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WO2012138147A3 - Forme cristalline de l'acide 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylique et son procédé de préparation - Google Patents

Forme cristalline de l'acide 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylique et son procédé de préparation Download PDF

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Publication number
WO2012138147A3
WO2012138147A3 PCT/KR2012/002575 KR2012002575W WO2012138147A3 WO 2012138147 A3 WO2012138147 A3 WO 2012138147A3 KR 2012002575 W KR2012002575 W KR 2012002575W WO 2012138147 A3 WO2012138147 A3 WO 2012138147A3
Authority
WO
WIPO (PCT)
Prior art keywords
crystalline form
indol
pyrazole
cyano
isopropyl
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.)
Ceased
Application number
PCT/KR2012/002575
Other languages
English (en)
Other versions
WO2012138147A2 (fr
Inventor
Jung Min Yun
Ki Sook Park
Joo Yong Yoon
Ju Young Lee
Geun Tae Kim
Cheol Kyu Jung
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.)
LG Chem Ltd
Original Assignee
LG Life Sciences Ltd
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 LG Life Sciences Ltd filed Critical LG Life Sciences Ltd
Priority to CN201280016696.6A priority Critical patent/CN103459381B/zh
Priority to JP2014503602A priority patent/JP6008937B2/ja
Publication of WO2012138147A2 publication Critical patent/WO2012138147A2/fr
Publication of WO2012138147A3 publication Critical patent/WO2012138147A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne une forme cristalline du composé de formule (1) et son procédé de préparation.
PCT/KR2012/002575 2011-04-06 2012-04-05 Forme cristalline de l'acide 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylique et son procédé de préparation Ceased WO2012138147A2 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201280016696.6A CN103459381B (zh) 2011-04-06 2012-04-05 1-(3-氰基-1-异丙基-吲哚-5-基)吡唑-4-甲酸晶型及其生产方法
JP2014503602A JP6008937B2 (ja) 2011-04-06 2012-04-05 １−（３−シアノ−１−イソプロピル−インドール−５−イル）ピラゾール−４−カルボン酸の結晶形とその製造方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20110031490 2011-04-06
KR10-2011-0031490 2011-04-06

Publications (2)

Publication Number Publication Date
WO2012138147A2 WO2012138147A2 (fr) 2012-10-11
WO2012138147A3 true WO2012138147A3 (fr) 2012-11-29

Family

ID=46969691

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2012/002575 Ceased WO2012138147A2 (fr) 2011-04-06 2012-04-05 Forme cristalline de l'acide 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylique et son procédé de préparation

Country Status (5)

Country Link
JP (1) JP6008937B2 (fr)
KR (1) KR101424013B1 (fr)
CN (1) CN103459381B (fr)
TW (1) TWI548630B (fr)
WO (1) WO2012138147A2 (fr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106008488B (zh) * 2016-05-20 2018-10-30 广东东阳光药业有限公司 氰基吲哚类衍生物及其制备方法和用途
CN106045898B (zh) * 2016-06-28 2019-05-24 广东东阳光药业有限公司 一种吲哚类化合物及其制备方法和用途
BR112019008388A2 (pt) * 2016-11-28 2019-07-09 Teijin Pharma Ltd fármaco terapêutico ou fármaco profilático para nefropatia diabética.
TWI884455B (zh) 2020-11-04 2025-05-21 南韓商Ｌｇ化學股份有限公司 １－（３－氰基－１－異丙基－吲哚－５－基）吡唑－４－羧酸結晶之製備方法及包含彼之醫藥組成物
AR124178A1 (es) 2020-12-01 2023-02-22 Lg Chemical Ltd Formulación compuesta para administración oral que comprende ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico y un proceso para su preparación
MX2023005461A (es) 2020-12-01 2023-05-22 Lg Chemical Ltd Formulacion compuesta para administracion oral que comprende acido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxilico y un proceso para su preparacion.
AU2022257531A1 (en) 2021-04-16 2023-10-26 Lg Chem, Ltd. Oral formulation containing 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid
WO2022231263A1 (fr) * 2021-04-27 2022-11-03 주식회사 엘지화학 Procédé de préparation d'un intermédiaire pour la synthèse d'un inhibiteur de la xanthine oxydase
KR20220147531A (ko) * 2021-04-27 2022-11-03 주식회사 엘지화학 잔틴 옥시다아제 저해제의 제조 방법
WO2022233264A1 (fr) * 2021-05-07 2022-11-10 江苏新元素医药科技有限公司 Classe d'inhibiteurs de xanthine oxydase
BR112023026415A2 (pt) 2021-06-15 2024-03-05 Lg Chemical Ltd Composição farmacêutica que compreende ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico
AR126164A1 (es) 2021-06-17 2023-09-27 Lg Chemical Ltd Formulación compuesta para dosificación oral que comprende ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico
TWI822151B (zh) * 2021-07-02 2023-11-11 南韓商Ｌｇ化學股份有限公司 製備黃嘌呤氧化酶抑制劑的方法
US20250282753A1 (en) * 2022-04-27 2025-09-11 Atom Bioscience America Corporation Compounds useful for reducing uric acid
TW202342455A (zh) * 2022-04-27 2023-11-01 大陸商江蘇新元素醫藥科技有限公司 可用於痛風的化合物

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997027186A1 (fr) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-(pyrazol-3-yl-ethyl)-4-(indol-3-yl)-piperidine utilisee comme medicaments agissant sur le systeme nerveux central
WO2007113647A1 (fr) * 2006-04-04 2007-10-11 Pfizer Products Inc. Formes polymorphes de (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-méthyl-1h-pyrazol-4υl)-1-oxo-2,6-dihydro-1h-[1,2]diazépino[4,5,6-cd]indol-8-yl)acétamide

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2133332T1 (sl) * 2007-04-11 2014-02-28 Kissei Pharmaceutical Co., Ltd. (aza)indolinski derivat in njegova uporaba v medicinske namene
WO2008126901A1 (fr) * 2007-04-11 2008-10-23 Kissei Pharmaceutical Co., Ltd. Composé hétérocyclique contenant de l'azote et composition pharmaceutique le contenant
TWI423962B (zh) * 2009-10-07 2014-01-21 Lg Life Sciences Ltd 有效作為黃嘌呤氧化酶抑制劑之新穎化合物、其製備方法及含該化合物之醫藥組成物

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997027186A1 (fr) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-(pyrazol-3-yl-ethyl)-4-(indol-3-yl)-piperidine utilisee comme medicaments agissant sur le systeme nerveux central
WO2007113647A1 (fr) * 2006-04-04 2007-10-11 Pfizer Products Inc. Formes polymorphes de (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-méthyl-1h-pyrazol-4υl)-1-oxo-2,6-dihydro-1h-[1,2]diazépino[4,5,6-cd]indol-8-yl)acétamide

Also Published As

Publication number Publication date
TWI548630B (zh) 2016-09-11
CN103459381A (zh) 2013-12-18
TW201245182A (en) 2012-11-16
JP2014510133A (ja) 2014-04-24
CN103459381B (zh) 2015-12-09
KR101424013B1 (ko) 2014-08-18
JP6008937B2 (ja) 2016-10-19
KR20120114174A (ko) 2012-10-16
WO2012138147A2 (fr) 2012-10-11

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