IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
|
| 출원번호 |
US-0490877
(2009-06-24)
|
| 등록번호 |
US-8114995
(2012-02-14)
|
|
발명자
/ 주소 |
- Hansen, Henrik C.
- Chopade, Shubham P.
- Citineni, Janakiram R.
- Short, Robert P.
- Yiannikouros, George P.
|
| 출원인 / 주소 |
|
| 대리인 / 주소 |
Finnegan, Henderson, Farabow, Garrett, & Dunner LLP
|
| 인용정보 |
피인용 횟수 :
17 인용 특허 :
58 |
초록
▼
The present disclosure relates to methods for preparing compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and in the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for
The present disclosure relates to methods for preparing compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and in the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
대표청구항
▼
1. A method of preparing a compound of Formula I: and solvates, hydrates, tautomers, and pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, and R4 are each independently selected from alkoxy, alkyl, amido, aryloxy, cycloalkyl, halogen, heterocyclyl, hydrogen, and nitro;R6 is selected f
1. A method of preparing a compound of Formula I: and solvates, hydrates, tautomers, and pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, and R4 are each independently selected from alkoxy, alkyl, amido, aryloxy, cycloalkyl, halogen, heterocyclyl, hydrogen, and nitro;R6 is selected from alkyl, alkoxy, and halogen;R5 is hydrogen, or R5 and R6 may be taken together with the carbon atoms to which they are attached, to form a ring selected from aryl, cycloalkyl, and heterocycyl;R8 is selected from alkyl, alkoxy, halogen, and hydrogen;W is C and p is 1; comprisinga) reacting an aldehyde of Formula II: wherein R5, R6 and R8 are as defined above, with ethylene carbonate to form a compound of Formula III: b) reacting the compound of Formula III with a compound of Formula IV wherein R1, R2, R3, and R4 are as defined above, to form the compound of Formula I. 2. The method according to claim 1, wherein R6 and R8 are each independently selected from alkyl and halogen. 3. The method according to claim 2, wherein R6 and R8 are each methyl. 4. The method according to claim 1, wherein R1 and R3 are each independently selected from alkoxy, alkyl, halogen, and hydrogen. 5. The method according to claim 4, wherein R1 and R3 are each methoxy. 6. The method according to claim 1, wherein the compound of Formula I is selected from: 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one;2-(3-chloro-4-(2-hydroxyethoxy)phenyl)-5,7-dimethoxyquinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3-methoxyphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-6,7-dimethoxyquinazolin-4(3H)-one;N-(2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-4-oxo-3,4-dihydroquinazolin-6-yl)acetamide;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethylquinazolin-4(3H)-one;5,7-dichloro-2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-6-methoxyquinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5-methoxyquinazolin-4(3H)-one;6-bromo-2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one; and2-(4-(2-hydroxyethoxy)-3-methylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one, and solvates, hydrates, tautomers, and pharmaceutically acceptable salts thereof. 7. The method according to claim 6, wherein the compound of Formula I is 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one, or a solvate, hydrate, tautomer, or pharmaceutically acceptable salt thereof.
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