首页> 外国专利> Tiepino 3,2-b dihydropyridines, Pharmaceutical compositions that include, use of such compounds for preparing medicaments, apparatus for Administering Pharmaceutical compositions and processes for preparing these compounds

Tiepino 3,2-b dihydropyridines, Pharmaceutical compositions that include, use of such compounds for preparing medicaments, apparatus for Administering Pharmaceutical compositions and processes for preparing these compounds

机译:Tiepino [3,2-b]二氢吡啶,药物组合物,包括这些化合物在制备药物中的用途,药物组合物的给药装置和制备这些化合物的方法

摘要

1. Tiepino [3, 2-B] dihydropyridine (1) or its pharmaceutically acceptable salts, wherein R1, R2, R3, R4 and R5 are independent of H, oh, halogen, cyanogen, NO2, tar, alcoxi c1-8, c1-8, hydrogen carbide C1-4, c1-8 pitch, difluoromethane, difluoromethy, difluoromethyleti and sulfur fluoride; e. Oxadiazol (composed of R1 and R2);X a n d y were selected from (a) R7 and R6; (b) R10 and (CH2) m-nr8r9; (c) R7 and R11; and (d) R10 and R11: H, C1-5 linear or separable tar, alternative tar, arilo, 3-piserial, 3-piterial n-replace, 2-pirrolidinil methyleno-replace, respectively; In this case, the 3-piseriallo n-permutation of the above 3-piseriallo n-permutation and the 3-piseriallo n-permutation of the 2-pirroilidinil methen-permutation can be replaced by the c1-8 of linear chain or branch or the c1-8 tar of benzene, and the alternatives can be replaced by Alcoy c1-8, alcoiloxi C2-8, fenilacetiloxi, benzoiloxi, halogeno, p-tosiloxi, mesiloxi, amino, carboacioxi,Where (I) r 'and R' are independent of group H; c1-8 is linear or isolated, c1-7 is cyclopropyl, phenyl, benzene and phenylethyl, or O (II) r 'and R' combine to form a heterocyclic ring, which is composed of piperidine, pirrolidino, morfolino, tiomorfolino, piperazino, 2-tieno, 3-tieno. a. The n-substitution of a heterocyclic derivative is replaced by H, c1-8 linear matrix or derivative, benzhidril, phenyl and / or phenyl (with NO2, halogenated, c1-8 linear or derivative, alcox c1-8 and / or trifluorometric);R7 was selected from arilo, 3-piridio, 2-tieno and 3-tieno, R8 was the last (CH2) P (isocycloethane) or (CH2) P (arilo);R9 is selected from h, asphalt, cyclopropyl compounds, arilo and arilalquilo; R10 is selected from h, amine, asphalt, arilo, sulfur trifluoride and alcoximetry; R11 is selected from the group consisting of the only asphalt - Oh, rental ore, lake, cyclic carbonate, cyclic carbonate, replaced by asphalt, cyclic carbonate, aril-c (o) or '. -Tar-aril-c (o) or ',alquil-OC (O) R-alquil-C (O) R-alquil-C (O) OR-alquil-N (R) C (O) RAnd the last one -- N ''c (o) o r',R '' and R '' were independently selected from the hydrogen, amine, tar, arilo, cyclopentadiene and non cyclopentene groups mixed with arilo, which contained amines mixed with halogen, cyanogen, NO2, lactona, amine, leased non cyclopentene, hydrocarbon, arilo, cyclopentadiene and non cyclopentene, 1. Arilo, Amida, carbamato, carbamoile, carboaco Circo, asphalt, asphalt, halogenated tar, arilalquilo, Alcoy, isopropene and / or arilo alternative asphalt (optional to be replaced by Oh, halogeno, Ciano, NO2, acquilo, amino, demitlamino, alcox, aculfonilo, carbonoxy C1-4, asphalt and / or trifluorometyl);And m, N and P are all in one from 1 to 5. Pharmaceutical compounds containing these compounds, compounds for drug preparation, management devices for drug synthesis and processes for the preparation of these compounds are also disclosed.
机译:1. Tiepino [3,2-B]二氢吡啶(1)或其药学上可接受的盐,其中R1,R2,R3,R4和R5不依赖于H,OH,卤素,氰,NO2,焦油,醇c1-8, c1-8,碳化氢C1-4,c1-8沥青,二氟甲烷,二氟甲基,二氟甲基和氟化硫; e。恶二唑(由R1和R2组成); X a d d选自(a)R 7和R 6; (b)R10和(CH2)m-nr8r9; (c)R7和R11; (d)R 10和R 11:分别为H,C 1-5线性或可分离的焦油,替代焦油,芳基,3-piserial,3-piterial n-取代,2-pirrolidinilmethyleno-replace;在这种情况下,可以用线性链或支链的c1-8取代上述3-piseriallo n-置换的3-piseriallo n-置换和2-pirroilidinil methen-置换的3-piseriallo n-置换。苯的c1-8焦油,其替代品可被Alcoy c1-8,alcoiloxi C2-8,fenilacetiloxi,benzoiloxi,halolo,p-tosiloxi,mesiloxi,氨基,carbacioxi取代,其中(I)独立于H组; c1-8是线性或孤立的,c1-7是环丙基,苯基,苯和苯乙基,或O(II)r'和R'结合形成杂环,该环由哌啶,吡咯烷基,morfolino,tiomorfolino,piperazino组成,2-tieno,3-tieno。一种。杂环衍生物的n-取代被H,c1-8线性基体或衍生物,苄基地尔,苯基和/或苯基(具有NO2,卤代,c1-8线性或衍生物,alcox c1-8和/或三氟代)取代; R7选自arilo,3-piridio,2-tieno和3-tieno,R8是最后一个(CH2)P(异环乙烷)或(CH2)P(arilo); R9选自h,沥青,环丙基化合物, arilo和arilalquilo; R10选自h,胺,沥青,芳基,三氟化硫和酒精度法; R11选自唯一的沥青-哦,出租矿石,湖泊,环状碳酸盐,环状碳酸盐,被沥青,环状碳酸盐,Aril-c(o)或'代替。 -Tar-aril-c(o)或',alquil-OC(O)R-alquil-C(O)R-alquil-C(O)OR-alquil-N(R)C(O)R一个-N''c(o)o r',R''和R''独立地选自氢,胺,焦油,芳基,环戊二烯和与芳基混合的非环戊烯基,其中含有与卤素混合的胺,氰化物,NO2,内酰胺,胺,租用的非环戊烯,碳氢化合物,芳基,环戊二烯和非环戊烯,1.阿里洛,阿米达,卡马马托,卡巴莫莱,卡瓦科Circo,沥青,沥青,卤化焦油,芳烃,Alcoy,异丙基和/或芳基替代沥青(可选用Oh,卤素,Ciano,NO2,acquilo,氨基,二氨基,alcox,aculfonilo,羰氧基C1-4,沥青和/或三氟甲基取代);并且m,N和P都是合一的到5.还公开了含有这些化合物的药物化合物,用于药物制备的化合物,用于药物合成的管理装置以及用于制备这些化合物的方法。

著录项

  • 公开/公告号AR030198A1

    专利类型

  • 公开/公告日2003-08-13

    原文格式PDF

  • 申请/专利权人 ORTHO-MCNEIL PHARMACEUTICAL INC.;

    申请/专利号AR2001P101352

  • 发明设计人

    申请日2001-03-22

  • 分类号C07D495/04;A61K31/4365;A61P37/00;

  • 国家 AR

  • 入库时间 2022-08-22 00:04:04

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