Patents by Inventor Kurt Thiele
Kurt Thiele 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: 4668786Abstract: New derivatives of theophylline having the formula ##STR1## wherein R is hydrogen or a hydroxy group, and n is an integer of 0.ltoreq.n.ltoreq.3 and/or the pharmaceutically acceptable, acid addition salts thereof, exhibit in addition to other properties, histamine-serotinine- bradykynine- antagonistic, anti-anaphylactic and .beta.-adrenergic stimulating effects.Type: GrantFiled: December 26, 1985Date of Patent: May 26, 1987Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Felix Geissmann, Ludwig Zirngibl, Ulrich Jahn
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Patent number: 4603204Abstract: New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.Type: GrantFiled: March 11, 1983Date of Patent: July 29, 1986Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Felix Geissmann, Ludwig Zirngibl, Ulrich Jahn
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Patent number: 4554356Abstract: A process for the manufacture of imidazolylvinyl ethers of the formula ##STR1## wherein Im represents the substituted or unsubstituted 1-H-imidazol-1-yl group and An, R and Y are defined hereinbelow by condensation of a corresponding ketone of the formulaAr--CO--CHR--Im (II)with the splitting-off of a Z group, with a condensable substance of the formulaZ--Y (III)in the aqueous solution of a strong inorganic base, preferably in concentrated aqueous soda lye. The reaction may also be carried out in the presence of a second liquid organic phase, preferably benzene or toluene, especially in the presence of a phase transfer catalyst in this case. Through careful crystallization of the product manufactured according to this method, it is possible to manufacture approximately pure E-isomers of the imidazolylvinyl ether of formula (I), without the requirement of chromatographic separation.Type: GrantFiled: January 16, 1985Date of Patent: November 19, 1985Assignee: Siegfried AktiengesellschaftInventors: Ludwig Zirngibl, Kurt Thiele
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Patent number: 4554281Abstract: Compounds of the formula ##STR1## where R is a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a phenoxy group or a phenyl-C.sub.1 -C.sub.2 -alkoxy group, R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and R.sub.5 is hydrogen or a C.sub.1 -C.sub.4 -alkyl group and the groups R.sub.2, R.sub.3, and R.sub.4 are the same or different and are hydrogen, halogen atoms, C.sub.1 -C.sub.4 alkyl groups, C.sub.1 -C.sub.4 -alkylcarbonyl group, the aminosulfonyl group, the trifluoromethyl group and their acid addition salts are effective as antiepileptics.Type: GrantFiled: October 27, 1983Date of Patent: November 19, 1985Assignee: Degussa AktiengesellschaftInventors: Walter vonBebenburg, deceased, Joachim Heese, Jurgen Engel, Kurt Thiele
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Patent number: 4550175Abstract: For preparing substantially pure (Z)-1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)-0-(2,4-dichlorobenzyl)-ethano ne oxime ether having the formula ##STR1## i.e. the cis-isomer of said oxime ether in a stereospecifically pure form, the pure (Z)-stereoisomer of the corresponding ethanone oxime is first converted into an alkali salt in a polar solvent, such as acetone or dimethylformamide, using an alkali in an amount somewhat less than the equimolar amount with respect to the said ethanone oxime, and is then converted to the desired ether by reacting it at a temperature not higher than 40.degree. C. with a halogen compound capable of forming the desired ether. Isolation of the ether product is obtained as the free base or by precipitating it as an acid addition salt upon addition of a suitable organic or mineral acid, preferably nitric acid.Type: GrantFiled: March 15, 1984Date of Patent: October 29, 1985Assignee: Siegfried AktiengesellschaftInventors: Georg Mixich, Kurt Thiele
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Patent number: 4526898Abstract: 4-(2-Imidazolin-2-yl-amino)-2-methyl-indazole is a highly selective and effective .alpha..sub.2 -antagonist, .alpha..sub.1 -partial agonist and .alpha..sub.1s -agonist and displays anti-hypertensive activity and antagonistic activity on adrenaline and noradrenaline. It is useful as an .alpha.-adrenoceptor influencing and as an anti-hypertensively active drug.Type: GrantFiled: September 7, 1983Date of Patent: July 2, 1985Assignee: Siegfried AktiengesselschaftInventors: Istvan Molnar, Kurt Thiele, Felix Geissmann, Ulrich Jahn
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Patent number: 4483999Abstract: Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.Type: GrantFiled: March 1, 1977Date of Patent: November 20, 1984Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Quazi Ahmed, Rudolf Adrian, Ulrich Jahn
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Patent number: 4443612Abstract: 1-Aryl-2-(1H-imidazol-1-yl)-ethanone oxime ethers are known to exist as a mixture of isomers corresponding to the formulae: ##STR1## To prepare such an isomer in a stereospecifically pure form, the pure stereoisomer of the corresponding ethanone oxime is first converted into an alkali salt in a polar solvent, such as acetone or dimethylformamide, using an alkali in an amount somewhat less than the equimolar amount with respect to the said ethanone oxime, and is then converted to the desired ether by reacting it at a temperature not higher than 40.degree. C. with a halogen compound capable of forming the desired ether. Isolation of the ether product is obtained as the free base or by precipitating it as an acid addition salt upon addition of a suitable organic or mineral acid, preferably nitric acid.Type: GrantFiled: August 30, 1982Date of Patent: April 17, 1984Assignee: Siegfried AktiengesellschaftInventors: Georg Mixich, Kurt Thiele
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Patent number: 4436913Abstract: 1H- and 2H- indazole derivatives and pharmaceuticals containing these blood-pressure lowering 1H- and 2H- indazole derivatives of the formula ##STR1## and their acid addition salts, wherein R1 may be in position 1 or position 2 on the nitrogen atoms in formula I. The groups R1, R2 and R3 represent hydrogen or the usual lower molecular groups. The R group is a 2-imidazolinylamino group or a 3,4,5,6-tetryhydropyrimidinylamino group, wherein these groups may also be present in their tautomeric forms. These groups may also be in an aryl group in the R1 group, in which case the R group may also be a halogen atom. R may only represent one of the heterocyclic secondary or tertiary amino groups in the 4 or 7 position for the 1H- indazole derivatives when the R1 group is simultaneously an aryl or an aralkyl group.Type: GrantFiled: April 28, 1982Date of Patent: March 13, 1984Assignee: Siegfried AktiengesellschaftInventors: Istvan Molnar, Kurt Thiele, Felix Geissmann, Ulrich Jahn
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Patent number: 4330545Abstract: Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated C.sub.1 -C.sub.12 alkyl or a group --Z--Ar in which Ar has the above meaning and --Z-- is a saturated or unsaturated C.sub.1 -C.sub.12 alkylene wherein each of the alkyl and the alkylene may have a carbon chain once or twice interrupted by or, in the case of the alkylene, terminated on its Ar-end by oxy, thio, sulfinyl or sulfonyl bridges, always with the proviso that at least one of Ar and Y is a heterocyclic radical. These compounds are wide-spectrum fungicides and bactericides, and the preferred compounds among them are hydrophilic.Type: GrantFiled: May 19, 1980Date of Patent: May 18, 1982Assignee: Siegfried AktiengesellschaftInventors: Ludwig Zirngibl, Johanna Fischer, Kurt Thiele
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Patent number: 4305942Abstract: Therapeutic xanthine oxidase inhibitor composition containing as an active ingredient 3-dimethylamino-7-methyl-1,2-(n-propylmalonyl)-1,2-dihydro-1,2,4-benzotria zine dihydrate of the formula ##STR1## Uratic diathesis in warm-blooded animals is therapeutically treated by administering the aforementioned xanthine oxidase inhibitor to such animals, e.g., human, either orally or by means of an injection, thereby inhibiting their xanthine oxidase activity.Type: GrantFiled: October 28, 1980Date of Patent: December 15, 1981Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, James S. G. Cox, Johanna Fischer, Ulrich Jahn
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Patent number: 4275068Abstract: Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.Type: GrantFiled: April 23, 1979Date of Patent: June 23, 1981Assignee: Siegfried AGInventors: Kurt Thiele, Quazi Ahmed, Ulrich Jahn, Rudolf Adrian
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Patent number: 4214095Abstract: Novel compounds of the formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are different lower alkyls and R.sup.3 is a lower alkyl or a methyl pyridine group, and the acid addition salts of formula (1) compounds when R.sup.3 is methyl pyridine. The novel compounds have an asymmetric C-atom and may be in the form of the D,L racemates or the D or L stereoisomers.These compounds are useful in the treatment of hypercholesterolemia and hyperlipidemia because of their high effectiveness in reducing the level of cholesterol and lipids in the blood combined with very low general toxicities and substantially reduced hepatomegalitic effects.Type: GrantFiled: January 25, 1979Date of Patent: July 22, 1980Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Quazi Ahmed, Rudolf Adrian, Ulrich Jahn
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Patent number: 4211551Abstract: Herbicidal compositions for selective weed control comprising 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt thereof and the novel salts of 4-(4'-chlorobenzyl)-phenoxy acetic acid.A method for selectively controlling weeds by applying to a crop area an effective amount of 4-(4'-chlorobenzyl)-phenoxy acetic acid or a salt of said acid.Type: GrantFiled: November 10, 1977Date of Patent: July 8, 1980Assignee: Siegfried AGInventors: Kurt Thiele, Quazi Ahmed, Walter Scharen, Jacques Meyer
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Patent number: 4210657Abstract: Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C.sub.1 -C.sub.12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C.sub.1 -C.sub.12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by --O--, --S--, --SO-- or --SO.sub.2 -- bridges. These compounds are effective wide spectrum fungicides and bactericides.Type: GrantFiled: December 18, 1978Date of Patent: July 1, 1980Assignee: Siegfried AktiengesellschaftInventors: Ludwig Zirngibl, Johanna Fischer, Kurt Thiele
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Patent number: 4210656Abstract: .alpha.-Aryl-.beta.-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: ##STR1## Ar represents a substituted or unsubstituted aryl group, R an alkyl, aryl or aralkyl group, X an oxygen atom, a sulfur atom, a sulfinyl or a sulfonyl group and R1 a lower alkyl group or a nitro group. These compounds are effective wide spectrum fungicides and bactericides. To prepare these vinyl ethers, a corresponding 1-arylacylimidazole is o-alkylated in presence of NaH with a corresponding .alpha.-halogen ether, .alpha.-halogen thioether, .alpha.-halogen sulfinyl compound or a corresponding .alpha.-halogen sulfonyl compound.Type: GrantFiled: December 18, 1978Date of Patent: July 1, 1980Assignee: Siegfried AktiengesellschaftInventors: Ludwig Zirngibl, Johanna Fischer, Kurt Thiele
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Patent number: 4204998Abstract: Novel hydrazines are disclosed in which one of the nitrogen atoms forms a ring member of the five membered ring of a [4.3.0] heterobicyclic compound which may be substituted elsewhere in the ring system. Characteristic ring systems described include indole and benztriazole ring systems. The compounds possess anti-depressant properties as well as anti-microbial, in particular fungistatic and bacteriostatic, properties.Type: GrantFiled: May 5, 1978Date of Patent: May 27, 1980Assignee: Siegfried AktiengesellschaftInventors: Franz Schatz, Christian Stammbach, Kurt Thiele, Theodor W. Wagner-Jauregg, Ludwig Zirngibl, Johanna Fischer, Ulrich Jahn
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Patent number: 4182902Abstract: p-(p'-chlorobenzyl) phenoxyacetic acid.Type: GrantFiled: September 13, 1978Date of Patent: January 8, 1980Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Quazi Armed, Rudolf Adrian, Ulrich Jahn
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Patent number: 4177350Abstract: Antimycotically and antibacterially effective imidazole derivatives of the formula (1) ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen and lower alkyl; R.sup.4 is hydrogen, lower alkyl or selected from unsubstituted or substituted cycloalkyl, benzyl and phenyl groups wherein the substituents are selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, phenyl, cyano, nitro and amino, or wherein R.sup.4 is an unsubstituted or halosubstituted pyridyl, R.sup.5 is nitro or lower alkyl in any unsubstituted position of the imidazole ring, Ar is a phenyl group optionally substituted with at least one substituent which is halogen, lower alkyl, lower alkoxy or a C.sub.4 -C.sub.8 cycloalkyl, or wherein Ar is a benzyl group optionally substituted with a substituent of the type set forth for R.sup.Type: GrantFiled: October 12, 1978Date of Patent: December 4, 1979Assignee: Siegfried AktiengesellschaftInventors: Ludwig Zirngibl, Kurt Thiele
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Patent number: 4153803Abstract: Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.Type: GrantFiled: March 1, 1977Date of Patent: May 8, 1979Assignee: Siegfried AktiengesellschaftInventors: Kurt Thiele, Quazi Ahmed, Rudolf Adrian, Ulrich Jahn