Chalcogen Bonded Directly To The Hetero Ring Patents (Class 514/473)
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Publication number: 20080146660Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.Type: ApplicationFiled: February 13, 2008Publication date: June 19, 2008Applicants: The University of North Carolina at Chapel Hill, The University of Rochester Medical Center, Androscience CorporationInventors: Kuo-Hsiung Lee, Li Lin, Charles C-Y Shih, Ching-Yuan Su, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang
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Publication number: 20080125484Abstract: Natural and synthetic compounds having a lactone structure methods for using and making the compounds have been disclosed. The compounds are useful as anti-bacterial, anti-fungal and anti-inflammatory agents, and for treating proliferation disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. The compounds are also effective for treatment or prevention of inflammatory diseases such as atherosclerosis, lung fibrosis, systemic lupus erythematosus, pancreatitis, sarcoidosis, glomerulitis, and organ transplant rejection. They are also effective for treatment or prevention of bacterial and fungal infections, including treatment of peptic ulcers, gastritis, dyspepsia and gastric cancer, gingivitis and periodontitis.Type: ApplicationFiled: November 29, 2007Publication date: May 29, 2008Inventor: David Terrero
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Publication number: 20080119548Abstract: Obesity is a worldwide health issue, affecting children and adults in developed and developing countries. Obesity is a disorder of both energy metabolism and appetite regulation, and may be understood as a dysfunction of energy balance. Applicants have found a means for regulating food intake by a subject by administering a compound to the subject which affects neuronal energy balance. Applicants have found a means for regulating food intake by a subject administering a compound to the subject which targets the activity of AMPK, in particular inhibiting activation, in particular hypothalamic. Applicants have also found a method of inducing weight loss in a subject by decreasing the subjects appetite by administering a compound to the subject which increases the subject's neuronal energy balance.Type: ApplicationFiled: March 18, 2005Publication date: May 22, 2008Inventors: Gabrielle V. Ronnett, Frankcis P. Kuhajda, Jagan N. Thupari, Leslie E. Landree, Timothy H. Moran, Eun-Kyoung Kim
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Publication number: 20080118591Abstract: The invention relates to bactericidal formulations that come into contact with human body, particularly wash formulations including liquid soaps, comprising perfume ingredients active against gram-negative bacteria. Such compositions contact the target site, for example the skin surface, only for a short time, usually not longer than 30 seconds. Therefore the antibacterial action has to be of the bactericidal type and rapid. Furthermore, the bactericidal activity has to be sufficiently high to ensure an effect even when applied to wet substrates that will dilute the bactericidal formulation.Type: ApplicationFiled: November 15, 2005Publication date: May 22, 2008Inventor: Andreas Natsch
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Patent number: 7375133Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The analog or derivative is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In some embodiments, the invention may include a pharmaceutical composition including a carotenoid analog or derivative. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds.Type: GrantFiled: March 4, 2004Date of Patent: May 20, 2008Assignee: Cardax Pharmaceuticals, Inc.Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Publication number: 20080113923Abstract: A cubic liquid crystal composition comprising at least one amphiphilic compound having the following general formula (1) and having an IV/OV value of 0.65 to 0.95, and water or an aqueous medium: wherein R represents a hydrophilic group; X and Y each independently represent a hydrogen atom or together form an oxygen atom; n is an integer of 0 to 4; and m is an integer of 0 to 3.Type: ApplicationFiled: October 19, 2005Publication date: May 15, 2008Applicants: NATIONAL INSTITUTE OF ADVANCED INDUSTRIAL SCIENCE, KURARAY CO., LTD., CYTOPATHFINDER, INC.Inventors: Masakatsu Hatoh, Yoshiji Fujita, Toshitaka Ota, Masahisa Tanomura, Manzo Shiono
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Publication number: 20080103196Abstract: The present invention relates to novel diterpene compounds isolated from the fruiting body of Antrodia camphorata, especially to the new compounds of following structural formula: and pharmaceutically acceptable salt, solvate, hydrate or biologically active equivalent thereof. The present invention also relates to a pharmaceutical composition containing at least one of the novel diterpene compounds, and a use of the diterpene compound as a neuroprotective agent.Type: ApplicationFiled: October 25, 2006Publication date: May 1, 2008Inventors: Min-Nan Lai, Yueh-Hsiung Kuo, Young-Ji Shiao
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Publication number: 20080103191Abstract: Pharmaceutical composition comprising one or more entacapone derivatives and one or more pharmaceutically acceptable carriers, a process for producing the pharmaceutical composition, specific entacapone derivatives, a process for the preparation of entacapone derivatives, and the use of the entacapone derivatives for the preparation of a medicament.Type: ApplicationFiled: June 14, 2007Publication date: May 1, 2008Inventors: Klaus Hansen, Robert Kraemer, Thomas Lauterbach, Dirk Schmidt, Fritz Paar, Petra Pfeiffer, Detlef Geffken, Wolfgang Thimann, Katharina Wehner
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Patent number: 7345091Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The analog or derivative is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. In some embodiments, the invention may include a chemical compound including an at least partially water soluble carotenoid analog or derivative. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include a cyclic ring including at least one substituent. The substituent may be coupled to the cyclic ring with an ether functionality.Type: GrantFiled: March 4, 2004Date of Patent: March 18, 2008Assignee: Cardax Pharmaceuticals, Inc.Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Patent number: 7323495Abstract: Natural and synthetic compounds having a lactone structure methods for using and making the compounds have been disclosed. The compounds are useful as anti-bacterial, anti-fungal and anti-inflammatory agents, and for treating proliferation disorders such as melanoma, leukemia, breast cancer, lung cancer, ovarian cancer, colon cancer, esophagus cancer, liver cancer, and lymphatic cancer. The compounds are also effective for treatment or prevention of inflammatory diseases such as artherosclerosis, lung fibrosis, systemic lupus erythematosus, pancreatitis, sarcoidosis, glomerulitis, and organ transplant rejection. They are also effective for treatment or prevention of bacterial and fungal infections, including treatment of peptic ulcers, gastritis, dyspepsia and gastric cancer, gingivitis and periodontitis.Type: GrantFiled: November 5, 2003Date of Patent: January 29, 2008Assignee: Magnachem International Laboratories, Inc.Inventor: David Terrero
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Patent number: 7320997Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The analog or derivative is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. In some embodiments, the invention may include a pharmaceutical composition including a carotenoid analog or derivative. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include a cyclic ring including at least one substituent. The substituent may be coupled to the cyclic ring with an ester functionality.Type: GrantFiled: March 4, 2004Date of Patent: January 22, 2008Assignee: Cardax Pharmaceuticals, Inc.Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Patent number: 7317008Abstract: A method of treating ischemic reperfusion injury in a subject. The method may include administering to the subject an effective amount of a pharmaceutically acceptable formulation. The pharmaceutically acceptable formulation may include a synthetic analog or derivative of a carotenoid. The subject may be administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include a cyclic ring including at least one substituent. In some embodiments, a cyclic ring of a carotenoid analog or derivative may include at least one substituent. The substituent may be coupled to the cyclic ring with an ester functionality.Type: GrantFiled: March 4, 2004Date of Patent: January 8, 2008Assignee: Cardax Pharmaceuticals, Inc.Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Patent number: 7300948Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.Type: GrantFiled: September 29, 2005Date of Patent: November 27, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Bonneau, Patrick Deroy, Alexandre Gagnon, Jeffrey O′Meara, Bruno Simoneau, Christiane Yoakim
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Publication number: 20070259948Abstract: The present invention relates to compounds of formula (1), its solvates and pharmaceutically acceptable salts having antifungal activity and its pharmaceutical composition comprising an effective amount of compound of formula (1) wherein R is substituted alkyl, alkenyl, aryl, heteroaryl, 2-thienyl, 3-thienyl, halothienyl, haloalkyl, halophenyl, or pyrrolyl; and R1 and R2, each independent of the other, are hydrogen, halogen, or alkoxy. The invention also relates to a process for the preparation of said compounds by contacting the intermediate alcohol, prepared from 1,2-O-isopropylideneglyceraldehyde and substituted phenylacetates, with acid chlorides under appropriate conditions to obtain some of the preferred compounds of the invention.Type: ApplicationFiled: August 4, 2006Publication date: November 8, 2007Inventors: Mukund Keshav Gurjar, Radhika Dilip Wakharkar, Hanumant Bapurao Borate, Ramesh Ganesh Kelkar, Andiappan Murugan, Mohan Anand Chandavarkar, Shreerang Vidyadhar Joshi, Sharangi Ravindra Vaiude
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Patent number: 7285571Abstract: The present invention relate to a novel synergistic composition of lignans exhibiting anticancer activities for breast, cervix, neuroblastoma, colon, liver, lung, mouth, ovary and prostate cancer obtained from the plant extract of Cedrus deodra, said composition comprising of (?)-Matairesinol in the range of 9 to 13% by weight, (?)-Wikstromol in the range of 75 to 79% by weight, Dibenzylbutyrolactol in the range of 7 to 11% by weight, and Unidentified material in the range of 2.6 to 3% by weight; further, the synergistic composition of lignan is used in combination with pharmaceutically acceptable carriers for inhibiting growth of various human cancer cell lines selected from breast, cervix, neuroblastoma, colon, liver, lung, mouth, ovary and prostate tissues.Type: GrantFiled: June 17, 2003Date of Patent: October 23, 2007Assignee: Council of Scientific and Industrial ResearchInventors: Janaswamy Madhusudana Rao, Pullela Venkata Srinivas, Jhillu Singh Yadav, Kondapuram Vijaya Raghavan, Ajit Kumar Saxena, Mutiah Shanmugavel, Himani Kampasi, Gulam Nabi Qazi
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Patent number: 7262219Abstract: Disclosed are formulations of gamma-hydroxybutyrate in an aqueous medium that are resistant to microbial growth. Also disclosed are formulations of gamma-hydroxybutyrate that are also resistant to the conversion into GBL. Disclosed are methods to treat sleep disorders, including narcolepsy, with these stable formulations of GHB. The present invention also provides methods to treat alcohol and opiate withdrawal, reduced levels of growth hormone, increased intracranial pressure, and physical pain in a patient.Type: GrantFiled: May 7, 2004Date of Patent: August 28, 2007Assignee: Orphan Medical, Inc.Inventors: Harry Cook, Martha Hamilton, Douglas Danielson, Colette Goderstad, Dayton Reardan
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Patent number: 7230013Abstract: Compositions comprising a taxane having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: February 28, 2005Date of Patent: June 12, 2007Assignee: Florida State University Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 7223792Abstract: Acetogenins isolated from Annona muricata of the family Annonaceae are described. The substantially pure compounds of the invention exhibit to human tumor cell lines as well as selective cytotoxicity for various human tumor cell lines.Type: GrantFiled: December 7, 2001Date of Patent: May 29, 2007Assignees: Advpharma Inc.Inventor: Yang-Chang Wu
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Patent number: 7205289Abstract: The invention relates to novel active compound combinations of certain cyclic ketoenols and certain insecticidally active compounds that together have very good insecticidal and acaricidal properties.Type: GrantFiled: January 27, 2004Date of Patent: April 17, 2007Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Christoph Erdelen, Thomas Bretschneider
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Patent number: 7189753Abstract: A method of preventing the headache phase of migraine in a human comprises administration of a 5HT1 receptor agonist or administration of an over-the-counter or nonprescription drug to said human exhibiting prodrome symptoms of migraine. Suitably, the method comprises administration of a migraine headache phase-preventing effective amount of the 5HT1 agonist or over-the-counter or nonprescription drug. There is disclosed a preemptive prophylaxis migraine method using the following cognitive tests: Simple Reaction Time; Running Memory Continuous Performance Task; Matching to Sample; Mathematical Processing Task; and interpreting the results as a percent of baseline indicator of need for prophylaxis.Type: GrantFiled: May 22, 2000Date of Patent: March 13, 2007Inventors: Roger K. Cady, Donna Lee Gutterman, Stephen Venson O'Quinn
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Patent number: 7183316Abstract: Human papillomavirus (HPV) protein expression is downregulated in patients infected with HPV by administration of PPAR? ligand, selective inhibitor of cyclooxygenase-2 (COX-2), diaryl heterocycle, inhibitor of HPV protein from a natural source and/or certain non-steroidal anti-inflammatory drugs.Type: GrantFiled: March 14, 2002Date of Patent: February 27, 2007Assignee: Cornell Research Foundation, Inc.Inventors: Andrew J. Dannenberg, Kotha Subbaramaiah
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Patent number: 7173055Abstract: Novel pyraole derivatives of formula (I), wherein: X is oxygen or sufu, R1 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R2 is C1–C3haloalkyl; and R3 is halogen. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.Type: GrantFiled: November 11, 2000Date of Patent: February 6, 2007Assignee: Syngenta Crop Protection, Inc.Inventor: Harald Walter
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Patent number: 7132449Abstract: Compounds of general formula (I): wherein R1, R2, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.Type: GrantFiled: January 7, 2002Date of Patent: November 7, 2006Assignee: Amura Therapeutics LimitedInventor: Martin Quibell
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Patent number: 7132448Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative or a chloronicotinyl insecticide and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: August 3, 2004Date of Patent: November 7, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Albert Ahn, Richard Fisher, Christine M. Monro, Pierre R. Joseph
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Patent number: 7115605Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 5, 2004Date of Patent: October 3, 2006Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Patent number: 7078434Abstract: The present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated Ginkgolide B (GKB), a component of the extract of Ginkgo biloba leaves in a method for decreasing the expression of peripheral-type benzodiazepine receptor (PBR) in cells of a patient in need thereof. Further, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method for decreasing the proliferation of cancer cells in a patient. More particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method of decreasing cancer cell proliferation in a patient wherein the cancer cell is human breast cancer cell.Type: GrantFiled: August 11, 2000Date of Patent: July 18, 2006Assignees: Societe de Conseils de Recherches et d'Applications Scientifiques SAS, Georgetown UniversityInventors: Katy Drieu, Vassilios Papadopoulos
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Patent number: 7078404Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of formula I, in which the radicals have the given meanings, and to their physiologically tolerated salts and processes for preparing them. The compounds are, for example, suitable for use as antidiabetics.Type: GrantFiled: April 10, 2003Date of Patent: July 18, 2006Assignee: Sanofi-Aventis Deutschland GmbHInventors: Elisabeth Defossa, Dieter Kadereit, Karl Schoenafinger, Thomas Klabunde, Hans-Joerg Burger, Andreas Herling, Karl-Ulrich Wendt, Erich Von Roedern, Alfons Enhsen
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Patent number: 7078435Abstract: Autoinducer compounds which enhance gene expression in a wide variety of microorganisms, therapeutic compositions and therapeutic methods wherein gene expression within microorganisms is regulated are disclosed.Type: GrantFiled: October 10, 2003Date of Patent: July 18, 2006Assignee: Montana State UniversityInventor: Tom Livinghouse
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Patent number: 7064220Abstract: The present invention relates to the side chain functionalization of fimbrolides (halogenated 3-alkyl-5-methylene-2(5H)-furanones) and their synthetic analogues, that yields fimbrolides substituted with a halogen, an oxygen or a nitrogen functionality in the alkyl chain, especially fimbrolide alcohols, carboxylate and sulfinate and sulfonate esters, ethers, aldehydes, ketones, acids, amides, nitro derivatives, hydrophobic, hydrophilic and fluorophilic alkyl derivatives and a polymers.Type: GrantFiled: April 16, 1999Date of Patent: June 20, 2006Assignee: Unisearch Limited, A.C.N.Inventors: Roger Read, Naresh Kumar
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Patent number: 7056946Abstract: Taxanes having a carbonate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: November 24, 2003Date of Patent: June 6, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 7053118Abstract: The subject invention provides novel compositions of biologically active compounds which can advantageously be used for inhibiting pathological cellular proliferation. The compounds of the subject invention have utility for use in the treatment of cancer, including tumors.Type: GrantFiled: March 6, 2003Date of Patent: May 30, 2006Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Sarath P. Gunasekera, Ross E. Longley, Amy E. Wright, John K. Reed
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Patent number: 7037937Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).Type: GrantFiled: May 11, 2004Date of Patent: May 2, 2006Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Shyi-Tai M. Jan
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Patent number: 7026353Abstract: A method of inhibiting the growth of a Gram positive bacterium, the method comprising treating the bacterium with an effective amount of one or more furanones having the Formula as set out in the Figure, wherein the effective amount of the one or more furanones does not substantially adversely effect the survival of an animal cell when exposed to the one or more furanonesType: GrantFiled: May 9, 2003Date of Patent: April 11, 2006Assignee: Unisearch Limited, A.C.N.Inventors: Staffan Kjelleberg, Peter David Steinberg, Carola Holmstrom, Arthur Back
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Patent number: 7008666Abstract: The invention relates to a method of inhibiting myeloperoxidase activity in neutrophils in an individual by administering to the individual an effective amount of a lignan, where said lignan is enterolactone. The invention is further directed to a method inhibiting myeloperoxidase activity or oxidative burst of macrophages in an individual by administering to the individual an effective amount of a lignan where said lignan is enterolactone or hydroxymatairesinol or a mixture. Finally, the invention is directed to a method of inhibiting oxidative burst or myeloperoxidase activity in neutrophils in an individual by administering to the individual an effective amount of a lignan which is hydroxymatairesinol.Type: GrantFiled: November 26, 2001Date of Patent: March 7, 2006Assignee: Hormos Nutraceutical Oy Ltd.Inventors: Markku Ahotupa, John Eriksson, Lauri Kangas, Mikko Unkila, Janne Komi, Merja Perälä, Helena Korte
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Patent number: 6992104Abstract: Taxanes having a carbonate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: December 22, 2003Date of Patent: January 31, 2006Assignee: FSU Research Foundation, Inc.Inventor: Robert A. Holton
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Patent number: 6984662Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative and an insect growth regulator (IGR) in a solvent containing a quaternary ammonium salt to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: November 3, 2003Date of Patent: January 10, 2006Assignee: The Hartz Mountain CorporationInventors: Ian W. Cottrell, Christine M. Monro, Pierre R. Joseph, Albert Ahn, Richard Fisher
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Patent number: 6969731Abstract: HIV protease inhibitors are among the most powerful drugs in suppressing HIV in human patients. However, HIV developed resistance to all protease inhibitor drugs so far marketed or used in clinical trials. HIV generates resistance by mutating its protease. The strains of HIV containing mutant proteases less vulnerable to inhibitor drug are able to replicate better and maintain the infection. No effective principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr). A new inhibitor has been developed based on a new concept for designing resistance invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs. The new concept is, therefore, generally applicable for the design of other resistance invulnerable HIVPr inhibitor drugs.Type: GrantFiled: February 18, 2000Date of Patent: November 29, 2005Assignees: The University of Illinois, Board of Trustees, The Oklahoma Medical Research FoundationInventors: Jordan J. N. Tang, Arun K. Ghosh
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Patent number: 6964981Abstract: The present invention relates compounds that are NK-1 antagonists and that are of use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.Type: GrantFiled: September 10, 2001Date of Patent: November 15, 2005Assignee: Merck Sharp & Dohme Ltd.Inventors: Brian John Williams, Christopher John Swain, Simon Neil Owen
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Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
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Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6906051Abstract: The present invention relates to a class of compounds represented by the Formula I: or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?V?3 and/or the ?V?5 integrin.Type: GrantFiled: November 19, 2003Date of Patent: June 14, 2005Assignee: Pharmacia CorporationInventors: Peter Ruminiski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
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Patent number: 6906088Abstract: Taxanes having a carbamoyloxy substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: July 11, 2003Date of Patent: June 14, 2005Assignee: FSU Research Foundation, Inc.Inventors: Robert A. Holton, Weishuo Fang
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Patent number: 6900242Abstract: Compounds of Formula Ia and Ic having a lactone structure and an methylene group at the alpha-position of the lactone structure and methods for using and making the compounds have been disclosed. The lactone compounds can be reacted with an neucleaphilic agent to open the lactone ring to a compound of Formula Ib. The lactone of Formula Ia and its functional derivatives have been isolated from Securidaca virgata. These compounds are referred to as LMSV-6 or Securolide™. The purified compounds have demonstrated activity in assays for anti-bacterial and anti-fungal activities, and for treating proliferation disorders such as cancer. Based on the in vitro assays, the lactones are useful for treating proliferation disorders including, for example, breast cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, esophageal cancer, and leukemia.Type: GrantFiled: June 12, 2002Date of Patent: May 31, 2005Assignee: Magnachem International Laboratories, Inc.Inventor: David Terrero
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Patent number: 6894074Abstract: The invention relates to insecticidal mixtures comprising compounds of the formula (I) in which X?, Y?, Z?, n, G?, A? and B? are as defined above and agonists and/or antagonists of nicotinic acetylcholine receptors, for protecting plants against attack by pests.Type: GrantFiled: September 29, 2003Date of Patent: May 17, 2005Assignee: Bayer AktiengesellschaftInventors: Thomas Bretschneider, Reiner Fischer, Christoph Erdelen, Ernst Brück
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Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6878742Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof.Type: GrantFiled: June 5, 2003Date of Patent: April 12, 2005Assignees: Wyeth, ArQule, Inc.Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
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Patent number: 6878744Abstract: Vitamin C compositions comprise a Vitamin C compound, preferably a mineral ascorbate, and at least one compound of the group of 4-hydroxy-5-methyl-3(2H)-furanone and 3-hydroxy kojic acid.Type: GrantFiled: June 26, 2001Date of Patent: April 12, 2005Assignee: Oxycal Laboratories, Inc.Inventor: John C. Hegenauer
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Patent number: 6875784Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: October 2, 2003Date of Patent: April 5, 2005Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail Fedor Gordeev, Adam Renslo, Dinesh Vinoobhai Patel
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Patent number: 6864278Abstract: Sordarin derivatives prepared from C-11-hydroxysordarin are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.Type: GrantFiled: July 12, 2002Date of Patent: March 8, 2005Assignee: Merck & Co., Inc.Inventors: James M. Balkovec, Bruno Tse
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Patent number: RE39530Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.Type: GrantFiled: September 11, 2003Date of Patent: March 27, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann