IP Library Granted Patent US 8,809,532
Granted Patent B2
US 8,809,532 · App. 12/968,107 · Granted Aug 19, 2014

Aza-ring fused indole and indoline derivatives

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Quick Facts
Patent No.
US 8,809,532
App. No.
12/968,107
Granted
Aug 19, 2014
Kind
B2
Abstract

The present application relates to indole and indoline derivatives of formula (I) wherein a, R 1 , m, L, and Q are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions of such compounds.

Claims (25)

1. A compound of formula (I):

or a pharmaceutically acceptable salt thereof, wherein

a is a single or double bond;

m is 1;

L is a bond, —CH═CH— or —C≡C—;

Q is substituted or unsubstituted pyridyl;

R 1 is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 haloalkyl, —C(O)—C 1 -C 4 alkyl, —C(O)—C 1 -C 4 haloalkyl, —C(O)O—C 1 -C 4 alkyl, —C(O)O—C 1 -C 4 haloalkyl, or —C(O)NR e —C 1 -C 4 alkyl;

R e is hydrogen or alkyl;

wherein Q, when substituted, is independently substituted with 1, 2, 3, 4, or 5 substituents, wherein the substituent is halogen, cyano, C 1 -C 5 haloalkyl, C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 -C 5 alkynyl, hydroxy, C 1 -C 5 alkoxy, —O—C 1 -C 5 haloalkyl, —S—C 1 -C 5 alkyl, —S—C 1 -C 5 haloalkyl, —SO 2 —C 1 -C 5 alkyl, —SO 2 —C 1 -C 5 haloalkyl, C 1 -C 5 cyanoalkyl, or —NO 2 .

2. The compound of claim 1 , wherein Q is pyridin-3-yl, pyridin-4-yl, or 6-methylpyridin-3-yl.

3. The compound of claim 1 , wherein R 1 is C 1 -C 4 alkyl or C 1 -C 4 haloalkyl.

4. The compound of claim 1 , wherein R 1 is —C(O)—C 1 -C 4 alkyl or —C(O)—C 1 -C 4 haloalkyl.

5. The compound of claim 1 , wherein R 1 is —C(O)O—C 1 -C 4 alkyl, —C(O)O—C 1 -C 4 haloalkyl or —C(O)NR e —C 1 -C 4 alkyl.

6. The compound according to claim 1 or a pharmaceutically acceptable salt thereof, selected from the group consisting of:

2-methyl-6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

2-methyl-6-[(6-methylpyridin-3-yl)ethynyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

2-methyl-6-(pyridin-3-ylethynyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

2-methyl-6-(pyridin-4-ylethynyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

2-acetyl-6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole;

(cis)-2-methyl-6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole;

ethyl 6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxylate; and

N-ethyl-6-[(E)-2-(6-methylpyridin-3-yl)vinyl]-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carboxamide.

7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to claim 1 .

8. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) according to claim 1 or a pharmaceutically acceptable salt thereof, in combination with a pharmaceutically acceptable carrier.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 2, 2013
From: ABBOTT LABORATORIES
To: ABBVIE INC.
Reel/Frame 030137/0198 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2010
From: SHI, LEI
To: ABBOTT LABORATORIES
Reel/Frame 025520/0927 →