Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histamine H3 receptor (Ia). Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders.
Type:
Grant
Filed:
January 8, 2014
Date of Patent:
June 14, 2016
Assignee:
ARENA PHARMACEUTICALS, INC.
Inventors:
Jonathan A. Covel, Albert S. Ren, Graeme Semple, Thuy-Anh Tran, Zheng Wei, Yifeng Xiong
Abstract: The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.
Type:
Grant
Filed:
May 6, 2015
Date of Patent:
June 7, 2016
Assignee:
Novartis AG
Inventors:
John Vincent Calienni, Baoqing Gong, Prasad Kapa, Hui Liu
Abstract: The present invention relates to the prodrug of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-morpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide, rivaroxaban per se; processes for their preparation, and the application in treatment and/or prophylaxis of diseases, especially of thromboembolic disorders. The prodrug of a compound of formula (B) is chemically designated as 5-chloro-N-formyl-N-({(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide.
Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Abstract: Biologically active compounds, which are useful for treating a sexual disorder, are provided herein. Further provided are pharmaceutical compositions formulated for transdermal composition, which comprise a biologically active compound useful for treating a sexual disorder. The compounds and pharmaceutical compositions allow for a prolonged presence of a biologically active compound in plasma. Further provided herein are methods and uses of the compounds and pharmaceutical compositions described herein in the treatment of a sexual disorder, including female sexual disorders.
Abstract: The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.
Type:
Grant
Filed:
June 29, 2015
Date of Patent:
May 31, 2016
Assignee:
Glaxo Group Limited
Inventors:
Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr, Robert David Willacy
Abstract: The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
Type:
Grant
Filed:
July 26, 2012
Date of Patent:
May 31, 2016
Assignee:
SANOFI
Inventors:
Sven Ruf, Josef Pernerstorfer, Thorsten Sadowski, Georg Horstick, Herman Schreuder, Christian Buning, Klaus Wirth
Abstract: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. The imidazolidinedione compounds posses androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.
Abstract: A diagnostic imaging agent useful for positron emission tomography (PET) imaging as well as to improved hardware for producing such imaging agents is described. Flutemetamol (18F) Injection for the imaging of ?-amyloid plaques in the brain and methods and devices for preparing same are described including the automated synthesis and purification of [18F]flutemetamol by means of solid phase extraction (SPE).
Type:
Grant
Filed:
February 11, 2015
Date of Patent:
May 24, 2016
Assignee:
GE HEALTHCARE LIMITED
Inventors:
Eric Horn, Steven Fairway, Dimitrios Mantzilas, Nigel Powell
Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
Abstract: Form-II crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsulfonyl)acetamide and a method of producing the crystal are provided. The Form-II crystal exhibits diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2? when the spectrum is obtained by using Cu K? radiation: 9.0 degrees, 12.9 degrees, 20.7 degrees, and 22.6 degrees. The Form-II crystal can be produced by crystallizing the subject compound from an alcoholic solvent, a ketone solvent, a saturated hydrocarbon solvent, an ether solvent, water, or a mixture of these solvents. The crystal may be administered as an active ingredient to a subject for the purpose of treating or preventing certain diseases, disorders, and symptoms, or for promoting angiogenesis or gene therapy.
Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Type:
Grant
Filed:
August 27, 2014
Date of Patent:
May 10, 2016
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Melissa Fleury, Roland Gendron, Adam D. Hughes
Abstract: Disclosed is a method for preparing a dialkyl carbonate, in which a dialkyl carbonate such as dimethyl carbonate is economically prepared in an environmentally-friendly manner at a higher yield while reducing generation of a by-product. The method for preparing the dialkyl carbonate includes reacting urea, an alkyl carbamate having 1 to 3 carbon atoms, or a mixture thereof with a monovalent alcohol having 1 to 3 carbon atoms in the presence of a room temperature ionic liquid and a catalyst including a salt of a transition metal or a rare earth metal.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
May 10, 2016
Assignee:
RESEARCH INSTITUTE OF INDUSTRIAL SCIENCE & TECHNOLOGY
Inventors:
Joon Hyun Baik, Jae Cheon Koh, Kyong Tae Kim, Dong Jun Koh, Young Sam Sa, Yun Min Kim, Chul Ung Kim
Abstract: The invention relates to the use of quaternary pyridinium salts of formula (I), wherein R is NH2, CH3, or N(H)CH2OH group, and X is pharmaceutically acceptable counterion, for the preparation of vasoprotective agent for the treatment or prevention of conditions or diseases associated with dysfunction of vascular endothelium, oxidative stress, and/or insufficient production of endothelial prostacyclin PGI2, in particular but not exclusively if the above coincides with hypercholesterolemia, hypertriglyceridemia or low HDL level.
Abstract: The invention relates to PI3K inhibitors of the formula (I)• in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
Type:
Grant
Filed:
October 26, 2012
Date of Patent:
May 10, 2016
Assignee:
Novarits AG
Inventors:
Emmanuelle Briard, Pascal Furet, Andreas Lerchner, Peter Meier, Branko Radetich, David Andrew Sandham, Yanyi Zhu
Abstract: The present invention is directed to aminopyridine derived compounds of formula (A). The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinson's disease or cancer.
Type:
Grant
Filed:
December 30, 2013
Date of Patent:
April 26, 2016
Assignees:
H. Lundbeck A/S, Vernalis (R&D) Ltd.
Inventors:
Gitte Kobberøe Mikkelsen, Laurent David, Stephen Watson, Garrick Paul Smith, Douglas Stewart Williamson, I-Jen Chen
Abstract: The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
April 26, 2016
Assignee:
CHEMAPOTHECA, LLC
Inventors:
Harold Meckler, Brian Thomas Gregg, Jie Yang
Abstract: The present invention relates to compounds of formula (I) and to compositions comprising the same and to the use of the compounds and their compositions in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making said compounds.
Type:
Grant
Filed:
March 20, 2014
Date of Patent:
April 26, 2016
Assignee:
Respivert, Ltd.
Inventors:
John King-Underwood, Kazuhiro Ito, Peter John Murray, George Hardy, Frederick Arthur Brookfield, Christopher John Brown
Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Grant
Filed:
September 9, 2013
Date of Patent:
April 19, 2016
Assignees:
MERCK SHARP & DOHME CORP., MERCK CANADA INC.
Inventors:
Christian Beaulieu, David J. Bennett, Christopher J. Bungard, Ronald K. Chang, Sheldon Crane, Thomas J. Greshock, Li Hao, Kate Holloway, Jesse J. Manikowski, John A. McCauley, Daniel McKay, Carmela Molinaro, Oscar Miguel Moradei, Philippe G. Nantermet, Christian Nadeau, Satyanarayana Tummanapalli, William Shipe, Sanjay Kumar Singh, Vouy Linh Truong, Sivalenka Vijayasaradhi, Peter D. Williams, Catherine M. Wiscount