2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and
salts thereof
    11.
    发明授权
    2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and salts thereof 失效
    2,5-二氢-1,2-噻嗪(5,6-b)吲哚-3-甲酰胺-1,1-二氧化物及其盐

    公开(公告)号:US4137313A

    公开(公告)日:1979-01-30

    申请号:US872889

    申请日:1978-01-27

    摘要: Compounds of the formula ##STR1## WHEREIN R.sub.1 is hydrogen, methyl or ethyl;R.sub.2 is methyl or ethyl;Y is hydrogen, fluorine, chlorine, bromine, methoxy, methyl, ethyl or trifluoromethyl; andAr is 2-thiazolyl which may have one or two methyl or ethyl substituents attached thereto; 5,6-dihydro-4H-cyclopentathiazol-2-yl; 4,5,6,7-tetrahydro-2-benzothiazolyl; 2-benzothiazolyl; 3-isothiazolyl which may have a methyl substituent attached thereto; 2-pyridyl which may have a methyl or hydroxyl substituent attached thereto; 3-pyridyl; 4-pyridyl; 4-pyrimidinyl; pyrazinyl; 2-benzimidazolyl; 2-oxazolyl which may have a methyl substituent attached thereto; 2-benzoxazolyl; or phenyl which may have a fluoro, chloro, bromo, methyl, ethyl, trifluoromethyl or methoxy substituent attached thereto; and non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antiphlogistics and blood platelet aggregation inhibitors.

    摘要翻译: 式中的化合物,其中R1是氢,甲基或乙基; R2是甲基或乙基; Y是氢,氟,氯,溴,甲氧基,甲基,乙基或三氟甲基; 并且Ar是可以具有一个或两个连接到其上的甲基或乙基取代基的2-噻唑基; 5,6-二氢-4H-环戊基噻唑-2-基; 4,5,6,7-四氢-2-苯并噻唑基; 2-苯并噻唑基 可具有与其连接的甲基取代基的3-异噻唑基; 可以具有连接到其上的甲基或羟基取代基的2-吡啶基; 3-吡啶基; 4-吡啶基; 4-嘧啶基; 吡嗪基 2-苯并咪唑基; 可具有与其连接的甲基取代基的2-恶唑基; 2-苯并恶唑基; 或可具有与其连接的氟,氯,溴,甲基,乙基,三氟甲基或甲氧基取代基的苯基; 和与无机或有机碱形成的无毒的,药学上可接受的盐。 化合物及其盐可用作消炎剂和血小板聚集抑制剂。

    4-Hydroxy-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and
salts thereof
    13.
    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。

    Process for the preparation of
4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide
    18.
    发明授权
    Process for the preparation of 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide 失效
    制备4-羟基-1,2-苯并异噻唑-3(2H) - 酮-1,1-二氧化物的方法

    公开(公告)号:US4626325A

    公开(公告)日:1986-12-02

    申请号:US841392

    申请日:1986-03-19

    IPC分类号: C07D275/06 C25B3/02 C25C3/00

    CPC分类号: C07D275/06 C25B3/02

    摘要: The specification describes a process for preparing 4-hydroxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide, a sweetener, from 1,2-benzisothiazol-3(2H)-one-1,1-dioxide by anodic oxidation in the presence of trifluoroacetic acid or trifluoromethanesulfonic acid and, optionally, in the presence of salts which increase the conductivity. The oxidation is effected in an anhydrous medium and the 4-trifluoroacetoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide formed as an intermediate when, for example, trifluoroacetic acid is used is decomposed with water to obtain the desired end product.

    摘要翻译: 该说明书描述了由1,2-苯并异噻唑-3(2H) - 酮-1,1(2H) - 酮-1,1-二氧化物制备4-羟基-1,2-苯并异噻唑-3(2H) - 酮-1,1-二氧化物 通过在三氟乙酸或三氟甲磺酸存在下阳极氧化和任选地在增加导电性的盐的存在下进行阳离子氧化。 氧化是在无水介质中进行的,当使用例如三氟乙酸时形成的作为中间体的4-三氟乙酰氧基-1,2-苯并异噻唑-3(2H) - 酮-1,1-二氧化物用水分解 获得所需的最终产品。

    Condensed diazepinones and medicaments containing these compounds
    19.
    发明授权
    Condensed diazepinones and medicaments containing these compounds 失效
    浓缩二氮杂酮和含有这些化合物的药物

    公开(公告)号:US5179090A

    公开(公告)日:1993-01-12

    申请号:US779203

    申请日:1991-10-18

    IPC分类号: C07D487/18 C07D519/00

    CPC分类号: C07D487/18 C07D519/00

    摘要: Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.4 together represent an ethylene bridge,are suitable for the treatment of cholinergically induced spasms and motility disorders of the gastrointestinal tract and in the region of the evacuating bile ducts, for the symptomatic treatment of cystitis and of spasms from urelithiasis, for the treatment of relative incontinence, for the symptomatic treatment of bronchial asthma and bronchitis, and for the treatment of ischaemic heart diseases. The compounds are characterized by good selectivity.

    摘要翻译: (I)其中] + E,crc / B /表示二价基团之一的通式I的缩二氮杂酮类(I)其中一个二价基团(S)(T) V)X是= CH-基或氮原子,R表示低级烷基,其可以任选地被任选地带有卤素,甲基或甲氧基的苯基进一步取代,R4和R5代表氢,卤素或低级烷基,R6 是氢,氯或甲基,R7和R8表示低级烷基,R8还另外表示卤素,m,n,o和p表示数字0,1,2或3,具有以下限制:m + n和 o + p的和表示数字1,2或3,n + o和m + p之和各自表示数字1,2,3,4或5,其中,然而, m + n + o + p必须始终大于2,A1,A2,A3和A4表示氢,或者对于m,n,o和p分别表示数字1,A1和A2一起或A3 和A4一起代表乙烯桥,适合于处理o f胆碱能诱发胃肠道的痉挛和运动障碍以及排空胆管区域,用于膀胱炎和尿毒症痉挛的症状治疗,用于治疗相对失禁,用于支气管哮喘和支气管炎的症状治疗, 并用于治疗缺血性心脏病。 该化合物的特征在于良好的选择性。