Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts, hydrates, solvates, geometrical isomers, tautomers, optical isomers, or prodrug forms thereof, wherein X, Y, Z, R1, R2, R3 and R4 are as defined herein are capable of binding to the active site of protein kinase enzymes. In particular, they are inhibitors of a serine/threonine kinase more particularly Rho kinase (ROK, ROCK).

Abstract: The present invention relates to compounds of Formula (I): wherein R3-R8, X, and Y are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.

Abstract: Compounds of Formula (I): wherein R and R? are described herein, as are processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a 5-HT2A receptor-related disorder.

Abstract: Compounds of Formula (I): wherein X, Y, Z, and R1 are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a 5-HT2A receptor-related disorder.

Abstract: This invention concerns peptides (I) having intracellular potassium channel modulating activity comprising the amino acid sequence shown in SEQ ID No: 2:(N terminal function) (I) Met Ile Ser Ser Val Cys Val Ser Ser 1 5} Tyr Arg Gly Arg Lys Ser Gly Asn Lys 10 15 Pro Pro Ser Lys Thr Cys Leu Lys Glu Glu 20 25 (C terminal function)in which the cysteines are optionally linked via a disulphide bridge and wherein ______________________________________ Met represents L-methionine Ile represents L-isoleucine Ser represents L-serine Val represents L-valine Cys represents L-cysteine Tyr represents L-tyrosine Arg represents L-arginine Gly represents glycine Lys represents L-lysine Asn represents L-asparagine Pro represents L-proline Thr represents L-threonine Leu represents L-leucine Glu represents L-glutamic acid ______________________________________or a variant thereof,with the proviso that excluded is the 13-Lys variant (where 13-Arg is replaced by 13-Lys) in which the cysteines are not linked via a disulphide bridge

Abstract: This invention concerns a compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds with the nitrogen ring optional bonds being between one adjacent pair on ring atoms,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; said aryl or heteroaryl radicals being optionally substituted by one or more substituents the same or different,R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, optionally substituted C.sub.6 -C.sub.10 aryl, optionally substituted heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl,R' represents one or more optional substituents the same or different, selected from one or more of the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.

Abstract: This invention concerns a compound of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group; optionally substituted by one or more substituents the same or different,R' represents one or more optional substituents the same or different, selected from the following: halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6 )alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, optionally substituted C.sub.6 -C.sub.10 or heteroaryl or an optionally substituted (C.sub.6 -C.sub.10 aryl)alkyl or a heteroaryl alkyl radical; andR" represents one or more optional mono- or di- valent substituents in the 5, 7 or 8 positions the same or different: monovalent substituents being selected from the following: C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkanoyloxy, hydroxy, amino, C.

Abstract: This invention concerns compounds of generic formula: ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted line represents an optional bond,one of R.sup.1 and R.sup.5 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.16 aralkyl, --(CHR.sup.6).sub.n CHR.sup.7 CN, --(CHR.sup.6).sub.n CHR.sup.7 CONH.sub.2, --(CHR.sup.6).sub.n CHR.sup.7 COOR.sup.8, --(CHR.sup.6).sub.n CHR.sup.7 CH.sub.2 OH wherein n is 0 or 1, R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1 -C.sub.6 alkyl- or C.sub.7 -C.sub.16 aralkyl-, and R.sup.7 also represents hydroxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.2 -C.sub.7)alkanoyloxy(C.sub.1 -C.sub.6)alkyl-, (C.sub.1 -C.sub.6 alkoxy)carbonyl- and R.sup.8 is hydrogen or C.sub.1 -C.sub.6 alkyl;the other of R.sup.1 and R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.7 -C.sub.16 aralkyl; R.sup.3 is C.sub.6 -C.sub.10 aryl or heteroaryl group optionally substituted by one or more substituents the same or differnet,R.sup.2 and R.sup.

Abstract: This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group;R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl;R' represents one or more optional substituents the same or different, selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.

Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents 0, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.

Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents O, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.

Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.0 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.

Abstract: The invention provides a method of relieving inflammation in a mammal inflicted with an imflammatory disease which method comprises treating said mammal with a therapeutically effective amount of a compound of formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 represent hydrogen, loweralkyl, cycloloweralkyl, loweralkoxy, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, loweralkoxycarbonyl, aryl or aralkyl or 7-12 carbon atoms, or R.sup.1 and R.sup.2 taken together, or R.sup.2 and R.sup.3 taken together form a5,6, or 7 membered ring with the carbon atoms to which they are attached, which ring may be saturated or unsaturated and unsubstituted or substituted by loweralkyl or loweralkoxy, R.sup.

Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is O or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.

Abstract: The invention concerns a compound formula II ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are the same or different and represent hydrogen, or loweralkyl, cycloalkyl or lower aralkyl, any of which radicals may be substituted by lower alkyl, lower alkoxy or CF.sub.3 or phenyl radicals which may be substituted by lower alkyl or CF.sub.3 or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring R.sup.4 and R.sup.5 may also represent lower alkoxy, or cycloalkoxy, n is 1, 2, or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different with the provisos that (1) when R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are all hydrogen, R.sup.6 R.sup.7 are not both hydrogen, (2) when R.sup.1 and R.sup.3 are both phenyl and when R.sup.1 is methyl and R.sup.4 is methyl then R.sup.6 and R.sup.7 are not both methyl, and (3) when R.sup.1 is hydrogen or methyl, R.sup.

Abstract: The invention provides a compound of formula III ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and represent hydrogen or lower alkyl, cycloalkyl, lower aralkyl or phenyl radicals any of which radicals may be substituted by lower alkyl, lower alkoxy or trifluoromethyl or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring, R.sup.4 and R.sup.5 may also represent lower alkoxy or cycloalkoxy, n is 1, 2 or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different and esters of carboxylic acids with the hydroxy group shown, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined above, with the provisos that (1) R.sup.6 and R.sup.7 are other than hydrogen when R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are all hydrogen and (2) R.sup.6 and R.sup.7 are not both methyl when R.sup.4 is methyl.

Abstract: The invention concerns azo compounds of formula ##STR1## or a salt thereof, in which formula R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are each independently hydrogen or lower alkyl, R.sup.7 and R.sup.8 are each independently alkyl of 1 to 7 carbon atom or cycloalkyl of 5 to 7 carbon atoms optionally substituted by lower alkyl which possess anti-inflammatory activity.

Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.

Abstract: A process for preparing dihydro compounds of formula I, by rearranging compounds of formula II, e.g. in the presence of acids or noble metal catalysts, is described. The compounds II may be prepared from intermediates of formula III. ##STR1## In these formulae R.sup.1,R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, or alkyl, cycloalkyl, aralkyl, or aryl radicals any of which radicals may be substituted, or R.sup.1 and R.sup.2 taken together or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered ring which may be saturated or unsaturated and substituted or unsubstituted, R.sup.4 and R.sup.5 may also represent alkoxy, or cycloalkoxy, n is 1, 2 or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different and R.sup.6 and R.sup.7 represent hydrogen, alkyl, cycloalkyl, or aralkyl radicals.Most of the compounds I, II and III are novel and are claimed. They are intermediates for anti-ulcer agents.

Abstract: This invention relates to a method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--CR.sup.5 .dbd.CR.sup.6 -- (Ib)or--(CHR.sup.5).sub.n --CR.sup.6 .dbd. (Ic);R represents an optionally substituted aryl or heteroaryl radical; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur. Novel compositions and compounds of formula I are also disclosed.