Unsaturated Carbocyclic Ring Attached Directly To The Quinoline Ring System By Nonionic Bonding (e.g., Quinophthalones, Etc.) Patents (Class 546/173)
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Patent number: 8394794Abstract: 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: GrantFiled: March 21, 2008Date of Patent: March 12, 2013Assignee: Regents of The University of MinnesotaInventors: Chengguo Xing, Jignesh Doshi
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Patent number: 8394827Abstract: 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: GrantFiled: July 18, 2008Date of Patent: March 12, 2013Assignees: Kowa Co., Ltd., National University Corporation Nagoya UniversityInventor: Akio Suzumura
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Publication number: 20130059885Abstract: 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: ApplicationFiled: November 1, 2012Publication date: March 7, 2013Applicant: CADILA HEALTHCARE LIMITEDInventor: Cadila Healthcare Limited
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Publication number: 20130053413Abstract: 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: ApplicationFiled: October 31, 2012Publication date: February 28, 2013Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventor: Nissan Chemical Industries, Ltd.
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Publication number: 20130043460Abstract: 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: ApplicationFiled: December 12, 2011Publication date: February 21, 2013Inventors: Chien-Hong CHENG, Fang-ly WU, Chin-Hsien CHEN, Hsiu-Yun TSAI, Lun-Chia HSU
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Patent number: 8378107Abstract: 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: GrantFiled: October 1, 2009Date of Patent: February 19, 2013Assignee: Panmira Pharmaceuticals, LLCInventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
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Publication number: 20130038515Abstract: 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: ApplicationFiled: April 19, 2011Publication date: February 14, 2013Applicant: CANON KABUSHIKI KAISHAInventors: Tomonari Horikiri, Hiroyuki Tomono, Jun Kamatani
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Publication number: 20130033416Abstract: An organic compound contains indacenodiperylene as the basic skeleton.Type: ApplicationFiled: August 1, 2012Publication date: February 7, 2013Applicant: CANON KABUSHIKI KAISHAInventors: Jun Kamatani, Naoki Yamada, Tetsuya Kosuge, Takayuki Horiuchi, Yosuke Nishide, Hirokazu Miyashita, Akihito Saitoh
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Patent number: 8367679Abstract: 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: GrantFiled: December 8, 2009Date of Patent: February 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
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Publication number: 20130029949Abstract: Disclosed are substituted quinolines of formula 1 wherein R1 and R2 are defined herein, the processing of making and using the same.Type: ApplicationFiled: July 20, 2012Publication date: January 31, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: 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
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Patent number: 8354429Abstract: Compounds of formula I: wherein R4, R6 and R7 are defined herein, are useful as inhibitors of HIV replication.Type: GrantFiled: September 11, 2008Date of Patent: January 15, 2013Assignee: 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
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Publication number: 20120316151Abstract: 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: ApplicationFiled: February 22, 2011Publication date: December 13, 2012Inventors: Nicholas D. Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan M. Ghergurovich, Terence John Kiesow, Cynthia A. Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20120309741Abstract: 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: ApplicationFiled: August 16, 2012Publication date: December 6, 2012Inventors: Pascal FURET, Diana GRAUS PORTA, Vito GUAGNANO
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Publication number: 20120302524Abstract: 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: ApplicationFiled: December 28, 2010Publication date: November 29, 2012Applicants: GENERAL INCORPORATED ASSOCIATION PHARMA VALLEY PROJECT SUPPORTING ORGANIZATION, PHARMA DESIGN, INC., KABUSHIKI KAISHA YAKULT HONSHA, KUMAMOTO HEALTH SCIENCE UNIVERSITY, SHIZUOKA PREFECTUREInventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
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Publication number: 20120302566Abstract: 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: ApplicationFiled: November 30, 2011Publication date: November 29, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Remko Bakker, Matthias Eckhardt, Dieter Hamprecht, Elke Langkopf, Holger Wagner
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Publication number: 20120292571Abstract: 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: ApplicationFiled: December 28, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GmbHInventors: Arne Buesing, Holger Heil, Teresa Mujica-Fernaud, Irina Martynova
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Patent number: 8309721Abstract: 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: GrantFiled: September 14, 2010Date of Patent: November 13, 2012Assignee: SanofiInventors: Jean-Marie Ruxer, Victor Certal, Marcel Alasia, Luc Bertin, Herve Minoux, Patrick Mailliet, Frank Halley, Maria Mendez-Perez
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Publication number: 20120270858Abstract: 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: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Publication number: 20120264732Abstract: 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: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im
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Publication number: 20120245200Abstract: 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: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Yoshio OHARA, Yasutaka Takada, Hiroo Matsumoto, Akihiro Yoshida
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Patent number: 8221737Abstract: 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: GrantFiled: June 15, 2010Date of Patent: July 17, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20120165534Abstract: 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: ApplicationFiled: May 3, 2010Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Nitinchandra D. Patel, Chris H. Senanayake, Wenjun Tang, Xudong Wei, Nathan K. Yee
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Publication number: 20120156255Abstract: 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: ApplicationFiled: December 16, 2011Publication date: June 21, 2012Inventors: Jaipal Singh, Nicolas Chronos
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Publication number: 20120149693Abstract: 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: ApplicationFiled: May 5, 2010Publication date: June 14, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Raymond G. Booth
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Patent number: 8198300Abstract: 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: GrantFiled: April 29, 2010Date of Patent: June 12, 2012Assignee: Universidad De ChileInventors: Ricardo B. Maccioni, Leonardo P Navarrete, Aurelio San Martin
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Patent number: 8193199Abstract: 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 LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: 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
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Publication number: 20120135249Abstract: Aromatic and aromatic/heteroaromatic molecular structures with controllable electron conducting properties are derived from the incorporation of electron active substituents in selective positions.Type: ApplicationFiled: February 8, 2012Publication date: May 31, 2012Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: ROGER HARQUAIL FRENCH, ROSS GETTY, SIMONA PERCEC
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Publication number: 20120101126Abstract: 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: ApplicationFiled: October 25, 2011Publication date: April 26, 2012Applicant: Nissan Chemical Industries Ltd.Inventors: Paul Adriaan Van Der Schaaf, Fritz Blatter, Martin Szelagiewicz, Kai-Uwe Schöning
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Publication number: 20120101127Abstract: 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: ApplicationFiled: October 13, 2011Publication date: April 26, 2012Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Mingwei Zhou
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Publication number: 20120095010Abstract: 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: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
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Publication number: 20120037892Abstract: 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: ApplicationFiled: January 20, 2010Publication date: February 16, 2012Applicant: LG CHEM, LTD.Inventors: Hye-Young Jang, Jae-Chol Lee, Jae-Soon Bae, Jeung-Gon Kim, Seong-So Kim, Chang-Hwan Kim
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Publication number: 20120025183Abstract: 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: ApplicationFiled: April 22, 2010Publication date: February 2, 2012Applicant: CANON KABUSHIKI KAISHAInventors: Jun Kamatani, Takayuki Horiuchi, Naoki Yamada, Akihito Saitoh
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Publication number: 20120022255Abstract: 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: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20120022080Abstract: 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: ApplicationFiled: March 31, 2010Publication date: January 26, 2012Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
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Publication number: 20120022102Abstract: 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: ApplicationFiled: January 19, 2011Publication date: January 26, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Shriprakash Dhar DWIVEDI, Dhimant Jasubhai PATEL, Alpesh Pravinchandra SHAH
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Publication number: 20120016129Abstract: 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: ApplicationFiled: January 18, 2010Publication date: January 19, 2012Applicant: MSN Laboratories LimitedInventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Maramreddy Sahadeva Reddy
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Publication number: 20120010241Abstract: 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: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: SANOFIInventors: Luc Bertin, Jean-Christophe Carry, Patrick Mailliet, Herve Minoux, Fabienne Pilorge, Jean-Marie Ruxer
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Publication number: 20120001161Abstract: 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: ApplicationFiled: March 25, 2010Publication date: January 5, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Yohei Nakano, Kazunori Sugimoto, Kazumasa Nagao, Daisaku Tanaka, Tsuyoshi Tominaga
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Publication number: 20110319624Abstract: 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: ApplicationFiled: September 7, 2011Publication date: December 29, 2011Applicant: Nissan Chemical Industries, Ltd.Inventors: Yoshio Ohara, Yasutaka Takada, Hiroo Matsumoto, Akihiro Yoshida
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Publication number: 20110319445Abstract: 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: ApplicationFiled: October 1, 2009Publication date: December 29, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Deborah Volkots
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Publication number: 20110306621Abstract: 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: ApplicationFiled: February 8, 2010Publication date: December 15, 2011Inventors: Isao Kinoyama, Takehiro Miyazaki, Yohei Koganemaru, Nobuyuki Shiraishi, Yuichiro Kawamoto, Takuya Washio
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Publication number: 20110306587Abstract: 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: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. ALLEN, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Publication number: 20110275811Abstract: 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: ApplicationFiled: July 20, 2011Publication date: November 10, 2011Applicant: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Xiaolin Hao, Xiao He, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20110274648Abstract: 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: ApplicationFiled: November 4, 2010Publication date: November 10, 2011Inventors: Rico Lavoie, John A. Bender, Zhong Yang, Makonen Belema, Omar D. Lopez, Qi Chen, Gan Wang, Piyasena Hewawasam
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Publication number: 20110269962Abstract: Process for the preparation of ?-ketoester synthetic intermediates useful in the preparation of statins, in particular Pitavastatin.Type: ApplicationFiled: April 22, 2011Publication date: November 3, 2011Applicant: DIPHARMA FRANCIS S.R.L.Inventors: Maurizio TADDEI, Evita BALDUCCI, Emanuele ATTOLINO, Simone MANTEGAZZA, Gianmaria DELL'ANNA
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Publication number: 20110269793Abstract: 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: ApplicationFiled: April 29, 2010Publication date: November 3, 2011Inventor: Ricardo MACCIONI
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Publication number: 20110263565Abstract: 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: ApplicationFiled: July 28, 2009Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Thomas Karner, Ulrich Reiser
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Patent number: 8034945Abstract: 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: GrantFiled: May 2, 2006Date of Patent: October 11, 2011Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Karstens, Pedro Manuel Grima Poveda
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Publication number: 20110230498Abstract: 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: ApplicationFiled: December 8, 2009Publication date: September 22, 2011Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
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Patent number: 8022218Abstract: 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: GrantFiled: May 2, 2006Date of Patent: September 20, 2011Assignee: N.V. OrganonInventors: Pedro Manuel Grima Poveda, Willem Frederik Johan Karstens, Cornelis Marius Timmers