The Additional Hetero Ring Consists Of One Nitrogen And Four Carbons (e.g., Nicotine, Etc.) Patents (Class 514/343)
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Patent number: 8759377Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: November 23, 2010Date of Patent: June 24, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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Publication number: 20140171316Abstract: The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.Type: ApplicationFiled: August 10, 2012Publication date: June 19, 2014Applicant: BASF SEInventors: Prashant Deshmukh, Karsten Körber, Florian Kaiser, Markus Kordes, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
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Publication number: 20140155391Abstract: 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.Type: ApplicationFiled: December 5, 2013Publication date: June 5, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Oriana Esposito, Laura Carzaniga, Carmelida Capaldi
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Publication number: 20140155377Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20140154301Abstract: A method is provided of making a medicinal delivery system which satiates a craving in an individual when the medicinal delivery system is administered orally to the individual. A coating composition is applied on a saliva-soluble powder to establish a coated powder, the coating composition featuring an at least partially solubilized craving satiation medicinal compound. The coated powder is combined with an edible carrier base to establish a medicinal delivery system that rapidly releases medicine and buffer preferably followed by slower, sustained release.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: JSRNTI, LLCInventors: Tommy L. CHAU, John M. PINNEY, Jack E. HENNINGFIELD, Edward J. CONE, Saul M. SHIFFMAN, Joseph G. GITCHELL
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Patent number: 8742119Abstract: 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: GrantFiled: October 6, 2011Date of Patent: June 3, 2014Assignee: Agios Pharmaceuticals, Inc.Inventors: Francesco G. Salituro, Jeffrey O. Saunders
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Patent number: 8741935Abstract: A nicotine delivery product comprising the reaction product of a nicotine/cation exchange resin complex and an organic polyol; and a method for preparing it comprising (a) mixing an aqueous suspension of a nicotine/cation exchange resin complex with an organic polyol or an aqueous solution thereof, and (b) removing water from the mixture to produce said nicotine delivery product. The nicotine delivery product has a nicotine release rate of at least 80% over a 10 minute period. It is particularly suited for use in smoking substitution devices delivering nicotine such as chewing gum, patches, lozenges, melting tablets and tablets for chewing.Type: GrantFiled: December 2, 2004Date of Patent: June 3, 2014Assignee: Fertin Pharma A/SInventor: Carsten Andersen
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Patent number: 8735432Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.Type: GrantFiled: October 23, 2012Date of Patent: May 27, 2014Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20140142074Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
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Publication number: 20140142082Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: PHENEX PHARMACEUTICALS AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Patent number: 8728443Abstract: A method of producing a nicotine delivery product includes a mixture having nicotine, a cation exchange resin and water. The water content of the mixture is between 5 and 75 wt. % relative to the whole mixture. The mixture is combined with further components of the nicotine delivery product.Type: GrantFiled: May 31, 2010Date of Patent: May 20, 2014Assignee: Fertin Pharma A/SInventor: Carsten Andersen
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Patent number: 8728507Abstract: Use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for the non-systemic control of parasitic insects, such as fleas, lice and flies, on humans and on animals.Type: GrantFiled: October 31, 2007Date of Patent: May 20, 2014Assignee: Bayer Intellectual Property GmbHInventors: Hubert Dorn, Terence Hopkins
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Patent number: 8729063Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: December 20, 2012Date of Patent: May 20, 2014Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taishing Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8729129Abstract: Disclosed is a method of reducing bleed time in a subject by activation of the cholinergic anti-inflammatory pathway in said subject. The cholinergic anti-inflammatory pathway can be activated by direct or indirect stimulation of the vagus nerve. The cholinergic anti-inflammatory pathway can also be activated by administering an effective amount of cholinergic agonist or acetylcholinesterase inhibitor to the subject.Type: GrantFiled: March 24, 2005Date of Patent: May 20, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Kevin J. Tracey, Carol Ann Amella, Christopher Czura
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Publication number: 20140135320Abstract: 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: ApplicationFiled: November 8, 2013Publication date: May 15, 2014Applicant: Jacobus Pharmaceutical Company, Inc.Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Publication number: 20140135329Abstract: 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: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Publication number: 20140128436Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: November 8, 2013Publication date: May 8, 2014Applicant: ActiveSite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20140121213Abstract: 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: ApplicationFiled: July 3, 2012Publication date: May 1, 2014Inventors: Jeffrey Charles Boehm, Roderick S. Davis, Jeffrey Kerns, Guoliang Lin, Robert D. Murdoch, Hong NIE
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Publication number: 20140113938Abstract: 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: ApplicationFiled: January 2, 2014Publication date: April 24, 2014Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Patent number: 8703801Abstract: New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.Type: GrantFiled: December 7, 2010Date of Patent: April 22, 2014Assignee: University of Georgia Research Foundation, Inc.Inventors: Vasu Nair, Maurice O. Okello, Abdumalik A. Nishonov, Sanjaykumar Mishra
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Patent number: 8703721Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 12, 2011Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140107158Abstract: Disclosed herein are methods of treating a patient suffering a cognitive disorder.Type: ApplicationFiled: December 18, 2013Publication date: April 17, 2014Applicant: ALLERGAN, INC.Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Publication number: 20140107164Abstract: 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: ApplicationFiled: December 17, 2013Publication date: April 17, 2014Applicant: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Arielle Genevois-Borella, Marc Capet, Michel Cheve, Craig Harrison Miller
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Publication number: 20140107163Abstract: 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: ApplicationFiled: December 16, 2013Publication date: April 17, 2014Applicant: Targecept, Inc.Inventors: Srinvasa Rao Akireddy, Scott R. Breining, Timothy J. Cuthbertson, Gary Maurice Dull, Gregory J. Gatto, John Genus, Phillip S. Hammond, Joseph Pike Mitchener, JR., Julio A. Munoz, Pieter Albert Otten, Daniel Yohannes, Nikolai Fedorov
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Patent number: 8697722Abstract: The disclosure provides compounds capable of selectively or non-selectively modulating nicotinic acetylcholine receptors. The compounds, compositions, and methods described herein are useful, for example, in treating patients suffering from various medical conditions including pain, chemical addictions, Parkinson's disease, Alzheimer's disease, and neurodegenerative disorders. In one embodiment, the compounds comprise a 7- to 11-membered azabicyclo ring.Type: GrantFiled: November 2, 2007Date of Patent: April 15, 2014Assignee: SRI InternationalInventors: Faming Jiang, Taline Khroyan, Cris M. Olsen, Willma E. Polgar, Lawrence R. Toll, Nurulain T. Zaveri
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Publication number: 20140100212Abstract: 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.Type: ApplicationFiled: October 15, 2013Publication date: April 10, 2014Applicant: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu
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Publication number: 20140100211Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140099333Abstract: The present invention relates to pyrrolidinone derivatives. The pyrrolidinone derivatives are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The invention furthermore relates to the use of pyrrolidinone derivatives as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: October 8, 2013Publication date: April 10, 2014Applicant: SANOFIInventors: Lothar SCHWINK, Martin BOSSART, Heiner GLOMBIK, Matthias GOSSEL, Dieter KADEREIT, Thomas KLABUNDE, Thomas MAIER, Siegfried STENGELIN
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Patent number: 8691847Abstract: 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: GrantFiled: September 12, 2012Date of Patent: April 8, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song
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Publication number: 20140093513Abstract: 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: ApplicationFiled: May 24, 2013Publication date: April 3, 2014Applicant: Catabasis Pharmaceuticals, Inc.Inventors: Jill C. Milne, Michael R. Jirousek, Chi B. Vu
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Patent number: 8685992Abstract: The present invention refers to compounds derived from trisubstituted 1H-pyrrole rings and aromatic rings, which have the following formula (I): wherein: R1 and R2 represent, independently, an optionally substituted C6-C10 aryl radical or an optionally substituted heteroaryl radical; A and M represent, independently, a methylene group or a single bond, in which case the adjacent aromatic ring would be attached directly to the amide group; the Y?Z group represents together and indistinctly an oxygen atom, a sulfur atom, a cis-vinylidene group, an imino group, or a methine group with a sp2-hybridized carbon atom; X represents indistinctly a methine group, a cis-vinylidene group or a nitrogen atom; and W represents a hydroxyl group, an optionally substituted C1-C6 alkyl group, an optionally substituted heteroaryl group or an optionally substituted C6-C10 aryl group; or a salt, solvate or prodrug thereof, as well as to the process for their preparation and the use thereof for the treatment of cancer.Type: GrantFiled: October 1, 2010Date of Patent: April 1, 2014Assignees: Universidad del País Vasco, Ikerschem, S.L.Inventors: Fernando Pedro Cossío Mora, Aizpea Zubia Olascoaga, Yosu Vara Salazar, Eider Ion San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo
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Publication number: 20140088156Abstract: The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions.Type: ApplicationFiled: February 14, 2012Publication date: March 27, 2014Applicant: The Regents of the University of CaliforniaInventors: Bruce D. Hammock, Sung Hee Hwang, Aaron T. Wecksler, Christophe Morisseau
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Publication number: 20140088155Abstract: The present invention relates to a method of treating psychiatric symptoms in a subject having a NMDA receptor and a NE receptor which includes administering d-methadone, d-methadol, d-alpha-acetylmethadol, l-alpha-acetylmethadol, d-alpha-normethadol, l-alpha-normethadol, pharmaceutically acceptable salts thereof, or mixtures thereof, to the subject under conditions effective for the substance to bind to the NMDA receptor and NE receptor of the subject.Type: ApplicationFiled: March 14, 2013Publication date: March 27, 2014Inventors: Paolo L. Manfredi, Charles E. Inturrisi
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Publication number: 20140088148Abstract: Small molecule inhibitors of XBP1 splicing by IRE1 are provided, as well as methods for their use in treating or preventing cancer (e.g., endocrine resistant breast cancer), diabetes, and obesity.Type: ApplicationFiled: April 4, 2012Publication date: March 27, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Sivanesan Dakshanamurthy, Milton L. Brown, Robert Clarke, Ayesha N. Shahjahan, Jaqueline Smith
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Patent number: 8680122Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.Type: GrantFiled: October 30, 2006Date of Patent: March 25, 2014Assignee: Janssen Pharmacetica N.V.Inventors: Maud Urbanski, Amy Xiang, Roxanne Zeck
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Publication number: 20140080770Abstract: An arylalkylamine compound is represented by the following formula [I-e] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 17, 2013Publication date: March 20, 2014Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi MIYAZAKI, Junko OKABE, Kosuke YASUDA, Iwao TAKAMURO, Osamu SAKURAI, Tetsuya YANAGIDA, Yutaka HISADA
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Publication number: 20140066421Abstract: 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: ApplicationFiled: May 17, 2012Publication date: March 6, 2014Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. McHardy, Richard M. Corbett, Donald M. Maxwell, Michael W. Tidwell, Bismarck Campos, Christopher J. Bemben
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Publication number: 20140066420Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 16, 2013Publication date: March 6, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
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Patent number: 8663659Abstract: The invention relates to oral disintegrable films, which are mucoadhesive, which completely disintegrate in the mouth of a consumer within 1 to 10 minutes, and which include an alkaline substance and optionally a pharmaceutically active substance.Type: GrantFiled: March 6, 2008Date of Patent: March 4, 2014Assignee: Novartis AGInventors: Stephan Meyer, Greg Slominski, Christopher Edward Fankhauser
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Publication number: 20140057920Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057882Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and the treatment of certain conditions such as COPD.Type: ApplicationFiled: October 8, 2013Publication date: February 27, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, GABRIELE AMARI, LAURA CARZANIGA, CARMELIDA CAPALDI, ORIANA ESPOSITO, GINO VILLETTI, RENATO DE FANTI
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Publication number: 20140057916Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057892Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD) heart failure, ischemia, and anemia.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Patent number: 8658685Abstract: We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma.Type: GrantFiled: January 30, 2009Date of Patent: February 25, 2014Assignees: Activesite Pharmaceuticals, Inc., Joslin Diabetes CenterInventors: Lloyd P. Aiello, Tamie Jo Chilcote, Sukanto Sinha, Edward P. Feener
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Publication number: 20140051686Abstract: The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: July 11, 2013Publication date: February 20, 2014Inventors: Ulrich Abel, Holger Deppe, Achim Feurer, Ulrich Grädler, Kerstin Otte, Renate Sekul, Meinolf Thiemann, Andreas Goutopoulos, Matthias Schwarz, Xuliang Jiang
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Publication number: 20140050663Abstract: 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: ApplicationFiled: February 6, 2013Publication date: February 20, 2014Applicant: The Regents of the University of CaliforniaInventors: Jogeshwar Mukherjee, Sharon A. Kuruvilla
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Patent number: 8653000Abstract: 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: GrantFiled: September 30, 2011Date of Patent: February 18, 2014Assignee: BASF SEInventors: 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
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Publication number: 20140045801Abstract: The present invention relates to a method for the treatment and prevention of cluster headaches and migraines using the transdermal administration of pramipexole.Type: ApplicationFiled: August 9, 2012Publication date: February 13, 2014Applicant: MYLAN INC.Inventor: David Thomas Rossi
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Publication number: 20140045896Abstract: The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.Type: ApplicationFiled: May 2, 2012Publication date: February 13, 2014Applicant: XUANZHU PHARMA CO., LTD.Inventors: Hui Zhang, Mingwei Fan, Liang Sun