Abstract: The synthesis and activity of novel LpxA inhibitors is described, these inhibitors present antibacterial activity. The compounds were designed based on a receptor model developed using the crystal structure of LpxA and are arranged to have a favorable binding interaction at the active site of the enzyme. In particular, the compounds present the following formula (I) where V, W, X, Y and Z can be independently C, S, N or O and P1, P2 and P3 are ligands to bind to the three points of the proposed pharmacophore model. They can be chosen from a variety of groups.
Type:
Grant
Filed:
March 6, 2006
Date of Patent:
September 16, 2014
Inventors:
Fan Wu, Donald Weaver, Chris Barden, Christopher McMaster, David Byers, Annette Henneberry, Fuqiang Ban
Abstract: The present invention relates to a long-acting sustained-release dosage form for treatment of Parkinson Disease, comprising a dopamine receptor agonist and a pharmaceutically acceptable biodegradable polymer accessories, wherein the content of the dopamine receptor agonist in the sustained-release dosage form is 5-50% by weight, and the content of the pharmaceutically acceptable polymer accessories is 50-95% by weight.
Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
Type:
Application
Filed:
May 9, 2014
Publication date:
September 4, 2014
Applicant:
Aerie Pharmaceuticals, Inc.
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
Type:
Grant
Filed:
December 14, 2012
Date of Patent:
September 2, 2014
Assignee:
Ligand Pharmaceuticals Incorporated
Inventors:
Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
Type:
Application
Filed:
March 31, 2014
Publication date:
August 28, 2014
Applicant:
UCB Pharma GmbH
Inventors:
Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
Abstract: The present invention relates, in various embodiments, to a compound represented by Structural Formula (I), pharmaceutically acceptable salts or prodrugs thereof, and compositions comprising said compounds, or pharmaceutically acceptable salts or prodrugs thereof. Methods of using compounds of Structural Formulas (I) and (la) or compositions comprising compounds of Structural Formulas (I) and (la), or pharmaceutically acceptable salts or prodrugs thereof, to treat ischemia or ischemia-reperfusion injury are also disclosed.
Type:
Grant
Filed:
November 10, 2011
Date of Patent:
August 26, 2014
Assignee:
Ischemix LLC
Inventors:
Alexander B. Baguisi, Reinier Beeuwkes, Ralph Casale, Steven A. Kates, Alan S. Lader
Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, 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:
April 22, 2013
Date of Patent:
August 12, 2014
Assignee:
Sanofi
Inventors:
Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek
Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.
Type:
Application
Filed:
April 7, 2014
Publication date:
August 7, 2014
Applicant:
BHI Limited Partnership
Inventors:
Xianqi KONG, Mohamed ATFANI, Benoit BACHAND, Abderrahim BOUZIDE, Stephane CIBLAT, Sophie LEVESQUE, David MIGNEAULT, Isabelle VALADE, Xinfu WU, Daniel DELORME
Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Application
Filed:
March 18, 2014
Publication date:
August 7, 2014
Applicant:
Allergan, Inc.
Inventors:
PHONG X. NGUYEN, TODD M. HEIDELBAUGH, John R. Cappiello
Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
Type:
Grant
Filed:
December 13, 2010
Date of Patent:
July 29, 2014
Assignee:
Gowan Co.
Inventors:
Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
Abstract: Disclosed are compounds of formula (IA), formula (IV) or formula (V), wherein the variables are as defined herein, and pharmaceutical compositions containing them which are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction.
Type:
Grant
Filed:
August 20, 2007
Date of Patent:
July 22, 2014
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Keizo Koya, Lijun Sun, Shoujun Chen, Jun Jiang
Abstract: The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
Type:
Grant
Filed:
January 20, 2012
Date of Patent:
July 8, 2014
Assignee:
State of Oregon acting by and through the State Board of Higher Education on behalf of Oregon State University
Inventors:
James David White, David T. Wong, David B. Chan, Jongtae Yang, Rajan Juniku
Abstract: Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
Type:
Grant
Filed:
May 31, 2007
Date of Patent:
July 8, 2014
Assignee:
Amgen Inc.
Inventors:
Jay P. Powers, Michael Degraffenreid, Lisa Julian, Jacob Kaizerman, Dustin McMinn, Yosup Rew, Daqing Sun, Xuelei Yan, Zhulun Wang, Felix Gonzalez Lopez De Turiso
Abstract: The present invention relates to a pharmaceutical composition comprising specific compounds which may be obtained from Leontopodium alpinum Cass. (Edelweiss). A preferred compound is leoligin (=(2S,3R,4R)-4-(3,4-dimethoxybenzyl) -2-(3,4-dimethoxyphenyl)tetrahydrofuran-3-yl]methyl(2Z)-2-methylbut-2-enoat]). Corresponding means and methods in respect of medical uses of the compounds are described. The present invention also provides a medical device comprising, containing or having been contacted with the compound. The compounds provided herein may particularly be used in the treatment of hyperplastic diseases, in particular intimal hyperplasia, e.g. stenosis, restenosis, atherosclerosis and the like. Also envisaged herein is the use of these compounds in the treatment of proliferative diseases, such as leukemia, prostate cancer and lung cancer.
Type:
Grant
Filed:
July 17, 2009
Date of Patent:
July 1, 2014
Assignee:
Universität Innsbruck
Inventors:
Hermann Stuppner, Stefan Schwaiger, David Bernhard, Günther Laufer
Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.
Type:
Grant
Filed:
April 9, 2012
Date of Patent:
June 24, 2014
Assignee:
Aerie Pharmaceuticals, Inc.
Inventors:
Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
Abstract: The present invention relates to the use of rotigotine [(?)-5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1-naphthol] and its prodrugs and pharmaceutically acceptable salts for producing a pharmaceutical agent for treating depression.
Type:
Grant
Filed:
July 22, 2004
Date of Patent:
June 17, 2014
Assignee:
UCB Pharma GmbH
Inventors:
Dieter Scheller, Alexander Breidenbach, Norma Selve
Abstract: The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
February 20, 2013
Date of Patent:
June 17, 2014
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Ken Chow, Evelyn G. Corpuz, Wha-Bin Im
Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
Type:
Grant
Filed:
June 24, 2010
Date of Patent:
June 17, 2014
Assignee:
UCB Pharma GmbH
Inventors:
Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
Abstract: A process to produce a dry purified furan-2,5-dicarboxylic acid (FDCA) is described. After oxidation of 5-(hydroxymethyl)furfural (5-HMF), a crude FDCA stream is produced that is fed to a crystallization zone followed by a solid-liquid displacement zone to form a low impurity slurry stream. The solids in the low impurity slurry stream are dissolved in a dissolution zone to produce a hydrogenation feed that is hydrogenated in a hydrogenation reactor to generate a hydrogenated FDCA composition. The hydrogenated FDCA composition is routed to a crystallization zone to form a crystallized produce stream that is separated from liquid in a solid-liquid separation zone to generate a purified wet cake stream containing FDCA that can be dried in a drying zone to generate a dry purified FDCA product stream.
Abstract: Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.
Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.
Type:
Grant
Filed:
July 13, 2012
Date of Patent:
June 3, 2014
Assignee:
Gilead Sciences, Inc.
Inventors:
William J. Watkins, Eda Canales, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith
Abstract: A combination of a prostaglandin EP4 agonist and an effective amount of: a prostaglandin EP2 agonist, a skin growth factor, a small peptide, a small inhibitory RNA targeting excess chronic inflammation or fibrosis, a cytokine with beneficial anti-inflammatory activity, an adenosine A2a receptor agonist, an anti-oxidant, or a combination thereof, may be used to treat skin wounds or scars.
Type:
Application
Filed:
November 13, 2013
Publication date:
May 22, 2014
Applicant:
Allergan, Inc.
Inventors:
Guang L. Jiang, Robert M. Burk, Wha-Bin Im, Larry A. Wheeler
Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.
Type:
Application
Filed:
July 13, 2012
Publication date:
May 15, 2014
Inventors:
Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
Type:
Application
Filed:
November 8, 2013
Publication date:
May 15, 2014
Applicant:
Jacobus Pharmaceutical Company, Inc.
Inventors:
Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.
Type:
Application
Filed:
October 28, 2013
Publication date:
May 8, 2014
Applicant:
BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Abstract: The present invention relates to a compound of the following formula (I): as well as its process of preparation, pharmaceutical and cosmetics composition comprising it and use thereof, notably as an inhibitor of the sodium-dependent glucose co-transporter, such as SGLT1, SGLT2 and SGLT3, in particular in the treatment or prevention of diabetes, and more particularly type-II diabetes, diabetes-related complications, such as arthritis of the lower extremities, cardiac infarction, renal insufficiency, neuropathy or blindness, hyperglycemia, hyperinsulinemia, obesity, hypertriglyceridemia, X syndrome and arteriosclerosis, as well as for its use as an anticancer, anti-infective, anti-viral, anti-thrombotic or anti-inflammatory drug, or for lightening, bleaching, depigmenting the skin, removing blemishes from the skin, particularly age spots and freckles, or preventing pigmentation of the skin.
Abstract: A breast cancer resistance protein (BCRP/ABCG2) inhibitor. The BCRP inhibitor contains, as an active ingredient, an acrylonitrile derivative or a salt thereof.
Abstract: The present application relates generally to amino tetraline derivative compounds and methods of use, specifically, embodiments including compounds of formula (I) described herein, pharmaceutically acceptable salts and solvates. More specifically, this application relates to amino tetraline derivative compounds and uses of such compounds producing medicaments for the treatment of various disease and conditions including movement disorders and disorders of the central nervous system.
Type:
Grant
Filed:
August 15, 2013
Date of Patent:
April 8, 2014
Inventors:
Peter Gmeiner, Miriam Ruberg, Harald Huebner
Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.
Abstract: The present invention relates to a long-acting sustained-release dosage form for treatment of Parkinson Disease, comprising a dopamine receptor agonist and a pharmaceutically acceptable biodegradable polymer accessories, wherein the content of the dopamine receptor agonist in the sustained-release dosage form is 5-50% by weight, and the content of the pharmaceutically acceptable polymer accessories is 50-95% by weight.
Abstract: The present invention is directed to methods for the treatment of treatment-refractory depression or treatment-resistant depression comprising administering to a patient in need thereof, a therapeutically effective amount of esketamine as mono-therapy or as combination therapy with at least on antidepressant.
Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
Type:
Grant
Filed:
August 28, 2012
Date of Patent:
April 1, 2014
Assignee:
Pfizer Inc.
Inventors:
Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.
Type:
Application
Filed:
September 5, 2013
Publication date:
March 27, 2014
Applicant:
ZOETIS LLC
Inventors:
Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
March 25, 2014
Assignee:
Progenra
Inventors:
Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
Abstract: Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents.
Type:
Grant
Filed:
August 8, 2011
Date of Patent:
March 25, 2014
Assignee:
Rempex Pharmaceuticals, Inc.
Inventors:
Gavin Hirst, Raja Reddy, Scott Hecker, Maxim Totrov, David C. Griffith, Olga Rodny, Michael N. Dudley, Serge Boyer
Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
Type:
Application
Filed:
October 28, 2013
Publication date:
March 20, 2014
Inventors:
Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Type:
Application
Filed:
November 13, 2013
Publication date:
March 20, 2014
Applicant:
MANNKIND CORPORATION
Inventors:
John Bruce PATTERSON, David Gregory LONERGAN, Gary A. FLYNN, Qingping ZENG, Peter V. PALLAI
Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.
Type:
Grant
Filed:
November 3, 2008
Date of Patent:
March 18, 2014
Assignee:
MethylGene Inc.
Inventors:
Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
Abstract: This invention relates to novel 4-trimethylammoniobutyrates of the formula wherein A1, R1, m and n are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit carnitine palmitoyl transferase (CPT) activity, in particular CPT2 activity, and can be used as medicaments.
Type:
Grant
Filed:
October 5, 2012
Date of Patent:
March 18, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Mirjana Andjelkovic, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
Abstract: The present invention is directed to novel thiophene inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
Abstract: The invention relates to a compound of general formula (I) characterized in that: R1 is a C1-C4 alkyl group, and R2 is an optionally substituted nitrogen, sulfur or oxygen containing heteroaromatic ring.