NO950408L - Kinuclidine derivatives as squalene synthase inhibitors - Google Patents
Kinuclidine derivatives as squalene synthase inhibitorsInfo
- Publication number
- NO950408L NO950408L NO950408A NO950408A NO950408L NO 950408 L NO950408 L NO 950408L NO 950408 A NO950408 A NO 950408A NO 950408 A NO950408 A NO 950408A NO 950408 L NO950408 L NO 950408L
- Authority
- NO
- Norway
- Prior art keywords
- derivatives
- hydroxy
- squalene synthase
- nhch2
- och2
- Prior art date
Links
- 239000004059 squalene synthase inhibitor Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 108010022535 Farnesyl-Diphosphate Farnesyltransferase Proteins 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 102100037997 Squalene synthase Human genes 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- -1 hydroxy, amino Chemical group 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 208000035150 Hypercholesterolemia Diseases 0.000 abstract 1
- 125000005118 N-alkylcarbamoyl group Chemical group 0.000 abstract 1
- 125000005236 alkanoylamino group Chemical class 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004644 alkyl sulfinyl group Chemical class 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical class 0.000 abstract 1
- 125000004414 alkyl thio group Chemical class 0.000 abstract 1
- 125000005530 alkylenedioxy group Chemical class 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000001589 carboacyl group Chemical class 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical class 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000002923 oximes Chemical class 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000008584 quinuclidines Chemical class 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Kinuklidin-derivater med formel (I) og farmasøytisk godtagbare salter derav, 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 fra -CH2CH2-, -CH=CH-, -C=C-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S(0)n- og -S(O)nCH2- hvor n er O, l eller 2; og Ar er fenyl som eventuelt er usubstituert eller substituert med en eller flere substi- tuenter valgt fra halogen, hydroksy, amino, nitro, cyano, karboksy, karbamoyl, alkyl, alkenyl, alkynyl, alkoksy, alkyl- amino, dialkylamino, N-alkylkarbamoyl, N,N-dialkylkarbamoyl, - alkoksykarbonyl, alkyltio, alkylsulfinyl, alkylsulfonyl, halogen-alkyl, alkanoylamino, alkylendioksy, alkanoyl og oksim-derivater derav og 0-alkyl-etere av oksimene; forutsatt at når X er valgt fra -OCH2-, -NHCH2- og -S(O)nCH2-, er R1 ikke hydroksy; hemmer skvalen-syntase og er nyttige for behandling av sykdom- mer eller medisinske lidelser hvor hemning av skvalen-syntase er ønskelig. Anvendelse av slike heterocykliske derivater for behandling av lidelser så som hyperkolesterolemi og aterosklerose er angitt, så vel som nye forbindelser, frem- gangsmåter for fremstilling av dem og farmasøytiske preparater inneholdende dem.Quinuclidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, wherein: R 1 is hydrogen or hydroxy; R 2 is hydrogen; or R1 and R2 are bonded together such that CR1-CR2 is a double bond; X is selected from -CH2CH2-, -CH = CH-, -C = C-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -CH2S (O) n - and -S (O) nCH 2 - where n is 0, 1 or 2; and Ar is phenyl optionally unsubstituted or substituted with one or more substituents selected from halogen, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, dialkylamino, N-alkylcarbamoyl , N, N-dialkylcarbamoyl, - alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of the oxymers; provided that when X is selected from -OCH2-, -NHCH2- and -S (O) nCH2-, R1 is not hydroxy; inhibits squalene synthase and is useful for treating diseases or medical disorders where squalene synthase inhibition is desired. The use of such heterocyclic derivatives for the treatment of disorders such as hypercholesterolemia and atherosclerosis is disclosed, as well as novel compounds, methods of preparing them, and pharmaceutical preparations containing them.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB929216721A GB9216721D0 (en) | 1992-08-06 | 1992-08-06 | Therapeutic heterocyclic derivatives |
| PCT/GB1993/001648 WO1994003451A1 (en) | 1992-08-06 | 1993-08-04 | Quinuclidine derivatives as squalene synthase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO950408D0 NO950408D0 (en) | 1995-02-03 |
| NO950408L true NO950408L (en) | 1995-02-06 |
Family
ID=26301381
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO950408A NO950408L (en) | 1992-08-06 | 1995-02-03 | Kinuclidine derivatives as squalene synthase inhibitors |
Country Status (1)
| Country | Link |
|---|---|
| NO (1) | NO950408L (en) |
-
1995
- 1995-02-03 NO NO950408A patent/NO950408L/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO950408D0 (en) | 1995-02-03 |
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