Two Or More Px- Groups Attached To The Same 1,3-diazine (x Is Chalcogen) Patents (Class 514/88)
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Patent number: 8999959Abstract: The invention relates to medicine and can be used for treating liver lesions caused by chemical or biological agents. The drug for treating liver lesions caused by chemical or biological agents is embodied as 1-(4-bromophenyl)-6-hydroxy-5-nitroso-1,2,3,4-tetrahydropyrimidine-2.4-dione: (I), or salts thereof having the general formula: (II), where X is selected from Na+, K+, Li+, NH4+, NH2CONH3+ or another pharmacologically acceptable cation. The effectiveness of the preparation in treating liver diseases of different etiologies is increased.Type: GrantFiled: October 10, 2011Date of Patent: April 7, 2015Inventors: Viktor Veniaminovich TETS, Georgy Viktorovich TETS, Konstantin Andreevich Krasnov
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Patent number: 7511027Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: November 22, 2002Date of Patent: March 31, 2009Assignees: Georgetown University, University of Georgia Research Foundation, Inc.Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
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Patent number: 7115592Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).Type: GrantFiled: June 16, 2004Date of Patent: October 3, 2006Assignees: Institute of Organic Chemistry, Biochemistry of the Academy of Sciences of the Czech RepublicInventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy, Dana Hockova
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Patent number: 6818633Abstract: Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the compounds of formula (I).Type: GrantFiled: June 28, 2002Date of Patent: November 16, 2004Assignees: Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic, Rega Stichting v.z.w.Inventors: Jan M. R. Balzarini, Erik D. A. De Clercq, Antonin Holy
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Patent number: 6670342Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: March 29, 2001Date of Patent: December 30, 2003Assignees: Georgetown University, Cornell Research Foundation, Inc., University of Georgia Research Foundation, Inc.Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
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Patent number: 6645972Abstract: The present invention provides a novel method for treating leukemia in a host that has been previously treated with a Bcr-Abl tyrosine kinase inhibitor comprising administering to the host a therapeutically effective amount of a compound having the formula I: wherein B is cytosine or 5-fluorocytosine and R is selected from H, monophosphate, diphosphate, triphosphate, carbonyl substituted with a C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, and and where in each Rc is independently selected from the group comprising H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl an hydroxy protecting group.Type: GrantFiled: November 4, 2002Date of Patent: November 11, 2003Assignee: Shire BioChem Inc.Inventors: Jacques Jolivet, Francis Giles, Hagop Kantarjian
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Publication number: 20030027799Abstract: The present invention provides a novel method for treating a patient with cancer comprising administering to the patient a therapeutically effective amount of cisplatin and a compound having the formula I: 1Type: ApplicationFiled: March 28, 2002Publication date: February 6, 2003Applicant: Shire BioChem Inc.Inventor: Jacques Jolivet
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Patent number: 6444656Abstract: The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: wherein n, X, Q U R1′, R1, Z and R2 are defined here within. The compounds object of the present invention may be a single enantiomers or as mixtures of said enantiomers, the compounds may have a &agr;D, &agr;-L, &bgr;-D, &bgr;-L, R or S configuration at each chiral center or mixtures thereof. This invention also relates to pharmaceutical compositions containing them, alone or in combination with other therapeutic agents, and their use as antiviral agents, particularly against HIV and/or HBV infections in mammals.Type: GrantFiled: March 24, 2000Date of Patent: September 3, 2002Assignee: BioChem Pharma, Inc.Inventors: Nghe Nguyen-Ba, Rabindra Rej
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Patent number: 6300356Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.Type: GrantFiled: August 10, 2000Date of Patent: October 9, 2001Assignee: Merck & Co., Inc.Inventors: Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
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Patent number: 6200961Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.Type: GrantFiled: December 16, 1998Date of Patent: March 13, 2001Assignee: Aquatrols Corporation of America, Inc.Inventors: Stanley J. Kostka, Rennan Pan
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Patent number: 6201002Abstract: Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.Type: GrantFiled: January 6, 1998Date of Patent: March 13, 2001Assignee: Merck & Co., Inc.Inventors: Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
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Patent number: 5880111Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.Type: GrantFiled: June 7, 1995Date of Patent: March 9, 1999Inventors: Dan Farcasiu, John F. Hartmann, Pal Herczegh, Ferenc J. Sztaricskai
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5190930Abstract: Araliphatylaminoalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is an aromatically substituted aliphatic radical, R.sub.2 is hydrogen or a monovalent aliphatic radical and alk is a divalent aliphatic radical, and their salts, exhibit a pronounced regulatory action on the calcium metabolism and can be used as medicaments for the treatment of diseases that are attributable to calcium metabolsim disorders. They are prepared, for example, by reacting a compound of formula ##STR2## wherein X.sub.3 is carboxy and R.sub.0 is a radical R.sub.2, with phosphorous acid and phosphorus trichloride and hydrolysing the primary product.Type: GrantFiled: December 20, 1991Date of Patent: March 2, 1993Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 5133972Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.Type: GrantFiled: June 29, 1990Date of Patent: July 28, 1992Assignee: Ciba-Geigy CorporationInventors: Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
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Patent number: 5098931Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) and (II): ##STR1##Type: GrantFiled: September 24, 1990Date of Patent: March 24, 1992Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Wasyl Halczenko, George D. Hartman
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Patent number: 4971958Abstract: The present invention provides diphosphonic acid derivatives of the general formula: ##STR1## according to claim 1. These compounds are useful for the treatment or prophylaxis of calcium metabolism disturbance or disease.Type: GrantFiled: May 23, 1989Date of Patent: November 20, 1990Assignee: Boehringer Mannheim GmbHInventors: Elmar Bosies, Rudi Gall
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Patent number: 4871720Abstract: Aromatically substituted azacycloalkylalkanediphosphonic acids of the formula ##STR1## in which R represents an aromatically substituted azacycloaliphatyl radical that is bonded to the group alk by way of a nitrogen atom and that optionally contains an additional nitrogen atom, and alk represents a divalent aliphatic radical, and their salts, can be used for the treatment of illnesses that can be attributed to calcium metabolism disorders. They are manufactured, for example, by reacting a compound of the formulaR--alk--X.sub.3 (IV)in which X.sub.3 represents carboxy, carbamoyl or cyano, with phosphorus acid and phosphorus trichloride and in an intermediate of the formula ##STR2## obtained by starting from compounds of the formula IV in which X.sub.3 represents cyano or carbamoyl and by working up by hydrolysis, or in a salt thereof, replacing the amino group by hydroxy by treatment with nitrous acid.Type: GrantFiled: November 16, 1987Date of Patent: October 3, 1989Assignee: Ciba-Geigy CorporationInventor: Knut A. Jaeggi
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Patent number: 4824843Abstract: Novel N-(substituted-phenyl)-5-(2,5-dimethylphenoxy)-2,2-dimethylpentanamides which are useful in preventing the intestinal absorption of cholesterol, as well as novel pharmaceutical compositions and methods of use, as well as processes for their manufacture are herein described.Type: GrantFiled: June 25, 1987Date of Patent: April 25, 1989Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, Robert F. Meyer
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Patent number: 4584295Abstract: Heterocyclic compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and X are as defined hereinafter, process for their preparation, as well as pesticidal compositions containing these compounds as the active ingredient and methods for using the pesticidal compositions for the control of pests are described.Type: GrantFiled: December 27, 1983Date of Patent: April 22, 1986Assignee: Hoffmann-La Roche Inc.Inventor: Christoph Luthy