Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/277.4)
  • Publication number: 20110033393
    Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.
    Type: Application
    Filed: May 12, 2010
    Publication date: February 10, 2011
    Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
  • Publication number: 20110034515
    Abstract: This invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of formula (I) or a salt thereof
    Type: Application
    Filed: April 16, 2009
    Publication date: February 10, 2011
    Inventors: Kevin Dinnell, Andrew P. Lightfoot, Howard Robert Marshall
  • Publication number: 20110028486
    Abstract: The present invention relates to modulation of the ?7 nicotinic acetylcholine receptor (nAChR) by a compound of List A or a salt thereof, which may be represented, but is not limited to the compound N-[(2-Trifluoromethyl-1H-indol-5-yl)methyl]-5-(trifluoromethyl)-2-pyrimidinecarboxamide.
    Type: Application
    Filed: April 16, 2009
    Publication date: February 3, 2011
    Inventors: Kevin Dinnell, Andrew P. Lightfoot, Howard Robert Marshall
  • Publication number: 20110028468
    Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.
    Type: Application
    Filed: April 20, 2009
    Publication date: February 3, 2011
    Applicant: Shinonogi & Co., Ltd
    Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka, Takayuki Okuno, Hiroshi Yari, Keisuke Tonogaki, Naoki Kouyama
  • Publication number: 20110028455
    Abstract: Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X is —O—, —N(R3)—, —S—, —S(O)— or —S(O)2—; R2 is a C1-4 alkyl group or —CF3; and R1, R3, R4 and p are as defined herein; wherein the compounds are useful as kinase inhibitors. Also disclosed are pharmaceutical compositions containing, and intermediate compounds and methods for making the compounds of formula (I) and their pharmaceutically acceptable salts; and methods of using the foregoing to treat inflammatory and autoimmune diseases such as asthma, colitis, multiple sclerosis, psoriasis, arthritis, rheumatoid arthritis, inflammatory bowel disease, and joint inflammation.
    Type: Application
    Filed: December 12, 2008
    Publication date: February 3, 2011
    Applicant: Wyeth LLC
    Inventors: Diane Harris Boschelli, Yanong Daniel Wang, Amarnauth Shastrie Prashad, Zhong Li, Chuansheng Niu
  • Publication number: 20110028463
    Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.
    Type: Application
    Filed: July 2, 2008
    Publication date: February 3, 2011
    Applicant: Astellas Pharma Inc.
    Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
  • Publication number: 20110028519
    Abstract: Compounds of Formula I are described along with pharmaceutical formulations thereof, and methods of treating disorders such as diabetes and neurodegenerative diseases with such compounds.
    Type: Application
    Filed: October 11, 2010
    Publication date: February 3, 2011
    Inventor: Michael C. Pirrung
  • Patent number: 7879839
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: February 1, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
  • Publication number: 20110021556
    Abstract: The invention relates to 3,3 disubstituted pyrrole derivatives useful for treatment of diseases associated with monoamine reuptake inhibitors. Also provided pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: March 10, 2009
    Publication date: January 27, 2011
    Applicant: Hoffman-La Roche, Inc.
    Inventors: Matthew C. Lucas, Ryan Craig Schoenfeld, Robert James Weikert
  • Publication number: 20110015232
    Abstract: The present invention relates to novel IAP inhibitor compounds of: Formula (I).
    Type: Application
    Filed: October 10, 2007
    Publication date: January 20, 2011
    Inventors: Mark G. Charest, Christine Hiu-Tung CHEN, Ming Chen, Zhuoliang Chen, Miao Dai, Feng He, Huangshu Lei, Christopher Straub, Run-Ming David Wang, Leigh Zawel
  • Publication number: 20110009447
    Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.
    Type: Application
    Filed: April 24, 2001
    Publication date: January 13, 2011
    Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
  • Publication number: 20100331302
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 8, 2010
    Publication date: December 30, 2010
    Applicant: Chemocentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20100331323
    Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.
    Type: Application
    Filed: September 10, 2010
    Publication date: December 30, 2010
    Inventors: Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
  • Patent number: 7851625
    Abstract: Disclosed are processes for making 2, 3 disubstituted indole compounds such as compounds of general formula I comprised of the steps of a) reacting a bromoindole compound (i) with a dialkoxyl C1-5 borane in the presence of a ligand, a palladium catalyst and a base to make a compound of general formula (ii); or alternatively reacting compound (i) with a trialkyl magnesiate reagent, followed by treatment with a borate; b) reacting the product of step a with a R2-Hal where R2-Hal is defined herein.
    Type: Grant
    Filed: June 19, 2009
    Date of Patent: December 14, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ahmad Khodabocus, Zhi-Hui Lu, Chris Hugh Senanayake, Hanxun Wei, Yongda Zhang
  • Publication number: 20100311736
    Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.
    Type: Application
    Filed: October 22, 2008
    Publication date: December 9, 2010
    Inventors: Nicholas D. Adams, Michael Gerard Darcy, Neil W. Johnson, Jiri Kasparec, Steven David Knight, Kenneth Allen Newlander, Xin Peng, Lance H. Ridgers
  • Publication number: 20100298321
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: June 3, 2010
    Publication date: November 25, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
  • Publication number: 20100292187
    Abstract: The present invention provides compounds, pharmaceutical compositions, and methods of using such compounds or compositions for treating infection by a virus, or for affecting viral IRES activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: November 18, 2010
    Applicant: PTC THERAPEUTICS, INC.
    Inventors: Gary M. Karp, Peter Seongwoo Hwang, James J. Takasugi, Hongyu Ren, Richard Gerald Wilde, Anthony A. Turpoff, Alexander Arefolov, Guangming Chen, Jeffrey A. Campbell, Chunshi Li, Steven Paget, Nanjing Zhang, Xiaoyan Zhang, Jin Zhu
  • Publication number: 20100292225
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: May 14, 2010
    Publication date: November 18, 2010
    Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
  • Patent number: 7834016
    Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, X, Y, Q and Z have defined meanings.
    Type: Grant
    Filed: September 16, 2005
    Date of Patent: November 16, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Yannick Aimé Eddy Ligny, Imre Christian Francis Csoka, Luc Van Hijfte, Janine Arts, Bruno Schoentjes, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert
  • Patent number: 7834037
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of 5-lipoxygenase-activating protein (FLAP). Also described herein are methods of using such FLAP modulators, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions or diseases.
    Type: Grant
    Filed: October 27, 2007
    Date of Patent: November 16, 2010
    Assignee: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe
  • Publication number: 20100279340
    Abstract: Charged and neutral small fluorescent molecules based upon the styryl scaffold are useful as imaging agents for misfolded proteins such as amyloid plaque. Charged molecules are prepared using pyrrolidine catalyzed reactions by solution-phase synthesis. Neutral styryl molecules are prepared using acetic anhydride catalyzed reactions, Horner-Emmons reactions or Wittig reactions.
    Type: Application
    Filed: February 11, 2008
    Publication date: November 4, 2010
    Applicant: NYU
    Inventors: Thomas Wisniewski, Jaeki Min, Qian Li, Young-Tae CHANG
  • Publication number: 20100273828
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: August 26, 2008
    Publication date: October 28, 2010
    Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Müller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steve Swann, JR., Anil Vasudevan
  • Patent number: 7820672
    Abstract: The compounds are indolylmaleimide derivatives comprising either a substituted pyridyl or indolyl residue. The compounds have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, or acute or chronic transplant rejection.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: October 26, 2010
    Assignee: Novartis AG
    Inventors: Peter Von Matt, Jürgen Wagner
  • Publication number: 20100261698
    Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: October 14, 2010
    Inventors: Christopher Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
  • Publication number: 20100261724
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: October 23, 2008
    Publication date: October 14, 2010
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Patent number: 7803830
    Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Grant
    Filed: October 8, 2008
    Date of Patent: September 28, 2010
    Assignee: Roche Palo Alto LLC
    Inventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
  • Publication number: 20100240637
    Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, m, p, s, t, R1, R2, R3, R4, R5, R6, R7, R20, X, Y, Q and Z have defined meanings.
    Type: Application
    Filed: September 18, 2008
    Publication date: September 23, 2010
    Applicant: JANSSEN PHARMACEUTICAL NV
    Inventors: Virginie Sophie Poncelet, Sophie Coupa, Pierre-Henri Storck, Bruno Schoentjes
  • Publication number: 20100240650
    Abstract: The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
    Type: Application
    Filed: May 25, 2010
    Publication date: September 23, 2010
    Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly White, Hong Ye, Leonard R. Hecker, Bruce Conway, Keith Demarest
  • Patent number: 7799820
    Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: September 21, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura
  • Patent number: 7795250
    Abstract: The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
    Type: Grant
    Filed: June 8, 2005
    Date of Patent: September 14, 2010
    Assignee: Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
    Inventors: Stefania Colarusso, Immacolata Conte, Joerg Habermann, Frank Narjes, Simona Ponzi
  • Publication number: 20100228008
    Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.
    Type: Application
    Filed: June 17, 2009
    Publication date: September 9, 2010
    Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.
    Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
  • Publication number: 20100222368
    Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.
    Type: Application
    Filed: May 11, 2010
    Publication date: September 2, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Laurent DUBOIS, Yannick EVANNO, Andre MALANDA
  • Patent number: 7786146
    Abstract: This invention provides compounds of formula I where the dashed line represents an optional double bond; where R1 is phenyl, naphthyl, pyridyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazyl, furyl, thienyl, oxazolyl, isoxazolyl, thiazolyl, or isothiazolyl, optionally substituted, and other substituents are defined herein. Such compounds are potassium channel modulators.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: August 31, 2010
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Huanming Chen, Jianlan Song
  • Patent number: 7781591
    Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: August 24, 2010
    Assignee: Wyeth LLC
    Inventors: Derek Cecil Cole, Diane Harris Boschelli, Yanong Daniel Wang, Magda Asselin, Diane Marie Joseph-McCarthy, Amarnauth Shastrie Prashad, Allan Wissner, Russell Dushin, Biqi Wu, Lawrence Nathan Tumey, Chuan S. Niu, Joan Chen
  • Publication number: 20100197716
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Application
    Filed: April 16, 2010
    Publication date: August 5, 2010
    Inventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • Publication number: 20100197652
    Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: August 7, 2008
    Publication date: August 5, 2010
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
  • Publication number: 20100197657
    Abstract: The present invention provides 2-aryl or heteroaryl indole derivatives which are ASIC channel modulators, maceutical compositions containing such compounds, and methods of using them as therapeutic agents.
    Type: Application
    Filed: September 22, 2008
    Publication date: August 5, 2010
    Inventors: Ronald K. Chang, Christina Ng Di Marco, Scott D. Kuduk
  • Publication number: 20100197673
    Abstract: The present invention relates to indole or indazole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole or indazole compounds as an active ingredient.
    Type: Application
    Filed: August 18, 2008
    Publication date: August 5, 2010
    Applicant: LG Life Sciences Ltd
    Inventors: Soon Ha Kim, Hyoung Jin Kim, Sun Young Koo, Chul Woong Chung, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Hyo Shin Kwak, Dong Ook Seo, Eok Park
  • Publication number: 20100184975
    Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?0)NH(C1-3alkyl), -L-C(?O)N(C1-3alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3alkyl)2, -L-S(?O)2NH(C1-3alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.
    Type: Application
    Filed: March 8, 2010
    Publication date: July 22, 2010
    Applicant: Myriad Pharmaceuticals, Inc.
    Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
  • Patent number: 7750027
    Abstract: Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(?O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C?O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: July 6, 2010
    Assignee: Oxagen Limited
    Inventors: Richard Edward Armer, Eric Roy Pettipher, Mark Whittaker, Graham Michael Wynne, Julia Vile, Frank Schroer
  • Publication number: 20100168163
    Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, t, R1, R2, R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.
    Type: Application
    Filed: March 19, 2007
    Publication date: July 1, 2010
    Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Alain Philippe Poncelet, Camille Georges Wermuth, Bruno Giethlen, Jean-Marie Contreras, Muriel Joubert, Luc Van Hijfte
  • Publication number: 20100166881
    Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.
    Type: Application
    Filed: March 11, 2010
    Publication date: July 1, 2010
    Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
  • Publication number: 20100168429
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; R6; A1; A2; A3; A4, Q, T and J have the meanings indicated in the claims. The present invention provides a direct transition metal catalyzed process to a wide variety of multifunctional N-aminoindole or N-amino-azaindoles of the formula I from 2-halo-phenylacetylenes or (2-sulfonato)phenyl-acetylenes and N,N-disubstituted hydrazines, useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
    Type: Application
    Filed: October 9, 2009
    Publication date: July 1, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Nis HALLAND, Marc NAZARE, Andreas LINDENSCHMIDT, Omar AKYEK, Matthias URMANN, Jorge ALONSO
  • Publication number: 20100160373
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
    Type: Application
    Filed: December 15, 2009
    Publication date: June 24, 2010
    Inventors: Jacob Berger, Joan Marie Caroon, Nancy Elisabeth Krauss, Keith Adrian Murray Walker, Shu-Hai Zhao, Francisco Javier Lopez-Tapia
  • Publication number: 20100152183
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: December 4, 2009
    Publication date: June 17, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20100137280
    Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.
    Type: Application
    Filed: March 20, 2008
    Publication date: June 3, 2010
    Applicant: ABBOTT GMBH & CO. KG
    Inventors: Thomas Schultz, SR., Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
  • Publication number: 20100125082
    Abstract: The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Downs syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
    Type: Application
    Filed: November 13, 2009
    Publication date: May 20, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Jörg HOLENZ, Sofia KARLSTRÖM, Karin KOLMODIN, Johan LINDSTRÖM, Laszlo RAKOS, Didier ROTTICCI, Peter SÖDERMAN, Britt-Marie SWAHN, Stefan VON BERG
  • Publication number: 20100120749
    Abstract: The present invention is related to tetrahydroindole derivatives of Formula (I), pharmaceutical composition thereof, methods of preparation thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: March 28, 2008
    Publication date: May 13, 2010
    Applicant: GENKYO TEX SA
    Inventors: Patrick Page, Mike Orchard, Laeticia Fioraso-Cartier, Bianca Mottironi
  • Publication number: 20100113777
    Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
    Type: Application
    Filed: March 28, 2008
    Publication date: May 6, 2010
    Applicant: Asubio Pharma Co., Ltd.
    Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
  • Patent number: 7705022
    Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: April 27, 2010
    Assignee: Lankenau Institute for Medical Research
    Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway