摘要:
A compound of the formula (I): ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represent oxygen atom; A represents OH or acyloxy group having 1 to 4 carbon atoms; B represents hydrogen atom; A and B together represent a bond; R.sup.1 and R.sup.2 represent hydrogen atom or alkyl group having 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 together represent 1,2-ethylene, 1,3-propylene, 1,4-butylene or 1,5-pentylene, and these alkylene groups may be substituted by alkyl group having 1 to 4 carbon atoms; R.sup.3 represents amido group of the formula: ##STR2## wherein n, R.sup.4, R.sup.5, R.sup.6, R.sup.7. R.sup.8. R.sup.9, R.sup.10 and R.sup.11 represent specific groups, and the pharmacological acceptable salts of the compounds which can form salts have strong activity for lowering blood pressure, and process therefor and pharmaceutical use of the compounds.
摘要:
A compounds of the formula (I): ##STR1## wherein A represents OH or OC(O)CH.sub.3-n X.sub.n, B represents hydrogen atom, or A and B together represent a bond; R.sup.1 represents hydrogen atom, R.sup.2 represents hydrogen atom, C(Z)CH.sub.3-n X.sub.n or C(Z)NHCH.sub.3-n X.sub.n or R.sup.1 and R.sup.2 together represents (CH.sub.2).sub.m, (CH.sub.2).sub.m-1 C(Z), N(R.sup.3)(CH.sub.2).sub.2 C(Z), (CH.sub.2).sub.m-2 NHC(Z) or (CH.sub.2).sub.m-2 OC(Z) in which X represents fluorine atom, chlorine atom, bromine atom, a methyl group or a methoxy group and n represents 0 or an integer of 1 to 3, Z represents oxygem atom or sulfur atom, m represents an integer of 4 or 5 and R.sup.3 represents hydrogen atom or a methyl group, and pharmacological acceptable salts of the compounds which can form salts, processes therefor and pharmaceutical use of the compounds.
摘要:
Disclosed are cardiotonic medicines containing, as the active ingredient, at least one of compounds of formula (I) and their pharmacologically acceptable salts when they form salts. ##STR1## wherein X.sup.1 and X.sup.2 do not exist or represents an oxygen atom; A represents OH or a C.sub.1 -C.sub.4 acyloxy group; B represents a hydrogen atom or may form a chemical bond along with A; X is an oxygen atom, nitrogen, sulfur, etc.; R.sup.1 and R.sup.2 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc.; R.sup.3 and R.sup.4 each represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, etc., or they may together form a 1,4-butylene or 1,5-pentylene group. The compounds have a strong activity of reinforcing the contraction of cardiac muscles and a strong activity of reducing the rate of heart beats. As they are not toxic, they are useful as cardiotonic medicines.
摘要:
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译:本发明涉及式(I)或(II)的苯并吡喃衍生物或其药学上可接受的盐,其中R1和R2彼此独立地为氢原子,C1-6烷基或C6-14芳基,R3为氢原子或C1- C 1-6烷基羰基氧基或与R 4一起形成键,R 4为氢原子,或与R 3一起形成键,m为0〜4的整数,n为0〜4的整数,V为单键,CR 7 R 8, NR9,O,S,SO或SO2,R5是氢原子或C1-6烷基,R6是氢原子,C1-6烷基,C3-8环烷基,C3-8环烯基,氨基,C1-6烷基氨基, C 1-6烷基氨基,C 6-14芳基氨基,C 2-9杂芳基氨基,C 6-14芳基,C 2-9杂芳基或C 2-9杂环基,A是与苯环稠合的5-,6-或7-元环作为构成原子 的环,氧原子,氮原子或硫原子可以单独或组合1〜3的数量包含在t中的不饱和键的数量 环是1,2或3,包括待稠合的苯环的不饱和键,构成环的碳原子可以是羰基或硫代羰基。 这些化合物可用作抗心律不齐剂。
摘要:
The present invention provides a novel optically active bidentate phosphine ligand palladium complex of formula (I) or (II) which can be used for the preparation of optically active .beta.-hydroxyketones: ##STR1## �wherein Y.sup.- represents an anion pair which may form salt; X represents ##STR2## {wherein R.sup.1 represents hydrogen atom, C.sub.1-6 alkyl group, C.sub.1-6 alkoxyl group, cyano group, nitro group, halogen atom or phenyl group, etc.; m represents 1 or 2; when m is 2, two R.sup.1 s may be same or different}; andA and B each independently represents phenyl group or cyclohexyl group {said phenyl group and cyclohexyl group each is unsubstituted or substituted by R.sup.2 (R.sup.2 has the same meaning as defined in R.sup.1)}).
摘要:
The present invention provides novel α-amino acid derivatives of formula (1): (wherein, R1, R2, R3, R4, X and Y are as defined in the claims) or pharmaceutically acceptable salts, prodrugs or solvates thereof. The derivatives of formula (1) have βARK1 inhibitory activity and are useful for preventing or treating heart failure. Moreover, the derivatives of formula (1) also have antitumor activity, particularly dual inhibitory activity on Aurora kinase and CDK, and are useful for cell proliferative diseases such as cancer.
摘要:
This invention relates to benzopyran derivatives of the formula (1) or the formula (2) wherein R1 and R2 represent independently of each other hydrogen atom or C1-6alkyl group, R3 represents hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents hydrogen atom or C1-6 alkyl group, R5 represents C1-6 alkyl group substituted with C6-14 aryl group or heteroaryl group, R6 represents C1-6 alkyl group, C1-6 alkoxy group, halogen atom, nitro group, C(O)NH2, C(O)NHR8 or C(O)NR8R9, or pharmaceutically acceptable salts thereof. These compounds are useful as an antiarrhythmic agent
摘要:
The present invention provides medicines for treating cardiac insufficiency which contain as an active ingredient indane derivatives of formula (I) wherein R1 represents hydrogen atom, nitro group, cyano group, C1-6 alkylcarbonylamino, R2 and R3 each independently represent C1-6 alkyl group, R4 represents hydroxyl group or C1-6 alkylcarbonyloxy group or represents a bond or oxygen atom together with R5, R5 represents hydrogen atom or represents a bond or oxygen atom together with R4, R6 represents hydrogen atom, hydroxyl group or NR7R8, n means 0 or an integer of 1 to 4, X represents C═O, CH2, SO2 or NR16, Y represents NR17 when X is C═O, CH2 or SO2 and represents C═O when X is NR16, Z is absent when Y represents NR17 or represents NR18 when Y is C═O, W represents aromatic groups or lactam rings, or pharmaceutically acceptable salt thereof.
摘要:
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.
摘要翻译:本发明涉及式(I)或(II)的苯并吡喃衍生物或其药学上可接受的盐,其中R1和R2彼此独立地为氢原子,C1-6烷基或C6-14芳基,R3为氢原子或C1- C 1-6烷基羰基氧基或与R 4一起形成键,R 4为氢原子,或与R 3一起形成键,m为0〜4的整数,n为0〜4的整数,V为单键,CR 7 R 8, NR9,O,S,SO或SO2,R5是氢原子或C1-6烷基,R6是氢原子,C1-6烷基,C3-8环烷基,C3-8环烯基,氨基,C1-6烷基氨基, C 1-6烷基氨基,C 6-14芳基氨基,C 2-9杂芳基氨基,C 6-14芳基,C 2-9杂芳基或C 2-9杂环基,A是与苯环稠合的5-,6-或7-元环作为构成原子 的环,氧原子,氮原子或硫原子可以单独或组合1〜3的数量包含在t中的不饱和键的数量 环是1,2或3,包括待稠合的苯环的不饱和键,构成环的碳原子可以是羰基或硫代羰基。 这些化合物可用作抗心律不齐剂。
摘要:
This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3 including an unsaturated bond of the benzene ring to be fused, carbon atoms constituting the ring may be carbonyl or thiocarbonyl. These compounds are useful as an anti-arrhythmic agent.