Patents Issued in May 8, 2014
  • Publication number: 20140128362
    Abstract: The present invention provides compositions and methods based on genetic polymorphisms that are associated with response to statin treatment (particularly for reducing the risk of venous thrombosis). For example, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by these nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and variant proteins, and methods of using the nucleic acid molecules and proteins as well as methods of using reagents for their detection.
    Type: Application
    Filed: March 20, 2013
    Publication date: May 8, 2014
    Applicant: CELERA CORPORATION
    Inventors: Lance BARE, James J. DEVLIN, Frits R. ROSENDAAL, Pieter H. REITSMA, Irene D. BEZEMER
  • Publication number: 20140128363
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
  • Publication number: 20140128364
    Abstract: Disclosed herein is the use of tigemonam and carumonam in treating bacterial infection caused by bacteria producing K. pneumoniae carbapenemase (KPC) enzymes.
    Type: Application
    Filed: March 12, 2013
    Publication date: May 8, 2014
    Applicant: Rempex Pharmaceuticals
    Inventor: Olga Rodny
  • Publication number: 20140128365
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 8, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
  • Publication number: 20140128366
    Abstract: The present invention relates to substituted 1,3,4-oxadiazoles-2-thio azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Publication number: 20140128367
    Abstract: The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R1, R2, R7, R8a, E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.
    Type: Application
    Filed: June 14, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xianhai Huang, Jason Brubaker, Scott L. Peterson, John W. Butcher, Joshua T. Close, Michelle Martinez, Rachel Nicola MacCoss, Joon O. Jung, Phieng Siliphaivanh, Hongjun Zhang, Robert G. Aslanian, Purakkattle Johny Biju, Li Dong, Ying Huang, Kevin D. McCormick, Anandan Palani, Ning Shao, Wei Zhou
  • Publication number: 20140128368
    Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 8, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Andrew Stamford, Kallol Basu, Harold B. Wood, Duane DeMong, Wanying Sun, Joie Garfunkle, Christopher Moyes, Zhiyong Hu, Ping Liu, Scott D. Edmondson, Xing Dai, Byron Gabriel DuBois
  • Publication number: 20140128369
    Abstract: The present invention relates to novel benzyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 8, 2014
    Applicant: Allergan, Inc.
    Inventors: Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha Bin Im
  • Publication number: 20140128370
    Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.
    Type: Application
    Filed: January 9, 2014
    Publication date: May 8, 2014
    Applicant: NOVARTIS AG
    Inventors: Nigel Graham COOKE, Frédéric ZECRI, Nicolas SOLDERMANN, Romain WOLF, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Anette VON MATT, Ross Sinclair STRANG, Alexander Baxter SMITH, Paulo FERNANDES GOMES DOS SANTOS, Nadege GRAVELEAU, Frank STOWASSER, Nicola TUFILLI
  • Publication number: 20140128371
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
  • Publication number: 20140128372
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: March 7, 2013
    Publication date: May 8, 2014
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Markus FOLLMANN, Ingo HARTUNG, Philipp BUCHGRABER, Rolf JAUTELAT, Jorma HAßFELD, Niels LINDNER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva-Maria BECKER, Andreas KNORR
  • Publication number: 20140128373
    Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: February 1, 2012
    Publication date: May 8, 2014
    Inventors: Prabha N. Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
  • Publication number: 20140128374
    Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.
    Type: Application
    Filed: November 5, 2013
    Publication date: May 8, 2014
    Applicant: PFIZER INC
    Inventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
  • Publication number: 20140128375
    Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Inventors: Ian M. Bell, Harold B. Selnick
  • Publication number: 20140128376
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Genentech, Inc.
    Inventor: Xiaojing Wang
  • Publication number: 20140128377
    Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: UCB Pharma GmbH
    Inventor: Thomas STÖHR
  • Publication number: 20140128378
    Abstract: The present invention is directed to the use of a class of peptide Compounds for prevention, alleviation or/and treatment of refractory Status epilepticus.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: UCB Pharma GmbH
    Inventor: Thomas STÖHR
  • Publication number: 20140128379
    Abstract: The present invention provides pharmaceutical compositions for intranasal delivery of a benzodiazepine. The composition may contain a therapeutically effective amount of a benzodiazepine or a pharmaceutically acceptable salt thereof, and a permeation enhancer. The permeation enhancer may be propylene glycol or a Hsieh permeation enhancer. The present compositions have excellent bioavailability. After administration of the present compositions, therapeutically effective plasma levels of the benzodiazepine may be achieved rapidly. The present pharmaceutical composition may be used to treat a patient suffering from anxiety, epilepsy, insomnia, agitation, seizures, muscular disorders, alcohol dependence, and drug withdrawal.
    Type: Application
    Filed: March 29, 2012
    Publication date: May 8, 2014
    Applicant: CPEX Pharmaceuticals, Inc.
    Inventors: Nils Bergenhem, Carl Reppucci, Zhengmao Li
  • Publication number: 20140128380
    Abstract: The present invention provides compounds of Formula (I) that are useful for binding and/or modulating the biological activity of the melanocortin-1 receptor (MC1R). Compounds of this invention can be used to treat diseases and/or conditions in which modulation of MC1R is beneficial. Such diseases and/or conditions include, but are not limited to, hyperpigmentation (including melasma), hypopigmentation (including vitiligo), melanoma, basal cell carcinoma, squamous cell carcinoma, erythropoietic protoporphyria, polymorphous light eruption, solar urticaria, photosensitivity, sunburn, inflammatory diseases, aberrant fibroblast activity and pain.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Mimetica Pty Ltd
    Inventors: Mark Arnold Thomas Blaskovich, Peter Joseph Cassidy
  • Publication number: 20140128381
    Abstract: The present invention generally relates to intranasal pharmaceutical compositions comprising a benzodiazepine and methods of use thereof that can provide a therapeutic effect without a decrease in blood pressure and/or pulse after administration of the pharmaceutical composition.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Inventors: Gary Bream, Moise A. Khayrallah, Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
  • Publication number: 20140128382
    Abstract: The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or 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 uses, including Alzheimer's disease, are also disclosed.
    Type: Application
    Filed: April 12, 2012
    Publication date: May 8, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, Andrew W. Stamford, Jared N. Cumming, Chad E. Bennett, Eric J. Gilbert, Jack D. Scott, Younong Yu, Xuanjia Peng
  • Publication number: 20140128383
    Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
    Type: Application
    Filed: April 6, 2012
    Publication date: May 8, 2014
    Applicant: LABORATOIRE BIODIM
    Inventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
  • Publication number: 20140128384
    Abstract: The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect.
    Type: Application
    Filed: July 4, 2012
    Publication date: May 8, 2014
    Applicant: NANJING SANHOME PHARMACEUTICAL CO., LTD.
    Inventors: Yong Wang, Cang Zhang, Xiaorong Liu, Yan Zhang, Yunyun Wang, Wenping Zhang
  • Publication number: 20140128385
    Abstract: The present invention relates to the use of BACE-2 inhibitors and pharmaceutical compositions comprising BACE-2 inhibitors for treating metabolic disorders related to decreased ? cell mass and/or function.
    Type: Application
    Filed: January 13, 2012
    Publication date: May 8, 2014
    Inventor: Heinrich Ruegger
  • Publication number: 20140128386
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: November 4, 2013
    Publication date: May 8, 2014
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros VAKALOPOULOS, Ingo HARTUNG, Markus FOLLMANN, Rolf JAUTELAT, Alexander STRAUB, Jorma HAßFELD, Niels LINDNER, Dirk SCHNEIDER, Frank WUNDER, Johannes-Peter STASCH, Gorden REDLICH, Volkhart Min-Jian LI, Eva Maria BECKER-PELSTER, Andreas KNORR
  • Publication number: 20140128387
    Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.
    Type: Application
    Filed: November 5, 2013
    Publication date: May 8, 2014
    Applicants: SHANGHAI iNSTITUTE OF MATERIA MEDICA ACADEMY OF SCIENCES, SHANGHAI FOCHON PHARMACEUTICAL CO., LTD.
    Inventors: Weibo WANG, Meiyu Geng, Jian Ding, Xingdong Zhao, Jing Ai, Qiang Tian, Xia Peng, Weipeng Zhang, Hongbin Liu, Haohan Tan, Ling Chen
  • Publication number: 20140128388
    Abstract: Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro.
    Type: Application
    Filed: July 31, 2013
    Publication date: May 8, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
  • Publication number: 20140128389
    Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: October 15, 2010
    Publication date: May 8, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Randall L. Halcomb, Paul A. Roethle
  • Publication number: 20140128390
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.
    Type: Application
    Filed: September 5, 2013
    Publication date: May 8, 2014
    Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
  • Publication number: 20140128391
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Publication number: 20140128392
    Abstract: Disclosed herein are new heterocyclic compounds of Formula IIa: and compositions thereof, and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: March 19, 2010
    Publication date: May 8, 2014
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero
  • Publication number: 20140128393
    Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 8, 2014
    Applicant: EPIZYME, INC.
    Inventors: Sarah K. Knutson, Natalie Warholic, Heike Keilhack
  • Publication number: 20140128394
    Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is c1-6 alkyl; R2 is hydroxy, c1-6 alkyl that may have one or more substituents, —(C=0)-N(R2)(R4), or —(C=0)-0R5; R3 and R4 are the same or different, and each represents hydrogen or c1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or c1-6 alkyl that may have one or more 15 substituents; and n is 1 or 2; or a salt thereof.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshihiro URADE, Makoto KITADE, Kazuhiko SHIGENO, Keiko YAMANE, Katsunao TANAKA
  • Publication number: 20140128395
    Abstract: There is provided inter alia a compound which is an NK-1 receptor antagonist for use in the treatment or prevention of CNV. There is also provided a compound which is an NK-1 antagonist for use in the treatment of chemical burns of the eye particularly alkali burns of the eye. There is also provided a pharmaceutical composition for topical administration to the eye comprising an NK-1 antagonist and an antibiotic agent.
    Type: Application
    Filed: July 4, 2012
    Publication date: May 8, 2014
    Inventor: Giulio Ferrari
  • Publication number: 20140128396
    Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: January 7, 2014
    Publication date: May 8, 2014
    Applicant: Merck Patent GmbH
    Inventors: Oliver SCHADT, Dieter DORSCH, Frank STIEBER, Andree BLAUKAT
  • Publication number: 20140128397
    Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 8, 2014
    Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
  • Publication number: 20140128398
    Abstract: Compounds, compositions, and formulations, and accompanying methods useful for treating disorders arising from oxidative DNA damage, including oxidative DNA damage resulting from ionizing radiation or other therapy are described herein.
    Type: Application
    Filed: June 1, 2012
    Publication date: May 8, 2014
    Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
    Inventors: Mark R. Kelley, Michael R. Vasko
  • Publication number: 20140128399
    Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.
    Type: Application
    Filed: December 6, 2013
    Publication date: May 8, 2014
    Applicant: DUKE UNIVERSITY
    Inventors: Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David W. Zaas
  • Publication number: 20140128400
    Abstract: 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 Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: January 8, 2014
    Publication date: May 8, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Publication number: 20140128401
    Abstract: 8-Fluorophthalazin-1(2h)-one compounds of Formula I where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140128402
    Abstract: The present invention discloses a pharmaceutical combination comprising Hydroxychloroquine and a DPP-IV inhibitor or their pharmaceutically acceptable salts, solvates or prodrugs thereof, for preventing, slowing the progression of, delaying, improving, restoring, or treating a condition or a disease resulting from metabolic disorders.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Applicant: IPCA Laboratories Limited
    Inventors: Anil PAREEK, Gopakumar G. NAIR
  • Publication number: 20140128403
    Abstract: Use of 10H-benzo[g]pteridine-2,4-dione derivatives as photosensitizers in the inactivation of microorganisms.
    Type: Application
    Filed: June 22, 2012
    Publication date: May 8, 2014
    Inventors: Tim Maisch, Andreas Späth
  • Publication number: 20140128404
    Abstract: The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 8, 2014
    Applicant: REMYND NV
    Inventors: Gerard Griffioen, Matthias Nettekoven, Katrien Princen, Hasane Ratni, Walter Vifian
  • Publication number: 20140128405
    Abstract: Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt.
    Type: Application
    Filed: January 15, 2014
    Publication date: May 8, 2014
    Inventor: Alex Chervinsky
  • Publication number: 20140128406
    Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or x-N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.
    Type: Application
    Filed: June 27, 2012
    Publication date: May 8, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
  • Publication number: 20140128407
    Abstract: The present invention relates to a fast dissolving granulate formulation containing the veterinary drug azaperone and a method for preparing said granulate formulation.
    Type: Application
    Filed: June 21, 2012
    Publication date: May 8, 2014
    Applicant: ELANCO ANIMAL HEALTH IRELAND LIMITED
    Inventors: Dieter Bert Leen Ameye, Lieven Van Vooren, Peter Meerts, Geert Louise F. Van Beeck, Raja Satyanarayana Yekkala
  • Publication number: 20140128408
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
    Type: Application
    Filed: January 31, 2012
    Publication date: May 8, 2014
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Alan Kozikowski, Jay H. Kalin, Kyle V. Butier, Joel Bergman, Wayne W. Hancock
  • Publication number: 20140128409
    Abstract: The present invention relates to the use of indolinones of general formula substituted in the 6 position, wherein R1 to R6 and X are defined as in claim 1, the isomers and the salts thereof, particularly the physiologically acceptable salts thereof, as a medicament for the prevention or treatment of specific fibrotic diseases.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: John Edward PARK, Nveed CHAUDHARY, Gerald Juergen ROTH, Armin HECKEL, Thorsten LEHMANN-LINTZ, Joerg KLEY
  • Publication number: 20140128410
    Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.
    Type: Application
    Filed: March 18, 2013
    Publication date: May 8, 2014
    Applicant: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
  • Publication number: 20140128411
    Abstract: The present invention provides a fungicidal composition useful as an agricultural and horticultural fungicide having remarkably improved controlling effects against plant diseases, and a method for controlling plant diseases using the composition. A fungicidal composition comprising, as active ingredients, (a) 3-(2,3,4-trimethoxy-6-methylbenzoyl)-5-chloro-2-methoxy-4-methyl-pyridine (pyriofenone) or its salt and (b) at least one fungicide selected from the group consisting of bixafen, fluxapyroxad, penflufen, isopyrazam, fluopyram, ametoctradin, fenpyrazamine and sedaxane, and a method for controlling plant diseases, which comprises applying the fungicidal composition to plants.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 8, 2014
    Applicant: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Yuzuka Kawai