摘要:
##STR1## A compound represented by general formula (I), a pharmaceutical composition containing same, a process for the production thereof, and an intermediate therefor. In formula (I) R 1 represents lower alkyl which may be substituted by a substituent selected from the group consisting of mercapto, lower alkylthio, arylthio and lower acylthio; R 2 , R 3 and R 4 may be the same or different from one another and each represents lower alkyl; X represents oxygen or sulfur; and Y represents a single bond or lower alkylene. The compound (I) has a matrix metalloprotease inhibitory activity and is useful for preventing and treating diseases caused by the progress of connective tissue breakage.
摘要:
##STR1## A compound represented by general formula (I), a pharmaceutical composition containing same, a process for the production thereof, and an intermediate therefor. In formula (I) R 1 represents lower alkyl which may be substituted by a substituent selected from the group consisting of mercapto, lower alkylthio, arylthio and lower acylthio; R 2 , R 3 and R 4 may be the same or different from one another and each represents lower alkyl; X represents oxygen or sulfur; and Y represents a single bond or lower alkylene. The compound (I) has a matrix metalloprotease inhibitory activity and is useful for preventing and treating diseases caused by the progress of connective tissue breakage.
摘要:
A triazolylated tertiary amine compound represented by general formula (I) or a salt thereof, having an aromatase inhibitory activity and being useful for preventing and treating breast cancer, mastopathy, endometriosis, prostatomergaly, etc., wherein A represents a single bond, lower alkylene or carbonyl; B represents lower alkyl, aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; D represents aryl, a 5- or 6-membered heterocyclic group, or a bicyclic fused heterocyclic group; and E represents 4H-1,2,4-triazolyl, 1H-1,2,4-triazolyl or 1H-1,2,3-triazolyl.
摘要:
A substituted tertiary amino compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. They have an aromatase inhibiting activity and are useful as a prophylactic and/or therapeutic agent for breast cancer, mastopathy, endometriosis, prostatic-hypertrophy, and so forth.
摘要:
An azole derivative represented by the following general formula (I) ##STR1## (symbols in the formula have the following meanings; R.sup.1 and R.sup.2 : the same or different from each other and each represents a hydrogen atom, a lower alkyl group or a phenyl group which may be substituted with a halogen atom, A, B and D: the same or different from one another and each represents a group represented by the formula ##STR2## or a nitrogen atom, X and Y: the same or different from each other and each represents a single bond, a methylene group, an oxygen atom, a group represented by a formula S(O).sub.n, or a group represented by the formula ##STR3## R.sup.3 and R.sup.4 : the same or different from each other and each represents a hydrogen atom or a lower alkyl group, and n: 0, 1 or 2), a salt thereof, a hydrate thereof or a solvate thereof. This compound has a function to inhibit steroid 17-20 lyase and is useful as preventive and treating agents for prostatic cancer, prostatic hypertrophy, virilism, breast cancer, mastopathy, histeromyoma, and endometriosis.
摘要:
Oxazinobenzazole derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each independently represents a hydrogen atom or a lower alkyl group; R.sup.5 and R.sup.6 jointly form, in conjunction with the two adjacent carbon atoms, a substituted or unsubstituted 5- or 6-membered heterocyclic ring having at least two nitrogen atoms and optionally having one or more heteroatom(s) selected from the group consisting of an oxygen atom, a sulphur atom and a nitrogen atom; and m is an integer of 0 or 1, and pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as antispasmodic medicaments.
摘要:
Novel benzoxazine derivatives of the formula (I): ##STR1## are provided as well as their pharmaceutically acceptable salts and a method for their use as potassium channel activating agents 2-(3,4-Dihydro-2, 2-dimethyl-6-phenylsulfonyl-2H-1,4-benzoxazin-4-yl)pyridine N-oxide is illustrative of a benzoxazine derivative of formula (I). Also provided are intermediate compounds such as those of formula (II): ##STR2##