Abstract: The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
September 25, 2012
Date of Patent:
July 1, 2014
Assignee:
Gruenenthal GmbH
Inventors:
Robert Frank, Gregor Bahrenberg, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
Abstract: The present invention relates to aryl- or heteroaryl-substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Type:
Grant
Filed:
December 20, 2012
Date of Patent:
July 1, 2014
Assignee:
Epizyme, Inc.
Inventors:
Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah Kathleen Knutson, Timothy James Nelson Wigle, Masashi Seki, Syuji Shirotori, Satoshi Kawano
Abstract: A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
Type:
Application
Filed:
April 8, 2012
Publication date:
June 26, 2014
Applicant:
HANALL BIOPHARMA CO., LTD.
Inventors:
Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Type:
Grant
Filed:
October 6, 2011
Date of Patent:
June 3, 2014
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Francesco G. Salituro, Jeffrey O. Saunders
Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
Type:
Application
Filed:
June 20, 2013
Publication date:
May 15, 2014
Inventors:
Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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 invention relates to compounds of formula (I): where A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
Type:
Application
Filed:
October 3, 2011
Publication date:
May 8, 2014
Applicant:
SYNGENTA PARTICIPATIONS AG
Inventors:
Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Guillaume Berthon
Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.
Abstract: In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. In particular, the present invention also relates to methods and uses for treatment of respiratory or respiratory tract diseases, which comprises administering to a subject in need thereof an effective amount of a compound of the present invention.
Type:
Application
Filed:
July 3, 2012
Publication date:
May 1, 2014
Inventors:
Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
Type:
Grant
Filed:
September 12, 2012
Date of Patent:
April 8, 2014
Assignee:
Millennium Pharmaceuticals, Inc.
Inventors:
Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song
Abstract: The invention relates to new methods of modulating cholesterol by inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9) with fatty acid derivatives; and new methods for treating or preventing a metabolic disease comprising the administration of an effective amount of a fatty acid derivative. The present invention is also directed to fatty acid bioative derivatives and their use in the treatment of metabolic diseases.
Type:
Application
Filed:
May 24, 2013
Publication date:
April 3, 2014
Applicant:
Catabasis Pharmaceuticals, Inc.
Inventors:
Jill C. Milne, Michael R. Jirousek, Chi B. Vu
Abstract: The present invention relates to novel compounds of formula (II) that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating, or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
Type:
Grant
Filed:
July 25, 2012
Date of Patent:
March 18, 2014
Assignee:
AC Immune SA
Inventors:
Wolfgang Froestl, Nampally Sreenivasachary, Sophie Lohmann, Maria Pilar Lopez Deber, Andreas Muhs, Maria Pihlgren Bosch
Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.
Type:
Application
Filed:
May 17, 2012
Publication date:
March 6, 2014
Applicant:
SOUTHWEST RESEARCH INSTITUTE
Inventors:
Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
Abstract: Contemplated compositions and methods are employed to bind in vitro and in vivo to an ?4?2 nicotinic acetylcholine receptor in a highly selective manner. Where such compounds are labeled, compositions and methods employing such compounds can be used for PET and SPECT analysis. Alternatively, and/or additionally contemplated compounds can be used as antagonists, partial agonists or agonists in the treatment of diseases or conditions associated with ?4?2 dysfunction.
Type:
Application
Filed:
February 6, 2013
Publication date:
February 20, 2014
Applicant:
The Regents of the University of California
Inventors:
Jogeshwar Mukherjee, Sharon A. Kuruvilla
Abstract: The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
Type:
Grant
Filed:
September 30, 2011
Date of Patent:
February 18, 2014
Assignee:
BASF SE
Inventors:
Karsten Koerber, Florian Kaiser, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun
Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.
Type:
Application
Filed:
October 4, 2013
Publication date:
February 6, 2014
Applicant:
BASF SE
Inventors:
Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
February 4, 2014
Assignees:
Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
Inventors:
Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
Type:
Grant
Filed:
August 14, 2009
Date of Patent:
February 4, 2014
Assignee:
N30 Pharmaceuticals, Inc.
Inventors:
Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Application
Filed:
June 5, 2013
Publication date:
January 23, 2014
Inventors:
Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.
Type:
Grant
Filed:
February 24, 2011
Date of Patent:
January 21, 2014
Assignee:
Targacept, Inc.
Inventors:
Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve, Craig Harrison Miller
Abstract: The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions.
Type:
Grant
Filed:
November 30, 2009
Date of Patent:
January 21, 2014
Assignee:
Targacept, Inc.
Inventors:
Srinivasa Rao Akireddy, Scott R. Breining, Timothy J. Cuthbertson, Gary Maurice Dull, Gregory J. Gatto, John Genus, Philip S. Hammond, Joesph Pike Mitchener, Jr., Julio A. Munoz, Pieter Albert Otten, Daniel Yohannes, Nikolai Fedorov
Abstract: Provided is an organic light-emitting device having an optical output with high luminance and high color purity with extremely high efficiency. The organic light-emitting device includes an organic layer between the anode and the cathode, in which one of the anode and the cathode is a transparent electrode or a semi-transparent electrode and at least one layer of the organic layer contains at least one kind of indenopyrene compound having a specific structure.
Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
June 20, 2013
Publication date:
January 2, 2014
Inventors:
Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
Type:
Grant
Filed:
June 10, 2013
Date of Patent:
December 31, 2013
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
Type:
Grant
Filed:
August 24, 2010
Date of Patent:
December 10, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
Type:
Application
Filed:
December 7, 2012
Publication date:
November 28, 2013
Applicant:
Myrexis, Inc.
Inventors:
J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
Type:
Application
Filed:
August 2, 2013
Publication date:
November 28, 2013
Applicant:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
Type:
Application
Filed:
April 23, 2013
Publication date:
November 21, 2013
Applicants:
AbbVie Inc., AbbVie Deutschland GmbH & Co KG
Inventors:
AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
Abstract: The invention provides compounds of formula I blocking phosphorylcholine biosynthesis by means of the selective blocking of the choline kinase enzyme in tumor cells or in cells affected by parasitic infection and therefore being applicable in the treatment of tumors and parasitic diseases or diseases produced by viruses and fungi in animals, including human beings; as well as to a method for preparing the compounds of the invention and certain intermediates of said method.
Type:
Grant
Filed:
August 13, 2010
Date of Patent:
November 19, 2013
Assignees:
Universidad de Granada, Consejo Superior de Investigaciones Cientificas
Inventors:
Juan Carlos Lacal Sanjuán, Joaquin Campos Rosa, Miguel Ángel Gallo Meza, Antonio Espinosa Ubeda
Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
Type:
Application
Filed:
July 19, 2011
Publication date:
November 14, 2013
Applicants:
DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
Inventors:
Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
Type:
Application
Filed:
October 18, 2011
Publication date:
October 24, 2013
Applicant:
ELCELYX THERAPEUTICS, INC.
Inventors:
Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
Type:
Application
Filed:
March 13, 2013
Publication date:
October 10, 2013
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Application
Filed:
March 28, 2013
Publication date:
October 10, 2013
Applicant:
ChemoCentryx, Inc.
Inventors:
Solomon Ungashe, John J. Wright, Andrew Pennell, Zheng Wei
Abstract: The invention relates pyridine amide derivative of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are independently hydrogen, linear o branched (C1-C3)alkyl or joined together they form a cyclopropyl ring; R is independently selected from the group consisting of halogens and trifluoromethyl and p is 1, 2 or 3; A is C or N; E is a group of formula (B) or (C), wherein B is C(O)OH, C(O)O(C1-C3)alkyl, and C is selected from the group consisting of formula (I) m is 1,2 or 3, n is 0 or 1, W is —O—, —O(C1-C3 alkyl)-; —(C1-C3 alkyl)O—; —C(O)—; —C(?N—O(C1-C3 alkyl))-; —NH— or —NH(C1-C3alkyl)-; Ar is phenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, trifluoromethyl, trifluoromethoxy, methyl, —NH(C1-C3alkyl)-; —N(C1-C3alkyl)(C1-C3alkyl)-, a from 5 to 7 membered heterocyclic ring containing one nitrogen atom which is covalently bonded to Ar and optionally containing one or two heteroatoms selected from N, O and S; and a 5- or 6-member
Type:
Application
Filed:
December 10, 2010
Publication date:
October 3, 2013
Inventors:
Manuela Borriello, Lucio Rovati, Luigi Piero Stasi, Benedetta Buzzi, Fabrizio Colace
Abstract: The invention relates to enantiomerically pure 3-(phthalimido)piperidines and processes for preparing enantiomerically pure 3-(phthalimido)piperidines.
Abstract: Photochromic and electrochromic hexadiene compounds that are reversibly convertible between ring-open and ring-closed isomeric forms. The conversion between the different isomeric forms may be induced by light or electricity. The compounds may include a charge transfer moiety including electron donor and acceptor groups. The electron donor and acceptor are linearly conjugated in the ring-open form to enable electron transfer but are electrically insulated in the ring-closed form. Photoresponsive compounds may be synthesized by any of several methods disclosed, e.g., by reacting diene precursors with dienophiles in a condensation reaction. The compounds may be utilized in reactivity-gated photochromic or electrochromic applications. Compounds may be used in a method to selectively release a releasable agent, such as a small molecule.
Type:
Grant
Filed:
May 25, 2006
Date of Patent:
September 17, 2013
Assignee:
Switch Materials Inc.
Inventors:
Neil R. Branda, Bettina Wuestenberg, Vincent Lemieux, Michael Adams, Simon Gauthier
Abstract: The present invention relates to novel pesticidal arylpyrrolidine compounds (arylpyrrolidines) having the general formula (I) wherein A, X1, X2, X3, X4, R1, R2, R3, R4, and G are as defined in the application and their use as pesticide, in particular for combating animal pests which occur in the agricultural and/or the veterinary field, as well as to a preparation methods for preparing such compounds.
Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.
Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.
Type:
Grant
Filed:
August 2, 2011
Date of Patent:
August 20, 2013
Assignees:
Allergan, Inc., ExonHit Therapeutics SA
Inventors:
Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
Abstract: The present invention relates to inhibitors of 11-?-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
Type:
Grant
Filed:
April 20, 2010
Date of Patent:
August 13, 2013
Assignee:
AbbVie Inc.
Inventors:
Sridhar Peddi, Meena V. Patel, Jeffrey J. Rohde
Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
Type:
Grant
Filed:
March 23, 2009
Date of Patent:
August 6, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
July 30, 2013
Assignee:
Abbott GmbH & Co. KG
Inventors:
Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger
Abstract: The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.
Type:
Application
Filed:
March 7, 2013
Publication date:
July 18, 2013
Applicants:
The Board of Trustees of the University of Illinois, PsychoGenics, Inc.
Inventors:
Jayaraman Chandrasekhar, Alan P. Kozikowski, Jianhua Liu, Werner Tueckmantel, Joel R. Walker, Po-wai Yuen