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), GLP-1(9-36), and oxyntomodulin, 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, R1, R2, R3, R4, R5, n, p and q are as defined herein.
Type:
Grant
Filed:
July 24, 2015
Date of Patent:
October 25, 2016
Assignee:
Celgene International II SARL
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: This invention is directed to a compound of formula (I): wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).
Type:
Grant
Filed:
April 4, 2012
Date of Patent:
October 18, 2016
Assignee:
Sanofi
Inventors:
Christopher L. Vandeusen, Franz J. Weiberth, Harpal S. Gill, George Lee, Andrea Hillegass
Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.
Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.
Type:
Grant
Filed:
March 4, 2016
Date of Patent:
October 4, 2016
Assignee:
NOVARTIS AG
Inventors:
Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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:
August 17, 2015
Date of Patent:
October 4, 2016
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Christopher F. Claiborne, Stephen Critchley, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Stepan Vyskocil, Gabriel S. Weatherhead
Abstract: Embodiments of the present invention relates to compounds of the following formula: as well as compositions, methods of imaging and methods of treating subjects comprising the use of the compound, wherein the variables are defined herein.
Type:
Grant
Filed:
November 5, 2012
Date of Patent:
October 4, 2016
Assignee:
Vanderblit University
Inventors:
H. Charles Manning, Jason R. Buck, Dewei Tang
Abstract: N-(pyrid-4-yl)amides and N-(pyrimidin-4-yl)amides of formula (1) are described that are potent modulators (e.g., inhibitors) of an androgen receptor, and which are useful, for example, in the treatment of a dermatological disease or disorder; a disease or disorder of the sebaceous gland(s); acne; hyperseborrhoea; oily skin, seborrhoeic dermatitis; hyperpilosity or hirsutism; atopic dermatitis; or androgenic alopecia; especially acne. Also described, are compositions (e.g., pharmaceutical compositions, cosmetic compositions) comprising the compounds; methods of preparing the compositions; methods of modulating (e.g., inhibiting) and androgen receptors using the compounds and/or compositions; and medical and/or cosmetic use of the compounds and compositions.
Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
Type:
Grant
Filed:
August 5, 2015
Date of Patent:
September 27, 2016
Assignee:
NOVARTIS AG
Inventors:
Michael Scott Visser, Michael Joseph Luzzio, Julien Papillon
Abstract: Disclosed are inhibitors of human galactokinase of formula (1) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).
Type:
Grant
Filed:
September 23, 2011
Date of Patent:
September 20, 2016
Assignee:
UNIVERSITY OF UTAH RESEARCH FOUNDATION
Inventors:
Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, R4 and A are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
September 10, 2013
Date of Patent:
September 20, 2016
Assignee:
Hoffmann-LA Roche INC.
Inventors:
Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Xianfeng Lin, Haixia Liu, Alexander V Mayweg, Zongxing Qiu, Hong Shen, Guozhi Tang, Lisha Wang, Guolong Wu, Shixiang Yan, Weixing Zhang, Mingwei Zhou, Wei Zhu
Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
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.
Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) as inhibitors of the enzyme phosphodiesterase 10 (PDE-10), pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition of the enzyme Phosphodiesterase 10 such as neurological, psychiatric, respiratory or metabolic diseases.
Type:
Grant
Filed:
January 24, 2014
Date of Patent:
September 20, 2016
Assignee:
PALOBIOFARMA S.L.
Inventors:
Juan Camacho Gómez, Julio Castro Palomino Laria
Abstract: The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
March 17, 2015
Date of Patent:
September 13, 2016
Assignee:
Natco Pharma Limited
Inventors:
Amala Kompella, Adibhatla Kali Satya Bhujanga Rao, Sreenivas Rachakonda, Venugopala Krishna Gampa, Venkaiah Chowdary Nannapaneni
Abstract: The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
Type:
Grant
Filed:
March 12, 2014
Date of Patent:
September 6, 2016
Assignee:
NOVARTIS AG
Inventors:
Thomas Raymond Caferro, Zhuoliang Chen, Young Shin Cho, Abran Q. Costales, Julian Roy Levell, Gang Liu, James R. Manning, Martin Sendzik, Cynthia Shafer, Michael David Shultz, James Sutton, Yaping Wang, Qian Zhao
Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Type:
Grant
Filed:
August 28, 2012
Date of Patent:
August 30, 2016
Assignee:
CHDI Foundation, Inc.
Inventors:
Stephen Martin Courtney, Michael Prime, William Mitchell, Christopher John Brown, Paula C. De Aguiar Pena, Peter Johnson, Celia Dominguez, Leticia M. Toledo-Sherman, Ignacio Muñoz-Sanjuan
Abstract: The present invention is directed to secondary alcohol substituted triazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
November 11, 2013
Date of Patent:
August 30, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Christopher D. Cox, Vadim Y. Dudkin, Carol A. McVean, Thomas S. Reger, Justin T. Steen
Abstract: Compounds of formula (I): are described herein. Compounds of the disclosure are modulators of Kv3 channels and may be used in the prophylaxis or treatment of related disorders.
Abstract: Compounds of formula (I) and their use as pharmaceutical.
Type:
Grant
Filed:
December 17, 2012
Date of Patent:
August 23, 2016
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuβe
Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
Type:
Grant
Filed:
May 26, 2015
Date of Patent:
August 16, 2016
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang