Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 514/379)
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Patent number: 5580890Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5580893Abstract: Nitroxyalkylamide compounds having the formula: R.sup.1 --(A).sub.n --CONH--B'--ONO.sub.2 wherein R.sup.1 is an optionally substituted furyl, furyloxy, thienyl, thienyloxy, isoxazolyl, phenoxy, phenylthio or 1,4-dibenzodioxanyl, A is a C.sub.1 -C.sub.4 alkylene group; B' is a C.sub.1 -C.sub.4 alkylene group; and n is 0 or 1. The compounds of the present invention have a desirable vasodilator action for collateral vessels and an anti-anginal action, and are useful as therapeutic agents for treating angina pectoris.Type: GrantFiled: July 25, 1994Date of Patent: December 3, 1996Assignee: Sankyo Company, LimitedInventors: Sadao Ishihara, Fujio Saito, Mitsuru Kataoka, Hiroyuki Koike, Shigeki Miyake, Hiroshi Mizuno
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Patent number: 5580886Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: December 3, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5578626Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1-6 aliphatic hydrocarbyl group or a C.sub.1-4 aliphatic hydrocarbyl group substituted by a C.sub.3-6 alicyclic hydrocarbyl group or by a phenyl group, which phenyl group is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.2 represents hydrogen, R.sub.3 represents hydrogen, a 5-or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur which is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, or a group AR wherein A is a straight chain C.sub.1-4 aliphatic hydrocarbyl group terminally substituted by R which is hydrogen, a phenyl group or a 5-or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur, which phenyl or heterocyclyl group R is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.4 and R.sub.Type: GrantFiled: June 7, 1995Date of Patent: November 26, 1996Assignee: British Technology Group LimitedInventors: Edward A. Boyd, Brenda Costall, Mary E. Kelly, Philip J. Parsons
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Patent number: 5578624Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
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Patent number: 5578605Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 26, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5578627Abstract: This invention relates to a 1,2-benzoisoxazole derivative represented by the following general formula (I) or its salt: ##STR1##Type: GrantFiled: April 12, 1995Date of Patent: November 26, 1996Assignee: Toyama Chemical Co., Ltd.Inventors: Kenji Takeda, Nobuo Terashima, Joji Nakano, Hisashi Minami, Toyokazu Kobayashi, Kunikazu Furuhata, Tadakazu Takakura, Makoto Takata, Hiroyo Kawafuchi, Toru Hiraiwa
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Patent number: 5576343Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 1996Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5574032Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 12, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5573775Abstract: Methods for preventing and treating corneal haze resulting from exposure of the eye to laser irradiation are disclosed. The methods include administration of compositions of wound healing modulators to the eye. Compositions for use in preventing and treating the corneal haze are also disclosed.Type: GrantFiled: March 16, 1995Date of Patent: November 12, 1996Assignee: Alcon Laboratories, Inc.Inventors: Stella M. Robertson, Herman M. Kunkle, Jr.
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Patent number: 5571828Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5571821Abstract: Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: ##STR1## in which Ar.sup.1 is a 3- or 5-isoxazolyl and Ar.sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar.sup.2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar.sup.Type: GrantFiled: May 20, 1994Date of Patent: November 5, 1996Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji, Kalyanaraman Ramnarayan
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Patent number: 5571814Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5567720Abstract: Dense microspheres can be extracted and purified to substantial homogeneity from mammalian brain tissue, and used in the screening of therapies for potential effectiveness in impeding the formation of amyloid fibrils associated with Alzheimer's disease and other forms of cerebral amyloidosis. Compounds that, at in-tissue concentrations of 10.sup.-5 M or less, inhibit amyloid formation in a test animal injected intracerebrally with dense microspheres are particularly useful in inhibiting treating cerebral amyloidosis.Type: GrantFiled: June 27, 1994Date of Patent: October 22, 1996Assignee: DMS Pharmaceutical Inc.Inventor: Paul Averback
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Patent number: 5561128Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: October 1, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5559126Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5559116Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5559117Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 24, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski
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Patent number: 5556858Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 17, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
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Patent number: 5556855Abstract: A compound of the formula Het--NR--SO.sub.2 --Ph.sup.2 --A--Ph.sup.1 (COOH)(OH) and tautomic form, salts, solvates, C.sub.1-6 alkyl esters and pharmaceutical compositions of the compound. Ph.sup.1 and Ph.sup.2 are benzene rings with the proviso that carboxy and hydroxy are ortho to one another. Het includes an optionally substituted heterocyclic ring which includes conjugated double bonds and binds to nitrogen in NR. The compound is characterized in that A is a bridge which is stable against reduction because it is not azo, and in that R is hydrogen or lower alkyl.The invention also includes the preparation of the compound and its use as a drug, particularly for treating autoimmune diseases.Type: GrantFiled: December 29, 1994Date of Patent: September 17, 1996Assignee: Pharmacia ABInventors: Hubert Agback, Leif Ahrgren, Thomas Berglindh, Martin Haraldsson, G oran Smedeg.ang.rd, Lars-Inge Olsson
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Patent number: 5550130Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: August 27, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
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Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5541208Abstract: The present invention relates to compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof which are useful as potassium channel antagonists, particularly Maxi-K channel antagonists, and thus useful in treating Alzheimer's Disease and other cognitive disorders. This invention is also related to a method of making the compound of formula (I).Type: GrantFiled: January 24, 1994Date of Patent: July 30, 1996Assignee: Merck & Co., Inc.Inventors: Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Seok H. Lee, Owen B. McManus, Deborah L. Zink
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5521204Abstract: This invention is directed to certain 2-(alkoxycarbonylamino)- and 2-(alkoxycarbonylimino)benzlmidazole derivatives which are useful in the topical, oral or parenteral treatment of animals suffering from helminth infections.Type: GrantFiled: June 6, 1995Date of Patent: May 28, 1996Assignee: Pfizer Inc.Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
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Patent number: 5500443Abstract: A compound of formula (I): ##STR1## in which: X represents oxygen or methylene,n represents 1, 2 or 3,R.sub.1 represents hydrogen, aminocarbonyl or hydroxymethyl,R.sub.2 represents: ##STR2## in which R.sub.3 and R.sub.4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.Type: GrantFiled: February 22, 1995Date of Patent: March 19, 1996Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Olivier Muller, Mark Millan, Mauricette Brocco
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Patent number: 5498619Abstract: Aminoketone derivative compounds containing a heterocyclic ring bonded to an aminoketone moiety and useful as effective ingredients of centrally acting muscle relaxants and pollakiurea curing agents.(+)3-phenyl-5-[2-(1-pyrrolidinylmethyl)butyryl]isoxazole, which has a more remarkable central muscle relaxant action as compared with its racemic modification, can be effectively separated from the racemic modification using optically active 10-camphorsulfonic acid as the agent for the optical resolution.Type: GrantFiled: May 16, 1994Date of Patent: March 12, 1996Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Hideki Tanada, Kazuya Sakai, Seitaro Kajiya, Norio Ohto, Kazutoshi Horikomi, Akira Matsubara, Hideshi Shimizu, Akira Mizuchi
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Patent number: 5482962Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.Type: GrantFiled: July 22, 1994Date of Patent: January 9, 1996Assignee: Rohm and Haas CompanyInventor: Robert E. Hormann
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Patent number: 5476867Abstract: Compounds of formula (I) ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1-6 aliphatic hydrocarbyl group or a C.sub.1-4 aliphatic hydrocarbyl group substituted by a C.sub.3-6 alicyclic hydrocarbyl group or by a phenyl group, which phenyl group is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.2 represents hydrogen, R.sub.3 represents hydrogen, a 5- or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur which is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, or a group AR wherein A is a straight chain C.sub.1-4 aliphatic hydrocarbyl group terminally substituted by R which is hydrogen, a phenyl group or a 5- or 6-membered ring aromatic heterocyclyl group containing one or two heteroatoms selected from nitrogen, oxygen and sulphur, which phenyl or heterocyclyl group R is unsubstituted or substituted by a halogeno or C.sub.1-3 halogenoalkyl group, R.sub.4 and R.sub.Type: GrantFiled: August 15, 1994Date of Patent: December 19, 1995Assignee: British Technology Group LimitedInventors: Edward A. Boyd, Brenda Costall, Mary E. Kelly, Philip J. Parsons
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Patent number: 5475005Abstract: Benzimidazole anthelmintic agents of the formula (I) and their non-toxic salts, wherein R.sup.1, which is in the 5(6)-position, is either H or certain stated substituents, "alk" is a methylene or ethylene group; R.sup.2 is cyano, C.sub.1 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, C.sub.2 -C.sub.4 alkanoyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenoxy, aryl, heteroaryl, aryl-(C.sub.1 -C.sub.4 alkoxy) or heteroaryl-(C.sub.1 -C.sub.4 alkoxy), in which "aryl" means phenyl optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl, and C.sub.1 C.sub.4 alkylsulphonyl in which "heteroaryl" means thienyl, furyl or pyridininyl all optionally substituted by 1 to 3 substituents each independently selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulphinyl and C.sub.1 -C.sub.4 alkylsulphonyl; and R.sub.3 is a C.Type: GrantFiled: May 9, 1994Date of Patent: December 12, 1995Assignee: Pfizer Inc.Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
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Patent number: 5475010Abstract: The present invention concerns novel naphthazarin antibiotic derivatives having general formula I ##STR1## and the pharmaceutically acceptable addition salts thereof.Type: GrantFiled: May 26, 1994Date of Patent: December 12, 1995Assignee: Gruppo Lepetit S.p.A.Inventors: Aldo Trani, Clelia M. L. Dallanoce, Romeo Ciabatti
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Patent number: 5468765Type: GrantFiled: December 23, 1994Date of Patent: November 21, 1995Assignee: Pfizer Inc.Inventors: Bernard J. Banks, Christopher J. Dutton, Alexander C. Goudie
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Patent number: 5462953Abstract: The invention concerns a bicyclic heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 9-membered bicyclic heterocyclic moiety containing 1 or 2 N's and optionally a further N, O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 15, 1994Date of Patent: October 31, 1995Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Pierre A. R. Bruneau, Graham C. Crawley, Keith Oldham
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Patent number: 5459133Abstract: This invention is directed to treatment for increasing the accommodative ability of the eye, for the purpose of decreasing the severity of clinically evident presbyopia, an age-related loss of accommodative ability. The compounds and methods of the invention act by decreasing the tone of parts of the ciliary muscle which act to decrease accommodation, thereby increasing the contractile force of the remaining ciliary muscle, with resultant increased accommodative function.Type: GrantFiled: June 5, 1992Date of Patent: October 17, 1995Assignee: Telor Ophthalmic Pharmaceuticals, Inc.Inventor: Arthur H. Neufeld
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Patent number: 5434174Abstract: Methods of treating Irritable Bowel Syndrome (IBS) using a series of isoxazole derivatives that have both 5-HT1A agonist and M1 muscarinic activities, and formulations adapted for the treatment of IBS comprising those derivatives.Type: GrantFiled: April 20, 1993Date of Patent: July 18, 1995Assignee: Eli Lilly and CompanyInventors: Jaswant S. Gidda, John M. Schaus
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Patent number: 5385925Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.Type: GrantFiled: March 30, 1994Date of Patent: January 31, 1995Assignee: Dr. Karl Thomae GmbHInventors: Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
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Patent number: 5378715Abstract: Compounds of the formula ##STR1## inhibit endothelin, wherein: one of X and Y is N and the other is O; R is naphthyl or naphthyl substituted with R.sup.1, R.sup.2 and R.sup.3 ;R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.3 ; halo; hydroxyl; cyano; nitro; --C(O)H; --C(O)R.sup.6 ; CO.sub.2 H; --CO.sub.2 R.sup.6 ; --SH; --S(O).sub.n R.sup.6 ; --S(O).sub.m --OH; --S(O).sub.m --OR.sup.6 ; --O--S(O).sub.m --R.sup.6 ; --O--S(O).sub.m OH; --O--S(O).sub.m --OR.sup.6 ; --Z.sup.4 --NR.sup.7 R.sup.8 ; or --Z.sup.4 --N(R.sup.11)--Z.sup.5 --NR.sup.9 R.sup.10 ;R.sup.4 and R.sup.5 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z.sup.1, Z.sup.2 and Z.sup.Type: GrantFiled: July 15, 1993Date of Patent: January 3, 1995Assignee: Bristol-Myers Squibb Co.Inventors: Philip D. Stein, John T. Hunt, Natesan Murugesan
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Patent number: 5374644Abstract: Compounds of formula: ##STR1## and stereoisomers thereof, wherein X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted aralkyl, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, --CO.sub.2 R.sup.1, --CONR.sup.2 R.sup.3, or --COR.sup.Type: GrantFiled: December 31, 1991Date of Patent: December 20, 1994Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting
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Patent number: 5364866Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: October 30, 1992Date of Patent: November 15, 1994Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski
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Patent number: 5348968Abstract: The invention relates to a compound of formula (I): ##STR1## in which: R.sub.1 represents hydrogen or halogen, alkyl, alkoxy, cyano or aminocarbonyl or any one of the following: ##STR2## in which: m is equal to 1, 2 or 3,n is equal to 0, 1 or 2,T represents a CO or SO.sub.2,R.sub.4 or R.sub.5, which are identical or different, represent hydrogen or alkyl or phenyl,R.sub.2 represents hydrogen or alkyl, phenyl or acyl,R.sub.3 represents hydrogen, alkyl (optionally substituted by hydroxyl or phenyl) or alkoxycarbonyl,--X--Y.dbd. represents --N--C.dbd., --N--N.dbd.or else ##STR3## represents --O--N.dbd.; to its enantiomers, diastereoisomers and epimers and to its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: February 1, 1994Date of Patent: September 20, 1994Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Philippe Maillos, Olivier Muller, Michel Laubie, Tony Verbeuren, Jean-Jacques Descombes
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Patent number: 5330997Abstract: Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.Type: GrantFiled: February 24, 1993Date of Patent: July 19, 1994Assignee: Pfizer Inc.Inventors: Banavara L. Mylari, William J. Zembrowski
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Patent number: 5328915Abstract: Arthropodicidal compounds, compositions and arthropodicidal use of compounds having the formula ##STR1## wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m and n are as defined in the text.Type: GrantFiled: September 17, 1992Date of Patent: July 12, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventors: Jeffrey K. Long, Patrick D. Lowder, Thomas M. Stevenson
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Patent number: 5321037Abstract: Compounds of formula (I): ##STR1## [in which: either (a) the dotted line ( ) is a single bond; A=is oxygen; and B is a group of formula (II): ##STR2## (in which m is 0 and n is 0 or 1) or (b) the dotted line ( ) is a double bond; A=is said group of formula (II) in which m is 1 and n is 0 or 1; and B is absent; and R.sup.1 is hydrogen, halogen, alkyl, alkenyl, alkynyl, optionally substituted benzyl or optionally substituted phenyl; R.sup.2 is hydrogen, halogen, alkyl, optionally substituted phenyl or heterocyclic; or R.sup.1 and R.sup.2, together with the carbon atoms to which they are attached, are a hydrocarbon ring fused to the isoxazole ring; R.sup.3 and R.sup.4 are each hydrogen, alkyl, optionally substituted benzyl or optionally substituted phenyl; or R.sup.3, R.sup.4 and the nitrogen atom to which they are attached together represent an alicyclic amino group]; and salts thereof may be used for the treatment of cerebral circulatory problems and for use as centrally acting muscle relaxants.Type: GrantFiled: March 4, 1993Date of Patent: June 14, 1994Assignee: Sankyo Company, LimitedInventors: Mitsuo Nagano, Junichi Sakai, Nobuyoshi Iwata, Kazuo Kobayashi, Masao Kozuka, Kenji Yoshimi, Katsunori Kato, Yoshiko Kubo, Toshiyuki Tonohiro, Takao Hara
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Patent number: 5298517Abstract: This disclosure describes novel imidazole compounds having the formula: ##STR1## wherein R.sup.1 and R.sup.6 are described in the specification which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: October 7, 1993Date of Patent: March 29, 1994Assignee: American Cyanamid CompanyInventor: Jeremy I. Levin
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Patent number: 5294635Abstract: Certain spirocyclic heterocyclic compounds, and their pharmaceutically-acceptable salts, are inhibitors of the aldose reductase enzyme, and so are useful for the control of diabetic complications.Type: GrantFiled: September 17, 1992Date of Patent: March 15, 1994Assignee: Pfizer, Inc.Inventors: James F. Eggler, Eric R. Larson
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5256681Abstract: [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl]carbamates of formula (I) wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, halo, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 is C.sub.1-4 alkyl; and X is O, S, SO, SO.sub.2 or NR.sup.3, said R.sup.3 being hydrogen, C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.Type: GrantFiled: August 27, 1991Date of Patent: October 26, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Alfons H. M. Raeymaekers, Eddy J. E. Freyne, Gustaaf M. Boeckx
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Patent number: 5254595Abstract: Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group, in optically active or inactive form as well as their acid addition salts are described.A process for their preparation and pharmaceutical compositions containing the compounds of formula (i) or their pharmaceutically acceptable acid addition salts, are also described.Type: GrantFiled: January 9, 1992Date of Patent: October 19, 1993Assignee: Elf SanofiInventors: Umberto Guzzi, Marco Baroni, Sergio Boveri, Luciano Manara, Alberto Bianchetti
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Patent number: RE35279Abstract: The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives.The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton.The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.Type: GrantFiled: February 17, 1994Date of Patent: June 18, 1996Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Ei Mochida, Kimihiro Murakami, Kazuo Kato, Katsuaki Kato, Jun Okuda, Ichitomo Miwa