JPS5513273A - Readily absorbable thiazolidine prodrug of anti- inflammatory corticosteroid and its drug composition - Google Patents
Readily absorbable thiazolidine prodrug of anti- inflammatory corticosteroid and its drug compositionInfo
- Publication number
- JPS5513273A JPS5513273A JP7704779A JP7704779A JPS5513273A JP S5513273 A JPS5513273 A JP S5513273A JP 7704779 A JP7704779 A JP 7704779A JP 7704779 A JP7704779 A JP 7704779A JP S5513273 A JPS5513273 A JP S5513273A
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- formula
- compound
- group
- drug composition
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 229940079593 drug Drugs 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title abstract 2
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 title 1
- 230000003110 anti-inflammatory effect Effects 0.000 title 1
- 239000003246 corticosteroid Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 title 1
- 229940002612 prodrug Drugs 0.000 title 1
- 239000000651 prodrug Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002496 gastric effect Effects 0.000 abstract 1
- 125000000468 ketone group Chemical group 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 150000007530 organic bases Chemical class 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 210000001541 thymus gland Anatomy 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Abstract
NEW MATERIAL:A compound of formula I: [Z2 is oxo, β-hydroxyl group, etc.; R2 and R3 are H, alkyl, phenyl groups, etc., or may from -(CH2)n (n is an integer 5W7); R5 is -COOR11 (R11 is H, alkyl group, etc.); R10 is H, -COR11, etc.; R8 and R9 are H or alkyl groups] or formula II: [Z1 is oxo or β-hydroxyl group; R6 and R12 are H, -COR7 (R7 is alkyl, cycloalkyl group, etc.)].
EXAMPLE: 21-Acetyloxy-11β, 17α-dihydroxybregn-4-en-20-one-3, 2'-spiro (4'-carbohexoxy-1', 3'-thiazolidine).
USE: Anti-inflammatroy drugs effectively pernetrating into the skin and gastrointestinal wall, scarcely causing astrophyl or acting on thymus tissues, with a sufficiently high activity.
PROCESS: A compound wherein the keto group at the 3-position of formula I is reacted with a compound of formula III in a suitable organic solvent in the presence of an organic base.
COPYRIGHT: (C)1980,JPO&Japio
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92430578A | 1978-07-13 | 1978-07-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPS5513273A true JPS5513273A (en) | 1980-01-30 |
Family
ID=25450051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP7704779A Pending JPS5513273A (en) | 1978-07-13 | 1979-06-18 | Readily absorbable thiazolidine prodrug of anti- inflammatory corticosteroid and its drug composition |
Country Status (2)
| Country | Link |
|---|---|
| JP (1) | JPS5513273A (en) |
| AU (1) | AU4890479A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1994026767A1 (en) * | 1993-05-17 | 1994-11-24 | Endorecherche Inc. | Improved antiandrogens |
| US6110906A (en) * | 1989-03-10 | 2000-08-29 | Endorecherche, Inc. | Androgen derivatives for use in the inhibition of sex steroid activity |
| CN115974957A (en) * | 2021-10-15 | 2023-04-18 | 石家庄迪斯凯威医药科技有限公司 | Steroid derivatives and their pharmaceutical compositions and uses |
-
1979
- 1979-06-18 JP JP7704779A patent/JPS5513273A/en active Pending
- 1979-07-13 AU AU48904/79A patent/AU4890479A/en active Granted
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6110906A (en) * | 1989-03-10 | 2000-08-29 | Endorecherche, Inc. | Androgen derivatives for use in the inhibition of sex steroid activity |
| WO1994026767A1 (en) * | 1993-05-17 | 1994-11-24 | Endorecherche Inc. | Improved antiandrogens |
| CN115974957A (en) * | 2021-10-15 | 2023-04-18 | 石家庄迪斯凯威医药科技有限公司 | Steroid derivatives and their pharmaceutical compositions and uses |
Also Published As
| Publication number | Publication date |
|---|---|
| AU4890479A (en) | 1980-02-07 |
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