摘要:
The present invention relates to the use of a vasopeptidase inhibitor for the preparation of a medicament for use in the treatment and/or prevention of PAH.
摘要:
The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.
摘要:
The present invention provides new method of treatment of epilepsy with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.
摘要:
Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.
摘要翻译:式(A)化合物的用途,其中:当在4(5)位上连接到咪唑环上时,W是组胺H 3受体赋予拮抗作用和/或激动作用的残基; R 1和R 2可以相同或不同,各自独立地表示低级烷基或环烷基,或与它们所连接的氮原子一起,饱和氮 (i)所定义的非芳族不饱和含氮环(ii),如在H中用作制备用作拮抗剂和/或激动剂的药物所定义的吗啉代基或N-取代哌嗪基 组胺的3个受体。
摘要:
The subject of the present invention is the various polymorphic forms I, II, III, IV of benzyl (S,S)-2-(2-acetylsulphanylmethyl-3-benzo[1,3]dioxol-5-ylpropionyl-amino)propionate, hereinafter called Fasidotril, their methods of preparation and novel pharmaceutical compositions containing them.
摘要:
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.3 receptor, in particular psychotic and depressive states, to the treatment of drug-dependence states or to the treatment of disorders of a sexual nature.
摘要:
Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II). ##STR1##
摘要:
The new naphthamide derivatives according to the invention are characterized in that they correspond to the general formula (I), ##STR1## where X: represents either a hydrogen atom, or a chlorine or bromine atom, or an amino or aminoalkyl group, an aminosulphamoyl group, a sulphur-containing group such as thiocyanate, alkylthio, alkylsulphinyl or alkylsulphonyl, or a methoxy group, or a nitro group, or a cyano group, or an electron-attracting group;Y: represents an alkyl or alkenyl residue;Z: represents the residues originating from 2-aminomethyl-N-alkylpyrrolidine, 2-aminoethyl-N,N-diethylamine, 2-(aminoethyl)morpholine, 2-aminoethyl-N,N-dibutylamine, 4-amino-N-butylpiperidine or 2-(aminoethyl)pyrrolidine;R: a hydrogen or an OCH.sub.3 substituent.These new derivatives may be employed in the preparation of medicinal products intended for use as an antipsychotic, psychostimulatory, anti-autistic or antidepressant agent, an agent for treating Parkinson's disease or an antihypertensive agent.
摘要:
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.