Chalcogen Or Nitrogen Bonded Directly To The Hetero Ring Patents (Class 514/470)
  • Patent number: 6017952
    Abstract: This invention relates to derivatives of furan and thiophene, their composition, process of making and method of use as endothelin receptor antagonists.
    Type: Grant
    Filed: February 2, 1998
    Date of Patent: January 25, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Aiming Gao, Jia-Ning Xiang
  • Patent number: 5997891
    Abstract: 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: Grant
    Filed: August 18, 1998
    Date of Patent: December 7, 1999
    Assignee: IPA, LLC
    Inventors: Ronnie S. Fuerst, Richard Melker, Christopher D. Batich
  • Patent number: 5990160
    Abstract: 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: Grant
    Filed: May 14, 1999
    Date of Patent: November 23, 1999
    Assignee: Gruppo Lepetit, SpA
    Inventors: Khalid Islam, Stefania Stefanelli, Federica Sponga, Maurizio Denaro
  • Patent number: 5985898
    Abstract: 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: Grant
    Filed: June 16, 1998
    Date of Patent: November 16, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5972936
    Abstract: 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: Grant
    Filed: May 20, 1997
    Date of Patent: October 26, 1999
    Assignee: Darwin Discover Limited
    Inventors: Hazel Joan Dyke, John Gary Montana
  • Patent number: 5965529
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 12, 1999
    Assignees: The Board of Regents, University of Texas, Schering Aktiengesellschaft
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
  • Patent number: 5965608
    Abstract: 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: Grant
    Filed: July 21, 1998
    Date of Patent: October 12, 1999
    Assignee: Rockhurst University
    Inventor: Don E. Gibbs
  • Patent number: 5962413
    Abstract: 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: Grant
    Filed: September 22, 1997
    Date of Patent: October 5, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas System
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 5948762
    Abstract: 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: Grant
    Filed: July 17, 1997
    Date of Patent: September 7, 1999
    Assignees: Schering Aktiengesellschaft, The University of Texas System
    Inventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
  • Patent number: 5942546
    Abstract: 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: Grant
    Filed: November 20, 1997
    Date of Patent: August 24, 1999
    Assignee: Development Center for Biotechnology
    Inventors: Ji-Wang Chern, Yu-Ling Leu, Shan-Shue Wang, Chin-Fen Lee, Shih-Chung Hsu
  • Patent number: 5929121
    Abstract: 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: Grant
    Filed: December 13, 1996
    Date of Patent: July 27, 1999
    Assignee: Rhone-Poulenc Agro
    Inventors: Jorge Cepeda, Juan Bocanegra
  • Patent number: 5922760
    Abstract: 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: Grant
    Filed: June 19, 1997
    Date of Patent: July 13, 1999
    Assignee: Suntory Limited
    Inventors: Kengo Akimoto, Michihiro Sugano, Koji Yamada, Michiko Nonaka, Jiong-Yan Gu
  • Patent number: 5919800
    Abstract: 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: Grant
    Filed: November 3, 1995
    Date of Patent: July 6, 1999
    Assignee: Eli Lilly and Company
    Inventor: Alan David Palkowitz
  • Patent number: 5906987
    Abstract: 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: Grant
    Filed: March 10, 1997
    Date of Patent: May 25, 1999
    Assignees: Schering Aktiengesellschaft and Board of Regents, The University of Texas System
    Inventors: Kristof Chwalisz, Robert E. Garfield
  • Patent number: 5889046
    Abstract: 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: Grant
    Filed: February 1, 1996
    Date of Patent: March 30, 1999
    Assignee: Suntory Limited
    Inventors: Kengo Akimoto, Shiro Morimoto, Yasuo Matsumura, Hajime Yoshizumi, Tetsuo Murakami
  • Patent number: 5852052
    Abstract: 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: Grant
    Filed: December 9, 1996
    Date of Patent: December 22, 1998
    Assignee: Ruth Korth
    Inventor: Ruth Korth
  • Patent number: 5837645
    Abstract: 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: Grant
    Filed: July 1, 1996
    Date of Patent: November 17, 1998
    Inventors: Ronnie S. Fuerst, Richard Melker, Christopher D. Batich
  • Patent number: 5827879
    Abstract: 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: Grant
    Filed: October 3, 1997
    Date of Patent: October 27, 1998
    Assignee: Eli Lilly and Company
    Inventors: William J. Ehlhardt, James E. Ray, John E. Toth
  • Patent number: 5817683
    Abstract: 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: Grant
    Filed: April 8, 1996
    Date of Patent: October 6, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, Jia-Ning Xiang
  • Patent number: 5817653
    Abstract: Novel compounds of the formula: ##STR1## are disicosed which are endothelin receptor antagonists.
    Type: Grant
    Filed: April 12, 1996
    Date of Patent: October 6, 1998
    Assignee: SmithKline Beecham Corporation
    Inventors: John Duncan Elliott, John Gerald Gleason, David Taylor Hill
  • Patent number: 5814661
    Abstract: 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: Grant
    Filed: September 19, 1995
    Date of Patent: September 29, 1998
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Vito Ulderico Ruggiero, Piero Foresta
  • Patent number: 5804598
    Abstract: 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: Grant
    Filed: March 20, 1997
    Date of Patent: September 8, 1998
    Assignee: Rockhurst University
    Inventor: Don E. Gibbs
  • Patent number: 5792763
    Abstract: 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: Grant
    Filed: September 26, 1997
    Date of Patent: August 11, 1998
    Assignee: Eli Lilly and Company
    Inventors: James E. Fritz, Stephen W. Kaldor, Sidney Xi Liang, Upinder Singh, Yao-Chang Xu
  • Patent number: 5773463
    Abstract: 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: Grant
    Filed: January 22, 1996
    Date of Patent: June 30, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: John David Harling, Barry Sidney Orlek
  • Patent number: 5728696
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: March 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
  • Patent number: 5726208
    Abstract: 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: Grant
    Filed: October 11, 1996
    Date of Patent: March 10, 1998
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Bertrand Goument, Jean-Christophe Harmange, Joel Vian, Aimee Dessinges, Mark Millan, Valerie Audinot
  • Patent number: 5723469
    Abstract: 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: Grant
    Filed: July 11, 1996
    Date of Patent: March 3, 1998
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masaru Shibata, Kazuhiko Sugiyama, Norihisa Yonekura, Junetsu Sakai, Yoshiyuki Kojima, Shigeru Hayashi
  • Patent number: 5716624
    Abstract: 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: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5693676
    Abstract: 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: Grant
    Filed: June 20, 1996
    Date of Patent: December 2, 1997
    Assignee: Neptune Pharmaceutical Corporation
    Inventor: Stephen R. Gorfine
  • Patent number: 5684033
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: November 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: 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
  • Patent number: 5674894
    Abstract: 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: Grant
    Filed: May 15, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
  • Patent number: 5674876
    Abstract: 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: Grant
    Filed: January 20, 1995
    Date of Patent: October 7, 1997
    Assignee: Research Development Foundation
    Inventors: John C. Gilbert, Kimberly Kline, Kathiresan Krishnan, Maria Simmons Menchaca, Marian Pinto, Robert G. Sanders
  • Patent number: 5665766
    Abstract: 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: Grant
    Filed: January 30, 1995
    Date of Patent: September 9, 1997
    Assignee: Cal International Limited
    Inventors: William Byrne, Andrew Rynne
  • Patent number: 5663192
    Abstract: 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: Grant
    Filed: October 20, 1994
    Date of Patent: September 2, 1997
    Assignee: Eli Lilly and Company
    Inventors: Robert F. Bruns, Jr., Donald R. Gehlert, J. Jeffry Howbert, William H. W. Lunn
  • Patent number: 5656659
    Abstract: 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: Grant
    Filed: November 18, 1994
    Date of Patent: August 12, 1997
    Assignees: T Cell Sciences, Inc., The University of Mississippi
    Inventors: Robert D. Sindelar, Barton J. Bradbury, Teodoro Saul Kaufman, Stephen Hoi-Chuen Ip, Henry Clinton Marsh, Jr., Chew Lee
  • Patent number: 5646181
    Abstract: 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: Grant
    Filed: May 2, 1995
    Date of Patent: July 8, 1997
    Assignee: Research Foundation of State University of New York
    Inventors: Ho-Leung Fung, John Anthony Bauer
  • Patent number: 5643944
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: July 1, 1997
    Assignee: Board of Regents, The University of Texas System
    Inventors: Robert E. Garfield, Chandrasekhar Yallampalli
  • Patent number: 5637610
    Abstract: 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: Grant
    Filed: June 20, 1994
    Date of Patent: June 10, 1997
    Assignee: Suntory Limited
    Inventors: Ayako Nakabayashi, Yoshinori Kitagawa, Kengo Akimoto, Michihiro Sugano
  • Patent number: 5635527
    Abstract: 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: Grant
    Filed: February 6, 1996
    Date of Patent: June 3, 1997
    Assignee: The Green Cross Corporation
    Inventors: 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
  • Patent number: 5627200
    Abstract: 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: Grant
    Filed: September 26, 1994
    Date of Patent: May 6, 1997
    Assignee: Pfizer Inc
    Inventors: David K. Kreutter, Robert L. Dow
  • Patent number: 5622989
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: April 22, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Br aunlich, R udiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
  • Patent number: 5612368
    Abstract: 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: Grant
    Filed: October 25, 1995
    Date of Patent: March 18, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean Andrieux, Michel Langlois, Pierre Renard, Philippe Delagrange
  • Patent number: 5589505
    Abstract: 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: Grant
    Filed: June 5, 1995
    Date of Patent: December 31, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5576332
    Abstract: 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: Grant
    Filed: May 31, 1995
    Date of Patent: November 19, 1996
    Inventor: Nicholas S. Bodor
  • Patent number: 5576321
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: November 19, 1996
    Assignee: Eli Lilly and Company
    Inventors: Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
  • Patent number: 5565485
    Abstract: 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: Grant
    Filed: August 22, 1994
    Date of Patent: October 15, 1996
    Assignee: 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
  • Patent number: 5565488
    Abstract: 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: Grant
    Filed: May 23, 1995
    Date of Patent: October 15, 1996
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Braunlich, Rudiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
  • Patent number: 5554612
    Abstract: 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: Grant
    Filed: May 26, 1995
    Date of Patent: September 10, 1996
    Inventors: 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
  • Patent number: 5538969
    Abstract: 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: Grant
    Filed: May 26, 1995
    Date of Patent: July 23, 1996
    Assignee: 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
  • Patent number: 5536747
    Abstract: 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: Grant
    Filed: May 5, 1995
    Date of Patent: July 16, 1996
    Assignee: 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