Abstract: Novel imidazole derivatives as histamine receptor H3 antagonists and/or agonists, preparation thereof and therapeutical uses thereof. Chemical compounds for use as histamine receptor H3 agonists, partial agonists or antagonists, having general formula (Ia) or (Ib), the use thereof for making drugs, and methods for revealing the agonist, partial agonist or antagonist activity of such compounds in vivo, are disclosed.

Abstract: Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in:a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride;b) preparing the monoacetates (VII R) or (VII S) respectively;c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R);d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R);e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R.sub.1 SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).

Abstract: The invention relates to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): ##STR1## in which: the Z-Y entity represents an N--CH.sub.2, C.dbd.CH or CH--CH.sub.2 group;R.sup.1 represents a hydrogen, fluorine, bromine or iodine atom or a hydroxyl, methoxy, nitrile or nitro group;R.sup.2 represents a hydrogen or bromine atom or a hydroxyl, methoxy, nitrile or nitro group;the R.sub.1 and R.sub.2 substituents both being situated on the same ring of the naphthamide unit or each being situated on one of the rings;R.sup.3 and R.sup.4 can be identical or different and each independently represent a hydrogen or chlorine atom or a methoxy or methyl group or an electron-withdrawing group.The invention also relates to their therapeutic applications as partial agonists of the dopamine D.sub.3 receptor.The invention applies more particularly to the treatment of neuropsychiatric conditions involving the dopamine D.sub.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: Process for the synthesis of a-substituted acrylic acids and their application.Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II).

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## having antagonist properties to histamine H.sub.3 -receptors.

Abstract: Amino acid derivatives having both enkephalinase and ACE inhibiting properties corresponding to the formula: ##STR1##

Abstract: New amino acid derivatives, processes for their preparation, and their therapeutic application are described.These amino acid derivatives correspond to the general formulae ##STR1## These derivatives may be used as medicaments which exhibit an enkephalinase-inhibitory activity.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and prodrugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having antagonist properties to histamine H.sub.3 -receptors.

Abstract: Agonist compounds of the histamine H.sub.3 receptor for therapeutic use, pharmaceutical compositions acting as agonists of the said receptor and preparation process are disclosed.The compounds are derived from an amine R-NH.sub.2 having a high affinity for the histamine H.sub.3 receptor and to the primary amine function of which a group which gives rise to a bond that is capable of being slowly hydrolyzed in a neutral medium is attached. The pharmaceutical compositions contain these compounds and a pharmaceutically acceptable vehicle or excipient.These compounds are used for producing a medicinal product which inhibits the synthesis and the release of histamine, in particular, possessing sedative, sleep-regulating, anticonvulsant, antidepressant, anti-allergic, anti-inflammatory, antisecretory or anti-ulcerous effects.

Abstract: The (R) or (S) isomer of acetorphan or N-/(acetylthiomethyl)-2-oxo-1-phenyl-3-propyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-3-benzyl-2-propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Abstract: The invention claims as drugs which are active as agonists of the histamine H.sub.3 receptor, the O-[2-(4(5-imidazolyl)-ethyl] isothiourea, 4-(4(5)-imidazolyl) butyramidine and S-[2-(4(5)-imidazolyl)-ethyl] isourea as well as their N-methyl derivatives, these compounds being useful for the preparation of drugs to be used as hypnotic, sleep-inducer, tranquillizer, sedative, anxiolytic, anti-asthmatic and anti-inflammatory agents, notably for the bronchi, the skin or the eyes, or as anti-gastric ulcer agents.

Abstract: The (R) or (S) isomer of acetorphan or N-/(acetylthiomethyl)-2-oxo-1-phenyl-3-propyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-3-benzyl-2-propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Abstract: The compounds correspond to the general formula ##STR1## in which R.sub.1 represents a hydrogen atom or a group --COR.sub.2, in which R.sub.2 represents a benzene ring, cyclopentylmethyl, cyclohexylmethyl, cyclopentylethyl or cyclohexylethyl groups or cyclopentylamine, cyclohexylamine or phenylamine, chlorophenylamine or dichlorophenylamine groups; R represents a hydrogen atom or a group COR.sub.3, in which R.sub.3 represents an aliphatic group, a cyclane or benzene ring-system, a group a group (CH.sub.2).sup.m R.sub.4, a group --CH.dbd.CHR.sub.8 or a secondary amine group --NH(CH.sub.2).sub.n R.sub.

Abstract: The (R) or (S) isomer of acetorphan or N-/2-acetylthiomethyl)-1-oxo-3-phenylpropyl/(S) alanine methyl ester is prepared by splitting of racemic acetylthio-2-benzylpropanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Abstract: The (R) or (S) isomer of acetorphan or N-12-acetylthiomethyl-1-oxo-3-phenyl propyl/(S) alanine methyl ester is prepared by splitting of racemic 3-acetylthio-2-benzyl propanoic acid by reaction with ephedrin, separation of the enantiomeric salt obtained, then freeing of the acid and coupling with the corresponding amino acid ester. The obtained preparations possess remarkable therapeutic activities and can notably be used as drugs.

Abstract: Compounds of general formula ##STR1## in which R.sub.1 denotes H, CH.sub.3 or C.sub.2 H.sub.5, R denotes H or R.sub.2 and R.sub.2 denotes an alkyl, piperonyl, 3-(1-benzimidazolonyl)-propyl group; a group of formula ##STR2## in which n is 0, 1, 2, or 3, X is a single bond or alternatively --O--, --S--, --NH--, --CO--, --CH.dbd.CH-- or ##STR3## and R.sub.3 is H, CH.sub.3, F, CN or an acyl group; or alternatively a group of formula ##STR4## in which Z denotes an O or S atom or a divalent group NH, N --CH.sub.3 or N --CN, and R.sub.5 denotes an alkyl group, a cycloalkyl group which can bear a phenyl substituent, a phenyl group which can bear a CH.sub.3 or F substituent, a phenylalkyl(1-3 C) group or a naphthyl, adamantyl or p-toluenesulphonyl group. These compounds are useful to control the release of cerebral histamine and to increase the rate of renewal of cerebral histamine.

Abstract: This invention relates to aminoacid derivatives, and compositions containing the same and having enkephalinase-inhibiting, antalgic, antidiarrhea and hypotensive activities, of the formula ##STR1## whose variables are as set forth herein, for example ##STR2##

Abstract: A compound selected from the group consisting of a compound of the formula wherein the substituents are defined as in the specification having antagonist properties to histamine H3-receptors.