Polycyclo Ring System Patents (Class 514/510)
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Patent number: 5733929Abstract: There is disclosed a pharmaceutical composition for treating or preventing allergic rhinitis which comprises a quinone or hydroquinone derivative having thromboxane A.sub.2 receptor antagonism. This compound is hardly inactivated by in vivo metabolism and can maintain its effective blood level for a long term and exhibit excellent pharmacological activity in a low dose.Type: GrantFiled: January 30, 1996Date of Patent: March 31, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Mitsuru Shiraishi, Yasuko Ashida, Tatsumi Matsumoto
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Patent number: 5723493Abstract: (1) Naphthyloxyaetic acid represented by the compound of the formula (I): ##STR1## and non-toxic salts thereof, (2) process for the preparation of the compounds represented by the compound of the formula (I) described hereinbefore,(3) PGE.sub.2 antagonist or agonist containing the compound represented by the compound of the formula (I) as the active ingredient.The compounds represented by the compounds of the formula (I) can be adapted to medicines which possess an inhibitory effect of uterine contraction, an analgesic action, an inhibitory effect of digestive peristalsis, a sleep-inducing effect as PGE.sub.2 antagonists, and an uterine contractile activity, a promoting effect of digestive peristalsis, a suppressive effect of gastric acid secretion, hypotensive activity as PGE.sub.2 agonists. The compounds bind to PGE.sub.2 receptor and have an activity of antagonist or agonist against the action thereof.Type: GrantFiled: December 17, 1996Date of Patent: March 3, 1998Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Takayuki Maruyama, Nobuyuki Hamanaka
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Patent number: 5716989Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.Type: GrantFiled: November 27, 1991Date of Patent: February 10, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl Heinz Thierauch, Peter Verhallen
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Patent number: 5708018Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.Type: GrantFiled: February 2, 1996Date of Patent: January 13, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Susanne R. Haadsma-Svensson, Bengt R. Andersson, Clas A. Sonesson, Chiu-Hong Lin, R. Nicholas Waters, Kjell A. I. Svensson, Per A. E. Carlsson, Lars O. Hansson, N. Peter Stjernlof
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Patent number: 5700833Abstract: The present invention provides novel isocarbacyclin derivatives useful for search and study of prostacyclin receptor and as a therapeutic drug for central nervous system diseases, which derivatives are expressed by the following formula ?I!: ##STR1## ?where, R.sup.1 represents a hydrogen atom, an alkyl group, or cation of an appropriate amount, and R.sup.2 an alkylene group.Type: GrantFiled: January 31, 1996Date of Patent: December 23, 1997Assignees: Research Developement Corporation of Japan, Atsuo HazatoInventors: Yasuyoshi Watanabe, Masaaki Suzuki, Atsuo Hazato, Bengt Langstrom
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Patent number: 5696152Abstract: A composition containing taxol for the ex vivo preservation or perfusion of organs for implantation in a subject requiring such implantation, or for cardioplegia, is disclosed.Type: GrantFiled: May 7, 1996Date of Patent: December 9, 1997Assignee: Wisconsin Alumni Research FoundationInventor: James H. Southard
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Patent number: 5691375Abstract: A method is provided for preventing or reducing the risk of onset of a cardiovascular event by administering an HMG CoA reductase inhibitor such as pravastatin, to a patient which has one or more risk factors for a coronary and/or cerebrovascular event such as hypercholesterolemia.Type: GrantFiled: May 23, 1995Date of Patent: November 25, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Bruce D. Behounek, Mark E. McGovern, Adeoye Y. Olukotun
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Patent number: 5686465Abstract: Inhibitors of sex steroid activity, for example those having the general structure ##STR1## may be used as part of a pharmaceutical composition to provide antiestrogenic effects and/or to suppress estrogen synthesis. Such pharmaceutical compositions are useful for the treatment of breast cancer or other diseases whose progress is aided by activation of sex steroid receptors.Type: GrantFiled: June 7, 1995Date of Patent: November 11, 1997Assignee: Endorecherche Inc.Inventors: Fernand Labrie, Yves Merand
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Patent number: 5681860Abstract: A composition for the upregulation of expression of cell antigens, without inducing shedding, which comprises a protein kinase C activator is provided by this invention. Further provided by this invention is a method of detecting and treating tumor cells comprising contacting tumor cells with an effective amount of a protein kinase C activator for the upregulation of expression of antigens of tumor cells, without inducing antigen shedding, and detecting the presence of said antigen or then further contacting said tumor cells with an effective amount of an antibody directed to said antigen.Type: GrantFiled: September 21, 1993Date of Patent: October 28, 1997Assignee: The Trustees of Columbia University in the City of New YorkInventors: Paul B. Fisher, Jorge A. Leon
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Patent number: 5679828Abstract: Some betulinic acid and dihydrobetulinic acid acyl derivatives according to the present invention have been found to have potent anti-HIV activity. Introducing a C.sub.2 -C.sub.20 substituted or unsubstituted acyl group at the C.sub.3 -hydroxy group of betulinic acid and dihydrobetulinic acid produces the corresponding 3-O-acyl derivatives. The compounds of the present invention have the following formulae: ##STR1## where R may be a mono- or dicarboxylacyl group, substituted or unsubstituted, of from about 2 to about 20 carbon atoms, and R' may be hydrogen or a C.sub.2 -C.sub.10 substituted and unsubstituted alkyl or aryl group.Type: GrantFiled: June 5, 1995Date of Patent: October 21, 1997Assignees: Biotech Research Labs, Inc., University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Yoshiki Kashiwada, Fumio Hashimoto, Louis Mark Cosentino, Mark Manak
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Patent number: 5677334Abstract: Glucagon antagonists and methods relating thereto are disclosed. The glucagon antagonists include skyrin and skyrin analogs, and serve to inhibit the stimulation of a glucagon-induced response pathway, such as the adenylate cyclase response pathway or the inositol phosphate response pathway. The glucagon antagonists may be used within therapeutic compositions to treat disease states associate with elevated glucose levels, including diabetes and hyperglycemia. The present invention also discloses a biologically pure culture of ATCC accession number 74200, as well as methods relating to the production of glucagon antagonists by cultivating the same in a nutrient medium and recovering the glucagon antagonist therefrom.Type: GrantFiled: September 11, 1995Date of Patent: October 14, 1997Assignee: ZymoGenetics, Inc.Inventors: Robert R. West, Virender Labroo, James R. Piggott, Robert A. Smith, Patricia A. McKernan
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Patent number: 5670143Abstract: The preferred oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a number average molecular weight of <10,000. These oligomers are water-soluble, have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geomentry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The oligomers are useful for the treatment and/or diagnosis of AIDS and ARC.Type: GrantFiled: May 19, 1995Date of Patent: September 23, 1997Assignees: Merrell Pharmaceuticals Inc., The Dow Chemical CompanyInventors: Alan D. Cardin, Richard L. Jackson, Michael J. Mullins
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Patent number: 5670673Abstract: An improved method for isolating taxol and certain clinically important analogues of taxol from a crude extract of a naturally occurring Taxus species comprising treating the extract by reverse phase liquid chromatography on an adsorbent, causing the taxol and the taxol analogues to be adsorbed on the adsorbent, and recovering taxol and the natural analogues of taxol from the adsorbent by elution with an elutant. The compounds thus isolated in pure form are taxol, taxol-7-xyloside, 10-deacetyltaxol, 10-deacetyltaxol-7-xyloside, cephalomannine, cephalomannine-7-xyloside, 10-deacetylcephalomannine-7-xyloside, baccatin III, 10-deacetylbaccatin III, baccatin VI, brevitaxane A, and taxiflorine.Type: GrantFiled: May 5, 1995Date of Patent: September 23, 1997Assignee: University of FloridaInventor: Koppaka V. Rao
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Patent number: 5663203Abstract: The invention relates to a dermal application form of prostacyclin derivatives of Formula I ##STR1## wherein R.sub.1 means hydrogen or alkyl of 1-10 carbon atoms,A is a --CH.sub.2 --CH.sub.2 --, trans-CH.dbd.CH-- or --C.ident.C-group,W represents a hydroxymethyl group which is free or functionally modified at the hydroxy group, the OH-group being in the .alpha.- or .beta.-position,X is a CH.sub.2 -group or an oxygen atom,Z is hydrogen or a cyano group,D means a straight-chain or branched, saturated alkylene group of 1-5 carbon atoms,E is a --C.ident.C-linkage or a direct bond,R.sub.2 is a straight- or branched-chain, saturated alkyl group of 1-7 carbon atoms,R.sub.3 is a free or functionally modified hydroxy group,and, if R.sub.1 means a hydrogen atom, containing the salts thereof with physiologically compatible bases, for the treatment of ulcerations caused by arterial occlusive diseases, and other skin disorders.Type: GrantFiled: November 30, 1994Date of Patent: September 2, 1997Assignee: Schering AktiengesellschaftInventors: Roland Ekerdt, Georg Raptis, Alfred Pauls
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Patent number: 5661145Abstract: Methods of reducing plasma cholesterol levels and treating or preventing atherosclerosis comprising administering an effective amount of a combination of a cholesterol biosynthesis inhibitor and a .beta.-lactam cholesterol absorption inhibitor, as well as pharmaceutical compositions and kits useful in those methods, are disclosed.Type: GrantFiled: June 20, 1995Date of Patent: August 26, 1997Assignee: Schering CorporationInventor: Harry R. Davis
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Patent number: 5658576Abstract: A method for combatting cellulitis or reducing localized fatty excesses involves administering a body slimming amount of a composition which contains, as the sole slimming agent, an .alpha.-tocopherol, benzyl, xanthinol or hexyl nicotinate, or .alpha.-tocopherol acetate.Type: GrantFiled: September 16, 1994Date of Patent: August 19, 1997Assignee: L'OrealInventor: Etienne Soudant
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Patent number: 5658947Abstract: A composition and method of inhibiting tumor growth and treating malignant melanoma without toxic side effects are disclosed. Betulinic acid or a betulinic acid derivative is the active compound of the composition, which is topically applied to the situs of tumor. Betulinic acid is obtained by the steps of preparing an extract from the stem bark of Ziziphus mauritiana to mediate selective cytotoxic profile against human melanoma in the subject panel of human cancer cell lines, conducting a bioassay-directed fractionation based on the profile of biological activity using cultured human melanoma cells as the monitor, and obtaining betulinic acid.Type: GrantFiled: March 21, 1995Date of Patent: August 19, 1997Assignee: Board of Trustees of the University of IllinoisInventors: Tapas K. DasGupta, John M. Pezzuto
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Patent number: 5650167Abstract: Disclosed is a method of inhibiting hepatitis B infection by administering a therapeutically effective amount of a compound having the formula (Formula 1): ##STR1## wherein R1 is selected from the group consisting of H, lower alkanoyl, lower arylalkylacyl, arylacyl, and C-1-linked saccharide, and R2 is separately selected from the group consisting of H, lower alkyl, lower arylalkyl, aryl, and C-1-linked saccharide. The compounds may also be used to treat other conditions, such as inflammatory bowel disease, autoimmune diseases, transplant rejection, septic shock, and for protection against irradiation damage. Novel celastrol derivatives are also disclosed.Type: GrantFiled: November 16, 1995Date of Patent: July 22, 1997Assignee: DAWA IncorporatedInventor: Anthony C. Allison
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Patent number: 5648355Abstract: A method for treating endogenous, painful gastrointestinal conditions of non-inflammatory, non-ulcerative origin, such as abdominal migraine and irritable bowel syndrome, entails administering a pharmacologically effective amount of a mast cell degranulation-blocking agent.Type: GrantFiled: February 9, 1994Date of Patent: July 15, 1997Assignee: KOS Pharmaceutical, Inc.Inventor: Theoharis C. Theoharides
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Patent number: 5639773Abstract: This invention relates to an ocular hypotensive agent which comprises a compound represented by the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon residue that may be bound via a hetero atom; R.sup.2 represents hydrogen or a hydrocarbon residue that may have a substituent; R.sup.3 represents a group capable of forming an anion or a group capable of changing thereto; X is a covalent bond between the 2 benzene rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n represents 1 or 2; ring A is a benzene ring having 1 or 2 optional substituents in addition to the group represented by COOR.sup.2, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1994Date of Patent: June 17, 1997Assignees: Senju Pharmaceutical Co., Ltd., Takeda Chemical Industries, Ltd.Inventors: Keiji Kubo, Takahiro Ogawa, Takaaki Deguchi
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Patent number: 5622985Abstract: A method is provided for preventing or reducing the risk of a second heart attack in a patient having a substantially normal serum cholesterol level by administering an HMG CoA reductase inhibitor such as pravastatin, alone or in combination with an ACE inhibitor.Type: GrantFiled: April 19, 1995Date of Patent: April 22, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Adeove Y. Olukotun, John C. Alexander
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Patent number: 5618538Abstract: Methods of obtaining renewable sources of taxanes including taxol are provided. Compositions comprising taxanes which are useful as source materials for the further purification of taxanes are also disclosed. Specifically, a method of drying plant matter to preserve their taxane content and facilitate their extraction is disclosed. In addition, methods of extracting and purifying taxol and other taxanes from ornamental cultivars using a series of organic and aqueous solvents and normal phase chromatography columns are also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: April 8, 1997Assignee: The University of MississippiInventors: Hala N. ElSohly, Edward M. Croom, Jr., Mahmoud A. ElSohly, James D. McChesney
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Patent number: 5605930Abstract: Compositions and methods of treating anemia, cancer, AIDS, or severe .beta.-chain hemoglobinopathies by administering a therapeutically effective amount of phenylacetate or pharmaceutically acceptable derivatives thereof or derivatives thereof alone or in combination or in conjunction with other therapeutic agents including retinoids, hydroxyurea, and flavonoids. Intravesicle methods of treatment of cancers phenylacetate. Pharmacologically-acceptable salts alone or in combinations and methods of preventing AIDS and malignant conditions, and inducing cell differentiation are also aspects of this invention. A product as a combined preparation of phenylacetate and a retinoid, hydroxyurea, or flavonid (or other mevalonate pathway inhibitor) for simultaneous, separate, or sequential use in treating a neoplastic condition in a subject. Methods of modulating lipid metabolism and/or reducing serum triglycerides in a subject using phenylacetate.Type: GrantFiled: March 7, 1994Date of Patent: February 25, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventor: Dvorit Samid
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Patent number: 5602181Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.Type: GrantFiled: October 12, 1994Date of Patent: February 11, 1997Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5597839Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: January 28, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William R. Pilgrim
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Patent number: 5576011Abstract: Described is a method for repelling insects such as houseflies, horn flies and mosquitoes using the cyclic organic alcohol defined according to the structure: ##STR1## and/or the mixture of cyclic organic carbonates defined according to the structures: ##STR2## and devices useful in carrying out such method.Type: GrantFiled: April 25, 1995Date of Patent: November 19, 1996Assignees: International Flavors & Fragrances Inc., The University of FloridaInventors: Jerry F. Butler, Anna B. Marin, Craig B. Warren, Richard A. Wilson, Braja D. Mookherjee
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Patent number: 5538997Abstract: The invention relates to compounds of formula I ##STR1## wherein the substituents have various significances. They can be prepared by conventional methods, e.g. coupling, substitution, deprotection or protection reactions.They possess interesting pharmacological properties and are thus indicated for use in the treatment of retroviral infections, particularly as HIV proteinase inhibitors.Type: GrantFiled: January 3, 1994Date of Patent: July 23, 1996Assignee: Sandoz Ltd.Inventors: Andreas Billich, Brigitte Charpiot, Peter Ettmayer, Hubert Gstach, Philipp Lehr, Dieter Scholz
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Patent number: 5538983Abstract: Various first messengers linked to phospholipase C, including acetylcholine and interleukin-1, regulate the production both of the secreted form of the amyloid protein precursor and of amyloid .beta.-protein. Intracellular signals which are responsible for mediating these effects have now been identified, and that activation of phospholipase C may affect APP processing by either of two pathways, one involving an increase in protein kinase C and the other an increase in cytoplasmic calcium levels. The effects of calcium on APP processing appear to be independent of protein kinase C activation. The observed effects of calcium on APP processing are of therapeutic utility in the treatment of Alzheimer-type amyloidosis.Type: GrantFiled: April 29, 1994Date of Patent: July 23, 1996Assignee: The Rockefeller UniversityInventors: Joseph D. Buxbaum, Paul Greengard
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Patent number: 5538986Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.Type: GrantFiled: December 6, 1993Date of Patent: July 23, 1996Assignee: Schering CorporationInventors: Pauline C. Ting, Daniel M. Solomon, Richard J. Friary, Frank J. Villani, John J. Piwinski, Joe F. Lee, Dhiru B. Vashi
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Patent number: 5525347Abstract: The invention provides a pharmaceutical composition for treating performance anxiety and social phobia comprising a therapeutic amount for the treatment of a patient of a .beta.-adrenergic receptor blocking compound and an anti-diaphoretic compound. The preferred .beta.-adrenergic receptor blocking compound is the lipophilic .beta.-blocker propranolol HCL. The anti-diaphoretic compound of the present invention is preferably glycopyrrolate. The composition for treating performance anxiety and social phobia can further include a pharmaceutically acceptable carrier. A method of preventing or treating performance anxiety or social phobia in a patient comprising administering the composition of the invention to a patient in need of such treatment is also provided. The composition administered in the present method comprises a therapeutic amount of a .beta.-adrenergic receptor blocking compound and an anti-diaphoretic compound.Type: GrantFiled: January 31, 1995Date of Patent: June 11, 1996Assignee: Medical University of South CarolinaInventors: Charles H. Kellner, Cherry W. Jackson, C. Lindsay DeVane
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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: 5508304Abstract: Glucagon antagonists and methods relating thereto are disclosed. The glucagon antagonists include skyrin and skyrin analogs, and serve to inhibit the stimulation of a glucagon-induced response pathway, such as the adenylate cyclase response pathway or the inositol phosphate response pathway. The glucagon antagonists may be used within therapeutic compositions to treat disease states associate with elevated glucose levels, including diabetes and hyperglycemia. The present invention also discloses a biologically pure culture of ATCC accession number 74200, as well as methods relating to the production of glucagon antagonists by cultivating the same in a nutrient medium and recovering the glucagon antagonist therefrom.Type: GrantFiled: August 10, 1994Date of Patent: April 16, 1996Assignee: ZymoGenetics, Inc.Inventors: Robert R. West, Virender Labroo, James R. Piggott, Robert A. Smith, Patricia A. McKernan
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Patent number: 5502076Abstract: Vitamin E acetate, C.sub.3 -linked triesters, glycerin, t-butanol, and transesterified oil/polyethylene glycol are effective dispersing agents for use with hydrofluoroalkanes. Effective amounts of the above are effective in suspending medicaments which are useful in inhalation aerosols, and especially meter-dose inhalers.Type: GrantFiled: March 8, 1994Date of Patent: March 26, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Suresh C. Dixit, David Goldman, John J. Hu, Krish Sethachutkul
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5491167Abstract: Compounds of formula (I): ##STR1## and their salts and esters have the ability to inhibit the synthesis of cholesterol, and can thus be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.Type: GrantFiled: January 31, 1994Date of Patent: February 13, 1996Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Hiroshi Kogen, Teiichiro Koga, Eiichi Kitazawa, Nobufusa Serizawa
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Patent number: 5491170Abstract: .beta.-Carboxy sulfonyl compounds of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 is hydrogen or alkyl, 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: February 13, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5484587Abstract: Baits for diabroticine beetles are microspherical particles containing a homogeneous mixture of a toxicant for diabroticine beetles and a feeding stimulant in a binder containing a gelatin and a gum. Preferred formulations include carbaryl and buffalo gourd root powder.Type: GrantFiled: October 31, 1991Date of Patent: January 16, 1996Assignee: Micro Flo CompanyInventors: Keith Branly, James M. Gaggero, Chel W. Lew, Cathy S. Lamb
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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Patent number: 5476846Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.Type: GrantFiled: November 17, 1994Date of Patent: December 19, 1995Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Claude Lardy, Daniel Guerrier, Gilles Chavernac, Francois Collonges
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5466711Abstract: A method for treating or preventing a Pneumocystis carinii infection in a mammal by administering a certain naphthoquinone compound or physiologically acceptable salts thereof.Type: GrantFiled: May 20, 1992Date of Patent: November 14, 1995Assignee: Burroughs Wellcome Co.Inventors: Victoria S. Latter, Winston E. Gutteridge, Alan T. Hudson
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Patent number: 5464866Abstract: Substituted hydrindanes and their use in controlling angiogenesis-dependent diseases in warm blooded animals are disclosed.Type: GrantFiled: March 10, 1994Date of Patent: November 7, 1995Assignee: Alcon Laboratories, Inc.Inventors: Abbot F. Clark, Raymond E. Conrow
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Patent number: 5459149Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.Type: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5459134Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein R.sup.4 represents:(i) when B represents a closed ring, a group of the general formula: ##STR2## wherein U represents an oxygen atom or a sulfur atom; or (ii) when B represents a divalent group, a group of the general formula: ##STR3## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, n, m, p and q are as defined in the specification, and exclusing certain compounds as defined in the specification, depending on whether A represents a single bond or a group. The compounds are useful for the prevention and/or treatment of diseases induced by leukotrienes, 5.alpha.-reductase, phospholipase and aldose reductase in mammals, especially human beings.Type: GrantFiled: October 21, 1994Date of Patent: October 17, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tsumoru Miyamoto, Yoshinobu Arai
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Patent number: 5455265Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.Type: GrantFiled: February 11, 1993Date of Patent: October 3, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5455273Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.Type: GrantFiled: November 19, 1993Date of Patent: October 3, 1995Assignee: Karl Thomae GmbHInventors: Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
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Patent number: 5451401Abstract: Polyphosphonic acid ester compounds with flavorant, coolant and/or sweetener components, and tartar, plaque and/or calculus control compositions with improved taste comprising one or more polyphosphonic acid ester compounds are described.Type: GrantFiled: September 29, 1993Date of Patent: September 19, 1995Assignee: The Procter & Gamble CompanyInventors: Kim W. Zerby, Jeffrey C. Hayes
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Patent number: 5446058Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein A represents a single bond or a group as defined in the specification;B represents(i) a substituted or unsubstituted carbocyclic ring of 4 to 8 members being unreplaced or optionally having one, two or three carbon atom(s) replaced by oxygen, nitrogen and/or sulfur atom(s); or(ii) a divalent group of formula: ##STR2## T represents oxygen or sulfur; R.sup.1 represents a group of general formula: ##STR3## or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s);R.sup.2 represents hydrogen or a straight or branched alkyl group of from 1 to 6 carbon atom(s);R.sup.' represents hydrogen, a halogen atom, a hydroxy group, a nitro group or a group --COOR.sup.7 ;R.sup.Type: GrantFiled: November 29, 1991Date of Patent: August 29, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
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Patent number: 5441983Abstract: A method for inhibiting cell infection by an enveloped virus, by administering to an infection site, a therapeutically effective amount of a calix(n)arene compound derivatized, at its ring positions meta to the bridge attachements to the ring, with polar substitutent having a terminal carboxylate, phosphate, or sulfonate groups, including esters and amides which are cleavable in vivo. The compound may be administered orally, or topically, e.g., for treatment of herpes virus.Type: GrantFiled: August 6, 1992Date of Patent: August 15, 1995Assignee: Genelabs IncorporatedInventors: Kou M. Hwang, You M. Qi, Su-Ying Liu, William Choy, Jen Chen