Abbvie B.v.

Abbvie Inc.

Abbvie Bahamas Limited

Solvay Pharmaceuticals, B.v.

Abbvie Deutschland Gmbh and Co Kg

Abbott Healthcare Products B.v.

Abbivie Inc.

Wouter I Iwema Bakker

Hein K A C Coolen

Adrian Hobson

Axel Stoit

Maria J P Van Dongen

Cornelis G Kruse

Gustaaf J M Van Scharrenburg

Bernard J Van Vliet

Arnold Van Loevezijn

Martina A W Van Der Neut

Nicolas J-l D Leflemme

Pieter Smid

Jacobus A J Den Hartog

Leonardus A J M Sliedregt

Andrew C McCreary

Jennifer Venhorst

Raymond Bronger

Jan Zorgdrager

Eric Ronken

Hiskias G Keizer

Jan H Van Maarseveen

Martin De Haan

Agatha A M Rensink

Jurjen Frankena

Elizabeth Van Der Kam

Harmen Mons

Adrianus Van Den Hoogenband

Adrian D Hobson

Maria Jp Van Dongen

Arnoldus H J Herremans

Martinus Th M Tulp

Mayke B Hesselink

Martina Aw Van Der Neut

Gijsbert D Kuil

Dirk De Boer

Alex Stoit

Martin De Hann

Agatha M Rensink

Nicolas J-Ld Leflemme

Leonardus Ajm Sliedregt

Josephus HM Lange

Van Der Martina AW Neut

Van Arnold Loevezijn

Van Der Elizabeth Kam

Hein KAC Coolen

Agatha AM Rensink

Martina AW Van Der Neut

Nicolas J-LD Leflemme

Maria JP Van Dongen

Leonardus AJM Sliedregt

Jacobus AJ Den Hartog

Hein Kac Coolen

The present invention relates spiro-cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; &#x2014;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. 

Spiro-cyclic amine derivatives as S1P modulators

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.

Fused heterocyclic derivatives as S1P modulators

The present invention relates spiro-cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; &#x2014;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. 

The present invention relates to spiro-cyclic amine derivatives of the formula (I)  The compounds of the invention have affinity to SP receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) SP receptor(s) is (are) involved.

The present invention relates spiro-cyclic amine derivatives of the formula (1) wherein R1; R2; R3; Q; &#x2014;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. 

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.

Described are compounds that are modulators of the S1P receptors, and pharmaceutical compositions comprising the compounds. Also described are methods of using the compounds and compositions for treating, alleviating, or preventing S1P receptor mediated diseases and conditions.

Bisaryl (thio)morpholine derivatives as S1P modulators

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.

(Thio)morpholine derivatives as S1P modulators

Described are compounds that are modulators of the S1P receptors, and pharmaceutical compositions comprising the compounds. Also described are methods of using the compounds and compositions for treating, alleviating, or preventing S1P receptor mediated diseases and conditions. 

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. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

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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. 

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.

The present invention relates to bisaryl (thio)morpholine derivatives of the formula (I)  The compounds of the invention have affinity to S1 Preceptors and may be used in the treatment, alleviation or prevention of S1 Preceptor mediated diseases and conditions.

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. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in parkinson's disease, huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description.

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Hoofddorp, Netherlands

Wouter I Iwema Bakker