Patents by Inventor Istvan Stadler

Istvan Stadler 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: 4740523
    Abstract: The invention relates to novel interfuranylene-prostacyclin derivatives of the general formula (I) ##STR1## wherein R.sup.1 stands for hydrogen or a straight or branched chain C.sub.1-6 alkyl group, an inorganic cation or for the protonated form of a base containing an amino group;R.sup.2 stands for hydrogen, a C.sub.1-4 alkanoyl or benzoyl group, a monosubstituted benzoyl, trialkylsilyl or an alkoxyalkyl group;R.sup.3 stands for a straight or branched chain C.sub.1-6 alkyl group, a phenyl group optionally substituted by halogen or by a C.sub.1-4 alkyl group, a heteroaryl group optionally substituted by halogen or by a C.sub.1-4 alkyl group or a cycloalkyl group;A stands for an ethylene or for a cis- or trans-vinylene or --C.tbd.C-- group;B means a chemical bond, a --CHR.sup.5 --, --CHR.sup.5 --CH.sub.2 -- or a --CH.sub.2 --O-- group: andR.sup.5 means hydrogen or a C.sub.1-4 alkyl group.
    Type: Grant
    Filed: January 17, 1986
    Date of Patent: April 26, 1988
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar Rt
    Inventors: Geza Galambos, Jozsef Ivanics, Gyorgy Dorman, Karoly Kanay, Istvan Tomoskozy, Gabor Kovacs, Istvan Stadler, Peter Kormoczi, Pal Hadhazy, Sandor Virag, Miklos Kiss
  • Patent number: 4735965
    Abstract: The invention relates to new 7-oxo-PGI.sub.2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH.sub.2).sub.2 --, cis or trans --CH.dbd.CH-- or --C.tbd.C--;R.sup.1 is lower alkyl or hydrogen;B represents a chemical bond, --CH.sub.2 -- or --CR.sup.2 R.sup.3 ;R.sup.2 stands for lower alkyl or hydrogen;R.sup.3 represents lower alkyl or hydrogen;X is a chemical bond, --O-- or --CH.sub.2 --;R.sup.4 stands for C.sub.1-6 alkyl, C.sub.4-7 cycloalkyl, C.sub.1-6 fluoroalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, phenyl, substituted phenyl or heteroaryl.The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI.sub.2, they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks.
    Type: Grant
    Filed: May 28, 1986
    Date of Patent: April 5, 1988
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Gabor Kovacs, Geza Galambos, Istvan Tomoskozi, Karoly Kanai, Peter Gyory, Peter Kormoczy, Istvan Stadler, Laszlo Szekeres, Gyula Papp, Eva Udvary, Pal Hadhazy, Jeno Marton, Gyorgy Dorman
  • Patent number: 4623641
    Abstract: A new method is disclosed for the treatment and prevention of gastrointestinal ulcers or erosions which comprises the administration of a pharmaceutically effective amount of a PGI.sub.2 methyl ester-beta cyclodextrin complex to a patient in need of said treatment wherein the amount of the PGI.sub.2 methyl ester constitutes 1 to 15% by weight of the complex.
    Type: Grant
    Filed: September 9, 1985
    Date of Patent: November 18, 1986
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Jozsef Szejtli, Magdolna Szejtli nee Rengei, Gyorgy Cseh, Istvan Stadler
  • Patent number: 4588713
    Abstract: Compounds of the formula ##STR1## are disclosed wherein R.sup.1 stands for hydrogen, C.sub.1-4 straight or branched alkyl or pharmacologically acceptable cation,R.sup.2 stands for hydrogen, C.sub.1-4 alkanoyl, benzoyl, or benzoyl substituted by C.sub.1-4 alkyl or halogen, and R.sup.2 can further represent tetrahydropyranyl, trialkylsilyl or alkoxyalkyl,A stands for ethylene, cis or trans-vinylene or --C.dbd.C--,n may represent 2, 3 or 4. The compounds are highly effective in the inhibition of thrombocyte aggregation while at the same time exert only a very small hypotensive effect.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: May 13, 1986
    Assignee: Chinoin Gyogyszer Vegyeszeti Termekek Gyara Rt.
    Inventors: Peter Gyory, Geza Galambos, Karoly Kanay, Jozsef Ivanics, Gyorgy Dorman, Gabor Kovacs, Istvan Stadler, Sandor Virag, Istvan Tomoskozi, Peter Kormoczky, Marianna Kovacs
  • Patent number: 4451483
    Abstract: 2,3,4-trinor-1,5-inter-m-phenylene-prostacycline derivatives of the formula (I), ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1-4 alkyl group, an alkali metal cation or a primary, secondary, tertiary or quaternary ammonium cation,R.sup.2 and R.sup.3 each represent hydrogen or a C.sub.1-4 alkanoyl, benzoyl, substituted benzoyl, tetrahydropyranyl, ethoxyethyl or tri-(C.sub.1-4 alkyl)-silyl group,R.sup.4 is hydrogen or a C.sub.1-4 alkyl group, andR.sup.5 is a hexyl, heptyl, phenoxymethyl or m-trifluoromethylphenoxymethyl group, orR.sup.5 represents a group of the general formula ##STR2## and in this latter formula Z is an amino group or an optionally halo-substituted C.sub.1-4 alkanoylamino, benzoylamino or tosylamino group, andR.sup.6 is a C.sub.
    Type: Grant
    Filed: April 9, 1982
    Date of Patent: May 29, 1984
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Szekely, Krisztina Kekesi, Mariann Lovasz nee Gaspar, Sandor Botar, Pal Hadhazy, Istvan Rakoczi, Laszlo Muszbek, Judit Skopal, Istvan Stadler, Karoly Horvath, Gabor Kovacs, Peter Kormoczy
  • Patent number: 4438132
    Abstract: The invention relates to a process for the preparation of novel 4-oxo-PGI.sub.2 derivatives of formula I ##STR1## where (a) compounds of formula III ##STR2## are oxidized, then the obtained 5-substituted-4-oxo-PGI.sub.1 derivatives of general formula II ##STR3## are eliminated by the splitting off of the W-H-molecule, or (b) the compounds of formula IV ##STR4## are reacted in a solvent in the presence of a catalyst with compounds of general formula V ##STR5## then the obtained compounds of formula I are transformed if desired by saponification, hydrolysis, salt formation, insertion of a protection group to another compound which belongs to the compounds of formula I, too.The pharmaceutical products of the invention can be used for the treatment of circulatory diseases, they inhibit the aggregation of blood plaques, dilate the bronchi and inhibit the secretion of gastric acid.
    Type: Grant
    Filed: April 13, 1982
    Date of Patent: March 20, 1984
    Assignee: CHINOIN Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Gaza Galambos, Vilmos Simonidesz, Istvan Szekely, Jozsef Ivanics, Krisztina Kekesi, Gabor Kovacs, Istvan Stadler, Peter Kormoczy, Karoly Horvath
  • Patent number: 4425358
    Abstract: The invention relates to new optically active or racemic 13-thia-prostacycline derivatives of the Formula I ##STR1## wherein R.sup.1 is hydrogen, a pharmaceutically acceptable cation or a straight or branched chain alkyl group having 1-5 carbon atoms;R.sup.2 is straight or branched chain alkyl having 4-9 carbon atoms or monosubstituted phenoxymethyl;--A--B-- is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH-- of Z-- or E-- configuration or --C.tbd.C--;one of the symbols X and Y is hydrogen, methyl or ethyl and the other is hydroxy, tetrahydropyranyoxy, 1-ethoxy-ethoxy or trialkylsilyloxy; orX and Y together form a --O--CH.sub.2 --CH.sub.2 --O-- group;Z is a sulfur atom or a --SO-- group.
    Type: Grant
    Filed: April 21, 1982
    Date of Patent: January 10, 1984
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Csaba Szantay, Lajos Novak, Jozsef Aszodi, Vilmos Simonidesz, Geza Galambos, Gabor Kovacs, Sandor Virag, Istvan Stadler, Peter Kormoczy
  • Patent number: 4425349
    Abstract: The invention concerns new sulfur-containing isoquinoline derivatives. More particularly, the invention relates to isoquinoline derivatives of the general formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbamoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.
    Type: Grant
    Filed: May 25, 1982
    Date of Patent: January 10, 1984
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Kalman Takacs, Maria H. Papp, Gabor Kovacs, Ilona K. Ajzert, Antal Simay, Peter Literati Nagy, Marian E. Puskas, Gyula Sebestyen, Istvan Stadler, Zoltan Sumeghy
  • Patent number: 4379164
    Abstract: A compound having vasodilative, bronchodilative, stomach-mucosa-protective and platelet-aggregation-inhibiting activity has the formulaA 4-thia- or 4-sulfinyl-PGI.sub.1 -compound of the formula I ##STR1## wherein Q stands for --S-- or --SO--,A stands for C.sub.1-6 straight or branched chain alkylene,B stands for ethylene, vinylene or ethinylene,R.sup.1 represents hydrogen or C.sub.1-4 alkyl,R.sup.2 represents C.sub.1-8 straight or branched chain alkyl or mono-substituted aryl-oxy-methyl,R.sup.3 stands for hydrogen or acetyl, andZ represents --COOH, --CN, --CH.sub.2 OH or --COOW, wherein W stands for an equivalent of a pharmacologically acceptable cation or C.sub.1-4 alkyl.
    Type: Grant
    Filed: October 23, 1981
    Date of Patent: April 5, 1983
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Istvan Tomoskozi, Peter Gyory, Gabor Kovacs, Sandor Virag, Peter Kormoczy, Istvan Stadler
  • Patent number: 4373104
    Abstract: Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.
    Type: Grant
    Filed: July 1, 1980
    Date of Patent: February 8, 1983
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara
    Inventors: Kalman Takacs, Maria H. Papp, Gabor Kovacs, Ilona K. Ajzert, Antal Simay, Peter L. Nagy, Marian E. Puskas, Gyula Sebestyen, Istvan Stadler, Zoltan Sumeghy
  • Patent number: 4330553
    Abstract: New PGI.sub.2 derivatives and a process for their preparation are disclosed of the formula (I) ##STR1## wherein Q is hydrogen, a pharmacologically acceptable cation, or lower alkyl;A is cis or trans --CH.dbd.CH--, --C.tbd.C--, or --CH.sub.2 --CH.sub.2 --;R.sup.13 is hydrogen or a C.sub.1 to C.sub.4 alkanoyl or is a blockinggroup of the formula R.sup.7 R.sup.8 R.sup.9 Si or ##STR2## wherein R.sup.7, R.sup.8 and R.sup.9 are the same or different and can be straight or branched chain alkyl groups having 1 to 4 carbon atoms and R.sup.10 and R.sup.11 are the same or different and can be hydrogen or methyl, and R.sup.12 represents methyl or ethyl, or is tetrahydropyran-2-yl;R.sup.4 is hydrogen or lower alkyl inthe .alpha. or .beta. steric position;R.sup.1 and R.sup.2 are each hydrogen or lower alkyl;Y is methylene, oxygen or an --NH-- group; andR.sup.3 is lower alkyl or phenyl which can be monosubstituted phenyl.
    Type: Grant
    Filed: November 10, 1980
    Date of Patent: May 18, 1982
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Vilmos Simonidesz, Agnes Papp nee Behr, Gabor Kovacs, Jozsef Ivanics, Julia Der nee Foldvary, Istvan Stadler, Istvan Pallagi
  • Patent number: 4283413
    Abstract: New compounds and a process for making the same, for use in inhibiting aggregation in human blood and inhibiting the growth of tumors, said compounds being of the general formula: ##STR1## wherein R is hydrogen, alkanoyl, substituted alkanoyl, aralkanoyl or aroyl and represents .alpha. or .beta. steric position or .alpha. and .beta. position, with the provision that if R stands for p-phenyl-benzoyl then methoxy in the position 2 may stand only in .alpha. or only in .beta. steric position.
    Type: Grant
    Filed: December 12, 1979
    Date of Patent: August 11, 1981
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RT.
    Inventors: Tibor Szabo, Laszlo Institoris, Gabor Kovacs, Istvan Stadler, Bela Koszegi
  • Patent number: 4257962
    Abstract: Racemic or optically active compounds with antitumor activity of the formula: ##STR1## wherein X is oxygen or sulfur;R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkanoyl, benzoyl or phenyl-substituted benzoyl;R.sup.2 is hydrogen or C.sub.1 to C.sub.4 alkanoyl;R.sup.3 is C.sub.2 to C.sub.40 straight or branched chain alkyl substituted by hydroxy, epoxy, amino, C.sub.1 to C.sub.6 alkylamino, C.sub.1 to C.sub.6 dialkylamino, C.sub.1 to C.sub.6 alkanoyloxy or, C.sub.1 to C.sub.4 alkoxycarbonyl; cyclohexyl, phenyl unsubstituted or substituted by halogen, amino, C.sub.1 to C.sub.4 alkyl-substituted amino, C.sub.1 to C.sub.4 alkoxy, nitro, or hydroxy; C.sub.1 to C.sub.6 alkanoyl; allyl or phenyl-C.sub.1 to C.sub.4 alkyl unsubstituted or substituted by a C.sub.2 to C.sub.6 alkene group; or where X is sulfur R.sup.3 is as defined above or is C.sub.1 to C.sub.40 straight or branched chain alkyl; and.about. represents the exo- or endo-steric position in the ring and indicates an .alpha.- or .beta.
    Type: Grant
    Filed: September 15, 1978
    Date of Patent: March 24, 1981
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Tibor Szabo, Laszlo Institoris, Gabor Kovacs, Gyula Dalmadi, Bela Koszegi, Istvan Stadler
  • Patent number: 4204999
    Abstract: A process for the preparation of optically active or racemic lactone diol derivatives of the formula ##STR1## (for use as intermediates in the Corey prostaglandin synthesis). Optically active or racemic lactone diol derivatives are inclosed, in whichR.sup.3 and R.sup.4 are the same or different and stand for a hydrogen, or a lower alkanoyl optionally substituted with one, two or three halogen atoms, or form together a ##STR2## group, in which R.sup.5 and R.sup.6 are the same or different and stand for a hydrogen, alkyl or aryl, with a process for preparing them.According to the invention the above compound are prepared by reacting optically active or racemic lactone of the formula II with formaldehyde or with a formaldehyde polymerisate, in the presence of the mixture of a strong acid and water or of a lower alkane carboxylic acid optionally substituted with one, two or three halogen atoms, and then optionally subjecting the obtained compound of the general formula I, in which R.sup.3 and/or R.sup.
    Type: Grant
    Filed: October 20, 1978
    Date of Patent: May 27, 1980
    Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Tomoskozi, Gabor Kovacs, Istvan Szekely, Vilmos Simonidesz, Marianna Lovasz nee Gaspar, Borbala Keresztesnee Ordog, Julia Remport nee Radoczi, Istvan Stadler, Zsuzsa Visky nee Gombos, Csaba Szantay
  • Patent number: 4176122
    Abstract: A process for the preparation of bicyclic enon compounds in which a lactone diol is selectively oxidized to obtain a hydroxy-aldehyde with one hydroxyl group and, without isolation, the hydroxy-aldehyde is reacted with a phosphorus compound. The reaction product can be acylated or silylated.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: November 27, 1979
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek
    Inventors: Istvan Szekely, Istvan Tomoskozi, Gabor Kovacs, Vilmos Simonidesz, Marianna Lovasz nee Gaspar, Borbala nee Ordog Keresztes, Julia nee Radoczi Remport, Istvan Stadler, Zsuzsa nee Gombos Visky, Csaba Szantay
  • Patent number: 4126622
    Abstract: A compound of the formula is disclosed. ##STR1## wherein R.sup.3 and R.sup.4 are the same or different and are each hydrogen, lower alkanoyl, lower alkanoyl substituted by 1, 2, or 3 halogen atoms, or R.sup.3 and R.sup.4 together form an ##STR2## group in which R.sup.5 and R.sup.6 are the same or different and are each hydrogen, alkyl or aryl as well as a process for the preparation thereof.
    Type: Grant
    Filed: February 22, 1977
    Date of Patent: November 21, 1978
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RT
    Inventors: Istvan Tomoskozi, Gabor Kovacs, Istvan Szekely, Vilmos Simonidesz, Marianna Lovasz nee Gaspar, Borbala Keresztes nee Ordog, Julia Remport nee Radoczi, Istvan Stadler, Zsuzsa Visky nee Gombos, Csaba Szantay
  • Patent number: RE32519
    Abstract: Isoquinolines are disclosed of the formula (I) ##STR1## wherein R independently represents hydrogen, hydroxyl or alkoxy having 1 to 4 carbon atoms,R.sup.1 is hydrogen, alkyl having 1 to 4 carbon atoms and optionally substituted with phenyl, phenyl optionally substituted with one or more halogen or alkoxy group, cyano or carbomoyl,R.sup.2 is phenyl optionally substituted with one or more halogen, alkoxy or carboxyl, or a group of the general formula A ##STR2## wherein R.sup.3 is hydrogen, a straight or branched chained alkyl having 1 to 4 carbon atoms or phenyl,m and n independently represent 0, 1 or 2, with the proviso that m+n is at least 1,R.sup.4 is hydrogen, phenyl, hydroxyl, acyloxy, carboxyl, alkoxycarbonyl having 1 to 6 carbon atoms, carbamoyl, carbazoyl or dialkylamino containing 1 to 6 carbon atoms in the alkyl moiety, orR.sup.
    Type: Grant
    Filed: August 17, 1983
    Date of Patent: October 13, 1987
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara
    Inventors: Kalman Takacs, Maria H. Papp, Gabor Kovaacs, Ilona K. Ajzert, Antal Simay, Peter L. Nagy, Marian E. Puskas, Gyula Sebestyen, Istvan Stadler, Zoltan Sumeghy