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AR083755A1 - Formas solidas del acido (s)-2-amino-3-(4-(-2-amino-6-((r)-1-(4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico - Google Patents

Formas solidas del acido (s)-2-amino-3-(4-(-2-amino-6-((r)-1-(4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico

Info

Publication number
AR083755A1
AR083755A1 ARP110104110A ARP110104110A AR083755A1 AR 083755 A1 AR083755 A1 AR 083755A1 AR P110104110 A ARP110104110 A AR P110104110A AR P110104110 A ARP110104110 A AR P110104110A AR 083755 A1 AR083755 A1 AR 083755A1
Authority
AR
Argentina
Prior art keywords
phenyl
amino
pyrimidin
methyl
crystalline compound
Prior art date
Application number
ARP110104110A
Other languages
English (en)
Inventor
Qun Li
Weifeng Hu
Xiaogen Yang
Jiangqiong Zhao
Matthew Mangzhu Zhao
Original Assignee
Lexicon Pharmaceuticals 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 Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Publication of AR083755A1 publication Critical patent/AR083755A1/es

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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • A61P1/10—Laxatives
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se revelan formas sólidas del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico y de sus sales. También se revelan formas de dosificación farmacéuticas métodos de utilización de las mismas y procedimiento de preparación.Reivindicación 1: Un compuesto cristalino, el cual es el ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico o una sal del mismo. Reivindicación 2: El ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico cristalino que tiene un pico de DSC a alrededor de 126ºC. Reivindicación 3: Un compuesto cristalino, el cual es el besilato del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico. Reivindicación 5: El compuesto cristalino de la reivindicación 4, el cual tiene un punto de fusión de alrededor de 234ºC y/o un pico de DSC a alrededor de 238ºC. Reivindicación 14: Un compuesto cristalino, el cual es el dibesilato del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico. Reivindicación 15: El compuesto cristalino de la reivindicación 14, el cual tiene un punto de fusión de alrededor de 223ºC y/o un pico de DSC a alrededor de 227ºC. Reivindicación 17: Un compuesto cristalino, el cual es el edisilato del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico. Reivindicación 18: El compuesto cristalino de la reivindicación 17, el cual tiene un punto de fusión de alrededor de 252ºC y/o un pico de DSC a alrededor de 259ºC. Reivindicación 20: Un compuesto cristalino, el cual es el esilato del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico. Reivindicación 21: El compuesto cristalino de la reivindicación 20, el cual tiene un punto de fusión de alrededor de 214ºC y/o un pico de DSC a alrededor de 223ºC. Reivindicación 23: Un compuesto cristalino, el cual es el sulfato de isopropilo del ácido (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-cloro-2-(3-metil-1H-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico. Reivindicación 24: El compuesto cristalino de la reivindicación 23, el cual tiene un punto de fusión de alrededor de 194ºC y/o un pico de DSC a alrededor de 204ºC.
ARP110104110A 2010-11-05 2011-11-04 Formas solidas del acido (s)-2-amino-3-(4-(-2-amino-6-((r)-1-(4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico AR083755A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41042110P 2010-11-05 2010-11-05

Publications (1)

Publication Number Publication Date
AR083755A1 true AR083755A1 (es) 2013-03-20

Family

ID=45023872

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104110A AR083755A1 (es) 2010-11-05 2011-11-04 Formas solidas del acido (s)-2-amino-3-(4-(-2-amino-6-((r)-1-(4-cloro-2-(3-metil-1h-pirazol-1-il)fenil)-2,2,2-trifluoroetoxi)pirimidin-4-il)fenil)propanoico

Country Status (15)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013511544A (ja) * 2009-11-23 2013-04-04 レクシコン ファーマシューティカルズ インコーポレイテッド 過敏性腸症候群を治療するための方法及びアッセイ
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
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
JP2022507533A (ja) * 2018-11-16 2022-01-18 アルタバント・サイエンシズ・ゲーエムベーハー 肺動脈性高血圧症および他疾患に関連する肺動脈性肺高血圧症の治療法

Family Cites Families (5)

* 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
AU2006337137B2 (en) * 2005-12-29 2012-06-14 Tersera Therapeutics Llc Multicyclic amino acid derivatives and methods of their use
UA99270C2 (en) 2006-12-12 2012-08-10 Лексикон Фармасьютикалз, Инк. 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds and methods of their use
US20090062540A1 (en) 2007-08-24 2009-03-05 Bednarz Mark S Methods of preparing 4-phenyl-6-(2,2,2-trifluoro-1-phenylethoxy)pyrimidine-based compounds

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Publication number Publication date
EP2635569A1 (en) 2013-09-11
ZA201303049B (en) 2014-07-30
MX2013004921A (es) 2013-06-28
KR20130141572A (ko) 2013-12-26
TW201245183A (en) 2012-11-16
US8772483B2 (en) 2014-07-08
JP2013541589A (ja) 2013-11-14
CA2816963A1 (en) 2012-05-10
BR112013011015A2 (pt) 2016-08-23
SG189535A1 (en) 2013-06-28
AU2011323302A1 (en) 2013-05-30
US20120122904A1 (en) 2012-05-17
CN103228648A (zh) 2013-07-31
RU2013125756A (ru) 2014-12-10
WO2012061576A1 (en) 2012-05-10

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