Divalent Chalcogen Or Acyclic Nitrogen Double Bonded At 2-position, Or Tautomeric Equivalent Patents (Class 514/392)
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Patent number: 5750553Abstract: A compound in all possible racemic, enantiomeric and diastereoisomer forms of the formula ##STR1## wherein Y is --O--, Z.sub.2 is --CF.sub.3, Z.sub.1 is --CN or --NO.sub.2, X is --O-- or --S--, R.sub.3 is hydrogen or alkyl of 1 to 4 carbon atoms optionally substituted by at least one halogen or --CN and R.sub.4 and R.sub.5 are individually alkyl of 1 to 4 carbon atoms optionally substituted with a member of the group consisting of halogen, --OH, esterified or etherified or protected hydroxy and phenylthio optionally substituted by halogen or --OH, and wherein at least one of R.sub.4 and R.sub.5 is substituted having antiandrogenic activity.Type: GrantFiled: June 27, 1996Date of Patent: May 12, 1998Assignee: Roussel UclafInventors: Andre Claussner, Francois Goubet, Jean Teutsch
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Patent number: 5744466Abstract: Compounds of formula (I) ##STR1## wherein R and R.sup.1 are hydrogen, C.sub.1-4 alkyl or are linked to form a ring,A is a cycloalkyl or alkyl-cycloalkyl group,n is an integer from 0 to 3,W is an optionally substituted 5-or 6-membered heterocyclic ring; or W is an optionally substituted aryl, heteroaryl, aryloxy or thiophenoxy group; orW is a group --SO.sub.2 NR.sup.6 R.sup.7 --NHC(O)R.sup.6 R.sup.7 or --C(O)NHR.sup.6 R.sup.7 ;are useful in treating clinical conditions for which a "5-HT.sub.1 -like" receptor agonist is indicated.Type: GrantFiled: October 7, 1996Date of Patent: April 28, 1998Assignee: The Wellcome Foundation LimitedInventors: Robert Charles Glen, David Lawrence Selwood, Graeme Richard Martin, Christopher James Foster
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Patent number: 5731311Abstract: N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11)R.sup.12);R.sup.Type: GrantFiled: December 12, 1996Date of Patent: March 24, 1998Assignee: Berlex Laboratories, Inc.Inventors: Raju Mohan, Michael M. Morrissey
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Patent number: 5719170Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.Type: GrantFiled: December 11, 1996Date of Patent: February 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5712282Abstract: A method for therapeutically treating tardive dyskinesia, which comprises a compound having an enzyme-inhibitory activity against a phospho-diesterase as the active ingredient, is now provided. Rolipram is preferred as the active ingredient. When rolipram is administered to such rats as experimental model, which have tardive dyskinesia induced by consecutive administrations of haloperidol, there can be obtained such curative effect that the symptoms of tardive dyskinesia are suppressed dose-dependently.Type: GrantFiled: October 9, 1996Date of Patent: January 27, 1998Assignees: Masaomi Iyo, Meiji Seika Kaisha, Ltd.Inventors: Masaomi Iyo, Hajime Sasaki, Yohko Maeda, Kenji Hashimoto, Toshiya Inada, Yoshie Kitao
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Patent number: 5703104Abstract: Compounds, topical compositions and methods useful for preventing the penetration of toxic chemicals through the skin of a mammal are disclosed.The compounds of the invention provide an enhanced barrier for the skin of a mammal to further inhibit or decrease the passage of bioactive agents through the skin of a mammal either from the outside environment into the systems of said mammal or from the mammal into the outside environment.Type: GrantFiled: July 3, 1996Date of Patent: December 30, 1997Assignee: Durham Pharmaceuticals LLCInventors: James V. Peck, Gevork Minaskanian, Mark C. Sleevi
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Patent number: 5698563Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises bis(guanylhydrazone) of the formula ##STR1## capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: January 13, 1995Date of Patent: December 16, 1997Assignee: Alteon Inc.Inventors: Dilip R. Wagle, Michael E. Lankin, David H. Shih
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Patent number: 5691369Abstract: The cyclic ureas, and the pharmaceutically-acceptable salts and esters thereof, of the present invention are useful as antiarrhythmic and antifibrillatory agents and have the following general structure: ##STR1## wherein X, Y, A, L, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are defined as in the Specification.Type: GrantFiled: June 7, 1995Date of Patent: November 25, 1997Assignee: The Proctor & Gamble CompanyInventors: Stanford Salvatore Pelosi, Jr., Chia-Nien Yu
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Patent number: 5679706Abstract: A method for the concomitant treatment of ischemia and arrhythmia in mammalian species which includes administering a combination of a potassium channel opener having little or no effect on action potential duration in the heart and a class III antiarrhythmic compound.Type: GrantFiled: September 30, 1994Date of Patent: October 21, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. D'Alonzo, Gary J. Grover
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Patent number: 5676978Abstract: The present invention provides for the use of creatine compounds and hyperplastic inhibitory agents for prophylactic and/or therapeutic treatments of undesirable cell growth, e.g. tumors. The present invention provides methods of using creatine compounds, in combination with a hyperplastic inhibitory agent, to inhibit the growth of undesirable cells in a subject. The present invention is based, at least in part, on the discovery that creatine compounds and hyperplastic inhibitory agents, such as inhibitory agents, additively and synergistically combine to inhibit cell growth. The present invention further pertains to compositions for inhibiting undesirable cell growth in a subject. The compositions of the present invention include an effective amount of the creatine compound and a hyperplastic inhibitory agent in a pharmaceutically acceptable carrier. Other aspects of the invention include packaged creatine compounds and inhibitory agents.Type: GrantFiled: January 21, 1994Date of Patent: October 14, 1997Assignees: Amira, Inc., Dana-Farber Cancer InstituteInventors: Beverly A. Teicher, Donald W. Kufe, Rima Kaddurah-Daouk
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5672622Abstract: The present invention is a method of preventing or ameliorating the episodic recurrence of MS, comprising administering an effective amount of selective phosphodiesterase inhibitors of Type IV, e.g., Rolipram, e.g., wherein the severity of the episodic recurrences is ameliorated or the time period between episodes is lengthened.Type: GrantFiled: October 21, 1994Date of Patent: September 30, 1997Assignee: Berlex Laboratories, Inc.Inventors: Joseph Hedgepeth, Helmut Wachtel
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Patent number: 5663053Abstract: Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.Type: GrantFiled: November 30, 1994Date of Patent: September 2, 1997Assignees: SmithKline Beecham Corporation, The Johns Hopkins UniversityInventors: James David Winkler, Deirdre Mary Bernadette Hickey, Floyd Harold Chilton, III
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Patent number: 5648373Abstract: Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme inhibits the production of these inflammatory mediators and will be of therapeutic utility in a broad range of allergic and inflammatory diseases and disorders. Compounds are described herein which inhibit the action of CoA-IT and are therefore useful in the treatment of disease states caused thereby.Type: GrantFiled: August 6, 1993Date of Patent: July 15, 1997Assignees: SmithKline Beecham Corporation, The Johns Hopkins UniversityInventors: James David Winkler, Floyd Harold Chilton, III, Deirdre Mary Bernadette Hickey
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Patent number: 5643921Abstract: In accordance with the present invention novel methods for cardiopulmonary bypass and organ transplant, each employing a potassium channel activator, are disclosed. The use of a potassium channel activator has been found to reduce the damage or ischemia induced by the bypass and transplant procedures.Type: GrantFiled: September 26, 1990Date of Patent: July 1, 1997Assignee: E.R. Squibb & Sons, Inc.Inventor: Gary J. Grover
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Patent number: 5624947Abstract: Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists.Type: GrantFiled: June 20, 1995Date of Patent: April 29, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Linda E. Keown, Tamara Ladduwahetty, Monique B. Van Niel
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Patent number: 5618793Abstract: Compounds of the formula ##STR1## wherein R.sub.3, R.sub.4, J, K, Z, and Het are as set forth herein are described.The compounds of formula I are useful as agents in the treatment of fungal infections.Type: GrantFiled: August 1, 1995Date of Patent: April 8, 1997Assignee: Schering CorporationInventors: Alan B. Cooper, Anil K. Saksena, Raymond Lovey, Viyyoor Girijavallabhan, Ashit Ganguly
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Patent number: 5612364Abstract: Compositions containing, and methods for controlling intraocular pressure with, substantially pure apraclonidine are disclosed.Type: GrantFiled: November 8, 1995Date of Patent: March 18, 1997Assignee: Alcon Laboratories, Inc.Inventors: Billie M. York, John M. Yanni, Mark T. DuPriest
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Patent number: 5612363Abstract: N,N-di(aryl) cyclic urea derivatives, such as the compounds of the following formula: ##STR1## wherein R.sup.1 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.11, --C(NH)N(H)C(O)R.sup.9, or --C(NH)N(H)C(O)OR.sup.11 ;R.sup.2 and R.sup.3 are independently hydrogen, halo, lower alkyl, lower haloalkyl, aryl, --OR.sup.11, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, --N(R.sup.11)R.sup.12, --N(H)C(O)R.sup.11, or --N(H)S(O).sub.2 R.sup.11 ;R.sup.4 is halo, lower haloalkyl, imidazolyl, --C(NH)NH.sub.2, --C(NH)NHOR.sup.11, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)C(O)OR.sup.11, --OR.sup.11, --C(O)R.sup.13, --(CH.sub.2).sub.n C(O)OR.sup.11 (where n is 0 to 6), --C(O)N(R.sup.11)R.sup.12, or --N(R.sup.11)R.sup.12 ;R.sup.7 and R.sup.8 are independently hydrogen, lower alkyl, lower haloalkyl, 4-pyridinyl, --C(O)OR.sup.11, --C(O)N(R.sup.11)R.sup.12, or aryl (optionally substituted by one or more substituents selected from the group consisting of halo, hydroxy, lower alkyl, lower haloalkyl, lower alkoxy and --N(R.sup.11 R.sup.12);R.sup.Type: GrantFiled: June 2, 1995Date of Patent: March 18, 1997Assignee: Berlex Laboratories, Inc.Inventors: Raju Mohan, Michael M. Morrissey
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Patent number: 5612362Abstract: Compounds of formula (I) and salts and prodrugs wherein Q.sup.1 is a specified aryl group, the dotted line is an optional double bond, Z is O or NR.sup.3, R.sup.1 and R.sup.3 are H or specified optionally substituted alkyl or other substituents and R.sup.2 is an optionally substituted phenyl or group are tachykinin receptor antagonists useful in medicine.Type: GrantFiled: April 18, 1995Date of Patent: March 18, 1997Assignee: Merck Sharp & Dohme Ltd.Inventor: Angus M. MacLeod
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Patent number: 5605922Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.Type: GrantFiled: December 12, 1995Date of Patent: February 25, 1997Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Verney L. Sallee
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Patent number: 5604228Abstract: N,N-disubstituted-guanidines, e.g., of the formula ##STR1## wherein R and R' are substituted or unsubstituted hydrocarbon groups. Methods are provided for the treatment of psychosis and hypertension by administering an effective amount of an N,N'-disubstituted guanidine which, preferably, has a high affinity for the sigma receptor.Type: GrantFiled: April 12, 1994Date of Patent: February 18, 1997Assignees: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University, University of OregonInventors: John F. W. Keana, Eckard Weber
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Patent number: 5604251Abstract: Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain, process for their preparation and their useCompounds of the formula (I) ##STR1## in which R.sup.1 is, for example, ethyl,R.sup.2 is, for example, methyl,n is, for example, zero,R.sup.3 is, for example, COOH, andR.sup.4 is, for example, SO.sub.2 NHCONHCH.sub.3are highly active antagonists of angiotensin II receptors.Type: GrantFiled: June 7, 1995Date of Patent: February 18, 1997Assignee: Hoechst AktiengesellschaftInventors: Holger Heitsch, Rainer Henning, Adalbert Wagner, Hermann Gerhards, Reinhard Becker, Bernward Sch olkens
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Patent number: 5599840Abstract: A nutritional composition, adapted for consumption by mammals, contains (1) an orally ingestible diluent or carrier, except an oily carrier or diluent which comprises C.sub.8-18 saturated fatty acids, oleic acid and derivatives of these acids, and (2) a composition of matter which consists of (a) from about 13.0 to about 27.5% by weight of at least one compound selected from linolenic acid and its salts, esters and amides, calculated as the free acid, and (b) about 87.0 to about 72.5% by weight of at least one compound selected from linoleic acid and its salts, esters and amides thereof, calculated as the free acid, the salts, esters and amides of linolenic and linoleic acid being both physiologically hydrolyzable and pharmacologically acceptable. The invention also relates to a method for treating a mammal for the purpose of inducing therein at least one physiological effect selected from memory enhancement and analgesia, by administration of an effective amount of the nutritional composition.Type: GrantFiled: November 13, 1995Date of Patent: February 4, 1997Assignee: Bar Ilan UniversityInventor: Shlomo Yehuda
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Patent number: 5567717Abstract: A compound of the formula ##STR1## wherein Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in the specification.Type: GrantFiled: June 5, 1995Date of Patent: October 22, 1996Assignee: Sterling Winthrop, Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
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Patent number: 5567725Abstract: Cyclohexanol esters of the formula I ##STR1## are described in which the radicals have the given meaning. The compounds are pharmacologically active and may therefore be used as pharmaceuticals, in particular for treating diabetes and other diseases which are characterized by an elevated secretion of glucose from the liver or by an elevated activity of the glucose-6-phosphatase system.Type: GrantFiled: February 14, 1995Date of Patent: October 22, 1996Assignee: Hoechst AktiengesellschaftInventors: Horst Hemmerle, Gerrit Schubert, Peter Below, Andreas Herling, Hans-J org Burger
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Patent number: 5556855Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.Type: GrantFiled: December 29, 1994Date of Patent: September 17, 1996Assignee: Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, G oran Smedeg.ang.rd, Lars-Inge Olsson
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Patent number: 5554610Abstract: A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a vasodilator selected from the group consisting of ganglion blockers, sympathetic nerve blockers, and direct vasodilators; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.Type: GrantFiled: August 24, 1994Date of Patent: September 10, 1996Assignee: Beecham Group p.l.c.Inventors: Andrew J. Williams, Derek R. Buckle
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5550141Abstract: A method is described for inhibiting the production of acid mine drainage from the disposal of sulphide tailings and waste rock deposition during mining and milling of sulphide containing ores, which comprises adding to said sulphide tailings or waste rock deposition an effective amount of 2-mercapto-1-methyl imidazole or a 1,3,4-thiadiazole selected from the group consisting of 2,5-dimercapto-1,3,4-thiadiazole and 5-amino-2-thiol-1,3,4-thiadiazole to inhibit oxidation of sulphides and thereby prevent the formation of acid mine drainage.Type: GrantFiled: August 31, 1995Date of Patent: August 27, 1996Assignee: Natural Resources - CanadaInventors: W. Douglas Gould, Lyne Lortie, Genevi eve B echard
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Patent number: 5545654Abstract: A compound of formula (I), in which each of R.sub.1 and R.sub.2 is independently hydrogen, alkyi or, together with the carbon atom to which it is bonded, a cycloalkyl; and each of R.sub.3 and R.sub.4 is independently hydrogen, alkyl or substituted alkyl. The compounds are useful intermediates and prodrugs.Type: GrantFiled: January 3, 1994Date of Patent: August 13, 1996Assignee: Biochemie Gesellschaft m.b.H.Inventor: Ingolf Macher
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Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5538988Abstract: The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4-tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H-imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.Type: GrantFiled: March 17, 1995Date of Patent: July 23, 1996Inventors: Gregory R. Martinez, Owen W. Gooding, David B. Repke, Philip J. Teitelbaum, Keith A. M. Walker, Roger L. Whiting
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Patent number: 5536740Abstract: Dimethyl imidazolidinone in combination with either retinol or retinyl ester resulted in a synergistic enhancement in keratinocyte proliferation and synergistic inhibition of keratinocyte differentiation. The effects of the retinol or retinyl esters in combination with dimethyl imidazolidinone were analogous to treatment with retinoic acid.Type: GrantFiled: June 1, 1995Date of Patent: July 16, 1996Assignee: Elizabeth Arden Company, Division of Conopco, Inc.Inventors: Stewart P. Granger, Anthony V. Rawlings, Ian R. Scott
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Patent number: 5523316Abstract: Improved ophthalmic irrigating solutions are described. The solutions include one or more drugs for controlling intraocular pressure, an antioxidant/free radical scavenger, electrolytes, a cellular energy source, bicarbonate, and a buffer. Methods of using the solutions in connection with ophthalmic surgical procedures are also described.Type: GrantFiled: June 23, 1994Date of Patent: June 4, 1996Assignee: Alcon Laboratories, Inc.Inventors: Owen Gan, Rajni Jani, Ole J. Lorenzetti
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Patent number: 5519039Abstract: A method and pharmaceutical composition are described for treatment of acne vulgaris which comprises administering to a patient suffering from acne vulgaris an effective amount of a pharmaceutical composition comprising pantothenic acid or a derivative thereof which generates pantothenic acid in the body to form Coenzyme A (CoA), nicotinic acid or a derivative thereof which generates nicotinamide adenine dinucleotide (NAD) or nicotinamide adenine dinucleotide phosphate (NADP) in the body, and biotin, or a mixture thereof.Type: GrantFiled: October 7, 1991Date of Patent: May 21, 1996Inventor: Lit-Hung Leung
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Patent number: 5510353Abstract: Compounds of formulaA--X--Y--NH--Bwherein A is derived from optionally substituted benzothiophene, indole, 4-aza-and 7-aza-benzothiophene or-indole, A bearing in position 5 hydrogen, halogen, optionally substituted alkyl, hydroxy, nitro, amino, alkylamino, acylamino, alkoxycarbonyl, sulfamoyl, cyano, trimethylsilyl, carboxy, carbamoyl, phosphate, oxycarbamoyl, heterocyclic radical or ether or ester group, X-Y is --CR.sub.8 .dbd.N-- or CH(R.sub.8)--NH-- wherein R.sub.8 is -H or alkyl and attached at position 3 of A, and B is a heterocyclic radical or a residue ##STR1## wherein R.sub.10 is H, optionally substituted alkyl, cycloalkyl, aryl, adamantyl, acyl or carbamoyl and X.sub.2 is alkylthio or NR.sub.3 R.sub.10 wherein R.sub.3 is H or alkyl or R.sub.3 and R.sub.10 together with the nitrogen atom to which they are attached form a heterocyclic radical, in free form or in salt form, have pharmacological activity, e.g. for treating gastrointestinal disorders.Type: GrantFiled: January 9, 1995Date of Patent: April 23, 1996Assignee: Sandoz Ltd.Inventors: Rudolf K. A. Giger, Henri Mattes
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5502052Abstract: Ophthalmic pharmaceutical compositions useful in controlling elevated intraocular pressure associated with glaucoma and other ophthalmic conditions are described. A method of controlling elevated intraocular pressure with those compositions is also described. The compositions contain a combination of an alpha-2 agonist (e.g., para-amino clonidine) and a beta blocker (e.g., betaxolol).Type: GrantFiled: December 22, 1994Date of Patent: March 26, 1996Assignee: Alcon Laboratories, Inc.Inventor: Louis M. DeSantis
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Patent number: 5494934Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Medicine products.Type: GrantFiled: November 4, 1991Date of Patent: February 27, 1996Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5484786Abstract: Compounds of structure ##STR1## where W is selected from ##STR2## where Q is oxygen or sulfur, R.sup.5 and R.sup.6 are independently selected from hydrogen and alkyl, or R.sup.5 and R.sup.6, together with the nitrogen atoms to which they are attached, define a radical of formula ##STR3## L.sup.1 and L.sup.2 are independently selected from a valence bond, alkylene, propenylene, and propynylene, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is oxygen, >NR.sup.9 where R.sup.9 is hydrogen or alkyl, or ##STR4## where n=0, 1, or 2, and A is selected from ##STR5## inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.Type: GrantFiled: August 24, 1993Date of Patent: January 16, 1996Assignee: Abbott LaboratoriesInventors: Joseph F. Dellaria, Anwer Basha, Lawrence A. Black, Linda J. Chernesky, Wendy Lee
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Patent number: 5482944Abstract: The compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein X, m, n, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined herein are useful in the treatment of shock and other TNF.alpha.-related disorders.Type: GrantFiled: July 13, 1993Date of Patent: January 9, 1996Assignee: Pfizer Inc.Inventors: Eric R. Pettipher, Victoria L. Cohan
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Patent number: 5480900Abstract: Combinations of at least one clonidine derivative and at least one prostaglandin are used to treat glaucoma and ocular hypertension without some of the side effects typically associated with topical administration of prostaglandins.Type: GrantFiled: April 10, 1995Date of Patent: January 2, 1996Assignee: Alcon Laboratories, Inc.Inventors: Louis DeSantis, Jr., Verney L. Sallee
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Patent number: 5462965Abstract: A class of heterocyclic amino-alcohol compounds is described for treatment of CNS-related diseases, namely, for use as a neuroprotective agent, to reduce neurotoxic injury associated with conditions of hypoxia, anoxia or ischemia which typically follows stroke, myocardial infarct, perinatal asphyxia, or hypoglycemic events. Other examples of treatable CNS-related diseases include neurodegenerative diseases such as Parkinson's disease, Huntington's chorea and Alzheimer's disease, and also psychotic disorders such as schizophrenia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as a mediator to alter excitatory actions at the NMDA excitatory amino acid receptor complex.Type: GrantFiled: December 7, 1992Date of Patent: October 31, 1995Assignee: GD Searle & Co.Inventors: Joseph L. Roba, Claude L. Gillet, Michael F. Rafferty, Bevyn Jarrott, Philip M. Beart
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Patent number: 5459153Abstract: A method and pharmaceutical composition are described for treatment of acne vulgaris which comprises administering to a patient suffering from acne vulgaris an effective amount of a pharmaceutical composition comprising pantothenic acid or a derivative thereof which generates pantothenic acid in the body to form Coenzyme A (CoA), nicotinic acid or a derivative thereof which generates nicotinamide adenine dinucleotide (NAD) or nicotinamide adenine dinucleotide phosphate (NADP) in the body, and biotin, or a mixture thereof.Type: GrantFiled: September 10, 1990Date of Patent: October 17, 1995Inventor: Lit-Hung Leung
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Patent number: 5455243Abstract: Fibrinogen receptor antagonists of the formula: ##STR1## such as ##STR2## are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.Type: GrantFiled: December 20, 1993Date of Patent: October 3, 1995Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, Nathan Ihle, George D. Hartman, Laura M. Turchi, William F. Hoffman
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Patent number: 5447947Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an .alpha.-adrenergic antagonist, .alpha.-1-adrenergic antagonist, .alpha.2 adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine. Examples demonstrate relief of pain by application of phentolamine or clonidine.Type: GrantFiled: June 25, 1992Date of Patent: September 5, 1995Assignee: ARC 1Inventor: James N. Campbell
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Patent number: 5430043Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: August 24, 1993Date of Patent: July 4, 1995Assignee: G. D. Searle & Co.Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers
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Patent number: 5416114Abstract: A composition of matter which consists of (a) from about 13.0 to about 27.5% by weight of at least one compound selected from the group consisting of linolenic acid and derivatives thereof, calculated as the free acid, said derivatives or linolenic acid being both physiologically hydrolyzable and pharmacologically acceptable, and (b) about 87.0 to about 72.5% by weight of at least one compound selected from the group consisting of linoleic acid and derivatives thereof, calculated as the free acid, said derivatives of linoleic acid being both physiologically hydrolyzable and pharmacologically acceptable, is utilized e.g. as a pharmaceutical formulation or nutritional composition, in absence of an oily carrier or diluent which comprises at least one member of the group consisting of C.sub.Type: GrantFiled: July 20, 1993Date of Patent: May 16, 1995Assignee: Bar Ilan UniversityInventor: Shlomo Yehuda
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Patent number: 5403841Abstract: Topical ophthalmic compositions of carrageenans which are administrable as a drop but which become more viscous or gel upon instillation in the eye are disclosed. Methods for use of the compositions as topical ophthalmic vehicles for pharmaceutically active agents, and alone as lubricants or tear supplements, are also disclosed.Type: GrantFiled: August 18, 1993Date of Patent: April 4, 1995Assignee: Alcon Laboratories, Inc.Inventors: John C. Lang, Jamieson C. Keister, Paul J. T. Missel, Dimitri J. Stancioff