Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
Type:
Grant
Filed:
February 13, 2015
Date of Patent:
April 11, 2017
Assignee:
IMMUNOGEN, INC.
Inventors:
Wei Li, Michael Louis Miller, Ravi V. J. Chari
Abstract: The present invention provides a salt form, and compositions thereof, useful as an inhibitor of one or more protein kinases and which exhibits desirable characteristics for the same.
Type:
Grant
Filed:
October 21, 2013
Date of Patent:
March 28, 2017
Assignee:
Celgene CAR LLC
Inventors:
Steven Richard Witowski, William Frederick Westlin, III, Richland Wayne Tester
Abstract: The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
Type:
Grant
Filed:
October 31, 2013
Date of Patent:
March 28, 2017
Assignee:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Maria Menichincheri, Mauro Angiolini, Jay Aaron Bertrand, Michele Caruso, Paolo Polucci, Francesca Quartieri, Barbara Salom, Matteo Salsa, Fabio Zuccotto
Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof, wherein R12 or R13 on the A group is an amino substituent (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.
Type:
Grant
Filed:
February 25, 2015
Date of Patent:
March 21, 2017
Assignee:
ACHILLION PHARMACEUTICALS, INC.
Inventors:
Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Dawei Chen, Xiangzhu Wang, Atul Agarwal, Milind Deshpande, Jason Allan Wiles, Avinash S. Phadke
Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
Type:
Grant
Filed:
December 3, 2015
Date of Patent:
March 21, 2017
Assignee:
Celgene International II SÀRL
Inventors:
Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
Abstract: Provided herein are compounds that bind to dCK and methods for treating cancer.
Type:
Grant
Filed:
January 11, 2016
Date of Patent:
March 21, 2017
Assignees:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
Inventors:
Caius G. Radu, Zheng Li, Raymond M. Gipson, Jue Wang, Nagichettiar Satyamurthy, Arnon Lavie, Jennifer M. Murphy, David A. Nathanson, Michael E. Jung
Abstract: This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
Type:
Grant
Filed:
February 20, 2014
Date of Patent:
March 21, 2017
Assignee:
Janssen Sciences Ireland UC
Inventors:
David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Tim Hugo Maria Jonckers
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.
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
Abstract: The present invention relates to an improved process of preparing substantially pure alcaftadine comprising reacting substantially pure compound of structural formula VIII with more than 20 moles of oxidizing reagent in an organic solvent to obtain alcaftadine:
Abstract: The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically acceptable salt thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling endoparasites in warm-blooded animals.
Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
Type:
Grant
Filed:
January 5, 2016
Date of Patent:
February 21, 2017
Assignee:
Celgene Quanticel Research, Inc.
Inventors:
Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
Abstract: Disclosed are chemical entities of formula I: wherein X, Y, Z, R1, R3, R4, R5 and R6 are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of formula I, and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of formula I.
Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
Type:
Grant
Filed:
March 10, 2014
Date of Patent:
February 7, 2017
Assignee:
CHDI Foundation, Inc.
Inventors:
Celia Dominguez, Vahri Beaumont, Ignacio Muñoz-Sanjuán, Roland W. Bürli, Alan F. Haughan, Christopher A. Luckhurst, Michael Wall, Gilles Raphy, Beth Thomas
Abstract: Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.
Type:
Grant
Filed:
December 19, 2014
Date of Patent:
January 31, 2017
Assignee:
Signal Pharmaceuticals, LLC
Inventors:
Patrick Papa, Brian Edwin Cathers, Andrew Antony Calabrese, Brandon Wade Whitefield, Brydon Bennett, Daniel Cashion, Deborah Mortensen, Dehua Huang, Eduardo Torres, Jason Parnes, John Sapienza, Joshua Hansen, Katerina Leftheris, Matthew Correa, Maria Mercedes Delgado, Raj K. Raheja, Sogole Bahmanyar, Sayee Hegde, Stephen Norris, Veronique Plantevin-Krenitsky
Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
Type:
Grant
Filed:
August 21, 2015
Date of Patent:
January 31, 2017
Assignee:
Janssen Pharmaceutica NV
Inventors:
Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick Rene Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
Abstract: This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
Abstract: Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein D, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.
Type:
Grant
Filed:
August 6, 2014
Date of Patent:
January 31, 2017
Assignee:
Roche Palo Alto LLC
Inventors:
Chris Allen Broka, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley, Alam Jahangir, Clara Jeou Jen Lin, Daniel Warren Parish
Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0): wherein R1 represents a substituent, R2 represents a hydrogen atom, or a substituent, R3 represents a hydrogen atom, or a substituent, Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.
Type:
Grant
Filed:
October 17, 2014
Date of Patent:
January 24, 2017
Assignee:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventors:
Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
Abstract: The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of substituted indol-5-ol derivatives to modulate protein kinases and for treating protein kinase-mediated diseases.