IP Library Granted Patent US 10,029,984
Granted Patent B2
US 10,029,984 · App. 15/542,735 · Granted Jul 24, 2018

Mono- or di-substituted indole derivatives as dengue viral replication inhibitors

Inventors: Bart Rudolf Romanie Kesteleyn (Berlare, BE); Jean-François Bonfanti (Ande, FR); Tim Hugo Maria Jonckers (Heist-op-den-Berg, BE); Pierre Jean-Marie Bernard Raboisson (Rosieres, BE); Dorothée Alice Marie-Eve Bardiot (Heverlee, BE); Arnaud Didier M Marchand (Bierbeek, BE)
Assignees: Janssen Pharmaceuticals, Inc.; Katholieke Universiteit Leuven
C07D209/14A61K31/4045C07B2200/13
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Quick Facts
Patent No.
US 10,029,984
App. No.
15/542,735
Granted
Jul 24, 2018
Kind
B2
Abstract

The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using said compounds and also relates to said compounds for use as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.

Claims (18)

1. A compound of formula (I)

wherein:

R 1 is F, R 2 is F, CH 3 or OCH 3 and R 3 is H,

R 1 is H, R 2 is Cl or F and R 3 is CH 3 ,

R 1 is CH 3 , R 2 is OCH 3 , F or H and R 3 =H,

R 1 is H, R 2 is Cl or F and R 3 is H,

R 1 is CH 3 , R 2 is H and R 3 is F,

R 1 is F, R 2 is H and R 3 is CH 3 ,

R 1 is H, R 2 is OCH 3 and R 3 is H or Cl,

R 1 is H, R 2 is F and R 3 is F,

R 1 is CF 3 or OCF 3 , R 2 is H and R 3 is H,

R 1 is Cl, R 2 is OCH 3 and R 3 is H;

and a stereo-isomeric form, a pharmaceutically acceptable salt, solvate or polymorph thereof.

2. A compound of claim 1 selected from the group consisting of:

and a stereo-isomeric form, a pharmaceutically acceptable salt, solvate or polymorph thereof.

3. A pharmaceutical composition comprising a compound of claim 1 together with one or more pharmaceutically acceptable excipients, diluents or carriers.

4. A method of inhibiting the replication of dengue virus in a biological sample or patient, comprising administering to said sample or patient a dengue virus replication-inhibiting amount of the compound of claim 1 .

5. The method of claim 4 , further comprising administering an additional therapeutic agent.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: KESTELEYN, BART RUDOLF ROMANIE; JONCKERS, TIM HUGO MARIA; RABOISSON, PIERRE JEAN-MARIE BERNARD
To: JANSSEN INFECTIOUS DISEASES BVBA
Reel/Frame 042982/0028 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: BONFANTI, JEAN-FRANCOIS
To: JANSSEN-CILAG
Reel/Frame 042982/0088 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: BARDIOT, DOROTHÉE ALICE MARIE-EVE; MARCHAND, ARNAUD DIDIER M
To: CISTIM LEUVEN VZW
Reel/Frame 042982/0212 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: CISTIM LEUVEN VZW
To: KATHOLIEKE UNIVERSITEIT LEUVEN
Reel/Frame 042982/0480 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: JANSSEN-CILAG
To: JANSSEN PHARMACEUTICALS, INC.
Reel/Frame 042982/0558 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 12, 2017
From: JANSSEN INFECTIOUS DISEASES BVBA
To: JANSSEN PHARMACEUTICALS, INC.
Reel/Frame 042982/0652 →
Priority Claims (1)
EP 15151481 · Jan 16, 2015 · regional
Continuity (1)
Related Publication 20180002282A1 · Jan 4, 2018
Cited By (1)
US 12,702,657