摘要:
A compound of the formula or its pharmaceutically acceptable salt: where, in one example. R' is n-octanoyl, n is the integer O, R 2 is benzyl, R 3 is 1-carboxyethylammo, R 4 is hydrogen and R 5 is hydrogen and processes for their preparation and also a pharmaceutically composition comprising, as an effective ingredient, the above compound in association with pharmaceutically acceptable carriers.
摘要:
New semicarbazide derivatives of the formula: wherein R' is hydrogen, R 2 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, R 3 is lower alkyl, ar(lower)alkyl, lower alkenyl or aryl, or R 2 and R 3 are taken together to form (C 2 -C 6 )-alkylidene group optionally substituted with aryl or taken together with the adjacent nitrogen atom to form a saturated or unsaturated, 5- or 6-membered heterocyclic group optionally substituted with aryl; or R' and R 2 are taken together with the adjacent nitrogen atoms to form a saturated or unsaturated, 5- or 6-membered heterocyclic group or 1,2-diazaspiroalkane-1,2-diyl group, R 3 is hydrogen, lower alkyl, ar(lower)alkyl, lower alkeny or aryl; R 4 is aryl which may have substituent(s) selected from lower alkyl, halogen, lower alkoxy, lower alkylamino, halo(lower)alkyl, hydroxy, lower alkanoyl, esterified carboxy and carboxy, R 5 is hydrogen or lower alkyl, and X is 0 or S, provided that the lower alkyl group for R 3 is (C 3 -C 6 ) alkyl, when R 2 is hydrogen or (C 1 -C 2 ) alkyl and R 4 is aryl optionally having substituent(s) selected from groups consisting of halogen, lower alkyl, lower alkoxy and halo(lower)alkyl, and pharmaceutically acceptable salts thereof, and processes for preparation thereof and pharmaceutical composition comprising the same. These derivatives and salts thereof are useful as antiinflammatory and analgesic agents.
摘要:
A compound of the formula or its pharmaceutically acceptable salt: wherein R 1 is hydrogen or acyl; R 2 is carboxy or protected carboxy or a group of the formula: -COHN-R 2 wherein R 2 a is carboxy(lower)alkyl or protected carboxy(lower)alkyl; R 3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl ora graup oftheformula: R 3 a-CH-R 3 b wherein R 3 a is hydrogen, amino, protected amino or a cylamino, R 3 b is carboxy or protected carboxy; R P is carboxy, protected carboxy, carbamoyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl; ℓ isaninteger0or2, m is an integer 0 to 3 and n is an integer 0 to 1, with certain provisions, and pharmaceutically acceptable salts thereof and process for their preparation, and also a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.
摘要:
A compound of the formula or its pharmaceutically acceptable salt:
wherein R 1 is hydrogen or acyl; R 2 is carboxy or protected carboxy or a group of the formula:
-COHN-R 2 wherein R 2 a is carboxy(lower)alkyl or protected carboxy(lower)alkyl;
R 3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl ora graup oftheformula: R 3 a-CH-R 3 b wherein R 3 a is hydrogen, amino, protected amino or a cylamino, R 3 b is carboxy or protected carboxy; R P is carboxy, protected carboxy, carbamoyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl; ℓ isaninteger0or2, m is an integer 0 to 3 and n is an integer 0 to 1, with certain provisions, and pharmaceutically acceptable salts thereof and process for their preparation, and also a pharmaceutical composition comprising, as an effective ingredient, the above compound in association with a pharmaceutically acceptable, substantially nontoxic carrier or excipient.