Sulfonamides (i.e., Q-(o=)s(=o)-n, Wherein Q Is A Substituent And Wherein Any Substituent Attached To The Nitrogen Will Be Referred To As E) Patents (Class 514/601)
  • Patent number: 10676428
    Abstract: An effective therapeutic agent for the M2 channel comprising sulfonylamide or oxabicyclo structures effective for treating amantadine-resistant influenza A infections, and methods of treating amantadine-resistant influenza A infections through administration of the same.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: June 9, 2020
    Assignee: RAMOT AT TEL-AVIV UNIVERSITY LTD.
    Inventors: Nir Ben-Tal, Roger S. Armen, Laurence C. Eisenlohr, Jitendra Belani, Michael Miller, Inbar Fish, Ori Kalid
  • Patent number: 10562898
    Abstract: Provided is a compound having ?4 integrin inhibitory action. The compound is a sulfonamide derivative represented by the following formula (I), or pharmaceutically acceptable salt thereof: where R1 to R5, e to h, D, and B represent those as described in the specification.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: February 18, 2020
    Assignee: EA PHARMA CO., LTD.
    Inventors: Munetaka Tokumasu, Masatsugu Noguchi, Mizuki Kawahira, Kana Iwasaki, Nobuhiko Hayakawa, Wataru Miyanaga, Yuki Saitou, Yui Yamaura, Ayatoshi Ando, Atsushi Tsuruta, Misato Noguchi
  • Patent number: 10071099
    Abstract: Provided are a novel medicament for suppressing or preventing the metastasis of a malignant tumor such as carcinoma, a novel treatment or prevention method for suppressing or preventing the metastasis of a malignant tumor, etc. The medicament comprises a non-peptidic angiotensin type 2 receptor agonist as an active ingredient. In the medicament, the non-peptidic angiotensin type 2 receptor agonist may be, for example, a sulfonyl malonamide compound. The medicament may be a medicament for use in combination with an anticancer agent and/or an antitumor agent.
    Type: Grant
    Filed: April 3, 2015
    Date of Patent: September 11, 2018
    Assignee: NATIONAL CEREBRAL AND CARDIOVASCULAR CENTER
    Inventors: Kenji Kangawa, Hiroshi Hosoda, Takashi Nojiri
  • Patent number: 9738613
    Abstract: Compounds represented by Formula I: and/or a pharmaceutically acceptable salts, a prodrug, a solvate and a combination thereof, a pharmaceutical composition including the triazole derivative, and a method of treating a cancer disease in an individual are disclosed.
    Type: Grant
    Filed: May 18, 2015
    Date of Patent: August 22, 2017
    Assignee: National Central University
    Inventors: Duen-Ren Hou, Sharada Prasanna Swain
  • Patent number: 9663508
    Abstract: The present invention provides compounds of Formula (Ia), and pharmaceutically acceptable salts thereof. The compounds are useful as inhibitors of voltage-gated sodium channels, in particular Nav 1.7. as described in the specification. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention, as well as intermediates and processes useful for making the compounds.
    Type: Grant
    Filed: October 1, 2014
    Date of Patent: May 30, 2017
    Assignee: Amgen Inc.
    Inventors: Howard Bregman, Nagasree Chakka, Erin F. Dimauro, Hua Gao, Hakan Gunaydin, Hongbing Huang, Philip R. Olivieri, Laurie Schenkel, Matthew Weiss
  • Patent number: 9220696
    Abstract: The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1 -(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide with other compounds, to patients suffering from cancer are described.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: December 29, 2015
    Assignee: ARDEA BIOSCIENCES, INC.
    Inventor: Mark Chapman
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Patent number: 9000045
    Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: April 7, 2015
    Assignee: Japan Tobacco Inc.
    Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
  • Patent number: 8952031
    Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: March 5, 2012
    Date of Patent: February 10, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8933236
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Grant
    Filed: May 21, 2013
    Date of Patent: January 13, 2015
    Assignees: Xenon Pharmaceuticals Inc., Genentech, Inc.
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8906955
    Abstract: A method for treating an aging-related disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: December 9, 2014
    Inventors: Shuguang Lin, Meng Zheng
  • Publication number: 20140329811
    Abstract: The present invention provides a method for preferentially reducing the proliferation of cystic epithelial cells in the kidney or bile duct in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to preferentially reduce the proliferation of cystic epithelial cells over normal epithelial cells such as tubule epithelial cells in the kidney or bile duct. The present invention also provides a method for preventing or treating autosomal dominant polycystic kidney disease (ADPKD), autosomal recessive polycystic kidney disease (ARPKD), ARPKD associated congenital hepatic fibrosis, ARPKD associated Caroli's disease, or cholangiocarcinoma in a mammal in need thereof by administering a 20-HETE synthesizing enzyme inhibitor or a 20-HETE antagonist to the mammal in an amount sufficient to prevent or treat the disease.
    Type: Application
    Filed: June 12, 2014
    Publication date: November 6, 2014
    Inventors: William E. Sweeney, Ellis D. Avner, Richard J. Roman
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Publication number: 20140309206
    Abstract: The present invention relates to aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: June 27, 2014
    Publication date: October 16, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins
  • Publication number: 20140303253
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N-(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Application
    Filed: June 23, 2014
    Publication date: October 9, 2014
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventor: Stuart DIMOCK
  • Publication number: 20140275198
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver, and more specifically relates to a pharmaceutical composition for preventing or treating diabetes or fatty liver containing a CYP4A (cytochrome P450A) inhibitor as an active ingredient. According to the present invention, the CYP4A inhibitor suppresses endoplasmic reticulum stress, reduces the blood insulin concentration and suppresses apoptosis of liver cells, and hence exhibits effects in preventing or treating diabetes or fatty liver.
    Type: Application
    Filed: February 11, 2014
    Publication date: September 18, 2014
    Applicant: Korea Basic Science Institute
    Inventors: Gun-Hwa Kim, Soohyun Kim, Jong-Soon Choi, Seung II Kim, Edmond Changkyun Park
  • Publication number: 20140256701
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 11, 2014
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins, Sean Turner
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Publication number: 20140206741
    Abstract: The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
    Type: Application
    Filed: April 12, 2012
    Publication date: July 24, 2014
    Applicant: Sichuan Guokang Pharmaceutical Co., Ltd
    Inventors: Luyun Zhang, Fang Yang, Wanqi Shi, Ping Zhang, Ying Li, Shufan Yin
  • Patent number: 8778897
    Abstract: Methods for treating or preventing cardiomyopathy in a subject by administering an ?1 adrenergic receptor agonist, wherein the treatment does not result in increased blood pressure are provided.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 15, 2014
    Assignee: The Regents of the University of California
    Inventor: Paul C. Simpson, Jr.
  • Patent number: 8772343
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8759577
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Grant
    Filed: May 30, 2013
    Date of Patent: June 24, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventor: Stuart Dimock
  • Publication number: 20140148498
    Abstract: The instant invention provides methods and compositions for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions. The invention further provides pharmaceutical compositions and kits for the treatment and prevention of Marfan syndrome and related diseases, disorders and conditions.
    Type: Application
    Filed: April 13, 2012
    Publication date: May 29, 2014
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Harry C. Dietz, Jefferson J. Doyle, Jennifer Pardo Habashi, Tammy Holm
  • Patent number: 8686043
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Grant
    Filed: August 28, 2012
    Date of Patent: April 1, 2014
    Assignee: Pfizer Inc.
    Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
  • Patent number: 8673953
    Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: March 18, 2014
    Assignee: Allergan, Inc.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Patent number: 8664247
    Abstract: The present invention provides acyclic, geminal-dinitro organic compounds, methods of synthesizing the compounds, pharmaceutical compositions, therapeutic methods, and medical kits for treating various conditions using such compounds and pharmaceutical compositions. The compounds and compositions are useful in the treatment of cancer.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 4, 2014
    Assignees: RadioRx, Inc., Alliant Techsystems Inc.
    Inventors: Jan Scicinski, Bryan T. Oronsky, Robert Wardle, Louis Cannizzo, Nicholas A. Straessler
  • Patent number: 8653141
    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: April 19, 2012
    Date of Patent: February 18, 2014
    Assignee: AbbVie Inc.
    Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
  • Patent number: 8648116
    Abstract: This invention concerns N-(2-arylamino) aryl sulfonamide compounds which are inhibitors of MEK including crystalline polymorphic forms which exhibit a specific powder x-ray diffraction profile and/or a specific differential scanning calorimetry profile. This invention also concerns pharmaceutical compositions comprising the compounds described herein and methods of use of the compounds and compositions described herein, including the use in the treatment and/or prevention of cancer, hyperproliferative diseases and inflammatory conditions. The invention also concerns methods of making the compounds and compositions described herein.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: February 11, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Michel Vernier, Colin Edward Rowlings, Jean-Luc Girardet, Stuart Dimock, Barry Quart, Jeffrey N. Miner
  • Patent number: 8609076
    Abstract: The present invention relates to the use of polyols of formula (I): or a salt thereof, for preventing the hair from breaking. The invention also relates to a cosmetic composition comprising at least one such polyol or a salt thereof, in a cosmetically acceptable medium, and also to a cosmetic hair treatment process using the said composition.
    Type: Grant
    Filed: May 13, 2005
    Date of Patent: December 17, 2013
    Assignee: L'Oreal
    Inventors: Frederic Leroy, Michel Philippe, Philippe Barbarat, Christian Blaise
  • Patent number: 8609897
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • Publication number: 20130317000
    Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Applicants: XENON PHARMACEUTICALS INC., GENENTECH, INC
    Inventors: Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
  • Patent number: 8569378
    Abstract: The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G1, G2, G3 and G8 are each independently selected from —N? etc., Ring G6 is selected from divalent aryl etc., A is selected from amino etc., G4 is selected from oxygen etc., G5 is selected from oxygen etc., G7 is selected from —CH2— etc., and R2 is selected from C1-6 alkyl etc.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: October 29, 2013
    Assignees: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Toshiyuki Sakai, Hitoshi Iikura, Ikumi Hyoudoh, Toshihiro Aoki, Noriyuki Furuichi, Masayuki Matsushita, Fumio Watanabe, Sawako Ozawa, Masahiro Sakaitani, Pil-Su Ho, Yasushi Tomii, Kenji Takanashi, Naoki Harada
  • Publication number: 20130276352
    Abstract: A termite bait includes a plurality of cellulosic food material pieces palatable to termites embedded within a water resistant polyurethane foam matrix. Another termite bait includes a plurality of cellulosic food material pieces embedded within a water-absorbent polyurethane foam matrix. Yet another termite bait includes at least one cellulosic food material piece encapsulated within a water resistant polyurethane foam coating. Such termite baits can be used alone or in a monitoring device or other termite control device. Another termite control device includes a container, a cellulosic food material within the container and a water resistant polyurethane foam positioned to separate the food material from its environment. The container can contain a termite bait as described above or can include a chamber containing a cellulosic food material and at least one pocket containing a polyurethane foam barrier to reduce intrusion of water through the pocket to the food material.
    Type: Application
    Filed: March 15, 2013
    Publication date: October 24, 2013
    Inventor: Dow AgroSciences LLC
  • Patent number: 8536229
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, RO, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: September 17, 2013
    Assignee: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W Hart, Kaspar Zimmerman
  • Patent number: 8524778
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl sulfonamides and related compounds (collectively referred to herein as ‘BPSAAA compounds’), as described herein, and including, for example, biphenyl-4-sulfonic acid (hydroxyalkyl-phenyl)-amides and related compounds.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: September 3, 2013
    Assignee: PIMCO 2664 Limited
    Inventors: Iain Robert Greig, Robert Jurgen Van't Hof, Stuart Hamilton Ralston
  • Patent number: 8518860
    Abstract: A herbicidal suspension comprising (1) a sulfonylurea compound or its salt as a herbicidal component, (2) at least one surfactant selected from the group consisting of an alkoxylated sorbitol fatty acid ester and an alkoxylated sorbitan fatty acid ester, and (3) a water-immiscible diluent. A method for controlling undesired plants or inhibiting their growth, which comprises applying a herbicidally effective amount of the herbicidal suspension to the undesired plants or to a place where they grow.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: August 27, 2013
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Hiroshi Yoshii, Yoshiaki Ishihara, Ryu Yamada, Tatsuhiko Tsuruta
  • Patent number: 8518998
    Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: August 27, 2013
    Assignee: Sanofi-aventis Deutschland GmbH
    Inventors: Karl Rudolphi, Martin Michaelis, Hans Guehring
  • Patent number: 8501812
    Abstract: The invention relates to the treatment and prevention of type I diabetes. More specifically, the invention relates to compounds that treat or prevent the body's immune system from destroying ?-cells (i.e., insulin-producing cells in the pancreatic islets of Langerhans) by inhibition of JNK2, selective inhibition of JNK2, or inhibition of the expression of the MAPK9 gene or gene product. In one embodiment, the present invention contemplates the diagnosis, identification, production, and use of compounds which modulate MAPK9 gene expression or the activity of the MAPK9 gene product including but not limited to, JNK2, the nucleic acid encoding MAPK9 and homologues, analogues, and deletions thereof, as well as antisense, ribozyme, triple helix, antibody, and polypeptide molecules as well as small inorganic molecules. The present invention contemplates a variety of pharmaceutical formulations and routes of administration for such compounds.
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: August 6, 2013
    Assignee: University of Massachusetts
    Inventors: Roger J. Davis, Anja Jaeschke
  • Publication number: 20130184238
    Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 18, 2013
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130184342
    Abstract: The technology described herein relates to methods of inducing cell death. The technology described herein further relates to treating conditions including cancers and autoimmune diseases comprising administering inhibitors of double strand break repair. Also described herein are inhibitors of double strand break repair and methods of screening for such inhibitors.
    Type: Application
    Filed: March 13, 2013
    Publication date: July 18, 2013
    Applicant: THE JACKSON LABORATORY
    Inventor: THE JACKSON LABORATORY
  • Patent number: 8466316
    Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: June 18, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventor: Stuart Dimock
  • Patent number: 8461209
    Abstract: The invention provides a sulfonyl malonamide derivative, or a pharmacologically acceptable salt thereof or a solvate thereof, that has therapeutic and/or preventive effects(s) on various diseases due to its agonist action at AT2 receptor, and is useful as a pharmaceutical agent for the treatment and/or prevention of diseases involving the renin-angiotensin-aldosterone system (RAAS).
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: June 11, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tomohiro Yoshida, Hiroshi Sakashita, Atsushi Numata, Saori Tahara, Hisashi Kawasumi
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8404747
    Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.
    Type: Grant
    Filed: March 7, 2005
    Date of Patent: March 26, 2013
    Assignees: The General Hospital Corporation, Massachusetts Institute of Technology
    Inventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven Hersch
  • Patent number: 8399496
    Abstract: A method and a composition for treatment of pulmonary bacterial infections caused by gram-negative bacteria suitable for treatment of infection caused by Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans, and multidrug resistant Pseudomonas aeruginosa, using a concentrated formulation of aztreonam lysinate delivered as an aerosol or dry powder formulation.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: March 19, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Alan Bruce Montgomery, Manfred Keller, Frank-Christophe Lintz
  • Patent number: 8389500
    Abstract: The present invention 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 (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Patent number: RE45314
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: December 30, 2014
    Assignees: The Johns Hopkins University, Cardioxyl Pharmaceuticals, Inc.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish