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1. 发明申请

US20100152155A1 Histone Deacetylase Inhibitors 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20100152155A1
公开(公告)日：2010-06-17
申请号：US11918237
申请日：2006-05-15
申请人： David Festus Charles Moffat , Sanjay Ratilal Patel , Francesca Ann Mazzei , Andrew James Belfield , Sandra Van Meurs
发明人： David Festus Charles Moffat , Sanjay Ratilal Patel , Francesca Ann Mazzei , Andrew James Belfield , Sandra Van Meurs
IPC分类号： A61K31/506 , C07D403/04 , C07D409/14 , C07D417/14 , C07D405/14 , C07D403/14 , C07D401/14 , C07D413/14 , A61K31/5377 , C12N9/99 , A61P35/00 , A61P25/00 , A61P37/00 , A61P37/06 , A61P29/00 , A61P3/10 , A61P7/00 , A61P25/28 , A61P19/02
CPC分类号： C07D209/52 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D487/04
摘要： Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.
摘要翻译：式（I）化合物及其盐，N-氧化物，水合物和溶剂合物是组蛋白脱乙酰酶抑制剂，可用于治疗包括癌症的细胞增殖性疾病：（I）其中Q，V和W独立地表示-N ═或-C =; B是选自：（IIA），（IIB），（IIC），（IID）和（IIE）的二价基团。其中标有*的债券与含有Q，V和W的环通过 - [Linker1]相连，并且标记为**的债券与A至 - [Linker2] - 链接。 A是任选取代的单环，二环或三环碳环或杂环系; 和 - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团。

2. 发明授权

US07932246B2 Histone deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US07932246B2
公开(公告)日：2011-04-26
申请号：US11918237
申请日：2006-05-15
申请人： David Festus Charles Moffat , Sanjay Ratilal Patel , Francesca Ann Mazzei , Andrew James Belfield , Sandra Van Meurs
发明人： David Festus Charles Moffat , Sanjay Ratilal Patel , Francesca Ann Mazzei , Andrew James Belfield , Sandra Van Meurs
IPC分类号： A01N43/00 , A61K31/33
CPC分类号： C07D209/52 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D487/04
摘要： Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.
摘要翻译：式（I）化合物及其盐，N-氧化物，水合物和溶剂合物是组蛋白脱乙酰酶抑制剂，可用于治疗包括癌症的细胞增殖性疾病：（I）其中Q，V和W独立地表示-N ═或-C =; B是选自：（IIA），（IIB），（IIC），（IID）和（IIE）的二价基团。其中标有*的债券与含有Q，V和W的环通过 - [Linker1]相连，并且标记为**的债券与A至 - [Linker2] - 链接。 A是任选取代的单环，二环或三环碳环或杂环系; 和 - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团。

3. 发明申请

US20140163042A1 ENZYME INHIBITORS 有权
公开(公告)号：US20140163042A1
公开(公告)日：2014-06-12
申请号：US14179880
申请日：2014-02-13
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Charles Moffat , Kenneth William John Baker , Alastair David Graham Donald
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , Francesca Ann Mazzei , Stephen John Davies , Alan Hastings Drummond , David Festus Charles Moffat , Kenneth William John Baker , Alastair David Graham Donald
IPC分类号： C07D471/04 , C07C237/40 , C07D333/70 , C07C317/50 , C07D295/192 , C07D217/26
CPC分类号： C07C237/40 , C07C259/06 , C07C275/24 , C07C311/46 , C07C317/50 , C07C2601/08 , C07C2601/14 , C07D207/416 , C07D209/42 , C07D213/40 , C07D217/02 , C07D217/22 , C07D217/26 , C07D295/185 , C07D295/192 , C07D333/70 , C07D471/04
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O), —S(═O)2—, —C(═O)O—, —C(O)NR3—, —C(═S)—NR3, —C(═NH)NR3 or —S(═O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, Alk1 and Alk2 independently represent optionally substituted divalent C3-C7 cycloalkyl radicals, or optionally substituted straight or branched, C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals which may optionally contain or terminate in an ether (—O—), thioether (—S—) or amino (—NRA—) link wherein RA is hydrogen or optionally substituted C1-C3 alkyl; X1 represents a bond; —C(═O); or —S(═O)2—; —NR4C(═O)—, —C(═O)NR4—, —NR4C(═O)NR5—, —NR4S(═O)2—, or —S(═O)2NR4— wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system wherein the radicals R1R2NH—Y-L1-X1-[CH2]Z— and HONHCO-[LINKER]- are attached different ring atoms; and -[Linker]- represents a divalent linker radical linking a ring atom in A with the hydroxamic acid group CONIIOII, the length of the linker radical, from the terminal atom linked to the ring atom of A to the terminal atom linked to the hydroxamic acid group, is equivalent to that of an unbranched saturated hydrocarbon chain of from 3-10 carbon atoms.

4. 发明申请

US20100317678A1 HYDROXAMATES AS INHIBITORS OF HISTONE DEACETYLASE 有权
标题翻译：羟肟酸作为组胺脱乙酰酶的抑制剂
公开(公告)号：US20100317678A1
公开(公告)日：2010-12-16
申请号：US12446267
申请日：2006-10-30
申请人： David Festus Charles Moffat , Francesca Ann Day , Sanjay Ratilal Patel , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
发明人： David Festus Charles Moffat , Francesca Ann Day , Sanjay Ratilal Patel , Andrew James Belfield , Alistair David Graham Donald , Alan Hornsby Davidson , Alan Hastings Drummond
IPC分类号： A61K31/506 , C07D401/04 , C07D211/58 , A61K31/451 , C07D211/34 , A61P7/00 , A61P3/10 , A61P25/00 , A61P31/00 , A61P35/00 , A61P37/00 , A61P25/28 , C12N9/99
CPC分类号： C07D239/42
摘要： Compounds of formula (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: wherein Q, V and W independently represent —N═ or —C═; B is a divalent radical selected from (B1), (B2), (B3), (B4), (B5) and (B6). wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical; and R is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— or (b) a radical of formula R-L1-Y1—(CH2)z—,
摘要翻译：式（I）化合物及其盐，N-氧化物，水合物和溶剂化物是组蛋白脱乙酰酶抑制剂，可用于治疗细胞增殖性疾病，包括癌症：其中Q，V和W独立地表示-N =或-C ═; B是选自（B1），（B2），（B3），（B4），（B5）和（B6）的二价基团。其中标记为*的键与包含Q，V和W通过 - [Linker1] - 的环连接，并且标记为**的键与A至 - [Linker2] - 连接。 A是任选取代的单环，二环或三环碳环或杂环系; - [Linker1] - 和 - [Linker2] - 独立地表示键或二价连接基团; 并且R是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-或（b）式R-L1-Y1-（CH2）z-的基团的基团，

5. 发明申请

US20110190306A1 Inhibitors of PLK 审中-公开
标题翻译： PLK抑制剂
公开(公告)号：US20110190306A1
公开(公告)日：2011-08-04
申请号：US12989178
申请日：2009-04-23
申请人： David Festus Charles Moffat , Sanjay Ratilal Patel , Kenneth William John Baker , Carl Leslie North
发明人： David Festus Charles Moffat , Sanjay Ratilal Patel , Kenneth William John Baker , Carl Leslie North
IPC分类号： A61K31/519 , C07D475/00 , A61P35/00
CPC分类号： C07D475/00
摘要： Compounds of formula (I) are PLK inhibitors, useful for the treatment of cell proliferative diseases: wherein R1 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R2 is hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 is hydrogen, —CN, hydroxyl, halogen, optionally substituted (C1C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, —NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1-Y1— wherein L1 and Y1 are as defined in the claims and R is an carbon-linked, alpha alpha disubstituted amino acid or amino acid ester residue.
摘要翻译：式（I）化合物是可用于治疗细胞增殖性疾病的PLK抑制剂：其中R 1是氢或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（ C3-C6）环烷基; R 2是氢或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R 3是氢，-CN，羟基，卤素，任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基，-NR 5 R 6或C 1 -C 4烷氧基， R6独立地为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的具有至多12个环原子的单环或双环碳环或杂环或环系; T是式R-L1-Y1-的基团，其中L1和Y1如权利要求中所定义，R是碳连接的α-α取代的氨基酸或氨基酸酯残基。

6. 发明授权

US07973181B2 Hydroxamic acid derivatives as inhibitors of HDAC enzymatic activity 有权
公开(公告)号：US07973181B2
公开(公告)日：2011-07-05
申请号：US11919048
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： C07D333/70 , C07C229/36
CPC分类号： C07C259/06 , C07D333/70
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi— or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring.

7. 发明申请

US20100216802A1 PTERIDINE DERIVATIVES AS POLO-LIKE KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：作为类似于激素治疗癌症的类激酶抑制剂的哌替啶衍生物
公开(公告)号：US20100216802A1
公开(公告)日：2010-08-26
申请号：US12446008
申请日：2007-10-19
申请人： David Festus Charles Moffat , Sanjay Ratilal Patel , Stephen John Davies , Kenneth William John Baker , Oliver James Philps
发明人： David Festus Charles Moffat , Sanjay Ratilal Patel , Stephen John Davies , Kenneth William John Baker , Oliver James Philps
IPC分类号： A61K31/519 , C07D475/00 , A61P35/00
CPC分类号： C07D475/00
摘要： Compound of formula (I) are inhibitors of Polo-like kinases (PLKs), and are useful in treatment of cell proliferative diseases: wherein R1 and R2 are hydrogen, or an optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl group; R3 and R3′ are independently selected from hydrogen, —CN, hydroxyl, halogen, optionally substituted (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl or (C3-C6)cycloalkyl, —NR5R6 or C1-C4 alkoxy, wherein R5 and R6 are independently hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted mono- or bi-cyclic carbocyclic or heterocyclic ring or a ring system having up to 12 ring atoms; T is a radical of formula R-L1-Y1— wherein R is an alpha amino acid or alpha amino acid ester motif, linked to ring A by linker R-L1-Y1— as defined in the claims.
摘要翻译：式（I）化合物是Polo样激酶（PLK）的抑制剂，可用于治疗细胞增殖性疾病：其中R 1和R 2为氢，或任选取代的（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基或（C 3 -C 6）环烷基; R3和R3'独立地选自氢，-CN，羟基，卤素，任选取代的（C1-C6）烷基，（C2-C6）烯基，（C2-C6）炔基或（C3-C6）环烷基，-NR5R6或 C 1 -C 4烷氧基，其中R 5和R 6独立地是氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的具有至多12个环原子的单环或双环碳环或杂环或环系; T是式R-L1-Y1-的基团，其中R是通过如权利要求中所定义的连接体R-L1-Y1-连接到环A的α氨基酸或α氨基酸酯基序。

8. 发明授权

US09321718B2 Benzamide derivatives and their use as HSP90 inhibtors 有权
标题翻译：苯甲酰胺衍生物及其用作HSP90抑制剂
公开(公告)号：US09321718B2
公开(公告)日：2016-04-26
申请号：US13703387
申请日：2011-06-10
申请人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： C07D211/00 , C07D295/00 , C07D209/04 , C07D207/04 , C07D207/46 , A61K31/445 , C07C235/60 , C07D207/09 , C07D209/44 , C07D211/26 , C07D211/58 , C07D207/14
CPC分类号： A61K31/4468 , A61K31/216 , A61K31/40 , A61K31/4035 , A61K31/445 , C07C235/60 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D209/44 , C07D211/26 , C07D211/58
摘要： The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供了一种化合物，其为（a）式（I）的苯基酰胺衍生物或其互变异构体，或（b）其药学上可接受的盐，N-氧化物，水合物，前药或溶剂合物：其中R1，R2，R3， R4，R5，R6和R7如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

9. 发明申请

US20130143926A1 BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS 有权
标题翻译：苯扎林衍生物及其作为HSP90抑制剂的用途
公开(公告)号：US20130143926A1
公开(公告)日：2013-06-06
申请号：US13703387
申请日：2011-06-10
申请人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alastair David Graham Donald , Joanne McDermott , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： C07C235/60 , C07D207/09 , C07D211/26 , C07D209/44 , C07D211/58 , C07D207/14
CPC分类号： A61K31/4468 , A61K31/216 , A61K31/40 , A61K31/4035 , A61K31/445 , C07C235/60 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D209/44 , C07D211/26 , C07D211/58
摘要： The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供了一种化合物，其为（a）式（I）的苯基酰胺衍生物或其互变异构体，或（b）其药学上可接受的盐，N-氧化物，水合物，前药或溶剂合物：其中R1，R2，R3， R4，R5，R6和R7如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

10. 发明申请

US20090298924A1 HYDROXAMIC ACID DERIVATIVES AS INHIBITORS OF HDAC ENZYMATIC ACTIVITY 有权
标题翻译：作为HDAC酶活性抑制剂的羟基酸衍生物
公开(公告)号：US20090298924A1
公开(公告)日：2009-12-03
申请号：US11919048
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Sanjay Ratilal Patel , David Festus Charles Moffat
IPC分类号： A61K31/381 , C07C229/36 , A61K31/235 , C07D333/70 , C12N9/99
CPC分类号： C07C259/06 , C07D333/70
摘要： Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C═O)—, —S(O2)—, —C(═O)O—, —OC(═O)—, —(C═O)NR3—, —NR3(C═O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C═O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and B is a monocyclic heterocyclic ring of 5 or 6 ring atoms wherein R1 is linked to a ring carbon adjacent the ring nitrogen shown, and ring B is optionally fused to a second carbocyclic or heterocyclic ring of 5 or 6 ring atoms in which case the bond shown intersected by a wavy line may be from a ring atom in said second ring;
摘要翻译：式（I）化合物是组蛋白脱乙酰酶活性的抑制剂，可用于治疗例如癌症：其中Y 1为键， - （CO） - ， - S（O 2） - ， - C ）-O-，-OC（-O） - ， - （CO）NR 3 - ， - NR 3（CO） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（CO）NR 5 - 其中R 3和R 5独立地是氢或任选取代的（C 1 -C 6）烷基，L 1是式 - （Alk 1）m（O）n（Alk 2）p的二价基团其中m，n，p，Alk1，Alk2和Q 如权利要求中所定义; z为0或1; A表示任选取代的单环，双环或三环碳环或杂环系; - [连接子] - 表示二价连接基团; R是式（X）或（Y）的基团：其中R 1是羧酸基团（-COOH）或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R4是氢; 或（C 1 -C 6烷基） - ， - （CO）R 3， - （CO）OR 3或 - （CO ）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基或杂芳基（C 1 -C 6烷基） R 41是氢或任选取代的C 1 -C 6烷基; 并且B是5或6个环原子的单环杂环，其中R 1与所示的环氮相邻的环碳连接，并且环B任选地与5或6个环原子的第二碳环或杂环稠合，在这种情况下显示与波浪线相交的键可以来自所述第二环中的环原子;

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