KR101424013B1 - 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정형과 그의 제조방법 - Google Patents

1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정형과 그의 제조방법 Download PDF

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KR101424013B1
KR101424013B1 KR1020120035349A KR20120035349A KR101424013B1 KR 101424013 B1 KR101424013 B1 KR 101424013B1 KR 1020120035349 A KR1020120035349 A KR 1020120035349A KR 20120035349 A KR20120035349 A KR 20120035349A KR 101424013 B1 KR101424013 B1 KR 101424013B1
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윤정민
박기숙
윤주용
이주영
김근태
정철규
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주식회사 엘지생명과학
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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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (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)
KR1020120035349A 2011-04-06 2012-04-05 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정형과 그의 제조방법 KR101424013B1 (ko)

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KR20110031490 2011-04-06
KR1020110031490 2011-04-06

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KR20120114174A KR20120114174A (ko) 2012-10-16
KR101424013B1 true KR101424013B1 (ko) 2014-08-18

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

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220060488A (ko) 2020-11-04 2022-05-11 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정성 입자의 제조방법 및 이를 포함하는 약학적 조성물
KR20220077091A (ko) 2020-12-01 2022-06-08 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 안정한 경구용 제제
KR20220077092A (ko) 2020-12-01 2022-06-08 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제, 및 그의 제조방법
WO2022220636A1 (ko) 2021-04-16 2022-10-20 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
WO2022265382A1 (ko) 2021-06-15 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 약학적 조성물
WO2022265442A1 (ko) 2021-06-17 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
WO2023277660A1 (ko) * 2021-07-02 2023-01-05 주식회사 엘지화학 잔틴 옥시다아제 저해제의 제조 방법

Families Citing this family (7)

* Cited by examiner, † Cited by third party
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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
RU2735538C1 (ru) * 2016-11-28 2020-11-03 Тейдзин Фарма Лимитед Терапевтическое лекарственное средство или профилактическое лекарственное средство от диабетической нефропатии
KR20220147532A (ko) * 2021-04-27 2022-11-03 주식회사 엘지화학 잔틴 옥시다아제 저해제 합성을 위한 중간체의 제조 방법
KR20240005050A (ko) * 2021-04-29 2024-01-11 쟝쑤 애텀 바이오사이언스 앤드 파머수티컬 컴퍼니 리미티드 크산틴 옥시다아제 억제제
WO2023208103A1 (zh) * 2022-04-27 2023-11-02 江苏新元素医药科技有限公司 可用于痛风的化合物
TW202342456A (zh) * 2022-04-27 2023-11-01 大陸商江蘇新元素醫藥科技有限公司 可用於降尿酸的化合物

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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

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PL2133332T3 (pl) * 2007-04-11 2014-02-28 Kissei Pharmaceutical Pochodna aza(indolu) i jej zastosowanie do celów medycznych
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
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 (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

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220060488A (ko) 2020-11-04 2022-05-11 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정성 입자의 제조방법 및 이를 포함하는 약학적 조성물
WO2022098057A1 (ko) 2020-11-04 2022-05-12 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산의 결정성 입자의 제조방법 및 이를 포함하는 약학적 조성물
KR20220077091A (ko) 2020-12-01 2022-06-08 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 안정한 경구용 제제
KR20220077092A (ko) 2020-12-01 2022-06-08 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제, 및 그의 제조방법
WO2022119269A1 (ko) 2020-12-01 2022-06-09 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 안정한 경구용 제제
WO2022119270A1 (ko) 2020-12-01 2022-06-09 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제, 및 그의 제조방법
WO2022220636A1 (ko) 2021-04-16 2022-10-20 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
KR20220143593A (ko) 2021-04-16 2022-10-25 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
WO2022265382A1 (ko) 2021-06-15 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 약학적 조성물
WO2022265378A1 (ko) 2021-06-15 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 약학적 조성물
KR20220168172A (ko) 2021-06-15 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 약학적 조성물
KR20220168173A (ko) 2021-06-15 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 약학적 조성물
WO2022265442A1 (ko) 2021-06-17 2022-12-22 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
KR20220168999A (ko) 2021-06-17 2022-12-26 주식회사 엘지화학 1-(3-시아노-1-아이소프로필-인돌-5-일)피라졸-4-카르복실산을 포함하는 경구용 제제
WO2023277660A1 (ko) * 2021-07-02 2023-01-05 주식회사 엘지화학 잔틴 옥시다아제 저해제의 제조 방법

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WO2012138147A3 (en) 2012-11-29
JP6008937B2 (ja) 2016-10-19
CN103459381A (zh) 2013-12-18
JP2014510133A (ja) 2014-04-24
TWI548630B (zh) 2016-09-11
TW201245182A (en) 2012-11-16
CN103459381B (zh) 2015-12-09
KR20120114174A (ko) 2012-10-16
WO2012138147A2 (en) 2012-10-11

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