TWI548630B - １－（３－氰基－１－異丙基－吲哚－５－基）吡唑－４－羧酸結晶型及其製造方法 - Google Patents

１－（３－氰基－１－異丙基－吲哚－５－基）吡唑－４－羧酸結晶型及其製造方法 Download PDF

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TWI548630B
TWI548630B TW101111308A TW101111308A TWI548630B TW I548630 B TWI548630 B TW I548630B TW 101111308 A TW101111308 A TW 101111308A TW 101111308 A TW101111308 A TW 101111308A TW I548630 B TWI548630 B TW I548630B
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TW201245182A (en
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尹精敏
朴基淑
尹胄鏞
李周泳
金根泰
鄭哲圭
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Ｌｇ生命科學有限公司
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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)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW101111308A 2011-04-06 2012-03-30 １－（３－氰基－１－異丙基－吲哚－５－基）吡唑－４－羧酸結晶型及其製造方法 TWI548630B (zh)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
TW201245182A TW201245182A (en) 2012-11-16
TWI548630B true TWI548630B (zh) 2016-09-11

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TW101111308A TWI548630B (zh) 2011-04-06 2012-03-30 １－（３－氰基－１－異丙基－吲哚－５－基）吡唑－４－羧酸結晶型及其製造方法

Country Status (5)

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JP (1) JP6008937B2 (ja)
KR (1) KR101424013B1 (ja)
CN (1) CN103459381B (ja)
TW (1) TWI548630B (ja)
WO (1) WO2012138147A2 (ja)

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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
US20190374515A1 (en) * 2016-11-28 2019-12-12 Teijin Pharma Limited Therapeutic drug or prophylactic drug for diabetic nephropathy
EP4218755A4 (en) * 2020-11-04 2024-03-27 Lg Chem, Ltd. METHOD FOR PRODUCING CRYSTALLINE PARTICLES OF 1-(3-CYANO-1-ISOPROPYL-INDOLE-5-YL)PYRAZOLE-4-CARBONIC ACID AND PHARMACEUTICAL COMPOSITION THEREFROM
JP2023551524A (ja) 2020-12-01 2023-12-08 エルジー・ケム・リミテッド 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－カルボン酸を含む経口用製剤、およびその製造方法
JP2023551712A (ja) 2020-12-01 2023-12-12 エルジー・ケム・リミテッド 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－カルボン酸を含む安定した経口用製剤
US20240216331A1 (en) * 2021-04-16 2024-07-04 Lg Chem, Ltd. Oral formulation containing 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid
CN117255785A (zh) * 2021-04-27 2023-12-19 株式会社Lg化学 用于合成黄嘌呤氧化酶抑制剂的中间体的制备方法
CA3218011A1 (en) * 2021-04-29 2022-11-10 Jiangsu Atom Bioscience And Pharmaceutical Co., Ltd. A xanthine oxidase inhibitor
CN117425477A (zh) * 2021-06-15 2024-01-19 株式会社Lg化学 包含1-(3-氰基-1-异丙基-吲哚-5-基)吡唑-4-甲酸的药物组合物
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
WO2023208108A1 (zh) * 2022-04-27 2023-11-02 江苏新元素医药科技有限公司 可用于降尿酸的化合物
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 (3)

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WO1997027186A1 (de) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-(pyrazol-3-yl-ethyl)-4-(indol-3-yl)-piperidine als das zentralnervensystem beeinflussende mittel
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
WO2011043568A2 (en) * 2009-10-07 2011-04-14 Lg Life Sciences Ltd. Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same

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ES2431815T3 (es) * 2007-04-11 2013-11-28 Kissei Pharmaceutical Co., Ltd. Derivado de (aza)indol y uso del mismo para fines médicos
WO2008126901A1 (ja) * 2007-04-11 2008-10-23 Kissei Pharmaceutical Co., Ltd. 含窒素複素環化合物およびそれを含有する医薬組成物

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997027186A1 (de) * 1996-01-25 1997-07-31 MERCK Patent Gesellschaft mit beschränkter Haftung 1-(pyrazol-3-yl-ethyl)-4-(indol-3-yl)-piperidine als das zentralnervensystem beeinflussende mittel
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
WO2011043568A2 (en) * 2009-10-07 2011-04-14 Lg Life Sciences Ltd. Novel compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same

Also Published As

Publication number Publication date
WO2012138147A3 (en) 2012-11-29
KR101424013B1 (ko) 2014-08-18
KR20120114174A (ko) 2012-10-16
CN103459381B (zh) 2015-12-09
JP2014510133A (ja) 2014-04-24
CN103459381A (zh) 2013-12-18
JP6008937B2 (ja) 2016-10-19
TW201245182A (en) 2012-11-16
WO2012138147A2 (en) 2012-10-11

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