The Bicyclo Ring System Is 1,4-benzodiazepine (including Hydrogenated) Patents (Class 540/504)
  • Patent number: 11254664
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: March 17, 2020
    Date of Patent: February 22, 2022
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Kaicheng Zhu, Kevin McGrath, Solymar Negretti-Emmanuelli, Adam Szymaniak, Jianming Yu, In Jong Kim, Yat Sun Or
  • Patent number: 10000464
    Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting materials or as intermediates for performing that process.
    Type: Grant
    Filed: October 27, 2016
    Date of Patent: June 19, 2018
    Assignee: PAION UK LIMITED
    Inventors: Gary Stuart Tilbrook, Andreas Schumacher, Rene Emmenegger
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Patent number: 8946208
    Abstract: A composition for intranasal delivery of a drug comprising: includes: (i) the drug; and (ii) a non-aqueous vehicle containing (a) propylene glycol and at least one additional solvent selected from N-methylpyrrolidone, propylene carbonate, dimethyl sulfoxide and at least one propylene glycol fatty acid ester; (b) from about 40 to 100% by volume of N-methylpyrrolidone; or (c) from about 40 to 100% by volume of dimethyl sulfoxide (DMSO).
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: February 3, 2015
    Assignee: Archimedes Development Limited
    Inventors: Jonathan Castile, Alan Smith, Yu-Hui Cheng, Peter James Watts
  • Publication number: 20150030683
    Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.
    Type: Application
    Filed: February 15, 2013
    Publication date: January 29, 2015
    Inventors: Varghese John, Dale E. Bredesen, Stelios Tzannis
  • Patent number: 8871756
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.
    Type: Grant
    Filed: July 30, 2012
    Date of Patent: October 28, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
  • Patent number: 8759340
    Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: June 24, 2014
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Publication number: 20140135315
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: April 9, 2013
    Publication date: May 15, 2014
    Applicant: KuDOS Pharmaceuticals Limited
    Inventor: KuDOS Pharmaceuticals Limited
  • Patent number: 8673897
    Abstract: The invention provides 1,4-benzodiazepinone compounds, pharmaceutical compositions, and methods of treating autoimmune disorders, chronic inflammatory disorders, and hyperproliferative disorders. For example, the 1,4-benzodiazepinone compounds and pharmaceutical compositions are contemplated to be useful for treating rheumatoid arthritis, graft-versus-host disease, inflammatory bowel disease, and the like.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: March 18, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Alexander Ross Hurd, Chad Alan Van Huis
  • Patent number: 8604023
    Abstract: The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: December 10, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Clarke Bentley Taylor, Peter Laurence Toogood, Chad Alan Van Huis
  • Publication number: 20130274197
    Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
    Type: Application
    Filed: June 5, 2013
    Publication date: October 17, 2013
    Inventor: Gary D. Glick
  • Publication number: 20130196974
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.
    Type: Application
    Filed: July 30, 2012
    Publication date: August 1, 2013
    Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
  • Publication number: 20130190300
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.
    Type: Application
    Filed: December 17, 2012
    Publication date: July 25, 2013
    Applicant: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Anthony W. Opipari
  • Patent number: 8461153
    Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: June 11, 2013
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Patent number: 8450307
    Abstract: In part, the present invention is directed to antibacterial compounds.
    Type: Grant
    Filed: June 6, 2005
    Date of Patent: May 28, 2013
    Assignee: Affinium Pharmaceuticals, Inc.
    Inventors: Bruce J. Sargent, Henry Pauls, Judd M. Berman, Jailall Ramnauth, Peter Sampson, Andras Toro, Fernando J. Martin, Matthew D. Surman, Helene Y. Decornez, David D. Manning
  • Patent number: 8440652
    Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: May 14, 2013
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
  • Publication number: 20130023525
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Application
    Filed: April 24, 2012
    Publication date: January 24, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
  • Patent number: 8343961
    Abstract: The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: January 1, 2013
    Assignee: ArQule, Inc.
    Inventors: Robert Nicewonger, Audra Dalton, Chris Brassard, Mark A. Ashwell, Rocio Palma
  • Publication number: 20120329785
    Abstract: The present invention relates to novel compounds of formula (I) that are capable of inhibiting one or more kinases, especially SYK (Spleen Tyrosine Kinase), LRRK2 (Leucine-rich repeat kinase 2) and/or MYLK (Myosin light chain kinase) or mutants thereof. The compounds find applications in the treatment of a variety of diseases.
    Type: Application
    Filed: April 23, 2012
    Publication date: December 27, 2012
    Applicant: Origenis Gmbh
    Inventors: Michael Thormann, Andreas Treml, Michael Almstetter, Roland Koestler, Nasser Yehia
  • Patent number: 8318719
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: November 27, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
  • Publication number: 20120289498
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
    Type: Application
    Filed: July 10, 2012
    Publication date: November 15, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Gary D. Glick
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Publication number: 20120225857
    Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.
    Type: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
  • Publication number: 20120214801
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Application
    Filed: December 15, 2011
    Publication date: August 23, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Gary D. Glick
  • Patent number: 8242108
    Abstract: The described invention relates to compounds which modulate cell migration, and find use in, for example, wound healing, cancer progression and angiogenesis.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: August 14, 2012
    Assignee: University of Dundee
    Inventors: Ana Maria Schor, Seth Lawrence Schor, Rodolfo Marquez, David George Norman
  • Publication number: 20120184732
    Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.
    Type: Application
    Filed: September 22, 2010
    Publication date: July 19, 2012
    Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Motoaki Sato
  • Publication number: 20120165519
    Abstract: The present invention provides a compound of formula I or II or a pharmaceutically acceptable salt form thereof, wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, and A5, are as defined herein. The compounds of formula I or II have ALK and/or c-Met inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: March 6, 2012
    Publication date: June 28, 2012
    Applicant: Cephalon, Inc.
    Inventors: Gulzar Ahmed, Henry Joseph Breslin, Jason Burke, Matthew A. Curry, James L. Diebold, Bruce Dorsey, Benjamin J. Dugan, Daming Feng, Diane E. Gingrich, Tao Guo, Keith S. Learn, Joseph G. Lisko, Rong-qiang Liu, Eugen Mesaros, Karen Milkiewicz, Gregory R. Ott, Jay P. Theroff, Tho V. Thieu, Rabindranath Tripathy, Theodore L. Underiner, Gregory J. Wells, Craig A. Zificsak
  • Publication number: 20120142673
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: KuDOS PHARMACEUTICALS LIMITED
    Inventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Malagu, Niall Morrison Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
  • Patent number: 8188072
    Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: May 29, 2012
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Publication number: 20120094982
    Abstract: The invention provides a family of 1,4-benzodiazepinone compounds and methods for their use as therapeutic agents in treating cancer. Pharmaceutical compositions and methods of making the 1,4-benzodiazepinone compounds are provided.
    Type: Application
    Filed: April 16, 2010
    Publication date: April 19, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Clarke Bentley Taylor, Peter Laurence Toogood, Chad Alan Van Huis
  • Publication number: 20120077805
    Abstract: The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations.
    Type: Application
    Filed: July 21, 2011
    Publication date: March 29, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Gary D. Glick, Adam Matzger
  • Publication number: 20120040971
    Abstract: The present invention provides a family of benzodiazepinone compounds and pharmaceutical compositions thereof. The present invention also provides methods of treating certain skin conditions, e.g., atopic dermatitis, rosacea, or psoriasis, by administering a benzodiazepinone and methods of reducing the proliferation of keratinocyte cells by exposing such cells to a benzodiazepinone.
    Type: Application
    Filed: October 27, 2011
    Publication date: February 16, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Gary D. Glick
  • Patent number: 8097612
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Grant
    Filed: June 8, 2007
    Date of Patent: January 17, 2012
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Patent number: 8088759
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides novel 1,4-benzodiazepine-2,5-dione compounds, and methods of using novel 1,4-benzodiazepine-2,5-dione compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Grant
    Filed: November 1, 2006
    Date of Patent: January 3, 2012
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Patent number: 8039616
    Abstract: Use of a benzodiazepine of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in treating or preventing a hepatitis C infection, wherein: —R1 represents C1-6 alkyl, aryl or heteroaryl; —R2 represents hydrogen or C1-6 alkyl; —each R3 is the same or different and represents halogen, hydroxy, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 haloalkyl, C1-6 haloalkoxy, amino, mono(C1-6 alkyl)amino, di(C1-6 alkyl)amino, nitro, cyano, —CO2R?, —CONR?R?, —NH—CO—R?, —S(O)R?, —S(O)2R?, —NH—S(O)2R?, —S(O)NR?R? or —S(O)2NR?R?, wherein each R? and R? is the same or different and represents hydrogen or C1-6 alkyl; —n is from 0 to 3; —R4 represents hydrogen or C1-6 alkyl; —R5 represents C1-6alkyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, aryl-(C1-6 alkyl)-, heteroaryl-(C1-6 alkyl)-, carbocyclyl-(C1-6 alkyl)-, heterocyclyl-(C1-6 alkyl)-, aryl-(C1-6 hydroxyalkyl)-, heteroaryl-(C1-6hydroxyalkyl)-, carbocyclyl-(C1-6 hydroxyalkyl)-, heterocyclyl-(C1-6hydroxyalkyl)-, aryl-C(O)—
    Type: Grant
    Filed: September 19, 2005
    Date of Patent: October 18, 2011
    Assignee: AstraZeneca AB
    Inventors: Helena Dennison, Justin Warne, Keith Spencer, George Cockerill, James Lumley
  • Publication number: 20110245238
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Application
    Filed: June 17, 2011
    Publication date: October 6, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Manzer Durrani, William B. Geiss, David J. Fairfax, Dmytro O. Tymoshenko, Van-Duc Le, Lisa H. Peterson
  • Publication number: 20110195959
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
    Type: Application
    Filed: December 7, 2010
    Publication date: August 11, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventor: Gary D. Glick
  • Publication number: 20110195954
    Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as mentioned in the description, the tautomers thereof, the isomers thereof, the diastereomers thereof, the enantiomers thereof, the hydrates thereof, the mixtures thereof and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Application
    Filed: November 21, 2008
    Publication date: August 11, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
  • Publication number: 20110196147
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 4, 2011
    Publication date: August 11, 2011
    Inventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
  • Patent number: 7994313
    Abstract: The present invention relates to systems and methods for generating new forms of benzodiazepine and benzodiazepine related compounds as well as new compounds and formulations generated by such methods. In particular, the present invention provides high throughput systems and methods for generating and identifying new crystalline benzodiazepine and benzodiazepine related polymorphs and new unsolvated, solvated, and other forms of the compounds that find use as improved drugs and drug formations.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: August 9, 2011
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Adam Matzger
  • Publication number: 20110152252
    Abstract: The present invention relates to the use of a Shiga toxin B-subunit moiety as carrier for therapeutic agents, for example, anti-cancer agents such as anti-cancer agents that require intracellular uptake to exert their anti-cancer effects. In particular, the present invention provides conjugates comprising a Shiga toxin moiety covalently linked to an anti-cancer agent through a self-immolative spacer, and methods of using such conjugates to increase cellular uptake and/or specificity for cancer cells of the anti-cancer drug. Also provided are methods of treatment involving administration of such conjugates, and pharmaceutical compositions and kits useful for carrying out such methods of treatment.
    Type: Application
    Filed: December 18, 2007
    Publication date: June 23, 2011
    Applicants: INSTITUT CURIE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventors: Ludger Johannes, Abdessamed El Alaoui, Didier Decaudin, Sylvie Robine, Frederic Schmidt, Jean-Claude Florent
  • Publication number: 20110009393
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Application
    Filed: July 19, 2010
    Publication date: January 13, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Manzer Durrani, William B. Geiss, David J. Fairfax, Dmytro O. Tymoshenko, Van-Duc Le, Lisa H. Peterson
  • Publication number: 20110003784
    Abstract: Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
    Type: Application
    Filed: June 16, 2010
    Publication date: January 6, 2011
    Inventors: David S. Garvey, Gregory J. LaRosa, Jeremy R. Greenwood, Mark L. Brewer, Tan Quach, Jamie B. Côté, Judd Berman
  • Publication number: 20100331316
    Abstract: Novel hydroxamate histone deacetylase inhibitors of formula (I) wherein X is C?O or CH2 used as antineoplastic agent.
    Type: Application
    Filed: December 18, 2008
    Publication date: December 30, 2010
    Inventors: Francesco Paoletti, Maria Novella Romanelli, Cristina Cellai, Anna Laurenzana, Luca Guandalini
  • Patent number: 7851465
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine compounds, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, vascular abnormalities, and the like.
    Type: Grant
    Filed: March 7, 2008
    Date of Patent: December 14, 2010
    Assignee: The Regents of the University of Michigan
    Inventor: Gary D. Glick
  • Publication number: 20100286109
    Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.
    Type: Application
    Filed: July 22, 2010
    Publication date: November 11, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
  • Publication number: 20100273768
    Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II: wherein, variables Q1, Q2, R, X, Y1, Y2, Y2?, Y3, Y4, Y5, m, and p are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-II and at least one carrier, diluent or excipient.
    Type: Application
    Filed: April 23, 2010
    Publication date: October 28, 2010
    Inventors: Nolan James Dewdney, Ronald Charles Hawley, Rama Kondru, Yingjie Lai, Yan Lou
  • Publication number: 20100234417
    Abstract: A hetero-dimeric or hetero-oligomeric receptor, comprising at least one thyrotropin releasing hormone receptor subunit associated with at least one orexin receptor subunit.
    Type: Application
    Filed: November 9, 2007
    Publication date: September 16, 2010
    Applicant: DIMERIX BIOSCIENCE PTY LTD.
    Inventors: Kevin Donald George Pfleger, Ruth Marie Seeber, Heng See Boon, Karin Ann Eidne
  • Patent number: 7759338
    Abstract: The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and related compounds and methods of using benzodiazepine derivatives and related compounds as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, hyperproliferation, and the like.
    Type: Grant
    Filed: April 26, 2007
    Date of Patent: July 20, 2010
    Assignee: The Regents of the University of Michigan
    Inventors: Manzer Durrani, William B. Geiss, David J. Fairfax, Dmytro O. Tymoshenko, Van-Duc Le, Lisa Helen Peterson
  • Patent number: 7745426
    Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: June 29, 2010
    Assignees: D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.
    Inventors: Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro