Nitro Or Nitroso In Substituent Q Patents (Class 564/87)
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Patent number: 9079870Abstract: 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: GrantFiled: November 30, 2012Date of Patent: July 14, 2015Assignee: Indian Institute of Science Education and Research-PuneInventors: Harinath Chakrapani, Satish Ramesh Malwal
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Publication number: 20150024032Abstract: 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: ApplicationFiled: July 18, 2014Publication date: January 22, 2015Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
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Publication number: 20140378492Abstract: 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: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Inventors: HAIQING YUAN, RICHARD L. BEARD, MICHAEL E. GARST, JOHN E. DONELLO, XIAOXIA LIU, VEENA VISWANATH
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Publication number: 20140315130Abstract: The present invention provides photoacid generators for use in chemically amplified resists and lithographic processes using the same.Type: ApplicationFiled: March 19, 2014Publication date: October 23, 2014Applicant: University Of North Carolina At CharlotteInventors: Kenneth E. Gonsalves, Mingxing Wang
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Patent number: 8835684Abstract: 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: GrantFiled: July 21, 2010Date of Patent: September 16, 2014Assignee: Ampac Fine Chemicals LLCInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Publication number: 20140228219Abstract: 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: ApplicationFiled: May 29, 2012Publication date: August 14, 2014Inventors: Yosuke Nakashima, Yoshinobu Jin, Masato Konobe
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Publication number: 20140221668Abstract: 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: ApplicationFiled: June 29, 2012Publication date: August 7, 2014Applicant: BIAL-PORTELA & CA, S.A.Inventors: Alexander Beliaev, Jorge Bruno Reis Wahnon, David Alexander Learmonth, Jonathan Madec, Jean-Marie Schneider, William Maton
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Publication number: 20140121211Abstract: 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: ApplicationFiled: November 30, 2012Publication date: May 1, 2014Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNEInventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
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Publication number: 20140107160Abstract: 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: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 8642808Abstract: 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: GrantFiled: April 22, 2011Date of Patent: February 4, 2014Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Publication number: 20140024608Abstract: 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: ApplicationFiled: March 14, 2013Publication date: January 23, 2014Applicant: METHYLGENE INC.Inventors: Robert Deziel, Alain Ajamian
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Publication number: 20130324409Abstract: The present invention provides methods of regulating plant stress tolerance.Type: ApplicationFiled: March 14, 2013Publication date: December 5, 2013Inventors: SEAN R. CUTLER, ANDREW DEFRIES
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Patent number: 8552050Abstract: 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: GrantFiled: August 18, 2008Date of Patent: October 8, 2013Assignee: Beth Israel Deaconess Medical CenterInventors: Lewis C. Cantley, Matthew G. Vander Heiden, Heather R. Christofk
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Publication number: 20130252984Abstract: 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: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicant: ALLERGAN, INC.Inventors: Haiqing YUAN, Richard L. BEARD, Xiaoxia LIU, John E. DONELLO, Veena VISWANATH, Michael E. GARST
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Publication number: 20130165460Abstract: 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: ApplicationFiled: February 20, 2013Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Patent number: 8425890Abstract: 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: GrantFiled: February 23, 2010Date of Patent: April 23, 2013Inventors: David J. Schneider, Charles A. Schneider
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Publication number: 20130096105Abstract: 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: ApplicationFiled: November 30, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8193194Abstract: 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: GrantFiled: May 21, 2008Date of Patent: June 5, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Esther Martinborough, Tim Neubert, Tara Whitney, Danielle Lehsten, Tara Hampton, Nicole Zimmermann, Andreas P. Termin
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Publication number: 20120064062Abstract: 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: ApplicationFiled: September 13, 2011Publication date: March 15, 2012Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
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Publication number: 20110312918Abstract: 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: ApplicationFiled: December 8, 2009Publication date: December 22, 2011Applicant: Children's Hospital Medical CenterInventor: Rashmi Hegde
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Publication number: 20110313000Abstract: 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: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Patent number: 8076513Abstract: 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: GrantFiled: April 25, 2008Date of Patent: December 13, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Hartmut Burghard Zinser, Peter Hermann Hölzle
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Publication number: 20110237553Abstract: 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: ApplicationFiled: March 16, 2011Publication date: September 29, 2011Applicant: ABBOTT LABORATORIESInventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
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Patent number: 7964643Abstract: 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: GrantFiled: May 23, 2005Date of Patent: June 21, 2011Assignee: The University Court of the University of AberdeenInventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
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Publication number: 20110014186Abstract: 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: ApplicationFiled: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Publication number: 20100331284Abstract: 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: ApplicationFiled: May 24, 2010Publication date: December 30, 2010Applicant: NEUROTECH PHARMACEUTICALS CO., LTD.Inventors: Byoung Joo GWAG, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Publication number: 20100324093Abstract: 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: ApplicationFiled: August 26, 2010Publication date: December 23, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20100286444Abstract: 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: ApplicationFiled: July 21, 2010Publication date: November 11, 2010Applicant: Ampac Fine Chemicals LLCInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Publication number: 20100280074Abstract: 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: ApplicationFiled: December 3, 2009Publication date: November 4, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20100228054Abstract: 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: ApplicationFiled: November 23, 2006Publication date: September 9, 2010Applicant: BASF SEInventors: Michael Keil, Joachim Gebhardt, Michael Rack, Guido Mayer, Thomas Schmidt, Jan Hendrik Wevers, Sandra Lohr, Axel Pleschke
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Patent number: 7741519Abstract: 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: GrantFiled: February 1, 2008Date of Patent: June 22, 2010Assignee: ChemoCentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, John J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Patent number: 7700654Abstract: 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: GrantFiled: January 28, 2006Date of Patent: April 20, 2010Assignee: LTS Lohmann Therapie-Systeme AGInventors: Hans-Rainer Hoffmann, Rudolf Matusch, Aria Baniahmad
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Publication number: 20100093802Abstract: 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: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: Millennnium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20090312570Abstract: 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: ApplicationFiled: August 21, 2009Publication date: December 17, 2009Applicant: Anadys Pharmaceuticals, IncInventors: Stephen E. Webber, Frank Ruebsam, Martin Tran, Peter Dragovich, Liansheng Li, Douglas E. Murphy, David Kucera, Zhongxiang Sun, Chinh V. Tran
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Publication number: 20090275779Abstract: 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: ApplicationFiled: September 27, 2006Publication date: November 5, 2009Inventors: Tatsuyoshi Tanaka, Kazumi Okuro, Masaru Mitsuda
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Patent number: 7608736Abstract: 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: GrantFiled: June 23, 2004Date of Patent: October 27, 2009Assignee: Bayer CropScience GmbHInventors: Sergiy Pazenok, Mark James Ford, Günter Schlegel
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Publication number: 20090105473Abstract: 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: ApplicationFiled: November 6, 2008Publication date: April 23, 2009Applicant: 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
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Publication number: 20090054495Abstract: 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: ApplicationFiled: October 16, 2008Publication date: February 26, 2009Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
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Publication number: 20080312469Abstract: 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: ApplicationFiled: August 13, 2008Publication date: December 18, 2008Applicant: Ampac Fine Chemicals LLCInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Publication number: 20080242861Abstract: This invention relates to methods of preparing the compounds of formula (V): Each variable in this formula is defined in the specification.Type: ApplicationFiled: April 2, 2007Publication date: October 2, 2008Inventors: Chi-Feng Yen, Chang-Pin Huang, Cheng-Kung Hu, Ming-Chen Chou, Chi-Hsin Richard King
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Publication number: 20080182906Abstract: 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: ApplicationFiled: April 6, 2006Publication date: July 31, 2008Inventors: Claude Lardy, Marc Lecomte, Thierry Convard, Catherine Vidal
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Publication number: 20080177107Abstract: 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: ApplicationFiled: January 28, 2006Publication date: July 24, 2008Applicant: LTS LOHMANN THERAPIE-SYSTEMEInventors: Rudolf Matusch, Aria Baniahmad, Hans-Rainer Hoffmann
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Patent number: 7378550Abstract: The present invention is directed to processes for the synthesis of intermediates useful in the preparation of non-nucleoside reverse transcriptase inhibitors.Type: GrantFiled: March 26, 2004Date of Patent: May 27, 2008Assignee: SmithKline Beecham CorporationInventor: Michael Tolar Martin
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Publication number: 20080119555Abstract: 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: ApplicationFiled: May 23, 2005Publication date: May 22, 2008Inventors: Stuart Hamilton Ralston, Iain Robert Greig, Aymen Ibrahim Idris Mohamed, Robert Jurgen Van 'T Hof
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Patent number: 7321063Abstract: 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: GrantFiled: February 24, 2004Date of Patent: January 22, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D Tung, Mark A Murcko, Govinda R Bhisetti
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Patent number: 7256204Abstract: 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: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7227035Abstract: 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: GrantFiled: May 19, 2004Date of Patent: June 5, 2007Assignee: ChemocentryxInventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Patent number: 7208526Abstract: 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: GrantFiled: April 28, 2006Date of Patent: April 24, 2007Assignee: 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
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Patent number: 7169952Abstract: 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: GrantFiled: June 1, 2001Date of Patent: January 30, 2007Assignee: FMC CorporationInventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
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Patent number: RE39682Abstract: 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: GrantFiled: March 30, 2005Date of Patent: June 5, 2007Assignee: Ramot at Tel Aviv University Ltd.Inventor: Yoel Kloog