[EN] THIAZOLE DERIVATIVES AND THEIR USE AS VAP-1 INHIBITORS<br/>[FR] DERIVES DE THIAZOLE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE VAP-1
申请人:FUJISAWA PHARMACEUTICAL CO
公开号:WO2004067521A1
公开(公告)日:2004-08-12
A compound of the formula (I): R1-NH-X-Y-Z (I) wherein R1 is acyl; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond, lower alkylene or -COHN-; and Z is a groupe of the formulae (II) or (III) wherein R2 is a specified substituent or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor for preventing or treating a VAP-1associated disease, especially macular edema.
A platelet coagulation inhibitor which inhibits neither COX-1 nor COX-2 is provided. The inhibitor is a compound represented by general formula (I):
wherein Ar
1
and Ar
2
independently represent a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents, or a phenyl group optionally substituted with 1 to 3 substituents; R1 represents a lower acyl group, carboxyl group, a lower alkoxy carbonyl group, a lower alkoxy group, a lower alkyl group optionally substituted with 1 or 2 substituents, a carbamoyl group optionally substituted with 1 or 2 substituents, an oxamoyl group optionally substituted with 1 or 2 substituents, an amino group optionally substituted with 1 or 2 substituents, a 4- to 7-membered alicyclic heterocyclic group optionally substituted with 1 or 2 substituents, a phenyl group optionally substituted with 1 to 3 substituents, or a 5- or 6-membered aromatic heterocyclic group optionally substituted with 1 to 3 substituents; and R2 represents hydrogen atom, a halogeno group, or the like.
Compounds of formula (I) and pharmaceutically acceptable salts thereof:
wherein; each of R
1
to R
4
is independently selected from hydrogen and C
1-4
alkyl and each of rings A and B independently is optionally further substituted by up to three substituents, each of which is independently selected from the group consisting of halogen, hydroxy, C
1-4
alkoxy, C
1-4
alkyl, C
1-5
alkanoyl, CF
3
, CF
3
O and cyano; with the proviso that ring A must contain at least one CF
3
group, are useful in the treatment of diseases and conditions mediated by modulation of use-dependent voltage-gated sodium channels.
The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I):
wherein R
1
is optionally substituted C1-C8 alkyl and the like; R
2
is C1-C6 alkyl; R
3
is C1-C6 alkyl and the like; or R
2
and R
3
taken together with may form an optionally substituted 5 to 10 membered non-aromatic carbon ring; R
4
is hydrogen and the like; G is a group selected from the groups shown by the formula an the like:
wherein R
5
is hydrogen and the like; X
1
is a single bond and the like; X
2
is optionally substituted C1-C8 alkylene that may be replaced by one or two groups of —O—, or —N(R
6
)—, wherein R
6
is hydrogen and the like, and the like; X
3
is a single bond and the like;
a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
AMIDE AND UREA DERIVATIVES FOR THE TREATMENT OF METABOLIC DISEASES
申请人:Barba Oscar
公开号:US20100093733A1
公开(公告)日:2010-04-15
Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.