Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/219)
  • Patent number: 10329301
    Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a ?5-containing GABAA receptor agonist (e.g.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: June 25, 2019
    Assignee: AGENEBIO, INC.
    Inventors: Belew Mekonnen, John A. Butera, Jianxing Huang
  • Patent number: 10239889
    Abstract: The present invention provides compounds represented by formulas (1) to (VI) or pharmaceutically acceptable salts thereof:
    Type: Grant
    Filed: September 5, 2018
    Date of Patent: March 26, 2019
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Yoshiaki Ohashi, Yoshihiko Norimine, Tamaki Hoshikawa, Yu Yoshida, Yoshihisa Kobayashi, Nobuhiro Sato, Koji Hagiwara
  • Patent number: 10189797
    Abstract: Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.
    Type: Grant
    Filed: December 30, 2016
    Date of Patent: January 29, 2019
    Assignee: Duke University
    Inventors: Wei Chen, Herbert Kim Lyerly, Xiu-rong Ren, Jiangbo Wang, Hongtao Guo, Amy Hobeika, Robert A. Mook
  • Patent number: 10138231
    Abstract: Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: November 27, 2018
    Assignees: Centro de Investigacion Y Desarrollo de... (CIDEM), Laboratorio de Sintesis Organica de La Facultad...
    Inventors: Yamila Verdecia Reyes, Estael Ochoa Rodríguez, Alberto Ruiz Reyes, Yanier Nuñez Figueredo, Carmen Carillo Domínguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
  • Patent number: 10118926
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: November 6, 2018
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margaretha Henrica Maria Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
  • Patent number: 10081640
    Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: September 25, 2018
    Assignee: IMMUNOGEN, INC.
    Inventors: Baudouin Gérard, Manami Shizuka, Michael Louis Miller, Richard A. Silva
  • Patent number: 10059718
    Abstract: Provided herein are substituted fused quadracyclic compounds useful as inhibitors of MK2. The invention further provides pharmaceutical compositions of the compounds of the invention. The invention also provides medical uses of substituted fused quadracyclic compounds.
    Type: Grant
    Filed: January 3, 2017
    Date of Patent: August 28, 2018
    Assignee: Tabomedex Biosciences, LLC
    Inventors: Casey C. McComas, Michael H. Serrano-Wu, Joseph P. Vacca
  • Patent number: 9968619
    Abstract: A method of treating triple-negative breast cancer in a mammal comprising the step of: administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; —NR5—(CH2)m—R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom; or —NR7—CO—(CH2)n—R8 wherein R7 is a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and R8 is phenyl or pyridyl optionally substituted by a halogen atom, and R4 is —(CH2)n—CO—NH—R9 wherein a is an integer of 1-4, and R9 is alkyl having a carbon
    Type: Grant
    Filed: May 8, 2015
    Date of Patent: May 15, 2018
    Assignee: ONCOETHIX GMBH
    Inventors: Kay Noel, Maurizio D'Incalci
  • Patent number: 9879020
    Abstract: Novel methods of treating inflammation and airway constriction using GABAergic compounds with reduced benzo-diazepine-like CNS activity are provided. Novel compounds which selectively target alpha-4 and alpha-5 GABAA receptors and methods of using those compounds to treat bronchoconstriction and inflammation are provided herein.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: January 30, 2018
    Assignees: UWM Research Foundation, Inc., The Trustees of Columbia University in the City of New York
    Inventors: Douglas C. Stafford, James M. Cook, Alexander E. Arnold, Charles W. Emala, George Gallos, Michael Rajesh Stephen
  • Patent number: 9789120
    Abstract: The invention relates to compositions and methods for effecting male contraception.
    Type: Grant
    Filed: December 21, 2015
    Date of Patent: October 17, 2017
    Assignees: Dana-Farber Cancer Institute, Inc., Baylor College of Medicine
    Inventors: James Elliott Bradner, Martin Matzuk, Jun Qi
  • Patent number: 9556161
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: August 21, 2015
    Date of Patent: January 31, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Patrick Rene Angibaud, Lieven Meerpoel, Alexey Borisovich Dyatkin
  • Patent number: 9315497
    Abstract: The present invention relates to chemistry and pharmacy and, in particular, to the production of novel molecular entities, tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine and pyrimidodiazepine type fused with 1,4-dihydropyridine derivatives, having an effect on the central-nervous and vascular systems. Derivatives containing a dihydropyridine ring are used, by means of reactions with compounds of the ortho-phenylenediamine, ortho-diaminopyridine and ortho-diaminopyrimidine type, and also subsequent conversions to some thereof, to obtain tricyclic and tetracyclic derivatives of general formula I-XII that contain a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, in which the A ring is a substituted or unsubstituted benzene, pyridine or pyrimidine ring.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: April 19, 2016
    Assignee: Centro de Investigacion Y Desarrollo de . . . (CIDEM) Laboratorio de Sintesis Organica de La Facultad . . .
    Inventors: Yamila Verdecia Reyes, Estael Ochoa Rodriguez, Alberto Ruiz Reyes, Yanier Nuñez Figueredo, Carmen Carillo Dominguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
  • Patent number: 9301962
    Abstract: The invention relates to compositions and methods for effecting male contraception.
    Type: Grant
    Filed: May 16, 2011
    Date of Patent: April 5, 2016
    Assignees: Baylor College of Medicine, Dana Farber Cancer Institute, Inc.
    Inventors: James Elliott Bradner, Martin Matzuk, Jun Qi
  • Patent number: 9296863
    Abstract: A polyoctatriazacane molecule is disclosed that has a plurality of octatriazacane groups having the structure and a plurality of divalent bridging groups, each divalent bridging group comprising an aromatic group.
    Type: Grant
    Filed: June 16, 2014
    Date of Patent: March 29, 2016
    Assignee: International Business Machines Corporation
    Inventors: Dylan J. Boday, Jeannette M. Garcia, James L. Hedrick, Rudy J. Wojtecki
  • Patent number: 9296862
    Abstract: A polyoctatriazacane molecule is disclosed that has a plurality of octatriazacane groups having the structure and a plurality of divalent bridging groups, each divalent bridging group comprising an aromatic group.
    Type: Grant
    Filed: December 11, 2014
    Date of Patent: March 29, 2016
    Assignee: International Business Machines Corporation
    Inventors: Dylan J. Boday, Jeannette M. Garcia, James L. Hedrick, Rudy J. Wojtecki
  • Patent number: 9169253
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: October 27, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margaretha Henrica Maria Bakker, Viktor Lakics, Carolin Hoft
  • Patent number: 8999975
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2 and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are inhibitors of Cathepsin C.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Thorsten Oost, Alexander Pautsch, Stefan Peters, Doris Riether, Wolfgang Wienen
  • Patent number: 8987249
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: March 24, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ralf Anderskewitz, Florian Binder, Matthias Grauert, Marc Grundl, Peter Wilhelm Haebel, Thorsten Oost, Alexander Pautsch, Stefan Peters, Viktor Vintonyak
  • Publication number: 20150080325
    Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 1, 2014
    Publication date: March 19, 2015
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Kathryn Rogers, Holger Patzke
  • Publication number: 20150030616
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: June 26, 2014
    Publication date: January 29, 2015
    Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
  • Publication number: 20150025061
    Abstract: The present invention is directed to a method of enhancing visual acuity in a subject, comprising intravitreally administering to the subject in need of such enhancement, a therapeutically effective amount of an extrasynaptic GABAA receptor antagonist. The present invention is also directed to an ocular implant comprising a therapeutically effective amount of the extrasynaptic GABAA receptor antagonist.
    Type: Application
    Filed: July 10, 2014
    Publication date: January 22, 2015
    Inventor: Movses H. Karakossian
  • Patent number: 8927005
    Abstract: Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration in a subject.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: January 6, 2015
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Sreenivasu Mudumba, Philippe J M Dor, Thierry Nivaggioli, David A. Weber, Sidiq Farooq
  • Patent number: 8921358
    Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: March 28, 2013
    Date of Patent: December 30, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Edcon Chang, Matthew H. McNeill, Tracy Duong, Angie Vassar, Takehiro Hirano, Yoshito Terao
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140343046
    Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.
    Type: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
  • Patent number: 8889669
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: November 18, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Michael Louis Miller, Nathan Elliott Fishkin, Ravi V. J. Chari
  • Publication number: 20140288050
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 25, 2014
    Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
  • Publication number: 20140275042
    Abstract: Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyridine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity.
    Type: Application
    Filed: May 20, 2014
    Publication date: September 18, 2014
    Inventors: YAMILA VERDECIA REYES, Estael Ochoa Rodríguez, Alberto Ruiz Reyes, Yanier Nuñez Figueredo, Carmen Carillo Domínguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
  • Patent number: 8809320
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: February 22, 2013
    Date of Patent: August 19, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V. J. Chari
  • Patent number: 8802667
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: August 12, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V. J. Chari
  • Publication number: 20140221355
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
  • Publication number: 20140221356
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Patent number: 8765740
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: July 1, 2014
    Assignee: ImmunoGen, Inc.
    Inventors: Wei Li, Michael Miller, Nathan Fishkin, Ravi V. J. Chari
  • Patent number: 8759339
    Abstract: The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R=R?=(Formula II). n=1-9 and R?=methyl, ethyl, acetyl, benzyl, piperinoyl, 4-fluorophenyl, 4-chlorophenyl, 4-methoxyphenyl, pyridyl, pyrimidyl.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: June 24, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Jayanti Naga Srirama Chandra Murty, Arutla Viswanath
  • Publication number: 20140170111
    Abstract: The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, G, R1, U, V, W, W?, X, X?, Y and Y? are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: September 28, 2011
    Publication date: June 19, 2014
    Applicant: Merck Sharp & Dohmn Corp.
    Inventors: Craig A. Coburn, Brian J. Lavey, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20140155369
    Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.
    Type: Application
    Filed: January 16, 2014
    Publication date: June 5, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Izumi KAMO, Tadatoshi HASHIMOTO
  • Publication number: 20140121202
    Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: Promentis Pharmaceuticals, Inc.
    Inventors: Edward M. Johnson, Daniel G. Lawton
  • Patent number: 8710028
    Abstract: A powder composition for intranasal delivery includes a benzodiazepine drug and chitosan, a salt of chitosan, a derivative of chitosan or a salt of a derivative of chitosan.
    Type: Grant
    Filed: August 29, 2008
    Date of Patent: April 29, 2014
    Assignee: Archimedes Development Limited
    Inventors: Peter James Watts, Yu-Hui Cheng, Alan Smith, Jonathan Castile
  • Publication number: 20140080813
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Publication number: 20140080816
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: September 13, 2013
    Publication date: March 20, 2014
    Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margot Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
  • Publication number: 20140080814
    Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 20, 2014
    Inventor: Wilfried Braje
  • Publication number: 20130338148
    Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: August 21, 2013
    Publication date: December 19, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
  • Patent number: 8592406
    Abstract: There is provided a transnasal anticonvulsive pharmaceutical composition including a poorly soluble anticonvulsant. The anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether and fatty acid ester, wherein the fatty acid ester is selected from the group consisting of caprylocaproyl polyoxylglyceride, isopropyl palmitate, oleoyl polyoxylglyceride, sorbitan monolaurate 20, methyl laurate, ethyl laurate, and polysorbate 20. Also, the anticonvulsive pharmaceutical composition comprising a poorly soluble anticonvulsant as an active component, which is transnasally spray-administered, comprises diethylene glycol monoethyl ether, fatty acid ester, methylpyrrolidone, water and alcohol. Therefore, the transnasal anticonvulsive pharmaceutical composition may be useful to highly enhance the bioavailability of the poorly soluble anticonvulsant.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: November 26, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Myoung-Ki Baek, Jae-Hoon Jo, Hye-Jin Chang
  • Publication number: 20130302357
    Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 14, 2013
    Inventors: Wei Li, Nathan Elliott Fishkin, Robert Yongxin Zhao, Michael Louis Miller, Ravi V.J. Chari
  • Publication number: 20130302352
    Abstract: The present invention relates to methods for the prevention and/or treatment of memory impairment and for improving memory and particularly to methods for the prevention and/or treatment of memory impairment and improving memory comprising administering an agent that decreases activity of a GABAA receptor. The present invention also relates the use of an agent that decreases activity of a GABAA receptor for preventing or treating a memory deficit and for improving memory.
    Type: Application
    Filed: April 22, 2013
    Publication date: November 14, 2013
    Applicant: The Governing Council of the University of Toronto
    Inventor: Beverley A. Orser
  • Patent number: 8546382
    Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: October 1, 2013
    Assignee: Children's Medical Center Corporation
    Inventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
  • Patent number: 8541407
    Abstract: The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine 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, 2011
    Date of Patent: September 24, 2013
    Assignee: ArQule, Inc.
    Inventors: Syed M. Ali, Mark A. Ashwell, Eugene Kelleher, Steffi Koerner, Jean-Marc Lapierre, Jeffrey S. Link, Yanbin Liu, Magdi Moussa, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
  • Publication number: 20130237530
    Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating central nervous system (CNS) disorders with cognitive impairment that are responsive to agonists of ?5 subunit containing GABAA receptor, e.g., age-related cognitive impairment, Mild Cognitive Impairment (MCI), dementia, Alzheimer's Disease (AD), prodromal AD, post traumatic stress disorder (PTSD), schizophrenia and cancer-therapy-related cognitive impairment.
    Type: Application
    Filed: November 15, 2011
    Publication date: September 12, 2013
    Applicant: AGENEBIO, INC.
    Inventor: John A. Lowe, III
  • Publication number: 20130203731
    Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: August 8, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE LIMITED