IP Library Patent Application 11558616
Patent Application
App. No. 11/558,616

QUINAZOLINE DITOSYLATE SALT COMPOUNDS

Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US None
App. No.
11/558,616
Abstract

Ditosylate salts of 4-quinazolineamines are described as well as methods of using the same in the treatment of disorders characterized by aberrant erbB family PTK activity.

Claims (26)

1 . (canceled)

2 . A process for preparing a compound of formula (C),

comprising the steps of:

reacting a compound of formula (A)

with a compound of formula (B)

to form the compound of formula (C),

wherein U is an organic group;

and the compound of formula (A) is generated in situ; and

L is iodine or bromine;

R is —C(Q)(T)W where Q and T are independently selected from —OCH 3 or —OCH 2 CH 3 and W is hydrogen; and

Z is B(OH) 2 ;

or the compound of formula (A) is generated in situ; and

L is iodine or bromine;

R is —C(O)H; and

Z is B(OH) 2 ;

or the compound of formula (B) is generated in situ, and

L is B(OH) 2 ;

R is —C(O)H; and

Z is bromine.

3 . A process as claimed in claim 2 wherein U represents a phenyl or 1H-indazolyl group substituted by an R 2 group and optionally substituted by at least one independently selected R 4 group; wherein R 2 is selected from a group comprising benzyl, halo-, dihalo- and trihalobenzyl, benzoyl, pyridylmethyl, pyridylmethoxy, phenoxy, benzyloxy, halo-, dihalo- and trihalobenzyloxy and benzenesulphonyl; and each R 4 is selected from the group hydroxy, halo, C 1-4 alkyl, C 2-4 alkenyl, C 2-4 alkynyl, C,-4 alkoxy, amino, C 1-4 alkylamino, di[C 1-4 alkyl]amino, C 1-4 alkylthio, C 1-4 alkylsulphinyl, C 1-4 alkylsulphonyl, C 1-4 alkylcarbonyl, carboxy, carbamoyl, C 1-4 alkoxycarbonyl, C 1-4 alkanoylamino, N-(C 1-4 alkyl)carbamoyl, N,N-di(C 1-4 alkyl)carbamoyl, cyano, nitro and trifluoromethyl.

4 . A process as claimed in claim 3 wherein R 2 represents 3-fluorobenzyloxy.

5 . A process as claimed in claim 3 wherein the phenyl or 1H-indazolyl group of U is substituted by an R 4 group, wherein R 4 represents halo.

6 . A process as claimed in claim 1 wherein U is selected from the group consisting of 3-fluorobenzyloxy-3-chlorophenyl, benzyloxy-3-chlorophenyl, benzyloxy-3-trifluoromethylphenyl, (benzyloxy)-3-fluorophenyl, (3-fluorobenzyloxy)-3-fluorophenyl or (3-fluorobenzyl)indazolyl.

7 . A process as claimed in any claim 1 wherein the compound of formula (A) is generated in situ; L is iodine or bromine; and Z is B(OH) 2 .

8 . A process as claimed in any claim 1 wherein the compound of formula (A) is generated in situ; L is iodine; and Z is B(OH) 2 .

9 . A process as claimed in claim 1 wherein the compound of formula (C) is 5-(4-[3-chloro-4-(3-fluorobenzyloxy)-anilino]-6-quinazolinyl)-furan-2-carbaldehyde.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2015
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 036908/0903 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2015
From: GLAXOSMITHKLINE LLC
To: LEO OSPREY LIMITED
Reel/Frame 036776/0254 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 13, 2015
From: LEO OSPREY LIMITED
To: NOVARTIS AG
Reel/Frame 036776/0261 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 20, 2006
From: SMITHKLINE BEECHAM (CORK) LIMITED
To: SMITHKLINE BEECHAM CORPORATION
Reel/Frame 018654/0335 →