Bis(prop-2-enyl) 2-aminopentanedioate

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: Bis(prop-2-enyl) 2-aminopentanedioate
• 化学式: C₁₁H₁₇NO₄
• 分子量: 227.26
• InChiKey: JQTAOTLIRWYSFQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  16
• 可旋转键数：
  10
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  78.6
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• BLOCK COPOLYMERS FOR STABLE MICELLES
  申请人：Intezyne Technologies, Inc.

  公开号：US20130280306A1

  公开（公告）日：2013-10-24

  The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same. Compositions herein are useful for drug-delivery applications.

  本发明涉及聚合物化学领域，更具体地说是涉及多区块共聚物以及包含相同的多区块共聚物胶束。本发明的组合物适用于药物输送应用。
• HYBRID BLOCK COPOLYMER MICELLES WITH MIXED STEREOCHEMISTRY FOR ENCAPSULATION OF HYDROPHOBIC AGENTS
  申请人：SILL Kevin N.

  公开号：US20080274173A1

  公开（公告）日：2008-11-06

  The present invention relates to the field of polymer chemistry and more particularly to multiblock copolymers and micelles comprising the same.

  本发明涉及聚合物化学领域，更具体地说是涉及多嵌段共聚物以及包含该共聚物的胶束。
• [EN] POLYMER MICELLES CONTAINING ANTHRACYLINES FOR THE TREATMENT OF CANCER<br/>[FR] MICELLES POLYMÈRES CONTENANT DES ANTHRACYCLINES UTILISABLES À DES FINS DE TRAITEMENT DU CANCER
  申请人：INTEZYNE TECHNOLOGIES INC

  公开号：WO2010127271A1

  公开（公告）日：2010-11-04

  The present invention provides micelles having an anthracycline encapsulated therein, the micelles comprising a multiblock copolymer. The invention further provides methods of preparing and using said micelles, and compositions thereof.

  本发明提供了包含蒽环类药物的胶束，所述胶束包括多嵌段共聚物。该发明还提供了制备和使用所述胶束以及其组合物的方法。
• Hypophosphorous Acid Derivatives and their Therapeutical Applications
  申请人：Acher Francine

  公开号：US20090170813A1

  公开（公告）日：2009-07-02

  Hypophosphorous acid derivatives having Formula (I) wherein .M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group, or an a, β, or a β, g-cyclic amino acid; .R 1 is H or R, R being an hydroxy or a carboxy protecting group; .Z is H or an amino protecting group R′, benzyl oxycarbonyl, benzyl or benzyl substituted; .E is H or a C1-C3 alkyl, aryl, an hydrophobic group; .R 2 is selected in the group comprising: D-CH(R 6 )—C—(R 7 ,R 8 ), (R 11 ,R 12 )CH—C(R 9 ,R 10 ), D-CH(OH), D-[C(R 13 ,R 14 )] n3 —, C[(R 15 ,R 16 ,R 17 )] n4 , D-CH 2 , (R 18 )CH═C(R 19 ), D-(M 1 ) n6 —CO, Formula (II), PO(OH) 2 —CH 2 or (PO(OH) 2 —CH 2 ), (COOH—CH 2 )—CH 2 , with -D=H, OH, OR, (CH 2 ) n2 OH, (CH 2 ) n1 OR, COOH, COOR, (CH 2 ) n2 COOH, (CH 2 ) n1 COOR, SR, S(OR), SO 2 R, NO 2 , heteroaryl, C 1 -C 3 alkyl, cycloalkyl, heterocycloalkyl, (CH 2 ) n2 -alkyl, (COOH,NH 2 )—(CH 2 ) u1 -cyclopropyl-(CH 2 ) u2 —, CO—NH-alkyl, Ar, (CH 2 ) n2 —Ar, CO—NH—Ar; —R 3 to R 19 being H, OH, OR, (CH 2 ) n2 OH, (CH 2 ) n1 OR, COOH, COOR, (CH 2 ) n2 COOH, (CH 2 ) n1 COOR, C 1 -C 3 alkyl, cycloalkyl, (CH 2 )n1-alkyl, aryl, (CH 2 )n1-aryl, halogen, CF 3 , SO 3 H, (CH 2 ) x PO 3 H 2 , with x=0, 1 or 2, B(OH) 2 , Formula (III), NO 2 , SO 2 NH 2 , SO 2 NHR; SR, S(O)R, SO 2 R, benzyl; -M 1 is an alkylene or arylene group; -n1=1, 2 or 3, n2=1, 2 or 3, n3=0, 1, 2 or 3 and n4=1, 2 or 3, n5=1, 2 or 3, n6=0 or 1, u1 and u2, identical or different=0, 1 or 2, with the proviso that Formula (I) does not represent the racemic (3R,S) and the enantiomeric form (3R) of 3 amino,3-carboxy-propyl-2′-carboxy-ethylphosphinic acid; 3 amino,3-carboxy-propyl-4′carboxy,2′carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl-2′carboxy-butanoylphosphinic acid; 3 amino,3-carboxy-propyl-3′amino, 3′carboxy-propylylphosphinic acid; and 3 amino,3-carboxypropyl-7′amino-2′, 7′-dicarboxyheptylphosphinic acid, said hypophosphorous acid derivatives being diasteroisomers or enantiomers. Application as drugs.

  含有Formula (I)的次磷酸衍生物，其中.M是[C(R3,R4)]n1-C(E,COOR1,N(H,Z))基团，或者是一个可选择取代的Ar—CH(COOR1,N(H,Z))基团，或者是α，β或αβ，γ-环氨基酸；.R1是H或R，R是一个羟基或羧基保护基团；.Z是H或氨基保护基团R′，苄氧羰基，苄基或苄基取代；.E是H或C1-C3烷基，芳基，疏水基团；.R2是从以下群体中选择的：D-CH(R6)—C—(R7,R8)，(R11,R12)CH—C(R9,R10)，D-CH(OH)，D-[C(R13,R14)]n3—，C[(R15,R16,R17)]n4，D-CH2，(R18)CH═C(R19)，D-(M1)n6—CO，Formula (II)，PO(OH)2— 或(PO(OH)2— )，(COOH— )— ，其中-D=H，OH，OR，( )n2OH，( )n1OR，COOH，COOR，( )n2COOH，( )n1COOR，SR，S(OR)，SO2R，NO2，杂环芳基，C1-C3烷基，环烷基，杂环烷基，( )n2-烷基，(COOH,NH2)—( )u1-环丙基-( )u2—，CO—NH-烷基，Ar，( )n2—Ar，CO—NH—Ar；—R3到R19为H，OH，OR，( )n2OH，( )n1OR，COOH，COOR，( )n2COOH，( )n1COOR，C1-C3烷基，环烷基，( )n1-烷基，芳基，( )n1-芳基，卤素，CF3，SO3H，( )xPO3H2，其中x=0，1或2，B(OH)2，Formula (III)， ，SO2NH2，SO2NHR；SR，S(O)R，SO2R，苄基；-M1是一个烷基或芳基基团；-n1=1，2或3，n2=1，2或3，n3=0，1，2或3，n4=1，2或3，n5=1，2或3，n6=0或1，u1和u2，相同或不同=0，1或2，但Formula (I)不代表3-氨基，3-羧基-丙基-2′-羧基-乙磷酸的消旋体(3R,S)和对映体形式(3R)；3-氨基，3-羧基-丙基-4′羧基，2′羧基-丁酰磷酸；3-氨基，3-羧基-丙基-2′羧基-丁酰磷酸；3-氨基，3-羧基-丙基-3′氨基，3′羧基-丙基磷酸；和3-氨基，3-羧基丙基-7′氨基-2′，7′-二羧基庚基磷酸，所述的次磷酸衍生物为二对映异构体或对映体。用作药物的应用。
• THIOPHOSPHI(O)NIC ACID DERIVATIVES AND THEIR THERAPEUTICAL APPLICATIONS
  申请人：Acher Francine

  公开号：US20100137258A1

  公开（公告）日：2010-06-03

  The invention relates to thiophosphi(o)nic acid derivatives having formula (I) wherein. M is a [C(R 3 ,R 4 )]n1-C(E,COOR 1 ,N(H,Z)) group, or an optionally substituted Ar—CH(COOR 1 ,N(H,Z)) group (Ar designating an aryl or an heteroaryl group), or an α, β cyclic aminoacid group such as, formula (II) or a β, &ggr;-cyclic aminoacid group such as, formula (III). R 1 is H or R, R being an hydroxy or a carboxy protecting group, such as C 1 -C 3 alkyl, Ar (being aryl or heteroaryl), Z is H or an amino protecting group R′, such as C 1 -C 3 alkyl, C 1 -C 3 acyl, Boc, Fmoc, COOR, benzyl oxycarbonyl, benzyl or benzyl substituted such as defined with respect to Ar; E is H or a C1-C3 alkyl, aryl, an hydrophobic group such as (CH 2 ) n1 -alkyl, (CH 2 ) n1 -aryl (or heteroaryl), such as a benzyl group, or a xanthyl, alkyl xanthyl or alkyl thioxanthyl group, or —(CH 2 ) n1 -cycloalkyl, —(CH 2 ) n —(CH 2 —Ar) 2 , a chromanyl group, particularly 4-methyl chromanyle, indanyle, tetrahydro naphtyl, particularly methyl-tetrahydronaphtyl; or M is OM′, wherein M′ is as above defined for M; R 2 is selected in the group comprising: D-CH(R 6 )—C—(R 7 ,R 8 )—(R 11 ,R 12 )CH—C(R 9 .R 10 )-D-CH(OH)-D-[C(R 13 ,R 14 )] n3 —C[(R 15 ,R 16 ,R 17 ] n4 -D-CH 2 —(R 18 )CH═C(R 19 )-D-(M 1 )n6-CO-D-C(R,R′)—O-D-O—, formula (IV), PO(OH) 2 —CH 2 or (PO(OH) 2 —CH 2 ), (COOH—CH 2 )—CH 2 — with -D=H, OH, OR, (CH 2 ) n2 OH, (CH 2 ) n1 OR, COOH, COOR, (CH 2 ) n2 COOH, (CH 2 ) n1 C00R, SR, S(OR), SO 2 R, NO 2 , heteroaryl, C 1 -C 3 alkyl, cycloalkyl, heterocycloalkyl, (CH 2 ) n2 -alkyl, (COOH, NH 2 )—(CH 2 ) u1 -cyclopropyl-(CH 2 ) u2 —, CO—NH-alkyl, Ar, (CH 2 ) n2 —Ar, CO—NH—Ar, R being as above defined and Ar being an optionally substituted aryl or heteroaryl group, —R 3 to R 19 , identical or different, being H, OH, OR, (CH 2 ) n2 OH, (CH 2 ) n1 OR, COOH, COOR, (CH 2 ) n2 COOH, (CH 2 ) n1 COOR, C 1 -C 3 alkyl, cycloalkyl, (CH 2 ) n1 -alkyl, aryl, (CH 2 ) n1 -aryl, halogen, CF 3 , SO 3 H, (CH 2 )XPO 3 H 2 , with x=0, 1 or 2, B(OH) 2 , formula (V), NO 2 , SO 2 NH 2 , SO 2 NHR; SR, S(O)R, SO 2 R, benzyl; one of R 11 or R 12 being COOR, COOH, (CH 2 ) n2 —COOH, (CH 2 ) n2 —COOR, PO 3 H 2 the other one being such as defined for R 9 and R 10 ;—one Of R 15 , R 16 and R 17 is COON or COOR, the others, identical or different, being such as above defined;—one of R 18 and R 19 is COOH or COOR, the other being such as above defined;—M 1 is an alkylene or arylene group;—n 1 =1, 2 or 3;—n 2 =1, 2 or 3,—n 3 =0, 1, 2 or 3 and—n 4 =1, 2 or 3;—n 5 =1, 2 or 3;—n 6 =0 or 1,—u 1 and u 2 , identical or different=0, 1 or 2, Ar, and alkyl groups being optionally substituted by one or several substituents on a same position or on different positions, said substituents being selected in the group comprising: OH, OR, (CH 2 ) n1 OH, (CH2) n1 OR, COOH, COOR, (CH 2 ) n1 C00H, (CH 2 ) n1 COOR, C 1 -C 3 alkyl, cycloalkyl, (CH 2 ) n1 -alkyl, aryl, (CH 2 ) n1 -aryl, halogen, CF 3 , SO 3 H, (CH 2 ) x PO 3 H 2 , with x=0, 1 or 2, B(OH) 2 , formula (V), NO 2 , SO 2 NH 2 , SO 2 NHR; SR, S(O)R, SO 2 R, benzyl; R being such as above defined.

  本发明涉及具有以下式（I）的硫代磷酸衍生物，其中M是[C（R3，R4）]n1-C（E，COOR1，N（H，Z））基团，或者是一个可选择取代的Ar—CH（COOR1，N（H，Z））基团（Ar代表芳基或杂芳基），或者是α，β环氨基酸基团，如式（II）或β，γ-环氨基酸基团，如式（III）。R1是H或R，其中R是一个羟基或羧基保护基团，例如C1-C3烷基，Ar（代表芳基或杂芳基），Z是H或氨基保护基团R'，例如C1-C3烷基，C1-C3酰基，Boc，Fmoc，COOR，苄氧羰基，苄基或与Ar相关定义的苄基取代物；E是H或C1-C3烷基，芳基，疏水基团，如（CH2）n1-烷基，（ ）n1-芳基（或杂芳基），如苄基，或者是黄色素基团，如（ ）n1-环烷基，（ ）n-（ —Ar）2，一环色基团，特别是4-甲基色基，茚基，四氢萘基，特别是甲基-四氢萘基；或者M是OM'，其中M'如上定义为M；R2在组中选择：D-CH（R6）—C—（R7，R8）—（R11，R12）CH—C（R9.R10）-D-CH（OH）-D-[C（R13，R14）]n3—C（R15，R16，R17）n4-D- —（R18）CH═C（R19）-D-（M1）n6-CO-D-C（R，R'）—O-D-O—，式（IV），PO（OH）2— 或（PO（OH）2— ），（COOH— ）— —，其中-D=H，OH，OR，（ ）n2OH，（ ）n1OR，COOH，COOR，（ ）n2COOH，（ ）n1C00R，SR，S（OR），SO2R，NO2，杂芳基，C1-C3烷基，环烷基，杂环烷基，（ ）n2-烷基，（COOH，NH2）—（ ）u1-环丙基-（ ）u2—，CO—NH-烷基，Ar，（ ）n2—Ar，CO—NH—Ar，其中R如上定义，Ar是可选择取代的芳基或杂芳基，—R3到R19，相同或不同，为H，OH，OR，（ ）n2OH，（ ）n1OR，COOH，COOR，（ ）n2COOH，（ ）n1COOR，C1-C3烷基，环烷基，（ ）n1-烷基，芳基，（ ）n1-芳基，卤素，CF3，SO3H，（ ）XPO3H2，其中x=0，1或2，B（OH）2，式（V）， ，SO2NH2，SO2NHR；SR，S（O）R，SO2R，苄基；其中R11或R12之一为COOR，COOH，（ ）n2—COOH，（ ）n2—COOR，PO3H2，另一个如R9和R10定义的；其中R15，R16和R17之一为COON或COOR，其他的相同或不同，如上定义；其中R18和R19之一为COOH或COOR，另一个如上定义；其中M1是一个烷基或芳基基团；n1=1，2或3；n2=1，2或3；n3=0，1，2或3；n4=1，2或3；n5=1，2或3；n6=0或1；u1和u2，相同或不同=0，1或2，Ar和烷基基团可选择在同一位置或不同位置上由一个或多个取代基取代，所述取代基选择自羟基，OR，（ ）n1OH，（ ）n1OR，COOH，COOR，（ ）n1C00H，（ ）n1COOR，C1-C3烷基，环烷基，（ ）n1-烷基，芳基，（ ）n1-芳基，卤素， ，SO3H，（ ）xPO3H2，其中x=0，1或2，B（OH）2，式（V）， ，SO2NH2，SO2NHR；SR，S（O）R，SO2R，苄基；R如上定义。