Patents by Inventor Herbert Thomas

Herbert Thomas has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 4127670
    Abstract: N-(2-formamidophenyl)-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(formamido)-phenyl group are anthelminetic agents. The compounds, of which N-(2-formamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoformanilide.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: November 28, 1978
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Heinrich Kolling, Herbert Thomas
  • Patent number: 4120961
    Abstract: Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is O; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.
    Type: Grant
    Filed: July 20, 1977
    Date of Patent: October 17, 1978
    Assignee: E. Merck
    Inventors: Jurgen Seubert, Rolf Pohlke, Herbert Thomas, Peter Andrews
  • Patent number: 4113867
    Abstract: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.
    Type: Grant
    Filed: November 15, 1976
    Date of Patent: September 12, 1978
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Jurgen Seubert, Herbert Thomas, Peter Andrews
  • Patent number: 4094975
    Abstract: O-Alkyl-O-chloromethylsulfonylphenyl-thionophosphonic acid esters of the formula ##STR1## in which R represents alkyl with 1 to 6 carbon atoms,R' represents alkyl with 1 to 6 carbon atoms or phenyl andR" represents hydrogen or halogen,Which possess insecticidal, acaricidal and nematicidal properties.
    Type: Grant
    Filed: February 2, 1977
    Date of Patent: June 13, 1978
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Hans-Jochem Riebel, Rolf Schroder, Wilhelm Sirrenberg, Ingeborg Hammann, Bernhard Homeyer, Herbert Thomas
  • Patent number: 4088780
    Abstract: N-[2-(Substituted amido)phenyl]-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoanilide.
    Type: Grant
    Filed: May 26, 1976
    Date of Patent: May 9, 1978
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 4064270
    Abstract: A new class of N'-(aminoacylaminophenyl) acetamidines: ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R.sup.3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics.The products are obtained by treating a suitable amino-acid or a carbonyl-activated amino-acid, with the appropriate N'-(4-aminophenyl)-N,N-dimethylacetamidine. In addition, the products are obtained by treating a suitable N'-(haloacylaminophenylacetamidine with an appropriate amine.
    Type: Grant
    Filed: September 13, 1974
    Date of Patent: December 20, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Ekkehard Niemers, Hans Peter Schulz, Herbert Thomas, Peter Andrews
  • Patent number: 4051243
    Abstract: Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is 0; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.
    Type: Grant
    Filed: August 26, 1975
    Date of Patent: September 27, 1977
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Jurgen Seubert, Rolf Pohlke, Herbert Thomas, Peter Andrews
  • Patent number: 4032655
    Abstract: N-[2-(Substituted amido)phenyl]-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoanilide.
    Type: Grant
    Filed: June 7, 1976
    Date of Patent: June 28, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 4024176
    Abstract: N-[2-(Substituted amido)phenyl]-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoanilide.
    Type: Grant
    Filed: May 26, 1976
    Date of Patent: May 17, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 4024236
    Abstract: Helmintic infestations can be treated with an N-carbalkoxy-N'-(2-amido-5-alkylphenyl)-S-substituted-isothiourea. A typical embodiment is the treatment of Bunostomum trigonocephalum in sheep utilizing N-methoxycarbonyl-N'-(2-butyramido-5-n-butylphenyl)-S-methylisothiourea. Compositions adapted for this use are also described.
    Type: Grant
    Filed: May 19, 1975
    Date of Patent: May 17, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Arno Widdig, Engelbert Kuhle, Herbert Thomas, Hans Peter Schulz
  • Patent number: 4021571
    Abstract: N-[2-(Substituted amido)phenyl]-N'-carbonyl-S-substituted isothioureas bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenoxyphenyl)-N'-carbomethoxy-S-methylthiourea is a typical example, are prepared through the reaction of S-substituted N-(mercaptohalomethylene)carbamic acid ester and an appropriately substituted 2-aminoanilide, or through alkylation of the corresponding S-unsubstituted thiourea.
    Type: Grant
    Filed: June 4, 1976
    Date of Patent: May 3, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 4015012
    Abstract: New 4-acylaminophenylacetamidines of the formula: ##STR1## in which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
    Type: Grant
    Filed: May 21, 1975
    Date of Patent: March 29, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Ekkehard Niemers, Hans Peter Schulz, Herbert Thomas, Peter Andrews
  • Patent number: 4005123
    Abstract: N-[2-(Substituted amido)phenyl]-N'-carbonyl-S-substituted isothioureas bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)-phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenoxyphenyl)-N'-carbomethoxy-S-methylthiourea is a typical example, are prepared through the reaction of S-substituted N-(mercaptohalomethylene)carbamic acid ester and an apropriately substituted 2-aminoanilide, or through alkylation of the corresponding S-unsubstituted thiourea.
    Type: Grant
    Filed: July 11, 1975
    Date of Patent: January 25, 1977
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 4001411
    Abstract: 2-Acyl-4-oxo-hexahydro-4H-pyrazino[2,1-a]isoquinoline derivatives of the formula ##STR1## wherein COR is the acyl radical of an up to 26 carbon atom acid and their physiologically acceptable acid addition and quaternary ammonium salts, are anthelmintics and can be produced by reacting 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline with an acid or a reactive functional derivative thereof.
    Type: Grant
    Filed: December 16, 1974
    Date of Patent: January 4, 1977
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Jurgen Seubert, Herbert Thomas, Peter Andrews
  • Patent number: 3993682
    Abstract: N-[2-(Substituted amido)phenyl]-N',N"-bis-carbonylguanidines bearing an optionally substituted phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl group in the 4- or 5-position of the 2-(substituted amido)phenyl group are anthelmintic agents. The compounds, of which N-(2-acetamido-4-phenylthiophenyl)-N',N"-bis-carbomethoxyguanidine is a typical example, are prepared through the reaction of isothiourea-S-alkyl ether and an appropriately substituted 2-aminoanilide.
    Type: Grant
    Filed: April 28, 1975
    Date of Patent: November 23, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Herbert Thomas, Arno Widdig, Hartmund Wollweber
  • Patent number: 3993759
    Abstract: 2-Benzoyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline is used as an anthelmintic against cestodes and trematodes, preferably in admixture with a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 11, 1974
    Date of Patent: November 23, 1976
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rolf Pohlke, Friedrich Loebich, Herbert Thomas, Jurgen Thyssen
  • Patent number: 3993760
    Abstract: (-)-2-Benzoyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline is prepared by benzoylation of (-)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline, or cyclization of a compound of the formula ##SPC1##Wherein X is F, Cl, Br, I or O-tosyl and which has the optical configuration of the final product, or cyclization of a compound of the formula ##SPC2## wherein Y is OH, alkoxy, F, Cl, Br or I under HY-removing reaction conditions and which has the optical configuration of the final product, which is an anthelmintic.
    Type: Grant
    Filed: June 21, 1974
    Date of Patent: November 23, 1976
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rolf Pohlke, Friedrich Loebich, Jurgen Seubert, Herbert Thomas, Peter Andrews
  • Patent number: 3970699
    Abstract: New 4-acylaminophenylacetamidines of the formula: ##SPC1##In which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
    Type: Grant
    Filed: September 13, 1974
    Date of Patent: July 20, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hartmund Wollweber, Ekkehard Niemers, Hans Peter Schulz, Herbert Thomas, Peter Andrews
  • Patent number: 3968314
    Abstract: Benzoylphenylisothioureas of the formula: ##SPC1##WhereinR is alkyl of 1 to 12 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, alkenyl of 2 to 12 carbon atoms or aralkyl unsubstituted or substituted in the aryl moiety by one or more substituents selected from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and halogen;R.sup.1 is alkyl of 1 to 4 carbon atoms, cyclohexyl or phenyl; andR.sup.
    Type: Grant
    Filed: January 14, 1974
    Date of Patent: July 6, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Arno Widdig, Herbert Thomas, Hans Peter Schulz
  • Patent number: 3950395
    Abstract: Benzoylphenylguanidines of the formula ##SPC1##WhereinR.sup.1 is alkyl of 1 to 4 carbon atoms;R.sup.2 is hydrogen; alkyl of 1 to 18 carbon atoms unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, cyano, alkoxy of 1 to 4 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms, phenoxy, halophenoxy, alkylphenoxy and alkoxyphenoxy; cycloalkyl of 5 to 8 carbon atoms; aralkyl unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms and alkoxy of 1 to 4 carbon atoms; aryl unsubstituted or substituted by one or more substituents selected from the group consisting of halogen, alkyl of 1 to 4 carbon atoms and alkoxy of 1 to 4 carbon atoms;Z is OR.sup.1 wherein R.sup.1 is as above defined orR.sup.3 wherein R.sup.
    Type: Grant
    Filed: January 28, 1974
    Date of Patent: April 13, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinrich Kolling, Arno Widdig, Herbert Thomas, Hans Peter Schulz