Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/153)
-
Patent number: 8722892Abstract: The present invention relates to synthesis procedures and intermediates of a compound of formula: and the salts thereof.Type: GrantFiled: May 31, 2012Date of Patent: May 13, 2014Assignee: Janssen R&D IrelandInventors: Andras Horvath, Dominique Paul Michel Depre, Dominic John Ormerod
-
Publication number: 20140121207Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: ApplicationFiled: January 3, 2014Publication date: May 1, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
-
Publication number: 20140114075Abstract: A process for the preparation in high yields and purity of the compound 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide of formula (I) and of the pharmaceutically acceptable salts thereof is described. The process has various advantages over those previously described, in particular it avoids the use of acyl azide intermediates and their Curtius rearrangement. Novel intermediates useful for the preparation of compound (I) are also described.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: EOS ETHICAL ONCOLOGY SCIENCE S.p.A. in abbreviated form EOS S.p.A.Inventors: Silvano SPINELLI, Valeria LIVI
-
Publication number: 20140113890Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
-
Patent number: 8703798Abstract: An indoloquinoline wherein the quarternary N-5 atom is a straight C(1-5) chain, a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring; the 10 position is N—R10, O, S, S?O, CH2, or C?O, where R10 is a branched C(1-5) chain, a heteroatom chain, a straight chain substituted terminally by a cycloalkyl or aromatic ring, a branched chain substituted terminally by a cycloalkyl or aromatic ring, a heteroatom chain substituted terminally by a cycloalkyl or aromatic ring. In one embodiment the quarternary N-5 atom is —CH3 and the 10 position is N—(CH2)5-Ph.Type: GrantFiled: February 24, 2012Date of Patent: April 22, 2014Assignee: Florida A&M UniversityInventor: Seth Y. Ablordeppey
-
Publication number: 20140107096Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE
-
Publication number: 20140107097Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Taraneh Mirzadegan, Kelly Ganamet
-
Patent number: 8697720Abstract: Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side phenylether constituent and a right hand side thienopyridone constituent. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-Clostridium difficile agents.Type: GrantFiled: September 11, 2007Date of Patent: April 15, 2014Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong
-
2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS
Publication number: 20140094488Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.Type: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: SANOFIInventors: Alain BRAUN, Olivier DUCLOS, Gilbert LASSALLE, Franz LORGE, Valerie MARTIN, Olaf RITZELER, Aurelie STRUB -
Patent number: 8685971Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: GrantFiled: October 16, 2010Date of Patent: April 1, 2014Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.Inventors: Axel Ullrich, Robert Torka, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
-
Publication number: 20140088094Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.Type: ApplicationFiled: November 8, 2011Publication date: March 27, 2014Applicants: Merck Sharp & Dohme Corp., Lycera CorporationInventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
-
Publication number: 20140073792Abstract: An agricultural or horticultural fungicide contains as an active ingredient thereof at least one compound selected from the group consisting of nitrogenated heterocyclic compounds represented by formula (I) (wherein, R represents a group represented by CR1R2R3 or a cyano group, R1 to R3 represent hydrogen atoms, alkyl groups or hydroxyl groups, or the like, X1 represents a halogeno group or the like, m represents an integer of 0 to 5, X2 represents a halogeno group or the like, n represents an integer of 0 to 3, B represents a carbon atom or a nitrogen atom, D represents a 5- to 7-membered hydrocarbon ring, and A1 to A4 represent carbon atoms or nitrogen atoms, provided that A1 to A4 do not all represent carbon atoms when B represents a carbon atom) and salts thereof.Type: ApplicationFiled: May 17, 2012Publication date: March 13, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Yasuyuki Shiinoki, Masahiro Yokoyama, Juri Kitamura
-
Patent number: 8658670Abstract: Methionyl tRNA synthetase inhibitors (MetRS) are provided for use in therapy as antibacterial agents in Clostridium based infection.Type: GrantFiled: September 11, 2007Date of Patent: February 25, 2014Assignee: Crestone, Inc.Inventors: Joseph Guiles, Xicheng Sun, Nebojsa Janjic, Sarah Strong
-
Patent number: 8648196Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.Type: GrantFiled: October 30, 2012Date of Patent: February 11, 2014Assignee: Abbvie Inc.Inventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
-
Publication number: 20140030223Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: September 25, 2013Publication date: January 30, 2014Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
-
Publication number: 20140018365Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 26, 2011Publication date: January 16, 2014Applicants: MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WISSENSCCHAFTEN E.V., LEAD DISCOVERY CENTER GMBHInventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
-
Patent number: 8629102Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
-
Publication number: 20140012002Abstract: The present invention relates to compounds of general formula I wherein R100 and R200 are each independently hydrogen, C1-C10-alkyl which in case of C2-alkyl may be interrupted by one and in case of C3-C10-alkyl by one or two nonadjacent oxygen atoms, C5-C7-cycloalkyl, aryl, aryl-C1-C10-alkyl or aryloxy-C1-C10-alkyl, D is an m-valent (m=1, 2 or 3) donor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, A is an acceptor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, and the donor moiety D and the acceptor moiety A are ?-conjugated to one another. Furthermore, the present invention relates to the use of compounds of formula I for producing dye-sensitized solar cells and to dye-sensitized solar cells comprising compounds of formula I.Type: ApplicationFiled: July 1, 2013Publication date: January 9, 2014Inventors: Ingmar BRUDER, Robert Send, Simona Urnikaite, Tadas Malinauskas, Maryte Daskeviciene, Vytautas Getautis
-
Publication number: 20130344165Abstract: This disclosure relates to compounds and compositions for forming bone and methods related thereto. In certain embodiments, the disclosure relates to methods of forming bone comprising implanting a bone graft composition comprising a growth factor such as BMP in a subject at a site of desired bone growth or enhancement in combination with a JAB1 blocker.Type: ApplicationFiled: February 23, 2012Publication date: December 26, 2013Applicant: EMORY UNIVERSITYInventors: Scott D. Boden, Sreedhara Sangadala
-
Publication number: 20130343993Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by 5-HT6 receptor ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as 5-HT6 positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: December 26, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
-
Patent number: 8598354Abstract: Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R2 is methyl or haloalkyl; R4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R3 is aliphatic, aryl, aralkyl, or alkylaryl; and R5, R6, R7 and R8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO2R10, wherein R10 is H, alkyl, amino or haloalkyl; provided that in formula I, R5 and R7 are not both H or R6 is not H or methoxy; and in formula II that if R4 is carbonyldioxy then R7 is not methoxy.Type: GrantFiled: June 3, 2011Date of Patent: December 3, 2013Assignees: University of South Florida, Medicines for Malaria VentureInventors: Michael K. Riscoe, Jane X. Kelly, Rolf W. Winter, David J. Hinrichs, Martin J. Smilkstein, Aaron Nilsen, Jeremy Burrows, Dennis Kyle, Roman Manetsch, Richard M. Cross, Andrii Monastyrskyi, David L. Flanigan
-
Publication number: 20130317061Abstract: This invention relates to novel tris(hydroxymethyl)aminomethane, choline and N-methyl-D-glucamine salt forms of the following Compound (1) and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:Type: ApplicationFiled: July 30, 2013Publication date: November 28, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bing-Shiou YANG, Ka YIP
-
Patent number: 8586570Abstract: Peptidyl sensors comprise a metal-binding peptide and one or two kinase recognition sequences with a hydroxyamino acid that can be phosphorylated in the presence of a kinase.Type: GrantFiled: April 27, 2011Date of Patent: November 19, 2013Assignee: Massachusetts Institute of TechnologyInventors: Barbara Imperiali, Elvedin Lukovic, Dora Carrico-Moniz
-
Patent number: 8569506Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: July 24, 2012Date of Patent: October 29, 2013Assignee: Life Technologies CorporationInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue
-
Publication number: 20130267536Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
-
Publication number: 20130252940Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: May 7, 2013Publication date: September 26, 2013Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-ming Chan, Jeff Chen, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
-
Publication number: 20130252999Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.Type: ApplicationFiled: May 13, 2013Publication date: September 26, 2013Applicant: China Medical UniversityInventors: Sheng-Chu KUO, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
-
Publication number: 20130253006Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.Type: ApplicationFiled: May 13, 2013Publication date: September 26, 2013Applicant: China Medical UniversityInventors: Sheng-Chu KUO, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
-
Publication number: 20130245271Abstract: An objective of the present invention is to provide a process for producing 4-carbonyl oxyquinoline derivatives useful as agricultural and horticultural pesticides and fungicides. The objective can be attained by a process for producing 4-carbonyl oxyquinoline derivatives represented by general formula (1), the process including reacting a quinolone derivative with a halogenated compound or an acid anhydride in the presence of a phase transfer catalyst and a base.Type: ApplicationFiled: November 16, 2011Publication date: September 19, 2013Applicants: MEIJI SEIKA PHARMA CO., LTD., NIPPON KAYAKU CO., LTD.Inventors: Shizuo Shimano, Akinori Morikawa, Kenichi Yamamoto, Hiroki Hotta, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa
-
Publication number: 20130243865Abstract: Provided are pharmaceutical compositions in solid form comprising a selective modulator of PPAR-Y suitable for oral dosage to treat subjects having PPAR-Y mediated conditions. Provided further are methods of manufacturing the compositions, and methods of treating a PPAR-Y mediated condition.Type: ApplicationFiled: September 19, 2011Publication date: September 19, 2013Applicant: Intekrin Therapeutics, Inc., INC.Inventors: Kathleen M. Lee, Linda Higgins, Dennis Lanfear
-
Publication number: 20130237708Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.Type: ApplicationFiled: January 22, 2013Publication date: September 12, 2013Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Masaki Okamoto, Akira Sakuragi, Yoshikazu Mori, Muneki Kishida, Takanori Higashijima
-
Patent number: 8530183Abstract: The present invention provides compounds for use as zinc ligand sensors in cellular imaging. These compounds are sensitive imaging agents that can be used with techniques such a laser scanning microscopy in intact cells in culture or in tissue preparations.Type: GrantFiled: June 10, 2011Date of Patent: September 10, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Wen-Hong Li, Daliang Li
-
Patent number: 8530137Abstract: The present invention provides a photoresist composition having a sulfonium salt comprising an anion represented by the formula (IA): wherein R1 and R2 independently represent a hydrogen atom, a C1-C12 aliphatic hydrocarbon group, a C3-C20 saturated cyclic hydrocarbon group, a C6-C20 aromatic hydrocarbon group or a C7-C21 aralkyl group, and the aliphatic hydrocarbon group, the saturated cyclic hydrocarbon group, the aromatic hydrocarbon group and the aralkyl group can have one or more substituents selected from the group consisting of a hydroxyl group, a cyano group, a fluorine atom, a trifluoromethyl group and a nitro group, and one or more —CH2— in the aliphatic hydrocarbon group can be replaced by —O— or —CO—, or R1 and R2 are bonded each other to form a C4-C20 nitrogen-containing ring together with the nitrogen atom to which they are bonded, an acrylic resin having an acid-labile group and being insoluble or poorly soluble in an aqueous alkali solution but becoming soluble in an aqueous alkali solutioType: GrantFiled: February 11, 2011Date of Patent: September 10, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Tatsuro Masuyama, Satoshi Yamaguchi
-
Publication number: 20130225581Abstract: The present invention provides a nitrogen-containing aromatic heterocyclic derivative represented by formula (I): [wherein W represents CR3 (wherein R3 represents a hydrogen atom or the like) or the like, R4 represents a hydrogen atom or the like, R5 represents a hydrogen atom or the like, R9 represents substituted imidazolyl, R12 and R13 may be the same or different, each represent a hydrogen atom or the like, R22 and R23 may be the same or different, each represent a hydrogen atom or the like, R24 represents a hydrogen atom or the like, Y represents C—R25 (wherein R25 represents a hydrogen atom or the like) or the like] or a pharmaceutically acceptable salt thereof and a FGFR inhibitor comprising, as an active ingredient, the nitrogen-containing aromatic heterocyclic derivative or the pharmaceutically acceptable salt thereof, or the like.Type: ApplicationFiled: July 15, 2011Publication date: August 29, 2013Applicant: KYOWA HAKKO KIRIN CO., LTDInventors: Takayuki Furuta, Kazuo Kubo, Toshiyuki Atsumi, Maasa Yamanouchi
-
Publication number: 20130217690Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
-
Publication number: 20130210844Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: February 7, 2013Publication date: August 15, 2013Applicant: Glenmark Pharmaceuticals S.A.Inventor: Glenmark Pharmaceuticals S.A.
-
Publication number: 20130210721Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
-
Publication number: 20130202536Abstract: The invention relates to novel luminescent compositions of matter containing a fluorophore, synthetic methods for making the compositions, macromolecular conjugates of the compositions, and the use of the compositions in various methods of detection. The invention also provides kits containing the compositions and their conjugates for use in the methods of detection.Type: ApplicationFiled: January 13, 2011Publication date: August 8, 2013Applicants: NEW JERSEY INSTITUTE OF TECHNOLOGY, UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Arkady Mustaev, Maxim Kozlov, Salvatore Marras, Lev Krasnoperov, Laura Wirpsza, Shyamala Pillai
-
Patent number: 8501732Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: GrantFiled: July 11, 2012Date of Patent: August 6, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
-
Publication number: 20130197230Abstract: Methods of preparing compounds of formula i(1): or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 join together with the nitrogen atom to which they are attached form a 6 membered heterocycloalkyl group; X1 is H, Br, Cl or F; X2 is H, Br, Cl or F; s is 2-6; n1 is 1-2; and n2 is 1-2.Type: ApplicationFiled: November 13, 2009Publication date: August 1, 2013Inventors: Jo Ann Wilson, Sharique Zuberi, Sriram Naganathan, Erick Goldman, James Kanter
-
Patent number: 8497284Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: September 30, 2011Date of Patent: July 30, 2013Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
-
Publication number: 20130190258Abstract: Methods and small molecule compounds for inhibition of cancer cell proliferation are provided. One example of a class of compounds that may be used is represented by the compound of Formula I or a pharmaceutically acceptable salt, N-oxide or solvate thereof, wherein A, B, D, E, F, G, I, J, R, R1, R2, R2?, R3, R4, R5, R6, R7, R8, R9 are as described herein.Type: ApplicationFiled: January 24, 2013Publication date: July 25, 2013Inventors: John CASHMAN, Mark MERCOLA, Dennis SCHADE, Masanao TSUDA
-
Publication number: 20130190306Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: March 6, 2013Publication date: July 25, 2013Applicant: BioMarin Pharmaceutical Inc.Inventor: BioMarin Pharmaceutical Inc.
-
Publication number: 20130178499Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: October 7, 2011Publication date: July 11, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
-
Patent number: 8476429Abstract: An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.Type: GrantFiled: April 25, 2012Date of Patent: July 2, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Hiroaki Inagaki, Satoshi Komoriya, Makoto Takemura, Rie Miyauchi
-
Patent number: 8471028Abstract: The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an asymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.] to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.Type: GrantFiled: April 15, 2011Date of Patent: June 25, 2013Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Masaki Okamoto, Akira Sakuragi, Yoshikazu Mori, Muneki Kishida, Takanori Higashijima
-
Patent number: 8466157Abstract: Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl4. The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.Type: GrantFiled: September 6, 2011Date of Patent: June 18, 2013Assignees: University of South Florida, H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
-
Publication number: 20130123258Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: ApplicationFiled: October 26, 2012Publication date: May 16, 2013Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
-
Publication number: 20130123244Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Applicant: JANSSEN R&D IRELANDInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
-
Publication number: 20130123284Abstract: Provided herein are compounds useful for kinase inhibition.Type: ApplicationFiled: March 24, 2011Publication date: May 16, 2013Applicant: AMITECH THERAPEUTIC SOLUTIONS INCInventors: Lee Daniel Arnold, Eric A. Murphy