Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
  • Patent number: 10280142
    Abstract: There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a catalyst using the same compound.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: May 7, 2019
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Yoichiro Kuninobu, Motomu Kanai, Haruka Ida, Mitsumi Nishi
  • Patent number: 10085449
    Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
    Type: Grant
    Filed: June 27, 2017
    Date of Patent: October 2, 2018
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Ryo Horikoshi, Masahiro Nomura, Yasumichi Onozaki
  • Patent number: 9975851
    Abstract: A method for producing a compound represented by formula (I) comprises the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of trifluoroacetic acid as an acylating agent to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B), as follows
    Type: Grant
    Filed: March 4, 2015
    Date of Patent: May 22, 2018
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Nozomu Nakanishi, Shigeki Kitsuda, Yoshimasa Fukuda
  • Patent number: 9908852
    Abstract: There are provided a compound capable of being a novel ligand allowing regioselective borylation to be performed in the aromatic borylation reaction, and a catalyst using the same compound.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: March 6, 2018
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Yoichiro Kuninobu, Motomu Kanai, Haruka Ida, Mitsumi Nishi
  • Patent number: 9357776
    Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: June 7, 2016
    Assignee: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
  • Patent number: 9174939
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Grant
    Filed: August 31, 2012
    Date of Patent: November 3, 2015
    Assignee: Amakem NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Patent number: 8957214
    Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: February 17, 2015
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Ryo Horikoshi, Masahiro Nomura, Yasumichi Onozaki
  • Publication number: 20150025235
    Abstract: Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.
    Type: Application
    Filed: May 30, 2014
    Publication date: January 22, 2015
    Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
  • Patent number: 8927728
    Abstract: Photoreactive DNA cleaving conjugate compounds are provided comprising a DNA cleaving moiety which comprises an aryl alkyne group and a polyfunctional pH-regulated DNA-binding moiety which comprises at least one or two amino groups.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: January 6, 2015
    Assignee: The Florida State University Research Foundation, Inc.
    Inventors: Igor Alabugin, Wang-Yong Yang, Saumya Roy, Kemal Kaya, Qing-Xiang Sang
  • Patent number: 8927580
    Abstract: The present invention relates to dipyridyl thiosemicarbazone compounds of formula (I): wherein R1 is cyclohexyl or ethyl; as well as pharmaceutical compositions containing those compounds, and the use of those compounds and compositions in the treatment of cancer.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: January 6, 2015
    Assignee: Oncochel Therapeutics LLC
    Inventors: Des R. Richardson, David B. Lovejoy
  • Publication number: 20140350055
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: August 31, 2012
    Publication date: November 27, 2014
    Applicant: Amakem NV
    Inventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
  • Patent number: 8846932
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: September 30, 2014
    Assignee: University of Southern California
    Inventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
  • Publication number: 20140235671
    Abstract: Compounds of the invention are of the formula wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: Karus Therapeutics Limited
    Inventors: Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
  • Publication number: 20140213791
    Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5-to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].
    Type: Application
    Filed: August 24, 2012
    Publication date: July 31, 2014
    Applicant: MEIJI SEIKA PHARMA CO., LTD.
    Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
  • Publication number: 20140206725
    Abstract: The present invention relates to dipyridyl thiosemicarbazone compounds of formula (I): wherein R1 is cyclohexyl or ethyl; as well as pharmaceutical compositions containing those compounds, and the use of those compounds and compositions in the treatment of cancer.
    Type: Application
    Filed: December 16, 2011
    Publication date: July 24, 2014
    Inventors: Des R. Richardson, David B. Lovejoy
  • Publication number: 20140194349
    Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.
    Type: Application
    Filed: March 11, 2014
    Publication date: July 10, 2014
    Applicant: AbbVie Inc.
    Inventors: David A. DeGoey, Charles A. Flentge, William J. Flosi, David J. Grampovnik, Dale J. Kempf, Larry L. Klein, Ming C. Yeung, John T. Randolph, Xiu C. Wang, Su Yu
  • Patent number: 8771641
    Abstract: The present invention provides a novel radiolabeled aryloxyalinine derivative suitable for in vivo imaging. In comparison to known aryloxyalinine derivative in vivo imaging agents, the in vivo imaging agent of the present invention has better properties for in vivo imaging. The in vivo imaging agent of the present invention demonstrates good selective binding to the peripheral benzodiazepine receptor (PBR), in combination with good brain uptake and in vivo kinetics following administration to a subject.
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: July 8, 2014
    Assignee: GE Healthcare Limited
    Inventors: Harry John Wadsworth, Dennis O'Shea
  • Publication number: 20140155419
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 5, 2014
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
  • Patent number: 8735416
    Abstract: The field of the invention relates to the use of carbohydrate binding compounds as a medicine, their use to treat or prevent viral infections, their use to manufacture a medicine to treat or prevent viral infections and their use in a vaccination strategy. The present invention relates to the use of said compounds to manufacture a medicine to treat or prevent viral infections of subject, more in particular infections with viruses having glycosilated envelope proteins such as Retroviridae (i.e., Lentivirinae), like HIV (human immunodeficiency virus), Flaviviridae, like HCV (hepatitis C virus), Hepadnaviridae, like HBV (hepatitis B virus), Coronaviridae, like SARS corona virus, and Orthomyxoviridae, like influenza A, B, or C.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: May 27, 2014
    Assignee: Technische Universitaet Carolo-Wilhelmina zu Braunschweig
    Inventors: Jan Balzarini, Monika Mazik
  • Publication number: 20140107340
    Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptor
    Type: Application
    Filed: October 10, 2013
    Publication date: April 17, 2014
    Applicant: H. Lundbeck A/S
    Inventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
  • Patent number: 8697729
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Grant
    Filed: November 5, 2009
    Date of Patent: April 15, 2014
    Assignee: University of Southern California
    Inventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos Petasis
  • Publication number: 20140073058
    Abstract: Methods of using dyes and associated technology are provided. A dye, such as a monomeric dye or a dimeric dye, may be used in a nucleic acid gel staining application and/or a nucleic acid detection application. Such a dye and a salt that comprises an anion that is associated with a strong acid and a cation that is associated with a strong base may be used in such an application. A dimeric dye, such as a dimeric dye capable of forming a hairpin-like structure, may be used to stain and/or detect nucleic acids via a release-on-demand mechanism. A dimeric dye having low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, may be used to stain and/or detect nucleic acids.
    Type: Application
    Filed: August 8, 2013
    Publication date: March 13, 2014
    Applicant: Biotium, Inc.
    Inventors: Fei Mao, Wai-Yee Leung
  • Publication number: 20130338368
    Abstract: An object of the present invention is to provide a reagent for protein analysis that has still greater 1) rapidity and 2) high operability, that can be detected with 3) high sensitivity, and that can be detected using 4) a gel imager that carries out excitation with visible light or a detecting device having a highly versatile UV light source (UV transilluminator), and a method for protein analysis. The present invention relates to a composition for analysis of a protein, the composition containing a compound represented by Formula I or a salt thereof; when the composition is applied to a support containing a separated protein, staining and fixation of the protein being carried out thereby, and no destaining of the support after application being required.
    Type: Application
    Filed: June 13, 2013
    Publication date: December 19, 2013
    Inventors: Yoshio Suzuki, Nobuyuki Takagi, Tomoyuki Chimuro, Takuma Sano
  • Publication number: 20130319950
    Abstract: The present invention relates to urea-functionalized crystalline capsules self-assembled by sodium or potassium cation coordination and by hydrogen-bonding water bridges to selectively encapsulate tetrahedral divalent oxoanions from highly competitive aqueous alkaline solutions and methods using this system for selective anion separations from industrial solutions. The method involves competitive crystallizations using a tripodal tris(urea) functionalized ligand and, in particular, provides a viable approach to sulfate separation from nuclear wastes.
    Type: Application
    Filed: May 31, 2012
    Publication date: December 5, 2013
    Applicant: UT-BATTELLE, LLC
    Inventors: Radu Custelcean, Bruce A. Moyer, Arbin Rajbanshi
  • Publication number: 20130317027
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
  • Publication number: 20130310375
    Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • Publication number: 20130310378
    Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).
    Type: Application
    Filed: April 23, 2013
    Publication date: November 21, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KG
    Inventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
  • Publication number: 20130281703
    Abstract: Disclosed are methods and compositions for modulating the function of transcription factors, especially transcription factors that recruit epigenetic regulators (histone modifying enzymes) to specific DNA promoters. The targeted transcription factors include but are not limited to the myocyte enhancing factor (MEF2), the forkhead/winged helix transcription factor FOXP3 and the transcription factor GATA3. Also disclosed are small molecule modulators of MEF2 and its associated factors that include but not limited to histone deacetylases (HDACs), p300/CBP and Cabin1 and the therapeutic applications thereof.
    Type: Application
    Filed: March 13, 2013
    Publication date: October 24, 2013
    Inventors: Lin CHEN, Nimanthi JAYATHILAKA, Aidong HAN, Nicos A. PETASIS
  • Publication number: 20130253142
    Abstract: A novel separating agent for protein purification which not only can adsorb proteins in a sufficient amount for protein purification from a low concentration buffer but also can desorb the adsorbed protein easily just by altering the pH of the buffer and a simple and economical method for its production and a method for protein purification using it. One or two ligands selected from the group consisting of a ligand represented by the following formula (1): (wherein m is an integer of from 2 to 6) and a ligand represented by the following formula (2): (wherein each of R1 and R2 is independently a hydrogen atom or a C1-4 alkyl group, and n is an integer of from 1 to 6) are immobilized on a support via a urethane bond without intervention of a spacer arm.
    Type: Application
    Filed: May 17, 2013
    Publication date: September 26, 2013
    Applicant: TOSOH CORPORATION
    Inventors: Seiji MASUMOTO, Katsuo KOMIYA, Koji NAKAMURA
  • Patent number: 8518948
    Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.
    Type: Grant
    Filed: March 10, 2011
    Date of Patent: August 27, 2013
    Assignee: Ingenium Pharmaceuticals GmbH
    Inventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
  • Publication number: 20130172310
    Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.
    Type: Application
    Filed: September 12, 2012
    Publication date: July 4, 2013
    Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
  • Publication number: 20130158034
    Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.
    Type: Application
    Filed: June 21, 2012
    Publication date: June 20, 2013
    Applicant: Amgen Inc.
    Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
  • Patent number: 8461189
    Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard W. Heidebrecht, Jr., Thomas A. Miller, Matthew G. Stanton, David J. Witter
  • Patent number: 8455654
    Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: June 4, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20130137690
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Patent number: 8445520
    Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: May 21, 2013
    Assignee: Pfizer Inc.
    Inventors: Hengmiao Cheng, Xiao Hu, Kevin D. Jerome, Mark G. Obukowicz, Lisa Maria Olson, Paul V. Rucker, Ronald Keith Webber
  • Patent number: 8389553
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 24, 2008
    Date of Patent: March 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter
  • Publication number: 20130029961
    Abstract: Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Gruenenthal GmbH
    Inventors: Robert FRANK, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
  • Publication number: 20120322801
    Abstract: The present invention relates to new kinase inhibitors, more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In addition, the invention relates to methods of treatment and use of said compounds in the manufacture of a medicament for the application to a number of therapeutic indications including sexual dysfunction, inflammatory diseases, ophthalmic diseases and Respiratory diseases.
    Type: Application
    Filed: March 4, 2011
    Publication date: December 20, 2012
    Applicant: Amakem NV
    Inventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
  • Publication number: 20120288940
    Abstract: Photoreactive DNA cleaving conjugate compounds are provided comprising a DNA cleaving moiety which comprises an aryl alkyne group and a polyfunctional pH-regulated DNA-binding moiety which comprises at least one or two amino groups.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 15, 2012
    Applicant: The Florida State University Research Foundation, Inc.
    Inventors: Igor Alabugin, Wang-Yong Yang, Saumya Roy, Kemal Kaya, Qing-Xiang Sang
  • Publication number: 20120245341
    Abstract: The present invention provides an oligonucleotide derivative that enables to easily synthesize an oligonucleotide derivative chemically modified at the 3?-end with two moieties each having a benzene or pyridine structure with a few steps, an aromatic compound serving as a precursor for preparing the modification carrier for synthesizing oligonucleotide derivative, and the oligonucleotide derivative and the oligonucleotide construct using the same, that is chemically modified at the 3?-end with two moieties each having a benzene or pyridine structure, and has good permeability through a cell membrane and excellent nuclease resistance. The modification carrier for synthesizing oligonucleotide derivative, comprising a unit and a carrier carrying the unit directly or via a linker, wherein the unit is represented by the formula (a): wherein, R1 to R6 each independently represent hydrogen or a substituent other than hydrogen; Z1 and Z2 each independently represent CH or nitrogen; and X represents oxygen or sulfur.
    Type: Application
    Filed: December 8, 2009
    Publication date: September 27, 2012
    Inventors: Yukio Kitade, Yoshiaki Kitamura
  • Publication number: 20120225782
    Abstract: Compounds having the following generic formula are disclosed.
    Type: Application
    Filed: April 11, 2012
    Publication date: September 6, 2012
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Nneka T. Breaux, Michael R. Loso, Timothy C. Johnson, Jonathan M. Babcock, Benjamin M. Nugent, Timothy P. Martin, Annette V. Brown, Ronald Ross, JR., William C. Lo, Matthias S. Ober
  • Publication number: 20120220590
    Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.
    Type: Application
    Filed: July 30, 2010
    Publication date: August 30, 2012
    Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
  • Publication number: 20120208988
    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: Application
    Filed: November 11, 2011
    Publication date: August 16, 2012
    Applicant: MOLECULAR INSIGHTS PHARMACEUTICALS, INC.
    Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
  • Publication number: 20120196838
    Abstract: The invention relates to certain compounds according to Formula (I): or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders and immune disorders.
    Type: Application
    Filed: January 25, 2012
    Publication date: August 2, 2012
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
  • Publication number: 20120190684
    Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.
    Type: Application
    Filed: July 22, 2011
    Publication date: July 26, 2012
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
  • Patent number: 8211401
    Abstract: A compound of Formula I, a pharmaceutically acceptable salt, or solvate thereof: complexes with metals such as rhenium, technetium, and others to provide a complex for imaging tissues or treating disease, particularly where the metal is radioactive. Such complexes are specific to PSMA protein and can therefore be used in imaging or treating cancer of the prostate and other tissue where the protein is expressed.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
  • Patent number: 8211402
    Abstract: A compound that recognizes and binds to the CA-IX protein has Formula I, II, III, or IV. The compounds may include a radioactive element for radioimaging or therapeutic applications. Thus, pharmaceutical compositions may be prepared with one or more of the compounds of Formula I, II, III, or IV.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
  • Publication number: 20120157462
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Application
    Filed: January 30, 2008
    Publication date: June 21, 2012
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • Patent number: 8183239
    Abstract: The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.
    Type: Grant
    Filed: October 27, 2006
    Date of Patent: May 22, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Pascal Bonaventure, Nicholas I. Carruthers, Wenying Chai, Curt A. Dvorak, Jill A. Jablonowski, Dale A. Rudolph, Mark Seierstad, Chandravadan R. Shah, Devin M. Swanson, Victoria D. Wong