Leukemia Patents (Class 514/908)
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Patent number: 6432924Abstract: A composition, device, kit and method for countering or diagnosing cytidine deaminase or deoxycytidine deaminase over-expression or a disorder associated with it, or an increase in number or toxicity of pro-inflammatory cells that over-express cytidine deaminase or deoxycytidine deaminase or a disorder associated with it, utilizing an agent of the formula C7N3H8O2R1R2XX1, wherein X and X1 are each independently C or N, R1 is lower alkyl, alkenyl and alkynyl, halogen or haloalkyl, and R2 is H, —N3 —OH, amino or halogen; or pharmaceutically acceptable salts thereof.Type: GrantFiled: January 28, 2000Date of Patent: August 13, 2002Assignee: East Carolina UniversityInventor: Jonathan W. Nyce
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Patent number: 6372726Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.Type: GrantFiled: September 27, 1999Date of Patent: April 16, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Patent number: 6312737Abstract: The invention includes a method of inducing apoptosis in cancer cells by administering an extract of Melothria indica Lou to the cancer cells. The invention also includes a method of using an extract of Melothria indica Lou to induce apoptosis in cancer cells by administering the extract to the cancer cells. The cancer cells can be leukemia cells and prostate cancer cells. Further included in the invention is a method for purifying the Melothria indica Lou into an extract used for inducing apoptosis in cancer cells.Type: GrantFiled: May 10, 2000Date of Patent: November 6, 2001Assignee: Ambryx Biotechnology, Inc.Inventor: David Tsai
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Patent number: 6297354Abstract: The present invention relates to a class of pentapeptide analogs of LHRH. These compounds are useful in the treatment of disease conditions which are mediated by reproductive hormones, including benign prostate hyperplasia, prostate tumors, breast and ovaries tumors, cryptorchidism, hirsuitism, gastric motility disorders, dysmenorrhea, and endometriosis.Type: GrantFiled: August 12, 1999Date of Patent: October 2, 2001Assignee: Abbott LaboratoriesInventors: Fortuna Haviv, Wesley Dwight, Jonathan Greer
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Patent number: 6288074Abstract: Lymphoproliferative syndrome, including such diseases as malignant lymphoma, chronic lymphocytic leukemia, Hodgkin's lymphoma, and non-Hodgkin's lymphoma, is treated in human patients by the administration by a pharmacologically effective mode or route of an essentially pure opiate receptor antagonist, typified by Naltrexone and Naloxone, exerting substantially higher blocking action for Mu opiate receptor sites than against Delta opiate receptor sites at a low dose concentration which produces therapeutic results corresponding to those obtained by the administration of Naltrexone at a low dosage level in the range of 1.0 mg. to 10 mg. and at which Delta receptor blocking activity is at most small and Mu receptor blocking activity is significant and most preferably substantially exclusive. Naltrexone is suitable for oral administration and is preferred.Type: GrantFiled: November 15, 1999Date of Patent: September 11, 2001Inventor: Bernard Bihari
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Patent number: 6258779Abstract: The present invention provides the methods to isolate the proteins specifically induced apoptosis (programmed cell death) in prostate cancer cells (LNCAP), leukemia cells (HL-60), and breast cancer cells (MCF-70), but without effect in normal human lung fibroblast cells (CCD 39 Lu). P-1 has no effect on breast cancer cells. Five proteins have been isolated from the conditioned media of culture cells: (1) Apogen P-1: the proteins (Apogen P-1a, Apogen P-1b and Apogen P-1c) isolated from the conditioned medium of XC cells are able to induce apoptosis in prostate cancer cells (LNCAP) without effect in normal human lung fibroblast (CCD 39 Lu), colon cancer (T84), breast cancer (MCF-7) and leukemia (HL-60) cells. (2) Apogen P-2: the protein isolated from the conditioned medium of C3H1OT1/2 cells is able to induce apoptosis in prostate cancer cells (LNCAP) and breast cancer (MCF-7) without effect in normal human lung fibroblast (CCD 39 Lu) and colon cancer (T84) cells.Type: GrantFiled: October 7, 1999Date of Patent: July 10, 2001Inventors: David Tsai, Jenny Yu
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Patent number: 6238675Abstract: The present invention is directed to a method of preparation and the composition of a water soluble extract of the plant species Uncaria. The present invention is also directed to the pharmaceutical use of the composition for the enhancement of the immune, anti-inflammatory, anti-tumor and DNA repair processes of warm blooded animals. The present preparation of the water soluble extract of the plant species Uncaria results in the depletion of many of the ingredients which lead to various toxic side effects associated with other extracts or compositions derived from Uncaria. Also, the present preparation leads to the depletion of many of the active ingredients commonly associated with other extracts and compositions of the plant species Uncaria.Type: GrantFiled: November 16, 1999Date of Patent: May 29, 2001Assignee: CampaMed Corp.Inventor: Ronald W. Pero
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Patent number: 6228850Abstract: Use of betulinic acid and/or its derivatives for inhibiting and/or preventing angiogenesis is described. Compositions containing betulinic acid derivatives with or without betulinic acid can be used for these purposed.Type: GrantFiled: October 6, 1998Date of Patent: May 8, 2001Assignee: Dabur Research FoundationInventors: Manu Jaggi, Sunder Ramadoss, Praveen Rajendran, Mohammad Jamshed Ahmad Siddiqui
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Patent number: 6174873Abstract: Disclosed are compositions including an adenosine analog, wherein the composition comprises a dosage form suitable for oral (co)administration. Also disclosed are compositions including adenosine analogs, wherein the composition is in a dosage form including a pill, capsule, lozenge, or tablet, and compositions including adenosine analogs, wherein the composition is in a dosage form comprising a liquid. Additionally disclosed are methods of administering the inventive composition, and kits including the inventive compositions.Type: GrantFiled: November 4, 1998Date of Patent: January 16, 2001Assignee: SuperGen, Inc.Inventor: Simeon M. Wrenn, Jr.
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Patent number: 6156725Abstract: A pharmaceutical composition useful for killing or inhibiting multiplication of cancer cells. It is expected that the pharmaceutical composition will be useful in preventing, inhibiting, or modulating the hypersecretion of VIP, somatostatin, bombesin, Substance P, or a combination of VIP, somatostatin, bombesin, or Substance P. The composition may suitably comprise, consist of, or consist essentially of a therapeutically effective combination of peptide analogs of somatostatin, VIP, bombesin, and Substance P. Also provided is a method of treatment for humans or other animals suffering from cancer, the method comprising administering a therapeutically effective dose of the pharmaceutical composition so as to kill or inhibit the multiplication of cancer cells. The method of treatment may be particularly useful in the treatment of cancers of the colon and rectum.Type: GrantFiled: October 8, 1996Date of Patent: December 5, 2000Assignee: National Institute of ImmunologyInventors: Rama Mukherjee, Manu Jaggi
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Patent number: 6127423Abstract: The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions.Type: GrantFiled: July 31, 1998Date of Patent: October 3, 2000Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Hans Michael Jennewein, Christopher John Montague Meade, Andreas Ding
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Patent number: 6100290Abstract: Multiple sclerosis and rheumatoid arthritis can be treated effectively using photodynamic therapy. In this protocol, a photoactive compound is administered, allowed to distribute in the effected subject, and the subject is then irradiated to activate the photoactive compound. Alternatively, the blood of a subject to be treated can be subjected to PDT extracorporeally. In the case of rheumatoid arthritis, localized treatment at the joints may also be employed.Type: GrantFiled: September 14, 1998Date of Patent: August 8, 2000Assignees: QLT Inc., The University of British ColumbiaInventors: Julia G. Levy, Janice North
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Patent number: 6083530Abstract: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.Type: GrantFiled: May 26, 1998Date of Patent: July 4, 2000Assignee: The Liposome Company, Inc.Inventors: Lawrence D. Mayer, Marcel B. Bally, Pieter R. Cullis, Richard S. Ginsberg, George N. Mitilenes
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Patent number: 6071914Abstract: This invention relates to a method for inhibiting the growth of neoplasms, in a mammal having a prolactin profile. This method involves comparing the prolactin profile of the afflicted mammal to a standard prolactin profile for healthy mammals of the same species and sex and adjusting the prolactin profile of the afflicted mammal to conform to or approach the standard prolactin profile for a mammal of the same species and sex of the afflicted mammal, thereby inhibiting the neoplastic growth.Type: GrantFiled: May 31, 1996Date of Patent: June 6, 2000Assignees: The Board of Supervisors of Louisiana State University and Agricultural and Mechanical College, Ergo Research CorporationInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 6060505Abstract: Disclosed are modified bryostatins and their use as anticancer drugs.Type: GrantFiled: February 16, 1999Date of Patent: May 9, 2000Assignees: The United States of America as represented by the Department of Health and Human Services, Arizona Board of Regents of Arizona State UniversityInventors: Peter M. Blumberg, Zoltan Szallasi, George R. Pettit
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Patent number: 6051549Abstract: This invention identifies a biologically active group of peptide sequences from Type I repeat units of the extracellular matrix protein, human thrombospondin-1, identical or homologous to the sequence, KRFKQDGGWSHWSPWSSC (SEQ ID NO.30). The biological activities residing with the full sequences, portions thereof, and variants of the full or partial sequences are disclosed. The invention describes how biological activity may be enhanced by covalently linking these peptides to suitable carriers, preferably a branched, water-soluble polymer of low (or absent) toxicity and immunogenicity, such as polysucrose (Ficoll.TM.). The invention describes (1) a method for preparing such conjugates, (2) the use of the defined peptides or their conjugates in blocking or modifying the action on cellular processes of heparin (e.g.Type: GrantFiled: March 11, 1998Date of Patent: April 18, 2000Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: David D. Roberts, Henry C. Krutzsch, Nenghua Guo
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Patent number: 6048847Abstract: The invention relates to use of betulinic acid and/or its derivatives for treating, inhibiting, and/or preventing tumors or cancer growth more particularly, to treating leukemia, lymphomas, lung, prostate and ovarian cancer. This invention also relates to novel betulinic acid derivatives and a composition containing betulinic acid derivatives with or without betulinic acid.Type: GrantFiled: March 18, 1998Date of Patent: April 11, 2000Assignee: Dabur Research FoundationInventors: Sunder Ramadoss, Manu Jaggi, Mohammad Jamshed Ahmad Siddiqui
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Patent number: 6039949Abstract: The present invention is directed to a method of preparation and the composition of a water soluble extract of the plant species Uncaria. The present invention is also directed to the pharmaceutical use of the composition for the enhancement of the immune, anti-inflammatory, anti-tumor and DNA repair processes of warm blooded animals. The present preparation of the water soluble extract of the plant species Uncaria results in the depletion of many of the ingredients which lead to various toxic side effects associated with other extracts or compositions derived from Uncaria. Also, the present preparation leads to the depletion of many of the active ingredients commonly associated with other extracts and compositions of the plant species Uncaria.Type: GrantFiled: February 27, 1997Date of Patent: March 21, 2000Assignee: CampaMed, Inc.Inventor: Ronald W. Pero
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Patent number: 6025343Abstract: The present invention is directed to new nucleoside monophosphate derivatives of lipid ester residues of general formula (I) ##STR1## wherein R.sup.1 represents an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.2 represents hydrogen, an optionally substituted alkyl chain having 1-20 carbon atoms;R.sup.3, R.sup.4 and R.sup.5 represent hydrogen, hydroxy, azido, amino, cyano, or halogen;X represents a valence dash, oxygen, sulfur, a sulfinyl or sulfonyl group;Y represents a valence dash, an oxygen or sulfur atom;B represents a purine and/or pyrimidine base;with the proviso that at least one of the residues R.sup.3 or R.sup.5 is hydrogen;to their tautomers and their physiologically acceptable salts of inorganic and organic acids and/or bases, as well as to processes for their preparation, and to drugs containing said compounds.Type: GrantFiled: November 27, 1996Date of Patent: February 15, 2000Assignee: Roche Diagnostics GmbHInventors: Dieter Herrmann, Hans-Georg Opitz, Harald Zilch, Alfred Mertens
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Patent number: 6013674Abstract: This invention provides novel indenone derivatives, their pharmaceutical formulations and their use for the inhibition of leukocyte adherence to cells.Type: GrantFiled: May 1, 1998Date of Patent: January 11, 2000Assignee: Eli Lilly and CompanyInventors: John Michael Morin, Jr., Michael Dean Kinnick, Robert Theodore Vasileff, William Thomas Jackson
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Patent number: 6011041Abstract: The present invention is particularly directed to the use of a derivative of vinblastine, 3',4'-anhydrovinblastine (AHVB), which differs from vinblastine in that it possesses a double bond at the 3',4' position of the caranthine nucleus rather than the hydroxyl group that is present in the parent structure, as an antineoplastic agent in the therapeutic treatment of cancer. Specifically, the treatment of lymphoma with 3',4'-anhydrovinblastine is disclosed.Type: GrantFiled: July 26, 1996Date of Patent: January 4, 2000Assignee: University of British ColumbiaInventors: Bruce Schmidt, James Kutney, Lawrence Mayer
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Patent number: 6001882Abstract: The invention provides methods of using photoactivated hypericin compounds which, when photoactivated using visible or UV-A light, are useful for treating numerous diseases and disorders in mammals. The compounds of the invention are useful for inhibiting the proliferation and accumulation of mammalian leukocytes and for inducing apoptosis in mammalian leukocytes.Type: GrantFiled: July 3, 1997Date of Patent: December 14, 1999Assignee: The Trustees of the University of PennsylvaniaInventors: Floyd Eliot Fox, Alain H. Rook, Alfonso J. Tobia
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Patent number: 5994298Abstract: The present invention provides the methods to isolate the proteins specifically induced apoptosis (programmed cell death) in prostate cancer cells (LNCAP), leukemia cells (HL-60), and breast cancer cells (MCF-70), but without effect in normal human lung fibroblast cells (CCD 39 Lu). P-1 has no effect on breast cancer cells. Five proteins have been isolated from the conditioned media of culture cells: (1) Apogen P-1: the proteins (Apogen P-1a, Apogen P-1b and Apogen P-1c) isolated from the conditioned medium of XC cells are able to induce apoptosis in prostate cancer cells (LNCAP) without effect in normal human lung fibroblast (CCD 39 Lu), colon cancer (T84), breast cancer (MCF-7) and leukemia (HL-60) cells. (2) Apogen P-2: the protein isolated from the conditioned medium of C3H10T1/2 cells is able to induce apoptosis in prostate cancer cells (LNCAP) and breast cancer (MCF-7) without effect in normal human lung fibroblast (CCD 39 Lu) and colon cancer (T84) cells.Type: GrantFiled: September 8, 1998Date of Patent: November 30, 1999Inventors: David Tsai, Jenny Yu
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Patent number: 5908845Abstract: A compound comprising a polyether backbone bearing a plurality of ligands that are individually bound to chiral carbon atoms located within said backbone, at least one of said ligands including a moiety selected from the group consisting of a naturally occurring nucleobase, a nucleobase binding group and a DNA intercalator; a process of synthesizing the compound, monomers to be used in this process and their synthesis process and processes for using the compound in biochemistry and medicine.Type: GrantFiled: October 30, 1996Date of Patent: June 1, 1999Inventor: David Segev
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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: 5869464Abstract: The compounds of the invention are a 2'-deoxy-5-fluorouridine derivative represented by the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is a hydrogen atom or a group easily hydrolyzable in vivo, the other is a benzyl group which may optionally have at least one halogen atom or trifluoromethyl group as a substituent on the phenyl ring, and R.sub.3 is a lower alkyl group, and a pharmaceutically acceptable salt thereof.The compounds of the invention can be suitably used as an antitumor agent.Type: GrantFiled: August 21, 1995Date of Patent: February 9, 1999Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Makoto Nomura, Makoto Kajitani, Junichi Yamashita, Masakazu Fukushima, Yuji Shimamoto
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Patent number: 5846954Abstract: The present invention provides polyanionic, substituted CDs having cellular growth modulating-activity. The invention further provides CDs having anionic groups on one side of the CD molecule. Therapeutic methods for using, as well as methods of making the CD compounds of the invention, are also disclosed herein.Type: GrantFiled: June 23, 1997Date of Patent: December 8, 1998Assignee: The Trustees of the University of PennsylvaniaInventors: Madeleine M. Joullie, Paul B. Weisz
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Patent number: 5821236Abstract: 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumor therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.Type: GrantFiled: May 24, 1995Date of Patent: October 13, 1998Assignee: Glaxo Wellcome Inc.Inventors: Thomas Anthony Krenitsky, Devron Randolph Averett, George Walter Koszalka
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Patent number: 5820872Abstract: Methods and pharmaceutical compositions for improving the effectiveness of radiation therapy for treating a subject having an internal solid tumor malignancy are disclosed. The methods include irradiating the tumor to release tumor-derived antigens in vivo, preparing a cellular vaccine including the isolated antigens admixed with a preparation of altered antigen presenting cells and administering the cellular vaccine to the subject. In the preferred embodiments, the antigen presenting cells are leukocytes that have been photochemically altered by subjecting the cells to photopheresis.Type: GrantFiled: July 30, 1993Date of Patent: October 13, 1998Assignee: Yale UniversityInventors: Richard L. Edelson, Francis P. Gasparro
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Patent number: 5814632Abstract: An immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative, which is safe for the human, animals or the like, an immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative and (1) proline and/or glutamine, (2) an antibiotic, or (3) a water-soluble polymer or lecithin, which is safe for the human, animals or the like, and a process for the production thereof.Type: GrantFiled: April 12, 1995Date of Patent: September 29, 1998Assignee: Eisai Co., Ltd.Inventors: Seiichi Araki, Mamoru Suzuki, Masatoshi Fujimoto
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Patent number: 5807881Abstract: Multiple sclerosis and rheumatoid arthritis can be treated effectively using photodynamic therapy. In this protocol, a photoactive compound is administered, allowed to distribute in the effected subject, and the subject is then irradiated to activate the photoactive compound. Alternatively, the blood of a subject to be treated can be subjected to PDT extracorporeally. In the case of rheumatoid arthritis, localized treatment at the joints may also be employed.Type: GrantFiled: September 22, 1994Date of Patent: September 15, 1998Assignees: Quadra Logic Technologies, Inc., University of British ColumbiaInventors: Simon Leong, Agnes How-Ching Chan, David William Carey Hunt, Julia Levy, Martin Renke
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Patent number: 5795589Abstract: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a tranamembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problem related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.Type: GrantFiled: February 5, 1997Date of Patent: August 18, 1998Assignee: The Liposome Company, Inc.Inventors: Lawrence D. Mayer, Marcel B. Bally, Pieter R. Cullis, Richard S. Ginsberg, George N. Mitilenes
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Patent number: 5792748Abstract: This invention relates to a method for inhibiting the growth of neoplasms, in a mammal having a prolactin profile. This method involves comparing the prolactin profile of the afflicted mammal to a standard prolactin profile for healthy mammals of the same species and sex and adjusting the prolactin profile of the afflicted mammal to conform to or approach the standard prolactin profile for a mammal of the same species and sex of the afflicted mammal, thereby inhibiting the neoplastic growth.Type: GrantFiled: June 7, 1995Date of Patent: August 11, 1998Assignees: The General Hospital Corporation, The Board of Supervisors of Louisiana State University and Agricultural & Mechanical CollegeInventors: Anthony H. Cincotta, Albert H. Meier
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Patent number: 5776898Abstract: A method is disclosed treating a tumor in a host by administering a nonemulsified ultrapurified polymerized hemoglobin solution to the host and also administering a chemotherapeutic agent to the host. In a particularly preferred embodiment, the hemoglobin is bovine hemoglobin.Type: GrantFiled: June 7, 1995Date of Patent: July 7, 1998Assignees: Dana-Farber Cancer Institute, Biopure CorporationInventors: Beverly A. Teicher, Carl W. Rausch, Robert E. Hopkins, II
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Patent number: 5776966Abstract: Treatment with a set of porphyrin compounds using a photodynamic therapy approach is able selectively to lower elevated levels of activated leukocytes in a leukocyte population. This is particularly helpful in subjects containing such elevated levels of T-cell subsets, such as HIV-infected subjects.Type: GrantFiled: May 27, 1992Date of Patent: July 7, 1998Assignees: University of British Columbia, Quadra Logic Technologies Inc.Inventor: Janice North
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Patent number: 5747472Abstract: 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumour therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.Type: GrantFiled: May 31, 1995Date of Patent: May 5, 1998Assignee: Glaxo Wellcome Inc.Inventors: Thomas Anthony Krenitsky, Devron Randolph Averett, George Walter Koszalka, Gerald Wolberg
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Patent number: 5747502Abstract: The present invention relates to benzo?c!phenanthridinium derivative of the general formula A: ##STR1## wherein M and N individually represent a hydroxyl or lower alkoxy group, or M and N simultaneously represent a hydrogen atom or together form a methylenedioxy group, X.sup.- represents an acid residue or a hydrogen acid residue, and R represents a lower alkyl group, and a process for preparing such derivatives. The compounds exhibit both potent antitumor activity and platelet aggregation inhibition activity, and are expected to be useful for the treatment of tumors. The process has good reproducibility and may be effected under moderate conditions, and therefore the process is practically useful. In addition, hydrogen salts of the present compounds have an enhanced stability, which is an advantage in formulating the same into pharmaceutical preparations.Type: GrantFiled: March 16, 1992Date of Patent: May 5, 1998Assignee: Nippon Kayaku Kabushiki KaishaInventors: Miyoji Hanaoka, Hisao Ekimoto, Fumiko Kobayashi, Yukio Irie, Katsutoshi Takahashi, Masanobu Suzuki, Takeshi Nakanishi, Osamu Kogawa, Keizou Ishikawa
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Patent number: 5744455Abstract: Disclosed is a method for preventing cardiotoxicity in a human in need of such preventive treatment, the method including administering an effective amount of a bisdioxopiperazine. Also disclosed is a method for preventing cardiotoxicity induced by the administration of an anthracycline. Further, a tumoricidal, cardioprotective combination of agents is disclosed.Type: GrantFiled: September 3, 1993Date of Patent: April 28, 1998Assignee: New York UniversityInventors: James Leonard Speyer, Franco Mario Muggia, Michael David Green
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Patent number: 5686496Abstract: The new compound of formula ##STR1## may be prepared by conventional methods and used therapeutically as an LTB.sub.4 -receptor antagonist.Type: GrantFiled: March 28, 1997Date of Patent: November 11, 1997Assignee: Boehringer Ingelheim KGInventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Franz Birke, Armin Fugner, Hubert Heuer, Christopher Meade
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Patent number: 5679638Abstract: A method is disclosed treating a tumor in a host by administering a nonemulsified ultrapurified polymerized hemoglobin solution to the host and also administering a chemotherapeutic agent to the host. In a particularly preferred embodiment, the hemoglobin is bovine hemoglobin.Type: GrantFiled: July 20, 1993Date of Patent: October 21, 1997Assignees: Biopure Corporation, Dana Farber Cancer InstituteInventors: Beverly A. Teicher, Carl W. Rausch, Robert E. Hopkins, 2nd
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Patent number: 5665760Abstract: Disclosed are reconstituted lyophilized formulations for the treatment of mammalian tumors comprising a thioxanthenone antitumor agent in combination with mannitol or sucrose as a stabilizer in a lactate buffer.Type: GrantFiled: September 18, 1995Date of Patent: September 9, 1997Assignee: Sanofi Winthrop, Inc.Inventors: Stephen Brown, Gurdial Singh Sandhu
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Patent number: 5663193Abstract: The present invention is directed to non-peptide compounds which inhibit farnesyl-protein transferase (FPTase) and the farnesylation of the oncogene protein Ras. The invention also relates to the process for the preparation of a compound of this invention by cultivating a culture of Phoma sp. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: July 17, 1996Date of Patent: September 2, 1997Assignee: Merck & Co., Inc.Inventors: Carmen Cascales, Russell B. Lingham, Fernando Pelaez, Jon D. Polishook, Keith C. Silverman, Sheo B. Singh, Deborah L. Zink
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Patent number: 5641758Abstract: Novel cytarabine derivatives of the formula ##STR1## where R.sup.1, R.sup.2 and R.sup.3, which can be identical or different, are each selected from the group consisting of hydrogen, aliphatic C.sub.2 -C.sub.5 -acyl, benzoyl or carboxy-C.sub.1 -C.sub.3 -alkylcarbonyl are described. The compounds are suitable for use directly or in the form of immunoliposomes for controlling diseases. Methods of preparing the novel cytarabine derivatives are also disclosed.Type: GrantFiled: November 7, 1994Date of Patent: June 24, 1997Inventors: Michael Kluge, Herbert Schott
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Patent number: 5620703Abstract: A process for stimulating hematopoietic activity in animals which comprises administering to a patient in need therefor a therapeutically effective amount of an agent containing as its active ingredient a water-soluble or lipid-soluble transition metal compound in a lyotropic mesophase, the agent optionally containing one or more additional carriers for stimulating hematopoietic activity.Type: GrantFiled: March 31, 1994Date of Patent: April 15, 1997Assignee: Max-Delbruck-Centrum Fur Molekulare MedizinInventors: Regina Reszka, Iduna Fichtner
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Patent number: 5616330Abstract: This invention is directed to a composition of a taxine in a stable oil-in-water emulsion for intravenous administration. The invention also relates to a method for incorporating a taxine into an oil and making a stable oil-in-water emulsion.The composition includes a taxine, an oil, water and a surfactant. In a preferred embodiment, the taxine is taxol, the oil is safflower oil and the surfactant is lecithin, The taxine is incorporated into the oil by dissolving the taxine in a solution of an oil and a taxine co-solvent, such as isopropanol, for example. The co-solvent then is removed to form a solution of the taxine in oil. This solution may be dispersed in water with a surfactant to form a stable oil-in-water emulsion for intravenous administration.Type: GrantFiled: July 19, 1994Date of Patent: April 1, 1997Assignee: HemaGen/PFCInventors: Robert J. Kaufman, Thomas J. Richard, Ralph W. Fuhrhop
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Patent number: 5616567Abstract: The pyrimidine compounds of the present invention are represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein, R.sup.1 represents a hydroxyl or an amino which may be substituted by an acyl group; R.sup.2 represents a hydrogen atom or an alkyl having 1 to 4 carbons; R.sup.3 represents a hydrogen or a hydroxyl; and R.sup.4 and R.sup.5 each represent a hydrogen or together form a group --R.sup.6 R.sup.7 Si--O--SiR.sup.6' R.sup.7' --, wherein R.sup.6, R.sup.7, R.sup.6' and R.sup.7' are the same or different from one another and each represent an alkyl having 1 to 4 carbons. The compounds of the present invention exhibit an excellent antitumor effect.Type: GrantFiled: September 7, 1994Date of Patent: April 1, 1997Assignee: Sankyo Company, LimitedInventors: Takuma Sasaki, Akira Matsuda, Tohru Ueda, deceased
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Patent number: 5616341Abstract: A method for encapsulation of antineoplastic agents in liposomes is provided, having preferably a high drug:lipid ratio. Liposomes may be made by a process that loads the drug by an active mechanism using a transmembrane ion gradient, preferably a transmembrane pH gradient. Using this technique, trapping efficiencies approach 100%, and liposomes may be loaded with drug immediately prior to use, eliminating stability problems related to drug retention in the liposomes. Drug:lipid ratios employed are about 3-80 fold higher than for traditional liposome preparations, and the release rate of the drug from the liposomes is reduced. An assay method to determine free antineoplastic agents in a liposome preparation is also disclosed.Type: GrantFiled: August 26, 1993Date of Patent: April 1, 1997Assignee: The Liposome Company, Inc.Inventors: Lawrence D. Mayer, Marcel B. Bally, Pieter R. Cullis, Richard S. Ginsberg, George N. Mitilenes
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Patent number: 5580562Abstract: A Tripterygium wilfordii Hook F preparation having an improved LD.sub.50 in mice, an improved therapeutic activity:toxic index ratio and a lower amount of triptolide as compared to previous preparations is disclosed. The LD.sub.50 in mice of the T. wilfordii preparation is greater than about 860 mg/kg, the therapeutic activity:toxic index ratio is greater than about 2.6.times.10.sup.-3, and the amount of triptolide is less than about 1.3 .mu.g/mg. The preparation is useful for immunosuppression, in particular, the suppression of primary antibody response and suppression of autoimmune disease and for the treatment of rheumatoid arthritis.Type: GrantFiled: December 17, 1993Date of Patent: December 3, 1996Assignee: Board of Regents The University of Texas SystemInventors: Peter E. Lipsky, Xue L. Tao, Jian Cai
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Patent number: 5578583Abstract: Microemulsions, similar in chemical composition to the lipid portion of low density lipoprotein (LDL), but not containing the protein portion, can be used as vehicles for the delivery of chemotherapeutic or diagnostic agents to neoplastic cells, while avoiding normal cells. When these artificial microemulsion particles are injected in the bloodstream or incubated with plasma, they incorporate plasma apolipoproteins on to their surface. The microemulsions can then be incorporated into cells via receptors for LOL and deliver molecules which are incorporated in the core or at the surface of the microemulsion.Type: GrantFiled: February 13, 1995Date of Patent: November 26, 1996Assignee: Fundac ao E. J. ZerbiniInventor: Raul C. Maranh ao
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Patent number: 5578313Abstract: A method for treating neoplasia using sulfur-containing derivatives of carboxy-amino-amides, comprising vitaletheine and vitalethine and related compounds, is provided.Type: GrantFiled: October 4, 1994Date of Patent: November 26, 1996Assignee: The University of New MexicoInventors: Galen D. Knight, Terence J. Scallen