Patents by Inventor Bernward Scholkens

Bernward Scholkens 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: 5185324
    Abstract: The present invention relates to compounds of the general formula I ##STR1## in which A denotes a radical from the group comprising S, SO, SO.sub.2, O, CO, CS or a direct bond,B denotes the radical of an amino acid andD denotes a CH.sub.2 group or a radical --NR.sup.7 --, where R.sup.7 can be hydrogen or a (C.sub.1 -C.sub.4)alkyl radical;and in which R.sup.1 to R.sup.4 are defined as indicated in the description, to a process for the preparation thereof, to agents containing these, and to the use thereof.
    Type: Grant
    Filed: December 12, 1989
    Date of Patent: February 9, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5169841
    Abstract: The invention relates to compounds of the formula 1 ##STR1## in which A.sup.1 denotes a radical of the formulae ##STR2## A.sup.2 is absent or represents a radical of the formula ##STR3## R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and X and Y, independently of one another, represent --O-- or --NR.sup.13 --, and to the salts thereof. Also described is a process for the preparation of the compounds of the formula 1, corresponding pharmaceutical products, and the use thereof as medicines, and intermediates for the preparation of these compounds.
    Type: Grant
    Filed: November 3, 1988
    Date of Patent: December 8, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleeman, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5162362
    Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: November 10, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
  • Patent number: 5158959
    Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: October 27, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
  • Patent number: 5130310
    Abstract: Benzo[b]pyran derivatives of the formula I ##STR1## with E--D equal to CH--CHOH or C.dbd.CH;X equal to oxygen or sulfur;Y equal to oxygen, sulfur, SO, SO.sub.2 or NR.sup.9 ;R.sup.1 equal to CN, NO.sub.2, Hal, alkoxycarbonyl, SO.sub.1-2 -alkyl or SO.sub.1-2 -aryl;R.sup.2 equal to H, OH, alkoxy, alkyl, Hal, NR.sup.10 R.sup.11 ;R.sup.3 /R.sup.4 equal to alkyl;R.sup.5 /R.sup.6 equal to alkyl, (CH.sub.2).sub.1-6 COO-alkyl, (CH.sub.2).sub.1-6 CONR.sup.10 R.sup.11, (CH.sub.2).sub.0-6 COOH, (CH.sub.2).sub.1-6 CO-alkyl, CO.sub.2 -alkyl, alkylmercaptoalkyl, alkylsulfi(i)(o)nyl, hydroxyalkyl, mercaptoalkyl, aminoalkyl, N-(di)-alkylaminoalkyl or (CH.sub.2).sub.f Ar with f equal to zero-3;R.sup.7 /R.sup.8 equal to hydrogen, alkyl or phenyl, and m equal to zero-2are outstanding antihypertensives and spasmolytics. Preparation processes and use are described.
    Type: Grant
    Filed: January 19, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Weidman, Heinrich C. Englert, Bernward Scholkens, Martin Bickel
  • Patent number: 5116835
    Abstract: Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof.The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,X as desired can be absent or represents --O--, --S--, --CF.sub.2 --, --CO-- or --CHR.sup.8,p and q denote, independently of one another, 0, 1, 2, 3 or 4, andR.sup.1 to R.sup.4 are defined in the description, as well as the salts thereof.The invention furthermore relates to a process for the preparation of the compounds of the formula I and to the use thereof as medicines.
    Type: Grant
    Filed: December 7, 1989
    Date of Patent: May 26, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Ruger, Hansjorg Urbach, Dieter Ruppert, Bernward Scholkens
  • Patent number: 5091394
    Abstract: Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylakyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 -C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(5) are together an alkylene chain,and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmics.
    Type: Grant
    Filed: September 4, 1990
    Date of Patent: February 25, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich C. Englert, Hans-Jochen Lang, Wolfgang Linz, Bernward Scholkens, Wolfgang Scholz
  • Patent number: 5061722
    Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and 2 denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
    Type: Grant
    Filed: January 12, 1989
    Date of Patent: October 29, 1991
    Assignee: Hoechst AG
    Inventors: Volker Teetz, Rolf Geiger, Hansjorg Urbach, Reinhard Becker, Bernward Scholkens
  • Patent number: 5053519
    Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
    Type: Grant
    Filed: February 28, 1989
    Date of Patent: October 1, 1991
    Assignee: Hoechst AG
    Inventors: Volker Teetz, Rolf Geiger, Hansjorg Urbach, Reinhard Becker, Bernward Scholkens
  • Patent number: 5043344
    Abstract: Compounds I ##STR1## where R.sup.1 is H, alkyl, alkoxy, CO alkyl, COOH, carboxyalkyl, CONR.sub.2, CN, NO.sub.2, alkylsulfi(o)nyl, arylsulfi(i)-nyl; R.sup.2 is H, OH, alkoxy, alkyl or alkylcarbonyl, R.sup.3 /R.sup.4 are alkyl, m is zero or one and X is --CR.sup.6 .dbd.CR.sup.7 -(--CR.sup.8 .dbd.CR.sup.9) (R.sup.6 R.sup.9 are H or alkyl), where n is zero or 1, are described. They are active antihypertensives and spasmolytics for the bladder, intestine, gall bladder, uterus, trachea and ureter.
    Type: Grant
    Filed: March 29, 1989
    Date of Patent: August 27, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich C. Englert, Dieter Mania, Bernward Scholkens, Roland Utz
  • Patent number: 5025010
    Abstract: A description is given of compounds I ##STR1## with R(1) equal to H, alkyl, alkoxy, Hal, NO.sub.2, OH, acetamido or amino; R(2) equal to H, alk(en)yl or phenylalkyl; R(3) equal to H, (cyclo)alk(en)yl(alkyl), phenyl or phenylalkyl; R(4) equal to H, alkyl, alkoxy, Hal CF.sub.3, NO.sub.2, OH, acetamido or amino; A equal to --C.tbd.C-- or --CH.dbd.CH--; R(5) equal to various amines; m and n equal to 1-3; and their salts. Preparation processes are also described. Compounds I are excellent calcium agonists or calcium antagonists. They also act to regulate the blood glucose.
    Type: Grant
    Filed: October 17, 1989
    Date of Patent: June 18, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Raymond Oekonomopulos, Rainer Henning, Ulrich Lerch, Bernward Scholkens, Wolfgang Linz
  • Patent number: 4999371
    Abstract: 3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.
    Type: Grant
    Filed: February 2, 1988
    Date of Patent: March 12, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinrich C. Englert, Hans-Jochen Lang, Dieter Mania, Bernward Scholkens
  • Patent number: 4879403
    Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
    Type: Grant
    Filed: November 2, 1988
    Date of Patent: November 7, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Teetz, Rolf Geiger, Hansjorg Urbach, Reinhard Becker, Bernward Scholkens
  • Patent number: 4861755
    Abstract: The invention relates to new peptides of the formula ##STR1## in which X, A, B, C, N', E, F, G and Z have the meanings indicated in the description, to a process for their preparation, to agents containing them, and to their use.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: August 29, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gerhard Breipohl, Jochen Knolle, Wolfgang Konig, Bernward Scholkens
  • Patent number: 4857520
    Abstract: The invention relates to compounds of the formula I ##STR1## in which m denotes 1 or 2 and n denotes, 0, 1 or 2; R.sup.1 and R.sup.2 denote identical or different radicals from the series comprising hydrogen, optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, partly hydrogenated aryl and optionally substituted aralkyl; R.sup.3 and R.sup.4 denote identical or different radicals from the series comprising hydrogen, alkyl, alkenyl and optionally substituted aralkyl; Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxo, and X denotes optionally substituted alkyl, alkenyl, cycloalkyl, optionally substituted 4-piperidinyl, optionally substituted aryl or indolyl, processes for their preparation, medicaments containing these compounds and their use, and to intermediates in their preparation.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: August 15, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hansjorg Urbach, Rainer Henning, Bernward Scholkens, Reinhard Becker
  • Patent number: 4855286
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 is absent or denotes hydrogen, alkyl or acyl, A denotes an acyl radical or an amino acid residue, B denotes an amino acid residue, and R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and to their salts, to a process for their preparation, to pharmaceutical products containing them, and to their use as medicaments, and intermediates for the preparation of these compounds.
    Type: Grant
    Filed: July 28, 1987
    Date of Patent: August 8, 1989
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Adalbert Wagner, Heinz-Werner Kleemann, Dieter Ruppert, Bernward Scholkens
  • Patent number: 4727160
    Abstract: Compounds of the formula I ##STR1## in which the carboxyl group on carbon atom 3 is orientated in the endo-position relative to the bicyclic ring system of cis-configuration, and in which R.sup.1 denotes hydrogen, allyl, vinyl or a side-chain of a naturally occurring .alpha.-aminoacid, which may be protected, R.sup.2 denotes hydrogen, alkyl, alkenyl or aralkyl, Y denotes hydrogen or hydroxyl and Z denotes hydrogen, or Y and Z together denote oxygen, and X denotes alkyl, alkenyl or cycloalkyl, or aryl which is optionally mono-, di- or tri-substituted by alkyl, alkoxy, hydroxyl, halogen, nitro, amino, alkylamino, dialkylamino or methylenedioxy, or denotes indol-3-yl, a process for their preparation, agents containing these compounds and their use.
    Type: Grant
    Filed: October 9, 1984
    Date of Patent: February 23, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Teetz, Rolf Geiger, Hansjorg Urbach, Reinhard Becker, Bernward Scholkens
  • Patent number: 4624962
    Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.
    Type: Grant
    Filed: February 1, 1985
    Date of Patent: November 25, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
  • Patent number: 4595675
    Abstract: What are disclosed are indole, quinoline and isoquinoline compounds of the formula ##STR1## in which n denotes 0 or 1, m denotes 1 or 2, but (n+m).ltoreq.2, A together with the bridgehead carbon atoms denotes a benzene or a cyclohexane ring, Y.sub.1 denotes hydrogen, lower alkanoyl or lower cycloalkanoyl, benzoyl nicotinoyl or a radical of the formula II, and Y.sub.2 denotes methyl, amino, lower alkanoylamino, lower cycloalkanoylamino, benzoylamino or nicotinoylamino, and salts thereof, useful as hypotensive agents, and methods for making the same.
    Type: Grant
    Filed: January 2, 1985
    Date of Patent: June 17, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rolf Geiger, Volker Teetz, Bernward Scholkens, Hans Wissmann
  • Patent number: 4515803
    Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.
    Type: Grant
    Filed: September 1, 1982
    Date of Patent: May 7, 1985
    Assignee: Hoechst Aktiengesellschafat
    Inventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens