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1. 发明申请

US20100087515A1 IKK-BETA SERINE-THREONINE PROTEIN KINASE INHIBITORS 失效
标题翻译： IKK-BETA丝氨酸蛋白激酶激酶抑制剂
公开(公告)号：US20100087515A1
公开(公告)日：2010-04-08
申请号：US12513206
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
IPC分类号： A61K31/381 , C07D333/38 , C12N9/99 , A61P35/00 , A61P37/00 , A61P29/00 , A61P1/00 , A61P11/00
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; 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; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O)—, —S(═P)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; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7为氢或任选取代的（C1- C6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-的基团，其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= NH）-NR 3或-S（= O）2 NR 3 - ，其中R 3是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

2. 发明授权

US08003695B2 IKK-beta serine-threonine protein kinase inhibitors 失效
标题翻译： IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂
公开(公告)号：US08003695B2
公开(公告)日：2011-08-23
申请号：US12513206
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathan Gareth Williams
IPC分类号： A61K31/381 , C07D333/38
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: Formula (A) and (B) wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is (a) a radical of formula R1R2CHNH—Y-L1-X1—(CH2)z— wherein: z is 0 or 1; 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; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(═O)—, —S(═P)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; L is a divalent linker radical of formula -(Alk1)m(Q)(Alk2)p- wherein m, n, p, Q, AIk1 and AIk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：式（A）和（B）其中R 7为氢或任选取代的（C1- C6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是（a）式R1R2CHNH-Y-L1-X1-（CH2）z-的基团，其中：z为0或1; R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R2是天然或非天然α氨基酸的侧链; Y是键，-C（= O） - ， - S（= O）2 - ， - C（= O）O-，-C（= O）NR 3 - ， - C（= NH）-NR 3或-S（= O）2 NR 3 - ，其中R 3是氢或任选取代的C 1 -C 6烷基; L1是式 - （Alk1）m（Q）（Alk2）p的二价连接基团，其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

3. 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。

4. 发明申请

US20100069473A1 Inhibitors Of IKK-Beta Serine-Threonine Protein Kinase 失效
标题翻译： IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂
公开(公告)号：US20100069473A1
公开(公告)日：2010-03-18
申请号：US12447271
申请日：2007-10-29
申请人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
发明人： David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
IPC分类号： A61K31/381 , C07D333/36 , C12N9/99 , A61P35/00 , A61P37/00 , A61P29/00 , A61P11/00 , A61P17/00 , A61P3/10
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) 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; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; 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)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：其中R 7为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R是式（X）或（Y）的基团，R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R 6是氢或任选取代的C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂芳基或 - （C = O）R 3， - （C = O）OR 3或 - （C = O）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基; Y1是一个键， - （C = O） - ， - S（O 2） - ， - C（= O）O-，-OC（= O） - ， - （C = O）NR 3 - ， - NR 3 （O） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（C = O）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6）式 - （Alk1）m（Q）n（Alk2）p的二价连接基团其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

5. 发明授权

US08106091B2 Inhibitors of IKK-beta serine-threonine protein kinase 失效
标题翻译： IKK-β丝氨酸 - 苏氨酸蛋白激酶抑制剂
公开(公告)号：US08106091B2
公开(公告)日：2012-01-31
申请号：US12447271
申请日：2007-10-29
申请人： David Charles Festus Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
发明人： David Charles Festus Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Stuart Thomas Onions , Jonathon Gareth Williams
IPC分类号： A61K31/381 , C07D333/36
CPC分类号： C07D333/38
摘要： Compounds of formula (IA) or (IB) are inhibitors of IkB kinase (IKK) activity, and are useful in the treatment of autoimmune and inflammatory diseases: wherein R7 is hydrogen or optionally substituted (C1-C6)alkyl; ring A is an optionally substituted aryl or heteroaryl ring of 5-13 ring atoms; Z is a radical of formula R-L1-Y1—(CH2)z—, wherein: z is 0 or 1; R is a radical of formula (X) or (Y) 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; R6 is hydrogen, or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl or heteroaryl or —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl; 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)NR4—, wherein R3 and R4 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent linker radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims.
摘要翻译：式（IA）或（IB）的化合物是IkB激酶（IKK）活性的抑制剂，可用于治疗自身免疫性和炎性疾病：其中R 7为氢或任选取代的（C 1 -C 6）烷基; 环A是任选取代的5-13个环原子的芳基或杂芳基环; Z是式R-L1-Y1-（CH2）z-的基团，其中：z是0或1; R是式（X）或（Y）的基团，R 1是羧酸基团（-COOH）或可被一个或多个细胞内酯酶水解成羧酸基团的酯基; R 6是氢或任选取代的C 1 -C 6烷基，C 3 -C 7环烷基，芳基或杂芳基或 - （C = O）R 3， - （C = O）OR 3或 - （C = O）NR 3，其中R 3是氢或任选取代的（C 1 -C 6）烷基; Y1是一个键， - （C = O） - ， - S（O 2） - ， - C（= O）O-，-OC（= O） - ， - （C = O）NR 3 - ， - NR 3 （O） - ， - S（O 2）NR 3 - ， - NR 3 S（O 2） - 或-NR 3（C = O）NR 4 - ，其中R 3和R 4独立地是氢或任选取代的（C 1 -C 6）式 - （Alk1）m（Q）n（Alk2）p的二价连接基团其中m，n，p，Q，Alk1和Alk2如权利要求中所定义。

6. 发明授权

US08217050B2 Adenine derivative as inhibitors of HSP90 for the treatment of cancer 失效
标题翻译：腺嘌呤衍生物作为HSP90抑制剂治疗癌症
公开(公告)号：US08217050B2
公开(公告)日：2012-07-10
申请号：US12513658
申请日：2007-11-05
申请人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
IPC分类号： C07D473/34 , A61K31/52 , A61P11/06 , A61P37/06 , A61P19/02 , A61P3/10 , A61P17/06 , C07F7/18 , C07F7/10
CPC分类号： C07D473/34
摘要： The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供一种化合物，其为（a）式（I）的氨基酸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，水合物或溶剂合物：其中R1，R2，L1，Het A，x，y和W如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

7. 发明申请

US20100035901A1 ADENINE DERIVATIVE AS INHIBITORS OF HSP90 FOR THE TREATMENT OF CANCER 失效
标题翻译：作为HSP90抑制剂的ADENINE DERIVATIVE作为治疗癌症的药物
公开(公告)号：US20100035901A1
公开(公告)日：2010-02-11
申请号：US12513658
申请日：2007-11-05
申请人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
发明人： David Festus Charles Moffat , Simon Christopher Hirst , Stuart Thomas Onions
IPC分类号： A61K31/52 , C07D473/00
CPC分类号： C07D473/34
摘要： The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
摘要翻译：本发明提供一种化合物，其为（a）式（I）的氨基酸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，水合物或溶剂合物：其中R1，R2，L1，Het A，x，y和W如本文所定义。该化合物可用于治疗由HSP90介导的疾病。

8. 发明申请

US20130012512A1 P38 MAP kinase inhibitors 有权
公开(公告)号：US20130012512A1
公开(公告)日：2013-01-10
申请号：US13616696
申请日：2012-09-14
申请人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
发明人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
IPC分类号： A61K31/4439 , C07D405/14 , C07D413/14 , A61K31/5377 , A61P11/06 , A61K31/496 , C07D403/12 , A61K31/506 , A61K31/4178 , A61P11/00 , C07D401/12 , C07D401/14
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12
摘要： There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.

9. 发明申请

US20110294812A1 P38 MAP KINASE INHIBITORS 有权
标题翻译： P38 MAP激酶抑制剂
公开(公告)号：US20110294812A1
公开(公告)日：2011-12-01
申请号：US13133998
申请日：2009-12-11
申请人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
发明人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
IPC分类号： A61K31/4439 , C07D405/14 , C07D413/14 , C07D401/14 , A61K31/5377 , A61K31/496 , A61P11/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P1/04 , A61P19/02 , A61P29/00 , A61P35/00 , A61P35/04 , C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12
摘要： The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其包括其所有的立体异构体，互变异构体和同位素衍生物，其是p38丝裂原活化蛋白激酶的抑制剂（本文称为p38 MAP激酶抑制剂），特别是其α和γ激酶亚型，以及它们在治疗中的用途，包括药物组合，特别是治疗炎症性疾病，包括肺炎性疾病如COPD。

10. 发明申请

US20110212962A1 P38 MAP KINASE INHIBITORS 有权
标题翻译： P38 MAP激酶抑制剂
公开(公告)号：US20110212962A1
公开(公告)日：2011-09-01
申请号：US13121999
申请日：2009-10-02
申请人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
发明人： Kazuhiro Ito , Peter Strong , William Garth Rapeport , Peter John Murray , John King-Underwood , Jonathan Gareth Williams , Stuart Thomas Onions , Simon Christopher Hirst , David Michel Adrien Taddei , Catherine Elisabeth Charron
IPC分类号： A61K31/5377 , C07D401/12 , C07D405/14 , C07D413/14 , C07D401/14 , C07D403/12 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/4178 , A61P11/00 , A61P11/08 , A61P11/06 , A61P11/02 , A61P17/00 , A61P17/06 , A61P29/00 , A61P1/18 , A61P35/00 , A61P27/14 , A61P35/04 , A61P19/02
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12
摘要： There are provided inter alia compounds of formula (I) wherein R1, Ar, L, X, R3 and Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.
摘要翻译：特别是提供式（I）化合物，其中R 1，Ar，L，X，R 3和Q如在说明书中用于治疗，特别是治疗炎性疾病的说明书中所定义。

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