RU94015855A - QUINUCLIDINE DERIVATIVES, METHOD OF THEIR PRODUCTION, PHARMACEUTICAL COMPOSITION - Google Patents
QUINUCLIDINE DERIVATIVES, METHOD OF THEIR PRODUCTION, PHARMACEUTICAL COMPOSITIONInfo
- Publication number
- RU94015855A RU94015855A RU94015855/04A RU94015855A RU94015855A RU 94015855 A RU94015855 A RU 94015855A RU 94015855/04 A RU94015855/04 A RU 94015855/04A RU 94015855 A RU94015855 A RU 94015855A RU 94015855 A RU94015855 A RU 94015855A
- Authority
- RU
- Russia
- Prior art keywords
- derivatives
- denotes
- alkylcarbamoyl
- hydroxyl
- treatment
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title claims 2
- 150000008584 quinuclidines Chemical class 0.000 title claims 2
- 102100007210 FDFT1 Human genes 0.000 claims 2
- 108010022535 Farnesyl-Diphosphate Farnesyltransferase Proteins 0.000 claims 2
- -1 cyano, carboxyl Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 150000002923 oximes Chemical class 0.000 claims 2
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 208000009576 Hypercholesterolemia Diseases 0.000 claims 1
- 125000005118 N-alkylcarbamoyl group Chemical class 0.000 claims 1
- 125000005236 alkanoylamino group Chemical class 0.000 claims 1
- 125000003342 alkenyl group Chemical class 0.000 claims 1
- 125000003545 alkoxy group Chemical class 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical class 0.000 claims 1
- 125000003282 alkyl amino group Chemical class 0.000 claims 1
- 125000000217 alkyl group Chemical class 0.000 claims 1
- 125000004644 alkyl sulfinyl group Chemical class 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical class 0.000 claims 1
- 125000004414 alkyl thio group Chemical class 0.000 claims 1
- 125000005530 alkylenedioxy group Chemical class 0.000 claims 1
- 125000000304 alkynyl group Chemical class 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 125000001589 carboacyl group Chemical class 0.000 claims 1
- 125000004663 dialkyl amino group Chemical class 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical class 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 1
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
Claims (1)
в которой R1 обозначает водород или гидроксил; R2 - водород или R1 и R2 объединены вместе, так, что CR1 - CR2 обозначает двойную связь; Ar1 обозначает фенилен; Ar2 - 6- членный гетероарил, содержащий один или два атома азота; и где один из или оба Ar1 и Ar2 необязательно могут содержать один или более заместителей, таких, как галоген, гидроксил, амино, нитро, циано, карбоксил, карбомоил, алкил, алкенил, алкинил, алкоксил, алкиламино, диалкиламино, N - алкилкарбомоил, ди-N-N-алкилкарбамоил, алкоксикарбонил, алкилтио, алкилсульфинил, алкилсульфонил, галогеноалкил, алканоиламино, алкилендиокси, алканоил и его оксимные производные и простые O-алкиловые эфиры вышеуказанных оксимных производных; ингибируют скваленсинтазу и поэтому пригодны для лечения заболеваний и состояний, которые нужно лечить, где желательно ингибирование скваленсинтазы, например, для лечения гиперхолестеринемии и атеросклероза. Также предложены способы получения этих производных и фармацевтических композиций, содержащих эти производные, их использования в медицине.Quinuclidine derivatives of the indicated formula and their pharmaceutically acceptable salts;
in which R 1 denotes hydrogen or hydroxyl; R 2 is hydrogen or R 1 and R 2 combined together, so that CR 1 - CR 2 denotes a double bond; Ar 1 denotes phenylene; Ar 2 is a 6 membered heteroaryl containing one or two nitrogen atoms; and where one or both of Ar 1 and Ar 2 may optionally contain one or more substituents, such as halogen, hydroxyl, amino, nitro, cyano, carboxyl, carbomoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, dialkylamino, N - alkylcarbamoyl, di-NN-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkyl, alkanoylamino, alkylenedioxy, alkanoyl and its oxime derivatives and O-alkyl ethers of the above oxime derivatives; inhibit squalene synthase and therefore suitable for the treatment of diseases and conditions that must be treated, where inhibition of squalene synthase is desirable, for example, for the treatment of hypercholesterolemia and atherosclerosis. Also proposed methods for producing these derivatives and pharmaceutical compositions containing these derivatives, their use in medicine.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9211796.9 | 1992-06-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU94015855A true RU94015855A (en) | 1995-11-27 |
Family
ID=
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