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Aminotiofeno compounds (espirociclilamido)

机译:氨基噻吩化合物(espirociclilamido)

摘要

Aminoethylamine compounds (Spirulina) are effective tools for the treatment of tumors and cancers, such as mastitis / breast cancer, gastrointestinal estrogen tumor (GIST),Bacterial tumor, small cell lung cancer (SCLC),Acellular lymphoma NK / T cell, testicular cancer (half cell cancer)Thyroid cancer, malignant melanoma, ovarian cancer, adenosine chemical cancer, acute poliomyelitis (AML),Pediatric T-cell neurocytoma with breast cancer and acute lymphocytic leukemia Mastitis, leukaemia, hemangioma, large cell lymphoma, uterine cancer and prostate cancer. Item 1: the compound represented by formula (1), or the salt or positive oxidant acceptable from the formula, in the formula: and it is isomerized or cyclochloro 3-10 tar, any of which can be replaced by an independent R5 substitute of 1-5; X is isomerized or acylated, Any of them can choose to use 1-5 independent R21 substitutes, namely arilo, heteromorphic, cyclochloro 3-10oquilo, isocyclopropylene,cicloC3-10alquenilo o heterocicloalquenilo cada uno de los cuales est opcionalmente sustituido con 1-5 sustituyentes R3 independientes R1 es C0-6alquilo halogeno o haloalquilo R2 R21 y R3 son cada uno independientemente cicloC3-10alquilo oxo halogeno haloalquilo C0-6alquilo cianoC0-6alquilo nitroC0- -N (C0-6alquil) -N (C0-6alquil) (C0-6alquil)N (C0-6alquil) -N (C0-6alquil) (acil)acylC0-6alkyl, substituted acyl, guanidinoC0-6alkyl, hydroxyiminoC0-6alkyl, acylaminoC0-6alkyl, substituted acylamino, acyloxyC0-6alkyl, substituted acyloxy, arC0-6alkyl, arC0-6alkyl substituted, heteroalkylC6- heteroalkylC6-6alkylC6-6alkylC6-6alkyl-heteroalkylC6-alkylC6 , cianoaminoC0-6alquilo, C0-6alquilhidrazino, heterocyclic, arC0-6alquilhidrazino, alquilsulfonilC0- 6alquilo, arC0-6alquilsulfonilC0-6alquilo, alquilsulfinilC0-6alquilo, alquilsulfonamidoC0-6alquilo, arC0-6alquilsulfonamidoC0-6alquilo, aminoC0-6alquilsulfonilo, C0-6alquilaminosulfonilo, acilC1-6alquilsulfonilo , heterocyclylsulfonyl, aminoC0-6alkylsulfinyl, acylC1-6alkylsulfinyl, silyl, siloxy,alkenoxy, alkynoxy, C2-6alkenyl, acilC2-6alquenilo, C2-6, acilC2-6alquinilo, hidroxiC2-6alquinilo, aminoC2-6alquinilo, C1-6alcoxiC0-6alquilo, C1-6alquiltioC0-6alquilo, hidroxiC1- 6alcoxiC0-6alquilo, hidroxiC1-6alquiltioC0- 6alquilo, acilC1-6alcoxiC06alquilo, acilC1-6alquiltioC0-6alquilo, C0-6alquilaminoC1-6alcoxiC0-6alquilo, C0-6alquilaminoC1-6alquiltioC0-6alquilo, acilaminoC1-6alcoxiC0-6alquilo, acilaminoC1-6alquiltioC0- 6alquilo, arC0-6alquilaminoC0-6alquilo, arC0-6alquiltioC0- 6alkyl, arC0-6alkoxyC0-6alkyl, arC0-6alkylamino, arC0-6alkylaminoC0-6alkyl, arC0-6alkylthio, arC0-6alkoxy substituted, arC0-6alkylthio substituted, or arC0-6alkoxy substituted;y siempre que el compuesto no sea cis-N- (4-metil-5-oxo-1 4-diazaespiro 5 5 undec-9-il) -3- (quinolin-4-ilmetil) amino tiofeno-2-carboxamida cis- 2-1,2-chlorodi-hydrogen-fluorine] - fluorine [1] - fluorine] - spirit] - 1 - [1 - [1]]]]]]] - 1 - [1]] - key.
机译:氨基乙胺化合物(螺旋藻)是治疗肿瘤和癌症的有效工具,例如乳腺炎/乳腺癌,胃肠道雌激素瘤(GIST),细菌性肿瘤,小细胞肺癌(SCLC),无细胞淋巴瘤NK / T细胞,睾丸癌(半细胞癌)甲状腺癌,恶性黑色素瘤,卵巢癌,腺苷化学癌,急性脊髓灰质炎(AML),小儿T细胞神经细胞瘤伴乳腺癌和急性淋巴细胞白血病乳腺炎,白血病,血管瘤,大细胞淋巴瘤,子宫癌和前列腺癌癌症。第1项:式中由式(1)表示的化合物或该式可接受的盐或正氧化剂:并且它是异构化的或环氯的3-10焦油,其中任何一个都可以被一个独立的R5取代基取代1-5; X是异构的或酰化的,它们中的任何一个都可以选择使用1-5个独立的R21取代基,分别是arilo,杂晶,环氯3-10oquilo,异环丙烯,cicloC3-10 alquenilo o异cicloalquenilo cada uno de los cuales est opcionalmente sustituido con 1-5 ustustyentes R3独立R1和C0-6卤代卤素或卤代alquilo R2 R21和R3子cada uno独立性cicloC3-10alquilo氧代卤素卤代卤代alquilo C0-6alquilo钢琴C0-6alquilo nitroC0- -N(C0-6alquil)-N(C0-6al) N(C0-6烷基)-N(C0-6烷基)(芳基)酰基C0-6烷基,取代的酰基,胍基C0-6烷基,羟基亚氨基C0-6烷基,酰基氨基C0-6烷基,取代的酰基氨基,酰氧基C0-6烷基,取代的酰氧基,arC0-6烷基, arC0-6烷基取代的,杂烷基C6-杂烷基C6-6烷基C6-6烷基C6-6烷基-杂烷基C6-烷基C6,CianoaminoC0-6 alquilo,C0-6 alalhidrazino,杂环,arC0-6alquilhidrazino,alquilsulfililC0-6alquilo,arC0-6alalulfonililC0-6酰胺基C0-6烷基,arC0-6烷基磺酰胺基C0-6烷基,氨基C0-6烷基磺酰基,C0-6烷基氨基磺酰基,acilC1-6烷基磺酰基,杂环基磺酰基,氨基C0-6烷基亚磺酰基,酰基C1-6烷基亚磺酰基,甲硅烷基,甲硅烷基,甲氧基,硅烷基6,acilC2-6alquinilo,hidroxiC2-6alquinilo,氨基C2-6alquinilo,C1-6alcoxiC0-6alquilo,C1-6alquiltioC0-6alquilo,hidroxiC1-6-6alcoxiC0-6alquilo,hidroxiC1-6alquiltioC0-6alquilo,acilC1-6alcoloC0,6Cal6 6alquilaminoC1-6alcoxiC0-6alquilo,C0-6alquilaminoC1-6alquiltioC0-6alquilo,acilaminoC1-6alcoxiC0-6alquilo,acilaminoC1-6alquiltioC0-6alquilo,arC0-6alquilaminoC0-6alquilo,arC0-6alquilC0-6烷基,ArC0-6烷基C0-烷基,ArC0-6烷基6烷基氨基C0-6烷基,arC0-6烷硫基,arC0-6烷氧基取代的,arC0-6烷硫基取代的或arC0-6烷氧基取代的;辛基酸无顺式-N-(4-甲氧基-5-氧代-1 4-重氮杂螺5 undec-9-il)-3-(quinolin-4-ilmetil)氨基t No-2-羧酰胺顺式2-1,2-氯二氢-氟]-氟[1]-氟]-灵]-1-[1-[1]]]]]]-1-[1 ]]-键。

著录项

  • 公开/公告号AR051372A1

    专利类型

  • 公开/公告日2007-01-10

    原文格式PDF

  • 申请/专利权人 OSI PHARMACEUTICALS INC.;

    申请/专利号AR2005P103918

  • 发明设计人

    申请日2005-09-20

  • 分类号C07D409/14;C07D411/14;C07D471/10;C07D487/10;C07D491/10;C07D495/10;A61K31/4709;A61P35/00;C07D409/14;C07D333/36;C07D215/14;C07D317/66;

  • 国家 AR

  • 入库时间 2022-08-21 20:59:38

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