Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
  • Patent number: 8853205
    Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: October 7, 2014
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Venkata Kiran Vemuri
  • Publication number: 20140296208
    Abstract: There are provided compounds of formula I, wherein R1A to R1E, R2 to R5, L and X1 to X3 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Applicants: Topivert Pharma Limited, Respivert Limited
    Inventors: Thomas Matthew BAKER, Matthew Colin Thor FYFE, Gareth William HARBOTTLE, Vedran HASIMBEGOVIC, Premji MEGHANI, Aaron RIGBY, Colin SAMBROOK-SMITH, Stephen Malcolm THOM
  • Publication number: 20140288044
    Abstract: The invention relates to compounds, pharmaceutical compositions and medicaments comprising such compounds, and the use of these compounds, compositions, and medicaments in methods of treating diseases and disorders.
    Type: Application
    Filed: April 12, 2012
    Publication date: September 25, 2014
    Applicant: Alzheimer's Institute of America, Inc.
    Inventors: Ryan Holcomb, Paul R. Sebahar, Kazuyuki Suzuki, Donald A. McLeod, David M. Dastrup, Christophe Hoarau, Robert J. Halter, Matthew Gregory Bursavich, Mark D. Shenderovich, Burt Richards, Paul L. Bartel
  • Publication number: 20140288017
    Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 25, 2014
    Inventors: William L. Jorgensen, Karen S. Anderson
  • Publication number: 20140288049
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Application
    Filed: June 9, 2014
    Publication date: September 25, 2014
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Publication number: 20140288073
    Abstract: The present invention relates to a method of treating gastrointestinal stromal tumors (GIST), especially GIST, which is progressing after imatinib therapy or after imatinib and sunitinib therapy, using a combination comprising (a) a c-kit inhibitor and (b) a PI3K inhibitor or FGFR inhibitor.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 25, 2014
    Applicant: Novartis AG
    Inventors: John E. Monahan, Fang Li
  • Publication number: 20140288067
    Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: Epizyme, Inc.
    Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
  • Publication number: 20140275088
    Abstract: In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Timothy J. Cardozo, Jürgen Bosch, Sondra Maureen Nemetski
  • Publication number: 20140275083
    Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Thomas Raymond CAFERRO, Zhuoliang CHEN, Young Shin CHO, Abran Q. COSTALES, Julian Roy LEVELL, Gang LIU, James R. MANNING, Martin SENDZIK, Cynthia SHAFER, Michael David SHULTZ, James SUTTON, Yaping WANG, Qian ZHAO
  • Publication number: 20140275006
    Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
  • Publication number: 20140275085
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Michael D. Kaufman, Daniel L. Flynn, YuMi Ahn, Lakshminarayana Vogeti, Timothy Malcolm Caldwell
  • Publication number: 20140275086
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140275087
    Abstract: The present invention relates to pyrrolidine derivatives of the formula (I), or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such pyrrolidine derivatives, and the use of such pyrrolidine derivatives for therapeutic purposes. The pyrrolidine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 17, 2014
    Publication date: September 18, 2014
    Inventors: Wilhelm Amberg, Frauke Pohlki, Udo Lange, Ying X. Wang, Hongyu H. Zhao, Huan-Qiu Li, Jason T. Brewer, Irini Zanze, Justin Dietrich, Anil Vasudevan, Stevan W. Djuric, Yanbin Lao, Charles W. Hutchins
  • Publication number: 20140275082
    Abstract: Disclosed herein are compounds that inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: February 10, 2014
    Publication date: September 18, 2014
    Inventors: Zhi-Fu Tao, Xilu Wang, Michael Wendt, Andrew Souers, Andrew Judd, Aaron Kunzer, Gerard Sullivan
  • Publication number: 20140275003
    Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
  • Publication number: 20140271543
    Abstract: New pyridin-2(1H)-one derivatives 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: July 23, 2012
    Publication date: September 18, 2014
    Applicant: ALMIRALL, S.A.
    Inventors: Paul Robert Eastwood, Jordi Bach Taña, Lluis Miquel Pages Santacana
  • Publication number: 20140275057
    Abstract: The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.
    Type: Application
    Filed: September 2, 2011
    Publication date: September 18, 2014
    Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
  • Publication number: 20140275084
    Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic diseases. Provided herein are substituted imidazole-pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase enzymes. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Applicant: Quanticel Pharmaceuticals, Inc.
    Inventors: Toufike Kanouni, Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal
  • Patent number: 8835419
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: September 16, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. MacMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20140256701
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
  • Patent number: 8828996
    Abstract: The invention relates to morpholine spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: September 9, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Sabina Hadida-Ruah, Hayley Marie Binch, Michael Paul DeNinno, Lev Tyler Dewey Fanning, Bryan A. Frieman, Peter Diederik Jan Grootenhuis, Nicole Hilgraf, Pramod Joshi, Edward Adam Kallel, Mark Thomas Miller, Joseph Pontillo, Alina Silina, Urvi Jagdishbhai Sheth, Dennis James Hurley, Vijayalaksmi Arumugam
  • Patent number: 8828999
    Abstract: Pyrimidine compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof, are useful are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases and in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.
    Type: Grant
    Filed: February 26, 2013
    Date of Patent: September 9, 2014
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Ganapavarapu Sharma, Venkatesan Parameswaran, Gopalan Balasubramanian, Santosh Vishwakarma, Sanjeev Saxena
  • Patent number: 8822464
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: November 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Patent number: 8822451
    Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
  • Publication number: 20140243290
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Patent number: 8815856
    Abstract: Disclosed are crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.
    Type: Grant
    Filed: March 18, 2014
    Date of Patent: August 26, 2014
    Assignee: Glaxo Group Limited
    Inventors: Richard Bellingham, Andrew Mark Buswell, Victoria Ironmonger, Michael Urquhart
  • Publication number: 20140235639
    Abstract: Compounds of formula (I) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is a group selected from 2,6-dimethyl-3-pyridyl or 4,6-dimethyl-3-pyridyl, R4 represents methyl and R5 represents hydrogen or methyl or, R4 and R5 together with the nitrogen atom to which they are attached represent morpholino and pharmaceutically acceptable derivatives thereof are described, as are processes for their preparation, pharmaceutical compositions containing them and their use in medicine, particularly their use as oxytocin antagonists.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Inventors: Alan David Borthwick, Deirdre Mary Bernadette Hickey, John Liddle, Andrew McMurtrie Mason
  • Publication number: 20140235638
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 21, 2014
    Applicant: AbbVie Inc.
    Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
  • Publication number: 20140235640
    Abstract: The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Publication number: 20140235620
    Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
    Type: Application
    Filed: September 26, 2012
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
  • Publication number: 20140235579
    Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • Patent number: 8809331
    Abstract: Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: November 28, 2012
    Date of Patent: August 19, 2014
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet L. Gunzner-Toste, Daniel Shore, Zachary Kevin Sweeney, Shumei Wang, Guiling Zhao
  • Publication number: 20140228322
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Celgene Avilomics Research, Inc.
    Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
  • Patent number: 8802674
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: August 12, 2014
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet Gunzner-Tate, Daniel Shore, Zachary Kevin Sweeney, Shumei Wang, Guiling Zhao
  • Patent number: 8802669
    Abstract: Disclosed are dihydropyrimidine compounds and preparation methods, pharmaceutical compositions and uses thereof. Specifically, the compounds described herein in general formula (I), or their isomers, pharmaceutically acceptable salts or hydrates are provided, wherein each variable has the meaning as defined in the description. Also provided are a process for preparing the compounds of the general formula (I), the use of the compounds, an isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof as a medicament, in particular as a medicament for the treatment and/or prevention of Hepatitis B.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: August 12, 2014
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences, P.L.A. China
    Inventors: Song Li, Xiaoqian Xu, Guoming Zhao, Lili Wang, Hua Guan, Junhai Xiao, Wu Zhong, Zhibing Zheng, Yunde Xie, Xingzhou Li, Xiaokui Wang, Xinbo Zhou, Hongying Liu
  • Patent number: 8802657
    Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
    Type: Grant
    Filed: October 22, 2012
    Date of Patent: August 12, 2014
    Assignees: Millennium Pharmaceuticals, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Jennifer Cossrow, Bing Guan, John Howard Jones, Gnanasambandam Kumaravel, Alexey Lugovskoy, Hairuo Peng, Noel Powell, Brian C. Raimundo, Hiroko Tanaka, Jeffrey Vessels, Thomas Wynn, Zhili Xin
  • Patent number: 8802673
    Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof, which have a good affinity to the trace amine associated receptors TAAR1, so that they can be used for the treatment of depression, anxiety disorders and bipolar disorder.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: August 12, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: Guido Galley, Roger David Norcross, Philippe Pflieger
  • Patent number: 8802672
    Abstract: The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein R1, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: August 12, 2014
    Assignee: Richter Gedeon Nyrt.
    Inventors: Gizella Bartane Szalai, Eva Againe Csongor, Gyorgy Domany, Istvan Gyertyan, Bela Kiss, Judit Laszy, Katalin Saghy, Eva Schmidt, Sandor Farkas, Zsolt Komlodi
  • Publication number: 20140221366
    Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: June 11, 2012
    Publication date: August 7, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
  • Publication number: 20140221311
    Abstract: The present invention relates to compounds of Formula (I), or a form thereof, wherein ring A, R1, R2, R3, R3?, L, W, and V are as defined herein, useful as FLAP modulators. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I).
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Genesis M. Bacani, Wendy Eccles, Anne E. Fitzgerald, Steven D. Goldberg, Michael D. Hack, Natalie A. Hawryluk, William M. Jones, John M. Keith, Paul Krawczuk, Alec D. Lebsack, Alice Lee-Dutra, Jing Liu, Kelly J. McClure, Steven P. Meduna, Daniel J. Pippel, Mark D. Rosen, Zachary S. Sales
  • Publication number: 20140221374
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
    Type: Application
    Filed: March 16, 2012
    Publication date: August 7, 2014
    Applicant: Ruga Corporation
    Inventors: Jean-Michel Vernier, Stephanie Hopkins, Pierre-Yves Bounaud, Patrick O'Connor, David Matthews, Steve Bender
  • Publication number: 20140221361
    Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, C-19 modified triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formulas I and II: These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Inventors: Jacob Swidorski, Brian Lee Venables, Zheng Liu, Ny Sin, Nicholas A. Meanwell, Alicia Regueiro-Ren
  • Publication number: 20140213574
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Application
    Filed: April 16, 2014
    Publication date: July 31, 2014
    Applicant: Celgene Avilomics Research, Inc.
    Inventors: Juswinder Singh, Russell Petter, Richland Wayne Tester, Arthur F. Kluge, Hormoz Mazdiyasni, William Frederick Westlin, III, Deqiang Niu, Lixin Qiao
  • Publication number: 20140213580
    Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.
    Type: Application
    Filed: June 18, 2012
    Publication date: July 31, 2014
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
  • 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
  • Patent number: 8785440
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: July 22, 2014
    Assignees: Biogen Idec MA, Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Minna Bui, Patrick Conlon, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20140200218
    Abstract: Disclosed are crystalline forms of (3R,6R)-3-(2,3-dihydro-1H-inden-2-yl)-1-[(1R)-1-(2,6-dimethyl-3-pyridinyl)-2-(4-morpholinyl)-2-oxoethyl]-6-[(1S)-1-methylpropyl]-2,5-piperazinedione benzenesulfonate salt and pharmaceutical compositions thereof. Also disclosed are processes for the preparation the above compounds and methods for use thereof.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: Glaxo Group Limited
    Inventors: Richard Bellingham, Andrew Mark Buswell, Victoria Ironmonger, Michael Urquhart
  • Publication number: 20140200217
    Abstract: The invention provides methods for modulating, e.g., antagonizing, the activity of the Hedgehog signaling pathway, and for treating Hedgehog related disorders such as cancers (e.g., medulloblastoma). In particular, the invention provides methods for inhibiting aberrant growth states resulting from phenotypes such as Ptch loss-of-function, Hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function by administering to a mammal combinations of Smoothened inhibitors (e.g., a compound of Formula I, Formula II, or Formula III, or any of the compounds listed herein or incorporated by reference) and cholesterol biosynthesis pathway inhibitors (e.g., statins), Gli inhibitors, and/or Phosphatidylinositol 3-kinase (PI3K) inhibitors.
    Type: Application
    Filed: January 24, 2014
    Publication date: July 17, 2014
    Inventors: Marion Dorsch, John E. Monahan, Michael Patrick Morrissey, Shifeng Pan, Juliet Williams
  • 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: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or