Patents by Inventor Josef Heindl

Josef Heindl 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: 6271403
    Abstract: This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: August 7, 2001
    Assignee: Schering Aktiengesellschaft
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Künzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5986115
    Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: January 28, 1999
    Date of Patent: November 16, 1999
    Assignee: Schering AG
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5866560
    Abstract: This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
    Type: Grant
    Filed: August 20, 1997
    Date of Patent: February 2, 1999
    Assignee: Schering AG
    Inventors: Rolf Bohlmann, Dieter Bittler, Josef Heindl, Nikolaus Heinrich, Helmut Hofmeister, Hermann Kunzer, Gerhard Sauer, Christa Hegele-Hartung, Rosemarie Lichtner, Yukishige Nishino, Karsten Parczyk, Martin Schneider
  • Patent number: 5859054
    Abstract: Pharmacologically active leukotriene-B.sub.4 derivatives of general formula I, ##STR1## are described, in whichR.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sub.4, CONR.sub.5 R.sub.6, orR.sub.2 represents H or an organic acid radical with 1-15 C atoms,R.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,R.sub.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.10 cycloalkyl; C.sub.6 -C.sub.10 aryl radicals optionally substituted by 1-3 halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carboxyl or hydroxy; CH.sub.2 --CO--(C.sub.6 -C.sub.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: January 12, 1999
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5783602
    Abstract: The invention relates to leukotriene-B.sub.4 derivatives of general formula I, ##STR1## in which R.sub.1 represents CH.sub.2 OH, CH.sub.3, CF.sub.3 COOR.sub.4 CONR.sub.5 R.sub.6, andR.sub.3 symbolizes H; C.sub.1 -C.sub.14 alkyl, C.sub.3 -C.sub.10 cycloalkyl optionally substituted singly or multiply; C.sub.6 -C.sub.10 aryl radicals, independently of one another, optionally substituted singly or multiply by halogen, phenyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluoromethyl, chloromethyl, trifluoromethyl, carbonyl, carboxyl or hydroxy; or a 5- to 6-membered aromatic heterocyclic ring with at least 1 heteroatom,X and Y mean a direct bond, whereby the resulting olefin can be E- or Z-configured or X represents a fluorine atom in .alpha.- or .beta.-position, and Y means a hydrogen atom in .beta.-position.
    Type: Grant
    Filed: December 4, 1996
    Date of Patent: July 21, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5624943
    Abstract: The invention relates to new pyridine derivatives of general formula I which have useful properties, e.g., as leukotriene-B.sub.4 -antagonists. Pharmaceutical compositions containing these compounds can be used to treat various diseases.
    Type: Grant
    Filed: April 27, 1995
    Date of Patent: April 29, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5614634
    Abstract: Leukotriene-B.sub.4 analogs of formula I ##STR1## in which R.sup.1 means radical COOR.sup.2 with R.sup.2 meaning a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group or R.sup.1 means radical CH.sub.2 OH,B means an alkylene group with 1-3 C atoms in the chain, a radical ##STR2## or a radical ##STR3## with R.sup.3 meaning a hydrogen atom, a carboxy or methoxycarbonyl group, A means groups ##STR4## --NH--CO--, --CO--NH--, --OCH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --COCH.sub.2 -- or --CHOH--CH.sub.2 --,X means N or CH,D means groups or ##STR5## and . . . . . means a single or double bond, as well as optionally their salts with physiologically harmless bases, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: March 25, 1997
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5559134
    Abstract: The invention relates to leukotriene-B.sub.4 antagonists of formula I ##STR1## in which n represents a whole number from 2 to 5,X represents a direct bond, 1 to 6 methylene units, an ortho-, meta- or para-substituted phenyl ring or a meta- or para-substituted pyridine ring,Y represents a bond to a hydrogen atom and simultaneously to a hydroxy group, a double-bound oxygen atom or --O--CH.sub.2 --CH.sub.2 --O--,R.sub.1 and R.sub.2 represent the radical OH, --O--(C.sub.1 -C.sub.4)--alkyl, O--(C.sub.3 -C.sub.6)--cycloalkyl, --O--(C.sub.6 -C.sub.10)--aryl, --O--(C.sub.7 -C.sub.12)--aralkyl, O--(CH.sub.2)--CO-- (C.sub.6 -C.sub.10)--aryl or the radical NHR.sub.3 with R.sub.3 meaning hydrogen, (C.sub.1 -C.sub.4)--alkyl, (C.sub.3 -C.sub.6)--cycloalkyl or (C.sub.7 -C.sub.12)--aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates.
    Type: Grant
    Filed: March 23, 1995
    Date of Patent: September 24, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Bernd Buchmann, Werner Skuballa, Josef Heindl, Wolfgang Fr ohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5541202
    Abstract: 1. Leukotriene-B.sub.4 antagonists of formula I, ##STR1## are described, in whichX represents C.sub.1 -C.sub.4 -alkoxy or --S(O).sub.p --(C.sub.1 -C.sub.4)-alkyl,p represents 0, 1 or 2Y represents a hydrogen atom or the radical CO--A--COR.sub.2 with A meaning an alkylene group with 1-6 C atoms in the chain or a radical ##STR2## R.sub.1 and R.sub.2 represents the radical OH, --O--(C.sub.1 -C.sub.4)-alkyl, --O--(C.sub.3 -C.sub.6)-cycloalkyl, --O--(C.sub.7 -C.sub.12)-aralkyl or the radical NR.sub.3 R.sub.4 with R.sub.3 and R.sub.4 meaning hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.6 -C.sub.10)-aryl or (C.sub.7 -C.sub.12)-aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their use as pharmaceutical agents.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: July 30, 1996
    Assignee: Schering Aktiengesellscaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5502075
    Abstract: Leukotriene-B.sub.4 derivatives of formula I ##STR1## their salts with physiologically compatible bases and their cyclodextrin clathrates are described.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: March 26, 1996
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Fro/ hlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5440044
    Abstract: The present invention relates to a leukotriene-B.sub.4 analog according to formula I ##STR1## in which R.sup.1 is a COOR.sup.2 group, wherein R.sup.2 is a C.sub.2-4 -alkyl group;B is a C.sub.1-3 -alkylene group, a radical ##STR2## wherein R.sup.3 is a hydrogen atom or a carboxy or methoxycarbonyl group; ##STR3## . . . is a single or double bond; or optionally, their salts with physiologically compatible bases. The present invention also relates to the production of the latter leukotriene-B.sub.4 analogs and their use as pharmacological agents.
    Type: Grant
    Filed: December 3, 1993
    Date of Patent: August 8, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5414016
    Abstract: Leukotriene-B.sub.4 derivatives of formula I ##STR1## are described, in which R.sup.1 means CH.sub.2 OH, CH.sub.3, CF.sub.3, COOR.sup.5, CONR.sup.6 R.sup.7, orR.sup.1 together with R.sup.2 means a carbonyl group,R.sup.4 symbolizes H, C.sub.1 -C.sub.10 alkyl optionally substituted, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.10 aryl radical optionally substituted, or a 5-6-membered aromatic heterocyclic ring,A symbolizes a trans, trans-CH.dbd.CH--CH.dbd.CH, a --CH.sub.2 CH.sub.2 --CH.dbd.CH-- or a tetramethylene group,B symbolizes a C.sub.1 -C.sub.10 alkylene group, which optionally can be substituted by fluorine or the group ##STR2## D can mean a direct bond, oxygen, sulfur, --C.tbd.C--, --CH.dbd.CR.sup.6 or together withB can also mean a direct bond, their salts with physiologically compatible bases and their cyclodextrin clathrates.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: May 9, 1995
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5352701
    Abstract: 1. Leukotriene-B.sub.4 antagonists of formula I ##STR1## are described, in which X is a CH.sub.2 group or an oxygen atom,Y is C.sub.1 -C.sub.4 -alkoxy or --S(O).sub.p --C.sub.1 -C.sub.4 -alkyl,p is 0, 1 or 2Z is a hydrogen atom or the radical A-B-COOH with A being a hydroxymethylene group or a carbonyl group and B being an alkylene group with 1-6 atoms in the chain or a radical ##STR2## with the exception that B cannot mean the radical ##STR3## if X is a CH.sub.2 group, R.sub.1 is the radical OH, --O--(C.sub.1 --C.sub.4) -alkyl, --O--(C.sub.3-C.sub.6) -cycloalkyl, --O--(C.sub.7-C.sub.12) -aralkyl or the radical NHR.sub.4 with R.sub.4 being hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, C.sub.6 -C.sub.10 -aryl or (C.sub.7 -C.sub.12)-aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their use as pharmaceutical agents.
    Type: Grant
    Filed: May 5, 1993
    Date of Patent: October 4, 1994
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Roland Ekerdt, Claudia Giesen
  • Patent number: 5187286
    Type: Grant
    Filed: March 25, 1991
    Date of Patent: February 16, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Bernd Buchmann, Josef Heindl, Wolfgang Frohlich, Roland Ekerdt
  • Patent number: 5183925
    Abstract: The invention relates to leukotriene-B.sub.4 derivatives of formula I, ##STR1## in which n=1-10,R.sub.1 means radical CH.sub.2 OH, radical COOR.sub.4, radical CONHR.sub.5 or radical CONR.sub.6 R.sub.7,A means a cis, trans or trans, trans--CH.dbd.CH--CH.dbd.CH group or tetramethylene group,B means an alkylene group with up to 10 C atoms,D means a direct compound, oxygen, sulfur, a --C.tbd.C group or a --CH.dbd.CR.sub.8 group,B and D together mean a direct bond,R.sub.2 means a hydrogen atom or an acid radical of an organic acid with 1-15 C atoms andR.sub.3 means a hydrogen atom, an optionally substituted alkyl radical with 1-10 C atoms,a cycloalkyl radical with 3-10 C atoms, an optionally substituted aryl radical with 6-10 C atoms or a 5-6 member heterocyclic radical and if R.sub.4 means a hydrogen atom, their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their pharmaceutical use.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: February 2, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Werner Skuballa, Bernd Buchmann, Wolfgang Frohlich, Rolalnd Ederdt
  • Patent number: 5158957
    Abstract: 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single of double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 --CHR.sup.9 --COR.sup.10 or COR.sup.12,whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: October 27, 1992
    Assignee: Schering Aktiengesellschaft
    Inventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel
  • Patent number: 5037832
    Abstract: 2-Substituted ergolines ##STR1## wherein C.sub.2 C.sub.3 and C.sub.9 C.sub.10 represent a single or double bond;X is oxygen or sulfur;R.sup.2 is C.sub.1-10 alkyl, optionally halogen-substituted C.sub.2-10 alkenyl, CH.sub.2 YR.sup.3, CR.sup.12 (OR.sup.4)R.sup.5, CH.sub.2 -CHR.sup.9 -COR.sup.10 or COR.sup.12, whereinY is oxygen or sulfur,R.sup.3 is hydrogen, C.sub.1-4 alkyl, phenyl, C.sub.2-5 acyl or phenyl C.sub.1-4 alkyl,R.sup.4 is hydrogen or C.sub.2-5 acyl,R.sup.5 is C.sub.1-9 alkyl,R.sup.9 is COCH.sub.3 or COO-C.sub.1-4 alkyl,R.sup.10 is C.sub.1-4 alkyl or O-C.sub.1-4 alkyl,R.sup.12 is hydrogen or C.sub.1-9 alkyl; andR.sup.6 is C.sub.2-10 alkyl, C.sub.3-10 alkenyl or C.sub.4-10 cycloalkyl-C.sub.1-3 -alkyl,and acid addition salts, isomers and isomeric mixtures thereof are dopaminergic agonists and useful for treating Parkinson's Disease.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: August 6, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Thomas Brumby, Gerhard Sauer, Josef Heindl, Jonathan Turner, Gerhard Kuhne, Helmut Wachtel
  • Patent number: 4863929
    Abstract: Novel 12- and 13-substituted ergoline derivatives are suitable, e.g., as psychopharmaceuticals and for hypertension therapy.
    Type: Grant
    Filed: September 19, 1986
    Date of Patent: September 5, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Josef Heindl, Gertrud Schroeder, Helmut Wachtel
  • Patent number: 4835175
    Abstract: Indole derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, or benzylR.sub.2 is hydrogen, alkyl of up to 4 carbon atoms, free or esterified hydroxyalkyl of up to 4 carbon atoms, or free, amidated or esterified carboxy or carboxyalkyl,R.sub.3 is hydrogen or alkyl containing 1-6 carbon atoms,R.sub.4 is hydrogen or alkyl containing 1-6 carbon atoms andR.sub.5 is hydrogen, or alkyl, alkenyl, or cycloalkyl, all of which per se contain up to 6 carbon atoms, and all of which are optionally substituted by a free or esterified carboxy group or by an optionally substituted phenyl group; or a polymethylene group of up to 8 carbon atoms linking the first indole residue to a second indole residue of Formula Ia ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as defined above,and the physiologically acceptable salts thereof with acids and, optionally, their alkali metal and alkaline earth metal salts,possess valuable pharmacological properties, such as stimulating .beta.
    Type: Grant
    Filed: October 10, 1986
    Date of Patent: May 30, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Josef Heindl, Olaf Loge
  • Patent number: 4740509
    Abstract: Novel 12- and 13-bromoergoine derivatives are suitable as medicines for treating psychic disorders of the depressive array of symptoms and also as intermediates.
    Type: Grant
    Filed: September 19, 1986
    Date of Patent: April 26, 1988
    Assignee: Schering Aktiengesellschaft
    Inventors: Gerhard Sauer, Josef Heindl, Gertrud Schroeder, Helmut Wachtel