首页> 外国专利> Pirido compounds pirido - pyrrolo 3,2-g - and pirrolo 3,4 indole and pirido - pyrrolo 2,3 pirrolo 3,4-c carbazole, a process for their preparation, Pharmaceutical compositions containing compounds and Intermediates

Pirido compounds pirido - pyrrolo 3,2-g - and pirrolo 3,4 indole and pirido - pyrrolo 2,3 pirrolo 3,4-c carbazole, a process for their preparation, Pharmaceutical compositions containing compounds and Intermediates

机译:Pirido化合物pirido-pyrrolo [3,2-g]-和pirrolo [3,4]吲哚和pirido-pyrrolo [2,3] pirrolo [3,4-c]咔唑,其制备方法,含有化合物的药物组合物和中间体

摘要

Pyrido-pyrido-pyrrolo [3,2-g] pyrrolo [3,4-e] indole and pyrido-pyrrolo [2,3-a] pyrrolo [3,4-c] carbazole compounds of formula (1) in which : W1, W2 each represent, with the carbon atoms to which they are attached, a phenyl group or a pyridyl group; at least one of the groups W1 or W2 is understood to represent an identical or different pyridyl group, R1, R2, independently of each other,They represent a set of U-V formulas, where u represents a simple link or a C1-6 linear or branched asphalt chain, optionally replaced by one or more groups,Same or different, from halogen to hydrogen Xi, and / or optionally containing one or more unsaturated; V represents a group selected between hydrogen atom, halogen, cyanogen, nitrogen, azido, C1-6 linear tar or branched substance, arilo, C1-6 arilalquilo (wherein the tar part can be linear or branched substance).Hydroxy, alcoxi C1-6 linear or branched, ariloxi, arilalcoxi C1-6 (where alcoxi may be linear or branched);formyl, carboxy, aminocarbonyl, groups NR6R7, -C (O) -T1, -C (O) -NR6-T1, -NR6-C (O) -T1, -OC (O) -T1, -C (O) -O-T1, -O-T2-NR6R7, -O-T2-OR6, -O-T2-CO2R6, -NR6-T2-NR6R7, -NR6-T2-OR6, -NR6-T2-CO2R6 and -S ( O) t-R6, in which: R6 and R7, which may be the same or different, each represent a group selected from a hydrogen atom, a linear or branched C1-6 alkyl group, aryl and arylalkyl groups C1- 6 (in which the alkyl part can be linear or branched),O R6 + R7 and nitrogen atoms together form a single cycle or two cycle saturated heterocycle composed of 5 to 10 atoms. In the cycle system, the second selected abiotic atom is selectively contained. The choice between oxygen and nitrogen can be made by a group of C1-6 linear tar or 1. Branching, arilo, arilalquilo (C1-6), wherein the asphalt part is linear or branched, water Xi, alcoxi C1-6 linear or branched, ammonia water, monomer C1-6 linear or branched rented, and C1-6 cumin, each part of which can be linear or branched; T1 represents a group of C1-6 linear or branched asphalt, arilo,1. C-6 type arilalquilo C1-6, wherein the tar part is a linear or separated daughter, and a C1-6 type linear or separated daughter tar chain is selected from a group of substances selected from - or6, nr6r7, co2r6, C (o) R6 and C (o) nr6r7, wherein R6 and R7 are the substances defined above, And a linear or branched alquenileno c2-6 chain, replaced by a group of members selected from - or6, nr6r7, co2r6, C (o) R6 and - C (o) nr6r7, wherein R6 and R7 are the categories defined above; T 2 represents a linear or branched C1-6 asphalt chain; t represents an integer containing 0 to 2; R3 represents a group. Selected from the hydrogen atom1. C1-6 linear or branched C1-6 asphalt, arilo, arilalquilo C1-6 (wherein the asphalt part can be linear or branched);Cyclomethyldichloro, cyclomethylclara C1-6 (wherein the pitch part can be linear or branched),-Or6-nr6r7-o-t2-nr6r7-nr6-t2-nr6r7-nr6-t2-nr6r7, C1-6 oxyhydrogen tequila1. Di (hydroxy) C1-6 (each asphalt part can be linear or branched);-C (O) R6, -NH-C (O) R6, and a linear or branched C1-6 alkylene chain, substituted by one or more groups, identical or different, selected from halogen atoms, cyano, nitro groups, - OR6, -NR6R7, -CO2R6, -C (O) R6, linear or branched hydroxyalkylamino C1-6, di (hydroxyalkyl) amino C1-6 (in which each alkyl part can be linear or branched) and -C (O) -NHR6; groups R6, R7 and T2 have the same meanings as above; X represents a group selected from a hydrogen atom, and hydroxy, linear or branched C 1-6 alkoxy, mercapto and linear or branched C 1-6 alkylthio groups; Y represents a hydrogen atom, or X and Y form together,The carbon atom containing carbon atom is a group of carbon or sulfur carbides; X1 represents a group selected from the hydrogen atom, a group of hydrogen Xi, a linear or branched type of hydrogen oxygen C1-6, business opportunities and C1-6 linear or branched tar; Y1 represents a hydrogen atom, or X1 and Y1 are combined with carbon atoms. Carbon or sulfur carbide group; Q1 and Q2 represent hydrogen atom or Q1 and Q2, forming aromatic link with carbon atom carried by them; R4 represents a formula group (2),Among them: RA, Rb and RC, which may be the same or different, independent of each other,They represent a hydrogen atom, a halogen atom, a water Xi group, a C1-6 linear or separator group, ariloxi, arilalcoxi C1-6 (where the alcoxi part is linear or separator).1. C1-6 linear or branched tar, arilalquilo C1-6 (in which the tar part is linear or branched);Arilo, - nr6r7 (where R6 and R7 are the two types defined above),Azido, - n = N6 (where R6 is the above definition),Y-o-c (o) - R8, wherein R8 represents a linear or branched C1-6 hydrocarbon group (optionally replaced by one or more groups selected from halogen, hydroxyl, ammonia, C1-6 linear or branched lease and c1-6-6 diallamine), and each part can be linear or branched.Arilo, C1-6 arilalquilo (in which the tar part is linear or branched);Cyclopentadiene, or isocyclopropylene; RD represents a formaldehyde group or a u1-ra formula group, in which U1 represents a simple bond or more than one defined toluene and RA group; n is 0 or 1; R5 represents a group selected in the hydrogen atom, a C1-6 linear tar group or a branch group, C1-6 arilalquilo (in which the tar part is linear or branched);1. Arilsulfonilo, C1-6 are linear or branch C1-6 - and - C (o) - R6 (where R6 has the same meaning as above) or R4 and R5 jointly represent R4 and R5, provided that Q1 and Q2 together form an aromatic link, i.e. a set of formulas (3),Among them, carbon atom 1 is connected with nitrogen atom (a) in the cycle, and carbon atom 2 is connected with nitrogen atom (b) in the cycle;RA, Rb, RC and RD are defined as above; n is 0 or 1; its corresponding isomer and non corresponding isomer, and its added salt containing acid or acceptable basis of drug; arilo refers to a group of phenyl, northwest African, dihydrofluoroalkyl, tetrahydrofluoroalkyl, indenil or ind Nile River, Each group is replaced by one or more same or different groups selected from halogen, C1-6 linear tar or branch, C1-6 linear trihalotar or branch, hydroxyl, alcoxi C1-6 linear or branch.In addition, 1 or 2 groups of C1-6 linear tar or branched substance were selected to replace ammonia water. 1. Drug preparation procedures containing these substances and intermediates. Formula compounds (1) are useful as drugs. They are especially anti-tumor, so they are useful in the treatment of cancer.
机译:式(1)的吡咯并吡啶并吡咯并[3,2-g]吡咯并[3,4-e]吲哚和吡咯并吡咯并[2,3-a]吡咯并[3,4-c]咔唑化合物,其中: W1,W2分别以其所连接的碳原子表示苯基或吡啶基。 W 1或W 2基团中的至少一个被理解为彼此独立地表示相同或不同的吡啶基基团R 1,R 2。它们表示一组UV式,其中u表示简单连接或C 1-6线性或任选地被卤素至氢X 1相同或不同的一个或多个基团取代的支化沥青链,和/或任选地包含一种或多种不饱和基团; V代表选自氢原子,卤素,氰,氮,叠氮基,C 1-6线性焦油或支链物质,芳基,C 1-6芳基喹啉(其中焦油部分可以是直链或支链的物质)中的基团。 6个直链或支链的阿里洛西,阿里拉尔考昔C1-6(其中阿克洛西可以是直链或支链的);甲酰基,羧基,氨基羰基,基团NR6R7,-C(O)-T1,-C(O)-NR6-T1,-NR6 -C(O)-T1,-OC(O)-T1,-C(O)-O-T1,-O-T2-NR6R7,-O-T2-OR6,-O-T2-CO2R6,-NR6- T2-NR6R7,-NR6-T2-OR6,-NR6-T2-CO2R6和-S(O)t-R6,其中:R6和R7可以相同或不同,分别代表选自氢的基团原子,直链或支链的C 1-6烷基,芳基和芳烷基C 1-6(其中烷基部分可以是直链或支链的),O R6 + R7和氮原子一起形成一个单环或两个环的饱和杂环5至10个原子。在循环系统中,第二选择的非生物原子被选择性地包含。氧和氮的选择可以通过C1-6线性焦油或1的一组来进行。支链,芳基,芳烃(C1-6)(其中沥青部分为线性或支链),水Xi,醇C1-6线性或支链氨水,直链或支链的单体C1-6和C1-6孜然,其每部分可以是直链或支链的; T1代表一组C1-6线性或支链沥青arilo,1。 C-6型阿里洛基洛C1-6,其中焦油部分是直链或分离的子焦油链,C1-6型直链或分离的子焦油链选自-或6,nr6r7,co2r6,C( o)R6和C(o)nr6r7,其中R6和R7是上面定义的物质,以及直链或支链的alquenileno c2-6链,被选自-或or6,nr6r7,co2r6,C(o)的成员取代R6和-C(o)nr6r7,其中R6和R7是上面定义的类别; T 2表示直链或支链的C1-6沥青链; t表示一个包含0到2的整数; R 3代表一个基团。选自氢原子1。 C1-6直链或支链的C1-6沥青,芳基,芳烃基C1-6(其中沥青部分可以是直链或支链的);环甲基二氯,环甲基克拉C1-6(其中沥青部分可以是直链或支链的),-Or6- nr6r7-o-t2-nr6r7-nr6-t2-nr6r7-nr6-t2-nr6r7,C1-6氢氧龙舌兰酒。双(羟基)C1-6(每个沥青部分可以是直链或支链的);-C(O)R6,-NH-C(O)R6和直链或支链的C1-6亚烷基链,被一个或多个取代选自卤素原子,氰基,硝基,-OR6,-NR6R7,-CO2R6,-C(O)R6,直链或支链羟烷基氨基C1-6,二(羟烷基)氨基C1-6的相同或不同的基团其中每个烷基部分可以是直链或支链的)和-C(O)-NHR6;基团R6,R7和T2具有与上述相同的含义; X代表选自氢原子的基团,以及羟基,直链或支链的C 1-6烷氧基,巯基和直链或支链的C 1-6烷硫基; Y代表氢原子,或X和Y一起形成。含碳原子的碳原子是碳或碳化硫的基团; X 1代表选自氢原子的基团,氢X i的基团,直链或支链型氢氧C 1-6,商机和C 1-6直链或支链焦油; Y 1表示氢原子,或X 1和Y 1与碳原子结合。碳或碳化硫基团; Q1和Q2代表氢原子或Q1和Q2,与它们所携带的碳原子形成芳族键; R 4代表式(2),其中:RA,Rb和RC可以相同或不同,彼此独立。它们分别代表氢原子,卤素原子,水Xi基,C1-6线性或分离基团,ariloxi,Ari​​lalcoxi C1-6(其中alcoxi部分为线性或分离基)1。 C 1-6线性或支链焦油,阿里洛奎洛C 1-6(其中焦油部分为线性或支链);阿里洛--nr6r7(其中R6和R7是上面定义的两种类型),叠氮基,-n = N6(其中R6是上面的定义),Yoc(o)-R8,其中R8代表直链或支链的C1-6烃基团(任选地被一个或多个选自卤素,羟基,氨,C1-6直链或支链和C1的基团取代) -6-6二环胺),每个部分可以是直链或支链的.Arilo,C1-6阿里拉基洛(焦油部分是直链或支链的);环戊二烯或异环丙烯; RD表示甲醛基团或u1-ra式基团,其中U1表示单键或多个定义的甲苯和RA基团; n为0或1; R5代表选自氢原子的基团,C1-6直链的焦油基团或支链基团,C1-6芳烃基(其中焦油部分是直链或支链的); 1。 Arilsulfonilo,C1-6为直链或支链C1-6-和-C(o)-R6(其中R6与上述含义相同)或R4和R5共同代表R4和R5,条件是Q1和Q2共同形成芳族基连接,即一组式(3),其中,碳原子1在循环中与氮原子(a)相连,碳原子2在循环中与氮原子(b)相连; RA,Rb,RC和RD如上定义; n为0或1;其相应的异构体和非相应的异构体,及其加成的含酸或药物可接受的盐; arilo是指一组苯基,西北非洲,二氢氟烷基,四氢氟烷基,茚基或ind尼罗河,每个基团均被一个或多个相同或不同的基团取代,这些基团选自卤素,C1-6线性焦油或分支,C1-6线性三卤代另外,还选择了1或2组C1-6线性焦油或支链物质来代替氨水。 1.包含这些物质和中间体的药物制备程序。式化合物(1)可用作药物。它们尤其抗肿瘤,因此可用于治疗癌症。

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