IP Library Granted Patent US 9,663,498
Granted Patent B2
US 9,663,498 · App. 15/027,691 · Granted May 30, 2017

Aromatic heterocyclic compounds and their application in pharmaceuticals

Inventors: Yingjun Zhang (Dongguan, CN); Chuanfei Jin (Dongguan, CN); Wenhe Zhong (Dongguan, CN); Ji Zhang (Dongguan, CN); Li Gao (Dongguan, CN); Kangzhi Chen (Dongguan, CN)
Assignee: SUNSHINE LAKE PHARMA CO., LTD.
C07D405/12A61K31/454A61K31/496A61K31/5377A61K45/06C07D209/08C07D209/10C07D209/12C07D209/42C07D231/56C07D403/12
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Quick Facts
Patent No.
US 9,663,498
App. No.
15/027,691
Granted
May 30, 2017
Kind
B2
Abstract

Provided herein are novel aromatic heterocyclic compounds or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and their uses for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and methods for using such compounds or pharmaceutical compositions thereof to treat Alzheimer's disease.

Claims (16)

1. A compound having Formula (I)

or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein:

m is 0, 1, 2 or 3;

n is 1, 2 or 3;

R 1 is F, Cl, Br or CF 3 ; R 2 is C 1-6 haloalkyl; R 4 is C 1-6 alkoxy; R 5 is

 and wherein Q is N or CH and M is —NR 7 , and wherein R 7 is H, C 1-6 alkyl, C 3-6 cycloalkyl or oxetanyl; and each of A, X and Y is CH.

2. The compound according to claim 1 having Formula (II)

or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein:

m is 1, 2 or 3; and

n is 1.

3. The compound according to claim 1 , wherein R 2 is —CHF 2 , —CF 3 , —CH 2 CF 3 , —CF 2 CHF 2 , —CHFCF 3 , —CF 2 CF 3 , —CH 2 CF 2 CF 3 , or —CH 2 CF 2 CHF 2 .

4. The compound according to claim 1 , wherein each R 4 is independently methoxy, ethoxy, n-propoxy, iso-propoxy, n-butoxy, iso-butoxy, or tert-butoxy.

5. The compound according to claim 2 , wherein R 7 is H, methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, tert-butyl, —CH 2 CH 2 CH(CH 3 ) 2 , —CH 2 C(CH 3 ) 3 , cyclopropyl, cyclobutyl, cyclopentyl, or oxetanyl.

6. The compound according to claim 1 having one of the following structures:

or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising the compound according to claim 1 , and a pharmaceutically acceptable carrier, excipient, diluent, adjuvant, vehicle or a combination thereof.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 12, 2020
From: NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
To: SUNSHINE LAKE PHARMA CO., LTD.
Reel/Frame 052921/0778 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 21, 2019
From: SUNSHINE LAKE PHARMA CO., LTD.
To: NORTH & SOUTH BROTHER PHARMACY INVESTMENT COMPANY LIMITED
Reel/Frame 050781/0929 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 7, 2016
From: ZHANG, YINGJUN; JIN, CHUANFEI; ZHONG, WENHE; ZHANG, JI; GAO, LI; CHEN, KANGZHI
To: SUNSHINE LAKE PHARMA CO., LTD.
Reel/Frame 038373/0307 →
Priority Claims (1)
CN 2013 1 0712676 · Dec 20, 2013 · national
Continuity (1)
Related Publication 20160251339A1 · Sep 1, 2016