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).
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Patent number: 4740523Abstract: 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: GrantFiled: January 17, 1986Date of Patent: April 26, 1988Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyar RtInventors: Geza Galambos, Jozsef Ivanics, Gyorgy Dorman, Karoly Kanay, Istvan Tomoskozy, Gabor Kovacs, Istvan Stadler, Peter Kormoczi, Pal Hadhazy, Sandor Virag, Miklos Kiss
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Patent number: 4735965Abstract: 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: GrantFiled: May 28, 1986Date of Patent: April 5, 1988Assignee: 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
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Patent number: 4623641Abstract: 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: GrantFiled: September 9, 1985Date of Patent: November 18, 1986Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.Inventors: Jozsef Szejtli, Magdolna Szejtli nee Rengei, Gyorgy Cseh, Istvan Stadler
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Patent number: 4588713Abstract: 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: GrantFiled: January 14, 1985Date of Patent: May 13, 1986Assignee: 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
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Patent number: 4451483Abstract: 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: GrantFiled: April 9, 1982Date of Patent: May 29, 1984Assignee: 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
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Patent number: 4438132Abstract: 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: GrantFiled: April 13, 1982Date of Patent: March 20, 1984Assignee: 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
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Patent number: 4425358Abstract: 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: GrantFiled: April 21, 1982Date of Patent: January 10, 1984Assignee: 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
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Patent number: 4425349Abstract: 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: GrantFiled: May 25, 1982Date of Patent: January 10, 1984Assignee: 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
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Patent number: 4379164Abstract: 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: GrantFiled: October 23, 1981Date of Patent: April 5, 1983Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.Inventors: Istvan Tomoskozi, Peter Gyory, Gabor Kovacs, Sandor Virag, Peter Kormoczy, Istvan Stadler
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Patent number: 4373104Abstract: 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: GrantFiled: July 1, 1980Date of Patent: February 8, 1983Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek GyaraInventors: Kalman Takacs, Maria H. Papp, Gabor Kovacs, Ilona K. Ajzert, Antal Simay, Peter L. Nagy, Marian E. Puskas, Gyula Sebestyen, Istvan Stadler, Zoltan Sumeghy
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Patent number: 4330553Abstract: 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: GrantFiled: November 10, 1980Date of Patent: May 18, 1982Assignee: 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
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Patent number: 4283413Abstract: 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: GrantFiled: December 12, 1979Date of Patent: August 11, 1981Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RT.Inventors: Tibor Szabo, Laszlo Institoris, Gabor Kovacs, Istvan Stadler, Bela Koszegi
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Patent number: 4257962Abstract: 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: GrantFiled: September 15, 1978Date of Patent: March 24, 1981Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.Inventors: Tibor Szabo, Laszlo Institoris, Gabor Kovacs, Gyula Dalmadi, Bela Koszegi, Istvan Stadler
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Patent number: 4204999Abstract: 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: GrantFiled: October 20, 1978Date of Patent: May 27, 1980Assignee: 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
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Patent number: 4176122Abstract: 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: GrantFiled: February 22, 1977Date of Patent: November 27, 1979Assignee: Chinoin Gyogyszer es Vegyeszeti TermekekInventors: 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
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Patent number: 4126622Abstract: 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: GrantFiled: February 22, 1977Date of Patent: November 21, 1978Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RTInventors: 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
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Patent number: RE32519Abstract: 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: GrantFiled: August 17, 1983Date of Patent: October 13, 1987Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek GyaraInventors: Kalman Takacs, Maria H. Papp, Gabor Kovaacs, Ilona K. Ajzert, Antal Simay, Peter L. Nagy, Marian E. Puskas, Gyula Sebestyen, Istvan Stadler, Zoltan Sumeghy