The Ring Is A Benzene Ring Patents (Class 514/485)
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Patent number: 6342624Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.Type: GrantFiled: January 6, 2000Date of Patent: January 29, 2002Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 6297275Abstract: A method for controlling fungi using a phenylhydrazine derivative compound of the formula: wherein: X is phenyl, phenylalkoxy, phenoxy, or benzyl, alone or in combination with one or more halogen, alkyl, or alkylthio; Y is hydrogen, alkanoyl, haloalkanoyl, or alkoxy carbonyl; and R is hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, or phenylalkoxy.Type: GrantFiled: September 7, 1999Date of Patent: October 2, 2001Assignees: Uniroyal Chemical Company, Inc., Crompton Co./CieInventors: Mark Achiel Dekeyser, Kenneth Wesley Seebold, Jr., Gaik-Lean Chee
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Publication number: 20010002403Abstract: Methods for the treatment of cancers or viral infections in mammals are disclosed that include administration of an N-chlorophenylcarbamate, or an N-chlorophenylthiocarbamate, or a salt thereof. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: ApplicationFiled: December 22, 2000Publication date: May 31, 2001Applicant: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6232339Abstract: Phenylcarbamates of the formula I where: R1 is C1-C4-alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, C1-C4-alkyl and C1-C4-alkoxy; m is 0, 1 or 2, where the radicals R2 may be different if m is 2; R3 is hydrogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl; R4, R5 and R6 are each as defined in claim 1, and salts thereof, a process and intermediates for preparing these compounds and compositions comprising them for controlling animal pests and harmful fungi are described.Type: GrantFiled: July 21, 1999Date of Patent: May 15, 2001Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Hubert Sauter, Herbert Bayer, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Arne Ptock, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Volker Harries, Franz Röhl
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Patent number: 6197805Abstract: This invention is directed to a broad spectrum antimicrobial composition which comprises a mixture of an iodopropynyl compound in combination with 2-(methoxycarbonylamino)benzimidazole and, where desirable, an algicide said mixture provided in an amount sufficient to protect a substrate from attack by one or more organisms. The composition can be used broadly in industrial systems and more particularly with substrates such as paints, coatings, stucco, concrete, stone, cementaceous surfaces, wood, caulking, sealants, textiles, leather, wood, preservatives, metal working fluids, drilling muds, clay slurries, glazes, optical brightness, carpet backing, pigments and as a preservative for other aqueous and wet state products, and the like.Type: GrantFiled: May 27, 1999Date of Patent: March 6, 2001Assignee: Troy Technology Corporation, Inc.Inventor: Roger Errol Smith
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Patent number: 6177460Abstract: Methods for the treatment of cancers or viral infections in mammals are disclosed that include administration of an N-chlorophenylcarbamate, or an N-chlorophenylthiocarbamate, or a salt thereof. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.Type: GrantFiled: September 29, 1999Date of Patent: January 23, 2001Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 6172108Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptorType: GrantFiled: December 16, 1999Date of Patent: January 9, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
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Patent number: 6117900Abstract: The invention relates to the use of 2-amino-4-(4-fluorobenzylamino)-1-ethoxycarbonylaminobenzene of formula I ##STR1## or its pharmaceutically utilizable salts, for the prophylaxis and treatment of neuropathic pain.Type: GrantFiled: September 27, 1999Date of Patent: September 12, 2000Assignee: ASTA Medica AktiengesellschaftInventors: Chris Rundfeldt, Reni Bartsch, Angelika Rostock, Christine Tober, Rita Dost
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Patent number: 6060484Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: May 9, 2000Assignee: Eli Lilly and CompanyInventors: James E. Fritz, Stephen W. Kaldor, Jeffrey A. Kyle, John E. Munroe
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Patent number: 6043284Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: February 5, 1998Date of Patent: March 28, 2000Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 6040339Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.Type: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 5994398Abstract: Arylsulfonamides which have the general structure: with the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and n representing the groups and integers provided in the detailed description are provided herein. These compounds have activity as inhibitors of phospholipase A2, inhibitors of cytokine release and as inhibitors of neurodegeneration.Type: GrantFiled: December 11, 1996Date of Patent: November 30, 1999Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Russell E. Rydel, Eugene D. Thorsett
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Patent number: 5962511Abstract: A method of inhibiting human IL-5 gene transcriptions mRNA expression and protein production by human T-cells using one or more compounds selected from those shown by formula I shown below (where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group) and a therapeutic agent for allergic and eosinophilic inflammatory diseases which contains one or more compounds selected from those shown by the formula.Type: GrantFiled: June 22, 1998Date of Patent: October 5, 1999Assignee: Environmental Research Institute, Inc.Inventors: Hirokazu Okudaira, Akio Mori
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5942541Abstract: There are described new amino acid amide derivatives, some of which are known, of the formula (I) ##STR1## in which R.sup.1 to R.sup.8 have the meaning given in the description, and a process for their preparation. The amino acid amide derivatives of the formula (I) are used for the preparation of pesticides.Type: GrantFiled: July 18, 1997Date of Patent: August 24, 1999Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Heinz-Wilhelm Dehne
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Patent number: 5942548Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: March 24, 1998Date of Patent: August 24, 1999Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5886046Abstract: This invention relates to chemical compounds that contain adjacent carbonyl groups, which effectively inhibit the biological, chemical, and/or physical properties of enzymes and other medicinally-significant proteins. In particular, the invention relates to dicarbonyl compounds that are capable of acting as enzyme inhibitors, including irreversible inhibitors of HIV-1 protease.Type: GrantFiled: January 19, 1996Date of Patent: March 23, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Ralph F. Hirschmann, Amos B. Smith, III, Paul Sprengeler, Wenqing Yao, Paul Anderson
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Patent number: 5874465Abstract: Compounds having the structural formula: ##STR1## wherein: R is C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkyl, C.sub.7 -C.sub.9 aralkyl, or nitroso; R' is C.sub.1 -C.sub.4 alkyl; and R" is C.sub.1 -C.sub.4 alkyl. These compounds exhibit insecticidal and miticidal activity.Type: GrantFiled: October 24, 1996Date of Patent: February 23, 1999Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Co./CIE.Inventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5852053Abstract: The use of the compound I ##STR1## or its pharmaceutically utilizable salts for the propylaxis and treatment of the squelae of chronic reduced cerebral blood supply, in particular of stroke, and for the treatment of nuerodegenerative disorders is claimed.Type: GrantFiled: October 28, 1996Date of Patent: December 22, 1998Assignee: Asta Medica AktiengesellschaftInventors: Angelika Rostock, Chris Rundfeldt, Christine Tober, Reni Bartsch
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Patent number: 5849789Abstract: The use of the compound I ##STR1## or its pharmaceutically utilizable salts for the propylaxis and treatment of the sequel of chronic reduced cerebral blood supply, in particular of stroke, and for the treatment of neurodegenerative disorders is claimed.Type: GrantFiled: September 25, 1997Date of Patent: December 15, 1998Assignee: Asta Medica AktiengesellschaftInventors: Angelika Rostock, Chris Rundfeldt, Christine Tober, Reni Bartsch
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Patent number: 5830854Abstract: Tachykinin receptor antagonists are useful for the treatment of cystic fibrosis.Type: GrantFiled: June 27, 1995Date of Patent: November 3, 1998Assignee: Merck Sharp & Dohme, LimitedInventor: Richard John Hargreaves
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Patent number: 5824705Abstract: Carbamates of the formula I ##STR1## where the substituents have the following meanings: Z is methoxy, NH.sub.2, NHCH.sub.3, N(CH.sub.3).sub.2, CH.sub.3, C.sub.2 H.sub.5, CF.sub.3 or CCl.sub.3,X and Y are identical or different and each is hydrogen, F, Cl, Br, CF.sub.3, CN, NO.sub.2, alkoxy, alkenyloxy, alkynyloxy, alkyl, alkenyl or alkynyl or may be condensed together to form a substituted or unsubstituted aromatic or heteroaromatic, alicyclic or heterocyclic, partially or completely hydrogenated ring,R.sup.1 may also be substituted or unsubstituted and is O-alkyl, O-alkenyl, O-alkynyl, O-cycloalkyl, O-cycloalkenyl or O--CO.sub.2 -alkyl,A is --O--, --S--, --CR.sup.2 .dbd.CR.sup.3 --, CHR.sup.2 --O--, --CHR.sup.2 --S--, --CHR.sup.2 --O--N.dbd.C(R.sup.4)--, --CR.sup.2 .dbd.N--O--, --O--N.dbd.C(R.sup.4)--, --C.tbd.C--, --CHR.sup.2 --CHR.sup.3 --, --CHR.sup.2 --O--CO--, --O--CHR.sup.Type: GrantFiled: July 29, 1994Date of Patent: October 20, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Mueller, Hubert Sauter, Franz Roehl, Reinhard Doetzer, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5821260Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: October 13, 1998Assignee: Emory UniversityInventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
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Patent number: 5807884Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: October 4, 1994Date of Patent: September 15, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
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Patent number: 5792787Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: August 11, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Margaret K. Offermann
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Patent number: 5783596Abstract: Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of cardiovascular disease, including atherosclerosis, post-angioplasty restenosis, coronary artery diseases, and angina, as well as noncardiovascular inflammatory diseases that are mediated by VCAM-1.Type: GrantFiled: June 7, 1995Date of Patent: July 21, 1998Assignee: Emory UniversityInventors: Russell M. Medford, Margaret K. Offermann, R. Wayne Alexander, Sampath Parthasarathy
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Patent number: 5773465Abstract: Tartronic acid acetalic ethers and esters of the general formula: ##STR1## are provided and are useful in treatment of bone dysmetabolism. As examples, Ra and Rb may be hydrogen, B is a C.sub.2 -C.sub.12 acyl group, R is phenyl and n is 0-12.Type: GrantFiled: March 12, 1997Date of Patent: June 30, 1998Assignee: Dompe Farmaceutici S.p.A.Inventors: Carmelo A. Gandolfi, Lorella Cotini, Marco Mantovanini, Gianfranco Caselli, Gaetano Clavenna, Claudio Omini
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Patent number: 5773209Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
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Patent number: 5773231Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
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Patent number: 5750351Abstract: A method for the treatment of cardiovascular diseases and noncardiovascular inflammatory diseases that are mediated by VCAM-1 is provided that includes the removal, decrease in the concentration of, or prevention of the formation of oxidized polyunsaturated fatty acids, or interferes with a complex formed between a polyunsaturated fatty acid or an oxidized polyunsaturated fatty acid and a protein or peptide that mediates the expression of VCAM-1. A method is also provided for suppressing the expression of a redox-sensitive gene or activating a gene that is suppressed through a redox-sensitive pathway, that includes administering an effective amount of a substance that prevents the oxidation of the oxidized signal, and typically, the oxidation of a polyunsaturated fatty acid, or interferes with a complex formed between the oxidized signal and a protein or peptide that mediates the expression of the redox gene.Type: GrantFiled: June 7, 1995Date of Patent: May 12, 1998Assignee: Emory UniversityInventors: Russell M. Medford, R. Wayne Alexander, Sampath Parthasarathy, Bobby V. Khan
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5721270Abstract: A method of inhibiting human IL-5 gene transcription, mRNA expression and protein production by human T-cells using one or more compounds selected from those shown by formula I shown below (where R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.6 alkyl group) and a therapeutic agent for allergic and eosinophilic inflammatory diseases which contains one or more compounds selected from those shown by the formula.Type: GrantFiled: September 12, 1995Date of Patent: February 24, 1998Assignee: Environmental Research Institute, Inc.Inventors: Hirokazu Okudaira, Akio Mori
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Patent number: 5709890Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 20, 1997Date of Patent: January 20, 1998Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5658945Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: August 19, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5656615Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition contains a 10:1 to 1:10 mixture of (1) N-chlorophenyl carbamates and N-chlorophenylthiocarbamates and (2) N-phosphonoglycine derivatives which are systemic herbicides. This composition can also be used to treat viral infections.Type: GrantFiled: April 12, 1995Date of Patent: August 12, 1997Assignee: The Procter & Gamble CompanyInventor: James Berger Camden
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Patent number: 5646133Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.Type: GrantFiled: March 14, 1996Date of Patent: July 8, 1997Assignee: Donlar CorporationInventor: J. Larry Sanders
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Patent number: 5629341Abstract: This invention is a pharmaceutical composition that inhibits the growth of cancers and tumors in mammals, particularly in human and warm blooded animals. The composition is also effective against viruses. The composition contains N-chlorophenylcarbamates and N-chlorophenylthiocarbamates which are systemic herbicides.Type: GrantFiled: April 12, 1995Date of Patent: May 13, 1997Assignee: The Procter & Gamble CompanyInventor: James B. Camden
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Patent number: 5616612Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 25, 1995Date of Patent: April 1, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5574029Abstract: The present invention provides a method for treating anxiety in a human in need thereof, comprising administering an antianxiety amount of a muscarinic agonist compound of the general formula ##STR1## wherein X R.sup.43, R.sup.44, R.sup.45 and R.sup.46 are defined in the disclosure.Type: GrantFiled: May 23, 1995Date of Patent: November 12, 1996Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5545640Abstract: Disclosed herein are compounds which inhibit human immunodeficiency virus (HIV) protease activity and inhibit HIV replication in human cells. Thus, the compounds are indicated for the treatment of HIV infections. The compounds can be represented by the formula ##STR1## wherein X is a terminal group, for example, an aryloxycarbonyl, an alkanoyl or an arylalkyl carbamoyl; A is absent or an amino acid or a derived amino acid; either R.sup.1 or R.sup.2 is hydrogen while the other is alkyl or R.sup.1 and R.sup.2 are joined to form a cyclohexane; Q is hydrogen, hydroxy, halo or lower alkoxy; and Y is a terminal group, for example, an alkylamino, alkoxy or an optionally substituted anilino.Type: GrantFiled: April 4, 1995Date of Patent: August 13, 1996Assignee: Bio-Mega/Boehringer Ingeleheim Research Inc.Inventors: Pierre L. Beaulieu, Ingrid Guse
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Patent number: 5484811Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 B is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexyimethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: February 23, 1994Date of Patent: January 16, 1996Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5484812Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of ophthalmic disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, b, b, b-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: February 28, 1994Date of Patent: January 16, 1996Assignee: G.D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5459149Abstract: The present Application discloses pesticidally active compounds of formula (I):Q(CH.sub.2).sub.a (O).sub.b Q.sup.1 CR.sup.2 =CR.sup.3 CR.sup.4 =CR.sup.5 CXNR.sup.1 R.sup.xor a salt or propesticide thereof, wherein Q is an optionally substituted aromatic monocyclic or fused bicyclic ring system in which at least one ring is aromatic, or Q is a dihalovinyl group or a group R.sup.6 --C=C--where R.sup.6 is C.sub.1-4 alkyl, tri C.sub.1-4 alkylsilyl, halo or hydrogen; Q.sup.1 is a 1,2-cyclopropyl ring optionally substituted by one or more groups selected from C.sub.1-3 alkyl, halo, C.sub.1-3 haloalkyl, C.sub.2-3 alkynyl, or cyano; or Q.sup.1 is (CH.sub.2).sub.7 ; a=0 or 1; b=0 or 1; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different with at least one being hydrogen and the others being independently selected from hydrogen, halo, C.sub.1-4 alkyl or C.sub.1-4 haloalkyl; X is oxygen or sulphur;R.sup.1 is phenyl optionally substituted by 1-5 substituents chosen from: a) C.sub.1-4 alkyl, C.sub.Type: GrantFiled: September 20, 1994Date of Patent: October 17, 1995Assignee: Roussel UclafInventors: John E. Robinson, George S. Cockerill
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Patent number: 5436267Abstract: A novel N-phenylcarbamate compound or its salt where possible, which is useful as the active ingredient of a biocidal composition for control of harmful organisms, is represented by the following general formula (I): ##STR1## wherein R.sup.1 is unsubstituted or substituted alkyl; R.sup.2 is H, unsubstituted or substituted alkyl, alkenyl, alkynyl or cycloalkyl, or --COX.sup.1 wherein X.sup.1 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl or alkoxy; Z is --CH.sub.2 S--, --SCH.sub.2 --, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 SCH.sub.2 --, or --CH.sub.2 O--N.dbd.C(R.sup.4)--; R.sup.Type: GrantFiled: July 11, 1994Date of Patent: July 25, 1995Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Terumasa Komyoji, Itaru Shigehara, Norifusa Matsuo, Hiroshi Shimoharada, Takeshi Ohshima, Toshio Akagi, Shigeru Mitani
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Patent number: 5393776Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.Type: GrantFiled: May 13, 1994Date of Patent: February 28, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Bradley C. Pearce
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Patent number: 5384328Abstract: The present invention is directed to compounds of the following general Formula I, methods for using the compounds of Formula I, pharmaceutical compositions thereof, and processes for preparing the compounds. ##STR1## wherein X is oxygen or sulfur; wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl;wherein each of R.sub.1 and R.sub.2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a 5- or 6-membered monocyclic or fused bicyclic heterocyclic group, or a hydrocarbon chain having from 1 to 20 carbon atoms and from 1 to 3 double bonds.Type: GrantFiled: May 21, 1993Date of Patent: January 24, 1995Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5356931Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.Type: GrantFiled: January 4, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Rainer Otter, Christoph Kuenast, Uwe Kardorff, Wolfgang Steglich, Gunda Bertram
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Patent number: 5344845Abstract: Disclosed herein is a specific cinnamic acid derivative such as methyl 4-(4-acetoxy-3-methoxycinnamanide)-1-cyclohexanecarboxylate, or a pharmaceutically acceptable salt thereof. These compounds are useful as IV-type allergic reaction-suppressive drugs.Type: GrantFiled: December 4, 1992Date of Patent: September 6, 1994Assignee: Tsumura & Co.Inventors: Akihide Koda, Koji Waragai, Yutaka Ono, Hideyuki Ozawa, Hideki Kawamura, Masao Maruno, Takeshi Wakamatsu
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Patent number: 5312831Abstract: The invention relates to novel ureas and urethanes of Formula I: ##STR1## which stimulate cytokine production and may be used to accelerate recovery from neutropenia accompanying radio- or chemotherapy, bone marrow transplantation, or infections. Compounds in the invention or pharmaceutical compositions employing these compounds may be useful in the treatment of cancer, AIDS, aplastic anemia, myelodysplastic syndrome, and infectious diseases, and in the enhancement of immune response.Type: GrantFiled: May 12, 1993Date of Patent: May 17, 1994Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5268389Abstract: A method of inhibiting the growth or replication of viruses of the HIV group is disclosed. Also disclosed are compounds useful in the method and pharmaceutical formulations incorporating such compounds. The method involves the use of compounds having the general formula: ##STR1## wherein the substituent groups are as defined in the specification.Type: GrantFiled: September 26, 1990Date of Patent: December 7, 1993Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: William A. Harrison, Ethel E. Felauer, Walter G. Brouwer