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Phenylalanine derivatives as inhibitors of the dipeptidilpeptidasa for the Treatment or prevention of Diabetes

机译:苯丙氨酸衍生物作为二肽二肽肽酶的抑制剂,用于治疗或预防糖尿病

摘要

This refers to phenylalanine derivatives which are inhibitors of the Enzyme dipeptidilpeptidasa - IV (known as "inhibitors of DP IV") and which are useful in the Treatment or prevention of diseases in which the dipeptidilpeptidasa IV Enzyme is involved, such as di ABETES and particularly Type 2 diabetes.It also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the Prevention or treatment of such diseases in which the Enzyme is involved dipeptidilpeptidasa - IV.Claim 1: a compound of Structural formula (1), in which X is CH2 CHF, and CF2, S; W is CH2 CHF, or CF2; R2 is selected from the group consisting of; Methyl, Ethyl, CH2 COOH, - ciclopropilo, Coome, cooet, conhme, conme2, CONH2, conhet, - ilcarbonilo pyrrolidin-3-yl conmech2ph, - 1, - 1 - ilcar azetidin Bonilo fluoroazetidin - 1 -, 2 - (4 - ilcarbonilo, ilcarbonilo,And (tetrazol [- 5 - il) amino] carbonyl; and R4 is selected from the group consisting of 4 - fluorofenilo, 2,4 - difluorofenilo, 3,4 - difluorofenilo, 2-chlorophenyl - fluorofenilo, 2, 3 (metolsulfonol phenyl) - 3 - (ethoxycarbonyl) phenyl carboxifenilo - 3, 3 - (Aminocarbonyl) phenyl, 3 - [(tert butylamino) carbonyl] phenyl [3 - (phenylamino) carbonyl] phenyl [3 - (2 - ilamino thiazole) carbonyl] phenyl3 - [(tetrazol - 5 - ilamino) carbonyl] phenyl [[3 - (trifluoromethyl) sulfonyl] amino] phenyl (tetrazol - 3 - 5 - il) phenyl 4-fluoro-3 - (tetrazol - 5 - il) phenyl 2-fluoro-5 - (tetrazol - 5 - phenyl (IL), 3 - 5 - oxo 4,5-dihydro - 1,2,4 - Oxadiazoles - 3 - il) phenyl 4-fluoro-3 - (5 - oxo - Oxadiazoles 4,5-dihydro - 1,2,4 - phenyl - 3 - il), 3 - (5 - oxo - 4.5 - d Ihidro - 1,3,4-oxadiazol-2 il phenyl) - 3 - (5 - oxo - 4,5 dihydro - 1h-1,2,4-triazole il, phenyl - 3 - 3 - (1,3),4 - phenyl - 2 - Oxadiazoles, 3 (IL) - 1,2,4-triazole - 3 - il) phenyl 3 - [5 - (trifluoromethyl) - 1,2,4-triazole il] - phenyl - 3, 3 - (5 - ethoxy - 3 - The 1,2,4-triazole - phenyl - 3 - pyridin), ILO 6 - fluoro - pyridin - 3 - 6 - metoxipiridin ILO, IL - 3 -, 6 -, oxo - 1.6 - dihidropiridin - ILO - 3, 1 - methyl - 4 - oxo - 1.6 - dihidropiridin - ILO - 3, 6 - 1 - ethyl - oxo - 1,6 Dihydro - i 5bromo pyridin - 3, 6 - 1 - methyl - 3 - oxo - 1.6 - dihidropiridin - ILO, imidazo [1,2-a] pyridin - 6-yl [1,2,,4] triazolo [4,3-a] pyridin - 6-yl, 3 - (trifluoromethyl) [1,2,4] triazolo [4,3-a] pyridin - 6-yl, 3 - oxo 2,3 dihydro [1,2,4] triazolo [4,3-a] pyridin - 6-yl, 2 - methyl - 3 - oxo - 2,3 dihydro [1,2,4] triazolo [4,3-a] pyridin - 6 - 4 - 6 - aminoquinazolin ILO, ILO, 2 - (Acetylamino) imidazo [1,2-a] pyridin - il - 6, 3 - aminoimidazo [1,2-a] pyridin-3 - 3 - 6 - ILO, carboxipirazolo [1,5-a] pyridin-3 ILO - 5 - 6 - 5 - bromo -, oxo - 1.6 - dihidropiridin - ilo [1,2, 3,4] triazolo [1,5-a] pyridin - 6-yl [1,2,4] triazolo [1,5-a] pyridin - 7 - ILO and pyrazolo [1,5-a] pyrimidin-5-yl.
机译:这是指苯丙氨酸衍生物,它们是酶Depteptidilpeptidasa IV的抑制剂(称为“ DP IV抑制剂”),可用于治疗或预防涉及Dipeptidilpeptidasa IV酶的疾病,例如di ABETES本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗与酶有关的疾病中的用途,所述疾病涉及酶二肽基二肽-Ⅳ。权利要求1:结构式为( 1),其中X为CH 2 CHF,CF 2为S; W是CH2 CHF或CF2; R 2选自:甲基,乙基,CH2 COOH,-环丙氯,库姆,库克,conhme,conme2,CONH2,conhet,-ilcarbonilo pyrrolidin-3-yl conmech2ph,-1,-1-ilcar azetidin Bonilo氟氮杂环丁烷-1-,2-(4- ilcarbonilo,ilcarbonilo和(tetrazol [-5-il)氨基]羰基;和R4选自4-氟芬尼洛,2,4-二氟芬尼洛,3,4-二氟芬尼洛,2-氯苯基-氟芬尼洛,2 3(甲磺酸苯基)-3-(乙氧羰基)苯基羧苯-3,3-(氨基羰基)苯基,3-[(叔丁基氨基)羰基]苯基[3-(苯基氨基)羰基]苯基[3-(2--氨基氨基噻唑) )羰基]苯基3-[((四唑-5-氨基)羰基]苯基[[3--(三氟甲基)磺酰基]氨基]苯基(四唑-3-5-il)苯基4-氟-3-(四唑-5-il )苯基2-氟-5-(四唑-5-苯基(IL),3-5-氧代4,5-二氢-1,2,4-恶二唑-3-il)苯基4-氟-3-(5 -羰基-恶二唑4,5-二氢-1,2,4-苯基-3-il),3-(5-羰基-4.5-d Ihidr o-1,3,4-恶二唑-2-基苯基)-3-(5-氧代-4,5二氢-1h-1,2,4-三唑基,苯基-3-3-(1,3), 4-苯基-2-恶二唑,3(IL)-1,2,4-三唑-3-il)苯基3-[5-(三氟甲基)-1,2,4-三唑il]-苯基-3,3 -(5-乙氧基-3-1,2,4-三唑-苯基-3-吡啶),国际劳工组织6-氟-吡啶-3-6-甲氧西丁定国际劳工组织,伊利诺伊州-3-,6-,氧代-1.6- dihidropiridin-ILO-3,1-甲基-4-氧代-1.6-dihidropiridin-ILO-3,6-1-乙基-氧代-1,6 Dihydro-i 5溴吡啶-3,6-1-甲基-3-氧代-1.6-dihidropiridin-ILO,咪唑并[1,2-a]吡啶-6-基[1,2,,4]三唑并[4,3-a]吡啶-6-基3-(三氟甲基)[1, 2,4]三唑并[4,3-a]吡啶-6-基,3-氧代2,3二氢[1,2,4]三唑并[4,3-a]吡啶-6-基,2-甲基- 3-羰基-2,3二氢[1,2,4]三唑[4,3-a]吡啶-6-4-6-氨基喹唑啉ILO,ILO,2-(乙酰氨基)咪唑[1,2-a]吡啶-il-6-3-氨基咪唑并[1,2-a]吡啶3-6-3-6-ILO,卡波比尔azolo [1,5-a]吡啶3-ILO-5-6-5-溴-,羰基-1.6-dihidropiridin-ilo [1,2,3,4] triazolo [1,5-a]吡啶-6- yl [1,2,4]三唑并[1,5-a]吡啶-7-ILO和吡唑并[1,5-a]嘧啶-5-基。

著录项

  • 公开/公告号AR042654A1

    专利类型

  • 公开/公告日2005-06-29

    原文格式PDF

  • 申请/专利权人 MERCK & CO INC.;

    申请/专利号AR2003P104780

  • 发明设计人

    申请日2003-12-22

  • 分类号C07D207/10;A61K31/40;A61K31/41;A61K31/4196;A61K31/4245;A61K31/426;A61K31/437;A61K31/4427;A61K31/47;A61K31/497;A61K31/519;A61P31/10;C07D207/08;C07D277/04;C07D401/10;C07D403/10;C07D413/10;C07D417/10;C07D471/04;C07D487/04;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:47

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