Amidino Hydrazines Or Hydrazones (i.e., N-n=c-n Or N=c-n-n) Patents (Class 514/632)
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Patent number: 6248787Abstract: 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: June 19, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6180676Abstract: 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 30, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 6143728Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.Type: GrantFiled: November 14, 1997Date of Patent: November 7, 2000Assignee: The Picower Institute for Medical ResearchInventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
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Patent number: 6133320Abstract: Primary and secondary osteoporosis in a female or a male mammal is treated by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally; in further combination with one or more of an estrogen, a progestin, an anabolic steroid. Nitric oxide substrate or donor also can be combined with one or more of other medications acting on bone, such as bisphosphonate, calcitonin, fluoride, androgen and other novel therapeutic agents. Either nitric oxide donor or substrate by itself or combination with other medications as described above can be used in both women and men, (preferably human) for prevention and treatment of osteoporosis and other metabolic bone disorders.Type: GrantFiled: October 22, 1998Date of Patent: October 17, 2000Assignee: Board of Regents, The University of Texas SystemInventors: Chandrasekhar Yallampalli, Sunil J. Wimalawansa
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Patent number: 6114392Abstract: The invention relates to the use of agmatine, in the treatment of acute neurotrauma (such as stroke) and degenerative disorders of the central and peripheral nervous system (such as dementia).The invention further provides novel compounds of general formula I (which are quinuclidine derivatives), formula II (which are norbornane derivatives), formula III (which are adamantane derivatives), and formula IV (which are phenothiazine derivatives): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy, halogeno, amino, phenyl, or R.sub.4 NR.sub.5 ; R.sub.4 and R.sub.5 are each independently hydrogen, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH--NHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--(NR.sub.7 .dbd.)CNHR.sub.6, or (CH.sub.2)n--[NH(CH.sub.2)x]y--NH(NR.sub.7 .dbd.)CNHR.sub.6 wherein n is from 0-5, y is from 0-5 and each x is independently from 1-5; R.Type: GrantFiled: April 16, 1996Date of Patent: September 5, 2000Inventors: Gad M. Gilad, Varda H. Gilad
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Patent number: 6022900Abstract: 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: February 8, 2000Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5977181Abstract: The present invention is based on the discovery that nitric oxide (NO) is an important growth regulator in an intact developing organism. In particular, the present invention relates to a method of increasing in a mammal a population of hematopoietic stem cells in bone marrow which are capable of undergoing normal hematopoiesis and differentiation, wherein the bone marrow is contacted with an inhibitor of NO, such as an inhibitor of nitric oxide synthase (NOS), thereby producing bone marrow having an increased population of hematopoietic stem cells which are capable of undergoing normal hematopoiesis and differentiation. The present invention also relates to a method of increasing a population of cells in S phase in a tissue of a mammal, comprising contacting the tissue with an inhibitor of NO, such as an inhibitor of NOS. The invention also pertains to a method of regenerating tissue in an adult mammal comprising contacting a selected tissue (e.g.Type: GrantFiled: November 13, 1997Date of Patent: November 2, 1999Assignee: Cold Spring Harbor LaboratoryInventors: Grigori N. Enikolopov, Natalia I. Peunova, Boris A. Kuzin, Tatiyana Michurina
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Patent number: 5965529Abstract: Preeclampsia and preterm labor in a pregnant female mammal are treated by administering thereto a combination of a progestin and a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in further combination with one or more of a cyclooxygenase inhibitor, a PGI.sub.2 -mimetic, a thromboxane (TXA.sub.2) inhibitor, a compound possessing TXA.sub.2 -agonistic and TXA.sub.2 -inhibiting properties, a compound possessing TXA.sub.2 -antagonistic and PGI.sub.2 -memetic activities, and a TXA.sub.2 antagonist.Type: GrantFiled: June 6, 1995Date of Patent: October 12, 1999Assignees: The Board of Regents, University of Texas, Schering AktiengesellschaftInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallamp'al Li
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Patent number: 5962413Abstract: Dysmenorrhea, disfunctional uterine bleeding, preterm labor and postpartum labor in female mammals are treated by inhibiting uterine contractility by administering thereto a nitric oxide synthase substrate, a nitric oxide donor or both, optionally in combination with one or more of a prostaglandin inhibitor, a prostacyclin-mimetic, a progestin, an oxytocin antagonist or a .beta.-agonist in an amount effective to ameliorate the symptoms thereof; and inadequate menses treated and induction of abortion or stimulation of labor in a pregnant female is achieved by uterine contractility stimulation by administering thereto a nitric oxide inhibitor, either alone or optionally in a combination of progesterone antagonist, an oxytocin or oxytocin analogue antagonist or a prostaglandin.Type: GrantFiled: September 22, 1997Date of Patent: October 5, 1999Assignees: Schering Aktiengesellschaft, The University of Texas SystemInventors: Robert E. Garfield, Krzysztof Chwalisz, Radoslaw Bukowski, Chandra Yallampalli
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Patent number: 5891909Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 27, 1997Date of Patent: April 6, 1999Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Bruce E. Tomczuk, Carl Illig
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Patent number: 5869534Abstract: The in vivo oxidation of lipids and lipid-containing molecules has been discovered to be initiated by the concurrent reaction of such lipid materials with reducing sugars such as glucose, advanced glycosylation endproducts such as AGE-peptides, or a compound which forms advanced glycosylation endproducts, to form materials or particles known as AGE-lipids. AGE-lipids have been implicated in the aging process, the abnormal formation of lipofuscin and in various disease states such as diabetes and atherosclerosis. Diagnostic methods are contemplated, extending in utility from the detection of the onset and course of conditions in which variations in lipid oxidation, AGE-lipid levels, LDL levels, apolipoprotein levels, apolipoprotein receptor binding the like, may be measured, to drug discovery assays.Type: GrantFiled: March 11, 1993Date of Patent: February 9, 1999Assignee: The Picower Institute for Medical ResearchInventors: Richard J. Bucala, Helen Vlassara, Anthony Cerami
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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: 5837737Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 7, 1995Date of Patent: November 17, 1998Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5753684Abstract: 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: May 19, 1998Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
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Patent number: 5693673Abstract: Process for the preparation of 2,2'-(1-methyl 1,2-ethanediylidene)bis?hydrazine carboximidamide! by:a) reacting aminoguanidine hydrochloride with methylglyoxal aldehyde or methylglyoxal dimethyl acetal; andb) purifying the 2,2'-(1-methyl-1,2-ethanediylidene)bis?hydrazine carboximidamide! by crystallization from an acidic aqueous-isopropyl alcohol medium.Type: GrantFiled: May 30, 1996Date of Patent: December 2, 1997Assignee: SanofiInventors: Richard Philion, Steven A. Elenbaas
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Patent number: 5686495Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 6, 1995Date of Patent: November 11, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5659083Abstract: Process for the preparation of 2,2'-(1-methyl-1,2-ethanediylidine)bis[hydrazine carboximidamide] bya) removing impurities from aminoguanidine bicarbonate;b) reacting the aminoguanidine bicarbonate with methylglyoxal dimethyl acetal in an aqueous isopropyl medium; andc) purifying the 2,2'-(1-methyl-1,2-ethanediylidene)bis[hydrazine carboximidamide] by crystallization from an acidic aqueous-isopropanol medium.Type: GrantFiled: May 30, 1996Date of Patent: August 19, 1997Assignee: SanofiInventors: Richard Philion, Martin Robert Gray
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Patent number: 5652269Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.Type: GrantFiled: June 5, 1995Date of Patent: July 29, 1997Assignee: Cambridge NeuroScience, Inc.Inventors: Stanley M. Goldin, Subbarao Katragadda, Lain-Yen Hu, N. Laxma Reddy, James B. Fischer, Andrew Gannett Knapp, Lee David Margolin
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Patent number: 5646188Abstract: A compound of general formula I ##STR1## wherein n is 1 or 2; R.sub.1 and R.sub.2 are each independently hydrogen, hydroxy, substituted or unsubstituted C.sub.1-4 alkyl, substituted or unsubstituted C.sub.1-4 alkoxy or halogeno;R.sub.5 is hydrogen, substituted or unsubstituted C.sub.1-4 alkyl, amino or NR.sub.6 R.sub.7 ;R.sub.3, R.sub.4, R.sub.6 and R.sub.7 are each independently hydrogen or (CH.sub.2).sub.m --[NH(CH.sub.2).sub.x ].sub.y --NHR.sub.11 wherein m is from 0-5, y is from 0-5 and each x is independently from 1-5 and R.sub.11 is hydrogen or C(NH)NH.sub.2 ;provided that when R.sub.3 and R.sub.4 are both hydrogen, R.sub.5 is amino or NR.sub.6 R.sub.7 ; pharmaceutically acceptable salts and optically active isomers thereof.Type: GrantFiled: July 5, 1995Date of Patent: July 8, 1997Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Gad Gilad, Varda Gilad, Jeffrey Sterling, Yaacov Herzig, David Lerner, Alex Veinberg, Isaac Milman, Nina Finkelstein
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Patent number: 5614557Abstract: .alpha.-Fluoromethyl- or .alpha.-difluoromethylornithine, and certain derivatives thereof, can be used alone or in combination with cytotoxic agents for the treatment of neoplastic diseases.Type: GrantFiled: March 14, 1995Date of Patent: March 25, 1997Assignee: Marion Merrell et Compagnie C/O Merrell Pharmaceuticals Inc.Inventors: Philippe Bey, Michel Jung
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Patent number: 5514676Abstract: 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: February 3, 1995Date of Patent: May 7, 1996Assignees: The Rockefeller University, Alteon Inc.Inventors: Peter C. Ulrich, Anthony Cerami, Dilip R. Wagle, Michael E. Lankin, David H. Shih, San-Bao Hwang
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Patent number: 5494934Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Medicine products.Type: GrantFiled: November 4, 1991Date of Patent: February 27, 1996Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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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: 5464858Abstract: Inhibitors of nitric oxide formation from arginine useful for treating hypotension, inflammation, stroke and to restore vascular contractile sensitivity to the effects of .alpha..sub.1 adrenergic agonists are physiologically active compounds including N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties or monoalkyl carbon-substituted N.sup..delta. -substituted ornithine or N.sup..epsilon. -substituted lysine moieties, having the formula ##STR1## wherein R is (CH.sub.2).sub.y CH.sub.3 or H, R' is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, and R" is CH.sub.2 or C(H)(CH.sub.2).sub.y CH.sub.3, with y ranging from 0 to 5, and x is 0 or 1 and wherein none or only one of R, R' and R" provides an alkyl substituent on ornithine or lysine moiety, and wherein Q is a heme binding moiety and/or a sulfur-containing binding moiety and Q' is --NH.sub.2 when there is a double bond between the omega carbon and Q and Q' is .dbd.Type: GrantFiled: December 12, 1994Date of Patent: November 7, 1995Assignee: The Medical College of Wisconsin Research Foundation, Inc.Inventors: Owen W. Griffith, Krishnaswamy Narayanan
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Patent number: 5461076Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: November 30, 1994Date of Patent: October 24, 1995Inventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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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: 5444082Abstract: 3,9-disubstituted-spiro[5.5]undecanes and ##STR1## wherein, R, Y, A, B and n are defined in the specification, pharmaceutical compositions containing same for the treatment of cardiovascular disorders, such as heart failure and hypertension, are disclosed.Type: GrantFiled: June 28, 1993Date of Patent: August 22, 1995Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Marco Frigerio, Patrizia Ferrari, Piero Melloni, Giuliana Salani
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Patent number: 5420165Abstract: There are provided substituted acid amide, arylhydrazone compounds (amidrazones) of formula I ##STR1## the use thereof for the control of insect and acarid pests and methods and compositions for the protection of crops from the damage and loss caused by said pests.Type: GrantFiled: December 29, 1992Date of Patent: May 30, 1995Assignee: American Cyanamid CompanyInventors: Joseph A. Furch, David G. Kuhn, David A. Hunt
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Patent number: 5405871Abstract: Compounds of the formula ##STR1## wherein each of o and p, independently of the other, is 0, 1, 2, 3, 4 or 5, the radicals R.sub.1 being the same or different when o is greater than 1 and the radicals R.sub.2 being the same or different when p is greater than 1;each of R.sub.1 and R.sub.2, independently of the other, is C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, halogen, --NO.sub.2, --OH, C.sub.1 -C.sub.4 alkoxy, halo-C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, halo-C.sub.1 -C.sub.4 alkylthio, --O--S(.dbd.O)--R.sub.6, --O--S(.dbd.O).sub.2 --R.sub.6, phenoxy or --N(R.sub.11)SO.sub.2 R.sub.12 and/or two substituents R.sub.1 and/or two substituents R.sub.2 are, independently of one another, together --Y--Z--Y--;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or halo-C.sub.1 -C.sub.4 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl or naphthyl or mono- or di-substituted phenyl or naphthyl;R.sub.5 is --S--R.sub.7, --S(.dbd.O)--R.sub.7, --S(.dbd.O).Type: GrantFiled: April 6, 1994Date of Patent: April 11, 1995Assignee: Ciba-Geigy CorporationInventors: Roger G. Hall, Alfons Pascual, Odd Kristiansen
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Patent number: 5395855Abstract: Compounds of formula I ##STR1## wherein A, X, Z and R.sub.1 -R.sub.5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.Type: GrantFiled: March 28, 1994Date of Patent: March 7, 1995Assignee: Ciba-Geigy CorporationInventors: Jaroslav Stanek, Jorg Frei, Giorgio Caravatti
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Patent number: 5358969Abstract: A method is disclosed for inhibiting nitric oxide formation in a warm blooded mammal afflicted with an acute or chronic inflammatory disease which comprises administering to said mammal an effective nitric oxide inhibitory amount of methyl-, or 1,1-dimethyl-, or amino-substituted guanidines.Type: GrantFiled: August 24, 1993Date of Patent: October 25, 1994Assignee: Washington UniversityInventors: Joseph R. Williamson, John A. Corbett, Michael L. McDaniel, Ronald G. Tilton
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Patent number: 5296498Abstract: A compound of formula (I): ##STR1## in which: R.sub.1 represents substituted or unsubstituted phenyl or (C.sub.3 -C.sub.7) cycloalkyl,R.sub.2 represents trifluoromethyl or (C.sub.3 -C.sub.4) cycloalkyl,A represents --CH.sub.2 --, --CH.dbd.N--, .dbd.N-- or --NH--,R.sub.3 and R.sub.4, which may be identical or different, represent hydrogen or linear or branched (C.sub.1 -C.sub.6) alkyl or, with the nitrogen atoms to which they are attached, form a 5- or 6-membered heterocycle,R represents either hydrogen in the case where A=--CH.sub.2 --, --CH.dbd.N-- or --NH--, or a bond of the group A when the latter is equal to .dbd.N--,its enantiomers and epimers as well as its addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: January 19, 1993Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Charles Malen, Jean-Michel Lacoste, Guillaume de Nanteuil
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Patent number: 5288727Abstract: The present invention relates to a hydrazone compound of the formula (I) or its salt, a process for its preparation, an intermediate of the formula (II-5), a pesticidal composition containing said hydrazone compound or its salt as the active ingredient, and a pesticidal method of applying an effective amount thereof: ##STR1##Type: GrantFiled: February 13, 1992Date of Patent: February 22, 1994Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Tadaaki Toki, Toru Koyanagi, Kiyomitsu Yoshida, Hiroshi Sasaki, Masayuki Morita, Tetsuo Yoneda
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Patent number: 5272176Abstract: The present invention relates to 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 the 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: June 12, 1992Date of Patent: December 21, 1993Assignee: The Rockefeller UniversityInventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 5262152Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain novel amidrazones and derivatives thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the 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: May 28, 1992Date of Patent: November 16, 1993Assignees: The Rockefeller University, Alteon Inc.Inventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 5246970Abstract: A method is disclosed for inhibiting nitric oxide formation in a warm blooded mammal which comprises administering to said mammal an effective nitric oxide inhibitory amount of aminoguanidine.Type: GrantFiled: June 30, 1992Date of Patent: September 21, 1993Assignee: Washington UniversityInventors: Joseph R. Williamson, John A. Corbett, Michael L. McDaniel, Ronald G. Tilton
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Patent number: 5238963Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. 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 treThis invention was made in part with government support under Grant Number PHS AM 19655 awarded by the National Institutes of Health. The government has certain rights in the invention.Type: GrantFiled: December 10, 1991Date of Patent: August 24, 1993Assignee: The Rockefeller UniversityInventors: Anthony Cerami, Peter C. Ulrich, Michael Brownlee
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Patent number: 5232706Abstract: The preparation comprises a nucleus formed by a mixture of omeprazol or an alkali salt of omeprazol with a first basic compound; the nucleus has two coatings, the first of which is formed by one or more layers formed by a basic water soluble excipient and by a second basic compound, while the second coating is formed by an enteric coating.Type: GrantFiled: December 9, 1991Date of Patent: August 3, 1993Assignees: Esteve Quimica, S.A., Centro Genesis para la Investigacion, S.L.Inventor: Alberto Palomo Coll
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Patent number: 5177083Abstract: A method to treat or prevent retroviral infection by administering a novel conjugate is described. Lucifer Yellow and its analogs are conjugated to compounds having carbonyl functional groups for reaction with the semicarbazide moiety of Lucifer Yellow to obtain the semicarbazone conjugate.Type: GrantFiled: September 11, 1989Date of Patent: January 5, 1993Assignee: The Scripps Clinic and Research FoundationInventors: Darryl C. Rideout, John Elder
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Patent number: 5130337Abstract: The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain novel amidrazones and derivatives thereof. Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the 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: May 7, 1991Date of Patent: July 14, 1992Assignees: The Rockefeller University, Alteon Inc.Inventors: Peter C. Ulrich, Anthony Cerami
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Patent number: 5128360Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. 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: February 20, 1990Date of Patent: July 7, 1992Assignee: The Rockefeller UniversityInventors: Anthony Cerami, Peter C. Ulrich, Michael Brownlee
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Patent number: 5118709Abstract: 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 tumours. They are prepared in a manner known per se.Type: GrantFiled: August 29, 1990Date of Patent: June 2, 1992Assignee: Ciba-Geigy CorporationInventors: Erfinders J. Stanek, Giorgio Caravatti, Jorg Frei, Hans-Georg Capraro
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Patent number: 4990514Abstract: A solid, non-particulate, non-flowable, non-repellant insecticide bait composition for consumer household control of cockroaches, comprises an insecticide compound, a food attractant system, and a flowable binder, wherein said composition is more readily flowable and process able.Type: GrantFiled: April 27, 1987Date of Patent: February 5, 1991Assignee: The Clorox CompanyInventor: Francis J. Bruey
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Patent number: 4978684Abstract: The present invention relates to methods and agents for preventing the staining of teeth caused by the nonenzymatic browning of proteins in the oral cavity. Both oral and parenteral administration of the agents are disclosed. Suitable agents for the inhibition of nonenzymatic browning may be formulated as rinses and toothpastes, and include compounds capable of reacting with the carbonyl moiety of the early glycosylation product resulting from the initial reaction of a target protein in the nonenzymatic browning reaction. Preferred agents are those having an active nitrogen-containing substituent, as well as amino acids, their esters and amides. These preparations may further include known anti-plaque agents such as chlorhexidine.Type: GrantFiled: January 29, 1988Date of Patent: December 18, 1990Assignee: The Rockefeller UniversityInventors: Anthony Cerami, Michael A. Yamin
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Patent number: 4977145Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, which is (S)-1-[6-amino-2-[[hydroxy-(4-phenylbutyl)phosphenyl]oxy]-1-oxohexyl]-L-pr oline, fosinopril or zofenopril, alone or in combination with an antidepressant drug such as lithium, over a prolonged period of treatment.Type: GrantFiled: December 11, 1989Date of Patent: December 11, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Abraham Sudilovsky
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Patent number: 4870210Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di- lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.Type: GrantFiled: December 18, 1987Date of Patent: September 26, 1989Assignee: American Home Products CorporationInventor: John H. Musser
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Patent number: 4853402Abstract: By using .alpha.-mimetics, particularly compounds of general formulae I to III and the compounds listed in Table I, as feed additives in fattening animals, it has surprisingly been possible to improve the daily weight gain, the utilisation of fodder and the ratio of muscle to fat in favor of the proportion of muscle and protein.Type: GrantFiled: February 26, 1987Date of Patent: August 1, 1989Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Werner Bomann, Franz Esser, Ulrich Hamel, Helmut Stable
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Patent number: 4845103Abstract: A solid, non-particulate, non-flowable, non-repellant insecticide bait composition for consumer household control of cockroaches, comprises a pentadienone hydrazone insecticide compound, a food attractant system, and a binder.Type: GrantFiled: April 11, 1988Date of Patent: July 4, 1989Assignee: American Cyanamid CompanyInventors: Laura Spaulding, Nunzio R. Pasarela