Hetero Ring Patents (Class 544/212)
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Publication number: 20090069305Abstract: The present invention relates to substituted nitrogen-containing heteroaryl derivatives, pharmaceutical compositions containing them, and methods of using any of these derivatives and compositions for H4 receptor activity modulation and the treatment of states mediated by histamine H4 receptor activity.Type: ApplicationFiled: September 11, 2008Publication date: March 12, 2009Inventors: Michael D. Gaul, Bao-Ping Zhao, Xizhen Zhu
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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: 20090056587Abstract: A compound of Formula (1) or salt thereof: wherein: A1 and A2 are each independently optionally substituted aryl; Q1 and Q2 are each independently an optionally substituted arylene or polycyclic heteroarylene group each comprising a phenylene ring which is para connected to the —N?N— and the —NR— groups shown in Formula (1); and each R is independently H or a substituent; L is a linking group containing at least one group selected from sulfonic acid, phosphonic acid, carboxylic acid and sulfonamide groups. The compounds have good ozone and light fastness are especially suitable for use in ink jet printing inks.Type: ApplicationFiled: April 27, 2007Publication date: March 5, 2009Inventor: Gavin Wright
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Publication number: 20090047252Abstract: 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: February 19, 2009Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Aesop Cho, Choung U. Kim, Jie Xu
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Publication number: 20090023727Abstract: A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; if X=NRX, then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X=CRXRY then RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, optionally substituted C5-20 aryl, optionally substituted C3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and RY is selected from H, hydroxy, optType: ApplicationFiled: July 3, 2008Publication date: January 22, 2009Inventors: Muhammad Hashim Javaid, Keith Allan Menear, Niall Morrison Barr Martin, Graeme Cameron Murray Smith, David Alan Rudge, Craig Anthony Roberts
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Publication number: 20090008002Abstract: A novel compound, used for example, as a gas generating fuel, is defined as a compound having the structural formula of wherein: R4 is a triazine ring; R1 is selected from the group consisting of a tetrazolyl group, CH3, OCH3, —CN, —C2H, NCO, —NHNH2, NO, NO2, OH, Cl, —NHCONH2, —OCOR, NHNO2, substituted tetrazoles, and substituted triazoles; R2 is selected from the group consisting of a tetrazolyl group, CH3, OCH3, —CN, —C2H, NCO, —NHNH2, NO, NO2, OH, Cl, —NHCONH2, —OCOR, NHNO2, substituted tetrazoles, and substituted triazoles; R3 is selected from the group consisting of a tetrazolyl group, CH3, OCH3, —CN, —C2H, NCO, —NHNH2, NO, NO2, OH, Cl, —NHCONH2, —OCOR, NHNO2, substituted tetrazoles, and substituted triazoles.Type: ApplicationFiled: October 1, 2007Publication date: January 8, 2009Inventors: Sudhakar R. Ganta, Cory G. Miller, Graylon K. Williams
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Publication number: 20080312436Abstract: Benzazole substituted aminobenzenesulfonate derivatives of formula (A) (wherein X, Q and M are as defined in the specification) are useful as components of water-soluble fluorescent inks and dyes invisible in day-light. Novel intermediates for the above compounds are also disclosed.Type: ApplicationFiled: July 26, 2006Publication date: December 18, 2008Inventors: Boris Markovich Bolotin, Yevgeniy Alexeyevich Birgen, Maria Leonardovna Kukushkina, Yelena Viktorovna Yakovleva
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Patent number: 7462617Abstract: The invention relates to compounds of formula wherein the substituents are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention further relates to methods for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other d 1iseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: September 1, 2004Date of Patent: December 9, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Alberati-Giani, Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stalder
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Patent number: 7455917Abstract: Disclosed is a compound represented by formula 1: [formula 1] wherein each of A, X, Y, Y? and Y? has the same meaning as described herein. When used in an organic light emitting device, the compound represented by formula 1 has at least one function selected from the group consisting of hole injection, hole transport, light emitting, electron transport, electron injection, etc., depending on the type of each unit forming the trimer or substituents in each unit. An organic light emitting device is also disclosed. The organic light emitting device includes a first electrode, an organic film having one or more layers and a second electrode, laminated successively, wherein at least one layer of the organic film includes at least one compound represented by formula 1.Type: GrantFiled: October 18, 2004Date of Patent: November 25, 2008Assignee: LG Chem, Ltd.Inventors: Kong Kyeom Kim, Min Jeong Lee, Yeon Hwan Kim, Jun Gi Jang
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Publication number: 20080287444Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: ApplicationFiled: April 25, 2008Publication date: November 20, 2008Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20080269225Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: December 28, 2006Publication date: October 30, 2008Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara Miskowski, Janet L. Ralbovsky, Mark Schulz
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Publication number: 20080255136Abstract: The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.Type: ApplicationFiled: April 22, 2008Publication date: October 16, 2008Applicant: IRM LLCInventors: Baogen Wu, Yun He, Truc Nguyen, Kelli L. Kuhen, David Archer Ellis, Tao Jiang, Xiaohui He, Kunyong Yang, Badry Bursulaya
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Publication number: 20080251758Abstract: The invention relates to triazine compounds comprising both amino- and carboxyl-containing substituents and also to a process for preparing them.Type: ApplicationFiled: October 13, 2006Publication date: October 16, 2008Applicant: Evonik Degussa GmbhInventors: Jochen Kirchhoff, Peter Werle, Guenter Kreilkamp, Edeltraud Kruppa
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Publication number: 20080194545Abstract: The present invention is directed to compounds of formula I, pharmaceutical compositions comprising the compounds, and methods for making and using the inventive compounds.Type: ApplicationFiled: February 7, 2008Publication date: August 14, 2008Applicant: TRIUS THERAPEUTICSInventors: Xiaoming Li, John M. Finn, Mark T. Hilgers
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Patent number: 7410968Abstract: The present invention relates to compounds represented by formula (I): where the structural variables are as defined herein. The compounds are useful for promoting hydration of mucosal surfaces.Type: GrantFiled: August 26, 2005Date of Patent: August 12, 2008Assignee: PARION SCIENCES, Inc.Inventors: Michael R. Johnson, Bruce F. Molino, Jianzhong Zhang, Bruce Sargent
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Publication number: 20080176853Abstract: The invention provides for Triazine derivatives and their use to modulate protein kinase activity in a variety of conditions and diseases.Type: ApplicationFiled: December 14, 2007Publication date: July 24, 2008Applicant: Abraxis BioScience, Inc.Inventors: Chunlin Tao, Qinwei Wang, Neil P. Desai, Patrick Soon-Shiong
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Publication number: 20080146571Abstract: O-linked pyrimidin-4-amine-based compounds, pharmaceutical compositions comprising them, and methods of their use are described.Type: ApplicationFiled: December 12, 2007Publication date: June 19, 2008Inventors: David J. Augeri, Marianne Carlsen, Kenneth G. Carson, Qinghong Fu, Jason P. Healy, Alexander Heim-Riether, Theodore C. Jessop, Philip E. Keyes, Min Shen, James E. Tarver, Jerry A. Taylor, Xiaolian Xu
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Publication number: 20080139566Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: ApplicationFiled: January 24, 2008Publication date: June 12, 2008Inventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Publication number: 20080132509Abstract: Substituted biaryl analogues of Formula (I) are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localizations studies.Type: ApplicationFiled: December 13, 2005Publication date: June 5, 2008Applicant: Neurogen CorporationInventors: Charles A. Blum, Bertrand L. Chenard, Kevin J. Hodgetts, Xiaozhang Zheng
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Publication number: 20080119461Abstract: 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: November 5, 2007Publication date: May 22, 2008Inventors: Ny Sin, Brian Lee Venables, Li-Qiang Sun, Sing-Yuen Sit, Yan Chen, Paul Michael Scola
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Patent number: 7358252Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and its use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: November 7, 2006Date of Patent: April 15, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Paul J. Gilligan
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Publication number: 20080076771Abstract: A compound of the formula (I) useful as promoters of thrombopoiesis and megakaryocytopoiesis, wherein A, B, D, E, W, X, Y, Z, R1 and R2 are defined as above.Type: ApplicationFiled: September 12, 2005Publication date: March 27, 2008Inventors: Lawrence A. Reiter, Robert G. Linde
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Patent number: 7319099Abstract: The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.Type: GrantFiled: August 4, 2004Date of Patent: January 15, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Matthias Heinrich Nettekoven, Roger David Norcross, Emmanuel Pinard, Henri Stadler
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Publication number: 20080009497Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's Disease.Type: ApplicationFiled: July 5, 2007Publication date: January 10, 2008Inventors: Mark D. Wittman, Harold Mastalerz, Kurt Zimmermann, Mark G. Saulnier, Upender Velaparthi, Dolatrai M. Vyas, Guifen Zhang, Walter Lewis Johnson, David B. Frennesson, Xiaopeng Sang, Peiying Liu, David R. Langley
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Publication number: 20070299076Abstract: The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, n and R2 are as described herein; compositions thereof; and uses thereof.Type: ApplicationFiled: June 18, 2007Publication date: December 27, 2007Inventors: David W. Piotrowski, Yu Hui, John W. Benbow
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Patent number: 7285550Abstract: The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkinson's disease.Type: GrantFiled: April 9, 2004Date of Patent: October 23, 2007Assignee: Biogen Idec MA Inc.Inventors: Chi Vu, Russell C. Petter, Gnanasambandam Kumaravel
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Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
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Patent number: 7230100Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof and Q is oxygen, carbon or sulphur, comprising a coupling step of the pyrimidine base with a molecule of formula (B) described herein in a suitable coupling solvent, in the presence of catalytic amounts of an element or combination of elements of groups IB or IIB of the periodic table, a tertiary amine and a Lewis acid to obtained an intermediate of formula (D) which is deprotected in the subsequent step to generate the product of formula (A).Type: GrantFiled: April 7, 2006Date of Patent: June 12, 2007Assignee: Shire BioChem., Inc.Inventor: Qing Yu
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Patent number: 7208597Abstract: Triazine derivatives of formula (1) wherein R1 is C1–C20alkyl; C3–C7cycloalkyl; or C1–C20perfluoroalkyl; R2 is hydrogen; C1–C20alkyl; or C3–C7cycloalkyl; and R3 is hydrogen; C1–C20alkyl; C3–C7cycloalky; C1–C20perfluoroalky; C1C20alkyl-carbonyl; C3–C7cycloalkyl-carbonyl; C1–C20perfluoroalkyl-carbonyl; or phenylcarbonyl; are described. The compounds exhibit pronounced action against gram-positive and gram-negative bacteria and also against yeasts and moulds.Type: GrantFiled: July 22, 2003Date of Patent: April 24, 2007Assignee: Ciba Specialty Chemicals CorporationInventors: Werner Hölzl, Gabriele Eichacker, Andrea Preuss
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Patent number: 7157578Abstract: Corticotropin releasing factor (CRF) antagonists of Formula (I): and its use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.Type: GrantFiled: February 5, 2003Date of Patent: January 2, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Paul J. Gilligan
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Patent number: 7148240Abstract: The invention relates to benzofuran or benzothiophene derivatives of general formula: These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes of the cardiovascular system.Type: GrantFiled: August 23, 2001Date of Patent: December 12, 2006Assignee: Sanofi-AventisInventors: Jean-Louis Assens, Claude Bernhart, Frédérique Cabanel-Haudricourt, Dino Nisato
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Patent number: 7064129Abstract: Compounds are provided which are represented by the formula: where the structural variables are defined herein. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: August 18, 2004Date of Patent: June 20, 2006Assignee: Parion Sciences, Inc.Inventors: Michael R. Johnson, Bruce Molino, Jianzhong Zhang, Bruce Sargent
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Patent number: 7008798Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.Type: GrantFiled: March 22, 2002Date of Patent: March 7, 2006Assignee: Carnegie Mellon UniversityInventor: Alan S. Waggoner
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Patent number: 7002011Abstract: Compounds of the formula (I) or salts thereof are suitable for preparing active substances from the from the class of the aminotriazines of the formula (IV), for example herbicidal active substances. The compounds (I) can be prepared by chlorinating compounds of the formula (II) where, in the formulae, R1, R2, R3 and X are as defined in claim 1 and A and R have the meaning required in the active substances to be prepared, and they can be reacted with amines of the formula A—NH—R to give the active substances.Type: GrantFiled: July 2, 1999Date of Patent: February 21, 2006Assignee: Aventis CropScience GmbHInventors: Jürgen Zindel, Jens Hollander, Klemens Minn, Lothar Willms
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Patent number: 6998272Abstract: The subject invention pertains to macrocyclic compounds, and their use, the compounds having the formula (I) wherein X is a ring bearing an optionally-protected functional group or solid phase group R1, Y is a linker optionally bearing an optionally-protected functional group or solid phase group R2, m is at least 3, and each instance of X, Y, R1 and R2 may be the same or different.Type: GrantFiled: December 11, 2000Date of Patent: February 14, 2006Assignee: Prometic Biosciences, Ltd.Inventors: Dennis Lowik, Christopher Robin Lowe
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Patent number: 6995262Abstract: The invention relates to a novel polymethine dyes containing at least one acylsulfonamido group of the formula (I) in which n, Y, A and R have the meaning given in the claims, and at least one compound of the formulae (a) to (n) given in the claims. The polymethine dyes according to the invention are suitable for use as dyes and/or labels, in particular for staining or labeling biomolecules.Type: GrantFiled: July 24, 2000Date of Patent: February 7, 2006Assignee: Bayer CropScience AGInventors: Geert Deroover, Michael Missfeldt, Lydia Simon
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Patent number: 6989275Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.Type: GrantFiled: March 22, 2002Date of Patent: January 24, 2006Assignee: Carnegie Mellon UniversityInventor: Alan S. Waggoner
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Patent number: 6956032Abstract: The present invention pertains to luminescent dyes and methods for covalently attaching the dyes to a component or mixture of components so that the components may be detected and/or quantified by luminescence detection methods. The dyes are cyanine and cyanine-type dyes that contain or are derivatized to contain a reactive group. The reactive group is covalently reactive with amine, hydroxy and/or sulfhydryl groups on the component so that the dye can be covalently bound to the component. In addition, the dyes are preferably soluble in aqueous or other medium in which the component is contained. The components to be labeled can be either biological materials, such as antibodies, antigens, peptides, nucleotides, hormones, drugs, or non-biological materials, such as polymers, glass, or other surfaces. Any luminescent or light absorbing detecting step can be employed in the method of the invention.Type: GrantFiled: December 19, 2000Date of Patent: October 18, 2005Assignee: Carnegie Mellon UniversityInventor: Alan S. Waggoner
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Patent number: 6953798Abstract: Alkanoic acid derivatives of formula (1) are described: Ar1(Alka)rL1Ar2CH(R1)C(Ra)(Ra?)R??(1) Ar1 is an optionally substituted aromatic or heteroarotic group; L1 is a covalent bond or a linker atom or group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of ?4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: November 29, 1999Date of Patent: October 11, 2005Assignee: Celltech R&D LimitedInventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
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Patent number: 6949630Abstract: The cationic dyes of formula (1) specified in claim 1 are suitable especially for colouring keratin-containing fibres, more especially for colouring hair.Type: GrantFiled: September 17, 2002Date of Patent: September 27, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Jean-Marie Adam, Jean-Pierre Bacher
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Patent number: 6949544Abstract: The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: March 28, 2002Date of Patent: September 27, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Randy S. Bethiel, John Cochran, Young-Choon Moon, Suganthini Nanthakumar
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Patent number: 6943249Abstract: The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.Type: GrantFiled: March 17, 2003Date of Patent: September 13, 2005Assignees: Ash Stevens, Inc., Pharmion CorporationInventors: Dumitru Ionescu, Peter Blumbergs, Gary L. Silvey
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Patent number: 6903132Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.Type: GrantFiled: June 11, 2003Date of Patent: June 7, 2005Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.Inventors: Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen Thuy Do, Jun Feng, Yufeng Hong, Haitao Li, Ved P. Pathak, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins
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Patent number: 6894047Abstract: This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I wherein R1, R2 and R3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers.Type: GrantFiled: March 26, 2002Date of Patent: May 17, 2005Assignee: Pfizer Inc.Inventor: Banavara L. Mylari
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Patent number: 6887870Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: September 25, 2000Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
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Patent number: 6887831Abstract: The invention relates to novel substituted thienyl(amino)sulphonylureas of the general formula (I) in which A, Q, R1, R2, R3, R4 and R5 are each as defined in the description, to processes for their preparation and to their use as herbicides.Type: GrantFiled: July 25, 2000Date of Patent: May 3, 2005Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Joachim Kluth, Klaus-Helmut Müller, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Patent number: 6884804Abstract: The present invention provides compounds of formula I: wherein A is N or CR, and G, R1, R2 and R3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of Src mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: May 16, 2002Date of Patent: April 26, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventor: Young Choon-Moon
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Patent number: 6881737Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and polycystic kidney disease.Type: GrantFiled: April 10, 2002Date of Patent: April 19, 2005Assignee: Amgen Inc.Inventors: John L. Buchanan, Joseph L. Kim, Perry M. Novak, Joseph J. Nunes, Vinod F. Patel
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Patent number: 6870052Abstract: Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, fluorine, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro. The above compounds also inhibit DNA replication in mammalian cells.Type: GrantFiled: April 7, 2003Date of Patent: March 22, 2005Assignee: Southern Research InstituteInventors: John A. Secrist, III, Kamal N. Tiwari, John A. Montgomery
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Patent number: 6864255Abstract: The invention encompasses compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions, uses and methods for prophylaxis and treatment of cancer and angiogenesis-related disease.Type: GrantFiled: April 10, 2002Date of Patent: March 8, 2005Assignee: Amgen Inc.Inventors: Stephanie D. Geuns-Meyer, Lucian V. DiPietro, Joseph L. Kim, Vinod F. Patel