The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
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Publication number: 20130237538Abstract: The present invention relates to compounds of formulae I and II wherein the variables are as defined herein. These compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: March 12, 2013Publication date: September 12, 2013Applicant: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
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Patent number: 8518972Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: GrantFiled: February 10, 2011Date of Patent: August 27, 2013Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20130217705Abstract: The present invention provides, for example, the following compound: wherein ring Z is pyridine or a carbocycle, each of which is substituted or unsubstituted, ring A is a carbocycle or a heterocycle, each of which is substituted or unsubstituted, R1 is substituted or unsubstituted alkyl or the like, R2a, R2b, R4a and R4b are each independently hydrogen or substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.Type: ApplicationFiled: October 27, 2011Publication date: August 22, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Yasunori Mitsuoka, Yuuji Kooriyama
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Patent number: 8513420Abstract: The present invention relates to new compounds having an amino-naphthyridine group. In particular, the present invention relates to new compounds, its stereoisomers and pharmaceutically acceptable salts or solvates thereof having a first unit (moiety) selected from the group of a phenyl derivative, a biphenyl derivative or a diphenyl alkane derivative and at least one amino-naphthyridine group linked with the first unit via a linking group. In specific embodiments, the present invention relates to compounds having a phenyl derivative unit and three amino-naphthyridine groups bound to the phenyl derivative unit via a linking group as well as salts or solvates thereof, in particular, pharmaceutically acceptable salts or solvates thereof. Further, the present invention relates to pharmaceutical compositions comprising said compounds. The compounds are particularly useful for treating or preventing infections, like viral infections.Type: GrantFiled: March 18, 2008Date of Patent: August 20, 2013Inventor: Monika Mazik
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Publication number: 20130210818Abstract: New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: February 14, 2012Publication date: August 15, 2013Inventors: Zilin Huang, Jeff Jin, Timothy Machajewski, William R. Antonios-McCrea, Maureen McKenna, Daniel Poon, Paul A. Renhowe, Martin Sendzik, Cynthia Shafer, Aaron Smith, Yongjin Xu, Qiong Zhang, Zheng Chen
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Publication number: 20130210857Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: February 13, 2013Publication date: August 15, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8507443Abstract: The present invention is an antineoplastic agent characterized by including at least one of taxol and taxol derivatives and a protein which is a mutant of diphtheria toxin, having an activity to inhibit a binding between HB-EGF and EGFR and substantially not having a toxicity of diphtheria toxin as active ingredients.Type: GrantFiled: August 19, 2005Date of Patent: August 13, 2013Assignee: The Research Foundation for Microbial Diseases of Osaka UniversityInventors: Eisuke Mekada, Shingo Miyamoto
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Patent number: 8507682Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity, wherein these compounds selected from the group consisting of wherein A, B, C, D, X, Y, Z and R3 are defined in the specification. Said compounds are useful for treating a disease or condition of a mammal selected from the group consisting of ocular diseases; systemic vascular barrier related diseases; allergies and other inflammatory diseases; cardiac diseases or conditions; fibrosis; pain and wounds.Type: GrantFiled: September 28, 2010Date of Patent: August 13, 2013Assignee: Allergan, Inc.Inventors: Wenkiu K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
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Publication number: 20130203756Abstract: The present invention is directed to isoindolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: ApplicationFiled: October 24, 2011Publication date: August 8, 2013Inventors: Jamie L. Bunda, Christopher D. Cox, Vadim Y. Dudkin, Hannah D. Fiji, Michael J. Kelly, Mark E. Layton, Joseph E. Pero, William D. Shipe, Justin T. Sheen
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Publication number: 20130184253Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 19, 2012Publication date: July 18, 2013Applicant: NOVARTIS AGInventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian Hurley, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
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Publication number: 20130178458Abstract: In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: December 3, 2012Publication date: July 11, 2013Applicant: Vanderbilt UniversityInventor: Vanderbilt University
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Patent number: 8481738Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: November 10, 2011Date of Patent: July 9, 2013Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Richard Lowe, Willy Moree, Nicole Smith, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8481534Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 25, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8476433Abstract: The present invention relates to the field of chemical-pharmaceutical industry and medicine. An agent, exhibiting the properties of a cognitive function promoter, was selected from 1,3-dimethyl-5-[(4-pyridylamino)methylene]barbituric acid and 4-amino-1-(3-nitro-2-oxo-1-pheny-1,2-dihydro-1,6-naphthyridin-5-yl)pyridinium chloride. The compounds, that are proposed as agents, exhibit potent biological activity.Type: GrantFiled: April 28, 2011Date of Patent: July 2, 2013Assignee: UnikormInventors: Valery Aleksandrovich Parshin, Tatyana Vasilyevna Golovko, Nelya Zarifovna Tugusheva, Marina Igorevna Medvedeva, Vladimir Vladimirovich Granik
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Publication number: 20130165473Abstract: The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient.Type: ApplicationFiled: December 17, 2012Publication date: June 27, 2013Applicant: ASTRAZENECA ABInventor: AstraZeneca AB
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Patent number: 8471026Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: August 25, 2011Date of Patent: June 25, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20130150339Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.Type: ApplicationFiled: December 6, 2012Publication date: June 13, 2013Applicant: Amgen Inc.Inventor: Amgen Inc.
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Patent number: 8461178Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumors and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.Type: GrantFiled: November 24, 2010Date of Patent: June 11, 2013Assignee: Aeterna Zentaris GmbHInventors: Tilmann Schuster, Matthias Gerlach, Irene Seipelt, Emmanuel Polymeropoulos, Gilbert Mueller, Eckhard Guenther, Pascal Marchand, Julien Defaux
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Patent number: 8461179Abstract: The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.Type: GrantFiled: June 7, 2012Date of Patent: June 11, 2013Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Michael D. Kaufman, Peter A. Petillo
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Patent number: 8461329Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.Type: GrantFiled: December 25, 2009Date of Patent: June 11, 2013Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Tetsuo Takayama, Hajime Asanuma, Daisuke Wakasugi, Rie Nishikawa, Yoshinori Sekiguchi, Madoka Kawamura, Naoya Ono, Tetsuya Yabuuchi, Takahiro Oi, Yusuke Oka, Shoichi Kuroda, Fumito Uneuchi, Takeshi Koami
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Patent number: 8461083Abstract: The present invention relates to novel herbicidal [1,8]-naphthyridines of Formula (Ia) or (Ib), or an agronomically acceptable salt of said compound wherein R2, R3, R4, R5, R6, R7, R8, n, m, X and Q are as defined herein. The invention further relates to processes and intermediates for the preparation of the [1,8]-naphthyridines, to compositions which comprise the herbicidal compounds, and to their use for controlling weeds, in particular in crops of useful plants.Type: GrantFiled: March 16, 2009Date of Patent: June 11, 2013Assignee: Syngenta LimitedInventors: Glynn Mitchell, David Phillip Bacon, Ian Henry Aspinall, Emma Briggs, Alaric James Avery, James Alan Morris, Claire Janet Russell, Roger Salmon
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Publication number: 20130143899Abstract: The invention provides a novel class of compounds of Formula (I) (wherein A, Y, R2, R3, R4 and R5 are defined in the summary of the invention), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.Type: ApplicationFiled: February 4, 2011Publication date: June 6, 2013Inventors: Shifeng Pan, John E. Tellew, Yongqin Wan, Yongping Xie, Xing Wang, Xia Wang, Shenlin Huang, Zuosheng Liu, Qiong Zhang
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Publication number: 20130131342Abstract: The present invention relates to the field of chemical-pharmaceutical industry and medicine. An agent, exhibiting the properties of a cognitive function promoter, was selected from 1,3-dimethyl-5-[(4-pyridylamino)methylene]barbituric acid and 4-amino-1-(3 -nitro-2-oxo-1-pheny-1 ,2-dihydro-1 ,6-naphthyridin-5-yl)pyridinium chloride. The compounds, that are proposed as agents, exhibit potent biological activity.Type: ApplicationFiled: April 28, 2011Publication date: May 23, 2013Applicant: UNIKORMInventors: Valery Aleksandrovich Parshin, Tatyana Vasilyevna Golovko, Nelya Zarifovna Tugusheva, Marina Igorevna Medvedeva, Vladimir Vladimirovich Granik
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Publication number: 20130123244Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Applicant: JANSSEN R&D IRELANDInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20130115193Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: November 8, 2012Publication date: May 9, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8436011Abstract: The present invention relates to pyridopyridone derivatives of formula (I): in which the variables are as defined herein, to their preparation and to their therapeutic use as inhibitors of the kinase activity of PDGF (platelet-derived growth factor) ligand receptors and possibly of FLT3 (fms-like tyrosine kinase receptor) ligand receptors.Type: GrantFiled: January 6, 2011Date of Patent: May 7, 2013Assignee: SanofiInventors: Patrice Bellevergue, Gilbert Lassalle, Gary McCort, Valerie Martin, Pierre Savi, Cecile Volle-Challier
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Patent number: 8436180Abstract: The present application relates to novel substituted 4-aryl-1,4-dihydro-1,6-naphthyridine-3-carboxamides, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: GrantFiled: February 19, 2008Date of Patent: May 7, 2013Assignee: Bayer Intellectual Property GmbHInventors: Lars Bärfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche, Martina Klein, Klaus Münter, Barbara Albrecht-Küpper, Elke Hartmann
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Patent number: 8431594Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed.Type: GrantFiled: July 2, 2009Date of Patent: April 30, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
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Patent number: 8431039Abstract: The present invention relates to compounds represented by the following Formula Ia, in which each R1-R6 can in each case be independently selected from hydrogen or hydrocarbyl (e.g., methyl); R7 is a multivalent linking group, such as L1 is a divalent linking group, such as a bond or divalent optionally substituted hydrocarbyl; each L2 independently represents a flexible segment, such as divalent linear or branched C1-C25 alkyl; each L3 independently represents a rigid segment including, for example, optionally substituted phenylen-1,4-diyl groups; t is from 1 to 4; m and p are each independently from 0 to 4 for each t, provided that the sum of m and p is at least 1 for each t; and E can be hydrogen or optionally substituted hydrocarbyl. The present invention also relates to compositions, such as liquid crystal compositions, and articles, such as optical elements, that include the compound represented by Formula Ia.Type: GrantFiled: August 8, 2011Date of Patent: April 30, 2013Assignee: Transitions Optical, Inc.Inventors: Xiao-Man Dai, Ruisong Xu, Meng He, Anil Kumar, Rachael L. Yoest, Chenguang Li
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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: 20130102611Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.Type: ApplicationFiled: July 14, 2011Publication date: April 25, 2013Applicant: Novartis AGInventors: Steven John Charlton, Catherine Leblanc, Stephen Carl McKeown
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Publication number: 20130096122Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.Type: ApplicationFiled: December 6, 2012Publication date: April 18, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Patent number: 8415375Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy; each of U and V represents CH and W represents CH or N, or U represents N, V represents CH and W represents N, or each of U and V represents N and W represents CH; R2 represents hydrogen or fluorine when W represents CH or R2 represents hydrogen when W represents N; A represents O or CH2; Y represents CH or N; Q represents O or S; and n represents 0 or 1; and salts of such compounds.Type: GrantFiled: April 8, 2010Date of Patent: April 9, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
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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: 8410109Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: GrantFiled: July 28, 2006Date of Patent: April 2, 2013Assignee: Resverlogix Corp.Inventors: Norman C. W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Patent number: 8410273Abstract: Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:Type: GrantFiled: October 5, 2011Date of Patent: April 2, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Satoru Naito
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Publication number: 20130079365Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 A3 and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds of the present invention are useful as inhibitors of aldosterone synthase. The compounds may be used, for example, in the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: September 14, 2012Publication date: March 28, 2013Inventors: Johannes Aebi, Kurt Amrein, Serena Maria Fantasia, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Michelangelo Scalone, Xuefei Tan, Mingwei Zhou
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Publication number: 20130072494Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Publication number: 20130072679Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: September 13, 2012Publication date: March 21, 2013Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Henner Knust, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Mingwei Zhou
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Publication number: 20130065760Abstract: Substituted pyridines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.Type: ApplicationFiled: March 22, 2011Publication date: March 14, 2013Applicant: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Hans Wolfgang Hoeffken, Thomas Mietzner, William Karl Moberg
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Publication number: 20130053348Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: September 12, 2012Publication date: February 28, 2013Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Sing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
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Publication number: 20130040984Abstract: The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: GLAXO GROUP LIMITEDInventors: Francis Louis Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander George Steven Preston, David Matthew Wilson
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Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
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Publication number: 20130029994Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Inventors: Santosh C. Sinha, Liming Wang, Ken Chow, Mohammed I. Dibas, Michael E. Garst
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Patent number: 8357684Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: March 2, 2011Date of Patent: January 22, 2013Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
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Patent number: 8357688Abstract: Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.Type: GrantFiled: March 4, 2010Date of Patent: January 22, 2013Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
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Publication number: 20130018046Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Patent number: 8349830Abstract: The present invention is directed to aryl aminopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: October 26, 2010Date of Patent: January 8, 2013Assignee: Merck Sharp & DohmeInventors: Michael J. Breslin, Christopher D. Cox, Izzat T. Raheem