摘要:
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as "AAA compounds"), which, inter alia, are (selective) retinoic acid receptor α (RARα) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARα, and in the treatment of diseases and conditions that are mediated by RARα, that are ameliorated by the activation of RARα, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.
摘要:
Compounds of formula (I), wherein one of U and V is -CHR -, and the other of U and V is selected from -N(COR )-, -CH(COR )-,-N(SO2R )- and -CH(SO2R )-, in which R is H, -COOR , -CONR R or -COR and R is H, C1 to C6 hydrocarbyl (in which up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom), or a group of the formula -Q-R wherein Q is a bond, -NR - (in which R is H or C1 to C3 alkyl) or -O-, and R is aryl, substituted aryl, arylalkyl or (substituted aryl)alkyl; R is independently C1 to C3 alkyl; R is H or C1 to C15 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom; R is independently halo, alkyl, alkoxy, -NO2, -NH2 or -NHCOR ; X is H and Y is H or C1 to C10 hydrocarbyl wherein one or more hydrogen atoms may be replaced by halogen atoms, and one carbon atom may be replaced by a nitrogen, oxygen or sulphur atom; or X and Y together are =O or =CH2; Z is H, C1 to C15 hydrocarbyl (in which one or more hydrogen atoms may be replaced by a halogen atom, and up to three of the carbon atoms may be replaced by a nitrogen, oxygen or sulphur atom), or -(CHR )m-R (wherein R is H or C1 to C3 alkyl and R is phenyl, substituted phenyl or a group of the formula -COOR or -CONR R , in which R and R are independently H or C1 to C6 alkyl, or R and R together form a propylene, butylene, pentylene or hexylene group); m is from 1 to 3; and n and p are independently from 0 to 3, and pharmaceutically acceptable salts thereof are ligands at gastrin and/or cholecystokinin receptors.
摘要:
The present invention is concerned with benzotriazepinone derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-l or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.
摘要:
Compounds of formula (I) wherein R is selected from C1 to C6 alkyl, C1 to C6 alkoxy, C1 to C6 alkylthio, carboxy, carboxy (C1 to C6)alkyl, formyl, C1 to C6 alkylcarbonyl, C1 to C6 alkylcarbonylalkoxy, nitro, trihalomethyl, hydroxy, amino, C1 to C6 alkylamino, di(C1 to C6 alkyl)amino, aryl, C1 to C6 alkylaryl, halo, sulfamoyl and cyano; R is C1 to C20 hydrocarbylene, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 6 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group, and provided also that the atom in R which is linked to the -SO2- moiety is a carbon atom; R is hydrogen or C1 to C15 hydrocarbyl, in which one or more hydrogen atoms may be replaced by halogen atoms and up to 3 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group; X is a bond or -NR -, wherein R is hydrogen or non-aromatic C1 to C5 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen atoms and up to 2 carbon atoms may be replaced by oxygen, nitrogen or sulfur atoms, provided that R does not contain a -O-O- group), aryl(C1 to C3)alkyl or R represents a bond to R ; and a is from 0 to 2, and their pharmaceutically acceptable salts are useful as histamine H3 receptor ligands.
摘要:
Compounds of formula (I) wherein L is =N- or =CH-, one of X and Y is -NH-CH2-R (wherein R is cycloheptyl or 1-adamantyl) and the other is (II) in which R is H or methyl, T and T are independently H or Z(CH2)m-, wherein m is from 0 to 3 and Z is a carboxy group, a tetrazolyl group, CF3CONHSO2-, PhCONHSO2-, isopropyl-OC(O)NHSO2- or a group selected from (a), (b) and (c) (provided that T and T are not both H and that T and T are not both carboxy when L is =CH-); and n is from 0 to 5; and pharmaceutically acceptable salts thereof are potent gastrin and/or CCK antagonists.
摘要:
Compounds of formula (I) wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or -C(O)-CH2- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R7-O- or R7-N(R8)- (wherein R7 is H or C1 to C15 hydrocarbyl, up to two carbon atoms of the hydrocarbyl moiety optionally being replaced by a nitrogen, oxygen or sulphur atom provided that Y does not contain a -O-O- group, and R8 is H, C1 to C3 alkyl, carboxymethyl or esterified carboxymethyl), Z is selected from (i) -O-R9, (ii), (iii), (iv), wherein R9-R13, Q, Q', G, T, A, B, a and b are as defined in claim 1; or Z is absent and W is H, R1 is H, methyl, halo, carboxy, esterified carboxy, amidated carboxy, carboxymethyl, esterified carboxymethyl or amidated carboxymethyl, R2 is selected from the groups recited above for R1; R3 and R4 (or each R3 and R4 group, when m or n is 2 or more) are independently selected from halo, amino, nitro, cyano, sulphamoyl, C1 to C3 alkyl, C1 to C3 alkoxy, carboxy, esterified carboxy and amidated carboxy, R5 and R6 are independently selected from H and the groups recited above for R3; m, n = 0 to 4, with provisos as given in claim 1 and pharmaceutically acceptable salts thereof, are ligands at cholecystokinin and/or gastrin receptors.
摘要:
This invention relates to a compound of formula (I) wherein: W is N or N + -O - ; and R 1 to R 5 are as defined in the description, for use for the treatment of gastrin related disorders.
摘要:
Compounds of formula (I) or (II) wherein R is C4 to C20 hydrocarbyl (in which one or more hydrogen atoms may be replaced by halogen, and up to three carbon atoms may be replaced by oxygen, nitrogen or sulphur atoms, provided that R does not contain an -O-O- group), R is H or C1 to C3 alkyl, m is from 1 to 15, n is from 2 to 6, each X group is independently (a), or one X group is -N(R )-, -O- or -S- and the remaining X groups are independently (a), wherein R is H, C1 to C6 alkyl, -CO2R , -CONR 2, -CR 2OR or -OR (in which R and R are H or C1 to C3 alkyl), and R is H or C1 to C6 alkyl, each Y group is independently -C(R )R -, or up to two Y groups are -N(R )-, -O- or -S- and the remaining Y groups are independently -C(R )R -, wherein R is as defined above, one R group in the structure is imidazoyl or imidazoylalkyl and the remaining R groups are H or C1 to C6 alkyl, and Z is > C(R )NR - or > N-, wherein R is any of the groups recited above for R , and pharmaceutically acceptable salts thereof are ligands at histamine H3 receptors.
摘要:
Compounds of formula (Ia), (Ib) or (Ic), wherein A represents a group having two fused rings, or a group of formula (Id), R (m) represents up to 6 substituents, K represents -O-, -S-, -CH2-, -N(R )- or -N(COR )-, in which R is H or C1 to C3 alkyl, W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group, provided that at least one of W and X contains carbonyl, Y and Z are as given in the description and their pharmaceutically acceptable salts are ligands at CCK and/or gastrin receptors.
摘要:
The present invention is concerned with benzotriazepinone derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-l or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.