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US 7,407,977 B2Granted
Substituted N-acyl-2-aminothiazoles
AssigneeHoffman-La Roche Inc.
InventorsJianping Cai, Adrian Wai-Hing, Fariborz Firooznia, Kevin Richard Guertin, Lida Qi
Life of this patent
Estimating the term…
Abstract
There are presented compounds of the formula or a pharmaceutically acceptable salt thereof, which are useful in the treatment of diabetes, diabetic retinopathy, asthma and diarrhea.
Claims9
A compound of the formula
- or a pharmaceutically acceptable salt thereof, wherein
- X is —CH2—, —CH2CH2—, —(CH2)3— and O(CH2)—;
- R is a 5- or 6- membered saturated or unsaturated carbocyclic or heterocyclic ring which optionally may contain one or more hetero atoms and said rings being optionally substituted with one or more substituents selected from the group consisting of halogen, lower alkyl, acetamidomethyl, alkoxycarbonyl amidomethyl, a nitrile group, a sulfonamido group, alkylsulfonyl, alkoxy, benzyl, benzoyl, arylsulfonyl and acyl which benzyl, benzoyl or arylsulfonyl is optionally substituted by halogen, trihalo lower alkyl, lower alkyl, alkoxy, alkylsulfonyl or cyano;
- and
- R1 is selected from the group consisting of hydrogen, halogen, lower alkyl, alkoxy or a nitrile group.
2 more elements
A compound of the formula
- or the pharmaceutically acceptable salts thereof
- wherein R is phenyl or a heterocyclic ring selected from the group consisting of thienyl, pyridinyl, pyrazolyl, imidazolyl, furyl or piperidinyl, which phenyl or heterocyclic ring is optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, hydroxy, nitrile, lower-alkyl, sulfonamido, lower-alkyl-sulfonyl, lower-alkoxy-carbonyl, lower-alkoxy-C(O)—NH—CH2—, benzyl which is optionally substituted with CF3, benzoyl which is optionally substituted with CF3, or phenylsulfonyl
- which is optionally substituted with CF3
- X is —CH2—, —CH2CH2CH2—, —(CH2)3— and O(CH2)—;
- and
- R1 is selected from the group consisting of hydrogen, halogen, lower alkyl, alkoxy or a nitrile group.
3 more elements
A pharmaceutical composition comprising a compound of the formula
- or a pharmaceutically acceptable salt thereof, wherein
- X is —CH2—, —CH2CH2—, —(CH2)3— and O(CH2)—
- R is a 5- or 6-membered saturated or unsaturated carbocyclic or heterocyclic ring which optionally may contain one or more hetero atoms and said rings being optionally substituted with one or more substituents selected from the group consisting of halogen, hydroxy, lower alkyl, acetamidomethyl, alkoxycarbonyl amidomethyl, a nitrile group, a sulfonamido group, alkylsulfonyl, alkoxy, benzyl, benzoyl, arylsulfonyl and acyl which benzyl, benzoyl, or arylsulfonyl is optionally substituted by halogen, trihalo lower alkyl, lower alkyl, alkoxy, alkylsulfonyl or cyano;
- and
- R1 is selected from the group consisting of hydrogen, halogen, lower alkyl, alkoxy or a nitrile group
- together with a pharmaceutically acceptable excipient.
3 more elements
Dependencies are inferred from the claim text.