Spirobenzofuranone compounds
    22.
    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。

    5,6-Dihydroxy aminotetralol compounds
    23.
    发明授权
    5,6-Dihydroxy aminotetralol compounds 失效
    5,6-二羟基氨基四氢噻吩酚化合物

    公开(公告)号:US4104402A

    公开(公告)日:1978-08-01

    申请号:US741020

    申请日:1976-11-11

    IPC分类号: C07C87/28 A01N9/20

    摘要: Novel aminotetralol compounds of the formula ##STR1## wherein Z.sup.1 and Z.sup.2 are hydrogen or an alkyl group and R.sup.1 is a substituted acyclic hydrocarbon group or a cyclic hydrocarbon group, and their pharmaceutically acceptable salts, have excellent pharmacological activities such as strong bronchodilating activity or .beta.-adrenergic blocking activity. They are useful as medicines, for example, for treatment of asthma or arrhythmia.

    摘要翻译: 新颖的式“IMAGE”的氨基四氢化萘化合物,其中Z 1和Z 2为氢或烷基,R 1为取代的无环烃基或环状烃基及其药学上可接受的盐,具有优异的药理活性,例如强支气管扩张活性或β - 肾上腺素能阻滞活性。 它们作为药物有用,例如用于治疗哮喘或心律失常。

    2-piperazinone compounds and their use
    24.
    发明授权
    2-piperazinone compounds and their use 失效
    2-哌嗪酮化合物及其用途

    公开(公告)号:US5294713A

    公开(公告)日:1994-03-15

    申请号:US926171

    申请日:1992-08-07

    摘要: The compounds of the formula ##STR1## wherein G stands for an amidino group or an optionally cyclic amino group, these being respectively optionally substituted; D stands for a spacer having 2 to 6 atomic chain optionally bonded through a hetero-atom and/or a 5- to 6-membered ring (provided that the 5- to 6-membered ring is, depending on its bonding position, counted as 2 to 3 atomic chains); R.sup.1 stands for hydrogen, benzyl group or a lower alkyl group; R.sup.2 and R.sup.3 independently stand for a residual group formed by removing --CH(NH.sub.2)COOH from an .alpha.-amino acid, or R.sup.1 and R.sup.2 may form a 5- to 6-membered ring taken together with the adjacent N and C; X stands for hydrogen or an optionally substituted lower alkyl group; and Z stands for a group capable of forming an anion or a group convertible into an anion in a living body, or salts thereof and agents for inhibiting cell-adhesion, which are characterized by containing these compounds. The novel compounds and pharmaceutical agents are effective for prophylaxis and therapy of various diseases by controlling or inhibiting cell adhesion.

    摘要翻译: 式(*化学结构*)的化合物,其中G表示脒基或任选的环状氨基,它们分别任选被取代; D代表通过杂原子和/或5-至6-元环任选键合的具有2-6个原子的链的间隔物(条件是5-至6-元环取决于其键合位置,计为 2〜3个原子链); R1代表氢,苄基或低级烷基; R2和R3独立地表示通过从(α) - 氨基酸除去-CH(NH 2)COOH形成的残基,或者R 1和R 2可以与相邻的N和C一起形成5-至6-元环; X代表氢或任选取代的低级烷基; Z表示含有这些化合物的能够形成阴离子或可转化成活体中的阴离子的基团或其盐和抑制细胞粘附剂的基团。 新型化合物和药剂通过控制或抑制细胞粘附对各种疾病的预防和治疗是有效的。

    Piperidine derivatives, their production and use
    25.
    发明授权
    Piperidine derivatives, their production and use 失效
    哌啶衍生物,其生产和使用

    公开(公告)号:US4954625A

    公开(公告)日:1990-09-04

    申请号:US400680

    申请日:1989-08-30

    IPC分类号: A61K38/00 C07K5/02

    CPC分类号: C07K5/0222 A61K38/00

    摘要: Novel compounds of the formula: ##STR1## [wherein A is an .alpha.-amino acid residue; B is a group represented by the formula: ##STR2## wherein R.sup.4 is hydrogen, lower alkyl, aralkyl or amino-lower alkyl), whereby the linkage between the symbols A and B designates a peptide bond and the group R.sup.4 in B may be linked with A; R.sup.1 is hydrogen, lower alkyl or aralkyl; R.sup.2 is hydrogen, lower alkyl, aralkyl or acyl; X is alkylene] and salts thereof posses, for example, inhibitory activity on angiotensin converting enzyme, and are useful as an agent for diagnosis, prevention or treatment of hypertension as well as circulatory diseases such as cardiopathy and cerebral apoplexy.

    Condensed, seven-membered ring compounds and their use
    27.
    发明授权
    Condensed, seven-membered ring compounds and their use 失效
    浓缩的七元环化合物及其用途

    公开(公告)号:US4564612A

    公开(公告)日:1986-01-14

    申请号:US599187

    申请日:1984-04-11

    摘要: Novel condensed, seven-membered ring compounds of the formula: ##STR1## [wherein R.sup.1 and R.sup.2 each represent hydrogen, halogen, trifluoromethyl, lower alkyl or alkoxy, or both jointly form tri- or tetramethylene; R.sup.3 is hydrogen, lower alkyl or aralkyl; R.sup.4 is hydrogen or alkyl, aralkyl or cycloalkylalkyl which may be substituted; X is a group represented by the formula S(O).sub.n (where n is an integer of 0 to 2); Y is a carboxyl group which may be esterified or amidated; m is 1 or 2] and salts thereof.These compounds exhibit inhibitory activity on angiotensin converting enzyme and so forth, and are of value as an agent for diagnosis, prevention and treatment of hypertension.

    摘要翻译: 新颖的下式的缩合的七元环化合物:其中R 1和R 2各自代表氢,卤素,三氟甲基,低级烷基或烷氧基,或两者共同形成三 - 或四亚甲基; R3是氢,低级烷基或芳烷基; R4是氢或可以被取代的烷基,芳烷基或环烷基烷基; X为由式S(O)n(n为0〜2的整数)表示的基团。 Y是可被酯化或酰胺化的羧基; m为1或2]及其盐。 这些化合物对血管紧张素转换酶等具有抑制活性,作为高血压的诊断,预防和治疗药物具有价值。

    1-Azaxanthone derivatives
    30.
    发明授权
    1-Azaxanthone derivatives 失效
    1-氮杂酮衍生物

    公开(公告)号:US4255576A

    公开(公告)日:1981-03-10

    申请号:US970105

    申请日:1978-12-18

    CPC分类号: C07D491/04 C07D311/58

    摘要: The present invention relates to novel 1-azaxanthone derivatives, which are shown by the following formula: ##STR1## wherein m is 1 or 2R'.sub.1 is hydrogen, C.sub.1-6 alkyl, phenyl, C.sub.1-6 alkoxycarbonyl, hydroxy, C.sub.1-4 alkoxy, amino or C.sub.1-3 alkylamino;each of R.sub.2 is independently C.sub.1-6 alkyl, C.sub.1-4 alkoxy, halogen, nitro, hydroxy, carboxy, amino, C.sub.1-3 alkylamino or di(C.sub.1-3 alkyl) amino; orwhen m is 2, the two R.sub.2 groups may be independently as defined above or may form together with adjacent rings carbon atoms the butadienylene group;R.sub.3 is cyano, C.sub.1-6 alkoxycarbonyl, carboxamide, N-C.sub.1-3 alkylcarboxamide or N,N-di(C.sub.1-3 alkyl) carboxamide.The novel derivatives are useful as intermediates for 1-azaxanthone-3-carboxylic acid derivatives having effective antiallergic and bronchodilating activities.

    摘要翻译: 本发明涉及由下式表示的新颖的1-氮杂酮衍生物:其中m为1或2,R'1为氢,C1-6烷基,苯基,C1-6烷氧基羰基,羟基,C1- 4个烷氧基,氨基或C 1-3烷基氨基; 每个R 2独立地是C 1-6烷基,C 1-4烷氧基,卤素,硝基,羟基,羧基,氨基,C 1-3烷基氨基或二(C 1-3烷基)氨基; 或当m为2时,两个R 2基团可以独立地如上定义,或者可以与相邻的环碳原子一起形成亚丁二烯基; R 3是氰基,C 1-6烷氧基羰基,甲酰胺,N-C 1-3烷基羧酰胺或N,N-二(C 1-3烷基)甲酰胺。 该新型衍生物可用作具有有效抗过敏和支气管扩张活性的1-氮杂酮-3-羧酸衍生物的中间体。