The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
  • Patent number: 8901136
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 2, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Patent number: 8901135
    Abstract: Substituted bicyclic heteroaryls having the following formula where the variables are as defined herein, and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-pro
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: December 2, 2014
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Patent number: 8895036
    Abstract: The invention relates to transdermal compositions including nifedipine, pentoxifylline, ketamine hydrochloride, gabapentin, lidocaine, and prilocaine that may be used to treat conditions such as circulatory disorders and peripheral neuropathy. Additionally, methods of the invention are directed to treating conditions such as circulatory disorders, peripheral neuropathy, wound healing, blood flow issues, or the like, comprising the steps of transdermal or topical administration of the compositions.
    Type: Grant
    Filed: March 3, 2014
    Date of Patent: November 25, 2014
    Assignee: JCDS Holdings, LLC
    Inventor: Jay Richard Ray, II
  • Patent number: 8895570
    Abstract: The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: November 25, 2014
    Assignee: AstraZeneca AB
    Inventors: Phillip Abbott, Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada, Satoshi Onuma
  • Publication number: 20140343057
    Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Vito J. PALOMBELLA, David G. WINKLER
  • Publication number: 20140343033
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Applicant: Takeda Califomia, Inc.
    Inventors: Edcon Chang, Michael B. Wallace
  • Publication number: 20140341894
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: June 5, 2014
    Publication date: November 20, 2014
    Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Liansheng LI, Katrina CHAN, Christian ROMMEL
  • Publication number: 20140336175
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 13, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Publication number: 20140323441
    Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
  • Publication number: 20140323439
    Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient.
    Type: Application
    Filed: July 3, 2014
    Publication date: October 30, 2014
    Inventors: W. Michael GALLATIN, Roger G. ULRICH, Neill A. GIESE
  • Publication number: 20140309212
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: June 26, 2014
    Publication date: October 16, 2014
    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: 20140303151
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: October 9, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy
  • Publication number: 20140303177
    Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITED
    Inventors: Valerio BERDINI, Robert George BOYLE, Gordon SAXTY, David Winter WALKER, Steven John WOODHEAD, Paul Graham WYATT, Alastair DONALD, John CALDWELL, Ian COLLINS, Tatiana Faria DA FONSECA
  • Patent number: 8853156
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.
    Type: Grant
    Filed: August 5, 2009
    Date of Patent: October 7, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Publication number: 20140296261
    Abstract: The invention provides a compound represented by formula (I) which may modulate a kinase, and a pharmaceutical composition thereof, as well as the method for preventing or treating a protein kinase mediated disease or condition.
    Type: Application
    Filed: November 14, 2012
    Publication date: October 2, 2014
    Applicants: CENTAURUS BIOPHARMA CO., LTD., CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD,
    Inventors: Dengming Xiao, Jijun Li, Yan Zhu, Yuandong Hu, Huting Wang, Zhe Wang, Zanping Wang, Yongheng Wei, Yinghui Sun, Qiong Wu, Hui Zhang, Yong Peng, Fansheng Kong, Ying Sun, Hong Luo, Yongxin Han
  • Publication number: 20140296207
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: June 11, 2014
    Publication date: October 2, 2014
    Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
  • Patent number: 8846696
    Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: September 30, 2014
    Assignees: Cyclacel Limited, Cancer Research Technology Limited
    Inventors: Peter Martin Fischer, Michael Jarman, Edward McDonald, Bernard Nutley, Florence Raynaud, Stuart Wilson, Paul Workman
  • Publication number: 20140288099
    Abstract: Compound (I), and pharmaceutically acceptable salts thereof, are inducers of human interferon. Certain discrete and particular dosages of Compound (I) may be particularly useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and allergic asthma.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 25, 2014
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Claire Louise Ambery, Christopher David Edwards
  • Publication number: 20140275127
    Abstract: The present invention provides fused derivatives of Formula I: that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: May 29, 2014
    Publication date: September 18, 2014
    Applicant: Incyte Corporation
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
  • Patent number: 8835420
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: September 16, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
  • Patent number: 8828998
    Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating lupus, a fibrotic condition, or inflammatory myopathies and other conditions (e.g., skin conditions).
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: September 9, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Vito J. Palombella, David G. Winkler
  • Patent number: 8809349
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: August 19, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Patent number: 8809336
    Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the
    Type: Grant
    Filed: September 4, 2013
    Date of Patent: August 19, 2014
    Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, David Winter Walker, Steven John Woodhead, Paul Graham Wyatt, Alastair Donald, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca
  • Publication number: 20140227351
    Abstract: Taste masked multi-layered particles include an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and including a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture including 60-90% (w/w) EC and 10-40% (w/w) HPMC, where the pharmaceutically active ingredient is water-soluble and includes either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions including such particles.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Martin FOLGER, Stefan LEHNER, Annette GRAVE, Norbet POELLINGER, Randolph SEIDLER
  • Publication number: 20140228287
    Abstract: A pharmaceutical composition includes 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or a pharmaceutically acceptable form thereof as pharmaceutically active compound for the therapy of a metabolic disorder or metabolic disease of a predominantly carnivorous non-human animal. It is especially useful for the therapy of diabetes and related diseases of predominantly carnivorous mammals like cats or dogs. The invention further provides respective uses of such compositions and of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or pharmaceutically acceptable forms thereof.
    Type: Application
    Filed: April 16, 2014
    Publication date: August 14, 2014
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Frerich DE VRIES, Dirk HOERSTERMANN, Ingo LANG, Michael MARK, Randolph SEIDLER, Leo THOMAS
  • Patent number: 8802684
    Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, or C1-6alkoxy; R2 is a group having the structure: n is an integer having a value of 1 to 6; Het is a 6-membered saturated heterocycle containing one nitrogen atom wherein Het is attached to the —(CH2)n— moiety at any carbon atom of the heterocycle; R3 is hydrogen, C1-8alkyl, or C3-7cycloalkylC0-6alkyl; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: August 12, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Helene Bazin-Lee, Diane Mary Coe, Charlotte Jane Mitchell, Stephen Allan Smith
  • 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: 20140221400
    Abstract: The present invention relates to the use of MPO inhibitors for the treatment of multiple system atrophy. The present invention also relates to the use of MPO inhibitors for the treatment of Huntington's disease. The present invention also relates to the use of MPO inhibitors for neuroprotection.
    Type: Application
    Filed: November 8, 2013
    Publication date: August 7, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Hakan Eriksson, Werner Poewe
  • Publication number: 20140206685
    Abstract: The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: INTELLIKINE LLC
    Inventors: Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN, Troy Edward WILSON
  • Publication number: 20140206684
    Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: INTELLIKINE LLC
    Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Katrina CHAN, Christian ROMMEL, Liansheng LI
  • Patent number: 8785456
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: July 22, 2014
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Patent number: 8765772
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: July 1, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 8759361
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: June 24, 2014
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • 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
  • 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: 20140148433
    Abstract: The present application relates to novel bicyclic azaheterocycles, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 29, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Lars Bärfacker, Stefan Weigand
  • Publication number: 20140142113
    Abstract: A method of treating inflammatory diseases with Adenosine 2B receptor antagonists in particular with xanthine derived inhibitors. The method involves supplying a therapeutically active amount of the compounds of FIG. 1 and in particular compound 1.
    Type: Application
    Filed: November 11, 2013
    Publication date: May 22, 2014
    Inventors: Michael W. Burnet, Thomas Stohr, Martin Donsbach
  • Publication number: 20140135301
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • 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: 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
  • 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
  • Patent number: 8703754
    Abstract: The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: in the form of a maleate salt, may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: April 22, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
  • Patent number: 8703777
    Abstract: Provided herein are substituted bicyclic compounds, e.g., compounds of Formula IV, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for inhibiting phosphatidyl inositol-3 kinase (PI3 kinase), e.g., for the treatment of various diseases and conditions associated with PI3 kinase activity, including but not limited to, cancer, inflammatory disease, immune disease, and respiratory disease.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: April 22, 2014
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
  • Publication number: 20140107098
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Application
    Filed: December 19, 2013
    Publication date: April 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
  • Publication number: 20140100224
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: June 26, 2013
    Publication date: April 10, 2014
    Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of California
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20140100237
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 10, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
  • Publication number: 20140088099
    Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: November 20, 2013
    Publication date: March 27, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda REN, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
  • Patent number: 8680076
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
    Type: Grant
    Filed: October 20, 2011
    Date of Patent: March 25, 2014
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
  • Publication number: 20140057901
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: February 21, 2013
    Publication date: February 27, 2014
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20140045825
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: September 14, 2011
    Publication date: February 13, 2014
    Applicant: Exelixis, Inc.
    Inventor: James William Leahy