CN101065358A - 3-芳基氨基吡啶衍生物 - Google Patents
3-芳基氨基吡啶衍生物 Download PDFInfo
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- CN101065358A CN101065358A CNA2005800406885A CN200580040688A CN101065358A CN 101065358 A CN101065358 A CN 101065358A CN A2005800406885 A CNA2005800406885 A CN A2005800406885A CN 200580040688 A CN200580040688 A CN 200580040688A CN 101065358 A CN101065358 A CN 101065358A
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- alkyl
- fluoro
- iodo
- isonicotinamide
- phenyl amino
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
- C07D295/125—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
- C07D295/13—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Abstract
Description
实施例# | MEK抑制 | IC50[μM]C26 | IC50[μM]A375 | IC50 [μM]Miapaca |
1 | ++ | |||
2 | ++ | |||
3 | ++ | |||
4 | ++ | ++ | n.d. | |
5 | ++ | + | ++ | n.d. |
6 | + | |||
7 | ++ | ++ | ++ | ++ |
8 | ++ | ++ | ++ | ++ |
9 | ++ | + | ++ | n.d. |
10 | ++ | + | ++ | ++ |
11 | ++ | ++ | ++ | ++ |
12 | ++ | ++ | ++ | ++ |
13 | ++ | ++ | ++ | ++ |
14 | ++ | ++ | ++ | ++ |
15 | ++ | ++ | ++ | ++ |
16 | ++ | ++ | ++ | ++ |
17 | ++ | ++ | ++ | ++ |
18 | ++ | ++ | ++ | ++ |
19 | ++ | + | ++ | ++ |
20 | ++ | ++ | ++ | ++ |
21 | ++ | + | ++ | + |
22 | ++ | ++ | ++ | ++ |
23 | ++ | ++ | ++ | ++ |
24 | ++ | ++ | ++ | ++ |
25 | ++ | ++ | ++ | ++ |
26 | ++ | + | ++ | + |
27 | ++ | + | + | + |
28 | ++ | + | ++ | + |
29 | ++ | + | ++ | + |
30 | ++ | ++ | ++ | ++ |
31 | ++ | ++ | ++ | ++ |
32 | ++ | ++ | ++ | ++ |
33 | ++ | ++ | ++ | ++ |
34 | ++ | + | ++ | + |
35 | ++ | ++ | ++ | ++ |
36 | ++ | ++ | ++ | ++ |
37 | ++ | n.d. | n.d. | n.d. |
38 | + | n.d. | n.d. | n.d. |
39 | ++ | ++ | ++ | ++ |
40 | ++ | + | ++ | + |
41 | ++ | ++ | ++ | ++ |
42 | ++ | + | ++ | + |
43 | ++ | + | ++ | + |
44 | ++ | + | ++ | + |
45 | ++ | + | ++ | + |
46 | ++ | + | ++ | + |
47 | ++ | ++ | ++ | ++ |
48 | ++ | ++ | ++ | ++ |
49 | ++ | ++ | ++ | ++ |
50 | ++ | + | ++ | + |
51 | ++ | + | ++ | ++ |
52 | + | n.d. | n.d. | n.d. |
53 | ++ | ++ | ++ | ++ |
54 | + | + | ||
55 | ++ | + | ++ | + |
56 | + | + | ++ | + |
57 | + | n.d. | n.d. | n.d. |
58 | ++ | ++ | ++ | ++ |
59 | + | n.d. | n.d. | n.d. |
60 | ++ | ++ | ++ | ++ |
61 | ++ | + |
62 | ++ | + | ++ | |
63 | ++ | ++ | ||
64 | ++ | + | ++ | + |
65 | ++ | + | ++ | + |
66 | ++ | ++ | ||
67 | ++ | ++ | ++ | ++ |
68 | ++ | ++ | ++ | ++ |
69 | ++ | + | ++ | |
70 | ++ | ++ | ++ | ++ |
71 | ++ | + | ++ | + |
72 | ++ | + | ++ | + |
73 | ++ | |||
74 | ++ | + | ++ | + |
75 | ++ | ++ | ++ | ++ |
76 | ++ | + | ++ | + |
77 | ++ | + | ++ | + |
78 | ++ | + | ++ | |
79 | ++ | ++ | ++ | ++ |
80 | ++ | ++ | + | |
81 | ++ | + | ++ | + |
82 | ++ | + | ++ | + |
83 | ++ | ++ | ++ | ++ |
84 | ++ | + | ++ | |
85 | ++ | + | ++ | + |
86 | ++ | + | ++ | + |
87 | ++ | ++ | + | |
88 | ++ | + | + | + |
89 | + | n.d. | n.d. | n.d. |
90 | ++ | ++ | ++ | ++ |
91 | ++ | + | ++ | + |
92 | ++ | + | ++ | + |
93 | ++ | + | ++ | + |
94 | ++ | + | ||
95 | ++ | |||
96 | ++ | ++ | ++ | ++ |
97 | ++ | ++ | ++ | ++ |
98 | ++ | + | ++ | + |
99 | ++ | + | ++ | + |
100 | ++ | + | ++ | + |
101 | ++ | + | ++ | + |
102 | ++ | + | ++ | + |
103 | ++ | n.d. | n.d. | n.d. |
104 | ++ | n.d. | n.d. | n.d. |
105 | ++ | n.d. | n.d. | n.d. |
106 | ++ | n.d. | n.d. | n.d. |
107 | ++ | n.d. | n.d. | n.d. |
108 | ++ | n.d. | n.d. | n.d. |
109 | ++ | n.d. | n.d. | n.d. |
110 | ++ | n.d. | n.d. | n.d. |
111 | ++ | n.d. | n.d. | n.d. |
112 | ++ | n.d. | n.d. | n.d. |
113 | ++ | n.d. | n.d. | n.d. |
114 | ++ | n.d. | n.d. | n.d. |
115 | ++ | n.d. | n.d. | n.d. |
116 | ++ | n.d. | n.d. | n.d. |
117 | n.d. | n.d. | n.d. | n.d. |
118 | + | n.d. | n.d. | n.d. |
119 | + | n.d. | n.d. | n.d. |
120 | n.d. | n.d. | n.d. | |
121 | ++ | n.d. | n.d. | n.d. |
122 | n.d. | n.d. | n.d. | |
123 | ++ | n.d. | n.d. | n.d. |
124 | ++ | + | n.d. | n.d. |
125 | ++ | n.d. | n.d. | n.d. |
126 | + | n.d. | n.d. | n.d. |
127 | n.d. | n.d. | n.d. | |
128 | ++ | n.d. | n.d. | n.d. |
129 | ++ | n.d. | n.d. | n.d. |
实施例# | HLMt1/2[min] | RLMt1/2[min] | MLMt1/2[min] | Caco A-B | Caco B-A |
4 | ++ | ++ | n.d. | n.d. | n.d. |
9 | +++ | +++ | +++ | + | ++ |
123 | ++ | + | n.d. | n.d. | n.d. |
127 | +++ | +++ | + | ++ | ++ |
128 | +++ | ++ | n.d. | ++ | ++ |
129 | +++ | ++ | +++ | ++ | ++ |
Claims (14)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04024967 | 2004-10-20 | ||
EP04024967.4 | 2004-10-20 | ||
PCT/EP2005/011257 WO2006045514A1 (en) | 2004-10-20 | 2005-10-19 | 3-arylamino pyridine derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101065358A true CN101065358A (zh) | 2007-10-31 |
CN101065358B CN101065358B (zh) | 2015-03-11 |
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Application Number | Title | Priority Date | Filing Date |
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CN200580040688.5A Active CN101065358B (zh) | 2004-10-20 | 2005-10-19 | 3-芳基氨基吡啶衍生物 |
Country Status (22)
Country | Link |
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US (4) | US7956191B2 (zh) |
EP (1) | EP1802579B1 (zh) |
JP (1) | JP5214971B2 (zh) |
KR (1) | KR101318012B1 (zh) |
CN (1) | CN101065358B (zh) |
AR (1) | AR051248A1 (zh) |
AU (1) | AU2005298932B2 (zh) |
BR (1) | BRPI0518192B8 (zh) |
CA (1) | CA2582247C (zh) |
CY (1) | CY1114861T1 (zh) |
DK (1) | DK1802579T3 (zh) |
EA (1) | EA013212B1 (zh) |
ES (1) | ES2444866T3 (zh) |
HK (1) | HK1107347A1 (zh) |
MX (1) | MX2007004781A (zh) |
NO (1) | NO339639B1 (zh) |
PL (1) | PL1802579T3 (zh) |
PT (1) | PT1802579E (zh) |
SI (1) | SI1802579T1 (zh) |
UA (1) | UA94571C2 (zh) |
WO (1) | WO2006045514A1 (zh) |
ZA (1) | ZA200703912B (zh) |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2010068738A1 (en) | 2008-12-10 | 2010-06-17 | Dana-Farber Cancer Institute, Inc. | Mek mutations conferring resistance to mek inhibitors |
WO2011106298A1 (en) | 2010-02-25 | 2011-09-01 | Dana-Farber Cancer Institute, Inc. | Braf mutations conferring resistance to braf inhibitors |
CN102695505A (zh) * | 2009-08-11 | 2012-09-26 | 阿勒根公司 | 用于治疗眼睛病症的异噻唑 |
WO2012130159A1 (zh) * | 2011-03-31 | 2012-10-04 | 中国人民解放军军事医学科学院毒物药物研究所 | 氨基吡啶类衍生物及其用途 |
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