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).

  • Patent number: 7605162
    Abstract: 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: Grant
    Filed: October 27, 2008
    Date of Patent: October 20, 2009
    Assignee: Solvay Pharmaceuticals
    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
  • Publication number: 20090143406
    Abstract: 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: Application
    Filed: October 27, 2008
    Publication date: June 4, 2009
    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
  • Patent number: 7456182
    Abstract: 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: Grant
    Filed: June 12, 2006
    Date of Patent: November 25, 2008
    Assignee: 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
  • Patent number: 7371769
    Abstract: 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: Grant
    Filed: December 6, 2005
    Date of Patent: May 13, 2008
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Roelof van Hes, Pieter Smid, Cornelis G. Kruse, Martinus Th. M. Tulp
  • Publication number: 20070066634
    Abstract: 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: Application
    Filed: December 6, 2005
    Publication date: March 22, 2007
    Applicant: SOLVAY PHARMECEUTICALS B.V.
    Inventors: Roelof van Hes, Pieter Smid, Cornelis Kruse, Martinus Tulp
  • Patent number: 7067513
    Abstract: 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: Grant
    Filed: August 22, 2000
    Date of Patent: June 27, 2006
    Assignee: 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
  • Patent number: 6391896
    Abstract: 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: Grant
    Filed: July 3, 2001
    Date of Patent: May 21, 2002
    Assignee: Duphar International Research BV
    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
  • Patent number: 5296497
    Abstract: 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: Grant
    Filed: October 30, 1992
    Date of Patent: March 22, 1994
    Assignee: Duphar International Research B.V.
    Inventors: Jan Hartog, Roelof Van Hes, Berend Olivier, Ineke Van Wijngaarden
  • Patent number: 5162335
    Abstract: 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: Grant
    Filed: November 27, 1989
    Date of Patent: November 10, 1992
    Assignee: 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
  • Patent number: 4791132
    Abstract: 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: Grant
    Filed: September 9, 1987
    Date of Patent: December 13, 1988
    Assignee: Duphar International Research B.V.
    Inventors: Ineke Van Wijngaarden, Cornelis G. Kruse, Roelof Van Hes, Johannes A. M. Van Der Heyden
  • Patent number: 4783485
    Abstract: 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: Grant
    Filed: September 26, 1986
    Date of Patent: November 8, 1988
    Assignee: Duphar International Research B.V.
    Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt, Roelof Van Hes
  • Patent number: 4656193
    Abstract: 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: Grant
    Filed: September 20, 1985
    Date of Patent: April 7, 1987
    Assignee: Duphar International Research B.V.
    Inventors: Marius S. Brouwer, Arnoldus C. Grosscurt, Roelof van Hes
  • Patent number: 4572914
    Abstract: 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: Grant
    Filed: June 27, 1980
    Date of Patent: February 25, 1986
    Assignee: Duphar International Research B.V.
    Inventors: Roelof van Hes, Arnoldus C. Grosscurt
  • Patent number: 4439440
    Abstract: 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: Grant
    Filed: May 7, 1982
    Date of Patent: March 27, 1984
    Assignee: Duphar International Research B.V.
    Inventors: Roelof van Hes, Arnoldus C. Grosscurt
  • Patent number: 4379157
    Abstract: 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: Grant
    Filed: January 19, 1981
    Date of Patent: April 5, 1983
    Assignee: Duphar International Research B.V.
    Inventors: Roelof van Hes, Arnoldus C. Grosscurt, Wouter Balk