Thiomorpholines (i.e., Fully Hydrogenated 1,4-thiazines) Patents (Class 544/59)
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Patent number: 10654792Abstract: The invention generally relates to compounds having structure I: wherein x represents alkyl, aryl or het-aryl, each of y independently represents hydrogen or halogen and z represents hydrogen or alkyl. Further, said compounds are inhibitors of MEK 1, 2 and 5. Furthermore, the invention includes methods of making said compounds, compositions including said compounds and uses for inhibiting MEK 1, 2 and 5.Type: GrantFiled: December 19, 2016Date of Patent: May 19, 2020Assignee: DUQUESNE UNIVERSITY OF THE HOLY SPIRITInventors: Suravi Chakrabarty, Darlene Monlish, Patrick Flaherty, Jane E. Cavanaugh, Sneha Potdar
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Patent number: 9193699Abstract: Provided are compounds of formula (I): wherein R1, R2, R3, R4 and R5 are independently selected from the group comprising, inter aliae, H, optionally substituted, branched or linear C1-C12 alkyl, halogen atom and C1-C12 haloalkyl, and wherein A represents a single bond or an optionally substituted C1-C6 alkylene radical, notably useful for the treatment of human cancers.Type: GrantFiled: October 4, 2012Date of Patent: November 24, 2015Assignees: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (C.N.R.S.), UNIVERSITÉ D'AIX-MARSEILLE, L'INSTITUT PAOLI-CALMETTESInventors: Marc Lopez, Yves Collette, Lynda Mezil, Jean-Michel Brunel, Sebastien Combes
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Publication number: 20150083223Abstract: A fullerene derivative represented by the following formula (1): wherein “FLN” represents a fullerene core, R1 represents an optionally substituted C1-C24 alkyl group or an optionally substituted C7-C24 aralkyl group, R2 and R3 independently represent a hydrogen atom or an optionally substituted C1-C24 hydrocarbon group but excluding a case where both of R2 and R3 are hydrogen atoms, and R2 and R3 may combine together to form a ring.Type: ApplicationFiled: September 25, 2013Publication date: March 26, 2015Applicants: Tohoku University, Showa Denko K.K.Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
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Publication number: 20150031688Abstract: A dual thyrointegrin antagonist and a method for treating an angiogenesis-mediated disorder and/or a hyperthyroidism disorders by introducing the dual thyrointegrin antagonist into animals (e.g., mammals, human beings). The dual thyrointegrin antagonist includes a chemical structure having a thyroid hormone antagonist and ?v?3 integrin antagonist in the same molecule.Type: ApplicationFiled: October 9, 2014Publication date: January 29, 2015Inventor: Shaker A. Mousa
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Patent number: 8852846Abstract: The present invention provides a salt represented by the formula (I): wherein Q1 and Q2 independently each represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents a C1-C20 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, W represents a group represented by the formula (W1), (W2), (W3), (W4) or (W5): and Z+ represents an organic counter ion.Type: GrantFiled: April 4, 2012Date of Patent: October 7, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Yukako Anryu, Koji Ichikawa
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Patent number: 8604025Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: February 5, 2013Date of Patent: December 10, 2013Assignee: Cytokinetics, Inc.Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
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Patent number: 8563544Abstract: Provided herein are 2,5-disubstituted arylsulfonamide CCR3 antagonists, e.g., compounds of Formula I, and pharmaceutical compositions thereof: Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: GrantFiled: October 26, 2012Date of Patent: October 22, 2013Assignee: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei Ly, Garrett Thomas Potter
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Patent number: 8541572Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: September 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Patent number: 8530465Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: August 1, 2012Date of Patent: September 10, 2013Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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Patent number: 8519125Abstract: Compositions and methods are disclosed for substantially dry storage at ambient or elevated temperatures of biological samples such as nucleic acids, proteins and cells in a form from which the samples can be substantially recovered, using a dissolvable or dissociable dry storage matrix comprising a borate composition and a stabilizer as disclosed, such as any of a number of zwitterionic stabilizers.Type: GrantFiled: May 11, 2010Date of Patent: August 27, 2013Assignee: Biomatrica, Inc.Inventors: Scott E. Whitney, Sohela De Rozieres, Rolf Muller
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Publication number: 20130072677Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria.Type: ApplicationFiled: April 20, 2011Publication date: March 21, 2013Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTDInventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
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Patent number: 8343963Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.Type: GrantFiled: January 29, 2010Date of Patent: January 1, 2013Assignee: 4SC AGInventor: Stefano Pegoraro
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Patent number: 8304415Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: February 25, 2010Date of Patent: November 6, 2012Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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Process for preparing benzomorpholine derivatives by hydrogenating o-nitrophenoxy carbonyl compounds
Patent number: 8252924Abstract: A process for preparing benzomorpholine derivatives is described, in which an o-nitrophenoxy carbonyl compound is hydrogenated in the presence of extraneous metal-doped sponge metal catalysts based on nickel or cobalt with ring formation.Type: GrantFiled: December 18, 2009Date of Patent: August 28, 2012Assignee: SALTIGO GmbHInventors: Matthias Boll, Burkhard Koch -
Patent number: 8236565Abstract: In various aspects, the present teachings provide labeling reagents and sets of labeling reagents for the relative quantitation, absolute quantitation, or both, of hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols. In various aspects, the present teachings also provide methods for the analysis hydroxylated compounds including, but not limited to, hydroxylated ring containing compounds, steroids and sterols my MS/MS methods.Type: GrantFiled: May 29, 2007Date of Patent: August 7, 2012Assignee: DH Technologies Development Pte. Ltd.Inventors: Subhasish Purkayastha, Subhakar Dey, Sasi Pillai
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Patent number: 8232271Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: October 30, 2009Date of Patent: July 31, 2012Assignee: Roche Palo Alto LLCInventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
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Publication number: 20120149693Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.Type: ApplicationFiled: May 5, 2010Publication date: June 14, 2012Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Raymond G. Booth
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Patent number: 8173643Abstract: The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system.Type: GrantFiled: June 1, 2007Date of Patent: May 8, 2012Assignee: Beijing Molecule Science and Technology Co., Ltd.Inventors: Song Li, Wu Zhong, Junhai Xiao, Xinghai Ma, Lili Wang, Hongying Liu, Zhibing Zheng
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Patent number: 8148422Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
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Patent number: 8071762Abstract: The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X1-X5, R5-R8b, Z1-Z2 and Ar1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.Type: GrantFiled: April 30, 2008Date of Patent: December 6, 2011Assignee: Abbott LaboratoriesInventors: Arthur R. Gomtsyan, Erol K. Bayburt, Chih-Hung Lee, John R. Koenig, Robert G. Schmidt, Kirill A. Lukin, Gilles Chambournier, Margaret Chi-Ping Hsu, Marvin R. Leanna, Russell D. Cink
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Patent number: 8012962Abstract: The present invention relates to thiomorpholine derivatives of formula I or pharmaceutically acceptable salts thereof and their use in treating seizure disorders, anxiety disorders, bipolar disorders, neuropathic pain disorders and migraine pain disorders.Type: GrantFiled: November 3, 2009Date of Patent: September 6, 2011Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20110207739Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG -
Publication number: 20110112076Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of 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-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).Type: ApplicationFiled: July 13, 2009Publication date: May 12, 2011Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
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Publication number: 20110105485Abstract: There is provided a series of novel ?-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.Type: ApplicationFiled: July 21, 2010Publication date: May 5, 2011Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
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Patent number: 7893099Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: June 2, 2010Date of Patent: February 22, 2011Assignee: Hoffman-La Roche Inc.Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Ruben Alvarez Sanchez
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Publication number: 20100279996Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula I, wherein R1 and R2 are substituents, and W is a ring structure that are defined within.Type: ApplicationFiled: May 4, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Publication number: 20100279997Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.Type: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
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Patent number: 7772225Abstract: The present invention relates to novel N-sulfamoyl-piperidineamides of Formula I and their physiologically acceptable acid addition salts, to pharmaceutical compositions comprising them, processes for their preparation, and their use for the treatment of obesity and its concomitant and/or secondary diseases and related or other conditions.Type: GrantFiled: December 8, 2006Date of Patent: August 10, 2010Assignee: Solvay Pharmaceuticals GmbHInventors: Jochen Antel, Michael Firnges, Uwe Schoen, Harald Waldeck, Michael Wurl, Dania Reiche, Peter-Colin Gregory
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Patent number: 7767666Abstract: Certain substituted butyl and butynyl benzyl amine compounds are histamine H3 receptor and/or serotonin transporter modulators useful in the treatment of histamine H3 receptor- and/or serotonin-mediated diseases.Type: GrantFiled: June 21, 2007Date of Patent: August 3, 2010Assignee: Janssen Pharmaceutica NVInventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
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Patent number: 7741479Abstract: The present invention is directed to a compound having the formula wherein R1, R2, G, and Q are defined herein. The compounds of the present invention are useful as inhibitors of protein kinases such as MAP kinases, in particular p38 kinases. The present invention is also directed to compositions comprising a compound according to the above formula. The compounds and compositions described herein are useful for treating and preventing an inflammatory condition or disease. The present invention is also directed to a method of treating or preventing a protein kinase-mediated condition.Type: GrantFiled: December 7, 2005Date of Patent: June 22, 2010Assignee: Locus Pharmaceuticals, Inc.Inventors: Enrique Luis Michelotti, Eric Bruce Springman, Duyan Nguyen, Rupa S. Shetty, Younghee Lee, Kristofer Kent Moffett, Jennifer Lee Ludington, Ted Tsutomis Fujimoto, Zenon D. Konteatis, Bin Liu, Frank Hollinger, Bruce D. Dorsey
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Patent number: 7714126Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: November 17, 2006Date of Patent: May 11, 2010Assignee: Via Pharmaceuticals, Inc.Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Shiming Li, Lee Apostle McDermott, Yimin Qian, Weiya Yun
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Patent number: 7662849Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: June 4, 2004Date of Patent: February 16, 2010Assignee: ViroBay, Inc.Inventors: John W. Patterson, Soon H. Woo
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Patent number: 7659280Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.Type: GrantFiled: February 16, 2007Date of Patent: February 9, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
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Patent number: 7652134Abstract: The present invention relates to methods of preparing compounds having formula (1), (2), (5), and ((6A)-(6D)) comprising contacting the corresponding ester, an amine with formula NHR1R2, and a Lewis acid having formula MLn, wherein L is a halogen atom or an organic radical, n is 3-5, and M is a group III elemental atom, a group IV elemental atom, As, Sb, V or Fe, wherein A, B, V, X, Z, W, R1, R2, R5, Z1, Z2, Z3, Z4, Z5, Z6, Z7, and Z8 are substituents. Z4, Z5, Z6, Z7, and Z8 are substituents.Type: GrantFiled: June 9, 2005Date of Patent: January 26, 2010Assignee: Cylene Pharmaceuticals, Inc.Inventors: Jeffrey P. Whitten, Fabrice Pierre, Collin Regan, Michael Schwaebe, George Petros Yiannikouros, Michael Jung
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Publication number: 20100016295Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: July 31, 2006Publication date: January 21, 2010Applicant: Bayer Healthcare LLCInventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
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Patent number: 7638512Abstract: The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: June 23, 2008Date of Patent: December 29, 2009Assignee: WyethInventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
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Publication number: 20090291945Abstract: To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.Type: ApplicationFiled: April 7, 2009Publication date: November 26, 2009Applicant: Teijin Pharma LimitedInventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
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Publication number: 20090203681Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: ApplicationFiled: January 23, 2009Publication date: August 13, 2009Inventors: Li Chen, Yun He, Jason Christopher Wong
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Patent number: 7572790Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: April 7, 2004Date of Patent: August 11, 2009Assignee: SmithKline Beecham CorporationInventors: Nicola Mary Aston, Paul Bamborough, Katherine Louise Jones, Vipulkumar Kantibhai Patel, Stephen Swanson, Ann Louise Walker
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Publication number: 20090181943Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.Type: ApplicationFiled: April 9, 2008Publication date: July 16, 2009Applicant: METHYLGENE INC.Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
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Patent number: 7501408Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula (I): wherein Q is thiomorpholinyl; and A, R5, R6, R7, R8, R9 and Ar are substituents.Type: GrantFiled: October 31, 2007Date of Patent: March 10, 2009Assignee: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Patent number: 7470685Abstract: This invention features pyrimidine compounds of formula (I): R1 is in which one of Ra and Rb is H or alkyl, and the other is aryl or heteroaryl optionally substituted with Rd and Rem; each of R2 and R4 is H; R3 is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; X is NRc; Y is covalent bond, CH2, C(O), C?N—Rc, C?N—ORc, C?N—SRc, O, S, S(O), S(O2), or NRc; Z is N or CH; one of U and V is N, and the other is CRc; and W is O, S, S(O), S(O2), NRc, or NC(O)Rc; in which Rc is H, alkyl, aryl, heteroaryl, cyclyl, heterocyclyl, or alkylcarbonyl; Rd is halogen, CN, alkyl, alkyloxy, alkylcarbonyl, alkyloxycarbonyl, aryloxycarbonyl, heteroaryloxycarbonyl, hydroxyalkyl, alkylamino, or alkylaminocarbonyl; Re is halogen, CN, hydroxyl, alkyl, aryl, heteroaryl, alkoxyl, aryloxyl, or heteroaryloxyl; and m is 0, 1, 2, 3, or 4. The pyrimidine compounds can be used to treat an IL-12 overproduction-related disorder (e.g.Type: GrantFiled: January 21, 2005Date of Patent: December 30, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
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Publication number: 20080306054Abstract: The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; C1-5 hydrocarbyl and C1-5 hydrocarbyloxy; wherein the C1-5 hydrocarbyl and C1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C1-2 alkoxy, amino, mono- and di-C1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C1-5 hydrocarbyl-amino, wherein the acyclic C1-5 hydrocarbyl group and the mono and di-C1-5 hydrocarbylamino moieties in each instance are optionally substitType: ApplicationFiled: April 13, 2006Publication date: December 11, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead
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Patent number: 7446104Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.Type: GrantFiled: October 18, 2007Date of Patent: November 4, 2008Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
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Publication number: 20080255105Abstract: A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R1 is a C1-C6 alkyl group or a moiety -A1, -L1-A1, -A1-A1?, -L1-A1-A1?, -A1-L1-A1?, -A1-Y1-A1?, -A1-Het1-A1?, -L1-A1-Y1-A1?, -L1-A1-Het1-A1?, -L1-Het1-A1, -L1-Y1-A1, -L1-Y1-Het1-A1, -L1-Het1-Y1-A1, -L1-Y1-Het1-L1?, -A1-Y1-Het1-A1?, -A1-Het1-Y1-A1?, -A1-Het1-L1-A1?, -A1-L1-Het1-A1? or -L1-Het1-L1?; -A and B are the same or different and each represent a direct bond or a —CO—NR?—, —NR?—CO—, —NR?—CO2—, —CO—, —NR?—CO—NR?—, —NR?—S(O)2—, —S(O)2—NR?—, —SO2—, —NR?—, —NR?—CO—CO—, —CO—O—, —O—CO—, —(C1-C2 alkylene)-NR?— or —(C1-C2 hydroxyalkylene)-NR?-moiety, wherein R? and R? are the same or different and each represent hydrogen or C1-C4 alkyl; —R2 and R3 are the same or different and each represent C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy or halogen; n and m are the same or different and each represent 0 or 1; R4 is a C1-C6 alkyl group or a moiety -A4, -L4-A4, -A4-A4?, -L4-A4-A4?, -A4-L4Type: ApplicationFiled: September 18, 2006Publication date: October 16, 2008Inventors: Christopher James Wheelhouse, Alexander James Floyd Thomas, David John Bushnell, James Lumley, James Iain Salter, Malcolm Clive Carter, Neil Mathews, Christopher John Pilkington, Richard Martyn Angell
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Patent number: 7435851Abstract: The present invention provides substituted puleganic amides and compositions thereof, which are both useful as a topical treatment for skin, such as a repellant for insects and arthropods.Type: GrantFiled: September 29, 2006Date of Patent: October 14, 2008Assignee: E.I. du Pont de Nemours and CompanyInventor: Mark A. Scialdone
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Publication number: 20080194536Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: April 14, 2006Publication date: August 14, 2008Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
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Patent number: RE42562Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.Type: GrantFiled: April 26, 2007Date of Patent: July 19, 2011Assignee: Merck Frosst CanadaInventors: Xavier Billot, John Colucci, Robert N. Young, Yongxin Han, Marie-Claire Wilson
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Patent number: RE42700Abstract: The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.Type: GrantFiled: July 25, 2008Date of Patent: September 13, 2011Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State UniversityInventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs