IP Library Granted Patent US 7,973,160
Granted Patent B2
US 7,973,160 · App. 12/244,227 · Granted Jul 5, 2011

Nitrogen-containing aromatic derivatives

Assignee: Eisai R&D Management Co., Ltd.
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Quick Facts
Patent No.
US 7,973,160
App. No.
12/244,227
Granted
Jul 5, 2011
Kind
B2
Abstract

Compounds represented by the following general formula: [wherein A g is an optionally substituted 5- to 14-membered heterocyclic group, etc.; X g is —O—, —S—, etc.; Y g is an optionally substituted C 6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and T g1 is a group represented by the following general formula: (wherein E g is a single bond or —N(R g2 )—, R g1 and R g2 each independently represent a hydrogen atom, an optionally substituted C 1-6 alkyl group, etc. and Z g represents a C 1-8 alkyl group, a C 3-8 alicyclic hydrocarbon group, a C 6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.

Claims (17)

1. A compound represented by the following general formula:

wherein R c13 is a hydrogen atom, cyano, a halogen atom, formyl, an optionally substituted C 1-6 alkyl group, a group represented by the formula:

wherein V c21 is —CO— or methylene; V c22 and V c23 are each independently a hydrogen atom, optionally substituted C 1-6 alkyl group, optionally substituted C 2-6 alkenyl group, optionally substituted C 2-6 alkynyl group, optionally substituted C 3-8 alicyclic hydrocarbon group, optionally substituted 5- to 14-membered heterocyclic group, optionally substituted 5- to 14-membered aromatic heterocyclic group or optionally substituted C 6-14 aryl group, or a group represented by the formula: —V c21 —O—V c22 wherein V c21 and V c22 have the same definitions as above;

X y2 is an optionally substituted group selected from the group consisting of the following formulas:

wherein Z 12 is a hydrogen atom, optionally substituted C 1-6 alkyl group, optionally substituted C 2-6 alkenyl group, optionally substituted C 2-6 alkynyl group, optionally substituted C 3-8 alicyclic hydrocarbon group, optionally substituted C 6-14 aryl group, optionally substituted 5- to 14-membered heterocyclic group, optionally substituted 5- to 14-membered aromatic heterocyclic group or a group represented by the formula:

wherein Z 31 , Z 33 and Z 34 are each independently methylene, —CO—, —NH— or —O—, and Z 32 is a single bond, methylene, —CO—, —NH— or —O—, and R 1 and R 2 are each independently a hydrogen atom, optionally substituted C 1-6 alkyl group, optionally substituted C 2-6 alkenyl group, optionally substituted C 2-6 alkynyl group, optionally substituted C 3-8 alicyclic hydrocarbon group, optionally substituted C 2-7 acyl group or optionally substituted C 2-7 alkoxycarbonyl group; and

W 11 is an optionally substituted carbon atom or a nitrogen atom;

R c11 is a group represented by the formula —V c11 —V c12 —V c13 , wherein V c11 is a single bond, oxygen atom, optionally substituted benzene ring, optionally substituted 5- to 14-membered aromatic heterocyclic group or —CO—; V c12 is a single bond, oxygen atom or optionally substituted C 1-6 alkylene group; and V c13 is an optionally substituted C 1-6 alkyl group, an optionally substituted C 2-6 alkenyl group, an optionally substituted C 2-6 alkynyl group, an optionally substituted C 3-8 alicyclic hydrocarbon group, hydroxyl, carboxyl, an optionally substituted C 2-7 alkoxycarbonyl group, an optionally substituted 5- to 14-membered heterocyclic group, an optionally substituted 5- to 14-membered aromatic heterocyclic group, an optionally substituted C 6-14 aryl group, a group represented by the formula —NR c21 R c22 , wherein R c21 and R c22 are each independently a hydrogen atom or optionally substituted C 1-6 alkyl group, or a hydrogen atom; and

R c12 is a hydrogen atom, optionally substituted C 1-6 alkyl group or optionally substituted C 3-8 alicyclic hydrocarbon group;

with the exception of the following compounds (1) and (2):

(1) a compound wherein R 1 and R 2 are hydrogen atoms and Z 12 is a C 6-14 aryl group, a 5- to 14-membered heterocyclic group, a C 1-6 alkyl group substituted with a 5- to 14-membered aromatic heterocyclic group, a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, a C 2-6 alkenyl group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, a C 2-6 alkynyl group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, or a C 3-8 alicyclic hydrocarbon group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group; and

(2) a compound wherein X y2 is a group represented by the formula:

wherein Z 12 is a C 6-14 aryl group, a 5- to 14-membered heterocyclic group, a 5- to 14-membered aromatic heterocyclic group, a C 1-6 alkyl group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, a C 2-6 alkenyl group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, a C 2-6 alkynyl group substituted with a 5- to 10-membered heterocyclic group or a C 5-10 alicyclic hydrocarbon group, or a C 3-8 alicyclic hydrocarbon group,

a salt thereof or a hydrate of the foregoing.

2. A compound according to claim 1 , a salt of the compound or a hydrate of the foregoing, wherein R c11 is a group represented by the formula:

wherein V f11 is a single bond, an optionally substituted C 1-6 alkylene group or a group represented by the formula:

and V f12 is a hydrogen atom, a hydroxyl group, an optionally substituted 5- to 14-membered heterocyclic group, an optionally substituted 5- to 14-membered aromatic heterocyclic group, an optionally substituted C 6-14 aryl group or a group represented by the formula —NR f21 R f22 wherein R f21 and R f22 are each independently a hydrogen atom or an optionally substituted C 1-6 alkyl group.

Priority Claims (3)
JP 2000-320420 · Oct 20, 2000 · national
JP 2000-386195 · Dec 20, 2000 · national
JP 2001-046685 · Feb 22, 2001 · national
Continuity (4)
Division 11293785 · Dec 2, 2005
Division 10420466 · Apr 18, 2003
Continuation In Part PCTJP0109221 · Oct 19, 2001
Related Publication 20100197911A1 · Aug 5, 2010