Unsaturated Carbocyclic Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding (e.g., Quinophthalones, Etc.) Patents (Class 546/173)
  • Patent number: 8394794
    Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: March 12, 2013
    Assignee: Regents of The University of Minnesota
    Inventors: Chengguo Xing, Jignesh Doshi
  • Patent number: 8394827
    Abstract: The present invention is to provide an inhibitor that inhibits differentiation of T cells into Th1 cells. The inhibitor that inhibits differentiation of T cells into Th1 cells contains, as an active ingredient, pitavastatin or a salt thereof.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: March 12, 2013
    Assignees: Kowa Co., Ltd., National University Corporation Nagoya University
    Inventor: Akio Suzumura
  • Publication number: 20130059885
    Abstract: The present invention discloses a compound, which is alkali or alkaline earth metal salts of pitavastatin, wherein the alkali or earth metal comprise one or more of magnesium, zinc, potassium, strontium and barium.
    Type: Application
    Filed: November 1, 2012
    Publication date: March 7, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventor: Cadila Healthcare Limited
  • Publication number: 20130053413
    Abstract: The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous forms.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 28, 2013
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventor: Nissan Chemical Industries, Ltd.
  • Publication number: 20130043460
    Abstract: Disclosed is a carbazole serial compound, having a general formula as: wherein X is selected from a halogen atom, a cyano group, a substituted or non-substituted C1-40 alkyl group, a substituted or non-substituted C2-40 alkenyl group, a substituted or non-substituted C2-40 alkynyl group, a substituted or non-substituted C6-40 aryl group, a substituted or non-substituted C4-40 hetero aryl group, a substituted or non-substituted C6-40 aryl amino group, or a substituted or non-substituted C1-40 alkyl amino group. Each R is independently selected from a hydrogen atom, a cyano group, a substituted or non-substituted C1-40 alkyl group, a substituted or non-substituted C2-40 alkenyl group, a substituted or non-substituted C2-40 alkynyl group, a substituted or non-substituted C6-40 aryl group, a substituted or non-substituted C4-40 hetero aryl group, a substituted or non-substituted C6-40 aryl amino group, or a substituted or non-substituted C1-40 alkyl amino group.
    Type: Application
    Filed: December 12, 2011
    Publication date: February 21, 2013
    Inventors: Chien-Hong CHENG, Fang-ly WU, Chin-Hsien CHEN, Hsiu-Yun TSAI, Lun-Chia HSU
  • Patent number: 8378107
    Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: February 19, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
  • Publication number: 20130038515
    Abstract: There is provided a novel organic compound suitably used for a blue light-emitting device and an organic light-emitting device including the novel organic compound. The organic compound is an acephenanthryleno[4,5-k]benzo[e]acephenanthrylene derivative.
    Type: Application
    Filed: April 19, 2011
    Publication date: February 14, 2013
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Tomonari Horikiri, Hiroyuki Tomono, Jun Kamatani
  • Publication number: 20130033416
    Abstract: An organic compound contains indacenodiperylene as the basic skeleton.
    Type: Application
    Filed: August 1, 2012
    Publication date: February 7, 2013
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Jun Kamatani, Naoki Yamada, Tetsuya Kosuge, Takayuki Horiuchi, Yosuke Nishide, Hirokazu Miyashita, Akihito Saitoh
  • Patent number: 8367679
    Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
  • Publication number: 20130029949
    Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.
    Type: Application
    Filed: July 20, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias HOFFMANN, Daniel BISCHOFF, Georg DAHMANN, Jasna KLICIC, Gerhard SCHAENZLE, Stefan Ludwig Michael WOLLIN, Serge Gaston CONVERS-REIGNIER, Stephen Peter EAST, Frederic Jacques MARLIN, Clive McCARTHY, John SCOTT
  • Patent number: 8354429
    Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: January 15, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Youla S. Tsantrizos, Murray D. Bailey, Francois Bilodeau, Rebekah J. Carson, Rene Coulombe, Lee Fader, Teddy Halmos, Stephen Kawai, Serge Landry, Steven LaPlante, Sebastien Morin, Mathieu Parisien, Marc-Andre Poupart, Bruno Simoneau
  • Publication number: 20120316151
    Abstract: This invention relates to the use of triazolone derivatives of Formula (I) for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
    Type: Application
    Filed: February 22, 2011
    Publication date: December 13, 2012
    Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan M. Ghergurovich, Terence John Kiesow, Cynthia A. Parrish, Alexander Joseph Reif, Kenneth Wiggall
  • Publication number: 20120309741
    Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Inventors: Pascal FURET, Diana GRAUS PORTA, Vito GUAGNANO
  • Publication number: 20120302524
    Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
    Type: Application
    Filed: December 28, 2010
    Publication date: November 29, 2012
    Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTURE
    Inventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
  • Publication number: 20120302566
    Abstract: The present invention relates to compounds defined by formula (I) wherein the variables R1, R2, R3, m, and n are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are activators of the receptor GPR40 and thus are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Application
    Filed: November 30, 2011
    Publication date: November 29, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
  • Publication number: 20120292571
    Abstract: The present invention relates to coordination compounds which are used in an electron-transport layer in electronic devices, to ligands, and to the use thereof for the preparation of metal complexes, to a layer, and to an electronic device which comprise the compounds according to the invention, and to a process for the preparation of the compounds according to the invention.
    Type: Application
    Filed: December 28, 2010
    Publication date: November 22, 2012
    Applicant: MERCK PATENT GmbH
    Inventors: Arne Buesing, Holger Heil, Teresa Mujica-Fernaud, Irina Martynova
  • Patent number: 8309721
    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: Grant
    Filed: September 14, 2010
    Date of Patent: November 13, 2012
    Assignee: Sanofi
    Inventors: Jean-Marie Ruxer, Victor Certal, Marcel Alasia, Luc Bertin, Herve Minoux, Patrick Mailliet, Frank Halley, Maria Mendez-Perez
  • Publication number: 20120270858
    Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.
    Type: Application
    Filed: June 9, 2010
    Publication date: October 25, 2012
    Applicant: CALIFORNIA CAPITAL EQUITY, LLC
    Inventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
  • Publication number: 20120264732
    Abstract: The present invention relates to novel phenyl bicyclic methyl azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 18, 2012
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
  • Publication number: 20120245200
    Abstract: A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Yoshio OHARA, Yasutaka Takada, Hiroo Matsumoto, Akihiro Yoshida
  • Patent number: 8221737
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20120165534
    Abstract: Disclosed are methods for the preparation of bromo-substituted quinolines of the formula (I) where R is aryl, heteroaryl, alkyl, alkenyl or alkynyl, which are useful as intermediates in the preparation of agents for the treatment of hepatitis C viral (HCV) infections: Formula (I).
    Type: Application
    Filed: May 3, 2010
    Publication date: June 28, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Nitinchandra D. Patel, Chris H. Senanayake, Wenjun Tang, Xudong Wei, Nathan K. Yee
  • Publication number: 20120156255
    Abstract: A polymeric matrix for delivery of an HMG CoA reductase inhibitor such as a statin to tissue such as cardiac tissue in need thereof for the treatment or prevention of a disease or defect such as atrial fibrillation has been developed. In the preferred embodiment, a statin is delivered by means of a patch sutured to cardiac tissue at the time of cardiothoracic surgery. In the most preferred embodiment, the patch is a biodegradable material providing controlled or sustained release over a prolonged period of time, such as a week. Suitable materials include extracellular matrix, or other biodegradable hydrogels or polymeric materials providing sustained or controlled release of statin at the site of application.
    Type: Application
    Filed: December 16, 2011
    Publication date: June 21, 2012
    Inventors: Jaipal Singh, Nicolas Chronos
  • Publication number: 20120149693
    Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.
    Type: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Patent number: 8198300
    Abstract: Method for the prevention of the tau protein aggregation and treating Alzheimer's disease by administering a quinoline derivative compound of formula wherein R2 is 2-(4-aminophenyl) or 2-(4-methylphenyl) and R6 is methyl as an inhibitor of the tau protein aggregation.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: June 12, 2012
    Assignee: Universidad De Chile
    Inventors: Ricardo B. Maccioni, Leonardo P Navarrete, Aurelio San Martin
  • Patent number: 8193199
    Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemi
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: June 5, 2012
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20120135249
    Abstract: Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions.
    Type: Application
    Filed: February 8, 2012
    Publication date: May 31, 2012
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: ROGER HARQUAIL FRENCH, ROSS GETTY, SIMONA PERCEC
  • Publication number: 20120101126
    Abstract: The present invention is directed to new crystalline forms of Pitavastatin hemicalcium salt, referred to hereinafter as polymorphic Forms A, B, C, D, E and F, as well as the amorphous form. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and the amorphous form and pharmaceutical compositions comprising these crystalline forms or the amorphous form.
    Type: Application
    Filed: October 25, 2011
    Publication date: April 26, 2012
    Applicant: Nissan Chemical Industries Ltd.
    Inventors: Paul Adriaan Van Der Schaaf, Fritz Blatter, Martin Szelagiewicz, Kai-Uwe Schöning
  • Publication number: 20120101127
    Abstract: The present invention relates to compounds according to formula (I) and pharmaceutically acceptable salts or esters thereof, wherein R1 to R7 have the significance given herein. The compounds are activators of AMP-activated protein kinase (AMPK) and are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.
    Type: Application
    Filed: October 13, 2011
    Publication date: April 26, 2012
    Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Mingwei Zhou
  • Publication number: 20120095010
    Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
  • Publication number: 20120037892
    Abstract: The present invention relates to a novel cycloalkene derivative, and an organic electronic device using the same. The cycloalkene derivative according to the exemplary embodiment of the present invention may act as a hole injection, a hole transport, an electron injection, an electron transport, or a light emitting material in an organic light emitting diode and an organic electronic device, and in particular, may be used alone as a light emitting host or a dopant.
    Type: Application
    Filed: January 20, 2010
    Publication date: February 16, 2012
    Applicant: LG CHEM, LTD.
    Inventors: Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Jeung-Gon Kim, Seong-So Kim, Chang-Hwan Kim
  • Publication number: 20120025183
    Abstract: Provided is an acenaphtho[1,2-k]benzo[e]acephenanthrene derivative represented by general formula (1): wherein R1 to R16 are each independently selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group; and at least one of R1 to R8 and R10 to R15 is selected from a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group.
    Type: Application
    Filed: April 22, 2010
    Publication date: February 2, 2012
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Jun Kamatani, Takayuki Horiuchi, Naoki Yamada, Akihito Saitoh
  • Publication number: 20120022255
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: March 23, 2010
    Publication date: January 26, 2012
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Publication number: 20120022080
    Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.
    Type: Application
    Filed: March 31, 2010
    Publication date: January 26, 2012
    Applicant: RENASCIENCE CO., LTD.
    Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
  • Publication number: 20120022102
    Abstract: The present invention discloses a compound, which is alkali or alkaline earth metal salts of pitavastatin, wherein the alkali or earth metal comprise one or more of magnesium, zinc, potassium, strontium and barium.
    Type: Application
    Filed: January 19, 2011
    Publication date: January 26, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar DWIVEDI, Dhimant Jasubhai PATEL, Alpesh Pravinchandra SHAH
  • Publication number: 20120016129
    Abstract: Processes for preparing pravastatin, intermediates and pharmaceutically acceptable salts thereof are provided Crystalline forms of pravastatin, intermediates and pharmaceutically acceptable salts thereof are also disclosed.
    Type: Application
    Filed: January 18, 2010
    Publication date: January 19, 2012
    Applicant: MSN Laboratories Limited
    Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Maramreddy Sahadeva Reddy
  • Publication number: 20120010241
    Abstract: The invention relates to novel products having formula (I), wherein: R4 represents H, CH3, CH2CH3, CF3, F, Cl, Br, I; Het represents a heterocycle optionally substituted by one or more R1 or R?1 radicals selected from H, halogen, CF3, nitro, cyano, alkyl, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, phenylalkoxy, alkylthio, carboxy that is free or sterified with an alkyl radical, carboxamide, CO—NH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, S(O2)-N(alkyl)2, all of the alkyl, alkoxy and alkylthio radicals being optionally substituted; R being selected from the group comprising (A?), (B), (C), (D) and (F), wherein W1, W2, W3 represent independently CH or N, X represents O, S, NR2, C(O), S(O) or S(O)2; V represents H, Hal, —O—R2 or —NH—R2 with R2 representing H, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted; said products being in all isomer forms, as well as the salts and intended for use as drugs.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 12, 2012
    Applicant: SANOFI
    Inventors: Luc Bertin, Jean-Christophe Carry, Patrick Mailliet, Herve Minoux, Fabienne Pilorge, Jean-Marie Ruxer
  • Publication number: 20120001161
    Abstract: Disclosed is an organic electroluminescent element which has achieved both high luminous efficiency and low driving voltage by containing a light-emitting element material, which comprises a specific pyrene compound, in one of the layers that constitute the light-emitting element, preferably in a light-emitting layer or in an electron-transporting layer.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 5, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Yohei Nakano, Kazunori Sugimoto, Kazumasa Nagao, Daisaku Tanaka, Tsuyoshi Tominaga
  • Publication number: 20110319624
    Abstract: A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.
    Type: Application
    Filed: September 7, 2011
    Publication date: December 29, 2011
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Yoshio Ohara, Yasutaka Takada, Hiroo Matsumoto, Akihiro Yoshida
  • Publication number: 20110319445
    Abstract: Described herein are heteroaryl compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: October 1, 2009
    Publication date: December 29, 2011
    Applicant: AMIRA PHARMACEUTICALS, INC.
    Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
  • 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: 20110306587
    Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 11, 2011
    Publication date: December 15, 2011
    Inventors: Jennifer R. ALLEN, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
  • Publication number: 20110275811
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.
    Type: Application
    Filed: July 20, 2011
    Publication date: November 10, 2011
    Applicant: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Xiaolin Hao, Xiao He, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20110274648
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: November 4, 2010
    Publication date: November 10, 2011
    Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
  • Publication number: 20110269962
    Abstract: Process for the preparation of ?-ketoester synthetic intermediates useful in the preparation of statins, in particular Pitavastatin.
    Type: Application
    Filed: April 22, 2011
    Publication date: November 3, 2011
    Applicant: DIPHARMA FRANCIS S.R.L.
    Inventors: Maurizio TADDEI, Evita BALDUCCI, Emanuele ATTOLINO, Simone MANTEGAZZA, Gianmaria DELL'ANNA
  • Publication number: 20110269793
    Abstract: Method for the prevention of the tau protein aggregation and treating Alzheimer's disease by administering a quinoline derivative compound of formula wherein R2 is 2-(4-aminophenyl) or 2-(4-methylphenyl) and R6 is methyl as an inhibitor of the tau protein aggregation.
    Type: Application
    Filed: April 29, 2010
    Publication date: November 3, 2011
    Inventor: Ricardo MACCIONI
  • Publication number: 20110263565
    Abstract: The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: July 28, 2009
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Matthias Treu, Thomas Karner, Ulrich Reiser
  • Patent number: 8034945
    Abstract: The invention relates to a 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative according to Formula (I), wherein the substituents are defined as in the description, or a pharmaceutically salt thereof. The compounds of this invention are potent FSH receptor activators and may be used for treating fertility disorders in e.g. controlled ovarian hyperstimulation and IVF procedures.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: October 11, 2011
    Assignee: N.V. Organon
    Inventors: Cornelis Marius Timmers, Willem Frederik Karstens, Pedro Manuel Grima Poveda
  • Publication number: 20110230498
    Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Application
    Filed: December 8, 2009
    Publication date: September 22, 2011
    Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
  • Patent number: 8022218
    Abstract: The present invention relates to 4-phenyl-5-oxo-1,4)5,6,7,8-hexahydroquinoline derivatives according to Formula I, Formula I or a pharmaceutically acceptable salt thereof, wherein R1 is (1-6C)alkyl, (2-6C)alkenyl or (2-6C)aDcynyl; R2, R3 are independently halogen, (1-4C)allcyl, (2-4C)alkenyl, (2-4C)-alkynyl, (1-4C)aBcoxy, (3-4C)alkenyloxy or (3-4C)alkynyloxy; R4 is phenyl or (2-5C)-heteroaryl, both substituted with R7 and optionally substituted on the (hetero)aromatic ring with one or more substituents selected from hydroxy, amino, halogen, nitro, trifluoromethyl, cyano, (1-4C)alkyl, (1-4C)alkoxy, (1-4C)alkylthio and (di)(1-4C)-alkylamino. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these 4-phenyl-5-oxo-1,4,5,6,7,8-hexahydro-quinoline derivatives in therapy, more specifically for the treatment of infertility.
    Type: Grant
    Filed: May 2, 2006
    Date of Patent: September 20, 2011
    Assignee: N.V. Organon
    Inventors: Pedro Manuel Grima Poveda, Willem Frederik Johan Karstens, Cornelis Marius Timmers