The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
  • Patent number: 10328731
    Abstract: A printer for printing objects for marking electrical components, having a housing, a printing space formed inside of the housing, a printing device, a receiving device for a replaceable magazine for receiving the object to be printed, a control and evaluation unit, and an input and display device, wherein the receiving device can move between a loading and unloading position outside of the printing space and a printing position inside of the printing space. The printer has lower and upper housing parts, wherein the printing space, the printing device, the receiving device, and the control and evaluation unit are arranged in the lower housing part. A tablet computer is pivotably attached on the top side of the upper housing part, whereby the tablet computer can be locked in an upwardly pivoted position, and the upper housing part is mounted to pivot about a rotational axis on the lower housing part.
    Type: Grant
    Filed: January 19, 2017
    Date of Patent: June 25, 2019
    Assignee: PHOENIX CONTACT GMBH & CO. KG
    Inventors: Sandra Klocke, Peter Isaak, Albrecht Schierholz
  • Patent number: 10208050
    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: Grant
    Filed: August 4, 2017
    Date of Patent: February 19, 2019
    Assignee: ChemoCentryx, Inc.
    Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
  • Patent number: 10196395
    Abstract: The present disclosure relates to crystalline Form ? of a compound of formula (I) used for preparing a blood-cancer drug and preparation method thereof. The crystalline Form ? in the present disclosure has better stability, and its solubility and hygroscopicity meet the requirements of medical use. Form ? has simple preparation method and low manufacturing cost, and provides great value to future optimization and development of this drug.
    Type: Grant
    Filed: February 1, 2016
    Date of Patent: February 5, 2019
    Assignee: Crystal Pharmatech Co., Ltd
    Inventors: Minhua Chen, Yanfeng Zhang, Xiaojuan Diao, Nan Xia, Xiaoyu Zhang
  • Patent number: 10149849
    Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
    Type: Grant
    Filed: July 5, 2017
    Date of Patent: December 11, 2018
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Matthew Alexander, Joshua Hansen, Dehua Huang, Robert Hubbard, Raj K. Raheja, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, JingJing Zhao
  • Patent number: 10010507
    Abstract: Described herein are pharmaceutical formulations of Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one. Also disclosed are methods of using the Btk inhibitor, 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: Grant
    Filed: March 1, 2018
    Date of Patent: July 3, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Ching W. Chong, Robert Kuehl, Heow Tan, Harisha Atluri
  • Patent number: 9877968
    Abstract: 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: April 21, 2016
    Date of Patent: January 30, 2018
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 9840505
    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 PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: February 4, 2016
    Date of Patent: December 12, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Patent number: 9738644
    Abstract: Substituted isoquinolinone 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: Grant
    Filed: September 29, 2015
    Date of Patent: August 22, 2017
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
  • Patent number: 9737541
    Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: August 22, 2017
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
  • Patent number: 9512124
    Abstract: Provided herein are Aminopurine Compounds having the following structures: wherein R1, R2, and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: December 6, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Matthew Alexander, Sogole Bahmanyar, Joshua Hansen, Dehua Huang, Robert Hubbard, Brandon Jeffy, Jim Leisten, Mehran Moghaddam, Raj K. Raheja, Heather Raymon, Kimberly Schwarz, Marianne Sloss, Eduardo Torres, Tam Minh Tran, Shuichan Xu, JingJing Zhao, John Frederick Boylan
  • Patent number: 9486526
    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: June 3, 2014
    Date of Patent: November 8, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Patent number: 9388140
    Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: July 12, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
  • Patent number: 9346806
    Abstract: 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: October 13, 2011
    Date of Patent: May 24, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 9290497
    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: July 9, 2014
    Date of Patent: March 22, 2016
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Patent number: 9266893
    Abstract: Disclosed herein is a solid oral dosage form comprising at least one coating chosen from enteric coatings and delayed release coatings, at least one pharmaceutically acceptable excipient, and a compound, or a pharmaceutically acceptable salt thereof, having the structure:
    Type: Grant
    Filed: January 10, 2014
    Date of Patent: February 23, 2016
    Assignee: Pharmacyclics LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9216982
    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: June 5, 2014
    Date of Patent: December 22, 2015
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Patent number: 9212381
    Abstract: Synthesis of many proteins is tightly controlled at the level of translation and plays an essential role in fundamental processes such as cell growth and proliferation, signaling, differentiation or death. Methods that allow imaging and identification of nascent proteins allow for dissecting regulation of translation, both spatially and temporally, including in whole organisms. Described herein are robust chemical methods for imaging and affinity-purifying nascent polypeptides in cells and in animals, based on puromycin analogs. Puromycin analogs of the present invention form covalent conjugates with nascent polypeptide chains, which are rapidly turned over by the proteasome and can be visualized and specifically captured by a bioorthogonal reaction (e.g., [3+2] cycloaddition). The methods of the present invention have broad applicability for imaging protein synthesis and for identifying proteins synthesized under various physiological and pathological conditions in vivo.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: December 15, 2015
    Assignee: President and Fellows of Harvard College
    Inventors: Adrian Salic, Jing Liu
  • Patent number: 9212185
    Abstract: Disclosed herein are compounds of Formula (D) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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: Grant
    Filed: November 14, 2013
    Date of Patent: December 15, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9193735
    Abstract: Disclosed herein is a solid oral formulation comprising a therapeutically effective amount of a compound of Formula (A) formulated for release of the compound in the intestine, wherein the compound of Formula (A) has the structure:
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: November 24, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9181257
    Abstract: Disclosed herein are pyrazolo[3,4-d]pyrimidines that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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: Grant
    Filed: November 14, 2013
    Date of Patent: November 10, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9163026
    Abstract: Disclosed herein are compounds of Formula (D) that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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: Grant
    Filed: November 14, 2013
    Date of Patent: October 20, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9156847
    Abstract: Disclosed is a process for the preparation of the following compounds: where R1, R1a and R2a have the definitions in the description, as well as a process to prepare other intermediates that may be useful to synthesize downstream products, especially compounds that are useful as medicaments, for instance Bruton's tyrosine kinase (Btk) inhibitors such as ibrutinib. Also disclosed are other processes, other intermediates and compounds per se.
    Type: Grant
    Filed: March 11, 2014
    Date of Patent: October 13, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Philip Pye, Cyril Ben Haim, Matteo Conza, Ioannis Nicolaos Houpis
  • Patent number: 9156846
    Abstract: Disclosed herein is a solid oral formulation comprising a therapeutically effective amount of a compound of Formula (A) formulated for release of the compound in the intestine, wherein the compound of Formula (A) has the structure:
    Type: Grant
    Filed: January 15, 2014
    Date of Patent: October 13, 2015
    Assignee: PHARMACYCLICS LLC
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Patent number: 9073879
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: July 7, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
  • Publication number: 20150148354
    Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.
    Type: Application
    Filed: October 27, 2014
    Publication date: May 28, 2015
    Inventors: Benjamin Mark SKEAD, Christopher Peter WORRALL, Jonathan Charles Christian ATHERTON, Julian Scott NORTHEN, Philippe FERNANDES
  • Publication number: 20150141402
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Q, G, ring A, ring B, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, and m are defined herein. The novel purine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
    Type: Application
    Filed: November 20, 2014
    Publication date: May 21, 2015
    Applicant: PFIZER INC.
    Inventors: Douglas Carl Behenna, Hengmiao Cheng, Sujin Cho-Schultz, Theodore Otto Johnson, JR., John Charles Kath, Asako Nagata, Sajiv Krishnan Nair, Simon Paul Planken
  • Publication number: 20150141407
    Abstract: The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.
    Type: Application
    Filed: May 30, 2013
    Publication date: May 21, 2015
    Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Xiaofeng Wang, Kuo-Hsiung Lee
  • Publication number: 20150126488
    Abstract: [Problem] On the basis of a cathepsin S inhibitory effect, an excellent agent for treating or preventing autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like is provided. [Means for Solution] It was found that a nitrogen-containing bicyclic heterocyclic compound has the excellent cathepsin S inhibitory effect, thereby completing the invention. The compound of the present invention has the cathepsin S inhibitory effect, and can be used as an agent for preventing and/or treating autoimmune disease, allergic disease, graft rejection of an organ, bone marrow or tissue, systemic lupus erythematosus, or the like.
    Type: Application
    Filed: April 17, 2013
    Publication date: May 7, 2015
    Applicant: ASTELLAS PHARMA INC
    Inventors: Yutaka Nakajima, Sunao Imada, Yuji Takasuna, Naohiro Aoyama, Takahiro Nigawara, Shohei Shirakami, Fumiyuki Shirai, Junji Sato, Keita Nakanishi, Kaori Kubo
  • Publication number: 20150126506
    Abstract: 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: Application
    Filed: January 8, 2015
    Publication date: May 7, 2015
    Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
  • Publication number: 20150126509
    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: January 12, 2015
    Publication date: May 7, 2015
    Inventors: Randall L. Halcomb, Paul A. Roethle
  • Publication number: 20150105383
    Abstract: The invention relates to HDAC inhibitors, or combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of non-hodgkin's lymphoma in a subject in need thereof. Also provided herein are methods for treating non-hodgkin's lymphoma in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor, or a combination comprising an HDAC inhibitor and a PI3K inhibitor.
    Type: Application
    Filed: October 8, 2014
    Publication date: April 16, 2015
    Applicant: Acetylon Pharmaceuticals, Inc.
    Inventors: Steven Norman Quayle, Simon Stewart Jones
  • Publication number: 20150094299
    Abstract: 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: Application
    Filed: December 9, 2014
    Publication date: April 2, 2015
    Inventors: Shingo YAMAMOTO, Toshio YOSHIZAWA
  • Publication number: 20150087660
    Abstract: 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: Application
    Filed: February 27, 2013
    Publication date: March 26, 2015
    Inventor: Mahesh KANDULA
  • Publication number: 20150087643
    Abstract: 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: Application
    Filed: October 10, 2014
    Publication date: March 26, 2015
    Applicant: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8980871
    Abstract: 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: Grant
    Filed: September 19, 2008
    Date of Patent: March 17, 2015
    Assignees: Wake Forest University Health Sciences, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Daniel B. Kim-Shapiro, S. Bruce King, Daniel A. Sweeney, Mark T. Gladwin
  • Publication number: 20150057286
    Abstract: 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: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Ulrich REISER
  • Publication number: 20150057295
    Abstract: 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: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ulrich REISER, James MADDEN
  • Patent number: 8957081
    Abstract: 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: Grant
    Filed: September 11, 2012
    Date of Patent: February 17, 2015
    Assignee: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Publication number: 20150045361
    Abstract: 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 Lympho
    Type: Application
    Filed: October 22, 2014
    Publication date: February 12, 2015
    Inventors: 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
  • Publication number: 20150031672
    Abstract: 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: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150031689
    Abstract: 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: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Rangan Maitra, Alan Bradley Fulp, Yanan Zhang, Herbert H. Seltzman
  • Publication number: 20150025089
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Publication number: 20150025090
    Abstract: 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: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexandros Vakalopoulos, Dieter Lang, Frank Wunder, Walter Hübsch, Michael Hahn
  • Publication number: 20150018321
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 15, 2015
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
  • Publication number: 20150011545
    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: July 15, 2014
    Publication date: January 8, 2015
    Applicant: AstraZeneca AB
    Inventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
  • Publication number: 20150011569
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: January 8, 2015
    Inventors: Peter D. Katsikis, William A. Kinney, Harold R. Almond, Noshena Khan
  • Publication number: 20140377258
    Abstract: Provided herein are methods, kits, and pharmaceutical compositions that include a PI3 kinase inhibitor for treating cancers or hematologic disorders.
    Type: Application
    Filed: May 30, 2014
    Publication date: December 25, 2014
    Applicant: Infinity Pharmaceuticals, Inc.
    Inventors: Howard M. Stern, Jeffery L. Kutok
  • Publication number: 20140378446
    Abstract: 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: Application
    Filed: January 30, 2013
    Publication date: December 25, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury, Yan Shunqi, Longcheng Wang, Leah Lynn Frye
  • Patent number: 8907086
    Abstract: 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: Grant
    Filed: March 1, 2012
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
  • 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