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WO2012138147A3 - 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof - Google Patents

1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof 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
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WO
WIPO (PCT)
Prior art keywords
crystalline form
indol
pyrazole
cyano
isopropyl
Prior art date
Application number
PCT/KR2012/002575
Other languages
French (fr)
Other versions
WO2012138147A2 (en
Inventor
Jung Min Yun
Ki Sook Park
Joo Yong Yoon
Ju Young Lee
Geun Tae Kim
Cheol Kyu Jung
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 JP2014503602A priority Critical patent/JP6008937B2/en
Priority to CN201280016696.6A priority patent/CN103459381B/en
Publication of WO2012138147A2 publication Critical patent/WO2012138147A2/en
Publication of WO2012138147A3 publication Critical patent/WO2012138147A3/en

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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
    • C07D403/04—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

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

Abstract

The present invention relates to a crystalline form of the compound of formula (1), and a process for preparing the same.
PCT/KR2012/002575 2011-04-06 2012-04-05 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof WO2012138147A2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2014503602A JP6008937B2 (en) 2011-04-06 2012-04-05 Crystal form of 1- (3-cyano-1-isopropyl-indol-5-yl) pyrazole-4-carboxylic acid and process for producing the same
CN201280016696.6A CN103459381B (en) 2011-04-06 2012-04-05 1-(3-cyano group-1-sec.-propyl-indoles-5-base) pyrazoles-4-aminic acid crystal and production method thereof

Applications Claiming Priority (2)

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

Publications (2)

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

Family

ID=46969691

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2012/002575 WO2012138147A2 (en) 2011-04-06 2012-04-05 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid crystalline form and the producing method thereof

Country Status (5)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106008488B (en) * 2016-05-20 2018-10-30 广东东阳光药业有限公司 Cyanoindole analog derivative and its preparation method and application
CN106045898B (en) * 2016-06-28 2019-05-24 广东东阳光药业有限公司 A kind of Benzazole compounds and its preparation method and application
RU2735538C1 (en) * 2016-11-28 2020-11-03 Тейдзин Фарма Лимитед Therapeutic drug or preventive therapeutic agent for diabetic nephropathy
PE20240139A1 (en) 2020-11-04 2024-01-30 Lg Chemical Ltd METHOD FOR THE PREPARATION OF THE CRYSTALLINE AND PHARMACEUTICAL COMPOSITION 1-(3-CYANO-1-ISOPROPIL-INDOL-5-YL)PYRAZOLE-4-CARBOXYLIC ACID WHICH INCLUDES IT
TW202231270A (en) 2020-12-01 2022-08-16 南韓商Ｌｇ化學股份有限公司 Composite formulation for oral administration comprising 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazol-4-carboxyl acid and a process for the preparation thereof
MX2023005459A (en) * 2020-12-01 2023-05-23 Lg Chemical Ltd Stable oral formulation containing 1-(3-cyano-1-isopropyl-indol-5 -yl)pyrazole-4-carboxylic acid.
MX2023011500A (en) 2021-04-16 2023-10-04 Lg Chemical Ltd Oral formulation containing 1-(3-cyano-1-isopropyl-indol-5-yl)pyr azole-4-carboxylic acid.
WO2022231263A1 (en) * 2021-04-27 2022-11-03 주식회사 엘지화학 Method for preparing intermediate for synthesis of xanthine oxidase inhibitor
EP4335844A1 (en) * 2021-04-29 2024-03-13 Jiangsu Atom Bioscience and Pharmaceutical Co., Ltd. Class of xanthine oxidase inhibitors
JP2024520138A (en) 2021-06-15 2024-05-21 エルジー・ケム・リミテッド Pharmaceutical compositions comprising 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid
AR126164A1 (en) 2021-06-17 2023-09-27 Lg Chemical Ltd COMPOUND FORMULATION FOR ORAL DOSAGE COMPRISING 1-(3-CYANO-1-ISOPROPYL-INDOL-5-IL)PYRAZOLE-4-CARBOXYLIC ACID
TWI822151B (en) * 2021-07-02 2023-11-11 南韓商Ｌｇ化學股份有限公司 Method for preparing xanthine oxidase inhibitor
TWI870839B (en) * 2022-04-27 2025-01-21 大陸商杭州新元素藥業有限公司 Compounds for reducing uric acid
TW202342455A (en) * 2022-04-27 2023-11-01 大陸商江蘇新元素醫藥科技有限公司 Compounds for gout

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997027186A1 (en) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-pyrazol-3-yl-ethyl-4-indol-3-yl-piperidine used as medicine acting on the central nervous system
WO2007113647A1 (en) * 2006-04-04 2007-10-11 Pfizer Products Inc. Polymorphic forms of (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-methyl-1h-pyrazol-4υl)-1-oxo-2,6-dihydro-1h-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2477274C2 (en) * 2007-04-11 2013-03-10 Киссеи Фармасьютикал Ко., Лтд. Indole derivative and its use in therapeutic purposes
JP5330990B2 (en) * 2007-04-11 2013-10-30 キッセイ薬品工業株式会社 Nitrogen-containing heterocyclic compound and pharmaceutical composition containing the same
TWI423962B (en) * 2009-10-07 2014-01-21 Lg Life Sciences Ltd Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997027186A1 (en) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-pyrazol-3-yl-ethyl-4-indol-3-yl-piperidine used as medicine acting on the central nervous system
WO2007113647A1 (en) * 2006-04-04 2007-10-11 Pfizer Products Inc. Polymorphic forms of (2r,z)-2-amino-2-cyclohexyl-n-(5-(1-methyl-1h-pyrazol-4υl)-1-oxo-2,6-dihydro-1h-[1,2]diazepino[4,5,6-cd]indol-8-yl)acetamide

Also Published As

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

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