The Additional Hetero Ring Consists Of One Nitrogen And Four Carbons (e.g., Nicotine, Etc.) Patents (Class 514/343)
  • Patent number: 8614234
    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.
    Type: Grant
    Filed: September 3, 2010
    Date of Patent: December 24, 2013
    Assignee: Allergan, Inc.
    Inventors: Xialing Guo, Zhen Zhu
  • Publication number: 20130338197
    Abstract: There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: wherein A1 is C—X3 or nitrogen atom, etc., A2 and A3 are C—H, etc., A4 is C—H or nitrogen atom, etc., G is G-2a, etc., W is oxygen atom or sulfur atom, X1 is halogen atom, trifluoromethyl, etc., X2 is hydrogen atom, halogen atom, trifluoromethyl, etc., X3 is hydrogen atom, halogen atom, etc., Y1 is hydrogen atom, halogen atom, methyl, etc., R1 is trifluoromethyl, etc., R2 is E-3a, etc., R3 is hydrogen atom, etc., p is an integer of 0 to 2.
    Type: Application
    Filed: November 18, 2011
    Publication date: December 19, 2013
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takeshi Mita, Yukihiro Maizuru, Ken-ichi Toyama, Motoyoshi Iwasa, Hotaka Imanaka, Hiroto Matsui
  • Publication number: 20130338105
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: August 20, 2013
    Publication date: December 19, 2013
    Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
  • Publication number: 20130338146
    Abstract: Multifunctional nitroxide derivatives comprising a potassium channel opener and a reactive oxygen species (ROS) degradation catalyst that can act as an anti-oxidant, as well as pharmaceutical compositions comprising them are provided. The multifunctional compounds and pharmaceutical compositions are useful for treatment of diseases, disorders or conditions associated with oxidative stress or endothelial dysfunction.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 19, 2013
    Applicant: RADIKAL THERAPEUTICS INC.
    Inventors: Prakash Jagtap, Andrew Lurie Salzman
  • Publication number: 20130338154
    Abstract: Pyrrole compounds 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.
    Type: Application
    Filed: October 22, 2010
    Publication date: December 19, 2013
    Applicant: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender
  • Publication number: 20130338143
    Abstract: Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety.
    Type: Application
    Filed: November 15, 2011
    Publication date: December 19, 2013
    Applicant: Neuroderm, Ltd.
    Inventors: Oron Yacoby-Zeevi, Mara Nemas, Eduardo Zawozink
  • Patent number: 8609700
    Abstract: 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: Grant
    Filed: September 12, 2011
    Date of Patent: December 17, 2013
    Assignee: BASF SE
    Inventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
  • Publication number: 20130331372
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
    Type: Application
    Filed: October 25, 2011
    Publication date: December 12, 2013
    Inventors: Zhijian Lu, Yi-Heng Chen, Cameron Smith, Hong Li, Christopher F. Thompson, Julianne Hunt, Florida Kallashi, Ramzi Sweis, Peter Sinclair, Samantha E. Adamson, Guizhen Dong, Debra L. Ondeyka, Xiaoxia Qian, Wanying Sun, Petr Vachal, Kake Zhao
  • Patent number: 8603440
    Abstract: A compressed chewing gum tablet includes one or more pharmaceutically active ingredients and one or more enhancers, wherein the chewing gum tablet includes at least one chewing gum module including a chewing gum composition, and wherein the chewing gum composition includes chewing gum granules containing gum base, and wherein the enhancers are at least partly contained within at least a part of the chewing gum granules.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: December 10, 2013
    Assignee: Fertin Pharma A/S
    Inventors: Carsten Andersen, Gitte Lorenzen, Nicolai Arent, Bitten Thorengaard, Helle Wittorff
  • Patent number: 8604038
    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
  • Publication number: 20130324503
    Abstract: The present invention relates to methods of treatment for Parkinson Disease (PD) in a person by identifying gene variants which may indicate a more favorable response to specific medicaments, thereby allowing for personalized or individualized treatment. The present invention relates to a method of screening for a genetic predisposition to PD in a person. The present invention is also directed to a method of testing a person for the presence of particular gene variants, wherein the presence of a gene variant indicates a higher predisposition to PD, and the absence of a gene variant indicates a lower predisposition to PD, compared to a control sample. The present invention further relates to methods and kits for treating, or inhibiting the development of, PD in a person. The present invention is also directed to a method of identifying the heritage of an individual based on the genetic profile of the individual.
    Type: Application
    Filed: October 19, 2012
    Publication date: December 5, 2013
    Applicants: Health Research Inc., Emory University School of Medicine, National Institute of Environmental Health Sciences, Veterans Affairs Puget Sound Health Care System, Oregon Health & Science University
    Inventors: Haydeh Payami, Taye H. Hamza, Stewart A. Factor, John Nutt, Cyrus Zabetian, Honglei Chen, Erin Hill Burns
  • Publication number: 20130324501
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: June 4, 2013
    Publication date: December 5, 2013
    Inventors: Elisabetta ARMANI, Carmelida Capaldi, Laura Carzaniga, Oriana Esposito
  • Patent number: 8598168
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: December 3, 2013
    Assignee: MethylGene Inc.
    Inventors: Oscar Moradei, Isabelle Paquin, Sylvie Frechette, Tammy Mallais, Simon Roy, Roger Machaalani, Arkadii Vaisburg, Jeffrey M Besterman, Pierre Tessier, David Smil, Silvana Leit, Robert Déziel
  • Publication number: 20130317027
    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
  • Publication number: 20130310377
    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.
    Type: Application
    Filed: December 20, 2012
    Publication date: November 21, 2013
    Applicant: Rhizen Phamaceuticals SA
    Inventor: Rhizen Phamaceuticals SA
  • Publication number: 20130310378
    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.
  • Publication number: 20130310408
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 21, 2013
    Applicant: Bayer Intellectual Property GmbH
    Inventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
  • Publication number: 20130303525
    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
  • Publication number: 20130296274
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: September 14, 2011
    Publication date: November 7, 2013
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Patent number: 8575197
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: November 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
  • Publication number: 20130289079
    Abstract: The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form.
    Type: Application
    Filed: June 26, 2013
    Publication date: October 31, 2013
    Inventor: Li-Lan CHEN
  • Publication number: 20130289019
    Abstract: One embodiment of an aspect of the present invention is a method for lessening the symptoms of depression, anxiety, and post-traumatic stress disorder comprising the step of administering a therapeutically effective quantity of a cholinergic M1 receptor antagonist and a therapeutically effective quantity of one or more cholinomimetic agents to lessen the symptoms of depression, anxiety, and post-traumatic stress disorder. Typically, the cholinergic M1 receptor antagonist is selected from the group consisting of telenzepine, amytriptyline, biperiden, trihexyphenidyl, darifenacin, dicyclomine, and tiotropium. Another aspect of the present invention is directed to methods and compositions employing other therapeutic agents and combinations of therapeutic agents for emulating the theoretical pharmacological effects of the non-selective mAChR antagonist scopolamine. The invention also encompasses pharmaceutical compositions incorporating one or more therapeutic agents and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: April 25, 2013
    Publication date: October 31, 2013
    Applicant: Amazing Grace, Inc.
    Inventor: David T. Chau
  • Publication number: 20130289007
    Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 31, 2013
    Applicant: PTC Therapeutics Inc.
    Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
  • Publication number: 20130281387
    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
  • Publication number: 20130281443
    Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Applicant: THE SCRIPPS RESEARCH INSTITUTE
    Inventors: Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
  • Patent number: 8563736
    Abstract: A compound represented by Formula (1): The compound can be used as insecticides.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: October 22, 2013
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
  • Publication number: 20130274296
    Abstract: A method of preparing an orally ingestible hard boiled product, comprising: i) heating a sugar material to a first temperature sufficient to liquefy the sugar material; ii) cooling the liquefied sugar material to provide a cooled sugar material having a solid or semi-solid form; iii) heating the cooled sugar material to a second temperature, which is lower than the first temperature; iv) combining the sugar material with one or more temperature sensitive ingredients before, during, or after said heating step iii), but after said cooling step ii), such that an intimate mixture of the second liquefied sugar material and the one or more temperature sensitive ingredients is provided; and v) cooling the intimate mixture to form an orally ingestible product. Orally ingestible hard boiled products prepared according to this method are also provided.
    Type: Application
    Filed: April 17, 2012
    Publication date: October 17, 2013
    Inventors: Thaddeus J. Jackson, Frank Kelley St. Charles
  • Publication number: 20130267539
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. 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: Application
    Filed: June 5, 2013
    Publication date: October 10, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20130267492
    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
  • Patent number: 8552003
    Abstract: 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: Grant
    Filed: July 31, 2007
    Date of Patent: October 8, 2013
    Assignee: Novartis AG
    Inventors: 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
  • Publication number: 20130261156
    Abstract: 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: Application
    Filed: May 29, 2013
    Publication date: October 3, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yasuhiro Hiraishi, Muneo Nonomura
  • Publication number: 20130261100
    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
  • Patent number: 8545870
    Abstract: 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: Grant
    Filed: April 25, 2002
    Date of Patent: October 1, 2013
    Assignee: Pierre Fabre Medicament
    Inventors: Pierre Dupinay, Robert Torres, Christine Capon
  • Patent number: 8546588
    Abstract: 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: Grant
    Filed: February 25, 2011
    Date of Patent: October 1, 2013
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8546374
    Abstract: 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: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: 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
  • Publication number: 20130253013
    Abstract: 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: Application
    Filed: May 22, 2013
    Publication date: September 26, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Patent number: 8536205
    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
  • Publication number: 20130237570
    Abstract: 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: Application
    Filed: April 26, 2013
    Publication date: September 12, 2013
    Applicant: McNeil AB
    Inventors: Katarina E.A. Lindell, Anette K. Schluter, Gunner A. Bergengren, Bengt A. Bosson
  • Publication number: 20130237514
    Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 12, 2013
    Applicant: 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
  • Patent number: 8529914
    Abstract: 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: Grant
    Filed: September 2, 2010
    Date of Patent: September 10, 2013
    Inventors: Richard C. Fuisz, Joseph M. Fuisz
  • Publication number: 20130231334
    Abstract: 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: Application
    Filed: April 18, 2011
    Publication date: September 5, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Russell Slater, Peter Maienfisch, Patrik Hoegger, Alfred Rindlisbacher
  • Publication number: 20130231373
    Abstract: 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: Application
    Filed: August 27, 2010
    Publication date: September 5, 2013
    Applicant: Novartis AG
    Inventors: Clinton Alan Brooks, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Gang Liu, Michael David Schultz
  • Patent number: 8524710
    Abstract: 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: Grant
    Filed: October 24, 2011
    Date of Patent: September 3, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Banner, Uwe Grether, Wolfgang Haap, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Publication number: 20130225412
    Abstract: 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: Application
    Filed: February 28, 2012
    Publication date: August 29, 2013
    Inventors: Soroush Sardari Lodriche, Saeed Soltani, Roghieh Mirzazadeh
  • Publication number: 20130224114
    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.
    Type: Application
    Filed: March 25, 2013
    Publication date: August 29, 2013
    Applicant: The University of Sydney
    Inventor: The University of Sydney
  • Patent number: 8518976
    Abstract: 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: Grant
    Filed: December 18, 2007
    Date of Patent: August 27, 2013
    Assignee: Sanofi
    Inventors: Harmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
  • Patent number: 8518948
    Abstract: 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: Grant
    Filed: March 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Patent number: 8518943
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: August 27, 2013
    Assignee: UCB Pharma, S.A.
    Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
  • Publication number: 20130217714
    Abstract: 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: Application
    Filed: December 14, 2012
    Publication date: August 22, 2013
    Applicant: Trustees of Tufts College
    Inventor: Trustees of Tufts College
  • Publication number: 20130217686
    Abstract: A novel methylcyclohexane derivative, and a pharmaceutical composition including the same that is effective for the prevention or treatment of pain.
    Type: Application
    Filed: September 28, 2011
    Publication date: August 22, 2013
    Applicant: 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