Patents by Inventor Hans-Jochen Schliep
Hans-Jochen Schliep 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).
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Patent number: 5434149Abstract: The present invention relates to thiadiazinones of the formula I ##STR1## having a phosphodiesterase-inhibiting action and which are suitable for combating cardiovascular and asthmatic disorders.Type: GrantFiled: March 31, 1994Date of Patent: July 18, 1995Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Michael Klockow, Hans-Jochen Schliep, Michael Wolf
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Patent number: 5276027Abstract: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are each independently of one another H or A,R.sup.3 is H, OA or O--C.sub.m H.sub.2m+1-n X.sub.n,R.sup.4 is --O--C.sub.m H.sub.2m+1-n X.sub.n,X is F or Cl,A is alkyl having 1-6 C atoms,m is 1, 2, 3, 4, 5 or 6 andn is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13, and their salts have positive ionitropic activity and vasodilating action, and promote circulation. In addition, the compounds can be employed for the treatment of asthmatic disease and memory disorders, and have anti-depressive and anti-inflammatory properties.Type: GrantFiled: October 22, 1992Date of Patent: January 4, 1994Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Michael Klockow, Joachim Leibrock, Hans-Jochen Schliep, Christoph Seyfried, Michael Wolf
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Patent number: 5104881Abstract: New 2-arylimidazopyridines of the general formula I ##STR1## wherein --A.dbd.B-- is (a) --CH.dbd.N-- or (b) N.dbd.CH--,Ar is a phenyl radical, which, in case (a), is substituted by one or two alkynyloxy, cyanomethoxy, carboxymethoxy, and/or alkyloxycarbonylmethoxy groups, and can be substituted by one or two additional hydroxyl, alkyloxy, alkenyloxy and/or alkynyloxy groups, or which in case (b), is substituted by one to three hydroxyl, mercapto, and/or --Z--R groups, Z is --O--, --S-- or --SO-- andR is alkyl, alkenyl, alkynyl, hydroxyalkyl, cyanomethyl, carboxymethyl or alkyloxycarbonylmethyl, the alkyl, alkenyl, alkynyl and hydroxyalkyl groups each having up to 5 C atoms, but wherein in case (b), the phenyl radical is only substituted by hydroxyl or methoxy groups if it has at the same time at least one other substituent differing from these,and their physiologically acceptable salts show positive inotropic effects.Type: GrantFiled: March 29, 1984Date of Patent: April 14, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Klaus Minck, Hans J. Enenkel, Hans-Jochen Schliep
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Patent number: 4987133Abstract: New salicylic acid derivatives of the general formula I ##STR1## in which R.sup.1 is H or CH.sub.3,R.sup.2 is 4-(4-methyl-2-thiazolyl)-piperazino, 4-(tetrahydro-2-furoyl)-piperazino, 4-(4-methyl-2-thiazolyl)-homopiperazino, 4-benzamidopiperidino, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolino, 1-imidazolyl, tribromo-1-imidazolyl or 2-(3-indolyl-1,1-dimethyl-ethylamino andR.sup.3 is alkoxy having 1-C atoms, NH.sub.2 or alkylamino having 1-4 C atoms,as well as the physiologically acceptable acid addition salts thereof, exhibit effects on the circulation, especially effects lowering the blood pressure and relieving the heart, and diuretic effects.Type: GrantFiled: April 17, 1989Date of Patent: January 22, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Adolf Kurmeier, Wolf-Dietrich Weber, Hans-Eckart Radunz, Hans-Jochen Schliep
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Patent number: 4916128Abstract: Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently H, C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkinyl,R.sup.3 is also C.sub.1-15 -acyl,R.sup.6 is H, alkyl, alkoxyl, OH, F, Cl, Br or I andZ is (H, H), (H, alkyl), (alkyl, alkyl) or O,the alkyl, alkenyl, alkinyl and/or alkoxy groups in each case containing up to 5 C atoms, but wherein, if A is --CH.sub.2 CH.sub.2 -- and Z is O, one of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.6 must be other than H,and salts thereof demonstrate positive inotropic action and are suitable for combating cardiovascular diseases.Type: GrantFiled: June 6, 1988Date of Patent: April 10, 1990Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Jaime Piulats, Michael Klockow, Ingeborg Lues, Hans-Jochen Schliep
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Patent number: 4654344Abstract: 2-Aryltetraazaindenes of the formula ##STR1## wherein --A-- is --N.dbd.CH--CN.dbd.N-- or --CH.dbd.N--N.dbd.CH--, Ar is unsubstituted phenyl or phenyl mono-, di- or tri-substituted by hydroxyl, mercapto, dialkylamino, trifluoromethyl and/or --Z--R groups, Z is --O--, --S-- or --SO-- and R is alkyl, alkenyl, alkynyl or cyanomethyl, the alkyl, alkenyl and alkynyl groups each having up to 5 C atoms, and their physiologically acceptable salts, exhibit blood pressure, myocardial contraction, and anti-ulcer activities.Type: GrantFiled: December 20, 1985Date of Patent: March 31, 1987Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rochus Jonas, Michael Kloft, Hanns Wurziger, Juergen Harting, Hans J. Enenkel, Klaus-Otto Minck, Hans-Jochen Schliep
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Patent number: 4575505Abstract: 2-Aryltetraazaindenes of the formula ##STR1## wherein --A-- is --N.dbd.CH--CH.dbd.N-- or --CH.dbd.N--N.dbd.CH--, Ar is unsubstituted phenyl or phenyl mono-, di- or trisubstituted by hydroxyl, mercapto, dialkylamino, trifluoromethyl and/or --Z--R groups, Z is --O--, --S-- or --SO-- and R is alkyl, alkenyl, alkynyl or cyanomethyl, the alkyl, alkenyl and alkynyl groups each having up to 5 C atoms, and their physiologially acceptable salts, exhibit blood pressure, myocardial contraction, and anti-ulcer activities.Type: GrantFiled: July 26, 1984Date of Patent: March 11, 1986Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Michael Kloft, Hanns Wurziger, Jurgen Harting, Hans J. Enenkel, Klaus-Otto Minck, Hans-Jochen Schliep
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Patent number: 4477454Abstract: 2-Aryltetraazaindenes of the formula ##STR1## wherein --A-- is --N.dbd.CH--CH.dbd.N-- or --CH.dbd.N--N.dbd.CH--, Ar is unsubstituted phenyl or phenyl mono-, di- or tri-substituted by hydroxyl, mercapto, dialkylamino, trifluoromethyl and/or --Z--R groups, Z is --O--, --S-- or --SO-- and R is alkyl, alkenyl, alkynyl or cyanomethyl, the alkyl, alkenyl and alkynyl groups each having up to 5 C atoms, and their physiologically acceptable salts, exhibit blood pressure, myocardial contraction, and anti-ulcer activities.Type: GrantFiled: May 9, 1983Date of Patent: October 16, 1984Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rochus Jonas, Michael Kloft, Hanns Wurziger, Juergen Harting, Hans J. Enenkel, Klaus-Otto Minck, Hans-Jochen Schliep
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Patent number: 4309441Abstract: 13-Thiaprostanoic acid derivatives of the general formula I ##STR1## wherein A is --CO-- or --CHOH--; B is --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--; Q is 1,4-phenylene or 1,4-naphthylene; R.sup.1 is H or OH; R.sup.2 is H or CH.sub.3 ; R.sup.3 is alkyl with 1-8 carbon atoms or alkyl with 1-8 carbon atoms substituted by (a) phenyl, (b) phenyl substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; (c) phenoxy or (d) phenoxy substituted by at least one of CH.sub.3, F, Cl, Br, OH, OCH.sub.3 or CF.sub.3 ; and R.sup.4 is NH.sub.2, CH.sub.3, phenyl, p-acetylaminophenyl, p-benzoylaminophenyl or phenylamino. These compounds are useful for lowering blood pressure as well as for other pharmaceutical purposes. They also are useful intermediates for the preparation of other known pharmaceuticals such s the 13-thiaprostaglandins.Type: GrantFiled: November 21, 1979Date of Patent: January 5, 1982Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Hans-Eckart Radunz, Dieter Orth, Manfred Baumgarth, Hans-Jochen Schliep, Hans-Joachim Enenkel
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Patent number: 4289768Abstract: Phenothiazine derivatives of the formula ##STR1## wherein R is H, F, Cl, Br, I, CH.sub.3, CF.sub.3, CN, CH.sub.3 O or CH.sub.3 CO; Y is S, SO, or SO.sub.2 ; Z is imidazol-1-yl, 2-methyl-imidazol-1-yl, pyrazol-1-yl or benzimidazol-1-yl; and n is 1, 2 or 3; or the physiologically acceptable acid addition salts thereof; are useful as antihypertensive agents, for example.Type: GrantFiled: May 2, 1980Date of Patent: September 15, 1981Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Gante, Hans-Eckart Radunz, Dieter Orth, Hans-Jochen Schliep, Ernst Schorscher
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Patent number: 4260628Abstract: 2-Guanidinomethyl-indolines of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is H or alkyl of 1-6 carbon atoms, and the physiologically acceptable acid addition salts thereof have good antihypertensive properties.This is a division of application Ser. No. 939,046 filed Sept. 1, 1978, now abandoned.Type: GrantFiled: September 26, 1979Date of Patent: April 7, 1981Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Hans-Jochen Schliep, Ernst Schorscher
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Patent number: 4258062Abstract: New phenoxy-amino-propanols of formula ##STR1## wherein R.sup.1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.Type: GrantFiled: May 30, 1979Date of Patent: March 24, 1981Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Karl-Heinz Becker, Hans-Joachim Enenkel, Klaus Minck, Hans-Jochen Schliep
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Patent number: 4171370Abstract: New phenoxy-amino-propanols of formula ##STR1## wherein R.sup.1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.Type: GrantFiled: October 4, 1977Date of Patent: October 16, 1979Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Karl-Heinz Becker, Hans-Joachim Enenkel, Klaus Minck, Hans-Jochen Schliep
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Patent number: 3989833Abstract: Adenine derivatives of the formula ##SPC1##Wherein R is phenyl or thienyl, and the physiologically acceptable acid addition salts thereof, possess, with good compatibility, cardio-active properties and are produced by the reaction of a purine derivative of the formula ##SPC2##Wherein X is F, Cl, Br, I, SR.sub.1, SOR.sub.1, SO.sub.2 R.sub.1 or OSi(CH.sub.3).sub.3, R.sub.1 being alkyl of 1-4 carbon atoms, phenyl or benzyl, with an amine of the formula ##SPC3##Wherein R has the values given above, or a salt thereof.Type: GrantFiled: November 4, 1974Date of Patent: November 2, 1976Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Werner Mehrhof, Karl Heinz Becker, Hans-Jochen Schliep
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Patent number: 3985881Abstract: Novel isoquinoline derivatives of the formula ##SPC1##Wherein R.sub.1 is H or, together with R.sub.2, a C--N bond; R.sub.2 is H, R.sub.8 or, together with R.sub.1, a C--N bond; R.sub.3 is H, methyl or ethyl; R.sub.4 and R.sub.5 each are H or collectively a C--C bond; and R.sub.6 and R.sub.7 each are H or methoxy; R.sub.8 being acyl of 1-10 carbon atoms or alkyl of 1-17 carbon atoms optionally mono- or polysubstituted by phenyl, OH, ArCOO--, ArCONH--, piperidino, 3,4-dehydropiperidino, morpholino, carboxy, carbomethoxy and/or carbethoxy, Ar being 3,4,5-trimethoxyphenyl; and the physiologically acceptable acid addition salts and quaternary ammonium salts thereof, have cardiovascular activity and can be prepared by acylating a corresponding primary amine lacking the COAr group with 3,4,5-trimethoxybenzoic acid or a functional derivative thereof.Type: GrantFiled: December 9, 1974Date of Patent: October 12, 1976Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Werner Mehrhof, Rolf Pohlke, Karl Heinz Becker, Hans-Jochen Schliep
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Patent number: 3980797Abstract: Hexahydro-diazepino-indoles of the formula ##SPC1##Wherein R.sup.1 is H, F, Cl, CF.sub.3, alkyl or alkoxy each of 1 to 3 carbon atoms; R.sup.2 is H, alkyl or cycloalkyl or alkenyl each of up to 6 carbon atoms, or alkyl of up to 6 carbon atoms substituted by oxo oxygen and/or amino or alkylated amino of 2 to 6 carbon atoms and/or aryl of 6 to 8 carbon atoms; and Z is 0 or (H,H), and physiologically acceptable acid addition salts thereof, possess CNS depressant activity.Type: GrantFiled: June 13, 1975Date of Patent: September 14, 1976Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rochus Jonas, Helmut Muller-Calgan, Hans-Jochen Schliep