Nitrogen Attached Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/366)
  • Publication number: 20150051270
    Abstract: A compound of formula I, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein either Q1, CR6a and optionally R6b together form a cyclic moiety wherein: Q1 is selected from C1-2 alkylene, C1-2 alkenylene, OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo; R6a is a single bond and R6b is H; or R6a and R6b together form a double bond; and Q2 and Q3 are independently selected from H, R1 and R2; or Q2 and Q3 together form a cyclic moiety in which one of Q2 and Q3 is a cyclic moiety selected from OC1 alkylene and OC1 alkenylene moieties optionally substituted by oxo or a group R5 as here in below defined for R2 and the other of Q2 and Q3 is a cyclic moiety selected from C1-2 alkylene, C1-2 alkenylene and OC1 alkylene optionally substituted by oxo; R6a and R6b are each H or a cyclic moiety as defined above; and Q1 is selected from H, R1 and R2 and a cyclic moiety as defined above; and R1-4 are H or substituen
    Type: Application
    Filed: February 15, 2013
    Publication date: February 19, 2015
    Inventors: Shailesh Mistry, Etíenne Daras, Christophe Fromont, Gopal Jadhav, Peter Martin Fischer, Barrie Kellam, Stephen John Hill, Jillian Glenda Baker
  • Publication number: 20150031878
    Abstract: The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis.
    Type: Application
    Filed: March 15, 2013
    Publication date: January 29, 2015
    Inventors: Hee-Yong Kim, Juan Jose Marugan, Erika E. Englund, Samarjit Patnaik
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20140359951
    Abstract: An agent for oxidative coloring of keratin-containing fibers, in particular human hair, includes as oxidation dye precursor of the developer type at least one compound of formula (I).
    Type: Application
    Filed: August 22, 2014
    Publication date: December 11, 2014
    Inventors: Antje Gebert, Annika Koenen
  • Publication number: 20140288317
    Abstract: The present invention provides a novel radiolabelled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GE HEALTHCARE LIMITED
    Inventors: HARRY JOHN WADSWORTH, DENNIS O'SHEA
  • Patent number: 8815939
    Abstract: The present invention is directed to novel substituted sulfamide derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives form in the treatment of anxiety and related disorders; bipolar depression and mania; depression; epilepsy and related disorders; epileptogenesis; glucose related disorders; lipid related disorders; migraine; obesity; pain; substance abuse and as neuroprotective agents. The present invention is further directed to a process for the preparation of the novel substituted sulfamide derivatives.
    Type: Grant
    Filed: July 14, 2009
    Date of Patent: August 26, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: David F. McComsey, Michael H. Parker
  • Patent number: 8809385
    Abstract: The present invention is directed to a novel crystalline form of (2S)-(?)-N-(6-chloro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-sulfamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of anxiety and related disorders; bipolar depression and mania; depression; epilepsy and related disorders; epileptogenesis; glucose related disorders; lipid related disorders; migraine; obesity; pain; substance abuse; or for neuroprotection. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: August 19, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Steven J. Mehrman, Wenju Wu
  • Publication number: 20140179687
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: February 21, 2014
    Publication date: June 26, 2014
    Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
  • Publication number: 20140094493
    Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4al
    Type: Application
    Filed: February 6, 2012
    Publication date: April 3, 2014
    Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
  • Publication number: 20130184222
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 15, 2011
    Publication date: July 18, 2013
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
  • Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Publication number: 20130101684
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 25, 2013
    Applicant: Chromocell Corporation
    Inventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
  • Publication number: 20130085175
    Abstract: The present invention is directed to an improved process for the preparation of sulfamide derivatives.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Applicant: JOHNSON & JOHNSON
    Inventor: Johnson & Johnson
  • Publication number: 20130085176
    Abstract: The present invention is directed to a process for the preparation of sulfamide derivatives.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Applicant: JOHNSON & JOHNSON
    Inventor: JOHNSON & JOHNSON
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Patent number: 8377422
    Abstract: Compounds of formula (I) wherein R1-R5, n and m have the same meaning as given in the description, having cooling properties are disclosed. Furthermore a process of their production and consumer products comprising them are disclosed.
    Type: Grant
    Filed: December 4, 2008
    Date of Patent: February 19, 2013
    Assignee: Givaudan S.A.
    Inventors: Stefan Michael Furrer, Thomas Scott McCluskey
  • Publication number: 20120245141
    Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia,
    Type: Application
    Filed: March 29, 2012
    Publication date: September 27, 2012
    Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human Services
    Inventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
  • Publication number: 20120064062
    Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.
    Type: Application
    Filed: September 13, 2011
    Publication date: March 15, 2012
    Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
  • Patent number: 8084490
    Abstract: The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: December 27, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
  • Publication number: 20110306621
    Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on a serotonin 5-HT5A receptor modulating action. It was confirmed that acylguanidine derivatives, which has the characteristic structure in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent 5-HT5A receptor modulating action and excellent pharmacological action based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.
    Type: Application
    Filed: February 8, 2010
    Publication date: December 15, 2011
    Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
  • Publication number: 20110275663
    Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.
    Type: Application
    Filed: April 16, 2009
    Publication date: November 10, 2011
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20110182833
    Abstract: Compounds of formula (I) wherein R1-R5, n and m have the same meaning as given in the description, having cooling properties are disclosed. Furthermore a process of their production and consumer products comprising them are disclosed.
    Type: Application
    Filed: December 4, 2008
    Publication date: July 28, 2011
    Inventors: Stefan Michael Furrer, Thomas Scott McCluskey
  • Publication number: 20110105462
    Abstract: The present invention relates to novel 1-(2,3-dihydro-1,4-benzodioxin-2-yl)-methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically as dopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: April 28, 2009
    Publication date: May 5, 2011
    Applicant: NSAB, FILIAL AF NEUROSEARCH SWEDEN AB, SVERIGE
    Inventors: Clas Sonesson, Peder Svensson
  • Publication number: 20110105461
    Abstract: The present invention relates to novel 1-(2,3-dihydro-1,4-benzodioxin-2-yl)-methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically as dopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: April 28, 2009
    Publication date: May 5, 2011
    Applicant: NSAB, FILIAL AF NEUROSEARCH SWEDEN AB, SVERIGE
    Inventors: Clas Sonesson, Peder Svensson, Jonas Karlsson
  • Publication number: 20110104162
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Application
    Filed: June 15, 2009
    Publication date: May 5, 2011
    Applicant: Cytomics Systems
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20110082109
    Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 7, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
  • Publication number: 20110021514
    Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
    Type: Application
    Filed: November 13, 2008
    Publication date: January 27, 2011
    Applicants: RENOVIS, INC., PFIZER GLOBAL RESEARCH AND DEVELOPMENT
    Inventors: Matthew Cox, Donogh John Roger O'Mahony, Maria De Los Angeles Estiarte-Martinez, Tadashi Kawashima, Satoshi Nagayama, Yuji Shishido, Hirotaka Tanaka, Matthew Alexander James Duncton, Andrew Antony Calabrese
  • Patent number: 7851220
    Abstract: The present invention relates to methods to use non-steroidal ligands in nuclear receptor-based inducible gene expression system to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
    Type: Grant
    Filed: November 2, 2007
    Date of Patent: December 14, 2010
    Assignee: Intrexon Corporation
    Inventors: Robert Eugene Hormann, Colin M. Tice, Orestes Chortyk, Howard Smith, Thomas Meteyer
  • Patent number: 7846925
    Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.
    Type: Grant
    Filed: July 10, 2003
    Date of Patent: December 7, 2010
    Assignee: Merck Serono SA
    Inventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
  • Publication number: 20100261675
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
  • Publication number: 20100217012
    Abstract: Processes and intermediates are provided for the preparation of substituted aminomethyl 2,3,8,9-tetrahydiO-7H-1,4-dioxino[2.3-e]indo]-8-ones of the Formula (A) wherein the variables n, R and R3 are as described herein. Such compounds are useful, for example, as dopamine receptor agonists.
    Type: Application
    Filed: March 26, 2008
    Publication date: August 26, 2010
    Applicant: NEUROGEN CORPORATION
    Inventors: Zhe-qing Wang, Andrew J. Staab, Christopher K. Seekamp, George P. Luke
  • Publication number: 20100137401
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: February 2, 2010
    Publication date: June 3, 2010
    Applicant: Incyte Corporation
    Inventors: Wenqing Yao, Colin Zhang, Jincong Zhuo, Meizhong Xu, Konstantinos Agrios, Brian Metcalf
  • Publication number: 20100063138
    Abstract: The present invention is directed to novel substituted sulfamide derivatives, pharmaceutical compositions containing said derivatives and the use of said derivatives form in the treatment of anxiety and related disorders; bipolar depression and mania; depression; epilepsy and related disorders; epileptogenesis; glucose related disorders; lipid related disorders; migraine; obesity; pain; substance abuse and as neuroprotective agents. The present invention is further directed to a process for the preparation of the novel substituted sulfamide derivatives.
    Type: Application
    Filed: July 14, 2009
    Publication date: March 11, 2010
    Inventors: David F. McComsey, Michael H. Parker
  • Patent number: 7667053
    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: Grant
    Filed: April 8, 2003
    Date of Patent: February 23, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Laurie A. Castonguay, William K. Hagmann, Linus S. Lin, Shrenik K. Shah
  • Patent number: 7662979
    Abstract: The present invention provides methods for preparing compounds having activity as dopamine autoreceptor agonists and partial agonists at the postsynaptic dopamine D2 receptor. These compounds are useful for treating dopaminergic disorders, such as schizophrenia, schizoaffective disorder, Parkinson's disease, Tourette's syndrome, hyperprolactinemia, and drug addiction.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: February 16, 2010
    Assignee: Wyeth
    Inventor: Rocco J. Galante
  • Publication number: 20100035872
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Application
    Filed: August 4, 2009
    Publication date: February 11, 2010
    Applicant: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler
  • Patent number: 7652006
    Abstract: The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.
    Type: Grant
    Filed: February 6, 2004
    Date of Patent: January 26, 2010
    Assignee: Euro-Celtique S.A.
    Inventors: Ravi Upasani, Sui X Cai, Nancy C Lan, Yan Wang, George Field, David B Fick
  • Publication number: 20090318544
    Abstract: The present invention is directed to a novel crystalline form of (2S)-(?)-N-(6-chloro-2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-sulfamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of anxiety and related disorders; bipolar depression and mania; depression; epilepsy and related disorders; epileptogenesis; glucose related disorders; lipid related disorders; migraine; obesity; pain; substance abuse; or for neuroprotection. The present invention is further directed to a process for the preparation of the novel crystalline form.
    Type: Application
    Filed: June 19, 2009
    Publication date: December 24, 2009
    Inventors: Steven J. Mehrman, Wenju Wu
  • Patent number: 7601712
    Abstract: A compound represented by formula (I) wherein the symbols in the formula are the same meanings as those in specification, salts thereof, solvates thereof, or prodrugs thereof binds to DP receptor and shows antagonistic activity for DP receptor. Thus, it is useful for prevention and/or treatment of diseases such as allergic disease (e.g., allergic rhinitis, allergic conjunctivitis, atopic dermatitis, bronchial asthma and food allergy), systemic mastocytosis, disorders accompanied by systemic mast cell activation, anaphylaxis shock, bronchoconstriction, urticaria, eczema, diseases accompanied by itch (e.g., atopic dermatitis and urticaria), diseases (e.g., cataract, retinal detachment, inflammation, infection and sleeping disorders) which is generated secondarily as a result of behavior accompanied by itch (e.g.
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: October 13, 2009
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Atsushi Naganawa, Maki Iwahashi, Atsushi Kinoshita, Atsushi Shimabukuro, Seiji Ogawa, Koji Yano, Kaoru Kobayashi, Yutaka Okada, Yoko Kishida, Shouji Kawauchi, Kohki Tsukamoto, Yoko Matsunaga, Fumio Nambu
  • Publication number: 20090253684
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, COPD.
    Type: Application
    Filed: December 2, 2008
    Publication date: October 8, 2009
    Inventors: Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri, Jefferson Wright Tilley
  • Publication number: 20090247616
    Abstract: The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of anxiety and related disorders, which includes mono-therapy and alternatively, co-therapy with at least one anxiolytic.
    Type: Application
    Filed: March 26, 2008
    Publication date: October 1, 2009
    Inventor: Virginia L. Smith-Swintosky
  • Publication number: 20090247618
    Abstract: The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.
    Type: Application
    Filed: March 26, 2008
    Publication date: October 1, 2009
    Inventors: Scott A. Ballentine, Laura Reany
  • Publication number: 20090182141
    Abstract: The present invention is directed to novel processes for the preparation of sulfamide derivatives, useful in the treatment of epilepsy and related disorders.
    Type: Application
    Filed: January 6, 2009
    Publication date: July 16, 2009
    Inventors: Ahmed Abdel-Magid, Steven J. Mehrman, Caterina Ferraro
  • Publication number: 20090176773
    Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.
    Type: Application
    Filed: May 18, 2006
    Publication date: July 9, 2009
    Applicant: FORSCHUNGSVERBUND BERLIN E.V.
    Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
  • Publication number: 20090082395
    Abstract: Disclosed are amide, thioamide, urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.
    Type: Application
    Filed: September 9, 2008
    Publication date: March 26, 2009
    Inventor: Richard D. Gless, JR.
  • Patent number: 7488751
    Abstract: Compounds of the Formula I: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: February 10, 2009
    Assignee: Wyeth
    Inventors: Deborah Ann Evrard, Uresh Shantilah Shah, Gary Paul Stack
  • Patent number: 7476673
    Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.
    Type: Grant
    Filed: December 17, 2004
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
  • Publication number: 20090009061
    Abstract: The object of the present invention is to provide a composition for conductive materials from which a conductive layer having a high carrier transport ability can be made, a conductive material formed of the composition and having a high carrier transport ability, a conductive layer formed using the conductive material as a main material, an electronic device provided with the conductive layer and having high reliability, and electronic equipment provided with the electronic device.
    Type: Application
    Filed: July 27, 2005
    Publication date: January 8, 2009
    Inventors: Yuji Shinohara, Koichi Terao, Takashi Shinohara
  • Publication number: 20080318779
    Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.
    Type: Application
    Filed: August 10, 2005
    Publication date: December 25, 2008
    Applicant: ISHIHARA SANGYO KAISHA LTD
    Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda