摘要:
Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R' wherein R' is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.
摘要:
Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R' wherein R' is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.
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