摘要:
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.
摘要:
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.
摘要:
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.
摘要:
The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
摘要:
The present patent application concerns new compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing ring, A is a saturated C1-4 alkylene and B a C3-4 alkylene or alkenylene chain; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
摘要翻译:本专利申请涉及具有R 1和R 2的新的式(I)化合物与它们所连接的氮原子一起形成饱和含氮的 环,A是饱和C 1-4亚烷基和B a C 3-4亚烷基或亚烯基链; 它们的制备及其作为H3受体配体的用途,用于治疗例如 中枢神经系统疾病如阿尔茨海默病。
摘要:
The invention relates to compounds which constitute a class of medicaments which have an anti-inflammatory activity and which act by inhibiting leukotriene A4 (LTA4), and enzyme which is responsible for the biosynthesis of leukotriene LTB4, a major proinflammatory mediator. The invention also relates to therapeutic anti-inflammatory, applications of these compounds as well as for methods of preparing these compounds.
摘要:
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). ##STR1##
摘要:
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.