Patents by Inventor Axel Stoit

Axel Stoit 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: 8101619
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: January 24, 2012
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Roelof W. Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria L. Pras-Raves, Andrew C. McCreary, Bernard J. Van Vliet, Mayke B. Hesselink, Cornelis G. Kruse, Gustaaf J. M. Van Scharrenburg
  • Patent number: 8084473
    Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof.
    Type: Grant
    Filed: April 23, 2008
    Date of Patent: December 27, 2011
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel, legal representative
  • Patent number: 7964728
    Abstract: Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: June 21, 2011
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20110053962
    Abstract: Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition. The invention also relates to pharmaceutical compositions containing these compounds, to methods for preparing them, methods for preparing novel intermediates useful for their synthesis, methods for preparing compositions, and uses of such compounds and compositions, for example, their use in administering them to patients to achieve a therapeutic effect in disorders in which nicotinic receptors and/or dopamine transporters are involved, or that can be treated via manipulation of those receptors.
    Type: Application
    Filed: November 5, 2010
    Publication date: March 3, 2011
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Martina A.W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20110046171
    Abstract: This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis.
    Type: Application
    Filed: March 17, 2009
    Publication date: February 24, 2011
    Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A.M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Haan, Cornelis G. Kruse
  • Patent number: 7696383
    Abstract: Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: April 13, 2010
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Lechoslaw A. Turski, Axel Stoit, Cornelis G. Kruse, Sander Vader, Martinus Th. M. Tulp
  • Publication number: 20090018160
    Abstract: The present invention relates to heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof wherein the heterocycle comprises two double bonds which may be present at several positions, and which are represented by the dashed lines (---); the heterocycle contains two heteroatoms, W is N or NH; Y is CH, O or NH, wherein if Y is O, X1 is CH and X2 is C-Z-R2 or C—R3, wherein Z is NH, O, or S; and if Y is CH or NH, one of X1 and X2 is CH or N, wherein if X1 is CH or N, X2 is C-Z-R2 or C—R3, and if X2 is CH or N, X1 is C-Z-R2 or C—R3, wherein Z is NH or S; R1 is chosen from structures (a), (b) and (c): R2 is chosen from (C1-C10)alkyl, (C2-C10)alkenyl and (C2-C10)alkynyl, optionally independently substituted with one or more substituents chosen from halogen, hydroxy, cyano, oxo, (C1-C6)alkoxy, (C1-C6)alkylthio, (C1-C6)alkenyloxy, (C1-C6)alkenylthio, (C1-C4)alkoxy(C1-C4)alkoxy, (C5-C7)cycloalkyl, a 5-membered unsaturated heterocycle (optionally s
    Type: Application
    Filed: April 23, 2008
    Publication date: January 15, 2009
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel
  • Publication number: 20090005455
    Abstract: Embodiments of the invention relate to a compound of formula (1), or a tautomer, stereoisomer, hydrate, or solvate thereof, wherein R1 is H or CH3. Other embodiments of the invention relate to a pharmaceutical composition containing these compound, to methods for preparing these compounds, and to methods for preparing compositions containing these compounds. Yet other embodiments of the invention relate to the uses of these compounds and compositions containing it, such as for the manufacture of medicaments and pharmaceutical compositions for treating a condition chosen from depression, major depressive disorder, generalized anxiety disorder, obsessive compulsive disorder, social anxiety disorder, panic disorder, general depressive disorders, diabetic neuropathy, migraine and hot flashes.
    Type: Application
    Filed: June 23, 2008
    Publication date: January 1, 2009
    Inventors: Lechoslaw A. Turski, Axel Stoit, Cornelis G. Kruse, Sander Vader, Martinus Th.M. Tulp
  • Publication number: 20090005395
    Abstract: Embodiments of the present invention relate to a compound of formula (1A) or a pharmacologically acceptable salt, hydrate, or solvate thereof. Other embodiments of the present invention relate to a pharmaceutical composition containing this compound, to methods for preparing this compound, and to methods for preparing compositions containing this compound. Yet other embodiments of the invention relate to uses of this compound, and compositions containing it, for the manufacture of medicaments and pharmaceutical compositions for treating erectile dysfunction or pulmonary arterial hypertension.
    Type: Application
    Filed: June 23, 2008
    Publication date: January 1, 2009
    Inventors: Lechoslaw A. Turski, Axel Stoit, Cornelis G. Kruse, Sander Vader, Martinus Th.M. Tulp
  • Publication number: 20080009514
    Abstract: Azaindole derivatives of formula (I): wherein the symbols have the meanings given in the specification, are described. These compounds have a combination of partial nicotinic acetylcholine receptor agonism and dopamine reuptake inhibition.
    Type: Application
    Filed: July 3, 2007
    Publication date: January 10, 2008
    Inventors: Axel STOIT, Hein K.A.C. Coolen, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20070142397
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification.
    Type: Application
    Filed: December 6, 2005
    Publication date: June 21, 2007
    Applicant: SOLVAY PHARMECEUTICALS B.V.
    Inventors: Roelof Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Van Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Van Scharrenburg
  • Publication number: 20070072870
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
    Type: Application
    Filed: December 6, 2005
    Publication date: March 29, 2007
    Applicant: SOLVAY PHARMECEUTICALS B.V.
    Inventors: Roelof Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Van Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Van Scharrenburg
  • Publication number: 20060247256
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification.
    Type: Application
    Filed: December 6, 2005
    Publication date: November 2, 2006
    Inventors: Roelof Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Van Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Van Scharrenburg
  • Publication number: 20060122247
    Abstract: The invention relates to a group of novel aryloxyethylamine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): Z-T-Ar??(1) wherein: Z is a fragment of the general formula (2): and wherein the other symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
    Type: Application
    Filed: December 6, 2005
    Publication date: June 8, 2006
    Inventors: Roelof Feenstra, Axel Stoit, Jan-willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Scharrenburg
  • Publication number: 20060122189
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
    Type: Application
    Filed: December 6, 2005
    Publication date: June 8, 2006
    Inventors: Roelof Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Van Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Van Scharrenburg
  • Publication number: 20060122190
    Abstract: The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification, and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
    Type: Application
    Filed: December 6, 2005
    Publication date: June 8, 2006
    Inventors: Roelof Feenstra, Axel Stoit, Jan-Willem Terpstra, Maria Pras-Raves, Andrew McCreary, Bernard Van Vliet, Mayke Hesselink, Cornelis Kruse, Gustaaf Van Scharrenburg