Oxadiazoles (including Hydrogenated) Patents (Class 514/364)
  • Nitric oxide enhancing prostaglandin compounds, compositions and methods of use
    Patent number: 8846674
    Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.
    Type: Grant
    Filed: October 18, 2011
    Date of Patent: September 30, 2014
    Assignee: Nicox, S.A.
    Inventor: David S. Garvey
  • 2-thio-1,3,4-oxadiazoles azetidine derivatives as sphingosine-1 phosphate receptors modulators
    Patent number: 8846729
    Abstract: The present invention relates to 2-thio-1,3,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Grant
    Filed: November 7, 2013
    Date of Patent: September 30, 2014
    Assignee: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
  • Haloalkyl heteroaryl benzamide compounds
    Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • 4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators
    Patent number: 8846655
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Ra, and Y are defined herein.
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: September 30, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
  • Pharmaceutical composition for inhibiting apoptosis of neuron or neurodegeneration
    Patent number: 8841335
    Abstract: Provided is a pharmaceutical composition for inhibiting apoptosis of neurons or neurodegeneration. The pharmaceutical composition effectively prevents or treats diseases related to apoptosis of neurons or neurodegeneration.
    Type: Grant
    Filed: May 3, 2011
    Date of Patent: September 23, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol Hyoung Park, Hye Kyung Min, In Suk Park, Mi Jung Lim, Ji Won Lee, Jin Yong Chung, Yeo Jin Yoon, Joo Young Park
  • Compositions, formulations and methods for treating ocular diseases
    Publication number: 20140275103
    Abstract: Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Kevin Peters, Robert Shalwitz, John Janusz, Alexander Smith
  • NOVEL NON-STEROIDAL COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS
    Publication number: 20140275186
    Abstract: This invention relates to novel 4,5-dihydroisoxazoles and 4,5-dihydro[1,2,4]-oxadiazoles of formula (I), to their use as androgenic or antiandrogenic agents or androgen receptor modulators, and to methods of their preparation.
    Type: Application
    Filed: October 17, 2012
    Publication date: September 18, 2014
    Inventors: Juha Pulkkinen, Pekka Poutiainen, Tuomas Oravilahti, Jorma Palvimo, Mikael Perakyla, Reino Laatikainen, Tarja Ihalainen
  • OXABICYCLO [2.2.2] ACID GPR120 MODULATORS
    Publication number: 20140275173
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Hao Zhang, Peter T.W. Cheng, Sean Chen, Shiwei Tao, Shung C. Wu, Lidet A. Negash
  • 3,5-DISUBSTITUTED-1,3,4-OXADIAZOL-2(3H)-ONES AND COMPOSITIONS AND METHODS FOR CONTROLLING NEMATODE PESTS
    Publication number: 20140274690
    Abstract: Provided herein are new 3,5-disubstituted-1,3,4-oxadiazol-2(3H)-ones and derivatives thereof that exhibit nematicidal activity and are useful, for example, in methods for the control of unwanted nematodes.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Monsanto Technology LLC
    Inventors: Urszula J. Slomczynska, Matthew W. Dimmic, William P. Haakenson, JR., Al S. Wideman
  • HETEROCYCLIC DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONIST ACTIVITY
    Publication number: 20140275074
    Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 24, 2012
    Publication date: September 18, 2014
    Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
  • MINERALOCORTICOID RECEPTOR ANTAGONISTS
    Publication number: 20140275133
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Application
    Filed: October 8, 2012
    Publication date: September 18, 2014
    Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
  • SMALL MOLECULE MALARIAL ALDOLASE-TRAP ENHANCERS AND GLIDEOSOME INHIBITORS
    Publication number: 20140275088
    Abstract: In one aspect, the present invention relates to a method of identifying compounds useful in modifying the activity of Aldolase.
    Type: Application
    Filed: October 25, 2012
    Publication date: September 18, 2014
    Inventors: Timothy J. Cardozo, Jürgen Bosch, Sondra Maureen Nemetski
  • Novel S-Nitrosoglutathione Reductase Inhibitors
    Publication number: 20140275185
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Mandelamide heterocyclic compounds
    Patent number: 8835470
    Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R1 is phenyl substituted with zero to 3 substituents; and R1, R2, R3, R4, R5, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, 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 autoimmune diseases and vascular disease.
    Type: Grant
    Filed: April 21, 2011
    Date of Patent: September 16, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert J. Cherney, Yanlei Zhang
  • COMPOUNDS AND METHODS
    Publication number: 20140256740
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: September 11, 2014
    Applicant: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
    Publication number: 20140256744
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: May 21, 2014
    Publication date: September 11, 2014
    Inventors: Ryan Clark, Brian Andrew Stearns, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie M. Arruda
  • MICRORNA MODULATORS AND METHOD FOR IDENTIFYING AND USING THE SAME
    Publication number: 20140255386
    Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.
    Type: Application
    Filed: July 24, 2012
    Publication date: September 11, 2014
    Applicants: NORTH CAROLINA STATE UNIVERSITY, THE WISTAR INSTITUTE
    Inventors: Qihong Huang, Alexander Deiters, Kiranmai Gumireddy
  • Herbicidally active bicyclic 1,3-dione compounds
    Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
    Publication number: 20140249100
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: March 3, 2013
    Publication date: September 4, 2014
    Applicant: Aerpio Therapeutics Inc.
    Inventors: Robert Shalwitz Shalwitz, Kevin Gene Peters
  • HETEROCYCLIC COMPOUNDS
    Publication number: 20140249159
    Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.
    Type: Application
    Filed: May 16, 2012
    Publication date: September 4, 2014
    Inventors: Noriyuki Kurose, Kayoko Hata, Yasuyoshi Iso, Naoko Yamaguchi, Bin Shao, Laykea Tafesse, Xiaoming Zhou, Jianming Yu
  • 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
    Patent number: 8822511
    Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: September 2, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu
  • Pain-relieving compositions and uses therefor
    Patent number: 8822509
    Abstract: This invention discloses compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention discloses the use of sub-normovasodilatory doses of nitric oxide donors in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. According to some embodiments of the present invention, nitric oxide donors are administered by any suitable route so as to provide concentrations of NO that are about ½ to 10?15 of those known to induce vasodilation in normal circulations.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: September 2, 2014
    Assignee: The University of Queensland
    Inventor: Maree Therese Smith
  • Substituted 3-phenyl-1,2,4-Oxadiazole compounds
    Patent number: 8822510
    Abstract: Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; and Q is H, C1-6alkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: September 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Soo S. Koo, Anurag S. Srivastava, Robert V. Moquin, Scott Hunter Watterson
  • Biaryl oxyacetic acid compounds
    Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • COMPOUNDS, COMPOSITIONS, AND METHODS FOR PREVENTING METASTASIS OF CANCER CELLS
    Publication number: 20140242026
    Abstract: Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Inventors: Robert Shalwitz, Kevin Gene Peters
  • COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM
    Publication number: 20140243366
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: CalciMedica, Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF
    Publication number: 20140243334
    Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Oxadiazole derivatives
    Patent number: 8815919
    Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: August 26, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
  • SUBSTITUTED PYRAZOLES AS SPHINGOSINE RECEPTOR MODULATORS
    Publication number: 20140235587
    Abstract: The present invention relates to substituted pyrazoles, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 21, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • COMPOUNDS AND COMPOSITIONS AS SELECTIVE ESTROGEN RECEPTOR DEGRADERS
    Publication number: 20140235660
    Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 21, 2014
    Applicant: NOVARTIS AG
    Inventors: Heather Elizabeth BURKS, Michael A. DECHANTSREITER, Guo HE, Jill NUNEZ, Stefan PEUKERT, Clayton SPRINGER, Yingchuan SUN, Noel Marie-France THOMSEN, George Scott TRIA, Bing YU
  • COMPOUNDS FOR NONSENSE SUPPRESSION, AND METHODS FOR THEIR USE
    Publication number: 20140235586
    Abstract: The present invention relates to methods, compounds, and compositions for treating or preventing diseases associated with nonsense mutations in an mRNA by administering the compounds or compositions of the present invention. More particularly, the present invention relates to methods, compounds, and compositions for suppressing premature translation termination associated with a nonsense mutation in an mRNA.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: PTC Therapeutics, Inc.
    Inventors: Jeffrey A. Campbell, Atiyya Kahn, James Takasugi, Ellen Welch
  • 3,5-DISUBSTITUTED-4,5-DIHYDRO-1,2,4-OXADIAZOLES AND COMPOSITIONS AND METHODS FOR CONTROLLING NEMATODE PESTS
    Publication number: 20140235439
    Abstract: Provided herein are new 3,5-disubstituted-4,5-dihydro-1,2,4-oxadiazoles that exhibit nematicidal activity and are useful, for example, in compositions and methods for the control of unwanted nematodes.
    Type: Application
    Filed: February 14, 2014
    Publication date: August 21, 2014
    Applicant: Monsanto Technology LLC
    Inventors: Urszula J. Slomczynska, William P. Haakenson
  • SUBSTITUTED 1H-PYRAZOL-1,2,4-OXADIAZOLE DERIVATIVES AS SPHINGOSINE RECEPTOR MODULATORS
    Publication number: 20140235588
    Abstract: The present invention relates to substituted 1H-pyrazol-1,2,4-oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 13, 2014
    Publication date: August 21, 2014
    Applicant: Allergan, Inc.
    Inventors: Janet A. Takeuchi, Ling Li, Wha Bin Im, KEN CHOW
  • CRYSTALLINE FORMS OF 3-[5-(2-FLUOROPHENYL)-[1,2,4]OXADIAZOL-3-YL]-BENZOIC ACID
    Publication number: 20140235679
    Abstract: The present invention relates to crystalline forms of 3-[5-(2-fluorophenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid, pharmaceutical compositions and dosage forms comprising the crystalline forms, methods of making the crystalline forms and methods for their use for the treatment, prevention or management of diseases ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay.
    Type: Application
    Filed: April 25, 2014
    Publication date: August 21, 2014
    Applicant: PTC Therapeutics, Inc.
    Inventors: Neil G. Almstead, Peter Seongwoo Hwang, Young-Choon Moon
  • Use of I?B-kinase inhibitors in pain therapy
    Patent number: 8809358
    Abstract: The present invention relates to the use of I?B-kinase Inhibitors and methods for the prophylaxis and therapy for treating pain comprising administering such compounds.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: August 19, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Martin Michaelis, Olaf Ritzeler, Gerhard Jaehne, Karl Rudolphi, Gerd Geisslinger, Hans-Georg Schaible
  • Substituted bisphenyl butanoic acid derivatives as NEP inhibitors with improved in vivo Efficacy
    Publication number: 20140228415
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein X is defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Dean Franklin RIGEL
  • PYRROLINONE CARBOXAMIDE COMPOUNDS USEFUL AS ENDOTHELIAL LIPASE INHIBITORS
    Publication number: 20140228321
    Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 14, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
  • GAMMA SECRETASE INHIBITORS
    Publication number: 20140227302
    Abstract: Disclosed herein are compounds of Formula (I) (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: September 4, 2012
    Publication date: August 14, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett
  • THIAZOLE DERIVATIVES AND USE THEREOF
    Publication number: 20140228365
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Thiazole derivatives and use thereof
    Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Oxadiazole derivatives
    Patent number: 8802704
    Abstract: The invention relates to oxadiazole compounds of formula I. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnès Bombrun
  • Pyrazole oxadiazole derivatives as S1Pagonists
    Patent number: 8802663
    Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight
  • NO- AND H2S- RELEASING COMPOUNDS
    Publication number: 20140221316
    Abstract: This disclosure relates to novel compounds containing an H2S releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a H2S-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration.
    Type: Application
    Filed: August 15, 2012
    Publication date: August 7, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventors: Khosrow Kashfi, Ravinder Kodela
  • THERAPEUTIC COMPOUNDS
    Publication number: 20140221421
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Application
    Filed: January 9, 2014
    Publication date: August 7, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Steven S. BONDY, Carina E. CANNIZZARO, Chien-Hung CHOU, John O. LINK, Qi LIU, Scott D. SCHROEDER, Winston C. TSE, Jennifer R. ZHANG
  • N-HETERO-RING-SUBSTITUTED AMIDE DERIVATIVE
    Publication number: 20140221437
    Abstract: Compounds having an excellent hypoglycemic effect and ? cell- or pancreas-preserving effects or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 7, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Shigeo Yamanoi, Madoka Hatta, Hidenori Namiki, Koji Matsumoto, Tomomi Yoshitomi
  • COMPOSITIONS FOR AN ORALLY ACTIVE 1,2,4-OXADIAZOLE FOR THE TREATMENT OF DISEASE
    Publication number: 20140221436
    Abstract: The present invention relates to specific doses of and dosing regimens for using a 1,2,4-oxadiazole benzoic acid compound in treating or preventing diseases associated with nonsense mutations. In particular, the invention relates to specific doses and dosing regimens for the use of 3-[5-(2-fluoro-phenyl)-[1,2,4]oxadiazol-3-yl]-benzoic acid in mammals having diseases associated with nonsense mutations.
    Type: Application
    Filed: March 21, 2014
    Publication date: August 7, 2014
    Applicant: PTC Therapeutics, Inc.
    Inventors: Samit Hirawat, Langdon Miller
  • METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS OF USE THEREOF
    Publication number: 20140221332
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: May 25, 2012
    Publication date: August 7, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
  • Modulators of sphingosine phosphate receptors
    Patent number: 8796318
    Abstract: Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: August 5, 2014
    Assignee: The Scripps Research Institute
    Inventors: Edward Roberts, Hugh Rosen, Steven Brown, Miguel A. Guerrero, Xuemei Peng, Ramulu Poddutoori
  • 1,3,4-Oxadiazole-2-carboxamide compound
    Patent number: 8796320
    Abstract: Provided is a 1,3,4-oxadiazole-2-carboxamide compound which has STAT3 inhibitory activity and is useful as an anticancer agent. Provided is a 1,3,4-oxadiazole-2-carboxamide compound represented by formula (I) or a pharmacologically acceptable salt thereof (in the formula, Ar represents a furyl group or the like; R1 represents a hydrogen atom or the like; and —X—Y represents a diaryl group such as a biphenyl group).
    Type: Grant
    Filed: December 28, 2010
    Date of Patent: August 5, 2014
    Assignees: General Incorporated Association Pharma Valley Project Supporting Organization, Pharma Design, Shizuoka Prefecture, Kumamoto Health Science University, Kabushiki Kaisha Yakult Honsha
    Inventors: Akira Asai, Kenji Matsuno, Naohisa Ogo, Osamu Takahashi, Yoshiaki Masuda, Ayumu Muroya, Yasuto Akiyama, Tadashi Ashizawa, Tadashi Okawara
  • Heteroaryl substituted pyrazole derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
    Patent number: 8796253
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp