Thiomorpholines (i.e., Fully Hydrogenated 1,4-thiazines) Patents (Class 544/59)
  • Patent number: 9193699
    Abstract: 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: Grant
    Filed: October 4, 2012
    Date of Patent: November 24, 2015
    Assignees: 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-CALMETTES
    Inventors: Marc Lopez, Yves Collette, Lynda Mezil, Jean-Michel Brunel, Sebastien Combes
  • Publication number: 20150083223
    Abstract: 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: Application
    Filed: September 25, 2013
    Publication date: March 26, 2015
    Applicants: Tohoku University, Showa Denko K.K.
    Inventors: Tienan JIN, Weili Si, Yoshinori Yamamoto, Takeshi Igarashi
  • Publication number: 20150031688
    Abstract: 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: Application
    Filed: October 9, 2014
    Publication date: January 29, 2015
    Inventor: Shaker A. Mousa
  • Patent number: 8852846
    Abstract: 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: Grant
    Filed: April 4, 2012
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yukako Anryu, Koji Ichikawa
  • Patent number: 8604025
    Abstract: 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: Grant
    Filed: February 5, 2013
    Date of Patent: December 10, 2013
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, Jr.
  • Patent number: 8563544
    Abstract: 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: Grant
    Filed: October 26, 2012
    Date of Patent: October 22, 2013
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Garrett Thomas Potter
  • Patent number: 8541572
    Abstract: 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: Grant
    Filed: November 9, 2009
    Date of Patent: September 24, 2013
    Assignee: 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
  • Patent number: 8530465
    Abstract: 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: Grant
    Filed: August 1, 2012
    Date of Patent: September 10, 2013
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Patent number: 8519125
    Abstract: 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: Grant
    Filed: May 11, 2010
    Date of Patent: August 27, 2013
    Assignee: Biomatrica, Inc.
    Inventors: Scott E. Whitney, Sohela De Rozieres, Rolf Muller
  • Publication number: 20130072677
    Abstract: 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: Application
    Filed: April 20, 2011
    Publication date: March 21, 2013
    Applicants: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
  • Patent number: 8343963
    Abstract: 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: Grant
    Filed: January 29, 2010
    Date of Patent: January 1, 2013
    Assignee: 4SC AG
    Inventor: Stefano Pegoraro
  • Patent number: 8304415
    Abstract: 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: Grant
    Filed: February 25, 2010
    Date of Patent: November 6, 2012
    Assignee: National Defense Medical Center
    Inventors: Hsu-Shan Huang, Chia-Chung Lee
  • Patent number: 8252924
    Abstract: 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: Grant
    Filed: December 18, 2009
    Date of Patent: August 28, 2012
    Assignee: SALTIGO GmbH
    Inventors: Matthias Boll, Burkhard Koch
  • Patent number: 8236565
    Abstract: 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: Grant
    Filed: May 29, 2007
    Date of Patent: August 7, 2012
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Subhasish Purkayastha, Subhakar Dey, Sasi Pillai
  • Patent number: 8232271
    Abstract: 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: Grant
    Filed: October 30, 2009
    Date of Patent: July 31, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
  • Publication number: 20120149693
    Abstract: 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: Application
    Filed: May 5, 2010
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventor: Raymond G. Booth
  • Patent number: 8173643
    Abstract: 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: Grant
    Filed: June 1, 2007
    Date of Patent: May 8, 2012
    Assignee: Beijing Molecule Science and Technology Co., Ltd.
    Inventors: Song Li, Wu Zhong, Junhai Xiao, Xinghai Ma, Lili Wang, Hongying Liu, Zhibing Zheng
  • Patent number: 8148422
    Abstract: 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: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Patent number: 8071762
    Abstract: 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: Grant
    Filed: April 30, 2008
    Date of Patent: December 6, 2011
    Assignee: Abbott Laboratories
    Inventors: 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
  • Publication number: 20110275797
    Abstract: 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: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Patent number: 8012962
    Abstract: 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: Grant
    Filed: November 3, 2009
    Date of Patent: September 6, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
  • Publication number: 20110207739
    Abstract: 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: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Publication number: 20110112076
    Abstract: 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: Application
    Filed: July 13, 2009
    Publication date: May 12, 2011
    Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
  • Publication number: 20110105485
    Abstract: 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: Application
    Filed: July 21, 2010
    Publication date: May 5, 2011
    Inventors: Michael F. Parker, Katharine E. McElhone, Robert A. Mate, Joanne J. Bronson, Yonghua Gai, Carl P. Bergstrom, Lawrence R. Marcin, John E. Macor
  • Patent number: 7893099
    Abstract: 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: Grant
    Filed: June 2, 2010
    Date of Patent: February 22, 2011
    Assignee: 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
  • Publication number: 20100279996
    Abstract: 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: Application
    Filed: May 4, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100279997
    Abstract: 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: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 7772225
    Abstract: 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: Grant
    Filed: December 8, 2006
    Date of Patent: August 10, 2010
    Assignee: Solvay Pharmaceuticals GmbH
    Inventors: Jochen Antel, Michael Firnges, Uwe Schoen, Harald Waldeck, Michael Wurl, Dania Reiche, Peter-Colin Gregory
  • Patent number: 7767666
    Abstract: 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: Grant
    Filed: June 21, 2007
    Date of Patent: August 3, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: John M. Keith, Michael A. Letavic, Emily M. Stocking
  • Patent number: 7741479
    Abstract: 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: Grant
    Filed: December 7, 2005
    Date of Patent: June 22, 2010
    Assignee: 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
  • Patent number: 7714126
    Abstract: 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: Grant
    Filed: November 17, 2006
    Date of Patent: May 11, 2010
    Assignee: 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
  • Patent number: 7662849
    Abstract: 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: Grant
    Filed: June 4, 2004
    Date of Patent: February 16, 2010
    Assignee: ViroBay, Inc.
    Inventors: John W. Patterson, Soon H. Woo
  • Patent number: 7659280
    Abstract: 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: Grant
    Filed: February 16, 2007
    Date of Patent: February 9, 2010
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
  • Patent number: 7652134
    Abstract: 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: Grant
    Filed: June 9, 2005
    Date of Patent: January 26, 2010
    Assignee: Cylene Pharmaceuticals, Inc.
    Inventors: Jeffrey P. Whitten, Fabrice Pierre, Collin Regan, Michael Schwaebe, George Petros Yiannikouros, Michael Jung
  • Publication number: 20100016295
    Abstract: This invention relates to certain biphenyl amino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.
    Type: Application
    Filed: July 31, 2006
    Publication date: January 21, 2010
    Applicant: Bayer Healthcare LLC
    Inventors: Roger A. Smith, Derek Lowe, Tatiana Shelekhin, Georgiy Bondar, Philip Coish, Stephen J. O'Connor
  • Patent number: 7638512
    Abstract: 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: Grant
    Filed: June 23, 2008
    Date of Patent: December 29, 2009
    Assignee: Wyeth
    Inventors: An Thien Vu, Paige Erin Mahaney, Stephen Todd Cohn
  • Publication number: 20090291945
    Abstract: 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: Application
    Filed: April 7, 2009
    Publication date: November 26, 2009
    Applicant: Teijin Pharma Limited
    Inventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
  • Publication number: 20090203681
    Abstract: 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: Application
    Filed: January 23, 2009
    Publication date: August 13, 2009
    Inventors: Li Chen, Yun He, Jason Christopher Wong
  • Patent number: 7572790
    Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.
    Type: Grant
    Filed: April 7, 2004
    Date of Patent: August 11, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Nicola Mary Aston, Paul Bamborough, Katherine Louise Jones, Vipulkumar Kantibhai Patel, Stephen Swanson, Ann Louise Walker
  • Publication number: 20090181943
    Abstract: 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: Application
    Filed: April 9, 2008
    Publication date: July 16, 2009
    Applicant: METHYLGENE INC.
    Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
  • Patent number: 7501408
    Abstract: 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: Grant
    Filed: October 31, 2007
    Date of Patent: March 10, 2009
    Assignee: IRM LLC
    Inventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
  • Patent number: 7470685
    Abstract: 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: Grant
    Filed: January 21, 2005
    Date of Patent: December 30, 2008
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Mitsunori Ono, Elena Kostik, Yumiko Wada
  • Publication number: 20080306054
    Abstract: 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 substit
    Type: Application
    Filed: April 13, 2006
    Publication date: December 11, 2008
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: 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
  • Patent number: 7446104
    Abstract: Substituted phenylalkynes of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: November 4, 2008
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Richard Apodaca, Xiaohu Deng, Jill A. Jablonowski, Neelakandha Mani, Chennagiri R. Pandit, Wei Xiao
  • Publication number: 20080255105
    Abstract: 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-L4
    Type: Application
    Filed: September 18, 2006
    Publication date: October 16, 2008
    Inventors: 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
  • Patent number: 7435851
    Abstract: 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: Grant
    Filed: September 29, 2006
    Date of Patent: October 14, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Mark A. Scialdone
  • Publication number: 20080194536
    Abstract: 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: Application
    Filed: April 14, 2006
    Publication date: August 14, 2008
    Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
  • Publication number: 20080176838
    Abstract: The invention relates to compounds of formula (I) wherein R1-9, Z, n, X, A, and Rb have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament for the treatment of type 2 diabetes mellitus, obesity and lipid disorders.
    Type: Application
    Filed: June 8, 2005
    Publication date: July 24, 2008
    Applicant: SANTHERA PHARMACEUTICALS (DEUTSCHLAND) AG
    Inventors: Paul John Edwards, Silvia Cerezo-Galvez, Achim Feurer, Oliver Hill, Meinolf Thiemann, Victor Giulio Matassa, Sonja Nordhoff, Meritxell Lopez-Canet
  • Patent number: RE42562
    Abstract: 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: Grant
    Filed: April 26, 2007
    Date of Patent: July 19, 2011
    Assignee: Merck Frosst Canada
    Inventors: Xavier Billot, John Colucci, Robert N. Young, Yongxin Han, Marie-Claire Wilson
  • Patent number: RE42700
    Abstract: 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: Grant
    Filed: July 25, 2008
    Date of Patent: September 13, 2011
    Assignees: Sanford-Burnham Medical Research Institute, Oregon State University, SRI International, Molecular Medicine Research Institute, Department of Veterans Affairs, Wayne State University
    Inventors: Marcia Dawson, Joseph A. Fontana, Xiao-Kun Zhang, Mark Leid, Ling Jong, Peter D. Hobbs