At 2-position And At 4- Or 6-position Patents (Class 544/323)
  • Patent number: 5153324
    Abstract: A process for preparing herbicidal sulfonylureas which comprises mixing a sulfonylisocyanate and a heterocyclic amine in the absence of a solvent.
    Type: Grant
    Filed: December 26, 1991
    Date of Patent: October 6, 1992
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Teddy H. Grindstaff
  • Patent number: 5149700
    Abstract: This invention relates to substituted arylsulfonamides and benzamides possessing aniarrhythmic activity, to pharmaceutical compositions and to methods for production thereof.
    Type: Grant
    Filed: October 30, 1991
    Date of Patent: September 22, 1992
    Assignee: American Home Products Corporation
    Inventors: John W. Ellingboe, Jehan F. Bagli, Michael W. Winkley
  • Patent number: 5149357
    Abstract: Compound of the formula ##STR1## in which A is O, S, or NR.sup.3 ; G is CH or N; R and R.sup.1 are independently alkyl, alkoxy, haloalkoxy or alkylamino; R.sup.2 is phenyl, substituted phenyl, alkyl, cycloalkyl, haloalkyl or --CH.sub.2 [(R.sup.4)C(R.sup.5).sub.n --Z; R.sup.3 and R.sup.7 are, independently, hydrogen, alkyl, --C(O)NH.sub.2 or --C(O)alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, or halogen; R.sup.6 is halogen, alkyl, alkoxy, haloalkoxy, NO.sub.2, amino, alkyl substituted amino, or acyl substituted amino; n is 0 to 5; Z is cyano, amino, alkylamino, dialkylamino, --NHCO.sub.2 alkyl, alkoxy, alkylthio, alkylsulfonyl, alkenyl, alkynyl, phenyl or substituted phenyl; and Q is hydrogen, halogen, alkyl, alkoxy, haloalkoxy, nitro, amino, haloalkyl, alkythio, alkylsulfonyl, phenyl, substituted phenyl or phenoxy; or a 5 or 6 membered aromatic heterocycle having the formula ##STR2## in which "m" is 0 or 1; A' is O, S, or NR.sup.
    Type: Grant
    Filed: June 19, 1990
    Date of Patent: September 22, 1992
    Assignee: FMC Corporation
    Inventors: John A. Dixson, Natesan Murugesan, Keith D. Barnes
  • Patent number: 5147876
    Abstract: 2,6-di-, 2,4,6-, 2,5,6-tri- or 2,4,5,6-tetra-substituted pyrimidines, and 2,6-di-substituted pyridines. These compounds are useful for treatment of neurological diseases.
    Type: Grant
    Filed: December 29, 1989
    Date of Patent: September 15, 1992
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Akira Mizuchi, Kazutoshi Horikomi, Tadayuki Sasaki, Akira Awaya, Ikuo Tomino, Mitsuyuki Takesue, Noriaki Kihara
  • Patent number: 5145967
    Abstract: The present invention is directed to a method for preparing a 4-alkoxyalkyl-4-phenylaminopiperidine compound which comprises the steps of (a) reacting an N-substituted-4-piperidone compound with an aniline compound to form a Schiff base compound, (b) reacting the Schiff base compound with an anionic reagent having an anion stabilizing group to form an amine compound, and (c) reducing the amine compound in step (b) with a reducing agent to displace the anion stabilizing group.The anionic reagent in step (b) above has the general formula:X--CYM--Zwherein X is an anion stabilizing group, Y is hydrogen or lower-alkyl, Z is lower-alkoxy or phenylmethoxy, M is an alkali or alkaline earth metal, and C is a carbon atom.
    Type: Grant
    Filed: November 2, 1990
    Date of Patent: September 8, 1992
    Assignee: Anaquest, Inc.
    Inventors: Bor-Sheng Lin, H. Kenneth Spencer, Joseph W. Scheblein
  • Patent number: 5141941
    Abstract: Disclosed are a compound of the formula (I) or an acid addition salt thereof: ##STR1## wherein Q represents R.sup.1 , R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, n and z are defined as in the specification, preparation method thereof and fungicides containing the same.
    Type: Grant
    Filed: November 15, 1989
    Date of Patent: August 25, 1992
    Assignee: Ube Industries, Ltd.
    Inventors: Katsutoshi Fujii, Toshinobu Tanaka, Yasuhisa Fukuda
  • Patent number: 5129941
    Abstract: Sulfonylureas of the formula ##STR1## where A is a bond or a C.sub.1 -C.sub.10 -hydrocarbon radical,R.sup.1 is an optionally unsaturated hydrocarbon radical which is optionally substituted by halogen, optionally unsaturated alkoxy, alkylthio, alkylsulfonyl or alkylsulfinyl, cycloalkyl, optionally substituted phenyl or a heterocycle, or is optionally substituted phenyl, NRR' with R and R' being alkyl, alkoxy or alkylene (cyclic with N),Y is S, SO or SO.sub.2,R.sup.1 is optionally unsaturated alkoxy which is optionally substituted, or is cycloalkoxy, cycloalkenyloxy, cyclopropylmethyloxy, epoxypropyloxy, furfuryloxy, tetrahydrofurfuryloxy or optionally substituted phenoxyalkoxy or phenoxy,R.sup.3 is alkyl which is optionally unsaturated, or is alkoxy,R.sup.4 is optionally substituted pyrimidinyl, pyrimidinylmethyl, pyrimidinyl with a fused-on cyclopentane, oxolane, oxolene, oxane, pyridine or pyrazine ring or purinyl or triazolyl, andZ is O or S,have herbicidal and/or plant-growth-regulatory properties.
    Type: Grant
    Filed: July 17, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bierigner
  • Patent number: 5126345
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: June 30, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Patent number: 5126453
    Abstract: In a first stage of a process for the preparation of 6-piperidino-2,4-diaminopyrimidine-3-oxide at least one of the two amino groups of a compound having formula (1): ##STR1## where X represents a halogen atom or OH group, is protected by an addition reaction with an isocyanate having formula:R--N=C=OIn this formula R represents an alkyl group, or one of the amino groups. The resulting urea derivative is then oxidized to produce the corresponding N-oxide which is then reacted with piperidine. The protective group(s) are then eliminated by reaction with an organic or inorganic base.
    Type: Grant
    Filed: December 31, 1990
    Date of Patent: June 30, 1992
    Assignee: L'Oreal
    Inventors: Jean Maignan, Serge Restle, Gerard Lang
  • Patent number: 5125960
    Abstract: Herbicidal substituted arylsulphonylaminoguanidinoazines of the formula ##STR1## in which R.sup.1 represents in each case optionally substituted aryl, aralkyl or heteroaryl,R.sup.2 represents hydroxyl or amino, or represents in each case optionally substituted alkoxy or alkylamino,R.sup.3 represents hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X represents nitrogen or a --CH group,Y represents nitrogen or a --CR.sup.4 group, where R.sup.4 represents hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ represents nitrogen or a --CR.sup.5 group, where R.sup.5 represents hydrogen, halogen, hydroxyl, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino,with the exception of the compound N'-(4,6-dimethylpyrimidin-2-yl)-N"-(2-methoxycarbonyl-phenylsulphonylamino )-N"'-(2-methoxycarbonyl-phenylsulphonyl)guanidine.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: June 30, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Hans-Jochem Riebel, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
  • Patent number: 5118339
    Abstract: A pyrimidine or triazine derivative and its salt, said pyrimidine or triazine derivative having the formula: ##STR1## wherein R represents a group of the formula OR.sub.3 {wherein R.sup.3 represents a hydrogen atom, an alkyl gorup, etc.}, a group of the formula SR.sup.6 {wherein R.sup.6 represents a hydrogen atom, an alkyl group, etc.}, a group of the formula ##STR2## {wherein R.sup.7 and R.sup.8 represent a hydrogen atom, an alkyl group, etc.}, or an imidazolyl group:R.sup.1 represents a hydrogen atom, an alkyl group, etc.;R.sup.2 represents a hydroxyl group, an alkyl group, etc.;A and B represent an alkyl group, etc.;Y represents an oxygen atom, etc.; andZ represents a methine group or a nitrogen atom.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: June 2, 1992
    Assignees: Kumiai Chemical Co., Ihara Chemical Industry Co., Ltd.
    Inventors: Masatoshi Tamaru, Norihiro Kawamura, Masahiro Sato, Fumiaki Takabe, Shigehiko Tachikawa, Ryo Yoshida
  • Patent number: 5116404
    Abstract: The present invention provides novel uracil derivatives and pesticides which contain the novel uracil derivatives as an active ingredient, and exhibit preventing and controlling effects against harmful living things, especially agricultural insect pests, sanitary insect pests, stored product insect pests, house insect pests and veterinary insect pests at a very low drug-concentration.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: May 26, 1992
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Shigeru Ishii, Kazunari Nakayama, Kazuo Yagi, Jun Satow, Kenzou Fukuda, Kaoru Itoh, Toshiyuki Umehara, Masaki Kudo, Yoichi Inoue, Tsutomu Nawamaki, Shigeomi Watanabe
  • Patent number: 5104443
    Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is ethyl, propyl or isopropyl,R.sup.2 is halogen, NO.sub.2, CF.sub.3, CN, alkyl, alkoxy, alkylthio or alkoxycarbonyl,n is 0, 1, 2 or 3, Y is O or S,R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl or alkoxy;R.sup.4 is a heterocyclic radical of the formulae ##STR2## E is CH or N; G is O or CH.sub.2, R.sup.5 and R.sup.6 are hydrogen, halogen, or are alkyl, alkoxy or alkylthio, which are optionally substituted by halogen, alkoxy or alkylthio, or are --NR.sup.12 R.sup.13, --OCHR.sup.7 --CO.sub.2 R.sup.12, (C.sub.3 -C.sub.6 cycloalkyl, (C.sub.3 -C.sub.5)alkenyl, (C.sub.2 -C.sub.4) -alkynyl, (C.sub.3 -C.sub.5)alkenyloxy or (C.sub.3 -C.sub.5 (alkynyloxy; R.sup.7 is hydrogen or alkyl, R.sup.8 is alkyl, --CHF.sub.2 or --CH.sub.2 CF.sub.3 ; R.sup.9 and R.sup.10 are hydrogen, alkyl, alkoxy or halogen; R.sup.11 is hydrogen, alkyl, --CHF.sub.2 or CH.sub.2 CF.sub.3 ; R.sup.12 and R.sup.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: April 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5104440
    Abstract: The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylures of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, 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, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.P --C.sub.1 -C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.
    Type: Grant
    Filed: May 8, 1991
    Date of Patent: April 14, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Willy Meyer, Dieter Reinehr, Konrad Oertle, Rolf Schurter
  • Patent number: 5102443
    Abstract: Heterocyclically substituted phenoxysulfonylureas, processes for the preparation thereof, and the use thereof as herbicides or plant growth regulators. Compounds of the formula I or the salts thereof ##STR1## where R.sup.1 is (C.sub.1 -C.sub.8)alkyl, (C.sub.2 -C.sub.8)alkenyl or (C.sub.2 -C.sub.8)alkynyl, these radicals being substituted by halogen, saturated or unsaturated (C.sub.1 -C.sub.6)alkoxy, (C.sub.1 -C.sub.6)alkylthio, -sulfinyl or -sulfonyl, (C.sub.1 -C.sub.6)alkoxycarbonyl, NO.sub.2, CN or phenyl; furthermore is (C.sub.2 -C.sub.8)alkenyl, (C.sub.2 -C.sub.8)alkynyl or (C.sub.3 -C.sub.8)cycloalkyl, which can be substituted by halogen or by alkoxy or alkylthio; (C.sub.5 -C.sub.8)cycloalkenyl, cyclopropylmethyl, epoxypropyl; furfuryl, tetrahydrofurfuryl or phenoxy (C.sub.1 -C.sub.4)alkyl, it being possible for the last three substituents mentioned to be substituted by halogen, alkyl or alkoxy; or phenyl which can be substituted by halogen, alkyl, alkoxy, NO.sub.2, CF.sub.3, CN or OCHF.sub.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: April 7, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5100896
    Abstract: The present invention provides a compound of formula (I) ##STR1## and salts and solvates and pharmaceutically acceptable derivatives thereof, and describes processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of viral diseases, especially those caused by the Herpetoviridae.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: March 31, 1992
    Assignee: Glaxo Group Limited
    Inventors: Alan D. Borthwick, Keith Biggadike, Barrie E. Kirk, Richard Storer, Niall G. Weir, Anthony D. Baxter, Chi L. Mo
  • Patent number: 5096905
    Abstract: The invention relates to elaiophylin derivatives of the formulae (I), (I'), (III) and (III') ##STR1## in which the C.dbd.C double bonds in the 2,3 and 4,5 position may also be hydrogenated and in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings indicated. The invention furthermore relates to a process for the preparation of these elaiophylin derivatives, and the use thereof as pharmaceuticals, in particular as anthelmintic pharmaceuticals.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: March 17, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Kretzschmar, Peter Hammann, Dieter Duwel, Gerhard Wohner, Rudiger Marquardt, Klaus Kuhlein
  • Patent number: 5092917
    Abstract: Herbicidal aminoguanidinoazines of the formula ##STR1## in which R.sup.1 stands for an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and hetaryl,R.sup.2 stands for hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X stands for nitrogen or a --CH group,Y stands for nitrogen or a --CR.sup.3 group whereR.sup.3 stands for hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl, andZ stands for nitrogen or a --CR.sup.4 group whereR.sup.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: March 3, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Hans-Jochem Riebel, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 5087697
    Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. The invention also relates to pharmaceutical formulations and processes for the preparation of compounds according to the invention.
    Type: Grant
    Filed: December 19, 1990
    Date of Patent: February 11, 1992
    Assignee: Burroughs Wellcome Co.
    Inventor: Susan M. Daluge
  • Patent number: 5086177
    Abstract: A process for the preparation of an oxyguanidine of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2, R.sup.3 each is hydrogen or an organic or inorganic substituent,X is N or CH,Y is N or CR.sup.3, andZ is N or CR.sup.4,comprising reacting ##STR2## in which R.sup.5 is optionally substituted alkyl or aralkyl, or its hydrogen halide, with a hydroxylamine derivative of the formulaH.sub.2 N--O--R.sup.1 (III)at a temperature between about 0.degree. C. and 150.degree. C. New isothioureas of the formula ##STR3## are also shown.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: February 4, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Jochem Riebel, Klaus-Helmut Muller
  • Patent number: 5071469
    Abstract: This invention relates to certain herbicidal sulfonamides, agriculturally suitable compositions thereof and a method for their use as a general or selective preemergent or postemergent herbicide or as a plant growth regulant.
    Type: Grant
    Filed: January 24, 1990
    Date of Patent: December 10, 1991
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Steven P. Artz
  • Patent number: 5069710
    Abstract: N-((6-Trifluoromethylpyrimidin-2-yl)- aminocarbonyl)-2-carboalkoxybenzenesulfonamides of the general formula Ia ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or halogen;R.sup.2 is hydrogen, C.sub.1 -C.sub.5 -alkyl, C.sub.3 -C.sub.4 -alkenyl, C.sub.3 -C.sub.4 -alkynyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.3 -C.sub.5 -alkoxyalkyl, C.sub.3 -C.sub.5 -haloalkoxyalkyl or C.sub.5 -C.sub.6 -cycloalkyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.2 -alkyl, allyl, propargyl or C.sub.1 -C.sub.5 -alkoxy,R.sup.4 is halogen, C.sub.1 -C.sub.2 -alkyl, C.sub.1 -C.sub.3 -alkylthio or C.sub.1 -C.sub.3 -alkylamino,R.sup.3 not denoting hydrogen or C.sub.1 -C.sub.2 -alkyl when R.sup.4 is C.sub.1 -C.sub.2 -alkyl, and their environmentally tolerated salts, processes for their manufacture, and their use.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: December 3, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Karl-Otto Westphalen, Gerhard Hamprecht, Bruno Wuerzer, Norbert Meyer
  • Patent number: 5068271
    Abstract: Disclosed are novel 2,4,6 substituted pyrimidines where the substituents may be the same or different groups. At least one substituent must be N-alkyl paraphenylenediamino, and the other substituents may be various radicals containing sulfur, oxygen or nitrogen or hydrogen or alkyl groups. The compounds are useful as antioxidants and antiozonants for unsaturated compounds and polymers.
    Type: Grant
    Filed: July 30, 1990
    Date of Patent: November 26, 1991
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Edward L. Wheeler, Franklin H. Barrows, Robert J. Franko
  • Patent number: 5066662
    Abstract: Oxazolidin-2-ones and 1,2,4-oxadiazolin-5-ones substituted in the 4-position of the oxazolidin-2-one ring and the 3-position of the 1,2,4-oxadiazolin-5-one ring with a 5- or 6-member heteroaromatic, a bicyclic heteroaromatic group or a 5- or 6-member heterocyclic group either directly or via a one or two carbon bridge and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetycholine production or release.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: November 19, 1991
    Assignee: Warner-Lambert Company
    Inventors: Sheila H. Hobbs, Stephen J. Johnson
  • Patent number: 5066663
    Abstract: Substituted-hetero-cyclopentanones and cyclopentenones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: November 19, 1991
    Assignee: Warner-Lambert Company
    Inventor: Sheila H. Hobbs
  • Patent number: 5066665
    Abstract: Substituted isoxazolidin-3-ones and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
    Type: Grant
    Filed: May 21, 1990
    Date of Patent: November 19, 1991
    Assignee: Warner-Lambert Co.
    Inventor: Sheila H. Hobbs
  • Patent number: 5047409
    Abstract: Salts of thiazolidine-4-carboxylic acids with 6-Piperidino-2,4-diaminopyrimidine-3-oxide are described of Formula I. ##STR1## Compounds I are useful in the field of cosmetics and pharmaceuticals for the treatment of loss of hair or in pathological forms such as alopecia, flaking dermatitis, etc. . . . Topical formulations containing compounds I are also described.
    Type: Grant
    Filed: May 21, 1986
    Date of Patent: September 10, 1991
    Assignee: Serono OTC S.A.
    Inventors: Michele G. Di Schiena, Vittoria Orru
  • Patent number: 5043443
    Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4- (4'-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
    Type: Grant
    Filed: July 24, 1990
    Date of Patent: August 27, 1991
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
  • Patent number: 5030270
    Abstract: Sulfonylureas with heterocyclic substituents, a process for the preparation thereof, and the use thereof as herbicides or plant-growth regulators.Sulfonylureas with heterocyclic substituents, of the formula ##STR1## in which the variables are defined in the specification, as well as the salts thereof have herbicidal and plant-growth regulatory properties on mon- and dicotyledonous plants.
    Type: Grant
    Filed: August 3, 1989
    Date of Patent: July 9, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bieringer
  • Patent number: 5015284
    Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.
    Type: Grant
    Filed: April 6, 1989
    Date of Patent: May 14, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 4987135
    Abstract: A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: January 22, 1991
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Takahiro Haga, Nobutoshi Yamada, Hideo Sugi, Toru Koyanagi, Hiroshi Okada
  • Patent number: 4985563
    Abstract: In a first stage of a process for the preparation of 6-piperidino-2,4-diaminopyrimidine-3-oxide at least one of the two amino groups of a compound having formula (1): ##STR1## where x represents a halogen atom or OH group, is protected by an addition reaction with an isocyanate having formula:R--N=C=OIn this formula R represents an alkyl group, or one of the amino groups. The resulting urea derivative is then oxidized to produce the corresponding N-oxide which is then reacted with piperidine. The protective group(s) are then eliminated by reaction with an organic or inorganic base.
    Type: Grant
    Filed: July 29, 1988
    Date of Patent: January 15, 1991
    Assignee: L'Oreal
    Inventors: Jean Maignan, Serge Restle, Gerard Lang
  • Patent number: 4983608
    Abstract: This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or lowealkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: January 8, 1991
    Assignee: Hoechst-Roussell Pharmaceuticals, Inc.
    Inventors: Richard C. Effland, Joseph T. Klein, Larry Davis, Gordon E. Olsen
  • Patent number: 4980469
    Abstract: A process for the preparation of an oxyguanidine of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2, R.sup.3 and R.sup.4 each is hydrogen or an organic or inorganic substituent,X is N or CH,Y is N or CR.sup.3, andZ is N or CR.sup.4,comprising reacting ##STR2## in which R.sup.5 is optionally substituted alkyl or aralkyl, or its hydrogen halide, with a hydroxylamine derivative of the formulaH.sub.2 N--O--R.sup.1 (III)at a temperature between about 0.degree. C. and 150.degree. C. New isothioureas of the formula ##STR3## are also shown.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: December 25, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Jochem Riebel, Klaus-Helmut Muller
  • Patent number: 4970063
    Abstract: A compound has the following composition: ##STR1## or its corresponding ionic form: ##STR2## wherein: n equals 0, 1 or 2, andR.sub.1 and R.sub.2 may be identical or different and represent a hydrogen atom or a linear or branched low alkyl radical having 1 to 6 carbon atoms.
    Type: Grant
    Filed: July 29, 1988
    Date of Patent: November 13, 1990
    Assignee: L'Oreal
    Inventors: Gerard Lang, Jean Maignan, Serge Restle
  • Patent number: 4968796
    Abstract: Disclosed is a process for the preparation of a sulphonylisothiourea of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, and Z are as defined herein, which comprises reacting a sulphonic acid amide of the formulaR.sup.1 --SO.sub.2 --NH.sub.2, (II)or a metal salt thereof, with an N-heteroaryl-iminodithiocarbonic acid S,S-diester of the formula ##STR2## at a temperature between about 20.degree. C. and 200.degree. C. Intermediates and a process for their preparation are also disclosed.
    Type: Grant
    Filed: August 17, 1989
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventor: Hans-Jochem Riebel
  • Patent number: 4968781
    Abstract: A reactive dye of the formula ##STR1## in which Fa is the radical of an organic dye of the monoazo, polyazo, metal complex azo, anthraquinone, phthalocyanine, formazan, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide series, T is a negative substituent, one X is a detachable substituent and the other X is a group of the formula ##STR2## A is arylene, V is hydrogen, a substituted or unsubstituted C.sub.1 -C.sub.4 alkyl radical or a radical of the formula --(CH.sub.2).sub.q --SO.sub.2 --Z, Z is a --CH.dbd.CH.sub.2 or CH.sub.2 --Y radical and Y is an inorganic or organic radical which is detachable under alkaline conditions, q, m and n are independently of one another an integral number from 2 to 6, R and R' are independently of one another hydrogen or substituted or unsubstituted C.sub.1 -C.sub.4 alkyl, and r is 1 or 2.
    Type: Grant
    Filed: March 28, 1988
    Date of Patent: November 6, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Karl Seitz, Karl Hoegerle
  • Patent number: 4963180
    Abstract: Compounds of the formula I or their salts ##STR1## wherein R.sup.1 denotes substituted alkyl; (subst.) alkenyl; (subst.) alkynyl; R.sup.2 denotes halogen; nitro; (subst.) alkyl or (subst.) alkoxy; R.sup.3 denotes hydrogen; alkyl; alkenyl or alkynyl; R.sup.4 denotes a heterocyclic radical or the formulae ##STR2## where E is CH or N; and n denotes 0, 1, 2 or 3, possess excellent herbicidal and plant growth-regulating properties.
    Type: Grant
    Filed: August 3, 1988
    Date of Patent: October 16, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Lothar Willms, Heinz Kehne, Klaus Bauer, Hermann Bieringer
  • Patent number: 4960888
    Abstract: The invention relates to a new process for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine of the formula (I), ##STR1## which comprises reacting a pyrimidine derivative of the general formula (II), ##STR2## wherein R.sub.1 stantds for hydrogen or a ##STR3## group, wherein R means a C.sub.1-6 alkyl group or an aryl group optionally substituted by halogen;R.sub.2 stands for a hydroxyl group or an ##STR4## group, wherein R is as defined above; andX represents chlorine or bromine or an optionally mono- or polysubstituted arenesulfonyloxy group,with the proviso that R.sub.2 is different from a hydroxyl group when R.sub.1 stands for hydrogen, with piperidine and hydrolyzing, optionally after isolation, the thus-obtained 4-piperidino derivative of the general formula (III), ##STR5## wherein R.sub.1 and R.sub.2 are as defined above.
    Type: Grant
    Filed: March 9, 1989
    Date of Patent: October 2, 1990
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Andras Vedres, Csaba Szantay, Bela Stefko, Janos Kreidl, Andras Nemes, Gabor Blasko, Erik Bogsch, Denes Mathe, Istvan Hegedus, Adrien Szuchovszky, nee Gergely, Tamas Mester
  • Patent number: 4959474
    Abstract: A novel class of 2,4-diamino-6-(2,5-dialkoxybenzyl)-5-methyl[2,3-d]-pyrimidines is described. These compounds are antibacterial agents, active against certain Streptococcus species. They are also active antiproliferative agents.
    Type: Grant
    Filed: October 15, 1985
    Date of Patent: September 25, 1990
    Assignee: Burroughs Wellcome Co.
    Inventor: Eugene M. Grivsky
  • Patent number: 4954628
    Abstract: The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: September 4, 1990
    Assignees: Nitrokaelepek, Magyar Tudomanyos Akademia Kozponti Kemiai Kutato Intezete
    Inventors: Gabor Besenyei, Sandor Nemeth, Laszlo Simandi, Maria Belak, Maria Szabo, Jozsef Dukai, Lajos Nagy, Elemer Tomordi, Csaba Soptei, Erzsebet E. Dioszegine
  • Patent number: 4952679
    Abstract: Reactive dyes suitable for dyeing and printing cellulosic fiber materials by the cold pad-batch process having the formula ##STR1## wherein Fa is a monoazo or polyazo, metal complex azo, anthraquinone, phthalocyanine, formazane, azomethine, dioxazine, phenazine, stilbene, triphenylmethane, xanthene, thioxanthone, nitroaryl, naphthoquinone, pyrenequinone or perylenetetracarbimide dye radical, X.sub.1 is halogen, C.sub.1 -C.sub.4 -alkylsulfonyl, phenylsulfonyl, a sulfonic acid or phosphoric acid group or a quaternized ammonium group, X.sub.2 independently has the meaning of X.sub.1 or is C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 alkoxy, R is hydrogen or C.sub.1 -C.sub.4 -alkyl which is unsubstituted or substituted by halogen, hydroxy, cyano, carboxyl, sulfo, sulfato, C.sub.1 -C.sub.4 -alkoxycarbonyl or C.sub.1 -C.sub.4 -alkoxy, and r is 1 or 2.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: August 28, 1990
    Assignee: Ciba-Geigy Corporation
    Inventor: Karl Hoegerle
  • Patent number: 4952233
    Abstract: Herbicidally active sulphonylamino guanidinoazines of the formula ##STR1## in which R.sup.1 stands for a optionally substituted radical from the series comprising alkyl, aralkyl, aryl and hetaryl, R.sup.2 stands for an optionally substituted radical from the series comprising alkyl, aralkyl, aryl, hetaryl and dialkylamino, R.sup.3 stands for hydrogen, halogen, hydroxyl, alkyl, halogenoalkyl, alkoxyalkyl, alkoxy, halogenoalkoxy, alkylthio, halogenoalkylthio, amino, alkylamino or dialkylamino,X stands for nitrogen or a --CH-- grouping,Y stands for nitrogen or a --CR.sup.4 -- grouping,whereinR.sup.4 stands for hydrogen, halogen, cyano, alkyl, formyl, alkyl-carbonyl or alkoxy-carbonyl,Z stands for mitrogen or a --CR.sup.5 -- grouping,whereinR.sup.
    Type: Grant
    Filed: August 2, 1988
    Date of Patent: August 28, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus-Helmut Muller, Christa Fest, Rolf Kirsten, Theodor Pfister, Hans-Jochem Riebel, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
  • Patent number: 4948416
    Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4946956
    Abstract: Disclosed are novel 2,4,6 substituted pyrimidines where the substituents may be the same or different groups. At least one substituent must be N-alkyl parphenylenediamino, and the other substituents may be various radicals containing sulfur, oxygen or nitrogen or hydrogen or alkyl groups. The compounds are useful as antioxidants and antiozonants for unsaturated compounds and polymers.
    Type: Grant
    Filed: September 21, 1988
    Date of Patent: August 7, 1990
    Assignee: Uniroyal Chemical Company, Inc.
    Inventors: Edward L. Wheeler, Franklin H. Barrows, Robert J. Franko
  • Patent number: 4944792
    Abstract: N-phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the general formula ##STR1## and the salts of these compounds with amines, alkali metal or alkaline-earth metal bases or with quaternary ammonium bases have good selective, pre- and post-emergence, herbicidal and growth-regulating properties.The symbols in this formula have the following meanings:A is a C.sub.3 -C.sub.6 -alkynyl group, a C.sub.1 -C.sub.6 -alkyl group which is substituted by halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.1 -C.sub.4 -haloalkylsulfinyl or C.sub.1 -C.sub.4 -haloalkylsulfonyl, or it is a C.sub.2 -C.sub.6 -alkenyl group substituted by one of the above substituents,E is the methine group or nitrogen,X is oxygen, sulfur, or a sulfinyl or sulfonyl bridge,Z is oxygen or sulfur,m is the number one or two,R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.2 -C.sub.
    Type: Grant
    Filed: January 16, 1986
    Date of Patent: July 31, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Willy Meyer, Werner Fory, Karl Gass
  • Patent number: 4945093
    Abstract: A compound having formula: ##STR1## is described, where R.sub.3 and R.sub.4 may be identical or different and represent a hydrogen atom, alkyl, alkenyl, cycloalkyl;or R.sub.3 and R.sub.4 represent aryl aralkyl;or R.sub.3 and R.sub.4 together with the nitrogen atom linked thereto form a heterocycle;R.sub.1 and/or R.sub.2, independent of each other, represent hydrogen or carbanoyl having formula: ##STR2## where R.sub.7 represents alkyl, alkenyl, cycloalkyl, aryl or aralkyl. The compounds of formula (I) can be used in cosmetic or pharmaceutical compositions for the cosmetic treatment of hair, the treatment of alopecia, and also for the treatment of desquamating dermatitis.
    Type: Grant
    Filed: July 29, 1988
    Date of Patent: July 31, 1990
    Assignee: L'Oreal
    Inventors: Jean Maignan, Serge Restle, Gerard Lang
  • Patent number: 4942234
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: February 28, 1989
    Date of Patent: July 17, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
  • Patent number: 4940792
    Abstract: Novel substituted N-sulfonyl-N'-pyrimidinylureas or N-sulfonyl-N'-triazinylureas of the formula I ##STR1## have good pre- and postemergence selective herbicidal and growth regulating properties.In this formulaE is nitrogen or --CH.dbd.,the group ##STR2## is a phenyl, naphthyl, furyl, thiophenyl, pyrrole or pyridinyl radical which is substituted in accordance with the definitions ofR.sup.1 and R.sup.2,R.sup.3 and R.sup.4 are hydrogen, lower alkyl or lower alkoxy, or one of R.sup.3 and R.sup.4 may also be halogen, lower alkenyl, lower haloalkenyl, lower haloalkoxy, amino, lower alkylamino, --CH(OCH.sub.3).sub.2, a cyclized ketal group or a saturated 5- or 7-membered heterocycle which is bound through the nitrogen atom,R.sup.5 is hydrogen, lower alkyl, lower haloalkyl, or an unsubstituted or substituted phenyl, benzyl or naphthyl radical, andR.sup.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: July 10, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Werner Topfl, Willy Meyer, Hans-Dieter Schneider
  • Patent number: RE33298
    Abstract: The invention relates to new 1-(2-oxyaminosulphonylphenylsulphonyl)-3-heteroaryl-ureas of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl andR.sup.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: August 14, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt