N-p-n Or N-n-p Containing Patents (Class 514/138)
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Patent number: 10640461Abstract: 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: GrantFiled: March 14, 2016Date of Patent: May 5, 2020Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Patent number: 9738667Abstract: 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: GrantFiled: November 10, 2014Date of Patent: August 22, 2017Assignee: ADEKA CORPORATIONInventors: Takeshi Endo, Kozo Matsumoto, Ken-ichi Tamaso, Ryo Ogawa
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Patent number: 8946275Abstract: 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: GrantFiled: October 21, 2009Date of Patent: February 3, 2015Assignee: Threshold Pharmaceuticals, Inc.Inventors: Stewart Kroll, Mark Matteucci, Charles P. Hart, Jian-Xin Duan, Karen Curd
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Publication number: 20140194377Abstract: 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: ApplicationFiled: November 6, 2013Publication date: July 10, 2014Applicant: ZIOPHARM ONCOLOGY, INC.Inventors: John C. AMEDIO, JR., Barbara WALLNER, Philip B. KOMARNITSKY
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Patent number: 8697064Abstract: 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: GrantFiled: December 26, 2012Date of Patent: April 15, 2014Assignee: Pierre Fabre MedicamentInventors: Frédéric Marion, Jean-Philippe Annereau, Jacques Fahy
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Publication number: 20140072536Abstract: 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: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of NevadaInventors: Ryan Wuebbles, Dean Burkin
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Patent number: 8552048Abstract: Compositions containing, and, methods administering, TH302, are useful in treatment of cancer and other hyper-proliferative diseases.Type: GrantFiled: December 21, 2007Date of Patent: October 8, 2013Assignee: Threshold Pharmaceuticals, Inc.Inventors: Steve Ammons, Jian-Xin Duan, Donald Jung, Mark Matteucci
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Publication number: 20130183388Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: LANKENAU INSTITUTE FOR MEDICAL RESEARCHInventor: Lankenau Institute for Medical Research
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Publication number: 20130150310Abstract: 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: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: ARQULE, INC.Inventor: ARQULE, INC.
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Publication number: 20130121994Abstract: 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: ApplicationFiled: November 26, 2010Publication date: May 16, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: 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
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Publication number: 20130121986Abstract: 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: ApplicationFiled: December 26, 2012Publication date: May 16, 2013Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
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Publication number: 20130108582Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:Type: ApplicationFiled: May 18, 2012Publication date: May 2, 2013Inventors: Alfredo C. Castro, Michael J. Grogan, William Matsui, Karen J. McGovern, Martin R. Tremblay
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Publication number: 20120252748Abstract: 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: ApplicationFiled: March 28, 2012Publication date: October 4, 2012Inventor: Marie Monaco
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Publication number: 20120107307Abstract: 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: ApplicationFiled: March 23, 2010Publication date: May 3, 2012Applicant: ARDEA BIOSCIENCES INC.Inventors: Jean-Michel Vernier, Hong Woo Kim, Marion Hitchcock, Shunqi Yan
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Patent number: 7772215Abstract: 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: GrantFiled: May 18, 2006Date of Patent: August 10, 2010Assignee: Fuji Silysia Chemical Ltd.Inventor: Yoshiyuki Fueda
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Publication number: 20090156559Abstract: 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: ApplicationFiled: December 12, 2007Publication date: June 18, 2009Inventors: Edgardo Laborde, Andrew B. Kelson, Wenli Ma, Kevin T. Weber
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Publication number: 20080255056Abstract: 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: ApplicationFiled: April 4, 2008Publication date: October 16, 2008Applicant: ZIOPHARM Oncology, Inc.Inventors: John C. Amedio, Barbara P. Wallner, Philip B. Komarnitsky
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Patent number: 7304046Abstract: 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: GrantFiled: December 1, 2003Date of Patent: December 4, 2007Assignee: Purdue Research FoundationInventors: Richard F. Borch, Marcy Hernick, Carolee Flader
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Patent number: 6919322Abstract: Novel FBPase inhibitors of the formula I are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.Type: GrantFiled: March 7, 2001Date of Patent: July 19, 2005Assignee: Metabasis Therapeutics, Inc.Inventors: Brett C. Bookser, Qun Dang, K. Raja Reddy
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Patent number: 6413948Abstract: 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: GrantFiled: September 2, 1999Date of Patent: July 2, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Paul F. Jackson, Kevin L. Tays, Keith M. Maclin
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Patent number: 6121252Abstract: 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: GrantFiled: March 30, 1998Date of Patent: September 19, 2000Assignee: Guilford Pharmaceuticals Inc.Inventors: Paul F. Jackson, Takashi Tsukamoto, Yao-Sen Ko, Barbara S. Slusher
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Patent number: 5919816Abstract: 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: GrantFiled: October 17, 1997Date of Patent: July 6, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 5849797Abstract: 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: GrantFiled: February 24, 1997Date of Patent: December 15, 1998Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Shinichi Kondo, Yoko Ikeda, Tomio Takeuchi, Rie Shinei, Shuichi Gomi, Seiji Shibahara, Hiroo Hoshino
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Patent number: 4800194Abstract: 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: GrantFiled: December 5, 1986Date of Patent: January 24, 1989Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Thomas J. Moorehead, Allan V. Bayless
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Patent number: 4668667Abstract: 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: GrantFiled: August 1, 1985Date of Patent: May 26, 1987Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Thomas J. Moorehead, Allan V. Bayless