Chalcogen Or Nitrogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 514/380)
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Patent number: 8158825Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: GrantFiled: June 21, 2006Date of Patent: April 17, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20120083447Abstract: Methods of treating hypertension, pain, and resuscitative hemorrhagic shock using an adrenergic agent, like centhaquin, are disclosed. The methods treat mammals, including humans.Type: ApplicationFiled: April 29, 2010Publication date: April 5, 2012Applicant: MIDWESTERN UNIVERSITYInventor: Anil Gulati
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Publication number: 20120070513Abstract: Methods of treating diabetic ketoacidosis are disclosed. The methods utilize an endothelin antagonist to treat diabetic ketoacidosis in mammals, including humans.Type: ApplicationFiled: April 30, 2010Publication date: March 22, 2012Inventor: Anil Gulati
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Publication number: 20120071483Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate cell stress response for treating said disease.Type: ApplicationFiled: October 29, 2010Publication date: March 22, 2012Applicant: PHARNEXTInventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko
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Publication number: 20120064060Abstract: Provided are: a compound represented by formula (I): (wherein ring A and ring D each represent a cyclic group which may have a substituent(s); E and G each represent a bond or a spacer having 1 to 8 atoms in its main chain; L represents a hydrogen atom or a substituent; X represents amino which may have a substituent(s), or a heterocylic group which contains at least one nitrogen atom and which may have a substituent(s); n represents 0 to 3, and when n is 2 or more, a plurality of ring A's may be the same or different from one another); a salt, an N-oxide form, a solvate, or a prodrug thereof; and a medicament which includes those. The compound of formula (I) is capable of binding S1P receptors (in particular, EDG-1 and/or EDG-6), and useful for preventing and/or treating rejection in transplantation, autoimmune diseases, allergic diseases, etc.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Shinji NAKADE
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Publication number: 20120065173Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: September 2, 2011Publication date: March 15, 2012Inventors: Markus Berger, Lena Bergström, Jan Dahmén, Anders Eriksson, Balint Gabos, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Stinabritt Nilsson, Camilla Taflin, Darren McKerrecher, Hartmut Rehwinkel
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Publication number: 20120065063Abstract: The invention relates to 3-aryl-4-(2,6-dimethylbenzylidene)isoxazol-5(4H)-ones, to agrochemically active salts thereof, to the use thereof and to methods and compositions for controlling phytopathogenic harmful fungi and insects in and/or on plants or in and/or on seed of plants, to processes for producing such compositions and treated seed, and to the use thereof for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in animal health, in the protection of materials and in the domestic and hygiene sector. The present invention further relates to a process for preparing isoxazolone derivatives.Type: ApplicationFiled: June 22, 2011Publication date: March 15, 2012Applicant: Bayer CropScience AGInventors: Werner HALLENBACH, Oliver Guth, Thomas Seitz, Heinz-Juergen Wroblowsky, Philippe Desbordes, Ulrike Wachendorff-Neumann, Peter Dahmen, Arnd Voerste, Peter Lösel, Olga Malsam, Rachel Rama, Hiroyuki Hadano
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Publication number: 20120046290Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: October 31, 2007Publication date: February 23, 2012Inventors: Jacques Dumas, Uday Khire, Timothy B. Lowinger, Holger Paulsen, Bernd Riedl, William J. Scott, Roger A. Smith, Jill Wood, Holia Hatoum-Mokdad, Wendy Lee, Aniko Redman, Jeffrey Johnson, Robert Sibley
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Publication number: 20120046324Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.Type: ApplicationFiled: November 2, 2011Publication date: February 23, 2012Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20120035181Abstract: A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.Type: ApplicationFiled: April 26, 2010Publication date: February 9, 2012Applicant: NIPPON SUISAN KAISHA, LTD.Inventors: Fumi Kawano, Noritaka Hirazawa
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Publication number: 20120035141Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.Type: ApplicationFiled: October 11, 2011Publication date: February 9, 2012Applicant: ESPERION THERAPEUTICS, INC.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 8110568Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: GrantFiled: March 18, 2010Date of Patent: February 7, 2012Assignee: Genentech, Inc.Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20120024743Abstract: The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.Type: ApplicationFiled: February 5, 2010Publication date: February 2, 2012Applicant: EGIS GYOGYSZERGYAR NYILVANOSAN MUKODO RESZVENYTARSASAGInventors: Endre Mikulasik, Patrik Fazekas
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Publication number: 20120028944Abstract: The invention provides an ophthalmic composition which is an aqueous suspension comprising drug, cyclodextrin and water, the composition having an aqueous phase of from about 0.1% (w/v) to about 90% (w/v) of the drug in solution, as dissolved free drug and as dissolved drug/cyclodextrin complex(es), and a solid phase of from about 10% (w/v) to about 99.9% (w/v) of the drug as solid drug/cyclodextrin particles, suspended in the aqueous phase; the size of the solid particles being from about 10 nm to about 1 mm, the drug/cyclodextrin particles being capable of dissolving in aqueous tear fluid within 24 hours of application to the eye surface. The aqueous eye suspension can be in the form of eye drops, eye gel or eye mist.Type: ApplicationFiled: January 27, 2011Publication date: February 2, 2012Applicant: OCULIS EHFInventors: Thorsteinn Loftsson, Einar Stefansson
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Patent number: 8101657Abstract: The invention provides a plant disease and insect damage control composition including, as active ingredients, dinotefuran and at least one fungicidal compound; and a plant disease and insect damage prevention method that includes applying such a composition to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber. The invention provides a new plant disease and insect damage control composition and a plant disease and insect damage prevention method with very low toxicity to mammals and fishes, the composition and method showing an effect against plural pathogens and pest insects, including emerging resistant pathogens and resistant pest insect, by application to a plant body, soil, plant seed, stored cereal, stored legume, stored fruit, stored vegetable, silage, stored flowering plant, or export/import timber.Type: GrantFiled: November 22, 2007Date of Patent: January 24, 2012Assignee: Mitsui Chemicals, Inc.Inventors: Eiichi Yamada, Ryutaro Ezaki, Hidenori Daido
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Publication number: 20120015991Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 27, 2011Publication date: January 19, 2012Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard HUTCHINSON, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Publication number: 20120010184Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20120010186Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: MERCK FROSST CANADA LTD.Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau
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Publication number: 20110319333Abstract: The present application relates to methods of treating HIV-associated nephropathy (HIVAN) and/or focal segmental glomerulosclerosis (FSGS) using endothelin-1 (ET-1) antagonists. The application further relates to a composition for the treatment of HIVAN and/or FSGS. A kit for detecting the presence of ET-1 or ET-1-associated biomarker in a biological sample is also disclosed.Type: ApplicationFiled: June 16, 2011Publication date: December 29, 2011Applicant: MOREHOUSE SCHOOL OF MEDICINEInventors: Gale W. NEWMAN, Barbara A. JACOB-MUNGIN, Chamberlain OBIALO
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Publication number: 20110312932Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: August 25, 2011Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20110301211Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: December 15, 2009Publication date: December 8, 2011Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20110301142Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: December 15, 2009Publication date: December 8, 2011Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr, Lucy Zhao
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Publication number: 20110301134Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: December 10, 2009Publication date: December 8, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda
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Publication number: 20110294815Abstract: This invention relates to novel prostacyclin analogs and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel prostacyclin analogs that are derivatives of treprostinil. This invention also provides compositions comprising a compound of this invention and a carrier and the use disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering analogues of prostacyclin, such as treprostinil.Type: ApplicationFiled: June 26, 2009Publication date: December 1, 2011Inventor: Scott L. Harbeson
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Publication number: 20110288131Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3 and R4 are as defined in claim 1; or a salt or oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: January 13, 2010Publication date: November 24, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Myriem El Qacemi, Thomas Pitterna, Jerome Yves Cassayre, Peter Renold
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Publication number: 20110280824Abstract: The present disclosure provides copolymers including a first monomer including at least one phospholipid possessing at least one vinyl group and a second monomer including a furanone possessing vinyl and/or acrylate groups. Compositions, medical devices, and coatings including such copolymers are also provided.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: Tyco Healthcare Group LPInventor: Joshua B. Stopek
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Patent number: 8058300Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: June 3, 2010Date of Patent: November 15, 2011Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20110269764Abstract: The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate synapse function for treating said disease.Type: ApplicationFiled: October 29, 2010Publication date: November 3, 2011Applicant: PHARNEXTInventors: Daniel Cohen, Ilya Chumakov, Serguei Nabirochkin, Oxana Guerassimenko, Nathalie Cholet
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Publication number: 20110269804Abstract: A compound of formula (I): where A, B, C, G, m, n, o, p, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: July 24, 2009Publication date: November 3, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jérôme Yves Cassayre, Peter Renold, Thomas Pitterna, Vladimir Bobosik, Myriem El Qacemi, Anne Jacqueline Dalencon, Werner Zambach, Christopher Richard Ayles Godfrey, Pierre Joseph Marcel Jung, Jagadish Pabba
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Patent number: 8048899Abstract: are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 22, 2009Date of Patent: November 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
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Patent number: 8048902Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: GrantFiled: December 15, 2009Date of Patent: November 1, 2011Assignee: Amira Pharmaceuticals, Inc.Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Publication number: 20110257078Abstract: There is described a composition comprising a therapeutically active imidazole, and derivatives thereof, and an agent active on a bacterial cell surface selected from the group consisting of one or more of colistin, nisin, D-cycloserine, fosfomycin, fosfomycin trometamol, fosfomycin disodium and polymixin B, and derivatives thereof.Type: ApplicationFiled: July 17, 2009Publication date: October 20, 2011Applicant: E-THERAPEUTICS PLCInventors: Malcolm Philip Young, Catherine Mary Thomas
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Publication number: 20110251205Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 21, 2011Publication date: October 13, 2011Inventors: Urs Baettig, Anne-Marie D'Souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20110245221Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 30, 2009Publication date: October 6, 2011Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.Inventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Paolo Carminati, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati, Claudio Pisano
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Publication number: 20110245204Abstract: The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: ApplicationFiled: July 12, 2010Publication date: October 6, 2011Inventors: Kevin R. Lynch, Timothy L. MacDonald
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Publication number: 20110237559Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 12, 2008Publication date: September 29, 2011Applicant: Schering CorporationInventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
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Publication number: 20110230445Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20110224212Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.Type: ApplicationFiled: May 16, 2011Publication date: September 15, 2011Applicant: TYROGENEX, INC.Inventors: Congxin Liang, Ming Qi, Shu Gao, Zhigang Li
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Patent number: 8017638Abstract: Disclosed is a compound useful as an inhibitor of 11?-hydroxysteroid dehydrogenase type 1. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is a group of the formula: —C(?O)NR4R5, (wherein R4 and R5 are each independently, hydrogen, optionally substituted alkyl or the like) or a group of the formula: —NR6C(?O)R7, (wherein R6 and R7 are each independently, hydrogen, optionally substituted alkyl or the like), X and Y are each independently —O— or the like, Z is a bond or the like, R2 is optionally substituted alkyl, optionally substituted alkenyl or the like, R3 is optionally substituted alkyl, optionally substituted alkenyl or the like.Type: GrantFiled: March 28, 2007Date of Patent: September 13, 2011Assignee: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Nobuo Chomei, Koji Masuda, Satoru Tanaka
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Publication number: 20110207788Abstract: The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.Type: ApplicationFiled: August 21, 2006Publication date: August 25, 2011Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Andreas Haupt, Francisco Javier Garcia-Ladona, Wolfgang Wernet, Alfred Hahn
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Patent number: 8003617Abstract: The invention provides methods of treating a diabetic subject comprising administering a glucosylceramide synthase inhibitor to the subject.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: Genzyme CorporationInventors: Seng H. Cheng, Nelson S. Yew, Ronald K. Scheule, Hongmei Zhao
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Publication number: 20110201609Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.Type: ApplicationFiled: June 30, 2009Publication date: August 18, 2011Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South FloridaInventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
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Publication number: 20110196005Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: April 22, 2011Publication date: August 11, 2011Applicant: Amira Pharmaceuticals, Inc.,Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
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Publication number: 20110190256Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: ApplicationFiled: February 19, 2009Publication date: August 4, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Publication number: 20110178092Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.Type: ApplicationFiled: December 19, 2007Publication date: July 21, 2011Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
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Publication number: 20110172225Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: September 25, 2008Publication date: July 14, 2011Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20110165188Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: March 17, 2011Publication date: July 7, 2011Inventors: Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Way Tsun Yue
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Publication number: 20110166060Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.Type: ApplicationFiled: May 19, 2009Publication date: July 7, 2011Applicants: Massachusettes Institute of Technology, Children's Medical Center CorporationInventors: Emmanuel John Simons, Todd R. Hoare, Daniel S. Kohane, Robert S. Langer