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US 6,147,100 AGranted
Pyrrolidine derivatives having phospholipase A.sub.2 inhibitory activity
AssigneeShionogi & Co., Ltd.
InventorsKaoru Seno, Mitsuaki Ohtani, Fumihiko Watanabe
Life of this patent
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Abstract
A compound represented by the formula (I): ##STR1## wherein, for example, R.sup.1 is optionally substituted aralkyl, Z is nitrogen atom which optionally substituted with alkyl, X.sup.1 is --CH.sub.2 NHCO--, X.sup.2 is phenylene, X.sup.3 is a bond, Y.sup.2 is optionally substituted aryl, B is oxygen atom, its pharmaceutically acceptable salt, or hydrate thereof and a pharmaceutical composition which contains them as an active ingredient.
Claims23
A compound represented by the formula (I):
- ##STR353## wherein R.sup.1 is hydrogen atom, lower alkyl, optionally substituted aryl, aryl fused with a non-aromatic hydrocarbon ring or a non-aromatic heterocyclic ring, optionally substituted aralkyl, optionally substituted arylcarbonyl, or optionally substituted heteroaryl;
- Z is --S--, --SO--, --O--, --OCH.sub.2 --, --CONH--, CONHCH.sub.2--, --N(R.sup.16)-- (wherein R.sup.16 is hydrogen atom, alkyl, or aralkyl), or a bond;
- X.sup.1 is --(CH.sub.2).sub.q --CO-- (wherein q is an integer of 0 to 3), --(CH.sub.2).sub.r --CO--N(R.sup.17)-- (wherein R.sup.17 is hydrogen atom or lower alkyl, and r is an integer of 0 to 3), --CH.sub.2 NSO.sub.2 --, --(CH.sub.2).sub.s --N(R.sup.18)--CO-- (wherein R.sup.18 is hydrogen atom or lower alkyl, s is an integer of 0 to 3), --CH.sub.2 NHCOCH.sub.2 O--, --CH.sub.2 N(R.sup.19)COCH.dbd.CH-- (wherein R.sup.19 is hydrogen atom or lower alkyl), --CH.sub.2 NHCS--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 OCH.sub.2 --, --CH.sub.2 --N(R.sup.20)--CH.sub.2 -- (wherein R.sup.20 is hydrogen atom, lower alkyl, or acyl), alkylene, alkenylene, or a bond;
- X.sup.2 is optionally substituted arylene, optionally substituted heteroarylene, heterocyclediyl, --C.tbd.C--, or a bond;
- X.sup.3 is alkylene, alkenylene, or a bond;
- A, B, and E are each independently oxygen atom or sulfur atom;
- D is hydrogen atom or hydroxy lower alkyl;
- Y.sup.1 is --(CH.sub.2).sub.m CO--, --(CH.sub.2).sub.m CONH--, --(CH.sub.2).sub.m CSNH--, --(CH.sub.2).sub.m SO.sub.2 --, --(CH.sub.2).sub.m COO--, --(CH.sub.2).sub.n NHCO--, --(CH.sub.2).sub.n NHSO.sub.2 --, or a bond;
- m is an integer of 0 to 3;
- n is an integer of 1 to 3;
- Y.sup.2 is a substituent represented by the formula:
- ##STR354## wherein R.sup.2 and R.sup.3 are both hydrogen atom or one is optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted cycloalkyl, and the other is hydrogen atom or lower alkyl;
- R.sup.4, R.sup.5, G ring, J ring, and L ring are each independently optionally substituted aryl, optionally substituted heteroaryl, optionally substituted cycloalkyl, or cycloalkenyl;
- a broken line (-- -- --) represents the presence or absence of a bond;
- and p is an integer of 0 to 2;
- a broken line (-- -- --) represents the presence or absence of a bond;
- a wavy line (.about.) represents cis or trans configuration of D to E;
- provided that X.sup.1 is alkylene and X.sup.2 and X.sup.3 are both bonds when the carbon atom attached to D and the adjacent carbon atom in the ring is linked by a single bond, and Y.sup.1 is not a bond when X.sup.1 is --CH.sub.2 O--, its pharmaceutically acceptable salt, or hydrate thereof.
15 more elements
Dependencies are inferred from the claim text.