The Additional Hetero Ring Is A Cyclo In A Polycyclo Ring System [e.g., 2-(1-isothiochromanyl)-2-imidazoline Hydrochloride, Etc.] Patents (Class 548/311.4)
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Publication number: 20130196987Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.Type: ApplicationFiled: October 30, 2012Publication date: August 1, 2013Applicant: EISAI CO., LTD.Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
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Patent number: 8497376Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: October 16, 2008Date of Patent: July 30, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Carl R. Illig, Jinsheng Chen, Sanath K. Meegalia, Mark J. Wall
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Publication number: 20130188270Abstract: Compounds of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 for example independently of each other are hydro-gen, C1-C20alkyl, (II), COR16 or NO2, provided that at least one pair of R1 and R2, R2 and R3, R3 and R4, R5 and R6, R6 and R7, or R7 and R8 is (III); R9, R10, R11 and R12 for example independently of each other are hydrogen, C1-C20alkyl which optionally substituted; or R9, R10, R11, and R12 independently of each other are unsubstituted or substituted phenyl; X is CO or a direct bond; R13 is for example C1-C20alkyl which optionally is substituted, C2-C12alkenyl, C4-C8cycloalkenyl, C2-C12alkinyl, C3-C10-cycloalkyl, phenyl or naphthyl both of which are optionally substituted; R14 is for example hydrogen, C3-C8cycloalkyl, C2-C5alkenyl, C1-C20alkoxy, C1-C20alkyl, phenyl or naphthyl; R15 is for example C6-C20aryl or C5-C20heteroaryl; R16 is for example C6-C20aryl which is unsubstituted or substituted by one or more C1-C20alkoxy or C1-C20alkyl; are in particular suitable as photoinitiators for cType: ApplicationFiled: October 4, 2011Publication date: July 25, 2013Applicant: BASF SEInventors: Yuichi Nishimae, Hisatoshi Kura, Kazuhiko Kunimoto, Ryuhei Yamagami, Keita Tanaka
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Publication number: 20130190338Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8481582Abstract: Compounds of formula I and a method for their preparation are described: where R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, nitro, amino, alkylcarbonylamino, alkylamino or dialkylamino group; R4 signifies -alkyl-aryl or -alkyl-heteroaryl; X signifies CH2, oxygen atom or sulphur atom; n is 2 or 3; including the individual (R)- and (S)-enantiomers or mixtures of enantiomers thereof; and including pharmaceutically acceptable salts and esters thereof. The compounds have potentially valuable pharmaceutical properties for the treatment of cardiovascular disorders such as hypertension and chronic heart failure.Type: GrantFiled: May 6, 2008Date of Patent: July 9, 2013Assignee: Bial-Portela & CA, S.A.Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, David Alexander Learmonth, Alexander Beliaev
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Publication number: 20130165489Abstract: The present invention includes a method of inhibiting, suppressing or preventing a viral infection in a subject, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds useful within the invention.Type: ApplicationFiled: April 25, 2011Publication date: June 27, 2013Applicants: The Trustees of the University of Pennsylvania, Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Simon Cocklin, Sandhya Kortagere, Amos B. Smith, III
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Publication number: 20130164218Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: EMORY UNIVERSITYInventor: EMORY UNIVERSITY
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Publication number: 20130165460Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8470863Abstract: In its many embodiments, the present invention provides a novel class of chroman compounds of formula I as ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of prepaxing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions. wherein J is: Z is —[C(Rc)(Rc)]x—, where x is 1, 2, or 3.Type: GrantFiled: February 11, 2008Date of Patent: June 25, 2013Assignee: Merck Sharp & Dohme, Corp.Inventors: Junying Zheng, Kevin D. McCormick, Jianhua Chao, Christopher W. Boyce, Robert G. Aslanian, Younong Yu
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Publication number: 20130116232Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: ApplicationFiled: June 8, 2011Publication date: May 9, 2013Applicant: ARAGON PHARMACEUTICALS, INC.Inventors: Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Nicholas D. Smith
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MATERIAL FOR ORGANIC ELECTROLUMINESCENCE ELEMENT, AND ORGANIC ELECTROLUMINESCENCE ELEMENT USING SAME
Publication number: 20130092905Abstract: Provided is a material for an organic electroluminescence device, which further has a bulky carbazolyl group at each of the 3-position and 6-position of its central carbazole skeleton, and which has a dibenzofuran skeleton or a dibenzothiophene skeleton at the N atom of the central carbazole skeleton through a linking group as required. Also provided is an organic electroluminescence device, including one or more organic thin film layers including a light emitting layer between a cathode and an anode, in which at least one layer of the organic thin film layers contains the material for an organic electroluminescence device.Type: ApplicationFiled: February 14, 2011Publication date: April 18, 2013Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Masaki Numata, Hideaki Nagashima -
Publication number: 20130065897Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.Type: ApplicationFiled: December 22, 2010Publication date: March 14, 2013Applicant: PETER MACCALLUM CANCER INSTITUTEInventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
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Publication number: 20130032788Abstract: A carbazole-based compound of Formula 1 and an organic light-emitting diode including the same. The carbazole-based compound represented by Formula 1 has a triarylamine structure, wherein at least one of R1 to R5 is essentially a nitrogen-containing group. Thus, the carbazole-based compound has high glass transition temperature and/or high melting point, and is stable during electron injection, and when interposed between a pair of electrodes (anode and cathode) of an organic light-emitting diode, the carbazole-based compound may have excellent thermal resistance against Joule's heat generated in organic layers between the pair of electrodes, between the organic layers, or between the organic layer and the electrode during an operation of the organic light-emitting diode.Type: ApplicationFiled: January 31, 2012Publication date: February 7, 2013Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.Inventors: Sun-Young Lee, Yoon-Hyun Kwak, Bum-Woo Park, Dae-Yup Shin, Kwan-Hee Lee, Hye-In Jeong, Sam-Il Kho, Mie-Hwa Park
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Publication number: 20130035323Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Abbott GmbH & Co. KGInventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
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Publication number: 20130012532Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.Type: ApplicationFiled: March 14, 2011Publication date: January 10, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Tsutomu Nagata, Jun Kobayashi, Yoshiyuki Onishi, Masamichi Kishida, Kengo Noguchi
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Publication number: 20120328569Abstract: Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: March 2, 2011Publication date: December 27, 2012Inventors: Casey Cameron McComas, Nigel J. Liverton, Richard Soll, Peng Li, Xuanjia Peng, Hao Wu, Frank Narjes, Joerg Habermann, Uwe Koch, Shilan Liu
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Publication number: 20120302562Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
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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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Patent number: 8304421Abstract: Indole derivatives that are useful in the treatment of cancer as a chemotherapeutic agent or radiosensitizing agent.Type: GrantFiled: September 30, 2009Date of Patent: November 6, 2012Assignees: Vanderbilt University, University of Kentucky Research FoundationInventors: Peter A. Crooks, Thirupathi R. Yerramreddy, Narsimha R. Penthala, Michael L. Freeman, Sekhar R. Konjeti
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Publication number: 20120238541Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: September 17, 2010Publication date: September 20, 2012Applicant: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8252829Abstract: The present invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein each of Ring A, Ring B, T, R2, R2?, and RA is as defined and described herein and methods for treating subjects or patients with a disease, disorder, or condition.Type: GrantFiled: June 7, 2010Date of Patent: August 28, 2012Assignee: Link Medicine CorporationInventor: Mark E. Duggan
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Publication number: 20120214770Abstract: The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.Type: ApplicationFiled: May 1, 2012Publication date: August 23, 2012Applicant: BIONOMICS LIMITEDInventors: JASON HUGH CHAPLIN, GURMIT SINGH GILL, DAMIAN WOJCIECH GROBELNY, BERNARD LUKE FLYNN, GABRIEL KREMMIDIOTIS
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Patent number: 8247432Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs).Type: GrantFiled: May 19, 2011Date of Patent: August 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Patent number: 8242159Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.Type: GrantFiled: October 31, 2008Date of Patent: August 14, 2012Assignee: Dong-A Pharmaceutical. Co., LtdInventors: Yeong Geon Lee, Soo-Jung Choi, Tae-Kyung Kang, Mi-Jeong Seo, Chang-Yong Shin, Kyung-Seok Lee, Gook-Jun Ahn, Seul-Min Choi, Yong-Duck Kim, Dong-Hwan Kim, Kyung-Koo Kang, Hyun-Joo Shim, Dong-Sung Kim, Byoung-Ok Ahn, Moo-Hi Yoo
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Patent number: 8227497Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: June 22, 2011Date of Patent: July 24, 2012Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Patent number: 8227473Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: GrantFiled: July 17, 2009Date of Patent: July 24, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Patent number: 8222255Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: GrantFiled: September 25, 2008Date of Patent: July 17, 2012Assignees: Merck Sharp & Dohme Corp., Scynexis, Inc.Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, legal representative, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
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Publication number: 20120149702Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard CollegeInventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
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Publication number: 20120145973Abstract: The present invention relates to photochromic materials that include one or more indeno-fused naphthopyrans that have particular groups at the 7, 11, and 13 positions thereof, and at the position alpha to the oxygen of the pyran ring thereof. With some embodiments, hydrogen or an alkoxy group is bonded to the 7 position, an optionally substituted phenyl is bonded to the 11 position, two alkyl groups are bonded to the 13 position, and two optionally substituted phenyl groups are bonded to the position alpha to the oxygen of the pyran ring of the indeno-fused naphthopyran compound. The 13 position of the indeno-fused naphthopyrans is free of ether groups in which an ether oxygen is bonded to the 13 position, and hydroxyl. The present invention also relates to photochromic articles and compositions that include such indeno-fused naphthopyrans.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: TRANSITIONS OPTICAL INC.Inventors: Kevin E. Bancroft, Anu Chopra, Xiao-Man Dai, Beon-Kyu Kim, David B. Knowles, Jason R. Lewis, Victor A. Montes, Stephen D. Straight, Massimiliano Tomasulo, Barry Van Gemert, Robert W. Walters, Wenjing Xiao, Huayun Yu, Elizabeth A. Zezinka
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Patent number: 8187727Abstract: The present invention relates to a new imidazole derivative, a method for preparing the derivative, and an organic electronic device using the derivative. The imidazole derivative according to the invention can perform functions of hole injection, hole transportation, electron injection, electron transportation, and/or light emission in an organic electronic device including an organic light-emitting device. The organic electronic device according to the invention exhibits excellent characteristics in terms of efficiency, drive voltage and stability.Type: GrantFiled: July 18, 2006Date of Patent: May 29, 2012Assignee: LG Chem, Ltd.Inventors: Jae Soon Bae, Dong Hoon Lee, Dae Woong Lee, Jun Gi Jang
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Patent number: 8158666Abstract: A process for making (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3-dihydroimidazole-2-thione and pharmaceutically acceptable salts thereof, and for making intermediates useful in the formation of said compound.Type: GrantFiled: January 31, 2008Date of Patent: April 17, 2012Assignee: Bial-Portela & C.A., S.A.Inventors: Patrício Manuel Vieira Araújo Soares Da Silva, Alexander Beliaev, David Alexander Learmonth
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Patent number: 8153634Abstract: [Object] To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.Type: GrantFiled: May 29, 2009Date of Patent: April 10, 2012Assignee: Kowa Company, Ltd.Inventors: Yuki Yamaguchi, Minoru Koura, Sayaka Kurobuchi, Takayuki Matsuda, Ayumu Okuda, Hisashi Sumida, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya
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Patent number: 8153674Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of aldosterone synthase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, renal failure, in particular, chronic renal failure, restenosis, atherosderosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, increased formation of collagen, cardiac fibrosis and remodeling following hypertension and endothelial dysfunction. Finally, the present invention also provides a pharmaceutical composition.Type: GrantFiled: March 27, 2007Date of Patent: April 10, 2012Assignee: Novartis AGInventors: Christopher Adams, Julien Papillon, Gary Michael Ksander
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Patent number: 8153682Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: GrantFiled: July 18, 2008Date of Patent: April 10, 2012Assignee: Janssen Pharmaceutica, NVInventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20120083488Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: June 9, 2010Publication date: April 5, 2012Inventors: Kazutomo Kinoshita, Kohsuke Asoh, Noriyuki Furuichi, Toshiya Ito, Hatsuo Kawada, Nobuya Ishii, Hiroshi Sakamoto, WooSang Hong, MinJeong Park, Yoshiyuki Ono, Yashuharu Kato, Kenji Morikami, Takashi Emura, Nobuhiro Oikawa
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Publication number: 20120071506Abstract: The present invention relates to a method for treating a disorder selected from depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R1, R2, Q, W, X, Y, m, and n are as defined in the specification, and their pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers and tautomeric forms.Type: ApplicationFiled: November 23, 2011Publication date: March 22, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20120071523Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.Type: ApplicationFiled: May 5, 2010Publication date: March 22, 2012Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Christophe Antczak
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Publication number: 20120053132Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.Type: ApplicationFiled: November 1, 2011Publication date: March 1, 2012Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael Eissenstat, Dehui Duan
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Publication number: 20120053165Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: March 2, 2010Publication date: March 1, 2012Applicant: Pfizer Inc.Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
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Publication number: 20120040962Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.Type: ApplicationFiled: March 25, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8106052Abstract: The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated.Type: GrantFiled: April 5, 2010Date of Patent: January 31, 2012Assignee: Promega CorporationInventors: James J. Cali, Dieter Klaubert, William Daily, Samuel Kin Sang Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
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Publication number: 20120007063Abstract: The present invention relates to the use of dibenzofurans and dibenzothiophenes which have at least one nitrogen-bonded five-membered heterocyclic ring as a substituent as host, blocker and/or charge transport material in organic electronics. The present invention further relates to dibenzofurans and dibenzothiophenes which comprise at least one nitrogen-bonded five-membered heterocyclic ring and at least one carbazolyl radical as substituents, to a process for preparation thereof, and to the use of these compounds in organic electronics.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicant: BASF SEInventors: Nicolle LANGER, Christian Schildknecht, Christian Lennartz, Gerhard Wagenblast, Thomas Schäfer
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Publication number: 20120004230Abstract: The invention relates to imidazole derivatives which have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The invention also relates to a pharmaceutically-suitable acid-addition salt of the above compound. The invention further relates to a composition comprising an imidazole derivative as described above, or a pharmaceutically-suitable acid-addition salt thereof, and to processes for preparing such compounds.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20110312996Abstract: The embodiments provide compounds of the general Formulae VI, VII, VIII, IX, X, XI, XII, XIII, XIV, and XV as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: May 16, 2011Publication date: December 22, 2011Applicant: InterMune, Inc.Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
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Publication number: 20110286961Abstract: 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: December 1, 2010Publication date: November 24, 2011Inventors: Makonen Belema, Jeffrey Lee Romine, Van N. Nguyen, Gan Wang, Omar D. Lopez, Denis R. St. Laurent, Qi Chen, John A. Bender, Zhong Yang, Piyasena Hewawasam, Ningning Xu, Nicholas A. Meanwell, John A. Easter, Bao-Ning Su, Michael J. Smith
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Publication number: 20110263486Abstract: The invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein Y is —NRaRb, —NRc?ONRaRb, —NRcC?SNRaRb, —NRcC?NRdNaRb, heterocycle, —C?ONRaRb, heterocycle, or aryl; n is 0 to 8; m is 0, or 1; r is 0 to 3; t is 0 to 3; X is O or N; Z is CH2, C?O, C?S or a single bond; Z1 is CO—R2, CS—R2, (CH2)t—R2 or the side-chain of a naturally occurring amino acid; Z2 is CO—R2, CS—R2 or (CH2)t—R3 or the side-chain of a naturally occurring amino acid; Z3 is CO—R2, CS—R2 or (CH2)t—R4 or the side-chain of a naturally occurring amino acid; Z4 is H, alkyl, alkoxy, or cycloalkyl; R1, R2, R3, and R4 are independently from each other H, OH, SH, NH2, CN, NO2, alkyl, cycloalkyl, heterocycloalkyl, haloalkyl, alkylthio, haloalkyloxy, hydroxyalkyl, hydroxyalkylamino, alkylamino, alkylaryl, alkylsulfinyl, alkylsulfonyl, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, alkoxyalkyl, alkoxy, aryloxy, heteroaryl, aryl, or halogen.Type: ApplicationFiled: March 11, 2011Publication date: October 27, 2011Applicant: 4SC AGInventors: Johann LEBAN, Martin KRALIK
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Publication number: 20110251251Abstract: The invention relates to a crystalline polymorph of a pharmaceutically acceptable salt of an optically active anti-fungal imidazole compound of formula (III), the pharmaceutical and agricultural compositions containing such polymorph, its use in the treatment or prevention of skin or mucous membrane infections caused by fungi or yeasts in humans or pets, and its use in the treatment or prevention of agricultural diseases produced by such infectious agents.Type: ApplicationFiled: December 9, 2009Publication date: October 13, 2011Applicant: FERRER INTERNACIONAL, S.AInventors: Mónica Delgardo, Carles Albet, Inés Petschen, Marta Tarruella
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Publication number: 20110224255Abstract: The present invention is concerned with novel compounds of formula (I) which are inhibitors of a membrane tripeptidyl peptidase responsible for the inactivation of endogenous neuropeptides such as cholecystokinis (CCKs). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.Type: ApplicationFiled: May 19, 2011Publication date: September 15, 2011Inventors: Henry Joseph Breslin, Hans Louis Jos De Winter, Michael Joseph Kukla
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Publication number: 20110190247Abstract: In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: August 3, 2009Publication date: August 4, 2011Applicant: Schering CorporationInventors: Younong Yu, Manuel De Lera Ruiz, Christopher W. Boyce, Kevin D. McCormick
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Patent number: 7989484Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: April 28, 2009Date of Patent: August 2, 2011Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell