Chalcogen In The Hetero Ring Patents (Class 540/488)
  • Patent number: 9783512
    Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: October 10, 2017
    Assignee: Wisconsin Alumi Research Foundation
    Inventors: Jennifer Schomaker, Luke Boralsky, John Hershberger, Jared Rigoli, Christopher S. Adams
  • Patent number: 9221842
    Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: December 29, 2015
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Jennifer Schomaker, Luke Boralsky, John Hershberger, Jared Rigoli, Christopher S. Adams
  • Patent number: 8981087
    Abstract: Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: March 17, 2015
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva, Alexander Richard Liam Cecil, Thomas James Hill
  • Patent number: 8962610
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20140296201
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Publication number: 20140220122
    Abstract: The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo.
    Type: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: BHI Limited Partnership
    Inventors: Xianqi KONG, Mohamed ATFANI, Benoit BACHAND, Abderrahim BOUZIDE, Stephane CIBLAT, Sophie LEVESQUE, David MIGNEAULT, Isabelle VALADE, Xinfu WU, Daniel DELORME
  • Publication number: 20140120233
    Abstract: The present invention relates to a method for producing a novel lanthionine derivative having a CaSR agonist activity, an intermediate compound of the lanthionine derivative, and use of the intermediate compound for production of a CaSR agonist, a kokumi-imparting agent, and a food and/or beverage ingredient.
    Type: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Applicant: AJINOMOTO CO., INC.
    Inventors: Yumiko Kato, Toshimi Mizukoshi, Yumiko Suzuki, Seiichi Sato
  • Patent number: 8697863
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: March 7, 2013
    Date of Patent: April 15, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Elfatih Elzein, Dmitry Koltun, Xiaofen Li, Jeff Zablocki, Chandrasekar Venkataramani
  • Publication number: 20140045821
    Abstract: Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.
    Type: Application
    Filed: December 8, 2011
    Publication date: February 13, 2014
    Inventors: Peter Wipf, Qiming Jan Wang
  • Patent number: 8586732
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: November 19, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20130296304
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Application
    Filed: September 28, 2011
    Publication date: November 7, 2013
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20130274464
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: June 10, 2013
    Publication date: October 17, 2013
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 8551982
    Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
    Type: Grant
    Filed: March 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20130237522
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: April 19, 2013
    Publication date: September 12, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • Publication number: 20130210804
    Abstract: The present invention is directed to tricyclic compounds which are positive allosteric modulators of metabotropic glutamate receptors, particularly the mGluR5 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 15, 2013
    Inventors: Neville J. Anthony, Robert P. Gomez, Jing Li, Swati P. Mercer, Anthony J. Roecker, Craig A. Stump, Theresa M. Williams
  • Publication number: 20130190289
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 25, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130089624
    Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 11, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
  • Publication number: 20130079321
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 26, 2012
    Publication date: March 28, 2013
    Applicant: GENENTECH, INC.
    Inventor: GENENTECH, INC.
  • Patent number: 8362005
    Abstract: Compounds of formula (I): wherein variables B, m, n, J, R4, Ea, Eb, Ec, Re, Rf, RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: January 29, 2013
    Assignee: Merk. Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Howard G. Selnick
  • Publication number: 20130012492
    Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
    Type: Application
    Filed: June 29, 2012
    Publication date: January 10, 2013
    Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
  • Publication number: 20130005962
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-5-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu HAN, Kai GERLACH, Dhileepkumar KRISHNAMURTHY, Burkhard MATTHES, Herbert NAR, Roland PFAU, Henning PRIEPKE, Annette SCHULER-METZ, Chris H. SENANAYAKE, Peter SIEGER, Wenjun TANG, Wolfgang WIENEN, Yibo XU, Nathan K. YEE
  • Publication number: 20120282386
    Abstract: The present invention provides a variety of compounds having a CaSR agonist activity which possesses a superior kokumi-imparting function, and more particularly provides a kokumi-imparting composition, which contains the foregoing compound, and/or another substance having a CaSR agonist activity, in combination. The present invention also provides a kokumi-imparting composition which includes a lanthionine derivative and/or another substance having a CaSR agonist activity.
    Type: Application
    Filed: June 26, 2012
    Publication date: November 8, 2012
    Inventors: Seiichi Sato, Fumie Futaki, Reiko Yasuda, Sachise Eto, Yumiko Suzuki, Takaho Tajima, Yuzuru Eto, Yuki Tahara
  • Publication number: 20120277192
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: December 15, 2010
    Publication date: November 1, 2012
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Publication number: 20120189623
    Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:
    Type: Application
    Filed: April 3, 2012
    Publication date: July 26, 2012
    Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
  • Publication number: 20120184520
    Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 19, 2012
    Applicant: Astellas Pharma Inc.
    Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
  • Publication number: 20120178733
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: August 19, 2011
    Publication date: July 12, 2012
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • Publication number: 20120171245
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: December 15, 2011
    Publication date: July 5, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann
  • Patent number: 8202857
    Abstract: This invention relates to novel compounds of the Formula (I), (I*), (I**), I, Ia, Ib, Ic, Id, Ie, If, Ig, Il1-3, Im1-3, In1-3, or Io1-2, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: August 11, 2009
    Date of Patent: June 19, 2012
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Colin M. Tice, Suresh B. Singh, Yuanjie Ye, Wei Zhao, Katerina Leftheris
  • Patent number: 8198267
    Abstract: The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: June 12, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Swen Allerheiligen, Marcus Bauser, Hartmut Schirok, Michael Härter, Stephan Siegel, Ulrich Rester, Christoph Gerdes, Stefan Heitmeier, Georges Von Degenfeld, Anja Buchmüller, Elke Dittrich-Wengenroth, Uwe Saatman, Julia Strassburger, Mark Jean Gnoth, Dieter Lang
  • Patent number: 8129358
    Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: March 6, 2012
    Assignee: Novartis AG
    Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
  • Publication number: 20120040961
    Abstract: The present invention relates to novel pyrimido-diazepinone compounds, methods of modulating protein kinases, including MPS1 (TTK), ERK5 (BMK1, MAPK7), polo kinase 1, 2, 3, or 4, Ack1, Ack2, AbI, DCAMKL1, ABL1, AbI mutants, DCAMKL2, ARK5, BRK, MKNK2, FGFR4, TNK1, PLK1, ULK2, PLK4, PRKD1, PRKD2, PRKD3, ROS 1, RPS6KA6, TAOK1, TAOK3, TNK2, Bcr-Abl, GAK, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, AxI, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-H, Rsk1, SGK, TrkA, TrkB and TrkC, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: January 6, 2010
    Publication date: February 16, 2012
    Applicant: DANA-FARBER CANCER INSTITUTE
    Inventors: Nathanael S. Gray, Xianming Deng, Nicholas Paul Kwiatkowski
  • Publication number: 20120040962
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for treatment of hepatitis C.
    Type: Application
    Filed: March 25, 2010
    Publication date: February 16, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Leping Li, Min Zhong
  • Publication number: 20120029187
    Abstract: Novel herbicides are provided. A haloalkylsulfonanilide derivative represented by the formula (1) or an agrochemically acceptable salt thereof: the formula (1): wherein Z is —C(R9)(R10)— or —N(R11)—, A is an oxygen atom, a sulfur atom or —N(R12)—, W is an oxygen atom or a sulfur atom, m is an integer of from 0 to 3, n is an integer of from 0 to 3, m+n is from 1 to 3, R1 is halo C1-C6 alkyl, R2 is a hydrogen atom, C1-C6 alkyl or the like, each of R3 and R4 is independently a hydrogen atom, C1-C6 alkyl or the like, each of R5, R6, R7, R8, R9 and R10 is independently a hydrogen atom, a halogen, C1-C6 alkyl or the like, each of R11 and R12 is a hydrogen atom, C1-C6 alkyl, halo C1-C6 alkyl or the like, and X is independently a hydrogen atom, a halogen, C1-C6 alkyl, or the like.
    Type: Application
    Filed: April 14, 2010
    Publication date: February 2, 2012
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Masanori Kai, Takamasa Furuhashi, Yoshihide Masuzawa, Tetsuhiko Yano, Fumiyo Saito, Yoshihiko Nakaya
  • Patent number: 8048825
    Abstract: A haloalkylsulfonanilide derivative represented by general formula (I) or a salt thereof wherein R1 represents a halo(C1-C8)alkyl group, R2, R3, R4, R5, R6, R7, R8, R9 and R10 represent hydrogen atoms, etc., n represents 1 or 2, A represents an oxygen atom, W represents an oxygen atom, X represents a halogen atom and m represents an integer of 0 to 4, are compounds useful as herbicides having both of remarkable herbicidal effect and characteristics such as excellent crop-weed selectivity.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: November 1, 2011
    Assignee: Nihon Nohyaku Co., Ltd.
    Inventors: Tomokazu Hino, Yasuko Yamada, Toshihiko Shigenari, Koki Mametsuka
  • Publication number: 20110196147
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 4, 2011
    Publication date: August 11, 2011
    Inventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • Patent number: 7994160
    Abstract: Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula I indicates a single bond or a double bond; X is O, S or N—R5; R1, R2 are independently selected from the group consisting of H, NH2, NH—C1-C6-alkyl, OH, ?O, (i.e.
    Type: Grant
    Filed: July 12, 2006
    Date of Patent: August 9, 2011
    Assignee: Abbott GmbH & Co. KG
    Inventors: Sean C. Turner, Margaretha Bakker, Roland Grandel, Michael Vierling
  • Publication number: 20110160184
    Abstract: Compounds the following formula: wherein Z is as described in the specification, pharmaceutically acceptable salts thereof, compositions comprising the same, and methods of treating bipolar disorder, an anxiety disorder, a mood disorder or schizophrenia or other psychotic disorder with said compounds.
    Type: Application
    Filed: June 18, 2009
    Publication date: June 30, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Dean Brown, Steven Wesolowski, Dan Widzowski, James R. Damewood, M. Edward Pierson, Jr., Michael Wood, Philip Edwards, James Hulsizer, Ashokkumar Bhikkappa Shenvi, James Campbell Muir
  • Patent number: 7968707
    Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Grant
    Filed: February 27, 2007
    Date of Patent: June 28, 2011
    Assignee: Abbott Laboratories
    Inventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
  • Publication number: 20110152246
    Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
    Type: Application
    Filed: December 16, 2010
    Publication date: June 23, 2011
    Applicant: InterMune, Inc.
    Inventors: Brad Buckman, John B. Nicholas, Vladimir Serebryany, Scott D. Seiwert
  • Patent number: 7960373
    Abstract: The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: June 14, 2011
    Assignee: Sanofi-Aventis
    Inventors: Jidong Zhang, Yannick Benedetti, Frederico Nardi, Alain Commerçon
  • Publication number: 20110077236
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: December 2, 2010
    Publication date: March 31, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Kai GERLACH, Roland PFAU, Norbert HAUEL, Iris KAUFFMANN-HEFNER, Georg DAHMANN, Herbert NAR, Sandra HANDSCHUH, Wolfgang WIENEN, Annette SCHULER-METZ
  • Publication number: 20110077235
    Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula (I); wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: March 30, 2009
    Publication date: March 31, 2011
    Inventors: Edcon Chang, Tracy Duong, Takehiro Hirano, Matthew H. McNiell, Yoshito Terao, Angie Vassar
  • Publication number: 20100317848
    Abstract: The present invention relates to a process for the manufacturing of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) and their precursors in high optical purity to the precursors of the synthesis of substituted S-Amino-tetrahydrofuran-S-carboxylic acid amides of general formula (I) in high optical purity, and to the tautomers, enantiomers, diastereomers, mixtures and salts of substituted 3-amino-tetrahydrofuran-3-carboxylic acid amides of general formula (I) in high optical purity, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Application
    Filed: December 21, 2007
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Zhengxu Han, Kai Gerlach, Dhileepkumar Krishnamurthy, Burkhard Matthes, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Chris H. Senanayake, Peter Sieger, Wenjun Tang, Wolfgang Wienen, Yibo Xu, Nathan K. Yee
  • Publication number: 20100298293
    Abstract: The invention relates to novel substituted oxazolidinones, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases, and to the use thereof for producing medicaments for treatment and/or prophylaxis of diseases, especially of thromboembolic disorders.
    Type: Application
    Filed: June 13, 2008
    Publication date: November 25, 2010
    Applicant: BAYER SCHERING PHARMA ATIENGESELLSCHAFT
    Inventors: Swen Allerheiligen, Marcus Bauser, Hartmut Schirok, Michael Härter, Stephan Siegel, Ulrich Rester, Christoph Gerdes, Stefan Heitmeier, Georges Von Degenfeld, Anja Buchmüller, Elke Dittrich-Wengenroth, Uwe Saatman, Julia Strassburger, Mark Jean Gnoth, Dieter Lang
  • Patent number: 7820646
    Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:
    Type: Grant
    Filed: January 3, 2008
    Date of Patent: October 26, 2010
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
  • Publication number: 20100256082
    Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.
    Type: Application
    Filed: June 12, 2007
    Publication date: October 7, 2010
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventor: Robert J. Schotzinger
  • Publication number: 20100256113
    Abstract: As a result of extensive studies on NAD(P)H oxidase inhibitors, the present inventors found that a quinolone derivative having, at the 2-position, an alkyl group substituted with a heteroatom or the like has an excellent NAD(P)H oxidase inhibitory activity, and accomplished the present invention. The compound of the present invention has a reactive oxygen species production inhibitory activity based on the NAD(P)H oxidase inhibitory activity, and therefore can be used as an agent for preventing and/or treating diabetes, impaired glucose tolerance, hyperlipidemia, fatty liver, diabetic complications and the like.
    Type: Application
    Filed: September 25, 2008
    Publication date: October 7, 2010
    Applicant: Astellas Pharma Inc.
    Inventors: Kenichi Onda, Kenichiro Imamura, Fumie Sato, Hiroyuki Moritomo, Yasuharu Urano, Yuki Sawada, Naoki Ishibashi, Keita Nakanishi, Kazuhiro Yokoyama, Shigetada Furukawa, Kazuhiro Momose
  • Publication number: 20100249088
    Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.
    Type: Application
    Filed: October 23, 2008
    Publication date: September 30, 2010
    Applicant: Astellas Pharma Inc.
    Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
  • Publication number: 20100204201
    Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: April 15, 2010
    Publication date: August 12, 2010
    Inventors: Joseph P. Vacca, Linda S. Payne, Richard C.A. Isaacs