Nitrogen Attached Indirectly To Ring Carbon Of The Bicyclo Ring System By Acyclic Nonionic Bonding Patents (Class 548/503)
  • Patent number: 9975850
    Abstract: The present invention relates to the preparation of N-(2-(6-fluoro-1H-indol-3-yl)-ethyl)-3-(2,2,3,3-tetrafluoropropoxy)-benzylamine (Compound I), INN-name idalopirdine, and pharmaceutically acceptable salts thereof:
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: May 22, 2018
    Assignee: H. LUNDBECK A/S
    Inventors: Mikkel Fog Jacobsen, Florian Anton Martin Huber
  • Patent number: 8993616
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: May 16, 2013
    Date of Patent: March 31, 2015
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Publication number: 20140315965
    Abstract: The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.
    Type: Application
    Filed: December 20, 2012
    Publication date: October 23, 2014
    Inventors: James L. Gleason, John H. White, Dainis Kaldre, Joshua Fischer
  • Patent number: 8829040
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: February 28, 2014
    Date of Patent: September 9, 2014
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Publication number: 20140228409
    Abstract: The present invention provides a fused heterocyclic compound having an ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I?): wherein each symbol is as defined in the specification, provided that 2-(2-((4-cyanophenyl)amino)-2-oxoethoxy)-N-(9-ethyl-9H-carbazol-3-yl)acetamide and N-(4-cyanophenyl)-N?-(9-ethyl-9H-carbazol-3-yl)-3-methylpentanediamide are excluded, or a salt thereof.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 14, 2014
    Inventors: Satoshi Yamamoto, Junya Shirai, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Atsuko Ochida, Kazuko Yonemori, Hideyuki Nakagawa
  • Publication number: 20140179750
    Abstract: The disclosure relates to Prostaglandin receptor EP2 antagonists, derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing conditions and diseases in which EP2 receptor activation has a physiological role, such as but not limited to, brain injury, inflammatory diseases, neuroinflammation after a seizure, pain, endometriosis, cancer, rheumatoid arthritis, skin inflammation, vascular inflammation, colitis, and neurological disorders by administering a pharmaceutical composition comprising a compound disclosed herein to a subject in need thereof.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 26, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Jianxiong Jiang, Thota Ganesh, Yuhong Du, Pahk Thepchatri, Yi Quan, Ray J. Dingledine
  • Publication number: 20140128391
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.
    Type: Application
    Filed: November 1, 2013
    Publication date: May 8, 2014
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 8697739
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 15, 2014
    Assignee: Novartis AG
    Inventors: David Weninger Barnes, Gregory Raymond Bebernitz, Kevin Clairmont, Scott Louis Cohen, Robert Edson Damon, Robert Francis Day, Stephanie Kay Dodd, Christoph Gaul, Hatice Belgin Gulgeze Efthymiou, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Kai Lin, Justin Yik Ching Mao, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Liansheng Su
  • Publication number: 20140024694
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: July 15, 2013
    Publication date: January 23, 2014
    Applicant: GlaxoSmithKline Intellectual Property (No.2) Limit ed
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla
  • Publication number: 20140004174
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: May 20, 2013
    Publication date: January 2, 2014
    Applicant: Pharmacyclics, Inc.
    Inventors: Erik VERNER, Sriram BALASUBRAMANIAN, Joseph J. BUGGY
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130296281
    Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: June 16, 2011
    Publication date: November 7, 2013
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
  • Patent number: 8486984
    Abstract: The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: July 16, 2013
    Assignee: Abbott GmbH & Co., KG
    Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
  • Publication number: 20130178471
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Vextex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Patent number: 8466152
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: June 18, 2013
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8445697
    Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 21, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Patent number: 8440840
    Abstract: A dye including an anchoring group in its molecular structure, said anchoring group allowing a covalent coupling of said dye to a surface, for example a surface of a nanoporous semiconductor layer, said anchoring group being represented by formula 1 wherein attachment of said anchoring group within said molecular structure of said dye is at the terminal carbon marked with an asterisk in above formula, wherein G is selected from —COOH, —SO3H, —PO3H2, —BO2H2, —SH, —OH, —NH2, preferably —COOH, wherein A is selected from the group comprising H, —CN, —NO2, —COOR, —COSR, —COR, —CSR, —NCS, —CF3, —CONR2-OCF3, C6H5-mFm, wherein m=1-5, R being H or any straight or branched alkyl chain of general formula —CnH2n+I, n=O-12, preferably 0-4, or any substituted or non-substituted phenyl or biphenyl.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: May 14, 2013
    Assignee: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Publication number: 20130029846
    Abstract: The present invention relates to the use of bicyclic amidine compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to novel bicyclic amidines and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: March 28, 2011
    Publication date: January 31, 2013
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
  • Publication number: 20120184556
    Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.
    Type: Application
    Filed: July 23, 2010
    Publication date: July 19, 2012
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
  • Publication number: 20120095042
    Abstract: Provided are compounds of formula (I) wherein m is 0, 1 or 2; RI is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R2 is selected from hydrogen, methyl and ethyl; I) R3 is hydrogen, methyl, or ethyl; and R4 and R5 are independently selected from ethyl and isopropyl; and R3, R4 and R5 together have at least 6 carbon atoms: or II) any two or all of R3, R4 and R5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.
    Type: Application
    Filed: May 4, 2010
    Publication date: April 19, 2012
    Inventor: Stefan Michael Furrer
  • Patent number: 8143291
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: January 3, 2011
    Date of Patent: March 27, 2012
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Patent number: 8097643
    Abstract: The present invention refers to new sulfonamide derivatives, of general formula (1a, 1b, 1c), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemate, or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or their salt thereof s, preferably the corresponding, physiologically acceptable salt thereofs, or corresponding solvate thereofs; to the processes for their preparation, to their application as medicaments in human and/or veterinary therapeutics, and to the pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: January 17, 2012
    Assignee: Laboratorios del Dr. Esteve S. A.
    Inventors: Ramon Merce Vidal, Xavier Codony Soler, Alberto Dordal Zueras
  • Patent number: 8093275
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: June 22, 2010
    Date of Patent: January 10, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Minmin Yang
  • Publication number: 20110275677
    Abstract: The invention provides well-defined aryl and/or heteroaryl substituted indoles that are useful as sphingosine-1-phosphate agonists or antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: January 3, 2011
    Publication date: November 10, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Richard L. Beard, Haiqing Yuan, John E. Donello
  • Patent number: 8048886
    Abstract: The present invention relates to novel IAP inhibitor compounds of formula I:
    Type: Grant
    Filed: December 7, 2007
    Date of Patent: November 1, 2011
    Assignee: Novartis AG
    Inventors: Zhuoliang Chen, Run-Ming David Wang, Ming Chen, Christopher Sean Straub, Leigh Zawel
  • Patent number: 8044090
    Abstract: The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: October 25, 2011
    Assignee: Eli Lilly
    Inventors: Zhaogen Chen, Michael Philip Cohen, Matthew Joseph Fisher, Bruno Giethlen, James Ronald Gillig, Jefferson Ray McCowan, Shawn Christopher Miller, John Mehnert Schaus
  • Publication number: 20110230350
    Abstract: Use of substituted sulfonamides of the formula (I) or salts thereof for enhancing stress tolerance in plants to abiotic stress, especially for enhancing plant growth and/or for increasing plant yield.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 22, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Jens Frackenpohl, Ines Heinemann, Thomas Müller, Pascal Von Koskull-Döring, Jan Dittgen, Dirk Schmutzler, Christopher Hugh Rosinger, Isolde Häuser-Hahn, Martin Jeffrey Hills
  • Publication number: 20110207732
    Abstract: Compounds of the formula (I), in which X1, X2, X3, X4, R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: September 24, 2009
    Publication date: August 25, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Timo Heinrich, Hannes Koolman
  • Patent number: 8003647
    Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.
    Type: Grant
    Filed: April 10, 2008
    Date of Patent: August 23, 2011
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuo Shimizu, Yasushi Takigawa, Hideki Fujikura, Masato Iizuka, Masahiro Hiratochi, Norihiko Kikuchi
  • Patent number: 8003624
    Abstract: In its many embodiments, the present invention provides a novel class of indolines as inhibitors of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: August 23, 2011
    Assignees: Schering Corporation, Pharmacopeia, Inc.
    Inventors: Kevin D. McCormick, Christopher W. Boyce, Younong Yu
  • Patent number: 7989494
    Abstract: Polymorphic forms of N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2E-2-propenamide free base and salts thereof are prepared by various processes.
    Type: Grant
    Filed: June 7, 2007
    Date of Patent: August 2, 2011
    Assignee: Novartis AG
    Inventors: Murat Acemoglu, Joginder S. Bajwa, Piotr Karpinski, Dimitris Papoutsakis, Joel Slade, Frank Stowasser
  • Patent number: 7977352
    Abstract: Novel triazolopyridine 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, ECM degradation, joint degradation and/or inflammation, and others.
    Type: Grant
    Filed: November 30, 2007
    Date of Patent: July 12, 2011
    Assignee: Galapagos NV
    Inventors: Paul John Edwards, Wolfgang Schmidt, Veronique Birault, Friedrich Erich Karl Kroll, Andrew Burritt, Xueliang Tao, Martin James Inglis Andrews, Sébastien Laurent Xavier Martina
  • Publication number: 20110152539
    Abstract: Disclosed herein are processes for the preparation of a pharmaceutically active agent and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 20, 2010
    Publication date: June 23, 2011
    Applicant: H. LUNDBECK A/S
    Inventors: Frans Therkelsen, Michael Harold Rock, Svend Treppendahl
  • Patent number: 7956185
    Abstract: Compounds of formula (I) where X1, C1, and D1 are defined herein, are inhibitors of polo-like kinases. The compounds of formula (I) are useful for treatment of diseases of cellular proliferation, such as, for example, cancer.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 7, 2011
    Assignee: Abbott Laboratories
    Inventors: Robert B. Diebold, Stevan W. Djuric, Vincent L. Giranda, Laura A. Hexamer, Nan-Horng Lin, Julie M. Miyashiro, Thomas D. Penning, Magdalena Przytulinska, Thomas J. Sowin, Gerard M. Sullivan, Zhi-Fu Tao, Yunsong Tong, Anil Vasudevan, Le Wang, Keith W. Woods, Zhiren Xia, Henry Q. Zhang
  • Patent number: 7951940
    Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: May 31, 2011
    Assignee: NeurAxon, Inc.
    Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
  • Publication number: 20110124657
    Abstract: The present invention relates to compounds having pharmacological activity towards the 5-HT7 receptor; to a method for identifying them as 5-HT7 ligands, especially as agonists, by using a pharmacophore and a descriptor's profile filter; to pharmaceutical compositions comprising them; and to their use in therapy, in particular for the treatment and or prophylaxis of a disease in which 5-HT7 is involved, such as CNS disorders.
    Type: Application
    Filed: July 30, 2009
    Publication date: May 26, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Rosalia Pascual-Ramon, H. Helmut Buschmann
  • Patent number: 7947696
    Abstract: Novel phenylquinazoline derivatives of the formula (I), in which R1, R2, R3, R4 and R5 have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller
  • Patent number: 7939531
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: May 10, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Mark Bartlett, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, Jaehyeon Park, David Bernard Smith, Michael Soth, Hanbiao Yang, Calvin Wesley Yee
  • Publication number: 20110105543
    Abstract: This invention relates to novel triaryl derivatives, formula (I), a stereoisomer thereof or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein all of X, Y and Z represent CH; or one or two of X, Y and Z represent N; and the others of X, Y and Z represent CH; and R1, R2, R3, R4 and R5. independently of each other, represent hydrogen, halo, tri-fluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkoxy, alkyl, amino or sulfamoyl; or R1 and R2, together with the phenyl ring to which they are attached form an indolyl ring or a benzo-dioxolyl ring; and R3, R4 and R5 are as defined above; and R6 represents amino or nitro, which are found to be modulators of the nicotinic acetylcholine receptors.
    Type: Application
    Filed: March 9, 2009
    Publication date: May 5, 2011
    Applicant: NeuroSearch A/S
    Inventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
  • Patent number: 7932254
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1 and R are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: April 26, 2011
    Assignee: Roche Palo Alto
    Inventors: Daisy Joe DuBois, Robert Than Hendricks, Johannes Cornelius Hermann, Rama K. Kondru, Yan Lou, Timothy D. Owens, Calvin Wesley Yee
  • Publication number: 20110086877
    Abstract: Disclosed herein are methods of inhibiting the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing intoxication caused by bacteria of at least one bacterial strain in a subject, and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.
    Type: Application
    Filed: October 1, 2010
    Publication date: April 14, 2011
    Inventors: SINA BAVARI, RICK GUSSIO, JAMES C. BURNETT
  • Publication number: 20110039808
    Abstract: There is a need for pharmaceutical compounds which have activity at, at least one of a PPAR and a cannabinoid receptor. Thus there are provided such compounds, wherein the compound comprises: a PPAR pharmacophore and a cannabinoid pharmacophore linked together by a moiety comprising a fused bicyclic ring comprising a five membered ring fused with a six membered ring or a six membered ring fused with a six membered ring; wherein the cannabinoid pharmacophore comprises the fused bicyclic ring; and the PPAR pharmacophore comprises a salicylic acid, alkoxybenzylacetic acid or a alkoxyphenylacetic acid functionality; and wherein the PPAR pharmacophore is linked to the bicyclic ring of the cannabinoid pharmacophore through a linker comprising an amine or an amide functional group.
    Type: Application
    Filed: December 22, 2008
    Publication date: February 17, 2011
    Inventors: Pierre Desreumaux, Salvatore Bellinvia, Philippe Chavatte, Sergio Baroni
  • Publication number: 20110028463
    Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.
    Type: Application
    Filed: July 2, 2008
    Publication date: February 3, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
  • Publication number: 20110003836
    Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.
    Type: Application
    Filed: July 7, 2010
    Publication date: January 6, 2011
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
  • Patent number: 7851623
    Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-[(4-fluoro-2-methy-1-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline starting from a compound of Formula IX: wherein R4 is a protecting group; or an intermediate there between, using process steps, reagents and conditions as described.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: December 14, 2010
    Assignee: AstraZeneca AB
    Inventors: Euan Alexander Arnott, John Crosby, Matthew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
  • Publication number: 20100300521
    Abstract: The present invention relates to squarylium dyes including an anchoring group, to a method of synthesis of such dye, to an electronic device comprising such dye, and to uses of such dye.
    Type: Application
    Filed: October 27, 2008
    Publication date: December 2, 2010
    Applicant: Sony Corporation
    Inventors: Gerda Fuhrmann, Gabriele Nelles, Ameneh Bamedi Zilai, Akio Yasuda
  • Publication number: 20100292292
    Abstract: Methods and compositions useful in the treatment or prevention of synucleinopathies, such as Parkinson's disease, diffuse Lewy body disease, and multiple system atrophy, or other neurodegenerative diseases (e.g., amyotrophic lateral sclerosis, Huntington's disease, and Alzheimer's disease) are provided. The treatment including administering to a subject an indatraline derivative that inhibits the aggregation of ?-synuclein.
    Type: Application
    Filed: September 12, 2008
    Publication date: November 18, 2010
    Applicant: LINK MEDICINE CORPORATION
    Inventors: Peter T. Lansbury, JR., Craig J. Justman
  • Patent number: 7799933
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R1, R2, R3, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: September 21, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
  • Publication number: 20100197657
    Abstract: The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents.
    Type: Application
    Filed: September 22, 2008
    Publication date: August 5, 2010
    Inventors: Ronald K. Chang, Christina Ng Di Marco, Scott D. Kuduk
  • Publication number: 20100189648
    Abstract: A hydrophobic binding pocket on ubiquitin-protein ligase E3 is described, and used in designing the inhibitors disrupting ubiquitin conjugating enzyme E2 and E3 interaction. Four types of inhibitors designed by using the binding pocket are provided, which can be used for cancer treatment.
    Type: Application
    Filed: November 1, 2007
    Publication date: July 29, 2010
    Inventors: Lan Huang, Li Xing