Patents by Inventor Roelof Van Hes
Roelof Van Hes 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: 7605162Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: October 27, 2008Date of Patent: October 20, 2009Assignee: Solvay PharmaceuticalsInventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Publication number: 20090143406Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: ApplicationFiled: October 27, 2008Publication date: June 4, 2009Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T.M Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Patent number: 7456182Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as anxiety disorders, depression, Parkinson's disease, and schizophrenia. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0-2; R5 and R6 are independently H or alkyl (1-3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3-5, and R7 is alkyl (1-3C), alkoxy (1-3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2-4, and salts thereof.Type: GrantFiled: June 12, 2006Date of Patent: November 25, 2008Assignee: Solvay Pharmaceuticals, Inc.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Patent number: 7371769Abstract: The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula.Type: GrantFiled: December 6, 2005Date of Patent: May 13, 2008Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof van Hes, Pieter Smid, Cornelis G. Kruse, Martinus Th. M. Tulp
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Publication number: 20070066634Abstract: The present invention relates to a group of novel tetrahydropyridin-4-yl indoles with a dual mode of action: serotonin reuptake inhibition and affinity for dopamine-D2 receptors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said tetrahydropyridin-4-yl indoles. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The invention relates to novel tetrahydropyridin-4-yl indoles of the formula.Type: ApplicationFiled: December 6, 2005Publication date: March 22, 2007Applicant: SOLVAY PHARMECEUTICALS B.V.Inventors: Roelof van Hes, Pieter Smid, Cornelis Kruse, Martinus Tulp
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 6391896Abstract: The invention is related to the following compounds: wherein all variables are as defined in the specification. The compounds are useful for treating psychotic disorders.Type: GrantFiled: July 3, 2001Date of Patent: May 21, 2002Assignee: Duphar International Research BVInventors: Roelof Van Hes, Johannes A. M. Van Der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Patent number: 5296497Abstract: The invention relates to 3,4-dehydropiperidine derivatives having psychotropic activity, which compounds are represented by the general formula 1 ##STR1## wherein R is hydrogen or C.sub.1 -C.sub.3 alkyl;R.sub.2 is hydrogen, an unsubstituted or substituted C.sub.1 -C.sub.10 hydrocarbon group, or a group of the general formula ##STR2## wherein A is C.sub.2 -C.sub.10 alkylene,R.sub.5 is hydrogen or C.sub.1 -C.sub.3 alkyl, andR.sub.6 is unsubstituted or substituted aryl or heteroaryl, hydrocarbon, substituted or unsubstituted (hetero)aralkyl, or substituted or unsubstituted heterocyclic; or wherein R.sub.5 and R.sub.6 together with the carbamoyl group to which they are bound constitute a heterocyclic ring system;n has the value 1 or 2; andZ is a heterocyclic group.Type: GrantFiled: October 30, 1992Date of Patent: March 22, 1994Assignee: Duphar International Research B.V.Inventors: Jan Hartog, Roelof Van Hes, Berend Olivier, Ineke Van Wijngaarden
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Patent number: 5162335Abstract: The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.Type: GrantFiled: November 27, 1989Date of Patent: November 10, 1992Assignee: Duphar International Research B.V.Inventors: Maurits E. A. Vandewalle, Johan T. A. Van der Eycken, Ineke van Wijngaarden, Roelof van Hes, Antonius Hulkenberg, Christophorus M. J. F. Keet
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Patent number: 4791132Abstract: The invention relates to a group of new phenyl, pyrrolidin-2-yl substituted 5-ring heterocyclic compounds of the formula ##STR1## wherein A is an unsaturated heterocyclic 5-ring having at least one nitrogen or oxygen atom in the ring, with the proviso that the phenyl substituent is in a meta-position with respect to the 2-pyrrolidinyl substituent.The compounds have interesting pharmacological, notably antipsychotic properties.Type: GrantFiled: September 9, 1987Date of Patent: December 13, 1988Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Cornelis G. Kruse, Roelof Van Hes, Johannes A. M. Van Der Heyden
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Patent number: 4783485Abstract: The invention relates to new benzoylurea compounds having insecticidal and acaricidal activity, of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 halogen atoms;Ar is a para-phenylene group or a para-pyridylene group, which groups may be substituted with 1 or 2 substituents selected from the group consisting of chlorine, methyl and trifluoromethyl;B is an oxygen atom or represents a group having the formula ##STR2## wherein R.sub.Type: GrantFiled: September 26, 1986Date of Patent: November 8, 1988Assignee: Duphar International Research B.V.Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt, Roelof Van Hes
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Patent number: 4656193Abstract: The invention relates to new benzoylurea compounds of the general formula ##STR1## wherein R.sub.1 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of halogen and alkyl and haloalkyl having 1-4 carbon atoms,R.sub.2 is a hydrogen atom or represents 1 or 2 substituents which are selected from the group consisting of chlorine, methyl and trifluoromethyl, andR.sub.3 is a hydrogen atom or represents 1-3 alkyl and/or alkenyl groups each having 1-6 and/or 2-6 carbon atoms respectively,or wherein R.sub.3 together with the cyclohexyl ring to which it is attached forms a bi- or polycyclic hydrocarbyl group having 8-14 carbon atoms and, if desired, substituted with 1-3 alkyl groups each having 1-4 carbon atoms.The compounds have an insecticidal and acaricidal activity. After having been processed to compositions, the compounds may be used for the control of insects and/or mites in a dosage from 1 to 5000 g of active substance per hectare.Type: GrantFiled: September 20, 1985Date of Patent: April 7, 1987Assignee: Duphar International Research B.V.Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt, Roelof van Hes
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Patent number: 4572914Abstract: The invention relates to new pyrazoline derivatives and to insecticidal compositions on the basis of the compounds.The compositions can be used for controlling insects in a dosage from 0.01 to 1 kg of active substance per hectare.Type: GrantFiled: June 27, 1980Date of Patent: February 25, 1986Assignee: Duphar International Research B.V.Inventors: Roelof van Hes, Arnoldus C. Grosscurt
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Patent number: 4439440Abstract: The invention relates to new pyrazoline derivatives having insecticidal activity; the new compounds can be represented by the general formula ##STR1## wherein R is an alkoxycarbonyl group having 2 to 6 carbon atoms,X and Y are equal or different and represent hydrogen atoms or halogen atoms,and n is 2, 3 or 4.After having been processed to compositions, the compounds may be used for the control of insects in a dosage from 0.01 to 1 kg of active substance per hectare.Type: GrantFiled: May 7, 1982Date of Patent: March 27, 1984Assignee: Duphar International Research B.V.Inventors: Roelof van Hes, Arnoldus C. Grosscurt
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Patent number: 4379157Abstract: The invention relates to new sulphonyl compounds of the general formula ##STR1## wherein X is a halogen atom, a phenoxy group, or an alkyl group or alkoxy group having 1-4 carbon atoms and substituted, if desired, with halogen;R.sub.1 is a cyano group, andR.sub.2 is an amino group which, if desired, may be substituted with halogen, with one or two alkenyl groups or alkynyl groups having 2-6 carbon atoms or with one or two alkyl groups having 1-6 carbon atoms, which alkyl groups, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring, which ring may also contain a second hetero atom selected from the group consisting of nitrogen, oxygen and sulphur, or which alkyl groups may be substituted with an alkoxy group, having 1-4 carbon atoms, or with a dialkylamino group having 2-6 carbon atoms the alkyl groups of which, together with the nitrogen atom to which they are bound, may form a saturated heterocyclic ring;or whereinR.sub.1 and R.sub.Type: GrantFiled: January 19, 1981Date of Patent: April 5, 1983Assignee: Duphar International Research B.V.Inventors: Roelof van Hes, Arnoldus C. Grosscurt, Wouter Balk