Plural 1,3-diazine Rings Patents (Class 544/296)
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Patent number: 7683069Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor: wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.Type: GrantFiled: December 12, 2003Date of Patent: March 23, 2010Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Yoshihiro Usui, Masahiro Okuyama, Tokushi Hanano
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Publication number: 20100063069Abstract: The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.Type: ApplicationFiled: September 2, 2009Publication date: March 11, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Publication number: 20100063076Abstract: This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by compounds that block the endothelin signaling pathway that leads to vasoconstriction and in particular those diseases or conditions beneficially treated by endothelin receptor antagonists.Type: ApplicationFiled: July 20, 2009Publication date: March 11, 2010Inventor: Scott L. Harbeson
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Publication number: 20100056532Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 26, 2009Publication date: March 4, 2010Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20100048567Abstract: The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: April 16, 2009Publication date: February 25, 2010Applicant: Portola Pharmaceuticals Inc.Inventors: Zhaozhong Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrota, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey
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Publication number: 20100048568Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: September 30, 2009Publication date: February 25, 2010Applicant: SANOFI-AVENTISInventors: Suzanne C. Aldous, Michael W. Fennie, John Z. Jiang, Stanly John, Lan Mu, Brian Pedgrift, James R. Pribish, Barbara Rauckman, Jeffrey S. Sabol, Grzegorz T. Stoklosa, Sukanthini Thurairatnam, Christopher L. Vandeusen
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Publication number: 20100041568Abstract: A tri-podal compound according to formula (I) wherein, each Z is the same and is a substituted or unsubstituted N-heteroaromatic single-, multiple-, or fused-ring; and each A is the same, and can represent a direct bond between the cyclohexane ring and Z, or a carboxamide group (—C(O)—N(H)—). Use of the compounds in combinatorial libraries, methods of making the tripodal compounds, sensor devices for detecting carbohydrate targets, and methods of using the tripodal compounds to detect carbohydrate targets in a sample are also disclosed.Type: ApplicationFiled: October 16, 2007Publication date: February 18, 2010Applicant: UNIVERSITY OF ROCHESTERInventors: Benjamin L. Miller, Prakash B. Palde, Peter C. Gareiss
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Publication number: 20100034827Abstract: The invention is related to compounds of Formula (I), (II), or (III); or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 24, 2007Publication date: February 11, 2010Applicants: GILEAD SCIENCES, INC., KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Hongyan Guo, Choung U. Kim, Thorsten A. Kirschberg, Iii Young Lee, Michael L. Mitchell, Jong Chan Son, Lianhong Xu
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Publication number: 20100016344Abstract: Macrocyclic benzofused pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions and disorders using such compounds and compositions are described herein.Type: ApplicationFiled: July 10, 2009Publication date: January 21, 2010Applicant: ABBOTT LABORATORIESInventors: Brian D. Wakefield, Robert J. Altenbach, Lawrence A. Black, Marlon D. Cowart, Irene Drizin, Huaqing Liu
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Patent number: 7629347Abstract: The present invention relates to uses of the compounds of Formula I as well as pharmaceutically acceptable salts and stereoisomers thereof in methods to treat a variety of tumors in mammals involving abnormal tyrosine kinase signaling, the compounds represented as: wherein R1 and R2 are independently selected from the group consisting of H; alkyl; alkenyl; alkynyl; halogen; aryl; heteroaryl containing N, O, or S; the aryl and heteroaryl may be further substituted with halogen, an alkyl, alkenyl, and alkynyl; NZ1Z2, wherein Z1 and Z2 are independently selected from the group consisting of H and alkyl; and (CO)Y wherein Y is selected from the group consisting of H, alkyl, alkenyl, alkynyl, aryl, heteroaryl containing N, O, or S, and the aryl and heteroaryl may be further substituted with halogen, alkyl, alkenyl, and alkynyl; with the proviso that when R1 is hydrogen, R2 is a group other than hydrogen.Type: GrantFiled: October 9, 2003Date of Patent: December 8, 2009Assignee: Critical Outcome Technologies, Inc.Inventors: Wayne R. Danter, George Ma, Natalie Lazarowych, Stephen Houldsworth, Martyn Brown, Ghenadie Rusu, Jianhua Zhong
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Publication number: 20090291974Abstract: Stable acid addition salts of bosentan useful for the purification of bosentan base; the salts are in solid state and the starting acid has a pKa lower than 3.Type: ApplicationFiled: May 26, 2009Publication date: November 26, 2009Inventor: Jie ZHU
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Publication number: 20090281125Abstract: The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment of various diseases and conditions such as asthma.Type: ApplicationFiled: July 9, 2009Publication date: November 12, 2009Inventors: Tanisha D. Blake, Bruce C. Hamper, Wei Huang, James R. Kiefer, JR., Joseph B. Moon, Bradley E. Neal, Kirk L. Olson, Matthew J. Pelc, Barbara A. Schweitzer, Atli Thorarensen, John I. Trujillo, Steven R. Turner
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Publication number: 20090263472Abstract: Endothelin receptor antagonist nitroderivatives of general formula (I): having an improved pharmacological activity compared with their parent compounds. They can be employed for treating or preventing endothelial-related disorders, renal, pulmonary, cardiac and vascular diseases, and inflammatory processes.Type: ApplicationFiled: May 23, 2007Publication date: October 22, 2009Applicant: NICOX S.A.Inventors: Nicoletta Almirante, Stefano Biondi, Ennio Ongini
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Publication number: 20090264447Abstract: The present invention relates to the use of pyrimidine compounds of formula I wherein the variables have the meanings stated in the claims and in the description, for combating pathogenic fungi, new pyrimidine compounds of formula (I), and fungicidal and pharmaceutical agents containing the same.Type: ApplicationFiled: August 1, 2007Publication date: October 22, 2009Applicant: BASF SEInventors: Jochen Dietz, Bernd Müller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou
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Patent number: 7601729Abstract: Compounds of Formula (I): wherein: A represents bond, C1-6alkyl or CH?CH—C1-4alkyl; B represents bond, O, S, SO, SO2, CO, CR7R8, CO2R14, CONR14R15, N(COR14)(COR15), N(SO2R14)(COR15) or NR14R15; D represents bond, or C1-6alkyl; E represents substituted aryl or substituted or unsubstituted heteroaryl; Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, SO, SO2, CO, CNR5, CNOR5, CNNR5R6, NR11 or CR7R8; Y represents CR5OR11, CR5SR11, NOR5, CR5NR6R11, SO, SO2, CO, CNR5, CNOR5 or CS; R1 and R1? each independently represents H, C1-6alkyl or C1-4alkylaryl; R2 represents CO2R12, CH2OR12 or CONR12R13, CONR12OR13, NR12COR13, SR12, PO(OH)2, PONHR12 or SONHR12; R3 represents H, C1-6alkyl or C1-4alkylaryl; R4 represents optionally substituted aryl or heteroaryl; Z represents a bond, CH2, O, S, SO, SO2, NR5, OCR5R6, CR9R10O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R5 and R6 each independently represent H, C1-6 alkyl or C1-4 alkylaryl;Type: GrantFiled: September 10, 2004Date of Patent: October 13, 2009Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Publication number: 20090233918Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: March 14, 2007Publication date: September 17, 2009Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Kenji Fukunaga, Toshiyuki Kohara, Kazutoshi Watanabe, Yoshihiro Usui, Fumiaki Uehara, Satoshi Yokoshima, Daiki Sakai, Shin-ichi Kusaka, Kazuki Nakayama
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Patent number: 7585866Abstract: The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:Type: GrantFiled: July 31, 2003Date of Patent: September 8, 2009Assignee: Critical Outcome Technologies, Inc.Inventors: Wayne R. Danter, Martyn Brown, George Ma, Ghenadie Rusu, Jianhua Zhong, Natalie Lazarowych, Stephen Houldsworth
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Patent number: 7582641Abstract: The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.Type: GrantFiled: November 11, 2004Date of Patent: September 1, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven M. Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud LeTiran, Joseph Drumm
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Patent number: 7579349Abstract: A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man.Type: GrantFiled: October 11, 2004Date of Patent: August 25, 2009Assignee: AstraZeneca ABInventors: Thorsten Nowak, Andrew Peter Thomas
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Patent number: 7572793Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.Type: GrantFiled: September 20, 2002Date of Patent: August 11, 2009Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi-AventisInventors: Fumiaki Uehara, Keiichi Aritomo, Aya Shoda, Shinsuke Hiki, Masahiro Okuyama, Yoshihiro Usui, Mitsuru Ooizumi, Kazutoshi Watanabe
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Publication number: 20090197901Abstract: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHCOR?, NHSO2R?, CN, halogen, ?O, C(?O)H, C(?O)R?, CO2H, CO2R?, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R? groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ?O, C(?O)H, C(?O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.Type: ApplicationFiled: January 7, 2009Publication date: August 6, 2009Applicant: PHARMA MAR, S.A.Inventors: Modesto Remuinan, Juan Jose Gonzalez, Carlos del Pozo, Andres Francesh, Carmen Cuevas, Simon Munt, Ignacio Manzanares, Regan James Anderson, Jonathan Charles Morris
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Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
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Publication number: 20090160326Abstract: An organic EL element having one or a plurality of organic layers including a light emitting layer between a pair of electrodes is arranged such that at least one layer of the above-mentioned organic layers contains a compound as expressed by the following general formula (1) independently or as a mixture. (where, R1-R7 are selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group, and an aryloxy group, and they may be the same groups or the groups different from one another, and A1-A3 are selected from the group consisting of a phenyl group which is either substituted or unsubstituted and a 5 or 6 member heterocyclic ring group which is either substituted or unsubstituted, and they may be the same groups or the groups different from one another.Type: ApplicationFiled: December 22, 2008Publication date: June 25, 2009Applicant: Yamagata Promotional Organization for Industrial TechnologyInventors: Atsushi ODA, Masato KIMURA
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Publication number: 20090160315Abstract: An organic EL element having one or a plurality of organic layers including a light emitting layer between a pair of electrodes is arranged such that at least one layer of the above-mentioned organic layers contains a compound as expressed by the following general formula (1) independently or as a mixture. (where R1-R9 are selected from the group consisting of hydrogen, an alkyl group, a cycloalkyl group, an alkoxy group, a cycloalkoxy group, and an aryloxy group, and they may be the same groups or the groups different from one another, and A1-A4 are selected from the group consisting of a phenyl group which is either substituted or unsubstituted and a 5 or 6 member heterocyclic ring group which is either substituted or unsubstituted, and they may be the same groups or the groups different from one another.Type: ApplicationFiled: December 22, 2008Publication date: June 25, 2009Applicant: Yamagata Promotional Organization for Industrial TechnologyInventors: Atsushi ODA, Takayuki HORIUCHI, Masato KIMURA, Junichi TANAKA
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Publication number: 20090156811Abstract: A process for the preparation of 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-[2,2?]bipyrimidinyl-4-yl]-benzenesulfonamide, bosentan, comprising the reaction of a compound of formula (II) or a salt thereof, wherein Z is an optionally protected hydroxy group, with a compound of formula (III), in the presence of a base; and, if necessary, the removal of the hydroxy-protecting group, and/or, if desired, the conversion of a compound of formula (I) to a salt thereof, or vice versa; and novel intermediates useful for its synthesis.Type: ApplicationFiled: December 11, 2008Publication date: June 18, 2009Applicant: Dipharma Francis S.r.l.Inventors: Maurizio TADDEI, Diletta Naldini, Pietro Allegrini, Gabriele Razzetti, Simone Mantegazza
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Patent number: 7528157Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: December 22, 2006Date of Patent: May 5, 2009Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Publication number: 20090111795Abstract: A compound of formula (I): M-L-M, wherein L is a linker and each M is independently a group of formula (II): is useful in therapy, e.g. of respiratory diseases.Type: ApplicationFiled: February 3, 2006Publication date: April 30, 2009Inventors: Harry Finch, Christine Edwards, Nicholas Charles Ray, Anne O'Connor, Mary F. Fitzgerald
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Publication number: 20090105268Abstract: A compound of formula M-L-M (I) wherein L is a linker and each M is independently a group of formula (II) is useful in therapy, e.g. of respiratory diseases.Type: ApplicationFiled: June 26, 2006Publication date: April 23, 2009Inventors: Harry Finch, Christine Edwards, Nicholas Charles Ray, Mary Frances Fitzgerald
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Publication number: 20090099194Abstract: The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infections. The compounds provided interfere with the binding of SDF 1 to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis, or for reducing entry of HIV in to a cell while not reducing the capacity of the stem cells to proliferate. The compounds may be useful for long term treatment regimes.Type: ApplicationFiled: July 11, 2007Publication date: April 16, 2009Inventors: Dennis C. Liotta, James P. Snyder, Weiqiang Zhan
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Publication number: 20090088490Abstract: A simultaneous two-photon absorption three-dimensional recording material includes at least one kind of dye having at least one polymerizable group.Type: ApplicationFiled: September 26, 2008Publication date: April 2, 2009Applicant: FUJIFILM CORPORATIONInventors: Masaharu AKIBA, Hiroo TAKIZAWA
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Publication number: 20090082379Abstract: Compounds of formula (I): wherein Ra, Rb, R, X1 and X2 are as defined in the disclosure, pharmaceutical compositions comprising said compounds, processes for making and methods of using the same are provided.Type: ApplicationFiled: July 15, 2008Publication date: March 26, 2009Applicant: AVENTIS PHARMA S.A.Inventors: Frank HALLEY, Youssef El-Ahmad, Victor Certal, Corinne Venot, Anne Dagallier, Hartmut Strobel, Kurt Ritter, Sven Ruf
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Patent number: 7507754Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: August 14, 2007Date of Patent: March 24, 2009Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Publication number: 20090075188Abstract: This invention provides an azo compound represented by Formula (I), Formula (II), or Formula (III): wherein R1 and R2 each independently represent a hydrogen atom or a substituent; D1 and D2 each independently represent a coupler residue; Z1 and Z2 each independently represent —C(R3)? or —N?; and R3 represents a hydrogen atom or a substituent.Type: ApplicationFiled: September 12, 2008Publication date: March 19, 2009Applicant: FUJIFILM CORPORATIONInventors: Yuki MIZUKAWA, Hideki Takakuwa, Toru Fujimori
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Publication number: 20090074825Abstract: The present invention includes methods, articles, compositions and colorant dyes and pigments that include biocidal N-halamine dye composition having two or more heterocyclic ring structures attached to one or more N-halamine groups, wherein one or more halogens associate with the one or more one or more N-halamine groups to affect biocidal activity.Type: ApplicationFiled: September 19, 2008Publication date: March 19, 2009Applicant: Board of Regents, The University of Texas SystemInventors: Yuyu Sun, Jie Luo
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Patent number: 7504502Abstract: Compounds of the formula wherein, provided that at least one of R1, R2, and R3 is not hydrogen, R1, R2, and R3 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, and wherein R1 and R2 can also be alkoxy, aryloxy, arylalkyloxy, alkylaryloxy, polyalkyleneoxy, polyaryleneoxy, polyarylalkyleneoxy, polyalkylaryleneoxy, silyl, siloxane, polysilylene, polysiloxane, or wherein X is a direct bond, oxygen, sulfur, —NR40— wherein R40 is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl, or —CR50R60— wherein R50 and R60 each, independently of the other, is hydrogen, alkyl, aryl, arylalkyl, or alkylaryl.Type: GrantFiled: January 22, 2008Date of Patent: March 17, 2009Assignees: Xerox Corporation, University of MontrealInventors: Danielle C Boils-Boissier, Marcel P Breton, Jule W Thomas, Jr., Donald R Titterington, Jeffrey H Banning, H Bruce Goodbrand, James D Wuest, Marie-Eve Perron, Hugues Duval
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Publication number: 20090069327Abstract: 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 abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Bmx, b-RAF, c-RAF, c-SRC, KDR, CSK, FGFR3, JAK2, Lck, Met, PKC?, SAPK2?, Tie2, TrkB and P70S6K kinases.Type: ApplicationFiled: February 6, 2007Publication date: March 12, 2009Applicant: IRM LLCInventors: Qiang Ding, Pingda Ren, Qiong Zhang, Xia Wang, Taebo Sim, Pamela A. Albaugh, Nathanael S. Gray
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Publication number: 20090068140Abstract: 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: ApplicationFiled: February 13, 2008Publication date: March 12, 2009Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20090069351Abstract: The present application describes deuterium-enriched bosentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7501415Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.Type: GrantFiled: December 20, 2005Date of Patent: March 10, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alexander Aronov, Michael Hale, Francois Maltais, Gabriel Martinez-Botella, Judith Straub, Qing Tang
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Publication number: 20090054466Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.Type: ApplicationFiled: July 28, 2008Publication date: February 26, 2009Inventors: Romyr Dominique, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Agnieszka Kowalczyk, Qi Qiao, Achyutharao Sidduri
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Publication number: 20090029994Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 29, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Publication number: 20090023738Abstract: The present invention relates to diaminopyrimidines of the general formula I, process for their preparation, and the use thereof for the manufacture of pharmaceutical compositions for the treatment of disorders and indications connected with the EP2 receptor.Type: ApplicationFiled: June 19, 2008Publication date: January 22, 2009Inventors: Nico Braeuer, Bernd Buchmann, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
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Publication number: 20090023729Abstract: The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.Type: ApplicationFiled: July 28, 2008Publication date: January 22, 2009Applicant: Mitsubishi Tanabe Pharma CorporationInventors: Yoshinori Nakamura, Norimitsu Hayashi, Takanori Higashijima, Hitoshi Kubota, Kozo Oka
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Publication number: 20090005334Abstract: A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and uses of the compound, particularly in antisense therapy.Type: ApplicationFiled: February 19, 2008Publication date: January 1, 2009Applicant: Bio-Rad Laboratories Inc.Inventor: David Segev
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Publication number: 20090005403Abstract: The invention relates to compounds of the formula (I), in which A, R1, R2, R3 and R4 are as defined in the description, to processes and intermediates for their preparation and to their use for controlling pests.Type: ApplicationFiled: December 24, 2005Publication date: January 1, 2009Applicant: Bayer Cropscience AktiengesellschaftInventors: Thomas Bretschneider, Olga Malsam, Mark Wilhelm Drewes, Christian Arnold
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Publication number: 20090005394Abstract: This invention relates to novel endothelin receptor antagonists, derivatives, acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by compounds that block the endothelin signaling pathway that leads to vasoconstriction and in particular those diseases or conditions beneficially treated by endothelin receptor antagonists.Type: ApplicationFiled: January 11, 2008Publication date: January 1, 2009Inventor: Scott L. Harbeson
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Patent number: 7470686Abstract: The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.Type: GrantFiled: July 18, 2007Date of Patent: December 30, 2008Assignee: Laboratoires Serono SAInventors: Serge Halazy, Dennis Church, Monstserrat Camps, Pascale Gaillard, Jean-Pierre Gotteland
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Publication number: 20080318987Abstract: Methods and compositions for modulating bone formation and mineralization are described.Type: ApplicationFiled: February 15, 2008Publication date: December 25, 2008Inventor: Laurie H. GLIMCHER
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Publication number: 20080293937Abstract: The new fluorocarbon-functionalized and/or heterocycle-modified polythiophenes, in particular, ?,?-diperfluorohexylsexithiophene DFH-6T can be straightforwardly prepared in high yield and purity. Introduction of such modifications to a thiophene core affords enhanced thermal stability and volatility, and increased electron affinity versus the unmodified compositions of the prior art. Evaporated films behave as n-type semiconductors, and can be used to fabricate thin film transistors with FET mobilities ˜0.01 cm2/Vs—some of the highest reported to date for n-type organic semiconductors.Type: ApplicationFiled: May 1, 2008Publication date: November 27, 2008Inventors: Tobin J. Marks, Antonio Facchetti