (en) 2005-12-29 2011-03-01 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
US7855291B2 (en) 2005-12-29 2010-12-21 Lexicon Pharmaceuticals, Inc. Process for the preparation of substituted phenylalanines
DK1984344T3 (da) * 2005-12-29 2013-01-14 Lexicon Pharmaceuticals Inc Multicykliske aminosyrederivater og fremgangsmåder til anvendelse heraf
KR101582697B1 (ko) 2007-08-24 2016-01-05 렉시컨 파마슈티컬스 인코퍼레이티드 4-페닐-6-(2,2,2-트리플루오로-1-페닐에톡시)피리미딘-기재화합물의 제조 방법

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008073933A2 (en) * 2006-12-12 2008-06-19 Lexicon Pharmaceuticals, Inc. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
MINO R. CAIRA: "Crystalline Polymorphism of Organic Compounds", 《TOPICS IN CURRENT CHEMISTRY》 *
RICHARD J. BASTIN, ET.AL.: "Salt Selection and Optimisation Procedures for Pharmaceutical New Chemical Entities", 《ORGANIC PROCESS RESEARCH & DEVELOPMENT》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109180650A (zh) * 2018-08-28 2019-01-11 湖南华腾制药有限公司 一种氘代色氨酸羟化酶抑制剂的晶型
CN113242736A (zh) * 2018-11-16 2021-08-10 阿尔塔万特科学公司 一种治疗肺动脉高压和相关性肺动脉高压的方法

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EP2635569A1 (en) 2013-09-11
US8772483B2 (en) 2014-07-08
JP2013541589A (ja) 2013-11-14
ZA201303049B (en) 2014-07-30
US20120122904A1 (en) 2012-05-17
WO2012061576A1 (en) 2012-05-10
AR083755A1 (es) 2013-03-20
RU2013125756A (ru) 2014-12-10
BR112013011015A2 (pt) 2016-08-23
KR20130141572A (ko) 2013-12-26
TW201245183A (en) 2012-11-16
MX2013004921A (es) 2013-06-28
SG189535A1 (en) 2013-06-28
CA2816963A1 (en) 2012-05-10
AU2011323302A1 (en) 2013-05-30

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