Additional Oxygen Containing Hetero Ring Patents (Class 544/147)
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140275010
    Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8735441
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: October 5, 2012
    Date of Patent: May 27, 2014
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Publication number: 20140100169
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Application
    Filed: November 12, 2013
    Publication date: April 10, 2014
    Applicant: Onyx Therapeutics, Inc.
    Inventors: Kevin D. SHENK, Francesco PARLATI, Han-jie ZHOU, Catherine SYLVAIN, Mark S. SMYTH, Mark K. BENNETT, Guy J. LAIDIG
  • Patent number: 8673904
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: March 18, 2014
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Publication number: 20130196987
    Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.
    Type: Application
    Filed: October 30, 2012
    Publication date: August 1, 2013
    Applicant: EISAI CO., LTD.
    Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
  • Publication number: 20130041008
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Application
    Filed: October 5, 2012
    Publication date: February 14, 2013
    Applicant: ONYX THERAPEUTICS, INC.
    Inventor: Onyx therapeutics, Inc.
  • Patent number: 8357683
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: January 22, 2013
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Patent number: 8299067
    Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.
    Type: Grant
    Filed: March 25, 2009
    Date of Patent: October 30, 2012
    Assignees: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Chengyong Li, Shiwu Chen
  • Publication number: 20120237591
    Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.
    Type: Application
    Filed: May 8, 2012
    Publication date: September 20, 2012
    Applicant: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Patent number: 8263764
    Abstract: The invention relates to cyclic hydrazone compounds, compositions including the cyclic hydrazone compounds and methods of using and methods of making thereof. The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: September 11, 2012
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
  • Publication number: 20120115862
    Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1? and/or TNF-?. They can therefore be used for treatment of diseases connected with a disturbance in the immune system.
    Type: Application
    Filed: October 9, 2009
    Publication date: May 10, 2012
    Inventors: Stefan Laufer, Wolfgang Albrecht
  • Publication number: 20120088762
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Application
    Filed: December 16, 2011
    Publication date: April 12, 2012
    Applicant: ONYX THERAPEUTICS, INC.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Patent number: 8133888
    Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: March 13, 2012
    Assignee: Sun Pharma Advanced Research Company Ltd.
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Trinadha Rao Chitturi, Rajamannar Thennati
  • Patent number: 8101609
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: January 24, 2012
    Assignee: Apotex Pharmachem Inc.
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga
  • Publication number: 20110237566
    Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain macrolide compounds (for convenience, collectively referred to herein as “MC compounds”), which, inter alia, are useful in treatment of cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to treat proliferative conditions such as cancer, and in the treatment of diseases and conditions that are mediated by the regulation (e.g. inhibition) of cell proliferation, optionally in combination with another agent.
    Type: Application
    Filed: November 24, 2009
    Publication date: September 29, 2011
    Applicant: MERLION PHARMACEUTICALS PTE LTD
    Inventors: Rustum S. Boyce, Muhammad Sofian Asi Sihombing, Hiroki Sone
  • Publication number: 20110217335
    Abstract: Disclosed are macrocyclic compounds of formulae I, I?, II, II?, III, III?, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
    Type: Application
    Filed: January 15, 2009
    Publication date: September 8, 2011
    Applicant: UNIVERSITE DE STRASBOURG
    Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
  • Publication number: 20110172226
    Abstract: The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4; R3 is selected from the group consisting of alkyl, —O-alkyl, —NH-alkyl, aryl and heterocyclyl; R4 represents a moiety (A) wherein, X is selected from the group consisting of a single bond, alkylene, alkenylene, alkynylene, arylene or a heterocyclylene moiety; R5 and R6 are same or different and are independently selected from hydrogen, alkyl, aryl or heterocyclyl; or R5 and R6 may form together with the nitrogen atom to which they are attached a heterocyclyl ring system.
    Type: Application
    Filed: February 12, 2009
    Publication date: July 14, 2011
    Applicant: Sun Pharma Advanced Research Company Ltd.
    Inventors: Jiten Ranchhodbhai Patel, Gopalkumar Chimanlal Patel, Gaurav Sanjivkumar Sheth, Trinadha Rao Chitturi, Rajamannar Thennati
  • Publication number: 20110165225
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: May 26, 2009
    Publication date: July 7, 2011
    Inventors: Peter Cullis, Marcel Bally
  • Patent number: 7863270
    Abstract: The invention relates to cyclic hydrazone compounds and compositions including the cyclic hydrazone compounds according to formula (I): The compounds (and compositions) are useful, inter alia, in modulating IL-12 production and processes mediated by IL-12.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: January 4, 2011
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Zachary Demko, Lijun Sun, Howard P. Ng
  • Patent number: 7855201
    Abstract: The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin 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 prokineticin receptors are involved.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: December 21, 2010
    Assignee: Merck Sharp & Dohme. Corp.
    Inventors: Wayne J. Thompson, Jeffrey Y. Melamed
  • Publication number: 20100273790
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8: .
    Type: Application
    Filed: April 26, 2010
    Publication date: October 28, 2010
    Applicant: Apotex Pharmachem Inc.
    Inventors: Prabhudas BODHURI, Gamini Weeratunga
  • Publication number: 20100273798
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Application
    Filed: April 28, 2009
    Publication date: October 28, 2010
    Applicant: APOTEX PHARMACHEM INC.
    Inventors: Prabhudas BODHURI, Gamini Weeratunga
  • Patent number: 7816355
    Abstract: This invention provides a process for the preparation of S-Rivaroxaban and/or R-Rivaroxaban comprising reacting, in the presence of a first base, a compound of Formula 9: with a compound of Formula 8:
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: October 19, 2010
    Assignee: Apotex Pharmachem Inc
    Inventors: Prabhudas Bodhuri, Gamini Weeratunga
  • Patent number: 7803797
    Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof, are disclosed, wherein G, B, Y, and A are as described. Methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: September 28, 2010
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7799824
    Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.
    Type: Grant
    Filed: June 22, 2005
    Date of Patent: September 21, 2010
    Assignee: OraPharma, Inc.
    Inventors: Bharat Lagu, Michael Wachter
  • Publication number: 20100233279
    Abstract: Disclosed are novel analogues of the natural product radicicol A of formulae I, .Ia, pi, Ha, lib and HI, pharmaceutical compositions comprising the compounds. The compounds of the invention are kinase and phosphatase inhibitors and find utility in the treatment or prevention of kinase and phosphatase-mediated disorders. Also provided are uses and methods for the treatment or prevention of kinase- and phosphatase-mediated disorders and synthetic processes for the preparation of the compounds.
    Type: Application
    Filed: June 5, 2008
    Publication date: September 16, 2010
    Inventors: Nicolas Winssinger, Sofia Barluenga
  • Publication number: 20100144649
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Application
    Filed: February 19, 2010
    Publication date: June 10, 2010
    Applicant: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Patent number: 7691852
    Abstract: One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: April 6, 2010
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Kevin D. Shenk, Francesco Parlati, Han-Jie Zhou, Catherine Sylvain, Mark S. Smyth, Mark K. Bennett, Guy J. Laidig
  • Publication number: 20100004234
    Abstract: Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.
    Type: Application
    Filed: August 6, 2009
    Publication date: January 7, 2010
    Inventors: Daniel V. Santi, Ralph C. Reid, C. Richard Hutchinson, Kurt F. Sundermann, Janice Lau
  • Publication number: 20090312316
    Abstract: The present invention relates to derivatives of borrelidin that are useful in medicine, e.g. in the treatment of cancer or B-cell malignancies, or other diseases in which angiogenesis contributes to the pathology including ophthalmic disorders such as diabetic retinopathy as well as age related macular degeneration (AMD), corneal neovascularisation and retinopathy or prematurity. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies and other diseases in which angiogenesis is implicated in the pathogenic process.
    Type: Application
    Filed: May 17, 2007
    Publication date: December 17, 2009
    Inventors: Barrie Wilkinson, Steven Moss, Ming Zhang
  • Publication number: 20090247503
    Abstract: Provided herein are 5-demethoxyfumagillol and its derivatives. Also provided herein are methods of making the 5-demethoxyfumagillol and derivatives. Also provided herein are biological activities of the 5-demethoxyfumagillol and derivatives and methods of using same for treating diseases.
    Type: Application
    Filed: March 25, 2009
    Publication date: October 1, 2009
    Applicants: Versitech Limited, Morningside Ventures Limited
    Inventors: Dan Yang, Chengyong Li, Shiwu Chen
  • Patent number: 7528130
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: January 6, 2006
    Date of Patent: May 5, 2009
    Assignee: Immunogen Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Patent number: 7476669
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: January 13, 2009
    Assignee: Immunogen Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Patent number: 7429660
    Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
    Type: Grant
    Filed: August 13, 2004
    Date of Patent: September 30, 2008
    Assignee: Kudos Pharmaceuticals Limited
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffrey Hummersone, Roger John Griffin
  • Patent number: 7417042
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
    Type: Grant
    Filed: August 8, 2005
    Date of Patent: August 26, 2008
    Assignee: Proteolix, Inc.
    Inventors: Mark S. Smyth, Guy J. Laidig
  • Publication number: 20080176841
    Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.
    Type: Application
    Filed: June 13, 2007
    Publication date: July 24, 2008
    Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
    Inventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
  • Patent number: 7390898
    Abstract: Included within the scope of the present invention are potent taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.
    Type: Grant
    Filed: February 21, 2003
    Date of Patent: June 24, 2008
    Assignee: Immunogen Inc.
    Inventors: Erkan Baloglu, Michael Miller, Ravi V. J. Chari
  • Publication number: 20080146545
    Abstract: Disclosed are macrocyclic compounds of formulae I-V, which are analogs of the pochonin resorcylic acid lactones, and processes for the preparation of the compounds. The compounds disclosed are useful as inhibitors of kinases and Heat Shock Protein 90 (HSP 90). Also disclosed are pharmaceutical compositions comprising an effective kinase-inhibiting amount or an effective HSP90-inhibiting amount of the compounds and methods for the treatment of disorders that are mediated by kinases and HSP90.
    Type: Application
    Filed: August 10, 2007
    Publication date: June 19, 2008
    Inventors: Nicolas Winssinger, Sofia Barluenga, Martin Karplus
  • Patent number: 7297714
    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.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: November 20, 2007
    Assignee: IRM LLC
    Inventors: Hong Liu, Phillip Alper, Daniel Mutnick, Donald Karanewsky
  • Patent number: 7276499
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: October 2, 2007
    Assignee: Immunogen Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blattler
  • Patent number: 7271264
    Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: September 18, 2007
    Assignee: Eli Lilly and Company
    Inventors: Ronald Jay Hinklin, Owen Brendan Wallace
  • Patent number: 7232818
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: June 19, 2007
    Assignee: Proteolix, Inc.
    Inventors: Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
  • Patent number: 7217819
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: May 15, 2007
    Assignee: ImmunoGen, Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Patent number: 7049313
    Abstract: The application concerns a compound of formula I: wherein one of P and Q is O, and the other of P and Q is CH, where there is a double bond between whichever of Q and P is CH and the carbon atom bearing the R3 group; Y is either O or S; R1 and R2 are independently hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; R3 is a phenyl or pyridyl group, attached by a first bridge group selected from —S—, —S(?O)—, —S(?O)2—, —O—, —NRN— and CRC1RC2— to an optionally substituted C5-20 carboaryl group, the phenyl or pyridyl group and optionally substituted C5-20 carboaryl group being optionally further linked by a second bridge group, so as to form an optionally substituted C5-7 ring, the phenyl or pyridyl group being further optionally substituted.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: May 23, 2006
    Assignee: Kudos Pharmaceuticals Ltd.
    Inventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Stephen Philip Jackson, Mark James O'Connor, Alan Yin Kai Lau, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Laurent Jean Martin Rigoreau, Marc Geoffery Hummersone, Roger John Griffin
  • Patent number: 7008942
    Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.
    Type: Grant
    Filed: October 15, 2003
    Date of Patent: March 7, 2006
    Assignee: Immunogen, Inc.
    Inventors: Ravi V. J. Chari, Walter A. Blättler
  • Patent number: 6924285
    Abstract: The present invention relates to bicyclic heterocyclic groups of general formula wherein Ra, Rb, Rc, Rd and X are defined as in claim 1, the tautomers, the stereoisomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, as well as benign prostate hyperplasia (BPH), diseases of the lungs and respiratory tract, and the preparation thereof.
    Type: Grant
    Filed: March 27, 2003
    Date of Patent: August 2, 2005
    Assignee: Boehringer Ingelheim Pharma GmbH & Co.
    Inventors: Frank Himmelsbach, Birgit Jung, Flavio Solca
  • Patent number: 6849733
    Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.
    Type: Grant
    Filed: August 22, 1997
    Date of Patent: February 1, 2005
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Yufeng Hong, Vlad Edward Gregor, Anthony Lai Ling, Eileen Valenzuela Tompkins
  • Patent number: 6849658
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r?)(r?) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r? and r? are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of the compounds of formula (I).
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: February 1, 2005
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille