Ureido, Guanido Or Hydrazino In Acid Moiety Patents (Class 560/34)
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Patent number: 5707966Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 13, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5705487Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.Type: GrantFiled: September 1, 1995Date of Patent: January 6, 1998Assignee: Eli Lilly and CompanyInventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
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Patent number: 5698569Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: December 16, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5658944Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein Ar is a mono- or bicyclic aromatic group optionally containing one or two heteroatoms independently selected from nitrogen, oxygen and sulphur, said group being optionally substituted by one or more atoms or groups independently selected from halogen, nitro, amino, --NRR.sup.1 where R and R.sup.1 are independently selected from hydrogen, C.sub.1-8 alkyl and C.sub.1-8 alkanoyl, cyano, carboxyalkoxy, alkoxycarbonylalkoxy, C.sub.1-8 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-8 alkoxy (including cycloalkoxy and cycloalkylalkoxy), C.sub.Type: GrantFiled: April 14, 1995Date of Patent: August 19, 1997Assignee: The University of South CarolinaInventors: James Mood Chapman, Jr., Roy Lee Hawke, Karl Witold Franzmann, Kevin Julian O'Connor
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Patent number: 5643950Abstract: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.Type: GrantFiled: June 2, 1995Date of Patent: July 1, 1997Assignee: Ortho Pharmaceutical CorporationInventors: James P. Demers, Sigmond Johnson, Michele Ann Weidner-Wells, Ramesh M. Kanojia, Stephanie A. Fraga, Dieter Klaubert
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Patent number: 5631405Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: June 7, 1995Date of Patent: May 20, 1997Assignee: Pharm-Eco Laboratories, IncorporatedInventors: Biman Pal, Siya Ram, Bing Cai, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard L. Gabriel
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Patent number: 5624956Abstract: Novel urea derivatives and pharmaceutical compositions thereof are provided which inhibit platelet aggregation.Type: GrantFiled: May 24, 1995Date of Patent: April 29, 1997Assignee: The Monsanto CompanyInventors: Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
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Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5618966Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: May 16, 1995Date of Patent: April 8, 1997Assignee: Pharm-Eco Laboratories, IncorporatedInventors: Biman Pal, Siya Ram, Bing Cai, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard Gabriel
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Patent number: 5616614Abstract: The invention relates to a compound selected from those of general formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, an optical isomer, and an addition salt thereof with a pharmaceutically-acceptable base. Medicinal product which is useful in the treatment of disorders linked to abnormal melatonin activity.Type: GrantFiled: January 25, 1995Date of Patent: April 1, 1997Assignee: Adir ET CompagnieInventors: Said Yous, Daniel Lesieur, Patrick Depreux, B eatrice Guardiola-Lemaitre, G erard Adam, Pierre Renard, Daniel H. Caignard
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Patent number: 5616789Abstract: Disclosed are certain 3-phenylpyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediates useful in preparing the 3-phenylpyridazines are disclosed.Type: GrantFiled: June 6, 1995Date of Patent: April 1, 1997Assignee: Monsanto CompanyInventors: Michael S. South, Terri L. Jakuboski
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Patent number: 5616615Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is COOCH.sub.3 ; R.sup.1 is CH.sub.3 ; R.sup.2 is H; and R.sup.3 is selected from the group consisting of C.sub.6 H.sub.4 (p-Cl) and CH.sub.2 C.sub.6 H.sub.5.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 1997Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5614555Abstract: Amidinophenol derivatives of the formula (I) ##STR1## wherein the various symbols are as defined herein; which have inhibitory activities on PLA.sub.2 and on various proteases such as trypsin, plasmin, thrombin, kallikrein, especially trypsin, and are useful for the prevention and/or the treatment of various inflammatory diseases, allergic diseases, disseminated intravascular coagulation, pancreatitis, severity in pancreatitis and multiple organ failure.Type: GrantFiled: June 5, 1995Date of Patent: March 25, 1997Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Masanori Kawamura, Tsumoru Miyamoto
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Patent number: 5614522Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 24, 1995Date of Patent: March 25, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5612373Abstract: The invention concerns acid derivatives of formula IR.sup.1 --CON(R.sup.2)--N(R.sup.3)CO--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention also concerns processes for the preparation of the acid derivatives of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: Andrew G. Brewster, Peter W. R. Caulkett, Alan W. Faull, Robert J. Pearce, Richard E. Shute
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Patent number: 5610190Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV Protease.Type: GrantFiled: June 7, 1995Date of Patent: March 11, 1997Assignee: G. D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Ko-Chung Lin, Michael L. Vazquez, Richard A. Mueller, Kathryn L. Reed, Robert M. Heintz, Michael Clare, John N. Freskos, Eric T. Sun
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Patent number: 5602277Abstract: A compound of the Formula (I): ##STR1## or pharmaceutically-suitable salts or prodrug forms thereof, wherein: n is 0-1;m is 0;p is 0-1;R.sup.1 is --CO.sub.2 H;R.sup.2 is selected from the group consisting of H, --OH, and --NH.sub.2 ;R.sup.3 is H;R.sup.4 is --C(O)NHR.sup.8 ;R.sup.5 is --NHC(R.sup.6)NH.sub.2R.sup.6 is selected from the group consisting of .dbd.NH, .dbd.NOH, .dbd.NCN, .dbd.O, and .dbd.S; andR.sup.8 is selected from the group consisting of C.sub.1 -C.sub.4 linear or branched alkyl substituted with 0-3 halogens on each carbon.Type: GrantFiled: March 30, 1995Date of Patent: February 11, 1997Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, David A. Walsh
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Patent number: 5602275Abstract: 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: February 11, 1997Assignee: American Cyanamid CompanyInventors: Semiramis Ayral-Kaloustian, Steven R. Schow, Mila T. Du, James J. Gibbons, Jr.
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Patent number: 5599994Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: June 7, 1995Date of Patent: February 4, 1997Assignee: Pharm-Eco Laboratories, Inc.Inventors: Biman Pal, Siya Ram, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard L. Gabriel
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Patent number: 5597930Abstract: The present invention relates to aspartate-functional hydantoin prepolymers prepared by reacting a polyisocyanate having a functionality of at least 1.8 with a polyaspartate corresponding to the formula ##STR1## wherein X represents an organic group which has a valency of n and is inert towards isocyanate groups at a temperature of 100.degree. C. or less, andR.sub.1 and R.sub.2 may be the same or different and represent optionally substituted hydrocarbon radicals,R.sub.3 and R.sub.4 may be identical or different and represent hydrogen or organic groups which are inert towards isocyanate groups at a temperature of 100.degree. C. or less andn has a value of 2 to 6, preferably 2 to 4 and more preferably 2.The present invention is also directed to compositions suitable for the production of coatings, adhesives, elastomers, potting compounds or composite matrices containing these polyhydantoin prepolymers in combination with optionally blocked polyisocyanates.Type: GrantFiled: May 18, 1995Date of Patent: January 28, 1997Assignee: Bayer CorporationInventors: Douglas A. Wicks, Lyuba K. Gindin, Philip E. Yeske, E. Haakan Jonsson
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Patent number: 5597825Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: May 16, 1994Date of Patent: January 28, 1997Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5596044Abstract: The present invention relates to hydroxy-functional prepolymers containing urea groups and corresponding to the formula ##STR1## wherein R represents the residue obtained by removing the isocyanate groups from an organic monomeric diisocyanate, a polyisocyanate adduct or an NCO prepolymer containing hydantoin groups or hydantoin group precursors, R.sub.1 and R.sub.2 may be identical or different and represent organic groups which are inert towards isocyanate groups at a temperature of 100.degree. C. or less, R.sub.3 and R.sub.4 may be identical or different and represent hydrogen or organic groups which are inert towards isocyanate groups at a temperature of 100.degree. C. or less, R.sub.5 represents the hydrocarbon radical obtained by removing the amino and hydroxyl groups from an amino alcohol, n has a value of 1 to 3 and m has a value of 2 to 6.Type: GrantFiled: May 18, 1995Date of Patent: January 21, 1997Assignee: Bayer CorporationInventors: Lyuba K. Gindin, Douglas A. Wicks, Philip E. Yeske, E. Haakan Jonsson
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Patent number: 5576334Abstract: The invention concerns chemical compounds of formula IR.sup.1 --CON(R.sup.2)--CON(R.sup.3)--X.sup.1 --Q--X.sup.2 --GIand pharmaceutically acceptable metabolically labile esters or amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, X.sup.1, Q, X.sup.2 and G have the meanings given in the specification. The invention concerns processes for the preparation of the chemical compounds of formula I, pharmaceutical compositions containing them and their use as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa.Type: GrantFiled: June 27, 1994Date of Patent: November 19, 1996Assignee: Zeneca LimitedInventors: George R. Brown, Richard E. Shute
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Patent number: 5561211Abstract: The present invention relates to blocked polyisocyanates containing at least two isocyanate groups which are reversibly blocked with a monofunctional blocking agent for isocyanate groups and at least two isocyanate groups in the form of urea groups, which may be subsequently converted to thermally stable hydantoin groups. The present invention also relates to one-component coating compositions containing these blocked polyisocyanates and compounds containing at least two isocyanate-reactive groups.Type: GrantFiled: May 23, 1995Date of Patent: October 1, 1996Assignee: Bayer CorporationInventors: Kenneth P. Yonek, Lyuba K. Gindin, Douglas A. Wicks
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Patent number: 5530026Abstract: The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; andB is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloalkyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen;or a prodrug thereof, with the provisos that when A is NH and B is phenyl:a) B is substituted with at least one substituent other than hydrogen;b) B is not:1) mono-substituted in the 4 position with C.sub.1-2 alkyl, tert-butyl or n-butyl, halogen, OH, carboxy C.Type: GrantFiled: January 6, 1995Date of Patent: June 25, 1996Assignee: Universite LavalInventors: Rene C. Gaudreault, Patrick Poyet
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Patent number: 5523325Abstract: This invention relates to amidrazones, insecticidal amidrazone compositions, and methods of using such compositions.Type: GrantFiled: September 9, 1993Date of Patent: June 4, 1996Inventor: Richard M. Jacobson
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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Patent number: 5514716Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.Type: GrantFiled: February 25, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop, Inc.Inventors: Madhusudhan R. Gowravaram, Jeffrey Johnson, Ewell R. Cook, Robert C. Wahl, Alan M. Mathiowetz, Bruce E. Tomczuk, Ashis K. Saha
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Patent number: 5478946Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.Type: GrantFiled: November 30, 1993Date of Patent: December 26, 1995Assignee: Abbott LaboratoriesInventors: Ferid Murad, James F. Kerwin, Lee D. Gorsky
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Patent number: 5475138Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.This method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: July 7, 1994Date of Patent: December 12, 1995Assignee: Pharm-Eco Laboratories IncorporatedInventors: Biman Pal, Siya Ram, Bing Cai, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard Gabriel
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Patent number: 5475013Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 20, 1992Date of Patent: December 12, 1995Assignee: Monsanto CompanyInventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5475106Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted,R.sub.2 represents an alkoxy, optionally substituted cycloalkyloxy, cycloalkylalkyloxy, phenylalkyloxy, polyfluoroalkyloxy or cinnamyloxy radical or a radical --NR.sub.5 R.sub.6,R.sub.3 represents a phenylamino radical in which the phenyl ring is optionally substituted, an optionally substituted phenyl radical or a naphthyl, indolyl or quinolyl radical,R.sub.4 represents a substituted phenyl radical,R.sub.5 and R.sub.6, which may be identical or different, represent a hydrogen atom or an alkyl, optionally substituted phenyl, indanyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical, or alternatively R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocycle, their preparation and medicinal products containing them.Type: GrantFiled: October 8, 1992Date of Patent: December 12, 1995Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5468775Abstract: The present invention concerns enaminones having the formula: ##STR1## wherein R is from the group consisting of COOCH.sub.3 and COOC.sub.2 H.sub.5 ; R.sup.1 is from the group consisting of H and CH.sub.3 ; R.sup.2 is from the group consisting of H when R.sup.1 is CH.sub.3 and CH.sub.3 when R.sup.1 is H; and R.sup.3 is from the group of first radicals consisting of benzyl, phenethyl, disubstituted phenyl and trisubstituted phenyl. The substituted species are second radicals having positive lipophilicity selected from the group consisting of F, Cl, Br, and I.Type: GrantFiled: March 2, 1993Date of Patent: November 21, 1995Assignee: Howard UniversityInventors: Kenneth R. Scott, Jesse M. Nicholson, Ivan O. Edafiogho
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Patent number: 5462958Abstract: The present invention provides a novel benzene derivative useful as a preventive and medically treating medicine for arteriosclerosis, and a cholesterol O-acyl transferase inhibitor comprising the benzene derivative as an active ingredient.The benzene derivative according to the present invention is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a carboxyl group which may be protected or a group represented by the formula: ##STR2## wherein R.sup.5 represents a lower alkyl group or a hydroxyalkyl group and R.sup.6 represents a hydrogen atom or a hydroxyl group; R.sup.2 represents a hydrogen atom, a lower alkyl group or the like; R.sup.3 and R.sup.4 each represent a hydrogen atom or a hydroxyl group; and p is an integer of 1 to 6.Type: GrantFiled: May 19, 1994Date of Patent: October 31, 1995Assignee: Eisai Co., Ltd.Inventors: Kenji Hayashi, Nobuhisa Watanabe, Koichi Nose, Hiroshi Tanaka, Issei Ohtsuka, Motoji Kokushi, Hironobu Hiyoshi, Hiroko Kobayashi, Toshie Yamada, Toru Horie
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Patent number: 5451607Abstract: There are disclosed hydrazone derivatives of the general formula [I]: ##STR1## wherein R.sup.1 is halogen, etc.; R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.4 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; R.sup.5 is C.sub.1 -C.sub.6 alkyl, etc.; R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl, etc.; A is (CH.sub.2).sub.t, O, S(O).sub.n, etc.; a is an integer of 1 to 4; n is an integer of 0 to 2; and t is an integer of 1 to 3; as well as production processes therefor, insecticides and/or acaricides containing the same as an active ingredient and intermediate compounds thereof.Type: GrantFiled: April 19, 1993Date of Patent: September 19, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Toshiaki Taki, Hirosi Kisida, Shigeru Saito, Shinji Isayama
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Patent number: 5447957Abstract: This invention relates to the novel compounds and pharmaceutical compositions of Formula (I).This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I).Type: GrantFiled: June 2, 1994Date of Patent: September 5, 1995Assignee: SmithKline Beecham Corp.Inventors: Jerry L. Adams, Ralph F. Hall, George L. Seibel
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Patent number: 5428065Abstract: Pharmaceutical compounds of the formula: ##STR1## R.sup.1 to R.sup.8 are each hydrogen or C.sub.1-4 alkyl, m, n and p are each 0, 1, or 2, q is 0, 1, 2 or 3, X and Z are each C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxy, nitro, cyano, halo, trihalomethyl, carboxy, C.sub.1-4 alkoxy-carbonyl or phenyl, and in addition z, together with the phenyl ring to which it is attached, can be: ##STR2## Y is --O--, --S-- or --CH.sub.2 --, V is --(CH.sub.2).sub.r -- or --(CH.sub.2).sub.r S-- where r is 1 to 15, and W is hydrogen or optionally substituted phenyl; and salts thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 27, 1995Assignee: Lilly Industries LimitedInventors: Barry P. Clark, Graham H. Timms
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Patent number: 5403952Abstract: Novel substituted cyclic compounds of Formula I are found to be useful inhibitors of matrix metalloendoproteinase-mediated diseases including osteoarthritis, rheumatoid arthritis, septic arthritis, tumor invasion in certain cancers, periodontal disease, corneal ulceration, proteinuria, dystrophic epidermolysis bullosa, and coronary thrombosis associated with atherosclerotic plaque rupture. The matrix metalloendoproteinases are a family of zinc-containing proteinases including but not limited to stromelysin, collagenase, and gelatinase, that are capable of degrading the major components of articular cartilage and basement membranes. The inhibitors claimed herein may also be useful in preventing the pathological sequelae following a traumatic injury that could lead to a permanent disability. These compounds may also be useful as novel birth control agents by preventing ovulation or implantation.Type: GrantFiled: October 8, 1993Date of Patent: April 4, 1995Assignee: Merck & Co., Inc.Inventors: William Hagmann, Charles G. Caldwell, Paul R. Gooley
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Patent number: 5393914Abstract: The present invention provides a novel class of compounds, useful as gasoline detergent additives, comprising hydrocarbyloxypolyether allophonate esters of 2-hydroxy ethane. The present invention also provides a motor fuel composition containing the novel allophonate esters and further provides a method of synthesizing the allophonate esters of the present invention.Type: GrantFiled: September 1, 1992Date of Patent: February 28, 1995Assignee: Texaco Inc.Inventors: Sheldon Herbstman, Cadorette, Constance A.
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Patent number: 5376655Abstract: A derivative of p-guanidinobenzoic acid of the general formula (IA): ##STR1## wherein Y represents an oxygen atom or a sulfur atom and (a) when Y is an oxygen atom, (R.sup.1).sub.m is selected from the group consisting of:5-(4-guanidinobenzoyloxy)-3-methoxymethyl, 3,5-dicarboxy, 3,5-bis(isopropoxycarbonyl), 3,5-bistrifluoromethyl, 3-acetyl, 3,5-bis(N-ethylcarbamoyl), and 3,5-bis(N-propylcarbamoyl);(b) when Y is a sulfur atom, (R.sup.1).sub.m is selected from the group consisting of:2-methyl, 3-methyl, 4-fluoro, 2-chloro, 3-chloro, 2,5-dichloro 2,6-dichloro, 3,4-dichloro, 2-bromo, 2-methoxycarbonyl, and 4-(N,N-diethylaminosulfonyl);or an acid addition salt of said derivative. A method for the treatment or prevention of diseases induced by abnormal enhancing of degradation of proteins by the action of elastase in mammals subject to or suffering therefrom, including the step of administering an effective amount of a p-guanidinobenzoic acid as described herein, is also disclosed.Type: GrantFiled: June 2, 1993Date of Patent: December 27, 1994Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Hiroyuki Ohno
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Patent number: 5374656Abstract: This invention relates to compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl or alkoxycarbonyl radical or an unsubstituted or substituted phenyl radical,R.sub.2 represents an alkyl (1-8 C) or polyfluoroalkyl radical or an unsubstituted or substituted cycloalkyl radical,R.sub.3 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl, quinolyl or phenylamino radical in which the phenyl ring is optionally substituted, or a quinolylamino radical, andm is 0 or 1, the process for preparing them and the medicaments containing them.Type: GrantFiled: June 25, 1992Date of Patent: December 20, 1994Assignee: Rhone-Poulenc Rorer, S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5374769Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.Type: GrantFiled: December 24, 1992Date of Patent: December 20, 1994Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5367093Abstract: Compounds having the structural formula ##STR1## where X, Y, R and Z are defined in the specification are disclosed. The compounds of this invention are effective for controlling mites, nematodes, rice planthopper, tobacco budworm, and southern corn rootworm. Methods for making these compounds are also set forth.Type: GrantFiled: November 20, 1992Date of Patent: November 22, 1994Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical LTD/LTEEInventors: Mark A. Dekeyser, Paul T. McDonald
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Patent number: 5364884Abstract: The invention relates to arginine and arginine-like compounds and to methods employing these compounds as ocular hypotensive agents. These compounds are effective when applied topically, may be used in low concentrations and are nontoxic. Additionally, the invention includes several new arginine derivatives with varying lipophilicities particularly suited for topical administration.Type: GrantFiled: January 21, 1993Date of Patent: November 15, 1994Assignee: Baylor College of MedicineInventors: Rajender S. Varma, George C. Y. Chiou
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Patent number: 5364850Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.Type: GrantFiled: September 24, 1993Date of Patent: November 15, 1994Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
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Patent number: 5358965Abstract: The present invention relates to a hydrazone derivative represented by the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, processes for preparing the derivative, and uses of the derivative as an insecticide.The hydrazone derivative has a marked insecticidal effect on insect pests, especially against LEPIDOPTERA and COLEOPTERA.Type: GrantFiled: May 28, 1993Date of Patent: October 25, 1994Assignee: Nihon Nohyaku Co., Ltd.Inventors: Tomokazu Hino, Nobuharu Andoh, Hiroshi Hamaguchi, Atsushi Kanaoka
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Patent number: 5354738Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: September 4, 1992Date of Patent: October 11, 1994Assignees: G. D. Searle & Co., The Monsanto CompanyInventors: Foe S. Tjoeng, Jeffery A. Zablocki
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Patent number: 5338760Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents an alkyl radical, R.sub.2 represents a phenyl radical or a chain --(CH.sub.2).sub.m --R.sub.4 in which m is equal to 0, 1 or 2 and R, represents a hydroxyl, alkoxy or amino radical, R.sub.3 represents a hydrogen atom or an alkyl, alkoxy or alkylthio radical and n is equal to 0 or 1, their preparation and medicinal products containing them.Type: GrantFiled: September 11, 1992Date of Patent: August 16, 1994Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5338868Abstract: A process is disclosed for the preparation of a compound of the Formula (VI) ##STR1## wherein X is a hydrogen atom, or OH,Y is a hydrogen atom, OH or a methyl group,R.sup.2 is a CH--COOR group, or a group of the formula (XI) ##STR2## and R is a C.sub.1 to C.sub.2 alkyl group, which comprises the step of: reacting a condensed salt of the Formula (IV) ##STR3## wherein Me is Na.sup.+ or K.sup.+, with a reactive derivative of trifluoromethane-sulfonic acid of the Formula (V)F.sub.3 C--SO.sub.2 OH.The compounds of the Formula (VI) are intermediates in the preparation of penicillins and cephalosporins with antibiotic activity.Type: GrantFiled: May 24, 1991Date of Patent: August 16, 1994Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.Inventors: Karoly Ban, Annamaria Ban, Lajosne Pali, Marta Kruppa, Eva Somfai, Csaba Huszar
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Patent number: 5326875Abstract: A process for the preparation of alkylated azaglycine derivatives of the formula IX--(A).sub.n --N(R)--NH--CO--NH.sub.2, (I)is described in which X is an amino protective group, C.sub.1 -C.sub.8 -alkanoyl, C.sub.6 -C.sub.14 -arylcarbonyl or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl, A is amino acid or imino acid radicals optionally protected on the third function, n is 0-10, X being C.sub.1 -C.sub.8 -alkanoyl, C.sub.6 -C.sub.14 -arylcarbonyl or C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl if n=0, and R is C.sub.1 -C.sub.8 -alkyl, C.sub.6 -C.sub.14 -aryl-C.sub.1 -C.sub.4 -alkanoyl or C.sub.5 -C.sub.12 -heteroaryl-C.sub.1 -C.sub.4 -alkanoyl, which comprises reacting a compound of the formula X--(A).sub.n --NH--NH--CO--NH.sub.2, in which X, A and n have the abovementioned meanings, with a primary or secondary alcohol and excess DEAD, and a tri-C.sub.1 -C.sub.6 -alkylphosphine, tri-C.sub.6 -C.sub.14 -arylphosphine or pyridyl-di-C.sub.6 -C.sub.Type: GrantFiled: January 21, 1992Date of Patent: July 5, 1994Assignee: Hoechst AktiengesellschaftInventors: Patrice Talaga, Wolfgang Konig