IP Library Granted Patent US 7,498,334
Granted Patent B2
US 7,498,334 · App. 10/500,040 · Granted Mar 3, 2009

Pyrrolopyrimidines as phosphodiesterase VII inhibitors

Assignee: Merck Patent GmbH
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Quick Facts
Patent No.
US 7,498,334
App. No.
10/500,040
Granted
Mar 3, 2009
Kind
B2
Abstract

Pyrrolopyrimidine derivatives of the formula I in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.

Claims (16)

1. A compound selected from the group consisting of

ethyl 5 -isopropyl-4-oxo-7-p-tolyl-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidine-6-carboxylate,

ethyl 5 -methyl-4-oxo-7-(3-chlorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine -6-carboxylate,

ethyl 5 -methyl-4-oxo-7-(2-chlorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine -6-carboxylate,

ethyl 5 -methyl-4-oxo-7-(2-fluorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine -6-carboxylate,

ethyl 5 -propyl-4-oxo-7-(2-chlorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine -6-carboxylate,

ethyl 5 -methyl-4-oxo-7-(4-chlorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine -6-carboxylate,

methyl 5 -methyl-4-oxo-7-(2-chlorophenyl)-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidine-6- carboxylate,

methyl 5 -methyl-4-oxo-7-phenyl-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidine-6-carboxylate,

methyl 5 -methyl-4-oxo-7-(2-thienyl)-4,7-dihydro-3H-pyrrolo[2,3-d]-pyrimidine-6-carboxylate,

and pharmaceutically usable salts of these compounds, and stereoisomers thereof, including mixtures thereof in all ratios.

2. A medicament composition comprising at least one compound according to claim 1 and at least one excipient or adjuvant.

3. A method for the preparation of a medicament, which comprises bringing a compound of claim 1 into a form suitable for pharmaceutical administration.

4. A kit comprising separate packs of

(a) an effective amount of a compound of claim 1 , and

(b) an effective amount of a further medicament active ingredient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 23, 2004
From: EGGENWEILER, HANS-MICHAEL; WOLF, MICHAEL
To: MERCK PATENT GESELLSCHAFT
Reel/Frame 015977/0951 →
Priority Claims (1)
DE 101 63 991 · Dec 24, 2001 · national
Continuity (1)
Related Publication 20050059686A1 · Mar 17, 2005