N.v. Organon

Akzo Nobel N.v.

Pharmacopeia Drug Disclovery, Inc.

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

John Richard Morphy

Koc-Kan Ho

Michael H Ohlmeyer

Jeffrey John Letourneau

Christopher Mark Riviello

Steven G Kultgen

Irina Neagu

Patrick Anthony Jokiel

Susan Elizabeth Napier

Jui-Hsiang Chan

David Gani

Michael John Plater

Brad Sherborne

John J Baldwin

Tao Guo

Edward McDonald

Robert A Horlick

Simon James Anthony Grove

Adolph C Bohnstedt

Celia Kingsbury

Niall Morton Hamilton

Peter Christopher Ray

Friedrich Kroll

David C Rees

Kenneth C Appell

Friedrich Erich Karl Kroll

David Rees

Michael Ohhlmeyer

Zoran Rankovic

Zoran Rankovoc

Koc-Kan Hoc

Steven Laats

Angus Richard Brown

Peter Thomas Albert Littlewood

Michael John Kiczun

Jui Hsiang Chan

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

Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.

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The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; Ris H, when Y is NH; or Ris H, (C)alkyl or halogen, when Y is OH; Rand Rare independently H, (C)alkyl or halogen; Ris H or (C)alkyl, optionally substituted with halogen, (C)cycloalkyl, (C)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C)aryl and heterocyclic ring being optionally substituted with (C)alkyl, (C)alkyloxy or halogen; Ris H or (C)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.

6-substituted isoquinoline derivatives

The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression. 

2-(4-oxo-4H-quinazolin-3-yl)acetamides and their use as vasopressin V3 antagonists

There is provided a polymer having a side chain of general formula (I) in which R may be any suitable alkyl, oxyalkyl, aryl or oxyaryl linking group R is preferably Calkyl (especially &#x2014;CH&#x2014;), a benzene group or a group &#x2014;CH&#x2014;O-Phe-. Generally, the side chain will be attached to an ethylene moiety forming part of the backbone of the polymer. Preferred polymers include polystyrene. The polymer is useful as a support for solid phase chemical reactions especially combinatorial chemical synthesis. 

Vinyl sulphone modified polymer

The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives having the general formula I wherein n is 0, 1, 2 or 3; Rand Rare independently H, (C)alkyl or (C)alkyloxy;

N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives

A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed. The genus is represented by the formula I: A representative example is: 

2-(aminomethyl) arylamide analgesics

Embodiments of the present invention generally relate to carrying out organic chemistry on solid supports comprising derivatised functionalities, methods for synthesizing said supports, methods for synthesizing compounds comprising amine groups or N-containing heterocycles using said solid supports, intermediate compounds linked to said supports and uses thereof.

Solid phase supports

Growing community of inventors

Newhouse, United Kingdom

John Richard Morphy