Patents by Inventor Wolfgang Eberlein

Wolfgang Eberlein 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: 5807875
    Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-?(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
    Type: Grant
    Filed: December 11, 1996
    Date of Patent: September 15, 1998
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike Andrea Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 5641772
    Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: June 24, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
  • Patent number: 5620974
    Abstract: Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.
    Type: Grant
    Filed: July 22, 1994
    Date of Patent: April 15, 1997
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
  • Patent number: 5616620
    Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 1, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike A. Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
  • Patent number: 5610155
    Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 11, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
  • Patent number: 5571809
    Abstract: Disclosed are novel pyridodiazepines. These compounds, as well certain known 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.
    Type: Grant
    Filed: August 17, 1994
    Date of Patent: November 5, 1996
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
  • Patent number: 5468766
    Abstract: Pharmaceutical compositions are described which contain 1,5,6,7-tetrahydro-4H-indazol-4-ones of the formula ##STR1## some of these substances themselves being new. The pharmaceutical compositions may be used as analgesics, antipyretics and antiphlogistics.
    Type: Grant
    Filed: September 29, 1993
    Date of Patent: November 21, 1995
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Klaus Rudolf, Gunther Engelhardt
  • Patent number: 5366972
    Abstract: Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.
    Type: Grant
    Filed: July 13, 1993
    Date of Patent: November 22, 1994
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
  • Patent number: 5179090
    Abstract: Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.
    Type: Grant
    Filed: October 18, 1991
    Date of Patent: January 12, 1993
    Inventors: Klaus Rudolf, Wolfhard Engel, Wolfgang Eberlein, Gunter Trummlitz, Gerhard Mihm, Henri Doods, Norbert Mayer
  • Patent number: 5175158
    Abstract: New diazepinones of formula I ##STR1## wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human and veterinary medicine.
    Type: Grant
    Filed: October 24, 1988
    Date of Patent: December 29, 1992
    Assignee: Dr. Karl Thomae, GmbH
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Gunter Trummlitz, Gerhard Mihm, Norbert Mayer, Henri Doods
  • Patent number: 5026699
    Abstract: 5,11-Dihydro-6H-pyrido[2,3-b][1,4]-benzo-diazepinones substituted in the 11-position corresponding to general formula I ##STR1## wherein R.sup.1 and R.sup.2 represent hydrogen atoms or alkyl groups having 1 to 3 carbon atoms, A.sup.1 is a straight-chained or branched alkylene group with 1 to 5 carbon atoms, A.sup.2 is a methylene group or, if R.sup.1 is hydrogen and R.sup.2 is methyl, A.sup.2 may also be an ethylene group, and the physiologically acceptable acid addition salts thereof are suitable for treating bradycardia and bradyarrhythmia and spasm in the colon, bladder and bronchi.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: June 25, 1991
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gerhard Mihm, Wolfgang Eberlein, Welfhard Engel, Gunter Trummlitz, Norbert Mayer, Henri Doods, Rudolf Hammer
  • Patent number: 5011836
    Abstract: A method for treating abstructive respiratory passage disorders which comprises the use of 5,11-dihydro-11-[[(1-methyl-4-piperidinyl)-amino]carbonyl]-6H-dibenz[b,e]a zepin-6-one; 5,11-dihydro-11-[(1-methyl-4-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, alone or in combination.
    Type: Grant
    Filed: November 17, 1989
    Date of Patent: April 30, 1991
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Klaus Rudolf, Henri Doods, Norbert Mayer
  • Patent number: 5006522
    Abstract: Novel condensed diazepinone of general formula I are described, ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A.sup.1, A.sup.2 and R.sup.1 to R.sup.10 are as defined in herein useful as vagal pacemakers for treating bradycardia and bradyarrhythmia. The novel diazepinones also have spasmolytic properties on peripheral organs, antiemetic properties and are capable of promoting cerebral blood flow.
    Type: Grant
    Filed: May 30, 1989
    Date of Patent: April 9, 1991
    Assignee: Karl Thomae GmbH
    Inventors: Wolfhard Engel, Wolfgang Eberlein, Gerhard Mihm, Gunther Trummlitz, Norbert Mayer, Adriaan De Jonge
  • Patent number: 5002943
    Abstract: Novel condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, A.sup.1, A.sup.2 and R.sup.1 -R.sup.10 are as defined herein. The condensed diazepinones are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia and they have spasmolytic effects on peripheral organs, particularly the colon, bladder and bronchi.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: March 26, 1991
    Inventors: Gerhard Mihm, Wolfgang Eberlein, Wolfhard Engel, Gunter Trummlitz, Norbert Mayer, Adrian de Jonge, Henri Doods
  • Patent number: 5001122
    Abstract: A method for treating shock in a patient, which comprises administering to the patient a therapeutically effective amount of a diazepinone of the general formula: ##STR1## wherein A represents a 5,11-dihydro-6H-pyrido[2,3-b] [1,4] benzodiazepin-6-one group bound in the 11-position; a 5,10-dihydro-11H-dibenzo [b,e] [1,4] diazepin-11-one group bound in the 5-position; a 5,11-dihydro-10H-pyrido [3-2b] [1-4] benzodiazepin-10-one group bound in the 5-position; a 4,9-dihydro-10H-thieno [3,4-b] [1,5] benzodiazpin-10-one group bound in the 4-position, unsubstituted or substituted at the 1- or 3-position or both in the 1- and 3-position by an alkyl group having from 1 to 4 carbon atoms, or in the 3-positionby chlorine, fluorine or bromine; a 6-11-dihydro-5H-pyrido [2,3-b] [1,5] benzodiazepin-5-one group bound in the 11-position; or a 1-methyl-1,4,9,10-tetrahydropyrrolo-[3,2-b] [1,5] benzodiazepin-10-one group bound in the 4-position, unsubstituted or substituted at the 3-position by methyl or methyl or chlorine;R.sub.
    Type: Grant
    Filed: May 17, 1989
    Date of Patent: March 19, 1991
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Volker Trach, Wolfhard Engel, Gerhard Mihm, Norbert Mayer, Henri Doods, Richard Reichl
  • Patent number: 4971966
    Abstract: New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
    Type: Grant
    Filed: July 31, 1987
    Date of Patent: November 20, 1990
    Assignee: Karl Thomae GmbH
    Inventors: Wolfhard Engel, Wolfgang Eberlein, Gunter Trummlitz, Gerhard Mihm, Norbert Mayer, Adriaan de Jonge
  • Patent number: 4931436
    Abstract: New condensed diazepinones of general formula I are described ##STR1## wherein B represents one of the divalent groups ##STR2## and X.sup.1, X.sup.2, A, R.sup.1 to R.sup.10 and Z are defined as in the specification.
    Type: Grant
    Filed: August 9, 1988
    Date of Patent: June 5, 1990
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfhard Engel, Gunter Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Norbert Mayer, Adriaan De Jonge, Klaus Rudolf
  • Patent number: 4904673
    Abstract: (.+-.)-1-[4-[Ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]-N, N-dimethyl-4-piperidine carboxamide and (+)-1-[4-[ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]N,N-d imethyl-4-piperidinecarboxamide, as well as the physiologically acceptable acid addition salts of these compounds are suitable for the treatment of bradycardia and bradyarrhythmia.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: February 27, 1990
    Assignee: Dr. Karl Thomae, GmbH
    Inventors: Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Norbert Mayer, Adriaan de Jonge
  • Patent number: 4873236
    Abstract: There are described new condensed diazepinones of general formula ##STR1## wherein .circle.B represents one of the divalent groups ##STR2## and D represents the groups ##STR3## and X.sup.1, X.sup.2 represents a .dbd.CH-- group or, if .circle.B assumes the meaning of the divalent group S, U or W, they may also represent an N atom, A.sup.1 and A.sup.2 in general represent lower alkylene groups, Z represents a C--C bond or the groups, --O--, --S--, --CH.sub.2 --, or --(CH.sub.2).sub.2 --; R represents hydrogen or methyl, R.sup.1 and R.sup.2 generally represent alkyl groups which, together with the nitrogen atom between them, may also form a saturated monocylic, heterocyclic group, R.sub.3 represents alkyl, chlorine or hydrogen, R.sub.4 represents hydrogen or methyl, R.sup.5 and R.sup.6 represent hydrogen, halogen or alkyl, R.sub.7 represents hydrogen, chlorine or methyl, R.sup.8 represents hydrogen or lower alkyl, R.sup.9 represents hydrogen, halogen, lower alkyl and R.sup.10 represents hydrogen or methyl and R.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: October 10, 1989
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Wolfhard Engel, Wolfgang Eberlein, Gerhard Mihm, Gunter Trummlitz, Norbert Mayer, Adriaan De Jonge
  • Patent number: 4724236
    Abstract: Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.
    Type: Grant
    Filed: December 19, 1986
    Date of Patent: February 9, 1988
    Assignee: Karl Thomae GmbH
    Inventors: Wolfgang Eberlein, Gunter Trummlitz, Wolfhard Engel, Gerhard Mihm, Rudolf Hammer, Norbert Mayer, Antonio Giachetti, Adriaan de Jonge