The Cyano Is Bonded Directly To A Benzene Ring Patents (Class 514/524)
  • Patent number: 10294423
    Abstract: Disclosed are compounds represented by structural formula (I), methods of producing compounds represented by structural formula, and their use in inhibiting oxidation in an oxidizable material.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: May 21, 2019
    Assignee: Polnox Corporation
    Inventors: Ashok L. Cholli, Vijayendra Kumar
  • Patent number: 9907766
    Abstract: Sweetness receptor antagonists represented by formula (I): wherein each symbol is described herein, are useful for the prophylaxis or treatment of metabolic syndrome, diabetes, obesity and the like.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: March 6, 2018
    Assignee: AJINOMOTO CO., INC.
    Inventors: Yoshiro Kitahara, Koji Ohsumi, Seiji Kitajima, Shimpei Ogawa
  • Patent number: 9771592
    Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.
    Type: Grant
    Filed: January 24, 2014
    Date of Patent: September 26, 2017
    Assignees: The Johns Hopkins University, California Institute of Technology
    Inventors: Xinzhong Dong, Qin Liu, David J. Anderson
  • Patent number: 9376376
    Abstract: The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.
    Type: Grant
    Filed: March 6, 2013
    Date of Patent: June 28, 2016
    Assignees: SINOCHEM CORPORATION, SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD.
    Inventors: Changling Liu, Baoshan Chai, Huichao Li, Aiying Guan
  • Patent number: 9114147
    Abstract: This invention relates to a low cost rapid response diagnostic system to determine cortisol levels in patients selected as potential candidates for GCR (glucocorticoid receptor) antagonist therapy utilizing a GCR antagonist, such as ORG 34517. The rapid, sensitive, and inexpensive test can be used to determine patients who have non-normal cortisol production or disordered circadian rhythms as a method for selecting subjects for GCR antagonist therapy for whom it is likely to have beneficial and/or therapeutic effects, and can also be used to monitor changes in cortisol levels in response to treatment.
    Type: Grant
    Filed: December 9, 2013
    Date of Patent: August 25, 2015
    Assignee: Pop Test Oncology Limited Liability Company
    Inventors: Randice Lisa Altschul, Neil David Theise, Myron Rapkin, Rebecca O'Brien
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Publication number: 20150056160
    Abstract: An invention relating to therapeutic pharmacological agents and methods to chemically induce intracellular hyperthermia and/or free radicals for the diagnosis and treatment of infections, malignancy and other medical conditions. The invention relates to a process and composition for the diagnosis or killing of cancer cells and inactivation of susceptible bacterial, parasitic, fungal, and viral pathogens by chemically generating heat, and/or free radicals and/or hyperthermia—inducible immunogenic determinants by using mitochondrial uncoupling agents, especially 2,4 dinitrophenol and, their conjugates, either alone or in combination with other drugs, hormones, cytokines and radiation.
    Type: Application
    Filed: February 24, 2014
    Publication date: February 26, 2015
    Inventors: Nicholas Bachynsky, Woodie Roy
  • Publication number: 20150051199
    Abstract: The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections.
    Type: Application
    Filed: October 31, 2012
    Publication date: February 19, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Christopher Charles Frederick Hamlett, Gilbert Ebai Besong, Gianni Chessari, Maria Grazia Carr, Alessia Millemaggi, David Norton, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson, Steven Douglas Hiscock
  • Publication number: 20150038574
    Abstract: Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: February 5, 2015
    Applicant: Bikam Pharmaceuticals, Inc.
    Inventors: David S. Garvey, Judd Berman, Tan Quach
  • Publication number: 20150011628
    Abstract: The invention relates to substituted diphenylamine compounds using as antitumor agents. The structure of the compounds is represented as the general formula (I): The groups are as defined as specification. The compound represented by formula (I) showed potent antitumor activity, especially to cure or alleviate the cancer causing by cancer cells of human tissue or organ. The preferred cancers are: colon cancer, liver cancer, lymph cancer, lung cancer, esophageal cancer, breast cancer, central nervous system cancer, melanoma, ovarian cancer, cervical cancer, renal cancer, leukemia, prostatic cancer, pancreatic cancer, bladder cancer, rectal cancer, osteosarcoma, nasopharynx cancer or stomach cancer.
    Type: Application
    Filed: March 6, 2013
    Publication date: January 8, 2015
    Inventors: Changling Liu, Baoshan Chai, Huichao Li, Aiying Guan
  • Patent number: 8901170
    Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).
    Type: Grant
    Filed: June 22, 2007
    Date of Patent: December 2, 2014
    Assignee: BASF SE
    Inventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
  • Patent number: 8853266
    Abstract: This invention provides use of a SARM compound or a composition comprising the same in treating a variety of diseases or conditions in a subject, including, inter-alia, a diabetes disease, and/or disorder such as cardiovascular disease, atherosclerosis, cerebrovascular conditions, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: October 7, 2014
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller
  • Patent number: 8822467
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 2, 2014
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Brian F. McGuinness, Koc-Kan Ho, Suresh Babu, Guizhen Dong, Jingqi Duo, Thuy X. H. Le, Kurt W. Saionz
  • Publication number: 20140243374
    Abstract: This invention relates generally to the discovery of sulfonamide-containing compounds that are inhibitors of ?-secretase.
    Type: Application
    Filed: October 4, 2012
    Publication date: August 28, 2014
    Inventors: Corinne E. Augelli-Szafran, Dai Lu, HanXun Wei, Jing Zhang, Michael S. Wolfe, Dennis J. Selkoe, Cuiman Cai
  • Publication number: 20140213598
    Abstract: Disclosed is a substituted cyanoaniline compound or a salt thereof, wherein the compound has a structure represented by General Formula I. The compound of General Formula I has broad-spectrum fungicidal activity in the field of agriculture and effectively prevents against a variety of pathogens such as cucumber downy mildew, wheat powdery mildew, maize rust disease, rice blast and cucumber gray mold. In particular, even at a low dose, the compound effectively prevents and treats rice blast, cucumber gray mold, maize rust disease and cucumber downy mildew. Moreover, the raw materials for preparing the compounds are widely available and the synthesis method therefor is simple and convenient.
    Type: Application
    Filed: June 15, 2012
    Publication date: July 31, 2014
    Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATION
    Inventors: Changling Liu, Guang Huang, Jie Lan, Shulin Hao, Zhinian Li, Huichao Li, Aiying Guan, Airu Jiang, Ying Xu
  • Publication number: 20140155390
    Abstract: The present invention relates to a compound of Formula 1, 2 or 3: wherein A is N or —CR0—, where R0 is hydrogen, C1-C6 linear or branched chain alkyl, etc., Z is —CRe—, or, —N—, where Re is hydrogen, C1-C6 linear or branched chain alkyl,etc.; R1 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R2 are independently hydrogen or C1-C6 linear or branched chain alkyl; R3 and R4 are independently hydrogen, C1-C6 linear or branched chain alkyl, etc.;. R5 and R6 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.; R8 is hydrogen, C1-C6 linear or branched chain alkyl, etc.; R9 and R10 are independently hydrogen or C1-C6 linear or branched chain alkyl, etc.
    Type: Application
    Filed: December 2, 2013
    Publication date: June 5, 2014
    Applicant: Pfizer Inc.
    Inventors: James Thomas Anderson, Eugene Lvovich Piatnitski Chekler, Edmund L. Ellsworth, Bruce Kipp Erickson, Adam Matthew Gilbert, Anthony P. Ricketts, David P. Thompson, Rayomand Jal Unwalla, Patrick Robert Verhoest
  • Publication number: 20140121211
    Abstract: Disclosed herein are thiol mediated/activated prodrugs of SO2, particularly 2,4-dinitrophenylsulfonamide analogues, having Formula-I or pharmaceutically acceptable salts thereof exhibiting tunable release profiles of SO2 with significant therapeutic efficacy against bacterial infections. Further, the present invention provides pharmaceutical compositions comprising compound of Formula I or pharmaceutically acceptable salts thereof, along with pharmaceutically acceptable carriers/excipients.
    Type: Application
    Filed: November 30, 2012
    Publication date: May 1, 2014
    Applicant: INDIAN INSTITUTE OF SCIENCE EDUCATION AND RESEARCH -PUNE
    Inventors: Harinath CHAKRAPANI, Satish Ramesh Malwal
  • Patent number: 8669286
    Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.
    Type: Grant
    Filed: September 26, 2012
    Date of Patent: March 11, 2014
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Jeffrey D. Kearbey
  • Patent number: 8604068
    Abstract: The present invention comprises 2-cyanobenzenesulfonic acid amides of the formula (I) and isomeric forms thereof (I-A) and (I-B) wherein R1, R2, R3, R4, R5 and A have the aforesaid meaning for the control of animal pests with the use of penetration enhancers and/or ammonium or phosphonium salts.
    Type: Grant
    Filed: May 21, 2008
    Date of Patent: December 10, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Bernd Alig, Christian Arnold, Rolf Pontzen, Klaus-Helmut Müller
  • Publication number: 20130295009
    Abstract: The present invention relates to the use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is H or OH; R1, R2, R3, R4 and R5 are the same or different and are selected from hydrogen, halogen, alkyl having 1 to 5 carbon atoms, electron donor groups such as alkoxy having 1-5 carbon atoms or hydroxy, electron acceptor groups selected from cyano, nitro, trifluoroalkyl or amide; alkylamino, benzoyloxy, nitroxy, phenyl or sulpho; and the pharmacologically active salts thereof;
    Type: Application
    Filed: March 14, 2013
    Publication date: November 7, 2013
    Inventors: Torbjorn LUNDSTEDT, Anna SKOTTNER, Elisabeth SEIFERT
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130274323
    Abstract: Disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells, reducing resistance of a cancer cell to a chemotherapeutic agent, a method of inhibiting ABCG2, Pgp, or MRP1 in a mammal afflicted with cancer, and a method of increasing the bioavailability of an ABCG2 substrate drug in a mammal. The methods comprise administering effective amounts of certain compounds to the mammal, for example, a compound of the formula (I): wherein R1, R2, R3, X1, X2, X3, a, and b are as described herein. Uses of these compounds in the preparation of a medicament are also disclosed. Also disclosed are compounds of formula (II), pharmaceutical compositions comprising such compounds and uses thereof.
    Type: Application
    Filed: June 5, 2013
    Publication date: October 17, 2013
    Inventors: Curtis J. Henrich, Heidi R. Bokesch, Laura K. Cartner, Richard W. Fuller, Kirk R. Gustafson, Kentaro Takada, James B. McMahon, Susan E. Bates, Robert W. Robey, Suneet Shukla, Suresh V. Ambudkar, Michael C. Dean
  • Publication number: 20130217762
    Abstract: The present invention provides novel selective androgen receptor modulators and their salts and pharmaceutical compositions thereof.
    Type: Application
    Filed: October 5, 2012
    Publication date: August 22, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventor: Eli Lilly and Company
  • Publication number: 20130197039
    Abstract: The present invention provides compounds of Formula below: and analogues thereof where the various substituent groups, R1, R2, R3, R4, R5 A, and X are described herein; or a pharmaceutical salt thereof; a method of treating a condition such as hypertriglyceridemia and a process for preparing the compounds.
    Type: Application
    Filed: January 24, 2013
    Publication date: August 1, 2013
    Applicant: Eli Lilly and Company
    Inventor: Eli Lilly and Company
  • Publication number: 20130197013
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Application
    Filed: July 27, 2011
    Publication date: August 1, 2013
    Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
  • Patent number: 8445534
    Abstract: This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 21, 2013
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
  • Publication number: 20130102609
    Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Applicant: LIGAND PHARMACEUTICALS INC.
    Inventor: Ligand Pharmaceuticals Inc.
  • Patent number: 8399456
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: March 19, 2013
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
  • Patent number: 8389500
    Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: October 28, 2009
    Date of Patent: March 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Publication number: 20120322717
    Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.
    Type: Application
    Filed: May 22, 2009
    Publication date: December 20, 2012
    Inventors: Dakai Liu, Xiaofeng Li, Richard Jin, Yuaxin Liang, Wei Cheng, Riddhi Bhattacharyya, Guangrong Zhang
  • Publication number: 20120322823
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: August 28, 2012
    Publication date: December 20, 2012
    Inventors: Anton F. J. Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara E. Segelstein
  • Patent number: 8314137
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 20, 2012
    Assignee: Trustess of Dartmouth College
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20120289595
    Abstract: The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.
    Type: Application
    Filed: July 25, 2012
    Publication date: November 15, 2012
    Applicant: Catholic University Industry Academy Cooperation Foundation
    Inventor: Dong Heon Shin
  • Patent number: 8309602
    Abstract: The present invention relates to multi-substituted m-diarylanilines or pharmaceutically acceptable salts thereof, wherein X, R1-R7 are as defined in the claims, their preparation process, pharmaceutical compositions comprising them and their use for the manufacture of a medicament for anti-HIV.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: November 13, 2012
    Assignees: Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences P.L.A. China
    Inventors: Lan Xie, Bingjie Qin, Kuo-Hsiung Lee, Shibo Jiang, Hong Lu
  • Patent number: 8309603
    Abstract: This invention is directed to a feed composition and method of affecting the carcass composition by increasing the lean mass, reducing the fat mass, and/or reducing the percent fat mass comprising SARM compounds.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: November 13, 2012
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Jeff Kearbey
  • Publication number: 20120283267
    Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.
    Type: Application
    Filed: December 2, 2010
    Publication date: November 8, 2012
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Heidi G. Elmendorf, Colleen D. Walls, Christian Wolf
  • Publication number: 20120237446
    Abstract: The present invention relates to novel compounds (3-aminopropen-1-ones) useful for binding and imaging beta amyloid deposits and their use in detecting or treating Alzheimer's disease and amyloidosis.
    Type: Application
    Filed: March 26, 2012
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrike Röhn, Hermann Künzer, Tobias Heinrich, Markus Berger, Damian Brockschnieder, Sabine Krause, Thomas Dyrks, Andrea Thiele, Ursula Mönning, Ulf Bömer
  • Patent number: 8242118
    Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
    Type: Grant
    Filed: April 19, 2010
    Date of Patent: August 14, 2012
    Assignee: Axikin Pharmaceuticals Inc.
    Inventors: Yingfu Li, Akihiko Watanabe, Timothy B. Lowinger, Kevin Bacon, Norihiro Kawamura, Takuya Shintani, Tetsuo Kikuchi, Toshiya Moriwaki, Klaus Urbahns, Keiko Fukushima, Noriko Nunami, Takashi Yoshino, Toshiki Murata, Megumi Yamauchi, Hiroko Yoshino
  • Publication number: 20120196894
    Abstract: The present invention relates to compositions and methods that modulate at least one TRP family member. Specifically, the present invention relates to novel TRPA1 antagonists and their use in the treatment of pain such as chronic inflammatory and neuropathic pain. Compounds that can modulate one or more TRPA1 functions are useful in many aspects including, but not limited to, maintaining calcium homeostasis; maintaining sodium homeostasis; modulating intracellular calcium levels; modulating membrane polarization (membrane potential); modulating cation levels; and/or treating or preventing diseases, disorders, or conditions associated with calcium homeostasis, sodium homeostasis, calcium or sodium dyshomeostasis, or membrane polarization/hyperpolarization (including hypo and hyperexcitability), and/or treating or preventing diseases, disorders, or conditions associated with regulation or misregulation of TRPA1 expression or function.
    Type: Application
    Filed: September 28, 2010
    Publication date: August 2, 2012
    Inventors: Mark T. Bilodeau, Melissa Egbertson, Ahren Green, John C. Hartnett, Yiwei Li
  • Publication number: 20120178749
    Abstract: The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.
    Type: Application
    Filed: February 21, 2012
    Publication date: July 12, 2012
    Inventors: Michael Roth, Beatriz Fontoura, Shuguang Wei, Neal Satterly
  • Publication number: 20120015909
    Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).
    Type: Application
    Filed: March 30, 2011
    Publication date: January 19, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
  • Publication number: 20120004262
    Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
    Type: Application
    Filed: January 21, 2010
    Publication date: January 5, 2012
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Publication number: 20110229467
    Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.
    Type: Application
    Filed: April 29, 2011
    Publication date: September 22, 2011
    Applicant: PHIGENIX, INC.
    Inventor: Carlton D. DONALD
  • Patent number: 8008348
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
    Type: Grant
    Filed: June 7, 2004
    Date of Patent: August 30, 2011
    Assignee: University of Tennessee Research Foundation
    Inventors: Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller
  • Publication number: 20110196007
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: August 11, 2011
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20110195979
    Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.
    Type: Application
    Filed: February 7, 2011
    Publication date: August 11, 2011
    Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
  • Publication number: 20100331321
    Abstract: The invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.
    Type: Application
    Filed: December 18, 2008
    Publication date: December 30, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Johan Bylund, Maria E. Ek, Ylva Gravenfors, Jorg Holenz, Alexander Minidis, Gunnar Nordvall, Daniel Sohn, Karl S.A. Vallin, Jenny Viklund, Stefan Von Berg
  • Patent number: 7855229
    Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: December 21, 2010
    Assignee: University of Tennessee Research Foundation
    Inventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka
  • Publication number: 20100311582
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.
    Type: Application
    Filed: January 23, 2009
    Publication date: December 9, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
  • Patent number: 7846958
    Abstract: The use of benzophenones of the formula I in which R is hydrogen or C1-C4-alkyl and Hal is fluorine, chlorine or bromine for controlling Pseudocercosporella herpotrichoides in crop plants is described.
    Type: Grant
    Filed: July 11, 2003
    Date of Patent: December 7, 2010
    Assignee: BASF SE
    Inventors: Markus Gewehr, Ingo Rose, Bernd Müller, Eberhard Ammermann, Ann Orth, Henry Van Tuyl Cotter