R Contains Benzene Ring Patents (Class 514/615)
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Patent number: 5905072Abstract: Adjuvants for systemic fungicides in the form of a stable microemulsion comprise water, a mixture of methyl esters of fatty acids obtained by the transesterification of vegetable oils, an anionic surface-active agent, at least one non-ionic surface-active agent with an HLB of between 13-18 and a cloud point of >65.degree. and at least one non-ionic surface-active agent with an HLB of between 10 and 12. These adjuvants, which can additionally contain conventional components and/or formulation additives, improve the activity of systemic fungicides belonging to different chemical groups.Type: GrantFiled: February 9, 1996Date of Patent: May 18, 1999Assignee: Isagro S.p.A.Inventors: Luigi Capuzzi, Mario Ferri, Ernesto Signorini, Nicola Stramacchia, Claude Delestre, Luigi Mirenna
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Patent number: 5892114Abstract: The hetero-linked phenylglycinolamides are prepared by reaction of the corresponding hetero-linked phenylacetic acids with appropriate phenylglycinols. The hetero-linked phenylglycinolamides are suitable as active compounds in medicaments.Type: GrantFiled: April 10, 1997Date of Patent: April 6, 1999Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Ulrich Muller, Richard Connell, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Martin Beuck
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Patent number: 5866610Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.Type: GrantFiled: July 18, 1996Date of Patent: February 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Jan-Robert Schwark, Wolfgang Scholz, Udo Albus
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Patent number: 5859062Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: January 12, 1999Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5854289Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections, and autoimmune or other diseases in which activated macrophages are involved, such as septic shock, heumatoid arthritis and multiple sclerosis.Type: GrantFiled: April 15, 1996Date of Patent: December 29, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5849794Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: December 15, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5830876Abstract: A method of immunizing an individual against pathogen is disclosed. Also disclosed is a method of treating an individual who has a hyperproliferative disease, or of treating an individual who is infected by a pathogen. Specifically, the individual is injected with bupivacaine along with DNA in an expressible form, the DNA encoding an antigen. The encoded antigen can be from a protein from the pathogen or from a protein associated with the hyperproliferative disease.Type: GrantFiled: May 30, 1995Date of Patent: November 3, 1998Assignees: The Trustees of the University of Pennsylvania, The Wistar InstituteInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 5817637Abstract: Methods of prophylactic and therapeutic immunization of an individual against pathogen infection, diseases associated with hyperproliferative cells and autoimmune diseases are disclosed. The methods comprise the steps of administering to cells of an individual, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein which comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen, a hyperproliferative cell associated protein or a protein associated with autoimmune disease respectively. In each case, nucleotide sequence is operably linked to regulatory sequences to enable expression in the cells. The nucleic acid molecule is free of viral particles and capable of being expressed in said cells. The cells may be contacted cells with a cell stimulating agent. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed.Type: GrantFiled: January 13, 1997Date of Patent: October 6, 1998Assignees: The Trustees of the University of Pennsylvania, The Wistar InstituteInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 5756426Abstract: Described herein are compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom andY is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH andY is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: September 11, 1995Date of Patent: May 26, 1998Assignee: Novartis CorporationInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5733934Abstract: Indenoylguanidines of formula I and formula II, the process for their preparation, their use as medicaments, medicaments containing them, their use as diagnostic agents and medicaments containing them are described. Compounds I are useful for treating cardiac arrhythmias. Further they are useful as cardioprotective agents in mammals, which comprises administering the compound of formula-I or II with the above properties in combination with pharmaceutically accepted carrier to said mammal.Type: GrantFiled: April 16, 1996Date of Patent: March 31, 1998Assignee: Hoechst AktiengesellschaftInventors: Nigrogi Venkata Satya Ramakrishna, Tulsidas Sitaram More, Anagha Suhas Kulkarni, Bansi Lal, Rao Venkata Satya Veerabhadra Vadlamudi, Anil Vasantrao Ghate, Ravindra Dattatraya Gupte, Wolfgang Scholz, Hans Jochen Lang
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Patent number: 5700811Abstract: This invention is directed to compounds having the structure: ##STR1## wherein R.sub.1 and R.sub.2 are independently the same as or different from each other; when R.sub.1 and R.sub.2 are the same, each is a substituted or unsubstituted arylamino, cycloalkylamino, pyridineamino, piperidino, 9-purine-6-amine or thiazoleamino group; when R.sub.1 and R.sub.2 are different, R.sub.1 =R.sub.3 --N--R.sub.4, and n is an integer from about 4 to about 8. This invention also provides a method of selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells. The invention further provides pharmaceutical compositions comprising a therapeutically effective amount of the compounds of the present invention and a pharmaceutically acceptable carrier.Type: GrantFiled: May 19, 1994Date of Patent: December 23, 1997Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Ronald Breslow, Paul A. Marks, Richard A. Rifkind
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Patent number: 5700831Abstract: A compound of the formula ##STR1## wherein R is a) phenyl; phenyl(C.sub.1 -C.sub.4 alkoxy); phenoxy; or benzyl; the phenyl ring of each substituent being optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, di(C.sub.1 -C.sub.8 alkyl)amino, phenyl or phenoxy; or b) a 5- or 6-membered heterocyclic group comprising 1-3 heteroatoms selected from the group consisting of N, O or S, optionally substituted with one or more of halogen, nitro, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 haloalkyl, C.sub.1 -C.sub.8 haloalkoxy, or di-(C.sub.1 -C.sub.8 alkyl)amino. These compounds and pesticidal compositions prepared therefrom, are useful as plant protecting agents for the control of insects, nematodes, and mites.Type: GrantFiled: March 12, 1996Date of Patent: December 23, 1997Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd/LteeInventors: Mark Achiel Dekeyser, Paul Thomas McDonald
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Patent number: 5691376Abstract: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.Type: GrantFiled: October 17, 1996Date of Patent: November 25, 1997Assignee: American Home Products CorporationInventors: Thomas J. Caggiano, Joseph Prol, Jr.
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Patent number: 5650441Abstract: Antiviral compositions useful for the inhibition of HIV include various azo dye compounds which have the ability of inhibiting the binding of HIV rgp120 to CD4 cells on peripheral blood lymphocytes and affecting HIV replication. Also disclosed are methods for treating HIV viral infections with these compositions.Type: GrantFiled: October 11, 1994Date of Patent: July 22, 1997Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human ServicesInventors: Adorjan Aszalos, James C. Weaver, P. Scott Pine
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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: 5593972Abstract: Methods of prophylactic and therapeutic immunization of an individual against pathogen infection, diseases associated with hyperproliferative cells and autoimmune diseases are disclosed. The methods comprise the steps of administering to cells of an individual, a nucleic acid molecule that comprises a nucleotide sequence that encodes a protein which comprises at least one epitope that is identical or substantially similar to an epitope of a pathogen antigen, a hyperproliferative cell associated protein or a protein associated with autoimmune disease respectively. In each case, nucleotide sequence is operably linked to regulatory sequences to enable expression in the cells. The nucleic acid molecule is free of viral particles and capable of being expressed in said cells. The cells may be contacted cells with a cell stimulating agent. Methods of prophylactically and therapeutically immunizing an individual against HIV are disclosed.Type: GrantFiled: September 21, 1993Date of Patent: January 14, 1997Assignees: The Wistar Institute, The Trustees of the University of PennsylvaniaInventors: David B. Weiner, William V. Williams, Bin Wang
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Patent number: 5571829Abstract: Insecticidal compositions comprising a cytochrome P450 enzyme inhibitor compounds and an N,N'-dibenzoyl-N'-tert-alkyl-hydrazine have been discovered which exhibit enhanced efficacy over composition with an N,N'-dibenzoyl-N'-tert-alkylhydrazine alone.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Rohm and Haas CompanyInventor: Muthuvelu Thirugnanam
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Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
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Patent number: 5527787Abstract: A novel pharmaceutical composition having anti-bacterial and antiviral activity and method of treating diseases caused by bacterial and viral pathogens through stimulation of the immunologic system. The composition comprises selected amounts of chlorambucil, procarbazine and cyclophosphamide. Melphalan and liothyronine are primary options. Calcium may also be included as a desirable supplement. The method includes administering these components to a patient in an ordered, time-released manner.Type: GrantFiled: November 15, 1993Date of Patent: June 18, 1996Inventors: Zdzislaw Fiutowski, Leszek J. Fiutowski
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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: 5510363Abstract: Insecticidal compositions comprising a cytochrome P450 enzyme inhibitor compounds and an N,N'-dibenzoyl-N'-tert-alkyl-hydrazine have been discovered which exhibit enhanced efficacy over composition with an N,N'-dibenzoyl-N'-tert-alkylhydrazine alone.Type: GrantFiled: June 6, 1995Date of Patent: April 23, 1996Assignee: Rohm and Haas CompanyInventor: Muthuvelu Thirugnanam
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Patent number: 5506251Abstract: Insecticidal compositions comprising a cytochrome P450 enzyme inhibitor compounds and an N,N'-dibenzoyl-N'-tert-alkyl-hydrazine have been discovered which exhibit enhanced efficacy over composition with an N,N'-dibenzoyl-N'-tertalkylhydrazine alone.Type: GrantFiled: November 16, 1994Date of Patent: April 9, 1996Assignee: Rohm and Haas CompanyInventor: Muthuvelu Thirugnanam
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Patent number: 5480871Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.Type: GrantFiled: May 12, 1995Date of Patent: January 2, 1996Assignee: Chiron CorporationInventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
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Patent number: 5476849Abstract: The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with a carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.Type: GrantFiled: December 3, 1993Date of Patent: December 19, 1995Assignees: The Rockefeller University, Alteon Inc.Inventors: Peter C. Ulrich, Anthony Cerami, Dilip R. Wagle
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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: 5447916Abstract: Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.Type: GrantFiled: July 30, 1993Date of Patent: September 5, 1995Assignee: Chiron CorporationInventors: David C. Spellmeyer, Walter H. Moos, Eric J. Martin, Ronald N. Zuckermann, Gregory Stauber
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Patent number: 5424333Abstract: This invention relates to the anthelmintic use of compositions containing N'-substituted-N,N'-disubstitutedhydrazines. Specifically, the invention relates to methods of controlling helminths by contacting the helminths with a compound having a nucleus of the formula ##STR1## wherein X and X' are the same or different O, S, or NR and A', B', R.sup.1 and R.sup.2 are a variety of substituents.Type: GrantFiled: July 5, 1991Date of Patent: June 13, 1995Assignee: Rohm and Haas CompanyInventor: Keith D. Wing
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5401767Abstract: The present invention is directed to compounds which suppress immune responses and/or selectively inhibit complement. These compounds contain an aromatic ring and are substituted dihydrobenzofurans, spirobenzofuran-2(3H)-cycloalkanes, and their open chain intermediates. The compounds of the present invention, and the pharmaceutically acceptable salts thereof, interrupt the proteolytic processing of C5 to bioactive components, exhibit immunosuppressive activities, and have therapeutic utility in the amelioration of disease and disorders mediated by complement and/or immune activity.Type: GrantFiled: December 21, 1992Date of Patent: March 28, 1995Assignees: T Cell Sciences, Inc., The University of MississippiInventors: Robert D. Sindelar, Barton J. Bradbury, Teodoro Kaufman, Stephen H. Ip, Henry C. Marsh, Jr.
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Patent number: 5399589Abstract: Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R.sup.1, R.sup.2 and R.sup.3 independently of one another arehydrogen, substituted or unsubstituted alkyl, alkenyl or alkynyl orsubstituted or unsubstituted cycloalkyl or cycloalkylmethyl,substituted or unsubstituted cycloalkenyl or cycloalkenylmethyl,substituted or unsubstituted phenyl, phenylalkyl, phenylalkenyl, hetaryl- or hetarylalkyl radicals, where R.sup.2 and R.sup.3 may also. together with the nitrogen atom whose substituents they are, form a 5- or 6-membered ring, orR.sup.2 together with R.sup.3 is the group ##STR2## where R.sup.4 and R.sup.5 are one of the radicals R, R.sup.1, R.sup.2 or R.sup.3, or R.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, are monocyclic or polycyclic cycloalkyl, orR.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, form a 5- or 6-membered, saturated heterocycle containing O, S or --N(R.sup.Type: GrantFiled: November 29, 1993Date of Patent: March 21, 1995Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5376685Abstract: Compounds of formula I ##STR1## wherein A, X.sub.1, X.sub.2, X.sub.3, X.sub.4, Y, Z and R.sub.1 to R.sub.6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: May 7, 1993Date of Patent: December 27, 1994Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
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Patent number: 5358966Abstract: This invention relates to a method of controlling insects in turfgrass, ornamental plants or food crops using an insecticidally effective amount of certain N'- substituted-N,N'-diacylhydrazines having the formula ##STR1## wherein X is phenyl, 2-fluorophenyl, or phenyl or 2-fluorophenyl substituted at the 4-position with chloro, fluoro, iodo, methyl or ethyl andY is phenyl, 4-fluorophenyl, 2-chloro-4-fluorophenyl or phenyl substituted at the 2-position with chloro, bromo or iodo.Type: GrantFiled: June 8, 1993Date of Patent: October 25, 1994Assignee: Rohm and Haas CompanyInventors: William N. James, Jr., Harold E. Aller
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Patent number: 5358952Abstract: O.sup.6 -substituted guanine compounds of the formula ##STR1## wherein R is a benzyl group or a substituted benzyl group, cause a depletion of O.sup.6 -alkylguanine-DNA alkyltransferase (AGT) activity in mammalian cells. These compounds may be administered to a host so as to reduce AGT levels in tumor cells of the host in order to increase host responsiveness to anti-neoplastic alkylating agents, including chloroethylating agents, such as chloroethylnitrosoureas, for chemotherapeutic treatment of a number of neoplasms.Type: GrantFiled: December 12, 1991Date of Patent: October 25, 1994Assignees: The United States of America as represented by the Secretary of the Department of Health and Human Services, The Penn State Research FoundationInventors: Robert C. Moschel, M. Eileen Dolan, Anthony E. Pegg
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Patent number: 5358967Abstract: The present invention is a composition comprising an effective amount of an N'-alkyl-N'-(3,5-dimethylbenzoyl)-N-(substituted benzoyl)-hydrazine to treat wool for protection from keratin digesting insects, and an insect-proofing method using such compounds. The compositions and methods have particular application in treating wool.Type: GrantFiled: July 6, 1993Date of Patent: October 25, 1994Assignee: Rohm and Haas CompanyInventor: Glenn R. Carlson
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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: 5342835Abstract: Compounds of formula ##STR1## in which: CYCLE surrounded by a semicircle represents, with the two carbon atoms to which the semicircle is linked, a carbon-containing, optionally heterocyclic, ring containing at least one ethylenic or aromatic bond between the two carbon atoms which carry the --C(Z).dbd.Y group and the phenyl group, Y is oxygen or sulphur, Z is NR.sub.1 R.sub.2, R.sub.1 and R.sub.2, each represents optionally substituted alkyl, alkoxy or cycloalkyl; alkenyl or alkynyl; or --NR.sub.1 R.sub.2 represents saturated or unsaturated heterocyclyl;R.sub.3, R.sub.4 and R.sub.5, each represents a hydrogen or halogen atom (at least one of R.sub.3, R.sub.4 and R.sub.5 being other than hydrogen or halogen); optionally substituted amino; optionally halogenated hydroxylated alkyl, alkoxy, alkylalkoxy or alkylthio; or R.sub.3 and R.sub.4 (in the 3- and 4-positions) can together form a single divalent radical with 3 or 4 members containing 1 or 2 non-adjacent oxygen atoms; are useful as agricultural fungicides.Type: GrantFiled: January 3, 1992Date of Patent: August 30, 1994Assignee: Rhone-Poulenc AgrochimieInventors: Regis Pepin, Christian Schmitz, Guy-Bernard Lacroix, Philippe Dellis, Christine Veyrat
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Patent number: 5338762Abstract: A clear, efficacious, aqueous microemulsion of an agriculturally active carbamate ester insecticide.Type: GrantFiled: November 19, 1992Date of Patent: August 16, 1994Assignee: ISP Investments Inc.Inventor: Kolazi S. Narayanan
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Patent number: 5294643Abstract: Novel cinnamamide derivatives and the salts thereof are provided. An antihyperlipidemic composition is also provided. The composition comprises an active ingredient which is at least one selected from the group consisting of the above-mentioned cinnamamide derivative and the pharmaceutically acceptable salt thereof.Type: GrantFiled: July 5, 1990Date of Patent: March 15, 1994Assignee: Kanegafuchi Kagaku Kogyo KabushikiInventors: Yoshihide Fuse, Kenji Fujii, Keiji Kameyama, Taizo Kawabe, Toshiaki Miwa, Ikuo Katsumi
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Patent number: 5260339Abstract: Novel 4-phenyl-1,3-benzodiazepines and 2-amino-.alpha.-phenylphenethylamines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants. The 2-amino-.alpha.-phenylphenethylamines are useful as anticonvulsant and neuroprotective agents.Type: GrantFiled: October 8, 1992Date of Patent: November 9, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Lawrence L. Martin, Manfred Worm, Charles A. Crichlow
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Patent number: 5246709Abstract: A dosage form is disclosed comprising an antiemetic and antinausea drug for treating vomiting and nausea.Type: GrantFiled: September 21, 1992Date of Patent: September 21, 1993Assignee: Alza CorporationInventors: Francisco Jao, Hoa T. Huynh, Patrick S. L. Wong
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Patent number: 5229417Abstract: Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: December 5, 1991Date of Patent: July 20, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Richard C. Effland, Joseph T. Klein
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Patent number: 5225443Abstract: This invention relates to insecticidal compositions containing N-substituted-N'-substituted-N,N'-diacylhydrazines methods of using such compositions and novel insecticidal N-substituted-N'-substituted-N,N'-diacylhydrazines.Type: GrantFiled: June 24, 1991Date of Patent: July 6, 1993Assignee: Rohm and Haas CompanyInventors: Raymond A. Murphy, Adam C. Hsu
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Patent number: 5179127Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R is selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl and substituted or unsubstituted phenyl wherein the substituents are selected from one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl, nitro, (C.sub.1 -C.sub.4) haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl andR.sup.1 is selected from the group consisting of (C.sub.1 -C.sub.Type: GrantFiled: February 26, 1992Date of Patent: January 12, 1993Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5116877Abstract: A cinnamamide derivative represented by the formula ##STR1## wherein X is a halogen atom is useful as a muscle relaxant.Type: GrantFiled: January 29, 1990Date of Patent: May 26, 1992Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Hironaka Aihara, Michio Kurachi, Kazuyuki Tomisawa
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Patent number: 5112382Abstract: Compounds of the formula ##STR1## wherein A is selected from the group consisting of (1) phenyl, (2) naphthyl, (3) phenyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4) alkyl, nitro, (C.sub.1 -C.sub.4)haloalkyl, and (C.sub.1 -C.sub.4)thioalkyl, (4) naphthyl substituted with one or more halo, cyano, (C.sub.1 -C.sub.4)alkyl,nitro,(C.sub.1 -C.sub.4), and (C.sub.1 -C.sub.4) thioalkyl, (5) thiophene, (6) furan, (7) thiophene substituted with one or more substituents selected from halo and nitro, and (8) furan substituted with one or more substituents selected from halo and nitro;R disclose as microbicidally and fungicidally active.Type: GrantFiled: May 24, 1990Date of Patent: May 12, 1992Assignee: Rohm and Haas CompanyInventor: Adam C. Hsu
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Patent number: 5112861Abstract: The invention concerns a method for the treatment of Parkinson's Disease. The method comprises administering a catechol-O-methyl-transferase inhibiting amount of a compound having the formula I ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, alkylcarbamoyl of 2 to 5 carbon atoms or alkylcarbonyl of 2 to 5 carbon atoms, X represents nitro or cyano and R.sub.3 represents ##STR2## wherein R.sub.4 represents cyano or alkylcarbonyl of 2 to 5 carbon atoms and R.sub.5 represents cyano; alkylcarbonyl of 2 to 5 carbon atoms; or carbamoyl which is unsubstituted or substituted with alkyl of 1 to 8 carbon atoms, or hydroxyalkyl of 1 to 8 carbon atoms or pharmaceutically acceptable salts or esters thereof; and a sufficient amount of levodopa to treat Parkinson's Disease. A peripheral decarboxylase inhibitor such as carbidopa or benzerazide is also preferably administered.Type: GrantFiled: September 25, 1990Date of Patent: May 12, 1992Assignee: Orion-yhtyma OyInventors: Reijo Backstrom, Kalevi E. Heinola, Erkki J. Honkanen, Seppo K. Kaakkola, Pekka J. Kairisalo, Inge-Britt Y. Linden, Pekka I. Mannisto, Erkki A. O. Nissinen, Pentti Pohto, Aino K. Pippuri, Jarmo Pystynen
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Patent number: 5025033Abstract: A cholinesterase inhibiting agent which contains an alkylene diamine of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is a hydrogen atom or a hydrocarbon residue which may optionally be substituted, or R.sup.1 and R.sup.2 combinedly form, together with the adjacent nitrogen atom, a condensed heterocyclic group, R.sup.3 is a hydrogen atom or a hydrocarbon residue or an acyl group which may optionally be substituted and R.sup.4 is a hydrogen atom, or R.sup.3 and R.sup.4 combinedly form a group of the formula ##STR2## or --(CH.sub.2).sub.m+1 -- (m being 0, 1 or 2), A is --(CH.sub.2).sub.l -- (l being 0, 1 or 2) or --CH.dbd.CH--, X is a substituent or substituents and n is an integer of 4 to 7, or a salt thereof, which are useful as cerebral function improving agents for the prevention or treatment of senile dementia, Alzheimer's disease, Huntington's chorea, hyperkinesia, mania and so forth.Type: GrantFiled: January 25, 1989Date of Patent: June 18, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 4990511Abstract: Amide compounds having glutamate receptor-inhibiting activity and having the formula: ##STR1## (wherein R.sub.1 and R.sub.2 each is hydrogen atom, an alkyl group or an acyl group, or ##STR2## is a cyclic amino group, m is an integer of 1 to 3, n is an integer of 0 to 4, x is an integer of 2 to 6 and y is an integer of 0 to 3) or salts thereof, are provided. The compounds are useful as a medicine for therapy or/and prevention of sequelae of cerebral apoplexy in warm-blooded animals.Type: GrantFiled: August 2, 1989Date of Patent: February 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Terumi Nakajima, Koichi Shudo, Giichi Goto
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Patent number: 4985461Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-diacylhydrazines, methods of using such compositions and certain novel insecticidal N'-substituted-N,N'-diacylhydrazines.Type: GrantFiled: October 21, 1985Date of Patent: January 15, 1991Assignee: Rohm and Haas CompanyInventors: Adam C. Hsu, Harold E. Aller