Tricyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/249)
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Publication number: 20120207697Abstract: The present invention relates to novel quinazoline compounds and their use in perfume compositions. The novel quinazoline compounds of the present invention are represented by the following formula: an isomer or a mixture of isomers thereof, wherein the broken line represents a single or double bond.Type: ApplicationFiled: February 15, 2011Publication date: August 16, 2012Inventors: Michael G. Monteleone, Robert P. Belko, Franc T. Schiet, Paul D. Jones, Anthony T. Levorse, JR.
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Patent number: 8236950Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.Type: GrantFiled: December 19, 2007Date of Patent: August 7, 2012Assignee: Abbott LaboratoriesInventors: David A. Betebenner, Clarence J. Maring, Todd W. Rockway, Curt S. Cooper, David D. Anderson, Rolf Wagner, Rong Zhang, Akhteruzzaman Molla, Hongmei Mo, Tami J. Pilot-Matias, Sherie V L. Masse, Robert J. Carrick, Wenping He, Liangjun Lu
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Publication number: 20120196880Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.Type: ApplicationFiled: December 19, 2011Publication date: August 2, 2012Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
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Patent number: 8211903Abstract: Pyrimido isoquinoline derivatives represented by formula (I): wherein: R1, R2, R3, R4, R7, R8, R9, R10, and are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: GrantFiled: December 15, 2010Date of Patent: July 3, 2012Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Alistair Lochead, Mourad Saady, Philippe Yaiche
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Publication number: 20120157438Abstract: The present invention is directed to pyranyl aryl methyl benzoquinazolinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: August 26, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme CorpInventors: Scott D. Kuduk, Ronald K. Chang, Thomas J. Greshock
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Patent number: 8193528Abstract: The present invention relates to electronic devices, especially electroluminescent devices, comprising azapyrenes of formula (I), or formula (III), wherein Y1, Y2, Y3, Y4, X1, X2 and X3 are independently each other N, or CR4, with the proviso that at least one of the groups X1, X2 and X3 is a group CR4, R1 is hydrogen, F, —SiR100R101R102, or an organic substituent, R4 is hydrogen, F, —SiR100R101R102, or an organic substituent, or any of the substituents R1, R1? and R4, which are adjacent to each other, together form an aromatic, or heteroaromatic ring, or ring system, which can optionally be substituted, m is an integer of 1 to 6, and R100, R101 and R102 are independently of each other a C1-C8alkyl group, a C6-C24aryl group, or a C7-C12aralkyl group, which may optionally be substituted, and Q is a linking group; with the proviso that in the compound of formula (III) at least one of the substituents R1, or R4 is a group Q; especially as host for phosphorescent emitters, electron transporting materials, or emitType: GrantFiled: June 23, 2009Date of Patent: June 5, 2012Assignee: BASF SEInventors: Thomas Schäfer, Thomas Eichenberger, Kristina Bardon, Andrea Ricci, Natalia Chebotareva
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Publication number: 20120136150Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.Type: ApplicationFiled: July 15, 2010Publication date: May 31, 2012Applicant: SDS BIOTECH K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
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Patent number: 8168639Abstract: Novel heterocyclic compounds of formula I: A-B-D??Formula I or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of a moiety having general Formula II and a moiety having general Formula III: B is a moiety selected from the group consisting of: D is a moiety selected from the group consisting of: ?which exhibit a dopamine receptor (preferably a D4 receptor) and/or a serotonine receptor (preferably 5HTA1 agonistic activity), processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of medical conditions associated with the dopaminergic and/or serotonergic systems (e.g., sexual disorders, dyskinesia, anxiety) are disclosed.Type: GrantFiled: September 24, 2007Date of Patent: May 1, 2012Assignee: ATIR Holding S.A.Inventor: Vladimir Kogan
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Patent number: 8148388Abstract: The present invention is drawn to 2,4 (4,6) pyrimidine derived macrocyclcs, pharmaceutical compositions thereof, and methods of making said compounds. The compounds disclosed herein are inhibitors of EGF receptor tyrosine kinases and are useful for treating cell proliferative disorders, including atherosclerosis, restenosis, and cancer.Type: GrantFiled: December 8, 2005Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, N.V.Inventors: Eddy Jean Edgard Freyne, Marc Willems, Werner Constant Johan Embrechts, Kristof Van Emelen, Sven Franciscus Anna Van Brandt, Frederik Jan Rita Rombouts
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Publication number: 20120040966Abstract: The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.Type: ApplicationFiled: December 28, 2009Publication date: February 16, 2012Applicant: Southern Research Institute Office of Commercialization and Intellectual PropInventors: Joseph A. Maddry, Bill Severson, Colleen B. Jonsson, James W. Noah, Diana L. Noah, Xi Chen
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Publication number: 20120039913Abstract: The invention relates to Histamine H4 receptor antagonists or inhibitors of Histamine H4 receptor gene expression for the treatment and/or the prevention of vestibular disorders.Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: INSERM (institut National de la Sante de la Recher Medicale)Inventors: Gilles Desmadryl, Christian Chabbert
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Publication number: 20120022065Abstract: 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: September 30, 2011Publication date: January 26, 2012Applicant: 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
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Patent number: 8093254Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: GrantFiled: December 10, 2007Date of Patent: January 10, 2012Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
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Publication number: 20110312956Abstract: This invention provides novel arylindenopyrimidines of the Formula (I), and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A1 and/or A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.Type: ApplicationFiled: June 16, 2010Publication date: December 22, 2011Inventors: Paul JACKSON, Brian SHOOK
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Patent number: 8063056Abstract: Cyclopenta[g]quinazolines of the formula (I):— wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: March 3, 2010Date of Patent: November 22, 2011Assignee: BTG International LimitedInventors: Vasilios Bavetsias, Ann L Jackman
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Patent number: 8049010Abstract: The present invention publicly discloses a synthetic method and intermediates of rosuvastatin calcium and synthetic methods of the intermediates. The synthetic method uses 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-formaldehyde as the raw material, includes 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acrylonitrile (intermediate I) from a nitrilized reaction, and 4-4?-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acraldehyde (intermediate II) from an aldehydized reaction of the intermediate I, and further goes through such unit processes as side-chain extension, ketone-group reduction, ethyl-group hydrolysis and neutralization reaction or decomposition reaction to obtain rosuvastatin calcium. The nitrilized reagent can be phosphate diethylacetonitrile, acetonitrile, etc.; the aldehyde reductant can be diisobutyl aluminum hydride, red aluminum, etc.Type: GrantFiled: November 18, 2005Date of Patent: November 1, 2011Assignee: Anhui Qingyun Pharmaceuticals & Chemical Co., Ltd.Inventor: Qingyun Huang
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Publication number: 20110224198Abstract: The present invention is directed to benzoquinazilinone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: November 19, 2009Publication date: September 15, 2011Inventors: Scott D. Kuduk, Douglas C. Beshore, ChristinaNg Di Marco, Thomas J. Greshock
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Patent number: 8017614Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.Type: GrantFiled: October 17, 2008Date of Patent: September 13, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Brian C. Shook, Paul F. Jackson
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Patent number: 8017291Abstract: An image-forming material includes a perimidine-based squarylium dye represented by the following Formula (I): wherein, in Formula (I), R represents a hydrogen atom or a methyl group.Type: GrantFiled: January 26, 2009Date of Patent: September 13, 2011Assignee: Fuji Xerox Co., Ltd.Inventors: Minquan Tian, Kazuhiko Hirokawa, Yuka Ito, Suguru Nakaso, Shinji Hasegawa, Miho Watanabe, Takashi Matsubara, Kazunori Anazawa, Tomoco Miyahara, Makoto Furuki
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Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
Patent number: 8012965Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: GrantFiled: December 28, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20110207757Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Applicant: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Publication number: 20110186821Abstract: The present invention relates to electronic devices, especially electroluminescent devices, comprising azapyrenes of formula (I), or formula (III), wherein Y1, Y2, Y3, Y4, X1, X2 and X3 are independently each other N, or CR4, with the proviso that at least one of the groups X1, X2 and X3 is a group CR4, R1 is hydrogen, F, —SiR100R101R102, or an organic substituent, R4 is hydrogen, F, —SiR100R101R102, or an organic substituent, or any of the substituents R1, R1? and R4, which are adjacent to each other, together form an aromatic, or heteroaromatic ring, or ring system, which can optionally be substituted, m is an integer of 1 to 6, and R100, R101 and R102 are independently of each other a C1-C8alkyl group, a C6-C24aryl group, or a C7-C12aralkyl group, which may optionally be substituted, and Q is a linking group; with the proviso that in the compound of formula (III) at least one of the substituents R1, or R4 is a group Q; especially as host for phosphorescent emitters, electron transporting materials, or emitType: ApplicationFiled: June 23, 2009Publication date: August 4, 2011Applicant: BASF SEInventors: Thomas Schäfer, Thomas Eichenberger, Kristina Bardon, Andrea Ricci, Natalia Chebotareva
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Publication number: 20110190211Abstract: A cyclopenta[g]quinazoline derivative, containing an L-Glu-?-D-Glu dipeptide group, of formula (I): wherein R1 is amino, C1-4 hydroxyalkyl, C1-4 fluoroalkyl or methoxy-C1-4-alkyl; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl C2-4 halogenoalkyl or C1-4 cyanoalkyl; and Ar is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy, the compound (I) optionally being in the form of a pharmaceutically acceptable salt or ester; may be used for the treatment of rheumatoid arthritis or acute myeloid leukaemia.Type: ApplicationFiled: March 13, 2009Publication date: August 4, 2011Inventors: Gerrit Jansen, Ann Jackman
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Patent number: 7960400Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: August 27, 2007Date of Patent: June 14, 2011Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Publication number: 20110124666Abstract: The present invention is related to novel 3,4-dihydropyrimidine compounds of formula (I) having TRPA1 receptor antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the modulation of the TRPA1 receptors in animals, in particular humans.Type: ApplicationFiled: May 29, 2009Publication date: May 26, 2011Inventors: Henricus Jacobus Maria Gijsen, Didier Jean-Claude Berthelot, Michel Anna Jozef De Cleyn
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Publication number: 20110124649Abstract: Described herein are novel pyrimidine-pyridine compounds, methods of inhibiting methionine aminopeptidase and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, wherein a compound of the invention is administered to a subject.Type: ApplicationFiled: November 10, 2008Publication date: May 26, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Xiaoyi Hu, Xiaochun Chen, Dawei Ma, Shridhar Bhat
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Publication number: 20110105493Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.Type: ApplicationFiled: October 19, 2010Publication date: May 5, 2011Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Aihua Wang
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Publication number: 20110105492Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease wherein X, R2, R3, and R4 are as defined in the specification.Type: ApplicationFiled: October 19, 2010Publication date: May 5, 2011Inventors: Paul F. Jackson, Mark T. Powell, Brian Christopher Shook, Aihua Wang
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Publication number: 20110105541Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.Type: ApplicationFiled: October 19, 2010Publication date: May 5, 2011Inventors: Paul F. Jackson, Mark T. Powell, Brian Christopher Shook, Aihua Wang
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Publication number: 20110105494Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease. wherein X, R2, R3, and R4 are as defined in the specification.Type: ApplicationFiled: October 19, 2010Publication date: May 5, 2011Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Aihua Wang
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Publication number: 20110105540Abstract: This invention relates to a novel arylindenopyrimidine, A, and its therapeutic and prophylactic uses. Disorders treated and/or prevented include Parkinson's Disease.Type: ApplicationFiled: October 19, 2010Publication date: May 5, 2011Inventors: Paul F. JACKSON, Mark T. Powell, Brian Christopher Shook, Alhua Wang
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Publication number: 20110081365Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X3 is N; X4 is N Or CR3; X5 is —CR4?CR5.Type: ApplicationFiled: February 27, 2009Publication date: April 7, 2011Applicants: IRM LLC, Novartis 35Inventors: Alex Cortez, Yongkai Li, Pranab Mishra, Manmohan Singh, David Skibinski, Nicholas Valiante, Tom Yao-Hsiang Wu, Xiaoyue Zhang, Yefen Zou
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Patent number: 7910733Abstract: The image-forming material includes a perimidine-based squarylium dye represented by the following formula (I):Type: GrantFiled: September 26, 2008Date of Patent: March 22, 2011Assignee: Fuji Xerox Co., Ltd.Inventors: Minquan Tian, Yuka Ito, Shinji Hasegawa, Kazuhiko Hirokawa, Miho Watanabe, Makoto Furuki, Takashi Matsubara, Kazunori Anazawa, Tomoko Miyahara, Suguru Nakaso
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Patent number: 7902359Abstract: This invention relates to a compound of the following formula: wherein R1, R2, R3, G, and Z are defined herein. It also relates to is methods of treating autoimmune disease, cancer, and atherosclerosis with such a compound.Type: GrantFiled: December 11, 2007Date of Patent: March 8, 2011Assignee: Hutchison MediPharma Enterprises LimitedInventors: Tao Wang, Weihan Zhang, Xiaoqiang Yan, Weiguo Su, Jifeng Duan, Yu Cai
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Publication number: 20100331351Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections.Type: ApplicationFiled: January 21, 2010Publication date: December 30, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: David Ginsburg, Hongmin Sun, Scott Larsen, Bryan Yestrepsky
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Publication number: 20100239525Abstract: The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 30, 2009Publication date: September 23, 2010Applicant: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Sudharshan Eathiraj, Eugene Kelleher, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Rocio Palma, Manish Tandon, David Vensel, Neil Westlund, Hui Wu, Rui-Yang Yang
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Publication number: 20100240892Abstract: Disclosed are electroluminescent devices that comprise organic layers that contain certain organic compounds containing one ore more pyrimidine moieties. The organic compounds containing one ore more pyrimidine moieties are suitable components of blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in for example mobile phones, televisions and personal computer screens.Type: ApplicationFiled: June 7, 2010Publication date: September 23, 2010Inventors: THOMAS SCHÄFER, Patrice Bujard, Jonathan Rogers, Kristina Bardon
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Patent number: 7799775Abstract: This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X1 stands for hydrogen, lower alkyl, amino, etc., X2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0-4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT1A agonistic activity and 5-HT3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT1A agonistic activity and 5-HT3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT3 antagonistic agent which concurrently exhibits 5-HT1A agonistic activity, or administering 5-HT1A agonistic agent and 5-HT3 antagonistic agent simultaneously, in sequence or at an interval.Type: GrantFiled: February 25, 2005Date of Patent: September 21, 2010Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Michitaka Sato, Teruaki Matsui, Akira Asagarasu, Hiroyuki Hayashi, Sei-ichi Araki, Satoru Tamaoki, Nobuyuki Takahashi, Yukinao Yamauchi, Yoshiko Yamamoto, Norio Yamamoto, Chisato Ogawa
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Publication number: 20100216824Abstract: Cyclopenta[g]quinazolines of the formula (I):— wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring; p is an integer in the range 1 to 4; R2 is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1 -A5-CON(R)CH(Y4)Y5 -A8-X—Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: ApplicationFiled: March 3, 2010Publication date: August 26, 2010Applicant: BTG International LimitedInventors: Vasilios Bavetsias, Ann L. Jackman
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Patent number: 7781441Abstract: The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. Such compounds have good activity on the 5-HT5A receptor. Therefore, the invention provides methods for the treatment of certain CNS disorders with such compounds.Type: GrantFiled: April 27, 2006Date of Patent: August 24, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Luca Claudio Gobbi, Sabine Kolczewski, Thomas Luebbers, Jens-Uwe Peters, Lucinda Steward
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Publication number: 20100204226Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: February 10, 2010Publication date: August 12, 2010Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, JR., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Patent number: 7759356Abstract: This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant compounds and pharmaceutical compositions.Type: GrantFiled: October 23, 2008Date of Patent: July 20, 2010Assignee: Janssen Pharmaceutica, N.V.Inventors: Geoffrey R. Heintzelman, James Lawrence Bullington, Kenneth C. Rupert
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Publication number: 20100168416Abstract: Polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak
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Patent number: 7741482Abstract: Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.Type: GrantFiled: June 25, 2007Date of Patent: June 22, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Nina Finkelstein
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Patent number: 7705006Abstract: Cyclopenta[g]quinazolines of the formula (I): wherein: A is a group OR or NR0R1 wherein R0 and R1 are each independently hydrogen C1-4 alkyl, C1-4 alkenyl, C1-4 alkynyl, C1-4 hydroxyalkyl, C1-4 halogenoalkyl or C1-4 cyanoalkyl, or R0 and R1 together with the intermediate N form a five- or six-membered heterocyclic ring, p is an integer in the range 1 to 4, R2 is hydrogen C1-4 alkyl, C1-4 alkenyl, C1-4 alkynyl, C1-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar1 is phenylene, thiophenediyl, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy, and R3 is a group of one of the following formulae: -A1-Ar2-A2-Y1-A5-CON(R)CH(Y4)Y5-A5-X-Ar4 and pharmaceutically acceptable salts or esters thereof are of therapeutic value particularly in the treatment of cancer.Type: GrantFiled: March 26, 2007Date of Patent: April 27, 2010Assignee: BTG International LimitedInventors: Vasilios Bavetsias, Ann L Jackman
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Patent number: 7692008Abstract: Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.Type: GrantFiled: June 25, 2007Date of Patent: April 6, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Nina Finkelstein
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Patent number: 7692009Abstract: Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.Type: GrantFiled: June 25, 2007Date of Patent: April 6, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Nina Finkelstein
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Patent number: 7692010Abstract: Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.Type: GrantFiled: June 25, 2007Date of Patent: April 6, 2010Assignee: Teva Pharmaceutical Industries Ltd.Inventor: Nina Finkelstein