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).
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Patent number: 11427598Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (I) 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: GrantFiled: August 31, 2020Date of Patent: August 30, 2022Assignee: ABBVIE DEUTSCHLAND GMBH & CO. KGInventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Maria J. P. van Dongen, Nicolas J.-L. D. Leflemme, Adrian Hobson
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Publication number: 20210130364Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (I) 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: ApplicationFiled: August 31, 2020Publication date: May 6, 2021Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme, Adrian Hobson
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Patent number: 10807991Abstract: The present invention relates spiro-cyclic amine derivatives of the formula (I) 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: GrantFiled: November 13, 2018Date of Patent: October 20, 2020Assignees: 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
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Publication number: 20190218227Abstract: 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: ApplicationFiled: November 13, 2018Publication date: July 18, 2019Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme, Adrian Hobson
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Patent number: 10179791Abstract: 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)aType: GrantFiled: July 8, 2011Date of Patent: January 15, 2019Assignees: 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
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Patent number: 9951084Abstract: 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: GrantFiled: August 5, 2016Date of Patent: April 24, 2018Assignees: 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
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Publication number: 20160340363Abstract: 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: ApplicationFiled: August 5, 2016Publication date: November 24, 2016Inventors: Axel Stoit, Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Maria J.P. van Dongen, Nicolas J.-L.D. Leflemme, Adrian Hobson
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Patent number: 9273017Abstract: 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: GrantFiled: March 30, 2015Date of Patent: March 1, 2016Assignee: AbbVie Bahamas LimitedInventors: Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
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Publication number: 20150239857Abstract: 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: ApplicationFiled: March 30, 2015Publication date: August 27, 2015Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
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Patent number: 9045441Abstract: 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: GrantFiled: August 27, 2010Date of Patent: June 2, 2015Assignee: ABBVIE BAHAMAS LIMITEDInventors: Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena, Adrian Hobson
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Patent number: 8901108Abstract: 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: GrantFiled: September 11, 2013Date of Patent: December 2, 2014Assignee: AbbVie Bahamas LimitedInventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A. M. Rensink, Jennifer Venhorst, Martina A. W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
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Patent number: 8735388Abstract: 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: GrantFiled: October 16, 2013Date of Patent: May 27, 2014Assignee: AbbVie B.V.Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders
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Publication number: 20140080861Abstract: 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: ApplicationFiled: October 16, 2013Publication date: March 20, 2014Applicant: ABBVIE B.V.AInventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders
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Publication number: 20140011775Abstract: 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: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Abbott Healthcare Products B.V.Inventors: Arnold van Loevezijn, Wouter I. Iwema Bakker, Axel Stoit, Agatha A.M. Rensink, Jennifer Venhorst, Martina A.W. Van Der Neut, Martin De Hann, Cornelis G. Kruse
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Patent number: 8586606Abstract: 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: GrantFiled: November 21, 2011Date of Patent: November 19, 2013Assignee: AbbVie B.V.Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Louise Terwel
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Patent number: 8563723Abstract: 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: GrantFiled: March 17, 2009Date of Patent: October 22, 2013Assignee: Abbott Healthcare Products, B.V.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
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Publication number: 20130196998Abstract: 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)aType: ApplicationFiled: July 8, 2011Publication date: August 1, 2013Applicant: 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
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Publication number: 20120220552Abstract: 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: ApplicationFiled: August 27, 2010Publication date: August 30, 2012Inventors: Wouter I. Iwema Bakker, Hein K.A.C. Coolen, Axel Stoit, Harmen Mons, Eric Ronken, Elizabeth Van Der Kam, Jurjen Frankena
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Patent number: 8252930Abstract: 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: GrantFiled: November 5, 2010Date of Patent: August 28, 2012Assignee: Solvay Pharmaceuticals B.V.Inventors: Axel Stoit, Hein K. A. C. Coolen, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Publication number: 20120095039Abstract: 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: ApplicationFiled: November 21, 2011Publication date: April 19, 2012Inventors: Axel Stoit, Hein K.A.C. Coolen, Cornelis G. Kruse, Jan H. Reinders, Louise Terwel