Amidine, Azomethine, Ketimine Or Oxime In Acid Moiety Patents (Class 560/35)
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Patent number: 6323366Abstract: The present invention provides a method for the preparation of a wide range of primary arylamines. The arylamines are prepared in two efficient, straightforward transformations: 1) an activated aryl group and an imine group are combined, in the presence of a transition metal catalyst, under conditions wherein the transition metal catalyst catalyzes the formation of a carbon-nitrogen bond between the activated carbon of the arene and the imine nitrogen; and 2) the resulting N-aryl imine is transformed, via any of a number of standard protocols, to the primary arylamine. The method of the invention may also be exploited in the preparation of vinylamines.Type: GrantFiled: July 24, 1998Date of Patent: November 27, 2001Assignee: Massachusetts Institute of TechnologyInventors: John P. Wolfe, Jens Ahman, Joseph P. Sadighi, Robert A. Singer, Stephen L. Buchwald
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Patent number: 6319925Abstract: Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R1 is C1-C4alkyl; R2 is hydrogen, C1-C4alkyl or cyclopropyl; and in which R3 and R4 are as defined herein, are fungicidal, acaricidal and insecticidal active ingredients for agriculture. They can be employed as formulated crop protection compositions.Type: GrantFiled: December 22, 1997Date of Patent: November 20, 2001Assignee: Bayer AktiengesellschaftInventor: Hugo Ziegler
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Patent number: 6313166Abstract: Compounds of the formula I and the isomers thereof, in which either a) X is an N atom and Y is OR11 or N(R12)R13, or b) X is CH and Y is OR11, and in which furthermore: R11 is C1-C4alkyl; R12 and R13, independenty, are hydrogen or C1-C4alkyl; A is an O atom or the group NR4; and wherein R1, R2 and R3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: June 22, 1999Date of Patent: November 6, 2001Assignee: Bayer AktiengesellschaftInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, René Zurflüh
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Patent number: 6313339Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.Type: GrantFiled: February 17, 2000Date of Patent: November 6, 2001Inventors: Ronald Ross, Jr., Duyan Vuong Nguyen, Steve Howard Shaber
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Patent number: 6313344Abstract: Compounds of formula (I), wherein either X is CH or N, Y is OR1 and Z is O, or X is N, Y is NHR8 and Z is O, S or S(═O); R1, R2 and R3 are as defined according to the specification; m is 0, 1 or 2; R5 is, for example, halogen, C1-C6alkyl, halo-C1-C6alkyl or C3-C6cycloalkyl; n is 0, 1, 2, 3 or 4; R9 is methyl, fluoromethyl or difluoromethyl; A and R7 are as defined according to the specification; D is O, S, —S(═O) or S(═O)2; G is C1-C6aalkylene; T—R6 is R6, —C(═N—O—A1—R77)—R6; —SiR14(R15)—R6; —C(═O)—R6; —C(R16)═C(R17)—R6, —C≡C—R6 or —D—R6; R6 is C1-C4alkyl or unsubstituted or substituted aryl or heteroaryl; A1 and R77 are as defined above for A and R7; L is U—R18, P(OR)vR11R12, P(S)wR11R12 or N(aryl)R13; v and w are 0 or 1; U—R18 is —C(═O)—C(═O)—R18; —C(OH)—C(OH)—R18; —C(═N&mdType: GrantFiled: May 27, 1998Date of Patent: November 6, 2001Assignee: Bayer AktiengesellschaftInventors: Stephan Trah, Henry Szczepanski, Ottmar Franz Hüter, Roger Graham Hall, Saleem Farooq, Alfons Pascual
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Patent number: 6310096Abstract: Certain cyclohexadiene derivatives are useful as pesticides. The derivatives are of the formula: wherein X is N; Y is O; S, S═O or NR5; Z is OR2, SR2, N(R3)R4; V is a direct bond or a 1 to 4 membered, saturated or unsaturated carbon chain which is unsubstituted or substituted by C1-C3alkyl, halogen, hydroxy, C1-C4alkoxy, halo-C1-C4alkoxy or oxo; W is hydrogen or C1-C6 alkyl or a group of the formula: wherein n is an integer of from 0 to 5 and each D is identical or different and represents a moiety selected from the group consisting of halogen, cyano, nitro, C1 to C12 alkyl, halo-C1 to C12 alkyl, C2 to C12 alkenyl, halo-C2 to C12 alkenyl, C2 to C12 alkynyl, halo-C2 to C12 alkynyl, C3 to C6 cycloalkyl, halo-C3 to C6 cycloalkyl, C3 to C6 cycloalkylmethyl, halo-C3 to C6 cycoloalkylmethyl, etc.Type: GrantFiled: June 1, 2000Date of Patent: October 30, 2001Assignee: Bayer AktiengesellschaftInventor: Henry Szczepanski
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Publication number: 20010031788Abstract: The present invention relates to compounds of the general formula (1) 1Type: ApplicationFiled: May 30, 2001Publication date: October 18, 2001Inventors: Andreas Schoop, Gerhard Mueller, Ulf Brueggemeier, Delf Schmidt, Beatrix Stelte-Ludwig, Joerg Keldenich
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Patent number: 6303818Abstract: The present invention relates to certain oxime ether compounds, compositions containing these compounds, and methods for controlling fungi by the use of a fungitoxic amount of the compounds or compositions.Type: GrantFiled: August 8, 2000Date of Patent: October 16, 2001Assignee: Dow AgroSciences LLCInventors: Lixin Zhang, Steven Howard Shaber
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Patent number: 6291702Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: February 8, 2000Date of Patent: September 18, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6265432Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of bums, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 11, 2000Date of Patent: July 24, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6251944Abstract: The present invention relates to a class of compounds represented by Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 integrin.Type: GrantFiled: April 8, 1999Date of Patent: June 26, 2001Assignee: G. D. Searle & CompanyInventors: Barbara B. Chen, Helen Y. Chen, Glen J. Gesicki, Richard A. Haack, James W. Malecha, Thomas D. Penning, Joseph G. Rico, Thomas E. Rogers, Peter G. Ruminski, Mark A. Russell, Stella S. Yu
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Publication number: 20010001799Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: January 12, 2001Publication date: May 24, 2001Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans P. Wessel
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Patent number: 6225499Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene. In one embodiment, the invention provides a process for preparing aminophenylacetylenes comprising reacting a N-benzylidene aminophenylhalide with a terminal acetylene in the presence of a base and the catalyst system to produce a novel N-benzylidene aminophenylacetylene, and hydrolyzing the N-benzylidene aminophenylacetylene to the aminophenylacetylene.Type: GrantFiled: July 14, 1997Date of Patent: May 1, 2001Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6225349Abstract: Hydroximic acid halides of the formula I where the substituents have the following meanings: X is NOCH3, CHOCH3 or CHCH3; Y is O or NH; R1 is halogen; R2 is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl or aryl; R3 is unsubstituted or substituted alkyl, alkoxyalkyl, cycloalkyl-alkyl, alkenyl and alkynyl, their salts, processes for their preparation, and their use.Type: GrantFiled: July 28, 1999Date of Patent: May 1, 2001Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Bernd Müller, Wassilios Grammenos, Reinhard Kirstgen, Andreas Gypser, Arne Ptock, Thomas Grote, Franz Röhl, Michael Rack, Roland Götz, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6201020Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using compounds of the formula: A is O or S; R is C1-C10 straight or branched chain alkyl, C2-C10 straight or branched chain alkenyl, C2-C10 straight or branched chain alkynyl, aryl, heteroaryl, carbocycle, or heterocycle; D is a bond, or a C1-C3 straight or branched chain alkyl, C2-C3 straight or branched chain alkenyl, C2-C3 straight or branched chain alkynyl, wherein any of the carbon atoms of said alkyl, alkenyl, or alkynyl of D are optionally replaced with oxygen, nitrogen, or sulfur; and X is aryl, heteroaryl, carbocycle, or heterocycle.Type: GrantFiled: December 31, 1998Date of Patent: March 13, 2001Assignee: Guilford Pharmaceuticals, Inc.Inventors: Jie Zhang, Larisa E. Serdyuk, Jia-He Li
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Patent number: 6197825Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.Type: GrantFiled: May 28, 1998Date of Patent: March 6, 2001Assignee: Florida International UniversityInventor: David Alan Becker
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Patent number: 6187812Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the index have the following meanings: X is oxygen or sulfur; R is hydrogen or alkyl; R1 is hydrogen or alkyl; R2 is cyano, nitro, trifluoromethyl, halogen, alkyl or alkoxy; m is 0, 1 or 2, it being possible for the R2 radicals to be different if m is 2; R3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino; R4 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, unsubstituted or substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, alkenyl, alkenyloxy, alkenylthio, alkenylamino, N-alkenyl-N-alkylamino, alkynyl, alkynyloxy, alkynylthio, alkynylamino, N-alkynyl-N-alkylamino; unsubstituted or substituted cycloalkyl, cycloalkoxy, cycloalkylthio, cycloalkylamino, N-cycloalkyl-N-alkylamino, cycloalkenyl, cycloalkenyloxy, cycloalkenylthio, cycloalkenylamino, N-cycloalkenyl-N-alkylamino, heterocyclyl, heterocyclyloxy, heterocyclyType: GrantFiled: February 3, 2000Date of Patent: February 13, 2001Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Müller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Röhl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6187816Abstract: Phenylketiminooxybenzyl compounds of the general formula I where: X is O or NH; R1 is fluorine, chlorine, alkyl, haloalkyl, alkoxy and haloalkoxy; R2 is halogen, alkyl, haloalkyl and alkoxy; R3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, cycloalkyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy or CRa═NORb (Ra=hydrogen or alkyl; Rb=alkyl, alkenyl or alkynyl); n is 1, 2 or 3, and salts thereof, processes for their preparation and their use for controlling animal pests and harmful fungi.Type: GrantFiled: September 14, 1999Date of Patent: February 13, 2001Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Hubert Sauter, Herbert Bayer, Thomas Grote, Andreas Gypser, Reinhard Kirstgen, Bernd Müller, Arne Ptock, Franz Röhl, Roland Götz, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6177462Abstract: Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Y is O, S or NR6; A is independently hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R6 is independently hydrogen or (C1-C4)alkyl; R2 is independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl; R3 is independently hydrogen or (C1-C4)alkyl; R4 and R5 is independently hydrogen, (C1-C4)alkyl, aryl, aralkyl, aryl(C2-C8)alkenyl, aryl(C2-C8)alkynyl, heterocyclic, or heterocyclic(C1-C4)alkyl wherein if one of R4 and R5 is hydrogen or (C1-C4)alkyl than the other of R4 and R5 is other than hydrogen or (C1-C4)alkyl, and its enantiomers and stereoisomers and agronomically acceptable salts.Type: GrantFiled: January 26, 1999Date of Patent: January 23, 2001Assignee: Rohm and Haas CompanyInventors: Zhang Lixin, Li Zongcheng, Li Zhinian, Zhang Hong, Liu Changling, Li Bin, Steven Howard Shaber
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Patent number: 6175034Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6169103Abstract: Fluorine-substituted biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, stromelysin-1, and collagenase-3, and for the treatment of atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, multiple sclerosis, renal disease, and other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.Type: GrantFiled: February 24, 1999Date of Patent: January 2, 2001Assignee: Warner-LambertInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6160012Abstract: Leukotriene-B.sub.4 derivatives of general formula (I), in which R.sub.1 represents H, CF.sub.3, CH.sub.2 OH, and R.sub.2 represents H or an organic acid radical; R.sup.3 symbolizes H, C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl, or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom; R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; A symbolizes a trans, trans--CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group; B symbolizes a C.sub.1 -C.sub.10 -- straight-chain or branched-chain alkylene group or group (a) or (b); D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sub.7, or together with B can also mean a direct bond; R.sub.5 and R.sub.6 are the same or different and represent H or C.sub.1 -C.sub.4 alkyl, or R.sub.6 represents H and R.sub.5 represents C.sub.1 -C.sub.15 alkanoyl or R.sub.8 represents SO.sub.2 ; R.sub.7 means H, C.sub.1 -C.sub.5 alkyl, chlorine, bromine; R.sub.Type: GrantFiled: March 27, 2000Date of Patent: December 12, 2000Assignee: Schering AktiengesellschaftInventors: Bernd Buchmann, Wolfgang Frohlich, Claudia Giesen, Hartwig Hennekes, Stefan Jaroch, Werner Skuballa
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Patent number: 6156924Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: December 5, 2000Assignee: Eli Lilly and CompanyInventors: William J. Hornback, Scott C. Mauldin, John E. Munroe
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Patent number: 6156923Abstract: The invention relates to a process for the preparation of compounds of the formula ##STR1## or, if appropriate, a tautomer thereof, in each case in the free form or in salt form, in whichA, X, Y, Z, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.9 and n are as defined in claim 1 and the C.dbd.N double bond marked with E has the E configuration, which comprisesa1) reacting either a compound of the formula (II) mentioned above with a compound of the formula (III) mentioned above, in which X.sub.1 is a leaving group, ora2) a compound of the formula (IV) mentioned above, if appropriate in the presence of a base, with a compound of the formula (V) mentioned above, orb1) reacting a compound of the formula (VI) mentioned above with a compound of the formula R.sub.7 --A--X.sub.2 (VII), in which X.sub.Type: GrantFiled: December 6, 1996Date of Patent: December 5, 2000Assignee: Novartis CorporationInventors: Saleem Farooq, Stephan Trah, Hugo Ziegler, Rene Zurfluh
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Patent number: 6150374Abstract: The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation.Type: GrantFiled: September 29, 1997Date of Patent: November 21, 2000Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6127568Abstract: Phenylacetic acid derivatives of the formula I ##STR1## where the substituents and the index have the following meanings: X is NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 and [sic] CHCH.sub.2 CH.sub.3 ;R.sup.1 is hydrogen and [sic] alkyl;R.sup.2 is cyano, nitro, trifluoromethyl, halogen, alkyl and [sic] alkoxy;m is 0, 1 or 2, it being possible for the R.sup.2 radicals to be different if m is 2;R.sup.3 is hydrogen, cyano, nitro, hydroxyl, amino, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, alkylamino or dialkylamino;R.sup.4 and R.sup.5 are as defined in the specification.Type: GrantFiled: August 18, 1998Date of Patent: October 3, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 6124356Abstract: A fungicidal compound of formula (I): or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, E is --NR.sup.1 --C(CH.sub.3).dbd.N-- or --N.dbd.C(CH.sub.3)--NR.sup.1 --, R.sup.1 is H, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or optionally substitute benzyl, R.sup.2 is H, C.sub.1-4 alkyl, halo(C.sub.1-4)alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkynyl, and R.sup.3 is optionally substituted aryl or optionally substituted heterocyclyl.Type: GrantFiled: January 6, 1999Date of Patent: September 26, 2000Assignee: Zeneca LimitedInventors: George Tseriotis, Ian Henry Aspinall, Paul Anthony Worthington
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Patent number: 6124494Abstract: The present invention provides compounds which inhibit. an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: September 26, 2000Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6124493Abstract: There is described a process for the preparation of a compound of formula I ##STR1## in which process: a) a compound of formula II ##STR2## is reacted with an organolithium compound of formula IIILi--R.sub.7 (III)b) the resulting lithium complex is reacted with a compound of formula IVY.sub.1 --CO--CO--Y.sub.1 IVto form a compound of formula V ##STR3## c) that compound is, in either order, c1) oximated with O-methylhydroxylamine; or oximated with hydroxylamine and then methylated or fluoromethylated or difluoromethylated;c2) reacted with a chloroformic acid ester.X, m, Y, R.sub.1 to R.sub.3 and R.sub.7 are as defined in the description.Type: GrantFiled: October 19, 1998Date of Patent: September 26, 2000Assignee: Novartis Finance CorporationInventors: Jean-Marie Assercq, Hans-Dieter Schneider, Albert Pfiffner, Werner Pfaff
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Patent number: 6121317Abstract: Compounds of formula (1), (Gibberellins), and their pharmaceutically acceptable derivatives to promote ulcer-healing, healing of surgical wounds or open fractures and treatment of bronchitis or thrombophlebitis in animals including humans or cultivation of skin cell lines in vitro ##STR1## wherein A is COOR, where R is hydrogen, unsubstituted or substituted C.sub.1-20 alkyl, allyl, aryl, arylalkyl, amidine, NR.sup.4 R.sup.5 or an unsaturated or saturated ring containing one or more hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur; R.sup.4 and R.sup.5 may or may not be the same, are hydrogen, or C.sub.1-20 alkyl, allyl, aryl, arylalkyl or an unsaturated or saturated ring containing one or more hetero-atoms selected from the group consisting of nitrogen and sulfur; B is hydrogen, hydroxyl, mercaptan, or halogen, or A and B together form a --CO--O-- linkage; R.sup.1 is hydrogen, hydroxyl, mercaptan, halogen, amino, azido, NR.sup.4 R.sup.5, unsubstituted or substituted C.sub.Type: GrantFiled: November 9, 1998Date of Patent: September 19, 2000Assignee: Australian Biomedical Company Pty. Ltd.Inventors: Minne Wu, David Shine Wu
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Patent number: 6118017Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.Type: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6110944Abstract: The present invention provides compounds having the structureAr.sub.1 --Q--Ar.sub.2 --O--(CH.sub.2).sub.n --Zand pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: August 29, 2000Assignee: G. D. Searle & Co.Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell
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Patent number: 6103923Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: August 15, 2000Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6103922Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: August 15, 2000Assignee: Eli Lilly and CompanyInventors: William J. Hornback, John E. Munroe
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Patent number: 6100429Abstract: This invention provides a process for preparing aminoarylacetylenes comprising reacting a N-arylmethylidene aminoarylhalide with a terminal acetylene in the presence of a base and a catalyst system comprising a palladium catalyst and a cuprous salt to produce a novel N-arylmethylidene aminoarylacetylene, and hydrolyzing the N-arylmethylidene aminoarylacetylene to the aminoarylacetylene.Type: GrantFiled: June 16, 1999Date of Patent: August 8, 2000Assignee: Catalytica Pharmaceuticals, Inc.Inventor: John M. Gruber
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Patent number: 6100426Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: August 8, 2000Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6096917Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: January 6, 1999Date of Patent: August 1, 2000Assignee: Eli Lilly and CompanyInventors: William J. Hornback, Scott C. Mauldin, John E. Munroe
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Patent number: 6080767Abstract: The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.Type: GrantFiled: June 27, 1997Date of Patent: June 27, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Scott I. Klein, Kevin R. Guertin, Alfred P. Spada
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Patent number: 6063956Abstract: Compounds with fungicidal and insecticidal properties having formula ##STR1## wherein X is N or CH; Z is O, S or NR.sub.8 ; A is hydrogen, halo, cyano, (C.sub.1 -C.sub.12)alkyl, or (C.sub.1 -C.sub.12)alkoxy; R.sub.1 and R.sub.8 are independently hydrogen or (C.sub.1 -C.sub.4)alkyl; R.sub.2 is hydrogen, (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.2 -C.sub.8)alkynyl, halo(C.sub.2 -C.sub.8)alkynyl, aryl, aralkyl, heterocyclic, heterocyclic(C.sub.1 -C.sub.4)alkyl or C(R.sub.10).dbd.N--OR.sub.9 ; R.sub.3 is hydrogen, (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, halo(C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.2 -C.sub.8)alkynyl, halo(C.sub.2 -C.sub.8)alkynyl, aryl, aralkyl, aryl(C.sub.3 -C.sub.7)cycloalkyl, heterocyclic or heterocyclic(C.sub.1 -C.sub.4)alkyl; R.sub.4 and R.sub.Type: GrantFiled: January 27, 1999Date of Patent: May 16, 2000Assignee: Rohm and Haas CompanyInventors: Ronald Ross, Steven Howard Shaber, Duyan Vuong Nguyen
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Patent number: 6043282Abstract: Azinooxime ethers of the formula I ##STR1## (X=NOCH.sub.3, CHOCH.sub.3, CHCH.sub.3 ; Y=O, NZ, where Z=H, alkyl; R.sup.1 =H, alkyl; R.sup.2 =cyano, nitro, trifluoromethyl, halogen, alkyl, alkoxy; m=0, 1, 2, it being possible for the radicals R.sup.2 to be different if m=2; R.sup.3 =H, cyano, alkyl, haloalkyl, alkoxy, cycloalkyl; R.sup.4, R.sup.5, R.sup.6 =indepedently of one another H, unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl), and their salts, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests.Type: GrantFiled: July 29, 1998Date of Patent: March 28, 2000Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Muller, Ruth Muller, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6034131Abstract: A diphenyl ether of the formula I, ##STR1## or a salt or N-oxide thereof wherein Q is C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3, C(CONH.sub.2).dbd.CHOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, C(CONHCH.sub.3).dbd.NOCH.sub.3 or N(OCH.sub.3)--CO.sub.2 CH.sub.3 ;n is 0 or 1;R.sup.1 is hydrogen or a carbon bonded organic radical;R.sup.2 is hydrogen or an organic radical bonded via C, O, S or N;x is 0, 1 or 2;R.sup.3 is cyano, nitro, halogen or an organic radical bonded via C, O, S or N; ory is 0, 1, 2 or 3;R.sup.4 is cyano, halogen, alkyl, haloalkyl or alkoxy,intermediates and processes for its preparation, and its use.Type: GrantFiled: September 3, 1998Date of Patent: March 7, 2000Assignee: BASF AktiengesellschaftInventors: Klaus Oberdorf, Wassilios Grammenos, Hubert Sauter, Thomas Grote, Bernd Muller, Reinhard Kirstgen, Herbert Bayer, Arne Ptock, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6028093Abstract: Fungicidal mixtures, comprisinga) a carbamate of the formula I ##STR1## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, and/orb) an oxime ether of the formula II, ##STR2## where the substituents have the following meanings: X is oxygen or amino;Y is CH or N;Z is oxygen, sulfur, amino or C.sub.1 -C.sub.4 -alkylaminoR' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkyl-methyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio; andc) a carbamate of the formula III(CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 CH.sub.Type: GrantFiled: October 21, 1998Date of Patent: February 22, 2000Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann, Klaus Schelberger, Maria Scherer, Dietrich Mappes, Joachim Leyendecker, Herbert Bayer, Ruth Muller
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Patent number: 6017925Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.Type: GrantFiled: January 13, 1998Date of Patent: January 25, 2000Assignee: Merck & Co., Inc.Inventor: Mark E. Duggan
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Patent number: 6013606Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.Type: GrantFiled: June 30, 1997Date of Patent: January 11, 2000Assignee: BASF AkteingesellschaftInventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schafer, Christoph-Sweder von dem Bussche-Hunnefeld, Peter Munster, Reinhard Kirstgen, Albrecht Harreus, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
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Patent number: 5994359Abstract: 2-Iminooxyphenylacetic acid derivatives ##STR1## where the substituents and the index have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3 (Ia), C(CONHCH.sub.3).dbd.NOCH.sub.3 (Ib), C(CONH.sub.2).dbd.NOCH.sub.3 (Ic), C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3 (Id) or C(CO.sub.2 CH.sub.3).dbd.CHCH.sub.3 (Ie);R.sup.2 is cyano, nitro, halogen, alkyl, haloalkyl or alkoxy;m is 0, 1 or 2;R.sup.3 is hydrogen, cyano, hydroxyl, halogen,alkyl, haloalkyl, alkoxyalkyl, alkoxy, haloalkoxy, alkylthio, cyclopropyl, alkenyl,unsubstituted or substituted aryloxyalkyl, benzyl or benzyloxy,R.sup.4 is hydrogen, cyano,unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl and hetaryl;unsubstituted or substituted alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, heterocyclyloxy, aryloxy and hetaryloxy;unsubstituted or substituted arylthio and hetarylthio;--Q--C(R.sup.5).dbd.N--Y.sup.1 --R.sup.6 or --Q--O--N.dbd.CR.sup.7 R.sup.8,R.sup.3 and R.sup.Type: GrantFiled: June 25, 1998Date of Patent: November 30, 1999Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Hubert Sauter, Reinhard Kirstgen, Herbert Bayer, Ruth Muller, Bernd Muller, Klaus Oberdorf, Wassilios Grammenos, Norbert Gotz, Michael Rack, Albrecht Harreus, Franz Rohl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann
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Patent number: 5985921Abstract: Compounds of the formula ##STR1## in which n, q, A, X, G, Y, Z, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.9 are as defined in claim 1, and, where appropriate, E/Z isomers, E/Z isomer mixtures and/or tautomers thereof, in each case in the free form or in an agrochemically suitable salt form, can be used as agrochemical active compounds and can be prepared in a manner known per se.Type: GrantFiled: December 6, 1996Date of Patent: November 16, 1999Assignee: Novartis CorporationInventors: Saleem Farooq, Stephen Trah, Hugo Ziegler, Rene Zurfluh, Alfons Pascual, Henry Szczepanski, Roger Graham Hall
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Patent number: 5981585Abstract: Compounds of the formula I ##STR1## and the isomers thereof, in which either a) X is an N atom and Y is OR.sub.11 or N(R.sub.12)R.sub.13, orb) X is CH and Y is OR.sub.11,and in which furthermore:R.sub.11 is C.sub.1 -C.sub.4 alkyl;R.sub.12 and R.sub.13, independently, are hydrogen or C.sub.1 -C.sub.4 alkyl;A is an O atom or the group NR.sub.4 ; and whereinR.sub.1, R.sub.2 and R.sub.3 are as defined herein, are pesticidal active ingredients. They can be used for pest control, in particular as microbicides, insecticides and acaricides in agriculture, horticulture and in the hygiene sector.Type: GrantFiled: November 12, 1997Date of Patent: November 9, 1999Assignee: Novartis Finance CorporationInventors: Hugo Ziegler, Stephan Trah, Saleem Farooq, Rene Zurfluh
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Patent number: 5981581Abstract: Phenylacetic acid derivatives of the formula I ##STR1##Type: GrantFiled: January 29, 1998Date of Patent: November 9, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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Patent number: RE37438Abstract: A class of acetamidine derivatives of general formula (I) wherein R1 is hydrogen, C1-6 hydrocarbyl group optionally substituted by halo, halo, nitro, cyano or a group XR3 wherein X is oxygen, C(O)m wherein m is 1 or 2, S(O)n wherein n is 0, 1 or 2, or a group NR4 wherein R4 is hydrogen or C1-6 alkyl; and R3 is hydrogen, C1-6 alkyl, or a group NR5R6 wherein R5 and R6 are independently hydrogen or C1-6 alkyl, provided that R3 is not NR5R6 when X is oxygen or S(O)n; R1a and R1b are independently selected from hydrogen and halo; R2 is a C1-14 hydrocarbyl group which may optionally contain one or two heteroatoms, the group R2 being optionally substituted by one or more groups independently selected from halo; N3; nitro; CF3; ZR7 wherein Z is oxygen, C(O)m′ wherein m′ is 1 or 2, S(O)n′ wherein n′ is 0, 1 or 2, or a group NR8 wherein R8 is hydrogen or C1-6 alkyl and R7 is hydrogen, C1-6 alkyl or a group NR9R10 wherein R9 and R10 are independently hydrogen or C1-6 alkyl; or RType: GrantFiled: May 4, 1999Date of Patent: November 6, 2001Assignee: Glaxo Wellcome Inc.Inventors: Jeffrey Alan Oplinger, Edward Patrick Garvey, Eric Steven Furfine, Barry George Shearer, Jon Loren Collins