Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
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Patent number: 6017952Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.Type: GrantFiled: February 2, 1998Date of Patent: January 25, 2000Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Aiming Gao, Jia-Ning Xiang
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Patent number: 5997891Abstract: This invention relates to novel compositions containing temporary visual indicators and methods for using these compositions. Specifically, this invention relates to a sunscreen composition containing an indicator that is visible when the substance is applied to the skin, but becomes invisible shortly after application. The continued presence of the indicator allows the indicator to be reactivated temporarily to the visible form so that a user can verify the presence of the sunscreen. The visible indicator ensures that the sunscreen is applied evenly and completely to the area to be protected, but becomes invisible so as not to interfere with the action of the sunscreen or discolor the skin.Type: GrantFiled: August 18, 1998Date of Patent: December 7, 1999Assignee: IPA, LLCInventors: Ronnie S. Fuerst, Richard Melker, Christopher D. Batich
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Patent number: 5990160Abstract: The present invention concerns the use of puberulic or puberulonic acid as inhibitors of the enzyme iositol monophosphatase (EC 3.1.3.25) and thus useful in the treatment of manic or depressive symptoms.Type: GrantFiled: May 14, 1999Date of Patent: November 23, 1999Assignee: Gruppo Lepetit, SpAInventors: Khalid Islam, Stefania Stefanelli, Federica Sponga, Maurizio Denaro
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Patent number: 5985898Abstract: A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 16, 1998Date of Patent: November 16, 1999Assignee: Eli Lilly and CompanyInventor: Alan David Palkowitz
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Patent number: 5972936Abstract: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).Type: GrantFiled: May 20, 1997Date of Patent: October 26, 1999Assignee: Darwin Discover LimitedInventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 5965529Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.Type: GrantFiled: June 6, 1995Date of Patent: October 12, 1999Assignees: The Board of Regents, University of Texas, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
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Patent number: 5965608Abstract: Synthetic derivatives or intermediates of xylomollin are identified which can be used as insect feeding deterrents. The identified derivatives or intermediates exhibiting antifeeding activity include glutaraldehyde and carbocyclic or heterocyclic dialdehydes wherein the aldehyde groups are positioned on adjacent carbons of the carbocyclic or heterocyclic rings. The active compounds also include the hemiacetal hemiacetal equivalents, the acetal hemiacetal equivalents and the vinyl ether equivalents of the dialdehydes.Type: GrantFiled: July 21, 1998Date of Patent: October 12, 1999Assignee: Rockhurst UniversityInventor: Don E. Gibbs
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Patent number: 5962413Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or a prostaglandin.Type: GrantFiled: September 22, 1997Date of Patent: October 5, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5948762Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or-oxytocin analogue antagonist or a prostaglandin.Type: GrantFiled: July 17, 1997Date of Patent: September 7, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5942546Abstract: A compound of the formula: ##STR1## wherein X is arylene, heteroarylene, fused arylene, fused heteroarylene, or deleted; Y is sulfonyl, --O--, or deleted; R.sub.1 is aryl, heteroaryl, fused aryl, or fused heteroaryl; R.sub.2 is H, lower alkyl, lower alkoxy, halo, nitro, cyano, haloalkyl, hydroxyl, carboxyl, amido, amino, or aminoalkyl; or a salt thereof are disclosed. Also disclosed are a pharmaceutical composition which contains an excipient and an effective amount of a compound of the above formula and a method of treating cancer which involves the administration of an effective amount of such a compound to a patient in need thereof.Type: GrantFiled: November 20, 1997Date of Patent: August 24, 1999Assignee: Development Center for BiotechnologyInventors: Ji-Wang Chern, Yu-Ling Leu, Shan-Shue Wang, Chin-Fen Lee, Shih-Chung Hsu
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Patent number: 5929121Abstract: A method for the protection of trees of the families Musaceae or Plantanginaceae from destructive pests whereby the trees to be protected share a common root system.Type: GrantFiled: December 13, 1996Date of Patent: July 27, 1999Assignee: Rhone-Poulenc AgroInventors: Jorge Cepeda, Juan Bocanegra
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Patent number: 5922760Abstract: An agent for the prevention or alleviation of allergy symptoms contains as an effective component a dioxabycyclo?3.3.0!octane derivative represented by the following general formula (I): ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently represent a hydrogen atom or alkyl group of 1-3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 together represent a methylene or ethylene group, and n, m and l represent 0 or 1.An agent for the prevention or alleviation of allergy symptoms also contains as an effective component an antioxidant in addition to the dioxabicyclo?3.3.0!octane derivative.Type: GrantFiled: June 19, 1997Date of Patent: July 13, 1999Assignee: Suntory LimitedInventors: Kengo Akimoto, Michihiro Sugano, Koji Yamada, Michiko Nonaka, Jiong-Yan Gu
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Patent number: 5919800Abstract: The present invention provides a method for inhibiting endometriosis comprising administering to a woman an effective amount of a compound of formula I ##STR1## wherein R.sup.1a is --H or --OR.sup.7a in which R.sup.7a is --H or a hydroxy protecting group;R.sup.2a is --H, halo, or --OR.sup.8a in which R.sup.8a is --H or a hydroxy protecting group;R.sup.3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andZ is --O-- or --S--;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 3, 1995Date of Patent: July 6, 1999Assignee: Eli Lilly and CompanyInventor: Alan David Palkowitz
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Patent number: 5906987Abstract: The symptoms of climacterium in male mammals, e.g., hypertension, cardiovascular disease and osteoporosis, are ameliorated by the administration to an afflicted individual one or both of a nitric oxide substrate and/or nitric acid donor, in combination with an androgen, an aromatase inhibitor or both, wherein the circulating levels of testosterone in the afflicted individual are increased.Type: GrantFiled: March 10, 1997Date of Patent: May 25, 1999Assignees: Schering Aktiengesellschaft and Board of Regents, The University of Texas SystemInventors: Kristof Chwalisz, Robert E. Garfield
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Patent number: 5889046Abstract: The present invention discloses a preventive or ameliorant of hypertension or medical symptoms caused by it and a food or beverage that prevents or ameliorates hypertension or medical symptoms caused by it that contain for its active ingredient dioxabicyclo?3.3.0!octane derivative represented by the formula (2). ##STR1## wherein, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are respectively and independently a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 collectively represent a methylene group or ethylene group, and n, m and L represent 0 or 1.Type: GrantFiled: February 1, 1996Date of Patent: March 30, 1999Assignee: Suntory LimitedInventors: Kengo Akimoto, Shiro Morimoto, Yasuo Matsumura, Hajime Yoshizumi, Tetsuo Murakami
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Patent number: 5852052Abstract: The invention refers to the treatment and prevention of lyso paf-mediated disorders with an effective amount of at least one antagonists against lyso paf receptors. Lyso paf or paf receptor antagonists were administered with or without an antagonist against production of ether phospholipids. Lyso paf antagonists are Ginkgoloides which are administered, for example, by food or topically.Type: GrantFiled: December 9, 1996Date of Patent: December 22, 1998Assignee: Ruth KorthInventor: Ruth Korth
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Patent number: 5837645Abstract: This invention relates to novel compositions containing temporary visual indicators and methods for using these compositions. Specifically, this invention relates to a sunscreen composition containing an indicator that is visible when the substance is applied to the skin, but becomes invisible shortly after application. The continued presence of the indicator allows the indicator to be reactivated temporarily to the visible form so that a user can verify the presence of the sunscreen. The visible indicator ensures that the sunscreen is applied evenly and completely to the area to be protected, but becomes invisible so as not to interfere with the action of the sunscreen or discolor the skin.Type: GrantFiled: July 1, 1996Date of Patent: November 17, 1998Inventors: Ronnie S. Fuerst, Richard Melker, Christopher D. Batich
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Patent number: 5827879Abstract: This invention provides certain substituted 2,3-dihydrobenzofurylsulfonamide derivatives and methods for using them in the treatment of susceptible neoplasms in mammals. Also provided are certain novel pharmaceutical formulations employing these benzenesulfonamide derivatives in combination with a carrier.Type: GrantFiled: October 3, 1997Date of Patent: October 27, 1998Assignee: Eli Lilly and CompanyInventors: William J. Ehlhardt, James E. Ray, John E. Toth
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Patent number: 5817683Abstract: Naphthoic derivatives of the Formula (I) ##STR1## wherein the variables are defined herein; and pharmaceutical compositions containing these compounds, and their use as endothelin receptor antagonists are disclosed.Type: GrantFiled: April 8, 1996Date of Patent: October 6, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Jia-Ning Xiang
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Patent number: 5817653Abstract: Novel compounds of the formula: ##STR1## are disicosed which are endothelin receptor antagonists.Type: GrantFiled: April 12, 1996Date of Patent: October 6, 1998Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, John Gerald Gleason, David Taylor Hill
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Patent number: 5814661Abstract: A therapeutical method for treating endotoxic shock which comprises administering to a patient in need thereof a (3-phthalidyliden) alkyl ester of carnitine or alkanoyl carnitine, is disclosed.Type: GrantFiled: September 19, 1995Date of Patent: September 29, 1998Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Vito Ulderico Ruggiero, Piero Foresta
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Patent number: 5804598Abstract: Synthetic derivatives or intermediates of xylomollin are identified which can be used as insect feeding deterrents. The identified derivatives or intermediates exhibiting antifeeding activity include glutaraldehyde and carbocyclic or heterocyclic dialdehydes wherein the aldehyde groups are positioned on adjacent carbons of the carbocyclic or heterocyclic rings. The active compounds also include the hemiacetal hemiacetal equivalents, the acetal hemiacetal equivalents and the vinyl ether equivalents of the dialdehydes.Type: GrantFiled: March 20, 1997Date of Patent: September 8, 1998Assignee: Rockhurst UniversityInventor: Don E. Gibbs
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Patent number: 5792763Abstract: This invention provides novel 5-HT.sub.1F agonists of formula ##STR1## where X, Y, Z,and R are defined in the specification, which are useful for the prevention and treatment of migraine and associated disorders.Type: GrantFiled: September 26, 1997Date of Patent: August 11, 1998Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Stephen W. Kaldor, Sidney Xi Liang, Upinder Singh, Yao-Chang Xu
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Patent number: 5773463Abstract: This invention describes the use of aminoindane and amino-tetrahydronaphthalene derivatives of general formula (I) ##STR1## in which Ar, X, R.sub.1, R.sub.2 and n are defined in claim 1, for the manufacture of a medicament for the treatment of disorders in which a calcium channel antagonist is indicated. Novel compounds falling within formula (I) are also claimed.Type: GrantFiled: January 22, 1996Date of Patent: June 30, 1998Assignee: SmithKline Beecham p.l.c.Inventors: John David Harling, Barry Sidney Orlek
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Patent number: 5728696Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: June 5, 1995Date of Patent: March 17, 1998Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5726208Abstract: New compounds of formula: ##STR1## wherein: --A--D--E, X, n, Y and Z are as defined in the description, in racemic form and in the form of optical isomers,and their addition salts with pharmaceutically acceptable acids.Those compounds may be used as medicaments.Type: GrantFiled: October 11, 1996Date of Patent: March 10, 1998Assignee: Adir et CompagnieInventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
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Patent number: 5723469Abstract: The present invention provides an agricultural or horticultural fungicide including an effective amount of an amino-acid derivative represented by the formula: ##STR1## wherein R.sup.1 represents a lower alkyl group (optionally having at least one same or different substituent of a halogen atom, an alkoxy group, and a cyano group), R.sup.2 represents an ethyl group, or an n-propyl group, R.sup.3 represents a hydrogen atom or a lower alkyl group, R.sup.4 represents a hydrogen atom, R.sup.5, R.sup.6, and R.sup.7 independently represent a hydrogen atom or a lower alkyl group, R.sup.8 represents a hydrogen atom, or a lower alkyl group, Z.sup.1 and Z.sup.2 independently represent an oxygen atom or a sulfur atom, Z.sup.3 represents an oxygen atom, or a sulfur atom, Q represents a phenyl group, m represents an integer from 0 to 2, and n represents 0 or 1.Type: GrantFiled: July 11, 1996Date of Patent: March 3, 1998Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
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Patent number: 5716624Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 15, 1994Date of Patent: February 10, 1998Assignee: C.I.R.D. GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5693676Abstract: A pharmaceutical composition contains a nitric oxide donor and advantageously an optional corticosteroid and/or topical anesthetic. The composition is useful in a method for treating anal disorders such as anal fissure, anal ulcer, hemorrhoidal disease, levator spasm, and so forth, by topical application to or proximate the affected area.Type: GrantFiled: June 20, 1996Date of Patent: December 2, 1997Assignee: Neptune Pharmaceutical CorporationInventor: Stephen R. Gorfine
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Patent number: 5684033Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: June 5, 1995Date of Patent: November 4, 1997Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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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: 5674876Abstract: The present invention provides an antiproliferative p-heteroatom-substituted phenol compound having the structure formula ##STR1## wherein m is 0 to 3, n is 0 to 4 when Het is nitrogen, wherein R is selected from the group consisting of hydrogen, alkyl, arylmethyl and acyl; R.sup.1 is alkyl; R.sup.2 is selected from the group consisting of hydrogen and alkyl; R.sup.3 is selected from the group consisting of alkyl and acyl when Het is nitrogen, R.sup.4 is selected from the group consisting of hydrogen and alkyl; R.sup.5 is selected from the group consisting of hydrogen and alkyl; and R.sup.6 and R.sup.7 are selected from the group consisting of hydrogen, alkyl and R.sup.6 and R.sup.7 together may represent oxygen. Also provided are various methods for the treatment of a pathological cell proliferative disease comprising administering to an animal) a pharmacologically and therapeutically effective dose of a pharmaceutical composition comprising a p-heteroatom-substituted phenols or an analog thereof.Type: GrantFiled: January 20, 1995Date of Patent: October 7, 1997Assignee: Research Development FoundationInventors: John C. Gilbert, Kimberly Kline, Kathiresan Krishnan, Maria Simmons Menchaca, Marian Pinto, Robert G. Sanders
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Patent number: 5665766Abstract: A pharmaceutical product for the relief of the symptoms of angina pectoris and the like comprises an ester of an organic nitrate and a salicylate or derivative thereof having anti-platelet activity.Type: GrantFiled: January 30, 1995Date of Patent: September 9, 1997Assignee: Cal International LimitedInventors: William Byrne, Andrew Rynne
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Patent number: 5663192Abstract: This invention provides methods for treating or preventing a condition associated with an excess of neuropeptide Y which methods comprise administration of one or more substituted benzofurans, benzothiophenes or indoles.Type: GrantFiled: October 20, 1994Date of Patent: September 2, 1997Assignee: Eli Lilly and CompanyInventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
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Patent number: 5656659Abstract: The present invention is directed to compounds which suppress immune responses and/or selectivly inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the phamaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activites, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.Type: GrantFiled: November 18, 1994Date of Patent: August 12, 1997Assignees: T Cell Sciences, Inc., The University of MississippiInventors: Robert D. Sindelar, Barton J. Bradbury, Teodoro Saul Kaufman, Stephen Hoi-Chuen Ip, Henry Clinton Marsh, Jr., Chew Lee
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Patent number: 5646181Abstract: Pharmaceutical compositions in topical or parenteral form containing organic nitrites are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the nitrite-containing compositions are also disclosed, as are certain novel organic nitrite compounds.Type: GrantFiled: May 2, 1995Date of Patent: July 8, 1997Assignee: Research Foundation of State University of New YorkInventors: Ho-Leung Fung, John Anthony Bauer
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Patent number: 5643944Abstract: The stimulation of ovulation in a female may be achieved by administering a nitric oxide source, optionally in further combination with one or more of clomiphene, a gonadotropin, and an LH-RH agonist.Type: GrantFiled: June 7, 1995Date of Patent: July 1, 1997Assignee: Board of Regents, The University of Texas SystemInventors: Robert E. Garfield, Chandrasekhar Yallampalli
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Patent number: 5637610Abstract: A food, drink, pharmaceutical, cosmetic composition or food additive comprising a dioxabicyclo[3.3.0]octane derivative represented by the following general formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represent a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 and/or R.sup.4 and R.sup.5 together form a methylene group or an ethylene group, and n, m and l are 0 or 1; and antioxidant.Type: GrantFiled: June 20, 1994Date of Patent: June 10, 1997Assignee: Suntory LimitedInventors: Ayako Nakabayashi, Yoshinori Kitagawa, Kengo Akimoto, Michihiro Sugano
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5627200Abstract: This invention relates to methods for treating intestinal motility disorders, intestinal ulcerations, including inflammatory bowel disease, ulcerative colitis, Crohn's disease and proctitis, and gastrointestinal ulcerations, depression, prostate disease and dyslipidemia by administering a .beta..sub.3 -adrenoceptor antagonist or agonist.Type: GrantFiled: September 26, 1994Date of Patent: May 6, 1997Assignee: Pfizer IncInventors: David K. Kreutter, Robert L. Dow
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Patent number: 5622989Abstract: 6-Amino-benzofuryl- and thienyl-derivatives can be prepared by reacting appropriate amino-substituted benzoyl phenols with appropriate substituted acetophenones and subsequent modification of the substituents. The compounds are useful for the treatment of actual and chronic inflammatory diseases, particularly of the airways and the gastro-intestinal tract.Type: GrantFiled: May 23, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Gabriele Br aunlich, R udiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
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Patent number: 5612368Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar, X, R.sub.1 and R.sub.2 are as defined in the description and a medicinal product containing the same in order to treat a disorder of the melatoninergic system.Type: GrantFiled: October 25, 1995Date of Patent: March 18, 1997Assignee: Adir et CompagnieInventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
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Patent number: 5589505Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle quinic acid or a topically effective salt thereof, or quinolactone.Type: GrantFiled: June 5, 1995Date of Patent: December 31, 1996Assignee: Tristrata Technology, Inc.Inventors: Ruey J. Yu, Eugene J. Van Scott
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Patent number: 5576332Abstract: New soft .beta.-adrenergic blocking agents, useful in the treatment or prevention of cardiovascular disorders and in the treatment of glaucoma, have the formula ##STR1## wherein n is an integer from 0 to 10; R is C.sub.6 -C.sub.12 cycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkyl-C.sub.p H.sub.2p --, C.sub.6 -C.sub.18 polycycloalkenyl-C.sub.p H.sub.2p -- or C.sub.6 -C.sub.12 cycloalkenyl-C.sub.p H.sub.2p -- (wherein p is 0, 1, 2 or 3), or together with the adjacent ##STR2## group represents a variety of other complex ester groupings; R.sub.1 is C.sub.1 -C.sub.7 alkyl; and Ar is a divalent radical containing at least one aromatic nucleus. The corresponding pharmaceutically acceptable acid addition salts are also described.Type: GrantFiled: May 31, 1995Date of Patent: November 19, 1996Inventor: Nicholas S. Bodor
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Patent number: 5576321Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 1996Assignee: Eli Lilly and CompanyInventors: Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
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Patent number: 5565485Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: August 22, 1994Date of Patent: October 15, 1996Assignee: Merck & Co., Inc.Inventors: Scott W. Bagley, Theodore P. Broten, Prasun K. Chakravarty, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Nancy J. Kevin, Douglas J. Pettibone, Ralph A. Rivero, Thomas F. Walsh, David L. Williams, Jr., Richard B. Toupence, Jay M. Matthews
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Patent number: 5565488Abstract: The inventive Oxalylamino-benzofuran- and benzothienyl-derivatives are prepared by reacting the appropriate amino substituted benzofuranes and benzothiophenes with oxalic acid derivatives. The inventive compounds are suitable for the prevention and treatment of acute and chronic inflammatory processes, particularly of the airways.Type: GrantFiled: May 23, 1995Date of Patent: October 15, 1996Assignee: Bayer AktiengesellschaftInventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
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Patent number: 5554612Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: September 10, 1996Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5538969Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.Type: GrantFiled: May 26, 1995Date of Patent: July 23, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
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Patent number: 5536747Abstract: The disclosed 6-substituted derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil.Type: GrantFiled: May 5, 1995Date of Patent: July 16, 1996Assignee: Syntex (U.S.A.) Inc.Inventors: John W. Patterson, David Morgans, Jr., David B. Smith, Fancisco X. Talamas, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fernandez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert