Plural Nitrogens In The Hetero Ring Patents (Class 540/460)
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Publication number: 20100113440Abstract: Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.Type: ApplicationFiled: February 8, 2008Publication date: May 6, 2010Applicant: Tibotec Pharmaceuticals, Ltd.Inventors: Anna Karin Gertrud Linnea Belfrage, Björn Olof Classon, Karin Charlotta Lindquist, Karl Magnus Nilsson, Pierre Jean-Marie Bernard Raboisson, Åsa Annica Kristina Rosenquist, Bertil Bengt Samuelsson, Horst Jürgen Wähling
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Publication number: 20100113488Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: ApplicationFiled: December 19, 2007Publication date: May 6, 2010Inventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Peter W. Glunz, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata, Luciano Mueller
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Publication number: 20100086482Abstract: The present invention describes a process for preparing new looped dendrimer and dendron compounds by controlling the molar amount of branch cell reagent monomer that is combined with various cores bearing core-XR functionalities (e.g., primary, or secondary amines, thiol, or epoxy functionalities). These looped, macrocyclic structures are more robust to various conditions, with greater resistance to acid/base hydrolysis. Alternatively, the looped, macrocyclic structure may offer new orientations that would qualify it as a better chelation ligand for metals, and other similar uses.Type: ApplicationFiled: December 28, 2007Publication date: April 8, 2010Applicant: Dendritic Nanotechnologies, Inc.Inventors: Donald A. Tomalia, Douglas R. Swanson, Baohua Huang, Veera Reddy Pulgam
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Publication number: 20100063121Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. 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: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
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Publication number: 20100056522Abstract: An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.Type: ApplicationFiled: March 28, 2008Publication date: March 4, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Shinji Yoneda, Koushi Fujisawa, Katsuhiko Watanabe, Junko Fujikawa, Atsushi Shimazaki, Tomoko Kirihara, Hisashi Tajima
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Patent number: 7662812Abstract: This invention relates to novel diazabicyclic aryl derivatives which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: February 13, 2006Date of Patent: February 16, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B Timmermann, Gunnar Olsen, Elsebet Østergaard Nielsen, Tino Dyhring
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Publication number: 20100036116Abstract: The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.Type: ApplicationFiled: August 7, 2009Publication date: February 11, 2010Inventors: Michelangelo Scalone, Helmut Stahr
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Publication number: 20100029731Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: ApplicationFiled: July 16, 2009Publication date: February 4, 2010Applicants: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION, Dana-Farber Cancer Institute, Inc.Inventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Ann E. Youngman
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Publication number: 20100029715Abstract: Provided are crystalline forms of the compound of formula (I), which is a macrocyclic inhibitor of HCV, processes for the preparation thereof, and pharmaceutical compositions comprising these crystalline forms.Type: ApplicationFiled: February 1, 2008Publication date: February 4, 2010Inventors: Sigrid Carl Maria Stokbroekx, Carina Leys, Kelly Ann Swinney, Stijn Wuyts, Andras Horvath
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Publication number: 20100022767Abstract: The synthesis of syringolin A and B and derivatives thereof as well as to pharmaceutical compositions containing the syringolin A or B or derivatives thereof and the use of syringolin A and B and derivatives thereof for prophylaxis and treatment of cancer.Type: ApplicationFiled: July 24, 2009Publication date: January 28, 2010Applicant: MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WISSENSCHAFTEN E.V.Inventors: Markus Kaiser, Jérôme Clerc
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Publication number: 20100022578Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturateType: ApplicationFiled: November 16, 2007Publication date: January 28, 2010Inventors: Pierre Jean-Marie Raboisson, Herman Augustinus De Kock, David Craig Mc Gowan, Wim Van De Vreken, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Publication number: 20100022500Abstract: The present invention relates to novel macrocyclic compounds of the formula wherein R1, R2, R3, U, V, W, X, Y, Z and n are as defined in the specification, the number of ring atoms included in the macrocyclic ring being 14, 15, 16 or 17, in free base form or in acid addition salt form, to their preparation, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: September 25, 2009Publication date: January 28, 2010Inventors: Yves AUBERSON, Claudia Betschart, Ralf Glatthar, Kurt Laumen, Rainer MacHauer, Marina Tintelnot-Blomley, Thomas J. Troxler, Siem Jacob Veenstra
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Publication number: 20100022768Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: August 20, 2009Publication date: January 28, 2010Applicant: AnaSpec IncInventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Patent number: 7652003Abstract: Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, n and X are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are methods of treating a cognitive or neurodegenerative disease comprising administering to a patient I need of such treatment a combination of at least one compound of formula I and at least one compound selected from the group consisting of ?-secretase inhibitors other than those of formula I, HMG-CoA reductase inhibitors, gamma-secretase inhibitors, non-steroidal anti-inflammatory agents, N-methyl-D-aspartate receptor antagonists, cholinesterase inhibitors and anti-amyloid antibodies.Type: GrantFiled: July 26, 2005Date of Patent: January 26, 2010Assignee: Schering-Plough CorporationInventors: Andrew W Stamford, Ying Huang, Guoqing Li, Corey O Strickand, Johannes H. Voigt
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Publication number: 20100016578Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: September 18, 2009Publication date: January 21, 2010Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
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Publication number: 20100009953Abstract: The present invention provides a method for the treatment of ocular or dermal diseases and/or conditions, e.g. an aqueous deficient dry eye state, uveitis or phacoanaphylactic endophthalmitis in an eye, or balanitis, psoriasis, or atopic dermatitis of the skin, said method comprising administering, topically to the eye or the skin, a therapeutically effective amount of a novel cyclosporin A derivative selected from the group consisting of compounds represented by the formula: wherein R1 is S-Alk-R wherein Alk is an alkylene linkage, preferably a methylene or poly methylene linkage, e.g. a C2 to C6 polymethylene linkage, or a polyalkenylene linkage, e.g. a C3 to C6 alkenylenyl linkage, R is R is —N?C(NR3R4)(NR5R6) or NR7[(NR3R4)C?NR5], i.e. guanidines or —N?C(R8)(NR9R10), i.e.Type: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: ALLERGAN, INC.Inventor: Michael E. Garst
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Publication number: 20100010215Abstract: Inverted cucurbituril compounds having at least one pair of hydrogen atoms protruding into an internal molecular cavity thereof.Type: ApplicationFiled: July 24, 2006Publication date: January 14, 2010Applicant: THE UNIVERSITY OF MARYLANDInventors: Lyle David Isaacs, Simin Liu, Kimoon Kim, Sang-Kyu Park, Young Ho Ko, Hyunuk Kim, Youngkook Kim, Narayanan Selvapalam
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Publication number: 20090312300Abstract: Disclosed are cyclosporine derivatives in which the 3-Sarcosine carbon and 5-Valine nitrogen are each substituted by a non-hydrogen substituent, and their use as pharmaceuticals, in particular for the treatment of hepatitis C virus.Type: ApplicationFiled: June 5, 2009Publication date: December 17, 2009Inventors: Keqiang Li, Ahmed Mamai, Michael Robert Peel
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Publication number: 20090312540Abstract: Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target, in particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.Type: ApplicationFiled: May 26, 2009Publication date: December 17, 2009Inventors: Pierre Deslongchamps, Yves Dory, Luc Ouellet, Gerald Villeneuve, Mahesh Ramaseshan, Daniel Fortin, Mark L. Peterson, Hamid R. Hoveyda, Sylvie Beaubien, Eric Marsault, Graeme L. Fraser
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Publication number: 20090312541Abstract: The present invention relates to novel intermediates of formula VII, or an acid addition salt or a solvate thereof, wherein R1 is —(CO)NH2, —CH2NH2 or —CN; R2?R3?H or R2 and R3 together form a cyclic boronate or borate ester; X is a helping group selected from the group consisting of i) a five or six membered heterocyclic aromatic ring and derivatives thereof comprising at least one N-atom being a part of an imine-group, wherein said N-atom forms the point of connection to the cyclohexapeptide ring, and ii) tetrazolyl and derivatives thereof for which a nitrogen atom forms the point of connection to the cyclohexapeptide ring, and a process for the preparation of caspofungin utilizing said intermediates.Type: ApplicationFiled: June 13, 2008Publication date: December 17, 2009Applicant: ALPHARMA APSInventors: Audun Heggelund, Ole Heine Kvernenes, Vidar Bjornstad
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Publication number: 20090304629Abstract: The present invention relates to compounds of Formula I, II or III, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: wherein W is a substituted or unsubstituted heterocyclic ring system. The compounds inhibit serine protease activity, particularly the activity of hepatitis c virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis c virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: January 9, 2009Publication date: December 10, 2009Inventors: Zhenwei Miao, Ying Sun, Suanne Nakajima, Datong Tang, Frank Wu, Guoyou Xu, Yat S. Or, Zhe Wang
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Publication number: 20090306033Abstract: Compounds are disclosed of general formula (I): wherein A, B and R1 are as defined in the description, and their use as pharmaceuticals.Type: ApplicationFiled: June 5, 2009Publication date: December 10, 2009Inventors: Keqiang Li, Ahmed Mamai, Michael Robert Peel
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Publication number: 20090297472Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: May 28, 2009Publication date: December 3, 2009Inventors: Alan Xiangdong Wang, Paul Michael Scola
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Publication number: 20090286843Abstract: The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: October 20, 2008Publication date: November 19, 2009Inventors: LAWRENCE M. BLATT, STEVEN W. ANDREWS, KEVIN R. CONDROSKI, GEORGE A. DOHERTY, YUTONG JIANG, JOHN A. JOSEY, APRIL L. KENNEDY, MACHENDER R. MADDURU, PETER J. STENGEL, STEVEN M. WENGLOWSKY, BENJAMIN T. WOODARD, LAURA WOODARD
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Publication number: 20090281139Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.Type: ApplicationFiled: July 23, 2009Publication date: November 12, 2009Inventors: Eldon Scott Priestley, Daniel L. Cheney, Nicolas Ronald Wurtz, Peter W. Glunz
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Publication number: 20090281140Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; R4 is aryl or Het; n is 3, 4, 5, or 6; R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het; R6 is C1-6alkoxy, or dimethylamino; R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl optionally substituted with one, two or three substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitroType: ApplicationFiled: July 28, 2006Publication date: November 12, 2009Applicant: Medivir ABInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux, Karl Magnus Nilsson, Bengt Bertil Samuelson, Åsa Annica Kristina Rosenquist, Vladimir Ivanov, Michael Pelcman, Anna Karin Gertrud Linnea Belfrage, Per-Ola Mikael Johansson, Sandrine Marie Helene Vendeville
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Publication number: 20090281141Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, and stereoisomers thereof, wherein X is N, CH and where X bears a double bond it is C; R1 is —OR1, —NH—SO2R6; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; R4 is isoquinolinyl optionally substituted with one, two or three substituents each independently selected from C1-6alkyl, C1-6alkoxy, hydroxy, halo, polyhaloC1-6alkyl, polyhaloC1-6alkoxy, amino, mono- or diC1-6alkylamino, mono- or diC1-6alkylaminocarbonyl, C1-6alkylcarbonyl-amino, aryl, and Het; n is 3, 4, 5, or 6; each dashed line (represented by - - - - - ) represents an optional double bond; R5 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R6 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; each aType: ApplicationFiled: July 28, 2006Publication date: November 12, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Abdellah Tahri, Dominique Louis nestor Ghislain Surleraux, Wim Van De Vreken, Ismet Dorange, Yvan Simonnet, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Hans Kristian Wallberg
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Patent number: 7611888Abstract: The present disclosure provides a rotaxane compound that can be used to separate molecules within a linkage layer formed on a solid substrate of a biochip by a predetermined distance. The compound is represented by Formula 1, in which a compound of Formula 3 vertically passes through a cavity of cucurbituril or its derivative of Formula 2. It further provides gene chips, protein chips and sensors for biomaterial assays which use the rotaxane molecules to allow biomaterials to be immobilized on a linkage layer such that they are regularly spaced apart from each other by a predetermined distance.Type: GrantFiled: July 5, 2004Date of Patent: November 3, 2009Assignee: Postech FoundationInventors: Kimoon Kim, Jin Koo Kang, Woo Seong Jeon, Miran Noh, Dongwoo Kim, Kangkyun Baek
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Publication number: 20090269305Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: April 14, 2009Publication date: October 29, 2009Applicant: InterMune, Inc.Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
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Publication number: 20090247512Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 taken together with the nitrogen atom to which they are attached form a bicyclic ring system selected from wherein said ring system may optionally be substituted with 1-3 substituents; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each of which may be optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturaType: ApplicationFiled: January 16, 2008Publication date: October 1, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Carl Erik Daniel Jonsson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Susana Ayesa Alvarez, Bjorn Olof Classon, Hans Kristian Wallberg
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Patent number: 7592331Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.Type: GrantFiled: December 21, 2006Date of Patent: September 22, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Eldon Scott Priestley, Daniel L. Cheney, Nicholas Ronald Wurtz, Peter W. Glunz
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Publication number: 20090227650Abstract: Novel crystalline forms of lestaurtinib are described, including six co-crystal forms, nineteen solvate forms, three anhydrate forms and one hemihydrate form. Methods of their preparation and use are also described.Type: ApplicationFiled: January 16, 2009Publication date: September 10, 2009Applicant: Cephalon, Inc.Inventors: Stephen Bierlmaier, Laurent Courvoisier, Raymond Scott Field, R.Curtis Haltiwanger, Martin J. Jacobs, Robert E. McKean, Mehran Yazdanian
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Publication number: 20090203760Abstract: The present invention relates to novel cyclic or constrained acyclic compounds which modulate the activity of G protein-coupled receptors and are useful in the treatment of conditions mediated by G protein-coupled receptors, for example, inflammatory conditions.Type: ApplicationFiled: August 19, 2008Publication date: August 13, 2009Applicant: THE UNIVERSITY OF QUEENSLANDInventors: David FAIRLIE, Stephen Maxwell Taylor, Angela Monique Finch, Allan Wong
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Publication number: 20090202480Abstract: Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.Type: ApplicationFiled: February 3, 2009Publication date: August 13, 2009Applicant: Idenix Pharmaceuticals, Inc.Inventors: Christophe Claude Parsy, Francois-Rene Alexandre, Dominique Surleraux, Michel Derock, Frederic Leroy
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Publication number: 20090191153Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: December 3, 2008Publication date: July 30, 2009Inventors: Ying Sun, Deqiang Niu, Guoyou Xu, Yat Sun Or, Zhe Wang
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Patent number: 7566719Abstract: The present invention relates to compounds of Formula I or II, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: GrantFiled: March 6, 2008Date of Patent: July 28, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Suanne Nakajima, Zhenwei Miao, Ying Sun, Datong Tang, Guoyou Xu, Brian Porter, Yat Sun Or, Zhe Wang
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Publication number: 20090186869Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: June 26, 2008Publication date: July 23, 2009Applicant: Gilead Sciences, Inc.Inventors: Jeromy J. Cottell, John O. Link, Scott D. Schroeder, James Taylor, Winston C. Tse, Randall W. Vivian, Zheng-Yu Yang
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Publication number: 20090170218Abstract: Methods and reagents are disclosed for determining the presence and/or amount of cyclosporin A in a medium suspected of containing cyclosporin A. In the method a combination is provided in a medium. The combination comprises (i) the sample, (ii) a first member of a signal producing system (sps) associated with a first support wherein the first sps member is capable of activating a second member of the sps and wherein the first support is associated with a first member of a specific binding pair, and (iii) the second sps member associated with a second support wherein the second sps member is activatable by the first sps member. The second support comprises either (I) cyclosporin C or cyclosporin A and the combination further comprises a conjugate of an antibody for cyclosporin A and a second member of the specific binding pair or (II) antibody for cyclosporin A and the combination further comprises a conjugate of cyclosporin A and a second member of the specific binding pair.Type: ApplicationFiled: January 2, 2008Publication date: July 2, 2009Applicant: DADE BEHRING INC.Inventors: Yi Feng Zheng, Deb K. Vickery, Susan C. Swann
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Publication number: 20090163706Abstract: The present invention relates to a new process for the preparation of macrocyclic HCV protease inhibitor compounds of the formula wherein R1 is an amino protecting group and X is halogen by way of a ring closing metathesis approach.Type: ApplicationFiled: December 19, 2008Publication date: June 25, 2009Inventors: Stefan Hildbrand, Kurt Puentener, Michelangelo Scalone
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Publication number: 20090156800Abstract: The present invention relates to a process for the preparation of macrocyclic compounds that are useful as hepatitis C virus (HCV) protease inhibitor compounds.Type: ApplicationFiled: December 4, 2008Publication date: June 18, 2009Inventors: Seble Wagaw, Matthew Ravn, Kenneth Engstrom, Guoyou Xu, Zhe Wang, Ying Sun, Deqiang Niu, Yat Sun Or
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Publication number: 20090156627Abstract: The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and ----- have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.Type: ApplicationFiled: October 24, 2008Publication date: June 18, 2009Inventors: Edmond J. Lavoie, Joseph E. Rice, Leroy F. Liu
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Publication number: 20090156799Abstract: Chemically reactive carbocyanine dyes that are intramolecularly crosslinked between the 1-position and 3?-position, their bioconjugates and their uses are described. 1,3?-crosslinked carbocyanines are superior to those of conjugates of spectrally similar 1,1?-crosslinked or non-crosslinked dyes. The invention includes derivative compounds having one or more benzo nitrogens.Type: ApplicationFiled: October 6, 2008Publication date: June 18, 2009Inventors: Zhenjun Diwu, Jianheng Zhang, Yi Tang, Xiang Guobing
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Publication number: 20090149491Abstract: The present invention discloses compounds of formula I, II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. More specifically, the invention relates to oxime compounds containing a carbocyclic P2 unit. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: November 13, 2008Publication date: June 11, 2009Inventors: Dong Liu, Yat Sun Or, Zhe Wang
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Patent number: 7544798Abstract: Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.Type: GrantFiled: February 1, 2007Date of Patent: June 9, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Vittorio Farina, Fabrice Gallou, Nizar Haddad, Xiao-jun Wang, Xudong Wei, Jinghua Xu, Yibo Xu, Nathan K. Yee, Li Zhang
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Publication number: 20090123480Abstract: The invention relates to bivalent mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.Type: ApplicationFiled: November 13, 2008Publication date: May 14, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Yuefeng Peng, Qian Cai
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Publication number: 20090118312Abstract: Compounds of the formula I: and N-oxides, salts, and stereoisomers thereof wherein A is OR1, NHS(?O)pR2; wherein; R1 is hydrogen, C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl; R2 is C1-C6alkyl, C0-C3alkylenecarbocyclyl, C0-C3alkyleneheterocyclyl; p is independently 1 or 2; n is 3, 4, 5 or 6; — denotes an optional double bond; L is N or CRz; Rz is H or forms a double bond with the asterisked carbon; Rq is H or when L is CRz, Rq can also be C1-C6alkyl; Rr is quinazolinyl, optionally substituted with one two or three substituents each independently selected from C1-C6 alkyl, C1-C6alkoxy, hydroxyl, halo, haloC1-C6alkyl, amino, mono- or dialkylamino, mono- or dialkylaminocarbonyl, C1-C6alkyl-carbonylamino, C0-C3alkylenecarbocyclyl and C0-C3 alkyleneheterocyclyl; R5 is hydrogen, C1-C6alkyl, C1-C6alkoxyC1-C6alkyl or C3-C7cycloalkyl; R6 is hydrogen, C1-C6alkyl, C1-C6alkoxy, C0-C3alkylenecarbocyclyl, C0-C3alkylene-heterocyclyl, hydroxy, bromo, chloro or fluoro have utility in the treatType: ApplicationFiled: July 28, 2006Publication date: May 7, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Lili Hu, Karin Charlotta Lindquist, Mats Stefan Lindstrom, Anna Karin Gertrud Linnea Belfrage, Horst Jurgen Wahling, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Sven Crister Sahlberg, Hans Kristian Wallberg, Pia Cecilia Kahnberg, Bjorn Olof Classon
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Publication number: 20090111982Abstract: The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: December 22, 2008Publication date: April 30, 2009Inventors: Lawrence M. Blatt, Steven W. Andrews, Kevin R. Condroski, George A. Doherty, Yutong Jiang, John A. Josey, April L. Kennedy, Machender R. Madduru, Peter J. Stengel, Steven M. Wenglowsky, Benjamin T. Woodard, Laura Woodard
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Publication number: 20090105091Abstract: The present invention provides a compound of the general formula (I), wherein X is the connection between the CO-hydrazine and the NR1-oxalic acid or ester group, and uses and synthesis methods. These compounds represent amino acid derivatives, wherein the amine group is turned into an acidic group by the oxalic acid group and the carboxylic acid is turned into an amine functionality by the hydrazine group; as well as peptidomimetics comprising the compound and methods for their synthesis.Type: ApplicationFiled: November 24, 2006Publication date: April 23, 2009Applicant: TECHNISCHE UNIVERSITAT WIENInventors: Ulrich Jordis, Jaywant B. Phopase
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Publication number: 20090105471Abstract: The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: December 22, 2008Publication date: April 23, 2009Inventors: Lawrence M. Blatt, Steven W. Andrews, Kevin R. Condroski, George A. Doherty, Yutong Jiang, John A. Josey, April L. Kennedy, Machender R. Madduru, Peter J. Stengel, Steven M. Wenglowsky, Benjamin T. Woodard, Laura Woodard
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Publication number: 20090105302Abstract: Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by - - - - -) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR6, —NH—SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy-carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optioType: ApplicationFiled: July 28, 2006Publication date: April 23, 2009Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Carl Erik Daniel Jonsson, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov, Lourdes Salvador Oden, Susana Ayesa Alvarez, Bjorn Olof Classon