Nitro Or Nitroso In Substituent Q Patents (Class 564/87)
  • Patent number: 9079870
    Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogs, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.
    Type: Grant
    Filed: November 30, 2012
    Date of Patent: July 14, 2015
    Assignee: Indian Institute of Science Education and Research-Pune
    Inventors: Harinath Chakrapani, Satish Ramesh Malwal
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20140378492
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: September 10, 2014
    Publication date: December 25, 2014
    Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
  • Publication number: 20140315130
    Abstract: The present invention provides photoacid generators for use in chemically amplified resists and lithographic processes using the same.
    Type: Application
    Filed: March 19, 2014
    Publication date: October 23, 2014
    Applicant: University Of North Carolina At Charlotte
    Inventors: Kenneth E. Gonsalves, Mingxing Wang
  • Patent number: 8835684
    Abstract: The present invention provides a new process for the preparation of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2R,3S-derivative, but also the 2S,3S-, 2S,2R- and the 2R,3R-derivatives.
    Type: Grant
    Filed: July 21, 2010
    Date of Patent: September 16, 2014
    Assignee: Ampac Fine Chemicals LLC
    Inventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
  • Publication number: 20140228219
    Abstract: The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.
    Type: Application
    Filed: May 29, 2012
    Publication date: August 14, 2014
    Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
  • Publication number: 20140221668
    Abstract: The present invention relates to a process for preparing (R)-5-(2-(benzylamino)ethyl)-1-(6,8-difluorochroman-3-yl)-1H-imidazole-2(3H)-thione, and pharmaceutically acceptable salts thereof, especially the hydrochloride salt. The invention also relates to a process for making intermediates useful in the formation of said compound, and to the intermediates, per se.
    Type: Application
    Filed: June 29, 2012
    Publication date: August 7, 2014
    Applicant: BIAL-PORTELA & CA, S.A.
    Inventors: Alexander Beliaev, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Jonathan Madec, Jean-Marie Schneider, William Maton
  • Publication number: 20140121211
    Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 1, 2014
    Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNE
    Inventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Patent number: 8642808
    Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: February 4, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
  • Publication number: 20140024608
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: January 23, 2014
    Applicant: METHYLGENE INC.
    Inventors: Robert Deziel, Alain Ajamian
  • Publication number: 20130324409
    Abstract: The present invention provides methods of regulating plant stress tolerance.
    Type: Application
    Filed: March 14, 2013
    Publication date: December 5, 2013
    Inventors: SEAN R. CUTLER, ANDREW DEFRIES
  • Patent number: 8552050
    Abstract: The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: October 8, 2013
    Assignee: Beth Israel Deaconess Medical Center
    Inventors: Lewis C. Cantley, Matthew G. Vander Heiden, Heather R. Christofk
  • Publication number: 20130252984
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: March 12, 2013
    Publication date: September 26, 2013
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
  • Publication number: 20130165460
    Abstract: The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: February 20, 2013
    Publication date: June 27, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8425890
    Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: April 23, 2013
    Inventors: David J. Schneider, Charles A. Schneider
  • Publication number: 20130096105
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: November 30, 2012
    Publication date: April 18, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Patent number: 8193194
    Abstract: In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: June 5, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
  • Publication number: 20120064062
    Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.
    Type: Application
    Filed: September 13, 2011
    Publication date: March 15, 2012
    Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
  • Publication number: 20110312918
    Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: Children's Hospital Medical Center
    Inventor: Rashmi Hegde
  • Publication number: 20110313000
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Patent number: 8076513
    Abstract: A process for the preparation of N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives in which a (1-benzyl-2-hydroxy-3-isobutylamino-propyl)-carbamic acid derivative is reacted with a p-nitrophenylsulfonyl halide to provide the desired product in a high yield and degree of purity.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: December 13, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Hartmut Burghard Zinser, Peter Hermann Hölzle
  • Publication number: 20110237553
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: March 16, 2011
    Publication date: September 29, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Patent number: 7964643
    Abstract: The present invention pertains to compounds of the following formula (wherein RP, r, q, RN, Ralk, and Q are as defined herein) and compositions comprising those compounds. The compounds may be used to inhibit osteoclast survival, formation, and/or activity; to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption; in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease; and/or in the treatment of conditions associated with inflammation or activation of the immune system.
    Type: Grant
    Filed: May 23, 2005
    Date of Patent: June 21, 2011
    Assignee: The University Court of the University of Aberdeen
    Inventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
  • Publication number: 20110014186
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: March 23, 2009
    Publication date: January 20, 2011
    Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
  • Publication number: 20100331284
    Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.
    Type: Application
    Filed: May 24, 2010
    Publication date: December 30, 2010
    Applicant: NEUROTECH PHARMACEUTICALS CO., LTD.
    Inventors: Byoung Joo GWAG, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
  • Publication number: 20100324093
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: August 26, 2010
    Publication date: December 23, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20100286444
    Abstract: The present invention provides a new process for the preparation of 2R,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2R,35-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2R,3S-derivative, but also the 2S,3S-, 2S,2R- and the 2R,3R-derivatives.
    Type: Application
    Filed: July 21, 2010
    Publication date: November 11, 2010
    Applicant: Ampac Fine Chemicals LLC
    Inventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
  • Publication number: 20100280074
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: December 3, 2009
    Publication date: November 4, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20100228054
    Abstract: The invention relates to methods for producing sulfonamides of formula I, wherein the variables have the designations cited in the description, by reacting m-nitro-benzoic acid chlorides of formula II with aminosulfons of formula III, under the influence of B equivalents of base IV. Said method is characterised in that, during step a) the aminosulfon of formula III is reacted with B1 equivalents of base IV, and during step b), the reaction mixture resulting from step a) is reacted with m-nitro-benzoic acid chlorides of formula II and B2 equivalents of base IV; B, B1 and B2 having the designations cited in the description.
    Type: Application
    Filed: November 23, 2006
    Publication date: September 9, 2010
    Applicant: BASF SE
    Inventors: Michael Keil, Joachim Gebhardt, Michael Rack, Guido Mayer, Thomas Schmidt, Jan Hendrik Wevers, Sandra Lohr, Axel Pleschke
  • Patent number: 7741519
    Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
    Type: Grant
    Filed: February 1, 2008
    Date of Patent: June 22, 2010
    Assignee: ChemoCentryx, Inc.
    Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
  • Patent number: 7700654
    Abstract: A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinoma, the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
    Type: Grant
    Filed: January 28, 2006
    Date of Patent: April 20, 2010
    Assignee: LTS Lohmann Therapie-Systeme AG
    Inventors: Hans-Rainer Hoffmann, Rudolf Matusch, Aria Baniahmad
  • Publication number: 20100093802
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: December 17, 2009
    Publication date: April 15, 2010
    Applicant: Millennnium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20090312570
    Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: August 21, 2009
    Publication date: December 17, 2009
    Applicant: Anadys Pharmaceuticals, Inc
    Inventors: Stephen E. Webber, Frank Ruebsam, Martin Tran, Peter Dragovich, Liansheng Li, Douglas E. Murphy, David Kucera, Zhongxiang Sun, Chinh V. Tran
  • Publication number: 20090275779
    Abstract: The present invention relates to a method for producing an optically active benzylamine derivative which is useful as an intermediate for pharmaceutical products and the like. In the present invention, an optically active benzylalcohol derivative is reacted with a sulfonylamide derivative in the presence of a phosphine derivative and an azodicarbonyl compound, to obtain an optically active benzylsulfonylamide derivative as a novel compound. Then, the thus-obtained optically active benzylsulfonylamide derivative is reacted with a thiol derivative, thereby producing an optically active benzylamine derivative. According to the present invention, the compound can be easily produced by a simple and short process without racemization.
    Type: Application
    Filed: September 27, 2006
    Publication date: November 5, 2009
    Inventors: Tatsuyoshi Tanaka, Kazumi Okuro, Masaru Mitsuda
  • Patent number: 7608736
    Abstract: The invention relates to a process for the preparation of a compound of formula (I): Which comprises reaction of a compound of formula (II) with a compound of the formula (III) in the presence of a chlorinating agent, followed by reaction of the resultant compound of the formula (IV) with a compound of formula (V) in the presence of a base: wherein the various symbols are as defined in claim 1.
    Type: Grant
    Filed: June 23, 2004
    Date of Patent: October 27, 2009
    Assignee: Bayer CropScience GmbH
    Inventors: Sergiy Pazenok, Mark James Ford, Günter Schlegel
  • Publication number: 20090105473
    Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
    Type: Application
    Filed: November 6, 2008
    Publication date: April 23, 2009
    Applicant: ANADYS PHARMACEUTICALS, INC.
    Inventors: Stephen E. Webber, Frank Ruebsam, Martin Tran, Peter Dragovich, Liansheng Li, Douglas E. Murphy, David Kucera, Zhongxiang Sun, Chinh V. Tran
  • Publication number: 20090054495
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 16, 2008
    Publication date: February 26, 2009
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20080312469
    Abstract: The present invention provides a new process for the preparation of 2S,3S—N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S—N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2R- and the 2R,3R-derivatives.
    Type: Application
    Filed: August 13, 2008
    Publication date: December 18, 2008
    Applicant: Ampac Fine Chemicals LLC
    Inventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
  • Publication number: 20080242861
    Abstract: This invention relates to methods of preparing the compounds of formula (V): Each variable in this formula is defined in the specification.
    Type: Application
    Filed: April 2, 2007
    Publication date: October 2, 2008
    Inventors: Chi-Feng Yen, Chang-Pin Huang, Cheng-Kung Hu, Ming-Chen Chou, Chi-Hsin Richard King
  • Publication number: 20080182906
    Abstract: The invention relates to compounds of the general formula (I) wherein R1, R2, R3, R4, R5, R6, i and j have the meanings given in claim 1, and to the use thereof as caspase-10 inhibitors, especially for the treatment of diabetic retinopathy.
    Type: Application
    Filed: April 6, 2006
    Publication date: July 31, 2008
    Inventors: Claude Lardy, Marc Lecomte, Thierry Convard, Catherine Vidal
  • Publication number: 20080177107
    Abstract: A process for isolating N-butylbenzenesulfonamide (NBBS) from biological material, the chemical synthesis of benzenesulfonamide derivatives, the use of NBBS and benzenesulfonamide derivatives for treating benign prostatic hyperplasia and/or prostate carcinomas the production of medicaments for the treatment thereof, and the use of NBBS and benzenesulfonamide derivatives as a lead substance in the development of active substances for treating benign prostatic hyperplasia and/or prostate carcinoma are provided.
    Type: Application
    Filed: January 28, 2006
    Publication date: July 24, 2008
    Applicant: LTS LOHMANN THERAPIE-SYSTEME
    Inventors: Rudolf Matusch, Aria Baniahmad, Hans-Rainer Hoffmann
  • Patent number: 7378550
    Abstract: The present invention is directed to processes for the synthesis of intermediates useful in the preparation of non-nucleoside reverse transcriptase inhibitors.
    Type: Grant
    Filed: March 26, 2004
    Date of Patent: May 27, 2008
    Assignee: SmithKline Beecham Corporation
    Inventor: Michael Tolar Martin
  • Publication number: 20080119555
    Abstract: The present invention pertains to certain aryl alkyl sulfonamides and derivatives thereof which, inter alia, inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formula: wherein: Ar1 is independently C5-20aryl (e.g., biphenyl, phenanthryl, fluorenyl, or carbazolyl, most preferably biphenyl), and is optionally substituted; RN is independently —H, acyl, C5-20aryl-C1-7alkyl, C3-20heterocyclyl, or C1-7alkyl, and is optionally substituted; Ralk is a C2-10alkylene group, and is optionally substituted; and Q is independently —H or an organic group having from 1 to 30 atoms selected from carbon, nitrogen, oxygen, sulfur, phosphorus, fluorine, chlorine, bromine, and iodine (e.g., an oxy-type group, an amine-type group, etc.); and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof.
    Type: Application
    Filed: May 23, 2005
    Publication date: May 22, 2008
    Inventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
  • Patent number: 7321063
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: January 22, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger D Tung, Mark A Murcko, Govinda R Bhisetti
  • Patent number: 7256204
    Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: August 14, 2007
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
  • Patent number: 7227035
    Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: June 5, 2007
    Assignee: Chemocentryx
    Inventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
  • Patent number: 7208526
    Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: April 28, 2006
    Date of Patent: April 24, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Matthias Koerner, Manfred Kubbies, Raymond Lau, Ulrike Reiff, Georg Tiefenthaler, Wolfgang von der Saal, Timothy Woodcock
  • Patent number: 7169952
    Abstract: A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: January 30, 2007
    Assignee: FMC Corporation
    Inventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
  • Patent number: RE39682
    Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
    Type: Grant
    Filed: March 30, 2005
    Date of Patent: June 5, 2007
    Assignee: Ramot at Tel Aviv University Ltd.
    Inventor: Yoel Kloog