首页> 外国专利> Compounds of piridilo Signalling Pathway inhibitors of Hedgehog (hh).

Compounds of piridilo Signalling Pathway inhibitors of Hedgehog (hh).

机译：刺猬（hh）的piridilo Signaling Pathway抑制剂化合物。

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Item 1: a compound of Formula 1, in which a is a thyroid cancer or heterosexual; X is a tar, nr4c (o),NR4C (S)N (C (O) R1) C (O)NR4SO NR4SO2 NR4C (O) NH NR4C (S) NH C (O) NR4 C (S) NR4 NR4PO o NR4PO (OH)Y is absent, CHR4, O, S, SO, SO2, or NR4; R1 is selected from the group consisting of alkyl, a carbocycle, or a heterocycle each of which is optionally substituted with hydroxyl, halogen, amino, carboxyl, amidino, guanidino, carbonyl, nitro, cyano, acyl, alkyl, haloalkyl, sulfonyl, sulfinyl, alkoxy, alkylthio, carbamoyl, acylamino, sulfamoyl, sulfonamide, a carbocycle, or a heterocycle; wherein said amino, amidino, alkyl, acyl, sulfonyl, sulfinyl, alkoxy, alkylthio, carbamoyl, acylamino, sulfamoyl, sulfonamide, carbocycle, and heterocycle is optionally substituted with, halogen, haloalkyl, hydroxyl, carboxyl, carbonyl, or an amino, alkyl, alkoxy,acyl, sulfonyl, sulfinyl, phosphinate, carbocycle, or heterocycle that is optionally substituted by hydroxyl, carboxyl, carbonyl, amino, halogen, haloalkyl, alkyl, alkoxy, alkylthio, sulfonyl, sulfinyl, acyl, a carbocycle, or a heterocycle; R2 is halogen, hydroxyl, alkyl, acyl, or alkoxy, where each alkyl, acyl, and alkoxy is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl, or alkoxy; R3 is halogen, hydroxyl, carboxyl, alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, a carbocycle or a heterocycle where each alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide,Sulfur, sulfonyl, thyroid and heterocycle can be selectively replaced by hydroxyl, halogenated, amino, nitro, tar, acid, ammonium sulfonyl or Alcoy; R4 is h or tar; m is 0-3; n is 0-3; salt and solution. Item 37: the process of manufacturing a compound of formula 2, in which the B-ring is a carbohydrate or heterocycle; R3 is halogenation, hydroxyl, carbohydrate, hydrocarbon, ACIO, alcoxi, alcoxibonilo, carbamoyilo, aculsulfuro, asphalt, asphalt, thyroid or a different cycle, in which each asphalt, ACIO, alcoxi, alcoxicarbonilo, Ammonium carbamate ammonium sulfite ammonium sulfitecarbocycle and heterocycle is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R6 in each case is independently hydroxyl, halogen, amino, carbonyl, nitro, cyano, acyl, alkyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, alkoxy, alkylcarbamoyl, alkanoylamine, alkylsulfamoyl, alkylsulfonamide, a carbocycle or a heterocycle; wherein said amino, alkyl, carbonyl, acyl, sulfonyl, alkylsulfonyl, alkylsulfinyl, alkoxy, alkylcarbamoyl, alkanoylamine, alkylsulfamoyl, alkylsulfonamide, carbocycle and heterocycle substituent is optionally substituted with amino, halogen, hydroxyl, carbonyl,Or a carbohydrate or non carbohydrate that can be selectively substituted with hydroxyl, amino, halogenated, halogenated, asphalt, tar, alcoxi or acilo; or 0-3; and m are 0-3; including the reaction to formula compound (3), wherein q is Ci, Br or I; formula compound (4) is br, I or other compound; and producing a compound 1. Formula (5);The formula compound (5) is reduced to a formula compound (6), and the formula compound (6) reacts with a formula compound (7), in which Q 'is a halide, or R is an active group; the formula compound 2 is produced.

机译：第1项：式1化合物，其中a为甲状腺癌或异性; X是焦油，nr4c（o），NR4C（S）N（C（O）R1）C（O）NR4SO NR4SO2 NR4C（O）NH NR4C（S）NH C（O）NR4 C（S）NR4 NR4PO o缺少NR4PO（OH）Y，CHR4，O，S，SO，SO2或NR4; R1选自烷基，碳环或杂环，它们各自任选地被羟基，卤素，氨基，羧基，a基，胍基，羰基，硝基，氰基，酰基，烷基，卤代烷基，磺酰基，亚磺酰基取代，烷氧基，烷硫基，氨基甲酰基，酰氨基，氨磺酰基，磺酰胺，碳环或杂环;其中所述氨基，a基，烷基，酰基，磺酰基，亚磺酰基，烷氧基，烷硫基，氨基甲酰基，酰基氨基，氨磺酰基，磺酰胺，碳环和杂环任选地被卤素，卤代烷基，羟基，羧基，羰基或氨基，烷基取代，烷氧基，酰基，磺酰基，亚磺酰基，次膦酸酯，碳环或杂环，其任选地被羟基，羧基，羰基，氨基，卤素，卤代烷基，烷基，烷氧基，烷硫基，磺酰基，亚磺酰基，酰基，碳环或杂环取代; R2是卤素，羟基，烷基，酰基或烷氧基，其中每个烷基，酰基和烷氧基任选地被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R 3是卤素，羟基，羧基，烷基，酰基，烷氧基，烷氧基羰基，氨基甲酰基，烷基硫化物，亚磺酰基，磺酰基，碳环或杂环，其中每个烷基，酰基，烷氧基，烷氧基羰基，氨基甲酰基，烷基硫化物，硫，磺酰基，甲状腺和杂环可以被羟基，卤代，氨基，硝基，焦油，酸，磺酰铵或铝制取代R4是h或tar; m为0-3; n为0-3;盐和溶液。第37项：制备式2化合物的方法，其中B环是碳水化合物或杂环; R3是卤代，羟基，碳水化合物，碳氢化合物，ACIO，阿尔克西，alcoxibonilo，氨甲酰氨基，aculsulfuro，沥青，沥青，甲状腺或不同的循环，其中每个沥青，ACIO，alcoxi，alcoxicarbonilo，氨基甲酸铵，亚硫酸铵，亚硫酸铵，亚硫酸铵碳环和杂环任选地被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R 6在每种情况下分别是羟基，卤素，氨基，羰基，硝基，氰基，酰基，烷基，磺酰基，烷基磺酰基，烷基亚磺酰基，烷氧基，烷基氨基甲酰基，烷酰基胺，烷基氨基磺酰基，烷基磺酰胺，碳环或杂环;其中所述氨基，烷基，羰基，酰基，磺酰基，烷基磺酰基，烷基亚磺酰基，烷氧基，烷基氨基甲酰基，烷酰基胺，烷基氨基磺酰基，烷基磺酰胺，碳环和杂环取代基任选地被氨基，卤素，羟基，羰基，或可被羟基，氨基，卤代，卤代，柏油，焦油，醇类或乙酰基选择性取代;或0-3;和m为0-3;包括与式化合物（3）的反应，其中q是Ci，Br或I;式（4）化合物为br，I或其他化合物;制备化合物1。式（5）;将式（5）还原为式（6），使式（6）与式（7）反应，其中Q′为卤化物，或R是一个活跃的基团;制备式化合物2。

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公开/公告号AR071319A1

专利类型
公开/公告日2010-06-09

原文格式PDF
申请/专利权人 GENENTECH INC.;CURIS INC;
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申请/专利号AR2009P101292
发明设计人
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申请日2009-04-13
分类号C07D213/40;C07D401/12;C07D401/14;C07D405/12;C07D409/12;C07D413/12;C07D417/12;A61K31/4402;A61K31/4427;A61P35/00;
国家 AR
入库时间 2022-08-21 18:47:31

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