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    Dinucleotide and oligonucleotide analogues
    1.
    发明授权
    Dinucleotide and oligonucleotide analogues 失效
    二核苷酸和寡核苷酸类似物

    公开(公告)号：US6087490A

    公开(公告)日：2000-07-11

    申请号：US155198

    申请日：1998-10-08

    申请人： Anthony David Baxter ,  Eric Keith Baylis ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Roger John Taylor

    发明人： Anthony David Baxter ,  Eric Keith Baylis ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Roger John Taylor

    IPC分类号： C07H19/06 ,  C07H21/00 ,  C07H19/00 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C07H19/06 ,  C07H21/00 ,  Y02P20/55

    摘要： A compound which is a dinucleotide analogue of formula ##STR1## or a salt thereof, where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical,R.sup.1 is hydrogen or Y.sup.1,R.sup.2 and R.sup.3 are each independently hydrogen, halogen, hydroxy or --OY.sup.2,R.sup.4 is hydrogen, halogen, hydroxy, --OY.sup.3 or R.sup.7,R.sup.5 is hydrogen, halogen or R.sup.8,R.sup.6 is hydrogen, Y.sup.4 or a phosphoramidyl group,Z is a group of formula II, III or IV ##STR2## where R.sup.9 is hydrogen, halogen, hydroxy, --OY.sup.5 or R.sup.13, R.sup.10 is hydrogen, halogen or R.sup.14, R.sup.11 is hydroxy, R.sup.15 or --OR.sup.15 where R.sup.15 is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, and R.sup.12 is hydrogen, R.sup.12.sub.a or --OCOR.sup.12.sub.a where R.sup.12.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4 and Y.sup.5 are each indpendently a hydroxy-protecting group, and R.sup.7, R.sup.8, R.sup.13 and R.sup.14 are each independently a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.10 aromatic group or a C.sub.7 to C.sub.13 araliphatic group.

    摘要翻译： PCT No.PCT / GB97 / 00651 Sec。 371日期：1998年10月8日 102（e）日期1998年10月8日PCT 1997年11月3日PCT PCT。 公开号WO97 / 35869 日期1997年10月2日为式或二价核苷酸类似物的化合物或其盐，其中B1和B2各自独立地为一价核苷碱基，R1为氢或Y1，R2和R3各自独立地为氢，卤素，羟基或 -OY2，R4是氢，卤素，羟基，-OY3或R7，R5是氢，卤素或R8，R6是氢，Y4或磷酰胺基，Z是式II，III或IV的基团，其中R9是氢， 卤素，羟基，-OY5或R13，R10为氢，卤素或R14，R11为羟基，R15或-OR15，其中R15为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或 C7至C13芳脂族基团，R12为氢，R12a或-OCOR12a，其中R12a为C1至C10脂族基团，C3至C8脂环族基团，C6至C10芳族基团或C7至C13芳脂族基团，Y1，Y2， Y3，Y4和Y5各自独立地为羟基保护基，R7，R8，R13和R14各自独立地为C1至C10脂族基团，C3t C 8脂环族基团，C 6至C 10芳族基团或C 7至C 13芳脂基基团。

    Oligonucleotide analogues
    2.
    发明授权
    Oligonucleotide analogues 失效
    寡核苷酸类似物

    公开(公告)号：US5670489A

    公开(公告)日：1997-09-23

    申请号：US463139

    申请日：1995-06-02

    申请人： Anthony David Baxter ,  Eric Keith Baylis ,  Stephen Paul Collingwood ,  Roger John Taylor ,  Alain De Mesmaeker ,  Chantal Schmit

    发明人： Anthony David Baxter ,  Eric Keith Baylis ,  Stephen Paul Collingwood ,  Roger John Taylor ,  Alain De Mesmaeker ,  Chantal Schmit

    IPC分类号： G01N33/569 ,  A61K31/665 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61P31/12 ,  A61P31/16 ,  C07F9/6512 ,  C07F9/655 ,  C07F9/6561 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/04

    CPC分类号： C07H21/00 ,  C07H19/04

    摘要： A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical; R.sup.1 is R.sup.1.sub.a or Z; R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy; R.sup.5 is R.sup.5.sub.a or Z; R.sup.6 is hydrogen or R.sup.6.sub.a ; R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group; R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.5 hydrocarbyl groups; R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups; R.sup.9 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion; R.sup.10 and R.sup.11 are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical; R.sup.x and R.sup.y are independently hydrogen, halogen, hydroxy, a C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkenoxy, C.sub.6 -C.sub.10 aryloxy or C.sub.7 -C.sub.16 aralkyloxy group, which is substituted or unsubstituted, or --OCOR.sub.z ; R.sup.z is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl or C.sub.7 -C.sub.16 aralkyl group; and Z is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being substituted or unsubstituted.

    摘要翻译： 式Ⅰ的二核苷酸类似物，其中B1和B2各自独立地是一价核苷碱基; R1为R1a或Z; R1a，R2，R3和R4各自独立地为氢，卤素或羟基; R5为R5a或Z; R6是氢或R6a; R7是氢，烷​​基-N，N-二烷基磷酰胺基或R7a，R8是R8a或Z，或者所指示的R7O和R8一起表示异丙烯二氧基; R5a和R8a各自独立地为氢，卤素，羟基，-OR10，-OCOR10或被三个C1-C5烃基取代的甲硅烷氧基; R6a和R7a各自独立地为C1-C10脂族基团，C6-C15芳族基团，C7-C30芳脂族基团，-COR11，-SO2R11或被三个C1-C15烃基取代的甲硅烷基基团; R9是氢，C1-C8脂族基团，C3-C8脂环族基团，C6-C15芳族基团，C7-C13芳脂族基团，碱金属离子或铵离子; R 10和R 11各自独立地为C 1 -C 10脂族基团，C 3 -C 8脂环族基团，C 6 -C 15芳族基团或C 7 -C 16芳脂族基团; Rx和Ry独立地是氢，卤素，羟基，C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基，C7-C16芳烷基，C1-C10烷氧基，C2-C10链烯氧基，C6-C10 取代或未取代的芳氧基或C7-C16芳烷氧基，或-OCORz; Rz是取代或未取代的C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基或C7-C16芳烷基; Z为C6-C10芳氧基硫代羰氧基，C6-C10芳基为取代或未取代的。

    Oligonucleotide analogues
    3.
    发明授权
    Oligonucleotide analogues 失效
    寡核苷酸类似物

    公开(公告)号：US06562960B1

    公开(公告)日：2003-05-13

    申请号：US09142212

    申请日：1998-10-09

    申请人： Anthony David Baxter ,  Stephen Paul Collingwood ,  Mark Edward Douglas ,  Roger John Taylor

    发明人： Anthony David Baxter ,  Stephen Paul Collingwood ,  Mark Edward Douglas ,  Roger John Taylor

    IPC分类号： C07H2100

    CPC分类号： C07H21/00

    摘要： An oligonucleotide analogue having 10 to 200 natural and/or synthetic nucleoside units, linked by internucleoside linkages, at least one of the internucleoside linkages being of formula where the indicated methylene group is attached to a 3′ carbon atom of a nucleoside, the indicated oxygen atom is attached to a 5′-carbon atom of an adjacent nucleside, R1 is hydrogen, hydroxy, O—, thiol, S—, —NH2 or a group of formula R1a, —OR1a, —SR1a, —NHR1b, or —NR1bR1c wherein R1a is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group; and R1b and R1c are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group or R1b and R1c together with the nitrogen atom to which they are attached denote a five- or six-membered heterocyclic ring, and X is oxygen or sulfur.

    摘要翻译： 具有10至200个天然和/或合成的核苷单位的寡核苷酸类似物，通过核苷间键连接，至少一个位于所指定的亚甲基上的核苷间键与核苷的3'碳原子连接，所指示的氧原子 连接在相邻核苷酸的5'-碳原子上，R 1是氢，羟基，O-，硫醇，S-，-NH 2或式R1a，-OR1a，-SR1a，-NHR1b或-NR1bR1c的基团，其中 R1a是未取代或取代的C1至C10烷基，C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基; R1b和R1c各自独立地为未取代或取代的C1至C10烷基，C2至C10烯基，C3至C8环烷基，C6至C10芳基或C7至C13芳烷基或R1b和R1c与它们所连接的氮原子一起 表示五元或六元杂环，X是氧或硫。

    Intermediates for dinucleotide and oligonucleotide analogues
    4.
    发明授权
    Intermediates for dinucleotide and oligonucleotide analogues 失效

    公开(公告)号：US5952478A

    公开(公告)日：1999-09-14

    申请号：US793725

    申请日：1997-04-14

    申请人： Anthony David Baxter ,  Roger John Taylor ,  Stephen Paul Collingwood

    发明人： Anthony David Baxter ,  Roger John Taylor ,  Stephen Paul Collingwood

    IPC分类号： A61K31/70 ,  A61K31/7024 ,  A61K31/7042 ,  A61K31/7048 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7135 ,  A61P31/12 ,  A61P35/00 ,  A61P43/00 ,  C07D405/04 ,  C07F9/32 ,  C07F19/00 ,  C07H9/04 ,  C07H13/02 ,  C07H13/04 ,  C07H13/06 ,  C07H13/08 ,  C07H19/01 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H23/00 ,  C07H19/00 ,  A01N43/04 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C07H9/04 ,  C07H13/04 ,  C07H13/08 ,  C07H19/04 ,  C07H21/00 ,  Y02P20/55

    摘要： A compound of formula (I) or salts thereof, where R.sup.0 is hydrogen or together with R.sup.7 O denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.1 is hydrogen, R.sup.1.sub.a or a group of formula (II), R.sup.1.sub.a is R.sup.1.sub.b or a protecting group Q, R.sup.1.sub.b is C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R.sup.2 is R.sup.2.sub.a or --OR.sup.15 or together with R.sup.5 denotes an oxy group --O--, provided that R.sup.2 is --OR.sup.15 when R.sup.1 is a group of formula (II), R.sup.2.sub.a is a C.sub.1 -C.sub.20 aliphatic group, a C.sub.3 -C.sub.10 cycloaliphatic group, a C.sub.6 -C.sub.15 aromatic group, a C.sub.7 -C.sub.16 araliphatic group, or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R.sup.3 is R.sup.3.sub.a or Z, R.sup.3.sub.a is hydrogen, halogen, hydroxy, R.sup.16, --OR.sup.16, OCOR.sup.16, --OSO.sub.2 R.sup.16, or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, R.sup.4 is hydrogen, halogen or R.sup.17, R.sup.5 is R.sup.5.sub.a or Z or together with R.sup.2 denotes an oxy group --O--, R.sup.5.sub.a is hydrogen, halogen, hydroxy, R.sup.18, --OR.sup.18, --OCOR.sup.18, --OSO.sub.2 R.sup.18, or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, or together with R.sup.6 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.6 is halogen, hydroxy, --OR.sup.19, --OCOR.sup.19, --OSO.sub.2 R.sup.19 or B.sup.1, or together with R.sup.5 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, provided that R.sup.6 is not B.sup.1 when R.sup.1 is a group of formula (II) in which R.sup.14 is B.sup.2, R.sup.7 is hydrogen or R.sup.7.sub.a, R.sup.7.sub.a is R.sup.20, --COR.sup.20, --SO.sub.2 R.sup.20 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyl, or together with the attached oxygen atom and R.sup.0 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.8 is hydrogen, halogen, hydroxy, R.sup.21, --OR.sup.21, --OCOR.sup.21, --OSO.sub.2 R.sup.21 or together with R.sup.10 denotes a valence bond, R.sup.9 is hydrogen, halogen or R.sup.22, R.sup.10 is hydrogen, halogen, hydroxy, R.sup.23, --OR.sup.23, --OCOR.sup.23 or --OSO.sub.2 R.sup.23, or together with R.sup.8 denotes a valence bond, R.sup.11 is hydrogen, halogen or R.sup.24, R.sup.12 is hydrogen or R.sup.12.sub.a, or R.sup.12 O-- together with R.sup.13 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.12.sub.a is R.sup.25, --COR.sup.25, --SO.sub.2 R.sup.25 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyl, R.sup.13 is R.sup.13.sub.a or Z, R.sup.13.sub.a is hydrogen, halogen, hydroxy, R.sup.26, --OR.sup.26, --OCOR.sup.26, --OSO.sub.2 R.sup.26 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, or together with R.sup.14 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, or together with R.sup.12 O-- denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.14 is halogen, hydroxy, --OR.sup.27, --OCOR.sup.27, --OSO.sub.2 R.sup.27, or B.sup.2 or together with R.sup.13 denoted a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, provided that R.sup.14 is not B.sup.2 when R.sup.6 is B.sup.1, R.sup.15 is hydrogen or R.sup.15.sub.a, R.sup.15.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.15 aromatic group or a C.sub.7 to C.sub.16 araliphatic group, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, R.sup.23, R.sup.24, R.sup.25, R.sup.26 and R.sup.27 are independently a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.10 cycloaliphatic group, a C.sub.6 to C.sub.15 aromatic group or a C.sub.7 to C.sub.30 araliphatic group, B.sup.1 and B.sup.2 are independently each a monovalent nucleoside base radical, and Z is substituted or unsubstituted C.sub.6 to C.sub.10 aryloxythiocarbonyloxy. ##STR1##

    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    8.
    发明授权
    8-Quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
    8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：US06919337B2

    公开(公告)日：2005-07-19

    申请号：US10644328

    申请日：2003-08-20

    申请人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Ret Naef ,  David Andrew Sandham

    发明人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Ret Naef ,  David Andrew Sandham

    IPC分类号： C07D473/04 ,  C07D473/06 ,  A61K31/5355 ,  A61P15/10 ,  C07D473/02

    CPC分类号： C07D473/04 ,  C07D473/06

    摘要： A compound of formula (I) R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

    摘要翻译： 式（I）R 1的化合物是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基， 烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基， 氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基，R 0 任选地与5元杂环基稠合并且任选地被一个或多个选自卤素，氰基，羟基，烷基，羟基烷基，烷氧基烷基，烷硫基的取代基取代的喹啉基，异喹啉基或氧代二氢异喹啉基 烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。

    8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors
    9.
    发明授权
    8-quinolinxanthine and 8-isoquinolinxanthine derivatives as PDE 5 inhibitors 失效
    8-喹啉黄嘌呤和8-异喹啉黄嘌呤衍生物作为PDE 5抑制剂

    公开(公告)号：US07019136B2

    公开(公告)日：2006-03-28

    申请号：US10937639

    申请日：2004-09-09

    申请人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Reto Naef ,  David Andrew Sandham

    发明人： Gurdip Bhalay ,  Stephen Paul Collingwood ,  Robin Alec Fairhurst ,  Sylvie Felicite Gomez ,  Reto Naef ,  David Andrew Sandham

    IPC分类号： C07D239/02

    CPC分类号： C07D239/545 ,  A61K31/522 ,  C07D473/04 ,  C07D473/06

    摘要： A compound of formula (I): R1 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R2 is hydrogen, alkyl, hydroxyalkyl, alkylcarbonyloxyalkyl, alkoxyalkyl, alkylthioalkyl, alkenyl, cycloalkylalkyl, heterocyclylalkyl, aralkyl in which the aryl ring thereof is optionally fused to a 5-membered heterocyclic group or is optionally substituted by one or more substituents selected from alkoxy, amino, alkylamino, dialkylamino, acylamino, halogen, hydroxy, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl, alkylsulfonylamino or dialkylaminosulfonylamino, R3 is hydrogen or alkyl optionally substituted by hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, R5 is a quinolinyl, isoquinolinyl or oxodihydroisoquinolinyl group optionally fused to a 5-membered heterocyclic group and optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, alkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxy, alkylthio, alkenyl, alkoxycarbonyl, alkynyl, carboxyl, acyl, a group of formula —N(R6)R7, aryl optionally substituted by one or more substituents selected from halogen or alkoxy, or heteroaryl having 5 or 6 ring atoms attached through a ring carbon atom to the indicated carbon atom, and R6 and R7 are each independently hydrogen or alkyl optionally substituted by hydroxy or alkoxy or one of R6 and R7 is hydrogen and the other is acyl, or R6 and R7 together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclyl group.

    摘要翻译： 式（I）化合物：R 1是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 2是氢，烷基，羟基烷基，烷基羰氧基烷基，烷氧基烷基 ，烷基硫代烷基，烯基，环烷基烷基，杂环基烷基，芳烷基，其中其芳基环任选地与5元杂环基稠合，或任选地被一个或多个选自烷氧基，氨基，烷基氨基，二烷基氨基，酰氨基，卤素，羟基 ，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基，烷基磺酰基氨基或二烷基氨基磺酰基氨基，R 3是氢或任选被羟基，烷氧基或烷硫基取代的烷基，R 4是氢或烷基， 任选地与5元杂环基稠合的喹啉基，异喹啉基或氧代二氢异喹啉基，任选地被一个或多个选自卤素，氰基，羟基，烷基，羟烷基，烷氧基烷基，烷硫基 烷基，烷氧基，烷硫基，烯基，烷氧基羰基，炔基，羧基，酰基，式-N（R 6）R 7的基团，任选地被一个或多个 选自卤素或烷氧基的取代基或具有5或6个环原子通过环碳原子连接到指定碳原子的杂芳基，R 6和R 7各自独立地 任选被羟基或烷氧基取代的氢或烷基或R 6和R 7中的一个是氢，另一个是酰基或R 6和 R 7与它们所连接的氮原子一起表示5-或6-元杂环基。