Abstract: The invention relates to N-[4-(quinolin-4-yloxy)cyclohexyl(methyl)](hetero)arylcarboxamides, intermediates and methods for their production, use thereof for treating and/or preventing diseases and use thereof for producing medicinal products and use thereof for treating and/or preventing diseases, especially of hyperproliferative diseases.
Type:
Grant
Filed:
June 24, 2013
Date of Patent:
August 30, 2016
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Duy Nguyen, Hermann Künzer, Hortensia Faus Gimenez, Benjamin Bader, Silke Köhr, Martin Fritsch
Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) br’omodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.
Type:
Grant
Filed:
November 18, 2014
Date of Patent:
August 23, 2016
Assignee:
Forma Therapeutics, Inc.
Inventors:
Kenneth W. Bair, Torsten Herbertz, Goss S. Kauffman, Katherine J. Kayser-Bricker, George P. Luke, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Adam C. Talbot, Mark J. Tebbe
Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Type:
Grant
Filed:
January 10, 2014
Date of Patent:
August 2, 2016
Assignee:
VENATORX PHARMACEUTICALS, INC.
Inventors:
Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson
Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.
Type:
Grant
Filed:
April 15, 2015
Date of Patent:
August 2, 2016
Assignee:
OTSUKA PHARMACEUTICAL CO., LTD.
Inventors:
Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori
Abstract: The present invention relates to a process for preparing substituted indole derivatives. More particularly, the invention refers to a new method to synthesize indole-derivatives by oxidative C—H-functionalization.
Abstract: The present invention relates to quinoline compounds, and pharmaceutically acceptable compositions thereof, useful as antagonists of P2X7, and for the treatment of P2X7-related disorders.
Type:
Grant
Filed:
June 4, 2015
Date of Patent:
July 26, 2016
Assignee:
Merck Patent GmbH
Inventors:
Srinivasa R. Karra, Yufang Xiao, Jeyaprakashnarayanan Seenisamy, Jayashankaran Jayadevan
Abstract: The present application relates to a series of substituted imidazo[1,2-a]pyridine compounds of formula (I), pharmaceutically acceptable salts, pharmaceutically acceptable solvates or stereoisomers thereof, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
April 29, 2015
Date of Patent:
July 19, 2016
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
Abstract: The present invention relates to novel compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
Type:
Grant
Filed:
December 23, 2013
Date of Patent:
July 19, 2016
Assignee:
Cadila Healthcare Limited
Inventors:
Ranjit C. Desai, Vrajesh Pandya, Pankaj Ramanbhai Patel
Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.
Type:
Grant
Filed:
January 9, 2013
Date of Patent:
July 19, 2016
Assignee:
X-Chem, Inc.
Inventors:
Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
Abstract: The present invention relates to an improved and industriously advantageous process by means of providing coupling/condensing of wet mass of (1-cyclopropyl-6,7-difluoro-8-methoxy-4-oxo-1,4-dihydro-3-quinoline carboxylic acid-O3,O4)bis(acyloxy-O)borate with (S,S)-2,8-diazabicyclo[4.3.0]nonane to give 1-cyclopropyl-7-[S,S]-2,8-diazabicyclo-[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride (Moxifloxacin hydrochloride) of Formula-I with high purity.
Abstract: (E)-2-(2-Quinolin-2-yl-propenyl)-phenol, 2-Quinolin-2-yl-ylethynyl-phenol and salts thereof are useful as medicaments, especially for treatment of an angiogenesis-related disease or disorder.
Type:
Grant
Filed:
July 15, 2013
Date of Patent:
July 12, 2016
Assignees:
UNIVERSITY COLLEGE DUBLIN NATIONAL UNIVERSITY OF IRELAND, DUBLIN, THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMEBERS OF BOARD, OF THE COLLEGES OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN
Inventors:
Breandan Douglas Kennedy, Alison Reynolds, Claire Kilty, Jacintha O'Sullivan, Andrew Douglas Baxter
Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I: wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
Type:
Grant
Filed:
November 18, 2014
Date of Patent:
July 12, 2016
Assignee:
Forma Therapeutics, Inc.
Inventors:
Kenneth W. Bair, Torsten Herbertz, Goss S. Kauffman, Katherine J. Kayser-Bricker, George P. Luke, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Adam C. Talbot
Abstract: A new medical therapy, and more particularly certain quinoline compounds which are anti-angiogenic integrin aplha5beta1 inhibitors, for use in the treatment of fibrosis, or a fibrosis-related disease, such as a fibrotic disease affecting the lung, liver, kidney, skin, epidermis, endodermis, muscle, tendon, cartilage, heart, stomach, large intestine, small intestine, colon, uterus, nervous system, testis, adrenal gland, artery, vein, biliary tract, or eye.
Abstract: The invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. The present invention is directed to novel bis-quarternary cinchona alkaloid salts and the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis. On certain substrates and under specific reaction conditions, the inventors have discovered that the use of bis-quarternary cinchona alkaloid salts in asymmetric phase transfer catalysis surprisingly provides for a more active and efficient process as compared to mono-quarternary catalysts.
Abstract: The present invention relates to a pharmaceutical composition for inhibiting angiogenesis and a novel sulfonyl amide derivative compound which can be useful for the prevention or treatment of angiogenesis-related diseases or disorders. Since the compound used as an active ingredient in the pharmaceutical composition of the invention is specifically bound to UQCRB and inhibits biological functions thereof, apoptosis is not induced and angiogenic responses are inhibited. Therefore, the compound used as an active ingredient in the pharmaceutical composition of the invention can be useful as an effective and safe angiogenesis inhibitory agent.
Type:
Grant
Filed:
May 23, 2011
Date of Patent:
June 21, 2016
Assignee:
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Inventors:
Ho Jeong Kwon, Gyoon Hee Han, Hye Jin Jung, Jeong Jea Seo
Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.
Abstract: The present invention relates to compounds of formula (I) and (IV), and pharmaceutically acceptable salts, tautomers, stereoisomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are for use in the treatment of disorders that are ameliorated by inhibition of HDAC such as cancer and hemoglobinopathies like ?-thalassemia or sickle cell anemia.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
June 21, 2016
Assignees:
IRBM-SCIENCE PARK S.P.A., C.N.C.C.S. SCARL COLLEZIONE NAZIONALE DEI COMPOSTI CHIMICI E CENTRO SCREENING
Inventors:
Sergio Altamura, Alberto Bresciani, Giulia Breveglieri, Danilo Fabbrini, Roberto Gambari, Steven Harper, Ralph Laufer, Edith Monteagudo, Emanuela Nizi, Paola Pace, Vincenzo Summa
Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
Type:
Grant
Filed:
May 12, 2014
Date of Patent:
June 21, 2016
Assignee:
Centrexion Therapeutics Corporation
Inventors:
Riccardo Giovannini, Yunhai Cui, Henri Doods, Marco Ferrara, Stefan Just, Raimund Kuelzer, Iain Lingard, Rocco Mazzaferro, Klaus Rudolf