Sulfur Containing Hetero Ring Patents (Class 548/527)
  • Patent number: 10683283
    Abstract: The invention relates to substituted ureas, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: June 16, 2020
    Assignee: MEBIAS DISCOVERY, INC.
    Inventors: Brett A. Tounge, Shariff Bayoumy, Lawrence C. Kuo, Scott Dax
  • Patent number: 9535069
    Abstract: A method for measuring cancer related substances including cancer cell-derived free DNA by Raman spectroscopy, involving steps for preparing a biochip having a meso-crystal region of silver oxides containing a silver peroxide, adding a blood serum or a biological sample solution dropwise onto the meso-crystal region of said biochip, selectively trapping the cancer-related substances having a positive charge in the sample, irradiating the trapped cancer-related substance with an exciting laser light and detecting a surface enhanced Raman scattering therefrom, wherein cancer diseases are evaluated on the basis of the intensity of the Surface Enhance Raman Scattering (SERS). In the carbon-specific D band and G band in the Raman scattering spectrum, a characteristic peak spectrum of the cancer-related substance can be detected in the proximity of the methyl group characteristic of 2900 cm?1.
    Type: Grant
    Filed: November 5, 2015
    Date of Patent: January 3, 2017
    Inventors: Hiroaki Ito, Yuki Hasegawa, Katsuyuki Hasegawa
  • Publication number: 20150141427
    Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. 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 in the treatment of cancers.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Applicant: Novartis AG
    Inventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150111944
    Abstract: The invention relates to compounds of formula (I): where A1, A2, A3, A4, G, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 23, 2015
    Applicant: Syngenta Participations AG
    Inventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
  • Patent number: 9006458
    Abstract: A compound for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) and a method of forming the compound is provided. The compound has Formula I: wherein W is selected from the group consisting of an optionally substituted aryl group and an optionally substituted heteroaryl group; each Y independently is NR1R2, wherein R1 and R2 are independently selected from the group consisting of H and C1-C6 alkyl, or R1 and R2 combine to form together with the nitrogen to which they are attached a heterocyclic group with 4 to 5 carbon atoms, is used to denote a single or a double bond, and Z is NH, NH2, NH—(C?O)—(CH2)n—SH, wherein n=1 to 10, or or a tautomer or stereoisomer thereof, or a salt thereof. A method and device for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) is also provided.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: April 14, 2015
    Assignee: Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Kaustabh Kumar Maiti, Dinish Unnimadhava Kurup Soudamini Amma, Chit Yaw Fu, Malini Olivo, Kiat Seng Jason Soh, Seong-Wook Yun
  • Publication number: 20150073004
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: November 18, 2014
    Publication date: March 12, 2015
    Inventors: Imre BATA, Veronika BARTONE BODOR, Attila VASAS, Peter BUZDER-LANTOS, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Zsuzsanna SZAMOSVOLGYI
  • Publication number: 20150073139
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 12, 2015
    Inventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
  • Patent number: 8962863
    Abstract: The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments of the invention, the compounds are useful for treating ocular disorders, such as, for example, glaucoma, lowering of elevated intraocular pressure, and the like. In other embodiments, the compounds are useful for treating irritable bowel disease. In further embodiments, the compounds are useful in promoting hair growth. In still further embodiments, the compounds are useful in promoting wound healing, scar reduction, and the like.
    Type: Grant
    Filed: August 20, 2013
    Date of Patent: February 24, 2015
    Assignee: Allergan, Inc.
    Inventors: Danny T. Dinh, Michael E. Garst, David W. Old, Elizabeth T. Syage, Boris Gorin, Christopher M. Lanthier, Jan Oudenes
  • Publication number: 20150038545
    Abstract: The present invention refers to compounds derived from hydroxyphenyl 1H-pyrrole rings, which have the following formula (I): as well as to the procedure for their preparation, pharmaceutical compositions comprising the same and the use thereof for the treatment and/or prevention of a condition mediated by histone deacetylase such as cancer, hematological malignancies, autoimmune diseases, inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases and psychiatric disorders, cardiovascular diseases, endocrine and metabolic disorders, by inhibiting histone deacetylases and the therapeutic use of biological processes related to the mentioned inhibition.
    Type: Application
    Filed: April 4, 2012
    Publication date: February 5, 2015
    Applicants: UNIVERSIDAD DEL PAÍS VASCO, IKERCHEM, S.L.
    Inventors: Fernando Pedro Cossío Mora, Yosu Ion Vara Salazar, Eider San Sebastián Larzabal, Dorleta Otaegui Ansa, María del Carmen Masdeu Margalef, Eneko Aldaba Arévalo, Maialen Aginagalde Unanue, Sergio Villafruela Cáneva, María Remedios Alcalá Caffarena, Aizpea ZUubia Olascoaga
  • Patent number: 8946447
    Abstract: The invention relates to compounds of formula (I) where A1, A2, A3, A4, G, R1, R2, R3 and R4 are as defined in claim 1; or a salt or JV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: February 3, 2015
    Assignees: Syngenta Limited, Syngenta Crop Protection LLC
    Inventors: Peter Renold, Jérôme Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
  • Patent number: 8940776
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: January 27, 2015
    Assignee: Genzyme Corporation
    Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
  • Publication number: 20150014607
    Abstract: There is provided an organic nonlinear optical material including a polymer binder and a compound represented by the following Formula (I): wherein, in Formula (I), R1 and R2 each independently represent a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group; R3 represents a hydrogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted aryl group; and L represents a divalent linking group connecting a nitrogen atom and an oxopyrroline ring having a dicyanomethylidene group in a ?-conjugated system containing an azo group (—N?N—).
    Type: Application
    Filed: September 26, 2014
    Publication date: January 15, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Akihiro KANEKO, Masaaki TSUKASE, Masataka SATOU
  • Publication number: 20150011553
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 3, 2014
    Publication date: January 8, 2015
    Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • Patent number: 8927589
    Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: January 6, 2015
    Assignee: Allergan, Inc.
    Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8895535
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: November 25, 2014
    Assignee: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Publication number: 20140343070
    Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug the
    Type: Application
    Filed: August 1, 2014
    Publication date: November 20, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20140329796
    Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 16, 2014
    Publication date: November 6, 2014
    Applicant: Ajinomoto Co., Inc.
    Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
  • Patent number: 8853679
    Abstract: A semiconducting compound comprising the structure: where R1 to R4 independently comprise, but are not limited to, optionally substituted straight, branched or cyclic alkyl chains having 2 to 20 (e.g. 2 to 12) carbon atoms, alkoxy, amino, amido, silyl, alkyl, alkenyl, aryl or hetero aryl; where X1 and X2 independently comprise S, O, NR5 or SiR6R7 where R8 to R7 independently comprise C1 to C5 branched, straight or cyclic alkyl chains; and where Ar1 comprises a heterocyclic ring, and where n is an integer between 1 and 4.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Cambridge Display Technology Limited
    Inventors: Sheena Zuberi, Tania Zuberi
  • Patent number: 8853212
    Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: February 17, 2011
    Date of Patent: October 7, 2014
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • 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
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Publication number: 20140275005
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: May 5, 2014
    Publication date: September 18, 2014
    Applicant: Sanofi
    Inventor: Zhongli GAO
  • Patent number: 8815871
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: August 26, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
  • 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
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G 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: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140213588
    Abstract: The present invention provides compounds of Formula (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. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.
    Type: Application
    Filed: September 26, 2012
    Publication date: July 31, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20140187788
    Abstract: The present invention provides processes for the preparation of compounds of formula (I) including processes comprising a. reacting a a compound comprising a thietane moiety in which the carbon atom at the 3 position of the thietane moiety is bonded to a nitrogen atom; wherein the nucleophile is selected the group consisting of: N3?, a sulfonamide having two hydrogen atoms bound to the nitrogen atom, a diimide having a hydrogen atom bound to the nitrogen atom or an anion thereof, NH2OH and NH3; and b. when the nucleophile used in step a. is N3? or NH2OH, reacting the compound produced in step a. with a suitable reducing agent to give a compound of formula (I); or when the nucleophile used in step a. is a sulfonamide, reacting the compound produced in step a. with a reagent suitable for cleaving the S—N bond of the sulfonamide group to give a compound of formula (I); or when the nucleophile used in step a. is a diimide, reacting the compound produced in step a.
    Type: Application
    Filed: July 5, 2012
    Publication date: July 3, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Jerome Yves Cassayre, Edouard Godineau, Mohamed Abdelouahab Boussemghoune, Helmars Smits
  • Publication number: 20140121260
    Abstract: The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: MedWell Laboratories Ltd.
    Inventors: Taher NASSAR, Raiyn Nureldin, Rayan Anwar
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Patent number: 8691816
    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: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140094489
    Abstract: The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) wherein each symbol is as described in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 6, 2013
    Publication date: April 3, 2014
    Applicant: AJINOMOTO CO., INC.
    Inventors: Tamotsu SUZUKI, Takahiro KOSHIBA, Munetaka TOKUMASU, Koji OHSUMI
  • Patent number: 8686025
    Abstract: Disclosed herein is a compound having a structure Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: December 15, 2008
    Date of Patent: April 1, 2014
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Robert M. Burk
  • Patent number: 8673961
    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: Grant
    Filed: August 14, 2009
    Date of Patent: March 18, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140066426
    Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: August 29, 2013
    Publication date: March 6, 2014
    Inventors: Stefan SCHUNK, Melanie REICH, Henning STEINHAGEN, Nils DAMANN, Michael HAURAND, Achim KLESS, Philip SKONE, Richard HAMLYN, Robert KIRBY, Marc ROGERS, Kathy SUTTON
  • Publication number: 20140058117
    Abstract: The present invention provides synthetic processes for the preparation of a variety of well-defined substituted gamma lactams. The compounds that can be prepared by the process of the invention are useful for treating a variety of conditions. In some embodiments of the invention, the compounds are useful for treating ocular disorders, such as, for example, glaucoma, lowering of elevated intraocular pressure, and the like. In other embodiments, the compounds are useful for treating irritable bowel disease. In further embodiments, the compounds are useful in promoting hair growth. In still further embodiments, the compounds are useful in promoting wound healing, scar reduction, and the like.
    Type: Application
    Filed: August 20, 2013
    Publication date: February 27, 2014
    Applicant: Allergan, Inc.
    Inventors: Danny T. Dinh, Michael E. Garst, David W. Old, Elizabeth T. Syage, Boris Gorin, Christopher M. Lanthier, Jan Oudenes
  • Publication number: 20140046069
    Abstract: Arylpyrrolidines of Formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal paracite-controlling agents.
    Type: Application
    Filed: September 13, 2011
    Publication date: February 13, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jun Mihara, Mamoru Hatazawa, Daiei Yamazaki, Hidetoshi Kishikawa, Kei Domon, Hidekazu Watanabe, Norio Sasaki, Tetsuya Murata, Koichi Araki, Eiichi Shimojo, Teruyuki Ichihara, Tadashi Ishikawa, Katsuhiko Shibuya, Ulrich Goergens, Peter Bruechner, Reiner Fischer, Johannes-Rudolf Jansen, Tobias Kapferer, Simon Maechling, Michael Maue, Arnd Voerste
  • Patent number: 8642642
    Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: February 4, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
  • Publication number: 20140024647
    Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 18, 2012
    Publication date: January 23, 2014
    Inventor: Akira Yukimasa
  • Publication number: 20140011845
    Abstract: Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.
    Type: Application
    Filed: December 30, 2011
    Publication date: January 9, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephane Andre Marie Jeanmart, Long Lu, Yaming Wu, Lisheng Mao, Michel Muehlbeach
  • Publication number: 20130338132
    Abstract: Compounds represented by the following formula (I), are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.
    Type: Application
    Filed: June 14, 2012
    Publication date: December 19, 2013
    Applicant: Ajinomoto Co., Inc.
    Inventors: Takahiro Koshiba, Munetaka Tokumasu, Taisuke Ichimaru, Koji Ohsumi, Tadakiyo Nakagawa, Tatsuhiro Yamada, Kayo Matsumoto, Tamotsu Suzuki
  • Patent number: 8586623
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: November 19, 2013
    Assignee: UCB Pharma, S.A.
    Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
  • Publication number: 20130299799
    Abstract: A photoelectric conversion device comprising an electrically conductive film, an organic photoelectric conversion film, and a transparent electrically conductive film, wherein the organic photoelectric conversion film contains a compound represented by the following formula (1) and an n-type organic semiconductor: wherein each of R1 and R2 independently represents a substituted aryl group, an unsubstituted aryl group, a substituted heteroaryl group or an unsubstituted heteroaryl group, each of R3 to R11 independently represents a hydrogen atom or a substituent provided that an acidic group is excluded, m represents 0 or 1, n represents an integer of 0 or more, R1 and R2, R3 and R4, R3 and R5, R5 and R6, R6 and R8, R7 and R8, R7 and R9, or R10 and R11 may be combined each other to form a ring, and when n is an integer of 2 or more, out of a plurality of R7's and R8's, a pair of R7's, a pair of R8's, or a pair of R7 and R8 may be combined each other to form a ring.
    Type: Application
    Filed: July 18, 2013
    Publication date: November 14, 2013
    Inventors: Katsuyuki YOFU, Kimiatsu NOMURA, Mitsumasa HAMANO, Tetsuro MITSUI
  • Publication number: 20130296245
    Abstract: Provided are a compound of formula (I), pharmaceutically acceptable salts thereof, preparation methods and applications thereof for inhibiting thrombin, and applications in the treatment and prevention of thrombin-mediated and thrombin-related diseases.
    Type: Application
    Filed: November 14, 2011
    Publication date: November 7, 2013
    Inventors: Min Li, Hanbin Shan, Yu Huang, Zhedong Yuan, Xiong Yu
  • Publication number: 20130296274
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: September 14, 2011
    Publication date: November 7, 2013
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
  • Patent number: 8575197
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I): wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: November 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Kentaro Asahi, Hiroyuki Tobinaga
  • Publication number: 20130281453
    Abstract: Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 24, 2013
    Applicant: The Scripps Research Institute
    Inventors: Benjamin Cravatt, Daniel Nomura, Jae W. Chang, Raymond E. Moellering, Dan Bachovehin, Weiwei Li