Patents by Inventor Heinz-Werner Kleemann

Heinz-Werner Kleemann 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: 5719169
    Abstract: The invention relates to benzoylguanidines of the formula I: ##STR1## to pharmaceutically acceptable salts of these compounds and to a process for preparing compounds of the formula I, which comprise reacting a compound of the formula II ##STR2## with guanidine. The compounds of the invention are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: February 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5708034
    Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.
    Type: Grant
    Filed: October 31, 1996
    Date of Patent: January 13, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
  • Patent number: 5698581
    Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.
    Type: Grant
    Filed: April 7, 1995
    Date of Patent: December 16, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5679712
    Abstract: Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4), R(5) are as defined in the specification, and pharmaceutically tolerated salts thereof.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5670544
    Abstract: There are described benzoylguanidines of the formula I ##STR1## where R(1) is hydrogen, Hal, --NO.sub.2, --CN, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where m is zero to 2, R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), n is zero to 4, where R(5) also has the meaning of H,R(6) is H or (C.sub.1 -C.sub.4)-alkyl, where R(5) and R(6) together can be 4 or 5 methylene groups,R(2) is --SR(10), --OR(10), --NRH(10), --NR(10)R(11), --CHR(10)R(12), ##STR2## where R(10) and R(11) are identical or different and are--?CHR(16)!.sub.s --(CH.sub.2).sub.p --(CHOH).sub.q --(CH.sub.2).sub.r --(CH.sub.2 OH).sub.t --R(21) or --(CH.sub.2).sub.p --O--(CH.sub.2 --CH.sub.2 O).sub.q --R(21)R(12) and R(13) are hydrogen or alkyl or, together with the carbon atom carrying them, form a cycloalkyl,R(14) is H, (cyclo)alkyl or --C.sub.n H.sub.2n --R(15),R(3) is defined as R(1), or is alkyl, hydrogen or --X--R(22) where X is oxygen, S or NR(16),and their pharmaceutically tolerable salts.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: September 23, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
  • Patent number: 5641792
    Abstract: Benzoylguanidines substituted by heterocyclic N-oxide, process for their preparation, their use as a medicament or diagnostic agent, medicament containing them and intermediate products for their preparationBenzoylguanidines of the formula I ##STR1## with the meanings given in the text for the substituents, are described. These are compounds which have an outstanding activity on the cardiovascular system.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: June 24, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5635525
    Abstract: A compound of the formula ##STR1## in which the symbols have the following meaning: X is a monocyclic radical having 3, 4 or 5 ring atoms,R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.12 and R.sup.13 are, for example, an alkyl radical,q is zero or 1,L is, for example, a methylene group andA is the radical, for example, of a heterocycleare highly active as antagonists of angiotensin II receptors.They can be used as pharmaceuticals or diagnostics.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: June 3, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Holger Heitsch, Adalbert Wagner, Heinz-Werner Kleemann, Hermann Gerhards, Bernward Scholkens
  • Patent number: 5631293
    Abstract: Amino acid-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent and a medicament containing themBenzoylguanidines of the formula I ##STR1## in which the radicals R(1) to R(5) have the meanings given in the description, are described. They are prepared by reacting a compound of the formula II ##STR2## in which R(1) to R(5) and L have the meanings given in the description, with guanidine. The compound I is suitable for the preparation of cardiovascular medicaments.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: May 20, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5612365
    Abstract: Angiotensin II receptor antagonists for the treatment and prophylaxis of coronary heart disease.Antagonists for angiotensin II receptors of the AT.sub.1 subtype can be employed for the prophylaxis and combating of coronary heart disease.Furthermore these compounds, such as, for example, azoles of the formula (I) ##STR1## can also be used for the therapy of cognitive and erectile dysfunction.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: March 18, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Holger Heitsch, Gabriele Wiemer, Adalbert Wagner, Heinz-Werner Kleemann
  • Patent number: 5591754
    Abstract: Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them.The invention relates to benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is R(3)-S(O).sub.n -- or R(4)R(5)N--O.sub.2 S-- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O).sub.n or R(4)R(5)N-- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl,and in which R (4) and R (5) can also together be a C.sub.4 -C.sub.7 -chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics.
    Type: Grant
    Filed: May 5, 1995
    Date of Patent: January 7, 1997
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Heinrich Englert, Wolfgang Scholz, Udo Albus
  • Patent number: 5571842
    Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: November 5, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5567734
    Abstract: Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.r -perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6); X is 1-3; R(1) is H, alkyl or --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; R(2), R(3), R(4) and R(5) are defined as R(1), with the condition, however, that R(1), R(2), R(3), R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2), R(3), R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.
    Type: Grant
    Filed: January 23, 1995
    Date of Patent: October 22, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5559153
    Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).
    Type: Grant
    Filed: August 11, 1994
    Date of Patent: September 24, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
  • Patent number: 5547953
    Abstract: Substituted 1-oxo-1,2-dihydroisoquinolinoylguanidines and 1,1-dioxo-2H-1,2-benzothiazinoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and also a medicament containing them. Acylguanidines I ##STR1## with X equal to carbonyl or sulfonyl; R(1) equal to H, (cyclo)alkyl, phenyl; R(2) equal to H, alkyl, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine. The compounds have no unwanted salidiuretic but very good antiarrhythmic properties. They are able, as a consequence of inhibition of the cellular Na.sup.+ /H.sup.+ exchange mechanism, to be used for the treatment of all acute or chronic ischemia-induced damage.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: August 20, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
  • Patent number: 5516805
    Abstract: 3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themThere are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen.The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: May 14, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jochen Lang, Heinrich Englert, Andreas Weichert, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
  • Patent number: 5482957
    Abstract: Azole derivatives, process for their preparation, and their useAzole derivatives of the formula (I) ##STR1## in which A, L, O, R.sup.1, X, Y, Z and q have the meanings given, process for their preparation, pharmaceutical preparations and the use of the compounds are described. Azole derivatives of the formula I where the symbols have for example the following meanings:R.sup.1 is (C.sub.2 -C.sub.10)-alkyl,Z is nitrogen,X and Y are independently of one another CR.sup.2,L is --CH.sub.2 --,q is zero or 1,A is a biphenyl radical which is substituted for example by R.sup.15,R.sup.2 is halogen or hydrogen,R.sup.15 is SO.sub.2 --NH--CO--OR.sup.6 andR.sup.6 is phenyl,are highly active antagonists of angiotensin II receptors.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: January 9, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Adalbert Wagner, Heinrich Englert, Heinz-Werner Kleemann, Hermann Gerhards, Bernward Scholkens, Reinhard Becker, Wolfgang Linz, Jean-Paul Vevert, John-Claude Caille
  • Patent number: 5475004
    Abstract: Antagonists for angiotensin II receptors of the AT.sub.1 subtype can be employed for the prophylaxis and combating of coronary heart disease.Furthermore these compounds, such as, for example, azoles of the formula (I) ##STR1## can also be used for the therapy of cognitive and erectile dysfunction.
    Type: Grant
    Filed: June 29, 1993
    Date of Patent: December 12, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Holger Heitsch, Gabriele Wiemer, Adalbert Wagner, Heinz-Werner Kleemann
  • Patent number: 5468764
    Abstract: Angiotensin II receptor antagonists for the treatment of disturbances in cardiac rhythm.Antagonists for angiotensin II receptors of the AT, subtype can be employed for combating cardiac arrhythmias, using azole derivatives.
    Type: Grant
    Filed: June 29, 1993
    Date of Patent: November 21, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Holger Heitsch, Wolfgang Linz, Adalbert Wagner, Heinz-Werner Kleemann
  • Patent number: 5444068
    Abstract: Imidazo-fused iso- and heterocycles, process for their preparation, compositions containing them and their useA compound of the formula ##STR1## in which the symbols have the following meaning: X is a monocyclic radical having 3,4 or 5 ring atoms,R.sup.1,R.sup.2,R.sup.3,R.sup.4,R.sup.12 and R.sup.13 are, for example, an alkyl radical,q is zero or 1,L is, for example, a methylene group andA is the radical, for example, of a heterocycleare highly active as antagonists of angiotensin II receptors. They can be used as pharmaceuticals or diagnostics.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: August 22, 1995
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Holger Heitsch, Adalbert Wagner, Heinz-Werner Kleemann, Hermann Gerhards, Bernward Scholkens
  • Patent number: 5235057
    Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are identical or different and are hydrogen or aralkyl, R.sup.3 is alkyl, cycloalkyl or cycloalkylalkyl, R.sup.4 and R.sup.5 are identical or different and are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl or a heterocyclic radical and R.sup.6 and R.sup.7 are identical or different and are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl or arlkyl or R.sup.6 and R.sup.7, together with the carbon atom carrying them, are cycloalkyl. The novel compounds are prepared by a carbonyl olefination according to Wittig. They are intermediates for the preparation of pharmaceuticals, in particular of inhibitors of renin and HIV protease.
    Type: Grant
    Filed: June 28, 1991
    Date of Patent: August 10, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Werner Kleemann, Rainer Henning, Hansjorg Urbach