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1. 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。

2. 发明申请

US20110046210A1 SUBSTITUTED THIOPENECARBOXAMIDES AS IKK-BETA SERINE-, THREONINE-PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为IKK-BETA SERINE-，THREONIN-PROTEIN激酶抑制剂的替代噻托溴铵
公开(公告)号：US20110046210A1
公开(公告)日：2011-02-24
申请号：US12989271
申请日：2009-04-23
申请人： David Festus Charles Moffat , Stephen John Davies
发明人： David Festus Charles Moffat , Stephen John Davies
IPC分类号： A61K31/381 , C07D333/38 , A61P37/00 , A61P29/00 , A61P35/00 , A61P19/02 , A61P17/06 , A61P1/00 , A61P1/04 , A61P3/10 , A61P25/28 , C12N9/99
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are IKK inhibitors useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; A is an optionally substituted aryl or heteroaryl of 5-13 ring atoms; Z is a radical of formula R1C(R2)(R3)NH—Y-L1-X1-(CH2)z— wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular esterase enzymes to a carboxylic acid group; and R2 and R3 independently represent the side chain of a natural or non-natural alpha amino acid but neither of R2 and R3 is hydrogen, or R2 and R3 taken together with the carbon atom to which they are attached form a C3-C7 cycloalkyl ring, and z, Y, L1 and X1 are as defined in the claims.
摘要翻译：式（IA）或（IB）化合物是可用于治疗自身免疫性和炎性疾病的IKK抑制剂：其中R 7是氢或任选取代的（C 1 -C 6）烷基; A是任选取代的5-13个环原子的芳基或杂芳基; Z是式R1C（R2）（R3）NH-Y-L1-X1-（CH2）z-的基团，其中R1是羧酸基（-COOH）或可被一个或多个细胞内可水解的酯基酯酶到羧酸基团; 并且R 2和R 3独立地表示天然或非天然α氨基酸的侧链，但R 2和R 3都不是氢，或者R 2和R 3与它们所连接的碳原子一起形成C 3 -C 7环烷基环，z，Y，L1和X1如权利要求中所定义。

3. 发明授权

US6093716A Substituted 2-pyrimidineamines and processes for their preparation 失效
标题翻译：取代的2-嘧啶胺及其制备方法
公开(公告)号：US6093716A
公开(公告)日：2000-07-25
申请号：US931271
申请日：1997-09-15
申请人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
发明人： Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
IPC分类号： A61K31/506 , A61P1/04 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/00 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/505 , C07D401/12 , C07D403/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14
摘要： Compounds of general formula (1): ##STR1## are described wherein Het is an optionally substituted heteroaromatic group; R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group; R.sup.2 is a hydrogen or halogen atom or a group --X.sup.1 --R.sup.2a where X.sup.1 is a direct bond or a linker atom or group, and R.sup.2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.3 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein kinase inhibitors, particularly the kinases p56.sup.lck, ZAP-70 and protein kinase C and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to have a role.
摘要翻译：描述通式（1）的化合物：其中Het是任选取代的杂芳基; R1是氢原子或直链或支链烷基; R2是氢或卤素原子或-X1-R2a，其中X1是直接键或连接原子或基团，R2a是任选取代的直链或支链烷基，烯基或炔基; R3是任选取代的芳族或杂芳族基团; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是选择性蛋白激酶抑制剂，特别是激酶p56lck，ZAP-70和蛋白激酶C，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的蛋白激酶作用具有作用的其它疾病。

4. 发明授权

US6057329A Fused polycyclic 2-aminopyrimidine derivatives 失效
标题翻译：稠合多环2-氨基嘧啶衍生物
公开(公告)号：US6057329A
公开(公告)日：2000-05-02
申请号：US997174
申请日：1997-12-22
申请人： Jeremy Martin Davis , Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
发明人： Jeremy Martin Davis , Peter David Davis , David Festus Charles Moffat , Mark James Batchelor
IPC分类号： A61K31/517 , A61P1/04 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/06 , C07D239/70 , C07D239/84 , C07D401/12 , C07D403/12 , C07D471/04 , C07D495/04 , C07D487/04
CPC分类号： C07D401/12 , C07D239/70 , C07D471/04 , C07D495/04
摘要： Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.
摘要翻译：式（1）的稠合多环2-氨基嘧啶：其中Ar是任选取代的芳族或杂芳族基团; X是碳原子或氮原子; Y是碳或氮原子; Z是连接基团; A与X和Y一起形成任选取代的单环或双环芳族或杂芳基; 并描述了其盐，溶剂合物，水合物和N-氧化物。这些化合物是蛋白酪氨酸激酶p56lck和p59fyn的有效和选择性抑制剂，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的p56lck和/或p59fyn活性具有作用的其它疾病。

5. 发明授权

US5922741A 5-aminopyrazoles useful as tyrosine kinase inhibitors 失效
标题翻译： 5-氨基吡唑可用作酪氨酸激酶抑制剂
公开(公告)号：US5922741A
公开(公告)日：1999-07-13
申请号：US839211
申请日：1997-04-22
申请人： Peter David Davis , Jeremy Martin Davis , David Festus Charles Moffat
发明人： Peter David Davis , Jeremy Martin Davis , David Festus Charles Moffat
IPC分类号： A61K31/00 , A61K31/415 , A61K31/4155 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61P11/00 , A61P11/06 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07D231/12 , C07D231/38 , C07D401/04 , C07D405/04 , C07D409/04 , C07D401/06
CPC分类号： C07D231/38 , C07D401/04 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (1) are described: ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X.sup.1 is an oxygen or sulphur atom;R.sup.1 is a hydrogen atom or a methyl group;R.sup.2 is a hydrogen atom or a group --Alk.sup.1 or --X.sup.2 Alk.sup.1 where Alk.sup.1 is an optionally substituted aliphatic or heteroaliphatic group and X.sup.2 is a --C(O)--, --C(S)--, or --S(O).sub.n group where n is an integer 1 or 2;R.sup.3 is a hydrogen atom or a group --Alk.sup.2, �where Alk.sup.2 is as defined for Alk.sup.1 !, --X.sup.2 Alk.sup.2, --Ar.sup.1 �where Ar.sup.1 is an optionally substituted aromatic or heteroaromatic group!, --Alk.sup.2 Ar.sup.1, or --X.sup.2 Alk.sup.2 Ar.sup.1 ;and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective inhibitors of the protein tyrosine kinase p56.sup.lck and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck activity is believed to have a role.
摘要翻译：描述通式（1）的化合物：其中Ar是任选取代的芳族或杂芳族基团; X1是氧或硫原子; R1是氢原子或甲基; R2是氢原子或基团-Alk1或-X2Alk1，其中Alk1是任选取代的脂族或杂脂族基团，X 2是-C（O） - ， - C（S） - 或-S（O）n基团，其中 n是整数1或2; R3是氢原子或基团-Alk2 [其中Alk2如Alk1所定义]，-X2Alk2，-Ar1 [其中Ar1是任选取代的芳族或杂芳族基团]，-Alk2Ar1或-X2Alk2Ar1; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是蛋白酪氨酸激酶p56lck的选择性抑制剂，并且可用于预防和治疗免疫疾病，过度增殖性疾病和其中认为不适当的p56lck活性具有作用的其它疾病。

6. 发明授权

US08148531B2 Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
标题翻译：喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂
公开(公告)号：US08148531B2
公开(公告)日：2012-04-03
申请号：US11918898
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
IPC分类号： C07D215/00
CPC分类号： C07D215/42 , C07D215/233 , C07D215/36 , C07D215/44 , C07D239/90 , C07D239/94 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or —NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; 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-C7 cycloalkyl, 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 D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.
摘要翻译：式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（= O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q为≡N-，═CH-或≡C（X1） - 其中X1为氰基，环丙基或卤素; 连接基团L2如权利要求中所定义; 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，C 3 -C 7环烷基，芳基，芳基（C 1 -C 6烷基） - ，杂芳基，杂芳基（C 1 -C 6烷基） - ，（C = O）R 3， - （C = O）OR 3 ，或 - （C = O）NR 3，其中R3是氢或任选取代的（C1-C6）烷基，C3-C7环烷基，芳基，芳基（C1-C6烷基） - ，杂芳基或杂芳基（C1-C6烷基） ; R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。

7. 发明申请

US20110039920A1 INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE 审中-公开
标题翻译： IKK-BETA丝氨酸蛋白激酶激酶的抑制剂
公开(公告)号：US20110039920A1
公开(公告)日：2011-02-17
申请号：US12989022
申请日：2008-04-23
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
IPC分类号： A61K31/381 , C07D333/38 , C12N9/99 , A61P35/00 , A61P37/06 , A61P29/00 , A61P19/02 , A61P3/10 , A61P11/06 , A61P1/04 , A61P25/28
CPC分类号： C07D333/38
摘要： Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5(carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl(2S,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl O-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and tert-Butyl N-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
摘要翻译：（2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5（氨基甲酰基氨基）-2-噻吩基]苯基}戊-4-烯酸酯; 5- {3- [4-氨甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-降冰片烯环戊酯; （2S，4E）-2-氨基-5- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -5-甲基苯基}戊-4-烯酸酯; 环戊基（25,4E）-2-氨基-5- {5- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基] -2-甲基苯基}戊-4-烯酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; 环戊基O- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苯基} -L-高丝氨酸酯; N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸酯的环戊基酯; 和N- {3- [4-氨基甲酰基-5-（氨基甲酰基氨基）-2-噻吩基]苄基} -L-丙氨酸叔丁酯通过细胞内羧酸酯酶水解成相应的羧酸，并且可用于抑制IKK和bgr; 活动。

8. 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。

9. 发明申请

US20090131461A1 Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity 失效
标题翻译：喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂
公开(公告)号：US20090131461A1
公开(公告)日：2009-05-21
申请号：US11918898
申请日：2006-05-04
申请人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
发明人： Alan Hornsby Davidson , Stephen John Davies , David Festus Charles Moffat
IPC分类号： A61K31/517 , C07D215/20 , A61K31/47 , C07D401/02 , A61P35/00 , A61P37/00 , A61K31/506 , C07D239/72
CPC分类号： C07D215/42 , C07D215/233 , C07D215/36 , C07D215/44 , C07D239/90 , C07D239/94 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X is cyano, cyclopropyl or halo; linker radicals L are as defined in the claims; 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-C7 cycloalkyl, 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 D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.
摘要翻译：式（IA）或（IB）的化合物是极光激酶活性的抑制剂：式（IA），（IB）其中-L1Y1- [CH2] z-是连接基，其中Y1，L1和z如索赔; R6是C1-C4烷氧基，氢或卤素; W表示键，-CH 2 - ， - O - ， - S - ， - S（-O）2 - 或-NR 5 - ，其中R 5是氢或C 1 -C 4烷基; Q是-N-，-CH-或-C（X1） - ，其中X是氰基，环丙基或卤素; 连接基自由基L如权利要求中所定义; 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; 且D为5或6个环原子的单环杂环。

10. 发明授权

US07012076B2 Bicyclic amine derivatives as inhibitors of class 1 receptor tyrosine kinases 失效
标题翻译：双环胺衍生物作为1类受体酪氨酸激酶的抑制剂
公开(公告)号：US07012076B2
公开(公告)日：2006-03-14
申请号：US10239941
申请日：2001-03-29
申请人： David Festus Charles Moffat , Peter David Davis
发明人： David Festus Charles Moffat , Peter David Davis
IPC分类号： C07D239/94 , A61K31/505
CPC分类号： C07D239/94
摘要： Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O2)— or —C(O)— group; R1 is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R1a) group where R1a is as defined for R1 and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.
摘要翻译：描述了式（1）的稠合双环胺，其中Ar是芳基或杂芳基; Y是-S（O）2 - 或-C（O） - 基; R 1是氢或卤素原子或烷基，卤代烷基，烷氧基，卤代烷氧基或氰基; X是氮原子或C（R 1a）基团，其中R 1a如R 1所定义，并且可以相同或不同 ; W和Z各自为碳原子，与U一起形成任选取代的五元或六元单环芳族或杂芳族基团; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物能够抑制1类受体酪氨酸激酶的活性，并且可用于预防和治疗过度增殖性疾病如癌症，牛皮癣，再狭窄，动脉粥样硬化和纤维化。

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