摘要:
A compound of formula II' ##STR1## in which R.sub.I is an ethoxy group or a chlorine atom; R.sub.II is hydrogen, a chlorine atom or a methyl group; R.sub.III is a chlorophenyl group or a methoxyphenyl group; R.sub.IV is an amino group, a group NR.sub.9 R.sub.10 or NR.sub.9 R.sub.XI, or a piperazin-1-yl radical substituted in the 4-position by a (C.sub.2 -C.sub.10)alkylene group substituted by an amino group which is free or carries a protective group; R.sub.10 is (CH.sub.2).sub.p R.sub.35 or a (C.sub.2 -C.sub.10)alkylene group substituted by R.sub.21 ; R.sub.XI is a (C.sub.1 -C.sub.12)alkyl group or a group .omega.-R.sub.32 R.sub.33 N(C.sub.1 -C.sub.4)-alkylcarbonyl; and R.sub.21 is R.sub.36 ; a group OR.sub.37 ; a group NR.sub.32 R.sub.33 ; a cyano group; a group S(C.sub.1 -C.sub.7)alkyl; a group SO(C.sub.1 -C.sub.7)alkyl; or a group SO.sub.2 (C.sub.1 -C.sub.7)alkyl; R.sub.35 is a piperid-4-yl group which is unsubstituted or substituted in the 1-position by a (C.sub.1 -C.sub.7)alkoxycarbonyl group or by a (C.sub.1 -C.sub.7)alkyl group; or a pyrid-2-yl group; R.sub.37 is R.sub.13 ; a (C.sub.3 -C.sub.7)cycloalkyl group; a (C.sub.1 -C.sub.6)alkylene group substituted by R.sub.24 ; a (C.sub.2 -C.sub.6)alkylene group substituted by a hydroxyl or a (C.sub.1 -C.sub.7)alkoxy group; or a (C.sub.2 -C.sub.6)alkylene group substituted by an amino group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups or by a protective group; R.sub.24 is a carboxyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl group; a benzyloxycarbonyl group; or a carbamoyl group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups.
摘要:
The present invention deals with 4-amidino chroman and 4-amidino pyrano (3,2-c) pyridine derivatives, a process for their preparation and pharmaceutical compositions containing them. Said derivatives have antihypertensive and antiarythmic activities. They respond to formula ##STR1## in which: A+B=--CH.dbd.CH--CH.dbd.N-- ou --CH.dbd.CR.sub.4 --CR.sub.5 .dbd.CH--;X=N, N.fwdarw.O, C-Z;R.sub.1 =H, CN, NO.sub.2, C.sub.1 -C.sub.4 alkyl, OH, C.sub.1 -C.sub.4 alcoxy, CF.sub.3 CO--, CH.sub.3 --SO.sub.2 --,.rho.--SO.sub.2 --;R.sub.2 =H;R.sub.3 =OH ou OCOCH.sub.3ou R.sub.2 +R.sub.3 =double bond.
摘要翻译:本发明涉及4-脒基色满和4-脒基吡喃(3,2-c)吡啶衍生物,其制备方法和含有它们的药物组合物。 所述衍生物具有抗高血压和抗血栓活性。 它们响应式(I)其中:A + B = -CH = CH-CH = N-O -CH = CR4-CR5 = CH-; X = N,N-> O,C-Z; R1 = H,CN,NO2,C1-C4烷基,OH,C1-C4烷氧基,CF3CO-,CH3-SO2-, R2 = H; R3 = OH o OCOCH3 ou R2 + R3 =双键。
摘要:
The invention describes a method of synthesizing a compound of the formula ##STR1## in which X=O or NR,Z=an electron-attracting group,R=H, CN or NO.sub.2,R.sub.1 +R.sub.2 +N--C.dbd.X=a 5-membered or 6-membered heterocycle, andR.sub.3 =H, R.sub.4 =OH or R.sub.3 +R.sub.4 =a bond,said method involving intermediates of the formula ##STR2## in which R.sub.5 =H, Br or N(R.sub.1)CXR.sub.2. This method of synthesis does not involve the epoxide derivative of the chroman.The novel compounds of formula (IX) form a further subject of the invention.
摘要:
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要:
The present invention deals with 4-amidino chroman and 4-amidino pyrano (3,2-c) pyridine derivatives, a process for their preparation and pharmaceutical compositions containing them. Said derivatives have antihypertensive and antiarythmic activities. They respond to formula ##STR1## in which: A+B.dbd.--CH.dbd.CH--CH.dbd.N-- ou --CH.dbd.CR.sub.4 --CR.sub.5 .dbd.CH--; X.dbd.N,N.fwdarw.O, C--Z;R.sub.1 .dbd.H, CN, NO.sub.2, C.sub.1 -C.sub.4, alkyl, OH, C.sub.1 -C.sub.4 alkoxy, CF.sub.3 CO--, CH.sub.3 --SO.sub.2 --, .rho.--SO.sub.2 --;R.sub.2 .dbd.H;R.sub.3 .dbd.OH ou OCOCH.sub.3 ou R.sub.2 +R.sub.3 .dbd.double bond.
摘要翻译:本发明涉及4-脒基色满和4-脒基吡喃(3,2-c)吡啶衍生物,其制备方法和含有它们的药物组合物。 所述衍生物具有抗高血压和抗血栓活性。 它们响应式(I)其中:A + B = -CH = CH-CH = N-O -CH = CR4-CR5 = CH-; X = N,N-> O,C-Z; R1 = H,CN,NO2,C1-C4,烷基,OH,C1-C4烷氧基,CF3CO-,CH3-SO2-, R2 = H; R3 = OH o OCOCH3 ou R2 + R3 =双键。
摘要:
The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the V1b receptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要翻译:本发明涉及以下化合物:并且对V 1 B 1 N 2受体具有亲和力和选择性,并且对V 1b和V N 2 >精氨酸 - 加压素受体1a> 1a。 本发明还涉及制备它们的方法,可用于制备它们的式(II)中间体化合物,含有它们的药物组合物及其用于制备药用产品的用途。
摘要:
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要:
The invention relates to compounds of formula: as well as the possible salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, which have affinity for and selectivity towards the V1b receptors or towards both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to the process for preparing them, to the intermediate compounds of formula (II) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for the preparation of medicinal products.
摘要:
The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors.The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.
摘要:
The invention relates to compounds of formula: and to solvates and/or hydrates thereof, with affinity for and selectivity towards the Vreceptors or both the V1b and V1a receptors of arginine-vasopressin. The invention also relates to a process for preparing them, to the intermediate compounds of formula (II) which are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.