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US 2009/0023733 A1Published application
Piperidine Derivatives, Their Process for Preparation, Their Use as Therapeutic Agents and Pharmaceutical Compositions Containing Them
OwnerPeter Cage, Mark Furber +3inventors
InventorsPeter Cage, Mark Furber, Christopher Luckhurst, Matthew Perry, Brian Springthorpe
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Abstract
The present invention provides a compound of a formula (I): [Chemical formula should be inserted here. Please see paper copy] wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.
Claims11
A compound of formula (I):
- wherein:
- Ar1 is phenyl or naphthyl, either of which is optionally substituted by chloro, fluoro, methyl or CF3;
- Ar2 is phenyl, naphthyl, imidazolyl, pyrazinyl, thienyl, thiazolyl, thiadiazolyl, pyridinyl, pyrimidinyl, benzimidazolyl, quinolinyl, quinazolinyl, isoquinolinyl, 5-phenylamino-1,3,4-oxadiazolyl, dihydroquinazolinyl, 3-pyridinyl-1,2,4-oxadiazolyl, pyridazinyl or quinoxalinyl;
- wherein Ar2 is substituted by CO2R′ or tetrazolyl;
- and Ar2 is optionally additionally substituted by one or more of halogen, hydroxy, nitro, S(O)r(C1-6 alkyl), S(O)2NH2, S(O)2NH(C1-6 alkyl), S(O)2N(C1-6 alkyl)2, NH2, NH(C1-6 alkyl), N(C1-6 alkyl)2, cyano, C1-6 alkyl, C1-6 alkoxy, C(O)NH2, C(O)NH(C1-6 alkyl), C(O)N(C1-6 alkyl)2, CO2H, CO2(C1-6 alkyl), NHC(O)(C1-6 alkyl), NHS(O)2(C1-6 alkyl), C(O)(C1-6 alkyl), CF3 or OCF3;
- wherein alkyl or alkoxy groups are optionally substituted by NR1R2;
- R1 and R2 are independently hydrogen or C1-4 alkyl or together with the nitrogen to which they are attached form a ring (for example azepine, pyrrolidine, piperidine,
- homopiperidine, morpholine or piperazine), the latter optionally substituted on the distal nitrogen by C1-4 alkyl;
- R′ is hydrogen, C1-6 alkyl or phenyl(C1-4 alkyl);
- wherein the phenyl is optionally substituted with halogen, hydroxy, nitro, S(O)t(C1-4 alkyl), S(O)2NH2, S(O)2NH(C1-4 alkyl), S(O)2N(C1-4 alkyl)2, cyano, C1-4 alkyl, C1-4 alkoxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2, CO2H, CO2(C1-4 alkyl), NHC(O)(C1-4 alkyl), NHS(O)2(C1-4 alkyl), C(O)(C1-4 alkyl), CF3 or OCF3;
- or CO2R′ is (CO2—)pRp+ wherein Rp+ is a univalent cation (for example an alkali metal cation) or two carboxylates may coordinate to a divalent cation (for example an alkaline earth metal cation);
- or tetrazolyl is (tetrazolylg−)Rg+ wherein Rg+ is a univalent cation (for example an alkali metal cation) or two tetrazoles may coordinate to a divalent cation (for example an alkaline earth metal cation);
- and,
- r and t are, independently, 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof;
- provided:
- that when Ar1 is 3,4-difluorophenyl then Ar2 is not 2-(CO2CH3)phenyl.
14 more elements
Dependencies are inferred from the claim text.