N.v. Organon

Other

Merck Sharp + Dohme Corp.

Akzo Nobel N.v.

Merck Sharp + Dohme B.v.

Msd Oss B.v.

Simon James Anthony Grove

Mingqiang Zhang

Robert Gilfillan

Ronald Palin

Julia Adam-Worrall

Mohammad Shahid

Koc-Kan Ho

Dirk Leysen

Duncan R Rae

Steven G Kultgen

John Richard Morphy

Fredericus Antonius Dijcks

Craig Jamieson

Celia Kingsbury

Niall Morton Hamilton

John Kinnaird Ferguson MacLean

Ian Craig Carlyle

Brad Sherborne

Simon N Thorn

Ashvinkumar Dhirubhai Mistry

John Kinnaird Ferguson Maclean

Gerardus Stephanus Franciscus Ruigt

Angus Richard Brown

Joannes Theodorus Maria Linders

Minggiang Zhang

Julia Adam-Worall

Michael Ohhlmeyer

Peter Thomas Albert Littlewood

Michael John Kiczun

Angus John Morrison

Simon Nicholas Thorn

Duncan Robertson Rae

The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain. 

Amino-heteroaryl derivatives as HCN blockers

The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein Rrepresents the group CONRRwhich is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; Rand Rare independently H or (C)alkyl; and Ris cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain. 

2-(1,2-benzisoxazol-3-yl)benzylamine derivatives

The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein Ris (C)alkyl, halo(C)alkyl, (C)alkyloxy, or halo(C)alkyloxy; Ris H, (C)alkyl, halo(C)alkyl, (C)alkyloxy, halo(C)alkyloxy or halogen; Ris H, (C)alkyl or halo(C)alkyl; Ris H, (C)alkyl or halo(C)alkyl; Ris H, (C)alkyl or halo-(C)-alkyl; or Rand R, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C)cycloalkyl group, optionally substituted with halogen; Ris H, (C)alkyl, halo(C)alkyl, (C)alkyloxy, halo(C)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

(Pyrrolidin-2-yl)phenyl derivatives

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R, Rand Rare independently H or (C)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, CF, halogen, nitro, cyano, NRR, NRCOR, and CONRR; Rand Rare independently H or (C)-alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

(Pyrido/thieno)-[f]-oxazepine-5-one derivatives

The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; Ris hydrogen, halogen, CN or (1C-4C)alkyl; Ris hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; Rand Rare independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; Ris hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; Ris hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or Ris optionally halogenated (1C-4C)alkyl; each Rindependently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.

Compounds with medicinal effects due to interaction with the glucocorticoid receptor

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R, Rand Rare independently H or (C)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, CF, halogen, nitro, cyano, NRR, NRCOR, and CONRR; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO; R, R, Rand Rare independently selected from H, (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, halogen, nitro, cyano, NRR, NRCOR, and CONRR, R, Rand Rare independently H or (C)alkyl; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system. 

Benzoxazepine derivatives and their use as AMPA receptor stimulators

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

(Pyrido/thieno)&#x2014;[f]&#x2014;oxazepine-5-one derivatives

The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO; R, R, Rand Rare independently selected from H, (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, halogen, nitro, cyano, NRR, NRCOR, and CONRR, R, Rand Rare independently H or (C)alkyl; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these benzoxazepine derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system 

Benzoxazepines derivatives and their use as AMPA receptor stimulators

The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

Benzylamine derivatives which are useful in treating psychiatric disorders

Growing community of inventors

Newhouse, United Kingdom

Simon James Anthony Grove