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首页> 外国专利> Benzo de isoquinolin-1,3 - dionas replaced, a procedure for the preparation, Pharmaceutical compositions containing them, a method for Controlling the thrombotic Disorders which employs,A method to induce an anti Adhesive effect on blood platelets using benzo de I

Benzo de isoquinolin-1,3 - dionas replaced, a procedure for the preparation, Pharmaceutical compositions containing them, a method for Controlling the thrombotic Disorders which employs,A method to induce an anti Adhesive effect on blood platelets using benzo de I

机译：替换了苯并[de]异喹啉-1,3-二氧萘醌的制备方法，包含它们的药物组合物，采用的控制血栓性疾病的方法，使用苯并[de]诱导对血小板的抗粘连作用的方法一世

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摘要

Benzo [de] isoquinolin-1,3-diones substituted, of formula (1) where R represents H, A or CH2-Ph, R1 represents ûHet, -N - [(CH2) s-OH] 2, -N- [(CH2) s-OA] 2, -NA- (CH2) s-Ar, -NA- (CH2) m-R5, -Y- (CH2) m-R5, -Y- (CH2) 2-NHA, -Y- (CH2) 2-NH- (CH2) s-OH, -Y- (CH2) 2-NA2, -Y- (CH2) m-OH, -Y- (CH2) n- (CHR4) -R3 , -Y- (CH2) n-R4, R4, -Y- (CH2) n-Het- (CH2) or -R6, -Y- (CH2) n-Ar '- (CH2) o-R6, -Het û (CH2) n-Ar, Het-Het, -Y- (CH2) s-Ar 'û (CH2) or -R11, -Y- [XO] t- [X1-O] u-X2-R5 oY- (CH2) n-NA- (CH2) o-R5, R2 represents H, OH, OA, COOH, COOA, CH (Ph) -Ph, Ar, Het1, R5, R7 or R8, R3 represents CH3, R4 represents ûCH = CH2, -Ar, COOA, COOH, of formula (2) or (3),R5 represents NH2, NHA, NA2, NHAr, -NH- (CH2) n-OH or ûNH- (CH2) n-OA, R6 represents H or R5, R7 represents ûAr '- (CH2) n-R8 or ûAr'- (CH2) n-R5, R8 represents CONH2, CONHA, CONA2, CONH- (CH2) or -Ar, CONH- (CH2) or-Het, CONH- (CH2) or-R5, CONH- (CH2) or -CH (Ar1) -Ar2, CONH- (CH2) or - (CH (A) -Ph, CONH- (CH2) o-Ar 'û NH-CO-Ar, CONH-Ar' ûHet or CHA-CONH2, R11 represents ûNH - (C = NH) -NH2, NH- (C = NH) -NHA, -NH- (C = NH) -NA2, -NA- (C = NH) -NH2, NA- (C = NH) -NHA or û NA- (C = NH) -NA2, Ar 'represents phenylene, cycloalkylene or biphenylene, which may be unsubstituted or mono or disubstituted with A, OH, OA, Hal, CN, NH2, NHA, NA2, NO2, CF3, CO-A, SO2NH2, SO2NAH, SO2NA2, Ar represents phenyl, cycloalkyl, naphthyl, cyclohex-1-enyl,Biphenyls, bicycloxilo, 4-cyclohexil-fenilo, benzo [1.3] dioxol-5-ilo or indanyl, not substituted or only substituted with a, oh, OA, o-ph, o-ch2-ph, o-ph-ch3, O (cycloquilo),Hal, CN, NH2, Nha, Nha, Na2, nh-c (o) a, (CH2) n-nh2, (CH2) n-na2, NO2, CF3, C (o) a, so2-ph, so2nh2, so2nah, so2na2, so2na-ph, AR1 and ar2 independently represent phenyl, het represents a mono or Bi periodic, partially or completely saturated, ring 5 to 10 members, It may contain one or two N atoms and / or one or two O atoms, and may be inconsistent with CN, Hal, oh, OA, CF3, a, NO2, Co, Co, Co-A or R5. Het1 represents a heterocycle or single cycle or double cycle partial unsaturated ring with 5 to 10 members, It may contain one or two n's and / or one or two o's and / or it may be a monkey or with Hal, oh, OA,A represents C1-6 straight or branched chain alkyl, Hal represents F, Cl, Br or I, X, X1, X2 independently represents alkylene of 1 to 12 C atoms, Y represents O, S or NH, i is 1 , 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12, m is 3, 4, 5, 6, 7, 8, 9, 10, 11, or 12, n, or are independently 0, 1, 2, 3 or 4, s is 1, 2, 3, or 4, t is 0, 1 or 2, u is 1 or 2, considering that when R2 represents Ar or H,R1 does not represent acceptable salts and solutions for formula (4) and its drugs. A procedure for the preparation of a formula compound (I), wherein a formula compound (1) is released from a functional derivative thereof by treatment with a solvent or hydrogenolysis agent, or (b) reacts with a formula compound (5), wherein R9 represents Cl, Br, No2or1 and R1 have the meaning set forth in Labor Law No. 1 and contain a formula compound: H2n - (CHr) i-r2, where R, R2 and I have the meaning set forth in Labor Law No. 1 and, if necessary,The remaining R9 is converted to R1 (c) and the remaining R1 or (c) reacts with a formula compound (6), wherein R9 represents Cl, Br, NO2, or R1 and R1, with the same meaning as requirement (1),Contains a formula compound: L - (CHr) i-r2, where l represents Cl, Br or I, Oh or reactive and sterile OH group, and R, R2 and I have the meaning referred to in claim 1 and, if necessary, convert the remaining R9 to R1, or (d) convert the remaining R and / or R2 and / or R9 to another R and / or R2 and / or R9, for example, A group of amino acids will be converted into a group of Guardin through contact with amitriptyl agent to react with bromination or hydrogen iodide. Through the docking of Suzuki and boricos acid, corresponding coupling products will be obtained, reducing a nitro group, a hydrogen sulfide group or a hydrogen sulfide group,By disinfecting the OH group or separating ether from the OA group, leasing a major or minor aminobenzene group, partially or completely hydrogenating with a CN group, separating an ester group or disinfecting the remaining anthrax acid, or nuclear or electrical substitution, Y / O (E) is converted into a formula group or acid (1) as one of its salts or solutions. 1. Containing at least an effective amount of a formula compound (1) or a salt thereof or a physiologically acceptable solution thereof, and effectively resisting the pharmaceutical composition of glycol acetone,Especially for the control of thrombus disorder and its consequences. These sequelae include myocardial infarction, arteriosclerosis, chest colic, acute coronary syndrome, peripheral circulatory disorders, stroke, transitional ischemic anemia, angioplasty or post implantation reintegration or recovery of health.
机译：式（1）的取代的苯并[de]异喹啉-1,3-二酮被取代，其中R代表H，A或CH2-Ph，R1代表ûHet，-N-[（CH2）s-OH] 2 --N- [ （CH 2）s-OA] 2，-NA-（CH 2）s-Ar，-NA-（CH 2）m-R 5，-Y-（CH 2）m-R 5，-Y-（CH 2）2-NHA，- Y-（CH2）2-NH-（CH2）s-OH，-Y-（CH2）2-NA2，-Y-（CH2）m-OH，-Y-（CH2）n-（CHR4）-R3， -Y-（CH2）n-R4，R4，-Y-（CH2）n-Het-（CH2）或-R6，-Y-（CH2）n-Ar'-（CH2）o-R6，-Hetû （CH2）n-Ar，Het-Het，-Y-（CH2）s-Ar'û（CH2）或-R11，-Y- [XO] t- [X1-O] u-X2-R5 oY-（ CH2）n-NA-（CH2）o-R5，R2代表H，OH，OA，COOH，COOA，CH（Ph）-Ph，Ar，Het1，R5，R7或R8，R3代表CH3，R4代表ûCH=式（2）或（3）的CH2，-Ar，COOA，COOH，R5代表NH2，NHA，NA2，NHAr，-NH-（CH2）n-OH或NH-（CH2）n-OA，R6代表在H或R5中，R7代表ûAr'-（CH2）n-R8或ûAr'-（CH2）n-R5，R8代表CONH2，CONHA，CONA2，CONH-（CH2）或-Ar，CONH-（CH2）或- Het，CONH-（CH2）或-R5，CONH-（CH2）或-CH（Ar1）-Ar2，CONH-（CH2）或-（CH（A）-Ph，CONH-（CH2）o-Ar'û NH-CO-Ar，CO NH-Ar'ûHet或CHA-CONH2，R11代表ûNH-（C = NH）-NH2，NH-（C = NH）-NHA，-NH-（C = NH）-NA2，-NA-（C = NH ）-NH 2，NA-（C = NH）-NHA或-NA-（C = NH）-NA 2，Ar'表示亚苯基，亚环烷基或亚联苯基，它们可以是未取代的或被A，OH，OA，Hal单取代或二取代的，CN，NH 2，NHA，NA 2，NO 2，CF 3，CO-A，SO 2 NH 2，SO 2 NAH，SO 2 NA 2，Ar代表苯基，环烷基，萘基，环己-1-烯基，联苯，双环己基，4-环己基-苯胺基，苯并[1.3 ] dioxol-5-ilo或茚满基，未被取代或仅被a，oh，OA，o-ph，o-ch2-ph，o-ph-ch3，O（cycloquilo），Hal，CN，NH2，Nha， Nha，Na2，nh-c（o）a，（CH2）n-nh2，（CH2）n-na2，NO2，CF3，C（o）a，so2-ph，so2nh2，so2nah，so2na2，so2na-ph， AR1和ar2独立地代表苯基，het代表一个5到10个环的单或Bi周期性，部分或完全饱和的环，它可以包含一个或两个N原子和/或一个或两个O原子，并且可能与CN不一致， Hal，哦，OA，CF3，a，NO2，Co，Co，Co-A或R5。 Het1表示具有5至10个成员的杂环或单环或双环部分不饱和环，它可以包含一个或两个n和/或一个或两个o和/或它可以是猴子或带有Hal，哦，OA，A表示C1-6直链或支链烷基，Hal表示F，Cl，Br或I，X，X1，X2独立表示1至12个碳原子的亚烷基，Y表示O，S或NH，i为1,2,3 ，4、5、6、7、8、9、10、11或12，m为3、4、5、6、7、8、9、10、11或12，n或独立为0， 1，2，3或4，s为1，2，3或4，t为0，1或2，u为1或2，考虑到当R2代表Ar或H时，R1不代表可接受的盐和溶液用于式（4）及其药物。制备式化合物（I）的方法，其中式化合物（1）通过用溶剂或氢解剂处理而从其功能性衍生物中释放，或（b）与式化合物（5）反应，其中R 9表示Cl，Br，No2or1和R1具有《劳动法》第1号中规定的含义，并包含式化合物：H2n-（CHr）i-r2，其中R，R2和I具有《劳动法》第1号中规定的含义。在必要时，将剩余的R9转化为R1（c），剩余的R1或（c）与式化合物（6）反应，其中R9代表Cl，Br，NO2或R1和R1，其中与要求（1）的含义相同，包含一个通式化合物：L-（CHr）i-r2，其中l表示Cl，Br或I，Oh或反应性和无菌OH基，R，R2和I的含义与权利要求1中的化合物，并且如果需要，将剩余的R9转化为R1，或者（d）将剩余的R和/或R2和/或R9转化为另一个R和/或R2和/或R9，例如，酸通过与阿米替林试剂接触而与溴化或碘化​​氢反应，可将其转化为一组Guardin。通过铃木和硼酸的对接，可以获得相应的偶联产物，还原硝基，硫化氢或硫化氢基团;通过消毒OH基团或从OA基团中分离醚，出租主要或次要氨基苯Y / O（E）被CN基团部分或完全加氢，分离一个酯基团或对残留的炭疽酸进行消毒或核取代或​​电取代后，被转化为式组或酸（1），为其盐之一或解决方案。 1.至少包含有效量的式化合物（1）或其盐或其生理学上可接受的溶液，并且有效地抵抗乙二醇丙酮的药物组合物，特别是用于控制血栓疾病及其后果。这些后遗症包括心肌梗塞，动脉硬化，胸绞痛，急性冠状动脉综合症，周围循环系统疾病，中风，过渡性缺血性贫血，血管成形术或植入后再整合或健康恢复。

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