Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/300)
  • Patent number: 7790758
    Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 7, 2010
    Assignee: Glaxo Group Limited
    Inventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
  • Patent number: 7790757
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: September 7, 2010
    Assignee: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
  • Publication number: 20100216758
    Abstract: An active ingredient is a compound represented by the general formula [I]: [wherein R1 and R2 represent a lower alkyl group, a C3-6 cycloalkyl group or the like, X1 and X2 represent methine, an Ar—Y1—Y2—Y3-substituted methine or the like, however either of them is an Ar—Y1—Y2—Y3-substituted methine, X3 to X8 represent methine, —N— or the like, Y1 and Y3 represent a single bond, —O— or the like, Y2 represent a single bond, a lower alkylene group or the like, W represent —(O)—(CH2)n-(O)— or the like, n represents an integer of 1 to 4, L and Z2 represent a single bond or a methylene group, Z1 represents a single bond, a C1-4 alkylene group or the like, and Ar represents an aromatic carbocyclic group or the like]. The compound acts as a melanin-concentrating hormone receptor antagonist and useful as a therapeutic agent for obesity or the like.
    Type: Application
    Filed: August 3, 2006
    Publication date: August 26, 2010
    Inventors: Makoto Ando, Etsuko Sekino, Yuji Haga, Norikazu Otake, Minoru Moriya
  • Publication number: 20100204481
    Abstract: Compounds incorporating aryl substituted olefinic amine are provided. Representative compounds are (4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-pyrimidinyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-methoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(6-amino-5-methyl-3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (2R)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-bromo-3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-ethoxy-3-pyridyl)-4-penten-2-amine, (2S)-(4E)-N-methyl-5-(3-pyridyl)-4-penten-2-amine, (4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine and (2S)-(4E)-N-methyl-5-(5-isopropoxy-3-pyridyl)-4-penten-2-amine.
    Type: Application
    Filed: April 21, 2010
    Publication date: August 12, 2010
    Applicant: Targacept, Inc.
    Inventors: William Scott Caldwell, Gary Maurice Dull, Balwinder Singh Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared Miller Wagner, Peter Anthony Crooks
  • Publication number: 20100173951
    Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.
    Type: Application
    Filed: June 4, 2008
    Publication date: July 8, 2010
    Inventors: Lawrence Wennogle, Peng Li, Jun Zhao
  • Publication number: 20100172836
    Abstract: The present invention relates to methods of synthesizing 18F-radiolabeled styrylpyridine and its tosylate precursor. The present invention further relates to stable pharmaceutical compositions comprising 18F-radiolabeled styrylpyridine.
    Type: Application
    Filed: December 29, 2009
    Publication date: July 8, 2010
    Applicant: AVID RADIOPHARMACEUTICALS, INC.
    Inventors: Tyler Benedum, Geoff Golding, Nathaniel Lim, Wei Zhang
  • Patent number: 7745426
    Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: June 29, 2010
    Assignees: D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.
    Inventors: Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro
  • Patent number: 7741323
    Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.
    Type: Grant
    Filed: April 13, 2005
    Date of Patent: June 22, 2010
    Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.
    Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
  • Publication number: 20100152252
    Abstract: The present invention relates to heterocyclyl-substituted-ethylamino-phenyl compounds of general formula (I), wherein K-L-M-N, Z and R1, R2, R3, R4 are as described in the claims methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans or animals.
    Type: Application
    Filed: December 21, 2007
    Publication date: June 17, 2010
    Applicant: LABORATORIOS DEL DR. ESTEVE,S.A.
    Inventors: Mónica Garcia-López, Antonio Torrens-Jover, Luz Romero-Alonso, Helmut H. Buschmann
  • Publication number: 20100152207
    Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
    Type: Application
    Filed: April 4, 2008
    Publication date: June 17, 2010
    Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
  • Publication number: 20100137377
    Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.
    Type: Application
    Filed: April 9, 2008
    Publication date: June 3, 2010
    Inventors: Anders Klarskov Petersen, Soren Ebdrup
  • Publication number: 20100121061
    Abstract: The present invention generally relates to nicotinic compounds, in the form of aryl substituted olefinic compounds, as well as pro-drug, N-oxide, metabolite and pharmaceutically acceptable salt forms thereof. Methods of modulating neurotransmitter release via administration of the compounds, pro-drugs, N-oxides and/or pharmaceutically acceptable salts are also disclosed.
    Type: Application
    Filed: December 8, 2009
    Publication date: May 13, 2010
    Applicant: Targacept, Inc.
    Inventors: William S. Caldwell, Gary M. Dull, Balwinder S. Bhatti, Srishailkumar B. Hadimani, Haeil Park, Jared M. Wagner, Peter A. Crooks, Patrick M. Lippiello, Merouane Bencherif
  • Publication number: 20100113522
    Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Application
    Filed: October 13, 2009
    Publication date: May 6, 2010
    Applicant: Amgen Inc.
    Inventors: Lawrence R. McGee, Jonathan B. Houze, Steven M. Rubenstein
  • Publication number: 20100111900
    Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: October 30, 2009
    Publication date: May 6, 2010
    Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
  • Publication number: 20100113276
    Abstract: The use of N2-phenylamidines of formula (I) as herbicides is described. In this formula (I), R2, R3, R4, R5 and R6 are different radicals and A is a bond or various 1- or polyatomic bridging elements.
    Type: Application
    Filed: March 4, 2008
    Publication date: May 6, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Birgit Kuhn, Harald Jakobi, Thomas Mueller, Joerg Tiebes, Heinz Kehne, Dirk Schmutzler, Martin Hills, Christopher Rosinger, Klaus Kunz, Mark Wilheim Drewes, Dieter Feucht, Thomas Seitz, Benoit Hartmann, Ralf Dunkel, Joerg Nico Greul, Oliver Guth, Kerstein Ilg, Darren James Mansfeld, Wahed Ahmed Moradi, Peter Dahmen, Ulrike Wachendorf-Neumann, Arnd Voerste, Dale Robert Mitchell, Jean-Pierre Andre Vors, Dale Robert Mitchell, Tom Hough
  • Patent number: 7687052
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: March 30, 2010
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20100075971
    Abstract: This invention relates to novel diaryl ureas, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with cytotoxic therapies.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 25, 2010
    Inventors: Jacques DUMAS, Wendy Lee, Yuanwei Chen, Lila Adnane, William J. Scott, Sharad Verma, Jianqing Chen, Zhi Chen, Lin Yi
  • Publication number: 20100076032
    Abstract: N-Substituted sulfoximines are effective at controlling insects.
    Type: Application
    Filed: November 11, 2009
    Publication date: March 25, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Yuanming Zhu, Richard Brewer Rogers, Jim Xinpei Huang
  • Patent number: 7674808
    Abstract: 4-pyridone (4-pyridinone) derivatives of Formula I and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: March 9, 2010
    Assignee: Glaxo Group Limited
    Inventors: Jose Maria Bueno Calderon, Jesus Chicharro Gonzalo, Milagros Lorenzo Garcia, M Pilar Manzano Chinchon
  • Patent number: 7666442
    Abstract: The present invention provides a composition comprising an effective amount of benfotiamine and an effective amount of pyridoxamine in a suitable vehicle for topical application. The present compositions are useful in improving the appearance of aged skin characterized by wrinkles, loss of elasticity, and hyperpigmentation caused by chronoaging and/or photoaging of skin, by inhibiting particularly skin damage resulting from reactive carbonyl species (RCS), glycation of skin proteins, formation of advanced glycation endproducts (AGEs) and formation of advanced lipoxidation endproducts (ALEs).
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: February 23, 2010
    Assignee: Tracie Martyn International, LLC
    Inventor: Marius Morariu
  • Publication number: 20100041893
    Abstract: The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
    Type: Application
    Filed: October 22, 2009
    Publication date: February 18, 2010
    Inventors: KEVIN R. CAMPOS, Artis Klapars, J. Christopher McWilliams, C. Scott Shultz, Debra J. Wallace, Alex M. Chen, Lisa F. Frey, Andrey V. Peresypkin, Yaling Wang, Robert M. Wenslow, Cheng-Yi Chen
  • Publication number: 20100041892
    Abstract: The present invention provides an agent for the prophylaxis or treatment of diabetes, which is associated with a fewer side effects such as body weight gain, adipocyte accumulation, cardiac hypertrophy and the like, and which contains a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: May 5, 2009
    Publication date: February 18, 2010
    Inventors: Hidenori Abe, Takeshi Wakabayashi, Kentarou Rikimaru
  • Publication number: 20100016376
    Abstract: The present invention relates to a pyridone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
    Type: Application
    Filed: October 26, 2007
    Publication date: January 21, 2010
    Applicant: LG Life Sciences Ltd.
    Inventors: Hye Kyung Chang, Yeong Soo Oh, Yong Jin Jang, Sung Sub Kim, Kyeong Sik Min, Chul Woong Chung, Mi Jeong Park, Jung Gyu Park
  • Publication number: 20090318703
    Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.
    Type: Application
    Filed: October 27, 2008
    Publication date: December 24, 2009
    Applicant: ONO PHARMACEUTICAL CO., LTD
    Inventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
  • Patent number: 7629365
    Abstract: 3-Chloro-6-(hydroxymethyl)-2-methyl-5-[4-({4-[(trifluoromethyl)oxy]phenyl}oxy)phenyl]-4(1H)-pyridinone, having the following formula: is described along with its pharmaceutically acceptable salts, processes for its preparation, pharmaceutical formulations thereof and its uses in treatment of certain parasitic infections such as malaria.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: December 8, 2009
    Assignee: Glaxo Group Limited
    Inventors: Jose Maria Bueno Calderon, Jesus Chicharro Gonzalo, M Pilar Manzano Chinchon
  • Publication number: 20090298890
    Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Application
    Filed: July 5, 2007
    Publication date: December 3, 2009
    Applicant: BAYER CROPSCIENCE SA
    Inventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Philippe Desbordes, Pierre Genix, Benoit Hartmann, Amos Mattes, Klaus Kunz, Rudiger Fischer, Oliver Gaertzen, Oswald Ort, Darren Mansfield, Alain Villier
  • Publication number: 20090275611
    Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: April 2, 2007
    Publication date: November 5, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Publication number: 20090275751
    Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
    Type: Application
    Filed: February 27, 2009
    Publication date: November 5, 2009
    Inventors: Satoshi NAGATO, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito, Takaisa Hanada, Masatake Ueno, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Yoshio Urawa, Hiroyuki Naka, Anthony John Groom, Leanne Rivers, Terrence Smith
  • Publication number: 20090274632
    Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
    Type: Application
    Filed: August 19, 2008
    Publication date: November 5, 2009
    Applicant: Senomyx, Inc.
    Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest
  • Patent number: 7608720
    Abstract: The present invention relates to a novel process for the preparation of 2-amino-methylpyridine derivatives of the formula (I), comprising reacting in a first step 2-substituted pyridine derivatives of the formula (II), with a nitroalkane of the formula (III), in the presence of a base resulting in 2-nitromethylpyridine derivatives of the formula (IV) and hydrogenating these 2-nitromethylpyridine derivatives of the formula (IV) in a second step in the presence of a catalyst and in the presence of an acid, where in the formulae n, X, Y, R1, R2 and A are as defined in the description.
    Type: Grant
    Filed: April 26, 2004
    Date of Patent: October 27, 2009
    Assignee: Bayer Cropscience AG
    Inventors: Jorn Stolting, Brian Burton
  • Patent number: 7605164
    Abstract: Certain substituted benzamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: October 20, 2009
    Assignee: Cytokinetics, Inc.
    Inventors: Fady Malik, Adam Lewis Tomasi, Bainian Feng, Erica Anne Kraynack, Kathleen A. Elias, Pu-Ping Lu, Whitney Walter Smith, Xiangping Qian, David J. Morgans, Jr.
  • Publication number: 20090258884
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Application
    Filed: April 16, 2009
    Publication date: October 15, 2009
    Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, JR.
  • Publication number: 20090253688
    Abstract: The present invention relates to semicarbazide derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
    Type: Application
    Filed: February 14, 2005
    Publication date: October 8, 2009
    Applicant: Merck Patent GmbH
    Inventors: Hans-Peter Buchstaller, Dirk Finsinger, Frank Stieber, Matthias Wiesner, Christiane Amendt, Christian Sirrenberg, Frank Zenke, Matthias Grell
  • Publication number: 20090240053
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Application
    Filed: May 28, 2009
    Publication date: September 24, 2009
    Applicant: Purdue Neuroscience Company
    Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
  • Patent number: 7585883
    Abstract: The present invention is directed to substituted pyridines, methods for their preparation and methods for their use in the treatment and/or prevention of mast cell related conditions.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: September 8, 2009
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Ankush Argade, David Carroll, Alexander B. Rossi
  • Publication number: 20090221596
    Abstract: The invention relates to compounds of the formula (I) in which A1, A2, R1, R2, R3, R4, R5 and X are as defined in the description, to processes and intermediates for their preparation, and to their use for controlling pests.
    Type: Application
    Filed: May 6, 2006
    Publication date: September 3, 2009
    Inventors: Iris Escher, Michael Müller, Peter Jeschke, Michael Beck, Oliver Gaertzen, Olga Malsam, Peter Lösel, Ulrich Ebbinghaus-Kintscher, Christian Arnold, Karl-Josef Haack
  • Publication number: 20090209767
    Abstract: The invention relates to 2-(butyl-1-sulfonylamino)-N-[1(R)-(6-methoxy-pyridin-3-yl)propyl]benzamide of the formula I and to its pharmaceutically acceptable salts, their preparation and use, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation or atrial flutters.
    Type: Application
    Filed: April 29, 2009
    Publication date: August 20, 2009
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Joachim BRENDEL, Heinz GOEGELEIN, Klaus WIRTH, Gert Ulrich KUERZEL
  • Publication number: 20090137529
    Abstract: The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.
    Type: Application
    Filed: May 11, 2007
    Publication date: May 28, 2009
    Inventors: William K. Hagmann, Milton L. Hammond
  • Publication number: 20090137587
    Abstract: A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents —CH2—O—, —CH?CH— or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
    Type: Application
    Filed: August 23, 2006
    Publication date: May 28, 2009
    Inventors: Akira Naya, Toshihiro Sakamoto, Yuji Haga, Norikazu Otake
  • Publication number: 20090131456
    Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.
    Type: Application
    Filed: January 26, 2009
    Publication date: May 21, 2009
    Inventors: Julian M.C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
  • Publication number: 20090123369
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Application
    Filed: August 5, 2008
    Publication date: May 14, 2009
    Applicant: The Trustees of The University of Pennsylvania
    Inventors: Hank F. Kung, Mei Ping Kung
  • Patent number: 7531535
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: May 12, 2009
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Donald J. P. Pinto, Jennifer X. Qiao
  • Publication number: 20090118512
    Abstract: 6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5-a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced depro
    Type: Application
    Filed: March 30, 2007
    Publication date: May 7, 2009
    Inventors: Pierre Martin, Andreas Boudier, Michael Quirmbach, Robert Mah, Nathalie Jotterand
  • Publication number: 20090118338
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: October 10, 2008
    Publication date: May 7, 2009
    Inventors: Weichuan Caroline Chen, Paul Krenitsky, Pramod Joshi, Andreas Termin, Dean Wilson
  • Patent number: 7528255
    Abstract: The invention relates to the use of a group of aryl ureas in treating raf mediated diseases and pharmaceutical compositions for use in such therapy of the formula wherein, Y is NHR Hal is chlorine or bromine, R is H, CH3 or CH2OH, and X1 to X7 are each, independently, H, OH or —OC(O)C1-C4 alkyl, or a salt purified stereoisomer thereof, wherein at least one of X1 to X7 is OH or —OC(O)C1-C4 alkyl.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: May 5, 2009
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy Lowinger, William Scott, Roger Smith, Jill Wood
  • Publication number: 20090105310
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: May 11, 2007
    Publication date: April 23, 2009
    Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Cangming Yang, Ashley Rouse Lins
  • Publication number: 20090105309
    Abstract: Compounds of formula (I): and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective ?2-adrenoreceptor agonist is indicated, for example asthma or chronic obstructive pulmonary disease (COPD).
    Type: Application
    Filed: October 20, 2004
    Publication date: April 23, 2009
    Applicant: GLAXO GROUP LIMITED
    Inventors: Philip Charles Box, Diane Mary Coe, Heather Hobbs
  • Patent number: 7517880
    Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: April 14, 2009
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
  • Patent number: 7514564
    Abstract: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: April 7, 2009
    Assignee: Amgen Inc.
    Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Qi Huang, Joseph L. Kim, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan, Tae-Seong Kim
  • Publication number: 20090088458
    Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.
    Type: Application
    Filed: July 28, 2006
    Publication date: April 2, 2009
    Inventors: Robert S. Meissner, James J. Perkins, Yuntae Kim, Barbara Hanney, Carol A. McVean