JP5976322B2 - テトラヒドロ−イミダゾ[1,5−a]ピラジン誘導体塩、その製造方法及び医薬用途 - Google Patents

テトラヒドロ−イミダゾ[1,5−a]ピラジン誘導体塩、その製造方法及び医薬用途 Download PDF

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Publication number
JP5976322B2
JP5976322B2 JP2011552307A JP2011552307A JP5976322B2 JP 5976322 B2 JP5976322 B2 JP 5976322B2 JP 2011552307 A JP2011552307 A JP 2011552307A JP 2011552307 A JP2011552307 A JP 2011552307A JP 5976322 B2 JP5976322 B2 JP 5976322B2
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salt
acid
imidazo
tetrahydro
trifluorophenyl
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Japanese (ja)
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JP2012519193A (ja
JP2012519193A5 (https=
Inventor
タン・ペンチョ
スン・ピャオヤン
ヤン・ファンロン
リャン・ジンドン
シェン・グァンユァン
ワン・ヤン
ファン・ジャン
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2011552307A 2009-03-05 2010-03-03 テトラヒドロ−イミダゾ[1,5−a]ピラジン誘導体塩、その製造方法及び医薬用途 Expired - Fee Related JP5976322B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN200910047075A CN101824036A (zh) 2009-03-05 2009-03-05 四氢咪唑并[1,5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用
CN200910047075.4 2009-03-05
PCT/CN2010/000257 WO2010099698A1 (zh) 2009-03-05 2010-03-03 四氢咪唑并[1,5-a]吡嗪衍生物的盐,其制备方法及其在医药上的应用

Publications (3)

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JP2012519193A JP2012519193A (ja) 2012-08-23
JP2012519193A5 JP2012519193A5 (https=) 2016-07-21
JP5976322B2 true JP5976322B2 (ja) 2016-08-23

Family

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JP2011552307A Expired - Fee Related JP5976322B2 (ja) 2009-03-05 2010-03-03 テトラヒドロ−イミダゾ[1,5−a]ピラジン誘導体塩、その製造方法及び医薬用途

Country Status (12)

Country Link
US (1) US8518946B2 (https=)
EP (1) EP2404921B1 (https=)
JP (1) JP5976322B2 (https=)
KR (1) KR101731602B1 (https=)
CN (2) CN101824036A (https=)
AU (1) AU2010220722B2 (https=)
CA (1) CA2753862C (https=)
MX (1) MX2011009190A (https=)
RU (1) RU2523543C2 (https=)
UA (1) UA106225C2 (https=)
WO (1) WO2010099698A1 (https=)
ZA (1) ZA201107284B (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101899048B (zh) * 2009-05-27 2013-04-17 上海恒瑞医药有限公司 (R)-7-[3-氨基-4-(2,4,5-三氟-苯基)-丁酰]-3-三氟甲基-5,6,7,8-四氢-咪唑并[1,5-a]吡嗪-1-羧酸甲酯的盐
CN103724352B (zh) * 2012-10-16 2017-11-28 江苏盛迪医药有限公司 一种dpp‑iv抑制剂的中间体、其制备方法和通过其制备dpp‑iv抑制剂的方法
CN103664962A (zh) * 2013-12-20 2014-03-26 南京华威医药科技开发有限公司 哌嗪类衍生物
CN103910734B (zh) * 2014-03-28 2016-01-13 南京华威医药科技开发有限公司 一种具有哌嗪结构的dpp-4抑制剂
US10189841B2 (en) 2015-11-20 2019-01-29 Forma Therapeutics, Inc. Purinones as ubiquitin-specific protease 1 inhibitors
US11098058B2 (en) 2017-07-14 2021-08-24 Genentech, Inc. Bicyclic ketone compounds and methods of use thereof
SG11202002877RA (en) 2017-10-31 2020-04-29 Hoffmann La Roche Bicyclic sulfones and sulfoxides and methods of use thereof
JP7553450B2 (ja) * 2018-12-28 2024-09-18 フォーマ セラピューティクス,インコーポレイテッド ユビキチン特異的プロテアーゼ1を阻害するための組成物
CN113620957B (zh) * 2020-05-08 2022-04-19 盛世泰科生物医药技术(苏州)有限公司 一种胺甲基吡嗪类化合物的制备方法
CN113773323B (zh) * 2020-06-10 2023-05-12 江苏恒瑞医药股份有限公司 3r-氨基取代丁酰胺衍生物的制备方法
CN113880825B (zh) * 2020-07-01 2025-03-14 浙江海正药业股份有限公司 四氢异喹啉类衍生物的盐、其制备方法及其医药应用
JP2024504328A (ja) * 2021-01-21 2024-01-31 ザ スクリプス リサーチ インスティテュート 肺疾患の治療のための肺胞2型細胞増殖の小分子調節因子
CN114057751B (zh) * 2022-01-17 2022-04-12 盛世泰科生物医药技术(苏州)有限公司 一种dpp-iv抑制剂及其关键中间体的制备方法
CN115583935A (zh) * 2022-11-03 2023-01-10 浙江工业大学 一种4-(2,4,5-三氟苯基)-3-氧丁酸酯的制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
FR2780974B1 (fr) * 1998-07-08 2001-09-28 Sod Conseils Rech Applic Utilisation de derives d'imidazopyrazines pour preparer un medicament destine a traiter les pathologies qui resultent de la formation de la proteine g heterotrimetrique
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
UA74912C2 (en) * 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
CN101468988A (zh) * 2007-12-26 2009-07-01 上海恒瑞医药有限公司 哌嗪类衍生物,其制备方法及其在医药上的应用

Also Published As

Publication number Publication date
KR101731602B1 (ko) 2017-04-28
CA2753862A1 (en) 2010-09-10
JP2012519193A (ja) 2012-08-23
WO2010099698A1 (zh) 2010-09-10
CN101824036A (zh) 2010-09-08
US20120065209A1 (en) 2012-03-15
CA2753862C (en) 2017-05-23
EP2404921A1 (en) 2012-01-11
HK1154574A1 (en) 2012-04-27
MX2011009190A (es) 2011-09-26
EP2404921A4 (en) 2012-08-15
CN102159578B (zh) 2013-04-10
ZA201107284B (en) 2012-12-27
AU2010220722B2 (en) 2015-05-07
AU2010220722A1 (en) 2011-10-27
UA106225C2 (ru) 2014-08-11
RU2011137858A (ru) 2013-04-10
KR20110132561A (ko) 2011-12-08
CN102159578A (zh) 2011-08-17
EP2404921B1 (en) 2017-11-22
RU2523543C2 (ru) 2014-07-20
AU2010220722A2 (en) 2011-11-03
US8518946B2 (en) 2013-08-27

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