Patents by Inventor Hein K. A. C. Coolen

Hein K. A. C. Coolen 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).

  • Publication number: 20190218227
    Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
    Type: Application
    Filed: November 13, 2018
    Publication date: July 18, 2019
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme, Adrian Hobson
  • Patent number: 10179791
    Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: January 15, 2019
    Assignees: AbbVie B.V., AbbVie, Inc.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
  • Patent number: 9951084
    Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
    Type: Grant
    Filed: August 5, 2016
    Date of Patent: April 24, 2018
    Assignees: Abb Vie B.V., Abb Vie, Inc.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
  • Patent number: 9670220
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: June 6, 2017
    Assignees: Abbvie B.V., AbbiVie Inc.
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
  • Publication number: 20160340363
    Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved.
    Type: Application
    Filed: August 5, 2016
    Publication date: November 24, 2016
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme, Adrian Hobson
  • Patent number: 9273017
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
    Type: Grant
    Filed: March 30, 2015
    Date of Patent: March 1, 2016
    Assignee: AbbVie Bahamas Limited
    Inventors: Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
  • Publication number: 20150284403
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
    Type: Application
    Filed: June 18, 2015
    Publication date: October 8, 2015
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog, Adrian Hobson
  • Publication number: 20150239857
    Abstract: The present invention relates to (thio)morpholine derivatives of the formula (I), wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —CO—O—, —
    Type: Application
    Filed: March 30, 2015
    Publication date: August 27, 2015
    Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
  • Patent number: 9096612
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
    Type: Grant
    Filed: September 5, 2013
    Date of Patent: August 4, 2015
    Assignees: AbbVie B.V., AbbVie Inc.
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
  • Patent number: 9045441
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) or a pharmaceutically acceptable salt, a solvate or hydrate thereof; with the proviso that the derivative of formula (I) is not 2-(4-ethylphenyl)-4-morpholinoethanol or 4-[4-(2-hydroxyethyl)-2-morpholinyl]benzeneacetonitrile or a pharmaceutically acceptable salt, a solvate or hydrate thereof. The compounds of the disclosure have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of S1P receptor mediated diseases and conditions.
    Type: Grant
    Filed: August 27, 2010
    Date of Patent: June 2, 2015
    Assignee: ABBVIE BAHAMAS LIMITED
    Inventors: Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
  • Patent number: 8796262
    Abstract: This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: August 5, 2014
    Assignees: AbbVie B.V., AbbVie Inc.
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
  • Patent number: 8735388
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor medicated diseases and conditions.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: May 27, 2014
    Assignee: AbbVie B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders
  • Publication number: 20140080861
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to mascarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or prevention muscarinic receptor medicated diseases and conditions.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 20, 2014
    Applicant: ABBVIE B.V.A
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders
  • Publication number: 20140066433
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) The variables R1-R4, z, A, Q, X and Y are as defined in the claims. The following heterocycles are exemplified sub-structures of formula (I): The compounds of formula (I) are modulators of the S1P receptor (Sphingosine-1-phosphate receptor), More specifically, they are agonists of S1P5. The compounds have therapeutic use in treatment of cognitive disorders, age-relate cognitive decline and dementia.
    Type: Application
    Filed: September 5, 2013
    Publication date: March 6, 2014
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog, Adrian Hobson
  • Patent number: 8586606
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: November 19, 2013
    Assignee: AbbVie B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Louise Terwel
  • Publication number: 20130203737
    Abstract: The present invention relates to a fused heterocyclic derivative of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl, each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl optionally substituted with one or more fluoro atoms, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, dimethylamino, and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, and phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, Z is a linking group —W—(Cn-alkylene)-T- wherein W is attached to R1 and sel
    Type: Application
    Filed: July 8, 2011
    Publication date: August 8, 2013
    Applicant: ABBVIE B.V.
    Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Leonardus A.J.M. Sliedregt, Maria J.P. van Dongen, Jacobus A.J. den Hartog
  • Publication number: 20130196998
    Abstract: The present invention relates to spiro-cyclic amine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkenyl, (2-4C)alkynyl, (1-4C)alkyl each optionally substituted with CN or one or more fluoro atoms, (3-6C)cycloalkyl, (4-6C)cycloalkenyl or a (8-10C)bicyclic group, each optionally substituted with halogen or (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, cyano, (1-6C)alkyl optionally substituted with one or more fluoro atoms, (1-6C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino and (3-6C)cycloalkyl optionally substituted with phenyl which may be substituted with (1-4C)alkyl or halogen, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl optionally substituted with one or more fluoro atoms, monocyclic heterocycle optionally independently substituted with halogen, (1-6C)a
    Type: Application
    Filed: July 8, 2011
    Publication date: August 1, 2013
    Applicant: AbbVie B.V.
    Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme
  • Publication number: 20120220552
    Abstract: The present disclosure relates to (thio)morpholine derivatives of the formula (I) wherein R1 is selected from cyano, (2-4C)alkynyl, (1-4C)alkyl, (3-6C)cycloalkyl, (4-6C)cycloalkenyl, (6-8C)bicycloalkyl, (8-10C)bicyclic group, each optionally substituted with (1-4C)alkyl, phenyl, biphenyl, naphthyl, each optionally substituted with one or more substituents independently selected from halogen, (1-4C)alkyl optionally substituted with one or more fluoro atoms, (2-4C)alkynyl, (1-4C)alkoxy optionally substituted with one or more fluoro atoms, amino, di(1-4C)alkylamino, —SO2-(1-4C)alkyl, —CO-(1-4C)alkyl, —CO—O-(1-4C)alkyl, —NH—CO-(1-4C)alkyl and (3-6C)cycloalkyl, phenyl substituted with phenoxy, benzyl, benzyloxy, phenylethyl or monocyclic heterocycle, each optionally substituted with (1-4C)alkyl, monocyclic heterocycle optionally substituted with halogen, (1-4C)alkyl or with phenyl optionally substituted with (1-4C)alkyl, and bicyclic heterocycle optionally substituted with (1-4C)alkyl; A is selected from —
    Type: Application
    Filed: August 27, 2010
    Publication date: August 30, 2012
    Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena
  • Patent number: 8252930
    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: November 5, 2010
    Date of Patent: August 28, 2012
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Martina A. W. Van Der Neut, Cornelis G. Kruse
  • Publication number: 20120095039
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor mediated diseases and conditions.
    Type: Application
    Filed: November 21, 2011
    Publication date: April 19, 2012
    Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel