Patents by Inventor Rochus Jonas

Rochus Jonas 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: 6417188
    Abstract: Arylalkanoylpyridazine derivatives of the formula I and their physiologically acceptable salts and solvates, in which R1, R2, Q and B have the meanings indicated in Claim 1, show an inhibition of phosphodiesterase IV and can be employed for the treatment of asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, autoimmune disorders, such as, for example, rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumor growth or tumor metastases, sepsis, memory disorders, atherosclerosis and AIDS.
    Type: Grant
    Filed: December 13, 2000
    Date of Patent: July 9, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Franz-Werner Kluxen
  • Patent number: 6399611
    Abstract: Aralkylpyridazinone derivatives of the formula I and their physiologically acceptable salts in which R1, R2, R3, R4, R5 and Q have the meanings indicated in claim 1, show inhibition of phosphodiesterase IV and can be employed for the treatment of inflammatory processes and of allergies, asthma and autoimmune disorders.
    Type: Grant
    Filed: April 19, 1996
    Date of Patent: June 4, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Norbert Beier
  • Patent number: 6376493
    Abstract: A group of compounds of, the preparation of, and the methods of use of benzoylpyridazine derivatives and the physiologically acceptable salts and solvates thereof, which have valuable pharmacological properties while well tolerated. They selectively inhibit phosphodiesterase IV with an intracellular increase in the CAMP level, and have an inhibitory effect on the formation of tumor necrosis factor.
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: April 23, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Franz-Werner Kluxen
  • Patent number: 6143777
    Abstract: Aminothiophenecarboxamides of the formula I ##STR1## and their physiologically acceptable salts, whereinR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, A and n have the meanings stated in claim 1, exhibit phosphodiesterase V inhibition and can be used for the treatment of diseases of the cardiovascular system and for the therapy of disturbances of potency.
    Type: Grant
    Filed: April 14, 1999
    Date of Patent: November 7, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
  • Patent number: 6130223
    Abstract: The invention relates to thienopyrimidine of the formula (I) as well as to their physiologically acceptable salts, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and n have the meaning cited in claim 1. Said compounds exhibit a phosphodiesterase V inhibition and can be used in the treatment of cardiovascular dieases and for the treatment and/or therapy potency disorder.
    Type: Grant
    Filed: June 11, 1999
    Date of Patent: October 10, 2000
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Pierre Schelling, Maria Christadler, Franz-Werner Kluxen
  • Patent number: 6025354
    Abstract: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.
    Type: Grant
    Filed: January 20, 1998
    Date of Patent: February 15, 2000
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Michael Klockow
  • Patent number: 5869516
    Abstract: 5-Pyrazolinone derivatives of the general formula I: ##STR1## in which the R.sup.1 -R.sup.3 variables are as defined herein and the physiologically acceptable salts thereof; processes for the preparation of these compounds, and in particular their use as selective inhibitors of cGMP-specific phosphodiesterase (cGMP PDE), thus as pharmaceutically active compounds.
    Type: Grant
    Filed: May 16, 1996
    Date of Patent: February 9, 1999
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Michael Arlt, Rochus Jonas, Maria Christadler, Gunter Schneider, Michael Klockow
  • Patent number: 5859008
    Abstract: Arylalkyl diazinone derivatives of the formula I ##STR1## and their physiologically acceptable salts, in whichR.sup.1, R.sup.2, R.sup.3, R.sup.4, B, Q and X have the meanings indicated in claim 1, exhibit phosphodiesterase IV inhibition and can be employed for the treatment of inflammatory processes and also of allergies, asthma and autoimmune disorders.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: January 12, 1999
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Norbert Beier
  • Patent number: 5747489
    Abstract: Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: May 5, 1998
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Rochus Jonas, Michael Wolf, Michael Klockow
  • Patent number: 5705497
    Abstract: 3-Alkoxycarbonyl thiadiazinones of the formula I ##STR1## and physiologically unobjectionable salts thereof, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Q and n have the meanings described herein, exhibit a positively inotropic action and can be employed for the therapy of cardiac insufficiency.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: January 6, 1998
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Inge Lues, Norbert Beier, Klaus-Otto Minck
  • Patent number: 5434149
    Abstract: 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: Grant
    Filed: March 31, 1994
    Date of Patent: July 18, 1995
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Michael Klockow, Hans-Jochen Schliep, Michael Wolf
  • Patent number: 5378702
    Abstract: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the meaning given in claim 1, show antiarrhythmic action and are suitable for the control of cardiovascular disorders.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rochus Jonas, Ingeborg Lues, Klaus-Otto Minck, Michael Klockow
  • Patent number: 5276027
    Abstract: 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: Grant
    Filed: October 22, 1992
    Date of Patent: January 4, 1994
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Michael Klockow, Joachim Leibrock, Hans-Jochen Schliep, Christoph Seyfried, Michael Wolf
  • Patent number: 5206363
    Abstract: The invention relates to a process for the resolution of enantiomers of 5-heteroaryl-1,3,4-thiadiazinones of formula I by the kinetic resolution of racemates, characterized in that racemic I is dissolved in an inert solvent or solvent mixture and acylated with a chiral acid chloride. The resulting mixture of diastereoisomers is reacted with an amine or alcohol, thereby achieving a complete resolution of one of the diastereoisomers and a very slight or partial resolution of the other diastereoisomer into the enantiomers on which they are based, the resolution products are then separated off and the remaining pure diastereoisomer is converted to the corresponding pure enantiomer by reaction with an amine or an alcohol.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: April 27, 1993
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Peter Ersing
  • Patent number: 5137885
    Abstract: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning given in claim 1, show positively inotropic and vasodilating action and are suitable for combating cardiovascular diseases.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: August 11, 1992
    Assignee: Merck Patent Gesellschaft Mit Beschraenkter Haftung
    Inventors: Rochus Jonas, Ingeborg Lues, Norbert Beier, Michael Klockow, Klaus-Otto Minck
  • Patent number: 5104881
    Abstract: 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: Grant
    Filed: March 29, 1984
    Date of Patent: April 14, 1992
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Rochus Jonas, Klaus Minck, Hans J. Enenkel, Hans-Jochen Schliep
  • Patent number: 5026705
    Abstract: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononculear of binuclear heteroaryl radical which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2 R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl andR.sup.6 and R.sup.7 are each H, or together are a C--C bond, and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: June 25, 1991
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
  • Patent number: 4923869
    Abstract: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononuclear of binuclear heteroaryl radial which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl, andR.sup.6 and R.sup.7 are each H, or together are a C--C bond,and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: May 8, 1990
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
  • Patent number: 4916128
    Abstract: 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: Grant
    Filed: June 6, 1988
    Date of Patent: April 10, 1990
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Rochus Jonas, Jaime Piulats, Michael Klockow, Ingeborg Lues, Hans-Jochen Schliep
  • Patent number: 4654344
    Abstract: 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: Grant
    Filed: December 20, 1985
    Date of Patent: March 31, 1987
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rochus Jonas, Michael Kloft, Hanns Wurziger, Juergen Harting, Hans J. Enenkel, Klaus-Otto Minck, Hans-Jochen Schliep