Nitrogen Bonded Directly To The -c(=x)- Group Patents (Class 549/487)
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Publication number: 20120245185Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: November 8, 2010Publication date: September 27, 2012Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120196865Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.Type: ApplicationFiled: July 19, 2010Publication date: August 2, 2012Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
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Publication number: 20120122862Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.Type: ApplicationFiled: January 30, 2012Publication date: May 17, 2012Inventors: Haiyan Jia, Ian Zachary, Michelle Tickner, Lili Cheng, Chris Chapman, Katie Ellard, Basil Hartzoulakis, Ashley Jarvis, Rosemary Lynch, Jamie Nally, David Selwood, Mark Stewart
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Publication number: 20120116090Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: December 6, 2011Publication date: May 10, 2012Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, Bing Li
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Publication number: 20120115851Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.Type: ApplicationFiled: January 18, 2012Publication date: May 10, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120059012Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Publication number: 20120004198Abstract: Provided herein are non-peptide GLP-1 receptor modulator compounds, for example, of Formula I, pharmaceutical compositions comprising such compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of a metabolic disorder.Type: ApplicationFiled: February 2, 2011Publication date: January 5, 2012Applicant: ARGUSINA INC.Inventors: Jiayu LIAO, Yufeng Hong, Yong Wang, Thomas W. Von Geldern, Kanyin E. Zhang
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Publication number: 20110318359Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.Type: ApplicationFiled: December 2, 2009Publication date: December 29, 2011Inventors: Edward P. Feener, Allen Clermont
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Publication number: 20110306646Abstract: The present invention relates to a N-(Phenylcycloalkyl)carboxamide or N-(Benzylcycloalkyl)carboxamide or its thiocarboxamide derivative of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, substituted or non-substituted 5-membered heterocyclyl group, T represents an oxygen or a sulphur atom, B represents a non aromatic carbocycle that can be substituted by one to four C1-C8-alkyl groups, and X, Z1, Z2 and Z3 represent various substituents; their process of preparation; the preparation of intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: February 16, 2010Publication date: December 15, 2011Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20110306542Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.Type: ApplicationFiled: June 9, 2011Publication date: December 15, 2011Applicant: Receptos, Inc.Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
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Patent number: 8067638Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.Type: GrantFiled: June 20, 2006Date of Patent: November 29, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Akiyoshi Kai, Takeo Wakita, Hiroyuki Katsuta, Kei Yoshida, Hidetaka Tsukada, Yusuke Takahashi, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido
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Publication number: 20110275663Abstract: The present invention relates to the use of acylthiourea or acylurea derivatives for the treatment of pathologies involving a tissue dysfunction associated with a deregulation of the Hedgehog protein signalling pathway, and also to novel acylthiourea or acylurea derivatives as such, to their use as a medicinal product, and to pharmaceutical compositions containing them.Type: ApplicationFiled: April 16, 2009Publication date: November 10, 2011Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Angèle Schoenfelder, André Mann, Maurizio Taddei, Antonio Solinas, Fabrizio Manetti
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Publication number: 20110224154Abstract: A composition for promoting lacrimal secretion which can be used safely and effectively in the lacrimal secretion promoting therapy, not in the conventional supplemental therapy of lacrimal fluid components is provided. The composition for promoting lacrimal secretion comprising a peptide derivative represented by the formula (I): and a contact lens which retains and/or contains the composition are provided.Type: ApplicationFiled: June 19, 2009Publication date: September 15, 2011Applicants: KINKI UNIVERSITY, FUSO PHARMACEUTICAL INDUSTRIES, LTD.Inventors: Atsufumi Kawabata, Hiroyuki Nishikawa, Kenzo Kawai, Yoshiko Kawai
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Publication number: 20110213156Abstract: A compound represented by the following general formula (I): [wherein R1 and R2 represent an alkyl group, X represents —S—, —O— or —NH—, Y represents C or N, R3 represents hydrogen atom or a C1-10 alkyl group, Z represents —CO—N(R5)— (R5 represents hydrogen atom or a C1-6 alkyl group) or —C(R6)?C(R7)—CO—NH— (R6 and R7 represent hydrogen atom or a C1-6 alkyl group), Ar represents an aryldiyl group or a heteroaryldiyl group, and R4 represents —COOH, —OCH2—COOH, —CH2—COOH, or —CH2—CH2—COOH], which has a retinoid action and is useful as an active ingredient of a medicament.Type: ApplicationFiled: August 14, 2008Publication date: September 1, 2011Applicant: RESEARCH FOUNDATION ITSUU LABORATORYInventors: Hideaki Muratake, Masayuki Noguchi, Koichi Shudo
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Patent number: 8008297Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: April 4, 2008Date of Patent: August 30, 2011Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valerie Perron
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Novel 1, 2-Disubstituted Amido-anthraquinone Derivatives, Preparation Method and application thereof
Publication number: 20110207739Abstract: A series of novel 1,2-disubstituted amido-anthraquinone derivatives, and the preparation method and application of said derivatives. Said application includes said derivatives with therapeutically effective amount being prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG -
Patent number: 7994093Abstract: The invention relates to a fungicidally active compound of formula (I): where Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, provided that the ring is not 1,2,3-triazole, the ring being substituted by groups R8, R9 and R10; X is a single or double bond; Y is O, S, N(R11) or (CR12R13)(CR14R15)m(CR16R17)n; m is 0 or 1; n is 0 or 1; and R1 to R17 each, independently, have a range of values; to the preparation of these compounds, to novel intermediates used in the preparation of these compounds, to agrochemical compositions which comprise at least one of the novel compounds as active ingredient, to the preparation of the compositions mentioned and to the use of the active ingredients or compositions in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: GrantFiled: August 28, 2009Date of Patent: August 9, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
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Publication number: 20110178101Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 18, 2011Publication date: July 21, 2011Inventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20110178102Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: June 30, 2004Publication date: July 21, 2011Applicant: ALBERT EINSTEIN COLLEGE OF MEDICINE OF YESHIVA UNIVERSITYInventors: Vern L Schramm, Anthony A. Suave
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Patent number: 7964735Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: GrantFiled: July 21, 2006Date of Patent: June 21, 2011Assignee: Bayer Cropscience AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Publication number: 20110136792Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: October 20, 2010Publication date: June 9, 2011Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian, Kshitij Chhabilbhai Thakkar
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Publication number: 20110054017Abstract: The present application relates to novel substituted furan derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: January 29, 2009Publication date: March 3, 2011Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
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Patent number: 7880020Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.Type: GrantFiled: June 3, 2009Date of Patent: February 1, 2011Assignee: Topotarget UK LimitedInventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E S Duffy
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100261760Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: ApplicationFiled: June 22, 2010Publication date: October 14, 2010Applicant: Asterand UK LimitedInventors: Alexander William Oxford, Richard John Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Publication number: 20100216849Abstract: This invention relates to novel biphenylcarboxamides of the formula (I) in which R, Z, X, Y, m, n and A are as defined in the disclosure, to a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.Type: ApplicationFiled: April 30, 2010Publication date: August 26, 2010Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Ulrike Wachendorff-Neumann, Peter Dahmen, Peter Lösel, Karl-Heinz Kuck, Astrid Mauler-Machnik, Jörg Nico Greul
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Publication number: 20100179218Abstract: Compounds of the following formula are disclosed: Methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of treating patients by administration of the pharmaceutical compositions are disclosed.Type: ApplicationFiled: February 5, 2010Publication date: July 15, 2010Applicant: QLT Inc.Inventors: WILLIAM L. MATIER, Ghanshyam Patil
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Patent number: 7745483Abstract: Novel 2-halofuryl/thienyl-3-carboxamides of the formula (I) in which A, Hal, R, M and Z are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: January 22, 2005Date of Patent: June 29, 2010Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Peter Dahmen, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20100144785Abstract: The present invention relates N-(aromatic, 6-membered, fused, (hetero)aryl-methylene)-N-cycloalkyl carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3 and B represents an aromatic, 6-membered, fused, (hetero)aryl; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20100144817Abstract: The present invention relates to N-cycloalkyl-benzyl-thiocarboxamide or N-cycloalkyl-benzyl-N-substituted-carboximidamide amide derivatives of formula (I) wherein A represents a carbo-linked, unsaturated or partially saturated, 5-membered heterocyclyl; T represents S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl and Z2; Z3, X and n represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: June 10, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20100137336Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 10, 2008Publication date: June 3, 2010Inventor: Christelle Boléa
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Publication number: 20100130556Abstract: A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L? is a single bond, —O— or —C(?O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.Type: ApplicationFiled: August 9, 2006Publication date: May 27, 2010Applicant: ASTERAND UK LIMITEDInventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Shirley Ann Brunton, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd
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Publication number: 20100105900Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2008Publication date: April 29, 2010Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Patent number: 7670991Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I) in which Q, R1, R2, R3, R4, R5, Y and Z have one of the meanings given in the disclosure, to processes for their preparation, and to their use.Type: GrantFiled: May 3, 2002Date of Patent: March 2, 2010Assignee: Bayer CropScience AGInventors: Hans-Georg Schwarz, Klaus-Helmut Muller, Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Shinichi Narabu, Akihiko Yanagi, Shinichi Shirakura, Toshio Goto, Yoshihiro Yamaguchi
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100041715Abstract: The invention provides certain well-defined benzamides that are useful as sphingosine-1-phosphate antagonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.Type: ApplicationFiled: August 12, 2009Publication date: February 18, 2010Applicant: ALLERGAN, INC.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
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Publication number: 20100022605Abstract: Described herein are N-hydroxyamlde antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical compositions compound of Formula (I): or a salt, solvate ti hydrate thereof, wherein A is (a) eachindicates a point of attachment.Type: ApplicationFiled: December 4, 2006Publication date: January 28, 2010Inventors: Rakesh Kumar Jain, Mikhail Fedorovich Gordeev, Jason Gustaf Lewis, Charles Francavilla
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Publication number: 20090318703Abstract: A carboxylic acid derivative of formula (I): wherein R1 is —COOH, —COOR6, etc.; A is a single bond, alkylene, etc.; R2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a heterocyclic ring; Q is alkylnene-Cyc2, etc.; D is a linking chain; and R3 is alkyl, a carbocyclic ring or a heterocyclic ring, or a non-toxic salt thereof. The compound of formula (I) binds to PGE2 receptor, especially subtypes EP3 and/or EP4 and show the antagonizing activity, are useful for the prevention and/or treatment of diseases induced pain, itch, urticaria, allergy, urinary frequency, urinary disturbance, Alzheimer's disease, cancer, dysmenorrhea, endometriosis, etc.Type: ApplicationFiled: October 27, 2008Publication date: December 24, 2009Applicant: ONO PHARMACEUTICAL CO., LTDInventors: Kousuke Tani, Masaki Asada, Kaoru Kobayashi, Masami Narita, Mikio Ogawa
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Publication number: 20090298899Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: ApplicationFiled: December 30, 2008Publication date: December 3, 2009Inventors: Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Publication number: 20090258912Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: November 21, 2006Publication date: October 15, 2009Inventors: Pierre-Yves Coqueron, Darren James Mansfield, Philippe Desbordes, Heiko Rieck, Pierre Genix, Alain Villier, Marie-Claire Grosjean-Cournoyer
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Publication number: 20090215623Abstract: Novel 3-acylaminobenzanilides of the formula (I) wherein R1 represents phenyl which may be substituted or a 5-member or 6-member heterocyclic ring group, which may be substituted, containing at least one hetero-atom selected from the group consisting of N, O, and S; R2 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; R3 represents C1-6 haloalkyl, C1-6 haloalkoxy, C1-6 haloalkylthio, C1-6 haloalkylsulfinyl, or C1-6 haloalkylsulfonyl; R4 represents halogen, C1-6 alkyl, or C1-6 haloalkyl; X represents halogen, C1-6 alkyl, or C1-6 haloalkyl; and n represents 0 or 1 and the compounds are used as insecticides, and a use of the new compounds as insecticides.Type: ApplicationFiled: July 21, 2006Publication date: August 27, 2009Applicant: BAYER CROPSCIENCE AGInventors: Akihiko Yanagi, Yukiyoshi Watanabe, Katsuaki Wada, Tetsuya Murata, Jun Mihara, Katsuhiko Shibuya, Eiichi Shimojo, Akira Emoto
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Patent number: 7569602Abstract: A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii) an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.Type: GrantFiled: October 15, 2004Date of Patent: August 4, 2009Assignee: Asterand UK LimitedInventors: David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Alexander William Oxford, Richard Jon Davis, Robert Alexander Coleman, Kenneth Lyle Clark
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Publication number: 20090192172Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: December 8, 2005Publication date: July 30, 2009Applicant: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Patent number: RE43327Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.Type: GrantFiled: January 8, 2002Date of Patent: April 24, 2012Assignee: Aminex Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur