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US4267114A
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19-Hydroxy-19-methyl-6,9α-epoxymethano-PGF compounds
Assignee: Pharmacia and Upjohn Co
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Filing: 1980-03-03
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Granted: 1981-05-12
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Expires: 2000-03-03
Abstract
Abstract The present invention provides novel 19-hydroxy-19-methyl-6,9α-epoxy-methano-PGF compounds which are useful for pharmacological purposes, e.g., anti-asthmatic indications.
Inventors
- 👤 John C. Sih
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 20:28
CPC Classifications
C; C07; C07D; C07D257/00; C07D257/02; C07D257/04; C07C; C07C405/00; C07C405/0008; C07C405/0041; C07D307/00; C07D307/77; C07D307/93; C07D307/935; C07D307/937
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
387 words
A prostacyclin-type compound of the formula ##STR3## wherein A 2 is --CH 2 O-- with --CH 2 bonded to the cyclopentane ring and E 1 is --CH 2 --; wherein L 1 is (1) --(CH 2 ) n --, wherein n is one to 5, inclusive, (2) --(CH 2 ) p --CF 2 --, wherein p is 2, 3, or 4; or (3) --CH 2 --CH═CH--; wherein M 1 is ##STR4## wherein Q is oxo, α--H:β--H, α--OH:β--R 4 , or α--R 4 :β--OH, wherein R 4 is hydrogen or alkyl of one to 4 carbon atoms, inclusive; wherein R 1 is (1) --COOR 3 , (2) --CH 2 OH, (3) --CH 2 N(R 7 )(R 8 ), (4) --CO--N(R 7 )(R 8 ), (5) --CO--NH--SO 2 --R 15 , or (6) tetrazolyl, wherein R 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 3 , (h) --(p-Ph)--NH--CO--(p-Ph)--NH--CO--CH 3 , (i) --(p-Ph)--NH--CO--(p-Ph), (j) --(p-Ph)--NH--CO--CH 3 , (k) --(p-Ph)--NH--CO--NH 2 , (l) --(p-Ph)--CH═N--NH--CO--NH 2 , (m) β--naphthyl, (n) --CH 2 --CO--R 16 , wherein --(Ph)-- is inter-phenylene and --(p-Ph) is inter-para-phenylene or para-phenyl; wherein R 16 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl, or (o) a pharmacologically acceptable cation; wherein R 7 and R 8 are hydrogen, alkyl of one to 12 carbon atoms, inclusive, benzyl, or phenyl, being the same or different, and wherein R 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, in the alkoxy group wherein R 2 is hydrogen, hydroxyl, or hydroxymethyl, wherein R 5 and R 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 5 and R 6 is fluoro only when the other is hydrogen or fluoro, and wherein X is (1) trans--CH═CH--, (2) cis--CH═CH--, (3) --C.tbd.C--, or (4 ) --CH 2 CH 2 --.
Claim 2
Dependent Claim
387 words
A prostacyclin-type compound of the formula ##STR3## wherein A 2 is --CH 2 O-- with --CH 2 bonded to the cyclopentane ring and E 1 is --CH 2 --; wherein L 1 is (1) --(CH 2 ) n --, wherein n is one to 5, inclusive, (2) --(CH 2 ) p --CF 2 --, wherein p is 2, 3, or 4; or (3) --CH 2 --CH═CH--; wherein M 1 is ##STR4## wherein Q is oxo, α--H:β--H, α--OH:β--R 4 , or α--R 4 :β--OH, wherein R 4 is hydrogen or alkyl of one to 4 carbon atoms, inclusive; wherein R 1 is (1) --COOR 3 , (2) --CH 2 OH, (3) --CH 2 N(R 7 )(R 8 ), (4) --CO--N(R 7 )(R 8 ), (5) --CO--NH--SO 2 --R 15 , or (6) tetrazolyl, wherein R 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 3 , (h) --(p-Ph)--NH--CO--(p-Ph)--NH--CO--CH 3 , (i) --(p-Ph)--NH--CO--(p-Ph), (j) --(p-Ph)--NH--CO--CH 3 , (k) --(p-Ph)--NH--CO--NH 2 , (l) --(p-Ph)--CH═N--NH--CO--NH 2 , (m) β--naphthyl, (n) --CH 2 --CO--R 16 , wherein --(Ph)-- is inter-phenylene and --(p-Ph) is inter-para-phenylene or para-phenyl; wherein R 16 is phenyl, p-bromophenyl, p-biphenylyl, p-nitrophenyl, p-benzamidophenyl, or 2-naphthyl, or (o) a pharmacologically acceptable cation; wherein R 7 and R 8 are hydrogen, alkyl of one to 12 carbon atoms, inclusive, benzyl, or phenyl, being the same or different, and wherein R 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, in the alkoxy group wherein R 2 is hydrogen, hydroxyl, or hydroxymethyl, wherein R 5 and R 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 5 and R 6 is fluoro only when the other is hydrogen or fluoro, and wherein X is (1) trans--CH═CH--, (2) cis--CH═CH--, (3) --C.tbd.C--, or (4 ) --CH 2 CH 2 --.
Claim 3
Dependent Claim
13 words
A compound according to claim 1, wherein R 1 is --CH 2 OH.
Claim 4
Dependent Claim
21 words
A compound according to claim 2, wherein M 1 is ##STR5## with bonds to A 2 and L 1 as shown.
Claim 5
Dependent Claim
26 words
A compound according to claim 3, wherein L 1 is --(CH 2 ) 2 -- Q is α--OH:β--H, R 2 is hydroxyl, and X is trans--CH═CH--.
Claim 6
Dependent Claim
11 words
A compound according to claim 2, wherein M 1 is ##STR6##
Claim 7
Dependent Claim
26 words
A compound according to claim 5, wherein L 1 is --(CH 2 ) 2 --, Q is α--OH:β--H, R 2 is hydroxyl, and X is trans--CH═CH--.
References Cited (Backward Citations)
US4123441A
Cited
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| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
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| 3.5 Years (Year 4) | 1984-05-11 | 1984-11-10 | 1985-05-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-05-11 | 1988-11-10 | 1989-05-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-05-11 | 1992-11-10 | 1993-05-12 | $7700.00 | Window Closed / Lapsed |