Patents by Inventor Derk Hamminga
Derk Hamminga 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: 5332746Abstract: The invention relates to a group of new 8,9-annelated-.beta.-carbolines and 8,9-annelated-3,4-dihydro-.beta.-carbolines having interesting fibrinolytic properties. In particular the compounds can be used as orally active fibrinolytics.The compounds have the general formulae 1 and 2 ##STR1## wherein R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bound and the intermediate carbon atom constitute a heterocyclic group consisting of 5-10 ring atoms.Type: GrantFiled: May 8, 1991Date of Patent: July 26, 1994Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5328905Abstract: New 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carboline derivatives of the formula ##STR1## wherein R.sub.1 -R.sub.7 are as defined herein; and pharmaceutically acceptable salts and prodrugs thereof. A method of dissolving blood clots using this compound and a pharmaceutical composition having fibrinolytic activity comprising this compound are also part of the present invention.Type: GrantFiled: December 23, 1991Date of Patent: July 12, 1994Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5326768Abstract: The present invention concerns 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivatives of the formula ##STR1## wherein R.sub.0, Z, A, B and C are as defined herein. Such derivatives are useful in the treatment of symptoms which are caused by over-excitation of 5-hydroxytryptamine receptors.Type: GrantFiled: September 28, 1992Date of Patent: July 5, 1994Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Derk Hamminga, Wouter Wouters
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Patent number: 5223625Abstract: The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.Type: GrantFiled: July 16, 1992Date of Patent: June 29, 1993Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
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Patent number: 5198437Abstract: 1,7-Annelated esters and amides of indolecarboxylic acids having formula 2, ##STR1## wherein R.sub.1 is halogen;n has a value of 0-2;Z together with the carbon atom, the nitrogen atom and the intermediate carbon atom, forms a heterocyclic group consisting of 6 ring atoms in which, besides the nitrogen atom already present, a second hetero atom of S is present, which ring may be annelated with a benzene ring;R.sub.3 is hydrogen, halogen, alkyl, alkoxy or alkylthio having 1-4 carbon atoms; andR.sub.2 is a group --CO--Y--R.sub.7 wherein Y is an oxygen atom, or a group --NR.sub.6, wherein R.sub.6 is hydrogen or alkyl having 1-3 C-atoms, and R.sub.7 represents a group of the formula ##STR2## wherein p has the value 1 or 2, q has the value 2 or 3, R.sub.8 is hydrogen or alkyl or hydroxyalkyl having 1 or 2 C-atoms, r is 0 or 1, and R.sub.10 is absent.Type: GrantFiled: December 17, 1990Date of Patent: March 30, 1993Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
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Patent number: 5183822Abstract: The present invention is concerned with compounds of formula 1 ##STR1## wherein R.sub.0 is alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, halogen,Z, together with the carbon atom and the nitrogen atom and the intermediate carbon atom, constitutes a heterocyclic group which consists of 5-8 ring atoms, in which, besides the already present nitrogen atom, a second hetero atom from the group N, O, or S may be present, which ring may be substituted with 1-4 methyl group, or which ring may be annelated with a phenyl group optionally substituted with fluorine, or a methyl or methoxy group;A is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.3, R.sub.4 and R.sub.Type: GrantFiled: December 21, 1990Date of Patent: February 2, 1993Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Derk Hamminga, Wouter Wouters
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Patent number: 5102901Abstract: The invention relates to a group of new 3-N substituted carbamoyl-indole derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.Type: GrantFiled: April 13, 1990Date of Patent: April 7, 1992Assignee: Duphar International Research B.V.Inventors: Ineke van Wijngaarden, Hans H. Haeck, Derk Hamminga, Wouter Wouters
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Patent number: 5100884Abstract: The invention relates to new 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carboline derivatives of the formula ##STR1## wherein the symbols have the following meanings: R.sub.1 is hydrogen, straight or branched alkyl having 1-6 C-atoms, fluorinated or hydroxylated alkyl having 1-6 C-atoms;n has the value of one;R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bonded and the intermediate carbon atom constitute a heterocyclic group consisting of 8 ring atoms;R.sub.4 is hydrogen, straight or branched alkyl having 1-8 C-atoms, alkoxy- or alkylthioalkyl having 2-6 C-atoms, alkenyl or alkynyl having 2-8 C-atoms, which groups may be substituted with one or more fluorine atoms or hydroxy groups, or with one phenyl group containing 0-3 groups R.sub.10, or cycloalkyl group having 3-7 C-atoms, or R.sub.4 is cycloalkyl having 3-8 C-atoms which may be substituted with one or more fluorine atoms, alkyl groups having 1-4 C-atoms, cycloalkyl groups having 3-5 C-atoms, or R.sub.Type: GrantFiled: October 30, 1989Date of Patent: March 31, 1992Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke Van Wigngaarden, Johannes W. C. M. Jansen
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Patent number: 5066649Abstract: The invention relates to a new group of 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carbolines of the formula ##STR1## and the salts and prodrugs thereof. The meanings of R.sub.1, n, Z, R.sub.2, R.sub.3, and R.sub.4 are defined within the body of the specification.It has been found that the compounds have good fibrinolytic properties and can be used in particular as orally active fibrinolytics.Type: GrantFiled: January 16, 1990Date of Patent: November 19, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke van Wijngaarden, Johannes W. C. M. Jansen
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Patent number: 5049563Abstract: Annelated indoleketones with an imidazolylalkyl substituent having the formula (2): ##STR1## wherein R.sub.1 is alkyl or alkoxy having 1-4 C-atoms, hydroxy, halogen, trifluoromethyl, a group R.sub.5 R.sub.6 N or R.sub.5 R.sub.6 -N-CO, wherein R.sub.5 and R.sub.6 are hydrogen or alkyl having 1-4 C-atoms or wherein R.sub.5 R.sub.6 N is a saturated 5-6 ring, and n has the value 0, 1 or 2;A is a group of formula 3, 4 or 5 ##STR2## wherein one of the groups R.sub.2, R.sub.3 and R.sub.4 is hydrogen, alkyl having 1-4 C-atoms, cycloalkyl having 3-6 C-atoms or alkenyl having 2-4 C-atoms and the two other groups, independently of each other, are hydrogen or alkyl having 1-4 C-atoms,p has the value 0-3, and q has the value 2-5. These compounds (and pharmaceutically acceptable acid addition salts thereof) have good antagonistic activity of "neuronal" 5-hydroxytryptamine(5-HT)receptors, and the lower toxicity.Type: GrantFiled: July 3, 1989Date of Patent: September 17, 1991Assignee: Duphar International Research B.V.Inventors: Hans H. Haeck, Derk Hamminga, Ineke van Wijngaarden, Wouter Wouters
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Patent number: 5037844Abstract: The present invention is concerned with compounds of formula 1: ##STR1## wherein R.sub.1 is straight or branched alkyl having 1-4 C-atoms, halogen or cyano;n has the value 0-1;R.sub.2 is hydrogen, (1-6 C)alkyl, (3-6 C)alkenyl, (3-6 C)alkenyl, (3-6 C)cycloalkyl, (3-6 C)cycloalkyl-(1-4 C) alkyl, phenyl, phenyl-(1-3 C)alkyl, COOR.sub.6, COR.sub.6, CONR.sub.6 R.sub.7 or SO.sub.2 --R.sub.6, wherein R.sub.6 and R.sub.7 independently of each other are hydrogen, (1-6 C)alkyl, (3-6 C)cycloalkyl, phenyl or phenyl-(1-4 C)alkyl, wherein the benzene ring is optionally substituted with a methyl group or a halogen atom, with the proviso that R.sub.6 is not hydrogen when R.sub.2 is a group COOR.sub.6 or SO.sub.2 R.sub.6 ;R.sub.3 is hydrogen, straight or branched (1-6 C)alkyl or a phenyl-(1-3 C)alkyl group optionally substituted in the benzene ring; andA is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.8, R.sub.9 and R.sub.Type: GrantFiled: July 20, 1990Date of Patent: August 6, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke van Wijngaarden
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Patent number: 5010076Abstract: Compounds corresponding to the formula I ##STR1## in which R.sup.1 represents hydrogen, lower alkyl or cycloalkylalkyl with 4-7 carbon atoms,R.sup.2 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andR.sup.3 represents hydrogen, halogen, lower alkyl or lower alkoxy, orR.sup.2 and R.sup.3 together denote an alkylenedioxy group,R.sup.4 represents cycloalkyl with 5 to 6 carbon atoms, thiophene or optionally substituted phenyl,R.sup.5 represents hydrogen or halogen,R.sup.6 represents hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl, andZ represents an alkylene chain with 2-4 carbon atoms, which can optionally be mono- or disubstituted by lower alkyl or onto which a 5-6-membered carbocyclic ring can optionally be fused, or represents an --X--CH.sub.2 --CH.sub.2 -- chain,which have pharmacologically valuable properties, are described, together with a method for their preparation.Type: GrantFiled: March 7, 1990Date of Patent: April 23, 1991Assignee: Kali-Chemie Pharma GmbHInventors: Harald Waldeck, Werner Benson, Horst Zeugner, Klaus-Ullrich Wolf, Peter-Colin Gregory, Derk Hamminga, Ineke van Wijngaarden
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Patent number: 4985420Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.Type: GrantFiled: December 7, 1988Date of Patent: January 15, 1991Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Hans H. Haeck, Ineke Van Wijngaarden, Wouter Wouters
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Patent number: 4985424Abstract: The invention relates to a group of new substituted 1,7-annelated 1H-indazole derivatives being strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors.Type: GrantFiled: June 12, 1990Date of Patent: January 15, 1991Assignee: Duphar International Research B.V.Inventors: Ineke van Wijngaarden, Derk Hamminga, Hans H. Haeck, Wouter Wouters
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Patent number: 4950759Abstract: The invention relates to a group of new substituted 1,7-annelated 1H-indazole derivatives being strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors.Type: GrantFiled: July 3, 1989Date of Patent: August 21, 1990Assignee: Duphar International Research B.V.Inventors: Ineke van Wijngaarden, Derk Hamminga, Hans H. Haeck, Wouter Wouters
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Patent number: 4939136Abstract: The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.Type: GrantFiled: June 24, 1988Date of Patent: July 3, 1990Assignee: Duphar International Research B.V.Inventors: Hans H. Haeck, Derk Hamminga, Ineke Van Wijngaarden, Wouter Wouters