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:
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:
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:
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:
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.
摘要:
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.
摘要:
The present invention relates to .alpha.,.beta.-dimethylhistamine, of the rmula: ##STR1## in racemic form, or an optical isomer form or mixture of diastereoisomers and its acid addition salts. It may be prepared from an alkyl 2-amino 3-(1H-imidazol-4-yl)-carboxylate.
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:
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.