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1. 发明授权

US08044211B2 P38 MAP kinase inhibitors 有权
标题翻译： P38 MAP激酶抑制剂
公开(公告)号：US08044211B2
公开(公告)日：2011-10-25
申请号：US12299333
申请日：2007-05-01
申请人： David Charles Festus Moffat , Stephane Pintat , Stephen Davies
发明人： David Charles Festus Moffat , Stephane Pintat , Stephen Davies
IPC分类号： C07D213/72 , C07D239/02 , A61K31/505 , A61K31/44
CPC分类号： C07D213/73
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2)z—X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; 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 is the side chain of a natural or non-natural alpha amino acid.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，因此可用于治疗特别是包括类风湿性关节炎和COPD的炎性病症：其中：G是-N =或-CH =; D是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R6是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式-A-（CH2）z-X1-L1-Y-NH-CHR1R2的基团，其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z，Y，L1和X1如说明书中所定义; 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。

2. 发明授权

US08778953B2 Inhibitors of P38 map kinase 有权
标题翻译： P38地图激酶抑制剂
公开(公告)号：US08778953B2
公开(公告)日：2014-07-15
申请号：US12867774
申请日：2009-02-27
申请人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
发明人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
IPC分类号： A01N43/54 , A61K31/505 , A01N43/40 , A61K31/44 , C07D239/02 , C07D213/72
CPC分类号： C07D213/73
摘要： Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; 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 are as defined in the claims.
摘要翻译：式（I）化合物是可用于治疗自身免疫性和炎性疾病的p38 MAP激酶抑制剂：其中：G为-N =或-CH =; D是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R6是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式（IA）的基团; 其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z为0或1; -X1-L1-Y-是连接基或键; 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; 并且R 2和R 3如权利要求中所定义。

3. 发明申请

US20110034520A1 Inhibitors of P38 Map Kinase 有权
标题翻译： P38地图激酶抑制剂
公开(公告)号：US20110034520A1
公开(公告)日：2011-02-10
申请号：US12867774
申请日：2009-02-27
申请人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
发明人： David Festus Charles Moffat , Stephen John Davies , Stephane Pintat
IPC分类号： A61K31/4418 , C07D213/73 , A61P29/00 , A61P37/06 , A61P17/00 , A61P11/00 , A61P11/06 , A61P3/10
CPC分类号： C07D213/73
摘要： Compounds of formula (I) are p38 MAP kinase inhibitors useful for the treatment of autoimmune and inflammatory diseases: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted CrC3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula (IA); wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z is O or 1; —X1-L1-Y— is a linker radical or bond; 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 are as defined in the claims.
摘要翻译：式（I）化合物是可用于治疗自身免疫性和炎性疾病的p38 MAP激酶抑制剂：其中：G为-N =或-CH =; D是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R6是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式（IA）的基团; 其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z为0或1; -X1-L1-Y-是连接基或键; 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; 并且R 2和R 3如权利要求中所定义。

4. 发明申请

US20090099185A1 P38 Map Kinase Inhibitors 有权
标题翻译： P38图激酶抑制剂
公开(公告)号：US20090099185A1
公开(公告)日：2009-04-16
申请号：US12299333
申请日：2007-05-01
申请人： David Charles Festus Moffat , Stephane Pintat , Stephen Davies
发明人： David Charles Festus Moffat , Stephane Pintat , Stephen Davies
IPC分类号： A61K31/4412 , C07D211/76 , C12N9/99 , C07D413/12 , A61K31/5377 , A61P1/00 , A61P17/06 , A61P11/06 , A61P3/10 , A61P19/02 , A61P37/00 , A61P37/06
CPC分类号： C07D213/73
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, and are therefore of utility in the treatment of, inter alia, inflammatory conditions including rheumatoid arthritis and COPD: wherein: G is —N═ or —CH═; D is an optionally substituted divalent mono- or bi-cyclic aryl or heteroaryl radical having 5-13 ring members; R6 is hydrogen or optionally substituted C1-C3 alkyl; P represents hydrogen and U represents a radical of formula (IA); or U represents hydrogen and P represents a radical of formula -A-(CH2), —X1-L1-Y—NH—CHR1R2 wherein A represents an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members; z, Y, L1, and X1 are as defined in the specification; 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 is the side chain of a natural or non-natural alpha amino acid.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，因此可用于治疗特别是炎性病症，包括类风湿性关节炎和COPD：其中：G是-N-或-CH-; D是任选取代的具有5-13个环成员的二价单环或双环芳基或杂芳基; R6是氢或任选取代的C 1 -C 3烷基; P表示氢，U表示式（IA）的基团; 或U表示氢，P表示式-A-（CH2），-X1-L1-Y-NH-CHR1R2的基团，其中A表示任选取代的具有5-13个环成员的二价单环或双环碳环或杂环基; z，Y，L1和X1如说明书中所定义; 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。

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