CN102516184B - 包含β-氨基的DPP-IV抑制剂及其制备方法以及用于预防和治疗糖尿病或肥胖症的含有所述抑制剂的药物组合物 - Google Patents

包含β-氨基的DPP-IV抑制剂及其制备方法以及用于预防和治疗糖尿病或肥胖症的含有所述抑制剂的药物组合物 Download PDF

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Publication number
CN102516184B
CN102516184B CN201110329468.1A CN201110329468A CN102516184B CN 102516184 B CN102516184 B CN 102516184B CN 201110329468 A CN201110329468 A CN 201110329468A CN 102516184 B CN102516184 B CN 102516184B
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China
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compound
formula
dpp
amino
acid
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CN102516184A (zh
Inventor
金兴载
郭祐宁
申昌烈
金夏东
闵种弼
朴间珍
李在荣
崔圣贤
尹泰铉
金海鲜
张志勉
金美庆
孙文虎
金舜会
刘武嬉
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Dong-A ST Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
    • C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201110329468.1A 2007-04-19 2008-04-18 包含β-氨基的DPP-IV抑制剂及其制备方法以及用于预防和治疗糖尿病或肥胖症的含有所述抑制剂的药物组合物 Active CN102516184B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2007-0038462 2007-04-19
KR20070038462 2007-04-19

Related Parent Applications (1)

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CN2008800126267A Division CN101663282B (zh) 2007-04-19 2008-04-18 包含β-氨基的DPP-Ⅳ抑制剂及其制备方法以及用于预防和治疗糖尿病或肥胖症的含有所述抑制剂的药物组合物

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CN102516184A CN102516184A (zh) 2012-06-27
CN102516184B true CN102516184B (zh) 2015-03-25

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CN2008800126267A Active CN101663282B (zh) 2007-04-19 2008-04-18 包含β-氨基的DPP-Ⅳ抑制剂及其制备方法以及用于预防和治疗糖尿病或肥胖症的含有所述抑制剂的药物组合物

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Country Status (15)

Country Link
US (1) US8030315B2 (cg-RX-API-DMAC7.html)
EP (1) EP2142519B1 (cg-RX-API-DMAC7.html)
JP (1) JP5148686B2 (cg-RX-API-DMAC7.html)
KR (1) KR101007497B1 (cg-RX-API-DMAC7.html)
CN (2) CN102516184B (cg-RX-API-DMAC7.html)
AU (1) AU2008241692B2 (cg-RX-API-DMAC7.html)
BR (1) BRPI0810246B1 (cg-RX-API-DMAC7.html)
CA (1) CA2683696C (cg-RX-API-DMAC7.html)
ES (1) ES2526338T3 (cg-RX-API-DMAC7.html)
IL (1) IL201524A (cg-RX-API-DMAC7.html)
MX (1) MX2009011276A (cg-RX-API-DMAC7.html)
NZ (1) NZ580701A (cg-RX-API-DMAC7.html)
PT (1) PT2142519E (cg-RX-API-DMAC7.html)
RU (1) RU2419615C1 (cg-RX-API-DMAC7.html)
WO (1) WO2008130151A1 (cg-RX-API-DMAC7.html)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101054911B1 (ko) * 2008-10-17 2011-08-05 동아제약주식회사 디펩티딜펩티다아제-ⅳ의 활성을 저해하는 화합물 및 다른 항당뇨 또는 항비만 약물을 유효성분으로 함유하는 당뇨 또는 비만의 예방 및 치료용 약학적 조성물
JP5475864B2 (ja) * 2009-03-30 2014-04-16 ドン ア ファーマシューティカル カンパニー リミテッド ジペプチジルペプチダーゼ−ｉｖ阻害剤及び中間体の改良された製造方法
SG174974A1 (en) 2009-03-30 2011-11-28 Dong A Pharm Co Ltd Improved method for preparing dipeptidyl peptidase-iv inhibitor and intermediate
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
KR20110107287A (ko) * 2010-03-24 2011-09-30 동아제약주식회사 비알콜성 지방간 질환의 예방 및 치료용 약학적 조성물
KR101180174B1 (ko) 2010-04-23 2012-09-05 동아제약주식회사 신규한 벤즈아미드 유도체
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
KR101290029B1 (ko) 2011-01-20 2013-07-30 에스티팜 주식회사 시타글립틴의 중간체 제조방법
CN102321014A (zh) * 2011-05-27 2012-01-18 沈阳亿灵医药科技有限公司 新型双苯基吡啶类衍生物
US20140336196A1 (en) * 2011-05-27 2014-11-13 Merck Sharp & Dohme Corp. Phosphoric acid salts of sitagliptin
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (en) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
CN105142621A (zh) 2012-10-24 2015-12-09 国家健康科学研究所 用于预防或治疗糖尿病和促进β-细胞存活的TPL2激酶抑制剂
CN105555275B (zh) * 2013-06-26 2021-04-20 东亚St株式会社 含有dpp-iv抑制剂的用于预防和治疗肾脏疾病的组合物
EP3273981B1 (en) 2015-03-24 2020-04-29 INSERM - Institut National de la Santé et de la Recherche Médicale Method and pharmaceutical composition for use in the treatment of diabetes
KR101709127B1 (ko) 2015-06-16 2017-02-22 경동제약 주식회사 Dpp-iv 억제제의 제조를 위한 신규 중간체, 이의 제조방법 및 이를 이용한 dpp-iv 억제제의 제조방법
CN107382757A (zh) * 2017-08-11 2017-11-24 苏州信恩医药科技有限公司 不对称烯丙基取代反应在依格列汀中间体合成中的应用
CN107417554A (zh) * 2017-08-15 2017-12-01 苏州信恩医药科技有限公司 一种依格列汀中间体的合成方法
KR20220165346A (ko) 2021-06-08 2022-12-15 동아에스티 주식회사 에보글립틴의 안정성이 개선된 제제

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002088070A (ja) * 2000-09-18 2002-03-27 Mitsubishi Rayon Co Ltd 新規ピペラジノン誘導体およびその製造方法
WO2005056003A1 (en) * 2003-12-09 2005-06-23 Santhera Pharmaceuticals (Schweiz) Gmbh Dpp-iv inhibitors
WO2005056541A1 (ja) * 2003-12-11 2005-06-23 Mitsubishi Pharma Corporation α-アミノ酸誘導体及びその医薬用途
WO2005095343A1 (en) * 2004-03-05 2005-10-13 Santhera Pharmaceuticals (Schweiz) Gmbh Dpp-iv inhibitors
WO2005121131A1 (en) * 2004-06-08 2005-12-22 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
WO2005123685A1 (en) * 2004-06-16 2005-12-29 Astrazeneca Ab Tetrahydroquinolones and aza-analogues thereof for use as dpp-iv inhibitors in the treatement of diabetes

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1187342C (zh) * 2000-05-25 2005-02-02 弗·哈夫曼-拉罗切有限公司 取代的1－氨基烷基内酰胺化合物及其作为毒蕈碱受体拮抗剂的用途
DE60114413T2 (de) * 2000-05-25 2006-07-27 F. Hoffmann-La Roche Ag Substituierte 1-aminoalkyl-lactame und deren verwendung als muscarinrezeptor-antagonisten
WO2004032836A2 (en) * 2002-10-07 2004-04-22 Merck & Co., Inc. Antidiabetic beta-amino heterocylcic dipeptidyl peptidase inhibitors
HRP20050343A2 (en) 2002-10-18 2007-03-31 Merck & Co. Inc. Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CN1882551A (zh) 2003-07-31 2006-12-20 麦克公司 用作用于治疗或预防糖尿病的二肽基肽酶－iv酶抑制剂的六氢二氮杂吖庚因酮
WO2006104997A2 (en) 2005-03-29 2006-10-05 Merck & Co., Inc. Tartaric acid salts of a dipeptidyl peptidase-iv inhibitor
JP2008031064A (ja) * 2006-07-27 2008-02-14 Astellas Pharma Inc ジアシルピペラジン誘導体

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002088070A (ja) * 2000-09-18 2002-03-27 Mitsubishi Rayon Co Ltd 新規ピペラジノン誘導体およびその製造方法
WO2005056003A1 (en) * 2003-12-09 2005-06-23 Santhera Pharmaceuticals (Schweiz) Gmbh Dpp-iv inhibitors
WO2005056541A1 (ja) * 2003-12-11 2005-06-23 Mitsubishi Pharma Corporation α-アミノ酸誘導体及びその医薬用途
WO2005095343A1 (en) * 2004-03-05 2005-10-13 Santhera Pharmaceuticals (Schweiz) Gmbh Dpp-iv inhibitors
WO2005121131A1 (en) * 2004-06-08 2005-12-22 Santhera Pharmaceuticals (Schweiz) Ag Dpp-iv inhibitors
WO2005123685A1 (en) * 2004-06-16 2005-12-29 Astrazeneca Ab Tetrahydroquinolones and aza-analogues thereof for use as dpp-iv inhibitors in the treatement of diabetes

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Medicinal Chemistry Letters》.2006,(第17期),49-52. *
Tesfaye Biftu.(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.《Bioorganic &amp *

Also Published As

Publication number Publication date
JP5148686B2 (ja) 2013-02-20
BRPI0810246A2 (pt) 2015-08-18
IL201524A (en) 2014-09-30
BRPI0810246B1 (pt) 2021-11-30
WO2008130151A1 (en) 2008-10-30
AU2008241692A1 (en) 2008-10-30
CA2683696C (en) 2012-05-22
IL201524A0 (en) 2010-05-31
EP2142519B1 (en) 2014-09-24
US8030315B2 (en) 2011-10-04
EP2142519A4 (en) 2011-07-13
RU2419615C1 (ru) 2011-05-27
AU2008241692B2 (en) 2011-02-10
HK1138272A1 (en) 2010-08-20
CN102516184A (zh) 2012-06-27
CN101663282A (zh) 2010-03-03
NZ580701A (en) 2011-07-29
KR101007497B1 (ko) 2011-01-12
HK1172613A1 (en) 2013-04-26
PT2142519E (pt) 2014-12-11
JP2011500508A (ja) 2011-01-06
CA2683696A1 (en) 2008-10-30
KR20080094604A (ko) 2008-10-23
US20100120790A1 (en) 2010-05-13
MX2009011276A (es) 2010-01-15
EP2142519A1 (en) 2010-01-13
ES2526338T3 (es) 2015-01-09
CN101663282B (zh) 2012-02-15

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