Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: 4-[4-(2-Adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid and pharmaceutically-acceptable salts thereof and a particular crystalline form of the Agent (Form 1); their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: A compound of Formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Abstract: A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen-protecting group, and removing the group R7—, and thereafter if desired or necessary, removing any protecting group R6 to obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed.

Abstract: Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.

Abstract: Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6.

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.

Abstract: Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof, possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.

Abstract: Compounds of formula (I), wherein G1 is CH or N; G2 is CH or N; R1 is a variety of optional substituents; L1 is (1-4C)alkylene; T1 is CH or N; R2 and R3 are independently hydrogen or (1-4C)alkyl or are joined to form a ring; X1 and X2 represent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.

Abstract: Heterocyclic amides of formula (1) wherein: m is 0, 1 or 2; n is 0, 1 or 2; B is phenyl or heterocyclyl; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 and R3 are independently selected from, for example, C5-7cycloalkyl, cyano(C1-4)alkyl, C1-4alkyl (optionally substituted with 1 or 2 R8 groups), —OR8 and R8; R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, heterocyclyl, aryl, —COCOOR9, —C(O)N(R9)(R10), (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from for example, hydroxy, C1-4alkoxy, heterocyclyl and C1-4alkanoyl; R14 is selected from for example, hydrogen, halo, C1-4alkyl, C5-7cycloalkyl, C1-4alkoxy, cyano, cyano(C1-4)alkyl, —COR3, (R2)(R3)NCO—, and (R2)(R3)NSO2—; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activ

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and C1-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.

Abstract: A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4, R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen-protecting group, and removing the group R7—, and thereafter if desired or necessary, removing any protecting group R6 to obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed.

Abstract: Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed.

Abstract: The invention relates to heterocyclic derivatives of formula (I) A—B—X1—T1(R2)—L1—T2(R3)—X2—Q??(I) or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Abstract: Heterocyclic amides of formula (1) wherein: m is 0, 1 or 2; n is 0, 1 or 2; B is phenyl or heterocyclyl; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 and R3 are independently selected from, for example, C5-7cycloalkyl, cyano(C1-4)alkyl, C1-4alkyl (optionally substituted with 1 or 2 R8 groups), OR8 and R8; R4 is independently selected from for example hydrogen, halo, nitro, cyano, hydroxy, C1-4alkyl, and C1-4alkanoyl; R8 is selected from for example hydroxy, heterocyclyl, aryl, —COCOOR9, —C(O)N(R9)(R10), (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from for example, hydroxy, C1-4alkoxy, heterocyclyl and C1-4alkanoyl; R14 is selected from for example, hydrogen, halo, C1-4alkyl, C5-7cycloalkyl, C1-4alkoxy, cyano, cyano(C1-4)alkyl, —COR3, (R2)(R3)NCO—, and (R2)(R3)NSO2—; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory

Abstract: Heterocyclic amides of formula (1) wherein: X is N or CH; R4 and R5 together are either —S—C(R6)?C(R7)— or —C(R7)?C(R6)—S—; R6 and R7 are independently selected from, for example hydrogen, halo and Cl-4alkyl; A is phenylene or heteroarylene; n is 0, 1 or 2; R1 is selected from for example halo, nitro, cyano, hydroxy, carboxy; R2 is hydrogen, hydroxy or carboxy; R3 is selected from for example hydrogen, hydroxy, aryl, heterocyclyl and C1-4alkyl(optionally substituted by 1 or 2 R8 groups); R8 is selected from for example hydroxy, —COCOOR9, —C(O)N(R9)(R10), —NHC(O)R9, (R9)(R10)N— and —COOR9; R9 and R10 are selected from for example hydrogen, hydroxy, C1-4alkyl (optionally substituted by 1 or 2 R13); R13 is selected from hydroxy, halo, trihalomethyl and C1-4alkoxy; or a pharmaceutically acceptable salt or pro-drug thereof; possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity.