摘要:
The invention relates to 3-aminopyridazine derivatives.These compounds have the formula ##STR1## in which: R.sub.V is a linear or branched C.sub.1 -C.sub.4 alkyl group;R.sub.6 is hydrogen, a C.sub.1 -C.sub.3 alkoxy or a hydroxyl group; andZ is a group ##STR2## in which: n.sub.1 and n.sub.2 independently are zero or one,Y.sub.1 and Y.sub.2 independently are hydrogen or a C.sub.1 -C.sub.3 alkyl group, andT is a dialkylamino group in which the alkyls are C.sub.1 -C.sub.3, if Y.sub.1 or Y.sub.2 is other than hydrogen, or T is a heterocycle selected from: ##STR3## Application: drugs active on the central nervous system.
摘要:
The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors and to drugs containing them.These derivatives have the following formula: ##STR1## in which: X represents a group (CH.sub.2).sub.n, n representing an integer equal to 2, 3 or 4, or alternatively a vinylene group or a methylvinylene group;R.sub.1 and R.sub.2, considered independently, represent hydrogen or a substituent occupying one of the free positions of the benzene ring and selected from the group comprising halogens, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a thiol group, a nitro group and an optionally substituted amino group;Y represents oxygen, sulfur or a group --NH--; andR.sub.3 is an amino groupApplication: agonists of the cholinergic receptors.
摘要:
The invention relates to novel tricyclic derivatives which are agonists of cholinergic receptors.These derivatives have the formula ##STR1## in which X=O, S, --OCH.sub.2 -- or --SCH.sub.2 --; R.sub.1 =H or halogen; and R.sub.2 = ##STR2## in which Alk is an alkylene group and R.sub.3, an R.sub.4, which are identical or different, are hydrogen or a lower alkyl group, or R.sub.3 and R.sub.4, with the nitrogen atom to which they are bonded, form a 5- or 6-membered cyclic amino group optionally containing a second heteroatom; or R.sub.2 is a group ##STR3## where R.sub.5 =C.sub.1 -C.sub.4 -alkyl. Application: agonists of cholinergic receptors.
摘要:
The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
摘要:
The present invention relates to imidazo[1,2-b]-pyridazines having the formula: ##STR1## in which: R.sub.1 represents hydrogen, a halogen atom, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.1 -C.sub.4 alkyl group occupying one of the free positions of the benzene ring; R.sub.2 represents hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; R.sub.3 denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or a phenyl group; and R.sub.4 R.sub.5 represent hydrogen or a C.sub.1 -C.sub.4 alkyl group, or R.sub.4 and R.sub.5 form, together with the nitrogen atom to which they are bonded, a 5-membered or 6-membered heterocycle optionally containing a second heteroatom. Application: drugs, especially for the treatment of cortical cholinergic deficiencies.
摘要:
The present invention relates to pyridazine derivatives of formula: ##STR1## which are useful as ligands of cholinergic receptors, in particular, receptors of the M.sub.1 type.
摘要:
The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.
摘要:
The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A′, identical or different, are respectively either a group A1 and A′1 of formula (1) wherein n=2 to 4; R′1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3. B and B′, identical or different, represent respectively either the group B1 and B′1, if A and A′ respectively represent A1, A′1, B1, B′1 representing a group R1 which has the same definition as R′1 above, but cannot be a hydrogen atom; or respectively the groups B2 and B′2, if A and A′ represent A2, B2 or B′2 being the group R1 as defined above, or a group of formula (2) wherein —Ra is RS— or RCO—, wherein R is a C1-C6 alkyl, substituted if required, a phenyl or benzyl, wherein the phenyl is substituted if required, the latter being optionally substituted; R2 is hydrogen, C1-C5 alkyl, or a —CH2-COO— (C1-C5)alkyl group; and R3 is hydrogen, C1-C5 alkyl or alkenyl, substituted if required, a phosphate, an alkoxy wherein the alkyl is a C1-C3 alkyl, or aryloxy; or an alkyl (or arylcarbonyloxy; or R2 and R3 form together a cycle with 5 or 6 C; R and R3 can be bound to form a cycle. ± represents: either a single bond when A and A′ represent A1 and A′1: or when A and A′ represent A2, and B2 and B′2 Represent (3) either, when A and A′ are —CHO or —COCH3 and B2 and B′2 are R1, a group of formula (4) or a group of formula (5) wherein (a) represents a bond towards Z and (b) a bond towards the nitrogen atom. Z is a C9-C21 alkyl, if required with insertion of one or several bonds, and/or one or several heteroatoms O and/or S and/or several aromatic cycles, and the pharmaceutically acceptable salts of said compounds. Said precursors and cyclized thiazolium derivatives are useful as antiparasitic medicines in particular antimalarial and antibabesiosis.
摘要:
New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;R.sub.1 is (C.sub.1 -C.sub.6) alkyl optionally substituted by a phenyl itself optionally substituted, a (C.sub.3 -C.sub.6) cycloalkyl, optionally substituted phenyl, furyl, thienyl or acyl;R.sub.2 is hydrogen, a halogen or a (C.sub.1 -C.sub.6) alkyl optionally substituted by amino or dialkylamino;R.sub.3 is hydrogen, (C.sub.1 -C.sub.6) alkyl optionally substituted by an aryl, or R--CO--(CH.sub.2).sub.n -- [n being 1, 2 or 3, and R being (C.sub.1 -C.sub.6) alkoxy, amino, (alkyl or dialkyl)amino, morpholino or methylpiperazinyl]; andX is hydrogen or a halogen.These compounds and their physiologically tolerated salts can be used in medical treatment of coronary smooth-muscle dysfunctions.
摘要翻译:新的咪唑并[1,2-c]喹唑啉化合物,可用作冠状平滑肌松弛剂,对应于下式:其中:Y为氧或硫; R 1是任选被苯基本身任选取代的(C 1 -C 6)烷基,(C 3 -C 6)环烷基,任选取代的苯基,呋喃基,噻吩基或酰基; R 2是氢,卤素或任选被氨基或二烷基氨基取代的(C 1 -C 6)烷基; R 3是氢,任选被芳基取代的(C 1 -C 6)烷基,或R-CO-(CH 2)n - [n是1,2或3,并且R是(C 1 -C 6)烷氧基,氨基,(烷基或 二烷基)氨基,吗啉代或甲基哌嗪基]; X是氢或卤素。 这些化合物及其生理耐受盐可用于治疗冠状动脉平滑肌功能障碍。