Two Of The Cyclos Share At Least Three Ring Members Or A Ring Carbon Is Shared By Three Of The Cyclos (i.e., Bridged Or Peri-fused) Patents (Class 546/72)
Abstract: The invention relates to 4-acylamino-1-azaadamantanes represented by general formula (I): ##STR1## wherein R represents an alkyl group, a substituted alkyl group, an aryl group or a substituted aryl group, useful in particular, for the treatment of cardiovascular diseases.
Abstract: (+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]-cyclohepten-5,10-imine, and its pharmaceutically acceptable salts is useful as an anxiolytic, antidepressant, anticonvulsant, muscle relaxant and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease. The racemate of the compound is produced by a four-step synthetic process in about 65% yield from 5H-dibenzo[a,d]cyclohepten-5-one.
Type:
Grant
Filed:
September 3, 1982
Date of Patent:
October 16, 1984
Assignee:
Merck & Co., Inc.
Inventors:
Dean R. Bender, Sandor Karady, Theresa Rothauser
Abstract: 5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants.
Type:
Grant
Filed:
June 12, 1981
Date of Patent:
August 16, 1983
Assignee:
Merck & Co., Inc.
Inventors:
Paul Anderson, Marcia E. Christy, Ben E. Evans
Abstract: Dibenzo[a,d]cycloocten-5,12-(and 6,12)-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anxiolytics, antidepressants, anticonvulsants, muscle relaxants and in the treatment of mixed anxiety-depression, minimal brain dysfunction and extrapyramidal disorders such as Parkinson's disease.
Type:
Grant
Filed:
October 1, 1979
Date of Patent:
May 11, 1982
Assignee:
Merck & Co., Inc.
Inventors:
Paul S. Anderson, Marcia E. Christy, Ben E. Evans, David C. Remy
Abstract: A pyrido[3,2,1-jk]carbazol derivative represented by the formula (I) ##STR1## wherein R represents a hydroxy group, an alkoxy group which may be substituted with a halogen atom or with a 4-methyl-1-piperidinyl group, a hydrazino group or a ##STR2## group, Y represents an alkoxy group, a halogen atom, a nitro group, an amino group, an alkanoylamino group or alkyl group, and n is 0, 1 or 2; and the pharmaceutically acceptable salts thereof having antimicrobial, anti-cancer and antiviral activities, and a process for preparing the same.
Abstract: 10,11-Dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease. They are prepared by treatment of a 5H-dibenzo[a,d]cyclohepten-5-one with ammonia to give the 5-imine, acylation of the imine, treatment of the protected imine with an organolithium to provide the 5-substituted-5-acylamino compound, treatment with acid or base to cause ring closure to a 5-substituted-5,10-acylimino compound followed by removal of the protecting group, either hydrolytically or hydrogenolytically.
Abstract: Benzocycloheptapyridines with an imine bridge in the cycloheptane ring, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.
Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substituent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.
Abstract: The subject of the invention are dyestuffs of the formula ##STR1## wherein R is hydrogen or a hydrocarbon radicalQ is arylX is .dbd.C(W) -- or .dbd.N--,W is a nitrile ester or amide groups andA represents the remaining members of a heterocyclic radical.The dyestuffs are preferably suitable for dyeing polyester fibres which are dyed in orange, red, violet or bluish shades with good fastness to light.
Abstract: Compounds of the tropane (8-azabicyclo[3.2.1]octane) series having an aromatic substiutent in the 2-position and a carboalkoxy group in the 3-position are prepared by reacting a tropane-3-carboxylate having a double bond in the 2,3-position with an aryl Grignard reagent. Transformations of the substituent on nitrogen are subsequently effected. Compounds where the 3-carboalkoxy group is in the exo configuration possess hypoglycemic activity, and those where the 3-carboalkoxy group is in the endo configuration possess narcotic antagonist activity.
Abstract: Apomorphine derivatives are prepared in improved yield by rearrangement of the corresponding morphine derivative in the presence of anhydrous orthophosphoric acid under a partial vacuum and hydrolysis of the resulting phosphate esters in an aqueous medium.
Type:
Grant
Filed:
May 18, 1978
Date of Patent:
July 24, 1979
Assignee:
Sterling Drug Inc.
Inventors:
Roman R. Lorenz, Edward D. Parady, William H. Thielking