Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
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Publication number: 20120010203Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: September 23, 2011Publication date: January 12, 2012Applicant: SANOFI-AVENTISInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN, Bodo SCHEIPER
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Publication number: 20120010191Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: May 6, 2011Publication date: January 12, 2012Applicants: GENENTECH, INC., GILEAD CONNECTICUT, INC.Inventors: Antonio J.M. BARBOSA, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
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Publication number: 20120004234Abstract: This invention provides for certain phthalazine-containing compounds of the formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof, wherein G is an optionally substituted N—N containing heteroaryl group and the variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: February 4, 2010Publication date: January 5, 2012Applicant: Schering CorporationInventors: Jason L. Davis, Michael John Mayer, Hubert B. Josien
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Publication number: 20120004237Abstract: Choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: MEDIGENE AGInventor: Richard Ian MATTHEWS
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Publication number: 20120004233Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 26, 2010Publication date: January 5, 2012Applicant: AMIRA PHARMACEUTICALS, INCInventors: Brian Andrew Stearns, Ryan Clark
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Publication number: 20110312966Abstract: The present invention relates to new dithiinopyridazinone derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinone derivatives.Type: ApplicationFiled: April 14, 2011Publication date: December 22, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Jürgen BENTING, Ulrike WACHENDORFF-NEUMANN, Philippe Rinolfi
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Patent number: 8076331Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.Type: GrantFiled: July 29, 2010Date of Patent: December 13, 2011Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Lars J. S. Knutsen, Catherine P. Prouty, Babu G. Sundar, Kevin J. Wells-Knecht
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Publication number: 20110301167Abstract: The present invention is directed to pyrazolo[4,3-c]cinnolin-3-one 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: February 12, 2010Publication date: December 8, 2011Inventors: Douglas C. Beshore, Scott D. Kuduk
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Patent number: 8063047Abstract: The invention relates to novel chemical compounds of Formula I compositions and methods of using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: GrantFiled: May 12, 2008Date of Patent: November 22, 2011Assignees: Centre National de la Recherche Scientifique (CNRS), Northwestern University, Universite de StrasbourgInventors: Martin Watterson, Linda Van El Dik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Veleniza, Wenhui Hu, Magdaena Zasadzki
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Publication number: 20110281877Abstract: The present invention relates to new dithiinopyridazinedione derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinedione derivatives.Type: ApplicationFiled: April 14, 2011Publication date: November 17, 2011Applicant: Bayer CropScience AGInventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Jürgen Benting
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Patent number: 8058429Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.Type: GrantFiled: May 5, 2010Date of Patent: November 15, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
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Patent number: 8048541Abstract: An electroluminescence device has an anode, a cathode and an emitting layer located between the anode and the cathode. The emitting layer contains a compound selected from a group consisting of neutral red and its derivatives.Type: GrantFiled: December 17, 2008Date of Patent: November 1, 2011Assignee: City University of Hong KongInventors: Shuit-Tong Lee, Chun Sing Lee, Pengfei Wang, Zhiyuan Xie
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Publication number: 20110264026Abstract: The invention relates generally to optical agents, including Type 1 phototherapeutic agents, for biomedical applications, such as phototherapy. Provided are fused ring azo and diaza compounds comprising a plurality of fused rings including a first ring having an intra-ring azo or intra-ring diaza group capable of activation upon exposure to electromagnetic radiation in visible and/or infrared regions of the electromagnetic spectrum. Optical agents of the invention enable a versatile phototherapy platform for treatment of a range of pathological conditions, including the treatment of cancers, stenosis and inflammation. The invention further provides preparations and formulations comprising the fused ring azo and diaza compounds and methods of making and using the fused ring azo and diaza compounds as optical agents in in vivo or ex vivo biomedical procedures.Type: ApplicationFiled: November 23, 2009Publication date: October 27, 2011Inventor: Raghavan Rajagopalan
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Publication number: 20110237581Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: March 31, 2011Publication date: September 29, 2011Inventors: Bing Wang, Daniel Chu
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Publication number: 20110224214Abstract: Disclosed is a novel process for preparing crystalline Form II of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide.Type: ApplicationFiled: February 15, 2011Publication date: September 15, 2011Applicant: SANOFI-AVENTIS U.S. LLCInventor: William L. ROCCO
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Patent number: 8012976Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: GrantFiled: July 27, 2009Date of Patent: September 6, 2011Assignee: BioMarin Pharmaceutical Inc.Inventors: Bing Wang, Daniel Chu
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Publication number: 20110195958Abstract: Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.Type: ApplicationFiled: October 9, 2009Publication date: August 11, 2011Applicant: US Dept. of Health and Human ServicesInventors: Craig J. Thomas, Douglas S. Auld, James Inglese, Amanda P. Skoumbourdis, Jian-Kang Jiang, Matthew B. Boxer
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Publication number: 20110196153Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.Type: ApplicationFiled: February 8, 2011Publication date: August 11, 2011Inventors: Bing Wang, Daniel Chu, Yongbo Liu, Quan Jiang, Lei Lu
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Publication number: 20110190266Abstract: Provided herein are compounds having the structure set forth in Formula (I): wherein the variables Y, Z, A, B, R1, R2, R3, R1?, R2?, R3?, R4 and R5 are as defined herein and methods of their synthesis. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: February 4, 2011Publication date: August 4, 2011Inventors: Daniel Chu, Bing Wang
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Publication number: 20110183986Abstract: Polycyclic aryl and 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 catalytic activity are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: July 28, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
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Publication number: 20110172235Abstract: This invention relates to novel substituted triazolophthalazines and pharmaceutically acceptable salts thereof. This 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 administering selective ?5 receptor partial or full inverse agonists.Type: ApplicationFiled: August 13, 2010Publication date: July 14, 2011Applicant: CoNCERT Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Publication number: 20110142796Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: ApplicationFiled: December 18, 2008Publication date: June 16, 2011Applicant: Amgen IncInventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. Mcgee, Rajiv Sharma, Xiaodong Wang, Dustin L. Mcminn, Jeffrey T. Mihalic, Jeffrey Deignan
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Patent number: 7943615Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-4 enzyme is involved.Type: GrantFiled: December 8, 2006Date of Patent: May 17, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
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Publication number: 20110105511Abstract: 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: July 2, 2009Publication date: May 5, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rajinder Singh
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Publication number: 20110105512Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase AxI. Methods of using the compounds in treating diseases or conditions associated with AxI activity are also disclosed.Type: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventor: Rajinder Singh
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Publication number: 20110098274Abstract: 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: January 7, 2011Publication date: April 28, 2011Applicant: 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: 7932253Abstract: N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-4-(6,9-difluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-benzamide is a CD80 antagonist, useful in the treatment of diseases which benefit from immuno-inhibition.Type: GrantFiled: August 9, 2004Date of Patent: April 26, 2011Assignee: MediGene AGInventor: Ian Richard Matthews
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Publication number: 20110065712Abstract: The invention provides compounds that inhibit CK2 and/or Pim kinases and compositions containing such compounds. These tricyclic compounds and compositions containing them are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, pathogenic infections, and certain immunological disorders.Type: ApplicationFiled: September 16, 2010Publication date: March 17, 2011Applicant: CYLENE PHARMACEUTICALS , INC.Inventors: Mustapha HADDACH, Fabrice Pierre
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Patent number: 7888357Abstract: A novel class of pyridazine compositions and related methods of use.Type: GrantFiled: October 26, 2005Date of Patent: February 15, 2011Assignees: Northwestern University, Universite de Strasbourg, Centre National de la Recherche ScientifiqueInventors: Daniel Martin Watterson, Anastasia Velentza, Magdalena Zasadzki, Jacques Haiech, Jean-Jacques Bourguignon, Anu R. Sawkar, Thomas J. Lukas, Salida Mirzoeva, Linda J. Van Eldik, Marcel Hibert
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Publication number: 20110034451Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN, Bodo SCHEIPER
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Patent number: 7875712Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: September 23, 2008Date of Patent: January 25, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Publication number: 20110003824Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: September 16, 2010Publication date: January 6, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORDTEDInventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 7858598Abstract: Provided herein are compounds or hypochlorous acid probes which can be used as reagents for measuring, detecting and/or screening, directly or indirectly, hypochlorous acid or hypochlorite. Provided also herein are methods that can be used to measure, directly or indirectly, the amount of hypochlorous acid or hypochlorite in chemical samples and biological samples such as cells and tissues in living organisms. Specifically, the methods include the steps of contacting the hypochlorous acid probes disclosed herein with the samples to form one or more fluorescent compounds, and measuring fluorescence properties of the fluorescent compounds. Provided also herein are high-throughput screening fluorescent methods for detecting or screening hypochlorous acid or compounds that can increase or decrease, directly or indirectly, the level of hypochlorous acid or hypochlorite in chemical and biological samples.Type: GrantFiled: February 21, 2008Date of Patent: December 28, 2010Assignee: Morningside Ventures Limited & Versitech LimitedInventors: Dan Yang, Zhen-Ning Sun, Yan Chen, Fengqin Liu
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Patent number: 7855206Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 9, 2007Date of Patent: December 21, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jason M. Cox, Hong Dong
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Publication number: 20100317665Abstract: A novel class of pyridazine compositions and related methods of use.Type: ApplicationFiled: July 7, 2010Publication date: December 16, 2010Inventors: D.M. Watterson, Anastasia Velentza, Magdalena Zasadzki, Jacques Halech, Jean-Jacques Bourguignon, Anu R. Sawkar, Thomas J. Lukas, Salida Mirzoeva, Linda J. Van Eldik, Marcel Hibert
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Patent number: 7851472Abstract: The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.Type: GrantFiled: August 31, 2005Date of Patent: December 14, 2010Assignee: NYCOMED GmbHInventors: Beate Schmidt, Steffen Weinbrenner, Dieter Flockerzi, Raimund Kuelzer, Hermann Tenor, Hans-Peter Kley
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Patent number: 7842758Abstract: The invention concerns compounds, oligomers, and polymers that contain: (I), (II), (III), or (IV) groups; where “-” indicates points of attachment.Type: GrantFiled: January 10, 2007Date of Patent: November 30, 2010Assignee: The Trustees Of The University Of PennsylvaniaInventors: Michael J. Therien, Kimihiro Susumu
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Patent number: 7829561Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: GrantFiled: July 1, 2008Date of Patent: November 9, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Guy Brenchley
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Publication number: 20100280007Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.Type: ApplicationFiled: June 15, 2010Publication date: November 4, 2010Applicant: CEPHALON, INC.Inventors: Edward R. Bacon, Thomas R. Bailey, Nadine C. Becknell, Sankar Chatterjee, Derek Dunn, Greg A. Hostetler, Robert L. Hudkins, Kurt A. Josef, Lars J.S. Knutsen, Ming Tao, Allison L. Zulli
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Publication number: 20100278739Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.Type: ApplicationFiled: July 13, 2010Publication date: November 4, 2010Inventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
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Patent number: 7816357Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I. including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R4, R5, m and n are described herein.Type: GrantFiled: December 17, 2004Date of Patent: October 19, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Guixue Yu, William R. Ewing, Amarendra B. Mikkilineni, Annapurna Pendri, Bruce A. Ellsworth, Philip M. Sher, Samuel Gerritz, Chongqing Sun, Natesan Murugesan, Ximao Wu
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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7750008Abstract: The present invention provides compounds which inhibit poly(ADP-ribose) polymerase (“PARP”), compositions containing these compounds and methods for using these PARP inhibitors to treat, prevent and/or ameliorate the effects of the conditions described herein.Type: GrantFiled: August 13, 2009Date of Patent: July 6, 2010Assignee: Eisai Inc.Inventors: Vincent Kalish, Jie Zhang, Weizheng Xu, Jia-He Li, Amy D. Xing, Qun Liu
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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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Publication number: 20100148662Abstract: An electroluminescence device has an anode, a cathode and an emitting layer located between the anode and the cathode. The emitting layer contains a compound selected from a group consisting of neutral red and its derivatives.Type: ApplicationFiled: December 17, 2008Publication date: June 17, 2010Applicant: CITY UNIVERSITY OF HONG KONGInventors: Shuit-Tong Lee, Chun Sing Lee, Pengfei Wang, Zhiyuan Xie
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Patent number: 7737272Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.Type: GrantFiled: February 15, 2008Date of Patent: June 15, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
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Publication number: 20100144744Abstract: Novel compounds are provided which are 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors. 1 1-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 1 1-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L are defined herein and Z is selected from the following bicyclic heteroaryl groups: (a), (b), (c), (d).Type: ApplicationFiled: April 16, 2008Publication date: June 10, 2010Inventors: Jun Li, James J. Li, Stephen P. O'Connor, Haixia Wang, Lawrence J. Kennedy, Jeffrey A. Robl, Lawrence G. Hamann
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Patent number: 7732447Abstract: The present invention is directed to fused [d]pyridazin-7-ones. The invention is also directed to methods for making and using the fused [d]pyridazin-7-ones. In particular, the compounds of the present invention may be effective in the treatment of diseases or disease states related to the activity of VEGFR2, MLK1 and CDK5 enzymes, including, for example, angiogenic disorders and neurodegenerative diseases.Type: GrantFiled: June 21, 2007Date of Patent: June 8, 2010Assignee: Cephalon, Inc.Inventors: Nadine C. Becknell, Robert L. Hudkins
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Publication number: 20100137320Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: February 26, 2009Publication date: June 3, 2010Inventors: Xianhai Huang, Anandan Palani, Robert G. Aslanian, Wei Zhou
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Patent number: 7713975Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.Type: GrantFiled: January 12, 2006Date of Patent: May 11, 2010Assignee: Alcon, Inc.Inventors: Mark R. Hellberg, Steven T. Miller, Andrew Rusinko