Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
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Publication number: 20110281853Abstract: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Inventors: Rishi Arora, David E. Zembower
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Publication number: 20110275719Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
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Publication number: 20110275619Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.Type: ApplicationFiled: December 4, 2009Publication date: November 10, 2011Applicant: PURDUE RESEARCH FOUNDATIONInventor: Arun K. Ghosh
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Publication number: 20110263580Abstract: This invention relates to a method for treating or preventing diseases associated with the deposition of ?-amyloid peptide in the brain, such as Alzheimer's disease, said method involving administration of a gamma-secretase inhibitor in an intermittent dosing regime to a patient in need thereof.Type: ApplicationFiled: December 4, 2009Publication date: October 27, 2011Inventor: Thomas Miller
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Patent number: 8039493Abstract: The invention is concerned with novel biaryl sulfonamide derivatives of formula (I) wherein R1 to R3 and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.Type: GrantFiled: September 17, 2008Date of Patent: October 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Ulrike Obst Sander, Tanja Schulz-Gasch, Matthew Wright
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Patent number: 8039495Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: October 15, 2010Date of Patent: October 18, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110251162Abstract: The present subject matter relates to pathogenesis of MRSA. Specifically, the present disclosures identifies the pro-inflammatory properties of PVL as the cause of MRSA. Viewed from this new perspective, the present subject matter achieves novel methods and apparatus for treating MRSA infection in a subject involving the administration of an anti-inflammatory drug to the subject. Furthermore the present subject matter teaches methods and apparatus for treating a Panton-Valetine leukocidin associated infection in a subject involving the administration of an anti-inflammatory drug to the subject.Type: ApplicationFiled: September 25, 2009Publication date: October 13, 2011Applicant: CEDARS-SINAI MEDICAL CENTERInventors: George Y. Liu, Ching Wen Tseng
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Publication number: 20110230428Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 22, 2009Publication date: September 22, 2011Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20110218219Abstract: The present invention relates to substituted sulphonamido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: October 28, 2009Publication date: September 8, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Ingo Hartung, Marion Hitchcock, Florian Puhler, Gerhard Siemeister, Roland Neuhaus
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Patent number: 8013019Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: July 1, 2010Date of Patent: September 6, 2011Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
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Publication number: 20110160223Abstract: Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.Type: ApplicationFiled: November 2, 2010Publication date: June 30, 2011Inventors: Raymond J. Dingledine, Stephen F. Traynelis
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Patent number: 7960584Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.Type: GrantFiled: March 17, 2006Date of Patent: June 14, 2011Assignee: Amorepacific CorporationInventors: Young-Ger Suh, Hee-Doo Kim, Hyeung-Geun Park, Uh Taek Oh, Yong-Sil Lee, Seol Rin Park, Chong Hyon Ryu, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Joon Ho Bae
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Publication number: 20110124733Abstract: A method of treatment or prophylaxis of diabetes, obesity, dyslipidemia or metabolic syndrome, includes administering an effective amount of a benzylamine derivative represented by Formula (I): wherein, R1 represents an alkyl group having 1 to 6 carbon atoms; R2 represents an alkyl group having 1 to 6 carbon atoms; R3 and R5 each independently represent a halogen atom, an alkyl group having 1 to 6 carbon atoms, a haloalkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms; and R4 representa a hydrogen atom or an alkoxy group having 1 to 6 carbon atoms, or a pharmaceutically acceptable acid addition salt thereof.Type: ApplicationFiled: July 31, 2009Publication date: May 26, 2011Applicant: TORAY INDUSTRIES, INC.Inventors: Ko Hasebe, Satoru Yoshikawa, Hideki Kozono, Seiji Okazaki
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Publication number: 20110117055Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.Type: ApplicationFiled: November 18, 2010Publication date: May 19, 2011Inventors: James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
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Publication number: 20110118322Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 15, 2010Publication date: May 19, 2011Inventors: David Robert Bolin, Yimin Qian, Kshitij Chhabilbhai Thakkar, Lin Yi, Weiya Yun
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Publication number: 20110105533Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.Type: ApplicationFiled: June 25, 2010Publication date: May 5, 2011Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
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Publication number: 20110082109Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AJINOMOTO CO., INC.Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
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Patent number: 7915448Abstract: This invention provides a compound of the formula (I): wherein A and B are independently CR12 or N; D and E are each independently CR9 or N; R1 represents (C1-C6)alkyl; R2 represents hydrogen, halogen, hydroxy, (C1-C6) alkyl, halo(C1-C6) alkyl, hydroxy(C1-C6) alkyl, (C1-C6)alkoxy or (C1-C6)alkoxy-(C1-C6)alkyl; R3, R4, R5, R6, R10 and R11 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkyl or (C1-C6)alkoxy-(C1-C6)alkyl; or R3 and R4 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered carbocyclic ring or heterocyclic ring in which one or two non-adjacent carbon atoms are optionally replaced by an oxygen atom, a sulfur atom or NH; R7 and R9 each independently represent hydrogen, halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, hydroxy(C1-C6)alkyl, (C1-C6)alkoxy, hydroxy(C1-C6)alkoxy, (C1-C6)alkoxy-(C1-C6)alkyl, (C1-C6)alkoxy-(C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkylsulfinyl, (C1-C6)alkylsulfonyl, NH2, [(C1-C6Type: GrantFiled: October 13, 2009Date of Patent: March 29, 2011Assignee: Pfizer Inc.Inventors: Takeshi Hanazawa, Misato Hirano, Tadashi Inoue, Satoshi Nagayama, Kazunari Nakao, Yuji Shishido, Hirotaka Tanaka
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Publication number: 20110065760Abstract: The present invention is related to a compound of the formula (I), (II), (III), (IV), (V): wherein Z1, Z2, Z3 and Z4 are each and independently selected from the group comprising C(O)—, —C(S)—, —C(O)—NR10—, —C(S)—NR11—, —C(N—CN)—NR12—, —S(O)—, —S(O2)—, —S(O)—NR13—, and S(O2)—NR14—, —O—, —S— or are each and individually absent; X is a spacer and is independently selected from the group comprising -M1-L1-K-L2-M2-, wherein Y.Type: ApplicationFiled: November 23, 2009Publication date: March 17, 2011Applicant: Jerini AGInventors: Jochen KNOLLE, Mike Schutkowski, Gerd Hummel, Thomas Tradler, Laurence Jobron, Claudia Christner, Dirk Scharn, Roland Stragies, Christoph Gibson, Frank Osterkamp
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Patent number: 7906538Abstract: Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.Type: GrantFiled: October 31, 2007Date of Patent: March 15, 2011Assignee: Schering-Plough Animal Health CorporationInventors: Adam Gerhardt Meyer, Kevin Norman Winzenberg, David G. Sawutz, Andris Juris Liepa
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Publication number: 20110052492Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: November 3, 2010Publication date: March 3, 2011Inventors: Matthias FRIEBE, Peter Muschick, Andreas Huth
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Publication number: 20110046120Abstract: The present disclosure provides methods and compositions for treating Impulse Control disorders including, for example, pathological gambling using ?2-adrenergic agonists, ?-adrenergic receptor antagonists, or both.Type: ApplicationFiled: October 25, 2007Publication date: February 24, 2011Inventor: Igor Elman
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Publication number: 20110039802Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylone, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereofType: ApplicationFiled: July 2, 2010Publication date: February 17, 2011Inventors: Yasuyuki KAWANISHI, Hideyuki TAKENAKA, Kohji HANASAKI, Tetsuo OKADA
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Publication number: 20110039925Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: April 17, 2009Publication date: February 17, 2011Inventors: Richard W. Heidebrecht, Chaomin Li, Benito Munoz, Andrew Rosenau, Laura M. Surdi, Paul Tempest
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Publication number: 20110021526Abstract: A method for treating diabetic complications by administration of a beta-blocker is disclosed. Diabetic complications arise from diabetes and have few or no existing treatment options. The present invention describes the use of a beta-blocker in the treatment of a diabetic. The present invention also describes the inhibition of aldose reductase, one of the chief causative factors of diabetic complications. Also provided are methods of diabetic wound healing. Compositions for treating diabetic complications, such as diabetic wounds, are disclosed. The present invention includes employing a topical formulation of a beta-blocker, having substantially no antibacterial activity, to improve the process of diabetic wound healing. The present invention also involves increasing the rate of collagen accumulation of the healing epithelialized tissue in the wound of a diabetic individual.Type: ApplicationFiled: January 24, 2008Publication date: January 27, 2011Applicant: VLife Science Technologies Pvt. Ltd.Inventor: Supreet K. Deshpande
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Publication number: 20110021514Abstract: Compounds are disclosed that have a formula represented by the following: 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, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: November 13, 2008Publication date: January 27, 2011Applicants: RENOVIS, INC., PFIZER GLOBAL RESEARCH AND DEVELOPMENTInventors: Matthew Cox, Donogh John Roger O'Mahony, Maria De Los Angeles Estiarte-Martinez, Tadashi Kawashima, Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka, Matthew Alexander James Duncton, Andrew Antony Calabrese
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Publication number: 20110015230Abstract: This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: ApplicationFiled: January 28, 2009Publication date: January 20, 2011Applicant: Amorepacific CorporationInventors: Song Seok Shin, Jin Kwan Kim, Sun-Young Kim, Ki-Wha Lee, Byoung young Woo, Joo-Hyun Moh, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Hyun-Ju Koh, Young-Ho Park
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel
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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: 20100331280Abstract: There is provided a method of modifying vasoactivity by regulating a soluble A? pro-inflammatory pathway. Also provided is a method of modifying inflammatory reactions in microglia and neurons by regulating a soluble A? pro-inflammatory pathway. A method of treating patients with vascular disease by modifying an intracellular soluble A? pro-inflammatory pathway is also provided. A pharmaceutical composition consisting essentially of an effective amount of a soluble A? pro-inflammatory pathway regulator in a pharmaceutically effective carrier is also provided.Type: ApplicationFiled: October 20, 2009Publication date: December 30, 2010Inventors: Daniel C. Paris, Terrence C. Town, Michael J. Mullan
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Patent number: 7829564Abstract: ?-and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: December 7, 2007Date of Patent: November 9, 2010Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Publication number: 20100280017Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.Type: ApplicationFiled: July 12, 2010Publication date: November 4, 2010Applicant: Gruenenthal GmbHInventors: Klaus SCHIENE, Guenter HAASE, Babette-Yvonne KOEGEL, Elmar FRIDERICHS, Ulrich JAHNEL
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Publication number: 20100273758Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: ApplicationFiled: July 1, 2010Publication date: October 28, 2010Inventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
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Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
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Publication number: 20100267705Abstract: The present invention relates to an improved pharmaceutical composition and in particular to a pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of a lipophilic active ingredient with milk as a solubilizing/dispersing agent and methods for the preparation thereof.Type: ApplicationFiled: November 28, 2008Publication date: October 21, 2010Applicant: Pharmathen S.A.Inventor: Panayotis Macheras
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Publication number: 20100240657Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: July 1, 2008Publication date: September 23, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Martin Steegmaier, Steffen Steurer, Irene Waizenegger
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Publication number: 20100234295Abstract: Use of a composition for treating Alzheimer's disease, osteoporosis, sleep apnea, erectile dysfunction, McArdle disease, or a carbohydrate metabolism disorder, or for reducing aging or fatigue. The composition includes a first agent selected from the group consisting of an oxidative phosphorylation inhibitor, an ionophore, and an adenosine 5?-monophosphate-activated protein kinase activator; a second agent that possesses anti-inflammatory activity; and a third agent that possesses serotonin activity.Type: ApplicationFiled: March 15, 2010Publication date: September 16, 2010Inventor: Chien-Hung Chen
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Patent number: 7790758Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: GrantFiled: February 13, 2006Date of Patent: September 7, 2010Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Publication number: 20100222317Abstract: The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders.Type: ApplicationFiled: November 23, 2006Publication date: September 2, 2010Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Elizabeth Mary Naylor
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Publication number: 20100215710Abstract: Methods for increasing rate of healing of wounds in epithelial tissues by administration of beta-2 adrenergic receptor antagonists to target patients are provided. Methods for decreasing cell growth around implanted devices and methods for decreasing wound contraction by administration of beta-2 adrenergic receptor agonists are also provided. Pharmaceutical compositions and kits including beta-2 adrenergic receptor agonists and antagonists are described, as are devices coated with beta-2 adrenergic receptor agonists.Type: ApplicationFiled: April 10, 2006Publication date: August 26, 2010Inventors: Roslyn Rivkah Isseroff, Christine E. Pullar
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Publication number: 20100210524Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.Type: ApplicationFiled: July 21, 2008Publication date: August 19, 2010Inventors: Theresa Apelqvist, Joakim Löfstedt, Thomas Norin, Mattias Wennerstål, Xiongyu Wu, Lars Hagberg
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Publication number: 20100210693Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: May 3, 2010Publication date: August 19, 2010Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
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Patent number: 7776909Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2-membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: February 4, 2004Date of Patent: August 17, 2010Assignee: Dompe Pha.R.Ma S.p.A.Inventors: Alessio Moriconi, Marcello Allegretti, Riccardo Bertini, Cinzia Bizzarri, Maria Candida Cesta, Francesco Colotta
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Publication number: 20100204333Abstract: Pharmaceutical modified release dosage form comprising at least one cyclooxygenase enzyme inhibitor or its pharmaceutically acceptable salts, esters, prodrugs, solvates, hydrates, or derivatives thereof as active agent, with a pharmaceutically acceptable carrier for controlling the release of the cyclooxygenase enzyme inhibitor is provided. The dosage form preferably provides a release of not more than about 60% of the cyclooxygenase enzyme inhibitor in 1 hour and not less than about 75% of the cyclooxygenase enzyme inhibitor after 12 hours when tested in accordance with the dissolution method (I) described herein employing Distilled water with 2.0% Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (II) described herein employing pH 7.0 Phosphate buffer with 2.0% Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (III) described herein employing 0.001 N Hydrochloric acid with 1.Type: ApplicationFiled: July 19, 2006Publication date: August 12, 2010Applicant: PANACEA BIOTEC LTD.Inventors: Rajesh Jain, Kour Chand Jindal, Sukhjeet Singh, Munish Talwar
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Patent number: 7767715Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: April 8, 2009Date of Patent: August 3, 2010Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
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Patent number: 7763657Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.Type: GrantFiled: March 15, 2006Date of Patent: July 27, 2010Assignee: Amorepacific CorporationInventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-Il Kim, Byoung Young Woo
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Publication number: 20100168070Abstract: The invention relates to substituted 1,2-ethylenediamines of general formula (I), wherein the radicals R1-R13, A, B, L and i are as defined in the description and in the claims. The invention also relates to the use thereof for treating Alzheimer's disease (AD) and similar diseases.Type: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Inventors: Niklas Heine, Klaus Fuchs, Christian Eickmeier, Stefan Peters, Cornelia Dorner-Ciossek, Sandra Handschuh, Herbert Nar, Klaus Klinder
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Publication number: 20100168089Abstract: An in vitro method of screening for candidate compounds for the preventive or curative treatment of acne entails determination of the ability of a compound to inhibit the expression or the activity of TACE, and also to the administration of inhibitors of the expression or of the activity of this enzyme, in the treatment of acne.Type: ApplicationFiled: December 17, 2009Publication date: July 1, 2010Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: JÉRÔME AUBERT, ISABELLE CARLAVAN, JOHANNES VOEGEL
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Publication number: 20100168108Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.Type: ApplicationFiled: January 18, 2010Publication date: July 1, 2010Applicant: Adolor CorporationInventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
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Patent number: RE42889Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: April 23, 2007Date of Patent: November 1, 2011Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw