IP Library Granted Patent US 41,289
Granted Patent E1
US 41,289 · App. 12/009,446 · Granted Apr 27, 2010

Ultrashort acting hypnotic barbiturates

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Quick Facts
Patent No.
US 41,289
App. No.
12/009,446
Granted
Apr 27, 2010
Kind
E1
Abstract

The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.

Claims (19)

1. A compound selected from the group consisting of:

3-methyl-4,6-dioxo-5-phenylhexahydropyrimidine-5-acetic Acid, Adamantanemethyl Ester adamantan- 1 - ylmethyl ( 1 - methyl - 4 , 6 - dioxo - 5 - phenyl - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-phenylhexahydropyrimidine-5-acetic Acid, Cyclohexyl Ester cyclohexyl 2 -( 1 - methyl - 4 , 6 - dioxo - 5 - phenyl - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-δ 2 -cyclopentylhexahydropyrimidine-5-acetic Acid Adamantanemethyl Ester adamantan- 1 - ylmethyl ( 5 - cyclopent - 2 - en - 1 - yl - 1 - methyl - 4 , 6 - dioxo - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-δ 2 -cyclopentylhexahydropyrimidine-5-acetic Acid Cyclohexyl Ester cyclohexyl 2 -( 5 -( cyclopent - 2 - enyl )- 1 - methyl - 4 , 6 - dioxo - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

and pharmaceutically acceptable salts thereof.

2. A compound selected from the group consisting of:

3-methyl-4,6-dioxo-5-phenylhexahydropyrimidine-5-acetic Acid, Neopentyl Ester neopentyl 2 -( 1 - methyl - 4 , 6 - dioxo - 5 - phenyl - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-phenylhexahydropyrimidine-5-acetic Acid Isobutyl Ester isobutyl 2 -( 1 - methyl - 4 , 6 - dioxo - 5 - phenyl - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-δ 2 -cyclopentylhexahydropyrimidine-5-acetic Acid Neopentyl Ester neopentyl 2 -( 5 -( cyclopent - 2 - enyl )- 1 - methyl - 4 , 6 - dioxo - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

3-methyl-4,6-dioxo-5-δ 2 -cyclopentylhexahydropyrimidine-5-acetic Acid Isobutyl Ester isobutyl 2 -( 5 -( cyclopent - 2 - enyl )- 1 - methyl - 4 , 6 - dioxo - 2 - thioxohexahydropyrimidin - 5 - yl ) acetate

and pharmaceutically acceptable salts thereof.

3. A compound selected from the group consisting of:

4,6-dioxo-5-allyl-5-isopentylhexahydropyrimidine-3-aceticacid, Ethyl Ester ethyl 2 -( 5 - allyl - 5 - isopentyl - 4 , 6 - dioxo - 2 - thioxotetrahydropyrimidin - 1 ( 2 H )- yl ) acetate

3-ethoxycarbonyl-4,6-dioxo-5-allyl-5-isopentylhexahydropyrimidine ethyl 5 - allyl - 5 - isopentyl - 4 , 6 - dioxo - 2 - thioxotetrahydropyrimidine - 1 ( 2 H )- carboxylate

and pharmaceutically acceptable salts thereof.

4. A composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier or diluent.

5. A composition comprising the compound according to claim 2 and a pharmaceutically acceptable carrier or diluent.

6. A composition comprising the compound according to claim 3 and a pharmaceutically acceptable carrier or diluent.

Assignments (1)
SECURITY AGREEMENT Recorded Oct 18, 2010
From: ARYX THERAPEUTICS, INC.
To: AYER CAPITAL PARTNERS MASTER FUND, L.P.; MPM BIOVENTURES III, L.P.; MPM BIOVENTURES III-QP, L.P.; MPM BIOVENTURES III GMBH & CO. BETEILIGUNGS KG; MPM BIOVENTURES III PARALLEL FUND, L.P.; AYER CAPITAL PARTNERS KESTREL FUND, L.P.; MPM ASSET MANAGEMENT INVESTORS 2002 BVIII LLC
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