Polycylo Ring System Having A Ring Nitrogen In The System Patents (Class 514/80)
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Publication number: 20140243287Abstract: The present invention relates to pyrazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: February 24, 2014Publication date: August 28, 2014Applicant: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, Ken Chow
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Publication number: 20140243288Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.Type: ApplicationFiled: September 29, 2012Publication date: August 28, 2014Inventors: Hui Zhang, Aichen Wang
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Publication number: 20140235579Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Inventors: John M. McCall, Donna L. Romero, Michael Clare
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Publication number: 20140221314Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.Type: ApplicationFiled: May 31, 2012Publication date: August 7, 2014Applicant: NewGen Therapeutics, Inc.Inventors: Wang Shen, Jack Maung, Aimin Zhang, Xiaoling Zheng
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Publication number: 20140206649Abstract: Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;Type: ApplicationFiled: February 24, 2012Publication date: July 24, 2014Inventors: Jayant Thatte, Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Jae-Kyu Jung, Anthony Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter, Sonja Strah-Pleynet, Lars Thoresen, Yifeng Xiong, Dawei Yue, Xiuwen Zhu
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Publication number: 20140194388Abstract: A pharmaceutical composition comprising a CHK inhibitor, and an Hsp90 inhibitor according to the following formulae or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.Type: ApplicationFiled: May 25, 2012Publication date: July 10, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Publication number: 20140193363Abstract: 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: ApplicationFiled: January 15, 2014Publication date: July 10, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
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Publication number: 20140178461Abstract: Novel compounds and pharmaceutical compositions thereof administered by the respiratory route for prevention and/or treatment of lung and brain cancer and precancerous conditions thereof.Type: ApplicationFiled: September 23, 2013Publication date: June 26, 2014Inventor: Basil RIGAS
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Publication number: 20140171392Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 13, 2013Publication date: June 19, 2014Applicant: Novartis AGInventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
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Patent number: 8754078Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: GrantFiled: February 7, 2013Date of Patent: June 17, 2014Assignee: ArQule, Inc.Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
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Publication number: 20140162984Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: ApplicationFiled: August 21, 2012Publication date: June 12, 2014Applicant: ASTRAZENECA ABInventors: Nicola Murdoch HERON, Andrew Austen MORTLOCK, Frederic Henri JUNG, Georges Rene PASQUET
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Publication number: 20140162964Abstract: Disclosed is a new use for sphingosine-1-phosphate (S1P) receptor agonists in the treatment of progressive dementia or brain degenerative diseases.Type: ApplicationFiled: December 2, 2013Publication date: June 12, 2014Applicant: NOVARTIS AGInventors: Volker Brinkmann, Nicole Kaneider, Christian J. Wiedermann
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Patent number: 8735384Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein ring A, B1, B2, B3, L, R1, R2, ring Z, m and n of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).Type: GrantFiled: January 14, 2011Date of Patent: May 27, 2014Assignee: Amgen Inc.Inventors: Nick A. Paras, James Brown, Yuan Cheng, Stephen A. Hitchcock, Ted Judd, Patricia Lopez, Ana Elena Minatti, Thomas Nixey, Timothy Powers, Christopher M. Tegley, Qiufen Xue, Bryant Yang, Wenge Zhong
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Publication number: 20140141972Abstract: This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: E I DU PONT NEMOURS AND COMPANYInventors: RICHARD ALAN BERGER, Isaac Billy Annan, George Philip Lahm, John Lindsey Flexner, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140140973Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140128345Abstract: Described are drug delivery systems incorporating electrospun fibers that comprise and deliver physicochemically diverse drug compounds. Such fibers provide significant advantages in drug agent release, such as adaptability for solid dosage delivery to mucosal tissues. This is in addition to allowing for controlled drug release. Systems and methods for large-scale electrospinning productivity are described, including novel microarchitectures allowing for variable pharmacokinetics in drug release.Type: ApplicationFiled: November 6, 2013Publication date: May 8, 2014Applicant: UNIVERSITY OF WASHINGTONInventors: Kim A. Woodrow, Cameron Ball, Anna Blakney, Emily Krogstad, Huarong Nie
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Publication number: 20140121102Abstract: The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula (I) wherein A1, A2, L, p, R1, R2, R3, R4 and R5 are as defined in claim 1 and component B is an insecticide. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: May 30, 2012Publication date: May 1, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Myriem El Qacem, Jerome Yves Cassayre
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Publication number: 20140107073Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: ApplicationFiled: October 4, 2013Publication date: April 17, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Patent number: 8697674Abstract: The present invention relates to pharmaceutical compositions comprising xanthurenic acid derivatives, and methods of use thereof.Type: GrantFiled: December 29, 2004Date of Patent: April 15, 2014Assignee: Naturon, Inc.Inventors: Neal S. Bricker, Stewart Shankel, Christopher D. Cain, Mark Mitchnick, Michael Schmertzler
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Publication number: 20140100195Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: October 5, 2012Publication date: April 10, 2014Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
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Publication number: 20140100194Abstract: The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: December 5, 2013Publication date: April 10, 2014Applicant: Janssen Pharmaceutica, NVInventors: Raymond W Colburn, Scott L. Dax, Christopher M. Flores, Jay M. Matthews
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Patent number: 8691938Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: GrantFiled: June 10, 2010Date of Patent: April 8, 2014Assignee: AbbVie Inc.Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi
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Publication number: 20140087992Abstract: Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.Type: ApplicationFiled: September 20, 2013Publication date: March 27, 2014Inventors: Ashvinikumar V. Gavai, George V. DeLucca, Daniel O'Malley, Patrice Gill, Claude A. Quesnelle, Brian E. Fink, Yufen Zhao, Francis Y. Lee
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Patent number: 8673883Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.Type: GrantFiled: April 26, 2013Date of Patent: March 18, 2014Assignee: Retrophin, Inc.Inventors: Andrew Vaino, Marek Biestek, Martin Shkreli
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Patent number: 8664202Abstract: The present invention is directed to a stabilized cross-linked hydrogel matrix comprising a first high molecular weight component and a second high molecular weight component that are covalently linked, and at least one stabilizing or enhancing agent, wherein the first high molecular weight component and the second high molecular weight component are each selected from the group consisting of polyglycans and polypeptides. This stabilized hydrogel matrix may be prepared as bioactive gels, pastes, slurries, cell attachment scaffolds for implantable medical devices, and casting or binding materials suitable for the construction of medical devices. The intrinsic bioactivity of the hydrogel matrix makes it useful as a gel or paste in multiple applications, including as a cell attachment scaffold that promotes wound healing around an implanted device, as gels and pastes for induction of localized vasculogenesis, wound healing, tissue repair, and regeneration, as a wound adhesive, and for tissue bulking.Type: GrantFiled: October 4, 2011Date of Patent: March 4, 2014Assignee: Pioneer Surgical Technology, Inc.Inventors: Francis V. Lamberti, Richard Chris Klann, Ronald Stewart Hill
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Publication number: 20140051664Abstract: Methods for treating cancer in a subject, comprising administering to the subject an effective amount of a compound represented by the following structural formula a tautomer, or a pharmaceutically acceptable salt thereof in combination with radiotherapy. The variables depicted in the structural formula are defined herein.Type: ApplicationFiled: February 22, 2012Publication date: February 20, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Kevin P. Foley, David Proia
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Publication number: 20140051625Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.Type: ApplicationFiled: October 25, 2013Publication date: February 20, 2014Applicant: MBC Pharma, Inc.Inventors: Alexander Karpeisky, Shawn Patrick Zinnen
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Publication number: 20140051665Abstract: Method for treating a subject with prostate cancer, comprising administering to the an effective amount of a compound represented by the following structural formula: a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.Type: ApplicationFiled: February 23, 2012Publication date: February 20, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Publication number: 20140045794Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.Type: ApplicationFiled: October 21, 2013Publication date: February 13, 2014Applicant: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle
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Publication number: 20140045791Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: July 15, 2013Publication date: February 13, 2014Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Ann-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran
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Patent number: 8647829Abstract: Methods and kits for binding and releasing biological targets, comprising, a binder comprising an environmentally reactive molecular switch that can switch between a high affinity state, to bind the target, to a low affinity state, to release the target.Type: GrantFiled: July 7, 2009Date of Patent: February 11, 2014Assignee: General Electric CompanyInventors: Aaron Dulgar-Tulloch, Ernest William Kovacs, Evelina Roxana Loghin, Anup Sood
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Patent number: 8647830Abstract: The present invention relates to an in vitro method for medical diagnosis, prognosis and therapy follow-up for patients having a cardiac disease or being suspected of developing or having a cardiac disease comprising the steps of: providing a sample of a patient having a cardiac disease or being suspected of developing or having a cardiac disease, determining amino-terminal proANp or partial peptides thereof having from 12 to 98 amino acids in said sample using at least one antibody that binds specifically to a partial sequence of amino-terminal proANP, attributing the determined amino-terminal proANP level or the level of partial peptides thereof to a clinical picture wherein the attribution is carried out independent of the BMI of the patient. The present invention further concerns a rapid test assay and a kit for conducting the method of the present invention and the use of antibodies suitable for the method and assays according to the present invention.Type: GrantFiled: May 6, 2008Date of Patent: February 11, 2014Assignee: B.R.A.H.M.S. GmbHInventors: Andreas Bergmann, Jana Papassotiriou, Joachim Struck, Nils Morgenthaler, Stefan Anker
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Publication number: 20140038920Abstract: The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases.Type: ApplicationFiled: March 7, 2012Publication date: February 6, 2014Applicant: FONDAZIONE TELETHONInventors: Andrea Ballabio, Carmine Settembre, Diego Luis Medina Sanabria
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Publication number: 20140031318Abstract: The invention relates to solid forms of the Formula (I) wherein X is —PO(OH)2, —PO(OH)O?M+, or —PO(O?)2.2M+, wherein M is a monovalent cation such as Na+, K+, Li+, or NH4+. The invention also provides pharmaceutically acceptable compositions comprising the solid form of the compound and method of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 18, 2013Publication date: January 30, 2014Inventors: Hardwin O'DOWD, DAINIUS MACIKENAS, Bin SONG
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Publication number: 20140024619Abstract: The present invention provides a benzazepine compound that can maintain for a long period of time the blood level of tolvaptan enabling to provide the desired pharmaceutical effects. The benzazepine compound of the present invention is represented by general formula (1) wherein R1 represents a —CO—(CH2)n—COR2 group (wherein n is an integer of 1 to 4, and R2 is (2-1) a hydroxy group; (2-2) a lower alkoxy group optionally substituted with a hydroxy group, a lower alkanoyl group, a lower alkanoyloxy group, a lower alkoxycarbonyloxy group, a cycloalkyloxycarbonyloxy group, or 5-methyl-2-oxo-1,3-dioxol-4-yl; or (2-3) an amino group optionally substituted with a hydroxy-lower alkyl group), or the like.Type: ApplicationFiled: September 24, 2013Publication date: January 23, 2014Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Kazumi KONDO, Yasuhiro MENJO, Takahiro TOMOYASU, Shin MIYAMURA, Yuso TOMOHIRA, Takakuni MATSUDA, Keigo YAMADA, Yusuke KATO
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Publication number: 20140024618Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: September 23, 2013Publication date: January 23, 2014Applicant: LG LIFE SCIENCES LTD.Inventors: Soon Ha KIM, Hyoung Jin KIM, Sun Young KOO, Sung Bae LEE, Heui Sul PARK, Seung Hyun YOON, Seung Yup PAEK, Hyo Shin KWAK, Dong Ook SEO, Eok PARK
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Patent number: 8633173Abstract: This application relates, in part, to compounds of the general Formula I and/or salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of inhibiting at least JAK2 in subjects in recognized need thereof for the treatment of diseases or disorders for which inhibition of at least JAK2 is indicated.Type: GrantFiled: June 18, 2013Date of Patent: January 21, 2014Assignee: Cephalon, IncInventors: Matthew A. Curry, Bruce D. Dorsey, Benjamin J. Dugan, Diane E. Gingrich, Eugen F. Mesaros, Karen L. Milkiewicz
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Publication number: 20140018320Abstract: There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C?W, NR4, NC(?O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent paiType: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Applicant: Summit Corporation PLCInventors: GRAHAM MICHAEL WYNNE, STEPHEN PAUL WREN, PETER DAVID JOHNSON, PAUL DAMIEN PRICE, OLIVIER DE MOOR, GARY NUGENT, RICHARD STORER, RICHARD JOSEPH PYE, COLIN RICHARD DORGAN
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Publication number: 20140005146Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.Type: ApplicationFiled: March 16, 2012Publication date: January 2, 2014Inventors: Stephen T. Wrobleski, Jagabandhu Das, Lidia M. Doweyko, Junqing Guo, John Hynes, Bin Jiang, James Kempson, Shuqun Lin, Steven H. Spergel, John S. Tokarski, Hong Wu, Bingwei Vera Yang
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Publication number: 20140005145Abstract: Methods for treating breast cancer, comprising administering to the subject an effective amount of a selective estrogen receptor modulator and an effective amount of a compound represented by the following structural formula: (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.Type: ApplicationFiled: December 7, 2011Publication date: January 2, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: David Proia
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Patent number: 8618079Abstract: Novel imidazo[1,2-?]pyridinyl bisphosphonate compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating abnormal calcium and phosphate metabolism, including bone and joint diseases and other disorders.Type: GrantFiled: September 22, 2009Date of Patent: December 31, 2013Assignee: Isis Innovation LimitedInventors: Frank Hallock Ebetino, Adam Mazur, Mark Walden Lundy, Robert Graham Russell
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Publication number: 20130331358Abstract: The present invention provides a benzoazepine compound represented by following general formula (1): or a salt thereof, wherein R represents a hydrogen atom, a hydroxy group optionally protected with a protecting group, etc., R1 represents a hydrogen atom or hydroxy-protecting group, and X represents an oxygen atom or a sulfur atom. The benzoazepine compound of the present invention and salts thereof have high solubility in water, and can be suitably used for injections.Type: ApplicationFiled: August 12, 2013Publication date: December 12, 2013Applicant: Otsuka Pharmaceutical Co., Ltd.Inventors: Makoto KOMATSU, Fumitaka GOTO, Yasuhiro MENJO, Keigo YAMADA, Takakuni MATSUDA, Yusuke KATO
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Publication number: 20130331357Abstract: A composition comprising a proteasome inhibitor, and an Hsp90 inhibitor according to the following formulae (I) or (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder such as cancer in a subject in need thereof, using pharmaceutical combinations described herein.Type: ApplicationFiled: January 10, 2012Publication date: December 12, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Julie Friedland
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Patent number: 8603980Abstract: The present invention relates to methods and compositions for modulating platelet activity by inhibiting or activating glutamate receptors. The invention further relates to preventing or treating thrombotic diseases.Type: GrantFiled: January 16, 2008Date of Patent: December 10, 2013Assignee: The Johns Hopkins UniversityInventors: Craig N. Morrell, Charles J. Lowenstein
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Patent number: 8592395Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: July 23, 2010Date of Patent: November 26, 2013Assignee: GlaxoSmithKline LLCInventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
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Patent number: 8592396Abstract: Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure wherein R1, R2, R3, R4, R5, R6, Y and X are as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related disease employing the above compounds is also provided.Type: GrantFiled: April 14, 2011Date of Patent: November 26, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Wei Meng, Peter T. W. Cheng
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Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
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Publication number: 20130289001Abstract: The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.Type: ApplicationFiled: April 26, 2013Publication date: October 31, 2013Applicant: Retrophin, Inc.Inventors: Andrew VAINO, Marek Biestek, Martin Shkreli
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Publication number: 20130289002Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: June 3, 2013Publication date: October 31, 2013Inventors: Arnaud Le Tiran, Anne-Laure Grillot, Paul S. Charifson, Youssef Laafiret Bennani, Hardwin O'Dowd, Emanuele Perola
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Patent number: 8563569Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: October 27, 2011Date of Patent: October 22, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Rajinder Singh