Nitrogen Or Chalcogen Attached Indirectly To The Thiazole Ring By Nonionic Bonding Patents (Class 548/214)
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Patent number: 5686471Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl or aralkyl having from 1 to about 3 carbon atoms; or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 and R.sub.2 are each independently hydrogen or straight, branched or cyclic alkyl, unsubstituted or substituted, carboxyl, carboxamido, alkoxycarbonyl or alkylcarbonyl; and(f) Het is a heteroaryl group comprising one or more rings containing from about 5 to about 8 atoms in the rings and wherein at least one ring has at least one heteroatom selected from O, N, or S,pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.Type: GrantFiled: February 1, 1996Date of Patent: November 11, 1997Assignee: The Procter & Gamble CompanyInventors: Zhuoliang Chen, John Michael Janusz
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Patent number: 5684198Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.Type: GrantFiled: August 23, 1996Date of Patent: November 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Keith Russell, Cyrus John Ohnmacht, Keith Hopkinson Gibson
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Patent number: 5683686Abstract: There are disclosed a controlling agent and an antifouling composition against harmful aquatic organisms, which include a particular N-phenylisothiazolone derivative of the formula: ##STR1## wherein X.sup.1 and X.sup.2 are the same or different and are independently hydrogen, chlorine or bromine; and R is haloalkoxy. Also disclosed is a method for preventing or inhibiting the adhesion of harmful aquatic organisms to water-exposed articles, which includes applying the antifouling composition to the water-exposed articles.Type: GrantFiled: December 27, 1994Date of Patent: November 4, 1997Assignees: Chugoku Marine Paints, Ltd., Sumitomo Chemical Company, LimitedInventors: Makoto Tsuboi, Shuhei Yuki, Akiko Kakimizu, Kenji Arai, Masato Mizutani
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Patent number: 5679670Abstract: 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: December 15, 1994Date of Patent: October 21, 1997Assignee: Alcon Laboratories, Inc.Inventors: Thomas Robert Dean, Hwang-Hsing Chen, Jesse Albert May
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5675024Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: November 22, 1995Date of Patent: October 7, 1997Assignee: AllerganInventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 5659044Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: April 5, 1995Date of Patent: August 19, 1997Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Chen Zhao, Thomas J. Sowin
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Patent number: 5646147Abstract: Acaricidal, insecticidal and nematicidal substituted (hetero)arylalkyl ketone oxime O-ethers, processes for their preparation, agents containing them, and their use as pesticides.The invention relates to compounds of the formula ##STR1## in which Ar.sup.1 and Ar.sup.2 are aryl or heteroaryl, each of which is optionally substituted, and R is an optionally substituted aliphatic or alicyclic radical, to processes for their preparation, and to agents containing these compounds, and to their use for controlling animal pests.Type: GrantFiled: April 20, 1994Date of Patent: July 8, 1997Assignee: Hoechst AktiengesellschaftInventors: Birgit Kuhn, Gerhard Salbeck, deceased, Uwe Doller, Stefan Schnatterer, Hans-Herbert Schubert, Werner Knauf, Anna Waltersdorfer, Manfred Kern
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Patent number: 5631253Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.Type: GrantFiled: December 2, 1994Date of Patent: May 20, 1997Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5631279Abstract: This invention relates to perhydroisoindole derivatives of 08/448,402 formula (I), wherein radicals R are phenyl radicals optionally 2-or 3-substituted by a halogen atom or a methyl radical; R.sub.1 is optionally substituted phenyl, cyclohexadienyl, naphthyl, indenyl or optionally substituted heterocyclyl; R.sub.2 is H, halogen, OH, alkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, acyloxy, acyloxy, carboxy, optionally substituted alkyloxycarbonyl, benzyloxycarbonyl, amino or acylamino; and R.sub.3 is optionally 2-substituted phenyl; optionally salts thereof where applicable; and preparation thereof. Said derivatives are particularly useful as neurokinin A antagonists.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Andre Crespo, Veronique Fardin, Jean-Marc Guillaume, Jean-Luc Malleron, Jean-Francois Peyronel
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Patent number: 5631376Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5624950Abstract: Perhydroisoindole derivatives of formula I, wherein the substituents are as defined in the specification, are particularly suitable as substance P antagonists. Several processes for preparing the compounds are also taught.Type: GrantFiled: January 29, 1996Date of Patent: April 29, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Daniel Achard, Serge Grisoni, Evelyne James-Surcouf, Jean-Luc Malleron, Anne Morgat, Jean-Fran.cedilla.ois Peyronel, Jean-Fran.cedilla.ois Sabuco, Michel Tabart
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Patent number: 5621109Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed wherein the terms R.sub.1, R.sub.2, R.sub.5, R.sub.6, Y, Y', m and n are herein defined.Type: GrantFiled: May 31, 1995Date of Patent: April 15, 1997Assignee: Abbott LaboratoriesInventors: Daniel W. Norbeck, Hing L. Sham, Dale J. Kempf, Chen Zhao
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Patent number: 5618943Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.Type: GrantFiled: December 29, 1994Date of Patent: April 8, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Alan T. Johnson, Richard L. Beard, Min Teng, Tae K. Song, Harold N. Wong, Roshantha A. Chandraratna
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Patent number: 5616720Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: April 6, 1995Date of Patent: April 1, 1997Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao, Daniel S. Reno
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Patent number: 5604229Abstract: 2-Amino-1,3-propanediol compounds of the formula (I) ##STR1## wherein R is an optionally substituted straight- or branched carbon chain, an optionally substituted aryl, an optionally substituted cycloalkyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is a hydrogen, an alkyl, an aralkyl, an acyl or an alkoxycarbonyl, pharmaceutically acceptable salts thereof and immunosuppressants comprising these compounds as active ingredients.The 2-amino-1,3-propanediol compounds of the present invention show immunosuppressive action and are useful for suppressing rejection in organ or bone marrow tranplantation, prevention and treatment of autoimmune diseases or as reagents for use in medicinal and pharmaceutical fields.Type: GrantFiled: June 17, 1994Date of Patent: February 18, 1997Assignees: Yoshitomi Pharmaceutical Industries, Ltd., Taito Co., Ltd.Inventors: Tetsuro Fujita, Shigeo Sasaki, Masahiko Yoneta, Tadashi Mishina, Kunitomo Adachi, Kenji Chiba
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Patent number: 5602160Abstract: 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: April 17, 1995Date of Patent: February 11, 1997Assignee: 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: 5599793Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: February 4, 1997Assignee: Eli Lilly and CompanyInventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5594021Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides 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.Type: GrantFiled: June 6, 1995Date of Patent: January 14, 1997Assignee: Texas Biotechnology CorporationInventors: Ming F. Chan, Bore G. Raju, Adam Kois, Erik J. Verner, Chengde Wu, Rosario S. Castillo, Venkatachalapathi Yalamoori, Vitukudi N. Balaji
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Patent number: 5589439Abstract: Herbicidal novel tetrazolinone derivatives of the formula: ##STR1## wherein R.sup.1 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, andR.sup.2 is alkyl, haloalkyl, cycloalkyl, alkenyl, haloalkenyl, alkynyl, alkoxy or phenyl which is optionally substituted, orR.sup.1 and R.sup.2 form, together with the nitrogen atom to which R.sup.1 and R.sup.2 are bonded, a 5- or 6-membered heterocyclic ring, optionally fused to a carbocyclic ring optionally and independently substituted by C.sub.1-4 alkyl, andR.sup.3 is a 5-membered heterocyclic radical containing at least one hereto atom selected from the group consisting of nitrogen, oxygen, and sulfur, optionally substituted by at least one substitutent selected from the group consisting of halogen, benzyl, phenyl, halogen-substituted phenyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkyl-sulfonyl and C.sub.Type: GrantFiled: July 28, 1995Date of Patent: December 31, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Toshio Goto, Koichi Moriya, Fritz Maurer, Seishi Ito, Katsuaki Wada, Kazuhiro Ukawa, Ryo Watanabe, Asami Ito, Natsuko Minegishi
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Patent number: 5585486Abstract: Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is (CR.sub.5 R.sub.6).sub.n, (CR.sub.5 R.sub.6).sub.n,-aryl, (CR.sub.5 R.sub.6).sub.n -heteroaryl, X-(CR.sub.5 R.sub.6).sub.n, X-(CR.sub.5 R.sub.6).sub.n -aryl or X-(CR.sub.5 R.sub.6).sub.n -heteroaryl wherein aryl and heteroaryl may be optionally substituted;X is 0 or NR.sub.5 ;R.sub.5 and R.sub.6 are independently H or lower alkyl;R.sub.2 is H, halo, lower alkyl or (CR.sub.5 R.sub.6).sub.n -aryl;R.sub.3 and R.sub.4 are independently H or alkyl;A is a D or L isomer of an amino acid selected from the group consisting of alanine, valine, leucine, isoleucine, proline, phenylalanine, glycine, tyrosine, methionine, asparagine, glutamine, aspartic acid, glutamic acid, lysine, arginine, histidine and .beta.-thienylalanine;Z is CH.sub.2 or O; andn is 0-4;pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1.beta.Type: GrantFiled: May 12, 1995Date of Patent: December 17, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill, Gary J. Speier, Catherine P. Prouty, Stanley J. Schmidt
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Patent number: 5578574Abstract: This invention relates to L-arginine aldehyde derivatives, having the formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: March 2, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: Robert T. Shuman, Robert B. Rothenberger, Kenneth D. Kurz, Daniel J. Sall, Gerald F. Smith, Michael R. Wiley
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Patent number: 5574000Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, 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 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkythio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: November 17, 1994Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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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: 5565584Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 20, 1995Date of Patent: October 15, 1996Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hanner, Brian S. Freed, Gregory H. Merriman
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Patent number: 5565418Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: April 5, 1995Date of Patent: October 15, 1996Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck, Hing L. Sham, Chen Zhao, Thomas J. Sowin, Daniel S. Reno, Michael S. Allen, Arthur J. Copper, Jien-Heh J. Tien
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Patent number: 5565469Abstract: Angiotensin-II inhibiting benzimidazoles, useful for the treatment of hypertension.Type: GrantFiled: March 13, 1995Date of Patent: October 15, 1996Assignee: Dr. Karl Thomae GmbHInventors: Gerhard Mihm, Norbert Hauel, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5563159Abstract: There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C.sub.1 -C.sub.6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a phenyl group, a heterocyclic group, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, a bicycloalkyl group or a tricycloalkyl group, all of which may be substituted. Also disclosed are a fungicidal/insecticidal/acaricidal agent containing the dithiocarbonimide derivative as an active ingredient, an intermediate for use in the production of the dithiocarbonimide derivative, and a process for producing the dithiocarbonimide derivative from the intermediate.Type: GrantFiled: December 2, 1994Date of Patent: October 8, 1996Assignee: Sumitomo Chemical Company, LimitedInventors: Tomoyuki Kusaba, Tadashi Ohsumi, Tsuguhiro Katoh, Makoto Fujimura, Norio Kimura, Kazuya Ujihara, Kimitoshi Umeda
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Patent number: 5556874Abstract: 2-Thioindoles (2-selenoindoles) and analogous 2-indolinethione (2-indolineselenone) and polysulfide (selenide) compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds, and methods for inhibiting protein kinase dependent disease in a mammal or treating aberrant cell growth in a mammal, using said compositions, are disclosed.Type: GrantFiled: May 10, 1995Date of Patent: September 17, 1996Assignee: Warner Lambert CompanyInventors: Ellen M. Dobrusin, Howard D. H. Showalter, William A. Denny, Brian D. Palmer, Gordon W. Rewcastle, Moana Tercel, Andrew M. Thompson
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Patent number: 5554627Abstract: Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.Type: GrantFiled: April 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
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Patent number: 5550142Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: May 8, 1995Date of Patent: August 27, 1996Assignee: Merck Frosst Canada Inc.Inventors: Yves Ducharme, Jacques Y. Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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Patent number: 5543534Abstract: Compounds of Formula 1 ##STR1## wherein X is S or O; R.sub.1 -R.sub.5, m, o, X, Y, A, B are as defined in the specification.Type: GrantFiled: December 29, 1994Date of Patent: August 6, 1996Assignee: AllerganInventors: Vidyasagar Vuligonda, Min Teng, Richard L. Beard, Alan T. Johnson, Yuan Lin, Roshantha A. Chandraratna
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Patent number: 5541321Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##Type: GrantFiled: March 30, 1995Date of Patent: July 30, 1996Assignee: Abbott LaboratoriesInventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao
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Patent number: 5541320Abstract: A process is disclosed for the preparation of a substituted diaminoalcohol of the formula: ##STR1##Type: GrantFiled: March 30, 1995Date of Patent: July 30, 1996Assignee: Abbot LaboratoriesInventors: William R. Baker, John K. Pratt, Daniel W. Norbeck, Chen Zhao
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Patent number: 5538939Abstract: Acylamino-substituted isoxazole or isothiazole derivatives of the formula I ##STR1## where X is oxygen or sulfur;R.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl or phenyl;R.sup.2 is CN, CONH.sub.2, CSNH.sub.2, or haloalkyl;R.sup.3 is hydrogen or unsubstituted or substituted alkyl or cycloalkyl;R.sup.4 is alkoxy, unsubstituted or substituted alkyl, cycloalkenyl, cycloalkyl, alkenyl or alkynyl, an unsubstituted or substituted 5-membered or 6-membered heterocyclic radical or unsubstituted or substituted phenyl;haloalkyl, alkoxy, haloalkoxy, alkylthio and/or haloalkylthio,and agriculturally useful salts of the isoxazole or isothiazole derivatives I, useful as herbicides.Type: GrantFiled: August 24, 1994Date of Patent: July 23, 1996Assignee: BASF AktiengesellschaftInventors: Peter Muenster, Ernst Schefczik, Hartmann Koenig, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5538991Abstract: Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 14, 1994Date of Patent: July 23, 1996Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee
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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: 5521317Abstract: There is disclosed a process for the preparation of an indanylamine compound of general formula ##STR1## wherein R.sup.1 represents an optionally substituted alkyl group, and R.sup.2, R.sup.3 and R.sup.4 independently represent a hydrogen atom or an optionally substituted alkyl group, the process including the steps of hydrogenating a compound of general formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described above and R.sup.5 and R.sup.6 independently represent a halogen atom, a hydroxyl, nitro or cyano group, or an optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylcarboxy or alkylamino group provided that R.sup.5 and R.sup.6 represent different atoms or groups, and subsequent rearrangement and derivatization of the product thereof. Compounds of general formula I may be used to prepare preferred stereoisomers of fungicidal N-indanyl carboxamide compounds.Type: GrantFiled: October 12, 1994Date of Patent: May 28, 1996Assignee: American Cyanamid Co.Inventor: Paul H. Briner
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Patent number: 5521200Abstract: A compound of the general formula I; ##STR1## is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions and methods of treatment are also disclosed.Type: GrantFiled: November 1, 1994Date of Patent: May 28, 1996Inventors: Winston Ho, Bruce E. Maryanoff, David F. McComsey, Samuel O. Nortey
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Patent number: 5521143Abstract: Isoxazolines or isothiazolines having the formula (I), or their salts, in which (Z).sub.n, X and R have the definition given in the first claim, are useful as safeners against the phytotoxic side effects of herbicides, preferably in cereal crops.Type: GrantFiled: January 29, 1993Date of Patent: May 28, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz-Josef Loher, Klaus Bauer, Hermann Bieringer
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Patent number: 5514679Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.Type: GrantFiled: May 13, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
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Patent number: 5508450Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.Type: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5506237Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the carbon and nitrogen atoms to which it is attached, a heterocycle,B represents, with the nitrogen atom to which it is attached, a heterocycle,n is equal to 1, 2, 3 or 4,R represents phenyl substituted by at least one halogen or alkyl, hydroxyl, alkoxy, trifluoromethyl, nitro, amino, cyano, carboxyl or alkoxycarbonyl, benzyl, thienyl or pyridyl. The compounds may be used as medicaments.Type: GrantFiled: March 23, 1994Date of Patent: April 9, 1996Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Bernard Protevin, Georges Remond, Jean Lepagnol, Veronique Heidet
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Patent number: 5506356Abstract: An N-acylamino acid derivative of the formula: ##STR1##Type: GrantFiled: January 20, 1995Date of Patent: April 9, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Hajime Morishima, Yutaka Koike, Masato Nakano, Shugo Atsuumi, Seiichi Tanaka, Kenji Matsuyama
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Patent number: 5500425Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.Type: GrantFiled: September 9, 1994Date of Patent: March 19, 1996Assignee: Aktiebolaget AstraInventors: Lars-Gunnar Larsson, Lucy A. Renyl, Svante B. Ross, Daniel D. Sohn, Seth-Olov Thorberg
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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: 5494919Abstract: The present invention is directed to certain piperidine, pyrrolidine, and hexahydro-1H-azepine compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.3, R.sub.4, R.sub.5, A, W, X, Y, and n axe as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which s are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 27, 1996Assignee: Merck & Co., Inc.Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
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Patent number: 5492920Abstract: The present invention is directed to certain novel compounds identified as substituted piperidines, pyrrolidines and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A, X, Y and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Ravi Nargund, Arthur A. Patchett, Lihu Yang
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Patent number: 5492916Abstract: The present invention is directed to certain novel compounds identified as di- and tri-substituted piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein R.sub.1, R.sub.4, R.sub.5, A,X,Y, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such di and tri substituted piperidines, pyrrolidines, and hexahydro-1H-azepines as the active ingredient thereof are also disclosed.Type: GrantFiled: October 17, 1994Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Gregori J. Morriello, Arthur A. Patchett, Lihu Yang
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Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi