Phosphorus Containing Patents (Class 514/48)
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Patent number: 6043223Abstract: Improved compositions and methods for increasing permeability of abnormal brain tissue to pharmaceutical agents. Cyclic GMP specific phosphodiesterase inhibitors are combined with bradykinin or a bradykinin analog to provide enhanced permeability of brain capillaries which is limited to abnormal brain tissue. Neuropharmaceutical and neurodiagnostic agents introduced into the bloodstream are directed selectively to the abnormal brain tissue. The pharmaceutical preparation composed of bradykinin or a bradykinin analog and a cyclic GMP specific phosphodiesterase inhibitor may be administered either intravenously or directly into the carotid artery.Type: GrantFiled: November 12, 1997Date of Patent: March 28, 2000Assignee: The Regents of the University of CaliforniaInventor: Keith L. Black
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Patent number: 6040297Abstract: 5,5'-Pyrophosphates of non-naturally occurring nucleosides selected from 1-(1-thyminyl)-3-azido-2, 3-dideoxy-D-riboside, 1(5-fluoro-1-uracilyl)-2, 3-dideoxy-D-riboside, 1-(1-uracilyl)-3-azido-2, 3-dideoxy-D-riboside, 1-(9-guaninyl)-2, 3-dideoxy-D-riboside, 1-(9-hypoxanthinyl)-2, 3-dideoxy-D-riboside, 1-(1-cytosinyl)-2, 3-dideoxy-D-riboside, and 1-(9-adeninyl)-2, 3-dideoxy-D-riboside, are described as well as their manufacture and use as therapeutic agents against tumors and retroviral infections including HIV infections. The compounds may be administered as the active ingredients of pharmaceutical compositions or as prodrugs encapsulated within biological carriers, e.g. transformed erythrocytes, for targeting to specific cell populations responsible for the development of the noted pathological disorders.Type: GrantFiled: January 14, 1997Date of Patent: March 21, 2000Assignees: Biosearch Italia, S.p.A., Gruppo Lepetit, S.p.A.Inventors: Antonio De Flora, Umberto Benatti, Marco Giovine
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Patent number: 6004939Abstract: It was found that normal human stem cells produce a regulated non-processive telomerase activity, while cancer cells produce a processive telomerase activity. Nucleotide analogs, such as 7-deaza-2'-deoxyquanosine-5'-triphosphate (7-deaza-dGTP) were found to be substrates for processive telomerase and incorporated into telomeric sequence. The incorporation of this nucleotide subsequently affected the processivity of telomerase, converting processive telomerase to non-processive telomerase. The incorporation of this nucleotide analogs was also found to inhibit formation of G-quartets by telomeric sequence. Other methods for converting cancer processive telomerase to the more benign non-processive telomerase include partially cleaving the telomerase RNA.Type: GrantFiled: June 20, 1997Date of Patent: December 21, 1999Assignees: CTRC Research Foundation Board of Regents, The University of Texas SystemInventors: Shih-Fong Chen, Ira Maine, Sean M. Kerwin, Terace M. Fletcher, Miquel Salazar, Blain Mamiya, Makoto Wajima, Bradford E. Windle
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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: 5985338Abstract: The present invention relates generally to a method of producing plant proteins for use in nutritional products that have reduced levels of phytoestrogens, manganese or nucleotides. More specifically, this invention is directed to a method of using ion exchange technology to remove phytoestrogens, manganese or nucleotides from plant proteins. This invention is also directed to the plant protein product resulting from the inventive process and to nutritional products that use the plant protein product as a source of amino nitrogen.Type: GrantFiled: June 30, 1998Date of Patent: November 16, 1999Assignee: Abbott LaboratoriesInventors: John D. Suh, Karin M. Ostrom, Louis I. Ndife, Paul S. Anloague, James N. Chmura, Andre Daab-Krzykowski, Paul W. Johns, Diane M. Garcia, Terrence B. Mazer, Fu-I Mei
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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: 5958884Abstract: Methods and compositions for treating patients having erectile dysfunction are described. The method involves the step of treating a patient with a combination of an AT.sub.1 specific Angiotensin II antagonist and Angiotensin II agonist. Preferably the AT.sub.1 specific Angiotensin II antagonist is an AT.sub.1 specific Angiotensin II antagonist. The composition is a pharmaceutical composition including an equivalent molecular ratio of an AT.sub.1 specific Angiotensin II antagonist and Angiotensin II agonist.Type: GrantFiled: March 25, 1998Date of Patent: September 28, 1999Assignee: The Brigham and Women's Hospital, Inc.Inventors: Imre Kifor, Gordon Williams
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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: 5902793Abstract: This invention is directed to a method for stimulating, the proliferation of V.gamma.2V.delta.2 T cells comprising contacting V.gamma.2V.delta.2 T cells with a V.gamma.2V.delta.2 T cell proliferation stimulating amount of a compound selected from the group-consisting of a monoalkyl phosphate, a hydroxy monoalkyl phosphate, a carboxy monoalkyl phosphate, a monoalkyl pyrophosphate, an alkenyl pyrophosphate, a .gamma.-monoalkyl nucleoside triphosphate, a .gamma.-monoalkyl deoxnucleoside triphosphate, a .gamma.-alkenyl nucleoside triphosphate, and a .gamma.-alkenyl deoxynucleoside triphosphate.Type: GrantFiled: June 16, 1997Date of Patent: May 11, 1999Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Barry R. Bloom, Yoshimasa Tanaka, Shigetoshi Sano
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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: 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: 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: 5804563Abstract: The invention is directed to synthetic receptor(s) which comprises a polyfunctional organic template covalently linked to two or more oligomers which may independently be the same or different and may independently be straight chain or branched. The template may be linked to an identifier which uniquely defines the synthetic receptor. The identifier is a stable chemical molecule or a plurality of stable chemical molecules distinguishable and detectable to picomolar levels or may be an oligonucleotide. In an preferred embodiment, the template is covalently linked to a solid support which is linked to an identifier.Type: GrantFiled: April 8, 1996Date of Patent: September 8, 1998Assignee: The Trustees of Columbia University in The City of New YorkInventors: W. Clark Still, Ge Li
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Patent number: 5801159Abstract: Purine derivatives are provided for treatment of cellular stress, particularly hypoxia. By administering the purine derivatives by themselves or in conjunction with other compounds, particularly electron acceptor compounds and/or amino acids, the time for irreversible cellular changes, particularly mortality, can be greatly extended.Type: GrantFiled: February 23, 1996Date of Patent: September 1, 1998Assignee: Galileo Laboratories, Inc.Inventors: Guy Miller, Lillian Lou, John Nakamura
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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: 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: 5739120Abstract: The present invention relates to new liponucleotide analog compounds having useful antiviral activity, represented by general formula (I): ##STR1## wherein R.sup.1 is a saturated or unsaturated alkyl having 6-22 C atoms; R.sup.2 is a saturated or unsaturated alkyl having 12-20 C atoms; R.sup.3 and R.sup.4 are each hydrogen or hydroxy; and B is one of the nucleoside bases of formula (a): ##STR2## wherein R.sup.5 is a hydrogen, halogen, hydroxy, amino, mercapto, or C.sub.1 -C.sub.4 alkyl amino; R.sup.6 is a hydrogen, halogen or amino; W is a nitrogen or C--R.sup.8 where R.sup.8 is hydrogen, halogen, amino or C.sub.1 -C.sub.4 alkyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 30, 1997Date of Patent: April 14, 1998Assignee: Boryung Pharmaceutical Co., Ltd.Inventors: Woo Hyun Paik, Won Sup Shin, Jae Seung Lee, Hee Sang Chai
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Patent number: 5736530Abstract: Guanylic acid derivatives according to either of the formulae: ##STR1## in which Me is a metal trace element indispensable for the enzymatic activity of physiological processes.These derivatives, prepared in gastro-resistant galenic form with in situ release of active ingredients, are proposed for the treatment of psychasthenia, depression, anxiety and geriatric disorders.Type: GrantFiled: January 29, 1997Date of Patent: April 7, 1998Assignee: Societe de Recherche Auvergnate pour l'Innovation en Oligotherapie-Inolig o-Inventors: Dat Xuong Nguyen, Jean Rapin, Patrick Lambropoulos, Jean Daver
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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: 5728705Abstract: This invention provides a method of selectively decreasing pulmonary vascular resistance in a subject by administering endobronchially a drug chosen from among cAMP analogs, cGMP analogs, phosphodiesterase inhibitors, nitric oxide precursors, nitric oxide donors, and nitric oxide analogs.Type: GrantFiled: October 4, 1993Date of Patent: March 17, 1998Assignee: The Trustees of Columbia University in the City of New YorkInventors: Charles A. Lawson, David J. Pinsky, Arthur Smerling, David M. Stern
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Patent number: 5712258Abstract: Purine-containing compounds that modulate cardiac muscle contractility are provided, as well as methods for modulating cardiac muscle contractility and receptors that bind the compounds.Type: GrantFiled: March 23, 1995Date of Patent: January 27, 1998Assignee: The Trustees of the University of PennsylvaniaInventor: Bruce T. Liang
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Patent number: 5693521Abstract: Acyloxyalkyl esters of phosphate-containing second messengers which are capable of permeating cell membranes. Once inside the cell, the ester derivatives undergo enzymatic conversion to the biologically active form of the second messenger. Acyloxyalkyl esters of second messengers, such as cAMP, cGMP, inositol triphosphate and inositol tetraphosphate are disclosed.Type: GrantFiled: April 9, 1993Date of Patent: December 2, 1997Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Carsten Schultz
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Patent number: 5691307Abstract: Novel O.sup.6 -substituted guanine compounds and pharmaceutical compositions thereof are useful for effectively reducing O.sup.6 -alkylguanine-DNA alkyltransferase (AGT). The novel compounds are useful for treating tumors and when used with anti-neoplastic alkylating agents enhance the chemotherapeutic treatment of tumor cells in a host.Type: GrantFiled: June 7, 1994Date of Patent: November 25, 1997Assignees: The United States of America as represented by the Department of Health and Human Services, The Penn State Research Foundation, Arch Development CorporationInventors: Robert C. Moschel, M. Eileen Dolan, Anthony E. Pegg, Mark G. McDougall, Mi-Young Chae
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Patent number: 5668113Abstract: It has been found that 1,5-anhydrohexitol nucleoside analogues, wherein a 4-substituted-2,3,4-trideoxy-1,5-anhydrohexitol is coupled via its 2-position to the heterocyclic ring of a pyrimidine or purine base, exhibit remarkable anti-viral properties against herpes viruses, pox viruses and related viruses.The new nucleoside analogues are represented by the general formula I ##STR1## wherein B is a heterocyclic ring derived from a pyrimidine or purine base, X represents H, N.sub.3, F, Cl, Br, I, amino, --NHR.sup.2, --N(R.sup.2).sub.2, --OR.sup.2, --SR.sup.2 or CN, R.sup.1 and R.sup.2 are the same or different and hydrogen, alkyl, acyl or phosphate groups are represented, or wherein X is hydrogen and a double bond is situated between the 3- and 4- position of the 1,5-anhydrohexitol ring.Pharmaceutically acceptable salts and esters thereof are included.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Stichting Rega VZWInventors: Erik Desire Alice De Clercq, Piet Andre Maurits Herdewlin, Arthur Albert Edgard Van Aerschot
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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: 5654285Abstract: There are disclosed compounds of formula I, ##STR1## wherein Q represents CR.sup.1 R.sup.2,R represents O or CR.sup.3 R.sup.4,W represents O or CH.sub.2,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen or halogen,X represents S(O).sub.n R.sup.5, alkyl C.sub.1-6 alkoxy C.sub.1-6, acylamino C.sub.1-6, CONR.sup.6 R.sup.7, NR.sup.8 R.sup.9, halogen, a 5- or 6-membered S containing heterocycle, or phenyl optionally substituted by alkyl C.sub.1-6,n represents 0, 1 or 2,R.sup.5 represents aryl or alkyl C.sub.1-6 optionally substituted by one or more substituents selected from hydroxy, alkoxy C.sub.1-6, halogen and aryl;R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently represent hydrogen or alkyl C.sub.1-6,Y represents NH.sub.2 or alkoxy C.sub.1-6, andZ represents an acidic moiety,in addition, when R represents CR.sup.3 R.sup.4, then --Q--Z may also represent hydroxy or --OP(O)(OH).sub.2,and pharmaceutically acceptable salts thereof, with certain provisos, for use as pharmaceuticals.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Astra Pharmaceuticals LimitedInventors: Anthony H. Ingall, Peter A. Cage
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Patent number: 5641500Abstract: The instant invention is directed to the use of a pharmaceutical composition containing an effective amount of adenosine or an adenosine analog or derivative as an agent useful in the treatment of hormone-independent cancers, such as prostate cancer. The invention is also directed to diagnostic uses of these compounds to determine effective treatment regimes for specific tumors, a process for screening for new, therapeutically useful analogs of these compounds, and the use of these compounds in facilitating the extraction of intracellular components.Type: GrantFiled: May 15, 1995Date of Patent: June 24, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Jane B. Trepel, Wei-Gang Fang, Farzaneh Pirnia, Charles E. Myers, Jr.
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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: 5593976Abstract: The invention relates to ureido derivatives of substituted pyrroles of formula ##STR1## wherein each of m and n, being the same, is an integer of 1 to 3; W is oxygen of sulphur;each of the B groups, which are the same, isa) a saturated or unsaturated, carbocyclic or condensed carbocyclic ring substituted by one or more acid groups;b) a saturated or unsaturated, heteromonocyclic or heterobicyclic ring, containing one or more heteroatoms chosen from nitrogen, oxygen and sulphur, substituted by one or more acid groups;c) a pyranyl or furanyl sugar residue substituted by one or more acid groups; ord) a --CH.sub.2 (CHA).sub.8 CH.sub.2 A group, wherein each A group, being the same or different, is an acid group and r is 0, 1 or 2;and the pharmaceutically acceptable salts thereof, which are useful as angiogenesis inhibitors.Type: GrantFiled: April 21, 1995Date of Patent: January 14, 1997Assignee: Farmitalia Carlo Erba S r lInventors: Nicola Mongelli, Giovanni Biasoli, Alfredo Paio, Maria Grandi, Marina Ciomei
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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: 5571524Abstract: An agent for curing ischemic myocardial disease which contains an effective amount of diadenosine 5',5'"-p.sup.1,p.sup.4 -tetraphosphate (Ap4A) of formula (I): ##STR1## or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignees: Unitika Ltd., Fujirebio, Inc.Inventors: Masafumi Kitakaze, Masatsugu Hori, Takenobu Kamada, Hiroshi Nakajima, Akihiro Sekine, Tetsuaki Yamaura
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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: 5449664Abstract: Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine;X and X' are H, OH or F, provided that at least one is H;Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H;Y' and Z together form a cyclic phosphate ester, provided that Y is H; orZ is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, andwhen X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine;and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.Type: GrantFiled: December 16, 1991Date of Patent: September 12, 1995Assignee: Syntex (U.S.A.) Inc.Inventors: Julien P. H. Verheyden, Hans Maag, Ernest J. Prisbe
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Patent number: 5422343Abstract: The invention provides an anti-MRSA prophylactic/therapeutic composition containing as an active ingredient at least one nucleic acid component selected from among inosine, guanosine n'-monophosphate (GMP) (n'=2', 3'or 5'), uridine and thymidine.Type: GrantFiled: March 5, 1993Date of Patent: June 6, 1995Assignee: Otsuka Pharmaceutical Factory, Inc.Inventors: Sigeru Yamamoto, Hiroomi Yokoyama
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Patent number: 5415873Abstract: The instant invention is directed to the use of a pharmaceutical composition containing an effective amount of adenosine or an adenosine analog or derivative as an agent useful in the treatment of hormone-independent cancers, such as prostate cancer. The invention is also directed to diagnostic uses of these compounds to determine effective treatment regimes for specific tumors, a process for screening for new, therapeutically useful analogs of these compounds, and the use of these compounds in facilitating the extraction of intracellular components.Type: GrantFiled: October 4, 1993Date of Patent: May 16, 1995Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Jane B. Trepel, Wei-Gang Fang, Farzaneh Pirnia, Charles E. Myers, Jr.
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Patent number: 5391550Abstract: Disclosed are methods and compositions of matter for increasing the intracellular synthesis of ATP. The compositions comprise amino acids, metabolites, electrolyte and/or a pentose sugar. When applied to wounds, the invention increases the rate of wound repair and has a antimicrobial effect. When administered orally, the invention increases ATP blood levels and physical performance levels.Type: GrantFiled: October 2, 1989Date of Patent: February 21, 1995Assignee: Raymond A. RoncariInventors: Francis J. Carniglia, Alan J. Kenyon
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Patent number: 5246708Abstract: Methods are provided for promoting wound healing in animals by administering compositions containing two or more of the following 2'-deoxyribonucleosides: 2'-deoxyadenosine, 2'-deoxyguanosine, 2'-deoxy-cytidine, or thymidine. 3'- and 5'-phosphate derivatives of these 2'-deoxynucleosides are also effective in promoting wound healing.Type: GrantFiled: July 13, 1992Date of Patent: September 21, 1993Assignee: Pro-Neuron, Inc.Inventors: Reid W. von Borstel, Michael K. Bamat
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Patent number: 5231174Abstract: The present invention is concerned wtih new 2'-isomeric 2 2',3'-dideoxy-2'.beta.-D-nucleosides and their derivatives where the base moiety has .beta.-stereochemistry but is transposed from the normal 1'-position to the 2'-position and the carbohydrate moiety has the D-configuration at the 4'-position. These compounds are resistant towards hydrolytic cleavage of the glycosidic bond and are resistant to enzymatic deamination. They have potential in the treatment or prophylaxis of viral infections, particularly retroviral infections and especially AIDS.Type: GrantFiled: February 27, 1992Date of Patent: July 27, 1993Assignee: University of Iowa Research FoundationInventor: Vasu Nair
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Patent number: 5219570Abstract: Agglomerated psyllium husk comprising edible acid uniformly dispersed throughout the agglomerating coating. Preferred are maltodextrin-containing agglomerates of psyllium husk comprising citric acid uniformly dispersed throughout the maltodextrin coating. This agglomerated psyllium husk has improved mixability and dispersilibity in liquids.Type: GrantFiled: March 25, 1992Date of Patent: June 15, 1993Assignee: The Procter & Gamble CompanyInventor: Melvin A. Barbera
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Patent number: 5192749Abstract: Nucleosides compounds of Formula I: ##STR1## wherein B is a purine or a pyrimidine;X and X' are H;Y is H;Y' is OH, F or H;or Y' and X' together makes a bond;Z is ##STR2## where n is zero, one, two or three; or Y' and Z together form a cyclic phosphate ester; Z' is --CN, --CH.sub.3, CH.sub.2 N.sub.3 or --CH.sub.2 J,where J is a halogen atom;or Z' and Y' together are --CH.sub.2 O--; and pharmaceutically acceptable esters, ethers, amides, N-acyl moieties and salts thereof.Type: GrantFiled: May 21, 1990Date of Patent: March 9, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Counde O-Yang, Keith A. M. Walker, Walter Kurz, Helen Y. Wu
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Patent number: 5187163Abstract: Novel anti-viral compounds comprise phosphate-linked dimers of anti-viral nucleoside derivatives, or salts or esters of such nucleoside dimers. Pharmaceutical compositions containing the dimers and methods of treatment utilizing the same are disclosed.Type: GrantFiled: January 28, 1992Date of Patent: February 16, 1993Assignee: Baker Norton Pharmaceuticals, Inc.Inventors: Phillip Frost, Jack Fishman, Elliot Hahn, Jing J. Lu
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Patent number: 5187162Abstract: Methods of preventing neural tissue damage caused by excitotoxicity due to increased release of excitatory amino acids by increasing extracellular concentrations of adenosine in and around the neural tissue are provided. These methods are especially useful in treating neurodegenerative diseases such as Parkinson's Disease, Alzheimer's Disease, Amyotrophic Lateral Sclerosis or Huntington's Disease.Type: GrantFiled: September 12, 1990Date of Patent: February 16, 1993Assignee: Gensia PharmaceuticalsInventors: Paul Marangos, Harry E. Gruber
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Patent number: 5130302Abstract: A novel class of pharmaceutically active boronated nucleosides are provided. The nucleosides are boronated at a ring nitrogen of the purine or pyrimidine or analogues thereof. Also provided are phosphate esters of these nucleosides and oligomers thereof. Methods of making and using the boronated nucleosides are also disclosed.Type: GrantFiled: December 20, 1989Date of Patent: July 14, 1992Assignee: Boron Bilogicals, Inc.Inventors: Bernard F. Spielvogel, Anup Sood, Iris H. Hall, Barbara Ramsay Shaw
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Patent number: 5118672Abstract: This invention provides compounds and pharmaceutical compositions that include compounds of the formula: ##STR1## in which A, B, and C are hydrogen, halogen, or azido; D is hydrogen, halogen, azido, or OH; A and B or C and D can be replaced with a double bond; R is an aldohexose, aldohexosamine, or N-acetyl aldohexosamine, W is O or S; X is O, S, or CH.sub.2 ; Y is a purine or pyrimidine base, Z is C, S, or O, and wherein when Z is S or O, A and C are not present. The compounds of this inverntion have enhanced pharmaceutical or biological activity or increased intracellular absorption compared to the corresponding parent nucleoside as a function of the 5'-diphosphohexose moiety. Many of these compounds have antiviral, including anti-HIV, activity. Others have antibacterial activity. In one embodiment, the invention is a method to treat HIV infection and opportunistic infections concomitantly.Type: GrantFiled: July 11, 1990Date of Patent: June 2, 1992Assignees: University of Georgia Research Foundation, Emory University, UAB Research FoundationInventors: Raymond F. Schinazi, Jean-Pierre Sommadossi, Chung K. Chu, William M. Shafer