The Ring Nitrogen Is Bonded Directly To Nonshared Ring Carbons Of The Five-membered Hetero Ring (e.g., Isoindole, Etc.) Patents (Class 514/416)
  • Patent number: 10124071
    Abstract: The present invention provides for a novel liquid formulation for solubilizing poorly soluble ST-246 in cyclodextrins and a novel process of making the formulation.
    Type: Grant
    Filed: January 16, 2018
    Date of Patent: November 13, 2018
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William Weimers, Gopi Krishna Kasi, N K Peter Samuel, Tove C. Bolken, Dennis E. Hruby
  • Patent number: 10112899
    Abstract: Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: October 30, 2018
    Assignee: ViiV HEALTHCARE UK LIMITED
    Inventors: Brian Alvin Johns, Emile Johann Velthuisen, Jason Gordon Weatherhead, Lita Suwandi, David Temelkoff
  • Patent number: 10001483
    Abstract: Provided herein are uses of gene and protein biomarkers as a predictor of clinical sensitivity of Kaposi's sarcoma (KS) or Kaposi's sarcoma-associated herpesvirus (KSHV) induced lymphoma and patient response to treatment with an immunomodulatory compound. Further provided herein are methods for the treatment or management of Kaposi's sarcoma or KSHV-induced lymphoma with an immunomodulatory compound, alone or in combination with doxorubicin.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: June 19, 2018
    Assignees: Celgene Corporation, The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Robert Yarchoan, Jerome B. Zeldis, Mark N. Polizzotto, David A. Davis, Irini Sereti, Thomas S. Uldrick, Denise Whitby, Vikram Khetani
  • Patent number: 9907859
    Abstract: The present invention provides for a novel liquid formulation for solubilizing poorly soluble ST-246 in cyclodextrins and a novel process of making the formulation.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: March 6, 2018
    Assignee: Siga Technologies, Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William Weimers, Gopi Krishna Kasi, N K Peter Samuel, Tove′ C. Bolken, Dennis E. Hruby
  • Patent number: 9845308
    Abstract: Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: December 19, 2017
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Lawrence Wayne Dillard, Chengguo Dong, Yi Fan, Lanqi Jia, Stephen D. Lotesta, Andrew Marcus, Suresh B. Singh, Colin M. Tice, Jing Yuan, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9782377
    Abstract: A composition having a normalizing action for infradian rhythm and/or a synchronization promoting action for circadian rhythm (biological clock) containing arachidonic acid and/or an arachidonic acid-containing compound.
    Type: Grant
    Filed: March 26, 2004
    Date of Patent: October 10, 2017
    Assignee: SUNTORY HOLDINGS LIMITED
    Inventors: Kengo Akimoto, Yoshiko Ono, Hiroshi Kawashima, Katsuya Nagai
  • Patent number: 9421191
    Abstract: Disclosed in certain embodiments is a pharmaceutical composition for parenteral administration comprising: an aqueous solution comprising ketorolac or a pharmaceutically acceptable salt thereof in an amount from about 0.1 mg/mL to about 10 mg/mL; and a pharmaceutically acceptable excipient; wherein the formulation is substantially free of alcohol.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: August 23, 2016
    Assignee: RTU PHARMACEUTICALS, LLC
    Inventors: Joseph V. Pergolizzi, Alexander Mironov, Chad James Pickens, Douglas Giles Johnson
  • Patent number: 9233097
    Abstract: The present invention provides for a novel liquid formulation for solubilizing poorly soluble ST-246 in cyclodextrins and a novel process of making the formulation.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: January 12, 2016
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. Stone, William C. Weimers, Gopi Krishna Kasi, Peter N. K. Samuel, Tove Bolken, Dennis E. Hruby
  • Patent number: 9023886
    Abstract: Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: May 5, 2015
    Assignee: Celgene Corporation
    Inventors: Ming J. Chen, Ho-Wah Hui, Thomas Lee, Paul Kurtulik, Sekhar Surapaneni
  • Publication number: 20150111890
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof,that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: April 19, 2013
    Publication date: April 23, 2015
    Inventors: Lisa A. Hasvold, Dachun Liu, Chang Hoon Park, John K. Pratt, George S. Sheppard, Le Wang
  • Publication number: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as 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: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Publication number: 20150057255
    Abstract: The invention relates to methods for treating pruritus with NK-1 receptor antagonists such as serlopitant. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonists such as serlopitant. In addition, the invention encompasses treatment of a pruritus-associated condition with serlopitant and an additional antipruritic agent, and the use of serlopitant as a sleep aid, optionally in combination with an additional sleep-aiding agent.
    Type: Application
    Filed: June 24, 2014
    Publication date: February 26, 2015
    Inventors: Xiaoming ZHANG, Edward F. SCHNIPPER, Andrew J. PERLMAN, James W. LARRICK
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Publication number: 20140378521
    Abstract: The invention relates to methods for treating pruritus with an NK-1 receptor antagonist. The invention further relates to pharmaceutical compositions comprising NK-1 receptor antagonist.
    Type: Application
    Filed: June 24, 2013
    Publication date: December 25, 2014
    Inventors: Xiaoming ZHANG, Edward F. SCHNIPPER, Andrew J. PERLMAN, James W. LARRICK
  • Publication number: 20140378473
    Abstract: This invention relates to novel diarylamino compounds that bind to the sigma-2 receptor, to pharmaceutical compositions comprising such compounds, and to methods for inhibiting or restoring synapse loss in neuronal cells, modulating a membrane trafficking change in neuronal cells, and treating cognitive decline and neurodegenerative diseases and disorders therewith.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: COGNITION THERAPEUTICS, INC.
    Inventors: Susan M. Catalano, Gilbert Rishton, Nicholas J. Izzo
  • Patent number: 8916552
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: December 23, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Patent number: 8889729
    Abstract: Indole derivatives, compositions including same, and methods utilizing same for the treatment of amyloid associated diseases, such as type II diabetes mellitus, Alzheimer's dementia or diseases, systemic and localized amyloidosis, and prion-related encephalopathies are provided.
    Type: Grant
    Filed: June 6, 2010
    Date of Patent: November 18, 2014
    Assignee: Tel Aviv University Future Technology Development L.P.
    Inventors: Ehud Gazit, Tomer Cohen
  • Publication number: 20140323519
    Abstract: This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I).
    Type: Application
    Filed: April 20, 2012
    Publication date: October 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: M. Arshad Siddiqui, Lianyun Zhao, Amit K. Mandal
  • Patent number: 8835485
    Abstract: The present invention provides a means for prevention and treatment of sarcopenia by administration of a substance that both reduces the sensibility of beta-adrenergic receptors and of 5-HT1a receptors. (S)-pindolol, (S)-propanol, tertalol, or bopindolol are preferred for this purpose.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: September 16, 2014
    Assignee: PsiOxus Therapeutics Limited
    Inventors: Jochen Springer, Stefan Anker, Andrew Coats, John Beadle
  • Publication number: 20140243348
    Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.
    Type: Application
    Filed: January 22, 2014
    Publication date: August 28, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
  • Publication number: 20140228360
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
    Type: Application
    Filed: December 20, 2013
    Publication date: August 14, 2014
    Applicant: Epizyme, Inc.
    Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof
  • Publication number: 20140199368
    Abstract: Provided herein are compositions and related methods useful for prevention or mitigation of ionizing radiation-induced esophagitis. The compositions comprise compounds comprising a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent or mitigate esophageal damage caused by radiation.
    Type: Application
    Filed: November 15, 2011
    Publication date: July 17, 2014
    Applicant: University of Pittsburg-Of the Commonwealth System of Higher Education-Office of Technolology Manage
    Inventors: Michael W. Epperly, Xiang Gao, Joel S. Greenberger, Song Li, Peter Wipf
  • Publication number: 20140194485
    Abstract: Provided herein are isoindole derivatives, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 10, 2014
    Applicant: Celgene Corporation
    Inventors: Hon-Wah Man, Louise Michelle Cameron, Anthony Joseph Frank
  • Patent number: 8748632
    Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: June 10, 2014
    Assignees: Sanford-Burnham Medical Research Institute, The Regents of the University of California
    Inventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique, Svetlana Semenova, Athinia Markou
  • Patent number: 8748411
    Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 10, 2014
    Assignee: Centro de Ingenieria Genetica y Biotechnologia
    Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
  • Patent number: 8722723
    Abstract: A compound represented by the following general formula (I) (R1 and R2 represent hydrogen atom, an alkyl group, a halogen atom, etc.; R3 and R4 represent hydrogen atom, an alkyl group, an alkoxy group, or an alkenyl group; R5 represents hydrogen atom, an alkyl group, or nitro group, and R6 represents hydrogen atom or an alkyl group), which acts on the transcription process of genes.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 13, 2014
    Assignee: Research Foundation Itsuu Laboratory
    Inventors: Nobuko Fujimaki, Madoka Nakagomi, Koichi Shudo
  • Patent number: 8722708
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6?R7?); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7? are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: May 13, 2014
    Assignees: Merck Sharp & Dohme Inc., Pharmacopeia Drug Discovery, Inc.
    Inventors: Andrew Stamford, Guoqing Li, William Greenlee, Zhaoning Zhu, Brian McKittrick, Robert Mazzola, Ying Huang, Tao Guo, Thuy X. H. Le, Gang Qian, Yuefei Shao
  • Patent number: 8716527
    Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2- substituted-p-quinone derivatives as disclosed herein.
    Type: Grant
    Filed: March 4, 2009
    Date of Patent: May 6, 2014
    Assignee: Edison Pharmaceuticals, Inc.
    Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christopher R. Cornell
  • Patent number: 8716252
    Abstract: Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: May 6, 2014
    Assignee: Celgene Corporation
    Inventors: Peter H. Schafer, Anthony J. Frank, Hon-Wah Man, Sai L. Shankar
  • Patent number: 8716326
    Abstract: The present invention relates to an amide compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition comprising the same. The inventive amide compound facilitates bone formation and inhibits bone loss, and is therefore useful for preventing and treating bone disorders such as osteoporosis, osteodystrophy, bone fracture, periodontal disease, Paget's disease, bone metastasis, and rheumatoid arthritis.
    Type: Grant
    Filed: May 14, 2010
    Date of Patent: May 6, 2014
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Jung Nyoung Heo, Bum Tae Kim, Hyuk Lee, Sung Youn Chang, Zang Hee Lee, Seong Hwan Kim, Hyun-Mo Ryoo
  • Publication number: 20140093561
    Abstract: Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders.
    Type: Application
    Filed: January 9, 2012
    Publication date: April 3, 2014
    Applicant: CELGENE CORPORATION
    Inventors: Ming J. Chen, Ho-Wah Hui, Thomas Lee, Paul Kurtulik, Sekhar Surapaneni
  • Publication number: 20140080802
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: October 28, 2013
    Publication date: March 20, 2014
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
  • Publication number: 20140018404
    Abstract: Provided herein are controlled release oral dosage forms of poorly soluble drugs, methods of making the dosage forms, and methods of their use for the treatment of various diseases and/or disorders.
    Type: Application
    Filed: December 15, 2011
    Publication date: January 16, 2014
    Applicant: Celgene Corporation
    Inventors: Ming J. Chen, Ho-wah Hui, Xiaole Shen
  • Patent number: 8618158
    Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.
    Type: Grant
    Filed: June 25, 2009
    Date of Patent: December 31, 2013
    Assignee: Cancer Research Technology Limited
    Inventors: Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcastle, Eric Valeur, Anna Frances Watson, Martin Noble
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130317010
    Abstract: To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HT5A receptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HT5A receptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed.
    Type: Application
    Filed: August 1, 2013
    Publication date: November 28, 2013
    Applicant: Astellas Pharma Inc
    Inventors: Wataru HAMAGUCHI, Isao KINOYAMA, Yohei KOGANEMARU, Takehiro MIYAZAKI, Osamu KANEKO, Ryuichi SEKIOKA, Takuya WASHIO
  • Publication number: 20130295141
    Abstract: The present invention relates to ?-hydroxy and amino-substituted carboxylic acids, which act as matrix metalloproteinase inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for their synthesis, and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune, and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase.
    Type: Application
    Filed: July 8, 2013
    Publication date: November 7, 2013
    Inventors: Viswajanani J. SATTIGERI, Venkata P. PALLE, Manoj Kumar KHERA, Ranadheer REDDY, Manoj Kumar TIWARI, Ajay SONI, Abdul Rehman Abdul RAUF, Sony JOSEPH, Arpita MUSIB, Sunanda G. DASTIDAR, Punit Kumar SRIVASTAVA
  • Patent number: 8575193
    Abstract: Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: November 5, 2013
    Assignee: 4SC AG
    Inventors: Thomas Maier, Christian Hesslinger, Barbara Beckers
  • Publication number: 20130281450
    Abstract: The present invention provides for compounds of formula (I) wherein A, Y, J, R1, R2, and R3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.
    Type: Application
    Filed: March 12, 2013
    Publication date: October 24, 2013
    Inventors: John K. Pratt, Dachun Liu, Chang H. Park, George S. Sheppard, Lisa A. Hasvold, Le Wang
  • Publication number: 20130261120
    Abstract: The present invention relates to: *combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; *use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and *a kit comprising such a combination.
    Type: Application
    Filed: September 29, 2011
    Publication date: October 3, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Florian Pühler, Marion Hitchcock
  • Patent number: 8530469
    Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: September 10, 2013
    Assignee: Astex Therapeutics Ltd.
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
  • Patent number: 8513235
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: August 20, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • Publication number: 20130210880
    Abstract: The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 15, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Patent number: 8466169
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: June 18, 2013
    Assignee: Sanofi
    Inventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
  • Publication number: 20130143926
    Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
    Type: Application
    Filed: June 10, 2011
    Publication date: June 6, 2013
    Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
  • Publication number: 20130136770
    Abstract: Provided herein are methods for modulating immune responses to a respiratory viral infection (e.g., influenza, rhinovirus, coronavirus, or paramyxovirus) in a subject, wherein the methods comprise administering to the subject a compound (e.g., a PDE4 modulator or an immunomodulatory compound), or a pharmaceutically acceptable salt, solvate, hydrate, or stereoisomer thereof. Also provided herein are methods for treating, preventing, ameliorating, and/or delaying the onset of one or more symptoms associated with or resulting from a respiratory viral infection (e.g., influenza, rhinovirus, coronavirus, or paramyxovirus) in a subject, wherein the methods comprise administering to the subject a compound (e.g., a PDE4 modulator or an immunomodulatory compound), or a pharmaceutically acceptable salt, solvate, hydrate, or stereoisomer thereof.
    Type: Application
    Filed: April 5, 2011
    Publication date: May 30, 2013
    Applicant: CELGENE CORPORATION
    Inventor: Jerome B. Zeldis
  • Publication number: 20130116204
    Abstract: Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.
    Type: Application
    Filed: December 21, 2010
    Publication date: May 9, 2013
    Applicant: Celgene Corporation
    Inventors: Peter H. Schafer, Anthony J. Frank, Hon-Wah Man, Sai L. Shankar
  • Publication number: 20130102626
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 25, 2013
    Inventors: Peter Wipf, Marie Celine Frantz
  • Publication number: 20130072519
    Abstract: Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.
    Type: Application
    Filed: May 9, 2011
    Publication date: March 21, 2013
    Inventors: Edward Lee Conn, David Hepworth, Yingmei Qi, Benjamin Neil Rocke, Roger Benjamin Ruggeri, Yan Zhang
  • Publication number: 20130059853
    Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
    Type: Application
    Filed: April 28, 2011
    Publication date: March 7, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen