摘要:
The invention provides a novel heterocyclic ring condensed benzothiazine compound which is effective for prevention or remedy of disease, in which histamine, leukotriene and the like participate. The heterocyclic ring condensed benzothiazine compound of the present invention or a pharmacologically acceptable salt thereof is effective for prevention or remedy of disease, in which a chemical mediator, such as histamine, leukotriene and the like, participate, for example, asthma, allergic coryza, atopic dermatitis, hives, hay fever, gastrointestinal allergy, food allergy and the like. Further, the heterocyclic ring condensed benzothiazine compound of the present invention, its pharmacologically acceptable salt or hydrates thereof is represented by the following formula: In the formula, the ring Het represents an unsaturated heterocyclic ring; R1 and R2 are the same as or different from each other, and each represents halogen atom, a lower alkyl group that may be substituted with a halogen atom, a lower alkoxy group that may be substituted with a halogen atom, a lower alkyl lower alkoxy group, cyano group; D represents a lower alkylene group and the like that may have a substituent; Q represents, for example, the formula —NR20R2 (in the formula, R20 and R21 are the same as or different from each other, and each represents hydrogen atom, a lower alkyl group that may be substituted with a halogen atom, an aryl group that may have a substituent, an arylalkyl group that may have a substituent, a heteroaryl group that may have a substituent or a heteroarylalkyl group that may have a substituent, or R20 and R21 may form a 3- to 8-membered ring along with the nitrogen atom to which they are bound); and x represents an integer of from 1 to 2.
摘要:
A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
摘要:
A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##
摘要:
A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
摘要:
A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
摘要:
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
摘要翻译:二苯基甲烷衍生物。 式(I)为新的(其中R 1和R 2各自为H,OH或低级烷氧基; U = -C XY或= NOW; X = H,CN或-COR 6; R 6 = OH或NH 2; Y = COOR 3,-CONR 4 R 5,-CH 2 NHSO 2 -C 6 H 5或-C(R 8)= NR 7; R 3 = H或低级烷氧基; R 10 =支链1-3C亚烷基; R 4和R 5各自为H,低级烷基或低级芳基烷基; 低级烷氧基或芳基; R8 = -VR9; V = O,S或N; R9 =烷基或芳基; W = -CH2-CO-CH2-COOR13,-CH2-C(= NOR14)-CH2-COOR15,-CH (CN) - (CH 2)q -COOR 16或 - (CH 2)pZ; R 13 = H或低级烷基; R 14 =低级烷基; R 15 = H或低级烷基; R 16 = H或低级烷基; q = = -SH,-SCN或衍生自5-或6-元环选择的单价gp,通过环中具有1个或更多个S的环; p = 1或2。
摘要:
A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##
摘要:
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
摘要翻译:二苯基甲烷衍生物。 式(I)为新的(其中R 1和R 2各自为H,OH或低级烷氧基; U = -C XY或= NOW; X = H,CN或-COR 6; R 6 = OH或NH 2; Y = COOR 3,-CONR 4 R 5,-CH 2 NHSO 2 -C 6 H 5或-C(R 8)= NR 7; R 3 = H或低级烷氧基; R 10 =支链1-3C亚烷基; R 4和R 5各自为H,低级烷基或低级芳基烷基; 低级烷氧基或芳基; R8 = -VR9; V = O,S或N; R9 =烷基或芳基; W = -CH2-CO-CH2-COOR13,-CH2-C(= NOR14)-CH2-COOR15,-CH (CN) - (CH 2)q -COOR 16或 - (CH 2)pZ; R 13 = H或低级烷基; R 14 =低级烷基; R 15 = H或低级烷基; R 16 = H或低级烷基; q = = -SH,-SCN或衍生自5-或6-元环选择的单价gp,通过环中具有1个或更多个S的环; p = 1或2。
摘要:
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower arylalkyl, --CH2--NHSO2--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
摘要翻译:二苯基甲烷衍生物。 式(I)为新的(其中R 1和R 2各自为H,OH或低级烷氧基; U = -C XY或= NOW; X = H,CN或-COR 6; R 6 = OH或NH 2; Y = COOR 3,-CONR 4 R 5,-CH 2 NHSO 2 -C 6 H 5或-C(R 8)= NR 7; R 3 = H或低级烷氧基; R 10 =支链1-3C亚烷基; R 4和R 5各自为H,低级烷基或低级芳基烷基; 低级烷氧基或芳基; R8 = -VR9; V = O,S或N; R9 =烷基或芳基; W = -CH2-CO-CH2-COOR13,-CH2-C(= NOR14)-CH2-COOR15,-CH (CN) - (CH 2)q -COOR 16或 - (CH 2)pZ; R 13 = H或低级烷基; R 14 =低级烷基; R 15 = H或低级烷基; R 16 = H或低级烷基; q = = -SH,-SCN或衍生自5-或6-元环选择的单价gp,通过环中具有1个或更多个S的环; p = 1或2。
摘要:
A new diphenyl-methane derivative is useful to inhibit agglomeration of blood and is defined by the formula, including a diphenylethylene derivative and a benzophenone oxime ether derivative. ##STR1## in which R1 and R2 each are hydrogen, hydroxyl or a lower alkoxy, U is .dbd.CXY or .dbd.N--O--W,X is hydrogen, cyano or --COR6, R6 being hydroxyl or an amino, Y is --R10--COOR3, R3 being hydrogen or a lower alkoxy, R10 being an alkylene having 1 to 3 carbon atoms, straight or branched, --CO--NR4R5, R4 and R5 each being hydrogen, a lower alkyl or a lower aralalkyl, --CH2--NHSO3--C6H5 or --C(R8).dbd.NR7, R7 being a lower alkoxy or an aryl, R8 is --VR9, V being oxygen, sulfur or nitrogen, R9 being an alkyl or an aryl,W is --CH2--CO--CH2--COOR13, R13 being hydrogen or a lower alkyl, --CH2--C(.dbd.NOR14)--CH2--COOR15, R15 being hydrogen or a lower alkyl, R14 being a lower alkyl, --CH(CN)--(CH2)q--COOR16, R16 being hydrogen or a lower alkyl, q being an integer of 1 to 3, or --(CH2)p--Z, Z being --SH, --SCN or a monovalent group derived from a five- or six-membered ring which may be substituted by a ring having one or more sulfur atoms in the ring, p being 1 or 2.
摘要翻译:二苯基甲烷衍生物。 式(I)为新的(其中R 1和R 2各自为H,OH或低级烷氧基; U = -C XY或= NOW; X = H,CN或-COR 6; R 6 = OH或NH 2; Y = COOR 3,-CONR 4 R 5,-CH 2 NHSO 2 -C 6 H 5或-C(R 8)= NR 7; R 3 = H或低级烷氧基; R 10 =支链1-3C亚烷基; R 4和R 5各自为H,低级烷基或低级芳基烷基; 低级烷氧基或芳基; R8 = -VR9; V = O,S或N; R9 =烷基或芳基; W = -CH2-CO-CH2-COOR13,-CH2-C(= NOR14)-CH2-COOR15,-CH (CN) - (CH 2)q -COOR 16或 - (CH 2)pZ; R 13 = H或低级烷基; R 14 =低级烷基; R 15 = H或低级烷基; R 16 = H或低级烷基; q = = -SH,-SCN或衍生自5-或6-元环选择的单价gp,通过环中具有1个或更多个S的环; p = 1或2。