Abstract: Cocaine analogs are disclosed. The analogs, certain 6-alkyl substituted tropane derivatives, bind to the cocaine binding site on dopamine transporter, without interfering with the dopamine receptor. The craving for cocaine is thereby blocked. The analogs may readily be synthesized stereoselectively, and are relatively resistant to metabolic degradation.
Type:
Grant
Filed:
March 9, 1998
Date of Patent:
November 10, 1998
Assignee:
Board of Supervisors of Louisiana State University and Agricultural and Mechanical College
Abstract: This invention provides novel bis-indolemaleimide macrocycle derivatives of the formula: ##STR1## wherein R.sub.1, R.sub.2, X, W, and Y are as defined in the specification. The invention further provides the preparation, pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Type:
Grant
Filed:
November 14, 1997
Date of Patent:
October 13, 1998
Assignee:
Eli Lilly and Company
Inventors:
Michael R. Jirousek, John H. McDonald, III, Christopher J. Rito
Abstract: Pyrimido?5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are:4-?(3-Chloro-4-fluorophenyl)amino!-6-?1-methyl-4-piperidinylamino!pyrimido? 5,4-d!pyrimidine, and4-?(3-Chloro-4-fluorophenyl)amino!-6-?trans-4-dimethyl-aminocycohexylamino! pyrimido?5,4-d!pyrimidine.
Type:
Grant
Filed:
March 5, 1997
Date of Patent:
October 13, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Georg Dahmann, Thomas von Ruden, Thomas Metz
Abstract: Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I): ##STR1## wherein R.sup.1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group;R.sup.2 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a C1-4 alkyl group;R.sup.5 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.6, R.sup.7 and R.sup.8 is independently a hydrogen atom or a C1-4 alkyl group;P is a hydroxyl group;Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group;P may form together with Q an ether bond;R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group;X is a single bond, an --NR.sup.
Abstract: The present invention relates to novel N-substituted naphthofused lactams and salts thereof of the formula ##STR1## Compounds of the general formula I possess the ability to stimulate the release of endogenous growth hormone. Thus, these compounds may be used in the treatment of conditions which require stimulation of growth hormone production or secretion such as in humans with growth hormone deficiency or where increased growth hormone plasma levels are desired, for instance in elderly patients or in livestock.
Type:
Grant
Filed:
January 29, 1997
Date of Patent:
October 6, 1998
Assignee:
Novo Nordisk A/S
Inventors:
Henning Thogersen, Birgit Sehested Hansen, Bernd Peschke, Thomas Kruse Hansen, Knud Erik Andersen
Abstract: This invention provides a series of substituted bisindole propanamides which are useful as tachykinin receptor antagonists and as serotonin agonists. This invention also provides methods for the treatment of related disorders as well as pharmaceutical formulations which employ these novel compounds.
Abstract: The present invention relates to new 2-Phenyl-1-?4-(amino-1-yl-alk-1-ynyl)benzyl!-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below.
Type:
Grant
Filed:
April 14, 1997
Date of Patent:
July 14, 1998
Assignee:
American Home Products Corporation
Inventors:
Chris P. Miller, Michael D. Collini, Bach D. Tran
Abstract: A compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3, which are identical or different, represent hydrogen, halogen, alkyl, nitro, cyano, aminosulfonyl, imidazolyl, or pyrrolyl, or alternatively, when two of them are situated on adjacent carbons, may form with the carbon atoms to which they are attached a benzene ring on C.sub.3 -C.sub.7 cyloalkylR.sub.4 represents hydroxyl, alkoxy, phenoxy, or amino,their isomers as well as their addition salts with a pharmaceutically-acceptable base, and medicinal products containing the same which are useful as inhibitors of the the pathological phenomena linked to hyperactivation of the neurotransmission pathways by the excitatory amino acids.
Type:
Grant
Filed:
July 10, 1997
Date of Patent:
July 7, 1998
Assignee:
Adir et Compagnie
Inventors:
Alex Cordi, Patrice Desos, Jean Lepagnol, Philippe Morain, Pierre Lestage
Abstract: The compound of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are centrally active muscarinic agents.
Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3 to R.sup.10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; R.sup.11 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.12 is hydrogen, C.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
June 30, 1998
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Francisco Javier Fernandez-Gadea, Victor Karel Sipido, Jose Ignacio Andres-Gil, Theo Frans Meert
Abstract: There is provided an improved method for the conversion of 5,6-dicarboxyl-3-pyridylmethyl ammonium halide to 5-(alkoxymethyl)pyridine-2,3-dicarboxylate salt via a single step closed reaction with the appropriate alcohol and a base at a temperature of about 120.degree.-180.degree. C.The product pyridinedicarboxylate salt is an important intermediate in the manufacture of pyridine imidazolinone herbicidal agents.