N-p-n Or N-n-p Containing Patents (Class 514/138)
  • Patent number: 10640461
    Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: May 5, 2020
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Patent number: 9738667
    Abstract: Provided is a novel phosphorus-containing compound represented by general formula (I). The compound has reactivity with a glycidyl group and is therefore capable of providing a curing epoxy resin composition that is expected to achieve flame retardation and reduction of dielectric constant. wherein m is a number of 1 to 10; R1, R2, R3, and R4 are each hydrogen, alkyl, or aryl; R5 is alkyl, alkanediyl, alkanetriyl, alkanetetrayl, or an aromatic group; X is oxygen or sulfur; Y is oxygen, sulfur, or ?NR?; and R? is hydrogen, alkyl, or aryl.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: August 22, 2017
    Assignee: ADEKA CORPORATION
    Inventors: Takeshi Endo, Kozo Matsumoto, Ken-ichi Tamaso, Ryo Ogawa
  • Patent number: 8946275
    Abstract: Cancer can be treated by administration of a hypoxia-activated prodrug, such as TH-302, alone or in combination with other anticancer agents and/or radiation therapy. In combination therapy, the hypoxia-activated prodrug and another anti-cancer agent or radiation therapy may be administered within the same 24-hour period, and administration of the hypoxia-activated prodrug may be completed prior to beginning administration of the other anticancer agent or radiation therapy.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: February 3, 2015
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Stewart Kroll, Mark Matteucci, Charles P. Hart, Jian-Xin Duan, Karen Curd
  • Publication number: 20140194377
    Abstract: Disclosed herein are crystalline compounds of formula (I) wherein A+ represents a hydroxylated aliphatic ammonium species; and X and Y independently represent leaving groups.
    Type: Application
    Filed: November 6, 2013
    Publication date: July 10, 2014
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: John C. AMEDIO, JR., Barbara WALLNER, Philip B. KOMARNITSKY
  • Patent number: 8697064
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: April 15, 2014
    Assignee: Pierre Fabre Medicament
    Inventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
  • Publication number: 20140072536
    Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 13, 2014
    Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of Nevada
    Inventors: Ryan Wuebbles, Dean Burkin
  • Patent number: 8552048
    Abstract: Compositions containing, and, methods administering, TH302, are useful in treatment of cancer and other hyper-proliferative diseases.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 8, 2013
    Assignee: Threshold Pharmaceuticals, Inc.
    Inventors: Steve Ammons, Jian-Xin Duan, Donald Jung, Mark Matteucci
  • Publication number: 20130183388
    Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.
    Type: Application
    Filed: February 26, 2013
    Publication date: July 18, 2013
    Applicant: LANKENAU INSTITUTE FOR MEDICAL RESEARCH
    Inventor: Lankenau Institute for Medical Research
  • Publication number: 20130150310
    Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
    Type: Application
    Filed: February 7, 2013
    Publication date: June 13, 2013
    Applicant: ARQULE, INC.
    Inventor: ARQULE, INC.
  • Publication number: 20130121994
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of proliferative diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: November 26, 2010
    Publication date: May 16, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marcus Koppitz, Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Tobias Marquardt, Christof Wegscheid-Gerlach, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner, Ulf Bömer
  • Publication number: 20130121986
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: December 26, 2012
    Publication date: May 16, 2013
    Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
  • Publication number: 20130108582
    Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
    Type: Application
    Filed: May 18, 2012
    Publication date: May 2, 2013
    Inventors: Alfredo C. Castro, Michael J. Grogan, William Matsui, Karen J. McGovern, Martin R. Tremblay
  • Publication number: 20120252748
    Abstract: The present invention relates to methods for predicting the responsiveness of a patient to a breast cancer treatment regimen by assaying a biological sample to determine the level of expression of the long-chain fatty acyl-CoA synthetase 4 (ACSL4) in the biological sample. The present invention also provides ACSL4 inhibitors and uses of ACSL4 inhibitors as adjuvant therapies in breast cancer treatment regimens.
    Type: Application
    Filed: March 28, 2012
    Publication date: October 4, 2012
    Inventor: Marie Monaco
  • Publication number: 20120107307
    Abstract: This invention concerns N-(ortho phenylamino dihydropyridyl)sulfonamides and N-(ortho phenylamino dihydropyridyl), N?-alkyl sulfamides which are inhibitors of MEK and are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: March 23, 2010
    Publication date: May 3, 2012
    Applicant: ARDEA BIOSCIENCES INC.
    Inventors: Jean-Michel Vernier, Hong Woo Kim, Marion Hitchcock, Shunqi Yan
  • Patent number: 7772215
    Abstract: A novel water detection composition for use in place of blue gel and a water detection indicator. The water detection composition comprises, as active components, a porphyrin complex, and at least one inorganic acid salt of a metal selected from a group consisting of alkali metals, alkaline earth metals, Al and Fe. The porphyrin complex is: wherein M is P, X is selected from a group consisting of a halogen and OH, and R2 is phenyl, and the water detection composition is supported by a silica gel.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: August 10, 2010
    Assignee: Fuji Silysia Chemical Ltd.
    Inventor: Yoshiyuki Fueda
  • Publication number: 20090156559
    Abstract: 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N-bis(2-chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.
    Type: Application
    Filed: December 12, 2007
    Publication date: June 18, 2009
    Inventors: Edgardo Laborde, Andrew B. Kelson, Wenli Ma, Kevin T. Weber
  • Publication number: 20080255056
    Abstract: Disclosed herein are crystalline compounds of formula (I) wherein A+ represents a hydroxylated aliphatic ammonium species; and X and Y independently represent leaving groups.
    Type: Application
    Filed: April 4, 2008
    Publication date: October 16, 2008
    Applicant: ZIOPHARM Oncology, Inc.
    Inventors: John C. Amedio, Barbara P. Wallner, Philip B. Komarnitsky
  • Patent number: 7304046
    Abstract: The invention provides a compound of formula I: wherein R1, Ra, Rb, Rc, and Rd have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds or salts. The compounds are useful for treating cancer in animals.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: December 4, 2007
    Assignee: Purdue Research Foundation
    Inventors: Richard F. Borch, Marcy Hernick, Carolee Flader
  • Patent number: 6919322
    Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
    Type: Grant
    Filed: March 7, 2001
    Date of Patent: July 19, 2005
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
  • Patent number: 6413948
    Abstract: The present invention relates to a method of treating a glutamate abnormality and a method of effecting a neuronal activity in an animal using a NAALADase inhibitor, and a pharmaceutical composition comprising an effective amount of a NAALADase inhibitor for treating a glutamate abnormality and effecting a neuronal activity in an animal.
    Type: Grant
    Filed: September 2, 1999
    Date of Patent: July 2, 2002
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
  • Patent number: 6121252
    Abstract: The present invention relate to phosphinic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.
    Type: Grant
    Filed: March 30, 1998
    Date of Patent: September 19, 2000
    Assignee: Guilford Pharmaceuticals Inc.
    Inventors: Paul F. Jackson, Takashi Tsukamoto, Yao-Sen Ko, Barbara S. Slusher
  • Patent number: 5919816
    Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.
    Type: Grant
    Filed: October 17, 1997
    Date of Patent: July 6, 1999
    Assignee: BioNumerik Pharmaceuticals, Inc.
    Inventors: Frederick H. Hausheer, Thomas J. Dodd
  • Patent number: 5849797
    Abstract: Now are provided (R)-3,6-diamino-N-(.omega.-aminoalkyl)-hexanamides which are novel compounds having the general formula (I): ##STR1## wherein n stands for 2-5, and which may be for example, (R)-3,6-diamino-N-(2-aminoethyl)hexanamide (n=2) and (R)-3,6-diamino-N-(3-aminopropyl)hexanamide (n=3). Their preparation process is also provided. These novel compounds and acid addition salts thereof have activities inhibitory against Gram-positive bacteria, Gram-negative bacteria and AIDS virus, as well as tumor cells and are chemically stable.These novel compounds and their salts are useful as chemotherapeutic agents for diseases caused by these bacteria or virus and also as antitumor agent.
    Type: Grant
    Filed: February 24, 1997
    Date of Patent: December 15, 1998
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Shinichi Kondo, Yoko Ikeda, Tomio Takeuchi, Rie Shinei, Shuichi Gomi, Seiji Shibahara, Hiroo Hoshino
  • Patent number: 4800194
    Abstract: The present invention involves compounds of the class of acylphosphorotriamides and methods for altering the blood plasma lipid content of mammals which comprises systemically administering to mammals an effective but nontoxic amount of a composition comprising such compounds.
    Type: Grant
    Filed: December 5, 1986
    Date of Patent: January 24, 1989
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Thomas J. Moorehead, Allan V. Bayless
  • Patent number: 4668667
    Abstract: The present invention involves compounds of the class of acylphosphorotriamides and methods for altering the blood plasma lipid content of mammals which comprises systemically administering to mammals an effective but nontoxic amount of a composition comprising such compounds.
    Type: Grant
    Filed: August 1, 1985
    Date of Patent: May 26, 1987
    Assignee: Norwich Eaton Pharmaceuticals, Inc.
    Inventors: Thomas J. Moorehead, Allan V. Bayless