Phosphorus Containing Patents (Class 514/51)
  • Patent number: 6001817
    Abstract: 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: Grant
    Filed: January 12, 1998
    Date of Patent: December 14, 1999
    Assignee: Unitech Pharmaceuticals, Inc.
    Inventor: Jiajiu Shaw
  • Patent number: 5985849
    Abstract: 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: Grant
    Filed: May 4, 1998
    Date of Patent: November 16, 1999
    Assignee: Astra Pharmaceuticals Ltd.
    Inventors: Nicholas Kindon, Premji Meghani, Stephen Thom
  • Patent number: 5981506
    Abstract: 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: Grant
    Filed: January 9, 1998
    Date of Patent: November 9, 1999
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
  • Patent number: 5981507
    Abstract: 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: Grant
    Filed: December 12, 1996
    Date of Patent: November 9, 1999
    Assignee: Advanced Magnetics, Inc.
    Inventors: Lee Josephson, Ernest V. Groman, Yong-Qian Wu
  • Patent number: 5972904
    Abstract: 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: Grant
    Filed: January 9, 1998
    Date of Patent: October 26, 1999
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
  • Patent number: 5965519
    Abstract: 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: Grant
    Filed: July 23, 1996
    Date of Patent: October 12, 1999
    Assignee: Oregon Health Sciences University
    Inventors: Milton B. Yatvin, Michael HB Stowell
  • Patent number: 5939402
    Abstract: 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: Grant
    Filed: March 11, 1998
    Date of Patent: August 17, 1999
    Assignee: Lipitek International, Inc.
    Inventors: Alexander L. Weis, Kirupathevy Pulenthiran
  • Patent number: 5914331
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: June 22, 1999
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
  • Patent number: 5900407
    Abstract: 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: Grant
    Filed: February 6, 1997
    Date of Patent: May 4, 1999
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Benjamin R. Yerxa, Karla M. Jacobus, William Pendergast, Janet L. Rideout
  • Patent number: 5885972
    Abstract: 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: Grant
    Filed: October 2, 1996
    Date of Patent: March 23, 1999
    Assignee: Genencor International, Inc.
    Inventors: Alexander L. Weis, Charles T. Goodhue
  • Patent number: 5877163
    Abstract: A method of treating AIDS with 3'-azido-3'-deoxythymidine in combination with interleukin II or phosphonoformate is presented.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: March 2, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: Janet Litster Rideout, David Walter Barry, Sandra Nusinoff Lehrman, Martha Heider St. Clair, Phillip Allen Furman
  • Patent number: 5852000
    Abstract: 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: Grant
    Filed: June 18, 1996
    Date of Patent: December 22, 1998
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Kazuo Ichihara, Hiroomi Yokoyama
  • Patent number: 5852001
    Abstract: 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: Grant
    Filed: December 23, 1996
    Date of Patent: December 22, 1998
    Assignee: The Endowment for Research in Human Biology
    Inventors: Bert L. Vallee, Aniello Russo
  • Patent number: 5846516
    Abstract: 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: Grant
    Filed: June 3, 1992
    Date of Patent: December 8, 1998
    Assignee: Alliance Pharmaceutial Corp.
    Inventors: Jean G. Riess, Jacques Greiner, Alain Milius, Pierre Vierling, Frederic Guillod, Sylvie Gaentzler
  • Patent number: 5827833
    Abstract: Triciribine and analogs are effective antiviral agents.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: October 27, 1998
    Assignees: Regents of the University of Michigan, Wake Forest University
    Inventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
  • Patent number: 5827831
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: October 27, 1998
    Assignee: NeXstar Pharmaceuticals, Inc.
    Inventors: Karl Y. Hostetler, Raj Kumar, Nagarajan C. Sridhar
  • Patent number: 5817638
    Abstract: 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: Grant
    Filed: June 1, 1995
    Date of Patent: October 6, 1998
    Assignee: NeXstar Pharmaceuticals, Inc.
    Inventor: Karl Y. Hostetler
  • Patent number: 5811408
    Abstract: 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: Grant
    Filed: February 21, 1997
    Date of Patent: September 22, 1998
    Assignee: Yamasa Corporation
    Inventors: Yuichi Yoshimura, Akira Matsuda, Shinji Miura, Takuma Sasaki, Hiroshi Satoh
  • Patent number: 5811421
    Abstract: 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: Grant
    Filed: July 16, 1996
    Date of Patent: September 22, 1998
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Kennan Joseph Fahey, Charles David Jones, Charles Willis Lugar, III
  • Patent number: 5798340
    Abstract: 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: Grant
    Filed: May 6, 1996
    Date of Patent: August 25, 1998
    Assignee: Gilead Sciences, Inc.
    Inventors: Norbert W. Bischofberger, Robert J. Jones, Murty N. Arimilli, Michael S. Louie, Ernest J. Prisbe, William A. Lee
  • Patent number: 5792773
    Abstract: 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: Grant
    Filed: November 15, 1996
    Date of Patent: August 11, 1998
    Assignees: Yale University, University of Georgia Research Foundation
    Inventors: Chung K. Chu, Yung-Chi Cheng, Fucheng Qu
  • Patent number: 5789391
    Abstract: 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: Grant
    Filed: July 3, 1996
    Date of Patent: August 4, 1998
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Karla Jacobus, Janet Rideout, Ben Yerxa, William Pendergast, Suhaib Siddiqi, David Drutz
  • Patent number: 5780220
    Abstract: 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: Grant
    Filed: February 3, 1995
    Date of Patent: July 14, 1998
    Assignee: Trustees of the University of Pennsylvania
    Inventors: David B. Weiner, Yosef Refaeli, David N. Levy
  • Patent number: 5770582
    Abstract: 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: Grant
    Filed: April 10, 1995
    Date of Patent: June 23, 1998
    Assignee: Pro-Neuron, Inc.
    Inventors: Reid Warren von Borstel, Michael Kevin Bamat
  • Patent number: 5763418
    Abstract: 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: Grant
    Filed: August 13, 1996
    Date of Patent: June 9, 1998
    Assignees: Akira Matsuda, Sasaki Takuma, Taiho Pharmaceutical Co., Ltd.,
    Inventors: Akira Matsuda, Sasaki Takuma
  • Patent number: 5747473
    Type: Grant
    Filed: August 18, 1995
    Date of Patent: May 5, 1998
    Assignee: Medivir AB
    Inventors: Bjorn Olof Classon, Bengt Bertil Samuelsson, Ingemar Sven-Anders Kvarnstrom, Lars Goran Svansson, Stefan Carl Tore Svensson
  • Patent number: 5731290
    Abstract: The invention provides diet supplements for pre-operative treatment of patients due for surgery.
    Type: Grant
    Filed: February 27, 1995
    Date of Patent: March 24, 1998
    Assignee: Novartis Corporation
    Inventor: Heinz Schneider
  • Patent number: 5703058
    Abstract: 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: Grant
    Filed: January 27, 1995
    Date of Patent: December 30, 1997
    Assignee: Emory University
    Inventors: Raymond F. Schinazi, Dennis C. Liotta
  • Patent number: 5700590
    Abstract: 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: Grant
    Filed: January 11, 1996
    Date of Patent: December 23, 1997
    Assignee: Abbott Laboratories
    Inventors: Marc Leif Masor, James Lee Leach, Bruce Edward Molitor, John Durand Benson, Jeffrey H. Baxter
  • Patent number: 5698532
    Abstract: 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: Grant
    Filed: July 10, 1996
    Date of Patent: December 16, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joseph Armstrong Martin, Gareth John Thomas
  • Patent number: 5696097
    Abstract: 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: Grant
    Filed: September 15, 1995
    Date of Patent: December 9, 1997
    Assignees: Yamasa Corporation, Akira Matsuda, Takuma Sasaki
    Inventors: Akira Matsuda, Takuma Sasaki, Satoshi Shutou, Akihiro Fujii, Takashi Ono, Shinji Sakata, Takanori Miyashita
  • Patent number: 5686428
    Abstract: Combinations of 3'-azido-3'deoxythymidine and phsphonoformate have been found to produce a synergistic inhibitory effect against human immunodeficiency virus (HIV).
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: November 11, 1997
    Assignee: Aktiebolaget Astra
    Inventors: Bertil F. H. Eriksson, Raymond F. Schinazi
  • Patent number: 5683990
    Abstract: 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: Grant
    Filed: August 21, 1986
    Date of Patent: November 4, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Janet Litster Rideout, David Walter Barry, Sandra Nusinoff Lehrman, Martha Heider St. Clair, Phillip Allen Furman
  • Patent number: 5679459
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 21, 1997
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Jean G. Riess, Jacques Greiner, Alain Milius, Pierre Vierling, Frederic Guillod, Sylvie Gaentzler
  • Patent number: 5654286
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: August 5, 1997
    Inventor: Karl Y. Hostetler
  • Patent number: 5651957
    Abstract: 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: Grant
    Filed: May 2, 1995
    Date of Patent: July 29, 1997
    Assignee: Molichem Medicines, Inc.
    Inventors: Luis Miguel Molina y Vedia, Monroe Jackson Stutts, Richard C. Boucher, Jr., David C. Henke
  • Patent number: 5633235
    Abstract: Triciribine and analogs are effective antiviral agents.
    Type: Grant
    Filed: July 5, 1994
    Date of Patent: May 27, 1997
    Assignees: Regents of the University of Michigan, Wake Forest University
    Inventors: Leroy B. Townsend, John C. Drach, Louis S. Kucera
  • Patent number: 5627161
    Abstract: 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: Grant
    Filed: March 8, 1993
    Date of Patent: May 6, 1997
    Assignee: Memorial Hospital for Cancer and Allied Diseases
    Inventor: M. Earl Balis
  • Patent number: 5627165
    Abstract: 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: Grant
    Filed: September 23, 1994
    Date of Patent: May 6, 1997
    Assignee: Drug Innovation & Design, Inc.
    Inventor: Arnold Glazier
  • Patent number: 5612060
    Abstract: 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: Grant
    Filed: May 25, 1995
    Date of Patent: March 18, 1997
    Inventor: J. Wesley Alexander
  • Patent number: 5604209
    Abstract: 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: Grant
    Filed: June 2, 1994
    Date of Patent: February 18, 1997
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Masaru Ubasawa, Satoshi Yuasa
  • Patent number: 5599796
    Abstract: 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: Grant
    Filed: November 4, 1994
    Date of Patent: February 4, 1997
    Assignee: Emory University
    Inventors: Raymond F. Schinazi, Thomas E. Keane, Dennis C. Liotta
  • Patent number: 5587362
    Abstract: 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: Grant
    Filed: January 28, 1994
    Date of Patent: December 24, 1996
    Assignees: Univ. of GA Research Foundation, Yale University
    Inventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Qing Yao
  • Patent number: 5585364
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: December 17, 1996
    Assignee: British Technology Group Limited
    Inventors: Richard T. Walker, Albert S. Jones
  • Patent number: 5567688
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 22, 1996
    Assignees: Univ. of GA Research Foundation, Yale University
    Inventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Oing Yao
  • Patent number: 5565438
    Abstract: 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: Grant
    Filed: June 6, 1995
    Date of Patent: October 15, 1996
    Assignees: University of GA Research Foundation, Yale University
    Inventors: Chung K. Chu, Yung-Chi Cheng, Balakrishna S. Pai, Gang-Oing Yao
  • Patent number: 5547941
    Abstract: 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: Grant
    Filed: December 9, 1994
    Date of Patent: August 20, 1996
    Assignee: Farmitalia Carlo Erba S.R.L.
    Inventors: Carlo Battistini, Silvia Fustinoni, Maria G. Brasca, Domenico Ungheri
  • Patent number: 5543401
    Abstract: 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: Grant
    Filed: December 9, 1994
    Date of Patent: August 6, 1996
    Assignee: Boehringer Mannheim Italia SpA
    Inventor: Robert L. Stolfi
  • Patent number: 5508270
    Abstract: 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: Grant
    Filed: February 28, 1994
    Date of Patent: April 16, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Anthony D. Baxter, Eric K. Baylis, Stephen P. Collingwood, Roger J. Taylor, Alain Mesmaeker, Chantal Schmit
  • Patent number: 5494900
    Abstract: 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: Grant
    Filed: January 6, 1994
    Date of Patent: February 27, 1996
    Assignee: Boehringer Mannheim Italia SpA
    Inventor: Robert L. Stolfi