The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Tricyclo Ring System Patents (Class 544/126)
  • Patent number: 10759792
    Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 4, 2015
    Date of Patent: September 1, 2020
    Assignee: The Johns Hopkins University
    Inventors: Daniel Emil Levy, Howard Schulman, Bheema Rao Paraselli, Nangunoori Sampath Kumar, Brahmaiah Dabbugoddu, Chundru Balasubramanyam
  • Patent number: 10508106
    Abstract: The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: December 17, 2019
    Assignees: ConverGene LLC, The United States of America, As Represented by the Secretary, Department of Health and Human Services
    Inventors: Jeffrey William Strovel, Makoto Yoshioka, David J. Maloney, Shyh Ming Yang, Ajit Jadhav, Daniel Jason Urban
  • Patent number: 10501457
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Grant
    Filed: November 30, 2016
    Date of Patent: December 10, 2019
    Assignee: OsteoQC Inc.
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Patent number: 10457677
    Abstract: Compounds of the formula (I), which are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: October 29, 2019
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Kai Schiemann
  • Patent number: 10022360
    Abstract: Described herein are polymeric nanoparticles that comprise 8-[4-(1-aminocyclobutyl)phenyl]-9-phenyl-2H-[1,2,4]-triazolo-[3,4-fJ[1,6]-naphthyridin-3-one (Compound A), or a pharmaceutically acceptable salt thereof, and methods of making and using such nanoparticles. The nanoparticle comprises about 50 to about 99.8 weight percent of a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic acid-co-glycolic acid)-poly(ethylene)glycol copolymer, wherein the total amount of poly(ethylene)glycol in the nanoparticle is about 10 to about 30 weight percent poly(ethylene)glycol and about 0.2 to about 30 weight percent of Compound A.
    Type: Grant
    Filed: March 12, 2015
    Date of Patent: July 17, 2018
    Assignees: Merck Sharp & Dohme Corp., Pfizer Inc.
    Inventors: Young Ho Song, Greg Troiano, Hong Wang, Maria Figueiredo, Michael H. Lam, Caroline McGregor
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9029387
    Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 12, 2015
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Patent number: 8999978
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Patent number: 9000153
    Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: April 7, 2015
    Assignee: Merck Patent GmbH
    Inventors: Thomas Fuchss, Werner Mederski, Frank Zenke
  • Publication number: 20150080366
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 19, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Publication number: 20150065499
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 5, 2015
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Publication number: 20150051204
    Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 19, 2015
    Applicant: SJT MOLECULAR RESEARCH, S.L.
    Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya
  • Publication number: 20150045359
    Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.
    Type: Application
    Filed: January 8, 2013
    Publication date: February 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
  • Patent number: 8952033
    Abstract: Disclosed herein are novel 4-anilinofuro[2,3-b]quinoline derivatives of formula (I): or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the Specification and Claims. Also disclosed are the preparation processes of these derivatives and their uses in the manufacture of pharmaceutical compositions and in the treatment of cancers.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: February 10, 2015
    Assignee: Kaohsiung Medical University
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Yu-Wen Chen, Pei-Jung Lu
  • Publication number: 20150031692
    Abstract: The present invention relates to new substituted pyrano and furanoquinolines having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.
    Type: Application
    Filed: January 24, 2013
    Publication date: January 29, 2015
    Inventors: José-Luis Diaz-Fernández, Ute Christmann
  • Patent number: 8940737
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: January 27, 2015
    Assignee: AbbVie Inc.
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
  • Publication number: 20150023990
    Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.
    Type: Application
    Filed: September 30, 2014
    Publication date: January 22, 2015
    Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
  • Publication number: 20150025067
    Abstract: Inhibitors of p67phox protein are provided herein, as well as pharmaceutical compositions and methods relating thereto.
    Type: Application
    Filed: February 13, 2013
    Publication date: January 22, 2015
    Applicant: CHILDREN'S HOSPITAL MEDICAL CENTER
    Inventors: Yi Zheng, Prakash Jagtap, Emily E. Bosco, Jaroslaw Meller, Marie-Dominique Filippi
  • Patent number: 8927715
    Abstract: This invention relates to novel compounds of the Formula (I*), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of Cortisol in a cell or the inhibition of the conversion of cortisone to Cortisol in a cell.
    Type: Grant
    Filed: August 24, 2007
    Date of Patent: January 6, 2015
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Salvacion Cacatian, Wei He, Robert Simpson, Zhenrong Xu, Wei Zhao
  • Publication number: 20140371207
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: December 13, 2013
    Publication date: December 18, 2014
    Applicants: Kyowa Hakko Kirin Co., Ltd., Millennium Pharmaceuticals, Inc.
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C.B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20140350007
    Abstract: The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.
    Type: Application
    Filed: July 23, 2014
    Publication date: November 27, 2014
    Inventors: In-Hae YE, Chun-Ho PARK, Jong-Hee CHOI, Dong-il KANG
  • Patent number: 8889675
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: November 18, 2014
    Assignee: AbbVie Inc.
    Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
  • Publication number: 20140336178
    Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
    Type: Application
    Filed: April 29, 2014
    Publication date: November 13, 2014
    Applicants: The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
  • Publication number: 20140329800
    Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 6, 2014
    Inventors: Daxin Gao, Heping Yang, Yajun Yu
  • Publication number: 20140315889
    Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 23, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
  • Patent number: 8853391
    Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: October 7, 2014
    Assignee: Merck Patent GmbH
    Inventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, Jr., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
  • Publication number: 20140288068
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: OssiFi Inc.
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Publication number: 20140249143
    Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 4, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
  • Patent number: 8822448
    Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
  • Publication number: 20140242121
    Abstract: The present invention relates to a compound of Formula I: or an enantiomer, diastereomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Application
    Filed: October 3, 2012
    Publication date: August 28, 2014
    Applicant: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Publication number: 20140235616
    Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 21, 2014
    Applicant: SANOFI
    Inventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
  • Patent number: 8785639
    Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 22, 2014
    Assignee: AbbVie Inc.
    Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
  • Publication number: 20140200199
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi Moussa, Neru Munshi
  • Publication number: 20140194414
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 10, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20140193453
    Abstract: This invention relates to compositions, and related compounds and methods, of conjugates of immunomodulatory agents and polymers or unit(s) thereof. The conjugates may be contained within synthetic nanocarriers, and the immunomodulatory agents may be released from the synthetic nanocarriers in a pH sensitive manner.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 10, 2014
    Applicant: SELECTA BIOSCIENCES, INC.
    Inventors: CHARLES ZEPP, GRAYSON B. LIPFORD, YUN GAO, LLOYD JOHNSTON, FEN-NI FU, MARK J. KEEGAN, SAM BALDWIN
  • Publication number: 20140179671
    Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: September 12, 2013
    Publication date: June 26, 2014
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
  • Publication number: 20140171407
    Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: February 17, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
  • Patent number: 8754078
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: June 17, 2014
    Assignee: ArQule, Inc.
    Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
  • Publication number: 20140148451
    Abstract: The present invention relates to compounds of formulas III and V that are useful as pharmaceutical agents, particularly as autophagy inhibitors.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 29, 2014
    Applicants: Translational Genomics Research Institute, Van Andel Research Institute
    Inventors: Jeffrey Paul MacKeigan, Katie Renee Martin, Megan Lynne Goodall, Stephen Gately, Tong Wang
  • 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
  • Patent number: 8716274
    Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and 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: Grant
    Filed: November 2, 2012
    Date of Patent: May 6, 2014
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140093505
    Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
    Type: Application
    Filed: June 4, 2012
    Publication date: April 3, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Patent number: 8685969
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: April 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
  • Patent number: 8680268
    Abstract: Disclosed are a novel sulfonic acid derivative compound and a novel naphthalic acid derivative compound with high solubility in organic solvents, good photosensitivity, and suitability as a photoacid generator and a polymerization initiator. The sulfonic acid derivative compound is represented by the formula (I) (wherein R01, R04, R05, and R06 represent a hydrogen atom; any one of R02 and R03 represents an alkoxy group having a carbon number of 4 to 18 which may be substituted with an alicyclic hydrocarbon group, a heterocyclic group, or a halogen atom and which may have a branch, or the like; and R07 represents an aliphatic hydrocarbon group having a carbon number of 1 to 18 which may be substituted with a halogen atom and/or an alkylthio group, or the like).
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: March 25, 2014
    Assignee: Adeka Corporation
    Inventors: Toshihiko Murai, Yoshie Makabe, Shohei Fujita
  • Publication number: 20140051695
    Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof where in formula I the variables R1, R2, R3, R4 and R5 are as defined in the claims and where X is C—R6 or N, Y is C—R7 or N, where R6 and R7 are, inter alia, hydrogen, halogen, alkoxy, haloalkoxy and the like. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: August 15, 2013
    Publication date: February 20, 2014
    Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Clarissa JAKOB
  • Publication number: 20140045834
    Abstract: Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Emmanuel Hubert Demont, Katherine Louise Jones, Robert J. Watson
  • Publication number: 20140038926
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: May 24, 2013
    Publication date: February 6, 2014
    Applicant: Corcept Therapeutics, Inc.
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Publication number: 20140031544
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 30, 2014
    Applicants: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Linghang Zhuang, Stefan Peters, Herbert Nar
  • Publication number: 20140023614
    Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.
    Type: Application
    Filed: March 21, 2012
    Publication date: January 23, 2014
    Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
  • Publication number: 20140018357
    Abstract: The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Jeremy Robert Greenwood