Abstract: Compounds of the general formula I ##STR1## wherein A is N; Ar is aryl, substituted aryl or benzofuranyl, wherein the substituents are selected from C.sub.1 -C.sub.8 alkoxy; B is CO or CH.sub.2 and HET is selected from any of piperizine, piperidine, hexahydroazepine, morpholine, thiomorpholine or pyrrolidine, which may be substituted with one of more oxo groups are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
Type:
Grant
Filed:
September 11, 1992
Date of Patent:
July 26, 1994
Assignee:
McNeilab, Inc.
Inventors:
Malcolm K. Scott, Allen B. Reitz, Frank J. Villani, Jr., C. Royce Rasmussen
Abstract: Novel 2,2,4-trialkyl-1,2-dihydroquinazoline-3-oxides and their synthesis are described. These compounds possess cardiotonic activity, and are useful for the treatment of heart failure.
Type:
Grant
Filed:
November 6, 1991
Date of Patent:
July 5, 1994
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Donald W. Combs, Robert Falotico, Victor Bandurco
Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
Abstract: Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I are also disclosed.
Type:
Grant
Filed:
September 11, 1992
Date of Patent:
May 24, 1994
Assignee:
McNeilab, Inc.
Inventors:
Malcolm K. Scott, Allen B. Reitz, Cynthia A. Maryanoff, Frank J. Villani, Jr.
Abstract: A process for converting 1,4- and 1,5-dicarbonyl sugars to pyrrolidine and piperidine amino sugars. Novel compounds resulting from this process are also described.
Type:
Grant
Filed:
September 17, 1990
Date of Patent:
March 1, 1994
Assignee:
McNeilab, Inc.
Inventors:
Allen B. Reitz, Ellen W. Baxter, Bruce E. Maryanoff
Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.
Abstract: Imidate derivatives of sulfamates having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and X are as herein defined have been found to be useful prodrug and exhibit anticonvulsant activity when converted to the active agent upon administration to a mammal and are thus useful in the treatment of conditions such as epilepsy. Further, the present invention encompasses pharmaceutical compositions containing a compound of formula (I) as well as methods for their use.
Abstract: A process for producing a compound of formula I: ##STR1## comprising reacting 5-(2-fluorophenyl)-1H-tetrazole with a Grignard reagent to produce the desired product is disclosed. Novel compounds produced by this process for use as intermediates in making certain angiotension II antagonists are also disclosed.
Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
Abstract: N-1 and C-5 heterocyclic pyrazoles, a method of their preparation, compositions containing the same and methods of their use are disclosed. The pyrazoles are useful in alleviating inflammatory and cardiovascular disorders in mammals.
Abstract: Compounds of the general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n and p are as herein defined; exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Compounds of this class are also useful for the treatment of glaucoma, peptic ulcers, hypertension, congestive heart failure and other types of edema. Furthermore, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.
Type:
Grant
Filed:
April 28, 1992
Date of Patent:
September 7, 1993
Assignee:
McNeilab, Inc.
Inventors:
Michael J. Costanzo, Bruce E. Maryanoff
Abstract: This invention relates to a tramadol N-oxide material, enantiomers and compositions thereof and their use. The tramadol N-oxide material and compositions thereof are pharmacologically useful in treating pain, diarrhea and tussive conditions. The tramadol N-oxide is also subject to less side-effects as compared to pure opiate based compositions, such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, the tramadol N-oxide material when administered orally exhibits analgesia for a longer duration than an equi-analgesic amount of tramadol.
Type:
Grant
Filed:
September 13, 1991
Date of Patent:
June 29, 1993
Assignee:
McNeilab, Inc.
Inventors:
Cynthia A. Maryanoff, Robert B. Raffa, Frank J. Villani
Abstract: Compounds of the general formula I: ##STR1## are disclosed as useful in the treatment or prevention of hypercholesterolemia, hyperlipoproteinemia and atherosclerosis. Novel intermediate compounds used to make the compound of formula I are also disclosed.
Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.
Abstract: Acetylene compounds of the formula (I): ##STR1## wherein Y, R.sub.1, R.sub.2 R.sub.3, and R.sub.4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess anti-hypertensive and anti-anginal properties and may be used in the treatment of humans. Methods for the preparation and use of such acetylene compounds are also disclosed.