Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/338)
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Publication number: 20140057891Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20140057920Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Patent number: 8658635Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: GrantFiled: June 3, 2009Date of Patent: February 25, 2014Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
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Patent number: 8658799Abstract: The present invention relates to a new process for the preparation of crystal modifications for use in the preparation of esomeprazole sodium salt. Further, the present invention also relates to the use of the new crystal modifications for the treatment of gastrointestinal disorders, pharmaceutical compositions containing them as well as the crystal modifications, as such.Type: GrantFiled: June 20, 2005Date of Patent: February 25, 2014Assignee: Astrazeneca ABInventors: Martin Bohlin, Ursula Noreland
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Publication number: 20140051728Abstract: The invention relates to a new use of dabigatran etexilate of formula I optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations which may be used for this purpose.Type: ApplicationFiled: October 28, 2013Publication date: February 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joanne VAN RYN, Andreas CLEMENS
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Publication number: 20140051660Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
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Publication number: 20140051686Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 11, 2013Publication date: February 20, 2014Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20140051700Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.Type: ApplicationFiled: August 20, 2012Publication date: February 20, 2014Inventor: Masashi Yanagisawa
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Publication number: 20140051689Abstract: Compounds of formula (I), and their use as in the treatment of infections involving viruses of the Pneumovirinae sub-family (RSV) are disclosed. In the formula ring (A) may be phenyl, pyridyl etc., (B-C) may be CH2—CH2 etc., (R1) may be phenyl and substituted forms thereof, (R2) may be assorted substituents.Type: ApplicationFiled: October 24, 2013Publication date: February 20, 2014Applicant: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Vanessa Anne Sanford, John Nicholas Lambert, Chin Yu Lim, Alistair George Draffan, Roland Henry Nearn, Jeffrey Peter Mitchell
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Publication number: 20140051688Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui
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Patent number: 8653070Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: December 14, 2010Date of Patent: February 18, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Yat Sun Or
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Publication number: 20140045778Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: ApplicationFiled: January 3, 2013Publication date: February 13, 2014Applicants: THE KITASATO INSTITUTE, MEIJI SEIKA PHARMA CO., LTD.Inventors: MEIJI SEIKA PHARMA CO., LTD., THE KITASATO INSTITUTE
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Publication number: 20140045829Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
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Publication number: 20140045811Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
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Publication number: 20140045897Abstract: Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a furazanobenzimidazole compound of general formula (I).Type: ApplicationFiled: January 19, 2012Publication date: February 13, 2014Inventors: Heidi Alexandra Lane, Felix Bachmann, Madlaina Breuleux, Michael Boutros, Daniel Gilbert, Xian Zhang
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Publication number: 20140045898Abstract: A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has no risk factors for major bleeding events, the method comprising administering to the patient a dosage of >150 mg b.i.d. to 300 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 6, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Paul Anthony REILLY
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Publication number: 20140045860Abstract: The invention relates to a compound of Formula I or a pharmaceutically acceptable ester, salt, prodrug or metabolite thereof;Type: ApplicationFiled: August 13, 2013Publication date: February 13, 2014Applicants: NEW YORK UNIVERSITY, THE BROAD INSTITUTE, INC.Inventors: Leigh C. Carmody, Ana Rodriguez, Esther Bettiol, Michelle Palmer, Andrew Germain, Benito Munoz, Sivaraman Dandapani, Michael Foley
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Publication number: 20140045899Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: October 24, 2013Publication date: February 13, 2014Applicant: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Publication number: 20140045815Abstract: 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 5, 2013Publication date: February 13, 2014Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: 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: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Publication number: 20140039004Abstract: The development of agents for gastroesophageal reflux disease, in which existing treatment is not effective, is strongly demanded. An object of the present invention is to provide an agent for preventing or relapse-preventing, treating or ameliorating such gastroesophageal reflux disease. 4-[({6-[Isobutyl(1,3-thiazol-2-ylsulfonyl)amino]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]-3-methyl benzoic acid, a salt thereof or a prodrug thereof is effective in the prevention or relapse prevention, treatment or amelioration of gastroesophageal reflux disease.Type: ApplicationFiled: July 26, 2013Publication date: February 6, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiroki OKADA, Takashi KONEMURA
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Publication number: 20140038969Abstract: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Inventors: Wu Yang, James R. Corte, Paul J. Gilligan, Donald J.P. Pinto, William R. Ewing, Yufeng Wang
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Publication number: 20140038942Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.Type: ApplicationFiled: February 10, 2012Publication date: February 6, 2014Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
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Publication number: 20140038944Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: October 4, 2013Publication date: February 6, 2014Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts, Nicholas Sean Flinn
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Publication number: 20140039010Abstract: Disclosed are a method for treating an aging-related disease and a method for screening a therapeutic agent for an aging-related disease. The method for treating an aging-related disease includes administering to a subject a progerin expression inhibitor as an active ingredient. The method for screening a therapeutic agent for an aging-related disease includes selecting a candidate drug inhibitory of progerin expression.Type: ApplicationFiled: March 19, 2012Publication date: February 6, 2014Applicant: Pusan National University Industry-University Cooperation FoundationInventors: Bum Joon Park, Nam Chul Ha, Gyu Yong Song, Ji Hyun Lee, Su Jin Lee, Youn Sang Jung
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Publication number: 20140039011Abstract: The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: October 8, 2013Publication date: February 6, 2014Applicant: SANOFIInventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
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Publication number: 20140030328Abstract: Dual release oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders.Type: ApplicationFiled: September 23, 2013Publication date: January 30, 2014Applicant: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETIInventors: Umit Cifter, Ali Turkyilmaz, Ibrahim Murat Uzer, Alper Terkinli, Levent Oner
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Publication number: 20140031317Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: October 1, 2013Publication date: January 30, 2014Applicant: Janssen Pharmaceutica, NVInventors: Vernon C Alford, JR., James C. Lanter, Raymond A. Ng
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Publication number: 20140030336Abstract: A pharmaceutical composition for the treatment or acute disorders is described. The composition comprises an essentially water-free, ordered mixture of at least one pharmaceutically active agent in the form of microparticles which are adhered to the surfaces of carrier particles which are substantially larger than the particles of the active agent or agents, and are essentially water-soluble, in combination with the bioadhesion and/or mucoadhesion promoting agent. The invention also relates to a method for preparing the composition and to the use of the composition for the treatment of acute disorders.Type: ApplicationFiled: July 30, 2013Publication date: January 30, 2014Applicant: Orexo ABInventors: Anders Pettersson, Christer Nystrom
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Patent number: 8637551Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: July 6, 2010Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme B.V.Inventor: Simon James Anthony Grove
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Patent number: 8637513Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: GrantFiled: October 23, 2008Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
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Patent number: 8637676Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: June 4, 2008Date of Patent: January 28, 2014Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20140024681Abstract: A compound having the structural formula (I) and pharmaceutically acceptable salt and/or hydrates thereof, (I) wherein Y is an arylester or an C1-C8 alkylaryl ester, selected from the group consisting of: benzene, toluene, xylene, benzoic acid, benzoate, nicotinate, isonicotinate and halobenzene, which can be unsubstituted or substituted with at least one nitric oxide releasing group; and/or at least one of hydroxide, —Cl, —Br, a C1-C8 alkyl, benzyl, a C1-C8 alkoxy, benzyloxy, —NHC(O)R, —NH2, —NO2—ONO2, —(CH2)nONO2, —OC(O)[(CH2)n]cyclicONO2, —OCOArONO2, —OCOAr(CH2)nONO2 or a C1-C5 haloalkyl ester, wherein R is a C1-C8 alkyl or a C1-C8 alkoxy group, n=1-8 and m=3-10, to produce a super-aspirin effect.Type: ApplicationFiled: January 20, 2012Publication date: January 23, 2014Applicants: The Provost,Fellowws, Foudation Scholars, and the Other Members of Board, of the College of the Holy, Solvotrin Therapeutics LtdInventors: John Francis Gilmer, Mark Ledwidge, Pat O'lynn, Shona Harmon, Mark Radomski, Carlos Medina Martin
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Publication number: 20140023709Abstract: Oral tablet compositions of dexlansoprazole or pharmaceutically acceptable salts or hydrated forms thereof having a gradual release and processes for the manufacture of the tablet composition and its use in the treatment of gastrointestinal disorders.Type: ApplicationFiled: September 23, 2013Publication date: January 23, 2014Applicant: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETIInventors: Umit Cifter, Ali Turkyilmaz, Ibrahim Murat Uzer, Alper Terkinli, Levent Oner
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Publication number: 20140024659Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.Type: ApplicationFiled: April 5, 2012Publication date: January 23, 2014Applicant: BASF SEInventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
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Publication number: 20140023706Abstract: A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.Type: ApplicationFiled: September 19, 2013Publication date: January 23, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marinus Jacobus Verwijs, Rossitza Gueroguieva Alargova, Ritu Rohit Kaushik, Irina Nikolaevna Kadiyala, Christopher Young
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Publication number: 20140024583Abstract: 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: July 15, 2013Publication date: January 23, 2014Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Patent number: 8633311Abstract: Described herein are methods and compositions for killing or preventing the growth of microbes. It has been discovered that a class of porphyrins can kill or prevent the growth of microbes. The porphyrins can be used in a number of different applications where microbes grow.Type: GrantFiled: July 29, 2009Date of Patent: January 21, 2014Assignee: Frontier Scientific, Inc.Inventors: Jerry C. Bommer, Glenn Prestwich, Charles Testa
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Publication number: 20140018368Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.Type: ApplicationFiled: July 1, 2013Publication date: January 16, 2014Applicants: Genetech, Inc., Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Publication number: 20140018367Abstract: The present application includes methods for using IL-8 as a biomarker for, e.g., tumor size, for example, during course of treatment with an anti-cancer agent such as an ERK inhibitor.Type: ApplicationFiled: September 25, 2013Publication date: January 16, 2014Inventors: Ahmed A. Samatar, Brian Long, Priva Dayananth, Diane Levitan, Marsha Smith
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Publication number: 20140018356Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: ApplicationFiled: April 4, 2013Publication date: January 16, 2014Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20140018326Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
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Patent number: 8629284Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.Type: GrantFiled: October 27, 2009Date of Patent: January 14, 2014Assignee: Syngenta Crop Protection, LLCInventors: Ottmar Franz Hueter, Peter Renold, Werner Zambach, Thomas Pitterna, Peter Maienfisch
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Patent number: 8629147Abstract: The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.Type: GrantFiled: November 2, 2006Date of Patent: January 14, 2014Assignee: ChemBridge CorporationInventors: Alexey Vyacheslavovich Anikin, Vidyasagar Reddy Gantla, Vlad Edward Gregor, Luyong Jiang, Yahua Liu, Danny Peter Claude McGee, Charles Chamchoumis Mikel, Jason Conrad Pickens, Thomas Roy Webb, Zheng Yan, Tong Zhu, Aleksander Kadushkin, Sergey Sviridov, Sergey Zozulya, Alexander Chucholowski, Douglas Eric McGrath
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Publication number: 20140011822Abstract: This document provides methods and materials for reducing venous stenosis formation of an arteriovenous fistula or graft. For example, methods and materials for using VEGF inhibitors to reduce venous stenosis formation of arteriovenous fistulas or grafts are provided.Type: ApplicationFiled: March 16, 2012Publication date: January 9, 2014Inventor: Sanjay Misra
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Publication number: 20140011846Abstract: The present invention relates to a substantially crystalline and free solid state form of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Form I), pharmaceutical compositions thereof, and methods of treatment therewith.Type: ApplicationFiled: July 2, 2013Publication date: January 9, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Ali Keshavarz-Shokri, Beili Zhang, Mariusz Krawiec
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
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Publication number: 20140005150Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 20, 2013Publication date: January 2, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
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Publication number: 20140005227Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 8, 2011Publication date: January 2, 2014Applicant: ABBVIE Deutschland GmbH & Co. KGInventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Moller, Wilfried Hornberger, Yanbin Lao, Gisela Backfisch, Marjoleen Nijsen