Abstract: 1-Arylsulphonyl, arylcarbonyl and arylthiocarbonyl pyridazino derivatives and processes for making said derivatives are described. The novel derivatives are non-steroidal heterocyclic compounds which act as selective progestins and/or antiprogestins having a high in-vitro affinity for either the uterine, breast or bone progestin receptor. As such, the non-steroidal heterocyclic derivatives are useful in contraception, menopause, osteoporosis or endometriosis.
Abstract: The present invention is directed to compounds of the following formula I: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, A, n, X, and Y are as defined hereinafter. The compounds of formula I are useful in treating central nervous system disorders. The compounds are ligands for the BZD binding site on GABA-A receptors, and are thus useful as muscle relaxants, hypnotics/sedatives including sleep-aids, anxiolytics, anticonvulsants/antiepileptics, anti-inebriants, and antidotes for drug overdose (particularly benzodiazepine overdose).
Type:
Grant
Filed:
February 16, 1995
Date of Patent:
June 17, 1997
Inventors:
Bruce E. Maryanoff, David F. McComsey, Winston Ho
Abstract: A granulation process for preparing a solid dosage form containing acetaminophen and diphenhydramine hydrochloride, as active agents is disclosed. In addition, the solid dosage form produced by the process is described.
Type:
Grant
Filed:
July 20, 1993
Date of Patent:
June 3, 1997
Assignee:
McNeil-PPC, Inc.
Inventors:
Kishor B. Parekh, Peter F. Eisenhardt, Robert Hitchner
Abstract: Novel benzylphosphonate compounds of the general formula I: ##STR1## are disclosed as useful in treating bone wasting diseases including postmenopausal osteoporosis in increasing in mammals bone formation and bone mass.
Type:
Grant
Filed:
December 9, 1993
Date of Patent:
July 2, 1996
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Keith Demarest, Charles Schwender, David Wustrow
Abstract: This invention relates to a composition comprising a tramadol material and a nonsteroidal antiinflammatory drug, and its use. The compositions are pharmacologically useful in treating pain and tussive conditions. The compositions are also subject to less opioid side-effects such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, where the components of the compositions are within certain ratios the pharmacological effects of the compositions are superadditive (synergistic).
Abstract: A compound of the general formula I: ##STR1## is disclosed as a potent anticonvulsant drug. Pharmaceutical compositions and methods of treatment are also disclosed.
Type:
Grant
Filed:
November 10, 1994
Date of Patent:
March 12, 1996
Assignee:
Ortho Pharmaceutical Corporation
Inventors:
Michael J. Costenzo, Bruce E. Maryanoff, David F. McComsey, Samuel O. Nortey
Abstract: This invention relates to compositions comprising a tramadol material selected from the group consisting of tramadol, its stereoisomers and its pharmaceutically acceptable salts and either codeine or oxycodone, and their use in treating pain. When the components, i.e., tramadol materials and either of codeine or oxycodone, of the composition are within certain ratios of pharmacological effects of the compositions are superaddditive (synergistic).
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: Sulfamate derivatives having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as herein defined, have been found to exhibit anticonvulsant activity 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 and novel intermediates are disclosed.
Type:
Grant
Filed:
December 22, 1992
Date of Patent:
January 24, 1995
Assignee:
McNeilab, Inc.
Inventors:
Michael J. Costanzo, 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: This invention relates to a composition comprising a tramadol material and acetaminophen, and its use. As used herein tramadol refers to various forms of tramadol. The compositions are pharmacologically useful in treating pain and tussive conditions. The compositions are also subject to less opioid side-effects such as abuse liability, tolerance, constipation and respiratory depression. Furthermore, where the components of the compositions are within certain ratios the pharmacological effects of the compositions are superadditive (synergistic).
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.
Abstract: Compounds of the general formula I: ##STR1## are disclosed as potent antipsychotic agents. Novel methods of use and intermediates used to make the compounds of formula I are also disclosed.