The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
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Publication number: 20150094299Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.Type: ApplicationFiled: December 9, 2014Publication date: April 2, 2015Inventors: Shingo YAMAMOTO, Toshio YOSHIZAWA
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Publication number: 20150087660Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of chronic diseases and inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.Type: ApplicationFiled: February 27, 2013Publication date: March 26, 2015Inventor: Mahesh KANDULA
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Publication number: 20150087643Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.Type: ApplicationFiled: October 10, 2014Publication date: March 26, 2015Applicant: Advinus Therapeutics Private LimitedInventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
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Patent number: 8980871Abstract: Provided herein are methods of treating hemolysis by administering an active compound in an amount sufficient to treat said hemolysis. It has been found that nitroxyl donors or similar compounds preferentially react with cell-free OxyHb, as compared to OxyHb encapsulated in a red blood cell, and reacts with MetHb to form iron-nitrosyl Hb or nitrite bound MetHb. It has also been found that such compounds reduce cell-free Hb and hemolysis. Active compounds are also contemplated for use in combination therapies, for example, in combination with the administration of red blood cells and/or an agent that promotes hematopoiesis, or in combination with the administration of a nitric oxide donor.Type: GrantFiled: September 19, 2008Date of Patent: March 17, 2015Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
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Publication number: 20150057295Abstract: This invention relates to 6-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich REISER, James MADDEN
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Publication number: 20150057286Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Ulrich REISER
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Patent number: 8957081Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: September 11, 2012Date of Patent: February 17, 2015Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20150045361Abstract: Substituted bicyclic heteroaryls 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-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: October 22, 2014Publication date: February 12, 2015Inventors: Yi CHEN, Timothy D. CUSHING, Jason A. DUQUETTE, Felix GONZALEZ LOPEZ DE TURISO, Xiaolin HAO, Xiao HE, Brian S. LUCAS, Lawrence R. MCGEE, Andreas REICHELT, Robert M. RZASA, Jennifer L. SEGANISH, Youngsook SHIN, Dawei ZHANG
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions 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 PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150031689Abstract: The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation.Type: ApplicationFiled: February 15, 2013Publication date: January 29, 2015Inventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
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Publication number: 20150025089Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
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Publication number: 20150025090Abstract: The present application relates to novel substituted azabicycles, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: March 5, 2013Publication date: January 22, 2015Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
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Publication number: 20150018321Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: September 25, 2014Publication date: January 15, 2015Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
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Publication number: 20150011569Abstract: The invention includes compositions that regulated PI3K p110 delta and are useful as an anti-viral therapy. The invention includes a method of inhibiting p110 delta, a component of PI3K p110 delta signaling pathway, or any combination thereof in a cell as an anti-viral therapeutic approach for treating a viral infection, for example influenza. The invention includes a method of modulating PI3K p110 delta in a cell infected with a virus by contacting the cell with an effective amount of a composition comprising an inhibitor of PI3K p110 delta.Type: ApplicationFiled: December 14, 2012Publication date: January 8, 2015Inventors: Peter D. Katsikis, William A. Kinney, Harold R. Almond, Noshena Khan
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Publication number: 20150011545Abstract: 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: ApplicationFiled: July 15, 2014Publication date: January 8, 2015Applicant: AstraZeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20140377258Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating cancers or hematologic disorders.Type: ApplicationFiled: May 30, 2014Publication date: December 25, 2014Applicant: Infinity Pharmaceuticals, Inc.Inventors: Howard M. Stern, Jeffery L. Kutok
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Publication number: 20140378446Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: January 30, 2013Publication date: December 25, 2014Applicant: Pharmacyclics, Inc.Inventors: Wei Chen, David J. Loury, Yan Shunqi, Longcheng Wang, Leah Lynn Frye
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Patent number: 8907086Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: March 1, 2012Date of Patent: December 9, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
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Patent number: 8901135Abstract: 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-proType: GrantFiled: May 10, 2012Date of Patent: December 2, 2014Assignee: 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
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Patent number: 8901136Abstract: 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: GrantFiled: June 6, 2013Date of Patent: December 2, 2014Assignee: 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
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Patent number: 8895570Abstract: 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: GrantFiled: December 14, 2011Date of Patent: November 25, 2014Assignee: AstraZeneca ABInventors: Phillip Abbott, Roger Victor Bonnert, Thomas McInally, Stephen Thom, Hiroki Wada, Satoshi Onuma
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Patent number: 8895036Abstract: 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: GrantFiled: March 3, 2014Date of Patent: November 25, 2014Assignee: JCDS Holdings, LLCInventor: Jay Richard Ray, II
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Publication number: 20140343057Abstract: 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: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Inventors: Vito J. PALOMBELLA, David G. WINKLER
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Publication number: 20140343033Abstract: 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: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Applicant: Takeda Califomia, Inc.Inventors: Edcon Chang, Michael B. Wallace
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Publication number: 20140341894Abstract: 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: ApplicationFiled: June 5, 2014Publication date: November 20, 2014Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Liansheng LI, Katrina CHAN, Christian ROMMEL
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Publication number: 20140336175Abstract: 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: ApplicationFiled: May 16, 2014Publication date: November 13, 2014Applicant: GlaxoSmithKline LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
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Publication number: 20140323439Abstract: 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: ApplicationFiled: July 3, 2014Publication date: October 30, 2014Inventors: W. Michael GALLATIN, Roger G. ULRICH, Neill A. GIESE
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Publication number: 20140323441Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: ApplicationFiled: November 8, 2012Publication date: October 30, 2014Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
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Publication number: 20140309212Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: 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
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Publication number: 20140303151Abstract: 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: ApplicationFiled: September 14, 2011Publication date: October 9, 2014Applicant: Exelixis, Inc.Inventor: James William Leahy
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Publication number: 20140303177Abstract: 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 theType: ApplicationFiled: June 20, 2014Publication date: October 9, 2014Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: 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
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Patent number: 8853156Abstract: 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: GrantFiled: August 5, 2009Date of Patent: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
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Publication number: 20140296261Abstract: 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: ApplicationFiled: November 14, 2012Publication date: October 2, 2014Applicants: 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
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Publication number: 20140296207Abstract: 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: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
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Patent number: 8846696Abstract: 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: GrantFiled: June 23, 2009Date of Patent: September 30, 2014Assignees: Cyclacel Limited, Cancer Research Technology LimitedInventors: Peter Martin Fischer, Michael Jarman, Edward McDonald, Bernard Nutley, Florence Raynaud, Stuart Wilson, Paul Workman
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Publication number: 20140288099Abstract: 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: ApplicationFiled: July 19, 2012Publication date: September 25, 2014Applicant: GLAXOSMITHKLINE LLCInventors: Claire Louise Ambery, Christopher David Edwards
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Publication number: 20140275127Abstract: 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: ApplicationFiled: May 29, 2014Publication date: September 18, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
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Patent number: 8835420Abstract: 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: GrantFiled: July 8, 2013Date of Patent: September 16, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
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Patent number: 8828998Abstract: 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: GrantFiled: March 15, 2013Date of Patent: September 9, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Vito J. Palombella, David G. Winkler
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Patent number: 8809349Abstract: 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: GrantFiled: January 10, 2012Date of Patent: August 19, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
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Patent number: 8809336Abstract: 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 theType: GrantFiled: September 4, 2013Date of Patent: August 19, 2014Assignees: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: 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
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Publication number: 20140227351Abstract: 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: ApplicationFiled: April 16, 2014Publication date: August 14, 2014Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Martin FOLGER, Stefan LEHNER, Annette GRAVE, Norbet POELLINGER, Randolph SEIDLER
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Publication number: 20140228287Abstract: 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: ApplicationFiled: April 16, 2014Publication date: August 14, 2014Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Frerich DE VRIES, Dirk HOERSTERMANN, Ingo LANG, Michael MARK, Randolph SEIDLER, Leo THOMAS
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Patent number: 8802684Abstract: 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: GrantFiled: September 20, 2013Date of Patent: August 12, 2014Assignee: GlaxoSmithKline LLCInventors: Helene Bazin-Lee, Diane Mary Coe, Charlotte Jane Mitchell, Stephen Allan Smith
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Publication number: 20140221400Abstract: 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: ApplicationFiled: November 8, 2013Publication date: August 7, 2014Applicant: ASTRAZENECA ABInventors: Hakan Eriksson, Werner Poewe
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Publication number: 20140221366Abstract: 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: ApplicationFiled: June 11, 2012Publication date: August 7, 2014Applicant: MERCK PATENT GMBHInventors: Timo Heinrich, Nadia Brugger, Kristopher Josephson
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Publication number: 20140206685Abstract: 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: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: INTELLIKINE LLCInventors: Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN, Troy Edward WILSON
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Publication number: 20140206684Abstract: 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: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: INTELLIKINE LLCInventors: Pingda REN, Yi LIU, Troy Edward WILSON, Katrina CHAN, Christian ROMMEL, Liansheng LI
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Patent number: 8785456Abstract: 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: GrantFiled: February 23, 2012Date of Patent: July 22, 2014Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Patent number: 8765772Abstract: 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: GrantFiled: August 7, 2009Date of Patent: July 1, 2014Assignee: GlaxoSmithKline LLCInventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi