AR042654A1 - DERIVATIVES OF PHENYLALANINE AS INHIBITORS OF DIPEPTIDILPEPTIDASE FOR THE TREATMENT OR PREVENTION OF DIABETES - Google Patents

DERIVATIVES OF PHENYLALANINE AS INHIBITORS OF DIPEPTIDILPEPTIDASE FOR THE TREATMENT OR PREVENTION OF DIABETES

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Publication number
AR042654A1
AR042654A1 ARP030104780A AR042654A1 AR 042654 A1 AR042654 A1 AR 042654A1 AR P030104780 A ARP030104780 A AR P030104780A AR 042654 A1 AR042654 A1 AR 042654A1
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AR
Argentina
Prior art keywords
phenyl
pyridin
oxo
triazolo
dihydro
Prior art date
Application number
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Spanish (es)
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR042654A1 publication Critical patent/AR042654A1/en

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente se refiere a derivados de fenilalanina que son inhibidores de la enzima dipeptidilpeptidasa -IV (abreviadamente en inglés "inhibidores de DP-IV") y que son útiles en el tratamiento o prevención de enfermedades en las que esta implicada la enzima dipeptidilpeptidasa-IV, tal como la diabetes y particularmente la diabetes tipo 2. También se refiere a composiciones farmacéuticas que comprende estos compuestos y el uso de estos compuestos y composiciones en la prevención o tratamiento de dichas enfermedades en las que está implicada la enzima dipeptidilpeptidasa-IV. Reivindicación 1: Un compuesto de fórmula estructural (1) en la que X es CH2, S, CHF, o CF2; W es CH2, CHF, o CF2; R2 se selecciona del grupo constituido por; metilo, etilo, CH2-ciclopropilo, COOH, COOMe, COOEt, CONHMe, CONMe2, CONH2, CONHEt, CONMeCH2Ph, pirrolidin-1-ilcarbonilo, azetidin-1-ilcarbonilo, 2-fluoroazetidin-1-ilcarbonilo, morfolin-4-ilcarbonilo, y [(tetrazol-5-il)amino]carbonilo; y R4 se selecciona del grupo constituido por 4-fluorofenilo, 2,4-difluorofenilo, 3,4-difluorofenilo, 2-clorofenilo, 2-fluorofenilo, 3-(metolsulfonol)fenilo, 3-(etoxicarbonil)fenilo, 3-carboxifenilo, 3-(aminocarbonil)fenilo, 3-[(terc-butilamino)carbonil]fenilo, , 3-[(fenilamino)carbonil]fenilo, 3-[(tiazol-2-ilamino)carbonil]fenilo, 3-[(tetrazol-5-ilamino)carbonil]fenilo, 3-[[(trifluorometil)sulfonil]amino]fenilo, 3-(tetrazol-5-il)fenilo, 4-fluoro-3-(tetrazol-5-il)fenilo, 2-fluoro-5-(tetrazol-5-il)fenilo, 3-(5-oxo-4,5-dihidro-1,2,4-oxadiazol-3-il)fenilo, 4-fluoro-3-(5-oxo-4,5-dihidro-1,2,4-oxadiazol-3-il)fenilo, 3-(5-oxo-4,5-dihidro-1,3,4-oxadiazol-2-il)fenilo, 3-(5-oxo-4,5-dihidro-1H-1,2,4-triazol-3-il)fenilo, 3-(1,3,4-oxadiazol-2-il)fenilo, 3-(1,2,4-triazol-3-il)fenilo, 3-[5-(trifluorometil)-1,2,4-triazol-3-il]fenilo, 3-(5-etoxi-1,2,4-triazol-3-il)fenilo, piridin-3-ilo, 6-fluoro-piridin-3-ilo, 6-metoxipiridin-3-il, 6-oxo-1,6-dihidropiridin-3-ilo, 1-metil-6-oxo-1,6-dihidropiridin-3-ilo, 1-etil-6-oxo-1,6-dihidropiridin-3-ilo, 5bromo-1-metil-6-oxo-1,6-dihidropiridin-3-ilo, imidazo[1,2-a]piridin-6-ilo, [1,2,4]triazolo[4,3-a]piridin-6-ilo, 3-(trifluorometil)[1,2,4]triazolo[4,3-a]piridin-6-ilo, 3-oxo-2,3-dihidro[1,2,4]triazolo[4,3-a]piridin-6-ilo, 2-metil-3-oxo-2,3-dihidro[1,2,4]triazolo[4,3-a]piridin-6-ilo, 4-aminoquinazolin-6-ilo, 2-(acetilamino)imidazo[1,2-a]piridin-6-il, 3-aminoimidazo[1,2-a]piridin-6-ilo, 3-carboxipirazolo[1,5-a]piridin-5-ilo, 5-bromo-6-oxo-1,6-dihidropiridin-3-ilo, [1,2,4]triazolo[1,5-a]piridin-6-ilo, [1,2,4]triazolo[1,5-a]piridin-7-ilo, y pirazolo[1,5-a]pirimidin-5-il.This refers to phenylalanine derivatives that are inhibitors of the enzyme dipeptidylpeptidase-IV (abbreviated in English "DP-IV inhibitors") and that are useful in the treatment or prevention of diseases in which the enzyme dipeptidylpeptidase-IV is involved , such as diabetes and particularly type 2 diabetes. It also refers to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of said diseases in which the enzyme dipeptidylpeptidase-IV is involved. Claim 1: A compound of structural formula (1) wherein X is CH2, S, CHF, or CF2; W is CH2, CHF, or CF2; R2 is selected from the group consisting of; methyl, ethyl, CH2-cyclopropyl, COOH, COOMe, COOEt, CONHMe, CONMe2, CONH2, CONHEt, CONMeCH2Ph, pyrrolidin-1-ylcarbonyl, azetidin-1-ylcarbonyl, 2-fluoroazetidin-1-ylcarbonyl, morpholin-4-yl-carbonyl and [(tetrazol-5-yl) amino] carbonyl; and R4 is selected from the group consisting of 4-fluorophenyl, 2,4-difluorophenyl, 3,4-difluorophenyl, 2-chlorophenyl, 2-fluorophenyl, 3- (metolsulfonol) phenyl, 3- (ethoxycarbonyl) phenyl, 3-carboxyphenyl, 3- (aminocarbonyl) phenyl, 3 - [(tert-butylamino) carbonyl] phenyl,, 3 - [(phenylamino) carbonyl] phenyl, 3 - [(thiazol-2-ylamino) carbonyl] phenyl, 3 - [(tetrazol- 5-ylamino) carbonyl] phenyl, 3 - [[(trifluoromethyl) sulfonyl] amino] phenyl, 3- (tetrazol-5-yl) phenyl, 4-fluoro-3- (tetrazol-5-yl) phenyl, 2-fluoro -5- (tetrazol-5-yl) phenyl, 3- (5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl) phenyl, 4-fluoro-3- (5-oxo- 4,5-dihydro-1,2,4-oxadiazol-3-yl) phenyl, 3- (5-oxo-4,5-dihydro-1,3,4-oxadiazol-2-yl) phenyl, 3- ( 5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl) phenyl, 3- (1,3,4-oxadiazol-2-yl) phenyl, 3- (1,2, 4-triazol-3-yl) phenyl, 3- [5- (trifluoromethyl) -1,2,4-triazol-3-yl] phenyl, 3- (5-ethoxy-1,2,4-triazol-3- il) phenyl, pyridin-3-yl, 6-fluoro-pyridin-3-yl, 6-methoxypyridin-3-yl, 6-oxo-1,6-dihydropyridin-3-yl, 1-methyl-6-oxo- 1,6-dihydropyridin-3-yl, 1-ethyl-6-oxo-1,6-dihydropyridin-3-yl, 5-bromo-1-methyl-6-oxo-1,6-dihydropyridin-3-yl, imidazo [1,2-a] pyridin-6- ilo, [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-yl, 4-aminoquinazolin-6-yl, 2- (acetylamino) imidazo [1,2-a] pyridin-6-yl, 3-aminoimidazo [1,2-a] pyridin-6-yl, 3-carboxypyrazolo [1,5-a] pyridin-5-yl, 5-bromo-6-oxo-1,6-dihydropyridin-3-yl, [1,2,4] triazolo [1 , 5-a] pyridin-6-yl, [1,2,4] triazolo [1,5-a] pyridin-7-yl, and pyrazolo [1,5-a] pyrimidin-5-yl.

ARP030104780 2003-06-19 2003-12-22 DERIVATIVES OF PHENYLALANINE AS INHIBITORS OF DIPEPTIDILPEPTIDASE FOR THE TREATMENT OR PREVENTION OF DIABETES AR042654A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US50123203P 2003-06-19 2003-06-19

Publications (1)

Publication Number Publication Date
AR042654A1 true AR042654A1 (en) 2005-06-29

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030104780 AR042654A1 (en) 2003-06-19 2003-12-22 DERIVATIVES OF PHENYLALANINE AS INHIBITORS OF DIPEPTIDILPEPTIDASE FOR THE TREATMENT OR PREVENTION OF DIABETES

Country Status (4)

Country Link
AR (1) AR042654A1 (en)
CL (1) CL2003002751A1 (en)
PE (1) PE20041058A1 (en)
TW (1) TW200500338A (en)

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Publication number Publication date
TW200500338A (en) 2005-01-01
PE20041058A1 (en) 2005-02-07
CL2003002751A1 (en) 2005-04-08

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