Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
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Publication number: 20120251579Abstract: The present invention provides for the purposeful utilisation of the induction of senescence in eukaryotic cells for induction of an antigen specific immune response. Such cells can be normal cells, pre-malignant and malignant cells as well as virally or bacterially infected cells, for the generation of an immune response, preferably a cellular or humoral immune response comprising T-cells and/or B-cells, whose immune response is directed specifically against antigens from those cells in which senescence was induced and then comprises an immune response against the senescent cells itself as well as to the non-senescent counterparts harbouring the same antigens.Type: ApplicationFiled: July 30, 2010Publication date: October 4, 2012Applicant: Helmholtz-Zentrum Fuer Infektionsforschung GmbHInventor: Lars Zender
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Patent number: 8278307Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: May 8, 2007Date of Patent: October 2, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
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Publication number: 20120245138Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: May 2, 2012Publication date: September 27, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20120245176Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, —CHF2 or —CH?CH2; V is —H, —CH3 or ?O; W is —NO2, —Cl, —Br, —CH2OH, or —CN; X is —Cl, —Br, —F, —CH3, —OCH3, or —CN; Y is —CH or —N; and Z is —CH or —N. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: ApplicationFiled: September 23, 2011Publication date: September 27, 2012Inventors: Christopher W. Cianci, Samuel Gerritz, Sean Kim, David R. Langley, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Patent number: 8273341Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: November 8, 2011Date of Patent: September 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Michael Graupe, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
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Publication number: 20120238550Abstract: There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C?O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (?O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C?O)0-1R12][(C?O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C?O)0-1R12][(C?O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R?14, wherein R12 and R13Type: ApplicationFiled: August 23, 2010Publication date: September 20, 2012Inventors: Lok Wai Lawrence Woo, Christian Bubert, Paul Michael Wood, Aurélien Putey, Atul Purohit, Barry Victor Lloyd Potter
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Patent number: 8268830Abstract: The invention provides a method of inhibiting the effects of platelet activating factor (PAF). For instance, a disease or condition mediated by PAF (particularly inflammation) can be treated or platelet aggregation can be inhibited. The invention also provides a method of inhibiting the production and/or release of interleukin 8 (IL-8) by cells. The effects of PAF and the production and/or release of IL-8 are inhibited according to the invention by a compound of the formula: wherein R1 and R2 are defined in the application, or a physiologically-acceptable salt thereof. The invention also provides pharmaceutical compositions comprising these compounds.Type: GrantFiled: December 28, 2011Date of Patent: September 18, 2012Inventors: David Bar-Or, C. Gerald Curtis, Nagaraja K. R. Rao, Greg Thomas
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Publication number: 20120232093Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: ApplicationFiled: May 24, 2012Publication date: September 13, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Rosa CUBERES-ALTISENT, Joerg HOLENZ
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Publication number: 20120232092Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: May 18, 2012Publication date: September 13, 2012Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
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Patent number: 8263600Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.Type: GrantFiled: June 15, 2011Date of Patent: September 11, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Stefan Sharpe, Joel Sequeira, David Harris, Shashank Mahashabde
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Publication number: 20120225880Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
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Publication number: 20120225854Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 23, 2011Publication date: September 6, 2012Applicant: AMGEN INC.Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, JR., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
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Publication number: 20120214817Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20120213791Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.Type: ApplicationFiled: November 4, 2011Publication date: August 23, 2012Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20120214789Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5 and R6 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.Type: ApplicationFiled: May 2, 2012Publication date: August 23, 2012Inventors: Michael Patrick Dillon, Ronald Charles Hawley, Li Chen, Lichun Feng, Minmin Yang
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Publication number: 20120207826Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Inventors: Thomas Julius Borody, Soledad Carsula
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Patent number: 8242117Abstract: Provided are 5-membered heterocycle-based p38 kinase inhibitors. Further provided are pyrazole and imidazole-based p38 kinase, including p38? and p38? kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the compounds and compositions are also provided, including methods of treatment, prevention, or amelioration of one or more symptoms of p38 kinase mediated diseases and disorders, including, but not limited to, inflammatory diseases and disorders.Type: GrantFiled: November 19, 2010Date of Patent: August 14, 2012Assignee: Novartis AGInventors: Olga M. Fryszman, Hengyuan Lang, Jiong Lan, Edcon Chang, Yunfeng Fang
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Publication number: 20120202794Abstract: Disclosed herein are compounds useful for treating a viral infection, such as HCV.Type: ApplicationFiled: January 19, 2012Publication date: August 9, 2012Applicant: PHARMASSET, INC.Inventors: MICHAEL JOSEPH SOFIA, RAMESH KAKARLA, JIAN LIU, DEVAN NADUTHAMBI, RALPH MOSLEY, HOLLY MICOLOCHICK STEUER
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20120202687Abstract: This document discloses molecules having the following formulas (“Formula One” & “Formula Two” and “Formula Three”) The Ar1, Het, Ar2, R1, R2, R3, R4, and R5 are further described herein.Type: ApplicationFiled: February 6, 2012Publication date: August 9, 2012Inventors: Gary D. Crouse, Thomas C. Sparks, William H. Dent, III, CaSandra L. McLeod, Lawrence C. Creemer, David A. Demeter, Amanda E. Fritz, Lindsey G. Fischer, Erich W. Baum
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Patent number: 8236806Abstract: The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.Type: GrantFiled: July 13, 2007Date of Patent: August 7, 2012Assignee: Korea Research Institute of Chemical TechnologyInventors: Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
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Publication number: 20120195985Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: March 21, 2012Publication date: August 2, 2012Applicant: Amgen Inc.Inventors: Stephen Hitchcock, Albert Amegadzie, Wenyuan Qian, Xiaoyang Xia, Scott S. Harried
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Publication number: 20120196864Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.Type: ApplicationFiled: August 4, 2010Publication date: August 2, 2012Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20120189623Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: April 3, 2012Publication date: July 26, 2012Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Publication number: 20120183498Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
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Patent number: 8222254Abstract: The invention relates to novel 5-hydroxytryptamine (5-HT) receptor modulator compounds of formula (I); wherein A, B, R1-R5, T, W, X, Y, Z and m are defined herein, to pharmaceutical compositions comprising these compounds and to their use in the treatment of conditions associated with 5-HT action.Type: GrantFiled: August 6, 2008Date of Patent: July 17, 2012Assignee: Prosarix LimitedInventors: Jonathan Richard Heal, Joseph Michael Sheridan, William Dennys Ormrod Hamilton, Simon James Grimshaw, Sorin Vasile Filip
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Publication number: 20120165303Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: March 2, 2012Publication date: June 28, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Sreenivas Punna, Edward J. Sullivan, Xuefei Tan, William D. Thomas, Solomon Ungashe, Yibin Zeng
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Publication number: 20120165324Abstract: Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: June 28, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders
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Patent number: 8207156Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: February 28, 2011Date of Patent: June 26, 2012Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
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Patent number: 8202872Abstract: The invention relates to compounds of formula I having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.Type: GrantFiled: March 1, 2007Date of Patent: June 19, 2012Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20120141606Abstract: The invention refers to the use of a sigma ligand of formula (I) to prevent or treat pain induced by a chemotherapeutic agent, especially pain induced by taxanes, vinca alkaloids or platinum-containing chemotherapeutic drugs.Type: ApplicationFiled: August 12, 2010Publication date: June 7, 2012Inventors: José Manuel Baeyens-Cabrera, Helmut Heinrich Buschmann, José Miguel Vela Hernández, Daniel Zamanillo-Castanedo, Francisco-Rafael Nieto-López
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Publication number: 20120142698Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: ApplicationFiled: August 6, 2010Publication date: June 7, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Publication number: 20120142702Abstract: A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.Type: ApplicationFiled: November 21, 2011Publication date: June 7, 2012Applicant: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Su-Lin Lee, Samuel K. Kulp
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Patent number: 8193176Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: GrantFiled: November 22, 2010Date of Patent: June 5, 2012Assignee: Taisho Pharmaceutical Co., LtdInventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Publication number: 20120135997Abstract: The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid ? proteins. The present invention provides a pharmaceutical composition for suppressing amyloid ? production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: Shionogi & Co., Ltd.Inventors: Issei Kato, Kazuya Kano
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Publication number: 20120135929Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 20, 2010Publication date: May 31, 2012Applicant: Ardea Biosciences Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
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Publication number: 20120129844Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: January 26, 2012Publication date: May 24, 2012Inventors: David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20120129870Abstract: The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.Type: ApplicationFiled: December 17, 2008Publication date: May 24, 2012Inventors: Wenying Chai, Jill A. Jablonowski, Dale A. Rudolph, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong
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Publication number: 20120115880Abstract: Compositions and methods for treating ocular cancer are provided. The composition is a subconjunctival formulation of nutlin-3 and its analogs. The composition provides for methods of treating ocular cancer, including retinoblastoma. The formulation has high penetration into ocular tissue with low toxicity.Type: ApplicationFiled: September 27, 2011Publication date: May 10, 2012Applicant: St. Jude Children's Research HospitalInventors: Michael A. Dyer, Jean-Christophe Marine, Aart Gerrit Jochemsen, R. Kip Guy
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Publication number: 20120115881Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: ApplicationFiled: July 9, 2010Publication date: May 10, 2012Applicant: GREEN CROSS CORPORATIONInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
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Publication number: 20120114600Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 3, 2011Publication date: May 10, 2012Applicant: THERAVANCE, INC.Inventors: Robert Murray McKINNELL, Daniel D. LONG, Lori Jean VAN ORDEN, Lan JIANG, Mandy LOO, Daisuke Roland SAITO, Shella ZIPFEL, Eric L. Stangeland, Kassandra Lepack, Gavin Ogawa
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Publication number: 20120101072Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: December 21, 2011Publication date: April 26, 2012Inventors: Joseph A. Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
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Publication number: 20120101082Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: December 19, 2011Publication date: April 26, 2012Inventors: ANDRZEJ ROMAN BATT, MARTIN LEE STOCKLEY, MICHAEL BRYAN ROE, CELINE Marguerite Simone HEENEY, ANDREW JOHN BAXTER, PETER HUDSON, RACHEL HANDY
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Patent number: 8163757Abstract: The present invention relates to compounds of formula (IA) or (IB) or pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: September 2, 2010Date of Patent: April 24, 2012Assignee: MediGene AGInventor: Ian Richard Matthews
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Publication number: 20120088778Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.Type: ApplicationFiled: October 10, 2011Publication date: April 12, 2012Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Robert C. Andrews, Ramesh Gopalaswamy, Anitha Hari, Kwasi S. Avor, Ghassan Qabaja, Xiao-Chuan Guo, Suparna Gupta, David R. Jones, Xin Chen
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Publication number: 20120088754Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: December 14, 2011Publication date: April 12, 2012Inventors: Kristof Van Emelen, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noëlle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van heusden
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Publication number: 20120088779Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Inventors: Bradley Paul MORGAN, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
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Publication number: 20120082623Abstract: The invention provides for methods of upregulating endogenous GDNF by inhibiting Shh signaling. The invention further provides a method for increasing the production of cholinergic neurons and dopamine neurons by subventricular zone (SVZ) neurogenesis in a subject. The invention further provides methods for treating a neurodegenerative disorder in a subject.Type: ApplicationFiled: September 30, 2011Publication date: April 5, 2012Inventor: Andreas H. Kottmann
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Publication number: 20120083487Abstract: Provided herein are compositions comprising a dextromethorphan analog according to Formula I or Formula II or a pharmaceutically acceptable salt thereof of either of the foregoing, and a co-agent, e.g., an antidepressant such as a serotonin norepinephrine reuptake inhibitor; a serotonin noradrenaline dopamine reuptake inhibitor; a norepinephrine dopamine reuptake inhibitor; a monoamine oxidase inhibitor; a selective serotonin reuptake inhibitor; and a tricyclic antidepressant or a pharmaceutically acceptable salt of any of the foregoing. The compositions are useful in the treatment of pseudobulbar affect, neuropathic pain, neurodegenerative diseases, brain injuries, and the like.Type: ApplicationFiled: October 30, 2009Publication date: April 5, 2012Inventor: Amanda Thomas
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Patent number: 8148367Abstract: Disclosed are compounds, pharmaceutical compositions, kits, articles of manufacture, methods of using, and methods of preparing compounds having the formula: wherein the variables are as defined herein. The disclosed compounds are inhibitors of Renin.Type: GrantFiled: January 9, 2008Date of Patent: April 3, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Lily Kwok, Betty Lam, Zhe Li, Zhiyuan Zhang