摘要:
The present invention relates to a new formulation of an enkephalinase inhibitor, such as racecadotril or dexecadotril, the process for the preparation thereof, and the use thereof in the treatment of diarrhea.
摘要:
Medicament comprising, in a pharmaceutically acceptable vehicle, an anti-psychotic or an antidepressant (A), which, on its own, has an undesirable effect of a gain in body weight or sedation, and an antagonist and/or inverse agonist (B) of the histamine H3 receptor, the antagonist and/or inverse agonist of the histamine H3 receptor being present in a therapeutically effective amount for ensuring at least one of the following three effects: suppression or at least limitation of the undesirable effect of weight gain, suppression or limitation of the undesirable effect on alertness, epilepsy/convulsions, increase in the precognitive effect of the treatment. Use of such an antagonist or inverse agonist for the preparation of a medicament which is to ensure at least one of the said three effects in a patient treated by such an antipsychotic or antidepressant.
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:使用式(A)化合物,其中:W是当连接到4(5)位的咪唑环时,其在组胺H3受体中具有拮抗作用和/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,与所定义的饱和含氮环(i)一起形成非芳族不饱和氮 - (ii)定义的吗啉基或N-取代的哌嗪子基团,其用于制备组胺的H3受体作为拮抗剂和/或激动剂的药物。
摘要:
The present invention relates to new compounds of formula (I) possessing agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents. The invention is also directed to pharmaceutical compositions containing these compounds and use of these compounds for treatment/prevention of immune mediated diseases and conditions or inflammatory diseases and conditions.
摘要:
The invention relates to a combination of modafinil and at least one histamine H3 receptor antagonist or inverse agonist, which can be used in particular for the treatment of narcolepsy-cataplexy and more generally for disorders of sleep, wakefulness and vigilance.
摘要:
The invention relates to new crystalline 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine monohydrochloride, the respective manufacture and methods of use, and compositions containing such a compound.
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 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). ##STR1##
摘要:
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.