Boron Or Silicon Containing Patents (Class 544/229)
  • Patent number: 4851028
    Abstract: 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: Grant
    Filed: September 2, 1987
    Date of Patent: July 25, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler, Hans-Georg Brunner
  • Patent number: 4849009
    Abstract: 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: Grant
    Filed: September 2, 1987
    Date of Patent: July 18, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
  • Patent number: 4845237
    Abstract: 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: Grant
    Filed: April 15, 1987
    Date of Patent: July 4, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Ann E. DeCamp, Leonard M. Weinstock, Thomas R. Verhoeven
  • Patent number: 4845258
    Abstract: 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: Grant
    Filed: April 4, 1988
    Date of Patent: July 4, 1989
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4831037
    Abstract: 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: Grant
    Filed: April 20, 1987
    Date of Patent: May 16, 1989
    Assignee: The Trustees of Princeton University
    Inventors: Edward C. Taylor, George P. Beardsley, James M. Hamby
  • Patent number: 4812458
    Abstract: 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: Grant
    Filed: September 2, 1987
    Date of Patent: March 14, 1989
    Assignee: A/S Ferrosan
    Inventors: Tage Honore, Jorgen Drejer, Poul Jacobsen, Flemming E. Nielsen
  • Patent number: 4804772
    Abstract: 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: Grant
    Filed: April 4, 1988
    Date of Patent: February 14, 1989
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4804774
    Abstract: 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: Grant
    Filed: April 4, 1988
    Date of Patent: February 14, 1989
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4804773
    Abstract: 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: Grant
    Filed: April 4, 1988
    Date of Patent: February 14, 1989
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 4795815
    Abstract: 1,2,4-Trisubstituted diazolidinones are intermediates to bicyclic pyrazolidinone antimicrobial compounds.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: January 3, 1989
    Assignee: Eli Lilly and Company
    Inventor: Robert J. Ternansky
  • Patent number: 4791110
    Abstract: 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: Grant
    Filed: May 5, 1986
    Date of Patent: December 13, 1988
    Assignee: Eli Lilly and Company
    Inventors: Wendell R. Arnold, William C. Dow, George W. Johnson
  • Patent number: 4783459
    Abstract: 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: Grant
    Filed: April 23, 1987
    Date of Patent: November 8, 1988
    Assignee: Schering Agrochemicals Ltd.
    Inventors: Ulrich Buhmann, Jurgen Westermann, Dietrich Baumert, Ernst Pieroh, Geoffrey R. Cliff, Ian C. Richards
  • Patent number: 4778797
    Abstract: 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: Grant
    Filed: September 9, 1985
    Date of Patent: October 18, 1988
    Assignees: Sanwa Kagaku Kenkyusho Co., Ltd., Shin-Etsu Chemical Co., Ltd.
    Inventors: Shigeshi Toyoshima, Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Koichi Ito
  • Patent number: 4775754
    Abstract: Oxazine, thiazine and diazine leuco dyes are synthesized through a reaction using a dicyclohexylcarbodiimide adduct. The adducts are themselves novel compounds.
    Type: Grant
    Filed: October 7, 1987
    Date of Patent: October 4, 1988
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Kim M. Vogel, Roger A. Mader
  • Patent number: 4772698
    Abstract: 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: Grant
    Filed: June 24, 1987
    Date of Patent: September 20, 1988
    Assignee: Th. Goldschmidt AG
    Inventors: Helmut Lammerting, Hans-Joachim Kollmeier
  • Patent number: 4769060
    Abstract: 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: Grant
    Filed: February 18, 1987
    Date of Patent: September 6, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Donald J. Dumas
  • Patent number: 4767443
    Abstract: 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: Grant
    Filed: September 13, 1985
    Date of Patent: August 30, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
  • Patent number: 4762835
    Abstract: 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: Grant
    Filed: December 16, 1986
    Date of Patent: August 9, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Alan J. Whittle, Roger Salmon, Edward McDonald
  • Patent number: 4752322
    Abstract: This invention relates to herbicidally active sulfonylurea compounds, agriculturally suitable compositions thereof and their method of use as herbicides or plant growth regulants.
    Type: Grant
    Filed: November 4, 1986
    Date of Patent: June 21, 1988
    Inventors: Donald J. Dumas, Marcus P. Moon
  • Patent number: 4751017
    Abstract: 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: Grant
    Filed: March 24, 1986
    Date of Patent: June 14, 1988
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Andreas Wachtler, Joachim Krause, Rudolf Eidenschink, Jurgen Eichler, Bernhard Scheuble
  • Patent number: 4743602
    Abstract: 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: Grant
    Filed: June 30, 1987
    Date of Patent: May 10, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Paul A. Worthington, Vivienne M. Anthony
  • Patent number: 4737184
    Abstract: 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: Grant
    Filed: May 10, 1985
    Date of Patent: April 12, 1988
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4723987
    Abstract: 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: Grant
    Filed: April 22, 1986
    Date of Patent: February 9, 1988
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Mary A. Hanagan
  • Patent number: 4719214
    Abstract: 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: Grant
    Filed: July 25, 1985
    Date of Patent: January 12, 1988
    Assignee: Southern Research Institute
    Inventors: Y. Fulmer Shealy, C. Allen O'Dell
  • Patent number: 4697009
    Abstract: 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: Grant
    Filed: June 18, 1986
    Date of Patent: September 29, 1987
    Assignee: Degussa Aktiengesellschaft
    Inventors: Ulrich Deschler, Peter Kleinschmit, Rudolf Michel
  • Patent number: 4678498
    Abstract: Novel compounds of Formula I are useful as herbicides and plant growth regulants.
    Type: Grant
    Filed: May 12, 1986
    Date of Patent: July 7, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Steven P. Artz
  • Patent number: 4670422
    Abstract: 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: Grant
    Filed: March 27, 1986
    Date of Patent: June 2, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Tamara Dejneka
  • Patent number: 4650868
    Abstract: 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: Grant
    Filed: May 1, 1985
    Date of Patent: March 17, 1987
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Susumu Nishimura, Hiroaki Nomura, Hiroshi Akimoto
  • Patent number: 4638004
    Abstract: 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: Grant
    Filed: May 15, 1985
    Date of Patent: January 20, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jorg Stetter, Heinz-Jurgen Wroblowsky, Robert R. Schmidt, Hans-Joachim Santel, Gerd Hanssler, Klaus Lurssen
  • Patent number: 4628048
    Abstract: 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: Grant
    Filed: March 18, 1986
    Date of Patent: December 9, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Rolf-Dieter Acker, Ernst Buschmann, Ernst-Heinrich Pommer, Eberhard Ammermann
  • Patent number: 4587247
    Abstract: 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: Grant
    Filed: February 25, 1985
    Date of Patent: May 6, 1986
    Assignee: Merck & Co., Inc.
    Inventors: Bruce O. Linn, Helmut H. Mrozik
  • Patent number: 4562185
    Abstract: 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: Grant
    Filed: March 15, 1984
    Date of Patent: December 31, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gerhard Jager, Rudolf Fauss, Kurt Findeisen, Benedikt Becker, Bernhard Homeyer
  • Patent number: 4560508
    Abstract: 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: Grant
    Filed: December 20, 1982
    Date of Patent: December 24, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Taisuke Matsuo, deceased, Michihiko Ochiai, Shoji Kishimoto
  • Patent number: 4556649
    Abstract: 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: Grant
    Filed: December 21, 1984
    Date of Patent: December 3, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
  • Patent number: 4550105
    Abstract: 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: Grant
    Filed: December 3, 1981
    Date of Patent: October 29, 1985
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Taisuke Matsuo, Shoji Kishimoto, Michihiko Ochiai
  • Patent number: 4543412
    Abstract: 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: Grant
    Filed: November 4, 1983
    Date of Patent: September 24, 1985
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flentge, Thomas R. Herrin
  • Patent number: 4524147
    Abstract: 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: Grant
    Filed: November 16, 1982
    Date of Patent: June 18, 1985
    Assignee: Mitsui Toatsu Chemicals, Incorporated
    Inventors: Isao Sakano, Tatsuro Yokoyama, Seitaro Kajiya, Yutaka Okazaki, Hiroshi Tokuda, Hiroshi Kawazura, Mikio Kumakura, Akira Awaya
  • Patent number: 4483988
    Abstract: 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: Grant
    Filed: July 19, 1982
    Date of Patent: November 20, 1984
    Assignee: Richardson Merrell Inc.
    Inventors: Albert A. Carr, Robert A. Farr, John M. Kane
  • Patent number: 4460587
    Abstract: 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: Grant
    Filed: November 29, 1982
    Date of Patent: July 17, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Isidoros Vlattas
  • Patent number: 4451652
    Abstract: 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: Grant
    Filed: May 24, 1982
    Date of Patent: May 29, 1984
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flentge, Curtis L. Kirkemo
  • Patent number: 4394505
    Abstract: 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: Grant
    Filed: April 16, 1982
    Date of Patent: July 19, 1983
    Assignee: Shionogi & Co., Ltd.
    Inventors: Susumu Kamata, Wataru Nagata
  • Patent number: 4336188
    Abstract: 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: Grant
    Filed: February 22, 1978
    Date of Patent: June 22, 1982
    Assignee: Snamprogetti, S.p.A.
    Inventors: Piergiorgio Zappelli, Antonio Rossodivita, Rosario Pappa, Luciano Re
  • Patent number: 4329460
    Abstract: 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: Grant
    Filed: June 13, 1979
    Date of Patent: May 11, 1982
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Osamu Miyashita, Koichi Matsumura, Hiroshi Shimadzu, Naoto Hashimoto
  • Patent number: 4311839
    Abstract: 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: Grant
    Filed: December 22, 1980
    Date of Patent: January 19, 1982
    Assignee: Polaroid Corporation
    Inventors: Alan L. Borror, Louis Cincotta, James W. Foley, Marcis M. Kampe
  • Patent number: 4277406
    Abstract: 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: Grant
    Filed: December 26, 1979
    Date of Patent: July 7, 1981
    Assignee: Polaroid Corporation
    Inventor: James W. Foley
  • Patent number: 4277407
    Abstract: 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: Grant
    Filed: December 26, 1979
    Date of Patent: July 7, 1981
    Assignee: Polaroid Corporation
    Inventor: James W. Foley
  • Patent number: 4271074
    Abstract: 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: Grant
    Filed: August 20, 1979
    Date of Patent: June 2, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Dieter Lohmann, Siegfried Wyler
  • Patent number: 4238401
    Abstract: 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: Grant
    Filed: July 24, 1978
    Date of Patent: December 9, 1980
    Assignee: General Electric Company
    Inventors: James A. Cella, Tyrone D. Mitchell
  • Patent number: 4237137
    Abstract: 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: Grant
    Filed: August 8, 1979
    Date of Patent: December 2, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhold Tacke, Anke Bentlage, Robertson Towart, Wulf Vater
  • Patent number: 4217452
    Abstract: 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: Grant
    Filed: December 27, 1976
    Date of Patent: August 12, 1980
    Assignee: Akzona Incorporated
    Inventor: Jacques Olivie