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US3971772A
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Steroidal[16α,17-b]1,4-dioxanes and Steroidal[16α,17-b]1,4-dioxins
Assignee: ER Squibb and Sons LLC
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Filing: 1975-05-19
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Granted: 1976-07-27
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Expires: 1995-05-19
Abstract
Abstract A series of novel steroidal [[16α,17-b]1,4-dioxanes and steroidal [ 16α,17-b]1,4-dioxins having useful anti-inflammatory properties is disclosed herein.
Inventors
- 👤 Christopher M. Cimarusti
- 👤 Seymour D. Levine
- 👤 Frank L. Weisenborn
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 07:16
CPC Classifications
C; C07; C07J; C07J71/00; C07J71/0005
Claims Analysis
Total Claims: 40
Claim 1
Independent Claim
27 words
A 3,20-diketo pregnene having an 11β-hydroxy group or an 11-keto group and having fused on the 16 and 17 positions a 1,4-dioxane ring or a 1,4-dioxin ring.
Claim 2
Dependent Claim
27 words
A 3,20-diketo pregnene having an 11β-hydroxy group or an 11-keto group and having fused on the 16 and 17 positions a 1,4-dioxane ring or a 1,4-dioxin ring.
Claim 3
Dependent Claim
18 words
A steroid in accordance with claim 1 having fused on the 16 and 17 positions a 1,4-dioxane ring.
Claim 4
Dependent Claim
18 words
A steroid in accordance with claim 1 having fused on the 16 and 17 positions a 1,4-dioxin ring.
Claim 5
Dependent Claim
63 words
A steroid in accordance with claim 1 wherein the fused 1,4-dioxane ring or 1,4-dioxin ring has the structural formula ##EQU15## wherein A 1 is ##EQU16## wherein R 1 is hydrogen, alkyl or aryl; R 2 is hydrogen, alkyl or arylalkyl; R 3 is alkyl, cycloalkyl or aryl; and R 4 and R 5 are the same or different and are alkyl or aryl.
Claim 6
Dependent Claim
16 words
A steroid in accordance with claim 4 wherein A 1 is --CH 2--CH 2 --, ##EQU17##
Claim 7
Dependent Claim
93 words
A steroid having the formula ##SPC22## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen; Y is hydrogen and Y' is hydroxyl or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl or chloro; Q is hydrogen, methyl or fluoro; A 1 is ##EQU18## R 1 is hydrogen, alkyl or aryl; R 2 is hydrogen, alkyl or arylalkyl; R 3 is alkyl, cycloalkyl or aryl; and R 4 and R 5 are the same or different and are alkyl or aryl.
Claim 8
Dependent Claim
93 words
A steroid having the formula ##SPC22## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen; Y is hydrogen and Y' is hydroxyl or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl or chloro; Q is hydrogen, methyl or fluoro; A 1 is ##EQU18## R 1 is hydrogen, alkyl or aryl; R 2 is hydrogen, alkyl or arylalkyl; R 3 is alkyl, cycloalkyl or aryl; and R 4 and R 5 are the same or different and are alkyl or aryl.
Claim 9
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU19##
Claim 10
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU20##
Claim 11
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU21##
Claim 12
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU22##
Claim 13
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU23##
Claim 14
Dependent Claim
12 words
A steroid in accordance with claim 6 wherein A 1 is ##EQU24##
Claim 15
Dependent Claim
11 words
A steroid in accordance with claim 6 wherein X is fluoro.
Claim 16
Dependent Claim
11 words
A steroid in accordance with claim 6 wherein Z is hydroxyl.
Claim 17
Dependent Claim
11 words
A steroid in accordance with claim 6 wherein Z is acyloxy.
Claim 18
Dependent Claim
11 words
A steroid in accordance with claim 6 wherein Z is halogen.
Claim 19
Dependent Claim
11 words
A steroid in accordance with claim 6 wherein Z is chlorine.
Claim 20
Dependent Claim
12 words
A steroid in accordance with claim 6 having the name 9-fluoro-5'ξ,11β,21-trihydroxypregn-4-eno-]16α,17-b][1,4]dioxane-3,20-dione, 21-acetate.
Claim 21
Dependent Claim
12 words
A steroid in accordance with claim 6 having the name 9-fluoro-2',3'-dihydro-11β,21-dihydroxy-5'-methylpregn-4-eno[16.alpha.,17-b][1,4]dioxin-3,20-dione, 21-acetate.
Claim 22
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 9-fluoro-2',3'-dihydro-11β,21-dihydroxypregn-4-eno[16α,17-b][1,4]dioxin-3,20-dione.
Claim 23
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-2',3'-dihydro-11β-hydroxy-5'-methylpregna-1,4-dieno[16α,17-b][1,4]dioxin-3,20-dione.
Claim 24
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 5'ξ-ethoxy-9-fluoro-11β,21-dihydroxypregn-4-eno-[16α,17-b][1,4]dioxane-3,20-dione.
Claim 25
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-5'ξ-ethoxy-9-fluoro-11β-hydroxypregn-4-eno[16α,17-b][1,4]dioxane-3,20-dione.
Claim 26
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 9-fluoro-5'ξ,11β,21-trihydroxypregn-4-eno-[16α,17-b][1,4]dioxane-3,20-dione.
Claim 27
Dependent Claim
12 words
A steroid in accordance with claim 6 having the name 9-fluoro-5'ξ,11β,21-trihydroxypregn-4-eno-[16α,17-b][1,4]dioxane-3,20-dione, 5',21-diacetate.
Claim 28
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-5'ξ,11α-dihydroxypregna-1,4-dieno[16α,17-b][1,4]dioxane-3,20-dione.
Claim 29
Dependent Claim
12 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-5'ξ,11β-dihydroxypregna-1,4-dieno[16α,17-b][1,4]dioxane-3,20-dione, 5'-acetate.
Claim 30
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-2',3'-dihydro-11β-hydroxypregna-1,4-dieno[16.alpha.,17-b][1,4]dioxin-3,20-dione.
Claim 31
Dependent Claim
13 words
A steroid in accordance with claim 6 having the name 9-fluoro-11β, 21-dihydroxypregn-4-eno[16α,17-b]-[1,4]dioxane-3,5',20-trione, 21-acetate.
Claim 32
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-2',3'-dihydro-11β-hydroxy-5'-phenylpregna-1,4-dieno[16α,17-b][1,4]dioxin-3,20-dione.
Claim 33
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-9-fluoro-11β-hydroxypregna-1,4-dieno-[16α,17-b][1,4]dioxane-3,20-dione.
Claim 34
Dependent Claim
13 words
A steroid in accordance with claim 6 having the name 11β, 21-dihydroxypregna-1,4-dieno[16α,17-b][1,4]-dioxane-3,20-dione, 21-acetate.
Claim 35
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-5'-(4-chlorophenyl)-9-fluoro-2',3'-dihydro-11β-hydroxypregna-1,4-dieno[16α,17-b][1,4]dioxin-3,20-dione.
Claim 36
Dependent Claim
11 words
A steroid in accordance with claim 6 having the name 21-chloro-5'-(1,1-dimethylethyl)-9-fluoro-2',3'-dihydro-11β-hydroxypregna-1,4-dieno[16α,17-b][1,4]dioxin-3,20-dione.
Claim 37
Dependent Claim
83 words
A steroid having the formula ##SPC23## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen: Y is hydrogen and Y' is hydroxyl, or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl or chloro; Q is hydrogen, methyl or fluoro; and A 2 is ##EQU25## -CH(O-R 7 ) 2 , or ##SPC24## R 1 is hydrogen, alkyl or aryl; R 6 is alkyl or aryl; R 7 is alkyl or arylalkyl.
Claim 38
Dependent Claim
83 words
A steroid having the formula ##SPC23## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen: Y is hydrogen and Y' is hydroxyl, or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl or chloro; Q is hydrogen, methyl or fluoro; and A 2 is ##EQU25## -CH(O-R 7 ) 2 , or ##SPC24## R 1 is hydrogen, alkyl or aryl; R 6 is alkyl or aryl; R 7 is alkyl or arylalkyl.
Claim 39
Dependent Claim
74 words
A steroid having the formula ##SPC25## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen; Y is hydrogen and Y' is hydroxyl, or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl, or chloro; Q is hydrogen, methyl or fluoro; A 3 is ##EQU26## or ##EQU27## and R 4 and R 5 are the same or different and are alkyl or aryl.
Claim 40
Dependent Claim
74 words
A steroid having the formula ##SPC25## and the 1,2-dehydro and 6,7-dehydro derivatives thereof, wherein Z is hydrogen, hydroxyl, acyloxy or halogen; Y is hydrogen and Y' is hydroxyl, or together Y and Y' are =O; X is hydrogen or halogen; P is hydrogen, methyl, or chloro; Q is hydrogen, methyl or fluoro; A 3 is ##EQU26## or ##EQU27## and R 4 and R 5 are the same or different and are alkyl or aryl.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1979-07-27 | 1980-01-26 | 1980-07-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-07-27 | 1984-01-26 | 1984-07-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-07-27 | 1988-01-26 | 1988-07-27 | $7700.00 | Window Closed / Lapsed |