4-Hydroxy-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and
salts thereof
    51.
    发明授权
    4-Hydroxy-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and salts thereof 失效
    4-羟基-2H-萘并({2,1-e {9-1,2-噻嗪-3-甲酰胺-1,1-二氧化物及其盐

    公开(公告)号:US3992535A

    公开(公告)日:1976-11-16

    申请号:US626623

    申请日:1975-10-29

    CPC分类号: C07D275/06 C07D279/02

    摘要: Compounds of the formula ##SPC1##WhereinR.sub.1 is hydrogen, methyl or ethyl, andAr is phenyl, 3-chlorophenyl, 3-bromophenyl, 2-fluorophenyl, 3-fluorophenyl, 4-fluorophenyl, 3-tolyl, 2-methoxyphenyl, 3-methoxyphenyl, 2-pyridyl, 4-methyl-2-pyridyl, 6-methyl-2-pyridyl, 3-hydroxy-2-pyridyl, 3-pyridyl, 4-pyridyl, 6-chloro-3-pyridazinyl, 2-pyrazinyl, 6-chloro-2-pyrazinyl, 6-chloro-4-pyrimidinyl, 2-thiazolyl, 4-methyl-2-thiazolyl, 4-ethyl-2-thiazolyl, 5-methyl-2-thiazolyl, 5-ethyl-2-thiazolyl, 4,5-dimethyl-2-thiazolyl, 4-ethyl-5-methyl-2-thiazolyl, 5-ethyl-4-methyl-2-thiazolyl, 2-benzothiazolyl, 4,5,6,7-tetrahydro-2-benzothiazolyl, 5,6-dihydro-7H-thiopyrano[4,3-d]thiazol-2-yl, 3-methyl-5-isothiazolyl, 1,3,4-thiadiazolyl, 5-methyl-1,3,4-thiadiazol-2-yl or 5-methyl-3-isoxazolyl,And non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds as well as their salts are useful as inhibitors of platelet adhesion and aggregation.

    摘要翻译: 式WHERE R1的化合物是氢,甲基或乙基,Ar是苯基,3-氯苯基,3-溴苯基,2-氟苯基,3-氟苯基,4-氟苯基,3-甲苯基,2-甲氧基苯基,3-甲氧基苯基, 2-吡啶基,4-甲基-2-吡啶基,6-甲基-2-吡啶基,3-羟基-2-吡啶基,3-吡啶基,4-吡啶基,6-氯-3-哒嗪基,2-吡嗪基,6-吡啶基, 4-氯-2-吡嗪基,6-氯-4-嘧啶基,2-噻唑基,4-甲基-2-噻唑基,4-乙基-2-噻唑基,5-甲基-2-噻唑基,5-乙基-2-噻唑基, 4,5-二甲基-2-噻唑基,4-乙基-5-甲基-2-噻唑基,5-乙基-4-甲基-2-噻唑基,2-苯并噻唑基,4,5,6,7-四氢-2- 苯并噻唑基,5,6-二氢-7H-噻喃并[4,3-d]噻唑-2-基,3-甲基-5-异噻唑基,1,3,4-噻二唑基,5-甲基-1,3,4-噻二唑基, 噻二唑-2-基或5-甲基-3-异恶唑基,以及与无机或有机碱形成的非毒性,药理学上可接受的盐; 化合物作为它们的盐作为板材粘合和聚集的抑制剂有用。

    Derivatives of 4-(4-biphenylyl)-butyric acid
    57.
    发明授权
    Derivatives of 4-(4-biphenylyl)-butyric acid 失效
    4-(4-联苯基) - 丁酸的衍生物

    公开(公告)号:US4021479A

    公开(公告)日:1977-05-03

    申请号:US406196

    申请日:1973-10-15

    摘要: Compounds of the formulas ##STR1## and ##STR2## wherein A is --CH.sub.2 -- or --CH(OH)--,R.sub.1 is hydrogen, halogen or, when R.sub.2 and R.sub.3 are other than both hydrogen, also methyl,R.sub.2 is hydrogen, halogen, cyano, nitro, amino or (alkanoyl of 1 to 4 carbon atoms)-amino,R.sub.3 is hydrogen or halogen,Provided, however, that at least one of R.sub.1, R.sub.2 and R.sub.3 is other than hydrogen, andR.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms, and non-toxic salts of the free acids (R.sub.4 = H) formed with inorganic or organic bases; the compounds as well as their salts are useful as antiphlogistics and antiproliferatives.

    摘要翻译: 其中A是-CH 2 - 或-CH(OH) - ,R 1是氢,卤素,或者当R 2和R 3不同于氢时,也是甲基,R 2是氢,卤素 ,氰基,硝基,氨基或(1至4个碳原子的烷酰基) - 氨基,R3是氢或卤素,提供,然而,至少一个R 1,R 2和R 3不是氢,并且R 4是氢或烷基 1至4个碳原子的无毒盐和无机或有机碱形成的游离酸(R4 = H)的无毒盐; 化合物及其盐可用作消炎剂和抗增殖剂。

    2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones
    60.
    发明授权
    2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones 失效
    2 - [(氨基) - 芳基 - 亚甲基] - 苯并[b]噻吩-3(2H) - 酮

    公开(公告)号:US4288437A

    公开(公告)日:1981-09-08

    申请号:US173173

    申请日:1980-07-28

    CPC分类号: C07D333/62 C07D333/64

    摘要: Compounds of the formula ##STR1## wherein Ar is phenyl; mono- or di-substituted phenyl, where the substituents are one to two halogens, one to two alkyls of 1 to 3 carbon atoms, or one amino, nitro, cyano or trifluoromethyl; or pyridinyl;R is hydrogen, chlorine, methyl or methoxy;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, methyl-(cycloalkyl of 3 to 8 carbon atoms) or --A--R.sub.4,where A is alkylene of 2 to 3 carbon atoms, and R.sub.4 is hydroxyl, methylamino, dimethylamino, N-methyl-ethylamino, diethylamino, pyrrolidino, piperidino, hexamethyleneimino, morpholino or 4-methyl-1-piperazinyl; orR.sub.1 and R.sub.2, together with each other and the nitrogen atom to which they are attached, form a 4- to 7-membered, saturated or mono-unsaturated, unsubstituted or substituted heterocycle which may contain nitrogen, oxygen, sulfur, sulfinyl or sulfonyl as additional ring members, where the substituents are alkyls of 1 to 3 carbon atoms.The compounds are useful as anticonvulsants.

    摘要翻译: 其中Ar是苯基的式IMAMA的化合物; 单取代或二取代的苯基,其中取代基是一至两个卤素,一至二个碳原子数为1至2个的烷基,或一个氨基,硝基,氰基或三氟甲基; 或吡啶基; R是氢,氯,甲基或甲氧基; R1是氢或甲基; R2是氢,1至6个碳原子的烷基,2至6个碳原子的烯基,2至6个碳原子的炔基,3至8个碳原子的环烷基,甲基 - 3至8个碳原子的环烷基或-A -R4,其中A为2至3个碳原子的亚烷基,R4为羟基,甲基氨基,二甲基氨基,N-甲基 - 乙基氨基,二乙基氨基,吡咯烷子基,哌啶子基,六亚甲基亚氨基,吗啉代或4-甲基-1-哌嗪基; 或R 1和R 2彼此连接并与它们相连的氮原子形成可含有氮,氧,硫,亚磺酰基或磺酰基的4-至7-元饱和或单不饱和的未被取代或取代的杂环 作为另外的环成员,其中取代基是1至3个碳原子的烷基。 该化合物可用作抗惊厥药。