Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Publication number: 20110301356Abstract: The present invention relates to a process for preparing 2-aminobiphenyls of the formula I in which n is 0, 1, 2 or 3, R1 is hydrogen, cyano or fluorine, and each R2 is independently selected from cyano, fluorine, C1-C4-alkyl, C1-C4-fluoroalkyl, C1-C4-alkoxy, C1-C4-fluoroalkoxy, C1-C4-alkylthio and C1-C4-fluoroalkylthio. The invention also relates to a process for preparing pyrazolecarboxamides of such 2-aminobiphenyls.Type: ApplicationFiled: February 18, 2010Publication date: December 8, 2011Applicant: BASF SEInventors: Thomas Zierke, Volker Maywald, Sebastian Peer Smidt
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Publication number: 20110301215Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: ApplicationFiled: June 6, 2011Publication date: December 8, 2011Applicant: Activesite Phamaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20110293520Abstract: The present invention relates to a compound represented by formula (E). The present invention also relates to a compound represented by the formula (E) for use in the treatment or prevention of diseases linked to protein aggregation and/or neurodegenerative diseases. Moreover, the present invention relates to pharmaceutical and diagnostic compositions comprising the compound of the invention as well as to a kit. Furthermore, the present invention relates to a method of imaging deposits of aggregated protein. A kit for preparing a detectably labelled compound of the present invention is also disclosed. Formula (E) wherein X, Y and L are independently nondirectionally selected from —C(R1)(R2)—, —C(R3)?, —N(R4)—, —N?, —N+(R5)?, —O— and —S—; M and Z are independently nondirectionally selected from formula (I) and formula (II).Type: ApplicationFiled: June 9, 2009Publication date: December 1, 2011Inventors: Armin Giese, Uwe Bertsch, Hans Kretzschmar, Mathias Habeck, Thomas Hirschberger, Paul Tavan, Christian Griesinger, Andrei Leonov, Sergey Ryazanov, Petra Weber, Markus Geissen, Martin H. Groschup, Jens Wagner
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Publication number: 20110294863Abstract: The present invention relates N-cycloalkyl-N-bicyclicmethylene-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group, T represents O or S, Z1 represents a C3-C7-cycloalkyl group, X represents N or a CZ7 and Y1, Y2, Z2, Z3, L1 and L2 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: January 27, 2010Publication date: December 1, 2011Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Pierre Genix, Benoit Hartmann
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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: 20110288305Abstract: The present invention relates to a novel process for the preparation of 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl halides and the intermediates occurring in this process, ethyl 5-chloro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylate and ethyl 5-fluoro-1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylate.Type: ApplicationFiled: April 22, 2011Publication date: November 24, 2011Applicant: Bayer CropScience AGInventors: Sergii Pazenok, Nobert Lui, Stephanie Gary
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Patent number: 8063036Abstract: Novel benzamide compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: April 7, 2010Date of Patent: November 22, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Publication number: 20110281925Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Applicant: THERAVANCE, INC.Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20110275636Abstract: Disclosed herein are new compounds of desazadesferrothiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: ApplicationFiled: May 4, 2011Publication date: November 10, 2011Applicant: FerroKin BioSciences, Inc.Inventor: James Malecha
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Patent number: 8053572Abstract: The present invention relates to a process for preparing known fungicidally effective alkylanilides from acid chlorides and aminoacetophenone via hydroxyalkyl-substituted carboxanilides, alkenylanilides and benzoxazine derivatives.Type: GrantFiled: March 1, 2006Date of Patent: November 8, 2011Assignee: Bayer CropScience AGInventor: Alexander Straub
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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: 20110263869Abstract: The present invention relates to methods of initiating a reaction represented by scheme (1), wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.Type: ApplicationFiled: December 16, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, LLCInventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
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Publication number: 20110257196Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.Type: ApplicationFiled: December 29, 2010Publication date: October 20, 2011Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. Dalton, Duane D. Miller, Charles Duke, Sunjoo Ahn
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Publication number: 20110257410Abstract: The present invention relates to methods of preparing compounds of formula (I) comprising the step of reacting the corresponding amide with the corresponding substituted aryl in the presence of a catalyst, which catalyst comprises copper and a ligand, Y is CHCHR6(R7) or C?C(A)Z, CY2(R2)Y3(R3), C?N—NR4(R5); Y2 and Y3 are, independently, O, S, N; A and Z are, independently, C1-6 alkyl; R1 is CF3 or CF2H; R2 and R3 are, independently, C1-8 alkyl, wherein R2 and R3 are optionally joined to form a 5-8 membered ring; R4 and R5 are, independently, C1-8 alkyl; B is a single bond or a double bond; R6 and R7 are, independently, hydrogen or C1-6 alkyl.Type: ApplicationFiled: December 16, 2009Publication date: October 20, 2011Applicant: SYNGENTA CROP PROTECTION, LLCInventors: George Robert Hodges, Lisa Mitchell, Alan James Robinson
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Patent number: 8030489Abstract: Provided is a compound which is useful as a therapeutic agent for chronic renal insufficiency and a therapeutic agent for diabetic nephropathy. The present inventors have made extensive studies on an ornithine derivative having an antagonistic action against an EP4 receptor, and as a result, they have found that by introducing cycloalkanediyl at a C terminal of the ornithine part of the compound of the present invention, the physicochemical properties such as solubility, and the like can be improved, thereby giving further preferred properties as a pharmaceutical. Therefore, they have completed the present invention. The compound of the present invention exhibits a good antagonistic action against an EP4 receptor, and thus, it is useful as a therapeutic agent for chronic renal insufficiency and diabetic nephropathy.Type: GrantFiled: March 25, 2008Date of Patent: October 4, 2011Assignee: Astellas Pharma Inc.Inventors: Tatsuya Zenkoh, Eisuke Nozawa, Keisuke Matsuura, Ryushi Seo
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Patent number: 8026195Abstract: The present invention relates to N-cycloalkyl-thiocarboxamide or N-cycloalkyl-N-substituted carboximidamide derivatives of formula (I) wherein A and B represent a 5-membered heterocyclyl groups, T represents an oxygen, sulphur or amino derivatives, Z1 represents a cycloalkyl group and Z2 and Z3 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: GrantFiled: July 30, 2007Date of Patent: September 27, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Arounarith Tuch
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Publication number: 20110230537Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: December 1, 2009Publication date: September 22, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ramya Rajan, Harald Walter, Daniel Stierli
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Publication number: 20110230521Abstract: Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: May 1, 2009Publication date: September 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Christian Harcken, Thomas Wai-Ho Lee, Pingrong Liu, John Lord, CAN Mao, Wang Mao, Brain Christopher Raudenbush, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer
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Patent number: 8022063Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.Type: GrantFiled: May 30, 2005Date of Patent: September 20, 2011Assignee: 7TM Pharma A/SInventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
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Publication number: 20110224273Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: September 9, 2010Publication date: September 15, 2011Applicant: AstraZeneca ABInventors: Martin John Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
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Patent number: 8017771Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.Type: GrantFiled: January 16, 2009Date of Patent: September 13, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
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Patent number: 8008232Abstract: The present invention relates to pyrazolecarboxanilides I in which the variables are as defined below: n is zero or 2; m is 2 or 3; X1 is fluorine or chlorine; X2 is halogen; Y is CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, methoxy or methylthio; p is zero or 1; R1 is fluorine, chlorine, bromine, C1-C4-alkyl or C1-C4-haloalkyl; R2 is hydrogen or halogen; R3 is hydrogen, methyl or ethyl; W is O or S; with the proviso that, if a) W=O, R1=methyl and R3 is hydrogen, R2 is not fluorine, or b) W=O, n=0, m=2, p=0, R2 and R3 are hydrogen, R1 is not trifluoromethyl or difluoromethyl, to processes for preparing these compounds, to compositions comprising them and to methods for using them for controlling harmful fungi.Type: GrantFiled: February 15, 2006Date of Patent: August 30, 2011Assignee: BASF AktiengesellschaftInventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Carsten Blettner, Wassilios Grammenos, Udo Hünger, Bernd Müller, Frank Schieweck, Anja Schwögler, Jan Klaas Lohmann, Joachim Rheinheimer, Peter Schäfer, Siegfried Strathmann, Reinhard Stierl
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Publication number: 20110207771Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: June 6, 2007Publication date: August 25, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington, Ramya Rajan
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Publication number: 20110207935Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of plasma uric acid level, prodrugs thereof, salts thereof or the like. In the formula (I), X1 and X2 represent CH or N; ring U represents aryl or heteroaryl; m represents integral number from 0 to 2; n represents integral number from 0 to 3; R1 represents a hydroxy group, amino or C1-6 alkyl; R2 represents C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or the like.Type: ApplicationFiled: October 14, 2009Publication date: August 25, 2011Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kazuo Shimizu, Masato Iizuka, Hideki Fujikura, Yasushi Takigawa, Masahiro Hiratochi
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Publication number: 20110207940Abstract: The present invention relates to a novel process for preparing 5-fluoro-1-alkyl-3-fluoroalkyl-1H-pyrazole-4-carbonyl chlorides, a useful intermediate in the manufacture of fungicides.Type: ApplicationFiled: November 19, 2010Publication date: August 25, 2011Applicant: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Marc Kosten, Guenter Bartels
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Patent number: 7994207Abstract: The present invention relates to a process for preparing fluoromethyl-substituted heterocyclic compounds of the general formula (I) in which R1 is H or F; R2 is an -[A-O]m—R3 group in which A is C2-C4-alkanediyl, R3 is C1-C4-alkyl and m is 1 or 2; by converting the corresponding chloromethyl-substituted compounds (II) in the presence of fluorinating agents, to processes for preparing the chloromethyl-substituted compounds (II), to processes for preparing amides of the general formula (IV) and to compounds of the general formulae (I) and (II).Type: GrantFiled: December 20, 2007Date of Patent: August 9, 2011Assignee: BASF SEInventors: Thomas Zierke, Michael Rack
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Patent number: 7994341Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.Type: GrantFiled: September 14, 2006Date of Patent: August 9, 2011Assignee: Syngenta LimitedInventors: Hans Tobler, Harald Walter, Josef Ehrenfreund, Camilla Corsi, Fanny Giordano, Martin Zeller, Gottfried Seifert, Shailesh Shah, Neil George, Ian Kevin Jones, Paul Edward Bonnett
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Publication number: 20110178310Abstract: The invention relates to a process for the preparation of fungicidally active compounds such as tricyclic amine derivatives (I). The process involves coupling of a carboxylic 5 acid e.g. a compound of formula (II) with an aniline, e.g. a compound of formula (III) in the presence of a boronic acid catalystor an antimony catalyst (II)(III)(I) wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.Type: ApplicationFiled: May 11, 2009Publication date: July 21, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, George Robert Hodges
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Patent number: 7981925Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: GrantFiled: August 26, 2009Date of Patent: July 19, 2011Assignee: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20110172436Abstract: The invention provides an Ethernet bridge or router comprising a network fabric adapted to provide interconnectivity to a plurality of Ethernet ports, each of the Ethernet ports being adapted to receive and/or transmit Ethernet frames, and wherein the Ethernet bridge or router further comprises an encapsulator connected to receive Ethernet Protocol Data Units from the Ethernet ports, wherein the encapsulator is operable to generate a Fabric Protocol Data Unit from a received Ethernet Protocol Data Unit, the Fabric Protocol Data Unit comprising a header portion, and a payload portion which comprises the Ethernet Protocol Data Unit concerned, and wherein the encapsulator is operable to transform Ethernet destination address information from the Ethernet Protocol Data Unit into a routing definition for the network fabric, and to include this routing definition in the header portion of the Fabric Protocol Data Unit. Also provided is a method of data delivery across a network.Type: ApplicationFiled: May 4, 2009Publication date: July 14, 2011Applicant: BASF SEInventors: Bernd Wolf, Volker Maywald, Michael Keil, Christopher Koradin, Michael Rack, Thomas Zierke, Martin Sukopp
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Patent number: 7977494Abstract: The present invention relates to a process for preparing substituted pyrazolyl chlorides by chlorinating aldehydes of the formula (II) under free-radical conditions.Type: GrantFiled: January 9, 2008Date of Patent: July 12, 2011Assignee: Bayer Cropscience AGInventors: Norbert Lui, Jens-Dietmar Heinrich, Alexander Straub, Thomas Wollner, James Mark Ford
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Publication number: 20110166343Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].Type: ApplicationFiled: March 14, 2011Publication date: July 7, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
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Publication number: 20110160165Abstract: The present invention provides compounds of Formula (I) and related methods and formulations: wherein: A represents a pyrazole ring optionally substituted by one or more R groups.Type: ApplicationFiled: March 1, 2011Publication date: June 30, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Sophie Huss, Jose M. Bueno, Jose M. Fiandor, Roger Frechette
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Patent number: 7968729Abstract: Methods useful for preparing compounds of formula I: and salts thereof are disclosed. Also disclosed are intermediates useful in the preparation of such compounds.Type: GrantFiled: March 26, 2010Date of Patent: June 28, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Mark S. Bednarz, Hugh Alfred Burgoon, Jr., Shinya Iimura, Ramanaiah C. Kanamarlapudi, Qiuling Song, Wenxue Wu, Jie Yan, Haiming Zhang
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Patent number: 7968728Abstract: The present invention relates to a novel process for preparing known fungicidally active 1,3-dimethyl-5-fluoro-1H-pyrazole-4-carboxamides from the corresponding acid fluoride and aniline derivatives in the presence of alkylpyridine derivatives as an acid acceptor.Type: GrantFiled: June 7, 2006Date of Patent: June 28, 2011Assignee: Bayer Cropscience AGInventors: Arnd Neeff, Sergiy Pazenok
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Publication number: 20110152533Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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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: 20110144153Abstract: [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.Type: ApplicationFiled: May 12, 2009Publication date: June 16, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo, Susumu Watanuki, Michihito Kageyama
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Publication number: 20110136831Abstract: An N-2-(hetero)arylethylcarboxamide derivative represented by the formula (I) wherein R1 and R2 are each independently a hydrogen atom etc., R3 and R4 are each independently a hydrogen atom etc., each Y is independently a halogen atom; a (C1-C6)alkyl group optionally substituted by halogen atom(s) etc., n is an integer of 1 to 5, A is a specific substituted cyclic group, E is C—H; C—Y (Y is as defined above); or a nitrogen atom, a salt thereof, and a pest controlling agent containing the derivative or salt as an active ingredient show superior performance as compared to the prior art technique, and are is useful particularly as plant disease controlling agents or nematocides having a broad control spectrum at a low dose.Type: ApplicationFiled: March 20, 2007Publication date: June 9, 2011Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Haseba, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Patent number: 7951833Abstract: New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: GrantFiled: February 3, 2009Date of Patent: May 31, 2011Assignee: AstraZeneca ABInventors: Gary Peter Tomkinson, Martin John Packer, James Stewart Scott, Paul Robert Owen Whittamore, Andrew Stocker
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Patent number: 7951953Abstract: This invention relates to a method for preparing a compound of Formula 1 wherein L, R1, R2 and X are as defined in the disclosure, comprising contacting a 2 pyrazoline of Formula 2 with bromine at a temperature of at least about 80° C. (Formula 1) (Formula 2). This invention also discloses preparation of a compound of Formula 3 wherein X, Z, R5, R6, R7, R8a, R8b and n are as defined in the disclosure, using a compound of Formula 1a wherein R10 is as defined in the disclosure, prepared by the aforesaid method for preparing a compound of Formula 1. (Formula 3) (Formula 4).Type: GrantFiled: March 14, 2006Date of Patent: May 31, 2011Assignee: E. I. du Pont de Nemours and CompanyInventor: Paul Joseph Fagan
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Patent number: 7951752Abstract: A compound of formula (I): F1 Het is a 5- or 6-membered heterocyclic ring containing one to three heteroatoms, each independently selected from oxygen, nitrogen and sulphur, the ring being substituted by groups R4, R5 and R6; R1 is hydrogen or halo; R2 is hydrogen or halo; R3 is optionally substituted C2-12 alkyl, optionally substituted C2-12 alkenyl, optionally substituted C2-12 alkynyl, optionally substituted C3-12 cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclyl; and R4, R5 and R6 are, independently, selected from hydrogen, halo, cyano, nitro, C1-4 haloalkyl, C1-4 alkoxyl (C(1-4) alkoxyl (C1-4) alkyl and C1-4 haloalkoxy (C1-4) alkyl, provided that at least one of R4, R5 and R6 is not hydrogen. The compounds of formula (I) have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.Type: GrantFiled: February 21, 2003Date of Patent: May 31, 2011Assignee: Syngenta Crop Protection, Inc.Inventors: Josef Ehrenfreund, Hans Tobler, Harald Walter
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Publication number: 20110124698Abstract: This invention relates to novel intermediates used in the preparation of iodopyrazolylcarboxanilides of the formula (I) in which R1, R2, R3, R4, R5, R6 and Z are as defined in the disclosure, and to the preparation of such intermediates.Type: ApplicationFiled: February 3, 2011Publication date: May 26, 2011Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
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Publication number: 20110118474Abstract: A process for preparing 1,3-disubstituted pyrazolecarboxylic esters of the formula (I) where X, Y, Z=hydrogen or halogen and R1=C1-C6-alkyl, by metering an enol ether of the formula III where R2 is C1-C6-alkyl at from (?41) to (?80)° C. into an alkyl hydrazine of the formula II H2N—NH-lower alkyl ??(II).Type: ApplicationFiled: July 10, 2009Publication date: May 19, 2011Applicant: BASF SEInventors: Bernd Wolf, Sebastian Peer Smidt, Volker Maywald, Christopher Koradin, Michael Keil, Thomes Zierke, Michael Rack
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Patent number: 7939673Abstract: The invention relates to a process for preparing 3-dihalomethylpyrazole-4-carboxylic acid derivatives of the formula (I) by reacting ?-fluoroamines of the formula (III) in the presence of Lewis acids with acrylic acid derivatives of the formula (II) to give vinamidinium salts of the formula (IV) and the subsequent reaction thereof with hydrazines, and to the vinamidinium salts of the formula (IV) themselves.Type: GrantFiled: August 22, 2007Date of Patent: May 10, 2011Assignee: Bayer CropScience AGInventors: Sergi Pazenok, Lui Norbert, Arnd Neeff
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Publication number: 20110105760Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.Type: ApplicationFiled: July 3, 2009Publication date: May 5, 2011Applicant: BASF SEInventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
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Publication number: 20110105766Abstract: A process for preparing substituted biphenyls of the formula I where R1=nitro or amino, R2=cyano, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio, n=from 0 to 3, and R3=hydrogen, cyano or halogen, which comprises reacting a halobenzene of the formula II in which Hal is chlorine or bromine, in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of the formula III where Ar is phenyl which is substituted if desired and R4 and R5 are each C1-C8-alkyl or C3-C6-cycloalkyl or together form a 2- to 7-membered bridge which may, if desired, bear a C1-C6-alkyl substituent, in a solvent or diluent, with a phenylboronic acid IVa a diphenylborinic acid IVb or a mixture of IVa and IVb.Type: ApplicationFiled: June 22, 2009Publication date: May 5, 2011Applicant: BASF SEInventors: Sebastian Peer Smidt, Volker Maywald, Kathrin Wissel-Stoll, Joachim Schmidt-Leithoff, Ansgar Gereon Altenhoff, Michael Keil
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Patent number: 7932283Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, 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: GrantFiled: April 5, 2007Date of Patent: April 26, 2011Assignee: Bayer Cropscience AGInventors: Hans-Georg Schwarz, Sandra Gassmann, Karl-Heinz Kuck, Peter Dahmen, Ulrike Wachendorff-Neumann, Stéphane Carbonne, Stéphanie Gary, Christopher Steele, Alain Villier, Jean-Pierre Vors
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Publication number: 20110092551Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: THERAVANCE, INC.Inventors: Paul ALLEGRETTI, Seok-Ki CHOI, Roland GENDRON, Paul R. FATHEREE, Keith JENDZA, Robert Murray McKINNELL, Darren McMURTRIE, Brooke OLSON
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Publication number: 20110092558Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: April 17, 2009Publication date: April 21, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, Harald Walter, Ramya Rajan