Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/259.2)
  • Patent number: 10934285
    Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, R1, R2 and R3 are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. 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 the aberrant activity of SHP2.
    Type: Grant
    Filed: June 12, 2017
    Date of Patent: March 2, 2021
    Assignee: NOVARTIS AG
    Inventors: Zhuoliang Chen, Jorge Garcia Fortanet, Rajesh Karki, Matthew J. Lamarche, Dyuti Majumdar, Lawrence Blas Perez, Martin Sendzik, Troy Douglas Smith, Fan Yang, Bing Yu
  • Patent number: 10369119
    Abstract: Compositions and methods including Bithionol are provided for treating, inhibiting, or preventing caspase-dependent pathogenic agents in a host cell or infected subject. Examples of caspase-dependent pathogenic agents include ricin, anthrax toxin, Botulinum neurotoxin A, diphtheria toxin, Pseudomonas aeruginosa exotoxin A, cholera toxin, Zika virus, and combinations thereof. Compositions and methods also include Bithionol in combination with an antibiotic for more effective clearance of the pathogen and/or toxins.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: August 6, 2019
    Assignee: Keck Graduate Institute of Applied Life Sciences
    Inventors: Mikhail Martchenko, William Leonardi
  • Patent number: 10328060
    Abstract: Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Grant
    Filed: November 1, 2015
    Date of Patent: June 25, 2019
    Assignees: SHANGHAI FOCHON PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, CHONGQING FOCHON PHARMACEUTICAL CO., LTD.
    Inventors: Xingdong Zhao, Jian Ding, Linghua Meng, Meiyu Geng, Tongshuang Li, Zuwen Zhou, Ling Chen, Qihong Liu, Xianlong Wang, Lijun Yang, Yue Rong, Rui Tan, Chuiliang Yu, Lihua Jiang, Yanxin Liu, Li Linghu, Jing Sun, Weibo Wang
  • Patent number: 10166202
    Abstract: The compounds D9-tetrahydrocannabinol (THC), cannabidiol (CBD) and capsaicin are useful for prevention, treatment, or both, of hepatic encephalopathy. The compounds capsaicin, 2-arachidonoylglycerol (2-AG), HU-308 and cannabidiol are useful for prevention, treatment, or both, of liver cirrhosis.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: January 1, 2019
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem, Hadasit Medical Research Services & Development Ltd., Aristotle University of Thessaloniki
    Inventors: Elliot Berry, Yosefa Avraham, Raphael Mechoulam, Yaron Ilan, Yossi Dagon, Iddo Magen, Nicholas Grigoriadis, Theofilos Poutachidis
  • Patent number: 10064866
    Abstract: This invention relates to methods of treating B-cell malignancies using a combination of inhibitors of JAK1 and/or JAK2 and inhibitors of PI3K?.
    Type: Grant
    Filed: April 7, 2015
    Date of Patent: September 4, 2018
    Assignee: Incyte Corporation
    Inventors: Peggy A. Scherle, Xuesong Liu
  • Patent number: 9988400
    Abstract: The present invention relates to certain thiazolopyrimidinone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: June 5, 2018
    Assignee: Genentech, Inc.
    Inventors: Yu Jiang, Guosheng Wu, Po-Wai Yuen, Elisia Villemure, Jacob Schwarz, Cuong Ly, Benjamin Sellers, Matthew Volgraf
  • Patent number: 9434746
    Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: September 6, 2016
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
  • Patent number: 9149546
    Abstract: A compound that is effective as a diagnostic imaging probe that targets amyloid including is represented by the following formula (1), or salt thereof: wherein R1 is a radioactive halogen substituent, A1 and A2 independently represent CH or N. A diagnostic agent for Alzheimer's disease includes the compound represented by the above formula or a salt thereof. The above compound and the above diagnostic agent for Alzheimer's disease transfer into brain after administration, and indicate good accumulation on amyloid deposited in the brain.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: October 6, 2015
    Assignee: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Yuki Okumura, Yoshifumi Maya, Yoshinari Shoyama, Takako Onishi
  • Patent number: 9051331
    Abstract: The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: June 9, 2015
    Assignee: Sanofi
    Inventors: Rosy Sher, Raymond Walter Kosley, Jr.
  • Publication number: 20150050325
    Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to a drug-eluting stent comprising said compounds and methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
    Type: Application
    Filed: January 16, 2013
    Publication date: February 19, 2015
    Applicant: The Rockefeller University
    Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua McCoy, Wenwei Huang, Min Shen, Jian-Kang Jiang
  • Publication number: 20140378475
    Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), 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: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
  • Publication number: 20140303149
    Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
    Type: Application
    Filed: April 2, 2014
    Publication date: October 9, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
  • Patent number: 8802666
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: August 12, 2014
    Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Publication number: 20140219960
    Abstract: The present invention relates a novel composition for preventing or treating hepatitis C virus, regulating the phosphorylation of a replicase. More specifically, it is possible to prevent or treat hepatitis C using a novel PRK2 inhibitor discovered through structure modeling, and to prevent or treat hepatitis C, particularly, interferon-insensitive hepatitis C through coadministration of an Hsp90 inhibitor.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 7, 2014
    Applicant: Industry-Academic Cooperation Foundation, Yonsei University
    Inventor: Jong-Won Oh
  • Publication number: 20140206536
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: WENMING ZHANG, CALEB WILLIAM HOLYOKE, JR., KENNETH ANDREW HUGHES, GEORGE PHILIP LAHM, THOMAS FRANCIS PAHUTSKI, JR., MY-HANH THI TONG, MING XU
  • Publication number: 20140142120
    Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating cancer in a subject. Also disclosed are methods of inhibiting SCF-Skp2 activity and a method of identifying inhibitors of SCF-Skp2 activity.
    Type: Application
    Filed: October 16, 2013
    Publication date: May 22, 2014
    Applicant: NEW YORK UNIVERSITY
    Inventors: Timothy Cardozo, Michele Pagano, Lily Wu, Leslie I. Gold
  • Publication number: 20140121222
    Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: January 2, 2014
    Publication date: May 1, 2014
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
  • Patent number: 8697707
    Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: April 15, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Caleb William Holyoke, Jr., Wenming Zhang, My-Hanh Thi Tong
  • Publication number: 20140080842
    Abstract: The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 20, 2014
    Applicant: B.R.A.I.N. Biotechnology Research and Information Network AG
    Inventors: Michael Krohn, Dirk Sombroek
  • Publication number: 20140079736
    Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula (I): Q-Y—R1—R2 (I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula (I) in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
    Type: Application
    Filed: April 11, 2012
    Publication date: March 20, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventor: Sanjay A. Desai
  • Publication number: 20140066448
    Abstract: The present invention provides substituted diamino-pyrimidine and substituted diamino-pyridine derivatives of Formula I; wherein X, Y, R1, R2, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: March 13, 2012
    Publication date: March 6, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Andrew P. Combs, Yun-Long Li, Song Mei, Eddy W. Yue
  • Patent number: 8642603
    Abstract: The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: February 4, 2014
    Assignee: Sanofi
    Inventors: Bin Cao, Vieroslava Gurunian, Sathapana Kongsamut, Raymond W. Kosley, Jr., Rosy Sher, Ryan E. Hartung
  • Publication number: 20140024659
    Abstract: The invention relates to N-substituted hetero-bicyclic compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic compounds. The N-substituted hetero-bicyclic compounds of the present invention are defined by the following formula I: wherein A, B, X, Het, R1, R2, W1, W2, W3 and W4 are defined as in the description.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: BASF SE
    Inventors: Ralph Paulini, Carsten Beyer, Henricus Maria Martinus Bastiaans, Nancy B. Rankl
  • Publication number: 20130338002
    Abstract: Disclosed are compounds of Formula 1, wherein X is O or S; Y is O or S; and R1, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 19, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: CALEB WILLIAM HOLYOKE, JR., WENWING ZHANG
  • Publication number: 20130289052
    Abstract: Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I): wherein each symbol is as defined in the present description; and metalaxyl or metalaxyl M.
    Type: Application
    Filed: February 18, 2011
    Publication date: October 31, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Norihisa Sakamoto, Emiko Sakamoto, Atsushi Iwata
  • Publication number: 20130289051
    Abstract: Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I) wherein each symbol is as defined in the description; and at least one disinfectant compound selected from Group (A); Group (A): a group consisting of tebuconazole, difenoconazole, triticonazole, imazalil, triadimenol, fluquinconazole, prochloraz, prothioconazole, diniconazole, diniconazole M, cyproconazole, tetraconazole, ipconazole, triforine, pyrifenox, fenarimol, nuarimol, oxpoconazole fumarate, pefurazoate, triflumizole, azaconazole, bitertanol, bromuconazole, epoxiconazole, fenbuconazole, flusilazole, flutriafol, hexaconazole, imibenconazole, myclobutanil, penconazole, propiconazole, simeconazole and triadimefon.
    Type: Application
    Filed: February 18, 2011
    Publication date: October 31, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Norihisa Sakamoto, Emiko Sakamoto, Atsushi Iwata
  • Publication number: 20130281466
    Abstract: Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I): wherein each symbol is as defined in the description; and at least one disinfectant compound selected from Group (A).
    Type: Application
    Filed: February 18, 2011
    Publication date: October 24, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Norihisa Sakamoto, Emiko Sakamoto, Atsushi Iwata
  • Publication number: 20130251761
    Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.
    Type: Application
    Filed: July 15, 2011
    Publication date: September 26, 2013
    Inventors: Barry S. Coller, Craig Thomas, Marta Filizola, Joshua Mccoy, Wenwei Huang, Min Shen
  • Patent number: 8518955
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: August 27, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: V. S. Prasada Rao Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganpati Kattige
  • Publication number: 20130165453
    Abstract: The invention provides for the use of protein kinase activators or boosters of nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF) or other neurotrophic factors to treat stroke. Specifically, the present invention provides methods of treating stroke comprising the steps of identifying a subject having suffered a stroke and administering to said subject an amount of a pharmaceutical composition comprising a protein kinase C (PKC) activator or 4-methylcatechol acetic acid (MCBA) and a pharmaceutically acceptable carrier effective to treat at least one symptom of stroke.
    Type: Application
    Filed: July 19, 2012
    Publication date: June 27, 2013
    Inventors: Miao-Kun Sun, Daniel L. Alkon
  • Publication number: 20130123240
    Abstract: The present disclosure relates generally to treating or preventing diseases associated with angiogenesis by administering to a patient certain compounds found to inhibit or substantially reduce angiogenesis. Compounds employed according to the present disclosure exhibit good anti-angiogenic activity as well as demonstrate a prophylactic effect for preventing and substantially reducing angiogenesis. Examples of such compounds include Ritanserin, Amiodarone, Terfenadinc, Perphenazine, Bithionol, and Clomipramine.
    Type: Application
    Filed: January 7, 2013
    Publication date: May 16, 2013
    Applicant: Southern Research Institute
    Inventor: Southern Research Institute
  • Publication number: 20130072467
    Abstract: The present invention provides a novel compound having a superior activity as an ERR-? modulator and useful as an agent for the prophylaxis or treatment of ERR-? associated diseases. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: August 3, 2012
    Publication date: March 21, 2013
    Inventors: Shigemitsu MATSUMOTO, Koji Ono, Yusuke Tominari, Taisuke Katoh, Kazuhiro Miwa, Atsushi Hasuoka, Shinichi Imamura
  • Patent number: 8372808
    Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: February 12, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Albee Messing, Woosung Cho, Jon Scott Thorson, Randal D. Goff
  • Publication number: 20130018044
    Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.
    Type: Application
    Filed: December 21, 2010
    Publication date: January 17, 2013
    Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
  • Patent number: 8349845
    Abstract: Use of a compound of formula (I) wherein R is an alicyclic group; an arylethyl group; or phenyl or benzyl substituted by halogen, lower alkyl, alkoxy, OH, NH2, NHalkyl, N(alkyl)2, CN or NO2; in the manufacture of a medicament for the therapy of hyperalgesic pain conditions and their symptoms.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: January 8, 2013
    Assignee: Sosei Group Corporation
    Inventors: Fei-Yue Zhao, Alistair Kerr Dixon, Jonathan Mark Treherne, Chizuko Koseki, Kevin Lee, David Spanswick
  • Publication number: 20130005655
    Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 3, 2013
    Applicant: Somaxon Pharmaceuticals, Inc.
    Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
  • Publication number: 20120322770
    Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.
    Type: Application
    Filed: August 21, 2012
    Publication date: December 20, 2012
    Inventor: Robert P. RICCIARDI
  • Publication number: 20120282255
    Abstract: The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated.
    Type: Application
    Filed: April 6, 2012
    Publication date: November 8, 2012
    Inventor: Greg Plucinski
  • Publication number: 20120184566
    Abstract: The present invention relates to a series of substituted dihydro benzocycloalkyl-oxymethyl oxazolopyrimidinones of formula (I): Wherein n, R1, R2, R3, R4, R5 and R6 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, cognition deficit disorders, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 19, 2012
    Applicant: SANOFI
    Inventors: Rosy SHER, Raymond Walter KOSLEY, JR.
  • Publication number: 20120122679
    Abstract: Disclosed are compounds of Formula 1, N-oxides and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, EC(?X1); a is 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 3, 2010
    Publication date: May 17, 2012
    Applicant: E. I. Du Pont De Nemours and Company
    Inventors: Wenming Zhang, Caleb William Holyoke, JR., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, JR., My-Hanh Thi Tong, Stephen Frederick McCann
  • Publication number: 20120122680
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 3, 2010
    Publication date: May 17, 2012
    Applicant: E.I. Du Pont de Nemours and Company
    Inventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
  • Publication number: 20120115722
    Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.
    Type: Application
    Filed: August 3, 2010
    Publication date: May 10, 2012
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Caleb William Holyoke, JR., Wenming Zhang, My-Hanh Thi Tong
  • Publication number: 20120115886
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 10, 2012
    Inventors: V. S. Prasada Rao LINGAM, Sachin Sundarial CHAUDHARI, Abraham THOMAS, Neelima KHAIRATKAR-JOSHI, Vidya Ganpati KATTIGE
  • Publication number: 20120108576
    Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.
    Type: Application
    Filed: November 30, 2011
    Publication date: May 3, 2012
    Applicant: ACHILLION PHARMACEUTICALS, INC.
    Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
  • Publication number: 20120108570
    Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.
    Type: Application
    Filed: January 6, 2012
    Publication date: May 3, 2012
    Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Miodrag Radulovacki, David W. Carley
  • Patent number: 8119647
    Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: February 21, 2012
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Prasada Rao V. S. Lingam, Sachin Sundarlal Chaudhari, Abraham Thomas, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20110281861
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.
    Type: Application
    Filed: July 2, 2009
    Publication date: November 17, 2011
    Inventors: John Joseph Deadman, Eric Dale Jones, Giang Thanh Le, David Ian Rhodes, Neeranat Thienthong, Nicholas Andrew Vandegraaff, Lisa Jane Winfield
  • Publication number: 20110046136
    Abstract: The present invention relates to functional proteins encoded by nucleic acid sequences comprising a nonsense mutation. The present invention also relates to methods for the production of functional proteins encoded by nucleic acid sequences comprising a nonsense mutation and the use of such proteins for prevention, management and/or treatment of diseases associated with a nonsense mutation(s) in a gene.
    Type: Application
    Filed: March 29, 2007
    Publication date: February 24, 2011
    Applicant: THERAPEUTICS, INC.
    Inventors: Neil G. Almstead, Guangming Chen, Hirawat Samit, Peter Seongwoo Hwang, Gary M. Karp, Langdon Miller, Young-Choon Moon, Hongyu Ren, James J. Takasugi, Ellen M. Welch, Richard G. Wilde, Paul Kennedy
  • Publication number: 20110015212
    Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: June 28, 2010
    Publication date: January 20, 2011
    Inventors: Yun-Long Li, Brian W. Metcalf, Andrew P. Combs
  • Publication number: 20110009366
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.
    Type: Application
    Filed: April 23, 2010
    Publication date: January 13, 2011
    Applicant: AVEXA LIMITED
    Inventors: Eric Dale Jones, Jonathan Alan Victor Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Vandegraff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherinie Macfarlane