Polycyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 546/276.7)
  • Publication number: 20110201580
    Abstract: The present invention relates to novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, methods of preparing such compounds, pharmaceutical compositions comprising them, combinations and therapeutic uses thereof. More particularly, the invention relates to glucocorticosteroids that are derivatives of pyrrolidine.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 18, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Eleonora GHIDINI, Andrea RIZZI, Andrea VIRDIS, Fabio RANCATI, Anna RENCUROSI
  • Publication number: 20110201590
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: August 25, 2009
    Publication date: August 18, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20110195986
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
    Type: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Guohua Zhao, William N. Washburn, James J. Mignone
  • Publication number: 20110193074
    Abstract: The present invention relates to a novel compound and an organic light emitting device using the compound, and the compound according to the present invention may largely improve a life span, efficiency, electrochemical stability and thermal stability of the organic light emitting device.
    Type: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Dae-Woong Lee, Sung-Kil Hong, Tae-Yoon Park, Yeon-Hwan Kim, Seong-So Kim
  • Publication number: 20110189127
    Abstract: The present invention relates to Tricyclic Indole Derivatives, compositions comprising at least one Tricyclic Indole Derivatives, and methods of using the Tricyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: June 10, 2009
    Publication date: August 4, 2011
    Inventors: Srikanth Venkatraman, Anilkumar Gopinadhan Nair, Kevin X. Chen, Francisco Valazquez, Qingbei Zeng, Duan Liu, Yueheng Jiang, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Stephen J. Gavalas, Patrick A. Pinto, Oleg B. Selyutin, Bancha Vibulbhan
  • Publication number: 20110166169
    Abstract: The invention relates to the novel substances in Formula (I): wherein Het is a heterocycle optionally substituted by one or a plurality of radicals R1 or R?1; R is selected from the group comprising Formula (A?), (B), (C), (D), or (E), with R1 and/or R?1 selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxyl, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalcoxy, alkylhio, or carboxy that is free or esterified by an alkyl, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—S02-alkyl, S(0)2-NHalkyl, or S(02)-N(alkyl)2 radical; all these radicals are optionally substituted; W1, W2, and W3 independently are CH or N; X is 0, S, NR2, C(O), S(O), or S(0)2; Z is optionally substituted H, Hal, -0-R2 or —NH—R2 with R2 being H, alkyl, cycloalkyl, or heterocycloalkyl; and these substances are all isomeric forms and salts thereof, used as drugs.
    Type: Application
    Filed: September 14, 2010
    Publication date: July 7, 2011
    Applicant: sanofi-aventis
    Inventors: Jean-Marie RUXER, Victor CERTAL, Marcel ALASIA, Luc BERTIN, Herve MINOUX, Patrick MAILLIET, Frank HALLEY, Maria MENDEZ-PEREZ
  • Publication number: 20110160243
    Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.
    Type: Application
    Filed: August 26, 2009
    Publication date: June 30, 2011
    Applicant: Arena Pharmaceuticals ,Inc.
    Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
  • Publication number: 20110152306
    Abstract: The present application relates to indole and indoline derivatives of formula (I) wherein a, R1, R2, R3, h, i, j, m, n, L, Q, and X are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.
    Type: Application
    Filed: December 14, 2010
    Publication date: June 23, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Lei Shi, William H. Bunnelle, Tao Li, Marc J. Scanio, Michael R. Schrimpf, Chih-Hing Lee
  • Patent number: 7956082
    Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: June 7, 2011
    Assignee: Shionogi & Co., Ltd
    Inventors: Akira Kugimiya, Michitaka Shichijo, Yoshiharu Hiramatsu, Natsuki Ishizuka
  • Publication number: 20110130400
    Abstract: The present invention relates to diazabicyclo[2.2.1]hept-2-yl analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
    Type: Application
    Filed: July 24, 2009
    Publication date: June 2, 2011
    Inventors: Michael Jonathan Bury, Mui Cheung, Hilary Schenck Eidam, Ryan Michael Fox, Krista Goodman, Eric Steven Manas
  • Publication number: 20110130409
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: June 2, 2011
    Applicant: ARENA PHARMACEUTICALS, INC.
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
  • Patent number: 7947256
    Abstract: This invention relates to new carbocyanine fluorophores comprising a biomolecule targeting moiety containing 1-6 aromatic moieties, wherein the targeting moiety is designed to attach to biocompatible molecules to form in vivo optical imaging agents.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: May 24, 2011
    Assignee: VisEn Medical, Inc.
    Inventors: Milind Rajopadhye, Kevin Groves
  • Publication number: 20110111162
    Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In formula (I), ring A is a benzene ring, etc.; ring B is a 5- or 6-membered heterocyclic ring; R1 is a group of general formula (II), etc.; R2 is an organic group having 1 to 30 carbon atoms, etc.; Y1 is an alkyl group having 1 to 10 carbon atoms, etc.; Z1 and Z2 are each, e.g., an alkyl group having 1 to 8 carbon atoms optionally substituted with a halogen atom and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq? is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.
    Type: Application
    Filed: September 26, 2008
    Publication date: May 12, 2011
    Applicant: ADEKA CORPORATION
    Inventors: Toru Yano, Yohei Aoyama
  • Publication number: 20110101312
    Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
    Type: Application
    Filed: December 21, 2009
    Publication date: May 5, 2011
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Daniel David LeCloux, Kalindi Dogra, Weishi Wu, Adam Fenninmore, Eric Maurice Smith
  • Publication number: 20110105474
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; R1 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1 C6 haloalkoxy; R2, R3 are, independently, hydrogen; C1-C6 alkyl; aryl; or taken together with the carbon atoms to which they are bound form a bridged bicyclic ring or a fused heterocycle; X is CH or nitrogen; Y is a bond, oxygen, (CH2)mCR4R5(CH2)n, or (CH2)oNR6(CH2)p; m, n, o, p, R4, R5 and R6 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: June 8, 2009
    Publication date: May 5, 2011
    Inventors: Florian Thaler, Mario Varasi, Stefania Gagliardi, Andrea Colombo, Saverio Minucci, Ciro Mercurio
  • Patent number: 7928105
    Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R31, u, and X are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: April 19, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
  • Patent number: 7923129
    Abstract: Provided is an organic light emitting device including: a pair of electrodes including an anode and a cathode; and at least one layer formed of an organic compound interposed between the pair of electrodes, in which the at least one layer formed of the organic compound layer contains at least one kind of the carbazole derivative represented by the following general formula (I). The organic light emitting device has an optical output with extremely high efficiency and a high luminance and has an extremely high durability.
    Type: Grant
    Filed: November 28, 2007
    Date of Patent: April 12, 2011
    Assignee: Canon Kabushiki Kaisha
    Inventors: Satoshi Igawa, Shinjiro Okada, Takao Takiguchi, Jun Kamatani
  • Publication number: 20110071180
    Abstract: The present invention relates to compounds of the following formula (I) that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
    Type: Application
    Filed: March 4, 2009
    Publication date: March 24, 2011
    Applicant: Targacept, Inc.
    Inventors: Srinivasa Rao Akireddy, Balwinder Singh Bhatti, Scott R. Breining, Philip S. Hammond, Ronald Joseph Heemstra, Anatoly A. Mazurov, Matt S. Melvin, Lan Miao, V. Srinivasa Murthy, Jon-Paul Strachan, Yunde Xiao
  • Publication number: 20110061723
    Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.
    Type: Application
    Filed: February 26, 2009
    Publication date: March 17, 2011
    Applicant: BASF SE
    Inventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
  • Patent number: 7902371
    Abstract: The present invention relates to the salt (1S,5S)-3-(5,6-dichloropyridin-3-yl)-3,6-diazabicyclo[3.2.0]heptane benzenesulfonate and to methods of preparing the salt.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: March 8, 2011
    Assignee: Abbott Laboratories
    Inventors: Gregory S. Wayne, Sean M. Mellican, Geoff G. Z. Zhang, David R. Willcox, Jeffrey M. Breting
  • Publication number: 20110039855
    Abstract: The present invention provides a compound of the Formula (I), or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, particularly reduced bone mass, osteoporosis, osteopenia, reduced muscle mass or strength, or erectile dysfunction comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: May 14, 2009
    Publication date: February 17, 2011
    Applicant: ELI LILLY AND COMPANY
    Inventors: Prabhakar Kondaji Jadhav, Venkatesh Krishnan, Euibong Jemes Kim
  • Publication number: 20110034434
    Abstract: The invention relates to prodrugs of fused heterocyclic inhibitors of D-amino oxidase (DAAO) and methods of treating diseases and conditions, wherein modulation of D-amino acid oxidase activity, D-serine levels, D-serine oxidative products and NMDA receptor activity in the nervous system of a mammalian subject is effective.
    Type: Application
    Filed: August 6, 2010
    Publication date: February 10, 2011
    Applicant: SEPRACOR INC.
    Inventors: Michele L. R. Heffernan, Richard Dennis, James M. Dorsey, Robert J. Foglesong, Michael L. Jones, Cyprian O. Ogbu, Mustapha Soukri, Kerry L. Spear, Michael A. Orsini
  • Publication number: 20110024725
    Abstract: The present invention relates to a novel anthracene derivative and an organic electronic device using the same. The organic electronic device according to the present invention shows excellent characteristics in efficiency, driving voltage, and life time.
    Type: Application
    Filed: May 16, 2008
    Publication date: February 3, 2011
    Inventors: Dong-Hoon Lee, Jae-Chol Lee, Jae-Soon Bae, Jun-Gi Jang, Kong-Kyeom Kim, Dae-Woong Lee
  • Publication number: 20110021490
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.
    Type: Application
    Filed: July 20, 2010
    Publication date: January 27, 2011
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Guillaume De Nanteuil, Bernard Cimetiere, Anne Dekeyne, Mark Millan
  • Publication number: 20110015235
    Abstract: This invention relates to novel phenylethynyl derivatives of 8-aza-bicyclo[3.2.1]octane useful as monoamine neurotransmitter re-uptake inhibitors. 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: February 4, 2009
    Publication date: January 20, 2011
    Inventors: Dan Peters, John Paul Redrobe, Elsebet Østergaard Nielsen
  • Patent number: 7872010
    Abstract: Provided herein are compositions of a class of substituted diazabicycloalkane derivative compounds, which are useful as modulators of nicotinic acetylcholine receptors. The compounds are useful in treating conditions and disorders prevented by, or ameliorated by, nicotinic acetylcholine receptors.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: January 18, 2011
    Assignee: Abbott Laboratories
    Inventors: Jennifer M. Frost, Jianguo Ji, Tao Li, Diana L. Nersesian, Karin R. Tietje
  • Publication number: 20110009456
    Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
    Type: Application
    Filed: December 21, 2009
    Publication date: January 13, 2011
    Applicant: Siga Technologies Inc.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
  • Publication number: 20110009386
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.
    Type: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts, Nicholas S. Flinn
  • Publication number: 20110009385
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: R3 is selected from cyclopentyl and cyclohexyl; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high dual efficacies for human cathepsin S and K and are useful for the treatment of rheumatoid arthritis, osteoarthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, cardiovascular diseases which exhibit significant damage and remodeling of extracellular matrix (ECM) and chronic pain.
    Type: Application
    Filed: August 9, 2010
    Publication date: January 13, 2011
    Applicant: Amura Therapeutics Limited
    Inventors: MARTIN QUIBELL, John P. Watts, Nicholas S. Flinn
  • Publication number: 20110003849
    Abstract: Compounds of the formula: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating diabetes, inflammation, atherosclerosis, hypertension, pain and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: February 24, 2009
    Publication date: January 6, 2011
    Inventors: Hong Shen, Fa-Xiang Ding, Steven L. Colletti
  • Publication number: 20110003737
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Application
    Filed: July 1, 2010
    Publication date: January 6, 2011
    Applicant: ALBANY MOLECULAR RESEARCH, INC.
    Inventors: Peter R. GUZZO, Matthew David SURMAN, Alan John HENDERSON, Mark HADDEN, Emily Elizabeth FREEMAN
  • 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
  • Publication number: 20100331324
    Abstract: Disclosed are fused heterocyclic compounds of Formula (I) or pharmaceutically-acceptable salts or stereoisomers thereof. Also disclosed are methods of using such compounds in the treatment of at least one androgen receptor-associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: June 26, 2008
    Publication date: December 30, 2010
    Inventors: Derek J. Norris, Ashvinikumar V. Gavai, James Aaron Balog, Joel F. Austin, Weifang Shan, Yufen Zhao, Andrew James Nation, Wen-Ching Han
  • Publication number: 20100331509
    Abstract: This invention relates generally to norbornene-monomer, poly(norbornene)homopolymer, and poly(norbornene)copolymer compounds containing a functionalized carbazole side chain, having desirable solution processability and host characteristics. It also relates to hole transport and/or electron blocking materials, and to organic host materials for an organic luminescence layer, an OLED device, and compositions of matter which include these compounds.
    Type: Application
    Filed: December 19, 2008
    Publication date: December 30, 2010
    Applicant: GEORGIA TECH RESEARCH CORPORATION
    Inventors: Yadong Zhang, Seth Marder, Carlos Zuniga, Stephen Barlow, Bernard Kippelen, Andreas Haldi, Benoit Domerq, Marcus Weck, Alpay Kimyonok
  • Publication number: 20100322901
    Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: December 17, 2007
    Publication date: December 23, 2010
    Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
  • Publication number: 20100304074
    Abstract: A novel indolium compound of general formula (I) and an optical recording material containing the indolium compound. In general formula (I), ring A is a benzene ring, etc.; R1 is a group of general formula (II), etc.; R2 is a C1-C30 organic group, etc.; Y1 is a C1-C10 alkyl group, etc.; Z1 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; Z2 is, e.g., a C1-C8 alkyl group optionally substituted with a halogen group and optionally interrupted by —O—, etc.; a is an integer of 0 to 6; b is an integer of 0 to 5; Anq- is a q-valent anion; q is 1 or 2; and p is a number necessary to neutralize an electric charge.
    Type: Application
    Filed: September 26, 2008
    Publication date: December 2, 2010
    Applicant: ADEKA CORPORATION
    Inventors: Toru Yano, Yohei Aoyama
  • Patent number: 7837784
    Abstract: The present invention relates to C. I. Pigment Red 254 for coloring, which can color an object to be colored so as to have a higher chroma than that with conventional technology and a production method for easily producing it. For the purpose, the inventors provide the production method for the pigment, wherein the intersection of mass tone ?H* and ?C* of a color coating film in an acrylic-melamine coating test is, on X-Y coordinate plane to which the ?H* is defined as the X-axis and the ?C* is defined as the Y-axis, within the surrounded region determined by specific three equations; and a production method for the pigment provides the production method of the pigment, including a process of heating crude pigment at 100-130° C. for 2-10 hours in an aprotic polar organic solvent which is strongly alkaline.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: November 23, 2010
    Assignee: DIC Corporation
    Inventors: Hirotsugu Nemoto, Shousaburou Tanaka, Takashi Sato
  • Patent number: 7834187
    Abstract: The present invention relates to a crystalline variable hydrate of (S)-(3-pyridinecarboxamide,6-[4-[2-[[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy]) -hemi-succinate, a pharmaceutical formulation containing said salt and to methods for treating obesity and/or Type 2 diabetes using said salt.
    Type: Grant
    Filed: July 14, 2005
    Date of Patent: November 16, 2010
    Assignee: Eli Lilly and Company
    Inventor: Julie Kay Bush
  • Publication number: 20100286119
    Abstract: The invention concerns compounds of general formula (I): Wherein n, X1, X2, X3, X4, Y, Z, Z1, Z2, Z3 and Z4 are as defined herein. The invention also concerns a process for the preparation of compounds of formula (I) and their therapeutic use.
    Type: Application
    Filed: July 19, 2010
    Publication date: November 11, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Laurent DUBOIS, Yannick EVANNO, Andre MALANDA, David MACHNIK, Catherine GILLE
  • Publication number: 20100286209
    Abstract: The present invention provides vinyl indazolyl compounds useful in the treatment of cancer.
    Type: Application
    Filed: May 4, 2010
    Publication date: November 11, 2010
    Inventors: Daohong Chen, Hong-Yu Li, Genshi Zhao
  • Patent number: 7812021
    Abstract: The invention relates to a compound of general formula wherein Ar, R1, R2, R3, R4, n, o, p, s, X and are as defined herein or to a pharmaceutically active salt thereof, including all stereoisomeric forms, individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. The compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: October 12, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer, Xihan Wu
  • Publication number: 20100256144
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Application
    Filed: June 26, 2008
    Publication date: October 7, 2010
    Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
  • Publication number: 20100256192
    Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 29, 2009
    Publication date: October 7, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Publication number: 20100227892
    Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
    Type: Application
    Filed: April 1, 2010
    Publication date: September 9, 2010
    Applicant: Siga Technologies Inc.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
  • Patent number: 7786125
    Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: April 7, 2009
    Date of Patent: August 31, 2010
    Inventor: Leu-Fen H. Lin
  • Publication number: 20100213826
    Abstract: A material for an organic photoelectric device, the material including a compound represented by the following Chemical Formula 1: wherein, in Chemical Formula 1, HTU and HTU? are independently hole transporting units, and R1 to R3 are independently a substituent selected from the group of hydrogen, a substituted or unsubstituted C6 to C30 aryl, a substituted or unsubstituted C2 to C30 heteroaryl, and a substituted or unsubstituted C1 to C30 alkyl, wherein the term “substituted” refers to one substituted with a halogen, a C1 to C30 alkyl, a C1 to C30 haloalkyl, a C6 to C30 aryl, a C2 to C30 heteroaryl, a C1 to C20 alkoxy, or combinations thereof.
    Type: Application
    Filed: May 3, 2010
    Publication date: August 26, 2010
    Inventors: Young-Hoon Kim, Eun-Sun Yu, Nam-Soo Kim, Mi-Young Chae
  • Publication number: 20100216833
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.
    Type: Application
    Filed: May 6, 2010
    Publication date: August 26, 2010
    Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
  • Patent number: 7781431
    Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Grant
    Filed: September 7, 2004
    Date of Patent: August 24, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
  • Patent number: 7767193
    Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.
    Type: Grant
    Filed: June 20, 2005
    Date of Patent: August 3, 2010
    Assignee: Targacept, Inc.
    Inventors: Anatoly A. Mazurov, Lan Miao
  • Publication number: 20100187977
    Abstract: Provided is an organic electroluminescent device (organic EL device) that is improved in luminous efficiency, fully secured of driving stability, and simply constructed. The EL device has a light-emitting layer disposed between an anode and a cathode stacked one upon another on a substrate and the light-emitting layer comprises a phosphorescent dopant and an indolocarbazole derivative as a host material. Examples of the indolocarbazole compounds include a compound represented by the following formula (2) or (3), wherein X is N or CH, at least one of Xs is N, and Ar1 to Ar3 each is a substituted or unsubstituted aromatic group.
    Type: Application
    Filed: November 8, 2007
    Publication date: July 29, 2010
    Applicant: NIPPON STEEL CHEMICAL CO., LTD.
    Inventors: Takahiro Kai, Masaki Komori, Toshihiro Yamamoto