Plural 1,3-diazoles Patents (Class 548/312.7)
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Patent number: 11981660Abstract: Provided herein are compounds useful in treating a central nervous system disorder associated with neuronal and/or axonal damage, methods for their preparation, and related pharmaceutical compositions. For example provided herein are compounds of Formula (I): and pharmaceutically acceptable salts and compositions including the same.Type: GrantFiled: March 21, 2019Date of Patent: May 14, 2024Assignees: UNIVERSITY OF MIAMI, Torrey Pines Institute for Molecular StudiesInventors: Vance Lemmon, Hassan Al-Ali, John Bixby, Marc Giulianotti
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Patent number: 10342781Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: July 25, 2017Date of Patent: July 9, 2019Assignee: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Patent number: 10174154Abstract: An epoxy curing agent is disclosed that can be obtained by reacting at least one carboxylic acid with at least one polyamine. The disclosed curing agent can be obtained by preparing an amidoamine with about 0.15 to about 0.30 molar excess of carboxylic acid.Type: GrantFiled: November 4, 2015Date of Patent: January 8, 2019Assignee: Evonik Degussa GmbHInventors: Gauri Sankar Lal, Sudhir Ananthachar, Stephen Michael Boyce
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Patent number: 9750722Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: October 8, 2015Date of Patent: September 5, 2017Assignee: CHEMOCENTRYX, INC.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Patent number: 9353082Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.Type: GrantFiled: December 23, 2009Date of Patent: May 31, 2016Assignee: BIAL—PORTELA & CA, S.A.Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmãmo de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
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Publication number: 20150084016Abstract: An organic electroluminescent element including a luminescent compound represented by the following formula (in which R1 to R14 each independently represent a hydrogen atom, a deuterium atom, an alkyl group, an aryl group, a heteroaryl group, a fluorine atom, a cyano group, an amino group, an alkoxy group, an aryloxy group, a thio group, or a silyl group, and 8 to 13 groups out of R1 to R14 each represent a hydrogen atom or a deuterium atom.) in a light emitting layer has high durability and excellent chromaticity.Type: ApplicationFiled: October 5, 2012Publication date: March 26, 2015Applicant: UDC IRELAND LIMITEDInventors: Toru Watanabe, Yuki Hirai, Tianhua Ouyang, Koji Takaku, Wataru Sotoyama, Tetsu Kitamura, Yasunori Yonekuta
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Patent number: 8980920Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.Type: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8962799Abstract: A method of imaging a region in a subject includes administering to the subject a complex of a metal chelated to a compound, and obtaining an image of the region in the subject.Type: GrantFiled: July 29, 2014Date of Patent: February 24, 2015Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Patent number: 8962670Abstract: Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.Type: GrantFiled: December 20, 2013Date of Patent: February 24, 2015Assignee: UWM Research Foundation, Inc.Inventors: Xiaohua Peng, Yunyan Kuang, Sheng Cao, Wenbing Chen, Yibin Wang
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Publication number: 20150025222Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.Type: ApplicationFiled: April 9, 2014Publication date: January 22, 2015Applicant: Biotium, Inc.Inventors: Fei MAO, Wai-Yee LEUNG, Ching-Ying CHEUNG, Lori Michelle ROBERTS
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Publication number: 20140329815Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 8840865Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecu le, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.Type: GrantFiled: September 30, 2013Date of Patent: September 23, 2014Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Patent number: 8822697Abstract: The present invention relates to a paramagnetic polynuclear metal complex having enhanced self-relaxation rate and thermodynamic stability, and more particularly, to a synthetic method of a novel DTPA-bis-amide-histidine ligand and DTPA-bis-amide-aspartic acid ligand, a novel gadolinium complex ([Gd(L)H2O]) using the ligand, and a paramagnetic polynuclear metal complex using the gadolinium complex. The paramagnetic polynuclear metal complex is able to fix three or more metals (one gadolinium and two metal ions), thereby providing more excellent self-relaxation rate than the commercially available contrast agents. Thus, it can be widely applied to an MRI contrast agent because of meeting the high self-relaxation rate required as a contrast agent of magnetic resonance imaging (MRI).Type: GrantFiled: November 11, 2009Date of Patent: September 2, 2014Assignee: Kyungpook National University Industry-Academic Cooperation FoundationInventors: Tae Jeong Kim, Yong Min Chang, Hee Kyung Kim
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Publication number: 20140238900Abstract: The present invention is related to formulations consisting by block copolymers ?,?-di-aryl or alkyl sulfonates of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w of bis-ammonium and block copolymers ?,?-di-amine of poly(ethylene oxide)w-poly(propylene oxide)-poly(ethylene oxide)w, that are effective in the dewatering and desalting crude whose specific gravities are within the range of 14 to 23° API.Type: ApplicationFiled: February 25, 2014Publication date: August 28, 2014Inventors: Eugenio Alejandro FLORES OROPEZA, Cesar Andres FLORES SANDOVAL, Reyna REYES MARTINEZ, Jose Gonzalo HERNANDEZ CORTEZ, Alfonso LOPEZ ORTEGA, Laura Veronica CASTRO SOTELO, Fernando ALVAREZ RAMIREZ, Arquimedes ESTRADA MARTINEZ, Flavio Salvador VAZQUEZ MORENO
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Publication number: 20140179902Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.Type: ApplicationFiled: September 30, 2013Publication date: June 26, 2014Applicant: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. BABICH, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Publication number: 20140179733Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ChemoCentryx, Inc.Inventors: Xi Chen, Dean R. Dragoli, Pingchen Fan, Juan C. Jaen, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang
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Patent number: 8722719Abstract: Provided is an ester of 3-[(4-dipropylamino-butyl)(4-{[(1H-imidazole-2-ylmethyl)(1-methyl-1H-imidazole-2-ylmethyl)amino]methyl}benzyl)amino]propionic acid which is easily hydrolyzed in serum. The amine compound of the present invention is an ester compound represented by general formula (1). (In general formula (1), n is 1-4, and R1 and R2 represent an alkyl group having 1-3 carbon atoms.Type: GrantFiled: September 30, 2011Date of Patent: May 13, 2014Assignee: Kureha CorporationInventors: Ryo Matsui, Toru Yamazaki, Shigeyuki Kikumoto
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Publication number: 20140127285Abstract: The present invention includes compound compositions and methods of making compounds that include an oligo-benzamide compound having at least two optionally substituted benzamides.Type: ApplicationFiled: October 28, 2013Publication date: May 8, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventor: Jung-Mo Ahn
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Patent number: 8692000Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.Type: GrantFiled: October 27, 2011Date of Patent: April 8, 2014Assignee: National University of SingaporeInventors: Choon Hong Tan, Kuo Wei Huang, Ting Ma, Xiao Fu
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Patent number: 8637561Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 17, 2010Date of Patent: January 28, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Lu Ying, Ce Wang, Xiaowen Peng, Yat Sun Or
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Publication number: 20140018507Abstract: A polyether compound containing oxirane monomer units in an average number per molecule of 5 to 200, wherein the polyether compound has a cationic group and cross-linkable group in the oxirane monomer units, and a cross-linkable composition containing this polyether compound and a cross-linking agent which enables cross-linking of the cross-linkable groups of the polyether compound are provided.Type: ApplicationFiled: March 30, 2012Publication date: January 16, 2014Applicant: ZEON CORPORATIONInventors: Shigetaka Hayano, Hiroyuki Yonemaru, Keisuke Ohta
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Patent number: 8562945Abstract: Complexes of heterocyclic radionuclides are prepared based upon ligands having substituted pyridyl and imidazolyl groups. The ligands are bifunctional, having amino acid residues that may act as a linker to a bioactive molecule, and a tridentate chelator that may complex the radionuclide. The bioactive molecule may be a peptide or somatostatin.Type: GrantFiled: December 4, 2009Date of Patent: October 22, 2013Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig Zimmerman, John Joyal, Kevin P. Maresca, John Marquis, Genliang Lu, Jian-cheng Wang, Shawn Hillier
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Publication number: 20130245280Abstract: Provided is an ester of 3-[(4-dipropylamino-butyl)(4-{[(1H-imidazole-2-ylmethyl)(1-methyl-1H-imidazole-2-ylmethyl)amino]methyl}benzyl)amino]propionic acid which is easily hydrolyzed in serum. The amine compound of the present invention is an ester compound represented by general formula (1). (In general formula (1), n is 1-4, and R1 and R2 represent an alkyl group having 1-3 carbon atoms.Type: ApplicationFiled: September 30, 2011Publication date: September 19, 2013Applicant: KUREHA CORPORATIONInventors: Ryo Matsui, Toru Yamazaki, Shigeyuki Kikumoto
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Patent number: 8519124Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.Type: GrantFiled: March 8, 2012Date of Patent: August 27, 2013Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Publication number: 20130217889Abstract: Compounds of formula (I): wherein R1 to R8, and X? are defined herein. Also disclosed are methods of making and using these compounds.Type: ApplicationFiled: October 27, 2011Publication date: August 22, 2013Applicant: National University of SingaporeInventors: Choon Hong Tan, Kuo Wei Huang, Ting Ma, Xiao Fu
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Publication number: 20130190355Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicants: Yale University, H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
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Patent number: 8436036Abstract: Compounds of the formula I: including any possible stereoisomers thereof, or a pharmaceutically acceptable salt and/or solvate thereof, as well as pharmaceutical formulations and the use of compounds of formula I as HCV inhibitors.Type: GrantFiled: April 23, 2010Date of Patent: May 7, 2013Assignee: Janssen R&D IrelandInventors: Samuel Dominique Demin, David McGowan, Stefaan Julien Last, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8426458Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 17, 2010Date of Patent: April 23, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Datong Tang
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Patent number: 8420686Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: February 17, 2010Date of Patent: April 16, 2013Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Datong Tang, Yao-Ling Qiu
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Publication number: 20130040963Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences, Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, David A. PAISNER
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Patent number: 8367845Abstract: One embodiment of the present invention relates to ionic liquids and ionic viscoelastics formed between [1] a small molecule or macromolecule containing two or more cations; and [2] a small molecule or macromolecule containing two or more anions. Another embodiment of the invention is the use of the inventive ionic liquids and ionic viscoelastics, formed between a small molecule or macromolecule containing two or more cations and a small molecule or macromolecule containing two or more anions, to form a crosslinked network. In certain embodiments, the ionic liquids formed can be viscous liquids, viscous liquid formed networks, or viscoelastic networks/gels. In certain embodiments, the ionic material of the invention may be used for a variety of applications including, but not limited to, lubricants, additives, gas separation, liquid separation, membranes, fuel cells, sensors, batteries, coatings, heat storage, liquid crystals, biocompatible fluids, solvents, and electronic materials.Type: GrantFiled: April 20, 2007Date of Patent: February 5, 2013Assignee: The Trustees of Boston UniversityInventors: Mark W. Grinstaff, Michel Wathier
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Publication number: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130005738Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Applicant: ARIAD Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
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Publication number: 20120316170Abstract: To provide a novel compound or an isotope thereof or a pharmaceutically acceptable salt thereof having S1P lyase inhibitory capacity and inducing the decrease in number of lymphocytes, and a pharmaceutical composition containing these as active ingredients. A compound represented by the general formula (I): or the general formula (II): or an isotope thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Daiichi Sankyo Company LimitedInventors: Nobuo Machinaga, Jun Chiba, Fumihito Muro, Hiroshi Yuita, Jun Watanabe
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Patent number: 8329159Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: August 8, 2007Date of Patent: December 11, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Van N. Nguyen
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Patent number: 8299270Abstract: A gel-like or solid electrolyte containing (i) an electrolyte solution containing an electrolyte dissolved in an organic solvent, (ii) a lamellar clay mineral and/or an organically modified lamellar clay mineral and (iii) a polyvalent onium salt compound and a photoelectric transducer element and a dye-sensitized solar cell using the same.Type: GrantFiled: August 14, 2007Date of Patent: October 30, 2012Assignee: The Yokohama Rubber Co., Ltd.Inventor: Tsukasa Maruyama
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Patent number: 8278307Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: May 8, 2007Date of Patent: October 2, 2012Assignee: ARIAD Pharmaceuticals, Inc.Inventors: William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
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Publication number: 20120232287Abstract: A detergent dispersant contains a nitrogen-containing compound represented by the following formula (1). A lubricating oil composition contains the detergent dispersant. Each symbol in the formula means the same as described in the description.Type: ApplicationFiled: September 29, 2010Publication date: September 13, 2012Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Junya Iwasaki, Izumi Terada
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Publication number: 20120226048Abstract: The present invention relates to a paramagnetic polynuclear metal complex having enhanced self-relaxation rate and thermodynamic stability, and more particularly, to a synthetic method of a novel DTPA-bis-amide-histidine ligand and DTPA-bis-amide-aspartic acid ligand, a novel gadolinium complex ([Gd(L)H2O]) using the ligand, and a paramagnetic polynuclear metal complex using the gadolinium complex. The paramagnetic polynuclear metal complex is able to fix three or more metals (one gadolinium and two metal ions), thereby providing more excellent self-relaxation rate than the commercially available contrast agents. Thus, it can be widely applied to an MRI contrast agent because of meeting the high self-relaxation rate required as a contrast agent of magnetic resonance imaging (MRI).Type: ApplicationFiled: November 11, 2009Publication date: September 6, 2012Applicant: Kyungpook National University Industry-Academic Cooperation FoundationInventors: Tae Jeong Kim, Yong Min Chang, Hee Kyung Kim
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Publication number: 20120207765Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.Type: ApplicationFiled: March 8, 2012Publication date: August 16, 2012Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
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Patent number: 8168627Abstract: Compounds having the structure (or their salts): are used to treat or reduce the likelihood of acquiring androgen-dependent diseases, such as prostate cancer, benign prostatic hyperplasia, polycystic ovarian syndrome, acne, hirsutism, seborrhea, androgenic alopecia and male baldness. The compounds can be formulated together with pharmaceutically acceptable diluents or carriers or otherwise made into any pharmaceutical dosage form. Combinations with other active pharmaceutical agents are also disclosed.Type: GrantFiled: March 16, 2010Date of Patent: May 1, 2012Assignee: Endorecherche, Inc.Inventors: Fernand Labrie, Rock Breton, Shankar Mohan Singh, Rene Maltais
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Patent number: 8114439Abstract: The invention relates to peptides of general formula (I): that can reduce or remove bags formed under the eyes, their stereoisomers and racemic or non-racemic mixtures thereof, and the cosmetically or dermopharmaceutically acceptable salts thereof, wherein X is cystenyl, seryl, threonyl or aminobutyryl; R1 is H or alkyl, aryl, aralkyl or acyl group; and R2 is amino, hydroxy or thiol, all of them substituted or non-substituted with aliphatic or cyclic groups. The invention also relates to a method of obtaining, cosmetic or dermopharmaceutical compositions containing them and their use for treating skin, preferably for reducing or removing bags formed under the eyes.Type: GrantFiled: September 22, 2005Date of Patent: February 14, 2012Assignee: Lipotec, S.A.Inventors: Arturo Puig Montiel, Juan Cebrían Puche, Elena Passerini
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Publication number: 20110263810Abstract: Process for preparing polymeric, ionic compounds comprising imidazolium groups, wherein an ?-dicarbonyl compound, an aldehyde, at least one amino compound having at least two primary amino groups, if appropriate an amino compound having only one primary amino group and a protic acid, where the carbonyl groups of the ?-dicarbonyl compound and of the aldehyde may, if appropriate, also be present as hemiacetal, acetal or hemiketal or ketal, are reacted with one another.Type: ApplicationFiled: December 10, 2009Publication date: October 27, 2011Applicant: BASF SEInventors: Michael Siemer, Sebastian Koltzenburg, Michael Klein
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Patent number: 8022072Abstract: An azolylmethylidenehydrazine derivative represented by the formula (I) wherein Ar is an aryl group optionally having substituent(s) or a heteroaryl group optionally having substituent(s), R1 and R2 are the same or different and each is an alkyl group, a cycloalkyl group, an aralkyl group optionally having substituent(s), an aryl group optionally having substituent(s), a heteroarylalkyl group optionally having substituent(s), or R1 and R2 are bonded to each other to form a nitrogen-containing heterocyclic group optionally having substituent(s), and X is CH or a nitrogen atom, or a pharmacologically acceptable salt thereof is useful as a medicament, particularly as an antifungal agent, or an anti-inflammatory agent or an antiallergic agent.Type: GrantFiled: June 17, 2008Date of Patent: September 20, 2011Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Hironobu Ogura, Yoshiyuki Tatsumi, Yuji Fukamizu
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Patent number: 8012985Abstract: The invention relates to compounds having an anti-parasitic, in particular antimalarial activity, characterized in that they correspond to general formula (I) Applications in particular as compounds with anti-parasitic activity.Type: GrantFiled: July 18, 2003Date of Patent: September 6, 2011Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Henri Vial, Michele Calas, Roger Escale, Valerie Vidal, Francoise Bressolle, Marie-Laure Ancelin
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Publication number: 20110172212Abstract: Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A1 and A2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH2, C(?O), NR11, or CHR35 and D represents a group represented by the following formula (6): [Formula 4] -Q-Y—B??(6) where Q represents a single bond, NR12, or a group represented by the formula (13): and Y represents a group represented by the following formula (7): [Formula 6] —(CR18R19)m3- or —(CR20R21)m4-z-(CR22R23)m5-??(7) where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents —NR25R26; and R1 to R26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: KUREHA CORPORATIONInventors: Atsushi SAITOU, Shigeyuki Kikumoto, Masahiro Ono, Ryo Matsui, Masashi Yamamoto, Tomohiro Sawa, Shigeru Suzuki, Mikiro Yanaka
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Publication number: 20110166132Abstract: The present invention provides compounds that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: December 12, 2008Publication date: July 7, 2011Applicant: Amgen Inc.Inventors: Stephen A. Hitchcock, Jian J. Chen, Mqhele Vellah Ncube, Thomas Nixey, Albert Amegadzie, Roxanne Kunz, Wenyan Qian, Ning Chen, Christopher M. Tegley, Frenel F. De Morin, Chester Chenguang Yuan, Qingyian Liu, Jiawang Zhu, Tanya A.N. Peterkin, Jeffrey A. Adams, Essa Hu, Frank Chavez, JR.
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Publication number: 20110130327Abstract: Multi-arm amine compounds and compositions for enhancing intracellular, in vitro, and in vivo delivery of drug, active, and therapeutic substances including ribonucleic acids. This disclosure provides novel compounds and compositions for making and using delivery materials and carriers which increase the efficiency of delivery of biologically active and pharmacologically active molecules. Embodiments of this disclosure may further provide delivery of various therapeutic agents including nucleic acid therapeutics such as regulatory RNA, interfering RNA, and agents for RNAi, as well as other protein and peptide therapeutics. In some aspects, this disclosure provides multi-arm amine compounds and compositions which can enhance permeation of a drug substance.Type: ApplicationFiled: November 26, 2010Publication date: June 2, 2011Applicant: MARINA BIOTECH, INC.Inventors: MICHAEL E. HOUSTON, JR., ROGER C. ADAMI, STEVEN C. QUAY, PHUONG NGUYEN, HARRY C. WANG, DIANE E. FRANK
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Publication number: 20110124664Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: ApplicationFiled: December 17, 2010Publication date: May 26, 2011Applicant: POLYMEDIX, INC.Inventors: Shaker Mousa, Dahui Liu
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Patent number: 7931824Abstract: A modular surfactant architecture based on room temperature ionic liquids (RTILs) has been developed that affords non-polymerizable and polymerizable amphiphiles that form lamellar (L), hexagonal (H) or bicontinuous cubic (Q) LLC phases when mixed with water or RTILs serving as the polar solvent. The amphiphiles are imidazolium salts having two or more imidazolium head groups joined by one or more spacers. Polymerization of the LLC assembly can produce polymeric materials having ordered nanopores, with the ordering of the pores determined by the LLC phase.Type: GrantFiled: July 3, 2007Date of Patent: April 26, 2011Assignee: The Regents of The University of ColoradoInventors: Douglas L. Gin, Jason E. Bara, Richard D. Noble, Xiaohui Zeng