Having -c(=x)-, Wherein X Is Chalcogen Bonded Directly To The Diazole Ring Patents (Class 548/374.1)
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Patent number: 8404861Abstract: The substituted pyrazolecarboxanilide derivatives represented by of the formula (I) wherein R1 is H, alkyl, alkylcarbonyl, alkenylcarbonyl, cycloalkyl, phenylalkyl, phenylcarbonyl and the like; R2 is H, halogen, alkyl, CN, OH, alkoxy, phenoxy, phenylthio, phenylsulfonyl and the like; G is alkyl, alkenyl, alkynyl, cycloalkyl, C3-C10 cycloalkenyl and the like; Z is O or S; X is H, halogen, CN, NO2, alkyl and the like; Y1 is H, alkyl, alkenyl, phenyl, alkoxyalkyl and the like; Y2 is H, halogen, CN, NO2, OH, mercapto, amino, carboxyl, C1-C6 alkyl, phenyl, phenoxy, heterocycle and the like, m is 1 or 2; and n is 1-3, and salts thereof exhibit a superior effect as agrohorticultural insecticides or acaricides.Type: GrantFiled: August 11, 2006Date of Patent: March 26, 2013Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Hideo Kanno, Kozo Machiya, Akiyuki Suwa, Noriaki Yasokawa, Shinsuke Fujioka
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Publication number: 20130072535Abstract: Compounds of Formula (I) wherein R1 is C1-C4alkyl or C1-C4 haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4halogenalkyl; R6 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; R7 is hydrogen, halogen, C1-C6alkyl, C2-C6alkenyl, C3-C6alkinyl, C3-C6cycloalkyl-C3-C6alkinyl, halophenoxy, halophenyi, C1-C6haloalkyl, C1-C6haloakoxy, C2-C6haloalkenyl, or C2-C6haloalkenyloxy; R8 is hydrogen, halogen, C1-C4alkyl, C2-C6alkenyl or C3-C6alkinyl; with the provisio that at least one of R6, R7 and R8 is different from hydrogen; n is 0 or 1, are suitable for use as microbriocides.Type: ApplicationFiled: May 12, 2011Publication date: March 21, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Daniel Stierli, Harald Walter
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Patent number: 8399679Abstract: The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-aryl-substituted trihalomethylpyrazoles, and the further processing thereof.Type: GrantFiled: September 14, 2012Date of Patent: March 19, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui
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Publication number: 20130053416Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 26, 2012Publication date: February 28, 2013Applicant: SANOFIInventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
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Publication number: 20130053387Abstract: 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: February 28, 2013Applicant: FerroKin BioScience, Inc.Inventor: James W. Malecha
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Patent number: 8383622Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.Type: GrantFiled: May 7, 2008Date of Patent: February 26, 2013Assignee: Shionogi & Co., Ltd.Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
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Patent number: 8378114Abstract: 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: GrantFiled: March 20, 2007Date of Patent: February 19, 2013Assignee: Nihon Nohyaku Co., Ltd.Inventors: Masatsugu Oda, Yoshihiro Matsuzaki, Koji Tanaka, Eiji Takizawa, Motohiro Hasebe, Nobutaka Kuroki, Akiyuki Suwa, Kenji Oshima
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Publication number: 20130041161Abstract: The invention relates to a process for the preparation of formula (I), which process comprises a) reacting the compound (II), with cyclopentadiene to (III); b) reacting this compound in the presence of an oxidant to the compound of formula (IV); c) hydrogenating this compound in the presence of a metal catalyst and an inert solvent under hydrogen atmosphere to the compound of formula (V); d) reacting this compound in the presence of a Brönsted acid followed by a reducing agent to the compound of formula (VI); e) reacting VI with a compound (VII), in the presence of a base to a compound of formula (VIII); f) converting the compound of formula VIII in the presence of an oxidising agent to the compound of formula (IX); and g) reacting the compound of formula IX in the presence of triphenylphosphane/carbon tetrachloride or triphenylphosphane/bromotrichloromethane to the compound of formula I.Type: ApplicationFiled: April 14, 2011Publication date: February 14, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Raphael Dumeunier, Hans Tobler
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Publication number: 20130041147Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3- oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.Type: ApplicationFiled: October 17, 2012Publication date: February 14, 2013Applicant: BASF SEInventor: BASF SE
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Publication number: 20130041160Abstract: The invention relates to a process for the preparation of a compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III) reacting the halobenzyne of formula (III) so formed with (IV) wherein R1 and R2 are hydrogen or C1-C6alkyl; to (V), b) hydrogenating V in the presence of a metal catalyst to (VI), c) ozonising (VI) to (VII) d) converting (VII) in the presence of a phosphane and CCI4 or CHCI3 to (VIII) (VIII), and either e1) reacting VIII with NH3 in the presence of a catalyst to (IX) and f) reacting IX in the presence of a base with the compound of formula (X), to the compound of formula (I); or e2) reacting the compound of formula (VIII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with (Xa), to the compound of formula (I).Type: ApplicationFiled: April 14, 2011Publication date: February 14, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Florian Schleth, Thomas Vettiger, Michael Rommel, Hans Tobler
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Patent number: 8372982Abstract: 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: GrantFiled: February 16, 2010Date of Patent: February 12, 2013Assignee: Bayer Cropscience AGInventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Philippe Rinolfi, Ulrike Wachendorff-Neumann
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Publication number: 20130035496Abstract: The invention relates to a process for the preparation of the compound of formula (I), which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species in an inert atmosphere to a halobenzyne of formula (X), reacting the halobenzyne of formula X so formed with cyclopentadiene to (III), b) reacting III in the presence of an inert solvent with an oxidant to (IV), c) reacing IV in the presence of a Lewis acid and a hydride source to (V), d) reacting V in the presence of an oxidizing agent, a base and an inert solvent to (VI), e) converting VI in the presence of a phosphane and CCL4 or CHCl3 to (VII), and either f1) reacting VII with NH3 in the presence of a catalyst to the compound of formula (VIII); and g) reacting VIII in the presence of a base with a compound of formula (IX), to the compound of formula (I); or f2) reacting the compound of formula (VII), in the presence of a solvent, a base, a copper catalyst and at least one ligand with the compoundType: ApplicationFiled: April 14, 2011Publication date: February 7, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Raphael Dumeunier, Florian Schleth, Thomas Vettiger, Michael Rommel, Stephan Trah
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Publication number: 20130035495Abstract: The invention relates to a process for the preparation of formula (I) which process comprises a) reacting a compound of formula (II), wherein X is chloro or bromo, with an organometallic species to (III), wherein X is chloro or bromo; reacting the halobenzyne with a fulvene (IV), to a compound of formula (V) wherein X is chloro or bromo; b) hydrogenating V in the presence of a suitable metal catalyst to a compound of formula (VI) wherein X is chloro or bromo; and either c1) reacting the compound of formula VI with NH3 in the presence of a catalyst comprising palladium and at least one ligand to the compound of formula (VII); and d) reacting the compound of formula VII in the presence of a base with a compound of formula (VIII), to the compound of formula I; or c2 reacting the compound of formula (VI) in the presence of a copper catalyst and a ligand with the compound of formula (VIIIa), to the compound of formula (I).Type: ApplicationFiled: April 14, 2011Publication date: February 7, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Denis Gribkov, Remo Stohler, Thomas Vettiger, Michael Rommel
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Patent number: 8367715Abstract: The invention relates to pyrazole derivatives of general formula (I): in which X represents chlorine or fluorine; to a process for preparing said derivatives, and to therapeutic uses of said derivatives.Type: GrantFiled: December 23, 2011Date of Patent: February 5, 2013Assignee: SanofiInventors: Pierre Yves Abecassis, Pascal Desmazeau, Michel Tabart
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Patent number: 8367714Abstract: Compounds of the following formula: wherein X is H or substituted with with at least one X being substituted; and halo is fluorine, chlorine, bromine, iodine; and stereoisomers and conjugable analogs thereof.Type: GrantFiled: August 28, 2008Date of Patent: February 5, 2013Assignees: Vanderbilt University, University of WashingtonInventors: Darryl J. Bornhop, Mingfeng Bai, Nephi Stella, Eric Stern
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Patent number: 8362272Abstract: A process for preparing 1,3-disubstituted pyrazole compounds.Type: GrantFiled: October 28, 2010Date of Patent: January 29, 2013Assignee: BASF SEInventors: Maximilian Dochnahl, Michael Keil, Bernd Wolf
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Patent number: 8362273Abstract: Process for preparing aminale and their use for preparing 1,3-disubstituted pyrazole compounds.Type: GrantFiled: October 28, 2010Date of Patent: January 29, 2013Assignee: BASF SEInventors: Maximilian Dochnahl, Michael Keil, Roland Goetz
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Publication number: 20130023668Abstract: The present invention relates to novel processes for the production of compounds of formula wherein Hal and Hal? are independently selected from Cl and F, and R1 is selected from Cl, F and H.Type: ApplicationFiled: September 17, 2012Publication date: January 24, 2013Applicant: SYNGENTA CROP PROTECTION, LLCInventor: Syngenta Crop Protection, LLC
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Patent number: 8357634Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: GrantFiled: August 23, 2010Date of Patent: January 22, 2013Assignee: Syngenta Crop Protection LLCInventors: Harald Walter, Ramya Rajan, Daniel Stierli
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Patent number: 8357635Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: GrantFiled: October 14, 2010Date of Patent: January 22, 2013Assignee: Syngenta Crop Protection LLCInventors: Harald Walter, Daniel Stierli
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Publication number: 20130012722Abstract: The present invention relates to a process for preparing a compound of formula (II) wherein R1 is CF3, CF2H or CFH2, and R2 and R3 are both independently C1-C6 alkyl, comprising a) reacting compounds of formula (IV), (V) and (VI) wherein R3 is as defined for the compound of formula (II), R4OM (V) wherein M is a lithium, sodium or potassium ion and R4 is C1-C6 alkyl, and (VI) wherein R1 is as defined for the compound of formula (II) and R5 is CrC6 alkyl, to form an enolate of formula (VII) wherein M is as defined for the compound of formula V and R1 and R3 are defined for the compound of formula (II), b) releasing the compound of formula (VIII) wherein R1 and R3 are as defined for the compound of formula (II), from the enolate of formula (VII) by means of an acid, and c) converting the compound of formula (VIII), in the presence of the salt formed from cation M and the anion of the acid in step b), to a compound of formula (II).Type: ApplicationFiled: March 14, 2011Publication date: January 10, 2013Applicant: Syngenta Crop Protection LLCInventors: Franz Linus Zumpe, Ralf Kohlbrenner
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Publication number: 20130012715Abstract: The invention describes a novel process for synthesizing pyrazoles by means of oxidative conversion of enamines with suitable N-containing carboxylic acid derivatives.Type: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: WESTFAELISCHE WILHELMS UNIVERSITAET MUENSTERInventors: Julia Neumann, Mamta Suri, Frank Glorius
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Patent number: 8350053Abstract: The present invention relates to a process for the regioselective synthesis of 1-alkyl-3-halo-alkylpyrazole-4-carboxylic acid derivatives by cyclization of 2,3-disubstituted acrylic acid derivatives with hydrazines in the presence of carbonyl compounds.Type: GrantFiled: February 26, 2009Date of Patent: January 8, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui, Arnd Neeff
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Patent number: 8350046Abstract: A process for preparing arylcarboxamides of the formula (I) where Ar=a mono- to trisubstituted phenyl, pyridyl or pyrazolyl ring, where the substituents are selected from halogen, C1-C4-alkyl and C1-C4-haloalkyl; M=thienyl or phenyl, which may bear a halogen substituent; Q=direct bond, cyclopropylene, fused bicyclo[2.2.1]heptane or bicyclo[2.2.1]heptene ring; R1=hydrogen, halogen, C1-C6-alkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, mono- to trisubstituted phenyl, where the substituents are selected from halogen and trifluoromethylthio, or cyclopropyl; by reacting an acid chloride of the formula (II) with an arylamine (III) in a suitable nonaqueous solvent, wherein, in the absence of an auxiliary base, a) the acid chloride (II) is initially charged, b) a pressure of from 0 to 700 mbar is established, c) the arylamine (III) is metered in an approximately stoichiometric amount and d) the product of value is isolated.Type: GrantFiled: May 6, 2009Date of Patent: January 8, 2013Assignee: BASF SEInventors: Wolfgang Reichert, Christopher Koradin, Sebastian Peer Smidt, Volker Maywald, Bernd Wolf, Michael Rack, Thomas Zierke, Michael Keil
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Patent number: 8344015Abstract: 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: GrantFiled: December 8, 2005Date of Patent: January 1, 2013Assignee: 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: 8344156Abstract: A halogenating agent is added to a mixture including a base, a fluoroalkylcarboxylic acid derivative and an acrylate derivative to produce a fluoroaclyacetic acid derivative represented by the following Formula (3): wherein Rf represents a fluorine containing alkyl group, R1 and R2 represent a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, an arylalkyl group or an acyl group, or together represent an atomic group that forms a 5- or 6-membered ring containing a nitrogen atom to which R1 and R2 are bonded; R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an arylalkyl group; and R4 represents an alkyl group, a cycloalkyl group, an aryl group, or an aryl alkyl group.Type: GrantFiled: March 11, 2009Date of Patent: January 1, 2013Assignee: Mitsui Chemicals Agro, Inc.Inventors: Hideki Umetani, Takeshi Kakimoto, Yoji Aoki
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Patent number: 8343970Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Patent number: 8343976Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas Ia, Ib, IIa, and IIb) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.Type: GrantFiled: April 19, 2010Date of Patent: January 1, 2013Assignee: Institute for OneWorld HealthInventors: Stephen David Penrose, Kevin James Doyle
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Patent number: 8344157Abstract: 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: GrantFiled: July 10, 2009Date of Patent: January 1, 2013Assignee: BASF SEInventors: Bernd Wolf, Sebastian Peer Smidt, Volker Maywald, Christopher Koradin, Michael Keil, Thomas Zierke, Michael Rack
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Publication number: 20120329847Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl or C1-C4haloalkyl; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4haloalkyl; R5 is hydrogen, halogen, C1-C4alkyl or C1-C4haloalkyl; G1 is a cyclohexenyl group which is mono- or polysubstituted by substituents selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl and phenyl; said cyclohexenyl group can form together with a C1-C4 alkylene group a bicyclic system which can be mono- or poly-substituted by substituents selected from the group consisting of C1-C6alkyl, C1-C6alkoxy, C3-C6cycloalkyl and phenyl; are suitable for use as microbiocides.Type: ApplicationFiled: February 3, 2011Publication date: December 27, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Daniel Stierli, Harald Walter
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Patent number: 8334390Abstract: The present invention relates N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group; T represents O, S, N—Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl group; X represents N or a CZ7 and Z2; Z3; L1 and L2 represent various substituents; their process of preparation; preparation 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: GrantFiled: July 31, 2008Date of Patent: December 18, 2012Assignee: Bayer Cropscience AGInventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Hiroyuki Hadano, Philippe Rinolfi, Jean-Pierre Vors
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Publication number: 20120316193Abstract: The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Inventors: Megan Foley, Bradley Tait, Matthew Cullen
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Publication number: 20120316150Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1, R2, R3, R4, R5 and R6 are as defined herein: and compositions, processes for the preparation, and uses thereof, e.g. in the treatment of endometriosis or uterine fibroids.Type: ApplicationFiled: June 18, 2012Publication date: December 13, 2012Inventors: KARL RICHARD GIBSON, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Publication number: 20120308587Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Roland Gendron, Adam D. Hughes
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Patent number: 8324263Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: July 24, 2008Date of Patent: December 4, 2012Assignee: Syngenta Crop Protection, LLCInventors: Daniel Stierli, Antoine Daina, Harald Walter, Ramya Rajan, Hans Tobler
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Patent number: 8314233Abstract: The present invention relates to a process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters, 2-(aminomethylidene)-4,4-difluoro-3-oxobutteric esters of the formula (I) in which R1, R2 and R3 independently of one another are C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C3-C10-cycloalkyl or benzyl or NR2R3 is a 5- to 10-membered heterocyclic radical, to a process for preparing compounds of the formula (I) wherein an appropriate 3-aminoacrylic ester is reacted with difluoroacetyl fluoride and to the use of compounds of the formula (I) in the process for preparing difluoromethyl-substituted pyrazol-4-ylcarboxylic acids and their esters.Type: GrantFiled: April 30, 2009Date of Patent: November 20, 2012Assignee: BASF SEInventors: Thomas Zierke, Volker Maywald, Michael Rack, Sebastian Peer Smidt, Michael Keil, Bernd Wolf, Christopher Koradin
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Publication number: 20120289707Abstract: 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 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 catalyst or an antimony catalyst wherein R1, R2, R3, R4, R5, R6, R7, X, Y and Het are defined in the specification.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Martin Charles Bowden, David Anthony Jackson, Alexandre Christian Saint-Dizier, George Robert Hodges
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Patent number: 8309592Abstract: 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: GrantFiled: July 31, 2008Date of Patent: November 13, 2012Assignee: Bayer Cropscience AGInventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Jean-Pierre Vors
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Patent number: 8304444Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: June 6, 2008Date of Patent: November 6, 2012Assignee: Syngenta Crop Protection, LLCInventors: Daniel Stierli, Harald Walter, Hans Tobler
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Publication number: 20120276006Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.Type: ApplicationFiled: June 21, 2012Publication date: November 1, 2012Applicant: Lantheus Medical Imaging, Inc.Inventors: David S. Casebier, Simon P. Robinson, Ajay Purohit, Heike S. Radeke, Michael T. Azure, Douglas D. Dischino
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Patent number: 8299260Abstract: The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-aryl-substituted trihalomethylpyrazoles, and the further processing thereof.Type: GrantFiled: July 23, 2010Date of Patent: October 30, 2012Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui
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Publication number: 20120264798Abstract: This invention provides new pharmaceutically useful compounds that are prodrugs of inhibitors of plasma kallikrein and methods and compositions for preventing or treating plasma kallikrein dependent diseases or conditions, such as diabetic macular edema or hemorrhagic stroke, by administering prodrugs of the formula:Type: ApplicationFiled: April 12, 2012Publication date: October 18, 2012Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto SINHA, Tamie Jo Chilcote, Joghee Raju Suresh, Sriram Narasimhan
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Patent number: 8288419Abstract: The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: GrantFiled: December 12, 2008Date of Patent: October 16, 2012Assignee: Actelion Pharmaceuticals, LtdInventors: Daniel Bur, Oliver Corminboeuf, Sylvaine Cren, Heinz Fretz, Corinna Grisostomi, Xavier Leroy, Julien Pothier, Sylvia Richard-Bildstein
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Publication number: 20120259128Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.Type: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Tomoyuki Ogawa, Koji Masuda
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Publication number: 20120259113Abstract: 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 9, 2012Publication date: October 11, 2012Applicant: THERAVANCE, INC.Inventors: Brooke Blair, Paul R. Fatheree, Melissa Fleury, Roland Gendron, Ryan Hudson, Robert Murray McKinnell, Michael Wilson
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Patent number: 8283383Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20120252830Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 7, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Gary Mark Coppola, Yuki Iwaki, Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi, Robert Sun
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Publication number: 20120245138Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: May 2, 2012Publication date: September 27, 2012Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Patent number: 8269020Abstract: The present invention relates to novel processes for the production of compounds of formula (I) wherein Hal and Hal? are independently selected from Cl and F, and R1 is selected from Cl, F and H.Type: GrantFiled: June 16, 2008Date of Patent: September 18, 2012Assignee: Syngenta Crop Protection LLCInventors: Martin Charles Bowden, Brian David Gott, Iacob Eremia Gutu, David Anthony Jackson
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Patent number: 8258169Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: GrantFiled: December 1, 2009Date of Patent: September 4, 2012Assignee: Syngenta Crop Protection, LLCInventors: Ramya Rajan, Harald Walter, Daniel Stierli