Claims
- 1. A compound having the structural formula Ia ##STR11## wherein R.sup.1 is (a) hydroxy,
- (b) OC(O)C.sub.1 -C.sub.5 alkyl,
- (c) O--C.sub.1 -C.sub.5 alkyl --OH, and
- (d) NHC(O)C.sub.1 -C.sub.5 alkyl; or
- wherein R.sup.2 is
- (a) straight chain C.sub.1 -C.sub.8 alkyl, or
- (b) phenyl-X,
- (c) C.sub.1 -C.sub.5 alkyl-R.sup.6 -phenyl-X;
- wherein R.sup.3 is
- (a) hydrogen,
- (b) C.sub.1 -C.sub.8 alkyl,
- (c) furanyl,
- (d) C.sub.1 -C.sub.5 alkyl-R.sup.6 -phenyl-X,
- (e) phenyl-X, or
- (f) Si (C.sub.1 -C.sub.5 alkyl).sub.3 ;
- wherein R.sup.4 is
- (a) phenyl-X,
- (b) C.sub.1 -C.sub.5 alkyl-phenyl-X,
- (c) halogen,
- (d) C.sub.1 -C.sub.8 alkyl,
- (e) OH,
- (f) OC.sub.1 -C.sub.5 alkyl-phenyl-X,
- (g) NHC(O)C.sub.1 -C.sub.5 alkyl, or
- (h) OC(O)C.sub.1 -C.sub.5 alkyl;
- (i) hydrogen, or
- (j) R.sup.4 together with two adjacent carbons on the ring to which it is attached form a cyclopentyl, hexyl, heptyl or octyl ring or an aromatic form thereof;
- wherein R.sup.5 is --(CH.sub.2).sub.c -- and .sub.c is 1;
- wherein R.sup.6 is,
- (a) O--,
- (b) S--, or
- (c) CH.sub.2 --;
- a is 1-4;
- wherein phenyl-X is phenyl substituted by 1 to 3 same or different substituent selected from the group
- (a) H,
- (b) halogen,
- (c) OH,
- (d) OC.sub.1 -C.sub.5 alkyl,
- (e) SC.sub.1 -C.sub.5 alkyl,
- (f) NH.sub.2,
- (g) N(C.sub.1 -C.sub.5 alkyl).sub.2,
- (h) NHC(O)C.sub.1 -C.sub.5 alkyl,
- (i) OC(O)C.sub.1 -C.sub.5 alkyl,
- (j) CF.sub.3,
- (k) CN, or
- (l) CO.sub.2 C.sub.1 -C.sub.5 alkyl;
- or pharmaceutically acceptable acid addition salts thereof; with proviso that where R.sup.1 is hydroxy or --NHC(O)C.sub.1 -C.sub.5 alkyl, R.sup.2 is not --C.sub.1 -C.sub.6 alkyl, R.sup.3 is not --C.sub.1 -C.sub.6 alkyl or phenyl-X and R.sup.4 is not halogen.
- 2. A compound according to claim 1 which is
- Ethanone, 1-(5,6-dihydro-2-methyl-4H-pyrrolo[1,2-b]pyrazol-3-yl)- , oxime.
- 3. A compound of claim 1 wherein R.sup.1 is hydroxy; R.sup.2 is straight chain C.sub.1 -C.sub.8 alkyl; R.sup.3 is straight chain C.sub.1 -C.sub.8 alkyl; and R.sup.4 is hydrogen.
- 4. A method for treating atherosclerosis or hypercholesterolemia by administering a therapeutically effective amount of a compound having the formula ##STR12## wherein R.sup.1 is (a) hydroxy,
- (b) OC(O)C.sub.1 -C.sub.5 alkyl,
- (c) O--C.sub.1 -C.sub.5 alkyl --OH, and
- (d) NHC(O)C.sub.1 -C.sub.5 alkyl; or
- wherein R.sup.2 is
- (a) straight chain C.sub.1 -C.sub.8 alkyl, or
- (b) phenyl-X,
- (c) C.sub.1 -C.sub.5 alkyl-R.sup.6 -phenyl-X;
- wherein R.sup.3 is
- (a) hydrogen,
- (b) C.sub.1 -C.sub.8 alkyl,
- (c) furanyl,
- (d) C.sub.1 -C.sub.5 alkyl-R.sup.6 -phenyl-X,
- (e) phenyl-X, or
- (f) Si (C.sub.1 -C.sub.5 alkyl).sub.3 ;
- wherein R.sup.4 is
- (a) phenyl-X,
- (b) C.sub.1 -C.sub.5 alkyl-phenyl-X,
- (c) halogen,
- (d) C.sub.1 -C.sub.8 alkyl,
- (e) OH,
- (f) OC.sub.1 -C.sub.5 alkyl-phenyl-X,
- (g) NHC(O)C.sub.1 -C.sub.5 alkyl, or
- (h) OC(O)C.sub.1 -C.sub.5 alkyl;
- (i) hydrogen, or
- (j) R.sup.4 together with two adjacent carbons on the ring to which it is attached form a cyclopentyl, hexyl, heptyl or octyl ring or an aromatic form thereof;
- wherein R.sup.5 is --(CH.sub.2).sub.c -- and .sub.c is 1;
- wherein R.sup.6 is,
- (a) O--,
- (b) S--, or
- (c) CH.sub.2 --;
- a is 1-4;
- wherein phenyl-X is phenyl substituted by 1 to 3 same or different substituent selected from the group
- (a) H,
- (b) halogen,
- (c) OH,
- (d) OC.sub.1 -C.sub.5 alkyl,
- (e) SC.sub.1 -C.sub.5 alkyl,
- (f) NH.sub.2,
- (g) N(C.sub.1 -C.sub.5 alkyl).sub.2,
- (h) NHC(O)C.sub.1 -C.sub.5 alkyl,
- (i) OC(O)C.sub.1 -C.sub.5 alkyl,
- (j) CF.sub.3,
- (k) CN, or
- (l) CO.sub.2 C.sub.1 -C.sub.5 alkyl;
- or pharmaceutically acceptable acid addition salts thereof; with proviso that where R.sup.1 is hydroxy or --NHC(O)C.sub.1 -C.sub.5 alkyl, R.sup.2 is not --C.sub.1 -C.sub.6 alkyl, R.sup.3 is not --C.sub.1 -C.sub.6 alkyl or phenyl-X and R.sup.4 is not halogen.
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a divisional of U.S. Ser. No. 08/313,684, filed September 1994, now pending, which is a continuation-in-part of International Application No. PCT/US93/04059, filed 5 May 1993, which was a continuation-in-part of U.S. Ser. No. 07/900,229 filed 17 Jun. 1992, now abandoned.
Foreign Referenced Citations (1)
Number |
Date |
Country |
0299209 |
Jun 1988 |
EPX |
Divisions (1)
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Number |
Date |
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Parent |
313684 |
Sep 1994 |
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Continuation in Parts (1)
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Number |
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900229 |
Jun 1992 |
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