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US 2017/0320838 A1Published application
Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (sstr4) agonists
AssigneeBoehringer Ingelheim International GmbH
InventorsRocco MAZZAFERRO, Marco FERRARA, Riccardo GIOVANNINI, Iain LINGARD, Klaus RUDOLF
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Abstract
The invention relates to morpholine and 1,4-oxazepane amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.
Claims16
A compound of formula (I)
- wherein
- m=0, p=1, q=1 or;
- m=1, p=1, q=1 or;
- m=0, p=2, q=1 or;
- m=0, p=1, q=2.
- A is selected from the group consisting of
- H and C1-6-alkyl;
- R1 and R2 are independently selected from the group consisting of
- H, C1-6-alkyl and C3-6-cycloalkyl, wherein at least one of R1 or R2 is C1-6-alkyl or C3-6-cycloalkyl, or wherein R1 and R2 together form a 2- to 5-membered alkylene-bridge incorporating 0 to 2 heteroatoms independently selected from the group consisting of N, O or S
- wherein the C1-6-alkyl, the C3-6-cycloalkyl or the alkylene-bridge is optionally substituted with halogens;
- W is selected from the group consisting of a
- mono- or bicyclic aryl, mono- or bicyclic heteroaryl, mono- or bicyclic heterocyclyl and mono- or bicyclic cycloalkyl.
- wherein each of these ring systems are optionally substituted with one or more R3 and wherein the heteroaryl comprises up to 4 heteroatoms and one or two 5- or 6-membered ring(s);
- R3 is independently selected from the group consisting of
- C1-6-alkyl, C3-8-cycloalkyl, C1-6-alkyl-O—, benzyl, halogen, HO—, NC—, mono- or bicyclic heteroaryl, and 5- or 6-membered monocyclic heterocyclyl containing one heteroatom selected from the group consisting of N, O or S(O)r, wherein the heteroaryl contains up to 4 heteroatoms and one or two 5- or 6-membered ring(s), and r is 0, 1 or 2,
- wherein the C1-6-alkyl, C3-8-cycloalkyl, C1-6-alkyl-O—, benzyl, heteroaryl and the heterocyclyl are optionally substituted with halogens, HO—, acetyl, C1-6-alkyl-O—, oxo, R4—S(O)2—, with R4 being aryl, C3-6-cycloalkyl and/or C1-6-alkyl;
- Y is selected from the group consisting of a bond and —CH2O—;
- or a salt of any of the above compounds
- with the provisio that
- N-[1-(3-methoxyphenyl)ethyl]morpholine-2-carboxamide and
- N-[1-(naphthalen-1-yl)ethyl]morpholine-2-carboxamide
- are excluded.
19 more elements
(canceled)
Dependencies are inferred from the claim text.