Boron Or Silicon Containing Patents (Class 544/229)
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Patent number: 4851028Abstract: A method of combating undesirable plant growth and of regulating plant growth, which comprises allowing a herbicidal or plant-regulating amount of a compound of the formula I ##STR1## in which R.sub.1 is SR.sub.2 ; OR.sub.2 ; O--CHR.sub.10 R.sub.2 ; N(R.sub.3) (CHR.sub.10 R.sub.4); N(R.sub.11)(CHR.sub.10 R.sub.4) or NR.sub.3 R.sub.4 ; R.sub.2 is optionally substituted C.sub.1 -C.sub.10 -alkyl C.sub.1 -C.sub.4 -haloalkyl; C.sub.3 -C.sub.8 -alkenyl; (3-methyloxetan-3-yl)methyl; C.sub.3 -C.sub.8 -alkynyl; or an optionally substituted radical from the group comprising phenyl, benzyl, C.sub.3 -C.sub.7 -cycloalkyl, furanyl or furfuryl R.sub.3 and R.sub.4 independently of one another are hydrogen; an optionally substituted phenyl or benzyl radical; C.sub.1 -C.sub.8 -alkyl; or C.sub.3 -C.sub.6 -cycloalkyl; or R.sub.3 and R.sub.Type: GrantFiled: September 2, 1987Date of Patent: July 25, 1989Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler, Hans-Georg Brunner
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Patent number: 4849009Abstract: 2-Arylmethyliminopyrazines of the formula I ##STR1## in which R.sub.1 is SR.sub.2 ; OR.sub.2 ; O--CHR.sub.10 R.sub.2 ; N(R.sub.3)(CHR.sub.10 R.sub.4); N(R.sub.11)(CHR.sub.10 R.sub.4) or NR.sub.3 R.sub.4 ; R.sub.2 is C.sub.1 -C.sub.10 - alkyl which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.4 -alkoxycarbonyl, mercaptoalkoxy, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylcarbonyl, mono- or di-C.sub.1 -C.sub.4 -alkylamino, C.sub.1 -C.sub.4 -haloalkoxy, tri-(C.sub.1 -C.sub.4 -alkoxy)-silyl, cyano, nitro or phenyl; C.sub.1 -C.sub.4 -haloalkyl; C.sub.3 -C.sub.8 -alkenyl; (3-methyl-oxetan-3-yl)methyl; C.sub.3 -C.sub.8 -alkynyl; or a radical from the group comprising phenyl, benzyl, C.sub.3 -C.sub.7 -cycloalkyl, furanyl or furfuryl which is unsubstituted or mono-, di- or trisubstituted by identical or different substituents from the group comprising halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylcarbonyl, nitro, C.sub.1 -C.sub.4 -alkoxy and C.sub.1 -C.sub.4 -haloalkyl; R.sub.Type: GrantFiled: September 2, 1987Date of Patent: July 18, 1989Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
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Patent number: 4845237Abstract: A novel acylation process using an alkali metal bromide and a dialkylaminopyridine to form a sterically hindered ester functionality from an alkanoyl chloride and an alcohol is disclosed.Type: GrantFiled: April 15, 1987Date of Patent: July 4, 1989Assignee: Merck & Co., Inc.Inventors: Ann E. DeCamp, Leonard M. Weinstock, Thomas R. Verhoeven
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Patent number: 4845258Abstract: Quinones may be perfluoroalkylated by means of perfluoroalkyltrihydrocarbyl silane using quaternary ammonium bifluorides, quaternary phosphonium bifluorides or alkali metal bifluorides as catalysts. The reaction--which is conducted under essentially anhydrous conditions, preferably in a suitable liquid phase reaction medium, most preferably a dipolar aprotic solvent--results in the formation of gem-disubstituted cyclohexadienones in which the gem substituents are a perfluoroalkyl group and a trihydrocarbylsiloxy group. These gem-disubstituted compounds in turn can be readily converted to perfluoroalkyl substituted aromatics, thus circumventing the traditional need for photochlorination followed by halogen exchange using hydrogen fluoride as a means of preparing perfluoroalkyl aromatic compounds.Type: GrantFiled: April 4, 1988Date of Patent: July 4, 1989Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 4831037Abstract: N-[4-(N'-[2-amino-4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylme thyl]-N'-acylamino)benzoyl]-L-glutamic acid derivatives are antineoplastic agents. The compounds are prepared through acylation of the corresponding N'-amino compound or hydrolysis of a protected N'-acylamino compound. A typical embodiment is N-[4-(N'-[2-amino-4(3H)-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylm ethyl]-N'-formylamino)benzoyl]-L-glutamic acid.Type: GrantFiled: April 20, 1987Date of Patent: May 16, 1989Assignee: The Trustees of Princeton UniversityInventors: Edward C. Taylor, George P. Beardsley, James M. Hamby
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Patent number: 4812458Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is halogen, CN, CF.sub.3, ethynyl, or N.sub.3 andR.sup.2 is SO.sub.2 C.sub.1-3 -alkyl, CF.sub.3, NO.sub.2, ethynyl, or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.Type: GrantFiled: September 2, 1987Date of Patent: March 14, 1989Assignee: A/S FerrosanInventors: Tage Honore, Jorgen Drejer, Poul Jacobsen, Flemming E. Nielsen
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Patent number: 4804772Abstract: Quinones may be perfluoroalkylated by means of perfluoroalkyltrihydrocarbyl silane using certain active alkali metal salt catalysts devoid of fluorine (e.g., LiN.sub.3, NaN.sub.3, KN.sub.3, NaCN KCN, CsCN, NaOH, KOH, K.sub.2 CO.sub.3, and Cs.sub.2 CO.sub.3). The reaction--which is conducted under essentially anhydrous conditions, preferably in a suitable liquid phase reaction medium, most preferably a dipolar aprotic solvent--results in the formation of gem-disubstituted cyclohexadienones in which the gem substituents are a perfluoroalkyl group and a trihydrocarbylsiloxy group. These gem-disubstituted compounds in turn can be readily converted to perfluoroalkyl substituted aromatics, thus circumventing the traditional need for photochlorination followed by halogen exchange using hydrogen fluoride as a means of preparing perfluoroalkyl aromatic compounds.Type: GrantFiled: April 4, 1988Date of Patent: February 14, 1989Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 4804774Abstract: Quinones may be perfluoroalkylated by means of perfluoroalkyltrihydrocarbyl silane using trialkylphosphites or hexahydrocarbylphosphorous triamides, or both as catalysts. The reaction --which is conducted under essentially anhydrous conditions, preferably in a suitable liquid phase reaction medium, most preferably a dipolar aprotic solvent--results in the formation of gem-disubstituted cyclohexadienones in which the gem substituents are a perfluoroalkyl group and a trihydrocarbylsiloxy group. These gem-disubstituted compounds in turn can be readily converted to perfluoroalkyl substituted aromatics, thus circumventing the traditional need for photochlorination followed by halogen exchange using hydrogen fluoride as a means of preparing perfluoroalkyl aromatic compounds.Type: GrantFiled: April 4, 1988Date of Patent: February 14, 1989Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 4804773Abstract: Quinones may be perfluoroalkylated by means of perfluoroalkyltrihydrocarbyl silane using an aminopyridine as catalyst. The reaction--which is conducted under essentially anhydrous conditions, preferably in a suitable liquid phase reaction medium, most preferably a dipolar aprotic solvent--results in the formation of gem-disubstituted cyclohexadienones in which the gem substituents are a perfluoroalkyl group and a trihydrocarbylsilyloxy group. These gem-disubstituted compounds in turn can be readily converted to perfluoroalkyl substituted aromatics, thus circumventing the traditional need for photochlorination followed by halogen exchange using hydrogen fluoride as a means of preparing perfluoroalkyl aromatic compounds.Type: GrantFiled: April 4, 1988Date of Patent: February 14, 1989Assignee: Ethyl CorporationInventor: G. Patrick Stahly
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Patent number: 4795815Abstract: 1,2,4-Trisubstituted diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds.Type: GrantFiled: October 29, 1987Date of Patent: January 3, 1989Assignee: Eli Lilly and CompanyInventor: Robert J. Ternansky
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Patent number: 4791110Abstract: Plants are protected from the damaging effects of Phycomycetous fungi by a series of pyridazines of formula ##STR1## wherein R.sup.3 is chloro, bromo, methyl, cyano or iodo;R is chloro, bromo, iodo, methyl, cyano or furan-2-ylmethoxy;R.sup.1 is hydrogen, methyl, ethyl or n-propyl;R.sup.2 is ##STR2## X is fluoro, chloro, bromo or iodo; X.sup.1 and X.sup.2 independently represent X or hydrogen, provided that no more than one of X.sup.1 and X.sup.2 is hydrogen;R.sup.4 is hydrogen, chloro, bromo, methyl or ethyl;R.sup.5 is hydrogen, chloro, methyl, ethyl, chloromethyl or dichloromethyl;or R.sup.4 and R.sup.5 combine with the group to which they are attached to form a C.sub.3 -C.sub.7 cycloalkyl group substituted with a R.sup.1 group;R.sup.6 is hydrogen, chloro, bromo, methyl or ethyl;R.sup.7 is hydrogen, methyl, ethyl, chloromethyl or dichloromethyl;one of m and n is 0 or 1, and the other is 0;p is 0-4.Type: GrantFiled: May 5, 1986Date of Patent: December 13, 1988Assignee: Eli Lilly and CompanyInventors: Wendell R. Arnold, William C. Dow, George W. Johnson
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Patent number: 4783459Abstract: There are described new pyrimidine derivatives of the general formula I ##STR1## in which n is 0, 1 or 2;R.sub.1 is(a) the group --CXR.sub.5, where X is oxygen or sulphur and R.sub.5 is hydrogen, a nitrogen or sulphur containing heterocyclic group, which can contain other hetero atoms, optionally substituted alkenyl, acyl, alkoxycarbonyl, alkyl substituted by aryloxy, or optionally substituted mono- or dialkylamino; or R.sub.5 is the group --NHR.sub.6, where R.sub.6 is substituted amino, substituted carbamoyl, optionally substituted alkylsulphonyl, acyl or arylsulphonyl, and when n is 0 or when X is sulphur, R.sub.5 can also be alkyl, haloalkyl, aryl, aralkyl, alkoxycarbonylalkyl or arylamino;(b) cyano or the group --CXYR.sub.7, where X and Y are the same or different and are oxygen, sulphur or optionally substituted imino and R.sub.Type: GrantFiled: April 23, 1987Date of Patent: November 8, 1988Assignee: Schering Agrochemicals Ltd.Inventors: Ulrich Buhmann, Jurgen Westermann, Dietrich Baumert, Ernst Pieroh, Geoffrey R. Cliff, Ian C. Richards
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Patent number: 4778797Abstract: Novel organo-silicone compounds represented by the formula, ##STR1## wherein R is hydrogen, halogen or alkyl group, R.sup.1, R.sup.2 and R.sup.3 are alkyl group, alkoxy group, phenyl radical, substituted phenyl radical, alkylcarbonyloxy group, or trialkylsilyloxy group, respectively, R.sup.4 is hydrogen, alkyl or alkenyl grup, and m and n are an integer, respectively but those do not represent same integer of 2, when all of R.sup.1, R.sup.2 and R.sup.3 represents methyl radical, a process for the manufacture of the compounds, and an anti-tumor agent which comprises as an effective component, at least one of the compounds.Type: GrantFiled: September 9, 1985Date of Patent: October 18, 1988Assignees: Sanwa Kagaku Kenkyusho Co., Ltd., Shin-Etsu Chemical Co., Ltd.Inventors: Shigeshi Toyoshima, Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Koichi Ito
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Patent number: 4775754Abstract: Oxazine, thiazine and diazine leuco dyes are synthesized through a reaction using a dicyclohexylcarbodiimide adduct. The adducts are themselves novel compounds.Type: GrantFiled: October 7, 1987Date of Patent: October 4, 1988Assignee: Minnesota Mining and Manufacturing CompanyInventors: Kim M. Vogel, Roger A. Mader
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Patent number: 4772698Abstract: Process for producing molded polyurethane parts using as internal release agents, compounds of the general formula ##STR1## in amounts of 0.5 to 10 weight percent, based on the reaction formulation, in which at least one R.sup.2 radical in the average molecule represents ##STR2## R.sup.3 is a divalent hydrocarbon radical with 2 to 4 carbon atoms and R.sup.4, R.sup.5 are univalent hydrocarbon radicals or together are part of a morpholine or a piperazine ring. The molded polyurethane parts can be removed from the mold using significantly lower tensional forces without residues being built up on the mold.Type: GrantFiled: June 24, 1987Date of Patent: September 20, 1988Assignee: Th. Goldschmidt AGInventors: Helmut Lammerting, Hans-Joachim Kollmeier
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Patent number: 4769060Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.Type: GrantFiled: February 18, 1987Date of Patent: September 6, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
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Patent number: 4767443Abstract: There are described novel, microbicidally active 5-(arylmethylimino)-pyrimidines of the formula I ##STR1## wherein R.sub.n --A-- is an unsubstituted or substituted phenyl, naphthyl, biphenyl, phenoxyphenyl or phenylthiophenyl, and R.sub.1 is an ether, thioether or amino function, these substances being produced according to the invention by substitution of the halogen atom in the claimed intermediates of the formula II ##STR2## The use of these substances in plant protection, and also further important intermediates, are likewise described.Type: GrantFiled: September 13, 1985Date of Patent: August 30, 1988Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
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Patent number: 4762835Abstract: A compound of formula: ##STR1## wherein R.sup.1 represents hydrogen or halogen, R.sup.2 represents an .alpha.-branched alkyl or a cycloalkyl group containing from 3 to 6 carbon atoms, Q represents hydroxy, halo, alkoxy of up to 6 carbon atoms or a group --OR where R represents the residue of an alcohol of formula ROH which forms an insecticidal ester when combined with crysanthemic acid, or 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylic acid, or 3-(2-chloro-3,3,3-trifluoroprop-1-en-1-yl)-2,2-dimethylcyclopropane carboxylic acid. The compounds are useful for combating insect and acarime pests.Type: GrantFiled: December 16, 1986Date of Patent: August 9, 1988Assignee: Imperial Chemical Industries PLCInventors: Alan J. Whittle, Roger Salmon, Edward McDonald
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Patent number: 4752322Abstract: This invention relates to herbicidally active sulfonylurea compounds, agriculturally suitable compositions thereof and their method of use as herbicides or plant growth regulants.Type: GrantFiled: November 4, 1986Date of Patent: June 21, 1988Inventors: Donald J. Dumas, Marcus P. Moon
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Patent number: 4751017Abstract: Heterocyclic boron compounds of the formula IR.sup.1 --A.sup.1 --Z.sup.1 --A.sup.2 --R.sup.2 (I)can be used as components of liquid-crystal phases. A.sup.1 is --A--, --A.sup.4 --A--, or --A--A.sup.4 -- and A is ##STR1## .Type: GrantFiled: March 24, 1986Date of Patent: June 14, 1988Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Andreas Wachtler, Joachim Krause, Rudolf Eidenschink, Jurgen Eichler, Bernhard Scheuble
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Patent number: 4743602Abstract: According to the invention there are provided compounds useful for combatting fungi having the general formula (I): ##STR1## and stereoisomers thereof, wherein one of X and Y, but not both, is a group of the formula (II): ##STR2## and the other of X and Y is a hydrogen atom, a halogen atom, or an alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy or haloalkyl group or a ##STR3## group wherein R.sup.9, R.sup.10 and R.sup.11 can be alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, Z is an oxygen atom, a sulphur atom or an --NH-group, A and B have the same significance as X or Y excluding a group of formula (II), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent a hydrogen atom, a halogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 and R.sup.6 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 and R.sup.8 each represent an alkyl group containing from 1 to 4 carbon atoms or R.sup.7 and R.sup.Type: GrantFiled: June 30, 1987Date of Patent: May 10, 1988Assignee: Imperial Chemical Industries PLCInventors: Paul A. Worthington, Vivienne M. Anthony
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Patent number: 4737184Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4723987Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1986Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary A. Hanagan
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Patent number: 4719214Abstract: There are disclosed compounds having the formula: ##STR1## wherein R is a group having the formula --C.tbd.CSi(CH.sub.3).sub.3, --C.tbd.CH, --CH.dbd.CH.sub.2, --CH.sub.2 CH.sub.2 Si(CH.sub.3).sub.3 or --CH.sub.2 X; X is bromo, chloro or iodo; and R' is hydrogen or an acyl group, with the proviso that when R is --CH.sub.2 X, R' is an acyl group. Certain of these compounds are active in inhibiting the replication of DNA viruses. Other of these compounds are useful as intermediates in the production of compounds which are active in inhibiting the replication of DNA viruses.Type: GrantFiled: July 25, 1985Date of Patent: January 12, 1988Assignee: Southern Research InstituteInventors: Y. Fulmer Shealy, C. Allen O'Dell
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Patent number: 4697009Abstract: The invention is directed to N-silylpropyl-N'-acyl ureas and their production from an alkali cyanate, a 3-halopropylsilane and in a given case, a cyclic acidamide. By heating the compounds of the invention the blocked isocyanate function can be set free.Type: GrantFiled: June 18, 1986Date of Patent: September 29, 1987Assignee: Degussa AktiengesellschaftInventors: Ulrich Deschler, Peter Kleinschmit, Rudolf Michel
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Patent number: 4678498Abstract: Novel compounds of Formula I are useful as herbicides and plant growth regulants.Type: GrantFiled: May 12, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Steven P. Artz
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Patent number: 4670422Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: March 27, 1986Date of Patent: June 2, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Donald S. Karanewsky, Tamara Dejneka
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Patent number: 4650868Abstract: 7-Deazapurine derivatives of the formula: ##STR1## wherein R.sup.1 is phenyl which has, at the ortho position and/or para position as substituents, at least one group represented by the formula --O--R.sup.3, --S--R.sup.4 or ##STR2## (wherein R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different and each is hydrogen or an alkyl or phenyl group which may be substituted, whereby R.sup.5 and R.sup.6, together with the adjacent nitrogen atom, may form a cyclic amino group which may be substituted, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each may represent a protective group), and may have a group or groups with a molecular weight of up to about 200 as a substituent at any position other than those having the said substituents introduced; R.sup.2 is an amino group which may be protected, or its salt, have a potent antitumor activity, and hence the compounds are useful as an antitumor agent.Type: GrantFiled: May 1, 1985Date of Patent: March 17, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Susumu Nishimura, Hiroaki Nomura, Hiroshi Akimoto
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Patent number: 4638004Abstract: Plant growth-regulating and fungicidally active novel substituted phenylsulphonylureas of the formula ##STR1## in which R is hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or nitro,Y is oxygen or sulphur,Het is ##STR2## T is --X--CH.sub.2 --Si(CH.sub.3).sub.3, or ##STR3## or, if Het is ##STR4## can also be ##STR5## --O--CH.sub.2 --CN or --O--CH.sub.2 --CO--CH.sub.3, E is nitrogen or CH,R.sup.1 and R.sup.2 each independently is alkyl, alkoxy, or alkoxyalkyl,X is oxygen, sulphur, the sulphinyl group or the sulphonyl group,X' is hydrogen or alkyl andR.sup.3 is hydrogen, alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl or optionally substituted aralkyl.Type: GrantFiled: May 15, 1985Date of Patent: January 20, 1987Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Heinz-Jurgen Wroblowsky, Robert R. Schmidt, Hans-Joachim Santel, Gerd Hanssler, Klaus Lurssen
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Patent number: 4628048Abstract: Organosilyl compounds of the general formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are alkyl, substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or substituted aryl, R.sup.4 and R.sup.5 are alkyl or hydrogen and Y is CH.sub.2, oxygen, nitrogen or alkyl-substituted nitrogen, their salts and fungicides containing these compounds.Type: GrantFiled: March 18, 1986Date of Patent: December 9, 1986Assignee: BASF AktiengesellschaftInventors: Rolf-Dieter Acker, Ernst Buschmann, Ernst-Heinrich Pommer, Eberhard Ammermann
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Patent number: 4587247Abstract: Novel substituted and unsubstituted 13-(alkoxy)methoxy derivatives of the avermectin aglycones are useful as anthelmintic and antiparasitic agents. The compounds are also useful as pesticides and insecticides against agricultural pests. Included herein are novel intermediates useful in the process for preparing said avermectin aglycone derivatives. Compositions of said derivatives and methods of administering said compositions are also disclosed.Type: GrantFiled: February 25, 1985Date of Patent: May 6, 1986Assignee: Merck & Co., Inc.Inventors: Bruce O. Linn, Helmut H. Mrozik
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Patent number: 4562185Abstract: The present invention relates to combating pests with five-membered nitrogen-containing heterocyclic compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in the description. Many of the compounds are new.Type: GrantFiled: March 15, 1984Date of Patent: December 31, 1985Assignee: Bayer AktiengesellschaftInventors: Gerhard Jager, Rudolf Fauss, Kurt Findeisen, Benedikt Becker, Bernhard Homeyer
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Patent number: 4560508Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.Type: GrantFiled: December 20, 1982Date of Patent: December 24, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, deceased, Michihiko Ochiai, Shoji Kishimoto
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Patent number: 4556649Abstract: Insecticidally active novel substituted malonic acid diamide insecticides of the formula ##STR1## wherein R.sup.1 represents aryl or heteroaryl, each of which can optionally be substituted,R.sup.2 represents hydrogen or trialkylsilyl, and represents alkyl, cycloalkyl, alkenyl, alkinyl, aralkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphenyl, arylsulphenyl, alkylsulphonyl, arylsulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, arylaminosulphonyl or arylalkylaminosulphonyl, each of which can optionally be substituted, and represents radicals of the formula--CO--NR.sup.5 R.sup.6whereinR.sup.5 and R.sup.6 independently of one another represent hydrogen, alkyl, cycloalkyl, aryl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphonyl or arylsulphonyl, it being possible for these radicals to be optionally substituted,R.sup.3 represents hydrogen or the radical R.sup.4,R.sup.7 and R.sup.Type: GrantFiled: December 21, 1984Date of Patent: December 3, 1985Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
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Patent number: 4550105Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.Type: GrantFiled: December 3, 1981Date of Patent: October 29, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Shoji Kishimoto, Michihiko Ochiai
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Patent number: 4543412Abstract: Phenobarbital conjugates for use as enzyme inhibitors having the formula: ##STR1## wherein Z is a biologically compatible counter ion, n and m is an integer from 2 to 6 and R and R.sub.1 are each lower alkyl.Type: GrantFiled: November 4, 1983Date of Patent: September 24, 1985Assignee: Abbott LaboratoriesInventors: Charles A. Flentge, Thomas R. Herrin
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Patent number: 4524147Abstract: Disclosed are uracil derivatives having the general formula ##STR1## where R represents a hydrogen atom or an alkyl radical having 1 to 4 carbon atoms. Also disclosed are a process for preparing these compounds and pharmaceutical compositions having immunomodulatory activity which comprise these compounds as the active ingredient.Type: GrantFiled: November 16, 1982Date of Patent: June 18, 1985Assignee: Mitsui Toatsu Chemicals, IncorporatedInventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Akira Awaya
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Patent number: 4483988Abstract: Novel analgesic and antipsychotic agents having the formula ##STR1## in which R.sub.1 is hydrogen, hydroxy or halogen and R.sub.4 is hydrogen or, R.sub.1 and R.sub.4 are both hydroxy; Z is hydrogen or straight chain lower alkyl having from 1 to 4 carbon atoms and X is methylene, carbonyl, hydroxymethylene, thio, sulfinyl or sulfonyl, or Z and X, taken together, are methylidenyl, with the proviso that when X is sulfonyl or sulfinyl, Z is other than hydrogen; R.sub.5 is hydrogen or halogen, and R.sub.2 is H, a straight or branched lower alkyl group having from 1 to 4 carbon atoms, the group ##STR2## or the group ##STR3## wherein R.sub.3 is hydroxy, amino, alkylamino or dialkylamino wherein the alkyl moiety is straight or branched and has from 1 to 4 carbon atoms, diastereomers, enantiomers and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 19, 1982Date of Patent: November 20, 1984Assignee: Richardson Merrell Inc.Inventors: Albert A. Carr, Robert A. Farr, John M. Kane
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Patent number: 4460587Abstract: 5-Diazacycloalkylimidazo[1,2-c][1,3]benzodiazepines, for example compounds of the formula ##STR1## in which e.g., R.sub.1, R.sub.2 and R.sub.4 are hydrogen, R.sub.3 is methyl and C.sub.n H.sub.2n is CH.sub.2 CH.sub.2, have neuroleptic and/or antihistaminic activity. The synthesis, pharmaceutical compositions and methods of treatment utilizing such compounds are described.Type: GrantFiled: November 29, 1982Date of Patent: July 17, 1984Assignee: Ciba-Geigy CorporationInventor: Isidoros Vlattas
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Patent number: 4451652Abstract: The present disclosure relates to a novel class of substituted theophylline salts useful as reagents in an irreversible enzyme inhibitor immunoassay for theophylline. The use of such reagents increases the sensitivity of the theophylline assay.Type: GrantFiled: May 24, 1982Date of Patent: May 29, 1984Assignee: Abbott LaboratoriesInventors: Charles A. Flentge, Curtis L. Kirkemo
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Patent number: 4394505Abstract: Novel 5-fluorouracil derivatives of the following general formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.10 aralkyl, C.sub.1 -C.sub.12 alkanoyl, C.sub.2 -C.sub.6 alkoxycarbonyl, C.sub.1 -C.sub.5 alkanoyloxymethyl, carbamoyl or tri-C.sub.1 -C.sub.5 alkylsilyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.10 aralkyl;X is hydrogen, halogen or C.sub.2 -C.sub.6 alkoxycarbonyl;Y is O, NR' (R' is hydrogen or C.sub.1 -C.sub.5 alkyl), S, SO or SO.sub.2 ; andn is an integer of 1-3.which are orally administrable anti-tumor agents.Type: GrantFiled: April 16, 1982Date of Patent: July 19, 1983Assignee: Shionogi & Co., Ltd.Inventors: Susumu Kamata, Wataru Nagata
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Patent number: 4336188Abstract: A method is disclosed for preparing functionalized adenine derivatives, said method comprising the step of reacting a compound which contains an adenine nucleus which has been halogen substituted in the 8-position, with a compound having the general formula M.sup.+- S--(CH.sub.2).sub.n --COO.sup.- M.sup.+ wherein M.sup.+ is the ion of an alkali metal and n is an integer, the reaction being carried out in a polar aprotic solvent. Procedures for preparing macromolecularized adenine compounds are also indicated by reacting a functionalized adenine derivative with a polymer which has at least one primary or secondary aminic group in its structure. This is a division of application Ser. No. 705,012 filed July 14, 1976, U.S. Pat. No. 4,091,203.Type: GrantFiled: February 22, 1978Date of Patent: June 22, 1982Assignee: Snamprogetti, S.p.A.Inventors: Piergiorgio Zappelli, Antonio Rossodivita, Rosario Pappa, Luciano Re
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Patent number: 4329460Abstract: New derivatives of the formula: ##STR1## (wherein X is O or NH; R.sub.1 is --OH which may optionally be etherified or esterified, etherified mercapto or --NH.sub.2 which may optionally be substituted; R.sub.2 and R.sub.3, respectively, mean H, lower alkyl or ##STR2## and Y is an esterified or amidated carboxyl group, or CN). These derivatives are produced, by fluorination of corresponding 1,2,3,4-tetrahydro-2,4-dioxopyrimidine compounds and can be converted into 5-fluorouracil derivatives under hydrolytic conditions. The new derivatives are able to prolong the lives of animals having carcinomas or have antiviral activity.Type: GrantFiled: June 13, 1979Date of Patent: May 11, 1982Assignee: Takeda Chemical Industries, Ltd.Inventors: Osamu Miyashita, Koichi Matsumura, Hiroshi Shimadzu, Naoto Hashimoto
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Patent number: 4311839Abstract: In one aspect, this invention relates to a method of synthesizing certain 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]isothiazole-1,1-dioxides (and -2,3-dihydronaphtho[1,8-de]-1,2-thiazine-1,1-dioxides) by reacting (a) a 3-(4'-OP-carbocyclic aryl)-benz[d]isothiazole-1,1-dioxide wherein P is a protecting group or a 3-(4'-OP-carbocyclic aryl)-naphtho[1,8-de]-1,2-thiazine-1,1-dioxide wherein P is a protecting group and (b) a carbocyclic aryllithium compound to give (c) the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydrobenz[d]-isothiazole-1,1-dioxide or the corresponding 3-(4'-OP-carbocyclic aryl)-3-(carbocyclic aryl)-2,3-dihydronaphtho-[1,8-de]-1,2-thiazine-1,1-dioxide.Type: GrantFiled: December 22, 1980Date of Patent: January 19, 1982Assignee: Polaroid CorporationInventors: Alan L. Borror, Louis Cincotta, James W. Foley, Marcis M. Kampe
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Patent number: 4277406Abstract: The present invention is concerned with novel triarylmethane dyes possessing in their triaryl structure a 4'-oxo-1'-naphthylidene (or a 4'-oxo-1'-phenylidene) moiety and a phenyl moiety substituted in the ortho-position to the central carbon atom with the group ##STR1## wherein R is alkyl, unsubstituted or substituted with a solubilizing group, and Y is an electron-withdrawing group, which compounds find utility in photographic products and processes.Type: GrantFiled: December 26, 1979Date of Patent: July 7, 1981Assignee: Polaroid CorporationInventor: James W. Foley
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Patent number: 4277407Abstract: The present invention is concerned with novel triarylmethane dyes possessing in their triaryl structure a 4'-oxo-1'-naphthylidene (or a 4'-oxo-1'-phenylidene) moiety and a phenyl moiety substituted in the ortho-position to the central carbon atom with the group ##STR1## wherein R is hydrogen; alkyl, unsubstituted or substituted with halo, alkoxy, carboxy-substituted alkoxy, phenoxy or phenyl; or phenyl, unsubstituted or substituted with halo, alkoxy, nitro, dimethylamino or alkyl, which compounds find utility in photographic products and processes.Type: GrantFiled: December 26, 1979Date of Patent: July 7, 1981Assignee: Polaroid CorporationInventor: James W. Foley
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Patent number: 4271074Abstract: The compounds according to the invention have the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are monovalent organic radicals or chlorine and Z is a tetravalent organic radical and A is a divalent organic grouping. These products are to be used as adhesion promoters, especially between inorganic solids and organic resins. 4 processes of preparation are given.Type: GrantFiled: August 20, 1979Date of Patent: June 2, 1981Assignee: Ciba-Geigy CorporationInventors: Dieter Lohmann, Siegfried Wyler
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Patent number: 4238401Abstract: Alkoxysilyl ethers of 1,3-dicarbonyl cyclic compounds, such as methoxy tris-5,5-dimethyl-cyclohexen-2-one-3-yloxy silane can be made by effecting reaction in the presence of an acid acceptor between an alkanol, a halosilane and a 1,3-dicarbonyl cyclic organic compound, for example, 5,5-dimethyl-1,3-cyclohexane dione. The alkoxysilyl ethers are useful as vulcanizing agents for silanol terminated polydiorganosiloxanes.Type: GrantFiled: July 24, 1978Date of Patent: December 9, 1980Assignee: General Electric CompanyInventors: James A. Cella, Tyrone D. Mitchell
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Patent number: 4237137Abstract: The invention provides sila-substituted 1,4-dihydropyridine derivatives useful as medicament which influence the circulation. Also included in the invention are methods for the procurement of said derivatives, compositions containing said derivatives and methods for the use of said derivatives.Type: GrantFiled: August 8, 1979Date of Patent: December 2, 1980Assignee: Bayer AktiengesellschaftInventors: Reinhold Tacke, Anke Bentlage, Robertson Towart, Wulf Vater
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Patent number: 4217452Abstract: The invention relates to a new synthesis for the preparation of tetracyclic compounds of the general formula: ##STR1## as well as the pharmaceutically acceptable salts thereof, in which: n is the number 1 or 2,m is the number 1, if n=2 and the number 2, if n=1,R.sub.1 and R.sub.2 stand for hydrogen, hydroxy, halogen, lower alkyl (1-4 C), lower alkoxy (1-4 C) or trifluoromethyl andR.sub.3 represents hydrogen, alkyl (1-6 C), aralkyl (7-10 C) or an amino alkyl group (1-6 C), in which the nitrogen atom has been substituted by two alkyl groups (1-4 C), or the nitrogen atom forms part of a heterocyclic 5- or 6-membered ring,having valuable biological properties.Type: GrantFiled: December 27, 1976Date of Patent: August 12, 1980Assignee: Akzona IncorporatedInventor: Jacques Olivie