Ring In Acid Moiety Patents (Class 514/484)
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Patent number: 5922761Abstract: In accordance with the present invention, there are provided methods for the in vivo reduction of free iron ion levels in a mammalian subject. The present invention employs a scavenging approach whereby free iron ions are bound in vivo to a suitable physiologically compatible scavenger. The resulting complex renders the free iron ions harmless, and is eventually excreted in the urine of the host. Further in accordance with the present invention, there are provided compositions and formulations useful for carrying out the above-described methods. An exemplary scavenger contemplated for use in the practice of the present invention is a dithiocarbamate-containing composition. This material binds to free iron ions, forming a stable, water-soluble dithiocarbamate-iron complex.Type: GrantFiled: September 6, 1996Date of Patent: July 13, 1999Assignee: Medinox, Inc.Inventor: Ching-San Lai
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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: 5840746Abstract: The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor.Type: GrantFiled: September 5, 1997Date of Patent: November 24, 1998Assignee: Merck Frosst Canada, Inc.Inventors: Yves Ducharme, Jacques Yves Gauthier, Petpiboon Prasit, Yves Leblanc, Zhaoyin Wang, Serge Leger, Michel Therien
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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: 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: 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: 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: 5728729Abstract: 3-Methoxy-2-phenyl-acrylic esters of the formula ##STR1## in which R represents optionally substituted alkyl, cycloalkyl or aryl andn represents a number 0 or 1,a process for their preparation and their use as pesticides.Type: GrantFiled: November 13, 1995Date of Patent: March 17, 1998Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Heinz-Wilhelm Dehne
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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: 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: 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: 5565490Abstract: p-Hydroxyaniline derivatives of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen, or unsubstituted or substituted alkyl;R.sup.2 and R.sup.3 independently of one another are halogen, alkyl, haloalkyl, alkoxy or haloalkoxy;R.sup.4 is unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl,OR.sup.5 or NR.sup.6 R.sup.7, whereR.sup.5, R.sup.6 are unsubstituted or substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl or aryl, andR.sup.7 is hydrogen or alkyl,and their salts, processes for their preparation, compositions containing them and their use for controlling harmful fungi or pests, and also compounds of the formula VI ##STR2## and their salts, processes for their preparation, compositions containing them and their use as intermediates and for controlling pests are described.Type: GrantFiled: November 10, 1994Date of Patent: October 15, 1996Assignee: BASF AktiengesellschaftInventors: Oliver Wagner, Karl Eicken, Norbert G otz, Harald Rang, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5545662Abstract: 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: March 14, 1994Date of Patent: August 13, 1996Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr
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Patent number: 5510378Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: April 23, 1996Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5504109Abstract: Amino-acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl, cycloalkenyl, unsubstituted or substituted aryl, unsubstituted or substituted aralkyl, unsubstituted or substituted heteroaryl, and unsubstituted or substituted heteroarylalkyl,R.sup.2, R.sup.5 are identical or different and represent hydrogen or lower alkyl,R.sup.3, R.sup.4 represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring,R.sup.6 represents unsubstituted or substituted straight-chain or branched cycloalkylalkyl, unsubstituted or substituted straight-chain or branched cycloalkenyl, alkyl, or alkyl-bridged cycloalkylalkyl.The compounds are useful as pesticidal agents.Type: GrantFiled: November 13, 1992Date of Patent: April 2, 1996Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Heinz-Wilhelm Dehne
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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: 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: 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: 5227401Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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.6 is independently selected from hydrido and methyl; wherein R.Type: GrantFiled: October 29, 1991Date of Patent: July 13, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5223535Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension. 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 each of R.sub.5 and R.sub.8 is independently propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.Type: GrantFiled: October 29, 1991Date of Patent: June 29, 1993Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5217994Abstract: Compounds of the general formula ##STR1## and the pharmaceutically acceptable salts thereof whereinn is an integer of from 0 to 6;Y is CH.sub.2, O, SO.sub.2, --CONH--, --NHCO--, or ##STR2## R.sup.1 and R.sup.2 are independently hydrogen,C.sub.1-8 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,amino C.sub.1-4 alkyl,C.sub.1-4 alkylamino C.sub.1-4 alkyl, orC.sub.3-8 cycloalkylwherein R.sup.1 and R.sup.2 may be unsubstituted or substituted with one or more groups chosen from R.sup.3, whereR.sup.3 ishydrogen,C.sub.1-6 alkyl,hydroxy C.sub.0-4 alkyl,carboxy C.sub.0-4 alkyl,C.sub.1-4 alkyloxy C.sub.0-4 alkyl,heterocyclyl C.sub.0-4 alkyl,aryl C.sub.0-4 alkyl,halogen, orCF.sub.3 ;R.sup.4 isC.sub.1-6 alkyl,heterocyclyl C.sub.0-4 alkyl, oraryl C.sub.0-4 alkyl;R.sup.5 ishydrogen,C.sub.1-6 alkyl,aryl C.sub.0-3 alkyl, orC.sub.1-6 alkylcarbonyloxymethylare used in a method of treating osteoporosis by inhibiting the bone resorption activity of osteoclasts.Type: GrantFiled: August 9, 1991Date of Patent: June 8, 1993Assignee: Merck & Co., Inc.Inventors: Melissa S. Egbertson, Robert J. Gould, George D. Hartman
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Patent number: 5210084Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl, orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.Type: GrantFiled: April 25, 1990Date of Patent: May 11, 1993Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Thomas Seitz, Wilhelm Brandes
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Patent number: 5177109Abstract: Compounds, compositions and methods are described for treating a CNS disorder such as a cognitive disorder, epilepsy, depression, Parkinson's disease, Alzheimer's disease, a neurodegenerative disease or neurotoxic injury. Compound of interest are 2-amino-4,5-methyleneadipic acid compounds and derivatives defined by the formula I: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, ##STR2## with each of R.sup.2, R.sup.3, R.sup.4 and R.sup.5 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein each of X and Y is independently selected from hydroxyl, alkoxy, alkylthio, amino and ##STR3## with each of R.sup.6 and R.sup.7 being independently selected from hydrido, alkyl, cycloalkyl, aryl and aralkyl; wherein any of R.sup.1 through R.sup.Type: GrantFiled: July 19, 1991Date of Patent: January 5, 1993Assignee: G. D. Searle & Co.Inventors: Roberto Pellicciari, Benedetto Natalini, Maura Marinozzi, Alexis A. Cordi, Joseph B. Monahan, Thomas H. Lanthorn
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Patent number: 5112859Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.Type: GrantFiled: September 14, 1990Date of Patent: May 12, 1992Assignee: American Home Products CorporationInventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
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Patent number: 5047420Abstract: Novel 1,3-diaryl cyclopentanes of the following general formula were prepared. ##STR1## These compounds were found to have potent and specific PAF (Platelet Activating Factor) antagonistic activities and as such useful in the treatment or amelioration of various diseases or disorders mediate by the PAF, for example, hypotension, inflammation, nephritis, stroke and other cardiovascular disorders, asthma, allergic and skin diseases, peptic or stomach ulcer, shock, lung edema, psoriasis, adult respiratory distress syndrome, pain including dental pain, and aggregation of platelets.Type: GrantFiled: August 21, 1989Date of Patent: September 10, 1991Assignee: Merck & Co., Inc.Inventors: Donald W. Graham, Tesfaye Biftu, John C. Chabala, Michael N. Chang, Yuan-Ching P. Chiang, Kathryn L. Thompson, Shu S. Yang
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Patent number: 4996201Abstract: 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.Type: GrantFiled: August 2, 1989Date of Patent: February 26, 1991Assignee: Warner-Lambert Co.Inventors: Stephen C. Bergmeier, Jeffrey A. Kester, Walter H. Moos, Haile Tecle, Anthony J. Thomas
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Patent number: 4983630Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.Type: GrantFiled: November 28, 1988Date of Patent: January 8, 1991Assignee: Schering AktiengesellschaftInventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
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Patent number: 4975444Abstract: Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.Type: GrantFiled: August 25, 1989Date of Patent: December 4, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James, Ryszard J. Kobylecki
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Patent number: 4963583Abstract: Novel 3-acyloxy-4-keto-.beta.-ionone derivatives of the formula I ##STR1## wherein Z is either the radical ##STR2## in which R.sub.1 represents C.sub.2 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy-C.sub.1 -C.sub.5 alkyl having a maximum number of 6 carbon atoms, cyclopropyl or cyclopropyl which is substituted by methyl or by halogen or represents the radical ##STR3## wherein R.sub.2 represents C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy-C.sub.1 -C.sub.5 alkyl having a maximum number of 6 carbon atoms, cyclopropyl or cyclopropyl which is substituted by methyl or by halogen and X represents either oxygen or sulphur, and ##STR4## display very effective microbicidal activity. They can especially be used in microbicidal compositions to control plant-pathogenic microorganisms, preferably fungi of the order Oomycetes.Type: GrantFiled: September 28, 1988Date of Patent: October 16, 1990Assignee: Ciba-Geigy CorporationInventor: Walter Kunz
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Patent number: 4960792Abstract: 2-Acylaminoalkyl-3-[1-(carboxycycloalkylcarbamoyl)cycloalkyl]propanoic acid derivatives (which may also be viewed as glutaramide derivatives) are useful in the treatment of hypertension, heart failure and renal insufficiency, based upon their inhibition of zinc-dependant, neutral endopiptidase.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Pfizer Inc.Inventors: John C. Danilewicz, Keith James
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Patent number: 4948807Abstract: Phenyl carbamates of the general formula ##STR1## wherein R.sub.1 to R.sub.5 are as defined in the claims, are useful as pharmaceuticals.Type: GrantFiled: March 8, 1989Date of Patent: August 14, 1990Assignee: Proterra AGInventors: Marta W. Rosin, Michael Chorev, Zeev Tashma
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Patent number: 4943307Abstract: The invention relates to a plant-protective solution containing 2.5 to 40 % by weight of one or more water-insoluble plant-protective ingredient(s) 20 to 71.5 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 10 to 71.5 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 1 to 15 % by weight of commonly used additives such as anionic and/or nonionic surface active agents and macromolecules.The invention also relates to the ready-for-use plant-protective suspension containing 0.2 to 10 % by weight of one or more water-insoluble plant-protective ingredient(s) with a particle size of 0.1 to 50 .mu.m, 0 to 60 % by weight of a fertilizer, 0.2 to 10 % by weight of dimethylformamide and/or dimethylsulfoxide and/or acetone as water-miscible solvent, 0.2 to 10 % by weight of furfurol and/or furfuryl alcohol as partially water-miscible solvent, 0.05 to 2.Type: GrantFiled: July 15, 1988Date of Patent: July 24, 1990Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Tamas Detre, Sandor ngyan, Laszlo Pap, Andras Szego, Zoltan Karadi, Klara Bertus nee Bende, Katalin Marmarosi nee Kellner
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4853382Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar represents a phenyl group optionally substituted by one or more substituents selected from halogen atoms, or the groups C.sub.1-6 alkyl, C.sub.1-6 alkoxy, nitro, --(CH.sub.2).sub.q R, [where R is hydroxy, --NR.sup.3 R.sup.4 (where R.sup.3 and R.sup.4 each represents a hydrogen atom, or a C.sub.1-4 alkyl group, or --NR.sup.3 R.sup.4 forms a saturated heterocyclic amino group which has 5-7 ring members and optionally contains in the ring one or more atoms selected from --O-- or --S-- or a group --NH-- or --N(CH.sub.3)--), --NR.sup.5 COR.sup.6 (where R.sup.5 represents a hydrogen atom or a C.sub.1-4 alkyl group, and R.sup.6 represents a hydrogen atom or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or --NR.sup.3 R.sup.4 group), --NR.sup.5 SO.sub.2 R.sup.7 (where R.sup.7 represents a C.sub.1-4 alkyl, phenyl or --NR.sup.3 R.sup.4 group), --COR.sup. 8 (where R.sup.8 represents hydroxy, C.sub.1-4 alkoxy or --NR.sup.3 R.sup.4), --SR.sup.Type: GrantFiled: November 24, 1987Date of Patent: August 1, 1989Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4760057Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.Type: GrantFiled: April 22, 1985Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Jose Alexander
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Patent number: 4735959Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.Type: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4730008Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar, R.sup.1, R.sup.2, X, Y and Q are defined in the specification and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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Patent number: 4728670Abstract: Biphenyl hydroxamic acids are provided having the structure ##STR1## wherein m is 1 to 7, X is S, O or NH, R is H, lower alkyl, aryl, aralkyl or cycloalkyl and R.sup.1 is H, lower alkyl, aryl, aralkyl, cycloalkyl, alkanoyl or aroyl.These compounds are inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.Type: GrantFiled: June 4, 1986Date of Patent: March 1, 1988Assignee: E. R. Squibb & Sons, Inc.Inventors: Martin F. Haslanger, Ravi K. Varma, Eric M. Gordon
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Patent number: 4513005Abstract: There are described pharmacologically active compounds, useful in the treatment of allergic/inflammatory disorders involving SRS-A as causal mediator and which, in free acid form, are of formula I, ##STR1## in which R.sub.1 is (i) an aliphatic, saturated or unsaturated hydrocarbyl radical of up to 20 carbon atoms, unsubstituted or substituted by at least one substituent selected from halogen, hydroxy, C.sub.3-6 alkoxy, C.sub.3-6 cycloalkyl, aryl or heteroaryl, the cycloalkyl, aryl or heteroaryl being unsubstituted or substituted by at least one substituent selected from hydroxy, halogen and alkyl, alkenyl or alkynyl of up to 10 carbon atoms,(ii) cycloalkyl of 3 to 8 carbon atoms unsubstituted or substituted by alkyl, alkenyl or alkynyl of up to 16 carbon atoms, or(iii) aryl or heteroaryl, unsubstituted or substituted by hydroxyl, C.sub.1-4 alkoxy, halogen or alkyl, alkenyl or alkynyl of up to 16 carbon atoms; and R.sub.Type: GrantFiled: June 9, 1982Date of Patent: April 23, 1985Assignee: Lilly Industries LimitedInventors: Stephen R. Baker, William B. Jamieson, William J. Ross, Alec Todd