Patents by Inventor Josef Roch
Josef Roch 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: 4728646Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: January 28, 1987Date of Patent: March 1, 1988Assignee: Dr. Karl Thomae GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4714698Abstract: The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.Type: GrantFiled: June 17, 1985Date of Patent: December 22, 1987Assignee: Dr. Karl Thomae GmbHInventors: Josef Roch, Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Rainer Zimmermann, Johannes Weisenberger
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Patent number: 4690923Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: March 15, 1985Date of Patent: September 1, 1987Assignee: Karl Thomae GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4629733Abstract: The present invention relates to novel indolinones of the general formula ##STR1## wherein R represents an aryl group having from 6 to 10 carbon atoms, unsubstituted or mono- or disubstituted by alkyl groups having from 1 to 5 carbon atoms, hydroxyl groups, alkoxy groups having from 1 to 3 carbon atoms, or halogen atoms, whereby the substituents may be the same or different and whereby the phenyl nucleus of the aryl group may also be substituted by an amino group, a hydroxyl group, or an alkanoylamino group with altogether from 1 to 3 carbon atoms; an aryl group having from 6 to 10 carbon atoms, substituted by 3 or 4 alkyl groups having from 1 to 5 carbon atoms each; a phenyl group substituted by a phenyl, halogenphenyl, or cycloalkyl group with 5 to 7 carbon atoms; an aralkyl group having from 7 to 11 carbon atoms; or a pentamethylphenyl, pyridyl, or quinolyl group; m represents the number 0, 1, or 2; and n represents the number 2, 3, 4, 5, or 6.Type: GrantFiled: July 27, 1984Date of Patent: December 16, 1986Assignee: Dr. Karl Thomae GmbHInventors: Erich Muller, Josef Nickl, Josef Roch, Berthold Narr
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Patent number: 4560685Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino;R.sub.2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; andR.sub.3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.Type: GrantFiled: June 18, 1984Date of Patent: December 24, 1985Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter HaftungInventors: Josef Roch, Josef Nickl, Erich Muller, Berthold Narr, Johannes Weisenberger, Rainer Zimmermann, Walter Haarmann
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Patent number: 4551464Abstract: Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: January 26, 1984Date of Patent: November 5, 1985Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter HaftungInventors: Erich Muller, Josef Nickl, Berthold Narr, Josef Roch, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4518596Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: January 31, 1984Date of Patent: May 21, 1985Assignee: Dr. Karl Thomae GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4518597Abstract: This invention is directed to novel benzoxazin-2-ones of the formula ##STR1## wherein A is a sulfur atom or an SO, SO.sub.2, R--N.dbd.S, or R--N.dbd.SO.sub.2 group where R is a hydrogen atom or an acyl group;D is an alkylene group;R.sub.1 is an alkyl, phenylalkyl, cycloalkyl, or phenyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a hydrogen or halogen atom or a nitro or alkyl group; andR.sub.6 is a hydrogen or halogen atom or an alkyl group,having valuable pharmacological properties, particularly an antithrombotic activity. The compounds of Formula I may be prepared by the methods used for analogous compounds.Type: GrantFiled: June 6, 1984Date of Patent: May 21, 1985Assignee: Dr. Karl Thomae GmbHInventors: Berthold Narr, Josef Nickl, Erich Muller, Josef Roch, Walter Haarmann, Johannes-Maximilian Weisenberger
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Patent number: 4478833Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted alkyl;R.sub.2 is hydrogen or optionally substituted alkyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form an optionally substituted cyclic imino group;R.sub.3 is an optionally substituted cyclic imino group; andR.sub.4 is substituted hydroxyl, mercapto or amino;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: December 16, 1981Date of Patent: October 23, 1984Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter HaftungInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4442111Abstract: Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.Type: GrantFiled: July 6, 1982Date of Patent: April 10, 1984Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter HaftungInventors: Erich Muller, Josef Nickl, Berthold Narr, Josef Roch, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4329347Abstract: Compounds of the formula ##STR1## wherein W is vinylene, methyl-vinylene, methylene or ethylene;m is 0, 1 or 2;D is straight or branched alkylene of 2 to 6 carbon atoms, straight or branched hydroxy-alkylene of 3 to 6 carbon atoms, or xylylene;R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.2 is cycloalkyl of 3 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 11 carbon atoms, heteroaryl, heteroarlkyl, 1,2,4-triazolyl, triphenylmethyl, 4,5-bis-(p-chlorophenyl)-oxazol-2-yl, N-methyl-cyclohexylamino-carbonylmethyl,-amino-iminomethyl or, when m is 1 or D is hydroxyalkylene or xylylene, also alkyl of 1 to 6 carbon atoms; andR.sub.3 and R.sub.4 are each hydrogen, halogen, alkyl of 1 to 4 carbon atoms, amino, acetylamino or nitro.The compounds of the invention are useful as cardiotonics and as antithrombotics.Type: GrantFiled: July 24, 1980Date of Patent: May 11, 1982Assignee: Boehringer Ingelheim GmbHInventors: Erich Muller, Josef Nickl, Josef Roch, Berthold Narr, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4260621Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is unsubstituted, mono-substituted or di-substituted piperidino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.Type: GrantFiled: September 13, 1979Date of Patent: April 7, 1981Assignee: Boehringer Ingelheim GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann
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Patent number: 4224322Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is unsubstituted, mono-substituted or di-substituted thiomorpholino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.Type: GrantFiled: September 13, 1979Date of Patent: September 23, 1980Assignee: Boehringer Ingelheim GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann
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Patent number: 4206214Abstract: Pharmaceutical dosage unit compositions containing, as a combination of active ingredients, dipyridamole and sulfinpyrazone, and a method of using the same as antithrombotics.Type: GrantFiled: August 1, 1978Date of Patent: June 3, 1980Assignee: Boehringer Ingelheim GmbHInventors: Laurence A. Harker, Hans W. Schroter, Walter Haarmann, Josef Roch
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Patent number: 4182887Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is mono- or di-substituted amino, where the substituents are selected from the group consisting of alkyl of 1 to 6 carbon atoms, cyclohexyl, allyl and benzyl; unsubstituted, mono-substituted or di-substituted pyrrolidino, piperidino, hexamethyleneimino, morpholino, piperazino, thiomorpholino, 1-oxido-thiomorpholino or 1,1-dioxido-thiomorpholino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl; 1,2,5,6-tetrahydropyridino; 1,2,3,4-tetrahydroisoquinolino; indolino; or 3,6-ethylene-hexamethyleneimino;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.Type: GrantFiled: September 19, 1977Date of Patent: January 8, 1980Assignee: Boehringer Ingelheim GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann
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Patent number: 4062973Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydroxyl, alkoxy of 1 to 6 carbon atoms, aralkoxy of 7 to 10 carbon atoms, amino, (alkyl of 1 to 3 carbon atoms)-amino, piperidino or morpholino, andn is 0, 1 or 2,Diastereoisomers thereof and, when R.sub.2 is hydroxyl, non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds, their diastereoisomers and the salts are useful as antithrombotics, anti-hypercholesteremics and anti-hyperglyceridemics.Type: GrantFiled: October 6, 1976Date of Patent: December 13, 1977Assignee: Boehringer Ingelheim GmbHInventors: Josef Nickl, Berthold Narr, Erich Muller, Josef Roch, Walter Haarmann
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Patent number: 3975384Abstract: Compounds of the formula ##SPC1##WhereinR.sub.1 is alkoxy of 1 to 3 carbon atoms, morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, or ##EQU1## where A is hydrogen, alkanoyl of 1 to 4 carbon atoms, alkenoyl of 2 to 4 carbon atoms, methoxy-(alkanoyl of 1 to 4 carbon atoms), carboxyl-(alkanoyl of 1 to 4 carbon atoms), acetyl-(alkanoyl of 1 to 4 carbon atoms), methoxy-(alkenoyl of 2 to 4 carbon atoms), carboxyl-(alkenoyl of 2 to 4 carbon atoms), acetyl-(alkenoyl of 2 to 4 carbon atoms), aminocarbonyl, mono(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, di-(alkyl of 1 to 4 carbon atoms)-aminocarbonyl, methoxymethylaminocarbonyl, pyridinoyl, salicyloyl, furanoyl, or (alkyl of 1 to 3 carbon atoms)-sulfonyl,R.sub.2 is morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxido-thiomorpholino, piperazino or N'-[acetyl-(alkanoyl of 1 to 3 arbon atoms)]-piperazino,R.sub.3 is hydrogen, chlorine, bromine, nitro, cyano, formyl, acetyl or carbalkoxy of 2 to 4 carbon atoms, andR.sub.Type: GrantFiled: August 14, 1974Date of Patent: August 17, 1976Assignee: Boehringer Ingelheim GmbHInventors: Berthold Narr, Josef Roch, Erich Muller, Walter Haarmann
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Patent number: 3975524Abstract: Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, alkyl of 1 to 3 carbon atoms, alkanoyl of 1 to 3 carbon atoms, or alkoxycarbonyl of 2 to 4 carbon atoms,R.sub.2 is morpholino, thiomorpholino or 1-oxido-thiomorpholino, andR.sub.3 is hydrogen, fluorine, chlorine, bromine, methyl, methoxy or nitro,And non-toxic, pharmacologicaly acceptable acid addition salts thereof; the compounds as well as the salts are useful as anticoagulants.Type: GrantFiled: April 11, 1975Date of Patent: August 17, 1976Assignee: Boehringer Ingelheim GmbHInventors: Josef Nickl, Erich Muller, Wolfgang Schroter, Walter Haarmann, Josef Roch
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Patent number: 3939268Abstract: Pharmaceutical compositions containing as an active ingredient a compound of the formula ##SPC1##WhereinR.sub.1 and R.sub.2, which may be identical to or different from each other, are each morpholino, thiomorpholino, 1-oxido-thiomorpholino, 1,1-dioxidothiomorpholino or piperidino, where each of these may optionally have a lower alkyl substituent attached thereto; piperazino; N'-acyl-piperazino; N'-carbamoyl-piperazino; N'-lower alkyl-piperazino; dialkanol-amino; or alkylenediamino; andR.sub.3 is hydrogen or methyl;Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and methods of using the same to inhibit thrombocyte aggregation and adhesiveness.Type: GrantFiled: September 4, 1974Date of Patent: February 17, 1976Assignee: Boehringer Ingelheim GmbHInventors: Josef Nickl, Erich Muller, Berthold Narr, Josef Roch