Abstract: A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoletic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: A compound of formula (I) wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: A compound of formula (I) wherein R1, R2, R3, R4, X, Y, and A are as defined herein. The compounds of the present invention are inhibitors of hematopoletic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne muscular dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: A compound of formula (I) wherein R, R1, R2, R3, Y, Y1, a, X, and Z are as defined herein. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) and can be useful in the treatment of Duchenne Muscular Dystrophy. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting H-PGDS activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

Abstract: The present invention disclosed compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.

Abstract: The present invention discloses compounds of Formula I. The present invention also discloses beta-3 agonists of formula I and methods for treating beta-3 mediated diseases and condition using the compounds of formula I, in particular methods for treating diabetes or obesity.

Abstract: A method is disclosed for rational design of a PPAR, FXR, LXR-alpha, or LXR-beta antagonist comprising chemical modification of a PPAR, FXR, LXR-alpha, or LXR-beta agonist to: a) prevent formation of a hydrogen bond between the agonist and tyrosine or histidine, or tryptophan involved in receptor activation; and/or b) displace the tyrosine or histidine, or tryptophan involved in receptor activation from its agonist bound position. Preferably, little or no additional changes are made in the structure of the agonist so that the resulting antagonist is a close structural analogue of the agonist.

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerbral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerebral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.

Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.

Abstract: A class of acetamidine derivatives of general formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR.sup.3 wherein X is oxygen, C(O).sub.m wherein m is 1 or 2, S(O).sub.n wherein n is 0, 1 or 2, or a group NR.sup.4 wherein R.sup.4 is hydrogen or C.sub.1-6 alkyl; and R.sup.3 is hydrogen, C.sub.1-6 alkyl, or a group NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-6 alkyl, provided that R.sup.3 is not NR.sup.5 R.sup.6 when X is oxygen or S(O).sub.n; R.sup.1a and R.sup.1b are independently selected from hydrogen and halo; R.sup.2 is a C.sub.1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R.sup.2 being optionally substituted by one or more groups independently selected from halo; N.sub.3 ; nitro; CF.sub.3 ; ZR.sup.7 wherein Z is oxygen, C(O).sub.m' wherein m' is 1 or 2, S(O).sub.n' wherein n' is 0, 1 or 2, or a group NR.sup.8 wherein R.sup.

Abstract: A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or R

Abstract: A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m?R13 wherein m? is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydroge