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: 8552003Abstract: The present invention is directed to a compound of the formula: or pharmaceutically acceptable salts thereof and use of such compounds for treating proliferative diseases such as cancer, in mammals.Type: GrantFiled: July 31, 2007Date of Patent: October 8, 2013Assignee: Novartis AGInventors: Mark G. Charest, Christine Hiu-Tung Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Ly Luu Pham, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming David Wang, Fan Yang, Leigh Zawel
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Publication number: 20130261156Abstract: The present invention provides a pharmaceutical composition or a solid preparation containing a stabilized pharmaceutically active ingredient and a stabilizing method thereof. According to the present invention, a pharmaceutical composition can be stabilized by containing a nonpeptidic pharmaceutically active ingredient having a primary or secondary amino group, an excipient and an acidic compound. In addition, a solid preparation containing a pharmaceutically active ingredient, titanium oxide, a plasticizer and a chain organic acid can enhance the stability of the pharmaceutically active ingredient during light irradiation.Type: ApplicationFiled: May 29, 2013Publication date: October 3, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Hiraishi, Muneo Nonomura
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Publication number: 20130261100Abstract: 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-memberType: ApplicationFiled: December 10, 2010Publication date: October 3, 2013Inventors: Manuela Borriello, Lucio Rovati, Luigi Piero Stasi, Benedetta Buzzi, Fabrizio Colace
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Patent number: 8546374Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.Type: GrantFiled: July 9, 2012Date of Patent: October 1, 2013Assignee: Abbvie Inc.Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
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Patent number: 8545870Abstract: The invention concerns a medicinal tablet to be sucked made with boiled sugar of solid consistency designed to dissolve in the buccal cavity, comprising at least an active principle. The invention is characterized in that it further comprises at least a matrix agent for slowing down the release of the active principle(s) which therefore remain in prolonged contact with the region of the mouth and the pharynx, the dissolving time in the buccal cavity being at least 15 minutes.Type: GrantFiled: April 25, 2002Date of Patent: October 1, 2013Assignee: Pierre Fabre MedicamentInventors: Pierre Dupinay, Robert Torres, Christine Capon
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20130253013Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 22, 2013Publication date: September 26, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
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Patent number: 8536205Abstract: 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: GrantFiled: May 25, 2006Date of Patent: September 17, 2013Assignee: Switch Materials Inc.Inventors: Neil R. Branda, Bettina Wuestenberg, Vincent Lemieux, Michael Adams, Simon Gauthier
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Publication number: 20130237570Abstract: This invention relates to a liquid pharmaceutical formulation for delivering nicotine to a subject. This invention also relates to a method and a system for delivering nicotine as well as manufacturing and use of said liquid pharmaceutical formulation.Type: ApplicationFiled: April 26, 2013Publication date: September 12, 2013Applicant: McNeil ABInventors: Katarina E.A. Lindell, Anette K. Schluter, Gunner A. Bergengren, Bengt A. Bosson
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Publication number: 20130237514Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.Type: ApplicationFiled: October 5, 2012Publication date: September 12, 2013Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
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Patent number: 8529914Abstract: A bioactive dose for delivering a bioactive agent to a mammal, includes a solid bioactive dosage unit containing at least one bioactive agent and a rapid release coating provided on at least one outer surface of the solid bioactive dosage unit, the rapid release coating containing a material having a property of rapidly modulating a pH of bodily fluids in which the material comes in contact in a direction towards an ideal absorptive pH or towards an ideal pH to hinder absorption of the at least one bioactive agent given the pKa that least at one bioactive agent.Type: GrantFiled: September 2, 2010Date of Patent: September 10, 2013Inventors: Richard C. Fuisz, Joseph M. Fuisz
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Publication number: 20130231373Abstract: The present teachings relate to compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula (I) and methods of use compounds of Formula (I) in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: September 5, 2013Applicant: Novartis AGInventors: Clinton Alan Brooks, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Gang Liu, Michael David Schultz
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Publication number: 20130231334Abstract: The invention relates to a method of controlling aphids that are resistant to neonicotinoid insecticides, using a trifluoromethylpyri(mi)dine derivative in free form or in agrochemically acceptable salt form as well as the use of compositions comprising said compound to control neonicontinoid resistant insects. In particular the methods relate to controlling neonicotinoid resistant insects in the Aphididae family, that are resistant to one or more neonicotinoid insecticides. Methods of the invention find particular use in controlling neonicotinoid resistant insects in crops of useful plants. Furthermore, the invention extends to methods of controlling plant viruses spread by neonicotinoid resistant insects.Type: ApplicationFiled: April 18, 2011Publication date: September 5, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Russell Slater, Peter Maienfisch, Patrik Hoegger, Alfred Rindlisbacher
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Patent number: 8524710Abstract: The invention relates to a compound of formula (I) wherein A1 to A4 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used, for example, as inhibitors of the cysteine protease cathepsin.Type: GrantFiled: October 24, 2011Date of Patent: September 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
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Publication number: 20130224114Abstract: 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.Type: ApplicationFiled: March 25, 2013Publication date: August 29, 2013Applicant: The University of SydneyInventor: The University of Sydney
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Publication number: 20130225412Abstract: The various embodiments herein provide a nano silicon carrier as a drug delivery mechanism. The nano silicon carrier comprises a diatom frustules loaded with a drug molecule to be released at the target site. The diatom frustules are of Hannaea arcus and Navicula inflexa species of diatom. The pore size of the diatom frustules is 1 to 100 nm. The diatom frustules are comb-like in structure. The diatom frustules are in the form of powdered diatomaceous earth. The drug delivery mechanism described in the embodiments herein is a controlled release mechanism. The nano silicon carrier described in the embodiments herein is also used for delivery of pesticides and herbicides in plants. The nano silicon carrier described in the embodiments herein is also used in hormone waste water treatment.Type: ApplicationFiled: February 28, 2012Publication date: August 29, 2013Inventors: Soroush Sardari Lodriche, Saeed Soltani, Roghieh Mirzazadeh
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Patent number: 8518943Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: August 27, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Patent number: 8518976Abstract: The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.Type: GrantFiled: December 18, 2007Date of Patent: August 27, 2013Assignee: SanofiInventors: Harmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
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Patent number: 8518948Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: GrantFiled: March 10, 2011Date of Patent: August 27, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20130217686Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.Type: ApplicationFiled: September 28, 2011Publication date: August 22, 2013Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Sung Jin Bae, Han Ju Yi, Sun Gwan Hwang, Mo Ses Jeong, Yeo Jin Yoon, Sang Mi Chae, Joo Young Park, Eun Ju Ryu
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Publication number: 20130217714Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.Type: ApplicationFiled: December 14, 2012Publication date: August 22, 2013Applicant: Trustees of Tufts CollegeInventor: Trustees of Tufts College
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Patent number: 8513161Abstract: Treatment with N-(2-phenylethyl)succinamic acid or its salts protects against inhibition of growth by a neonicotinoid compound applied as a seed treatment or applied directly on or near the root zone of the seedling.Type: GrantFiled: December 20, 2011Date of Patent: August 20, 2013Assignees: Valent Biosciences Corporation, Valent U.S.A. CorporationInventors: Franklin Paul Silverman, Dale O. Wilson, Jr., Jennifer C. Kochan, Nicole Higgs, Peter D. Petracek, Prem Warrior, Karen S. Arthur
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Patent number: 8513288Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.Type: GrantFiled: August 2, 2011Date of Patent: August 20, 2013Assignees: Allergan, Inc., ExonHit Therapeutics SAInventors: Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
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Patent number: 8513286Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: February 20, 2008Date of Patent: August 20, 2013Assignee: Syngenta Crop Protection LLCInventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
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Patent number: 8513274Abstract: The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I: In Formula I, R1 is H, C1-6 alkyl, or C1-6 alkyl-aryl. Each of R2 and R4 of Formula I are independently H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkoxy, —OR2a, —SR2a, —C(O)R2a, —C(O)OR2a, —C(O)NR2aR2b, —NR2aR2b, C1-6 alkyl-NR2aR2b, —N(R2a)C(O)R2b, —N(R2a)C(O)OR2b, —N(R2a)C(O)NR2aR2b, —OP(O)(OR2a)2, —S(O)2OR2a, —S(O)2NR2aR2b, —CN, —NO2, cycloalkyl, heterocycloalkyl, aryl or heteroaryl. Each of R2a and R2b of Formula I are independently H, C1-6 alkyl, C1-10 heteroalkyl or C1-6 alkyl-aryl. R3 of Formula I is absent, C1-6 alkyl or N-oxide. The compounds include the salts, hydrates and isomers thereof. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.Type: GrantFiled: March 15, 2010Date of Patent: August 20, 2013Assignee: Etzem, Inc.Inventors: Debra Ellies, William Rosenberg
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Publication number: 20130209540Abstract: The invention provides a multi-layered pharmaceutical composition comprising two or more formulations with varying properties. In some embodiments, the pharmaceutical compositions provide combinations of different organoleptic properties within the same product. In certain embodiment, these combinations allow for a modified release profile of active ingredients as the user enjoys the pharmaceutical composition. The invention further provides methods for making and using the pharmaceutical composition.Type: ApplicationFiled: February 10, 2012Publication date: August 15, 2013Inventors: Donna Walker Duggins, John-Paul Mua, Darrell Eugene Holton, JR., Daniel Verdin Cantrell
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Publication number: 20130210795Abstract: The present application relates to novel substituted dicyanopyridines, 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 prophylaxis of cardiovascular disorders.Type: ApplicationFiled: June 27, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexandros Vakalopoulos, Daniel Meibom, Peter Nell, Frank Sussmeier, Barbara Albrecht-Kupper, Katja Zimmermann, Joerg Keldenich, Dirk Schneider, Ursula Krenz
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Patent number: 8507493Abstract: 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: GrantFiled: April 20, 2010Date of Patent: August 13, 2013Assignee: AbbVie Inc.Inventors: Sridhar Peddi, Meena V. Patel, Jeffrey J. Rohde
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Patent number: 8506936Abstract: A nicotine chewing gum composition with improved stability.Type: GrantFiled: November 25, 2008Date of Patent: August 13, 2013Assignee: Watson Laboratories, Inc.Inventors: W. Crawford Hite, Malini Batheja, Mohsen Sadatrezaei
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Patent number: 8507535Abstract: The invention relates to a compound of formula wherein A is defined herein or to pharmaceutically active salts, stereoisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula I as well as racemic and non-racemic mixtures thereof. The present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: June 29, 2011Date of Patent: August 13, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Publication number: 20130203701Abstract: The invention provides pharmaceutical compositions containing omega-3 oil and a non-hydrophilic co-solvent that have an increased absorption rate. The pharmaceutical compositions may further contain one or more pharmaceutical organic molecules. The invention further provides kits containing these pharmaceutical compositions, methods for formulating pharmaceutical compositions containing omega-3 oil, and methods for decreasing the likelihood of developing cardiovascular disease, decreasing triglyceride or LDL cholesterol levels, decreasing pain or inflammation, treating diabetes, chronic pulmonary diseases, or irritable bowel syndrome, decreasing symptoms of an autoimmune disease or allergic conditions.Type: ApplicationFiled: September 15, 2011Publication date: August 8, 2013Applicant: Maine Natural Health, Inc.Inventor: Harry J. Leighton
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Publication number: 20130202673Abstract: The present invention comprises compositions, methods and kits for delivering drugs. The invention provides an implantable device for delivery of a pharmaceutical substance to a patient, comprising a core comprising a core polymeric material optionally containing a core pharmaceutical substance, surrounded by a first layer comprising a first-layer pharmaceutical substance and a first-layer polymeric material, optionally surrounded by one or more additional layers comprising an additional pharmaceutical substance and an additional polymeric material, where the core, first, and optional additional polymeric materials may be the same or different, and where the optional core pharmaceutical substance, first-layer pharmaceutical substance, and optional additional pharmaceutical substances are the same or different. Implantation of the device allows a controlled release of drug for an extended period of time. The device may be implanted subcutaneously in an individual in need of continuous treatment with a drug.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: Titan Pharmaceuticals, Inc.Inventor: Titan Pharmaceuticals, Inc.
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Patent number: 8501787Abstract: This invention is directed to compounds of structure (I). Particularly this invention is directed to compounds of structure (VIII) wherein the variables are defined as in the description. These compounds are integrin inhibitors and are useful in the treatment of diseases in which an inhibition of angiogenesis is desired.Type: GrantFiled: March 24, 2005Date of Patent: August 6, 2013Assignee: Shire Orphan Therapies GmbHInventors: Grit Zahn, Roland Stragies, Frank Osterkamp, Gunther Zischinsky, Jochen Knolle, Gerd Hummel, Sascha Birkner, Ulrich Reineke
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Publication number: 20130197023Abstract: A method of ameliorating an endoplasmic reticulum (ER) stress response and/or unfolded protein response (UPR) in cells expressing nicotinic acetylcholine receptors (nAChRs) comprises contacting a cell expressing nAChRs with an effective amount of a ligand for nAChRs. The contacting results in attenuating endogenously expressed ATF6 translocation, expression of XBP1, phosphorylation of eukaryotic initiation factor 2? (peIF2?), increased numbers of ER exit sites, increased trafficking of known associated proteins as well as other proteins such as growth factors and their receptors, changes in abundance of selected mRNA species, and phosphorylation, abundance, or subcellular compartmentalization of other proteins involved with ER stress and/or the UPR, and inhibiting upregulation of CCAAT/Enhancer-Binding Protein Homologous Protein (CHOP) levels in the cells.Type: ApplicationFiled: January 28, 2013Publication date: August 1, 2013Applicant: California Institute of TechnologyInventors: Henry A. Lester, Rahul Srinivasan, Christopher I. Richards, Brandon J. Henderson
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Patent number: 8497273Abstract: 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: GrantFiled: April 18, 2007Date of Patent: July 30, 2013Assignee: Abbott GmbH & Co. KGInventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger
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Patent number: 8492379Abstract: 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.Type: GrantFiled: December 2, 2008Date of Patent: July 23, 2013Assignee: The University of SydneyInventors: Michael Kassiou, Michelle Louise James, Christopher Andrew Luus
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Publication number: 20130184313Abstract: 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: ApplicationFiled: March 7, 2013Publication date: July 18, 2013Applicants: 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
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Publication number: 20130183278Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD as opposed to another neurodegenerative disease. The method of the invention comprises measuring the concentration of ?-synuclein (?-syn) and the concentration of unphosphorylated tau (tau) and/or phosphorylated tau (p-tau) in a cerebrospinal fluid sample taken from an individual. The method also comprises calculating the ratio of the concentration of tau and/or p-tau to the concentration of ?-syn, and thereby determining whether or not the individual has PD.Type: ApplicationFiled: July 6, 2011Publication date: July 18, 2013Applicant: United Arab Emirates UniversityInventors: Omar El-Agnaf, Lucilla Parnetti, Paolo Calabresi
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Publication number: 20130178456Abstract: 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: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130178502Abstract: The present invention relates to novel pyridine compounds of the formulae I and II, to their salts, to their tautomers, to their N-oxides, and to the salts of these N-oxides or tautomers. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The invention further relates to plant propagation material and to agricultural compositions comprising said compounds. wherein A is a radical of the formulae A1 or A2 # denotes the binding site to the remainder of formulae I or II; n is 0, 1, 2 or 3; Z is O, S or N—RN; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and RA and RN, are as defined in claim 1.Type: ApplicationFiled: September 12, 2011Publication date: July 11, 2013Applicant: BASF SEInventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
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Publication number: 20130178463Abstract: A buccal delivery system is disclosed suitable for delivery of a therapeutic agent to the oral cavity of a patient. The delivery system comprises a matrix for containing and releasing the therapeutic agent into the oral cavity and an alkyl N,N-disubstituted amino acetate in said matrix. A particularly preferred delivery system comprises a matrix containing an effective amount of therapeutic agent together with an alkyl N,N-disubstituted amino acetate, such as dodecyl 2-(N,N-dimethylamino) propionate salt.Type: ApplicationFiled: September 23, 2011Publication date: July 11, 2013Applicants: Rutgers, The State University of New Jersey, Nexmed Holdings, Inc.Inventors: Bassam B. Damaj, Richard Martin, Bozena Michniak-Kohn, Long-Sheng Hu
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Publication number: 20130177646Abstract: Solid pharmaceutical dosage form for the release of nicotine in the oral cavity comprising a core encapsulated by at least one film coating, wherein the core comprises nicotine and wherein the film coating comprises at least one film-forming polymer and at least one component for reduction of one or more organoleptically disturbing sensations, and where the at least one film coating is devoid of nicotine and devoid of buffer.Type: ApplicationFiled: January 23, 2012Publication date: July 11, 2013Applicant: McNeil ABInventors: Andreas Hugerth, Katarina Lindell, Fredrik Nicklasson, Kristina Thyresson
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Publication number: 20130178501Abstract: The present invention features a process for making a lozenge product including the steps of forming a powder blend containing an amorphous carbohydrate polymer into the desired shape of the lozenge product and applying radiofrequency energy to the shape for a sufficient period of time to soften or melt said amorphous carbohydrate polymer to fuse the shape into said lozenge product.Type: ApplicationFiled: December 18, 2012Publication date: July 11, 2013Applicant: McNEIL-PPC, Inc.Inventor: McNEIL-PPC, Inc.
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Publication number: 20130172321Abstract: The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).Type: ApplicationFiled: August 24, 2012Publication date: July 4, 2013Inventor: Eliahu Heldman
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Publication number: 20130172310Abstract: 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: ApplicationFiled: September 12, 2012Publication date: July 4, 2013Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 8476269Abstract: 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: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Patent number: 8476304Abstract: The present invention relates to methods and compositions of metadoxine and physiologically compatible active derivatives thereof, and their use for decreasing symptoms of alcohol consumption as well as in the prevention of alcohol consumption related symptoms in subjects in need thereof.Type: GrantFiled: July 3, 2012Date of Patent: July 2, 2013Assignee: Alcobra Ltd.Inventors: Gur Megiddo, Dalia Megiddo, Rina Yamin, Yaron Ilan, Shimon Amselem
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Patent number: 8476303Abstract: The compounds herein disclosed are N-aminopyrrolylmethyltetrahydropyridine analogs that have modifications on the phenyl rings by introducing groups with various electronic properties. These derivatives of N-aminopyrrolylmethyltetrahydropyridines have been shown to have anti-proliferative activity against cells. In particular, the compounds have been found to be effective in inhibiting the proliferation of cancer cells, such as cancer cells that originated in breast tissue. Additionally, it has been shown that the novel compounds have IC50 values against the breast cancer cells that are 6-10-fold less than the IC50 of tamoxifen.Type: GrantFiled: November 30, 2011Date of Patent: July 2, 2013Assignee: Florida A&M University Board of TrusteesInventors: Kinfe Ken Redda, Madhavi Gangapuram
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Publication number: 20130165483Abstract: This invention provides compounds of formula IB: wherein HY, R1, R2, R3, R15, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Millennium Pharmaceuticals, Inc.
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Publication number: 20130165464Abstract: This invention provides compounds of formula IB: and also provides compounds of formulas ID, IIB, VB, and IIC: wherein HY, R1, R2, G5, G6, G7, G8, and G9 are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: MILLENNIUM PHARMACEUTICALS, INC.