IP Library Granted Patent US 9,815,787
Granted Patent B2
US 9,815,787 · App. 15/103,085 · Granted Nov 14, 2017

Sulfonamide derivative or pharmaceutically acceptable acid addition salt thereof

Inventors: Hiroshi Nagase (Tsukuba, JP); Takashi Nagahara (Yokohama, JP)
Assignee: University of Tsukuba
C07D213/81C07C311/21C07C311/29C07C311/44C07D205/04C07D207/04C07D211/16C07D213/34C07D213/61C07D213/64C07D213/82C07D231/14C07D233/90C07D295/192C07D307/68C07D333/38C07D401/12C07D409/12
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Quick Facts
Patent No.
US 9,815,787
App. No.
15/103,085
Granted
Nov 14, 2017
Kind
B2
Abstract

The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Claims (36)

1. A compound represented by the formula (I)

wherein

R 1 is a hydrogen atom, alkyl having 1 to 4 carbon atoms or halogen,

R 2 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, —OH, —NR 2a R 2b (wherein R 2a is a hydrogen atom, alkyl having 1 to 6 carbon atoms or cycloalkyl having 3 to 8 carbon atoms, R 2b is a hydrogen atom, alkyl having 1 to 6 carbon atoms or cycloalkyl having 3 to 8 carbon atoms), or the formula (a) or (b)

(wherein n′ is an integer of 1 to 4)

R 3 is a hydrogen atom or alkyl having 1 to 4 carbon atoms,

R 4 is a hydrogen atom or alkyl having 1 to 4 carbon atoms,

R 5 is aryl or heteroaryl (wherein aryl or heteroaryl is optionally substituted by optionally selected 1 to 4 R 6 ),

R 6 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, —CN, —CF 3 , —CH 2 F, —CHF 2 , —OCF 3 , —OH, —NO 2 or —NR 6a R 6b (wherein R 6a is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CH 2 OMe or —CH 2 CH 2 OEt, R 6b is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CH 2 OMe or —CH 2 CH 2 OEt),

W is the formula (II):

(wherein

R 7 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or halogen,

R 8 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or halogen,

X is —N═ or —CR 9 ═,

Y is —N═ or —CR 9 ═,

R 9 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, —OH, —NR 10 R 11 , —CH 2 OR 10 , —CF 3 , —OCF 3 , —CN, —C(O)OR 10 , —C(O)NR 10 R 11 , the formula (III) or (IV),

(wherein n is an integer of 1 to 4)

X and Y are —CR 9 ═, each R 9 may be the same or different,

R 11 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CF 3 , —CH 2 CH 2 OH or —CH 2 CH 2 OMe,

R 11 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CF 3 , —CH 2 CH 2 OH or —CH 2 CH 2 OMe,

or a pharmaceutically acceptable acid addition salt thereof.

2. The compound according to claim 1 , wherein

R 1 is a hydrogen atom or alkyl having 1 to 4 carbon atoms,

R 2 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or halogen,

R 6 is alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, —CN, —CF 3 , —OH or —NR 6a R 6b (wherein R 6a is alkyl having 1 to 4 carbon atoms, R 6b is alkyl having 1 to 4 carbon atoms),

W is a compound of the formula (II):

(wherein

R 7 is a hydrogen atom, alkoxy having 1 to 4 carbon atoms or halogen,

R 8 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms or halogen,

X is —CR 9 ═ or —N═,

Y is —CR 9 ═ or —N═,

R 9 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, alkoxy having 1 to 4 carbon atoms, halogen, —OH, —NR 10 R 11 , —CH 2 OH, —C(O)OR 10 , —C(O)NR 10 R 11 or the formula (IV):

(wherein n is an integer of 1 to 4),

R 10 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CF 3 , —CH 2 CH 2 OH or —CH 2 CH 2 OMe, and

R 11 is a hydrogen atom, alkyl having 1 to 4 carbon atoms, —CH 2 CF 3 , —CH 2 CH 2 OH or —CH 2 CH 2 OMe,

or a pharmaceutically acceptable acid addition salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 15, 2016
From: NAGASE, HIROSHI; NAGAHARA, TAKASHI
To: UNIVERSITY OF TSUKUBA
Reel/Frame 039759/0125 →
Priority Claims (1)
JP 2013-257523 · Dec 12, 2013 · national
Continuity (1)
Related Publication 20160362376A1 · Dec 15, 2016