NO950756L - Kinuclidine derivatives as squalene synthetase inhibitors - Google Patents
Kinuclidine derivatives as squalene synthetase inhibitorsInfo
- Publication number
- NO950756L NO950756L NO950756A NO950756A NO950756L NO 950756 L NO950756 L NO 950756L NO 950756 A NO950756 A NO 950756A NO 950756 A NO950756 A NO 950756A NO 950756 L NO950756 L NO 950756L
- Authority
- NO
- Norway
- Prior art keywords
- hydroxy
- derivatives
- alkylcarbamoyl
- sch
- alkylamino
- Prior art date
Links
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Forbindelser med formel (I) (I) og deres farmasøytisk akseptable salter, hvor R1 er hydrogen eller hydroksy, R2 er hydrogen, eller R1 og R2 er bundet sammen slik at CR1-CR2 er en dobbeltbinding, X er valgt blant -CH2CH2-, -CH=CH-, -C=C-, -CH2O-, -CH2NH-, -NHCH2~, - CH2CO-, -COCH2-, -CH2S- og -SCH.,-, Ar1 er en fenylgruppe, Ar2 er en heteroarylgruppe, og hvor en eller begge av Ar1 og Ar2 eventuelt kan bære en eller flere substituenter som uavhengig er valgt blant halogen, hydroksy, amino, nitro, cyano, kar- boksy, karbamoyl, alkyl, alkenyl, alkynyl, alkoksy, alkyl- amino, di-alkylamino-, N-alkylkarbamoyl, di-N,N-alkylkarba- moyl, alkoksykarbonyl, alkyltio, alkylsulfinyl, alkylsulfonyl, halogenalkyl, karboksyalkyl og alkanoylamino, forutsatt at når R1 er hydroksy, er X ikke valgt blant -NHCH - og -SCH -, er inhibitorer for sgualen-syntetase og dermed nyttige ved behandling av medisinske tilstander hvor en senkning av koles- terol er fordelaktig, så som hyperkolesterolemi og atero- sklerose. Fremgangsmåter for fremstilling av disse derivater, og farmasøytiske blandinger inneholdende dem, er også beskrevet sammen med deres anvendelse innen medisin.Compounds of formula (I) (I) and their pharmaceutically acceptable salts wherein R1 is hydrogen or hydroxy, R2 is hydrogen, or R1 and R2 are bonded together so that CR1-CR2 is a double bond, X is selected from -CH2CH2-, -CH = CH-, -C = C-, -CH2O-, -CH2NH-, -NHCH2 ~, - CH2CO-, -COCH2-, -CH2S- and -SCH., -, Ar1 is a phenyl group, Ar2 is a heteroaryl group, and wherein one or both of Ar1 and Ar2 may optionally carry one or more substituents independently selected from halogen, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino , di-alkylamino, N-alkylcarbamoyl, di-N, N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkyl, carboxyalkyl and alkanoylamino, provided that when R1 is hydroxy, X is not selected from -NHCH - and -SCH -, are inhibitors of sgualene synthetase and thus useful in treating medical conditions where lowering cholesterol is beneficial, such as hypercholesterolemia and atherosclerosis Lerose. Methods for preparing these derivatives, and pharmaceutical compositions containing them, are also described together with their use in medicine.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB929218334A GB9218334D0 (en) | 1992-08-28 | 1992-08-28 | Heterocyclic compounds |
| PCT/GB1993/001802 WO1994005660A1 (en) | 1992-08-28 | 1993-08-24 | Quinuclidine derivatives as squalene synthase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO950756L true NO950756L (en) | 1995-02-27 |
| NO950756D0 NO950756D0 (en) | 1995-02-27 |
Family
ID=26301506
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO950756A NO950756D0 (en) | 1992-08-28 | 1995-02-27 | Kinuclidine derivatives as squalene synthetase inhibitors |
Country Status (1)
| Country | Link |
|---|---|
| NO (1) | NO950756D0 (en) |
-
1995
- 1995-02-27 NO NO950756A patent/NO950756D0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO950756D0 (en) | 1995-02-27 |
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