Claims
- 1. A thiazolidin-4-one derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof: ##STR115## wherein R.sup.1 is n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.8 alkynyl, C.sub.1 -C.sub.8 haloalkyl or a residue represented by the formula: ##STR116## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, t-butyldimethyl silyl, or phenyl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; and R.sup.2 is hydrogen or a residue represented by the formula ##STR117## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, t-butyldimethyl silyl, or phenyl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; and R.sup.3 is a residue represented by the formula
- --F--R.sup.9
- wherein F is C.sub.2 -C.sub.3 alkylene and R.sup.9 is an amino group represented by the formula ##STR118## wherein R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1 -C.sub.4 alkyl.
- 2. A compound according to claim 1, wherein R.sup.1 is n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, or a residue represented by the formula ##STR119## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2, and R.sup.2 is hydrogen.
- 3. A compound according to claim 1, wherein R.sup.1 is a residue represented by the formula: ##STR120## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; and R.sup.2 is hydrogen.
- 4. A compound according to claim 1, wherein R.sup.1 is n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, or a residue represented by the formula: ##STR121## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; R.sup.2 is hydrogen, and R.sup.3 is a residue represented by the formula:
- --F--R.sup.9
- wherein F is ethylene and R.sup.9 is an amino group represented by the formula: ##STR122## wherein R.sup.10 and R.sup.11 are independently hydrogen, methyl or ethyl.
- 5. A compound according to claim 1, wherein R.sup.1 is a residue represented by the formula ##STR123## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, and n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; R.sup.2 is hydrogen, and R.sup.3 is a residue represented by the formula:
- --F--R.sup.9
- wherein F is ethylene and R.sup.9 is an amino group represented by the formula ##STR124## wherein R.sup.10 and R.sup.11 are independently hydrogen, methyl or ethyl.
- 6. A pharmaceutical composition for treatment of a disease caused by the platelet activating factor, which comprises as an active ingredient a pharmaceutically effective amount of a compound represented by the formula ##STR125## wherein R.sup.1 is n-heptyl, n-octyl, n-noneyl, n-decyl, n-undecyl, n-dodecyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.8 alkynyl, C.sub.1 -C.sub.6 haloalkyl or a residue represented by the formula ##STR126## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, t-butyldimethyl silyl, or phenyl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; and
- R.sup.2 is hydrogen or a residue represented by the formula ##STR127## wherein B is a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, t-butyldimethyl silyl, or phenyl, n and n' each are an integer of 2 to 4, m is an integer of 1 to 3, and m' is an integer of 0 to 2; and
- R.sup.3 is a residue represented by the formula
- --F--R.sup.9
- wherein F is C.sub.2 -C.sub.3 alkylene and R.sup.9 is an amino group represented by the formula: ##STR128## wherein R.sup.10 and R.sup.11 are independently hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable inert carrier or diluent.
- 7. A pharmaceutical composition according to claim 6 wherein the disease is inflammation, circulatory disease, gastrointestinal ulceration or allergic disease.
- 8. A pharmaceutical composition according to claim 7 wherein the circulatory disease is DIC (disseminated intravascular coagulation) or endotoxin shock.
- 9. A pharmaceutical composition according to claim 7 wherein the allergic disease is asthma.
- 10. A pharmaceutical composition according to claim 7 wherein the gastrointestinal ulceration ia gastric ulcer.
- 11. A pharmaceutical composition according to claim 7 wherein the inflammation is nephritis or rheumatism.
- 12. A method for treatment of a disease caused by the platelet activating factor, which comprises administering to a patient a pharmaceutically effective amount of a compound represented by the formula: ##STR129## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in claim 6 or a pharmaceutically acceptable salt thereof.
Priority Claims (4)
Number |
Date |
Country |
Kind |
62-126391 |
May 1987 |
JPX |
|
62-139304 |
Jun 1987 |
JPX |
|
62-160481 |
Jun 1987 |
JPX |
|
63-12379 |
Jan 1988 |
JPX |
|
Parent Case Info
This is a division of application Ser. No. 07/196,058, filed May 19, 1988, U.S. Pat. No. 4,992,455 issued Feb. 12, 1991.
US Referenced Citations (6)
Foreign Referenced Citations (1)
Number |
Date |
Country |
0010420 |
Apr 1980 |
EPX |
Non-Patent Literature Citations (4)
Entry |
Chemical Abstracts, vol. 97, No. 25, Dec. 20, 1982, p. 853, Abstract No. 216166j. |
J. Am. Chem. Soc., 75, 109-114 (1953). |
J. Am. Chem. Soc., 76, 578-580 (1954). |
J. Am. Chem. Soc., 70, 3436-3439 (1948). |
Divisions (1)
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Number |
Date |
Country |
Parent |
196058 |
May 1988 |
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