摘要:
A process for preparing a chiral tetracyclic compound of formula (1), wherein R is hydrogen or a C1-C6-alkyl group and Z is oxygen, sulfur or -CH=CH-, the compounds having uses as dopamine agonists. The process involves reacting a chiral starting material and subsequent chiral intermediates in a series of chirality-preserving synthetic reactions.
摘要:
Novel compounds having formulas (I), (II) or (III) or pharmaceutically-acceptable salts or prodrugs thereof, which are useful for controlling synaptic transmission; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to controlling synaptic transmission in human or veterinary patients.
摘要:
Novel compounds having formulas (I), (II) or (III) or pharmaceutically-acceptable salts or prodrugs thereof, which are useful for controlling synaptic transmission; to therapeutically-effective pharmaceutical compositions of these compounds; and to the use of said compositions to controlling synaptic transmission in human or veterinary patients.
摘要:
Novel compounds are provided of formula (I), or a pharmaceutically acceptable salt, ester or amide thereof, wherein A is O, S, CHR2, CR2 or C when n is 0 and A and R6 taken together form a nitrogen-containing 5-, 6- or 7-membered ring, and n is zero or 1. The dotted lines represent optional double bonds. R1 is selected from hydrogen and a readily cleavable group. R2 is selected from hydrogen, alkyl, substituted alkyl, alkenyl and alkynyl. R3 is selected from alkyl, substituted alkyl, alkenyl, alkynyl, cycloalkyl, carbocyclic aryl, carbocyclic arylalkyl and heterocycle. R4 is selected from hydrogen and alkyl or, taken together with R3 and the carbon atom to which they are attached, forms a spirocycloalkyl ring of from 3 to 7 carbons. R5 is selected from hydrogen, alkyl and substituted alkyl or, taken together with R3 and the carbon atoms to which they are attached forms a cycloalkyl ring of from 5 to 7 carbons. R6 is selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, carbocyclic arylalkyl, alkanoyl of from 1 to 8 carbons, amino acid and dipeptide or, taken together with A when A is C and when n is 0, forms a nitrogen-containing 5-, 6-, or 7-membered ring. R7 is hydrogen or alkyl or, taken together with R6 or R8, forms a nitrogen-containing 5-, 6- or 7-membered ring, provided that when R6 is carbocyclic arylalkyl, R7 is not alkyl. R8 is hydrogen or alkyl or, taken together with R6 or R7, forms a nitrogen-containing 5-, 6-, or 7-membered ring or, taken together with the catechol ring at the 8-position and the carbon atoms to which they are attached, forms a 5-, 6- or 7-membered ring. The compounds of the invention are useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.
摘要:
L'invention concerne des nouveaux composés de la formule (I), où un sel, un esther ou un amide pharmaceutiquement acceptables de ceux-ci, dans laquelle A représente O, S, CHR2, CR2 ou C lorsque n est égal à 0, et A ainsi que R6 forment ensemble un anneau à 5, 6 ou 7 éléments contenant de l'azote, et n est égal à 0 ou à 1. Les lignes pointillées représentent des doubles liaisons facultatives. R1 est choisi entre l'hydrogène et un groupe facilement clivable. R2 est choisi entre hydrogène, alkyle, alkyle substitué, alcényle et alkynyle. R3 est choisi entre alkyle, alkyle substitué, alcényle, alkynyle, cycloalkyle, aryle carbocyclique, arylalkyle carbocyclique et un hétérocycle. R4 est choisi entre hydrogène et alkyle ou, pris avec R3 et l'atome de carbone auquel ils sont fixés, il forme un anneau spirocycloalkyle comportant 3 à 7 atomes de carbone. R5 est choisi entre hydrogène, alkyle et alkyle substitué ou, pris avec R3 et les atomes de carbone auxquels ils sont fixés, il forme un anneau cycloalkyle comprenant 5 à 7 atomes de carbone. R6 est choisi entre hydrogène, alkyle, acényle, alkynyle, cycloalkyle, arylalkylcarbocyclique, alcanoyle comportant 1 à 8 atomes de carbone, un acide aminé et bipeptide ou, pris ensemble avec A lorsque A représente C et lorsque n est égal à 0, il forme un anneau à 5, 6 ou 7 éléments contenant de l'azote. R7 représente hydrogène ou alkyle ou, pris avec R7 ou R8, il forme un anneau à 5, 6 ou 7 éléments contenant de l'azote, à condition que lorsque R6 représente arylalkyl carbocyclique, R7 ne représente pas alkyle. R8 représente hydrogène ou alkyle ou, pris avec R6 ou R7, il forme un anneau à 5, 6 ou 7 éléments contenant de l'azote, ou pris avec l'anneau de pyrocatéchine à la position 8 et les atomes de carbone auxquels ils sont fixés, il forme un anneau à 5, 6 ou 7 éléments. Les composés de l'invention sont utiles pour traiter les troubles neurologiques, psychologiques et cardiovasculaires liés à la dopamine, ainsi que dans le traitement de l'insuffisance cognitive, des troubles
摘要:
The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula (I) or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula (I) which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.
摘要:
A process for preparing a chiral tetracyclic compound of formula (1), wherein R is hydrogen or a C1-C6-alkyl group and Z is oxygen, sulfur or -CH=CH-, the compounds having uses as dopamine agonists. The process involves reacting a chiral starting material and subsequent chiral intermediates in a series of chirality-preserving synthetic reactions.
摘要:
The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula (I) or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula (I) which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.