IP Library Granted Patent US 7,375,103
Granted Patent B2
US 7,375,103 · App. 10/508,107 · Granted May 20, 2008

Optically active pyridine derivative and a medicament containing the same

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Quick Facts
Patent No.
US 7,375,103
App. No.
10/508,107
Granted
May 20, 2008
Kind
B2
Abstract

An optically active (−)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity

Claims (7)

1. An optically active (−)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido[2,3-d][1,3]oxazin-2-one of the formula (I):

or a salt thereof.

2. The compound or a salt as claimed in claim 1 , having an optical purity of at least 90% enantiomeric excess.

3. The compound or a salt as claimed in claim 1 , having an optical purity of at least 95% enantiomeric excess.

4. A pharmaceutical composition comprising the compound or a salt thereof as claimed in claim 1 , 2 or 3 and at least one pharmaceutically acceptable excipient.

5. A pharmaceutical composition having IκB kinase inhibitory activity comprising the compound or a salt thereof as claimed in claim 1 as an active ingredient, together with a pharmaceutically acceptable excipient.

6. A method of treating an inflammatory condition involving NF-κB activity selected from the group consisting of asthma; allergic rhinitis; atopic dermatitis; hives; conjunctivitis; vernal catarrh; chronic arthrorheumatism; systemic lupus erythematosus; psoriasis; diabrotic colitis; systemic inflammatory response syndrome (SIRS); polymyositis; dermatomyositis (DM); Polyaritis nodoa (PN); mixed connective tissue disease (MCTD); Sjoegren's syndrome; and gout in a subject, comprising administering to the subject an effective amount of the compound of claim 1 , 2 , or 3 .

Assignments (3)
MERGER Recorded Jan 12, 2010
From: BAYER HEALTHCARE AG
To: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
Reel/Frame 023769/0122 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 27, 2009
From: BAYER PHARMACEUTICALS CORPORATION
To: BAYER HEALTHCARE LLC
Reel/Frame 023027/0804 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 9, 2005
From: MURATA, TOSHIKI; SAKAKIBARA, SACHIKO; YOSHINO, TAKASHI; SATO, HIROKI; KORIYAMA, YUJI; NUNAMI, NORIKO; YAMAUCHI, MEGUMI; FUKUSHIMA, KEIKO; GROSSER, ROLF; FUCHIKAMI, KINJI; BACON, KEVIN; LOWINGER, TIMOTHY
To: BAYER AKTIENGESELLSCHAFT
Reel/Frame 015690/0450 →