Nitrogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/451)
  • Patent number: 5227500
    Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.
    Type: Grant
    Filed: July 17, 1991
    Date of Patent: July 13, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Carl G. Krespan
  • Patent number: 5225577
    Abstract: An organic nonlinear optical material comprising a 4-nitrophenylaminoacetaldehyde acetal of the following formula (I): ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent a hydrogen atom, or a linear or branched alkyl group having 1 to 6 carbon atoms, and R.sub.4 represents a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, a linear or branched alkoxy group having 1 to 6 carbon atoms, a hydroxyl group, a nitro group or a halogen atom.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: July 6, 1993
    Assignees: Naoya Ogata, Seizo Miyata, Ube Industries, Ltd., Research Development
    Inventors: Naoya Ogata, Yasuhiko Yokowo
  • Patent number: 5190573
    Abstract: Cyclohexenone oxime ethers ##STR1## where R.sup.1 is alkyl;A is substituted or unsubstituted alkylene or alkenylene, where methylene is replaced by an oxygen atom, a sulfur atom, a sulfoxyl group, a sulfonyl group or --NR.sup.a --,Z is phenyl or a 5- or 6-membered heteroaromatic structure;X is substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbony or phenyl;n is 0 to 3, or 1 to 5 where X is halogen;R.sup.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: March 2, 1993
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
  • Patent number: 5171747
    Abstract: The derivatives of the formula: ##STR1## wherein: R.sub.1 is H or C.sub.1 -C.sub.4 alkyl;X is an oxygen atom, a methylene group or a --CH.dbd.CH-- group;n is 1 or 2 when X is an oxygen atom or a methylene group and 0 or 1 when X is a --CH.dbd.CH-- group;D is an oxygen atom or a NOR group, wherein R.dbd.H or C.sub.1 -C.sub.4 alkyl;R.sub.3 is a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group;each of R.sub.2 and R'.sub.2 independently is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl or benzyl group; andR'.sub.2 and R.sub.3 may further form together a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- chain,useful as drugs.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: December 15, 1992
    Assignee: Delalande S.A.
    Inventors: Francois X. Jarreau, Vincenzo Rovei, Jean-Jacques Koenig, Alain R. Schoffs
  • Patent number: 5137913
    Abstract: The invention concerns a diaryl ether cyclic ether of the formula I, or a pharmaceutically-acceptable salt thereof, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;Ar.sup.2 is optionally substituted phenylene, or a 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-4C) alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino; andR.sup.3 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl and substituted (1-4C)alkyl.The invention also concerns processes for the manufacture of a diaryl ether cyclic ether of the formula I, or a pharmaceutically-acceptable salt thereof, and pharmaceutical compositions containing said cyclic ether. The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: December 12, 1991
    Date of Patent: August 11, 1992
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Thomas G. C. Bird, Philip N. Edwards
  • Patent number: 5128479
    Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: January 29, 1990
    Date of Patent: July 7, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5128368
    Abstract: Combatting fungi and bacteria with aminomethylheterocyclic compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl, in each case optionally substituted tetrahydronaphthyl, decahydronaphthyl, cycloalkyl or cycloalkenyl, furthermore alkyl which is substituted by cycloalkyl, cycloalkenyl, cycloalkyloxy or cycloalkylthio, where the cyclic radicals may optionally be substituted, furthermore optionally substituted aryl, in addition alkyl which is substituted by aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl, or alkenyl which is substituted by aryl, where the aryl radicals may in each case optionally be substituted;R.sup.2 represents hydrogen or methyl,R.sup.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: July 7, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Graham Holmwood, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 5098932
    Abstract: The invention concerns a cyclic ether derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl or naphthyl;A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;Ar.sup.2 is optionally substituted phenylene, or a 6 membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X--A.sup.3 -- wherein each of A.sup.2 and A.sup.3 is (1-6C)alkylene and X is oxy, thio, sulphinyl, sulphonyl or imino; andR.sup.3 is (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl or substituted (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.
    Type: Grant
    Filed: December 22, 1989
    Date of Patent: March 24, 1992
    Assignee: Imperial Chemical Industries PLC, ICI Pharma
    Inventor: Annie Hamon
  • Patent number: 5081276
    Abstract: The invention concerns new polyfunctional ethylenic monomers of the general formula (I): ##STR1## where R.sub.1 and R.sub.2 each represent --CHR.sub.3 R.sub.4 where R.sub.3 and R.sub.4 may be identical or different and represent H or an alkyl, alkenyl or aralkyl group. R.sub.1 and R.sub.2 may, alternatively, together form a radical --CH.sub.2 --(CR.sub.5 R.sub.6).sub.n --CHR.sub.7 where n=0 or 1 and R.sub.5, R.sub.6 and R.sub.7 may be identical or different and represent H or CH.sub.3.Particular monomers are:2-cyano-4,4-dimethoxy-3-hydroxy-1-butene;2-cyano-4,4-dibutoxy-3-hydroxy-1-butene.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: January 14, 1992
    Assignee: Societe Francaise Hoechst
    Inventors: Didier Wilhelm, Alain Blanc
  • Patent number: 5039681
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: February 14, 1990
    Date of Patent: August 13, 1991
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5022914
    Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl,A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,X is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.
    Type: Grant
    Filed: October 31, 1989
    Date of Patent: June 11, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
  • Patent number: 5017618
    Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.
    Type: Grant
    Filed: September 18, 1989
    Date of Patent: May 21, 1991
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4990505
    Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein the substituents are defined in the specification, and physiologically acceptable salts and solvates thereof.The compounds of formula (I) have a selective stimulant action at .beta..sub.2 -adrenoreceptors and are useful, in particular in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.
    Type: Grant
    Filed: April 18, 1989
    Date of Patent: February 5, 1991
    Assignee: Glaxo Group Limited
    Inventors: Ian F. Skidmore, Lawrence H. C. Lunts, Harry Finch, Alan Naylor, Ian B. Campbell
  • Patent number: 4988827
    Abstract: Ether-substituted isonitriles, Tc99m complexes thereof, and processes for myocardial tissue radioimaging using the Tc99m complexes.
    Type: Grant
    Filed: June 1, 1987
    Date of Patent: January 29, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Paul L. Bergstein, Vinayakam Subramanyam
  • Patent number: 4988729
    Abstract: Combattting fungi and bacteria with aminomethylheterocyclic compounds of the formula ##STR1## in which R.sup.1 represents hydrogen, alkyl, alkenyl, in each case optionally substituted tetrahydronaphthyl, decahydronaphthyl, cycloalkyl or cycloalkenyl, furthermore alkyl which is substituted by cycloalkyl, cycloalkenyl, cycloalkyloxy or cycloalkylthio, where the cyclic radicals may optionally be substituted, furthermore optionally substituted aryl, in addition alkyl which is substituted by aryl, aryloxy, arylthio, arylsulphinyl or arylsulphonyl, or alkenyl which is substituted by aryl, where the aryl radicals may in each case optionally be substituted;R.sup.2 represents hydrogen or methyl,R.sup.
    Type: Grant
    Filed: October 17, 1989
    Date of Patent: January 29, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kramer, Joachim Weissmuller, Graham Holmwood, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke
  • Patent number: 4985546
    Abstract: A substituted colorant which may be copolymerized with a condensation polymer to provide a covalently bound, nonextractable coloring, having the formula ##STR1## wherein R and R.sub.1 are independently selected from hydrogen or lower alkyl; R.sub.4 is selected from hydrogen or lower alkyl; x is 0 or 1; N and M are each integers of from 1 to about 100 and the sum of N and M is from 3 to about 100. The hydroxyl groups are protected by formation of a ring structure during alkoxylation and amination of the substituent.
    Type: Grant
    Filed: June 19, 1989
    Date of Patent: January 15, 1991
    Assignee: Milliken Research Corporation
    Inventors: John W. Miley, John W. Rekers
  • Patent number: 4977281
    Abstract: Primary amino polyoxyalkylene 1,3-dioxane or 1,3-dioxolane compounds are provided of the formula: ##STR1## wherein R and R.sub.1 are independently selected from hydrogen or a lower alkyl group; R.sub.2 and R.sub.3 are independently selected from hydrogen, phenyl or lower alkyl groups; R.sub.4 is selected from hydrogen or a lower alkyl group; x is 0 or 1; N and M are each integers of from 1 to about 100 and the sum of N an M is from 2 to about 100; also disclosed are polyoxyalkylene amino alcohol compounds which may be derived from the compounds of Formula I above having the formula: ##STR2## wherein R, R.sub.1, R.sub.4, x, N and M all have the values given above. Also provided is a process for preparing a primary amino polyoxyalkylene 1,3-dioxane or 1,3-dioxolane.
    Type: Grant
    Filed: December 21, 1987
    Date of Patent: December 11, 1990
    Assignee: Milliken Research Corporation
    Inventors: John W. Miley, John W. Rekers
  • Patent number: 4973714
    Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.
    Type: Grant
    Filed: November 22, 1988
    Date of Patent: November 27, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Carl G. Krespan
  • Patent number: 4971981
    Abstract: Novel substituted 1,3-dioxolan and 1,4-dioxan derivatives of formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently of the others represents hydrogen or C.sub.1 -C.sub.4 -alkyl or, if n=1,R.sub.2 and R.sub.4 together represent one of the radicals ##STR2## R.sub.7 represents hydrogen, halogen, methyl, ethyl, C.sub.1 -C.sub.2 -alkyl substituted by 1 to 5 halogen atoms, methoxy, ethoxy or C.sub.1 -C.sub.2 -alkoxy substituted by 1 to 5 halogen atoms;R.sub.8 represents a halogen, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 -alkyl substituted by 1 to 7 halogen atoms, C.sub.1 -C.sub.3 -alkoxy, C.sub.1 -C.sub.3 -alkoxy substituted by 1 to 7 halogen atoms, or cyano;U represents a grouping --CH.dbd. or --N.dbd.;X represents --O--, --S-- or --N(R.sub.9)--;Y represents --O--, --S--, --S(O)--, --S(O.sub.2)--, --CH.sub.2 --, --CO-- or --N(R.sub.9)--, whereinR.sub.9 represents hydrogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: November 20, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Friedrich Karrer
  • Patent number: 4968706
    Abstract: Compounds of formula I ##STR1## wherein Ar is an optionally substituted phenyl ring; B is a single bond, a group --(CH.sub.2 OCH.sub.2).sub.n being n=1 or 2, a 2,4-disubstituted-1,3-dioxolane ring or a 2,4-disubstituted-1,3-thioxolane ring, R is a single bond, an optionally substituted methylene or ethylene group and T is 2-, 3- or 4-pyridyl, an optionally salified or esterified carboxy group or a carboxyamide group. Said compounds are useful in treatment of respiratory diseases.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: November 6, 1990
    Assignee: Boehringer Mannhein Italia, S.p.A.
    Inventors: Silvano Spinelli, Roberto Di Domenico, Ernesto Menta, Bruno Lumachi, Licia Gallico, Sergio Tognella
  • Patent number: 4966726
    Abstract: The new compounds produced from a molecular structural element with two chirality centers and at least one mesogenic structural element are defined by the general formula (I) ##STR1## in which the symbols have the following meaning: Y.sup.1 =H, (C.sub.1 -C.sub.10)alkyl, MC--CH.sub.2 or MC--CO, MC denoting the molecular radical of a mesogenic carboxylic acid after splitting off a COOH group,Y.sup.2 =(C.sub.1 -C.sub.10)alkyl, MC--CH.sub.2 or MC--CO, it being possible for Y.sup.1 and Y.sup.2 to jointly represent a MC--CH group, which is then part of a dioxolane ring,X=COOR.sup.1, CONH.sub.2, CONR.sup.2 R.sup.3 or C.tbd.N,R.sup.1 =(C.sub.1 -C.sub.10)alkyl or MC--CH.sub.2, andR.sup.2, R.sup.3 =H and (C.sub.1 -C.sub.4)alkyl or, independently of each other, (C.sub.1 -C.sub.4)alkyl.Said esters preferably find application as dopants in twistable liquid crystal phases in which they produce temperature compensation and twisting.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: October 30, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunter Scherowsky, Manel Gunaratne
  • Patent number: 4950777
    Abstract: Novel derivatives of N-phenyl-3,4,5,6-tetrahydrophthalimide of the formula I given below have good pre- and post-emergence, selective-herbicidal properties, and they furthermore regulate and inhibit plant growth. The compounds correspond to the formula I ##STR1## wherein R is C.sub.1 -C.sub.3 -alkyl,n is zero, one or two,R.sub.1 and R.sub.2 independently of one another are each hydrogen or halogen,R.sub.3 is hydrogen, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl or a radical --CH.sub.2 YR.sub.4,R.sub.4 is C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.4 -alkenyl, C.sub.3 -C.sub.4 -alkynyl, C.sub.3 -C.sub.7 -cycloalkyl, benzyl or phenyl,Z is oxygen, or an oxime radical .dbd.N--O--Q, and the grouping --C(R.sub.3).dbd.Z can also be a ketal radical, andQ is hydrogen, a C.sub.1 -C.sub.10 -alkyl radical, a C.sub.3 -C.sub.8 -alkenyl radical or a C.sub.3 -C.sub.8 -alkynyl radical, a C.sub.3 -C.sub.7 -cycloalkyl or C.sub.3 -C.sub.7 -cycloalkenyl radical, a phenyl-C.sub.1 -C.sub.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: August 21, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Georg Pissiotas, Beat Bohner
  • Patent number: 4942169
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.
    Type: Grant
    Filed: March 10, 1989
    Date of Patent: July 17, 1990
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4940706
    Abstract: The present invention describes novel 2,4-disubstituted 1,3-dioxolanes having the formula I ##STR1## wherein R.sup.1 represents a long chain alkyl group; X is a covalent single bond, a carbonyl group, a carboxyl group, a carbamoyl group or a --O--P(.dbd.O)(O.sup.z)-- group; z is a negative charge (-) when q is zero, or z is an hydrogen atom when q is one; n is an integer from 2 to 10; R.sup.2, R.sup.3 and R.sup.4 are lower alkyl groups, or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents an aromatic cyclic ammonium group or R.sup.2 R.sup.3 R.sup.4 N.sup.+ represents a non-aromatic cyclic ammonium group in which two of the groups (R.sup.2, R.sup.3 or R.sup.4) form a non-aromatic ring together with the quaternary nitrogen atom; and A.sup.- is a pharmaceutically acceptable anion. These compounds are in vitro inhibitors of the platelet aggregation induced by the platelet activating factor (PAF) and, thus, useful for the treatment of the diseases in which this substance is involved.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: July 10, 1990
    Assignee: J. Uriach & Cia, S.A.
    Inventors: Javier Bartroli, Manuel Anquita, Elena Carceller
  • Patent number: 4937354
    Abstract: 3-(3,4,5,6-Tetrahydrophthalimido)-benzaldehydes of the type I ##STR1## or corresponding derivatives substituted in the phenyl ring are prepared by(a) acetalization of a 3-nitrobenzaldehyde III or of a corresponding derivative with an alcohol IV in the presence of an acidic catalyst to give the corresponding cyclic acetal V ##STR2## (b) reduction of the cyclic acetal V with hydrogen to give the corresponding amino compound II and(c) subsequent condensation of this aminophenyl acetal II with 3,4,5,6-tetrahydrophthalic anhydride in an acidic reaction medium.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: June 26, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Klaus Fischer, Lothar Rueb, Peter Plath
  • Patent number: 4936958
    Abstract: Enantiomer-free 2,2,4-trisubstituted 1,3-dioxolanes of the general formula: ##STR1## wherein R.sup.1 and R.sup.2 are either the same and are (a) hydrogen or(b) alkyl groups with 1 to 4 C atoms or(c) aryl groups or(d) arylalkyl groupsor R.sup.1 and R.sup.2 together are a 1,4-butanediyl or 1,5-pentanediyl group, and X is either a hydroxy group or, with the assumption that R.sup.1 and R.sup.2 are not aryl groups, NHR.sup.3 wherein R.sup.3 is alkyl with 1 to 8 C atoms or aryl, are produced by electrolysis of a substated theronic acid or erythornic acid or a salt thereof into a substituted 1,3-dioxolane-4-carbaldehyde. The substituted 1,3-dioxolane-4-carbaldehyde is converted by reduction or reductive amination, without being ioslated, into the enantiomer-free 2,2,4-trisubstituted 1,3-dioxolane. A substantial advantage of the electrochemical process is that only carbon dioxide and hydrogen are produced which escape by themselves as gases from the electrolyte.
    Type: Grant
    Filed: January 18, 1989
    Date of Patent: June 26, 1990
    Assignee: Lonza Ltd.
    Inventor: Robert Voeffray
  • Patent number: 4931581
    Abstract: A method and composition for the immunization of healthy useful plants against plant diseases containing as active ingredients compounds of formula ##STR1## in which: X is hydrogen, halogen, hydroxy, methyl, methoxy, HOOC or MOOC;Y is hydrogen, halogen, SO.sub.3 H, SO.sub.3 M, nitro, hydroxy or amino, M being the molar equivalent of an alkali metal or alkaline earth metal ion that is formed from a corresponding base or basic compound; andZ is cyano or --CO--A;A represents either --OH or --SH, the hydrogen atom of which may also be replaced by the molar equivalent of an inorganic or organic cationic residue,or wherein A represents any other organic residue which has a molecular weight of less than 900 and which may also contain one, or more than one, hetero atom, including the salts of the phytophysiologically tolerable 7-carboxylic acid or 7-thiocarboxylic acid with primary, secondary or tertiary amines or with inorganic bases.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: June 5, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Rolf Schurter, Walter Kunz, Robert Nyfeler
  • Patent number: 4929739
    Abstract: A novel complex of a class of tellurium and selenium compounds is disclosed, which is based on a complexing agent and the particular compound to be complexed.
    Type: Grant
    Filed: March 24, 1988
    Date of Patent: May 29, 1990
    Assignee: Bar-Ilan University
    Inventors: Benjamin Sredni, Leo Pavliv, Michael Albeck
  • Patent number: 4927968
    Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl and R is ##STR2## --CH.sub.2 OH or --CH.sub.2 X in which X is a conventional leaving group and Y is lower alkyl and the use thereof in a process for the preparation of certain histamine H.sub.2 -antagonists.
    Type: Grant
    Filed: April 11, 1988
    Date of Patent: May 22, 1990
    Assignee: Bristol-Myers Company
    Inventors: Aldo A. Algieri, Robert F. Farney
  • Patent number: 4908451
    Abstract: A process is disclosed for the preparation of .alpha.-substituted carbonyl compounds, wherein .alpha.-substituted ketone is prepared by the following reaction: ##STR1## .alpha.-azo ester is prepared by the following reaction: ##STR2## and .alpha.-hydrozono ester is prepared by the following reaction: ##STR3## wherein the .alpha.-azo ester and .alpha.-hydrazono ester obtained by the above reactions include novel compounds, which are also disclosed.
    Type: Grant
    Filed: March 23, 1988
    Date of Patent: March 13, 1990
    Assignee: Agency of Industrial Science and Technology
    Inventors: Masato Tanaka, Toshiyasu Sakakura
  • Patent number: 4902818
    Abstract: The manufacture of optically active bifunctional compounds of the general formula ##STR1## wherein R represents protected hydroxymethyl, protected formyl or alkoxycarbonyl and R.sup.1 represents a group of the formula ##STR2## in which R.sup.2 and R.sup.3 represents lower alkyl or cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom represent a heterocyclic ring, by isomerizing compounds of the general formula ##STR3## wherein R, R.sup.2 and R.sup.3 have the above significance and R.sup.3 can additionally signify hydrogen, is described.The compounds of formula I are potential intermediates in the manufacture of, interalia, natural vitamin E and natural vitamin K.sub.1.
    Type: Grant
    Filed: October 5, 1988
    Date of Patent: February 20, 1990
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans-Jurgen Hansen, Rudolf Schmid, Max Schmid
  • Patent number: 4849431
    Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.
    Type: Grant
    Filed: December 24, 1986
    Date of Patent: July 18, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 4845119
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent of each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substitutent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkyl;wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --; andwherein R.sup.9 is alkyl or up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 18, 1986
    Date of Patent: July 4, 1989
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 4833258
    Abstract: Novel intermediates and a novel process for their preparation, where said intermediates are useful in the preparation of 6-hydroxymethyl and related oxidation derivatives of mevinolin and analogs thereof, are disclosed.
    Type: Grant
    Filed: February 17, 1987
    Date of Patent: May 23, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Robert L. Smith, Ta Jyh Lee
  • Patent number: 4810806
    Abstract: There are disclosed halogenated dioxolanes of a specified formula, dioxoles made therefrom, polymers of the dioxoles, and processes for making the dioxolanes.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: March 7, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Carl G. Krespan
  • Patent number: 4792606
    Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Hermann-Dieter Krall
  • Patent number: 4783452
    Abstract: Coordination compounds of platinum(II) with 4,5-bis(aminomethyl)-1,3-dioxolane, intended for use in the treatment of cancer. The compounds may exist as monomers or as linear or cyclic polymers.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: November 8, 1988
    Assignee: Johnson Matthey Public Limited Company
    Inventors: Alan H. Haines, Christopher Morley
  • Patent number: 4780479
    Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: October 25, 1988
    Assignee: National Research Development Corporation
    Inventors: John A. Pickett, Ewen D. M. Macaulay
  • Patent number: 4761490
    Abstract: Certain tellurium compounds have been found to have the ability to stimulate the in vivo and in vitro production of cytokines and their receptors. These compounds may be utilized in the treatment of certain tumors, autoimmune diseases, immune diseases and infectious diseases.
    Type: Grant
    Filed: September 30, 1985
    Date of Patent: August 2, 1988
    Assignee: Bar-Ilan University
    Inventors: Michael Albeck, Benjamin Sredni
  • Patent number: 4739068
    Abstract: N-Phenylsulfonyl-N'-pyrimidinylureas and --N'-triazinylureas of the general formula ##STR1## and the salts of these compounds with amines, alkali metal bases and alkaline earth metal bases or with quaternary ammonium bases, have good selective herbicidal and plant growth regulating properties when applied pre- and postemergence.In the formulaR.sub.1 is hydrogen, halogen, nitro, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.5 alkenyl or C.sub.1 -C.sub.4 alkoxycarbonyl,R.sub.2 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy, each unsubstituted or substituted by 1 to 3 halogen atoms,R.sub.3 is halogen, hydrogen, --NR.sub.4 R.sub.5, C.sub.1 -C.sub.3 alkyl, unsubstituted or substituted by 1 to 3 halogen atoms or C.sub.1 -C.sub.4 alkoxy, or is C.sub.1 -C.sub.3 alkoxy, unsubstituted or substituted by methoxy, ethoxy, or 1 to 3 halogen atoms,R.sub.4 is hydrogen or methyl,R.sub.5 is hydrogen, C.sub.1 -C.sub.2 alkyl or methoxy,A is C.sub.1 -C.sub.4 alkylene or C.sub.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: April 19, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl Gass, Werner Fory, Willy Meyer, Werner Topfl
  • Patent number: 4727142
    Abstract: The invention relates to a process for the preparation of compounds of the formula I and salts or acid addition compounds thereof ##STR1## in which R denotes hydrogen, (halogenated) alkyl with the exception of CF.sub.3, a (substituted) aromatic radical, (substituted) heteroaryl, (substituted) phenoxy, (substituted) phenylthio, (substituted) phenylamino, halogen, hydroxyl, alkoxy, mercapto, (halogenated) cycloalkyl, alkylmercapto, amino, monoalkylamino or dialkylamino,R.sup.1 denotes (substituted alkyl, (substituted) phenyl or naphthyl, alkenyl, alkinyl, cycloalkyl, (substituted) benzyl or heteroaryl, and X denotes oxygen or sulfur, which comprises reacting a nitrile of the formula II with a compound of the formula IIIR--C.tbd.N (II)R.sup.
    Type: Grant
    Filed: April 18, 1986
    Date of Patent: February 23, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Fuss, Gunter Siegemund
  • Patent number: 4714710
    Abstract: There are described new compounds of general formula I ##STR1## in which R.sub.1 is aryl or aryl substituted by C.sub.1-4 -alkyl, halo-C.sub.1-4 -alkyl, phenyl-C.sub.1-4 -alkyl, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.2-4 -alkynyl, halo-C.sub.2-4 -alkynyl, phenyl-C.sub.2-4 -alkynyl, C.sub.1-4 -alkoxy, halo-C.sub.1-4 -alkoxy, phenyl-C.sub.1-4 -alkoxy, C.sub.2-4 -alkenyloxy, alkylsulphonyloxy, haloalkylsulphonyloxy, arylsulphonyloxy, halo-C.sub.2-4 -alkenyloxy, phenyl-C.sub.2-4 -alkenyloxy, halo, cyano, nitro, aryloxy, haloaryloxy, C.sub.1-4 -alkylaryloxy, or nitro-C.sub.1-4 -alkylaryloxy,R.sub.2 and R.sub.3 are the same or different and are hydrogen, fluorine, cyano or ethynyl,R.sub.4 is phenyl or pyridyl or these groups substituted by one or more of C.sub.1-6 -alkyl, halo-C.sub.1-6 -alkyl, phenyl-C.sub.1-6 -alkyl, C.sub.1-6 -alkyl interrupted by an O--, N-- or S-- atom, C.sub.2-4 -alkenyl, halo-C.sub.2-4 -alkenyl, phenyl-C.sub.2-4 -alkenyl, C.sub.1-4 -alkoxy, halo-C.sub.
    Type: Grant
    Filed: September 9, 1986
    Date of Patent: December 22, 1987
    Assignee: Schering Aktiengesellschaft
    Inventors: Heinrich Franke, Hartmut Joppien, Helga Franke
  • Patent number: 4701556
    Abstract: The invention relates to a process for the manufacture of a cephalosporin derivative of the formula I: ##STR1## in which X is a sulphur or oxygen atom or a sulphinyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art, R.sup.2 is a hydrogen atom or a 1-6C alkyl or 2-6C alkenyl radical, R.sup.3 is a hydrogen atom or one of a variety of radicals defined in the specification, and the pharmaceutically-acceptable acid- and base-addition salts thereof, characterized by reaction of a compound of the formula IX: ##STR2## in which R.sup.16 and R.sup.17 individually have one of the values given above for R.sup.2 and R.sup.3, or a derivative thereof in which the carbonyl group is masked, with a compound of the formula X: ##STR3## in which R.sup.18 is a hydrogen atom or any one of the cephalosporin 3-carboxylic acid protecting groups known in the art; whereafter, when R.sup.18 is other than a hydrogen atom, the protecting group R.sup.
    Type: Grant
    Filed: November 29, 1984
    Date of Patent: October 20, 1987
    Assignee: Imperial Chemical Industries PLC
    Inventor: Frank Loftus
  • Patent number: 4699986
    Abstract: There is presented optically uniform .beta.-lactams of the formulae ##STR1## wherein Z is a readily cleavable acyl group, R.sup.1 is amino or a group convertible into amino, R.sup.2 is hydrogen or a readily cleavable protecting group and R.sup.3 and R.sup.4 each are a lower hydrocarbon group which optionally contains oxygen and which is attached via a carbon atom, whereby these groups can also be joined with one another to form a ring, with the proviso that R.sup.1 is a readily cleavable acylamino when R.sup.2 is hydrogen,and the corresponding optical antipodes, their manufacture and use in the manufacture of antimicrobially-active .beta.-lactams as well as novel intermediates usable in their manufacture.
    Type: Grant
    Filed: August 26, 1985
    Date of Patent: October 13, 1987
    Assignee: Hofmann-La Roche Inc.
    Inventors: Christian N. Hubschwerlen, Gerard Schmid
  • Patent number: 4668700
    Abstract: Substituted aminoketals of the formula ##STR1## in which R.sup.1 to R.sup.4 are various organic radicals andR.sup.2 may also be hydrogen,are fungicidally active. Some of the compounds are new.
    Type: Grant
    Filed: July 13, 1984
    Date of Patent: May 26, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Kr/a/ mer, Wolf Reiser, Dieter Berg, Wilhelm Brandes, Paul Reinecke
  • Patent number: 4659818
    Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: April 21, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Ivan Kompis, Gerald Rey-Bellet, Guido Zanetti
  • Patent number: 4657926
    Abstract: Derivatives of carbonyl-group containing behavior modifying compounds, in which said carbonyl group has been converted to a photolabile group which regenerates the carbonyl group on exposure to radiation, are of value in various methods for the control of animal, and in particular insect, species.
    Type: Grant
    Filed: May 14, 1984
    Date of Patent: April 14, 1987
    Assignee: National Research Development Corporation
    Inventors: John A. Pickett, Ewen D. M. Macaulay
  • Patent number: 4648895
    Abstract: The invention relates to oxime ethers of the formula I ##STR1## wherein n is 1 or 2, each of R.sub.1 and R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl each of R.sub.3 and R.sub.4 is hydrogen, halogen, 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, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 haloalkylsulfinyl, C.sub.1 -C.sub.4 haloalkylsulfonyl or nitro; each of R.sub.5 and R.sub.6 independently of the other is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, phenyl or phenyl which is substituted by halogen, 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, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, carboxyl, carbamoyl, C.sub. 1 -C.sub.4 alkylcarbamoyl, nitro or cyano, or R.sub.5 and R.sub.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: March 10, 1987
    Assignee: Ciba-Geigy Corporation
    Inventors: Henry Martin, Urs Fricker
  • Patent number: 4642372
    Abstract: A process for the preparation of cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein Z is selected from the group consisting of --CN, --COOH and --COOR.sub.1, R.sub.1 is alkyl of 1 to 6 carbon atoms and R.sub.2 and R.sub.3 are alkyl of 1 to 4 carbon atoms or taken together with the carbon atom to which they are attached form a carbon homocycle of 3 to 6 carbon atoms comprising reacting at low temperatures in a solvent in the presence of a strong base a compound of the formula ##STR2## wherein Z has the above definitions and R is alkyl of 1 to 6 carbon atoms or together form a polymethylene of 2 to 3 carbon atoms with a sulfone of the formula ##STR3## wherein R.sub.2 and R.sub.3 have the above definitions and Y is an aromatic group followed by aqueous treatment to obtain a compound of the formula ##STR4## wherein Y, R, R.sub.2, R.sub.
    Type: Grant
    Filed: July 29, 1985
    Date of Patent: February 10, 1987
    Assignee: Roussel Uclaf
    Inventors: Jacques Martel, Jean Tessier, Jean-Pierre Demoute
  • Patent number: 4636568
    Abstract: There are disclosed certain aminoether compounds which are useful as intermediates in the preparation of photographic image dye providing materials. The aminoethers are represented either by the formula ##STR1## wherein R is hydrogen or an alcohol protecting group and R.sub.1 is hydrogen, alkyl or aralkyl such as benzyl or phenethyl; or the formula ##STR2## wherein R.sub.2 and R.sub.3 are alkyl having from 1 to 6 carbon atoms or R.sub.2 and R.sub.3 together represent the carbon atoms necessary to form, together with the oxygen atoms to which they are bonded and >CH, a five or six member saturated heterocyclic moiety which may include substituted rings and fused rings.
    Type: Grant
    Filed: August 27, 1984
    Date of Patent: January 13, 1987
    Assignee: Polaroid Corporation
    Inventors: Myron S. Simon, David P. Waller