Benzoquinone derivatives
    1.
    发明授权
    Benzoquinone derivatives 失效
    苯醌衍生物

    公开(公告)号:US4808339A

    公开(公告)日:1989-02-28

    申请号:US168321

    申请日:1988-03-18

    摘要: A novel benzoquinone derivative of the general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each is methyl or methoxy; n is an integer of 0 to 21; m is 0 or 1, Z is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or an alkyl group which may optionally be substituted or, R.sub.3 and R.sub.4 together with the adjacent nitrogen atom form a morpholino group), a group of the formula: --COR.sub.5 (wherein R.sub.5 is an .alpha.-amino acid residue or a substituted or unsubstituted glucosamine residue), a group of the formula: ##STR3## (wherein R.sub.6 is a divalent hydrocarbon group of 1 to 3 carbon atoms), a group of the formula: ##STR4## (wherein R.sub.6 has the same meaning as defined above) or a group of the formula: ##STR5## (wherein l is an integer of 1 to 4 and R.sub.7 is hydroxy, methoxy or methyl) has protocollagen-proline hydroxylase inhibiting activity, collagen biosynthesis inhibiting activity and 5-lipoxygenase suppressant activity, and is useful for the prevention and treatment of such diseases as pulmonary fibrosis, hepatocirrhosis, nephrosclerosis, arteriosclerosis, scleroderma, myelofibrosis and chronic arthritis or for the prevention and treatment of asthma, allergic rhinitis, urticaria, etc.

    摘要翻译: 一种新型的苯醌衍生物,其通式如下:其中R 1和R 2相同或不同,各自为甲基或甲氧基; n为0〜21的整数。 m为0或1,Z为下式的基团:其中R 3和R 4相同或不同,各自为氢或可任意取代的烷基,或者R 3和R 4与相邻的氮 原子形成吗啉基),式-COR5(其中R5是α-氨基酸残基或取代或未取代的葡糖胺残基)的基团,下式的基团:其中R 6是二价烃 具有1至3个碳原子的基团),下式的基团:其中R 6具有与上述相同的含义)或下式的基团: - (CH = CH)1-COR 7(其中l是 1〜4的整数,R7为羟基,甲氧基或甲基)具有协议的生物 - 脯氨酸羟化酶抑制活性,胶原合成抑制活性和5-脂氧合酶抑制活性,可用于预防和治疗肺纤维化,肝硬化, 肾硬化,动脉硬化,硬皮病,骨髓纤维化和慢性 关节炎或预防和治疗哮喘,过敏性鼻炎,荨麻疹等

    Quinine derivatines
    6.
    发明授权
    Quinine derivatines 失效
    奎宁衍生物

    公开(公告)号:US4818441A

    公开(公告)日:1989-04-04

    申请号:US165009

    申请日:1980-07-01

    摘要: A compound of the general formul: ##STR1## wherein .alpha. .beta. means a saturated bond or a double bond; each R independently of one another is a methyl group or a methoxy group, or two R's taken together represent a group of --CH.dbd.CH--CH.dbd.CH--; n is zero or an integer of 1 through 9; when .alpha. .beta. is a saturated bond, R.sub.2 is a hydrogen atom or hydroxyl group, and when .alpha. .beta. is a double bond, R.sub.2 is a hydrogen atom; when .alpha. .beta. is a double bond or when R.sub.2 is a hydroxyl group, R.sub.1 is a carboxyl group, a group of CH.sub.2.sub.2m OH (wherein m is an integer of 1 through 3) or a group of ##STR2## (wherein m is an integer of 1 through 3); when .alpha. .beta. is a saturated bond and R.sup.2 is a hydrogen atom, R.sub.1 is a hydroxymethyl group or a group of ##STR3## (wherein m is an integer of 1 through 3) has pharmacological actions such as membrane stabilizing activity (e.g. lysosomal membrane stabilizing activity), mitochondrial electron transport activity, hypotensive activity, activity to inhibit cardiac hypertrophy, tracheal muscle relaxant activity, cerebral circulation improving activity and cerebral ischemia preventive activity and is of value in the prophylaxis and treatment of hypertension, cardiac failure, asthma, cerebral apoplexy and other diseases, as a cardiac failure remedy, bronchodilator, cerebral circulation improving agent or the like.

    摘要翻译: 一般化合物的化合物:其中αβ表示饱和键或双键; 每个R彼此独立地是甲基或甲氧基,或两个R一起表示-CH = CH-CH = CH-的基团; n为0或1〜9的整数; 当αβ是饱和键时,R2是氢原子或羟基,当αβ是双键时,R2是氢原子; 当αβ是双键时,或当R2是羟基时,R1是羧基,CH22mOH(其中m是1至3的整数)或一组(其中m是 1〜3); 当αβ为饱和键且R 2为氢原子时,R 1为羟甲基或一组(其中m为1至3的整数)具有药物作用如膜稳定活性(例如溶酶体膜稳定 活性),线粒体电子传递活性,降血压活性,抑制心脏肥大的活性,气管肌松弛剂活性,脑循环改善活性和脑缺血预防活性,并且在预防和治疗高血压,心力衰竭,哮喘,脑中风中具有价值 和其他疾病,作为心力衰竭治疗,支气管扩张剂,脑循环改善剂等。

    Spiro compounds, their production and use
    7.
    发明授权
    Spiro compounds, their production and use 失效
    螺环化合物,其生产和使用

    公开(公告)号:US4362740A

    公开(公告)日:1982-12-07

    申请号:US188834

    申请日:1980-09-19

    摘要: New spiro compounds of the formula: ##STR1## wherein n is an integer of 1 to 4, and X is halogen, lower alkyl, nitro, amino which may be substituted, hydroxyl which may be substituted, acyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may be substituted, sulfamoyl which may be substituted, lower alkylthio or lower alkylsulfonyl, or two of X at the 5- and 6-positions together form --CH.dbd.CH--CH.dbd.CH--, exhibit inhibitory activity to thrombocyte aggregation and are useful for the prophylaxis or treatment of cardiovascular disturbance such as thrombosis.

    摘要翻译: 新的具有下式的螺环化合物:其中n为1〜4的整数,X为卤素,低级烷基,硝基,可被取代的氨基,可被取代的羟基,酰基,羧基,低级烷氧基羰基,氨基甲酰基 其可以被取代,可以被取代的氨磺酰基,低级烷硫基或低级烷基磺酰基,或者在5-和6-位X上的两个一起形成-CH = CH-CH = CH-,表现出对血小板聚集的抑制活性,并且是有用的 用于预防或治疗心血管疾病如血栓形成。

    Spirobenzofuranone compounds
    10.
    发明授权
    Spirobenzofuranone compounds 失效
    螺苯并呋喃酮化合物

    公开(公告)号:US4284644A

    公开(公告)日:1981-08-18

    申请号:US115548

    申请日:1980-01-25

    摘要: Novel spiro compounds of the formula: ##STR1## wherein Ring A represents a benzene ring or a naphthalene ring, said rings being unsubstituted or substituted by at least one of lower alkyl, nitro, halogen, amino which may optionally be substituted, hydroxyl which may optionally be substituted, acyl, sulfamoyl, carboxyl, lower alkoxycarbonyl, carbamoyl which may optionally be substituted, ureido which may optionally be substituted, thioureido which may optionally be substituted, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminomethyl which may optionally be substituted, cyano and phenyl, have gastric secretion inhibitive, anti-inflammatory and analgesic activities, and are of value as drugs.

    摘要翻译: 新的具有下式的螺环化合物:其中环A表示苯环或萘环,所述环为未取代的或被至少一个低级烷基,硝基,卤素,可任意取代的氨基,羟基取代,羟基可以 可任选被取代的,酰基,氨磺酰基,羧基,低级烷氧基羰基,可任选被取代的氨基甲酰基,可任选被取代的脲基,可任选取代的硫脲基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,可任意取代的氨基甲基, 氰基和苯基,具有胃分泌抑制作用,消炎止痛活性,具有药物价值。