Nitrogen Bonded Directly To The 1,3-diazine At 2-position By A Single Bond Patents (Class 514/275)
  • Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use
    Patent number: 9708309
    Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: July 18, 2017
    Assignee: ORYZON GENOMICS, S.A.
    Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez De La Cuesta, Maria de los Ángeles Estiarte-Martinez
  • Compositions for administration of zoledronic acid or related compounds for treating low back pain
    Patent number: 9707247
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, such as zoledronic acid in an acid or a salt form, or in a molecular complex can be used to treat or alleviate pain or related conditions.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: July 18, 2017
    Assignee: Antecip Bioventures II LLC
    Inventor: Herriot Tabuteau
  • Protein kinase C inhibitors and uses thereof
    Patent number: 9682976
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: June 20, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Matthew Duncton, Jing Zhang, Salvador Alvarez, Kin Tso, Sacha Holland, Rose Yen, Rao Kolluri, Thilo Heckrodt, Yan Chen, Esteban Masuda, Hui Li, Donald G. Payan, Ryan Kelley
  • Pharmaceutical gastro-retentive solid oral dosage form of nilotinib
    Patent number: 9682081
    Abstract: The present invention relates to a pharmaceutical gastro-retentive solid oral dosage form comprising nilotinib as the active ingredient. The invention is further related to methods of preparing said dosage form.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: June 20, 2017
    Assignee: Sun Pharmaceutical Industries Limited
    Inventors: Anuj Kumar Fanda, Ravish Sharma, Kumaravel Vivek, Lalit Kumar Khurana, Shavej Ahmad, Romi Barat Singh, Ajay Kumar Singla
  • Ethynyl derivatives
    Patent number: 9682959
    Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: June 20, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome
    Patent number: 9675626
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as complex regional pain syndrome.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: June 13, 2017
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Pyridyl-and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
    Patent number: 9670191
    Abstract: The present invention provides compounds of the formula (I), or the pharmaceutically acceptable salts thereof, wherein G, W, R2, R3, R4, R5 and R6 are as defined in the specification. Further objects of the invention are processes and intermediates for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: June 6, 2017
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Ermes Vanotti, Marina Caldarelli, Alessandra Cirla, Barbara Forte, Antonella Ermoli, Maria Menichincheri, Antonio Pillan, Alessandra Scolaro
  • Biomarkers to identify patients that will respond to treatment and treating such patients
    Patent number: 9663825
    Abstract: The invention relates to methods for using biomarkers to identify cancer patients that will or are likely to respond to treatment. Specifically, the invention relates to the use of one or more of three association studies of cancer types, gene mutations, or gene expression levels in order to identify cancer patients that will or are likely to respond to treatment with a histone deacetylase (HDAC) inhibitor, alone or in combination with another cancer treatment. The methods may, optionally, further include treating such patient with an HDAC inhibitor, alone or in combination with another cancer treatment.
    Type: Grant
    Filed: April 19, 2013
    Date of Patent: May 30, 2017
    Assignee: ACETYLON PHARMACEUTICALS, INC.
    Inventors: Min Yang, Simon S. Jones
  • Phosphoinositide 3-kinase inhibitors
    Patent number: 9663487
    Abstract: A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R and R6 are each independently (LQ)mY; R4 is H, halogen, optionally substituted aryl or optionally substituted alkyl; and; each X is independently CR7 or N. The compounds are PI3K inhibitors and therefore have potential utility in therapy.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 30, 2017
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva
  • Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome
    Patent number: 9662343
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as complex regional pain syndrome.
    Type: Grant
    Filed: November 11, 2016
    Date of Patent: May 30, 2017
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventor: Herriot Tabuteau
  • Substituted carboxylic acid derivatives as aggrecanase inhibitors for the treatment of osteoarthritis
    Patent number: 9656949
    Abstract: The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which ADAMTS5 is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, hepatocirrhosis, traumatic cartilage injuries, pain, allodynia or hyperalgesia.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: May 23, 2017
    Assignee: MERCK PATENT GMBH
    Inventors: Markus Klein, Sven Lindemann
  • Dihydropyrazole GPR40 modulators
    Patent number: 9656963
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: May 23, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Andres S. Hernandez, Bruce A. Ellsworth, William R. Ewing, Bin Chen
  • Pyrimidines as sodium channel blockers
    Patent number: 9656968
    Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: September 23, 2015
    Date of Patent: May 23, 2017
    Inventors: Chiyou Ni, Laykea Tafesse, Jiangcho Yao, Mark Youngman, Minnie Park, Bin Shao
  • Substituted indolyl alkyl amino derivatives as novel inhibitors of histone deacetylase
    Patent number: 9636341
    Abstract: This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, X and Y have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: August 20, 2015
    Date of Patent: May 2, 2017
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Marc Gustaaf Celine Verdonck, Patrick Rene Angibaud, Bruno Roux, Isabelle Noelle Constance Pilatte, Peter Ten Holte, Janine Arts, Kristof Van Emelen
  • Osteoclast inhibitors for bone marrow lesions
    Patent number: 9623038
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: April 18, 2017
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventors: Herriot Tabuteau, Graeme Jones
  • Fused bicyclic 2,4-diaminopyrimidine derivative as a dual ALK and FAK inhibitor
    Patent number: 9623026
    Abstract: The present invention provides a compound of formula (I) or a salt form thereof. The compound of formula (I) has ALK and FAK inhibitory activity, and may be used to treat proliferative disorders.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: April 18, 2017
    Assignee: Cephalon, Inc.
    Inventors: Shawn P. Allwein, Laurent Courvoisier, Martin J. Jacobs, Gregory R. Ott
  • Osteoclast inhibitors such as zoledronic acid for low back pain treatment
    Patent number: 9623036
    Abstract: Methods for the safe administration of imidazole or imidazolium compounds, and conditions that may be treated by these methods, are described herein.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: April 18, 2017
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventors: Herriot Tabuteau, Jaro I. Karppinen
  • Osteoclast inhibitors for joint conditions
    Patent number: 9610300
    Abstract: Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions.
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: April 4, 2017
    Assignee: ANTECIP BIOVENTURES II LLC
    Inventors: Herriot Tabuteau, Graeme Jones
  • Spiro azetidine isoxazole derivatives and their use as SSTR antagonists
    Patent number: 9605000
    Abstract: Provided is a compound represented by the following formula (1) or a salt thereof, which has an SSTR5 antagonistic action: wherein each symbol has the same definition as in the specification.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: March 28, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Masaki Ogino, Ryo Mizojiri, Takeshi Yamasaki, Hideki Hirose, Nobuyuki Takakura, Tohru Yamashita, Sachie Morimoto, Takashi Nakahata, Asato Kina
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: 9593082
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
    Type: Grant
    Filed: February 12, 2008
    Date of Patent: March 14, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ankush Argade, Arvinder Sran, David Carroll, Jeffrey Clough, Kin Tso, Somasekhar Bhamidipati, Sambaiah Thota, Rajinder Singh, Vanessa Taylor, Hui Li, Esteban Masuda
  • 2,4-pyrimidinediamine compounds and their uses
    Patent number: 9586908
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: March 7, 2017
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
  • Integrin antagonist conjugates for targeted delivery to cells expressing alpha-V-beta-3
    Patent number: 9586916
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula (I) for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to alpha-V-beta-3 integrin antagonists to target cells expressing alpha-V-beta-3.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: March 7, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Robert Alan Goodnow, Jr., Matthew Michael Hamilton, Agnieszka Kowalczyk, Achyutharao Sidduri
  • Polymorphic forms of nilotinib hydrochloride
    Patent number: 9580408
    Abstract: Crystalline Forms R5, R5a, R5b and R6 of nilotinib hydrochloride and processes for their preparation.
    Type: Grant
    Filed: April 23, 2014
    Date of Patent: February 28, 2017
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Vishweshwar Peddy, Ramanaiah Chennuru, Srividya Ramakrishnan
  • Kinase modulation and indications therefor
    Patent number: 9550768
    Abstract: Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: January 24, 2017
    Assignee: Plexxikon Inc.
    Inventors: Chao Zhang, Gideon Bollag, Gaston Habets, Jiazhong Zhang, Prabha N. Ibrahim, Guoxian Wu
  • Substituted pyrimidine-5-carboxamides as spleen tyrosine kinase inhibitors
    Patent number: 9533989
    Abstract: The present invention relates to compounds of formula (Ia), (Ib) or (Ic): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma, COPD, allergic rhinitis, chronic sinusitis, atopic dermatitis, psoriasis, rosacea, alopecia, allergic conjunctivitis and dry eye disease.
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: January 3, 2017
    Assignee: Ziarco Pharma Ltd.
    Inventors: Gavin A. Whitlock, Paul Alan Glossop
  • Combination therapy for MDS
    Patent number: 9504706
    Abstract: Disclosed are compositions and methods for the treatment of disorders such as myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML). The disclosed methods include administering to an individual in need of such treatment a composition that may include an IRAK1/4 inhibitor. In other aspects, the method may include administration of a BLC2 inhibitor.
    Type: Grant
    Filed: September 1, 2015
    Date of Patent: November 29, 2016
    Assignee: Children's Hospital Medical Center
    Inventors: Daniel Starczynowski, Garrett W. Rhyasen
  • Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
    Patent number: 9492471
    Abstract: The present invention provides methods of treating, stabilizing or lessening the severity or progression of a disease or disorder associated with BTK.
    Type: Grant
    Filed: November 19, 2013
    Date of Patent: November 15, 2016
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Tom Daniel, Kenichi Takeshita, Kenneth Foon, Jay Mei
  • Compounds modulating c-fms and/or c-kit activity and uses therefor
    Patent number: 9487515
    Abstract: Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use thereof.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: November 8, 2016
    Assignee: Plexxikon Inc.
    Inventors: Jiazhong Zhang, Prabha N. Ibrahim, Ryan Bremer
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: 9481654
    Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: November 1, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Ankush Argade, Kin Tso, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Somasekhar Bhamidipati, Vanessa Taylor, Esteban Masuda
  • Stable and soluble formulations of receptor tyrosine kinase inhibitors, and methods of preparation thereof
    Patent number: 9474756
    Abstract: The present disclosure relates to stable formulations of receptor tyrosine kinase inhibitors (TKI), e.g., pazopanib; methods of preparation thereof; and use of the disclosed formulations in sustained delivery of the active agent to a target site. The disclosure further relates to methods of converting one polymorphic Form of a TKI to another polymorphic Form and/or an amorphous form.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: October 25, 2016
    Assignee: ForSight Vision4, Inc.
    Inventors: Judit Horvath, Irina Astafieva, Signe Erickson, Kathleen Cogan Farinas
  • Crystal form of dabrafenib and preparation method and use thereof
    Patent number: 9458149
    Abstract: The invention relates to Crystal Form VII of dabrafenib and preparation method thereof, wherein Crystal Form VII has the advantage of being more stable at room temperature or in aqueous systems, and has low hygroscopicity, and thus is more suitable for a wet granulation process or being prepared into a suspension; and the present invention also relates to a pharmaceutical composition and formulations comprising Crystal Form VII, and their use in the treatment of Raf family kinase-related diseases.
    Type: Grant
    Filed: March 25, 2016
    Date of Patent: October 4, 2016
    Assignee: HANGZHOU PUSHAI PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Haiping Lao, Xiaoxia Sheng, Xiaohong Sheng
  • 2,4-pyrimidinediamine compounds and their uses
    Patent number: 9416112
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: September 12, 2014
    Date of Patent: August 16, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Methods and compositions for modulating Ire1, SRC and ABL activity
    Patent number: 9382230
    Abstract: Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: July 5, 2016
    Assignee: The Regents of the University of California
    Inventors: Peter Walter, Alexei Korennykh, Kevan M. Shokat, Chao Zhang, Janet Finer-Moore, Robert Stroud, Pascal Egea, Andrei Korostelev, Arvin Dar, Sebastian Bernales
  • Small molecules that promote skin regeneration
    Patent number: 9375439
    Abstract: Provided herein are small molecules for the induction of fibroblast proliferation and increased secretion or production of proteins. The small molecules described herein can be used for the promotion of skin regeneration. Also provided herein are methods for promoting skin regeneration and wound healing.
    Type: Grant
    Filed: January 8, 2014
    Date of Patent: June 28, 2016
    Assignee: International Stem Cell Corporation
    Inventors: Rodolfo Gonzalez, Maxim Poustovoitov, Ruslan Semechkin
  • Solid forms of 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
    Patent number: 9365524
    Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to 2-(tert-butylamino)-4-((1R,3R,4R)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: June 14, 2016
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Hon-Wah Man, Jean Xu, Marie Georges Beauchamps, Mohit Atul Kothare, Nanfei Zou, Ying Li, Lianfeng Huang, Daozhong Zou
  • Benzoimidazol-2-yl pyrimidines and pyrazines as modulators of the histamine H4 receptor
    Patent number: 9365548
    Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.
    Type: Grant
    Filed: January 28, 2015
    Date of Patent: June 14, 2016
    Assignee: Janssen Pharmaceutica NV
    Inventors: James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
  • Crystal form of Dabrafenib and preparation method of use thereof
    Patent number: 9365559
    Abstract: The invention relates to Crystal Hydrate Form VI of Dabrafenib and preparation method thereof, wherein Crystal Hydrate Form VI of Dabrafenib has the advantage of being more stable at room temperature or in aqueous systems, and has low hygroscopicity, and thus is more suitable for a wet granulation process or being prepared into a suspension; and the present invention also relates to a pharmaceutical composition and formulations comprising Crystal Hydrate Form VI of Dabrafenib, and their use in the treatment of Raf family kinase-related diseases.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: June 14, 2016
    Assignee: HANGZHOU PUSHAI PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Haiping Lao, Xiaoxia Sheng, Xiaohong Sheng
  • Process for preparing pan-CDK inhibitors of the formula (I), and intermediates in the preparation
    Patent number: 9359306
    Abstract: The invention relates to a novel process for the preparation of pan-CDK inhibitors of the formula (I), and intermediates of the preparation.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: June 7, 2016
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Joachim Krüger, Jörg Gries, Kai Lovis, Jorma Haβfeld
  • Kinase modulation, and indications therefor
    Patent number: 9358235
    Abstract: The present disclosure provides methods of using protein kinase inhibitors for treating diseases and conditions, including diseases and conditions associated with activity of any protein kinase selected from Fms protein kinase including any mutations thereof, Kit protein kinase any mutations thereof, Flt-3 protein kinase any mutations thereof and combinations thereof.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 7, 2016
    Assignee: Plexxikon Inc.
    Inventors: Gideon Bollag, Klaus-Peter Hirth, Prabha N. Ibrahim, Paul Lin, Brian West
  • Amino, amido and heterocyclic compounds as modulators of rage activity and uses thereof
    Patent number: 9353078
    Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.
    Type: Grant
    Filed: October 1, 2014
    Date of Patent: May 31, 2016
    Assignees: New York University, The Research Foundation for The State University of New York
    Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
  • Inhibitors of Bruton's tyrosine kinase
    Patent number: 9353087
    Abstract: The present invention provides a compound, solid forms, and compositions thereof, which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same. The present invention also provides methods of making provided compound and solid forms.
    Type: Grant
    Filed: June 7, 2013
    Date of Patent: May 31, 2016
    Assignees: Biogen MA Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Brian T. Hopkins, Xiongwei Cai, Timothy R. Chan, Patrick Conlon, Michael Humora, Tracy J. Jenkins, Michael J. Macphee, Xianglin Shi, Ross A. Miller, Andrew Thompson
  • 2,4-pyrimidinediamine compounds and their uses
    Patent number: 9346765
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Grant
    Filed: March 30, 2015
    Date of Patent: May 24, 2016
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Stem cell cultures
    Patent number: 9340525
    Abstract: The present invention relates compounds for stabilizing cells and methods of their use.
    Type: Grant
    Filed: February 24, 2014
    Date of Patent: May 17, 2016
    Assignee: The Scripps Research Institute
    Inventors: Yue Xu, Sheng Ding
  • Inhibition of biofilm organisms
    Patent number: 9339525
    Abstract: The present invention relates to a product comprising at least two antibiofilm agents wherein at least one of the antibiofilm agents is an antimicrobial peptide. The second antibiofilm agent is cysteamine. There is also provided the use of the product in the treatment of a microbial infection.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: May 17, 2016
    Assignee: Novabiotics Limited
    Inventors: Deborah O'Neil, Derry Mercer, Cedric Charrier
  • Fused bicyclic 2,4-diaminopyrimidine derivative as a dual ALK and FAK inhibitor
    Patent number: 9339502
    Abstract: The present invention provides a compound of formula (I) or a salt form thereof. The compound of formula (I) has ALK and FAK inhibitory activity, and may be used to treat proliferative disorders.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: May 17, 2016
    Assignee: Cephalon, Inc.
    Inventors: Shawn P. Allwein, Laurent Courvoisier, Martin J. Jacobs, Gregory R. Ott
  • Acid addition salt of substituted pyridine compound
    Patent number: 9321747
    Abstract: The present invention provides a salt of a substituted pyridine compound which has excellent CETP inhibition activity and is useful as a medicament. The present invention provides a salt of a compound represented by general formula (I): wherein R1 is optionally substituted alkoxy or the like.
    Type: Grant
    Filed: January 4, 2013
    Date of Patent: April 26, 2016
    Assignees: DAIICHI SANKYO COMPANY, LIMITED, UBE INDUSTRIES, LTD.
    Inventors: Yukinori Kawai, Noriaki Iwase, Osamu Kikuchi, Katsunori Takata, Takahiro Motoyama, Masahiko Hagihara
  • Crystalline pharmaceutically active ingredients
    Patent number: 9321733
    Abstract: The present invention is related to crystalline forms of rosuvastatin zinc (2:1) salt. The polymorphs are suitable for use as pharmaceutically active ingredients in the treatment of the diseases of the lipid metabolism including hypercholesterolemia, hyperlipidemia, dyslipidemia or atherosclerosis.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: April 26, 2016
    Assignee: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Imre Markovits, Ferenc Jurak, Gyorgyi Kovanyine Lax, Csaba Hamori, Balazs Havasi, Eva Sipos, Balazs Volk, Zsolt Runge, Krisztina Fodorne Kocsmar, Gyula Lukacs, Katalin Kataine Fadgyas, Monika Mezovari
  • Crystalline forms of 5-chloro-N2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2, 4-diamine
    Patent number: 9309229
    Abstract: The present invention describes specific crystalline forms of 5-chloro-N-(2-isopropoxy-5-methyl-4-(piperidin-4-ylphenyl)-N-2-(isopropylsulfonyl)phenyl)-2,4-diamine. The present invention further relates to methods for preparing said crystalline forms, pharmaceutical compositions comprising said crystalline forms, and methods of using said crystalline forms and pharmaceutical compositions to treat disease.
    Type: Grant
    Filed: December 15, 2011
    Date of Patent: April 12, 2016
    Assignee: Novartis AG
    Inventors: Lili Feng, Baoqing Gong, Piotr H. Karpinski, Liladhar Murlidhar Waykole
  • Benzyl sulfonamide derivatives as RORc modulators
    Patent number: 9302985
    Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Grant
    Filed: December 10, 2013
    Date of Patent: April 5, 2016
    Assignee: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
    Patent number: 9296703
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: October 4, 2013
    Date of Patent: March 29, 2016
    Assignee: University of Utah Research Foundation
    Inventors: Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, David J. Bearss, Sunil Sharma