Polycyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/207)
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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: 5571803Abstract: 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: December 22, 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: 5565482Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.Type: GrantFiled: September 29, 1995Date of Patent: October 15, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
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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: 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: 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: 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: 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: 5530117Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.Type: GrantFiled: May 31, 1995Date of Patent: June 25, 1996Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
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Patent number: 5527917Abstract: A process for the preparation of 1,2-benzisothiazoles of formula I ##STR1## wherein X is in any one of the 4 possible positions of the benzene ring and is hydrogen, halogen, nitro, C.sub.1 -C.sub.4 alkoxy, halo-C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy or C.sub.2 -C.sub.4 alkynyloxy, in which process a compound of formula II ##STR2## wherein X is as defined for formula I and R.sub.1 is hydrogen or an unsubstituted or substituted C.sub.1 -C.sub.12 hydrocarbon radical, is reacted in the presence of a catalytic amount of a strong acid.Compounds of formula I are known as pesticides, especially as nematicides.Type: GrantFiled: September 7, 1994Date of Patent: June 18, 1996Assignee: Ciba-Geigy CorporationInventors: Hans-Ruedi Kanel, Arthur Wegmann, Denis Neff
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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: 5521213Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: August 29, 1994Date of Patent: May 28, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 5514682Abstract: Compounds of formula (I) wherein F represents a Group of the formula (a) ; E represents a bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; and the rest of the variables are defined in the specification are selective agonists of 5HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.Type: GrantFiled: November 14, 1994Date of Patent: May 7, 1996Assignee: Merck Sharp & Dohme LimitedInventor: Leslie J. Street
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Patent number: 5504095Abstract: Aminobenzosultam derivatives, which are inhibitors of lipoxygenase, having the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Ar is cycloalkyl having five to seven carbon atoms, tetrahydropyranyl, pyridyl, oxazolyl, phenyl or substituted phenyl wherein said substituent is methyl, methoxy, fluoro, chloro or trifluoromethyl; n is an integer of 1 to 3; X is hydrogen, methyl, methoxy, fluoro, chloro or trifluoromethyl; Z is --NH--, --O--, or --CH.sub.2 --; and R.sup.1 is hydrogen or alkyl having one to three carbon atoms.Type: GrantFiled: December 20, 1994Date of Patent: April 2, 1996Assignee: Pfizer Inc.Inventors: Masami Nakane, Kunio Satake, Kazuo Ando, Hiroaki Wakabayashi
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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: 5495032Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein, R, R.sup.3, R.sup.4, X and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar-protic or a polar-aprotic solvent. The resulting compounds are useful as antibiotics.Type: GrantFiled: September 27, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5495018Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.Type: GrantFiled: December 8, 1994Date of Patent: February 27, 1996Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Joseph J. Hlavka, Raymond T. Testa
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Patent number: 5484763Abstract: There are provided substituted benzisoxazole and benzisothiazole compounds having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.Type: GrantFiled: February 10, 1995Date of Patent: January 16, 1996Assignee: American Cyanamid CompanyInventor: Peter J. Wepplo
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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: 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: 5451595Abstract: Benzisothiazoles of the general formula I ##STR1## in which the group RO-- is in one of the positions of the benzene ring and R is a pure or halogenated hydrocarbon radical which is aliphatic or cycloaliphatic, saturated or unsaturated, are active ingredients in crop protection products. They can be used for controlling nematodes which are parasites of plants.Type: GrantFiled: December 22, 1993Date of Patent: September 19, 1995Assignee: Ciba-Geigy CorporationInventor: Marius Sutter
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Patent number: 5447945Abstract: Nematicidal compositions which comprise as active ingredient compounds of formula I ##STR1## wherein R is nitro or halogen, and also processes for the preparation of the compounds of formula I, novel intermediates of the preparation process and methods of using the compounds and the compositions in the control of nematodes are described.Type: GrantFiled: June 14, 1994Date of Patent: September 5, 1995Assignee: Ciba-Geigy CorporationInventors: Marius Sutter, Walter Kunz
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Patent number: 5442059Abstract: The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 13, 1992Date of Patent: August 15, 1995Assignee: American Cyanamid CompanyInventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5440035Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: October 25, 1994Date of Patent: August 8, 1995Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5378680Abstract: Dicarboximides of the formulae Ia, Ib and Ic ##STR1## where X is oxygen or sulfur,R.sup.1 is hydrogen, halogen, cyano, alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylthio, haloalkoxy, haloalkylthio, alkylsulfonyl, haloalkylsulfonyl, phenyl, phenylalkyl, phenoxy or phenylthio, a 5-membered or 6-membered saturated or aromatic heterocyclic radical containing one or two hetero atoms selected from the group consisting of oxygen, sulfur and nitrogen, where the stated organic radicals may be further substituted, andR.sup.2 is hydrogen, hydroxyl, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, di-C.sub.1 -C.sub.Type: GrantFiled: August 19, 1992Date of Patent: January 3, 1995Assignee: BASF AktiengesellschaftInventors: Volker Maywald, Klaus Ditrich, Thomas Kuekenhoehner, Gerhard Hamprecht, Wolfgang Freund, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5374738Abstract: A process is provided for preparing 1,2-benzisothiazole-1,1-dioxides having structure (1): ##STR1## where R is a C.sub.1 -C.sub.20 alkyl or aryl radical, the process comprising the steps of:(a) preparing a solution in an anhydrous solvent of a saccharin salt having structure (2): ##STR2## where Z.sup.+ is a metallic cation other than magnesium; and (b) reacting heterogeneously the saccharin salt with an organomagnesium reagent in a relative magnesium to saccharin salt molar ratio of 1:1.Type: GrantFiled: November 22, 1993Date of Patent: December 20, 1994Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: Laurence Boen, David J. Batal, Stephen A. Madison
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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: 5350761Abstract: Disclosed are the compound of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl;Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl;Y represents SO.sub.2 (sulfonyl) or CO (carbonyl);A represents O (oxygen), S (sulfur), or a direct bond;B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond;X represents oxygen or sulfur,R.sub.Type: GrantFiled: July 30, 1993Date of Patent: September 27, 1994Assignee: Ciba-Geigy CorporationInventors: John H. Van Duzer, Dennis M. Roland
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Patent number: 5342836Abstract: A method of protecting 3-isothiazolones of the formula: ##STR1## wherein Y is (C.sub.1 -C.sub.18)alkyl or (C.sub.3 -C.sub.12)cycloalkyl each optionally substituted with one or more of hydroxy, halo, cyano, alkylamino, dialkylamine, arylamino, carboxy, carbalkoxy, alkoxy, aryloxy, alkylthio, arylthio, haloalkoxy, cycloaklylamino, carbamoxy, or isothiazolonyl; an unsubstituted or halo-substituted (C.sub.2 -C.sub.8)alkenyl or alkynyl; a (C.sub.7 -C.sub.10)aralkyl optionally substituted with one or more of halogen, (C.sub.1 -C.sub.4)alkyl or (C.sub.1 -C.sub.4)alkoxy; and an aryl optionally substituted with one or more of halogen, nitro, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkyl-acylamino, carb(C.sub.1 -C.sub.4)alkoxy or sulfamyl; and R and R.sup.1 is each independently H, halogen (C.sub.1 -C.sub.4)alkyl, (C.sub.4 -C.sub.Type: GrantFiled: August 11, 1992Date of Patent: August 30, 1994Assignee: Rohm and Haas CompanyInventor: Paul F. D. Reeve
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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: 5328902Abstract: The invention provides compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification. These compounds are useful as antibiotic agents.Type: GrantFiled: August 13, 1992Date of Patent: July 12, 1994Assignee: American Cyanamid Co.Inventors: Phaik-Eng Sum, Ving J. Lee, Raymond T. Testa
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Patent number: 5310925Abstract: Novel bleaches are reported. The bleaches are of the N-sulfonyloxaziridine type. Substrates such as fabrics may be bleached in an aqueous solution containing the oxaziridine.Type: GrantFiled: July 16, 1991Date of Patent: May 10, 1994Assignee: Lever Brothers Company, Division of Conopco, Inc.Inventors: David J. Batal, Stephen A. Madison
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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: 5260316Abstract: The compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl, biaryl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl-lower alkynyl, aryloxy-lower alkyl, arylthio-lower alkyl; C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, biaryl-lower alkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl, aryl-C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or aryloxy-aryl-lower alkyl; and aryl represents carbocyclic or heterocyclic aryl; Z represents C.sub.1 -C.sub.3 -alkylene or vinylene, each unsubstituted or substituted by lower alkyl; Y represents SO.sub.2 or CO; A represents O, S, or a direct bond; B represents lower alkylene; or B represents lower alkenylene provided that A represents a direct bond; X represents oxygen or sulfur; R.sub.Type: GrantFiled: June 3, 1992Date of Patent: November 9, 1993Assignee: Ciba-Geigy CorporationInventors: John H. Van Duzer, Dennis M. Roland
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Patent number: 5240923Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: October 9, 1991Date of Patent: August 31, 1993Assignee: Alcon Laboratories, Inc.Inventors: Thomas R. Dean, Hwang-Hsing Chen, Jesse A. May
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Patent number: 5225412Abstract: Novel benzisothiazole- and benzisoxazole-3-carboxamides, processes and intermediates for the preparation thereof, and methods of treating psychoses utilizing compounds and compositions thereof are disclosed.Type: GrantFiled: June 16, 1992Date of Patent: July 6, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Nicholas J. Hrib, John G. Jurcak
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Patent number: 5223616Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.Type: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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Patent number: 5223517Abstract: Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.Type: GrantFiled: August 23, 1991Date of Patent: June 29, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich E. Muller, Ulrich Niewohner, Elisabeth Perzborn, Erwin Bischoff, Hans-Georg Dellweg
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Spiro[1,2-benzisothiazole-3(2H),5'-oxazolidine]-2',4'-dione 1,1-dioxides as antihyperglycemic agents
Patent number: 5221686Abstract: This invention relates to novel spiro[1,2-benzisothiazole-3(2H),5'-oxazolidine]-2',4'-dione 1,1-dioxides characterized by the general formula (I), ##STR1## wherein R is lower alkyl containing 1 to 6 carbon atoms, cycloalkyl containing 5 to 6 carbon atoms, allyl, benzyl, halogen substituted benzyl, aralkyl containing 7 to 10 carbon atoms, halogen substituted aralkyl containing 7 to 10 carbon atoms; 3-phenyl-2-propynyl and halogen substituted 3-phenyl-2-propynyl and the pharmaceutically acceptable salts thereof, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated diabetic complications.Type: GrantFiled: August 4, 1992Date of Patent: June 22, 1993Assignee: American Home Products CorporationInventors: Jay E. Wrobel, Arlene Dietrich -
Patent number: 5210196Type: GrantFiled: May 23, 1991Date of Patent: May 11, 1993Assignee: BP Chemicals LimitedInventor: Johannes von Oppolzer
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Patent number: 5194606Abstract: Novel aminoketones useful as central muscle relaxants and their preparation processes are disclosed. The disclosed processes are novel processes which do not use any heavy metal in view of the facts that their products are will be used as drugs and which require no complex purification step such as liberation of the aminoketones from their hydrochlorides or the like.Type: GrantFiled: July 23, 1991Date of Patent: March 16, 1993Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Akira Matsubara, Kazuya Sakai, Hideki Tanada, Hironori Komatsu
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Patent number: 5182289Abstract: Heterobicyclic and heterocyclic intermediate compounds and their use in treating inflammation, hyperproliferative skin conditions such as psoriasis and allergy are disclosed.Type: GrantFiled: December 10, 1990Date of Patent: January 26, 1993Assignee: Schering CorporationInventors: Pauline C. Ting, Margaret H. Sherlock, Wing C. Tom, James J. Kaminski
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Patent number: 5180419Abstract: There are provided o-carboxy-(5-oxo-2-imidazolin-2-yl)benzo-(5-membered)-heterocyclic compounds and derivatives thereof and a method for the use therewith to control monocotyledenous and dicotyledenous plant species.Type: GrantFiled: November 22, 1991Date of Patent: January 19, 1993Assignee: American Cyanamid CompanyInventors: David M. Gange, Michael A. Guaciaro, Robert F. Doehner, Jr.
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Patent number: 5169951Abstract: Nematicidal compositions which comprise as active ingredient compounds of formula I ##STR1## wherein R is nitro or halogen, and also processes for the preparation of the compounds of formula I, novel intermediates of the preparation process and methods of using the compounds and the compositions in the control of nematodes are described.Type: GrantFiled: April 11, 1991Date of Patent: December 8, 1992Assignee: Ciba-Geigy CorporationInventors: Marius Sutter, Walter Kunz
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Patent number: 5149356Abstract: Herbicidal sulphonylaminocarbonyl-triazolinones having substituents which are bonded via sulphur, of the formula ##STR1## in which n represents the numbers 0, 1 or 2,R.sup.1 represents hydrogen, hydroxyl or amino, or represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkylamino, cycloalkylamino and dialkylamino,R.sup.2 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl and aryl, andR.sup.3 represents an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroaryl,as well as salts of compounds of the formula (I),Also new are the compounds of the following formula: ##STR2## in which n, R.sup.1 and R.sup.2 have the abovementioned meanings andZ represents halogen, alkoxy, aralkoxy or aryloxy.Type: GrantFiled: October 15, 1991Date of Patent: September 22, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5142060Abstract: Herbicidal substituted sulphonylaminotriazolinones of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the group consisting of alkyl, aralkyl, aryl and heteroaryl,R.sup.2 represents hydrogen or the group --SO.sub.2 --R.sup.1 where R.sup.1 has the abovementioned meaning,R.sup.3 represents hydrogen, halogen, hydroxyl, mercapto, amino or an optionally substituted radical from the group consisting of alkyl, cycloalkyl, aralkyl, aryl, alkoxy, alkenyloxy, alkinyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkenylthio, alkinylthio, aralkoxy, aralkylthio, alkylamino and dialkylamino,R.sup.4 represents hydrogen, halogen, hydroxyl, amino or an optionally substituted radical from the group consisting of alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylamino and dialkylamino,X represents nitrogen or a CH group,Y represents nitrogen or a CR.sup.5 group whereR.sup.Type: GrantFiled: October 17, 1991Date of Patent: August 25, 1992Assignee: Bayer AktiengesellschaftInventors: Klaus-Helmut Muller, Rolf Kirsten, Joachim Kluth, Klaus Konig, Hans-Jochem Riebel, Peter Babczinski, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 5137901Abstract: For binding 5-HT.sub.1 receptors and thereby treating central nervous system disorders, novel substituted aminomethyltetralins and their heterocyclic analogues of the formula ##STR1## in which Z--denotes a group of the formula ##STR2## R.sup.1, E and F can be hydrogen or other radicals, or salts thereof.Type: GrantFiled: September 26, 1989Date of Patent: August 11, 1992Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Rudolf Schohe, Peter-Rudolf Seidel, Thomas Glaser, Jorg Traber, Ulrich Benz, Teunis Schuurman, Jean-Marie V. De Vry
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Patent number: 5132428Abstract: A process for enantioselectively alkylating, at the asterisked carbon atom, a single enantiomer of a glycine derivative having the general formula ZCOCH(R)NY wherein Z is a moiety derived from a chiral sultam, R is hydrogen or C.sub.1 to C.sub.10 alkyl and Y is one or more groups rendering the nitrogen atom unreactive towards alkylating agents comprises:(i) reacting the glycine derivative with an enolising agent to produce the corresponding enolate of the glycine derivative, and(ii) thereafter reacting the enolate of the glycine derivative with an alkylating agent of formula R.sup.1 X to generate a single enantiomer of a product of formula ZCOC(R)(R.sup.1)NY where R.sup.1 is selected from C.sub.1 to C.sub.10 alkyl, C.sub.1 to C.sub.20 aralkyl, C.sub.2 to C.sub.10 alkenyl or substituted derivatives thereof and X is Cl, Br or I. The product of the process can be treated with first acid and then base to generate the enantiomerically pure alpha-amino acid of formula HO.sub.2 CC(R)(R.sup.1)NH.sub.Type: GrantFiled: November 5, 1990Date of Patent: July 21, 1992Assignee: BP Chemicals LimitedInventor: Wolfgang W. R. E. J. von Oppolzer
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Patent number: 5114960Abstract: Compounds of the formula ##STR1## wherein A taken together with the two carbon atoms denoted as .alpha. and .beta. is a group of the formula ##STR2## and the dotted line is the double bond present in formulas (i) and (iii); and wherein n is zero, 1, 2 or 3, one of R.sup.1 and R.sup.2 is carboxy or alkoxycarbonyl and the other is hydrogen, R.sup.3 is hydrogen, alkyl, alkoxy, aryloxy, azido, cyano or alkylthio, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 each, independently, is hydrogen or alkyl or, when R.sup.1 is carboxy or alkoxycarbonyl and n stands for 1, R.sup.4 and R.sup.6 taken together can be a carbon-carbon bond or, when R.sup.2 is carboxy or alkoxycarbonyl, R.sup.5 and R.sup.7 taken together can be a carbon-carbon bond, R.sup.8 is halogen, alkyl, haloalkyl or alkoxy and R.sup.9 is hydrogen, halogen, alkyl or alkoxy, and pharmaceutically acceptable salts of the compounds of formula I in which one of R.sup.1 and R.sup.Type: GrantFiled: June 26, 1990Date of Patent: May 19, 1992Assignee: Hoffmann-La Roche Inc.Inventors: Geoffrey Lawton, John M. Osbond, Christopher R. Self
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Patent number: 5096918Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.Type: GrantFiled: February 5, 1990Date of Patent: March 17, 1992Assignee: Imperial Chemical Industries PLCInventor: Keith B. Mallion