Chalcogen Bonded Directly To The Triazole Ring Patents (Class 514/384)
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Patent number: 6177454Abstract: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.Type: GrantFiled: February 29, 2000Date of Patent: January 23, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Tatsuya Maruyama, Kenichi Onda, Masahiko Hayakawa, Takumi Takahashi, Takayuki Suzuki, Tetsuo Matsui
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Patent number: 6166059Abstract: The present invention provides novel thiocyanato-triazolyl derivatives, and the acid addition salts and metal salt complexes thereof; a process for their preparation; and a method for their use as microbicides.Type: GrantFiled: November 17, 1998Date of Patent: December 26, 2000Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Stefan Dutzmann, Klaus Stenzel, Gerd Hanssler
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Patent number: 6166057Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.Type: GrantFiled: November 4, 1998Date of Patent: December 26, 2000Assignee: Monsanto CompanyInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 6159995Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: December 12, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase, Bernhard Neises, Gunter Billen
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Patent number: 6156766Abstract: Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharamaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypertensive action and cerebral.cndot.coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action.Type: GrantFiled: February 18, 1999Date of Patent: December 5, 2000Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masafumi Arita, Tadamasa Saitoh, Masanori Minoguchi, Keiji Yamagami, Hiroyuki Satoh
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Patent number: 6156321Abstract: The invention embodies the surprising discovery that Tissue Factor (TF) compositions and variants thereof specifically localize to the blood vessels within a vascularized tumor following systemic administration. The invention therefore provides methods and compositions comprising coagulant-deficient Tissue Factor for use in effecting specific coagulation and for use in tumor treatment. The TF compositions and methods of present invention may be used alone, as TF conjugates with improved half-life, or in combination with other agents, such as conventional chemotherapeutic drugs, targeted immunotoxins, targeted coaguligands, and/or in combination with Factor VIIa (FVIIa) or FVIIa activators.Type: GrantFiled: January 20, 1998Date of Patent: December 5, 2000Assignee: Board Of Regents, The University of Texas SystemInventors: Philip E. Thorpe, Steven W. King, Boning Gao
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Patent number: 6147077Abstract: A method of treating fungal infections with a mixture of isomers of 2R,4S-hydroxyitraconazole and their sulfate and phosphate derivatives is disclosed. Pharmaceutical compositions containing these compounds are also disclosed.Type: GrantFiled: April 29, 1999Date of Patent: November 14, 2000Assignee: Sepracor Inc.Inventors: Patrick Koch, Richard F. Rossi, Jr., Chris Hugh Senanayake, Stephen Alan Wald
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Patent number: 6143325Abstract: Extended-release nefazodone compositions containing nefazodone hydrochloride, ionic and non-ionic gelling polymers, an insoluble hydrophilic agent, and optional pharmaceutically acceptable excipients demonstrate pH-modulated release of nefazodone. These compositions are formulated into unit dosage forms for improved oral administration. The improvements comprise an extended drug release profile providing comparative levels of nefazodone with respect to immediate release dosage forms and, additionally, demonstrating the lack of a food effect.Type: GrantFiled: April 26, 1999Date of Patent: November 7, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Andrew B. Dennis, Peter Timmins, Alison C. Hodsdon
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Patent number: 6117896Abstract: .beta.-sheet mimetics and methods relating to the same are disclosed. The .beta.-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a .beta.-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.Type: GrantFiled: February 12, 1998Date of Patent: September 12, 2000Assignee: Molecumetics Ltd.Inventors: Maher N. Qabar, Michael K. McMillan, Michael S. Kahn, John E. Tulinsky, Cyprian O. Ogbu, Jessymol Mathew
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Patent number: 6114368Abstract: The present invention provides the composition for novel triazolyl disulphides, the acid addition salts and metal salt complexes of the triazolyl disulphides, a process for their preparation, and a method for their use as microbicides.Type: GrantFiled: November 5, 1998Date of Patent: September 5, 2000Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6080775Abstract: The present invention relates to novel sulphonyl-mercapto-triazolyl derivatives, their acid addition salts and metal salt complexes; a process for the preparation of the novel compounds; and a method for their use as microbicides.Type: GrantFiled: November 19, 1998Date of Patent: June 27, 2000Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6077861Abstract: Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, NO.sub.2, or ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.Type: GrantFiled: November 23, 1998Date of Patent: June 20, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey L. Romine, Scott W. Martin, Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff, John E. Starrett, Jr.
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Patent number: 6075023Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.Type: GrantFiled: February 17, 1998Date of Patent: June 13, 2000Assignee: BASF AktiengesellschaftInventors: Gerhard Peter Dohmen, Christoph Kunast, Reinhart Munk, Gerhard Rothhaas
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Patent number: 6066662Abstract: The invention provides hydroxylamine derivatives of formula (I) wherein A, R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, which are matrix metalloproteinase inhibitors and which also prevent TNF release. They are therefore useful for the control or prevention of degenerative joints diseases such as rheumatoid arthritis and osteoarthritis or for the treatment of invasive tumours, atherosclerosis or multiple sclerosis. They can be manufactured according to generally known methods.Type: GrantFiled: November 20, 1996Date of Patent: May 23, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, Paul Anthony Brown, William Henry Johnson
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Patent number: 6057352Abstract: Compounds of Formula (I), ##STR1## and their N-oxides and agriculturally suitable salts are disclosed which are useful as fungicides, wherein E is 1,2-phenylene optionally substituted with one of R.sup.3, R.sup.4, or both R.sup.3 and R.sup.4 ; A is O; S; N; NR.sup.5 ; or CR.sup.14 ; G is C or N; provided that when G is C, then A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, then A is N or CR.sup.14 and the floating double bond is attached to A; W is O; S; NH; N(C.sub.1 -C.sub.6 alkyl); or NO(C.sub.1 -C.sub.6 alkyl); X is OR.sup.1 ; S(O).sub.m R.sup.1 ; or halogen; R.sup.1 is C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; C.sub.2 -C.sub.6 alkenyl; C.sub.2 -C.sub.6 haloalkenyl; C.sub.2 -C.sub.6 alkynyl; C.sub.2 -C.sub.6 haloalkynyl; C.sub.3 -C.sub.6 cycloalkyl; C.sub.2 -C.sub.4 alkylcarbonyl; or C.sub.2 -C.sub.4 alkoxycarbonyl; R.sup.2 is H; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl; C.sub.2 -C.sub.6 alkenyl: C.sub.2 -C.sub.6 haloalkenyl; C.sub.2 -C.sub.Type: GrantFiled: November 13, 1997Date of Patent: May 2, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, Deborah Ann Frasier, Michael Henry Howard, Jr., Gerard Michael Koether
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Patent number: 6057353Abstract: Triazoyl mercaptides of the formula (I) ##STR1## in which M is an alkaline metal cation, an equivalent of an alkaline earth cation, an equivalent of a copper zinc, iron or nickel cation or an ammonium cation andR.sup.1 is various radicals, a process for the production of the novel substances and their use to combat undesired micro-organisms.Type: GrantFiled: October 23, 1998Date of Patent: May 2, 2000Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6051252Abstract: An orally administrable solid dosage form containing a compacted ribavirin composition having an advantageously high tap density of at least 0.6 g/mL as well as surprisingly rapid disintegration and dissolution rates and wherein the ribavirin is subsantially free of polymorphic forms of ribavirin is disclosed.Type: GrantFiled: May 7, 1999Date of Patent: April 18, 2000Assignee: Schering CorporationInventors: Stephen M. Liebowitz, Elliot I. Stupak, Imtiaz A. Chaudry, Winston A. Vadino, Frank E. Bowen
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Patent number: 6051592Abstract: The present invention provides the composition for novel acyl-mercapto-triazolyl derivatives, and the acid addition salts and metal salt complexes thereof; a process for their preparation; and a method for their use as microbicides.Type: GrantFiled: October 27, 1998Date of Patent: April 18, 2000Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6028093Abstract: Fungicidal mixtures, comprisinga) a carbamate of the formula I ##STR1## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, and/orb) an oxime ether of the formula II, ##STR2## where the substituents have the following meanings: X is oxygen or amino;Y is CH or N;Z is oxygen, sulfur, amino or C.sub.1 -C.sub.4 -alkylaminoR' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkyl-methyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio; andc) a carbamate of the formula III(CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 CH.sub.Type: GrantFiled: October 21, 1998Date of Patent: February 22, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer, Dietrich Mappes, Joachim Leyendecker, Herbert Bayer, Ruth Muller
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Patent number: 5998413Abstract: Anti-infective compositions for the treatment of a human in need of therapy for a systemic or topical fungal infection which comprise a pharmaceutically acceptable carrier and a therapeutically effective amount of (2R,4S) itraconazole or a pharmaceutically acceptable salt thereof, substantially free of its (2S,4R) stereoisomer.Type: GrantFiled: July 9, 1996Date of Patent: December 7, 1999Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Jean Louis Mesens, Jozef Peeters
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Patent number: 5998446Abstract: There are described compounds of the general formula I ##STR1## where the index and the substituents have the following meanings: R is cyano, halogen, alkyl or alkoxy;n is 0, 1 or 2, it being possible for the substituents R to differ from each other if n is 2;Het is a 5-membered heteroaromatic ring having three nitrogen atoms or two nitrogen atoms and one oxygen or sulfur atom and having attached to it an unsubstituted or substituted 6-membered aromatic or heteroaromatic ring;processes for their preparation, and their use.Type: GrantFiled: November 20, 1997Date of Patent: December 7, 1999Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Bernd Muller, Hubert Sauter, Klaus Oberdorf, Hartmann Konig, Norbert Gotz, Michael Rack, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann
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Patent number: 5994383Abstract: Antimicrobial compositions and methods for preparing and using same are provided. The antimicrobial compositions are surfactant-based and contain certain benzalkonium chloride homologs. The compositions are useful in treating infections in animals and humans, and can be applied to areas including the skin, nails, and mouth.Type: GrantFiled: November 18, 1997Date of Patent: November 30, 1999Assignee: Woodward Laboratories, Inc.Inventors: David L. Dyer, Kenneth B. Gerenraich
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Patent number: 5977149Abstract: Cyclic amides of Formula (I) which are useful as fungicides wherein: A is O; S; N; NR.sup.5 ;or CR.sup.14--, G is C or N; W is O or S; X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; R.sup.1, R.sup.2, and R.sup.5 are independently, in part, C.sub.1 -C.sub.6 alkyl; Y is, in part, --O--; --S(O).sub.n --,--CHR.sup.6 O--; or --CHR.sup.6 O--N.dbd.C(R.sup.7)--; Z is, in part, optionally substituted cycloalkyl, phenyl, pyridinyl, pyrimidinyl, or naphthyl; and R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.14, m, and n are defined in the disclosure, are disclosed.Type: GrantFiled: January 14, 1998Date of Patent: November 2, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5962436Abstract: Cyclic amides, including triazole containing cyclic amides, their N-oxides, agriculturally-suitable salts and compositions, and their methods of use as fungicides.Type: GrantFiled: August 21, 1997Date of Patent: October 5, 1999Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, Deborah Ann Frasier, Constance Happersett, Peter Paul Castro, Charlene Gross Sternberg
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Patent number: 5958957Abstract: The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.Type: GrantFiled: April 16, 1997Date of Patent: September 28, 1999Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl Moller, Peter Madsen
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Patent number: 5935986Abstract: There are described compounds of the general formula I ##STR1## in which the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen,unsubstituted or substituted alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy orin the event that n is greater than 1 additionally an unsubstituted or substituted bridge which is bonded to two adjacent ring atoms;R.sup.1, R.sup.2 are alkyl;R.sup.3 is a substituted pyrazole ?sic! or triazole ?sic! radical of the formulae A.1 to A.3 ##STR2## where the bond marked .circle-solid. is the bond to the oxygen, processes for their preparation, and their use.Type: GrantFiled: November 20, 1997Date of Patent: August 10, 1999Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Reinhard Kirstgen, Hartmann Konig, Michael Rack, Klaus Oberdorf, Franz Rohl, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
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Patent number: 5932583Abstract: Bis-oxime derivatives of the formula I ##STR1## W is oxygen or sulfur, and the other substituents defined as follows: R.sub.1 =hydrogen, C.sub.1 -C.sub.4 alkyl; cyclopropyl;R.sub.2 =hydrogen, C.sub.1 -C.sub.6 alkyl; halo(C.sub.1 -C.sub.6) alkyl; C.sub.2 -C.sub.6 alkoxyalkyl; C.sub.3 -C.sub.6 cycloalkyl; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; cyano; C.sub.1 -C.sub.6 alkoxycarbonyl; C.sub.1 -C.sub.6 alkyl-S(O).sub.n ; substituted or unsubstituted aryl-S(O).sub.n ; C.sub.1 -C.sub.6 alkoxy; substituted or unsubstituted aryloxy; substituted or unsubstituted heteroaryloxy; unsubstituted or mono- to trimethyl-substituted heterocyclyl; substituted or unsubstituted aryl-C.sub.1 -C.sub.6 alkyl; substituted or unsubstituted heteroaryl-C.sub.1 -C.sub.6 alkyl;R.sub.3 =hydrogen; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 haloalkyl having 1 to 5 halogen atoms; C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.2 -alkyl; unsubstituted or mono- to trihalo-substituted C.sub.1 -C.sub.6 alkenyl; C.sub.Type: GrantFiled: December 23, 1997Date of Patent: August 3, 1999Assignee: Novartis Crop Protection, Inc.Inventors: Hugo Ziegler, Stephan Trah, Rene Zurfluh, Anthony Cornelius O'Sullivan
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Patent number: 5922751Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed The compounds possess similar or improved PDE IV inhibition as compared to rolipram, with improved selectivity with regard to, e.g., PDE III inhibition. Preferred compounds are 3-(3-cyclopentyloxy-4-methoxy-benzylamino)-4-hydroxymethyl pyrazole and 3-(3-cyclopentyloxy-4-methoxybenzylamino)-4-methoxymethylpyrazole.Type: GrantFiled: January 10, 1997Date of Patent: July 13, 1999Assignee: Euro-Celtique, S.A.Inventors: David John Cavalla, Mark Chasin, Lloyd J. Dolby, Richard William Frith
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Patent number: 5914128Abstract: An orally administrable solid dosage form containing a compacted ribavirin composition having an advantageously high tap density of at least 0.6 g/mL as well as surprisingly rapid disintegration and dissolution rates and wherein the ribavirin is substantially free of polymorphic forms of ribavirin is disclosed.Type: GrantFiled: December 22, 1997Date of Patent: June 22, 1999Assignee: Schering CorporationInventors: Stephen M. Liebowitz, Elliot I. Stupak, Imtiaz A. Chaudry, Winston A. Vadino, Frank E. Bowen
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Patent number: 5905072Abstract: Adjuvants for systemic fungicides in the form of a stable microemulsion comprise water, a mixture of methyl esters of fatty acids obtained by the transesterification of vegetable oils, an anionic surface-active agent, at least one non-ionic surface-active agent with an HLB of between 13-18 and a cloud point of >65.degree. and at least one non-ionic surface-active agent with an HLB of between 10 and 12. These adjuvants, which can additionally contain conventional components and/or formulation additives, improve the activity of systemic fungicides belonging to different chemical groups.Type: GrantFiled: February 9, 1996Date of Patent: May 18, 1999Assignee: Isagro S.p.A.Inventors: Luigi Capuzzi, Mario Ferri, Ernesto Signorini, Nicola Stramacchia, Claude Delestre, Luigi Mirenna
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Patent number: 5880143Abstract: A wood preservative which contains a dimethylalkylamine, an aliphatic C.sub.8 -C.sub.20 -dicarboxylic acid and a triazole compound.Type: GrantFiled: August 27, 1997Date of Patent: March 9, 1999Assignee: BASF AktiengesellschaftInventors: Reimer Goettsche, Reiner Kober, Uwe Kardorff
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Patent number: 5859039Abstract: Triazolyl derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and represent optionally substituted alkyl, optionally substituted alkenyl, optionally substituted cycloalkyl, optionally substituted aralkyl, optionally substituted aralkenyl, optionally substituted aroxyalkyl, optionally substituted aryl or optionally substituted heteroaryl andX represents the groups --SH, --SR.sup.3, --SO--R.sup.3, --SO.sub.2 --R.sup.3 or --SO.sub.3 H, in whichR.sup.3 represents alkyl which is optionally substituted by fluorine and/or chlorine, alkenyl which is optionally substituted by fluorine and/or chlorine, optionally substituted aralkyl or optionally substituted aryl,and their acid addition salts and metal salt complexes,a plurality of processes for the preparation of the new substances, and their use as microbicides in plant protection and materials protection.Type: GrantFiled: June 19, 1997Date of Patent: January 12, 1999Assignee: Bayer AktiengesellschaftInventors: Manfred Jautelat, Ralf Tiemann, Stefan Dutzmann, Gerd Hanssler, Klaus Stenzel
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Patent number: 5852048Abstract: There is disclosed an ester compound of the formula (I), ##STR1## wherein R.sup.1 represents a methyl group or a hydrogen atom, R.sup.2 represents a proparqyl group or an allyl group, and R.sup.3 represents a (C.sub.1 -C.sub.5)alkyl group, a (C.sub.1 -C.sub.5)haloalkyl group or a (C.sub.3 -C.sub.5)cycloalkyl group and R.sup.4 represents a halogen atom or a hydrogen atom, and a pesticide containing the same as an active ingredient.Type: GrantFiled: March 1, 1996Date of Patent: December 22, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Furukawa, Kazunori Tsushima, Tomonori Iwasaki, Hirosi Kisida, Mikako Nakamachi, Yoji Takada
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Patent number: 5843997Abstract: The present invention provides novel compounds that affect excitatory amino acid receptors and are useful in the treatment of neurological disorders. This invention also provides synthetic methods for the preparation of the novel compounds.Type: GrantFiled: April 2, 1996Date of Patent: December 1, 1998Assignee: Eli Lilly and CompanyInventors: Lawrence J. Heinz, William H.W. Lunn, Darryle Darwin Schoepp
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Patent number: 5811442Abstract: Patients suffering from or susceptible to conditions of the vascular or circulatory system, particularly the microvasculature, which conditions are associated with decreased blood flow in regions of microcirculation (e.g., Raynaud's disease and Raynaud's phenomenon) are treated with pharmaceutical compositions incorporating an effective amount of an aryl substituted olefinic amine compound. The compounds incorporated into the pharmaceutical compositions of the present invention exhibit selective activity of to the .beta.2-containing nicotinic acetylcholine receptors and thereby yield beneficial therapeutic effects increasing vascular blood flow in regions of microcirculation.Type: GrantFiled: February 21, 1997Date of Patent: September 22, 1998Inventors: Merouane Bencherif, Patrick Michael Lippiello
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Patent number: 5807875Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-?(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.Type: GrantFiled: December 11, 1996Date of Patent: September 15, 1998Assignee: Dr. Karl Thomae GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike Andrea Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
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Patent number: 5756522Abstract: Disclosed are triazole derivatives represented by the following formula, insecticides and acaricides containing the triazole derivatives as active ingredients, and a method of controlling insect pests and mites. ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a halogen atom, 1-pyrrolyl group, a group represented by the formula NR.sup.2 R.sup.3 ; R.sup.5 represents a methyl or ethyl group substituted with at least one halogen atom; n represents 0, 1 or 2; Y represents a nitrogen atom or a group represented by the formula CX.sup.2 ; and X.sup.1 and X.sup.2 are the same or different and each represent a halogen atom, a nitro group or a cyano group.Type: GrantFiled: December 20, 1996Date of Patent: May 26, 1998Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroki Tomioka, Takashi Furukawa, Yoji Takada, Hirotaka Takano
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Patent number: 5750545Abstract: An agent for the prophylaxis and treatment of immune-related diseases, in particular, immunosuppressant, an agent for the prophylaxis and treatment of allergic diseases, an agent for the prophylaxis and treatment of eosinophil-related diseases and an eosinophilia inhibitor, comprising, as an active ingredient, a series of triazole derivatives of the following formula (I) ##STR1## or the following formula (III) ##STR2## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. A novel monocyclic or bicyclic triazole derivative. The agent for the prophylaxis and treatment of immune-related diseases, in particular, immunosuppressant, the agent for the prophylaxis and treatment of allergic diseases, the agent for the prophylaxis and treatment of eosinophil-related diseases, the eosinophilia inhibitor and the novel triazole derivative of the present invention all, have superior eosinophilia-inhibitory action and lymphocyte activation-inhibitory action.Type: GrantFiled: January 23, 1996Date of Patent: May 12, 1998Assignee: The Green Cross CorporationInventors: Fumihiko Akahoshi, Takehiro Okada, Shinji Takeda, Youichiro Naito, Chikara Fukaya, Shigeki Kuwahara, Masahiko Kajii, Hiroko Nishimura, Masanori Sugiura
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Patent number: 5747516Abstract: Dihydroisoxazoles, dihydroisothiazoles, dihydropyrazoles, dihydrothiazoles and dihydroimidazoles of Formula I ##STR1## wherein: A is O; S; N; NR.sup.5 ; or CR.sup.14 ;G is C or N; provided that when G is C, A is O, S or NR.sup.5 and the floating double bond is attached to G; and when G is N, A is N or CR.sup.14 and the floating double bond is attached to A;W is O or S;X is OR.sup.1, S(O).sub.m R.sup.1 or halogen; andY, Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.14, and n are defined in the disclosure, are disclosed.Also disclosed are fungicidal compositions containing these compounds, and use of these cyclic amide compounds for controlling plant diseases caused by fungal plant pathogens.Type: GrantFiled: May 8, 1996Date of Patent: May 5, 1998Assignee: E. I. du Pont de Nemours and CompanyInventors: Richard James Brown, King-Mo Sun, Deborah Ann Frasier
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Patent number: 5703065Abstract: The invention relates to compounds of the formula ##STR1## and to pharmaceutically acceptable salts thereof, wherein A, W, P, R.sup.3, Q and R.sup.1 are as defined herein. The compounds of formula I, and pharmaceutically acceptable salts thereof, are substance P antagonists and as such are useful in the treament of various inflammatory and central nervous system disorders.Type: GrantFiled: May 7, 1996Date of Patent: December 30, 1997Assignee: Pfizer Inc.Inventor: Harry R. Howard, Jr.
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Patent number: 5661170Abstract: Antimicrobial compositions useful in the treatment of microbial infections and as general cleansers are provided along with methods for their administration. The antimicrobial compositions are aqueous based and preferably contain a quaternary ammonium compound as a antimicrobial agent. The antimicrobial compositions also preferably contain a surfactant such as a cationic, nonionic, or amphoteric surfactant or mixtures thereof. A keratolytic agent, such as allantoin, is also preferably blended into the antimicrobial compositions. The antimicrobial compositions are ideally suited for subcutaneous, cutaneous, or mucosal membrane administration.Type: GrantFiled: June 12, 1996Date of Patent: August 26, 1997Assignee: Woodward Laboratories, Inc.Inventor: Daniel Frank Chodosh
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Patent number: 5637605Abstract: Compounds of formula I ##STR1## wherein Z, R, R.sub.1, R.sub.2 and X are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.Type: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: Ciba Geigy CorporationInventors: Marc Lang, Edmond Differding, Jaroslav Stanek
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Patent number: 5635522Abstract: A suppression of the human immune system is accomplished by administering to the person an effective amount of a non-toxic thioheterocycle compound having the formula ##STR1## wherein R1 is a heterocycle ring system, R2 is a hydrogen, alkyl or aryl group, and R3 is a hydrogen, alkyl, aryl or nitroaryl group.Type: GrantFiled: February 23, 1996Date of Patent: June 3, 1997Assignee: The University of SheffieldInventors: David N. Jones, John L. Maddocks
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Patent number: 5631281Abstract: Novel unnatural dipeptoids of .alpha.-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal tumors, or as antipsychotics are disclosed. Further the compounds are antianxiety agents, antiulcer agents, antidepressant agents, and are agents useful for preventing the withdrawal response produced by chronic treatment or use followed by chronic treatment followed by withdrawal from nicotine, diazepam, alcohol, cocaine, caffeine, or opiods. Also disclosed are pharmaceutical compositions and methods of treatment using the dipeptoids as well as processes for preparing them and novel intermediates useful in their preparation. An additional feature of the invention is the use of the subject compounds to prepare pharmaceutical and diagnostic compositions.Type: GrantFiled: April 28, 1994Date of Patent: May 20, 1997Assignee: Warner-Lambert CompanyInventors: David C. Horwell, Martyn C. Pritchard, Edward Roberts, Reginald S. Richardson, Julian Aranda
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Patent number: 5624916Abstract: 2-Aryl or 2-heterocyclyl-2, 2-disubstituted ethyl-1,2,4-triazoles have been shown to have fungicidal activity.Type: GrantFiled: June 12, 1995Date of Patent: April 29, 1997Assignee: Rohm and Haas CompanyInventors: Steven H. Shaber, Luong T. Nguyen
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Patent number: 5622917Abstract: The invention relates to new 1H-3-aryl-pyrrolidine-2,4-dione derivatives of the formula (I) ##STR1## in which A, B, X, Y and G have the meanings given in the description, to a plurality of processes for their preparation, and to their use as pesticides.Type: GrantFiled: January 3, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Bernd-Wieland Kr uger, Michael Ruther, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger
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Patent number: 5601801Abstract: Angiotensin convening enzyme (ACE) inhibitors can be labelled with Iodine-123, Iodine-125, Iodine-127 or Iodine-131, useful to image the kidneys and lungs for diagnosis and treatment of diseases such as essential hypertension, renal artery stenosis, or diabetes which are associated with a change in the amount of ACE present in the human body.Type: GrantFiled: August 2, 1994Date of Patent: February 11, 1997Assignee: Merck Frosst Canada, Inc.Inventors: Richard J. Flanagan, Duncan H. Hunter, Vincenzo Quiquero, Pamela Zabel
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Patent number: 5591692Abstract: Compositions and methods are disclosed for sanitizing aqueous media, which combine a chlorine-source composition and a glycoluril-source composition. The compositions are added together or separately, continuously or periodically, and by any of a variety of methods. The glycoluril compound stabilizes the chlorine and prolongs its useful life as a microbicidal agent.Type: GrantFiled: December 13, 1994Date of Patent: January 7, 1997Assignee: Bio-Lab, Inc.Inventors: Ronald L. Jones, Henry D. Caughman, Susan M. Shelor, Ellwood L. Lines, Jr.
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Patent number: 5583128Abstract: The invention relates to the use of aromatase inhibitors for contraception in female primates and to a method for contraception in female primates using such substances and to the use of those substances for the preparation of pharmaceutical compositions for contraception in female primates.Type: GrantFiled: September 2, 1994Date of Patent: December 10, 1996Assignee: Ciba-Geigy CorporationInventor: Ajay Bhatnagar