Polycyclo Ring System Patents (Class 514/510)
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Patent number: 7132403Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.Type: GrantFiled: January 20, 2004Date of Patent: November 7, 2006Assignees: Board of Trustees of Michigan State University, Regents of the University of CaliforniaInventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
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Patent number: 7119124Abstract: The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance (having low aqueous solubility and a substantial binding affinity to plasma proteins) and a plasma protein fraction in controlled aggregation state, whereby the said active substance and the said protein fraction are bound to each other by way of non-covalent bonds. It also covers processes for the preparation of the product and pharmaceutical formulation by dissolving the water-insoluble active substance in a water-miscible, pharmaceutically acceptable solvent, combining said solution with the aqueous solution of a plasma protein fraction in controlled aggregation state whereby a true solution is obtained containing the said active substance and the said protein fraction bound together by way of non-covalent bonds.Type: GrantFiled: January 21, 2003Date of Patent: October 10, 2006Assignee: Human Rt.Inventors: Lajos Hegedus, Krisztina Krempels, Krisztina Paal, Gabor Petho
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Patent number: 7109206Abstract: Disclosed are methods and compositions for reducing coronary artery stenosis, restoring blood flow to infarcted myocardium, improving myocardial perfusion, reducing heart attacks or other adverse cardiovascular events, or treating symptoms of inadequate myocardial function in a mammal involving administering to the mammal (a) a compound that includes eicosapentaeneoic acid or docosahexaeneoic acid and (b) a cholesterol-lowering therapeutic, combined with dietary restrictions (resulting in aggressive loading of marine lipids), whereby a serum LDL concentration of less than 75 mg/dl (and preferably less than 55 mg/dl) is achieved. One particular method involves administering to the mammal a combination that includes (a) a compound that includes an eicosapentaeneoic or docosahexaeneoic acid (for example, a marine lipid) and (b) a cholesterol synthesis or transfer inhibitor, and which may also optionally include aspirin and/or niacin.Type: GrantFiled: December 12, 2000Date of Patent: September 19, 2006Assignee: Heart Care PartnersInventors: Brian Seed, John C. Seed
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Patent number: 7101909Abstract: Novel multibinding compounds are disclosed. The compounds of this invention comprise 2–10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Ca++ channel, thereby modulating the biological activities thereof.Type: GrantFiled: June 25, 2004Date of Patent: September 5, 2006Assignee: Theravance, Inc.Inventors: Yu-Hua Ji, Maya Natarajan, John H. Griffin, Thomas E. Jenkins
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Patent number: 7081465Abstract: This invention relates to novel {overscore (?)}-substituted-naphthyloxy-amino alkanes, their preparation and use as antihyperglycemic agents and for the treatment and prevention of cardiovascular disorders (CVS) such as lipid lowering effects.Type: GrantFiled: October 27, 2003Date of Patent: July 25, 2006Assignee: Council of Scientific and Industrial ResearchInventors: Devdutt Chaturvedi, Atul Kumar, Reema Rastogi, Arivend Srivastava, Priti Tewari, Rehan Ahmad, Ramaesh Chander, Anju Puri, Geetika Bhatia, Farhar Rivizvi, Anil Kumar Rastogi, Suprabhat Ray
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Patent number: 7041701Abstract: The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in therapy. Preferably, the compound may be used for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation and acetylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia).Type: GrantFiled: May 23, 2001Date of Patent: May 9, 2006Assignees: Univerzita Palackeho V Olomouci, UniverzitaInventors: Marian Hajduch, Jan Sarek
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Patent number: 7026355Abstract: The present invention relates to the use of rhein or diacerhein compounds to treat and prevent vascular diseases that cause obstruction of the vascular system such as blood vessel restenosis and atherosclerosis.Type: GrantFiled: April 27, 2004Date of Patent: April 11, 2006Assignee: Transition Therapeutics Inc.Inventors: Tony Cruz, Aleksandra Pastrak
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Patent number: 7015247Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions, hydroxymethylacylfulvene analogs useful as antitumor drugs, and L-sugar illudin analogs useful as antitumor drugs.Type: GrantFiled: August 15, 2002Date of Patent: March 21, 2006Inventor: Alvin Guttag
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Patent number: 6984389Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.Type: GrantFiled: December 16, 2002Date of Patent: January 10, 2006Assignee: University of Connecticut Health CenterInventor: Zihai Li
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Patent number: 6967218Abstract: The present invention relates to formulations comprising a therapeutically effective amount of pravastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to release little or no pravastatin in the stomach but release a therapeutic amount of pravastatin in the small intestine, thereby limiting systemic exposure of the body to pravastatin and maximizing hepatic-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.Type: GrantFiled: January 10, 2003Date of Patent: November 22, 2005Assignee: Biovail Laboratories, Inc.Inventors: Jackie Butler, John Devane, Paul Stark
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Patent number: 6949557Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.Type: GrantFiled: April 29, 2003Date of Patent: September 27, 2005Assignee: Dabur Research FoundationInventors: Asish Kumar Banerjee, Venkatachalam Sesha Giri, Rama Mukherjee, Kamal K. Kapoor, Gautam Desiraju, Manu Jaggi, Anu T. Singh, Sankar Kumar Dutta, Kalapatapu V. V. M. Sairam
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Patent number: 6933291Abstract: The invention provides a composition and a method for lowering blood serum cholesterol levels or for preventing elevated blood serum cholesterol levels, as well as suitable composition comprising (a) one or more phytosterols and/orphytostanols or a mixture thereof capable of reducing cholesterol absorption in the intestine, (b) a composition capable of inhibiting cholesterol biosynthesis, and (c) a composition capable of increasing cholesterol metabolism, wherein at least one of compositions b. and c. is preferably derived from plants.Type: GrantFiled: December 1, 2000Date of Patent: August 23, 2005Assignee: N.V. NutriciaInventors: Chen Qi, Hendricus Bartholomeus Andreas De Bont, Luutsche Van Der Zee, Mirian Lansink, Klaske Van Norren
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Patent number: 6916837Abstract: Amidino derivatives represented by the following general formula (I): {where X is a group represented by R1SO2NR2— (wherein R1 represents optionally substituted C6-14 aryl, etc. and R2 represents hydrogen atom, etc.), etc., Ar1 represents 2,6-naphthylene, etc., R3 represents hydrogen atom, etc. and Y represents carboxyphenyl, etc.} and their pharmacologically acceptable salts or solvates.Type: GrantFiled: November 14, 2002Date of Patent: July 12, 2005Assignee: Eisai Co., Ltd.Inventors: Takashi Satoh, Yasushi Okamoto, Osamu Asano, Nobuhisa Watanabe, Tadashi Nagakura, Takao Saeki, Atsushi Inoue, Masahiro Sakurai
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Patent number: 6903076Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.Type: GrantFiled: November 26, 2003Date of Patent: June 7, 2005Assignees: Board of Trustees of Michigan State University, The Regents of the University of CaliforniaInventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
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Patent number: 6897237Abstract: A compound of the formula (I): wherein R1 is hydroxy and the like; R2 is optionally substituted lower alkyl and the like; R3 is hydrogen atom and the like; R4 is optionally substituted arylene and the like; R5 is —C?C— and the like; R6 is optionally substituted naphtyl and the like its optically active substance, its prodrug, their pharmaceutically acceptable salt, or solvate thereof.Type: GrantFiled: April 23, 2001Date of Patent: May 24, 2005Assignee: Shionogi & Co. Ltd.Inventors: Yozo Hori, Fumihiko Watanabe, Hiroshige Tsuzuki, Shingo Furue, Yoshinori Tamura
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Patent number: 6890946Abstract: The invention provides a method comprising the use of parthenolide, including its analogs, to treat cancer or conditions characterized by abnormal angiogenesis.Type: GrantFiled: June 21, 2002Date of Patent: May 10, 2005Assignee: Indiana University Research and Technology CorporationInventors: Harikrishna Nakshatri, Christopher J. Sweeney
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Patent number: 6884817Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.Type: GrantFiled: May 17, 2002Date of Patent: April 26, 2005Assignee: PG-TXL Company, L.P.Inventors: Chun Li, Sidney Wallace, Dong-Fang Yu, David J. Yang
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Patent number: 6881857Abstract: Disclosed herein are novel tricyclic diterpene compounds. These compounds, including their prodrug esters and acid-addition salts, are useful as Interleukin-1 and Tumor Necrosis Factor-? modulators, and thus are useful in the treatment of various diseases. Also disclosed are pharmaceutical compositions comprising a therapeutically effective amount of the novel compounds that are useful as anti-inflammatory analgesics, in treating immune disorders, as anti-cancer and anti-tumor agents, and in the treatment of cardiovascular disease, skin redness, and viral infection. Completely synthetic and semi-synthetic methods of making the compounds and their analogs are also disclosed, as are methods of using these synthetic and semi-synthetic compounds in the treatment of the above-listed disease states.Type: GrantFiled: February 4, 2002Date of Patent: April 19, 2005Assignees: Nereus Pharmaceuticals, Inc., University of CaliforniaInventors: Michael Palladino, Emmanuel A. Theodorakis
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Patent number: 6875746Abstract: Anthraquinones are described which have anticancer or antitumor activity and which are useful for inhibiting cancer cells and cells comprising tumors in vitro or in vivo. Preferably, the anthraquinones have the chemical formula: wherein R1 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R2 is a group containing 1-12 carbons selected from the group consisting of alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate and combinations thereof; and R3 is a group containing 1 to 12 carbons selected from the group consisting of methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, and combinations thereof.Type: GrantFiled: January 31, 2003Date of Patent: April 5, 2005Assignee: Board of Trustees of Michigan State UniversityInventors: Muraleedharan G. Nair, Robert H. Cichewicz, Navindra P. Seeram, Yanjun Zhang
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Patent number: 6872713Abstract: Saponins of formula (I), a stereoisomeric form thereof or a pharmaceutically acceptable addition salt thereof, wherein R1 to R12 have the meaning given in the description, can be isolated from plants of the family Myrsinaceae and used, to decrease the infectiousness of and reduce the mortality associated with protozoan parasites of the genus Leishmania which are responsible for a group of conditions known as leishmaniases.Type: GrantFiled: December 15, 1999Date of Patent: March 29, 2005Assignee: Janssen Pharmaceutica N.V.Inventors: Louis Jules Roger Marie Maes, Nils Albert Gilbert Germonprez, Luc Emiel Mathilde Van Puyvelde, Norbert G. M. De Kimpe, Tran Ngoc Ninh
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Patent number: 6838443Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.Type: GrantFiled: November 26, 2003Date of Patent: January 4, 2005Assignees: Board of Trustees of Michigan State University, The Regents of the University of California, The United States of America as represented by the Department of Veterans AffairsInventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
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Patent number: 6826033Abstract: The present invention relates to a compound formula (I) wherein X1 is bond or —O—CH2—, (II) or (III) R1 is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.Type: GrantFiled: March 21, 2003Date of Patent: November 30, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Minoru Sakurai, Kenichi Washizuka, Hitoshi Hamashima, Yasuyo Tomishima, Masashi Imanishi, Yutaka Nakajima, Hiroaki Ohtake, Satoru Kuroda, Masayoshi Murata, Hiroshi Kayakiri, Naoaki Fujii, Kiyoshi Taniguchi
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Patent number: 6822000Abstract: Bioerodible poly(orthoesters) useful as orthopedic implants or vehicles for the sustained delivery of pharmaceutical, cosmetic and agricultural agents contain hydrogen bonding groups and &agr;-hydroxy acid-containing groups.Type: GrantFiled: December 24, 2002Date of Patent: November 23, 2004Assignee: AP Pharma, Inc.Inventors: Steven Y. Ng, Jorge Heller
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Patent number: 6800615Abstract: Anthraquinones are described which are antihelminthic and in particular, are useful in compositions for inhibiting Schistosoma sp. in vitro or in vivo. The preferred anthraquinones have the formula: wherein R1, R2, R3, and R4 are each hydrogen, hydroxy, halogen, alkyl, substituted alkyl, alkene, substituted alkene, alkyne, aryl, substituted aryl, cyclic, substituted cyclic, acid group, carbohydrate, or combination thereof, R is a group containing 1 to 12 carbons such as methyl, alkyl, substituted alkyl, aldehyde, hydroxy, hydroxymethyl, acid group, carbohydrate, or combination thereof, and the halogen is I, F, Br, or Cl.Type: GrantFiled: December 12, 2002Date of Patent: October 5, 2004Assignees: Board of Trustees of Michigan State University, The Regent of the University of California, The United States of America as represented by the Department of Veterans AffairsInventors: Robert H. Cichewicz, Muraleedharan G. Nair, James H. McKerrow
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Patent number: 6797727Abstract: The present invention relates to the use of rhein or diacerhein compounds to treat and prevent vascular diseases that cause obstruction of the vascular system such as blood vessel restenosis and atherosclerosis.Type: GrantFiled: July 15, 2002Date of Patent: September 28, 2004Assignee: Transition Therapeutics Inc.Inventors: Tony Cruz, Aleksandra Pastrak
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Patent number: 6794409Abstract: The present invention discloses the use of ER&bgr;-selective ligands for production of medicaments for regulating fertility without additional use of a progestin. ER&bgr;-agonists are used for treatment of infertility and ER&bgr;-antagonists for contraception.Type: GrantFiled: February 27, 2002Date of Patent: September 21, 2004Assignee: Schering AGInventors: Christa Hegele-Hartung, Karl-Heinrich Fritzemeier, Hiroshi Yamanouchi, Olaf Peters, Dirk Kosemund, Gerd Mueller, Ingo Tornus, Gerd Schubert, Sven Ring
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Patent number: 6790864Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: October 22, 2002Date of Patent: September 14, 2004Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6770676Abstract: The present invention relates to 2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic acid derivatives represented by the formula: the pharmaceutically acceptable salts thereof, or the hydrates thereof. The compounds of the present invention are useful as a medicament, and in particular, are useful as modulators acting on group 2 metabotropic glutamate receptors, having effects for treating and/or preventing psychiatric disorders such as schizophrenia, anxiety and its associated diseases, depression, bipolar disorder, and epilepsy; and/or neurological diseases such as drug dependence, cognitive disorders, Alzheimer's disease, Huntington's chorea, Parkinson's disease, dyskinesia associated with muscular stiffness, cerebral ischemia, cerebral failure, myelopathy, and head trauma.Type: GrantFiled: December 6, 2002Date of Patent: August 3, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Toshihito Kumagai, Kosuke Kanuma, Kazunari Sakagami
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Patent number: 6767920Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration, a wavy line represents the &agr; configuration or the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are independently selected from the group consisting of O, S and CH2; provided that at least one of A or B is S; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents mayType: GrantFiled: January 16, 2003Date of Patent: July 27, 2004Assignee: Allergan, Inc.Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
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Publication number: 20040122090Abstract: The present invention relates to compositions and methods for treating a human patient afflicted with a neuropsychiatric disorder. Specifically, the invention provides for compositions and methods of modulating or antagonizing the activity of neuronal NMDA receptors, wherein such antagonistic activity is capable of modulating the glutamate induced excitatory response of the neurons, thereby inhibiting an excitotoxic effect, promoting a neurotrophic effect, and thereby providing a therapeutic effect that treats the neuropsychiatric disorder.Type: ApplicationFiled: July 7, 2003Publication date: June 24, 2004Inventor: Stuart A. Lipton
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Patent number: 6743826Abstract: The invention is related to water-soluble products and pharmaceutical formulations in solid or liquid form mainly for parenteral use. They consist of or comprise a therapeutically active substance (having low aqueous solubility and a substantial binding affinity to plasma proteins) and a plasma protein fraction in controlled aggregation state, whereby the said active substance and the said protein fraction are bound to each other by way of non-covalent bonds. It also covers processes for the preparation of the product and pharmaceutical formulation by dissolving the water-insoluble active substance in a water-miscible; pharmaceutically acceptable solvent, combining said solution with the aqueous solution of a plasma protein fraction in controlled aggregation state whereby a true solution is obtained containing the said active substance and the said protein fraction bound together by way of non-covalent bonds.Type: GrantFiled: April 27, 1999Date of Patent: June 1, 2004Assignee: Human RTInventors: Lajos Hegedus, Krisztina Krempels, Krisztina Paal, Gabor Petho
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Patent number: 6730699Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.Type: GrantFiled: November 20, 2002Date of Patent: May 4, 2004Assignee: PG-TXL Company, L.P.Inventors: Chun Li, Sidney Wallace, Dong-Fang Yu, David Yang
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Patent number: 6727279Abstract: The present invention relates to novel arylsulphonamides and analogues, to processes for their preparation and to their use for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy, craniocerebral trauma, pain and spasticity.Type: GrantFiled: August 21, 2002Date of Patent: April 27, 2004Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Frank Mauler, Jean-Marie-Victor de Vry, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schumacher, Michael-Harold Rock, Ervin Horvàth, Arno Friedl, Klaus-Helmut Mohrs, Siegfried Raddatz, Reinhard Jork
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Patent number: 6710073Abstract: Peripherally administered analogs and derivatives of Brefeldin A are used to enhance learning and reverse memory dysfunction through induced long term potentiation in hippocampal tissues.Type: GrantFiled: December 2, 1996Date of Patent: March 23, 2004Assignee: The Regents of the University of CaliforniaInventors: Katumi Sumikawa, Ken-Ichi Ito, James L. McGaugh
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Publication number: 20040029929Abstract: The present invention provides novel aminoadamantane derivatives, methods of making the derivatives, compositions including the novel aminoadamantane derivatives, and methods for the treatment and prevention of neurological diseases using the derivatives and compositions.Type: ApplicationFiled: August 4, 2003Publication date: February 12, 2004Inventors: Yuqiang Wang, Wenqing Ye, James W. Larrick, Jonathan S. Stamler, Stuart A. Lipton
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Patent number: 6689807Abstract: This invention relates to methods and compositions for the treatment of conditions associated with vascular insufficiency, and to methods and compositions for screening assays to select agents that are useful for this purpose. In particular the invention relates to HMG CoA reductase inhibitors and their use in promoting angiogenesis in vivo and in activating Akt in vascular endothelial cells in vitro and in vivo.Type: GrantFiled: June 8, 2000Date of Patent: February 10, 2004Assignee: Caritas St. Elizabeth's Medical Center of Boston, Inc.Inventor: Kenneth Walsh
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Publication number: 20040024057Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: ApplicationFiled: July 3, 2003Publication date: February 5, 2004Applicant: NitroMed, Inc.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunga, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 6638975Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).Type: GrantFiled: December 4, 2002Date of Patent: October 28, 2003Assignee: University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Pimenova Elena Valentinovna, Elena A. Goun
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Patent number: 6635672Abstract: The present invention relates to a prolactin lowering drug containing at least one bicyclic diterpene of the labdane or clerodane type: wherein R1=H, C1 to C3 alkyl or C1 to C3 acyl.Type: GrantFiled: September 24, 2001Date of Patent: October 21, 2003Assignee: Bionorica AGInventors: Wolfgang Wuttke, Hubertus Jarry, Michael Popp, Volker Christoffel, Barbara Spengler
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Patent number: 6630502Abstract: A method is provided for slowing the progression of atherosclerosis in hypertensive or normotensive patients and reducing or eliminating atherosclerotic lesions in such patients by administering a combination of a cholesterol lowering drug such as pravastatin, and an ACE inhibitor, especially one containing a mercapto moiety, such as captopril or zofenopril.Type: GrantFiled: December 2, 1991Date of Patent: October 7, 2003Assignee: E.R. Squibb & Sons, Inc.Inventors: James L. Bergey, Werner Tschollar, Cary S. Yonce, James C. Kawano
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Patent number: 6624192Abstract: The present invention provides a process for obtaining diacetylrhein, wherein diacetylrhein containing aloe-emodin components is subjected to a liquid—liquid partitioning between a polar organic solvent which is only partly miscible with water and an aqueous phase of pH 6.5 to 7.5 and the diacetylrhein is recovered and optionally recrystallized. The present invention is also concerned with diacetylrhein obtainable by this process and with pharmaceutical compositions containing it.Type: GrantFiled: November 2, 1994Date of Patent: September 23, 2003Assignee: Madaus AGInventors: Alfons Carcasona, Wolf Grimminger, Pentti Hêitala, Klaus Witthohn, Helga Zaeske
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Patent number: 6607712Abstract: An essential oil composition from Coleus forskohlii is used in compositions and methods for the treatment of skin infections and in the prevention and treatment of dental caries.Type: GrantFiled: February 20, 2002Date of Patent: August 19, 2003Assignee: Sabinsa CorporationInventors: Muhammed Majeed, Subbalakshmi Prakash
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Patent number: 6596764Abstract: The present invention provides a process for treating arthritis utilizing substantially pure diacetylrhein having an aloe-emodin content of less than 20 ppm.Type: GrantFiled: November 10, 1994Date of Patent: July 22, 2003Assignee: Laboratoire Medidom S.A.Inventors: Alfons Carcasona, Wolf Grimminger, Pentti Hietala, Helga Zaeske, Klaus Witthohn
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Patent number: 6593363Abstract: The present invention relates to diterpene derivatives prepared from the components which are extracted from Acanthopanax Koreanum and represented by Chemical Formula (1).Type: GrantFiled: September 15, 2000Date of Patent: July 15, 2003Assignees: Sae Han Pharm. Co., Ltd.Inventors: Young Ger Suh, Young Hoon Choi, Hye Kyung Lee, Young Ho Kim, Hyoung Sup Park
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Publication number: 20030077303Abstract: The present invention claims and discloses a pharmaceutical composition suitable for oral administration, in form of an emulsion pre-concentrate, comprising (i) a compound of formula (I); (ii) one or more surfactants; (iii) optionally an oil or semi-solid fat; said composition forming an in-situ oil-in-water emulsion upon contact with aqueous media such as gastrointestinal fluids. The composition may optionally also comprise one or more short-chain alcohols. The pharmaceutical composition is useful in the treatment of pain and inflammation.Type: ApplicationFiled: September 5, 2002Publication date: April 24, 2003Inventors: Christina Holmberg, Britta Siekmann
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Patent number: 6548534Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: July 27, 2001Date of Patent: April 15, 2003Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Patent number: 6541515Abstract: Compounds useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines are described. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. The culture Cytospora sp. MF 6608 (ATCC PTA-1691) is also disclosed, as well as processes for making a compound of the present invention employing the culture.Type: GrantFiled: August 9, 2001Date of Patent: April 1, 2003Assignee: Merck & Co., Inc.Inventors: Sheo Bux Singh, Hiranthi Jayasuriya, Ziqiang Guan, Keith C. Silverman, Russell B. Lingham, Anne W. Dombrowski, Daria J. Hazuda, Jon D. Polishook
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Patent number: 6521646Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.Type: GrantFiled: October 15, 2001Date of Patent: February 18, 2003Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
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Patent number: 6506796Abstract: Methods of cosmetically or therapeutically treating diseases or disorders in cell populations whose pathology is linked to an inadequate rate of apoptosis by administering a therapeutically effective amount of 6-3-(1-adamantyl)-4-hydroxyphenyl)-2-naphthanoic acid.Type: GrantFiled: July 25, 2000Date of Patent: January 14, 2003Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Laszlo Fesus, Zsuzsa Szondy, Uwe Reichert
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Patent number: 6479549Abstract: A novel carnosic acid derivative for promoting the synthesis of nerve growth factor (NGF), a composition comprising the carnosic acid derivative as an effective ingredient, as well as, a method of promoting the synthesis of NGF comprising administering an effective amount of the carnosic acid derivative as an effective ingredient to a subject requiring such promotion. The carnosic acid derivative, composition and method according to the present invention can safely and efficiently promote the production of NGF in the living body, without being accompanied by a side effect such as a loss of a quantitative balance of hormones in the living body.Type: GrantFiled: February 28, 2001Date of Patent: November 12, 2002Assignee: Nagase & Company, Ltd.Inventors: Kunio Kosaka, Toshitsugu Miyazaki, Toshio Yokoi