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US 2011/0237628 A1Published application
Cyclopentyl- and cycloheptylpyrazoles
AssigneeHoffmann-La Roche Inc.
InventorsGregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
Life of this patent
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Abstract
This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.
Claims16
A compound of the formula I,
- wherein
- A is —CH2— or —(CH2)3—,
- R1 is a ring selected from phenyl, naphthyl and heteroaryl, said ring being unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, lower halogenalkyl, hydroxy, lower alkoxy, lower halogenalkoxy and cyano;
- R2 is selected from the group consisting of hydrogen, methyl, ethyl, hydroxy, methoxy, fluoro, fluoromethyl, difluoromethyl and trifluoromethyl;
- R3 is selected from the group consisting of:
- unsubstituted cycloalkyl or cycloalkyl substituted 1 to 4 groups independently selected from methyl and fluoro;
- lower cycloalkylalkyl;
- unsubstituted phenyl;
- phenyl substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, lower halogenalkyl, hydroxy, lower alkoxy, lower halogenalkoxy and cyano;
- and
- heterocyclyl;
- R4 is selected from the group consisting of —C(O)—NH—R5,
- —CR7R8—OR6, —O—(CR7R8)n—R6;
- —CR7R8—SR6, —CR7R8—SO—R6, —CR7R8—SO2—R6,
- —CR7R8—NH—R6;
- —CH═CH—R6 and —(CH2)2—R6,
- wherein
- n is 0 or 1,
- R5 is selected from the group consisting of:
- lower alkyl;
- cycloalkyl;
- lower cycloalkylalkyl;
- cycloalkyl substituted with 1 to 3 substituents independently selected from the group consisting of hydroxy, carboxyl, tetrazolyl, lower carboxylalkyl, lower alkoxycarbonyl, lower alkoxycarbonylalkyl, lower carboxylalkoxy and lower alkoxycarbonylalkoxy;
- unsubstituted phenyl;
- and
- phenyl substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, lower halogenalkyl, hydroxy, lower alkoxy, lower halogenalkoxy, carboxyl, tetrazolyl, lower alkoxycarbonyl, lower alkoxycarbonylalkyl, lower carboxylalkyl, lower carboxylalkoxy, lower alkoxycarbonylalkoxy, cyano and cycloalkyloxy, wherein the cycloalkyl group is substituted by carboxyl, lower alkoxycarbonyl or tetrazolyl;
- unsubstituted pyridyl;
- and
- pyridyl substituted by a group selected from the group consisting of carboxyl, lower alkoxycarbonyl and tetrazolyl;
- R6 is selected from the group consisting of:
- lower alkyl;
- cycloalkyl;
- lower cycloalkylalkyl;
- cycloalkyl substituted with 1 to 3 substituents independently selected from the group consisting of hydroxy, carboxyl, tetrazolyl, lower carboxylalkyl, lower alkoxycarbonyl, lower alkoxycarbonylalkyl, lower carboxylalkoxy and lower alkoxycarbonylalkoxy;
- heterocyclyl;
- unsubstituted pyridyl;
- pyridyl substituted by carboxyl, lower alkoxycarbonyl or tetrazolyl;
- unsubstituted phenyl;
- and
- phenyl substituted with 1 to 3 substituents independently selected from the group consisting of lower alkyl, halogen, lower halogenalkyl, hydroxy, lower alkoxy, lower halogenalkoxy, carboxyl, tetrazolyl, lower alkoxycarbonyl, lower alkoxycarbonylalkyl, lower carboxylalkyl, lower carboxylalkoxy, lower alkoxycarbonylalkoxy, cyano and cycloalkyloxy, wherein the cycloalkyl group is substituted by carboxyl, lower alkoxycarbonyl or tetrazolyl;
- and
- R7 and R8 independently are selected from the group consisting of hydrogen, lower alkyl and lower halogenalkyl, or
- R7 and R8 together with the carbon atom to which they are attached form a cycloalkyl or alkoxycycloalkyl ring;
- or a pharmaceutically acceptable salt thereof.
41 more elements
Dependencies are inferred from the claim text.