摘要:
The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ib in which n=1 or 2 and for n=1, X is chloride, bromide, triflate and hydrogen sulfate and for n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula II is stirred with a cysteine ester of the formula III, in which R1 is branched or linear C1-10-alkyl or where n=0, 1 or 2 and R2 is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
摘要:
Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the meanings stated in the description, their preparation and use as calpain inhibitors.
摘要:
Improved method of production of 9-(Z)-retinoic acid, in which a) a β-formyl-crotonic acid C1-C10 alkyl or phenyl ester is reacted with an isolated 9-(Z)—C15-triarylphosphonium salt by the Wittig reaction in the presence of a base to the corresponding 9-(Z)-retinoic acid ester; which b) is then saponified with a base to the corresponding 9-(Z)-retinoic acid carboxylate and then, following protonation with an acid, the desired 9-(Z)-retinoic acid is obtained, and improved method for the enrichment and isolation of the 9-(Z)—C15-triarylphosphonium salt.
摘要:
Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, and also possible physiologically tolerated salts, in which the variables have the meanings indicated in the description.
摘要:
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH═CH—, —C═C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, —NHSO2—C1-C4-alkyl and —SO2—C1-C4-alkyl; and Y is phenyl, pyridine, pyrimidine and pyrazine and R4 is hydrogen, COOR9 and CO—Z in which Z is NR10R11 and R9 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R10 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which itself may also be substituted by one or two R12 radicals, and R11 is hydrogen, C1-C6-alkyl, branched or unbranched, which may also be and substituted by a phenyl ring which may also carry an R9 radical, and R12 can be hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, J, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, —NHCO—C1-C4-alkyl, —NHCO-phenyl, —NHSO2—C1-C4-alkyl, NHSO2-phenyl, —SO2—C1-C4-alkyl and —SO2-phenyl, R13 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and R14 is hydrogen, C1-C6-alkyl, linear or branched, and which may [lacuna] substituted by a phenyl ring which may itself also be substituted by one or two R12 radicals, and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
摘要:
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts.
摘要:
Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the variables have the following meanings: R1 [sic] can be C1-C6-alkyl, phenyl, naphthyl, quinolyl, pyridyl, pyrimidyl, pyridazyl, quinazolyl and quinoxalyl, where the rings can additionally be substituted by up to 2 radicals R4 [sic], and R2 [sic] is —(CH2)m—R8 [sic], where R8 [sic] can be phenyl, cyclohexyl- or indolyl and m=1 to 6, and X is a bond, —CH2—, —CH2CH2—, —CH═CH—, —C≡C—, —CONH—, —SO2NH— [sic], and and [sic] R1—X [sic] together are also and R3 [sic] is hydrogen and CO—NR6R7 [sic], R4 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched and unbranched, and —O—C1-C4-alkyl [sic]; R5 [sic] is hydrogen, C1-C4-alkyl [sic], which is branched or unbranched, and —O—C1-C4-alkyl [sic]; R6 [sic] is hydrogen, C1-C6-alkyl, which is branched and unbranched, and R7 [sic] is hydrogen, C1-C6-alkyl, which is branched or unbranched, and n is is [sic] a number 0, 1 or 2.
摘要:
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m, —CH═CH—, —C≡C—, and Y is phenyl, pyridine, pyrimidine and pyrazine and n is a number 0, 1 or 2, and m,q are, independently of one another, a number 0, 1, 2, 3 or 4.
摘要:
Heterocyclically substituted amides of the general formula I wherein the variables as defined in the specification are useful in pharmaceuticals for the treatment of diseases in which increased interleuken-1 levels occur.
摘要:
Use of pyrimidine derivatives of the formula I where the substituents are as defined in the description, and of their physiologically tolerated salts for producing medicaments for the prophylaxis and treatment of cerebral ischemia and strokes.