Patents Issued in January 21, 2016
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Publication number: 20160016900Abstract: The invention generally relates to compounds that function as TP antagonists for treating thrombosis and other cardiovascular, renal, or pulmonary diseases. In some embodiments, the invention provides a compound including a substituted nitro phenoxy phenyl, a sulfonylurea, and an alkyl group. In some embodiments, the invention provides a method of treating thrombosis by administering an antithrombotic compound that preferentially binds to a thromboxane receptor, has preferential binding for either TPalpha (TP?) or TPbeta (TP?) receptor subtype.Type: ApplicationFiled: April 17, 2013Publication date: January 21, 2016Inventors: B. Therese Kinsella, Patrick Guiry, Helen Reid, Barry O'Connor
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Publication number: 20160016901Abstract: The present invention relates to an isothiocyanate production method using an organic primary amine and thiourea as starting materials; to a composition for transporting and storing an N-substituted O-substituted thiocarbamate that includes an N-substituted O-substituted thiocarbamate and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the carbamate groups of the N-substituted O-substituted thiocarbamate being in the range of 1 to 100; to a composition for transporting and storing a compound with a thioureido group that includes a compound with a thioureido group and a hydroxy compound, the equivalent weight ratio of hydroxy groups of the hydroxy compound with respect to the thioureido groups of the compound with a thioureido group being in the range of 1 to 100; and to an isothiocyanate composition containing an isothiocyanate and a compound with a specific functional group.Type: ApplicationFiled: February 28, 2014Publication date: January 21, 2016Applicant: Asahi Kasei Chemicals CorporationInventors: Masaaki SHINOHATA, Yuji KOSUGI, Nobuhisa MIYAKE
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Publication number: 20160016902Abstract: A method for preparing selenium compounds, comprising following steps of: A. hydrolyzing lignin to obtain multiple-structural polyphenolic compounds; B. reacting the multiple-structural polyphenolic compounds with at least one kind of inorganic metal base to obtain multivalent phenolic hydroxyl carboxylate; and C. reacting the multivalent phenolic hydroxyl carboxylate with SeO2 to obtain multivalent phenolic hydroxyl carboxylic acid selenium complex salts, wherein the multivalent phenolic hydroxyl carboxylic acid selenium complex salts are organic selenium composition. The multivalent phenolic hydroxyl carboxylic acid selenium complex salts have characteristics of over 20% selenium content and no toxicity, and have revolutionary effects in killing bacteria, virus and cancer cell, enhancing human immunity, removing oxygen free radicals and etc.Type: ApplicationFiled: July 3, 2013Publication date: January 21, 2016Inventor: Gong Chen
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Publication number: 20160016903Abstract: The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the ? opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: July 15, 2015Publication date: January 21, 2016Inventors: Anita WEGERT, Bert NOLTE, Klaus LINZ, Stephanie HARLFINGER, Babette-Yvonne KOEGEL, Paul RATCLIFFE, Fritz THEIL, Olga GROEGER, Birgit BRAUN
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Publication number: 20160016904Abstract: The present invention relates to processes and intermediates useful in the preparation of (R)-2-(7-(4-cyclopentyl-3-(trifluromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid of Formula (I) and salts thereof, an S1P1 receptor modulator that is useful in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development and atherosclerosis).Type: ApplicationFiled: September 30, 2015Publication date: January 21, 2016Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Antonio Garrido Montalban, Daniel J. Buzard, John A. DeMattei, Tawfik Gharbaoui, Stephen R. Johannsen, Ashwin M. Krishnan, Young Mi Kuhlman, You-An Ma, Michael John Martinelli, Suzanne Michiko Sato, Dipanjan Sengupta
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Publication number: 20160016905Abstract: Provided is a stilbazolium derivative represented by the general formula (I): wherein R1, R2, R3, and R4 independently represent hydrogen, halogen, alkyl, hydroxyl, carboxyl, or amino; R5 represents hydrogen or alkyl; X represents oxygen or NR6 (R6 is hydrogen or alkyl); and Y? represents an anion. In the general formula (I), some or all of hydrogens maybe deuterium.Type: ApplicationFiled: June 23, 2015Publication date: January 21, 2016Inventors: Kazuyoshi Aoki, Shuji Okada
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Publication number: 20160016906Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.Type: ApplicationFiled: March 14, 2014Publication date: January 21, 2016Applicants: AMGEN INC., CYTOKINETICS, INC.Inventors: Sheng Cui, Henry Morrison, Karthik Nagapudi, Shawn Walker, Charles Bernard, Karl Bennett Hansen, Neil Fred Langille, Alan Martin Allgeier, Steven Mennen, Jacqueline Woo, Bradley Paul Morgan, Alex Muci
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Publication number: 20160016907Abstract: The present invention provides, in part, compounds of Formula I: N-oxides thereof, and pharmaceutically acceptable salts of the compounds or N-oxides; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, N-oxides, or salts, and their uses for treating M1-mediated (or M1-associated) disorders including, e.g., Alzheimer's disease, schizophrenia (e.g., its cognitive and negative symptoms), pain, addiction, and a sleep disorder.Type: ApplicationFiled: July 15, 2015Publication date: January 21, 2016Applicant: PFIZER INC.Inventors: MICHAEL AARON BRODNEY, JENNIFER ELIZABETH DAVOREN, MICHELLE RENEE GARNSEY, LEI ZHANG, STEVEN VICTOR O'NEIL
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Publication number: 20160016908Abstract: The present invention relates to novel compounds, pharmaceutical compositions containing such compounds and to their use in therapy.Type: ApplicationFiled: March 12, 2014Publication date: January 21, 2016Applicant: GlaxoSmithKline Intellectual Property (No.2) LimitedInventors: Dominique AMANS, Stephen John ATKINSON, Lee Andrew HARRISON, David Jonathan HIRST, Robert Peter LAW, Matthew LINDON, Alexander PRESTON, Jonathan Thomas SEAL, Christopher Roland WELLAWAY
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Publication number: 20160016909Abstract: The present invention provides novel intermediates of ivacaftor and process for its preparation. The present invention also provides process for the preparation of ivacaftor and pharmaceutically acceptable salt thereof using novel intermediates.Type: ApplicationFiled: February 14, 2014Publication date: January 21, 2016Inventors: Suresh THATIPALLY, Venkata Lakshmi Narasimha Rao DAMMALAPATI, Seeta Ramanjaneyulu GORANTLA, Satyanarayana CHAVA
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Publication number: 20160016910Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: February 28, 2014Publication date: January 21, 2016Applicant: Bristol-Meyers Squibb CompanyInventors: Mimi L. Quan, Zilun Hu, Cailan Wang, Peter W. Glunz
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Publication number: 20160016911Abstract: The present invention relates to the identification of compounds and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided compounds.Type: ApplicationFiled: September 28, 2015Publication date: January 21, 2016Inventors: Richard B. Silverman, Yinan Zhang
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Publication number: 20160016912Abstract: The present invention is directed to bendamustine esters and bendamustine amides and their use for the treatment of cancer.Type: ApplicationFiled: September 28, 2015Publication date: January 21, 2016Inventors: Roger P. BAKALE, Peter D. BROWN, Jian CHEN, Anthony S. DRAGER, Rachel Y. LABELL, Robert E. MCKEAN, Piyush R. PATEL, Renee C. ROEMMELE
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Publication number: 20160016913Abstract: Disclosed are compounds, such as pyridazinones, that can be, inter alia, used for treating cancer.Type: ApplicationFiled: March 11, 2014Publication date: January 21, 2016Applicant: THE BROAD INSTITUTE, INC.Inventors: Timothy A. Lewis, Benito Munoz, Lucian De Waal, Heidi Greulich, Matthew Meyerson, Lara Nicole Gechijian
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Publication number: 20160016914Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.Type: ApplicationFiled: July 13, 2015Publication date: January 21, 2016Inventors: Vladimir Ladziata, Peter W. Glunz, Zilun Hu, Yufeng Wang
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Publication number: 20160016915Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which n, m, R1, R2, and R3 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.Type: ApplicationFiled: May 6, 2015Publication date: January 21, 2016Inventors: Jerry Evarts, Leena Patel, Joshua Kaplan, Jennifer A. Treiberg, Stephane Perreault, Gary Phillips
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Publication number: 20160016916Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and, more particularly, to a compound represented by structural formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: ApplicationFiled: March 14, 2014Publication date: January 21, 2016Inventors: Vincent P. Sandanayaka, Sharon Shechter, Dirk Daelemans, Volker Leen, Wim Alfrons Dehaen, Sharon Shacham
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Publication number: 20160016917Abstract: The present invention relates to a method for preparing TDI (toluene diisocyanate) isocyanurate by using TDI, monohydric alcohol, solvent, antioxidant, catalyst and termination agent as the raw materials. The properties of the isocyanurate are improved by the process comprising the modification by monohydric alcohol and addition of the catalyst and solvent in several stages at an appropriate temperature. By adding the catalyst and solvent in batches at the condition of controlling both NCO % and the viscosity in the preparation process, and adjusting the solid content at each step, the resulting TDI isocyanurate has low content of free TDI, high xylene tolerance, small product color number, and high performance stability, which makes the product obtained by the isocyanurate have good application properties such as the drying, polishing and extinction properties of coating film, and such isocyanurate has good compatibility with other components.Type: ApplicationFiled: February 11, 2014Publication date: January 21, 2016Inventors: Xiao Zhang, Yulin Zhu, Zhenguang Wen, Kai Wang
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Publication number: 20160016918Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: ApplicationFiled: July 16, 2015Publication date: January 21, 2016Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20160016919Abstract: Provided is a photo-sensitive composition capable of yielding pixels having a high translucency and a large refractive index, with a less amount of development residue in the process of formation. The photo-sensitive resin composition contains an ultraviolet absorber represented by Formula (I); a photo-polymerization initiator; and a polymerizable monomer: wherein each of R1, R2 and R3 independently represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms; one of R4 and R5 represents an electron withdrawing group, and the other of R4 and R5 represents —SO2R6, —CO2R6, —COR6, —CN or —CONR6R7; each of R6 and R7 independently represents a hydrogen atom, alkyl group having 1 to 8 carbon atoms or aryl group.Type: ApplicationFiled: September 28, 2015Publication date: January 21, 2016Applicant: FUJIFILM CORPORATIONInventors: Yutaro NORIZUKI, Yukie WATANABE, Kazutaka TAKAHASHI
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Analogs of Peroxisome Proliferator Activated Receptor (PPAR) Agonists, and Methods of Using the Same
Publication number: 20160016920Abstract: Analogs of PPAR5 and analogs of 20-OH-PGE2, which are PPAR5 agonists and 20-OH-PGE2 antagonists, respectively, and methods of using the same for inducing osteogenesis or chondrogenesis, are disclosed.Type: ApplicationFiled: March 14, 2014Publication date: January 21, 2016Applicant: The University of ToledoInventors: Bruce E. Heck, Dong Hyun Kim, Paul Erhardt, Brian Kress -
Publication number: 20160016921Abstract: In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: ApplicationFiled: March 11, 2014Publication date: January 21, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
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Publication number: 20160016922Abstract: A disulfide compound represented by formula (1): (in formula (1), R1 and R2 each independently represent a hydrogen atom or an alkyl group; R3 and R4 each independently represent a hydrogen atom or a substituent; Y represents a single bond, —CO— or —COO—; Rf represents a linear or branched perfluoroalkylene group having 1 to 20 carbon atoms or a linear or branched perfluoroether group having 1 to 20 carbon atoms; when Y is a single bond or —CO—, n represents 0 and m represents an integer of 0 to 6; when Y is —COO—, n represents 1 or 2 and m represents an integer of 1 to 6; and p represents an integer of 2 or 3 and 1 represents an integer of 0 or 1 such that p+1=3).Type: ApplicationFiled: September 28, 2015Publication date: January 21, 2016Applicant: FUJIFILM CORPORATIONInventors: Tokihiko MATSUMURA, Yasuaki MATSUSHITA
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Publication number: 20160016923Abstract: In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiadiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein RN, R1, R2, R3, R4, ring A, RA, m, L1, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: ApplicationFiled: March 11, 2014Publication date: January 21, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Tanweer A. Khan, Jack D. Scott, Jared N. Cumming
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Publication number: 20160016924Abstract: A method for the production of ethylene oxide wherein the partial pressure of water vapor at the inlet of the reactor is at least about 8 kPa using a high purity carrier comprising alpha-alumina, a promoting amount of at least one Group IA metal, and a promoting amount of rhenium.Type: ApplicationFiled: March 12, 2014Publication date: January 21, 2016Inventors: Liping Zhang, Mark H. McAdon, Ernest R. Frank
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Publication number: 20160016925Abstract: The present invention relates to novel chemical compounds of the general formula 1—intermediate products in synthesis of androgen receptor inhibitors which are of interest as anticancer medicaments. The subject of the invention is also a method for preparation of novel compounds of the general formula 1.1—androgen receptor inhibitors. Substituted 3-(4-methylcarbamoyl-3-fluorophenylamino)tetrahydrofuran-3-encarboxylic acids, or their esters of the general formula 1, 1.1 and stereoisomers thereof, wherein: R1=C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3; wherein: R1=H, C1-C4alkyl; R2=H, CH2OCH2CH2Si(CH3)3.Type: ApplicationFiled: February 26, 2014Publication date: January 21, 2016Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Dmitry Vladimirovich Kravchenko, Anton Aleksandrovich Vorebey, Andrey Sergeevich Trifilenkov
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Publication number: 20160016926Abstract: A process is described for converting HMF to FDCA, comprising dissolving a quantity of HMF in water to form an aqueous solution including HMF, combining the aqueous solution including HMF with an oxygen source in the presence of a homogeneous metal salt catalyst, but in the substantial absence of any solvent for the HMF and the homogeneous metal salt catalyst other than water, and under conditions which are effective for oxidizing HMF in the presence of the catalyst to form FDCA, and then recovering an FDCA precipitate.Type: ApplicationFiled: March 5, 2014Publication date: January 21, 2016Inventor: Alexandra Sanborn
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Publication number: 20160016927Abstract: Provided are compounds of formula (I) and methods of controlling insects, acarines, nematodes or molluscs, which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest an insecticidally, acaricidally, nematicidally or molluscicidally effective amount of a compound of formula (I).Type: ApplicationFiled: March 6, 2014Publication date: January 21, 2016Applicant: SYNGENTA PARTICIPATIONS AGInventors: Long LU, Jerome Yves CASSAYRE, Torsten LUKSCH, Myriem EL QACEMI, Guillaume BERTHON, Yaming WU
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Publication number: 20160016928Abstract: The present invention relates to substituted chroman-6-yloxy-cycloalkanes of the formula (I) in which Ar, R1 to R4, p and q are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 7, 2014Publication date: January 21, 2016Applicant: SANOFIInventors: Werngard CZECHTIZKY, John WESTON, Nils RACKELMANN, Volker KRAFT, Petra ARNDT, Klaus WIRTH, Heinz GOEGELEIN, Olaf RITZELER
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Publication number: 20160016929Abstract: A compound according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein where the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1.Type: ApplicationFiled: December 23, 2013Publication date: January 21, 2016Inventors: Edward SAVORY, Daniel HILL, Oldrich KOCIAN
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Publication number: 20160016930Abstract: Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.Type: ApplicationFiled: July 16, 2015Publication date: January 21, 2016Inventors: Eugene Gillespie, Robert Damoiseaux, Chi-Lee Charlie Ho, Brian T. Chamberlain, Michael E. Jung, Kenneth A. Bradley
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Publication number: 20160016931Abstract: Compounds are provided that can exhibit anti-cancer and/or anti-inflammatory properties, in some aspects, methods of treating an inflammatory disease or a hyperproliferative disease, such as cancer, with the compounds are provided.Type: ApplicationFiled: March 13, 2014Publication date: January 21, 2016Inventors: Richard J. FORD, Jr., William G. BORNMANN, Ashutosh PAL, Lan V. PHAM, Zhenghong PENG, David MAXWELL, Archito TAMAYO
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Publication number: 20160016932Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: September 30, 2015Publication date: January 21, 2016Inventors: Sean Colm Turner, Margaretha Henrica Maria Bakker, Marcel van Gaalen, Falko Ernst Wolter, Wilfried Hornberger, Marjoleen Nijsen
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Publication number: 20160016933Abstract: A compound of formula (I) (I) wherein A, R1, R1a, R3 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: ApplicationFiled: March 10, 2014Publication date: January 21, 2016Inventors: Heather Finlay, Ashok Kumar Adisechan, Naveen Kumar Dhondi, Prashantha Gunaga, John Lloyd, Srinivasu Pothukanuri
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Publication number: 20160016934Abstract: There are provided compounds of formula I, wherein: Y represents NR2R3; one of R2 and R3 represents —[C2-4 alkylene-O]1-12—[C2-4 alkylene]-R2a and the other of R2 and R3 has a meaning given in the description; and R, R1, R2a, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: March 13, 2014Publication date: January 21, 2016Inventor: Matthew Colin Thor FYFE
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Publication number: 20160016935Abstract: The present invention is directed to 2-pyridyloxy-4-ether compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-pyridyloxy-4-ether compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: March 3, 2014Publication date: January 21, 2016Applicant: MERCK SHARP & DOHME CORP.Inventors: SCOTT D. KUDUK, JASON W. SKUDLAREK
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Publication number: 20160016936Abstract: The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: March 10, 2014Publication date: January 21, 2016Applicant: Merck Patent GmbHInventors: Ruoxi LAN, Xiaoling CHEN, Yufang XIAO, Bayard R. HUCK, Andreas GOUTOPOULOS
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Publication number: 20160016937Abstract: The invention relates to novel substituted pyrimidine compounds of general formula (I) in which the chemical groupings, substituents, variables and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.Type: ApplicationFiled: July 15, 2015Publication date: January 21, 2016Inventors: Antonio NARDI, Florian JAKOB, Ingo KONETZKI, Tobias CRAAN, Christian HESSLINGER, Robin DOODEMAN
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Publication number: 20160016938Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.Type: ApplicationFiled: July 15, 2015Publication date: January 21, 2016Inventors: Antonio NARDI, Florian JAKOB, Ingo KONETZKI, Tobias CRAAN, Christian HESSLINGER
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Publication number: 20160016939Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.Type: ApplicationFiled: February 27, 2014Publication date: January 21, 2016Inventors: Hassan PAJOUHESH, Richard HOLLAND, Lingyun ZHANG, Hossein PAJOUHESH, Jason LAMONTAGNE, Brendan WHELAN
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Publication number: 20160016940Abstract: The present invention relates to indole and indazole compounds of Formula (I) that activate 5? adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.Type: ApplicationFiled: September 24, 2013Publication date: January 21, 2016Applicant: Pfizer, Inc.Inventors: Samit Kumar Bhattacharya, Kimberly O'Keefe Cameron, Matthew Scott Dowling, David Christopher Ebner, David James Edmonds, Dilinie Prasadhini Fernando, Kevin James Filipski, Daniel Wei-Shung Kung, Esther Cheng Yin Lee, Aaron Christopher Smith, Meihua Mike Tu
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Publication number: 20160016941Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.Type: ApplicationFiled: March 11, 2014Publication date: January 21, 2016Applicant: TEMPLE UNIVERSITY OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Daniel J. CANNEY, Benjamin E. BLASS, Rong GAO, Magid ABOU-GHARBIA
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Publication number: 20160016942Abstract: The present invention is directed to substituted pyridine derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives in the treatment of disorders mediated by c-fms kinase. The present invention is further directed to a process for the preparation of said substituted pyridine derivatives.Type: ApplicationFiled: March 13, 2014Publication date: January 21, 2016Inventors: Jie CHEN, Matthew DONAHUE, Heng-Keeng LIM, Ronghui LIN, Rhys SALTER, Jiejun WU
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Publication number: 20160016943Abstract: Provided are a compound represented by Formula I, a pharmaceutically acceptable salt thereof, or a solvate thereof; and a pharmaceutical composition for cancer treatment and a pharmaceutical composition for a radiation sensitizer for cancer treatment, each pharmaceutical composition including the compound of Formula I, the pharmaceutically acceptable salt thereof, or the solvate thereof: wherein, in Formula I, —R1 is a C1-C3 alkoxy, ?O, or —OH, and —R2 is a 5- or 6-membered heteroaryl including 1 to 2 hetero atoms selected from nitrogen and oxygen, wherein a carbon of the 5- or 6-memberedheteroaryl is optionally substituted with a C1-C3 alkyl a C1-C3 alkoxy, or hydroxy.Type: ApplicationFiled: July 18, 2014Publication date: January 21, 2016Applicant: Korea Institute of Radiological & Medical SciencesInventors: Sung Hee Hong, In Seok Hong, Eun Jong Han, Kee Ho Lee
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Publication number: 20160016944Abstract: The present invention provides 3-{phenyl[(heterocyclylmethoxy)imino]methyl}-heterocyclyl derivatives of formula (I) Wherein A, X1 to X3, Y1 to Y5 represent various substituents.Type: ApplicationFiled: March 6, 2014Publication date: January 21, 2016Inventors: Anne-Sophie REBSTOCK, Christophe DUBOST, Pierre-Yves COQUERON, Simon MAECHLING, Helene LACHAISE, Philipe RINOLFI, Ulrike WACHENDORFF-NEUMANN
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Publication number: 20160016945Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.Type: ApplicationFiled: March 17, 2014Publication date: January 21, 2016Inventor: Chunlin Tao
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Publication number: 20160016946Abstract: Disclosed are small molecule non-peptidic compounds, as well as methods and compositions for the treatment of angiotensin-related diseases and disorders, including cardiovascular diseases, metabolic diseases, gastrointestinal diseases, renal diseases, inflammatory/autoimmune diseases, neurological diseases, bone marrow diseases and cancer.Type: ApplicationFiled: March 15, 2014Publication date: January 21, 2016Inventors: Nicos A. Petasis, Kathleen E. Rodgers, Stan G. Louie, Gere S. DiZerega, Kevin J. Gaffney
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Publication number: 20160016947Abstract: The present invention is directed to substituted pyridizinone compounds of formula I 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: March 10, 2014Publication date: January 21, 2016Applicant: MERCK SHARP & DOHME CORP.Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
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Publication number: 20160016948Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.Type: ApplicationFiled: June 19, 2015Publication date: January 21, 2016Applicant: GENENTECH, INC.Inventors: Marian C. Bryan, Bryan Chan, Emily Hanan, Timothy Heffron, Hans Purkey, Richard Leonard Elliott, Robert Heald, Jamie Knight, Michael Lainchbury, Eileen M. Seward
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Publication number: 20160016949Abstract: The present invention provides compounds of formula (I) wherein Y1, Y2, Y3, G, V1, V2, V3 and V4 are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: March 17, 2014Publication date: January 21, 2016Applicant: Syngenta Participations AGInventors: Kurt NEBEL, Martin POULIOT