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US 5,395,958 AGranted
Cyclopropene derivatives
AssigneeMitsubishi Kasei Corporation
InventorsRyoichi Ando, Yasuhiro Morinaka, Eiichi Nakamura
Life of this patent
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Abstract
The cyclopropene derivatives of the present invention are useful as the intermediates for producing cyclopropenone derivatives exhibiting strong inhibition activity of thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L and the like.
Claims3
Cyclopropene derivatives represented by formula (I):
- ##STR590## wherein:
- R.sup.1 represents hydrogen atom or a protective group for an amino group;
- R.sup.2 represents hydrogen atom, a protective group for an amino group or a C.sub.1 -C.sub.5 alkyl group;
- R.sup.4 and R.sup.6 independently represent a hydrogen atom or C.sub.1 -C.sub.5 alkyl group;
- R.sup.3 and R.sup.5 independently represent a hydrogen atom or C.sub.1 -C.sub.15 alkyl group optionally substituted with C.sub.3 -C.sub.10 cycloalkyl group or C.sub.6 -C.sub.10 aryl group;
- or when R.sup.5 and R.sup.6 are taken together, they represent a C.sub.2 -C.sub. 6 alkylene group;
- R.sup.7 and R.sup.8 represent --OR.sup.10 and --OR.sup.11, respectively, wherein R.sup.10 and R.sup.11 independently represent C.sub.1 -C.sub.5 alkyl group optionally substituted with phenyl group;
- or when R.sup.10 and R.sup.11 are taken together, they represent a C.sub.2 -C.sub.6 alkylene group optionally substituted with one or more C.sub.1 C.sub.5 alkyl groups;
- or when R.sup.7 and R.sup.8 are taken together, they represent .dbd.O;
- R.sup.9 represents a hydrogen atom, C.sub.1 -C.sub.15 alkyl group, C.sub.3 -C.sub.10 cycloalkyl group, C.sub.2 -C.sub.15 alkenyl group, C.sub.6 -C.sub.10 aryl group optionally substituted with one or more substituents selected from the group consisting of halogen atom, C.sub.1 -C.sub.5 alkyl group, hydroxyl group and C.sub.1 -C.sub.5 alkoxy group, heterocyclic selected from the group consisting of thienyl and furyl, optionally substituted with one or more substituents selected from the group consisting of C.sub.3 -C.sub.12 trialkylsilyl group, halogen atom, C.sub.1 -C.sub.5 alkyl group, hydroxyl group and C.sub.1 -C.sub.5 alkoxy group, or --CR.sup.12 R.sup.13 OH wherein R.sup.12 and R.sup.13 independently represent a hydrogen atom, C.sub.1 -C.sub.5 alkyl group or C.sub.6 -C.sub.10 aryl group;
- or when R.sup.12 and R.sup.13 are taken together they represent a C.sub.3 -C.sub.10 cycloalkyl group;
- and
- n represents 0.
10 more elements
Dependencies are inferred from the claim text.