Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Acyclic Nitrogen Patents (Class 546/265)
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Patent number: 11111216Abstract: The present invention includes novel polycationic amphiphilic compounds useful as antimicrobial agents. The present invention further includes methods useful for removing microorganisms and/or biofilm-embedded microorganisms from a surface. The present invention further includes compositions and methods useful for preventing or reducing the growth or proliferation of microorganisms and/or biofilm-embedded microorganisms on a surface.Type: GrantFiled: October 26, 2017Date of Patent: September 7, 2021Assignees: Temple University-Of The Commonwealth System of Higher Education, Villanova UniversityInventors: William M. Wuest, Kevin P. C. Minbiole
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Patent number: 10736319Abstract: Provided is a pest control composition containing a novel iminopyridine derivative and other pest control agents. Provided is a pest control composition containing an iminopyridine derivative represented by the following Formula (I) and at least one of other pest control agents: [in the formula (I), Ar represents a 5- to 6-membered heterocycle which may be substituted, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents hydrogen, halogen and the like, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z)].Type: GrantFiled: March 7, 2019Date of Patent: August 11, 2020Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Ryo Horikoshi, Yasumichi Onozaki, Satoshi Nakamura, Masahiro Nomura, Makoto Matsumura, Masaaki Mitomi
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Patent number: 10280142Abstract: 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: GrantFiled: November 21, 2017Date of Patent: May 7, 2019Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Yoichiro Kuninobu, Motomu Kanai, Haruka Ida, Mitsumi Nishi
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Patent number: 10085449Abstract: 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: GrantFiled: June 27, 2017Date of Patent: October 2, 2018Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Ryo Horikoshi, Masahiro Nomura, Yasumichi Onozaki
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Patent number: 9975851Abstract: 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 followsType: GrantFiled: March 4, 2015Date of Patent: May 22, 2018Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Nozomu Nakanishi, Shigeki Kitsuda, Yoshimasa Fukuda
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Patent number: 9908852Abstract: 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: GrantFiled: January 29, 2015Date of Patent: March 6, 2018Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Yoichiro Kuninobu, Motomu Kanai, Haruka Ida, Mitsumi Nishi
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Patent number: 9357776Abstract: 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: GrantFiled: August 24, 2012Date of Patent: June 7, 2016Assignee: MEIJI SEIKA PHARMA CO., LTD.Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
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Patent number: 9174939Abstract: 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: GrantFiled: August 31, 2012Date of Patent: November 3, 2015Assignee: Amakem NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Patent number: 8957214Abstract: 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: GrantFiled: August 26, 2011Date of Patent: February 17, 2015Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Ryo Horikoshi, Masahiro Nomura, Yasumichi Onozaki
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Publication number: 20150025235Abstract: 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: ApplicationFiled: May 30, 2014Publication date: January 22, 2015Inventors: Richard B. Silverman, Hua Wang, Mohammad Khanfar, Aleksey G. Kazantsev
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Patent number: 8927580Abstract: 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: GrantFiled: December 16, 2011Date of Patent: January 6, 2015Assignee: Oncochel Therapeutics LLCInventors: Des R. Richardson, David B. Lovejoy
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Patent number: 8927728Abstract: 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: GrantFiled: May 7, 2012Date of Patent: January 6, 2015Assignee: The Florida State University Research Foundation, Inc.Inventors: Igor Alabugin, Wang-Yong Yang, Saumya Roy, Kemal Kaya, Qing-Xiang Sang
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Publication number: 20140350055Abstract: 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: ApplicationFiled: August 31, 2012Publication date: November 27, 2014Applicant: Amakem NVInventors: Jo Alen, Sandro Boland, Arnaud Pierre Jean Bourin, Olivier Defert, Dirk Leysen
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Patent number: 8846932Abstract: 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: GrantFiled: March 13, 2013Date of Patent: September 30, 2014Assignee: University of Southern CaliforniaInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos A. Petasis
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Publication number: 20140235671Abstract: 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: ApplicationFiled: April 30, 2014Publication date: August 21, 2014Applicant: Karus Therapeutics LimitedInventors: Stephen Joseph SHUTTLEWORTH, Cyrille Davy TOMASSI
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Publication number: 20140213791Abstract: 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: ApplicationFiled: August 24, 2012Publication date: July 31, 2014Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventors: Nozomu Nakanishi, Yoshimasa Fukuda, Shigeki Kitsuda, Ikuya Ohno
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Publication number: 20140206725Abstract: 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: ApplicationFiled: December 16, 2011Publication date: July 24, 2014Inventors: Des R. Richardson, David B. Lovejoy
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Publication number: 20140194349Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: 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
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Patent number: 8771641Abstract: 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: GrantFiled: December 16, 2010Date of Patent: July 8, 2014Assignee: GE Healthcare LimitedInventors: Harry John Wadsworth, Dennis O'Shea
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Publication number: 20140155419Abstract: 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: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
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Patent number: 8735416Abstract: 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: GrantFiled: April 23, 2012Date of Patent: May 27, 2014Assignee: Technische Universitaet Carolo-Wilhelmina zu BraunschweigInventors: Jan Balzarini, Monika Mazik
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Publication number: 20140107340Abstract: The present invention is directed to benzamide containing compounds which inhibit the P2X7 receptorType: ApplicationFiled: October 10, 2013Publication date: April 17, 2014Applicant: H. Lundbeck A/SInventors: John Paul Kilburn, Lars Kyhn Rasmussen, Mikkel Jessing, Eman Mohammed Eldemenky, Bin Chen, Yu Jiang, Allen T. Hopper
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Patent number: 8697729Abstract: 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: GrantFiled: November 5, 2009Date of Patent: April 15, 2014Assignee: University of Southern CaliforniaInventors: Lin Chen, Nimanthi Jayathilaka, Aidong Han, Nicos Petasis
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Publication number: 20140073058Abstract: 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: ApplicationFiled: August 8, 2013Publication date: March 13, 2014Applicant: Biotium, Inc.Inventors: Fei Mao, Wai-Yee Leung
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Publication number: 20130338368Abstract: 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: ApplicationFiled: June 13, 2013Publication date: December 19, 2013Inventors: Yoshio Suzuki, Nobuyuki Takagi, Tomoyuki Chimuro, Takuma Sano
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Publication number: 20130319950Abstract: 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: ApplicationFiled: May 31, 2012Publication date: December 5, 2013Applicant: UT-BATTELLE, LLCInventors: Radu Custelcean, Bruce A. Moyer, Arbin Rajbanshi
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Publication number: 20130317027Abstract: 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: ApplicationFiled: December 7, 2012Publication date: November 28, 2013Applicant: 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
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Publication number: 20130310375Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20130310378Abstract: 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: ApplicationFiled: April 23, 2013Publication date: November 21, 2013Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KGInventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
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Publication number: 20130281703Abstract: 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: ApplicationFiled: March 13, 2013Publication date: October 24, 2013Inventors: Lin CHEN, Nimanthi JAYATHILAKA, Aidong HAN, Nicos A. PETASIS
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Publication number: 20130253142Abstract: 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: ApplicationFiled: May 17, 2013Publication date: September 26, 2013Applicant: TOSOH CORPORATIONInventors: Seiji MASUMOTO, Katsuo KOMIYA, Koji NAKAMURA
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Patent number: 8518948Abstract: 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: GrantFiled: March 10, 2011Date of Patent: August 27, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Publication number: 20130172310Abstract: 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: ApplicationFiled: September 12, 2012Publication date: July 4, 2013Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20130158034Abstract: 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: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: 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
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Patent number: 8461189Abstract: 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: GrantFiled: June 24, 2008Date of Patent: June 11, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Richard W. Heidebrecht, Jr., Thomas A. Miller, Matthew G. Stanton, David J. Witter
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Patent number: 8455654Abstract: 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: GrantFiled: July 18, 2011Date of Patent: June 4, 2013Assignees: Xerox Corporation, National Research Council of CanadaInventors: Rina Carlini, Darren Andrew Makeiff
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Publication number: 20130137690Abstract: 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: ApplicationFiled: January 28, 2013Publication date: May 30, 2013Inventors: 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
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Patent number: 8445520Abstract: 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: GrantFiled: December 21, 2011Date of Patent: May 21, 2013Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Xiao Hu, Kevin D. Jerome, Mark G. Obukowicz, Lisa Maria Olson, Paul V. Rucker, Ronald Keith Webber
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Patent number: 8389553Abstract: 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: GrantFiled: June 24, 2008Date of Patent: March 5, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Paul Harrington, Solomon Kattar, Thomas A. Miller, Matthew G. Stanton, Paul Tempest, David J. Witter
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Publication number: 20130029961Abstract: 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: ApplicationFiled: July 25, 2012Publication date: January 31, 2013Applicant: Gruenenthal GmbHInventors: Robert FRANK, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Publication number: 20120322801Abstract: 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: ApplicationFiled: March 4, 2011Publication date: December 20, 2012Applicant: Amakem NVInventors: Dirk Leysen, Olivier Defert, Nadzeya Kaval, Petra Blom, Sandro Boland
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Publication number: 20120288940Abstract: 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: ApplicationFiled: May 7, 2012Publication date: November 15, 2012Applicant: The Florida State University Research Foundation, Inc.Inventors: Igor Alabugin, Wang-Yong Yang, Saumya Roy, Kemal Kaya, Qing-Xiang Sang
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Publication number: 20120245341Abstract: 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: ApplicationFiled: December 8, 2009Publication date: September 27, 2012Inventors: Yukio Kitade, Yoshiaki Kitamura
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Publication number: 20120225782Abstract: Compounds having the following generic formula are disclosed.Type: ApplicationFiled: April 11, 2012Publication date: September 6, 2012Applicant: DOW AGROSCIENCES LLCInventors: 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
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Publication number: 20120220590Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
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Publication number: 20120208988Abstract: 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: ApplicationFiled: November 11, 2011Publication date: August 16, 2012Applicant: MOLECULAR INSIGHTS PHARMACEUTICALS, INC.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Publication number: 20120196838Abstract: 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: ApplicationFiled: January 25, 2012Publication date: August 2, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Junyi Zhang, Shoujun Chen, Lijun Sun
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Publication number: 20120190684Abstract: N-Azinyl-N?-aryl ureas and thioureas derivatives are effective at controlling insects.Type: ApplicationFiled: July 22, 2011Publication date: July 26, 2012Applicant: DOW AGROSCIENCES LLCInventors: Noormohamed M. Niyaz, Ricky Hunter, Timothy C. Johnson, Tony K. Trullinger, Annette V. Brown, Kristy Bryan
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Patent number: 8211401Abstract: 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: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier
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Patent number: 8211402Abstract: 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: GrantFiled: December 4, 2009Date of Patent: July 3, 2012Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, Genliang Lu, Shawn Hillier