Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/234.2)
  • Fused 2-aminothiazole compounds
    Patent number: 8765747
    Abstract: The present application relates to therapeutic organic compounds of formula (I), wherein Q, R1, R2, R3, and R4 are defined herein. The invention also relates to pharmaceutical compositions comprising an effective amount of a therapeutic organic compound; and methods for treating and preventing disease such as cancer comprising administering and effective amount of a therapeutic organic compound to a subject in need thereof.
    Type: Grant
    Filed: June 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Hwan Geun Choi, Taebo Sim, Nathanael Gray, Wenjun Zhou, Jae Won Chang, Jianming Zhang, Ellen Weisberg
  • HEPATITIS B ANTIVIRAL AGENTS
    Publication number: 20140178337
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Inventors: George D. Hartman, Osvaldo A. Flores
  • Substituted Imidazopyridines as HDM2 Inhibitors
    Publication number: 20140179680
    Abstract: The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Inventors: Matthew P. Christopher, Francesc Xavier Fradera Llinas, Michelle Machacek, Michelle Martinez, Michael Hale Reutershan, Manami Shizuka, Binyuan Sun, Christopher Francis Thompson, B. Wesley Trotter, Matthew E. Voss, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll
  • NOVEL PYRIMIDINE COMPOUNDS AS mTOR AND PI3K INHIBITORS
    Publication number: 20140178360
    Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGY
    Inventors: Mann-Yan KUO, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
  • INDAZOLE INHIBITORS OF THE WNT SIGNAL PATHWAY AND THERAPEUTIC USES THEREOF
    Publication number: 20140179696
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 26, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • PYRIDIN-2(1H)-ONE DERIVATIVES USEFUL AS MEDICAMENTS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS, TRANSPLANT REJECTION, IMMUNE-MEDIATED AND INFLAMMATORY DISEASES
    Publication number: 20140170110
    Abstract: Compounds having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
    Type: Application
    Filed: May 21, 2012
    Publication date: June 19, 2014
    Applicant: ALMIRALL, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
  • Fused Pyrazoles as FGFR Inhibitors
    Publication number: 20140171405
    Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Incyte Corporation
    Inventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
  • AZABENZOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
    Publication number: 20140171408
    Abstract: Provided are compounds of Formula I, stereoisomers, tautomers, solvates, prodrugs and pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, and methods of manufacturing a compound of Formula I.
    Type: Application
    Filed: February 20, 2014
    Publication date: June 19, 2014
    Applicant: Genentech, Inc.
    Inventors: Toby Jonathan Blench, Charles Ellwood, Simon Charles Goodacre, Yingjie Lai, Jun Liang, Calum MacLeod, Steven R. Magnuson, Vickie Hsiao-Wei Tsui, Karen Williams, Birong Zhang
  • METHODS AND COMPOSITIONS FOR STIMULATING NEUROGENESIS AND INHIBITING NEURONAL DEGENERATION USING ISOTHIAZOLOPYRIMIDINONES
    Publication number: 20140171428
    Abstract: The present invention provides methods and compositions comprising compounds useful for stimulating neurogenesis. The methods and compositions comprising compounds are also useful for inhibiting neuronal degeneration. Thus, the present invention can be used in the treatment of diseases and conditions characterized by neuronal loss and reduced neurogenesis including Alzheimer's disease, stroke, traumatic brain injury, traumatic nerve injury, and depression. This invention is useful for research products including single agents or mixtures of agents to promote, proliferate, differentiate, or maintain neurons from stem or progenitor cells.
    Type: Application
    Filed: November 13, 2013
    Publication date: June 19, 2014
    Applicant: NEURONASCENT, INC.
    Inventor: Judith KELLEHER-ANDERSSON
  • Pyrimidine substituted purine compounds as kinase (S) inhibitors
    Patent number: 8754080
    Abstract: The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: June 17, 2014
    Assignee: Verastem, Inc.
    Inventors: DiZhong Chen, Meredith Williams
  • Cycloalkyl containing thienopyrimidines for pharmaceutical compositions
    Patent number: 8754079
    Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
    Type: Grant
    Filed: February 25, 2011
    Date of Patent: June 17, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Joerg Kley, Elke Langkopf, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter, Phillip Black, Wesley Blackaby, Ian Linney
  • Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors
    Publication number: 20140163003
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: July 24, 2013
    Publication date: June 12, 2014
    Applicant: Forma Therapeutics, Inc.
    Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
  • Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors
    Publication number: 20140163006
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: July 24, 2013
    Publication date: June 12, 2014
    Applicant: Forma Therapeutics, Inc.
    Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
  • Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors
    Publication number: 20140163004
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: July 24, 2013
    Publication date: June 12, 2014
    Applicant: Forma Therapeutics, Inc.
    Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
  • Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors
    Publication number: 20140163007
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: July 24, 2013
    Publication date: June 12, 2014
    Applicant: Forma Therapeutics, Inc.
    Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
  • INHIBITORS OF BRUTON'S TYROSINE KINASE
    Publication number: 20140163027
    Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik Verner, Wei Chen
  • PYRAZOLO[3,4-d]PYRIMIDINE COMPOUNDS, THEIR PREPARATION AND USE AS SIGMA LIGANDS
    Publication number: 20140163010
    Abstract: New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments.
    Type: Application
    Filed: July 13, 2012
    Publication date: June 12, 2014
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Maria Rosa Cuberes-Altisent, Jordi Corbera-Arjona, Jose Luis Diaz-Fernanadez, Carmen Almansa-Rosales
  • Pyrido-[2,3-D] Pyrimidines and Their Use as Kinase Inhibitors
    Publication number: 20140163005
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: July 24, 2013
    Publication date: June 12, 2014
    Applicant: Forma Therapeutics, Inc.
    Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
  • 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER
    Publication number: 20140163026
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.
    Type: Application
    Filed: April 9, 2012
    Publication date: June 12, 2014
    Applicant: Afraxis Holdings, Inc.
    Inventors: David Campbell, Sergio G. Duron
  • DIHYDROPYRROLO PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS
    Publication number: 20140163023
    Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, T0, o have the meaning as cited in the description and the claims. The compounds of formula I are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds of formula I, the preparation of such compounds as well as the use as medicaments.
    Type: Application
    Filed: April 2, 2012
    Publication date: June 12, 2014
    Applicant: Cellzome Limited
    Inventors: Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, Jane Elizabeth Scanlon, Rita Joana Rodrigues Adrego
  • 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
    Publication number: 20140155393
    Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
    Type: Application
    Filed: November 8, 2011
    Publication date: June 5, 2014
    Applicant: Janssen Pharmaceuticals, Inc.
    Inventors: José Maria Cid-Núñez, Andrés Avelino Trabanco-Suárez, Juan Antonio Vega Ramiro, Daniel Oehlrich, Gary John Tresadern, Gregor James Macdonald
  • HETEROCYCLE AMINES AND USES THEREOF
    Publication number: 20140155379
    Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 5, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
  • SUBSTITUTED AZA-BICYCLIC IMIDAZOLE DERIVATIVES USEFUL AS TRPM8 RECEPTOR MODULATORS
    Publication number: 20140155395
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Application
    Filed: February 4, 2014
    Publication date: June 5, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • Chemical Compounds - 759
    Publication number: 20140155394
    Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
    Type: Application
    Filed: June 21, 2013
    Publication date: June 5, 2014
    Applicant: Astrazeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Pyrazolopyrimidine derivatives
    Patent number: 8741896
    Abstract: Compounds of the formula (I), in which X, R1 and R2 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: June 3, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Peter Buchstaller, Ulrich Emde, Markus Klein, Christina Esdar, Joerg Bomke
  • HETEROCYCLYL COMPOUNDS AS HISTAMINE H3 RECEPTOR LIGANDS
    Publication number: 20140148440
    Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.
    Type: Application
    Filed: November 15, 2010
    Publication date: May 29, 2014
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti
  • Oxazolopyrimidines as Edg-1 receptor agonists
    Patent number: 8735387
    Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R1, R2 and R3 are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Dieter Kadereit, Matthias Schaefer, Werngard Czechtizky
  • NEW MACROLIDES AND THEIR USE
    Publication number: 20140142100
    Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
    Type: Application
    Filed: January 24, 2014
    Publication date: May 22, 2014
    Applicant: BASILEA PHARMACEUTICA AG
    Inventors: Johannes Laurenz Kellenberger, Jürg Dreier
  • Purinone Derivatives as Tyrosine Kinase Inhibitors
    Publication number: 20140142099
    Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: November 19, 2013
    Publication date: May 22, 2014
    Applicant: Principia Biopharma Inc.
    Inventor: Timothy D. Owens
  • TRIAZOLOPYRAZINE
    Publication number: 20140142098
    Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Christian SMETHURST
  • PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING DEGENERATIVE BRAIN DISEASE AND METHOD OF SCREENING THE SAME
    Publication number: 20140142089
    Abstract: A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease.
    Type: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Changjoon Justin LEE, SEONMI JO, BOEUN YOON, HYUNAH CHOO, JI YOON KIM, DAESOO KIM
  • Pyrimido-pyridazinone compounds and methods of use thereof
    Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Pyrido-, Pyrazo- and Pyrimido-Pyrimidine Derivatives as mTOR Inhibitors
    Publication number: 20140135315
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: April 9, 2013
    Publication date: May 15, 2014
    Applicant: KuDOS Pharmaceuticals Limited
    Inventor: KuDOS Pharmaceuticals Limited
  • NOVEL BENZYLAMINE DERIVATIVES AND THEIR UTILITY AS CHOLESTEROL ESTER-TRANSFER PROTEIN INHIBITORS
    Publication number: 20140134235
    Abstract: The present invention provides, among other things, new benzylamine compounds, compositions comprising benzylamine compounds, methods of making benzylamine compounds, and methods of using benzylamine compounds for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism.
    Type: Application
    Filed: October 14, 2013
    Publication date: May 15, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Anima BARUAH, Dibyendu DE, Ish Kumar KHANNA, Sivaram PILLARISETTI, Santanu MAITRA, Christopher W. ALEXANDER, Jennepalli SREENU, Indu Dagar, Shanavas Alikunju
  • PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES
    Publication number: 20140135312
    Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicants: Astex Therapeutics Ltd., Novartis AG
    Inventors: Gilbert BESONG, Christopher Thomas Brain, Clinton A. Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Huo, Steven Howard, Yue Ll, Yipin Lu, Paul Mortenston, Troy Smith, Moo Je Sung, Steven Woodhead, Wojciech Wrona, Bharat Lagu
  • DERIVATIVES OF PURINE OR DEAZAPURINE USEFUL FOR THE TREATMENT OF (INTER ALIA) VIRAL INFECTIONS
    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
  • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    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
  • TARGETING AN HIV-1 NEF-HOST CELL KINASE COMPLEX
    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
  • Tetrahydro-Pyrido-Pyrimidine Derivatives
    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
  • PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME
    Publication number: 20140121205
    Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.
    Type: Application
    Filed: March 8, 2013
    Publication date: May 1, 2014
    Applicant: Usher III Initiative
    Inventors: Roland Werner Bürli, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
  • TREATMENT OF RHEUMATOID ARTHRITIS AND ASTHMA USING PI3 KINASE INHIBITORS
    Publication number: 20140120060
    Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating rheumatoid arthritis or asthma.
    Type: Application
    Filed: March 15, 2013
    Publication date: May 1, 2014
    Applicant: INFINITY PHARMACEUTICALS, INC.
    Inventors: Vito J. Palombella, Jeffrey L. Kutok
  • TREATMENT OF CANCERS USING PI3 KINASE ISOFORM MODULATORS
    Publication number: 20140120083
    Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating cancers or hematologic disorders.
    Type: Application
    Filed: March 15, 2013
    Publication date: May 1, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Howard M. STERN, Jeffery L. KUTOK
  • SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
    Publication number: 20140121200
    Abstract: Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
    Type: Application
    Filed: June 7, 2012
    Publication date: May 1, 2014
    Applicant: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Wei-Guo Su, Wei Deng, Jianguo Ji
  • Fused thiazole derivatives as kinase inhibitors
    Patent number: 8710054
    Abstract: A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Grant
    Filed: November 20, 2012
    Date of Patent: April 29, 2014
    Assignee: UCB Pharma, S.A.
    Inventors: Rikki Peter Alexander, Pavandeep Singh Aujla, Karen Viviane Lucile Crepy, Anne Marie Foley, Richard Jeremy Franklin
  • Phosphoinositide 3-kinase inhibitor with a zinc binding moiety
    Patent number: 8710219
    Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: April 29, 2014
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
  • Azaquinazoline Inhibitors of Atypical Protein Kinase C
    Publication number: 20140113882
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 24, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Antiplatelet agent
    Patent number: 8703760
    Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: April 22, 2014
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
  • Thiazole derivatives for the treatment of diseases such as cancer
    Patent number: 8703961
    Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: April 22, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Hannes Koolman
  • Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
    Patent number: 8703767
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: April 1, 2012
    Date of Patent: April 22, 2014
    Assignee: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Novel Heterocyclic Derivatives and Their Use in the Treatment of Neurological Disorders
    Publication number: 20140107118
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Application
    Filed: December 20, 2013
    Publication date: April 17, 2014
    Applicant: NOVARTIS AG
    Inventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE