The Additional Hetero Ring Is Six-membered Patents (Class 546/282.1)
  • Publication number: 20100234428
    Abstract: 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: Application
    Filed: March 10, 2010
    Publication date: September 16, 2010
    Applicant: GRUNENTHAL GMBH
    Inventors: Sven Kühnert, Beatrix Merla, Achim Kless, Gregor Bahrenberg, Wolfgang Schröder
  • Publication number: 20100222221
    Abstract: N-Alkoxyamides of 4-aminopicolinic acids and 6-amino-4-pyrimidinecarboxylates are selective herbicides for corn, canola and sugar beet.
    Type: Application
    Filed: February 25, 2010
    Publication date: September 2, 2010
    Applicant: Dow AgroSciences LLC
    Inventors: Joseph D. Eckelbarger, Paul R. Schmitzer, Carla N. Yerkes, Timothy A. Boebel, Norbert M. Satchivi, Gregory T. Whiteker
  • Publication number: 20100210466
    Abstract: Pyrandione, thiopyrandione and cyclohexanetrione compounds, which are suitable for use as herbicides.
    Type: Application
    Filed: December 12, 2007
    Publication date: August 19, 2010
    Applicants: SYNGENTA PARTICIPATIONS AG, SYNGENTA LIMITED
    Inventors: Michel Muehlebach, Christoper John Matthews, James Nicholas Scutt, Mangala Govenkar
  • Publication number: 20100197655
    Abstract: 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: Application
    Filed: January 12, 2010
    Publication date: August 5, 2010
    Inventors: 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
  • Publication number: 20100184989
    Abstract: 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: Application
    Filed: March 12, 2008
    Publication date: July 22, 2010
    Applicant: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng, Zhongxu Ren, Wen Zhang, Xuyuan Gu, Franco J. Duarte
  • Publication number: 20100145046
    Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.
    Type: Application
    Filed: November 20, 2009
    Publication date: June 10, 2010
    Inventors: Geoffrey W. Coates, John W. Kramer
  • Publication number: 20100127212
    Abstract: 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: Application
    Filed: April 1, 2008
    Publication date: May 27, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Lars Lietzau, Markus Czanta
  • Publication number: 20100127213
    Abstract: 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: Application
    Filed: April 1, 2008
    Publication date: May 27, 2010
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Markus Czanta, Andreas Taugerbeck, Renate Bender, Lars Lietzau
  • Publication number: 20100119503
    Abstract: 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: Application
    Filed: September 25, 2008
    Publication date: May 13, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
  • Publication number: 20100087320
    Abstract: 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: Application
    Filed: November 12, 2009
    Publication date: April 8, 2010
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark-Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Publication number: 20100087487
    Abstract: 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: Application
    Filed: March 7, 2008
    Publication date: April 8, 2010
    Applicants: 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
  • Patent number: 7691883
    Abstract: The present invention relates to a cinnamoyl compound represented by the formula (I):
    Type: Grant
    Filed: September 16, 2004
    Date of Patent: April 6, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshitaka Tomigahara, Kiyoshi Higashi, Junya Takahashi, Chizuko Takahashi
  • Publication number: 20100063087
    Abstract: 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: Application
    Filed: September 14, 2006
    Publication date: March 11, 2010
    Applicant: SPEEDEL EXPERIMENTA AG
    Inventor: Peter HEROLD
  • Publication number: 20100056528
    Abstract: 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: Application
    Filed: December 19, 2007
    Publication date: March 4, 2010
    Inventors: Avihai Yacovan, Iris Alroy, Alexander Aizikovich, Sima Mirilashvili, Flavio Gryszpan
  • Publication number: 20100048636
    Abstract: 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: Application
    Filed: November 13, 2006
    Publication date: February 25, 2010
    Inventors: 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
  • Publication number: 20100004290
    Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.
    Type: Application
    Filed: September 10, 2009
    Publication date: January 7, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
  • Publication number: 20090281062
    Abstract: 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: Application
    Filed: May 7, 2009
    Publication date: November 12, 2009
    Inventors: Lisa M. Frost, Stephen M. Courtney, Frederick A. Brookfield, Vincent J. Kalish
  • Patent number: 7604815
    Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.
    Type: Grant
    Filed: February 9, 2007
    Date of Patent: October 20, 2009
    Assignee: Dow AgroSciences LLC
    Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
  • Patent number: 7589085
    Abstract: 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: Grant
    Filed: August 6, 2004
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
  • Patent number: 7582676
    Abstract: 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: Grant
    Filed: February 12, 2004
    Date of Patent: September 1, 2009
    Assignee: Laboratorios Almirall, S.A.
    Inventors: Juan Francisco Caturla Javaloyes, Graham Warrellow
  • Patent number: 7582632
    Abstract: Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: September 1, 2009
    Assignee: Prosidion Limited
    Inventors: Matthew Colin Thor Fyfe, Lisa Sarah Gardner, Maseo Nawano, Martin James Procter, Chrystelle Marie Rasamison, Karen Lesley Schofield, Vilasben Kanji Shah, Kosuke Yasuda
  • Publication number: 20090181968
    Abstract: 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: Application
    Filed: November 22, 2006
    Publication date: July 16, 2009
    Applicant: ASTRAZENECA AB
    Inventors: 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: 20090163498
    Abstract: 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: Application
    Filed: June 11, 2008
    Publication date: June 25, 2009
    Applicant: CHEMOCENTRYX, INC.
    Inventors: Solomon Ungashe, J. J. Wright, Andrew Pennell, Zheng Wei, Anita Melikan
  • Publication number: 20090062346
    Abstract: The present application describes deuterium-enriched tipranavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 25, 2008
    Publication date: March 5, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7488824
    Abstract: 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: Grant
    Filed: March 5, 2004
    Date of Patent: February 10, 2009
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: David Anthony Jackson, Martin Charles Bowden
  • Publication number: 20090036420
    Abstract: 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: Application
    Filed: July 28, 2008
    Publication date: February 5, 2009
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20090005391
    Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
    Type: Application
    Filed: November 3, 2006
    Publication date: January 1, 2009
    Inventors: Matthew Colin Thor Fyfe, Martin James Procter
  • Patent number: 7459555
    Abstract: 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: Grant
    Filed: December 13, 2001
    Date of Patent: December 2, 2008
    Assignee: Rodenstock GmbH
    Inventors: Manfred Melzig, Claudia Mann, Udo Weigand
  • Publication number: 20080293730
    Abstract: Compounds of Formula (I): (formula) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
    Type: Application
    Filed: November 11, 2006
    Publication date: November 27, 2008
    Inventors: Matthew Colin Thor Fyfe, Martin James Procter
  • Publication number: 20080280952
    Abstract: 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: Application
    Filed: February 1, 2005
    Publication date: November 13, 2008
    Inventors: Gerard Martin Paul Giblin, Karamjit Singh Jandu, William Leonard Mitchell, Ian David Wall
  • Publication number: 20080274891
    Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as herbicides.
    Type: Application
    Filed: May 23, 2008
    Publication date: November 6, 2008
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Luthy, Jurgen Schaetzer
  • Publication number: 20080214617
    Abstract: 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: Application
    Filed: February 20, 2008
    Publication date: September 4, 2008
    Inventors: Hong Fu, Yaoquan Liu
  • Patent number: 7375100
    Abstract: 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: Grant
    Filed: June 3, 2004
    Date of Patent: May 20, 2008
    Assignee: Pfizer Inc
    Inventors: Alan Daniel Brown, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite
  • Patent number: 7368575
    Abstract: 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: Grant
    Filed: October 20, 2004
    Date of Patent: May 6, 2008
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Young-Dae Gong, Hyae-Gyeong Cheon, Young-Sik Cho, Jin-Soo Seo, Jong-Yeon Hwang, Ji-Yeon Park, Sung-Eun Yoo
  • Patent number: 7358359
    Abstract: 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: Grant
    Filed: July 22, 2005
    Date of Patent: April 15, 2008
    Assignee: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman
  • Patent number: 7354936
    Abstract: 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: Grant
    Filed: September 16, 2002
    Date of Patent: April 8, 2008
    Assignee: Almirall AG
    Inventors: Maria Isabel Crespo Crespo, Juan Miguel Jimenez Mayorga, Josep Lluis Matallana Julia, Joan Feixas Gras
  • Publication number: 20080070951
    Abstract: 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: Application
    Filed: December 30, 2004
    Publication date: March 20, 2008
    Applicant: Medivir AB
    Inventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
  • Patent number: 7329675
    Abstract: 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: Grant
    Filed: September 1, 2004
    Date of Patent: February 12, 2008
    Assignee: Aventis Pharma Limited
    Inventors: 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
  • Patent number: 7259166
    Abstract: 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: Grant
    Filed: April 10, 2006
    Date of Patent: August 21, 2007
    Assignee: 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
  • Patent number: 7186709
    Abstract: 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: Grant
    Filed: August 27, 2003
    Date of Patent: March 6, 2007
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Robert A. Stavenger, Timothy J. Mitchison, Zoltan Maliga
  • Patent number: 7132420
    Abstract: 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: Grant
    Filed: June 11, 2003
    Date of Patent: November 7, 2006
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Ramnarayan S. Randad, John W. Erickson, Michael A. Eissenstat, Lucyna Lubkowska
  • Patent number: 7115637
    Abstract: 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: Grant
    Filed: August 8, 2003
    Date of Patent: October 3, 2006
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Francesco Salituro, Vincent Galullo, Steven Bellon, Guy Bemis, John Cochran
  • Patent number: 7091221
    Abstract: 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: Grant
    Filed: December 19, 2000
    Date of Patent: August 15, 2006
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masahiko Kurauchi, Kiyonori Furuta, Hiroyuki Sato
  • Patent number: 7034035
    Abstract: 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, o
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: April 25, 2006
    Assignee: Dow AgroSciences LLC
    Inventors: 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
  • Patent number: 7026476
    Abstract: 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: Grant
    Filed: April 28, 2003
    Date of Patent: April 11, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier F. Cirillo, Steffen Breitfelder, Usha R. Patel, John R. Proudfoot, Alan D. Swinamer
  • Patent number: 6995162
    Abstract: 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: Grant
    Filed: January 10, 2002
    Date of Patent: February 7, 2006
    Assignee: 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
  • Patent number: 6953798
    Abstract: 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: Grant
    Filed: November 29, 1999
    Date of Patent: October 11, 2005
    Assignee: Celltech R&D Limited
    Inventors: John Robert Porter, John Clifford Head, Graham John Warrellow, Sarah Catherine Archibald
  • Patent number: 6919371
    Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: July 19, 2005
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: 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
  • Patent number: 6916933
    Abstract: 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: Grant
    Filed: September 24, 2003
    Date of Patent: July 12, 2005
    Assignee: Hoffman-La Roche Inc.
    Inventors: Gerald Lewis Kaplan, Achyutharao Sidduri, Jefferson Wright Tilley
  • Patent number: 6890928
    Abstract: 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: Grant
    Filed: September 5, 2003
    Date of Patent: May 10, 2005
    Assignee: Pharmacia Corporation
    Inventors: 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