Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 546/118)
  • Patent number: 8754082
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: June 17, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
  • Patent number: 8754103
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein W1, W2, W3, R1, Q, X1, X2 and X3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: June 17, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Gregory Notte, Eric Parkhill, Thao Perry, Jeff Zablocki
  • Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • 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
  • 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
  • Patent number: 8735586
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventors: Jorge Alonso, Andreas Lindenschmidt, Marc Nazaré, Matthias Urmann, Nis Halland, Omar Rkyek
  • Patent number: 8729107
    Abstract: Embodiments of the present disclosure provide a novel pyridine, pharmaceutical compositions comprising such pyridine, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord. In at least one embodiment of the method, the method comprises the step of administering to the mammal in need thereof with a pharmaceutical composition, or pharmaceutically acceptable salt, comprising 4-aminopyridine-3-methanol.
    Type: Grant
    Filed: September 9, 2010
    Date of Patent: May 20, 2014
    Assignee: Purdue Research Foundation
    Inventors: Richard B. Borgens, Riyi Shi, Stephen R. Byrn, Daniel T. Smith
  • Patent number: 8722703
    Abstract: The present invention relates to the use of compounds with fused amino pyridine core for the treatment of malignancies associated with brain and lung. The oral administration of compounds of the instant application results in effective brain penetration and provides for non-intrusive treatment of brain and lung tumors.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: May 13, 2014
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Changgeng Qian
  • Publication number: 20140128426
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 8, 2014
    Applicant: Siga Technologies Inc.
    Inventor: Siga Technologies Inc.
  • Publication number: 20140128389
    Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.
    Type: Application
    Filed: October 15, 2010
    Publication date: May 8, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Randall L. Halcomb, Paul A. Roethle
  • Publication number: 20140121219
    Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 1, 2014
    Applicant: Proximagen Limited
    Inventors: Edward Savory, Michael Higginbottom, Kathryn Oliver, Viet-Anh Anne Horgan
  • Publication number: 20140113917
    Abstract: The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2 antagonistic activity, wherein L, Y1, Y2, Y3, Y4, Y5, Z, R1, R2, R3 and n have one of the meanings as indicated in the specification and claims, to their use as medicaments, to pharmaceutical compositions containing said compounds and to pharmaceutical compositions containing said compounds in combination with one or more active substances.
    Type: Application
    Filed: March 15, 2012
    Publication date: April 24, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Boehringer Ingelheim International GmbH
  • Publication number: 20140113932
    Abstract: The present invention relates to a crystal of 1-ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)oxy]phenyl}-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one useful as a prophylactic or therapeutic agent for schizophrenia and the like, which shows an X-ray powder diffraction pattern having characteristic peaks at interplaner spacings (d) of 13.59 plus or minus 0.2 and 6.76 plus or minus 0.2 Angstroms in powder X-ray diffraction.
    Type: Application
    Filed: June 21, 2012
    Publication date: April 24, 2014
    Inventor: Katsuhiko Yamamoto
  • Patent number: 8703794
    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 and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: April 22, 2014
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 8703796
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: April 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer
  • Publication number: 20140100245
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.
    Type: Application
    Filed: November 27, 2013
    Publication date: April 10, 2014
    Applicant: SIGA TECHNOLOGIES, INC.
    Inventors: Dongcheng Dai, DENNIS E. HRUBY, TOVE C. BOLKEN, SEAN M. AMBERG, TRAVIS K. WARREN
  • Patent number: 8686150
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: April 1, 2014
    Assignee: Sanofi
    Inventors: Stephanie Hachtel, Oliver Plettenburg, Christian Schoenau, Matthias Loehn, Stefania Pfeiffer-Marek, Maria Mendez-Perez, Aimo Kannt, Juergen Dedio, Markus Kohlmann, Alexander Schiffer, Guillaume Begis, Olivier Duclos, Frederic Jeannot
  • Publication number: 20140088124
    Abstract: Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
    Type: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Inventors: Robert J. DeVita, QingMei Hong, Zhong Lai, Kevin D. Dykstra, Yang Yu, Jian Liu, Donald M. Sperbeck, Tianying Jian, Deodial Guiadeen, Ginger Xu-qiang Yang, Zhicai Wu, Shuwen He, Pauline C. Ting, Robert Aslanian, Jeffrey T. Kuethe, James Balkovec, Rongze Kuang, Gang Zhou, Heping Wu
  • Publication number: 20140088138
    Abstract: This invention relates to the discovery of novel forms of Compound 1, including solvates, hydrates, and other crystalline forms. These novel forms of Compound 1 may impart advantages in pharmaceutical formulations incorporating them, including improved stability and bioavailability.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 27, 2014
    Applicant: Debiopharm International SA
    Inventors: Noel Hamill, James Moody, Sébastien Chabaud, Arnaud Hamel
  • Publication number: 20140088110
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
  • Patent number: 8680098
    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: Grant
    Filed: February 25, 2011
    Date of Patent: March 25, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • Patent number: 8680089
    Abstract: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.
    Type: Grant
    Filed: January 17, 2011
    Date of Patent: March 25, 2014
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Zhenhua Huang, Yan Zhang, Yuntao Song
  • Patent number: 8673936
    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: Grant
    Filed: March 13, 2013
    Date of Patent: March 18, 2014
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Publication number: 20140073788
    Abstract: Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 13, 2014
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventors: Andrei W. Konradi, Jenifer L. Smith, Michael S. Dappen, Christopher M. Semko
  • Publication number: 20140073640
    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: Application
    Filed: August 12, 2013
    Publication date: March 13, 2014
    Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
  • Publication number: 20140073635
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: November 8, 2013
    Publication date: March 13, 2014
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • Patent number: 8669368
    Abstract: The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: March 11, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: David K. Leahy, Yu Fan, Collin Chan, Lopa V. Desai, Sunil S. Patel, Masano Sugiyama
  • Publication number: 20140066433
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 6, 2014
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog, Adrian Hobson
  • Patent number: 8664241
    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: Grant
    Filed: September 6, 2013
    Date of Patent: March 4, 2014
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Patent number: 8658646
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: February 25, 2014
    Assignee: Hoffmann-LaRoche Inc.
    Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
  • Patent number: 8658637
    Abstract: Compounds of Formula (IA) wherein R1, R2, R3, A, B, C, D, E, G, X, Y, and Z are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Daniel Kuzmich, Darren DiSalvo, Hossein Razavi, Michael Jason Burke
  • Patent number: 8658794
    Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: February 25, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
  • Publication number: 20140045831
    Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Ildiko Maria Buck, Gianni Chessari, Steven Howard, David Charles Rees, Alison Jo-Anne Woolford
  • Publication number: 20140038948
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Application
    Filed: June 25, 2013
    Publication date: February 6, 2014
    Applicant: Plexxikon Inc.
    Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
  • Patent number: 8637542
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PB kinases, tryosine kinases and protein kinases such as mTOR. Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: January 28, 2014
    Assignee: Intellikine, Inc.
    Inventors: Yi Liu, Pingda Ren, Liansheng Li, Katrina Chan, Troy Edward Wilson
  • Publication number: 20140018373
    Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.
    Type: Application
    Filed: December 22, 2011
    Publication date: January 16, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
  • Patent number: 8623347
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.
    Type: Grant
    Filed: January 14, 2009
    Date of Patent: January 7, 2014
    Assignee: Siga Technologies, Inc.
    Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Travis K. Warren
  • Publication number: 20140005170
    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: September 6, 2013
    Publication date: January 2, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Publication number: 20140005164
    Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
    Type: Application
    Filed: March 23, 2012
    Publication date: January 2, 2014
    Applicant: Siena Biotech S.p.A.
    Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
  • Publication number: 20140005206
    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 and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Application
    Filed: September 5, 2013
    Publication date: January 2, 2014
    Applicant: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Publication number: 20130345193
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130338164
    Abstract: Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 19, 2013
    Applicant: ELAN PHARMACEUTICALS, INC.
    Inventor: Elan Pharmaceuticals, Inc.
  • Patent number: 8609688
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: December 17, 2013
    Assignee: ArQule, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Patent number: 8604052
    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 and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases due to mutations in Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: July 10, 2013
    Date of Patent: December 10, 2013
    Assignee: Samumed, LLC
    Inventors: John Hood, David Mark Wallace, Sunil Kumar KC
  • Publication number: 20130324527
    Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 5, 2013
    Applicant: Janssen R&D Ireland
    Inventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdella Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
  • Patent number: 8598190
    Abstract: There are provided compounds of formula (I), wherein R1, R6, R8, Q2, Q3, Q3a, Q4, L and A have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation and/or cancer.
    Type: Grant
    Filed: September 25, 2009
    Date of Patent: December 3, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Roland Pfau, Kirsten Arndt, Henri Doods, Norbert Hauel, Klaus Klinder, Raimund Kuelzer
  • Patent number: 8598217
    Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: December 3, 2013
    Assignees: Astex Therapeutics Ltd., Novartis AG
    Inventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
  • Publication number: 20130317213
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • Patent number: 8592395
    Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: November 26, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant