The Other Cyclo In The Bicyclo Ring System Is Five-membered Patents (Class 544/262)
  • Patent number: 10668027
    Abstract: Described herein are methods of treating an Acanthamoeba infection in a subject in need thereof by administering an amount of allopurinol.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: June 2, 2020
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Andreas Seyfang, Timothy J. Locksmith, Adarsh Bellur, Deandre Wells, Matthew Doenges
  • Patent number: 10570142
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: August 22, 2018
    Date of Patent: February 25, 2020
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Swaroop K. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 10570116
    Abstract: Compounds of the formula I in which Z, W, Q, R and Y have the meanings indicated in claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: February 25, 2020
    Assignee: Merck Patent GmbH
    Inventors: Hans-Peter Buchstaller, Dieter Dorsch
  • Patent number: 10550124
    Abstract: The invention provides a series of conformationally stable kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: February 4, 2020
    Assignee: San Diego State University Foundation
    Inventors: Jeffrey L. Gustafson, Davis E. Smith, David Hecht, Isaac Marquez, Sean Toenjes
  • Patent number: 10435409
    Abstract: The present invention relates to a process for the preparation of 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one or Ibrutinib of Formula (I). The present invention further relates to a process for the preparation highly pure 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one or Ibrutinib(I).
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: October 8, 2019
    Assignee: SHILPA MEDICARE LIMITED
    Inventors: Sriram Rampalli, Lav Kumar Upalla, Chanti Babu Patneedi, Gopala Krishna Dasari, Akshay Kant Chaturvedi
  • Patent number: 10308612
    Abstract: A method for producing a 1-(acyloxy)alkyl carbamate derivative (III), using a fluorous alkyl carbonate derivative (I), and a fluorous alkyl carbonate derivative (I) and a method for producing the same. In the formula, R1 represents C1-C4 alkyl group or a C3-C6 cycloalkyl group, R2 represents a C1-C4 alkyl group or a hydrogen atom, and A represents a fluorous alkyl group (wherein the fluorous alkyl group represents a C2-C11 alkyl group in which 40% or more of the hydrogen atoms are replaced by fluorine atoms).
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: June 4, 2019
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsuyoshi Ueda, Yuzo Abe
  • Patent number: 10300064
    Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: May 28, 2019
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick
  • Patent number: 10072013
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: September 11, 2018
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 9975897
    Abstract: This invention relates to compounds of formula (I). The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.
    Type: Grant
    Filed: June 11, 2015
    Date of Patent: May 22, 2018
    Assignee: Loxo Oncology, Inc.
    Inventors: Mathew Calder, Nicolas E. S. Guisot
  • Patent number: 9944639
    Abstract: Disclosed are compounds of formula (I), their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, wherein R1-R4, and n are as defined in the specification, pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PI3K enzyme of a subject.
    Type: Grant
    Filed: July 1, 2015
    Date of Patent: April 17, 2018
    Assignee: Lupin Limited
    Inventors: Manojkumar Ramprasad Shukla, Nirmal Kumar Jana, Sachin Jaysing Mahangare, Prashant Popatrao Vidhate, Dipak Raychand Lagad, Anand Jagannath Tarage, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
  • Patent number: 9884869
    Abstract: Provided are ibrutinib polymorphs, e.g., crystalline ibrutinib Forms III, IV, V, VI, VII, VIII and Form IX and processes for producing these crystalline forms, stable amorphous ibrutinib and processes for preparing stable amorphous ibrutinib, pharmaceutical compositions comprising these forms and methods of using these crystalline and amorphous forms.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: February 6, 2018
    Assignee: PERRIGO API LTD.
    Inventors: Itai Adin, Sonia Krivonos, Yevgeny Rozenblat, Alex Weisman, Ana Fernadez Casares, Gloria Ten Figas, Revital Ben-Daniel
  • Patent number: 9828378
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
    Type: Grant
    Filed: July 7, 2015
    Date of Patent: November 28, 2017
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson
  • Patent number: 9795608
    Abstract: The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: October 24, 2017
    Assignee: PHARMASCIENCE, INC.
    Inventors: Alain Laurent, Yannick Rose
  • Patent number: 9744172
    Abstract: Compound of Formula I: are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.
    Type: Grant
    Filed: February 29, 2016
    Date of Patent: August 29, 2017
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Xiaodong Wang, Jing Liu, Chao Yang, Weihe Zhang, Stephen Frye, Dmitri Kireev
  • Patent number: 9745306
    Abstract: The present invention relates inter alia to a compound of formula (I) and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compounds.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 29, 2017
    Assignee: Respivert Limited
    Inventors: Rudy Laurent Maria Broeckx, Alex Herman Copmans, Alun John Smith, David Michel Adrien Taddei, Stuart Thomas Onions
  • Patent number: 9718825
    Abstract: The present invention relates to N-(4-(azaindazol-6-yl)-phenyl)-sulfonamides of the formula I, wherein Ar, n, X, Z, R1, R2 and R3 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds which modulate protein kinase activity, specifically the activity of serum and glucocorticoid regulated kinase (SGK), in particular of serum and glucocorticoid regulated kinase isoform 1 (SGK-1, SGK1), and are suitable for the treatment of diseases in which SGK activity is inappropriate, for example degenerative joint disorders or inflammatory processes such as osteoarthritis or rheumatism. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: August 1, 2017
    Assignee: SANOFI
    Inventors: Marc Nazare, Nis Halland, Friedemann Schmidt, Heinz-Werner Kleemann, Tilo Weiss, Joachim Saas, Carsten Struebing
  • Patent number: 9669033
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: June 6, 2017
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 9663439
    Abstract: The invention provides a 1-[3-(6,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d] pyridine-5-group)-4-ethoxy-benzenesulfonyl]-cis-3,5-dimethylpiperazine citrate or an Aildenafil citrate crystal form O and a preparation method thereof. And the invention also provides pharmaceutical compositions containing the Aildenafil citrate crystal form O and the use thereof in preparing drugs for treating Male Erectile Dysfunction (ED). The above crystal form O can be prepared through the steps of: dissolving a raw material, namely, the Aildenafil citrate in a mixture of distilled water and tetrahydrofuran, stirring, heating, filtering, stirring a filtrate, cooling, insulating heat, crystallizing, filtering and the like. The crystal form O can be adopted to prepare drugs with pharmaceutically acceptable excipients, so as to treat the male sexual dysfunction diseases.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: May 30, 2017
    Inventor: Guikun Liu
  • Patent number: 9655901
    Abstract: Described herein is allopurinol and pharmaceutical formulations thereof that can be administered to a subject infected with or suspected of being infected with an organism having an Nfa-1 protein and methods of using the allopurinol and pharmaceutical formulations thereof to treat infection with an organism having an Nfa-1 protein.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: May 23, 2017
    Assignee: University of South Florida
    Inventors: Andreas Seyfang, Adarsh Bellur, DeAndre Wells, Matthew Doenges
  • Patent number: 9580427
    Abstract: Provided herein are compounds such as the compounds having the structure of Formula (XI) and methods of using the same, such as methods of inhibiting kinases.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: February 28, 2017
    Assignee: The Regents of the University of California
    Inventors: John William Taunton, Jr., Jesse McFarland, Shyam Krishnan, Jonathan Choy
  • Patent number: 9546172
    Abstract: Disclosed herein are compounds such as those of Formula (I) 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: December 28, 2012
    Date of Patent: January 17, 2017
    Assignee: PHARMACYCLICS LLC
    Inventors: Wei Chen, David J. Loury
  • Patent number: 9533991
    Abstract: Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. 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: July 31, 2015
    Date of Patent: January 3, 2017
    Assignee: PHARMACYCLICS LLC
    Inventors: Wei Chen, Longcheng Wang, Zhaozhong J. Jia
  • Patent number: 9475818
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: October 25, 2016
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 9447102
    Abstract: The present invention relates to a novel family of inhibitors of protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: September 20, 2016
    Assignee: PHARMASCIENCE, INC.
    Inventors: Alain Laurent, Yannick Rose
  • Patent number: 9446130
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or pharmaceutically acceptable salts thereof. Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Grant
    Filed: January 17, 2014
    Date of Patent: September 20, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Jian Liu, Hao Wu, Shilan Liu, Chundao Yang, Shuling Zheng
  • Patent number: 9328120
    Abstract: The invention relates to novel 6-Cycloalkyl-pyrazolopyrimidinones according to formula (I). wherein R1 is a 5 or 6 membered aromatic heteroaryl-group, R2 is an optional substituent, D is optionally substituted cyclopentyl, cyclohexyl, tetrahydrofuranyl, tetrahydropyranyl or 2-, 3- or 4-pyridyl, m=1 or 2 and n is 0, 1 or 2. The new compounds are for use as the active entity of medicaments or for the manufacture of medicaments respectively, in particular medicaments for the treatment of conditions concerning deficits in perception, concentration, learning or memory. Such conditions may for example be associated with Alzheimer's disease, schizophrenia and other diseases. The new compounds are also for example for the manufacture of medicaments and/or for use in the treatment of these diseases, in particular for cognitive impairment associated with such disease. The compounds of the invention show PDE9 inhibiting properties.
    Type: Grant
    Filed: October 10, 2014
    Date of Patent: May 3, 2016
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Niklas Heine, Christian Eickmeier, Marco Ferrera, Riccardo Giovannini, Holger Rosenbrock, Gerhard Schaenzle
  • Patent number: 9290499
    Abstract: Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: March 22, 2016
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Xiaodong Wang, Jing Liu, Chao Yang, Weihe Zhaug, Stephen Frye, Dmitri Kireev
  • Patent number: 9273051
    Abstract: Disclosed herein are compounds of Formula (I) 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: September 14, 2012
    Date of Patent: March 1, 2016
    Assignee: Pharmacyclics LLC
    Inventors: Wei Chen, David J. Loury
  • Patent number: 9156844
    Abstract: Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C—R1 or N; —X1—X2— is CR15?N— or —NR19—CO—; and R1-R6, R15, R15 and R19 are as defined in the claims.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: October 13, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Christine Edwards, Janusz Kulagowski, Harry Finch
  • Patent number: 9150579
    Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: July 2, 2013
    Date of Patent: October 6, 2015
    Assignee: RHIZEN PHARMACEUTICALS SA
    Inventors: Swaroop Kumar V. S. Vakkalanka, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
  • Patent number: 9096611
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: August 4, 2015
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson
  • Patent number: 9040545
    Abstract: The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
    Type: Grant
    Filed: August 12, 2011
    Date of Patent: May 26, 2015
    Assignee: Cellzome Limited
    Inventors: Kathryn Bell, Nelly Piton, Claudio Dagostin, Cyrille Boussard, Andrew Ratcliffe, Nigel Ramsden
  • Publication number: 20150133661
    Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 14, 2015
    Inventors: Lee HONIGBERG, Erik VERNER, Joseph J. BUGGY, David LOURY, Wei CHEN
  • Patent number: 9029536
    Abstract: The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: May 12, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Joseph Raker, Takahiko Taniguchi, Masato Yoshikawa, Tomoaki Hasui, Jun Kunitomo
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Publication number: 20150119370
    Abstract: Compounds of Formula (I) or (II), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: August 29, 2014
    Publication date: April 30, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence P. WENNOGLE
  • Patent number: 9012463
    Abstract: Described herein are kinase inhibitor compounds of Formula IV: wherein Rb, R6, T, Y, and Z are defined herein. Also described herein are methods for synthesizing such inhibitors, and methods for using such inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate inhibitor of a protein, including a kinase.
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: April 21, 2015
    Assignee: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury, Tarak D. Mody, Erik Verner, Mark Stephen Smyth, Wenchen Luo
  • Publication number: 20150105408
    Abstract: There is provided inter alia 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-3-(2-chlorobenzyl)-4-oxo-3,4-dihydroquinazolin-5-yl)-N,N-bis(2-methoxyethyl)hex-5-ynamide in the form of a solid crystalline hydrate and in solid crystalline anhydrous form. There are also provided dry powder pharmaceutical compositions for inhalation containing such solid crystalline forms.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 16, 2015
    Inventors: Rudy Laurent Maria Broeckx, Walter Ferdinand Maria Filliers, Patrick Hubert, J Nieste, Alex Herman Copmans, Filip Marcel Vanhoutte, Carina Leys
  • Patent number: 8999999
    Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: April 7, 2015
    Assignee: Pharmacyclics, Inc.
    Inventors: Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
  • Patent number: 9000159
    Abstract: The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: April 7, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sachin Sundarlal Chaudhari, Sukeerthi Kumar, Abraham Thomas, Nisha Parag Patil, Ashok Bhausaheb Kadam, Vishal Govindrao Deshmukh, Sachin Vasantrao Dhone, Rajendra Prakash Chikhale, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20150094319
    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: September 29, 2014
    Publication date: April 2, 2015
    Inventors: Wei CHEN, Longcheng WANG, Zhaozhong J. JIA, David J. LOURY
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Publication number: 20150094295
    Abstract: The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: September 6, 2013
    Publication date: April 2, 2015
    Inventors: Tim Owens, Erik Verner
  • Patent number: 8993580
    Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tyrosine kinases and protein kinases such as mTOR. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: March 31, 2015
    Assignee: Intellikine LLC
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
  • Patent number: 8987233
    Abstract: Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: March 24, 2015
    Assignee: Pharmacyclics, Inc.
    Inventors: Zhengying Pan, Shyr Jiann Li, Heleen Scheerens, Lee Honigberg, Erik Verner
  • Patent number: 8987280
    Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: January 29, 2009
    Date of Patent: March 24, 2015
    Assignees: Genentech, Inc., F. Hoffmann-La Roche AG
    Inventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
  • Patent number: 8975266
    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: March 22, 2013
    Date of Patent: March 10, 2015
    Assignee: Pharmacyclics, Inc.
    Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
  • Publication number: 20150065505
    Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 5, 2015
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • Publication number: 20150065524
    Abstract: Polymorphs, hydrates, and solvates of chemical compounds that modulate kinase activity, including mTOR activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mTOR activity, are described herein.
    Type: Application
    Filed: August 10, 2012
    Publication date: March 5, 2015
    Applicant: Intellikine LLC
    Inventors: Pingda Ren, Michael Martin
  • Patent number: 8969555
    Abstract: The present invention provides compounds of the Formula I: wherein X is a bond or CH2; R is selected from the group consisting of R1 and R2 are each independently selected from the group consisting of CH and N; R3 is H or CH3; R4 is H or CH3; L is selected from the group consisting of —O(CH2)3—, —C(O)NH(CH2)2—, —CH2C(O)NH(CH2)2—, —(CH2)3N(C(O)CH3)CH2—, —(CH2)2N(C(O)CH3)CH2—, —(CH2)3NH—, (CH2)2OCH2—, —(CH2)4—, —(CH2)2NHCH2—, —(CH2)3O—, and —CH2O(CH2)2—; or a pharmaceutically acceptable salt thereof. Compounds of this invention are autotaxin inhibitors.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: March 3, 2015
    Assignee: Eli Lilly and Company
    Inventors: Thomas James Beauchamp, Yen Dao, Spencer Brian Jones, Bryan Hurst Norman, Lance Allen Pfeifer