Polycyclo Ring System Having The 1,3-thiazole Ring As One Of The Cyclos Patents (Class 546/270.1)
  • Publication number: 20100305067
    Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2Jalkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic ra
    Type: Application
    Filed: December 12, 2008
    Publication date: December 2, 2010
    Applicant: BIOTA EUROPE LTD
    Inventors: David John Haydon, Lloyd George Czaplewski
  • Publication number: 20100298141
    Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.
    Type: Application
    Filed: February 8, 2008
    Publication date: November 25, 2010
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
  • Publication number: 20100298291
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.
    Type: Application
    Filed: July 30, 2010
    Publication date: November 25, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
  • Publication number: 20100292227
    Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.
    Type: Application
    Filed: May 11, 2010
    Publication date: November 18, 2010
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: CHRISTIANE YOAKIM, MURRAY BAILEY, FRANCOIS BILODEAU, REBEKAH CARSON, LEE FADER, STEPHEN KAWAI, SEBASTIEN MORIN, CARL THIBEAULT, BRUNO SIMONEAU, SIMON SURPRENANT, YOULA TSANTRIZOS, STEVEN LAPLANTE
  • Publication number: 20100286110
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.
    Type: Application
    Filed: October 10, 2008
    Publication date: November 11, 2010
    Inventors: Matthew Colin Thor Fyfe, William Gattrell, Colin Peter Sambrook-Smith
  • Publication number: 20100273830
    Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.
    Type: Application
    Filed: July 14, 2008
    Publication date: October 28, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
  • Publication number: 20100261679
    Abstract: Disclosed herein are compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof, compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
    Type: Application
    Filed: October 16, 2008
    Publication date: October 14, 2010
    Inventors: James Sutton, Martin Sendzik, Weibo Wang
  • Publication number: 20100240620
    Abstract: The present application relates to novel aryl-substituted 3-cyano-5-thiazolyl- and 3-cyano-5-thiadiazolyl-1,4-dihydropyridines, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.
    Type: Application
    Filed: September 8, 2007
    Publication date: September 23, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Lars Barfacker, Peter Kolkhof, Karl-Heinz Schlemmer, Rolf Grosser, Adam Nitsche
  • Patent number: 7786125
    Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: April 7, 2009
    Date of Patent: August 31, 2010
    Inventor: Leu-Fen H. Lin
  • Patent number: 7786145
    Abstract: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: August 31, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jie Fei Cheng, Bin Liu, Thomas Arrhenius, Mark E. Wilson, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
  • Publication number: 20100216810
    Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: December 1, 2009
    Publication date: August 26, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Masanori OKANIWA, Terufumi TAKAGI
  • Publication number: 20100216844
    Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: February 19, 2010
    Publication date: August 26, 2010
    Inventors: Andreas Kling, Helmul Mack, Kaija Junios, Achim Mceller, Wllirled Hombarger, Charles W. Hulchins
  • Publication number: 20100210688
    Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: April 27, 2010
    Publication date: August 19, 2010
    Inventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
  • Publication number: 20100210762
    Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are e
    Type: Application
    Filed: August 15, 2008
    Publication date: August 19, 2010
    Applicant: FUJIFILM CORPORATION
    Inventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
  • Patent number: 7776861
    Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.
    Type: Grant
    Filed: January 23, 2006
    Date of Patent: August 17, 2010
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Xin Wen
  • Publication number: 20100200054
    Abstract: A compound for an organic photoelectric device, represented by the following Chemical Formula 1:
    Type: Application
    Filed: April 19, 2010
    Publication date: August 12, 2010
    Inventors: Ho-Kuk Jung, Myeong-Soon Kang, Jin-Seong Park, Nam-Soo Kim, Kyu-Yeol In, Eiu-Su Kang, Mi-Young Chae
  • Publication number: 20100197711
    Abstract: The present invention relates to benzothiazole compounds that mimic the activity of BH3 only proteins and are capable of binding to and neutralizing pro survival Bcl 2 proteins. The invention also relates to the use of such compounds in the regulation of cell death or cell survival and the treatment and/or prophylaxis of diseases or conditions associated with the deregulation of cell death or cell survival.
    Type: Application
    Filed: September 27, 2007
    Publication date: August 5, 2010
    Inventors: Keith Geoffrey Watson, Guillaume Laurent Lessene, Jonathan Bayldon Baell, David Ching Siang Huang, Ian Philip Street, Jerry McKee Adams, Peter Malcolm Colman, Brad Edmund Sleebs, Brian John Smith, Peter Edward Czabotar
  • Publication number: 20100196368
    Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
    Type: Application
    Filed: March 12, 2010
    Publication date: August 5, 2010
    Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
    Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
  • Publication number: 20100183743
    Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.
    Type: Application
    Filed: January 19, 2010
    Publication date: July 22, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
  • Publication number: 20100183852
    Abstract: 1. A compound of Formula (1) and salts thereof: wherein: R1 and R2 are independently H or optionally substituted alkyl; X and Y are independently CO2H or COSH; Q and T are independent substituents; a+n is 0 to 4; b+m is 0 to 4; and n+m are at least 1; also ink-jet compositions, processes and printed material.
    Type: Application
    Filed: May 12, 2008
    Publication date: July 22, 2010
    Inventor: Gavin Wright
  • Publication number: 20100179190
    Abstract: The present invention provides novel bicyclic pyrazolo kinase modulators and methods of using the novel bicyclic pyrazolo kinase modulators to treat diseases mediated by kinase activity.
    Type: Application
    Filed: November 14, 2008
    Publication date: July 15, 2010
    Applicant: SGX PHARMACEUTICALS, INC.
    Inventors: Pierre-Yves Bounaud, Andrew Vaino
  • Publication number: 20100179141
    Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
    Type: Application
    Filed: December 17, 2007
    Publication date: July 15, 2010
    Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, JR., Umar Faruk Mansoor
  • Publication number: 20100152195
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
    Type: Application
    Filed: December 16, 2009
    Publication date: June 17, 2010
    Inventors: Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100152185
    Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: December 7, 2009
    Publication date: June 17, 2010
    Inventors: Lin Chu, Mark T. Goulet, Feroze Ujjainwalla, Linda Chang, Richard Frenette, Yves Girard, Michel Therien, Dwight MacDonald, John H. Hutchinson
  • Patent number: 7737281
    Abstract: The present invention provides novel purine-based fluorescent dyes that may be used for staining, localizing and otherwise labeling target molecules, such as nucleic acids, for detection, amplification and quantification.
    Type: Grant
    Filed: July 7, 2005
    Date of Patent: June 15, 2010
    Assignee: Enzo Life Sciences, Inc. c/o Enzo Biochem, Inc.
    Inventor: Maciej Szczepanik
  • Publication number: 20100137317
    Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.
    Type: Application
    Filed: June 24, 2009
    Publication date: June 3, 2010
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20100130490
    Abstract: Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
    Type: Application
    Filed: May 20, 2008
    Publication date: May 27, 2010
    Inventors: Simon C. Ng, Keith B. Pfister, Martin Sendzik, James Sutton, Allan S. Wagman, Marion Wiesmann
  • Publication number: 20100120802
    Abstract: Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and Z is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.
    Type: Application
    Filed: January 15, 2010
    Publication date: May 13, 2010
    Inventors: Francesco MAKOVEC, Antonio Giordani, Roberto Artusi, Stefano Mandelli, Ilario Verpiliq, Simona Zanzola, Lucio Claudio Rovati
  • Publication number: 20100113789
    Abstract: The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect.
    Type: Application
    Filed: September 30, 2005
    Publication date: May 6, 2010
    Applicants: FUJIFILM CORPORATION
    Inventors: Masataka Ihara, Kiyosei Takasu, Khanitha Pudhom, Hiroshi Kitaguchi, Masayuki Kawakami, Kozo Sato
  • Publication number: 20100113414
    Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.
    Type: Application
    Filed: January 11, 2010
    Publication date: May 6, 2010
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Bodo BETZEMEIER, Trixi BRANDL, Steffen BREITFELDER, Ralph BRUECKNER, Thomas GERSTBERGER, Michael GMACHL, Matthias GRAUERT, Frank HILBERG, Christoph HOENKE, Matthias HOFFMANN, Maria IMPAGNATIELLO, Dirk KESSLER, Christian KLEIN, Bernd KRIST, Udo MAIER, Darryl McCONNELL, Charlotte REITHER, Stefan SCHEUERER, Andreas SCHOOP, Norbert SCHWEIFER, Oliver SIMON, Martin STEEGMAIER, Steffen STEURER, Irene WAIZENEGGER, Ulrike WEYER-CZERNILOFSKY, Andreas ZOEPHEL
  • Publication number: 20100098634
    Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.
    Type: Application
    Filed: July 24, 2009
    Publication date: April 22, 2010
    Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
  • Publication number: 20100098661
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives, compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient. Wherein ring Z, of formula (I), is a cyclopentyl, cyclopentenyl, 5-membered heterocycloalkyl, 5-membered heterocycloalkenyl or 5-membered heteroaryl ring.
    Type: Application
    Filed: December 17, 2007
    Publication date: April 22, 2010
    Inventors: Kevin X. Chen, Srikanth Venkatraman, F. George Njoroge, Stuart B. Rosenblum, Charles A. Lesburg, Jose S. Duca, Neng-Yang Shih, Francisco Velazquez, Gopinadhan N. Anilkumar, Qingbei Zeng, Joseph A. Kozlowski
  • Publication number: 20100063045
    Abstract: Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof.
    Type: Application
    Filed: March 28, 2008
    Publication date: March 11, 2010
    Applicant: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hasashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Patent number: 7674801
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: March 9, 2010
    Assignee: AstraZeneca AB
    Inventors: Gregory Steven Basarab, Shanta Bist, John Irvin Manchester, Brian Sherer
  • Patent number: 7671077
    Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: July 19, 2004
    Date of Patent: March 2, 2010
    Inventor: Leu-Fen Hou Lin
  • Patent number: 7655767
    Abstract: The present invention relates to the use of thiazolyl-pyridinium based dyes in optical layers for optical data recording, preferably for optical data recording using a laser with a wavelength up to 450 nm. The invention further relates to a write only read many (WORM) type optical data recording medium capable of recording and reproducing information with radiation of blue laser, which employs a thiazolyl-pyridinium based type dye in the optical layer. The present invention further relates to new thiazolyl-pyridinium based dyes, of formula (V), (VI) or (VIII).
    Type: Grant
    Filed: August 31, 2005
    Date of Patent: February 2, 2010
    Assignee: Clariant Finance (BVI) Limited
    Inventor: Andre Weiss
  • Patent number: 7655676
    Abstract: Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity against propionibacterium acne and are suitable for use in a method of treatment or prevention of acne.
    Type: Grant
    Filed: June 6, 2003
    Date of Patent: February 2, 2010
    Assignee: Naicons S.C.A.R.L.
    Inventors: Adriano Malabarba, Marco Cavaleri, Giorgio Mosconi, Daniela Jabes, Gabriela Romano
  • Publication number: 20090326222
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Application
    Filed: June 22, 2009
    Publication date: December 31, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Publication number: 20090275588
    Abstract: The invention relates to novel sulfonamide compounds and their use as orexin receptor antagonists.
    Type: Application
    Filed: April 10, 2007
    Publication date: November 5, 2009
    Applicant: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Cornella Zumbrunn Acklin
  • Publication number: 20090270407
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A, B, D, R1, R2, R3, X and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: April 23, 2009
    Publication date: October 29, 2009
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: CHI-PING TSENG, Brenton Todd Smith
  • Publication number: 20090258907
    Abstract: Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein X, R1, R2, R3, R4, L1, and m, are defined in the specification. Compositions comprising said compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using said compositions are also described.
    Type: Application
    Filed: April 7, 2009
    Publication date: October 15, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Steven L. Swann, Anil Vasudevan
  • Publication number: 20090221645
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, exhibit 5-HT1A agonism in addition to noradrenaline reuptake inhibition and optionally also 5-HT reuptake inhibition are useful for the treatment of obesity.
    Type: Application
    Filed: February 8, 2006
    Publication date: September 3, 2009
    Inventors: Oscar Barba, Graham John Dawson, Thomas Martin Krulle, Robert John Rowley, Donald Smyth, Gerard Hugh Thomas
  • Publication number: 20090221587
    Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Application
    Filed: August 14, 2006
    Publication date: September 3, 2009
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Andre Jeanguenat, Roger Graham Hall, Olivier Loiseleur, Stephan Trah, Patricia Durieux, Andrew Edmunds, Andrew Edmunds, Andre Stoller
  • Publication number: 20090209532
    Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.
    Type: Application
    Filed: July 17, 2006
    Publication date: August 20, 2009
    Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
  • Publication number: 20090197883
    Abstract: The instant invention provides compounds of Formula (I) which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: March 3, 2006
    Publication date: August 6, 2009
    Inventors: Helen M. Armstrong, Linda L. Chang, Richard Frenette, Dwight MacDonald, Hyun O. Ok, Michel Therien, Feroze Ujjainwalla
  • Publication number: 20090197877
    Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
    Type: Application
    Filed: June 21, 2007
    Publication date: August 6, 2009
    Applicant: Prolysis LTD.
    Inventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
  • Patent number: 7569695
    Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: August 4, 2009
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
  • 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
  • Patent number: 7553854
    Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: June 30, 2009
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: James C Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
  • Publication number: 20090162283
    Abstract: To provide a diagnostic drug which binds specifically to an amyloid aggregate and/or an amyloid deposit, to thereby realize imaging and quantification of a disease caused by amyloid aggregation and/or deposition. The invention provides a compound represented by formula (1): (wherein X1 represents an optionally substituted bicyclic heterocyclic group; X2 represents a hydrogen atom, a halogen atom, or a chelate-forming group; ring A represents a benzene ring or a pyridine ring; and ring B represents an optionally substituted 5-membered aromatic heterocyclic group which is bonded to the benzene ring or the pyridine ring via a carbon atom of ring B), a salt thereof, a solvate of any of these, or a transition metal coordination compound of any of these, and a diagnostic, preventive, or therapeutic drug containing the same.
    Type: Application
    Filed: November 30, 2006
    Publication date: June 25, 2009
    Applicants: Fujifilm RI Pharma Co., Ltd., Daiichi Sankyo Company, Limited
    Inventors: Kazunori Bando, Kazumi Taguchi