The Five-membered Hetero Ring Has At Least Sulfur And Nitrogen As Ring Hetero Atoms Patents (Class 544/133)
  • Patent number: 9428473
    Abstract: The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: August 30, 2016
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard Polniaszek, Steven Pfeiffer, Richard Yu, Aaron Cullen, Eric Dowdy, Duong Tran, Kenneth Kent, Zhongxin Zhou, Douglas Cordeau, Leah Easton-Scott
  • Publication number: 20150133451
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 14, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki TAKAMI, Yusuke TOMINARI, Zenyu SHIOKAWA, Akito SHIBUYA, Yusuke SASAKI, Tony GIBSON, Terufumi TAKAGI
  • Publication number: 20150133656
    Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 14, 2015
    Applicants: CARNA BIOSCIENCES INC., NATIONAL CANCER CENTER
    Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Publication number: 20150080570
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 19, 2015
    Applicants: Coferon, Inc., Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle
  • Patent number: 8975254
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Orion Corporation
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8969583
    Abstract: This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
    Type: Grant
    Filed: December 27, 2012
    Date of Patent: March 3, 2015
    Assignee: Allergan, Inc.
    Inventors: Thomas C. Malone, C. Eugene Hull, Sougato Boral, Julie A. Wurster, Michael R. Robinson, Jeffrey L. Edelman
  • Publication number: 20150057280
    Abstract: The invention relates to pyridylidene 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 pyridylidene 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 pyridylidene compounds. The N-substituted pyridylidene compounds of the present invention are defined by the following formula I: wherein X, Het, R1, R2, R3, R4 and R6 are defined as in the description.
    Type: Application
    Filed: March 27, 2013
    Publication date: February 26, 2015
    Applicant: BASF SE
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Korber
  • Publication number: 20150057272
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Application
    Filed: August 1, 2014
    Publication date: February 26, 2015
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Publication number: 20150051193
    Abstract: Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 19, 2015
    Inventors: Jeffrey S. Glenn, Michael A. Gelman, Brandon Tavshanjian, Kevan Shokat, Ingrid Choong
  • Patent number: 8957070
    Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Publication number: 20150038483
    Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, sub
    Type: Application
    Filed: March 26, 2013
    Publication date: February 5, 2015
    Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
  • Patent number: 8937065
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: January 20, 2015
    Assignee: Clevexel Pharma
    Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
  • Publication number: 20150018330
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 15, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
  • Patent number: 8933075
    Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: January 13, 2015
    Assignees: FUZIANS BIOMEDICALS, Inc., The UAB Research Foundation
    Inventors: Guoxin Wang, Ming Luo, Zhen Yang
  • Publication number: 20150005493
    Abstract: The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: September 3, 2014
    Publication date: January 1, 2015
    Inventors: Richard POLNIASZEK, Steven PFEIFFER, Richard YU, Aaron CULLEN, Eric DOWDY, Duong TRAN, Kenneth KENT, Zhongxin ZHOU, Doug CORDEAU, Leah EASTON-SCOTT
  • Patent number: 8920785
    Abstract: Cosmetic or dermatological preparations having an effective content of one or more thiazoles of the general formula.
    Type: Grant
    Filed: February 21, 2011
    Date of Patent: December 30, 2014
    Assignee: Beiersdorf AG
    Inventors: Ludger Kolbe, Cathrin Scherner
  • Patent number: 8921546
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: December 30, 2014
    Assignee: Ambit Biosciences Corporation
    Inventor: Qi Chao
  • Publication number: 20140364602
    Abstract: Methods and intermediates useful for preparing a compound of formula I: and salts thereof.
    Type: Application
    Filed: February 1, 2013
    Publication date: December 11, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Aaron J. Cullen, Richard Hung Chiu Yu
  • Patent number: 8883783
    Abstract: Solid forms comprising N-(5-tert-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: November 11, 2014
    Assignee: Ambit Biosciences Corporation
    Inventors: Shripad S. Bhagwat, Wei Lai, Stephan D. Parent, Melanie J. Roe, Alan Schwartz, Valeriya N. Smolenskaya
  • Publication number: 20140329674
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Publication number: 20140309210
    Abstract: A compound of formula I: stereoisomers or a pharmaceutically acceptable salt thereof, wherein X, X1, X2, X3, R1, R2, R3, R4, R5 and R6 are described herein, compositions including the compounds and methods of making and using the compounds for the treatment of diseases.
    Type: Application
    Filed: February 12, 2014
    Publication date: October 16, 2014
    Applicant: Genentech, Inc.
    Inventors: Jason Burch, Richard A. Goldsmith, Daniel Fred Ortwine, Richard Pastor, Zhonghua Pei
  • Patent number: 8853210
    Abstract: The invention provides methods and intermediates that are useful for preparing a compound of formula I: and salts thereof.
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: October 7, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard Polniaszek, Steven Pfeiffer, Richard Yu, Aaron Cullen, Eric Dowdy, Duong Tran, Kenneth Kent, Zhongxin Zhou, Doug Cordeau, Leah Easton-Scott
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Publication number: 20140275033
    Abstract: The invention provides novel inhibitors of cancer stem cells as well as cancer stem cell pathway kinase and other related kinases, pharmaceutical compositions and uses thereof in the treatment of cancer or a related disorder in a mammal, and methods of making such compounds and compositions.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Chiang Jia Li, Ji-Feng Liu, Wei Li, Amanda Gibeau, Harry Rogoff
  • Publication number: 20140275012
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Todd BOSANAC, Michael J. BURKE, Darren DISALVO, Wang MAO, John WESTBROOK
  • Patent number: 8822698
    Abstract: Novel amino acids derivatives, in particular some amino acid amides derivatives, their process of preparation and their use for inhibiting Met-triggered disorders, in particular cancer.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: September 2, 2014
    Assignees: Universite d'Aix-Marseille, Universite de Lorraine, Oreste Piccolo Studio di Consulenza Scientifica, Universitat de Barcelona, Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Flavio Maina, Rosanna Dono, Oreste Piccolo, Daniele Passarella, Francesco Colombo, Joan Bosch, Bernard Maigret, Vincent Leroux
  • Publication number: 20140243340
    Abstract: The present invention features compounds of formula I or pharmaceutically acceptable salts, solvates or prodrugs thereof, and methods of using the same to inhibit the metabolizing activities of CYP enzymes. The present invention also features methods of using these compounds, salts, solvates or prodrugs to improve the pharmacokinetics of drugs that are metabolized by CYP enzymes.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: AbbVie Inc.
    Inventors: Larry L. Klein, Hui-Ju CHEN, Ming C. YEUNG, Charles A. Flentge, John T. Randolph, Peggy Huang, Douglas K. Hutchinson, Dale J. Kempf
  • Publication number: 20140243525
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Application
    Filed: September 20, 2013
    Publication date: August 28, 2014
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Patent number: 8815857
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: August 9, 2012
    Date of Patent: August 26, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Angela Berry, John David Ginn, Tamara Denise Hopkins, Sabine Schlyer, Fariba Soleymanzadeh, John Westbrook, Maolin Yu, Zhonghua Zhang
  • Publication number: 20140228365
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Publication number: 20140221369
    Abstract: The invention provides 5-deuterium enriched 2,4-thiazolidinediones and 2,4-oxazolidinediones, such as 5-(4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-5-deutero-thiazolidine-2,4-dione, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating medical disorders, such as cancer, using the same.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Patent number: 8796256
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Patent number: 8796268
    Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: August 11, 2011
    Date of Patent: August 5, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
  • Publication number: 20140213584
    Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Application
    Filed: November 8, 2011
    Publication date: July 31, 2014
    Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.
    Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
  • Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Publication number: 20140199348
    Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.
    Type: Application
    Filed: February 12, 2013
    Publication date: July 17, 2014
    Applicant: KINETA, INC.
    Inventors: Shawn P. Iadonato, Kristin M. Bedard, Ernesto J. Muñoz, Myra W. Imanaka, Kerry W. Fowler
  • Publication number: 20140200197
    Abstract: 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: Application
    Filed: September 9, 2013
    Publication date: July 17, 2014
    Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
  • Patent number: 8779154
    Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: September 25, 2007
    Date of Patent: July 15, 2014
    Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
  • Publication number: 20140194412
    Abstract: The present invention provides an anticancer drug having a Ras function inhibitory action. The present invention provides a Ras function inhibitor comprising a compound represented by the formula (I?): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2012
    Publication date: July 10, 2014
    Applicants: KNC LABORATORIES CO., LTD., NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
    Inventors: Tohru Kataoka, Fumi Shima, Masahiro Neya, Daisuke Sasahara
  • Publication number: 20140187771
    Abstract: The invention provides an amorphous solid of a compound of formula (I) or of a salt thereof as well as compositions comprising the amorphous solids, and methods for making and using the amorphous solids.
    Type: Application
    Filed: April 30, 2012
    Publication date: July 3, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Joanna M. Koziara, Anne Luong, Keiko Sujino, Richard Yu
  • Patent number: 8765752
    Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: July 1, 2014
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventor: Munetaka Ohkouchi
  • Patent number: 8759379
    Abstract: The present application provides for a compound of Formula I, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
    Type: Grant
    Filed: December 19, 2008
    Date of Patent: June 24, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Manoj C. Desai, Hon C. Hui, Hongtao Liu, Lianhong Xu
  • Patent number: 8759536
    Abstract: Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Avixgen Inc.
    Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
  • Publication number: 20140163001
    Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 12, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
  • Publication number: 20140162998
    Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 12, 2014
    Applicant: Jikai Biosciences, Inc.
    Inventor: Yu GE
  • Publication number: 20140155597
    Abstract: The purpose of the present invention is to provide a novel compound which has an anti-fungal activity on pathogenic fungi including fungi belonging to the genus Candida, the genus Aspergillus and the genus Trichophyton and is useful as a medicinal agent.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya Tanikawa, Yasunobu Ushiki, Fumihito Ushiyama, Toru Yamaguchi, Naoya Ono, Keiko Yamamoto, Risa Tsuruta, Yasuhiro Tsutsui, Noritomo Fujino, Ayumu Mori