Abstract: Gemfibrozil formulations prepared from a single granulation of gemfibrozil and a release-control agent are disclosed. The release-control agent is present in an amount sufficient to provide both immediate and controlled release of gemfibrozil. A method of preparing the formulation and a compressed tablet are also disclosed.
Abstract: An anhydrous denture cleansing composition is disclosed comprising anhydrous perborate, a perborate monohydrate, a lubricant and compression aid, a monopersulfate, a sequestering agent, and, optionally, excipients, builders, colors, flavors, and surfactants.
Abstract: A novel process for the preparation of pharmaceutical compositions involving the stabilization of the active drug(s) through the reduction of residual alcohol present in a drug/carrier blend. The presence of residual alcohol in dried pharmaceutical compositions adversely affects many drugs which must be initially dissolved therein in order to achieve uniform distributions throughout the excipient carrier materials. Wherein not previously possible, its removal is achieved utilizing precise processing parameters in which water lost during the drying process is replenished during blending in a conventional solids processor.
Type:
Grant
Filed:
January 17, 1995
Date of Patent:
December 26, 1995
Assignee:
Warner-Lambert Company
Inventors:
Pankaj B. Gala, Gary D'Alonzo, Jatin J. Shah, Jay Weiss
Abstract: An anhydrous denture cleansing effervescent powder is disclosed comprising anhydrous perborate, a perborate monohydrate, a lubricant and compression aid, a monopersulfate, one or proteolytic enzymes, a sequestering agent, and, optionally, excipients, builders, colors, flavors, and surfactants.
Abstract: Novel methods of using thiazolidinone derivatives and related antihyperglycemic agents to treat populations at risk for developing noninsulin-dependent diabetes mellitus (NIDDM) and complications arising therefrom are disclosed. In one embodiment, the compounds of the invention are used to treat polycystic ovary syndrome in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus. In another embodiment, the compounds of the invention are used to treat gestational diabetes in order to prevent or delay the onset of noninsulin-dependent diabetes mellitus.
Type:
Grant
Filed:
August 23, 1994
Date of Patent:
October 10, 1995
Assignee:
Warner-Lambert Company
Inventors:
Tammy Antonucci, Dean Lockwood, Rebecca Norris
Abstract: The present invention discloses compounds which substantially inhibit HIV or the activation of HIV in HIV-infected individuals. The compounds, their derivatives, and pharmacologic salts may be formulated into a pharmacologic agent to treat HIV infections. These pharmacologic agents may be used to treat immunosuppression, and other diseases of the immune system. The present invention also provides methods for preparing the compounds and formulating the compounds into pharmacologic agents.
Type:
Grant
Filed:
December 19, 1994
Date of Patent:
August 22, 1995
Assignee:
Warner-Lambert Company
Inventors:
David T. Connor, Stephen J. Gracheck, Leonard Post
Abstract: The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT.sub.2 receptors to treat memory loss.
Type:
Grant
Filed:
April 13, 1994
Date of Patent:
August 22, 1995
Assignee:
Warner-Lambert Company
Inventors:
David T. Dudley, John C. Hodges, Thomas A. Pugsley, Michael D. Taylor
Abstract: Solid compositions of certain cholinergic compounds are stabilized in starch. Especially compositions of corn starch combined or mixed with the 0-substituted-1,2,5,6-tetrahydro-3-pyridine oxime ether, CI-979 HCl, a cognition activator, have been found stable in a heated environment of up to 60.degree. C. over 17 days such that no losses were detected by HPLC analysis. A solid peroral pharmaceutical formulation for the treatment of cognitive disorders is based on the bicomponent composition of active ingredient and stabilizer using appropriate amounts of other excipients or components known in the formulation art.
Type:
Grant
Filed:
February 1, 1993
Date of Patent:
June 13, 1995
Assignee:
Warner-Lambert Company
Inventors:
Hua-Pin Huang, Scott C. Wootton, Thomas N. Julian, Galen W. Radebaugh, Mahdi B. Fawzi
Abstract: Pharmaceutically useful compounds having acylcoenzyme A: cholesterol acyltransferase inhibitory activity having the general formula ##STR1## wherein Ar is di- or trisubstituted aryl or heteroaryl; R.sub.14 and R.sub.15 are each independently aryl, heteroaryl, hydrogen, fluorine, or alkyl, with the proviso that R.sub.14 and R.sub.15 are not both hydrogen, fluorine, or a straight or branched chain alkyl or a combination thereof; and R.sub.16 is a straight or branched hydrocarbon chain having 1 to 20 carbon atoms and is saturated or unsaturated and has 1 to 3 double bonds, the double bonds being adjacent or nonadjacent.
Abstract: Novel pharmaceutical compositions are comprised of the salt or ion pair formation of a non-steroidal anti-inflammatory drug and an antihistamine or other decongestant. The physico-chemical characteristics of these compositions show them to be substantially different from their parent acid or base and will enable the preparation of dual action sustained or enhanced relief therapy regimens. The compositions also possessed enhanced stability and therefore the multi-symptom relief can be incorporated into a number of dosage forms such as capsules, tablets, elixirs, ointments and the like.
Abstract: The present invention is directed to compounds of the following general Formula I, methods for using the compounds of Formula I, pharmaceutical compositions thereof, and processes for preparing the compounds. ##STR1## wherein X is oxygen or sulfur; wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl;wherein each of R.sub.1 and R.sub.2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a 5- or 6-membered monocyclic or fused bicyclic heterocyclic group, or a hydrocarbon chain having from 1 to 20 carbon atoms and from 1 to 3 double bonds.
Abstract: The present invention discloses the use of [R]-3-(2-deoxy-.beta.-D-erythropentofuranosyl)-3,6,7,8-tetrahydroimidazo-[ 4,5-d][1,3]diazepin-8-ol, also commonly known as pentostatin, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprised of such compounds, in the prophylactic or affirmative treatment of cerebral and cardiovascular disorders such as cerebral and myocardial ischemia. The invention also discloses the administration of pentostatin along with adenosine in the prophylactic or affirmative treatment of cerebral and cardiovascular disorders.
Abstract: Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R.sub.2 =R.sub.3 =H; R.sub.1 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, a heteroaromatic group or a hydrocarbon group having from one to 18 carbon atoms; R.sub.2 and R.sub.3 are hydrogen, halo, hydroxy, alkyl, alkenyl, cycloalkyl, phenyl, substituted phenyl, a heteroaryl, or form a spiroalkyl group; X is a heteromonocyclic 5-membered ring containing one to four heteroatoms, said heteroatoms being nitrogen, oxygen or sulfur, and combination thereof; and R.sub.4 is a hydrocarbon group having from one to 20 carbon atoms are described as well as methods of their manufacture.
Type:
Grant
Filed:
February 18, 1993
Date of Patent:
November 22, 1994
Assignee:
Warner-Lambert Company
Inventors:
Helen T. Lee, Patrick M. O'Brien, Joseph A. Picard, Claude F. Purchase, Jr., Bruce D. Roth, Drago R. Sliskovic, Andrew D. White
Abstract: Compounds of the formula ##STR1## wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl; wherein each of R.sub.1 and R.sub.2 is hydrogen, an aralkyl group, a straight or branched hydrocarbon group having from 1 to 20 carbon atoms and may be saturated or unsaturated, an alkyl group of from 1 to 6 carbon atoms wherein the terminal carbon is substituted, the group --(CH.sub.2).sub.p)--Q wherein p is zero to three and Q is a 5- or 6-membered monocyclic or fused bicyclic heterocycle, phenyl or NR.sub.1 R.sub.2 taken together form a monocyclic heterocyclic ring, and R.sub.3 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, --(CH.sub.2).sub.p --Q wherein p and Q are as defined above, an aralkyl group or a straight or branched hydrocarbon group having from 1 to 20 carbon atoms and being straight or branched, which compounds are useful in treating hypercholesterolemia.
Abstract: A solid composition for stabilizing the dosage of cognition activator CI-979 HCl by formation of a complex with cyclic polydextrose. In particular, compositions with HP.beta.CD have been found to stabilize CI-979 HCl even in the presence of other excipients such as sodium carbonate. Pharmaceutical formulations for the treatment of cognitive disorders in humans are based on the stabilizing composition of CI-979 HCl and cyclic polydextrose, including appropriate amounts of other excipients or components as known in the formulation art.
Type:
Grant
Filed:
February 1, 1993
Date of Patent:
November 8, 1994
Assignee:
Warner-Lambert Company
Inventors:
Hua-Pin Huang, Scott C. Wootton, Thomas N. Julian, Galen W. Radebaugh, Mahdi B. Fawzi
Abstract: Gemfibrozil formulations prepared from a single granulation of gemfibrozil and a release-control agent are disclosed. The release-control agent is present in an amount sufficient to provide both immediate and controlled release of gemfibrozil. A method of preparing the formulation and a compressed tablet are also disclosed.
Abstract: Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds which are azabicyclo[2.2.1]oximes, azabicyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes, and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms are disclosed.
Type:
Grant
Filed:
August 24, 1993
Date of Patent:
September 13, 1994
Assignee:
Warner-Lambert Company
Inventors:
Corinne E. Augelli-Szafran, Stephen D. Barrett, Bradley W. Caprathe, Adam A. Galan, Juan C. Jaen, David J. Lauffer, Walter H. Moos, Michael R. Pavia, Kathryn B. Sanders, Haile Tecle, Anthony J. Thomas
Abstract: Chiral compounds useful as radiosensitizers or chemosensitizers having the formula ##STR1## wherein X is halogen or ##STR2## intermediates used to prepare these compounds, and a novel process to prepare these compounds are described.
Type:
Grant
Filed:
August 5, 1993
Date of Patent:
August 30, 1994
Assignees:
Warner-Lambert Company, British Tech. Group
Inventors:
Vladimir Genukh Beylin, Anthony D. Sercel, Howard D. H. Showalter, Gerald E. Adams, Edward M. Fielden, Matthew A. Naylor, Ian J. Stratford
Abstract: The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT.sub.2 receptors.
Type:
Grant
Filed:
August 19, 1992
Date of Patent:
August 16, 1994
Assignee:
Warner-Lambert Company
Inventors:
David T. Dudley, John C. Hodges, Thomas A. Pugsley, Michael D. Taylor