Nitrogen Attached Directly To The 1,3-thiazole Ring By Nonionic Bonding Patents (Class 546/270.7)
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Publication number: 20130040951Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.Type: ApplicationFiled: August 4, 2010Publication date: February 14, 2013Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20130039870Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formulaType: ApplicationFiled: February 21, 2011Publication date: February 14, 2013Applicant: Beiersdorf AGInventors: Ludger Kolbe, Cathrin Scherner
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Patent number: 8354540Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: GrantFiled: July 27, 2011Date of Patent: January 15, 2013Assignee: Array BioPharma Inc.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Ronald Jay Hinklin, Ajay Singh
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Publication number: 20120329811Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: September 6, 2012Publication date: December 27, 2012Inventors: Christelle Boléa, Sylvain Celanire
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Publication number: 20120316188Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 14, 2011Publication date: December 13, 2012Inventor: Christelle Boléa
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Publication number: 20120309791Abstract: The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins.Type: ApplicationFiled: July 25, 2012Publication date: December 6, 2012Applicant: AC IMMUNE SAInventors: Wolfgang FROESTL, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas MUHS, Maria Pihlgren Bosch
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Publication number: 20120302569Abstract: This invention relates to phenyl thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Paul Francis JACKSON, Kristi Anne Leonard, Joseph Kent Barbay, Aihua Wang, Brett Andrew Tounge, Yan Zhang, Umar S.M. Maharoof
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Patent number: 8318778Abstract: This application relates to novel urea glucokinase activators and use of the compounds of the invention for preparation of a medicament for the treatment of various diseases, e.g. for the treatment of type 2 diabetes. Further encompassed is a pharmaceutical composition comprising a compound according to the invention and a process for preparing such.Type: GrantFiled: January 8, 2008Date of Patent: November 27, 2012Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Per Vedsø, Lise Brown Christiansen
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Publication number: 20120289698Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 13, 2012Publication date: November 15, 2012Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20120289551Abstract: Mineralocorticoid receptor antagonists, of which the following is exemplary.Type: ApplicationFiled: November 7, 2011Publication date: November 15, 2012Inventors: Xin GUO, Stephen J. BOYER, Di WU, Frank WU
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Publication number: 20120283268Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: June 15, 2012Publication date: November 8, 2012Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
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Patent number: 8304412Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: November 17, 2007Date of Patent: November 6, 2012Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
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Patent number: 8304437Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.Type: GrantFiled: March 25, 2011Date of Patent: November 6, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Publication number: 20120277242Abstract: Provided are compounds of Formula (I): wherein R2, R3, R13, L and D2 are as defined in the specification, which are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: June 11, 2012Publication date: November 1, 2012Applicant: ARRAY BIOPHARMA, INC.Inventors: Thomas Daniel AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Jay Bradford FELL, John P. FISCHER, Indrani W. GUNAWARDANA, Ronald Jay HINKLIN, Ajay SINGH, Timothy M. TURNER, Eli M. WALLACE
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Patent number: 8293919Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.Type: GrantFiled: July 23, 2008Date of Patent: October 23, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120264218Abstract: The slow kinetics and low efficiency of reprogramming methods to generate human induced pluripotent stem cells (iPSCs) impose major limitations on their utility in biomedical applications. Here we describe a chemical approach that dramatically improves (>200 fold) the efficiency of iPSC generation from human fibroblasts, within seven days of treatment. This will provide a basis for developing safer, more efficient, non-viral methods for reprogramming human somatic cells.Type: ApplicationFiled: October 15, 2010Publication date: October 18, 2012Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Tongxiang Lin, Sheng Ding
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Publication number: 20120264704Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: October 26, 2007Publication date: October 18, 2012Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
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Patent number: 8288380Abstract: A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1—W2 represents CH—CH, or Y represents a single bond and W1—W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.Type: GrantFiled: April 17, 2012Date of Patent: October 16, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Patent number: 8268811Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: October 30, 2009Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals Inc.Inventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Publication number: 20120202750Abstract: 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: ApplicationFiled: January 23, 2012Publication date: August 9, 2012Applicant: 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: 20120196864Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.Type: ApplicationFiled: August 4, 2010Publication date: August 2, 2012Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20120189579Abstract: The present invention concerns a substituted pyrrolidinone of the following formula I or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: (I), for the treatment of hepatitis C.Type: ApplicationFiled: July 9, 2010Publication date: July 26, 2012Applicant: VIVALISInventors: Amaya Berecibar, Philippe Guedat, Isabelle Valarche, Céline Mohamed-Arab, Christophe Matt
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Publication number: 20120172374Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
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Publication number: 20120165335Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Patent number: 8198271Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyleType: GrantFiled: May 25, 2009Date of Patent: June 12, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20120142677Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
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Patent number: 8178688Abstract: The present invention relates to novel benzamidine derivatives, process for the preparation thereof and pharmaceutical composition comprising the same. The novel benzamidine derivatives of the present invention are useful for the prevention and treatment of osteoporosis, bone fractures and allergic inflammatory diseases.Type: GrantFiled: August 4, 2005Date of Patent: May 15, 2012Assignee: Dong Wha Pharmaceutical Co., Ltd.Inventors: Jin Soo Lee, Seok Hoon Ahn, Young Goo Jin, Sang Mi Jin, Whui-Jung Park, Sae Kwang Ku, Yun Ha Hwang, Pan Soo Kim, Sun Shin Yi, Jei Man Ryu
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Publication number: 20120115870Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.Type: ApplicationFiled: January 11, 2012Publication date: May 10, 2012Applicant: ALCON RESEARCH, LTD.Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shepard, Mark R. Hellberg, Peter G. Klimko, Abbot F. Clark
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Patent number: 8168794Abstract: The present invention relates to new compounds of Formulas I and II, their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, in the inhibition of Pim kinase activity and/or the prophylaxis or treatment of cancer.Type: GrantFiled: February 26, 2009Date of Patent: May 1, 2012Assignee: Novartis AGInventors: Matthew Burger, Jiong Lan, Mika Lindvall, Gisele Nishiguchi, Michelle Tetalman
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Publication number: 20120101101Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: April 28, 2010Publication date: April 26, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda
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Patent number: 8163779Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: GrantFiled: December 17, 2007Date of Patent: April 24, 2012Assignee: Takeda San Diego, Inc.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Patent number: 8153804Abstract: Aryl pyridines, compositions comprising them, and methods of their use for the treatment, prevention and management of a variety of diseases and disorders are disclosed.Type: GrantFiled: July 31, 2006Date of Patent: April 10, 2012Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David J. Augeri, James E. Tarver, Jr., Qinghong Fu, Michael Victor Voronkov, Doan Hackley, Michael E. Mertzman, Marianne Carlsen
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Patent number: 8148380Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: GrantFiled: July 23, 2008Date of Patent: April 3, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120053210Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2011Publication date: March 1, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Patent number: 8124610Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: GrantFiled: July 14, 2008Date of Patent: February 28, 2012Assignee: Icagen Inc.Inventors: Alan Bradley Fulp, Matthew Scott Johnson, Christopher John Markworth, Brian Edward Marron, Darrick Conway Seconi, Christopher William West, Xiaodong Wang, Shulan Zhou
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Publication number: 20120029029Abstract: The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11?HSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. 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, disorders, or conditions in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.Type: ApplicationFiled: July 25, 2011Publication date: February 2, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Dharma Rao Polisetti, Suparna Gupta
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Publication number: 20120015929Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicant: ABBOTT LABORATORIESInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
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Publication number: 20120015941Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.Type: ApplicationFiled: July 23, 2008Publication date: January 19, 2012Applicant: CRESTONE, INC.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120014906Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: September 21, 2011Publication date: January 19, 2012Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Sultan Chowdhury, Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Qi Jia, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20120010187Abstract: The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: March 16, 2010Publication date: January 12, 2012Applicant: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, JR.
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Publication number: 20120004267Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: June 30, 2011Publication date: January 5, 2012Applicant: Gilead Sciences, Inc.Inventors: Britton Corkey, Gregory Notte, Jeff Zablocki
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Publication number: 20110313152Abstract: The present invention provide a tetrazolyl oxime derivative represented by formula (1) (in formula (1), X represents a halogen atom or the like, n1 represents an integer of 0 to 5, A represents a tetrazolyl group, Het represents a group represented by formula (4) or the like, in formula (4), R represents a halogen atom or the like, n2 represents an integer of 0 to 3, Z represents a group represented by formula (a), in formula (a), R50-R53 represents a hydrogen atom or the like, n3 represents an integer of 0 to 2, n4 represents 1 or 2, n5 represents 0 or 1) or salt thereof, and a plant disease control agent containing the same as an active ingredient.Type: ApplicationFiled: February 26, 2010Publication date: December 22, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
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Publication number: 20110312939Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 28, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20110306637Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: May 20, 2011Publication date: December 15, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20110301155Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: June 18, 2008Publication date: December 8, 2011Inventors: Tsuneo Yasuma, Shigekazu Sasaki, Osamu Ujikawa, Yasufumi Miyamoto, Stephen L. Gwaltney, Sheldon Cao, Andy Jennings
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Publication number: 20110294761Abstract: The present invention relates compounds for stabilizing cells and methods of their use.Type: ApplicationFiled: December 3, 2009Publication date: December 1, 2011Applicant: The Scripps Research InstituteInventors: Yue Xu, Sheng Ding
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Publication number: 20110294858Abstract: In one aspect, the invention relates to substituted 6-methylnicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Ya Zhou, Jason Manka, Gregor McDonald, José Manuel Bartolome-Nebreda