Imidazole derivatives
    1.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号:US4661603A

    公开(公告)日:1987-04-28

    申请号:US823633

    申请日:1986-01-29

    摘要: .alpha.-(2,6-dimethyl-4-carboxyphenyl)-2-methyl-5-(1-imidazolyl)-benzenemethanol, pharmaceutically acceptable metal salts forms thereof, acid addition salt forms thereof, amino acid addition salt forms thereof, hydrate forms thereof and mixtures thereof.Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects against liver disorders.

    摘要翻译: α-(2,6-二甲基-4-羧基苯基)-2-甲基-5-(1-咪唑基) - 苯甲醇,其药学上可接受的金属盐形式,其酸加成盐形式,其氨基酸加成盐形式,水合物 形式及其混合物。 这些化合物对凝血恶烷A2的生物合成具有抑制活性,对血小板聚集的抑制活性,血管扩张活性和对肝脏疾病的保护作用。

    Imidazole derivatives
    2.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号:US4581369A

    公开(公告)日:1986-04-08

    申请号:US556231

    申请日:1983-10-31

    摘要: An imidazole derivative of the formula: ##STR1## wherein each of R.sup.1 and R.sup.4 is a hydrogen atom or a lower alkyl group; each of R.sup.2 and R.sup.3 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aralkyloxy group, a nitro group or an amino group; A is --O--, --S--, --CH.dbd.CH-- pr --CH.dbd.N--; Z is an aryl group, a thienyl group, a pyridyl group or a furyl group, in which definition these aromatic (heterocyclic) rings may have 1 to 3 substituents, each substituent being independently selected from a halogen atom, a lower alkyl group, a cyclic alkyl group, a lower alkoxy group, a hydroxyl group, a carboxyl group, a lower alkoxycarbonyl group, a carboxy-lower-alkoxy group, a di-lower-alkylamino-lower-alkoxy group and a nitro group; and a pharmaceutically acceptable acid addition salt thereof, a method for preparing the same and a pharmaceutical composition containing such compound. Such compounds have inhibitory activities on biosynthesis of thromboxane A.sub.2, inhibitory activities on platelet aggregation, vasodilative activities and protective effects on liver disorders.

    摘要翻译: PCT No.PCT / JP83 / 00060 Sec。 371日期:1983年10月31日 102(e)1983年10月31日日期PCT提交1983年2月28日PCT公布。 出版物WO83 / 03096 日期:1983年9月15日。下式的咪唑衍生物:其中R 1和R 4各自为氢原子或低级烷基; R2和R3各自为氢原子,卤素原子,羟基,低级烷基,低级烷氧基,芳烷氧基,硝基或氨基; A是-O - , - S - , - CH = CH-Pr -CH = N-; Z是芳基,噻吩基,吡啶基或呋喃基,其中这些芳族(杂环)环可以具有1至3个取代基,每个取代基独立地选自卤素原子,低级烷基, 羟基,羧基,低级烷氧基羰基,羧基 - 低级烷氧基,二低级烷基氨基 - 低级烷氧基和硝基; 及其药学上可接受的酸加成盐,其制备方法和含有该化合物的药物组合物。 这些化合物对凝血恶烷A2的生物合成,对血小板聚集的抑制活性,血管扩张活性和对肝脏疾病的保护作用具有抑制活性。

    Tricycle substituted acetones
    3.
    发明授权
    Tricycle substituted acetones 失效
    三轮车替代丙酮

    公开(公告)号:US3974168A

    公开(公告)日:1976-08-10

    申请号:US503207

    申请日:1974-09-04

    摘要: Compounds of the formula: ##SPC1##WhereinOf X.sup.1 and X.sup.2 is a hydrogen atom, a halogen atom or an alkyl group having 1 to 4 carbon atoms;R.sup.1 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a group -B.sup.1 -R.sup.3 (wherein B.sup.1 is an alkylene group having 1 to 4 carbon atoms, and R.sup.3 is a carboxyl group, an alkoxycarbonyl group in which the alkoxy moiety has 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a di-alkyl-amino group in which each alkyl moiety has 1 to 4 carbon atoms);R.sup.2 is an alkyl group having 1 to 4 carbon atoms or a group -B.sup.2 -R.sup.4 (wherein B.sup.2 is an alkylene group having 2 to 4 carbon atoms, and R.sup.4 is a carboxyl group or a di-alkyl-amino group in which each alkyl moiety has 1 to 4 carbon atoms);A is a methylene group or a carbonyl group;Y is an oxygen atom, a sulfur atom or an alkyl-imino group in which the alkyl moiety has 1 to 4 carbon atoms; andRing P is a pyridine ring; andPharmaceutically acceptable salts thereof are disclosed.They are useful as anti-inflammatory agents, analgesics, antipyretics and antirheumatics.

    摘要翻译: 下式的化合物:

    Bis-(aminoalkoxy)-phenyl, pyridyl ketones, and use as immunological
agents
    4.
    发明授权
    Bis-(aminoalkoxy)-phenyl, pyridyl ketones, and use as immunological agents 失效
    双(氨基烷氧基) - 苯基,吡啶酮,并用作免疫剂

    公开(公告)号:US4465681A

    公开(公告)日:1984-08-14

    申请号:US403664

    申请日:1982-07-28

    摘要: Pyridine derivatives of the formula: ##STR1## or pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and each represents hydrogen atom or lower alkyl group, or R.sup.1 and R.sup.2, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form a heterocycle, A.sup.1 and A.sup.2 are the same or different and each represents alkylene or hydroxy-substituted alkylene group, Y.sup.1 and Y.sup.2 are the same or different and each represents oxygen or sulfur atom, and Z represents ##STR2## These compounds show pharmacological activities such as potentiating activity for leukocyte phagocytosis, potentiating activity for macrophage phagocytosis, potentiating activity for the production of rosette forming cells in the spleen and anti-adjuvant arthritis activity, and are useful as medicines.

    摘要翻译: PCT No.PCT / JP81 / 00374 Sec。 371日期1982年7月28日 102(e)日期1982年7月28日PCT 1991年12月9日PCT PCT。 出版物WO82 / 02045 日期:1982年6月24日。下式的吡啶衍生物:其中R 1,R 2,R 3和R 4相同或不同,各自表示氢原子或低级烷基,或者R 1和 R2或R3和R4与相邻氮原子一起形成杂环,A1和A2相同或不同,各自表示亚烷基或羟基取代的亚烷基,Y1和Y2相同或不同,各自表示氧或硫原子 ,Z表示这些化合物显示药理活性,例如白细胞吞噬的增强活性,巨噬细胞吞噬的增强活性,在脾中产生玫瑰花形成细胞的增强活性和抗佐剂关节炎活性,并且可用作药物 。

    1H-tetrazole derivatives
    5.
    发明授权
    1H-tetrazole derivatives 失效
    1H-四唑衍生物

    公开(公告)号:US4085111A

    公开(公告)日:1978-04-18

    申请号:US579173

    申请日:1975-05-20

    CPC分类号: C07D491/04 C07D495/04

    摘要: 1H-Tetrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein the ring P is pyridine ring; A is carbonyl, methylene or C.sub.2-4 alkylidene; Y is oxygen, sulfur or --N(R.sup.1)-- wherein R.sup.1 is hydrogen or C.sub.1-4 alkyl; each of X.sup.1 and X.sup.2 is hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenyl or substituted phenyl, any substitutent on the phenyl being halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethy; and R is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, hydroxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, carboxy-C.sub.1-4 alkyl, C.sub.1-4 alkoxycarbonyl-C.sub.1-4 alkyl or substituted or unsubstituted amino-C.sub.1-4 alkyl, any substituted amino being C.sub.1-4 alkyl- or di-C.sub.1-4 alkyl-amino, piperidino, 1-pyrrolidinyl, morpholino, 1-piperazinyl and 4-C.sub.1-4 alkyl-1-piperazinyl; are useful as antiallergic agents.

    摘要翻译: 下式的1H-四唑衍生物及其药学上可接受的盐,其中环P是吡啶环; A是羰基,亚甲基或C 2-4亚烷基; Y是氧,硫或-N(R 1) - ,其中R 1是氢或C 1-4烷基; X 1和X 2各自为氢,卤素,C 1-4烷基,C 1-4烷氧基,苯基或取代的苯基,苯基上任何取代基为卤素,C 1-4烷基,C 1-4烷氧基或三氟甲基; 并且R是氢,C 1-4烷基,C 2-4烯基,C 2-4炔基,羟基-C 1-4烷基,C 1-4烷氧基-C 1-4烷基,羧基-C 1-4烷基,C 1-4烷氧羰基-C 1 -4-烷基或取代或未取代的氨基-C 1-4烷基,任何取代的氨基是C 1-4烷基 - 或二-C 1-4烷基 - 氨基,哌啶子基,1-吡咯烷基,吗啉代,1-哌嗪基和4-C1-4 烷基-1-哌嗪基; 可用作抗过敏剂。

    Substituted alkanoic acids and derivatives
    6.
    发明授权
    Substituted alkanoic acids and derivatives 失效
    取代的链烷酸及其衍生物

    公开(公告)号:US3931205A

    公开(公告)日:1976-01-06

    申请号:US380415

    申请日:1973-07-18

    CPC分类号: C07D491/04 Y10S514/916

    摘要: Substituted alkanoic acids and derivatives thereof of the formula: ##SPC1##Wherein each of X.sup.1 and X.sup.2 is a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms; each of R.sup.1 and R.sup.2 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; A is a carbonyl group, a methylene group or an alkylidene group having 2 to 4 carbon atoms; Y is --O--, --S-- or --N(R)-- [wherein R is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms]; Z is OH or Q--B--N(R.sup.3)(R.sup.4) [wherein Q is O (oxygen atom) or NH, B is an alkylene group having 1 to 4 carbon atoms and each of R.sup.3 and R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R.sup.3 and R.sup.4 together with the adjacent nitrogen atom form a saturated heterocycle selected from the group consisting of pyrrolidine, piperidine, morpholine, piperazine and piperazine substituted by an alkyl group having 1 to 4 carbon atoms at the 4-position]; and ring P represents a pyridine or a pyridine N-oxide ring; and pharmaceutically acceptable salts thereof are useful as antirheumatics, analgesics, antipyretics and anti-inflammatory agents.

    摘要翻译: 下式的取代的链烷酸及其衍生物: