Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
Type:
Grant
Filed:
September 23, 2009
Date of Patent:
June 25, 2013
Assignee:
Cogenia SRL
Inventors:
Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
Abstract: The present invention provides a process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, having the R-configuration, of formula (IA), or S-configuration of formula (IB), selectively over the other enantiomer.
Abstract: The invention is directed to thiocarbonate compounds of Formula (I)-(III) and methods of treating atherosclerosis, neuropathy, nephropathy, retinopathy, inflammatory disorders, COPD, cardiovascular diseases, metabolic disorders, type I diabetes mellitus, type II diabetes mellitus, LADA, Wolfram Syndrome 1, Wolcott-Rallison syndrome, metabolic syndrome, dyslipidemia, hyperglycemia, or insulin resistance. The compounds of the invention are also useful for protecting pancreatic beta-cells and for reducing free fatty acids, triglycerides, advanced glycated end products, ROS, lipid peroxidation, tissue and plasma TNFalpha and IL6 levels, or for delaying or preventing cardiovascular complications associated with atherosclerosis.
Type:
Grant
Filed:
September 16, 2011
Date of Patent:
June 18, 2013
Assignee:
Genmedica Therapeutics SL
Inventors:
Julio Cesar Castro Palomino Laria, Luc Marti Clauzel, Antonio Zorzano Olarte, Silvia Garcia Vicente, Alec Mian
Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
Type:
Grant
Filed:
November 7, 2011
Date of Patent:
June 18, 2013
Assignee:
EnVivo Pharmaceuticals, Inc.
Inventors:
Amy Ripka, Gideon Shapiro, Richard Chesworth
Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Grant
Filed:
August 27, 2012
Date of Patent:
June 11, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
Abstract: A heterocyclic compound of formula 1 and an organic light-emitting device including an organic layer containing the heterocyclic compound. The heterocyclic compound of Formula 1 may be suitable as a material for an emission layer, an electron transport layer or an electron injection layer of an organic light-emitting device. Due to the inclusion of the heterocylic group in its molecular structure, the heterocyclic compound of Formula 1 may have a high glass transition temperature (Tg) or a high melting point, and may prevent crystallization. An organic light-emitting device manufactured using the heterocyclic compound of Formula 1, which has a symmetrical structure in which a chrysene group and an indole group are fused, has excellent durability when stored or operated.
Type:
Grant
Filed:
March 31, 2011
Date of Patent:
June 4, 2013
Assignee:
Samsung Display Co., Ltd.
Inventors:
Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Yoon-Hyun Kwak, Jin-O Lim, Jong-Hyuk Lee
Abstract: A method of preparing novel [11C]-labeled benzophenone/bezoxazole analogues is provided. The present invention also provides novel [11C]-labeled benzophenone/bezoxazole analogues prepared from the GMP synthesis method. Kit claims for preparing novel [11C]-labeled benzophenone/bezoxazole analogues and a method of use thereof are also provided.
Abstract: A rodenticidal compound of formula (I): as well as the isomers thereof, in particular enantiomers, diastereoisomers, tautomers or mixtures of isomers in all proportions, where: R1 is: H or (II) or (III) with X?H, OH, Cl, Br, F or N02; R2 is: (IV) or (V) or (VI) with X?H, OH, Cl, Br, F or NO2; R3 is: O or S or (VII) with X?H, OH, Cl, Br, F or N02. Compositions containing such compounds as well as a method of use thereof in controlling harmful rodents are also described.
Type:
Grant
Filed:
February 16, 2011
Date of Patent:
May 21, 2013
Assignee:
Liphatech
Inventors:
Romain Lasseur, Etienne Benoit, Philippe Berny, Stephane Besse
Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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:
February 18, 2011
Date of Patent:
May 14, 2013
Assignee:
F. Hoffmann-La Roche AG
Inventors:
Georgette Castanedo, Bryan Chan, Matthew C. Lucas, Brian Safina, Daniel P. Sutherlin, Zachary Sweeney
Abstract: A method for preparing saturated partially fluorinated alkoxy carboxylic acids or salts thereof by treating a compound: (II), where Rf represents a fluorinated, linear or branched alkyl residue interruptible by one or more oxygen atoms, n is 0 or 1, with a Z-anion in a reaction medium comprising water and an organic solvent, where the Z-anion is selected from CN—, SCN— and OCN— or combinations thereof. A method of making partially fluorinated ethers of the general formula (I) wherein Rf is defined as above, n is 0 or 1, and Z is nitrile (—CN), azide (—N3), thiocyanate (—SCN) or cyanate (—OCN) group, said method comprising treating a fluorinated olefin of the general formula (II) wherein the Z-anion is CN—, OCN—, SCN— or N3?. A compound of the general formula (I) as previously described where Z is selected from SCN, OCN and N3.
Type:
Grant
Filed:
November 24, 2009
Date of Patent:
May 14, 2013
Assignee:
3M Innovative Properties Company
Inventors:
Tilman Zipplies, Klaus Hintzer, Oleg Shyshkov
Abstract: Provided are process for the preparation of (R)- and/or (S)-Rivaroxaban, and compounds which are intermediate compounds used in the processes for the preparation of (R)- and/or (S)-Rivaroxaban.
Abstract: Vinylsilane compounds having a specific amino group, typically diethylaminopropyldimethylvinylsilane, N-methylpiperazinylpropyldimethylvinylsilane, and bistrimethylsilylaminopropyldimethylvinylsilane are novel and useful as a modifier for polymers.
Abstract: By oral administration of a compound represented by the following Formula (I): the blood level of Compound (IV): which has an excellent inhibitory action against blood coagulation factor VIIa and the anticoagulant action, reaches a level sufficient for expression of its pharmacological actions. Therefore, the compound of the present invention is useful as a therapeutic and/or prophylactic agent for diseases caused by thrombus formation.
Abstract: The present invention relates to fluorescent dyes in general. The present invention provides a wide range of fluorescent dyes and kits containing the same, which are applicable for labeling a variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis, and/or treatment of disease conditions.
Abstract: A method for making the compound of Formula I: is set forth using alkylation, amidation, chlorination and phosphate installation procedures.
Type:
Grant
Filed:
January 27, 2012
Date of Patent:
May 7, 2013
Assignee:
Bristol-Myers Squibb Company
Inventors:
Jonathan Clive Tripp, Dayne Dustan Fanfair, Mitchell J. Schultz, Saravanababu Murugesan, Richard J. Fox, Chung-Pin H. Chen, Sabrina E. Ivy, Joseph Francis Payack, Wendel W. Doubleday
Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
Type:
Grant
Filed:
October 5, 2012
Date of Patent:
April 30, 2013
Assignee:
Onyx Therapeutics, Inc.
Inventors:
Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
Abstract: The present invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are as defined in claim 1, medicinal products containing them and use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
Type:
Grant
Filed:
August 24, 2007
Date of Patent:
April 30, 2013
Assignee:
Abbott GmbH & Co. KG
Inventors:
Herve Geneste, Thorsten Oost, Astrid Netz, Charles W. Hutchins, Wolfgang Wernet, Wilfred Lubisch, Liliane Unger, Wilfried Hornberger
Abstract: Compounds of formula (I) in free or salt or solvate form, where T1, T2, and T3 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
Type:
Grant
Filed:
January 9, 2009
Date of Patent:
April 30, 2013
Assignee:
Novartis AG
Inventors:
Peter Hunt, Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
Abstract: A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds.
Type:
Grant
Filed:
March 8, 2011
Date of Patent:
April 16, 2013
Assignees:
National University Corporation Tohoku University, API Corporation