Claims
- 1. A prostacyclin-type compound of the formula ##STR3## wherein W is H or CH.sub.3 ; wherein A.sub.1 is --O-- (oxa) and E.sub.2 is --CH.sub.2 CH.sub.2 --;
- wherein L.sub.2 is --(CH.sub.2).sub.j --, wherein j is one to 4, inclusive;
- wherein M.sub.1 is ##STR4## wherein Q is oxo, .alpha.--H:.beta.--H, .alpha.--OH:.beta.--R.sub.4, or .alpha.--R.sub.4 :.beta.--OH,
- wherein R.sub.4 is hydrogen or alkyl of one to 4 carbon atoms, inclusive,
- wherein R.sub.1 is
- (1) --COOR.sub.3,
- (2) --CH.sub.2 OH,
- (3) --CH.sub.2 N(R.sub.7)(R.sub.8),
- (4) --CO--N(R.sub.7)(R.sub.8),
- (5) --CO--NH--SO.sub.2 --R.sub.15, or
- (6) tetrazolyl,
- wherein R.sub.3 is
- (a) hydrogen,
- (b) alkyl of one to 12 carbon atoms, inclusive,
- (c) cycloalkyl of 3 to 10 carbon atoms, inclusive,
- (d) aralkyl of 7 to 12 carbon atoms, inclusive,
- (e) phenyl,
- (f) phenyl substituted with one, 2, or 3 chloro or alkyl groups of one to 3 carbon atoms, inclusive;
- (g) --(Ph)--CO--CH.sub.3,
- (h) --(p--Ph)--NH--CO--(p--Ph)--NH--CO--CH.sub.3,
- (i) --(p--Ph)--NH--CO--(p--Ph),
- (j) --(p--Ph)--NH--CO--CH.sub.3,
- (k) --(p--Ph)--NH--CO--NH.sub.2,
- (l) --(p--Ph)--CH.dbd.N--NH--CO--NH.sub.2,
- (m) .beta.-naphthyl,
- (n) --CH.sub.2 --CO--R.sub.16,
- wherein --(Ph)-- is inter-phenylene and --(p--Ph) is inter-para-phenylene or para-phenyl;
- wherein R.sub.16 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl, or
- (o) a pharmacologically acceptable cation; wherein R.sub.7 and R.sub.8 are hydrogen, alkyl of one to 12 carbon atoms, inclusive, benzyl, or phenyl, being the same or different, and wherein R.sub.15 is hydrogen, alkyl of one to 12 carbon atoms, inclusive, phenyl, phenyl-substituted with one, 2, or 3 chloro or alkyl groups of one to 3 carbon atoms, inclusive, or phenyl substituted with hydroxycarbonyl or alkoxycarbonyl of one to 4 carbon atoms, inclusive,
- wherein R.sub.2 is hydrogen, hydroxyl, or hydroxymethyl,
- wherein R.sub.5 and R.sub.6 are hydrogen, alkyl of one to 4 carbon atoms, inclusive, or fluoro, being the same or different, with the proviso that one of R.sub.5 and R.sub.6 is fluoro only when the other is hydrogen or fluoro, and
- wherein X is
- (1) trans--CH.dbd.CH--,
- (2) cis--CH.dbd.CH--,
- (3) --C.tbd.C--, or
- (4) --CH.sub.2 CH.sub.2 --,
- with the further proviso that when R.sub.1 is --COOR.sub.3 wherein R.sub.3 is hydrogen or alkyl of one to 12 carbon atoms, inclusive; --CH.sub.2 OH; --CON(R.sub.7)(R.sub.8); or tetrazolyl; one of R.sub.5 or R.sub.6 is other than hydrogen.
- 2. A compound of claim 1, wherein W is H.
- 3. A compound of claim 1, wherein W is --CH.sub.3.
DESCRIPTION
The present invention is a continuation-in-part application of U.S. Ser. No. 126,512, filed Mar. 3, 1980 now U.S. Pat. No. 4,328,156, issued May 4, 1982, which is a division of Ser. No. 054,720, filed July 5, 1979, issued Sept. 30, 1980 as U.S. Pat. No. 4,225,507.
US Referenced Citations (2)
Number |
Name |
Date |
Kind |
4123441 |
Johnson et al. |
Oct 1978 |
|
4230721 |
Gandolfi et al. |
Oct 1980 |
|
Divisions (1)
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Number |
Date |
Country |
Parent |
054720 |
Jul 1979 |
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Continuation in Parts (1)
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Number |
Date |
Country |
Parent |
126512 |
Mar 1980 |
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