Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 6271256Abstract: Methods for controlling growth of gram negative bacteria, such as Helicobacter pylori, which are agents associated with disorders of the gastrointestinal tract of a mammal are described. They include administering a therapeutically effective amount of a polyether ionophore antibiotic to a mammal, such that growth of gram negative bacteria which are agents associated with disorders of the gastrointestinal tract of a mammal is controlled. Packaged pharmaceutical compositions for controlling gram negative bacteria are also described.Type: GrantFiled: November 30, 1999Date of Patent: August 7, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Barry Berkowitz, George Sachs, Chris Blackburn
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Patent number: 6262095Abstract: The invention concerns the therapeutic use of tricyclic salts and their pharmaceutically acceptable salts having the general formula: in which: A is either a sulfur atom, an oxygen atom, or an R3N radical where R3 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring. R1 is either a C1-C5 alkyl radical, or an R4NH radical where R4 is a hydrogen atom, a C1-C5 alkyl radical, or a substituted or unsubstituted aromatic ring, or a substituted or unsubstituted heteroaromatic ring, or an aromatic ring that may or may not be substituted by one or more acceptor or donor groups, or a heteroaromatic ring having one or more heteroatoms, which may or may not be substituted by acceptor or donor groups.Type: GrantFiled: October 14, 1998Date of Patent: July 17, 2001Assignee: Laboratoire InnotheraInventors: Odile Boutherin-Falson, Stéphanie Desquand-Billiald, Anita Favrou, Michel Finet, Olivier Tembo, Jean-Luc Torregrosa, Sylvie Yannic-Arnoult, Florence Domagala-Le Marquer
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Patent number: 6258851Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.Type: GrantFiled: October 8, 1999Date of Patent: July 10, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
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Patent number: 6255331Abstract: Disclosed are biocidal compositions comprising mixtures of formaldehyde-releasing imidazolidines, such as 1,3-dimethylol-5,3-dimethylhydantoin, and 3-isothiazolones stabilized with low levels of copper salts.Type: GrantFiled: August 16, 2000Date of Patent: July 3, 2001Assignee: Rohm and Haas CompanyInventors: Beverly Jean El A'mma, Susan Lynn Nagahashi
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Publication number: 20010004640Abstract: This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula 1Type: ApplicationFiled: January 12, 2001Publication date: June 21, 2001Inventors: Yoshiyuki Inada, Keiji Kubo
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Patent number: 6245349Abstract: The present invention provides drug delivery compositions in both concentrated and diluted forms for use as vehicles in the administration of various active agents. The drug delivery compositions are primarily designed for use with lipophilic, amphipathic, and sparingly water soluble active agents, preferably drugs. The drug delivery compositions are to be administered to an animal to effect uptake of the active agent. The primary mode of administration is by intravenous, intra-arterial, intrathecal, intraperitoneal, intraocular, intra-articular, intramuscular or subcutaneous injection. The concentrated drug delivery compositions are formulated with a phospholipid component, a component selected from propylene glycol or certain polyethylene glycol compounds, a high HLB surfactant, and the drug component, with water and/or an oil component optional. The concentrated drug delivery compositions can be diluted with an aqueous fluid to form an oil-in-water microemulsion composition.Type: GrantFiled: February 23, 1996Date of Patent: June 12, 2001Assignee: Élan Corporation plcInventors: Seang H. Yiv, Alex K. Tustian
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Publication number: 20010002400Abstract: The invention involves methods and materials for treating and preventing non-invasive fungus-induced mucositis. Specifically, the invention involves administrating an antifungal agent such that it contact mucus in an amount, at a frequency, and for a duration effective to prevent, reduce, or eliminate non-invasive fungus-induced rhinosinusitis. This invention also provides methods and materials for diagnosing non-invasive fungus-induced rhinosinusitis and culturing non-invasive fungus from a mammalian mucus sample as well as specific antifungal formulations and medical devices for treating and preventing non-invasive fungus-induced rhinosinusitis. In addition, the invention provides methods and materials for treating and preventing other non-invasive fungus-induced mucositis conditions such as chronic otitis media, chronic colitis, and Crohn's disease. Further, the invention involves methods and materials for treating and preventing chronic asthma symptoms.Type: ApplicationFiled: October 22, 1998Publication date: May 31, 2001Inventor: JENS PONIKAU
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Patent number: 6197804Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and *prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: May 16, 2000Date of Patent: March 6, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Steven Gregory Mischke
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Patent number: 6174910Abstract: The invention provides the use of an AT1 receptor antagonist, or a pharmaceutical salt thereof, for producing a pharmaceutical preparation for the stimulation of apoptosis and for the treatment of pathological symptoms which are substantially reduced, halted or prevented by apoptosis, and also corresponding pharmaceutical preparations.Type: GrantFiled: August 28, 1998Date of Patent: January 16, 2001Assignee: Novartis AGInventors: Marc De Gasparo, Gillian Rosemary Bullock, Leoluca Criscione
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Patent number: 6175013Abstract: This invention provides a series of substituted 2-imidazolines 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 compounds.Type: GrantFiled: June 10, 1994Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Philip A. Hipskind, J. Jeffry Howbert, Brian S. Muehl
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Patent number: 6174912Abstract: Corticotropin releasing factor (CRF) antagonists of Formulae (I) or (II): and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: August 21, 1998Date of Patent: January 16, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: James P. Beck, Paul J. Gilligan
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Patent number: 6153634Abstract: Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.Type: GrantFiled: December 15, 1999Date of Patent: November 28, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Christophe Michoud, Steven Gregory Mischke
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Patent number: 6150371Abstract: A method for preventing or treating autoimmune diseases (excluding type I diabetes) by administering an insulin resistance improving substance as an active ingredient.Type: GrantFiled: November 30, 1998Date of Patent: November 21, 2000Assignee: Sankyo Company, LimitedInventors: Toshihiko Fujiwara, Shinichi Kurakata, Takashi Fujita, Tsunemichi Hosokawa, Junichiro Fukushige, Hiroyoshi Horikoshi
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Patent number: 6136804Abstract: The invention provides a method for treating, preventing, or reducing the risk of developing a condition selected from the group consisting of acute coronary ischemic syndrome, thrombosis, thromboembolism, thrombotic occlusion and reocclusion, restenosis, transient ischemic attack, and first or subsequent thrombotic stroke, in a patient, comprising administering to the patient a therapeutically effective amount of an antiplatelet agent in combination with a therapeutically effective amount of a COX-2 inhibitor. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a COX-2 inhibitor, or a pharmaceutically acceptable salt thereof, and an antiplatelet agent, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 12, 1999Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventor: Steven A. Nichtberger
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Patent number: 6124277Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.Type: GrantFiled: March 11, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 6124331Abstract: This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: June 30, 1999Date of Patent: September 26, 2000Assignee: Synaptic Pharmaceutical CorporationInventors: Mohammad R. Marzabadi, Wai C. Wong, Stewart A. Noble
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Patent number: 6096755Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: February 1, 1999Date of Patent: August 1, 2000Assignee: BASF AktiengesellschaftInventor: Gerd Steiner
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Patent number: 6057347Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: September 16, 1997Date of Patent: May 2, 2000Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6051718Abstract: The present invention concerns 2-cyanoiminoimidazole derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; difluoromethyl; trifluoromethyl; C.sub.3-6 cycloalkyl; a saturated 5-, 6- or 7-membered heterocycle containing one or two heteroatoms selected from oxygen, sulfur or nitrogen; indanyl; 6,7-dihydro-5H-cyclopentapyridinyl; bicyclo[2.2.1]-2-heptenyl; bicyclo[2.2.1]heptanyl; C.sub.1-6 alkylsulfonyl; arylsulfonyl; or substituted C.sub.1-10 alkyl; R.sup.3 is hydrogen, halo or C.sub.1-6 alkyloxy; R.sup.4 is hydrogen; halo; C.sub.1-6 alkyl; trifluoromethyl; C.sub.3-6 cycloalkyl; carboxyl; C.sub.1-4 alkyloxycarbonyl; C.sub.3-6 cycloalkylaminocarbonyl; aryl; Het.sup.1 ; or substituted C.sub.1-6 alkyl; or R.sup.4 is --O--R.sup.7 or --NH--R.sup.8 ; R.sup.5 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.Type: GrantFiled: March 19, 1999Date of Patent: April 18, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Francisco Javier Fernandez-Gadea, Jose Ignacio Andres-Gil
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Patent number: 6017950Abstract: Methods for controlling growth of gram negative bacteria, such as Helicobacter pylori, which are agents associated with disorders of the gastrointestinal tract of a mammal are described. They include administering a therapeutically effective amount of a polyether ionophore antibiotic to a mammal, such that growth of gram negative bacteria which are agents associated with disorders of the gastrointestinal tract of a mammal is controlled. Packaged pharmaceutical compositions for controlling gram negative bacteria are also described.Type: GrantFiled: August 5, 1997Date of Patent: January 25, 2000Assignee: Millennium Pharmaceuticals, Inc.Inventors: Barry Berkowitz, George Sachs, Chris Blackburn
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Patent number: 6013644Abstract: The present invention is directed spiro-substituted azacycles of formula I: (wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, k, l and m are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: December 12, 1997Date of Patent: January 11, 2000Assignee: Merck & Co., Inc.Inventors: Sander G. Mills, Malcolm Maccoss, Martin S. Springer
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Patent number: 5990146Abstract: Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.Type: GrantFiled: August 17, 1998Date of Patent: November 23, 1999Assignee: Warner-Lambert CompanyInventors: Diane Harris Boschelli, William Alexander Denny, Annette Marian Doherty, James Marino Hamby, Sonya Shah Khatana, James Bernard Kramer, Brian Desmond Palmer, Howard Daniel Hollis Showalter
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Patent number: 5969133Abstract: A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.Type: GrantFiled: May 22, 1998Date of Patent: October 19, 1999Assignee: Shiongi BioResearch Corp.Inventors: Mitsunori Ono, Keizo Koya, Lijun Sun, Yumiko Wada, Wojciech Wrona, Natalie Dales, Xueliang Tao, Sylvia Holden
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Patent number: 5958960Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.Type: GrantFiled: May 13, 1998Date of Patent: September 28, 1999Assignee: Eli Lilly and CompanyInventors: Steven Marc Massey, James Allen Monn, Matthew John Valli
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Patent number: 5948789Abstract: A novel process for enantioselective synthesis of single enantiomers of omeprazole or its alkaline salts, of other optically pure substituted 2-(2-pyridinylmethyl-sulphinyl) -1H-benzimidazoles as well as of other structurally related sulphoxides or their alkaline salts. The claimed process is an asymmetric oxidation of a pro-chiral sulphide to the single enantiomers or an enantiomerically enriched form of the corresponding sulphoxide. The application also claims the enantiomeric sulphoxide products produced by the process and their use in medicine.Type: GrantFiled: July 14, 1995Date of Patent: September 7, 1999Assignee: Astra AktiebolagInventors: Magnus Erik Larsson, Urban Jan Stenhede, Henrik Sorensen, Sverker Per Oskar von Unge, Hanna Kristina Cotton
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Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5939415Abstract: The present invention relates to heterocyclic compounds with the formula ##STR1## in which R.sup.1 to R.sup.7, B, a, and X have the meanings indicated in the specification. These compounds can be used for the treatment of diseases of the rheumatic variety and for the prevention of allergically-induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 17, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
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Patent number: 5925374Abstract: A pour-on anthelmintic composition, including its method of preparation and use, the composition preferably having being prepared by mixing at a common temperature (I) a premix of an anthelmintic compound or compounds (for example a benzimidazole) with a transdermal vehicle (such as isopropyl myristate) with (ii) a premix of a non-ionic emulsifier with an oil capable of solubilising the emulsifier and, subsequent to the blending of the premixes (preferably after cooling), mixing the blend with a deflocculation agent/diluent or deflocculation agent/diluent mix.Type: GrantFiled: September 27, 1996Date of Patent: July 20, 1999Assignee: Bomac Laboratories LimitedInventors: Donald George McLaren, Wayne Frederick Leech
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5861389Abstract: Male menopause is characterized by significant decreases in serum levels of bioavailable androgens. The administration of aromatase inhibitors to men experiencing male menopause can remedy the relative androgen deficiency in men while at the same time approximating the physiological hormonal ratio of androgens to estrogens.Type: GrantFiled: June 13, 1997Date of Patent: January 19, 1999Assignee: Schering AktiengesellschaftInventors: Albert Radlmaier, Ursula-Friederike Habenicht, Friedmund Neumann
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Patent number: 5852014Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.Type: GrantFiled: June 2, 1995Date of Patent: December 22, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5843912Abstract: The present invention relates to compositions comprising analogues of purine nucleosides containing a ring-expanded ("fat") heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic, and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS) and hepatitis.Type: GrantFiled: August 23, 1995Date of Patent: December 1, 1998Assignees: Universy of Maryland, NabiInventors: Ramachandra Hosmane, Barry Burns
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Patent number: 5789410Abstract: Disclosed are compounds encompassed by the following general formula: ##STR1## wherein, A represents ethenylene, or A represents --X--CH.sub.2 --; where X is carbon or oxygen, provided that when X is oxygen, the oxygen is adjacent the 6-membered ring;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are inorganic or organic substituents; andR.sub.5 and R.sub.6 is are optionally substituted organic substituents; orNR.sub.5 R.sub.6 represents a carbocyclic or heterocyclic six membered ring optionally substituted with various orgainic or inorganic groups, which compounds can be used in the treatment of neuropsychological disorders.Type: GrantFiled: January 22, 1997Date of Patent: August 4, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Andrew Thurkauf
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Patent number: 5789431Abstract: The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.Type: GrantFiled: February 16, 1996Date of Patent: August 4, 1998Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Sheng-Chu Kuo, Toshiro Ibuka
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Patent number: 5776931Abstract: This invention provides a series of substituted 1H-naphth?2,3-d!imidazoles which are useful in treating a condition associated with an excess of neuropeptide Y. This invention also provides methods employing these substituted 1H-naphth?2,3-d!imidazoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these compounds.Type: GrantFiled: January 9, 1997Date of Patent: July 7, 1998Assignee: Eli Lilly and CompanyInventors: Anne Marie Nunes, Hamideh Zarrinmayeh
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Patent number: 5767141Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.Type: GrantFiled: March 8, 1995Date of Patent: June 16, 1998Assignee: Hoechst AktiengesellschaftInventors: Gerrit Schubert, Horst Hemmerle, Peter Below, Andreas Herling, Hans-Jorg Burger
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Patent number: 5763465Abstract: There are disclosed compounds of formula I,Ar--CH.sub.2 CH.sub.2 --NH--CR.sup.1 R.sup.2 --X--Y Iin whichAr represents a group, ##STR1## X represents a C.sub.1-12 alkylene chain optionally interrupted or terminated by one or more groups selected from --S(O).sub.n --, --O--, --C(Z)--, CR.sup.6 R.sup.7, phenylmethyne, --NR.sup.8 --, --CONH--, --NHCO-- and --NHCONH--,Y represents an optionally substituted aryl or cycloalkyl group,Z represents O or S,R.sup.1, R.sup.2, R.sup.5 and R.sup.9 each independently represent hydrogen or alkyl C.sub.1-6,R.sup.3 and R.sup.4 represent hydrogen, or R.sup.3 and R.sup.4 together form a group --S--, --NR.sup.9 -- or --CH.sub.2 --,R.sup.6 and R.sup.7 independently represent hydrogen, alkyl C.sub.1-6, fluoro, cyano, or CF.sub.3, provided that at least one of R.sup.6 and R.sup.7 is other than hydrogen,R.sup.8 represents hydrogen or alkyl C.sub.1-6, or when X is interrupted or terminated by more than one --NR.sup.8 -- group may together with another R.sup.8 group form the chain --CH.Type: GrantFiled: October 31, 1996Date of Patent: June 9, 1998Assignee: Astra Pharmaceuticals LimitedInventors: Roger V. Bonnert, Roger C. Brown, David R. Cheshire, Francis Ince, John Dixon
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Patent number: 5763459Abstract: A method for the treatment of anxiety in mammals comprises administering an effective amount of a 5-HT.sub.4 receptor antagonist.Type: GrantFiled: February 28, 1995Date of Patent: June 9, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Gordon Smith Baxter, Guy Anthony Kennett
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Patent number: 5726320Abstract: A process for the preparation of (+)-2-amino-bicyclo?3.1.0!-hexane-2-6-dicarboxylic acid, or a pharmaceutically acceptable salt thereof, which comprises hydrolysing (-)-2-spiro-5'-hydantoinbicyclo?3.1.0!hexane-6-carboxylic acid or a salt thereof, and optionally forming a pharmaceutically acceptable salt. Also disclosed are intermediates useful in the process.Type: GrantFiled: June 26, 1996Date of Patent: March 10, 1998Assignee: Eli Lilly and CompanyInventor: Roger Lewis Robey
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Patent number: 5723481Abstract: Described herein are of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.Type: GrantFiled: June 16, 1994Date of Patent: March 3, 1998Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
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Patent number: 5714508Abstract: Described herein are compounds of the formula ##STR1## wherein the substituents are defined as in the specification having inhibiting activity on the effects of angiotensin II.Type: GrantFiled: August 1, 1994Date of Patent: February 3, 1998Assignee: Roussel UclafInventors: Alain Corbier, Jean Paul Vevert, Jidong Zhang
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Patent number: 5710159Abstract: This invention relates to novel heterocycle compounds including but not limited to 3-?3-?3-(imidazolin-2-yl amino)propyloxy!isoxazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-pro pionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.Type: GrantFiled: May 9, 1996Date of Patent: January 20, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Matthew Ernst Voss, Prabhakar Kondaji Jadhav, Joanne Marie Smallheer, Douglas Guy Batt, William John Pitts, John Wityak
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Patent number: 5708017Abstract: The present invention is concerned with an oral pharmaceutical formulation containing a proton pump inhibitor (PPI) which is suitable for the treatment of gastric acid related diseases in man and animals. More specifically, the composition is a paste, and is particularly suitable for delivery of a proton pump inhibitor to horses.Type: GrantFiled: April 4, 1995Date of Patent: January 13, 1998Assignee: Merck & Co., Inc.Inventors: Kaushik J. Dave, James B. Williams
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Patent number: 5705498Abstract: Compounds of formula (I): ##STR1## wherein X.sup.g is O, S, SO, SO.sub.2, CH.sub.2, CH, N or NR wherein R is hydrogen or C.sub.1-6 alkyl;A is a saturated or unsaturated polymethylene chain of 2-4 carbon atoms;R.sub.1.sup.g and R.sub.2.sup.g are hydrogen or C.sub.1-6 alkyl;R.sub.3.sup.g is hydrogen, halo, C.sub.1-6 alkyl, amino, nitro or C.sub.1-6 alkoxy;R.sub.4.sup.g is hydrogen, halo, C.sub.1-6 alkyl or C.sub.1-6 alkoxy,Y is O or NH, or CO--Y together are a heterocyclic bioisostere;Z is of sub-formula: ##STR2## wherein --(CH.sub.2).sub.n.sup.1 is attached at carbon; and n.sup.1 is 0, 1, 2, 3 or 4;q is 0, 1, 2 or 3;R.sub.a is a straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by R.sub.7 wherein R.sub.7 is 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, or R.sub.7 is C.sub.2-7 alkoxycarbonyl or secondary or tertiary hydroxy substituted C.sub.1-6 alkyl; andR.sub.6 is hydrogen or C.Type: GrantFiled: May 4, 1995Date of Patent: January 6, 1998Assignee: SmithKline Beecham plc.Inventors: Laramie Mary Gaster, Paul Adrian Wyman
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Patent number: 5698576Abstract: Described herein are compounds of formula (I): ##STR1## ?in which: R.sup.1 and R.sup.2 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl, aromatic heterocyclic, cyano or halogen; R.sup.3 is hydrogen, optionally substituted alkyl, aralkyl or acyl; R.sup.4 and R.sup.5 are hydrogen, optionally substituted alkyl, cycloalkyl, alkenyl, aralkyl, arylalkenyl, aryl or aromatic heterocyclic!; and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.Type: GrantFiled: November 22, 1996Date of Patent: December 16, 1997Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
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Patent number: 5670059Abstract: A novel method and compositions are disclosed for the treatment of water in recirculating water systems. The method includes providing a boron level of at least 20 ppm in the water, continually eroding into the water a compressed sanitizer/algicide component including a halogen source material, a boron source material, and glycoluril, and periodically adding to the water an oxidizing clarifier comprising a chlorine source material, a non-halogen, chlorine source material, and a boron source material. The invention also provides novel water treatment chemicals including the compressed sanitizer/algicide component and the clarifier useful in the foregoing system. The system and compositions are safe and reliable, control algal and fungal growth and generally provide improved water quality for recirculating water systems.Type: GrantFiled: September 20, 1995Date of Patent: September 23, 1997Assignee: Bio-Lab, Inc.Inventors: Ronald L. Jones, Stephen L. Carlyle, Susan M. Shelor, Presley K. Mitchell, Ellwood LeRoy Lines, Jr.
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Patent number: 5665752Abstract: Described herein are compounds of formula (I): ##STR1## and pharmaceutically acceptable salts thereof are analgesics and anti-inflammatory agents as well having anti-ulcer and 5-lipoxygenase inhibitory activities.Type: GrantFiled: April 7, 1995Date of Patent: September 9, 1997Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Kazuyuki Wachi, Hachio Miyazawa, Yoshio Iizuka, Kazuo Hasegawa, Keiichi Tabata
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Patent number: 5648316Abstract: Described herein are new benzimidazole derivatives of the formula ##STR1## in which R represents cyano or the group ##STR2## X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are identical or different and represent halogen;Y represents alkyl, alkenyl or alkinyl, each of which is optionally substituted by halogen; or represents optionally substituted phenylalkyl or in each case optionally substituted cycloalkyl and cycloalkenyl; andZ represents hydrogen or halogen, a process for the preparation of these substances, and their use for controlling pests.Type: GrantFiled: October 29, 1996Date of Patent: July 15, 1997Assignee: Bayer AktiengesellschaftInventors: Lutz Assmann, Albrecht Marhold, Heinz-Wilhelm Dehne, Gerd Hanssler, Klaus Stenzel, Ulrike Wachendorff-Neumann
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Patent number: 5639756Abstract: An antidiabetic compound selected from those of formula (I): ##STR1## wherein A, B, C, D, n, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y and Z are as defined in the description.Medicaments containing the same.Type: GrantFiled: October 28, 1994Date of Patent: June 17, 1997Assignee: Adir et CompagnieInventors: Vera Alekseevna Anisimova, Margarita Valentinovna Levchenko, Tatyana Borisovna Korochina, Alexander Alexeyevich Spasov, Sergei Gennadyevich Kovalev, Galina Petrovna Dudchenko
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Patent number: 5637603Abstract: The present invention is directed to the use of disulfonyl methane compounds for the control of parasites in vertebrate animals.Type: GrantFiled: April 25, 1995Date of Patent: June 10, 1997Assignee: Eli Lilly and CompanyInventor: David I. Wickiser