Phosphorus Containing Patents (Class 514/51)
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Patent number: 6001817Abstract: A pharmaceutical composition, comprising cisplatin, a special carrier and, optionally, customary pharmaceutical excipients, is disclosed. The preparation of this pharmaceutical composition is also disclosed. The composition may be used to treat cancer and Acquired Immune Deficiency Syndrome (AIDS).Type: GrantFiled: January 12, 1998Date of Patent: December 14, 1999Assignee: Unitech Pharmaceuticals, Inc.Inventor: Jiajiu Shaw
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Patent number: 5985849Abstract: A compound of the formula (I) or salts thereof: ##STR1## wherein X, R.sup.1, Q.sup.1 and Q.sup.2 are as defined in the specification. The compounds have been found to be P2 7-TM G-protein receptor antagonists, especially to the P2 Y2 receptor, and are useful in therapy, for example as anti-inflammatory agents useful in the treatment of a number of inflammatory diseases such as asthma, inflammatory bowel disease, ARDS, psoriasis, rheumatoid arthritis, myocardial ischaemia, COPD, cystic fibrosis, arthrosclerosis, restenosis, peridontal disease, septic shock, osteoarthritis and stroke.Type: GrantFiled: May 4, 1998Date of Patent: November 16, 1999Assignee: Astra Pharmaceuticals Ltd.Inventors: Nicholas Kindon, Premji Meghani, Stephen Thom
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Patent number: 5981506Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: January 9, 1998Date of Patent: November 9, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5981507Abstract: Novel compositions of nucleotide analog prodrugs for the treatment of viral infections and cancer are herein disclosed. The prodrugs have a biocompatible polymeric carrier conjugated to the nucleotide analog via an amino-phosphate linkage. The amino group is provided by the carrier, which either inherently possesses a primary amine, or is modified with reactive groups that incorporate the primary amine onto the carrier. The carrier can be a polyamino acid, a polyvinylic polymer, a polysaccharide or combinations thereof, such as polylysine, HPMA, dextran, hydroxyethyl starch, or polyethylene glycol; the nucleotide analog can be ribavirin araA, AZT, acyclovir, 5-FUDR, araC or ddI. Methods of treating a viral infection of cancer using these prodrugs are also disclosed. The prodrugs endow the nucleotide analogs with substantially enhanced therapeutic efficacy and reduces toxicity in comparison to the nucleotide analog alone.Type: GrantFiled: December 12, 1996Date of Patent: November 9, 1999Assignee: Advanced Magnetics, Inc.Inventors: Lee Josephson, Ernest V. Groman, Yong-Qian Wu
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Patent number: 5972904Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: January 9, 1998Date of Patent: October 26, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5965519Abstract: This invention herein describes a method of facilitating the entry of drugs into cells and tissues at pharmokinetically useful levels and also a method of targeting drugs to specific organelles within the cell. This polar lipid/drug conjugate targeting invention embodies an advance over other drug targeting methods because through this method, intracellular drug concentrations may reach levels which are orders of magnitude higher than those achieved otherwise. Furthermore, it refines the drug delivery process by allowing therapeutic agents to be directed to certain intracellular structures. This technology is appropriate for use with antiproliferative, antibiotic, antimycotic, antiviral and antineoplastic drugs, in particular in combination with a multiplicity of other emollients and agents to make up topically-active substances such as salves, for rapid and efficient introduction of such agents through the epidermis for treatment of skin diseases and other disorders.Type: GrantFiled: July 23, 1996Date of Patent: October 12, 1999Assignee: Oregon Health Sciences UniversityInventors: Milton B. Yatvin, Michael HB Stowell
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Patent number: 5939402Abstract: The invention relates to novel nucleosides and nucleoside dimers containing an L-sugar in at least one of the nucleosides, and their pharmaceutical compositions.Type: GrantFiled: March 11, 1998Date of Patent: August 17, 1999Assignee: Lipitek International, Inc.Inventors: Alexander L. Weis, Kirupathevy Pulenthiran
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Patent number: 5914331Abstract: A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.Type: GrantFiled: June 7, 1995Date of Patent: June 22, 1999Assignee: Emory UniversityInventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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Patent number: 5900407Abstract: A method and preparation for the stimulation of tear secretion in a subject in need of such treatment is disclosed. The method comprises administering to the ocular surfaces of the subject a purinergic receptor agonist such as uridine 5'-triphosphate ?UTP!, dinucleotides, cytidine 5'-triphosphate ?CTP!, adenosine 5'-triphosphate ?ATP!, or their therapeutically useful analogs and derivatives, in an amount effective to stimulate tear fluid secretion. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: February 6, 1997Date of Patent: May 4, 1999Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 5885972Abstract: This invention relates to .alpha. and .beta.-L-pyranosyl nucleosides of Formula (I), wherein the nucleoside substitution on the pyranosyl carbohydrate molecule comprises a substituted or unsubstituted purine (adenine or guanine) or pyrimidine (cytosine, uracil, thymine and hypoxanthine) base. Also provided are methods to make the .alpha. and .beta.-L-pyranosyl nucleosides and methods of using such to treat cancer in a mammal.Type: GrantFiled: October 2, 1996Date of Patent: March 23, 1999Assignee: Genencor International, Inc.Inventors: Alexander L. Weis, Charles T. Goodhue
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Patent number: 5877163Abstract: A method of treating AIDS with 3'-azido-3'-deoxythymidine in combination with interleukin II or phosphonoformate is presented.Type: GrantFiled: July 10, 1997Date of Patent: March 2, 1999Assignee: Glaxo Wellcome Inc.Inventors: Janet Litster Rideout, David Walter Barry, Sandra Nusinoff Lehrman, Martha Heider St. Clair, Phillip Allen Furman
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Patent number: 5852000Abstract: This invention provides a cardiac rehabilitation agent comprising at least one species of the class consisting of purine nucleoside and purine nucleotide, e.g. a composition comprising inosine, cytidine, uridine, a salt of guanosine 5'-monophosphate, and thymidine in a molar ratio of 4:4:3:4:1. The cardiac rehabilitation agent of this invention is characterized by excellent cardiac function-restorative activity and no risk of side effect.Type: GrantFiled: June 18, 1996Date of Patent: December 22, 1998Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Kazuo Ichihara, Hiroomi Yokoyama
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Patent number: 5852001Abstract: A method of inhibiting ribonucleases is disclosed wherein a nucleotide compound having a diphosphate group contacts a ribonuclease so as to inhibit the ribonuclease from effectively catalyzing the depolymerization of ribonucleic acid. Novel compounds useful in the method are also disclosed.Type: GrantFiled: December 23, 1996Date of Patent: December 22, 1998Assignee: The Endowment for Research in Human BiologyInventors: Bert L. Vallee, Aniello Russo
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Patent number: 5846516Abstract: Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals;provided thatR.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.Type: GrantFiled: June 3, 1992Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutial Corp.Inventors: Jean G. Riess, Jacques Greiner, Alain Milius, Pierre Vierling, Frederic Guillod, Sylvie Gaentzler
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Patent number: 5827833Abstract: Triciribine and analogs are effective antiviral agents.Type: GrantFiled: December 19, 1996Date of Patent: October 27, 1998Assignees: Regents of the University of Michigan, Wake Forest UniversityInventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
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Patent number: 5827831Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn- glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.Type: GrantFiled: June 7, 1995Date of Patent: October 27, 1998Assignee: NeXstar Pharmaceuticals, Inc.Inventors: Karl Y. Hostetler, Raj Kumar, Nagarajan C. Sridhar
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Patent number: 5817638Abstract: Compounds for treating hepatitis B infections. The compounds consist of nucleoside analogues having anti-hepatitis B activity which are linked, commonly through a 5' phosphate of the pentose residue, to one of a selected group of lipids. The lipophilic nature of these compounds provides an advantage over the use of the nucleoside analogue alone, making it possible to incorporate them into the lamellar structure of liposomes, either alone or in combination with similar lipid molecules. In the form of appropriately sized liposomes, these anti-hepatitis B agents are preferentially taken up by the liver cells which have been found to harbor the target virus.Type: GrantFiled: June 1, 1995Date of Patent: October 6, 1998Assignee: NeXstar Pharmaceuticals, Inc.Inventor: Karl Y. Hostetler
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Patent number: 5811408Abstract: The present invention relates to 2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides having excellent antitumor activity, represented by formula ?I!: ##STR1## wherein B represents a pyrimidine or purine base, R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, a cyano group or alkyl group, and R.sub.3 represents hydrogen or a phosphoric acid residue, and a method for producing the same, and a use of the same.Type: GrantFiled: February 21, 1997Date of Patent: September 22, 1998Assignee: Yamasa CorporationInventors: Yuichi Yoshimura, Akira Matsuda, Shinji Miura, Takuma Sasaki, Hiroshi Satoh
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Patent number: 5811421Abstract: The present invention provides compounds of formula ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);R.sup.2 is C.sub.1 -C.sub.6 alkyl or C.sub.5 -C.sub.7 cycloalkyl which is optionally substituted with 1 to 3 substitutents selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, amino, nitro, and halo;X is --CH(OH)-- or --CH.sub.2 --;M is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;n is 2 or 3; andR.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Also provided are methods of using the compounds of the present invention for the treatment of various medical indications associated with post-menopausal syndrome, uterine fibroid disease, endometriosis, and aortal smooth muscle cell proliferation.Type: GrantFiled: July 16, 1996Date of Patent: September 22, 1998Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Kennan Joseph Fahey, Charles David Jones, Charles Willis Lugar, III
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Patent number: 5798340Abstract: Nucleotide analogs characterized by the presence of an amidate lirked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolysed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for the synthesis and use are described.Type: GrantFiled: May 6, 1996Date of Patent: August 25, 1998Assignee: Gilead Sciences, Inc.Inventors: Norbert W. Bischofberger, Robert J. Jones, Murty N. Arimilli, Michael S. Louie, Ernest J. Prisbe, William A. Lee
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Patent number: 5792773Abstract: The present invention relates to the discovery that certain .beta.-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV). In particular, the compounds according to the present invention show potent inhibition of the replication of the virus (viral growth) in combination with very low toxicity to the host cells (i.e., animal or human tissue). Compounds are useful for treating EBV infections in humans.Type: GrantFiled: November 15, 1996Date of Patent: August 11, 1998Assignees: Yale University, University of Georgia Research FoundationInventors: Chung K. Chu, Yung-Chi Cheng, Fucheng Qu
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Patent number: 5789391Abstract: A method of promoting drainage of congested mucous secretions in the sinuses of a subject in need of such treatment is disclosed. The method comprises administering to the sinuses of the subject a uridine phosphate such as uridine 5'-triphosphate (UTP) or P.sup.1,P.sup.4 -di(uridine-5') tetraphosphate (U.sub.2 P.sub.4), an analog of UTP, or any other analog, in an amount effective to promote drainage of congested fluid in the sinuses by hydrating mucous secretions or by stimulating ciliary beat frequency in the sinuses. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include any liquid suspension (including nasal drops or spray), oral form (liquid or pill), aerosol inhalation, powder form, topical, injected, intra-operative instillation or suppository form.Type: GrantFiled: July 3, 1996Date of Patent: August 4, 1998Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
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Patent number: 5780220Abstract: A method for treating an individual exposed to or infected with HIV is disclosed which comprises administering to said individual a therapeutically effective amount of one or more compounds which inhibit or prevent replication of said HIV by interfering with the replicative or other essential functions of Vpr expressed by said HIV, by interactively blocking the Vpr target in human cells, and thereby preventing translocation of the Vpr/target complex from the cytosol of said human cells to the nuclei of said cells, where Vpr carries on activities essential to replication of HIV. In preferred embodiments, the compound or compounds which interactively block the target are steroid hormone receptor antagonists, glucocorticoid receptor antagonists, or glucocorticoid receptor Type II antagonists, especially mifepristone (RU-486). Pharmaceutical compositions comprising these compounds, as well as a method for identifying them and a kit for use therein, are also disclosed.Type: GrantFiled: February 3, 1995Date of Patent: July 14, 1998Assignee: Trustees of the University of PennsylvaniaInventors: David B. Weiner, Yosef Refaeli, David N. Levy
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Patent number: 5770582Abstract: The invention relates to compositions comprising 2'-deoxyribonucleosides. The invention also relates to methods of accelerating the healing of wounds, abrasions, cuts, incisions, and superficial burns induced by heat, sunlight, chemical agents, or infections, and methods for ameliorating the effects of aging of the epidermal tissues comprising administering the compositions of the present invention to an animal.Type: GrantFiled: April 10, 1995Date of Patent: June 23, 1998Assignee: Pro-Neuron, Inc.Inventors: Reid Warren von Borstel, Michael Kevin Bamat
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Patent number: 5763418Abstract: The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: ##STR2## in which R.sup.a, R.sup.b and R.sup.c are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R.sup.1 and R.sup.2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R.sup.3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3'-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.Type: GrantFiled: August 13, 1996Date of Patent: June 9, 1998Assignees: Akira Matsuda, Sasaki Takuma, Taiho Pharmaceutical Co., Ltd.,Inventors: Akira Matsuda, Sasaki Takuma
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Patent number: 5747473Type: GrantFiled: August 18, 1995Date of Patent: May 5, 1998Assignee: Medivir ABInventors: Bjorn Olof Classon, Bengt Bertil Samuelsson, Ingemar Sven-Anders Kvarnstrom, Lars Goran Svansson, Stefan Carl Tore Svensson
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Patent number: 5731290Abstract: The invention provides diet supplements for pre-operative treatment of patients due for surgery.Type: GrantFiled: February 27, 1995Date of Patent: March 24, 1998Assignee: Novartis CorporationInventor: Heinz Schneider
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Patent number: 5703058Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a ?5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside or a ?5-carboxamido or 5-fluoro!-3'-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.Type: GrantFiled: January 27, 1995Date of Patent: December 30, 1997Assignee: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotta
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Patent number: 5700590Abstract: An improved enteral formula containing ribo-nucleotide equivalents (RNA, mono-, di- and triphosphate nucleotides, nucleosides and adducts such as activated sugars) at a level of at least 10 mg/100 Kcal (kilocalorie) of formula. More specifically, an infant formula containing at least 10 milligrams of nucleotide equivalents per 100 Kcal of formula where the nucleotide equivalents consist of RNA; mono-, di-, and triphosphate esters of adenosine, cytidine, guanosine, and uridine, and the d-ribose adducts thereof; and wherein the weight ratio of said cytidine nucleotide equivalents to said uridine nucleotide equivalents is 1.5:1 to 2.6:1; of said cytidine nucleotide equivalent to said adenosine nucleotide equivalents is 2:1 to 3.9:1; and of said cytidine nucleotide equivalents to said guanosine nucleotide equivalents is 1.75:1 to 2.8:1, is disclosed. The formula comprises carbohydrates, lipids, proteins, vitamins and minerals and four (4) ribo-nucleotide equivalents at specific levels and ratios.Type: GrantFiled: January 11, 1996Date of Patent: December 23, 1997Assignee: Abbott LaboratoriesInventors: Marc Leif Masor, James Lee Leach, Bruce Edward Molitor, John Durand Benson, Jeffrey H. Baxter
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Patent number: 5698532Abstract: This invention is directed to the novel pyrimidine derivative 1-?5-?2(S)-(2,4-dichloro-5-methoxyphenoxy) propionamido!-2,5-dideoxy-2-fluoro-.beta.-D-arabinofuranosly!-5-ethyluraci l and its use as an antiviral agent, as well as to intermediates useful in the synthesis of this compound.Type: GrantFiled: July 10, 1996Date of Patent: December 16, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Joseph Armstrong Martin, Gareth John Thomas
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Patent number: 5696097Abstract: Novel 2'-methylidenenucleotide compounds of the formula (I) ##STR1## wherein R is a hydrogen or a halogen, R.sup.1 and R.sup.2 are the same or different and each is a fatty acid residue or a hydrocarbon residue, and R.sup.3 and R.sup.4 are the same or different and each is a hydrogen, a halogen or an alkyl; salts thereof; methods for production thereof; and pharmaceutical use thereof. The compounds and salts thereof show an excellent antitumor effect in mammals. More specifically, they show a remarkable activity of inhibiting growth of mouse tumors, cultured human tumor cells, and human tumors transplanted to nude mice, and are useful for the treatment and prevention of recurrence of lung cancer, gastrointestinal cancer, breast cancer, cervical cancer, gynecological cancer, urinological cancer, leukemia, melanoma, lymphogenous metastatic tumor and the like in mammals. They are also useful as antitumor agents since they have an increased bioavailability and low toxicity.Type: GrantFiled: September 15, 1995Date of Patent: December 9, 1997Assignees: Yamasa Corporation, Akira Matsuda, Takuma SasakiInventors: Akira Matsuda, Takuma Sasaki, Satoshi Shutou, Akihiro Fujii, Takashi Ono, Shinji Sakata, Takanori Miyashita
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Patent number: 5686428Abstract: Combinations of 3'-azido-3'deoxythymidine and phsphonoformate have been found to produce a synergistic inhibitory effect against human immunodeficiency virus (HIV).Type: GrantFiled: February 4, 1994Date of Patent: November 11, 1997Assignee: Aktiebolaget AstraInventors: Bertil F. H. Eriksson, Raymond F. Schinazi
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Patent number: 5683990Abstract: Treatment of AIDS or humans carrying or infected with the AIDS virus or having antibodies to the AIDS virus is disclosed using the compound 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof. Also disclosed is the use of the 5'-mono-, di- and triphosphate of 3'-azido-3'-deoxythymidine or a pharmaceutically acceptable basic salt thereof for the same purpose. Additionally, there is disclosed the treatment of Kaposi's sarcoma with 3'-azido-3'-deoxythymidine (AZT) and the synergistic activity in the treatment of humans infected with HTLV-III of AZT and interferon as well as AZT and acyclovir and AZT and 2-amino-9-(2-hydroxyethoxymethyl)purine or an ester thereof.Type: GrantFiled: August 21, 1986Date of Patent: November 4, 1997Assignee: Glaxo Wellcome Inc.Inventors: Janet Litster Rideout, David Walter Barry, Sandra Nusinoff Lehrman, Martha Heider St. Clair, Phillip Allen Furman
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Patent number: 5679459Abstract: Perfluoroalkylated amphiphilic phosphorus compounds, corresponding to the formulae: ##STR1## wherein V is O or S;R.sup.1, R.sup.2 and R.sup.3 are H or substituted or unsubstituted perfluoroalkylated or hydrocarbon radicals;provided thatR.sup.1, R.sup.2 or R.sup.3 is a perfluoroalkylated radical; and Y and Z are radicals which can bear a part derived from a sugar, a polyol, or a hydrophilic polymer such as polyethyleneglycol, a perfluoroalkylated part or a part derived from a pharmaceutically active molecule, and method for their preparation and use. These compounds can be included in preparations, emulsions, dispersions, gels, microemulsions, notably for biomedical uses.Type: GrantFiled: June 6, 1995Date of Patent: October 21, 1997Assignee: Alliance Pharmaceutical Corp.Inventors: Jean G. Riess, Jacques Greiner, Alain Milius, Pierre Vierling, Frederic Guillod, Sylvie Gaentzler
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Patent number: 5654286Abstract: Typical treatment of psoriasis and other diseases of skin cell hyperproliferation using pharmaceutical compositions containing mono-, di, and tri-phosphate esters of antiproliferative nucleoside analogs and related analogs, DNA chain-terminating dideoxynucleosides and other nucleoside analogs. The useful phosphate esters include phosphoramidates and phosphothiorates, as well as polyphosphates having C and S bridging atoms.Type: GrantFiled: June 7, 1995Date of Patent: August 5, 1997Inventor: Karl Y. Hostetler
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Patent number: 5651957Abstract: A method of facilitating the clearance of retained pulmonary secretions in a subject using lantibiotics is disclosed. The method comprises administering to the lungs of the subject an effective amount of a lantibiotic. The lantibiotic is preferably administered by topically applying it to the respiratory epithelia, such as by generating an aerosol thereof which is then inhaled by the subject. A preferred lantibiotic for carrying out the present invention is duramycin. The method may be used in treating disorders such as cystic fibrosis, chronic bronchitis, and asthma. Also disclosed is a method of combatting tuberculosis comprising administering a lantibiotic to a subject in need of such treatment.Type: GrantFiled: May 2, 1995Date of Patent: July 29, 1997Assignee: Molichem Medicines, Inc.Inventors: Luis Miguel Molina y Vedia, Monroe Jackson Stutts, Richard C. Boucher, Jr., David C. Henke
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Patent number: 5633235Abstract: Triciribine and analogs are effective antiviral agents.Type: GrantFiled: July 5, 1994Date of Patent: May 27, 1997Assignees: Regents of the University of Michigan, Wake Forest UniversityInventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
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Patent number: 5627161Abstract: UDPG shows tumor-specific inhibition of PRPP and this suggests that this action might prove to be useful in combination therapy with inhibitors of purine and pyrimidine nucleotide synthesis in various rescue regimens. High levels of PRPP in tumors were greatly affected by treatment with UDPG.Type: GrantFiled: March 8, 1993Date of Patent: May 6, 1997Assignee: Memorial Hospital for Cancer and Allied DiseasesInventor: M. Earl Balis
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Patent number: 5627165Abstract: The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells and into tissues in vivo. Prodrugs for a variety of antiviral and anti-leukemic agents are described.Type: GrantFiled: September 23, 1994Date of Patent: May 6, 1997Assignee: Drug Innovation & Design, Inc.Inventor: Arnold Glazier
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Patent number: 5612060Abstract: An improved immunomodulatory therapy for enhancement of depressed host defense mechanisms as shown by improved allograft survival rates is disclosed. The therapy comprises the synergistic combination of an immunomodulatory diet consisting of an amino acid such as arginine, ornithine and their salts, a nucleotide such as RNA and fish oil as a source of omega-3-fatty acids together with an immunosuppressive treatment comprising the administration of a donor specific transfusion and cyclosporine.Type: GrantFiled: May 25, 1995Date of Patent: March 18, 1997Inventor: J. Wesley Alexander
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Patent number: 5604209Abstract: Antiviral agents which comprises as active ingredients one or more 2',3'-dideoxyribonucleosides or phosphoric esters thereof and 6-benzyl-1-ethoxymethyl-5-substituted uracil derivative of the formula (I): ##STR1## wherein X is oxygen or sulfur atom; R.sup.1 is ethyl or isopropyl; R.sup.2 and R.sup.3 are independently hydrogen atom, C.sub.1 -C.sub.3 alkyl or halogen atom, which compounds can inhibit HIV reverse transcriptase through different mechanisms and are synergistic in combination.Type: GrantFiled: June 2, 1994Date of Patent: February 18, 1997Assignee: Mitsubishi Chemical CorporationInventors: Masaru Ubasawa, Satoshi Yuasa
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Patent number: 5599796Abstract: Methods and compositions for treating urogenital tumors, and particular, cancer of the prostate, bladder, and kidney, with BCNT, are disclosed. Any boron-containing compound that is sufficiently lipophilic to pass through the appropriate urogenital membranes in a quantity high enough to achieve therapy on irradiation with low-energy neutrons can be used. Carboranyl-containing nucleosides and oligonucleotides are particularly suited for use in BNCT of urogenital tumors. Preferred compounds include 5-carboranyl-2'-deoxyuridine (CDU) and 5-o-carboranyl-1-(2-deoxy-2-fluoro-.beta.-D-arabinofuranosyl)uracil (CFAU). Nucleosides and oligonucleotides bearing an -O-[(carboran-1-yl)alkyl]phosphate, S-[(carboran-1-yl)alkyl]phosphorothioate, or Se-[(carboran-1-yl)alkyl]phosphoroselenoate in place of the (carboran-1-yl)phosphonate moiety can be used.Type: GrantFiled: November 4, 1994Date of Patent: February 4, 1997Assignee: Emory UniversityInventors: Raymond F. Schinazi, Thomas E. Keane, Dennis C. Liotta
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Patent number: 5587362Abstract: A compound, and a pharmaceutical composition comprising an effective mount to treat HBV or EBV of a compound, of the formula: ##STR1## wherein R is selected from the group consisting of 5-methyluracil, adenine and cytosine, and R' is hydrogen, acyl, or alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.Type: GrantFiled: January 28, 1994Date of Patent: December 24, 1996Assignees: Univ. of GA Research Foundation, Yale UniversityInventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Qing Yao
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Patent number: 5585364Abstract: Compounds of formula I or a pharmaceutically acceptable salt thereof: ##STR1## in which formula R.sub.1 represents an aliphatic hydrocarbyl group; Ar represents a substituted or unsubstituted aromatic nucleus;X represents --SO.sub.2 -- or --CO-- andR.sub.2 and R.sub.3 which may be identical or different represent moieties of formula (a), (b), (c), (d), (e), (f), (g), (h) or (i): ##STR2## wherein B represents the residue of a nucleoside base of formula (A), (G), (C), (H) or (T): ##STR3## provided that when R.sub.2 and R.sub.3 both represent an unsubstituted moiety of formula (a) B represents the residue of a nucleoside base which is of formula (A), (G), (C) or (H) are of value for their antiviral activity.Type: GrantFiled: June 6, 1995Date of Patent: December 17, 1996Assignee: British Technology Group LimitedInventors: Richard T. Walker, Albert S. Jones
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Patent number: 5567688Abstract: A method for the treatment of a human infected with HBV that includes administering an HBV-treatment amount of an L-nucleoside of the formula: ##STR1## wherein R is selected from the group consisting of 5-methyluracil, adenine and cytosine, and R' is hydrogen, acyl, alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.Type: GrantFiled: June 6, 1995Date of Patent: October 22, 1996Assignees: Univ. of GA Research Foundation, Yale UniversityInventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Oing Yao
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Patent number: 5565438Abstract: A method for the treatment of a human infected with EBV that includes administering an EBV-treatment amount of an L-nucleoside of the formula: ##STR1## wherein R is 5-methyluracil, and R' is hydrogen, acyl, alkyl or a monophosphate, diphosphate or triphosphate ester, or its pharmaceutically acceptable salt.Type: GrantFiled: June 6, 1995Date of Patent: October 15, 1996Assignees: University of GA Research Foundation, Yale UniversityInventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Oing Yao
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Patent number: 5547941Abstract: There are provided compounds of formula (I) ##STR1## wherein each group B is, independently, a naturally occurring or modified heterocyclic base linked through a nitrogen or a carbon atom of the ring to the sugar moiety;each group X is a, independently, hydrogen, fluorine, hydroxy, or a C.sub.1 -C.sub.6 alkoxy group;each group Y is, independently, hydrogen, sulphidryl or hydroxy; and the pharmaceutically acceptable salts thereof.A process for their preparation and pharmaceutical compositions comprising them are also described. The compounds of this invention can be useful as antivirals, particularly as anti-HIV (Human Immunodeficiency Virus) agents, namely as drugs to be used against AIDS (Acquired Immunodeficiency Syndrome) therapeutically and/or prophylatically.Type: GrantFiled: December 9, 1994Date of Patent: August 20, 1996Assignee: Farmitalia Carlo Erba S.R.L.Inventors: Carlo Battistini, Silvia Fustinoni, Maria G. Brasca, Domenico Ungheri
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Patent number: 5543401Abstract: A method of rescuing healthy cells of a cancer patient being treated with antipyrimidine antitumor compounds, or related compounds. Rescue is accomplished by administering UDPG after administering the antipyrimidine antitumor compound preferably with BAU administration.Type: GrantFiled: December 9, 1994Date of Patent: August 6, 1996Assignee: Boehringer Mannheim Italia SpAInventor: Robert L. Stolfi
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Patent number: 5508270Abstract: A compound of formula ##STR1## where R.sup.1 is hydrogen or a protecting group Q;R.sup.2 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion;R.sup.3 and R.sup.4 are independently hydrogen, halogen or hydroxy;R.sup.5 is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being unsubstituted or substituted, or R.sup.5.sub.a ;R.sup.5.sub.a is hydrogen, fluorine, chlorine, hydroxy, --OR.sup.8, --OCOR.sup.8 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.6 is hydrogen, a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.16 araliphatic radical, --COR.sup.9, --SO.sub.2 R.sup.9 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.7 is a monovalent nucleoside base radical, hydroxyl, --OR.sup.8 or --OCOR.sup.8, andR.sup.9 are independently a C.sub.Type: GrantFiled: February 28, 1994Date of Patent: April 16, 1996Assignee: Ciba-Geigy CorporationInventors: Anthony D. Baxter, Eric K. Baylis, Stephen P. Collingwood, Roger J. Taylor, Alain Mesmaeker, Chantal Schmit
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Patent number: 5494900Abstract: A method of rescuing healthy cells of a cancer patient being treated with antipyrimidine antitumor compounds, or related compounds. Rescue is accomplished by administering UDPG after administering the antipyrimidine antitumor compound preferably with BAU administration.Type: GrantFiled: January 6, 1994Date of Patent: February 27, 1996Assignee: Boehringer Mannheim Italia SpAInventor: Robert L. Stolfi