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    • 1. 发明授权
    • 2,5-Dihydro-1,2-thiazino(5,6-b)indole-3-carboxamide-1,1-dioxides and
salts thereof
    • 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
    • US4137313A
    • 1979-01-30
    • US872889
    • 1978-01-27
    • Gunter TrummlitzWolfhard EngelErnst SeegerWalter HaarmannGunther Engelhardt
    • Gunter TrummlitzWolfhard EngelErnst SeegerWalter HaarmannGunther Engelhardt
    • A61K31/54A61P7/02A61P29/00C07D209/42C07D513/04C07D513/14A61K31/38
    • C07D513/04C07D209/42C07D513/14Y10S514/822
    • 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.
    • 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。
    • 5. 发明授权
    • 4-Hydroxy-2H-naphtho[2,1-e]-1,2-thiazine-3-carboxamide-1,1-dioxides and
salts thereof
    • 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
    • US3992535A
    • 1976-11-16
    • US626623
    • 1975-10-29
    • Gunter TrummlitzHelmut TeufelWolfhard EngelErnst SeegerWalter HaarmannGunther Engelhardt
    • Gunter TrummlitzHelmut TeufelWolfhard EngelErnst SeegerWalter HaarmannGunther Engelhardt
    • C07D275/06C07D279/02C07D417/12C07D513/04A61K31/54
    • C07D275/06C07D279/02
    • 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.
    • 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。
    • 10. 发明授权
    • 2-[(Amino)-aryl-methylene]-benzo[b]thiophen-3(2H)-ones
    • 2 - [(氨基) - 芳基 - 亚甲基] - 苯并[b]噻吩-3(2H) - 酮
    • US4288437A
    • 1981-09-08
    • US173173
    • 1980-07-28
    • Wolfhard EngelGunter TrummlitzErnst SeegerJoachim Kahling
    • Wolfhard EngelGunter TrummlitzErnst SeegerJoachim Kahling
    • A61K31/38A61K31/381A61K31/44A61K31/4433A61K31/445A61K31/495A61K31/535A61P25/08C07D333/62C07D333/64C07D409/06
    • C07D333/62C07D333/64
    • 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.
    • 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。