Benzene Ring Bonded Directly To The Diazole Ring By Nonionic Bonding Patents (Class 514/391)
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Publication number: 20110212944Abstract: This invention relates to novel 2-oxo-1-pyrrolidines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as a synaptic vesicle protein 2A (SV2A) ligand and/or a sodium channel blocker.Type: ApplicationFiled: June 30, 2009Publication date: September 1, 2011Inventors: Julie Liu, Rose Persichetti
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Publication number: 20110207718Abstract: Methods of treating psychiatric disorders are provided which include administration of one or more anti-epileptic agents and, optionally, one or more a psychostimulants. Also provided are pharmaceutical compositions comprising, in combination, one or more anti-epileptic agents and one or more psychostimulants. Psychiatric disorders include those associated with impaired cognitive processing, degenerative disorders such as Mild Cognitive Impairment, Parkinson's disease, dementia, non-compliance with therapeutic regimes and eating disorders, although without limitation thereto.Type: ApplicationFiled: August 6, 2009Publication date: August 25, 2011Applicant: GOSFORTH CENTRE (HOLDINGS) PTY LTD.Inventor: Philip Bird
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Publication number: 20110178134Abstract: The invention relates to compounds of formula (I) wherein the groups have stated meanings, and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.Type: ApplicationFiled: August 6, 2010Publication date: July 21, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER, Antony BIGOT, Anita DIU-HERCEND, Gilles TIRABOSCHI
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Publication number: 20110177944Abstract: The present invention relates to a composition, comprising a 5-amino-3-oxo-2,3-dihydro-pyrazole of the formula I as defined in the claims and the description and at least one active compound II selected from groups A) to I) in a synergistically effective amount.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: BASF SEInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Egon Haden
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Publication number: 20110172171Abstract: The present invention relates to taurine or taurine-like substances for the prevention of brain oedema, particularly brain intramyelinic oedema and more particularly brain intramyelinic oedema induced by an anti-convulsive drug such as vigabatrin. The invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention of brain oedema.Type: ApplicationFiled: September 4, 2009Publication date: July 14, 2011Inventors: Serge Picaud, José-Alain Sahel, Firas Jammoul
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Patent number: 7973067Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: GrantFiled: December 10, 2008Date of Patent: July 5, 2011Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert D. Mazzola, Jr., John P. Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X. H. Le, Kurt W. Saionz, Suresh D. Babu, Rachel C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Patent number: 7968581Abstract: Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.Type: GrantFiled: September 10, 2009Date of Patent: June 28, 2011Assignee: Galapagos NVInventors: François Nique, Catherine Jagerschmidt, Florence Sylvie Namour, Roland Blanqué, Jean-Michel Lefrançois, Christophe Peixoto, Pierre Deprez, Nicolas Triballeau, Piet Tom Bert Paul Wigerinck
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Publication number: 20110130391Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.Type: ApplicationFiled: December 29, 2010Publication date: June 2, 2011Inventors: Richard G. Wilde, James J. Takasugi, Seongwoo Hwang, Ellen M. Welch, Guangming Chen
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Publication number: 20110112097Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: May 12, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Jaehne, Peter Below, Siegfried Stengelin, Matthias Gossel, Thomas Klabunde, Irvin Winkler
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Publication number: 20110098323Abstract: Organic compounds are described for use in inhibiting or preventing formation of bacterial biofilms.Type: ApplicationFiled: May 19, 2009Publication date: April 28, 2011Applicant: MICROBIOTIX, INC.Inventors: Timothy J. Opperman, John D. Williams, Norton P. Peet, Atiyya R. Khan, Steven M. Kwasny
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Publication number: 20110077581Abstract: The various embodiments of the present disclosure relate generally to compositions and methods for the targeted cellular delivery of nanoparticles. More particularly, the various embodiments of the present invention are directed to the cellular delivery of nanoparticles tethered to a ligand by way of a poly(ethylene glycol) linkage, wherein the ligand demonstrates a binding specificity for a cellular target. In an exemplary embodiment, the ligand is tamoxifen and the cellular target is the estrogen receptor, which is upregulated in many breast cancer cells.Type: ApplicationFiled: September 24, 2010Publication date: March 31, 2011Applicant: GEORGIA TECH RESEARCH CORPORATIONInventors: ADEGBOYEGA K. OYELERE, MOSTAFA A. EL-SAYED, ERIK C. DREADEN
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Publication number: 20110053947Abstract: The invention relates to compounds of formula (I) wherein the groups R and R?, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: March 3, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Publication number: 20110046154Abstract: The invention relates to the use of a compound selected from an aminopeptidase-inhibiting compound and an azaindole compound for producing a drug for preventing or treating cancerous metastases in humans or animals.Type: ApplicationFiled: January 21, 2009Publication date: February 24, 2011Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Pierre Roux, Marion De Toledo, Jean-Paul Leonetti, Christelle Anguille
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Publication number: 20110046185Abstract: The invention relates to compounds of formula (I) wherein the groups R and R? A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs.Type: ApplicationFiled: August 6, 2010Publication date: February 24, 2011Applicant: SANOFI-AVENTISInventors: Gerhard JAEHNE, Peter BELOW, Siegfried STENGELIN, Matthias GOSSEL, Thomas KLABUNDE, Irvin WINKLER
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Patent number: 7884244Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: March 28, 2008Date of Patent: February 8, 2011Assignee: Allergan, Inc.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20110021573Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: February 25, 2009Publication date: January 27, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
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Publication number: 20100330032Abstract: Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: June 24, 2010Publication date: December 30, 2010Inventors: Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Publication number: 20100311701Abstract: A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, O-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.Type: ApplicationFiled: June 2, 2010Publication date: December 9, 2010Applicants: Transform Pharmaceuticals, Inc, University Of South Florida, The Regents of the University Of MichiganInventors: Orn Almarsson, Magali Bourghol Hickey, Matthew Peterson, Michael J. Zaworotko, Brian Moulton, Nair Rodriguez-Hornedo
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Publication number: 20100292187Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.Type: ApplicationFiled: June 14, 2010Publication date: November 18, 2010Applicant: PTC THERAPEUTICS, INC.Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
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Publication number: 20100279991Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: ApplicationFiled: July 15, 2010Publication date: November 4, 2010Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100247583Abstract: Novel N-phenylacetamide compounds of formula (I): and cosmetic and pharmaceutical compositions containing same are useful for treating disorders of the sebaceous gland, e.g., acne, or have cosmetic applications.Type: ApplicationFiled: March 5, 2010Publication date: September 30, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Thibaud PORTAL, Laurence DUMAIS, Jérôme AUBERT, Laurent LAMY
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Publication number: 20100239668Abstract: Described is a layered or segmented controlled release pharmaceutical tablet adapted for separating one segment from another by breaking through a segment.Type: ApplicationFiled: June 19, 2007Publication date: September 23, 2010Inventors: Allan S. Kaplan, Lawrence Solomon
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Publication number: 20100234331Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: ApplicationFiled: May 24, 2010Publication date: September 16, 2010Inventors: Mingde Xie, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
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Patent number: 7795315Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: GrantFiled: January 23, 2009Date of Patent: September 14, 2010Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Yun He, Jason Christopher Wong
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Patent number: 7795287Abstract: A compound having a structure is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 30, 2007Date of Patent: September 14, 2010Assignee: Allergan, Inc.Inventor: David W. Old
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Publication number: 20100222311Abstract: Described herein are formulations of active pharmaceutical ingredients, where the active pharmaceutical ingredients or drugs are included in a solid suspension with one or more solid additives. The formulations described herein are useful for formulating any drug or active pharmaceutical ingredient, including those that have limited solubility in organic and/or aqueous solvent systems.Type: ApplicationFiled: October 17, 2008Publication date: September 2, 2010Applicant: PURDUE RESEARCH FOUNDATIONInventors: Markus Thommes, Rodolfo Pinal, Teresa M. Carvajal
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Publication number: 20100222298Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Applicant: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish ASOTRA, Xiaoli WANG, Zoltan BODOR
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Publication number: 20100210665Abstract: The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Type: ApplicationFiled: February 18, 2010Publication date: August 19, 2010Applicant: The Regents of the University of CaliforniaInventors: Charles L. Sawyers, Michael E. Jung, Charlie D. Chen, Samedy Ouk, Derek Welsbie, Chris Tran, John Wongvipat
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Publication number: 20100209541Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: January 22, 2010Publication date: August 19, 2010Inventor: Harry A. DUGGER, III
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Publication number: 20100210699Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H, alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl, hydroxyalkyl, alkoxyl, thioalkyl, haloalkyl, alkenyl, or alkynyl; R7 and R8 are H, halogen, OH, SH; alkoxyl or alkylthio optionally substituted by OH and/or halogen; one of R7 and R8 not being H or halogen; or one of R7 and R8 is a pharmaceutically acceptable ester or thioester grouping, or R6 is C1-3-alkyl or, together with either R1 or R2, represents C1-3 alkylene or alkenylene linking group, optionally substituted by methyl, trifluoromethyl, OH, orType: ApplicationFiled: March 31, 2010Publication date: August 19, 2010Inventors: Francois NIQUE, Catherine Jagerschmidt, Philippe Clement-Lacroix
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Publication number: 20100190752Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.Type: ApplicationFiled: January 26, 2010Publication date: July 29, 2010Applicant: Gruenenthal GmbHInventors: Klaus Schiene, Petra Bloms-Funke, Thomas Christoph
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Publication number: 20100190648Abstract: Structured agrochemical concentrates comprise agrochemical actives dispersed in a structured oil system of an oil and structurant oligomer including urethane and/or urea linkages and residues of a dimer or trimer component. The concentrate formulations may contain other components such as surfactants without the structurant loosing its effect a problem with known structurants. The concentrates can be readily diluted to give sprayable agrochemical formulations.Type: ApplicationFiled: May 18, 2007Publication date: July 29, 2010Applicant: Croda International PLCInventors: Peter James Tollington, Frederico Irou Roschzttardtz, Remco Benjamin van Triet, Eric Appelman, Hendrik Leendert Rieffe
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Publication number: 20100168194Abstract: The present invention provides compounds and methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: March 10, 2010Publication date: July 1, 2010Applicant: Wyeth LLCInventors: Michael Sotirios Malamas, Albert Jean Robichaud, Alexander Michael Porte, Koi Michele Morris, William R. Solvibile, Ji-In Kim, Schuyler Adam Antane
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Patent number: 7745637Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: February 16, 2007Date of Patent: June 29, 2010Assignee: GlaxoSmithKline LLCInventors: Kelly M. Aubart, Ajita Bhat, Sigfried B. Christensen, IV, Jack D. Leber, Xiangmin Liao
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Publication number: 20100160330Abstract: The present invention is directed to novel bicyclic heterocycles, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: October 15, 2009Publication date: June 24, 2010Inventors: Xuqing Zhang, Zhihua Sui
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Publication number: 20100125086Abstract: The present invention relates in general to an inhibitor of a glutaminyl peptide cyclotransferase-like protein (QPCTL), and the use thereof for the treatment and/or prevention of an inflammatory disease or disorder selected from the group consisting of (a) chronic and acute inflammations, e.g. rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis; (b) other inflammatory diseases, e.g. neuropathic pain, graft rejection/graft failure/graft vasculopathy, HIV infections/AIDS, gestosis, tuberous sclerosis, Guillain-Barré syndrome, chronic inflammatory demyelinising polyradiculoneuropathy and multiple sclerosis; (c) neuroinflammation; and (d) neurodegenerative diseases, e.g. mild cognitive impairment (MCI), Alzheimer's disease, neurodegeneration in Down Syndrome, Familial British Dementia, and Familial Danish Dementia, which may result from neuroinflammation.Type: ApplicationFiled: September 4, 2009Publication date: May 20, 2010Applicant: PROBIODRUG AGInventors: Hans-Ulrich Demuth, Stephan Schilling, Michael Wermann, Holger Cynis, Astrid Kehlen, Daniel Friedrich, Torsten Hoffmann, Kathrin Gans, Jens-Ulrich Rahfeld, Ulrich Heiser, Michael Almstetter, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Thormann, Andreas Tremel
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Publication number: 20100119475Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, X and Y are as defined herein are inhibitors of glutaminyl cyclase and are therefore useful in treating conditions that can be treated by modulation of glutaminyl cyclase activity.Type: ApplicationFiled: September 4, 2009Publication date: May 13, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Robert Sommer, Ulf-Torsten Gaertner, Antje Hamann, Michael Almstetter, Michael Thormann, Andreas Treml, Hans-Ulrich Demuth, Torsten Hoffman
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Publication number: 20100120838Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong Heon Kim, De-Yi Yang, Razia Rizvi
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Publication number: 20100113547Abstract: Novel compounds are disclosed that have a Formula represented by the following: wherein X, R1, R2a, R2b, R2c, R3a R3b, R4a, R4b, R4c, and m1 are as described herein. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cachexia, osteoporosis, sarcopenia, a decline in libido and/or sexual dysfunction.Type: ApplicationFiled: September 10, 2009Publication date: May 6, 2010Inventors: François Nique, Catherine Jagerschmidt, Florence Sylvie Namour, Roland Blanqué, Jean-Michel Lefrançois, Christophe Peixoto, Pierre Deprez, Nicolas Triballeau, Piet Tom Bert Paul Wigerinck
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Patent number: 7705030Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.Type: GrantFiled: July 28, 2008Date of Patent: April 27, 2010Assignee: Wyeth LLCInventors: Michael Sotirios Malamas, Ping Zhou, William Floyd Fobare, William Ronald Solvibile, Iwan Suwandi Gunawan, James Joseph Erdei, Yinfa Yan, Patrick Michael Andrae, Dominick Anthony Quagliato
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Publication number: 20100092534Abstract: Described herein are implantable medical devices useful in treating vascular conditions such as restenosis. In one embodiment, stents are described in which a combination of bioactive agents is described for local delivery in the vasculature. The combination of bioactive agents comprises at least one compound capable of inhibiting smooth muscle cell proliferation and at least one compound capable of mitigating MCP- and/or TF induction. For example, a compound capable of inhibiting smooth muscle cell proliferation is a mTOR inhibitor and a compound capable of mitigating MCP-1 and/or TF induction is a corticosteroid.Type: ApplicationFiled: October 10, 2008Publication date: April 15, 2010Applicant: Medtronic Vascular, Inc.Inventors: Ayala Hezi-Yamit, Iskender Matt Bilge, Jennifer Wong, Carol Sullivan, Natividad Vasquez
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Publication number: 20100087422Abstract: A method is described for treating attention deficit hyperactivity disorder (ADHD), by administering to the individual an anti-epileptic mood stabiliser at a dose which is sub-therapeutic for mood stabilisation, optionally in combination with a psychostimulant. Also described is a method of improving reading comprehension and/or fluency in an individual suffering from learning difficulties which method comprises administering to the individual an anti-epileptic mood stabiliser.Type: ApplicationFiled: February 7, 2008Publication date: April 8, 2010Applicant: GOSFORTH CENTRE (HOLDINGS) PTY LTDInventor: Philip Bird
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Publication number: 20100063120Abstract: Compounds of formula (I): wherein X is O or S, R1 is acyl, aldehyde, cycloalkyl, an optionally substituted alkyl, alkenyl or alkynyl, R2 is H. alkyl, hydroxyalkyl, haloalkyl, alkenyl, or alkynyl; substituted alkyl; alkylcarbonyl; R3 and R4 are H, halogen, alkyl, alkenyl, alkynyl, alkoxyl, alkylthio, hydroxyalkyl, haloalkyl, haloalkenyl, or haloalkynyl; or R3 and R4 form an, optionally aromatic or heterocyclic, optionally substituted ring, R5 is H, halogen, trifluoromethyl, —CN, or —NO2; not all of R3, R4, and R5 being H, R6 and R9 are H, halogen, OH; alkyl.Type: ApplicationFiled: May 31, 2007Publication date: March 11, 2010Inventors: Francois Nique, Catherine Robin-Jagerschmidt, Philippe Clement-Lacroix
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Patent number: 7666865Abstract: Compounds of the formula wherein m is 0, 1 or 2; wherein when m is 0, Z is O, when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each l1 and l2 is independently 0-5; l3 is 0 or 1; each of R1, R2 and R3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, O, and S or each of R1 and R2 may independently be halo, COOR, CONR2, CF3, CN or NO2, wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker; with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if l3 is 0, and either l1 and l2 is 0 or 1 and if R1 and/or R2 represent F in the para position, Z cannot be C or N; and are useful to treat pain.Type: GrantFiled: November 16, 2006Date of Patent: February 23, 2010Assignee: Neuromed Pharmaceuticals Ltd.Inventors: Terrance P. Snutch, Gerald W. Zamponi
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Publication number: 20100029618Abstract: Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.Type: ApplicationFiled: December 14, 2007Publication date: February 4, 2010Inventors: Daniel W. Gil, John E. Donello
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Publication number: 20100029484Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: July 17, 2009Publication date: February 4, 2010Inventors: John S. Kovach, Francis Johnson
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Patent number: 7625876Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: August 20, 2007Date of Patent: December 1, 2009Assignee: Hopital-Sainte-JustineInventors: Ernest G. Seidman, Yves Theoret
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Publication number: 20090286780Abstract: To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A 2-oxochromene derivative represented by the following general formula (1) or salt thereof, or their solvate.Type: ApplicationFiled: February 27, 2009Publication date: November 19, 2009Applicant: KOWA COMPANY, LTD.Inventors: Ayumu OKUDA, Takayuki MATSUDA, Toru MIURA, Hidefumi OZAWA, Ayako TOSAKA, Koichi YAMAZAKI, Yuki YAMAGUCHI, Sayaka KUROBUCHI, Yuuichirou WATANABE, Kimiyuki SHIBUYA
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Publication number: 20090281101Abstract: Compounds comprising a structure or a pharmaceutically acceptable salt thereof, or a prodrug thereof; wherein a dashed line represents the presence or absence of a bond are disclosed, wherein Y, A, B, and J are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: November 12, 2009Applicant: ALLERGAN, INC.Inventor: David W. Old