The Additional Hetero Ring Is Six-membered Patents (Class 546/282.1)
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Publication number: 20100234428Abstract: The invention relates to substituted 2-mercapto-3-aminopyridines, methods for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: March 10, 2010Publication date: September 16, 2010Applicant: GRUNENTHAL GMBHInventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
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Publication number: 20100222221Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.Type: ApplicationFiled: February 25, 2010Publication date: September 2, 2010Applicant: Dow AgroSciences LLCInventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
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4-PHENYL-PYRANE-3,5-DIONES,4-PHENYL-THIOPYRANE-3,6-DIONES AND CYCLOHEXANETRIONES AS NOVEL HERBICIDES
Publication number: 20100210466Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.Type: ApplicationFiled: December 12, 2007Publication date: August 19, 2010Applicants: SYNGENTA PARTICIPATIONS AG, SYNGENTA LIMITEDInventors: Michel Muehlebach, Christoper John Matthews, James Nicholas Scutt, Mangala Govenkar -
Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100184989Abstract: The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.Type: ApplicationFiled: March 12, 2008Publication date: July 22, 2010Applicant: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Zhongxu Ren, Wen Zhang, Xuyuan Gu, Franco J. Duarte
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Publication number: 20100145046Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: November 20, 2009Publication date: June 10, 2010Inventors: Geoffrey W. Coates, John W. Kramer
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Publication number: 20100127212Abstract: The invention relates to liquid-crystalline compounds of the formula I in which R1, R2, A1, A2, A3, A4, Z1, Z2, Z3, V, a, b and c have the meanings indicated in claim 1, and to liquid-crystalline media comprising at least one compound of the formula I and to electro-optical displays containing a liquid-crystalline medium of this type.Type: ApplicationFiled: April 1, 2008Publication date: May 27, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Lietzau, Markus Czanta
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Publication number: 20100127213Abstract: The present invention relates to dielectrically positive liquid-crystalline media comprising a dielectrically positive component, component A, comprising a dielectrically positive compound of the formula I in which the parameters have the meaning indicated in the specification, and optionally a second dielectrically positive component, component B, comprising one or more dielectrically positive compounds having a dielectric anisotropy of great than 3, and optionally a dielectrically neutral component, component C, and to liquid-crystal displays containing these media, especially active-matrix displays and in particular TN, IPS and FFS displays.Type: ApplicationFiled: April 1, 2008Publication date: May 27, 2010Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Markus Czanta, Andreas Taugerbeck, Renate Bender, Lars Lietzau
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Publication number: 20100119503Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: ApplicationFiled: September 25, 2008Publication date: May 13, 2010Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Publication number: 20100087320Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: ApplicationFiled: November 12, 2009Publication date: April 8, 2010Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Publication number: 20100087487Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) including any stereochemically isomeric form thereof, or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein all radicals are defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic glutamate receptors subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy.Type: ApplicationFiled: March 7, 2008Publication date: April 8, 2010Applicants: Ortho-McNeil Janssen Pharmaceuticals Inc., Addex Pharma S.A.Inventors: José Maria Cid-Núñez, Andrès Avelino Trabanco-Suárez, Gregor James MacDonald, Guillaume Albert Jacques Duvey
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Patent number: 7691883Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):Type: GrantFiled: September 16, 2004Date of Patent: April 6, 2010Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi, Chizuko Takahashi
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Publication number: 20100063087Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R ; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.Type: ApplicationFiled: September 14, 2006Publication date: March 11, 2010Applicant: SPEEDEL EXPERIMENTA AGInventor: Peter HEROLD
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Publication number: 20100056528Abstract: The invention provides sulfonamide compounds of formula (I) as defined herein, pharmaceutical compositions containing the same and methods of treatment using such compounds and pharmaceutical compositions. These compounds have a common wide range of beneficial therapeutic indications, in particular as analgesic and anti-inflammatory agents.Type: ApplicationFiled: December 19, 2007Publication date: March 4, 2010Inventors: Avihai Yacovan, Iris Alroy, Alexander Aizikovich, Sima Mirilashvili, Flavio Gryszpan
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Publication number: 20100048636Abstract: The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.Type: ApplicationFiled: November 13, 2006Publication date: February 25, 2010Inventors: John J. Baldwin, David A. Claremon, Colin Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Wei Zhao, Patrick T. Flaherty
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Publication number: 20100004290Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: ApplicationFiled: September 10, 2009Publication date: January 7, 2010Applicant: DOW AGROSCIENCES LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Publication number: 20090281062Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.Type: ApplicationFiled: May 7, 2009Publication date: November 12, 2009Inventors: Lisa M. Frost, Stephen M. Courtney, Frederick A. Brookfield, Vincent J. Kalish
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Patent number: 7604815Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 9, 2007Date of Patent: October 20, 2009Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Patent number: 7589085Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.Type: GrantFiled: August 6, 2004Date of Patent: September 15, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
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Patent number: 7582676Abstract: The present invention relates to 2-phenylpyran-4-derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, and their medical uses.Type: GrantFiled: February 12, 2004Date of Patent: September 1, 2009Assignee: Laboratorios Almirall, S.A.Inventors: Juan Francisco Caturla Javaloyes, Graham Warrellow
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Patent number: 7582632Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: GrantFiled: April 16, 2007Date of Patent: September 1, 2009Assignee: Prosidion LimitedInventors: Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Karen Lesley Schofield, Vilasben Kanji Shah, Kosuke Yasuda
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Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides
Publication number: 20090181968Abstract: The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.Type: ApplicationFiled: November 22, 2006Publication date: July 16, 2009Applicant: ASTRAZENECA ABInventors: Kosrat Amin, Johan Broddefalk, Yantao Chen, Karolina Nilsson, Claire Milburn, Helene Desfosses, Ziping Liu, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang -
Publication number: 20090163498Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: June 11, 2008Publication date: June 25, 2009Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ungashe, J. J. Wright, Andrew Pennell, Zheng Wei, Anita Melikan
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Publication number: 20090062346Abstract: The present application describes deuterium-enriched tipranavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 25, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7488824Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.Type: GrantFiled: March 5, 2004Date of Patent: February 10, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: David Anthony Jackson, Martin Charles Bowden
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090005391Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: November 3, 2006Publication date: January 1, 2009Inventors: Matthew Colin Thor Fyfe, Martin James Procter
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Patent number: 7459555Abstract: The present invention relates to photochromic 2H-naphtho[1,2-b]pyrans as well as their use in synthetic resins of all types, especially for ophthalmic purposes. In particular, the present invention relates to photochromic naphthopyran compounds, for which a further ring system is bonded to the f side of the naphthopyran. The inventive photochromic dyes generally have the general formula (I) wherein n, R1, R2, R3, X, B and B? are defined as in claim 1. The inventive compounds are distinguished by good darkening and decolorizing properties and a very good service life.Type: GrantFiled: December 13, 2001Date of Patent: December 2, 2008Assignee: Rodenstock GmbHInventors: Manfred Melzig, Claudia Mann, Udo Weigand
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Publication number: 20080293730Abstract: Compounds of Formula (I): (formula) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: November 11, 2006Publication date: November 27, 2008Inventors: Matthew Colin Thor Fyfe, Martin James Procter
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Publication number: 20080280952Abstract: The present invention relates to novel pyridine derivatives such as compounds of the formula (I): and the use of such compounds or pharmaceutical compositions thereof in the treatment of diseases, particularly pain, which are mediated by the activity of the cannabinoid 2 receptor.Type: ApplicationFiled: February 1, 2005Publication date: November 13, 2008Inventors: Gerard Martin Paul Giblin, Karamjit Singh Jandu, William Leonard Mitchell, Ian David Wall
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Publication number: 20080274891Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: ApplicationFiled: May 23, 2008Publication date: November 6, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
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Publication number: 20080214617Abstract: Carbamate compounds having a structure represented by formula I (where R1, R2, R3, R4, R5 and R6 are as defined herein) are useful as anti-tumor agents.Type: ApplicationFiled: February 20, 2008Publication date: September 4, 2008Inventors: Hong Fu, Yaoquan Liu
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Patent number: 7375100Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: June 3, 2004Date of Patent: May 20, 2008Assignee: Pfizer IncInventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
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Patent number: 7368575Abstract: When a multi-step process reaction is carried out in a solution, it generally requires several treatments and purification procedures to go through with after the reaction, however, the inventive method for preparing 2,2?-disubstituted-3,4-dihydro-7,8-disubstituted-6-amino benzopyran derivative using a solid-phased synthetic method simplifies the treatment and purification procedures after the reaction, which makes possible to efficiently construct numerous drug-like libraries.Type: GrantFiled: October 20, 2004Date of Patent: May 6, 2008Assignee: Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Hyae-Gyeong Cheon, Young-Sik Cho, Jin-Soo Seo, Jong-Yeon Hwang, Ji-Yeon Park, Sung-Eun Yoo
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7354936Abstract: The present invention relates to 2-(4-sulphonylphenyl)pyran-4-one derivatives of general formula processes for their preparation, pharmaceutical compositions containing them, and their medical uses.Type: GrantFiled: September 16, 2002Date of Patent: April 8, 2008Assignee: Almirall AGInventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Josep Lluis Matallana Julia, Joan Feixas Gras
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Publication number: 20080070951Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, —O—, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.Type: ApplicationFiled: December 30, 2004Publication date: March 20, 2008Applicant: Medivir ABInventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
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Patent number: 7329675Abstract: This invention is directed to physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and pharmaceutically acceptable salts of the compounds of formula (I) and N-oxides thereof, Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmnaceutical compositions comprising compoundS of formula (I), their phatmaceUtical use and methods for their preparation.Type: GrantFiled: September 1, 2004Date of Patent: February 12, 2008Assignee: Aventis Pharma LimitedInventors: Paul Joseph Cox, Shelley Bower, David John Aldous, Peter Charles Astles, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
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Patent number: 7259166Abstract: 2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a polar ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: April 10, 2006Date of Patent: August 21, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Wendy Lea Corbett, Joseph Samuel Grimsby, Nancy-Ellen Haynes, Robert Francis Kester, Paige Erin Mahaney, Jagdish Kumar Racha, Ramakanth Sarabu, Ka Wang
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Patent number: 7186709Abstract: The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.Type: GrantFiled: August 27, 2003Date of Patent: March 6, 2007Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
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Patent number: 7132420Abstract: The present invention provides an aspartic proteinase-inhibiting compound of the formula: wherein a, b, c, d, and e, can be the same or different and each are R7, OR7, SR7, NR7R8, NHCOR7, CO2R7, CN, NO2, NH2, N3, or a halogen, wherein R7 and R8 are independently H or an alkyl. Substituents R1 or R2 are each H or an alkyl. Substituent R3 is a straight chain or branched alkyl, alkenyl, or alkynyl substituent, or is a cycloalkyl. Substituent A is OH, NH2, or SH. Further provided are pharmaceutical compositions, which include a therapeutically effective amount of at least one of the foregoing compounds, and therapeutic methods of using the foregoing compounds.Type: GrantFiled: June 11, 2003Date of Patent: November 7, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Ramnarayan S. Randad, John W. Erickson, Michael A. Eissenstat, Lucyna Lubkowska
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Patent number: 7115637Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved 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: August 8, 2003Date of Patent: October 3, 2006Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
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Patent number: 7091221Abstract: According to the present invention, there are provided a novel partial ester of a nitrogenous carboxylic acid ester with cellulose, the partial ester being useful as an antibacterial agent, a flame retardant, etc., and a simple and convenient process for preparing the same. Fibers made of said partial ester have washing-resistant antibacterial property and flame retardancy. There can be prepared the partial ester of a nitrogenous carboxylic acid ester with cellulose by contacting a nitrogenous carboxylic acid ester with cellulose and heat-treating the mixture.Type: GrantFiled: December 19, 2000Date of Patent: August 15, 2006Assignee: Ajinomoto Co., Inc.Inventors: Masahiko Kurauchi, Kiyonori Furuta, Hiroyuki Sato
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Patent number: 7034035Abstract: The present invention relates to compounds of Formula I: wherein: a) ?represents a 6-membered heterocyclic aromatic ring in which X1 is N and X2, X3 and X4 are each independently CR?; R? is independently H, halogen, cyano, hydroxy, C1-C3 alkyl, C1-C3 haloalkyl, cyclopropyl, C1-C3 alkoxy, C1-C3 haloalkoxy, C1-C3 alkylthio, aryl, C1-C3 NHC(O)alkyl, NHC(O)H, C1-C3 haloalkylthio, C2-C4 alkenyl, C2-C4 haloalkenyl, C2-C4 alkynyl, C2-C4 haloalkynyl or nitro wherein adjacent R? substituents may form a ring; b) Z is O, S or NORZ in which RZ is H or C1-C3 alkyl; and c) A represents (i) C3-C14 cycloalkyl, containing 1 or 3 heteroatoms and 0-2 unsaturations, which may be unsubstituted or substituted with halogen, hydroxy, C1-C6 alkyl, C1-C6 haloalkyl, cyano, nitro, aroyl, aryloxy, heteroaryloxy, C1-C6 alkylthio, arylthio, heteroarylthio, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C8 acyloxy, aryl, heteroaryl, C1-C6 acyl, C1-C6 carboalkoxy or amido unsubstituted or substituted with one or two C1 -C6 alkyl groups, oType: GrantFiled: December 2, 2002Date of Patent: April 25, 2006Assignee: Dow AgroSciences LLCInventors: Michael J. Ricks, William H. Dent, III, Richard B. Rogers, Chenglin Yao, Bassam S. Nader, John L. Miesel, Gina M. Fitzpatrick, Kevin G. Meyer, Noormohamed M. Niyaz, Irene M. Morrison, Robert P. Gajewski
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Patent number: 7026476Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are and pharmaceutical compositions containing, intermediate compounds and processes of making such compounds.Type: GrantFiled: April 28, 2003Date of Patent: April 11, 2006Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
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Patent number: 6995162Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: January 10, 2002Date of Patent: February 7, 2006Assignee: Amgen Inc.Inventors: Guoqing Chen, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
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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: 6919371Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.Type: GrantFiled: September 17, 2003Date of Patent: July 19, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
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Patent number: 6916933Abstract: Compounds of Formula I have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4 and are useful for treating disease whose symptoms and or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: September 24, 2003Date of Patent: July 12, 2005Assignee: Hoffman-La Roche Inc.Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
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Patent number: 6890928Abstract: This invention is directed to aromatic sulfone hydroxamic acids (including hydroxamates) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.Type: GrantFiled: September 5, 2003Date of Patent: May 10, 2005Assignee: Pharmacia CorporationInventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffrey N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang