Plural Ring Nitrogens In The Bicyclo Ring System Patents (Class 514/234.5)
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Patent number: 8450315Abstract: Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: October 29, 2010Date of Patent: May 28, 2013Assignees: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Georgette Castanedo, Richard Goldsmith, Janet Gunzner, Tim Heffron, Kimberly Malesky, Simon Mathieu, Alan Olivero, Daniel P. Sutherlin, Vickie Tsui, Shumei Wang, Christian Wiesmann, Bing-Yan Zhu, Jennafer Dotson, Adrian Folkes, Stephen Shuttleworth, Sally Oxenford, Tim Hancox, Tracy Bayliss
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Publication number: 20130131059Abstract: This invention is directed to prodrugs of rho kinase (ROCK) inhibitors. These prodrugs are in general the ester or the amide derivatives of the parent compounds. These prodrugs are often weak inhibitors of ROCK, but their parent compounds have good activities. Upon instillation into the eyes, the ester or the amide group of these prodrugs is rapidly hydrolyzed into alcohol, amine, or acid, and the prodrugs are converted into the active base compounds. The prodrugs of ROCK inhibitors provide several advantages such as delivery of higher concentrations of the active species into the target site and reduction of ocular discomfort. The invention is also directed to a method of treating ophthalmic diseases such as glaucoma, allergic conjunctivitis, macular edema, macular degeneration, and blepharitis, by administering an effective amount of a ROCK prodrug compound of Formula I to the eyes of the patient in need of.Type: ApplicationFiled: January 17, 2013Publication date: May 23, 2013Applicant: INSPIRE PHARMACEUTICALS, INC.Inventor: Inspire Pharmaceuticals, Inc.
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Publication number: 20130131047Abstract: The present invention relates to inhibitors of ROCK1 and ROCK2 and methods of modulating the pharmacokinetic and/or pharmacodynamic properties of such compounds. Also provided are methods of inhibiting ROCK1 and or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: December 14, 2012Publication date: May 23, 2013Applicant: SURFACE LOGIX, INC.Inventor: SURFACE LOGIX, INC.
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Publication number: 20130121996Abstract: Six new mutations were found in exon 19 of the EGFR gene, the exon that is often mutated in tumors. The invention comprises methods of detecting the mutations, methods of prognosis and methods of predicting response to treatment based on the presence of absence of the mutations.Type: ApplicationFiled: October 30, 2012Publication date: May 16, 2013Applicant: ROCHE MOLECULAR SYSTEMS, INC.Inventor: Roche Molecular Systems, Inc.
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Patent number: 8440662Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: GrantFiled: October 31, 2011Date of Patent: May 14, 2013Assignee: Endo Pharmaceuticals, Inc.Inventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
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Publication number: 20130116246Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: GENENTECH, INC.Inventor: Genentech, Inc.
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Publication number: 20130116240Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.Type: ApplicationFiled: September 26, 2012Publication date: May 9, 2013Applicant: JAPAN TOBACCO INC.Inventor: Japan Tobacco Inc.
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Patent number: 8435988Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.Type: GrantFiled: October 3, 2011Date of Patent: May 7, 2013Assignee: GlaxoSmithKline LLCInventors: Junya Qu, Ralph Rivero, Robert Sanchez, Rosanna Tedesco
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Patent number: 8435970Abstract: The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I?) or a salt, solvate, tautomer or N-oxide thereof, wherein R1, E, A and M are as defined in the claims.Type: GrantFiled: June 29, 2007Date of Patent: May 7, 2013Assignee: Astex Therapeutics LimitedInventors: Jayne Elizabeth Curry, Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson
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Patent number: 8435980Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.Type: GrantFiled: July 15, 2010Date of Patent: May 7, 2013Assignee: AbbVie Inc.Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Jane Gong, Magdalena Przytulinska, Douglas Steinman, James Holms, Chunqiu Lai, Gui-Dong Zhu, Keith Woods
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Publication number: 20130109688Abstract: Compounds of formulae (I) and (II): or a pharmaceutically acceptable salt thereof, wherein: R1 is a nitrogen-containing 5 to 7-membered heteroaryl or heterocycle; R2 and R3 are each independently (LQ)mY, are described. The compounds are PI3K inhibitors and are useful for the treatment of cancer and immune-inflammatory diseases.Type: ApplicationFiled: April 26, 2011Publication date: May 2, 2013Applicant: KARUS THERAPEUTICS LIMITEDInventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva
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Publication number: 20130109678Abstract: The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection).Type: ApplicationFiled: April 6, 2011Publication date: May 2, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Roger Francis Martin, Jonathan White, Pavel Lobachevsky, David Winkler, Colin Skene, Sebastian Maruccio
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Publication number: 20130102602Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.Type: ApplicationFiled: October 20, 2011Publication date: April 25, 2013Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Publication number: 20130102603Abstract: The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: May 31, 2011Publication date: April 25, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20130102587Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.Type: ApplicationFiled: March 14, 2011Publication date: April 25, 2013Applicant: PROXIMAGEN LIMITEDInventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
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Patent number: 8426405Abstract: Compounds of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof are disclosed. Also disclosed are methods of treating a viral infection in a subject by administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.Type: GrantFiled: July 2, 2009Date of Patent: April 23, 2013Assignee: Avexa LimitedInventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Vandegraaff, Lisa Jane Winfield
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Patent number: 8426404Abstract: The invention provides a novel class of compounds having Formula Ia, wherein each variable is as defined; and pharmaceutical compositions comprising such compounds and methods of using such compounds for inhibiting c-Src, FGFR3, KDR and/or Lck.Type: GrantFiled: June 30, 2006Date of Patent: April 23, 2013Assignee: Novartis AGInventors: Guobao Zhang, Pingda Ren, Xia Wang, Nathanel Gray, Taebo Sim
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Patent number: 8426604Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: February 16, 2011Date of Patent: April 23, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130096118Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: June 16, 2011Publication date: April 18, 2013Inventors: Chunjian Liu, James Lin, George V. DeLucca, Batt G. Douglas, Qingjie Liu
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Publication number: 20130096113Abstract: Provided herein are heterocyclic compounds for treatment of CSF1R, FLT3, KIT, and/or PDGFR? kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Ambit Biosciences CorporationInventor: Ambit Biosciences Corporation
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Publication number: 20130096084Abstract: The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.Type: ApplicationFiled: June 22, 2011Publication date: April 18, 2013Inventors: Yongqi Deng, Liang Zhu, Gerald W. Shipps, JR., Sie-Mun Lo, Binyuan Sun, Xiaohua Huang, Corey Bienstock, Alan B. Cooper, Xiaolei Gao, Xin Yao, Hugh Y. Zhu, Joseph M. Kelly, Sobhana Babu Boga, Abdul-Basit Alhassan, Jayaram R. Tagat, Umar Faruk Mansoor, Kevin J. Wilson, Brendan M. O'Boyle, Matthew Hersh Daniels, Adam Schell, Phieng Siliphaivanh, Christian Fischer
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Publication number: 20130096117Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): And salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: October 2, 2012Publication date: April 18, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Nigel James PARR
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Publication number: 20130090323Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 30, 2011Publication date: April 11, 2013Applicant: Amgen Inc.Inventors: Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20130090337Abstract: Provision of crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride which has a superior rennin inhibitory activity and is useful as a prophylactic or therapeutic agent for hypertension and various organ disorders caused by hypertension, and the like. Crystal of 1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-ylcarbonyl)piperidin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride having an X-ray powder diffraction pattern showing characteristic peaks at interplanar spacings (d) of around 26.43±0.2, 7.62±0.2 and 4.32±0.2 angstroms.Type: ApplicationFiled: June 15, 2011Publication date: April 11, 2013Inventor: Masato Kitayama
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Patent number: 8415333Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.Type: GrantFiled: February 24, 2010Date of Patent: April 9, 2013Assignee: Respiratorious ABInventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
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Patent number: 8415486Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: GrantFiled: May 27, 2010Date of Patent: April 9, 2013Assignee: TetraLogic Pharmaceuticals Corp.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Publication number: 20130079329Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 13, 2012Publication date: March 28, 2013Inventors: John Hood, Sunil Kumar Kc
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Publication number: 20130072484Abstract: The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: UNIVERSITY OF GEORGIA RESEARCH FOUND
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Publication number: 20130072483Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1a, R1b, R1c, B, W, R3, R4 and R5 are defined herein. In another embodiment, the invention provides compounds of general Formula II wherein A1, A2, A3, A4, R1a, R1b, R1c, R2, R4, R5, W, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions.Type: ApplicationFiled: March 22, 2012Publication date: March 21, 2013Applicant: AMGEN INC.Inventors: Wenge ZHONG, Stephen Hitchcock, Vinod F. Patel, Michael Croghan, Thomas Dineen, Daniel Horne, Matthew Kaller, Charles Kreiman, Patricia Lopez, Holger Monenschein, Thomas Nguyen, Lewis Pennington, Qiufen Xue, Bryant Yang, Yuan Cheng
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Patent number: 8399461Abstract: The present invention relates to bicyclic heterocycles of general formula the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.Type: GrantFiled: November 3, 2007Date of Patent: March 19, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Birgit Jung
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Publication number: 20130065896Abstract: Provided is a novel compound which shows an antagonistic effect against T-type calcium channels, and is useful as a pharmaceutical product. A compound represented by general formula (I), and a pharmaceutical agent containing the same, are disclosed: wherein n represents the number of nitrogen atoms contained in the 6-membered fused aromatic ring, and is 0, 1 or 2; p represents the number of nitrogen atoms contained in the 6-membered aromatic ring, and is 0 or 1; X represents an oxygen atom, —SO2— or —N(R9)—; and R1 to R5 each represents a hydrogen atom or other substituents.Type: ApplicationFiled: May 24, 2011Publication date: March 14, 2013Applicant: TOA Eiyo Ltd.Inventors: Hidekazu Masaki, Hiroshi Takasugi, Tomoyuki Nagayama, Ryutaro Shimono, Yujiro Uchino, Koichi Takayanagi
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Publication number: 20130065884Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: March 18, 2011Publication date: March 14, 2013Inventors: Zaesung No, Jaeseung Kim, Priscille Brodin, Min Jung Seo, Young Mi Kim, Jonathan Cechetto, Heekyoung Jeon, Auguste Genovesio, Saeyeon Lee, Sunhee Kang, Fanny Anne Ewann, Ji Youn Nam, Thierry Christophe, Denis Philippe Cedric Fenistein, Heo Jamung, Jang Jiyeon
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Patent number: 8394797Abstract: The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to pyrazole derivatives of formula I and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use therapy and prophylaxis, in particular for the treatment of psychosis or pain.Type: GrantFiled: September 29, 2010Date of Patent: March 12, 2013Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Jordi Corbera Arjona, Maria Rosa Cuberes-Altisent, Joerg Holenz, Daniel MartĂnez-Olmo, David Vaño-Domenech
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Publication number: 20130059833Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.Type: ApplicationFiled: August 30, 2012Publication date: March 7, 2013Inventors: Stephan Bachmann, Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Markus Rudolph
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Publication number: 20130059836Abstract: Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.Type: ApplicationFiled: May 12, 2011Publication date: March 7, 2013Inventors: Xiaodong Wang, Jing Liu, Chao Yang, Weihe Zhaug, Stephen Frye, Dmitri Kireev
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Publication number: 20130059850Abstract: The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: May 4, 2011Publication date: March 7, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Abbas M Walji, Philippe G. Nantermet, Keith P. Moore, Rachel Anne Storr, Laura Vassallo, Constantine Kreatsoulas
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Publication number: 20130053382Abstract: The instant invention provides for compounds that inhibit PDK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: April 28, 2011Publication date: February 28, 2013Inventors: Sunil Paliwal, Matthew Paul Rainka, Ang Li, May Xiaowu Jiang, Hon-chung Tsui, Ronald J. Doll
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Publication number: 20130053381Abstract: The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.Type: ApplicationFiled: May 18, 2011Publication date: February 28, 2013Inventors: Yves Auberson, David Carcache, Andreas Lerchner, Joachim Nozulak
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Publication number: 20130053341Abstract: Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are de-scribed herein. Exemplary disorders include schizophrenia and cognitive deficit.Type: ApplicationFiled: December 30, 2010Publication date: February 28, 2013Inventors: Masaki Suzuki, Kazumi Kondo, Muneaki Kurimura, Krishna Reddy Valluru, Akira Takahashi, Takeshi Kuroda, Haruka Takahashi, Tae Fukushima, Shin Miyamura, Indranath Ghosh, Abhishek Dogra, Geraldine Harriman, Amy Elder, Satoshi Shimizu, Kevin J. Hodgetts, Jason S. Newcom
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Publication number: 20130053383Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: February 28, 2013Inventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Patent number: 8383620Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: December 23, 2010Date of Patent: February 26, 2013Assignee: Genentech, Inc.Inventors: Tracy Bayliss, Irina Chuckowree, Adrian Folkes, Sally Oxenford, Nan Chi Wan, Georgette Castanedo, Richard Goldsmith, Janet Gunzner, Tim Heffron, Simon Mathieu, Alan Olivero, Steven Staben, Daniel P. Sutherlin, Bing-Yan Zhu
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Publication number: 20130045965Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
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Publication number: 20130040912Abstract: The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: UNIVERSITY OF BASELInventors: Vladimir Cmiljanovic, Natasa Cmiljanovic, Bernd Giese, Matthias Wymann
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Publication number: 20130040931Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: ApplicationFiled: January 14, 2011Publication date: February 14, 2013Applicant: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20130040933Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof. Compounds of formula I are inhibitors of Janus kinases and as such are useful for the treatment of various diseases and conditions mediated by said enzymes, such as rheumatoid arthritis, asthma, COPD, ALS, and the like.Type: ApplicationFiled: April 21, 2011Publication date: February 14, 2013Inventors: Brandon Cash, Christian Fischer, Yudith Garcia, Joon Jung, Jason Katz, June Kim, Alexey Rivkin, Adam Schell, Tony Siu, David Witter, Hua Zhou
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Publication number: 20130035337Abstract: The present invention relates to a novel fused bicyclic heteroaryl derivative or a pharmacologically acceptable salt thereof, which has an excellent hypoglycemic effect or treats and/or prevents the onset of a disorder of carbohydrate or lipid metabolism or a disease mediated by peroxisome proliferator-activated receptor (PPAR) ?. A compound having the general formula (I): wherein R1 represents a C1-C6 alkyl group, a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; R2 represents a C1-C6 alkyl group; R3 represents a C6-C10 aryl group which may be substituted with 1 to 5 group(s) independently selected from Substituent Group a, or the like; Q represents a group represented by the formula ?CH— or a nitrogen atom; and Substituent Group a represents a halogen atom, a C1-C6 alkyl group, a C1-C6 hydroxyalkyl group, and the like, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: March 13, 2012Publication date: February 7, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kousei Shimada, Yoshiyuki Onishi, Makoto Mori, Eri Tokumaru
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Publication number: 20130029985Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: October 2, 2012Publication date: January 31, 2013Inventors: Julie Nicole HAMBLIN, Paul Spencer JONES, Suzanne Elaine KEELING, Joelle LE, Charlotte Jane MITCHELL, Nigel James PARR
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.