CN105358174A - 具细胞毒性和抗有丝分裂的化合物以及其使用方法 - Google Patents
具细胞毒性和抗有丝分裂的化合物以及其使用方法 Download PDFInfo
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- CN105358174A CN105358174A CN201480027374.0A CN201480027374A CN105358174A CN 105358174 A CN105358174 A CN 105358174A CN 201480027374 A CN201480027374 A CN 201480027374A CN 105358174 A CN105358174 A CN 105358174A
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Abstract
Description
化合物 | EC50(nM) |
A | 4.5 |
B | 59 |
115 | 36 |
C | 1.9 |
118 | 13 |
D | 0.033 |
E | 1.67 |
12 | 0.030 |
13 | 0.038 |
14 | 0.007 |
14 | 0.015 |
15 | 7.604 |
16 | 0.041 |
17 | 0.325 |
18 | 1.358 |
19 | 0.152 |
22 | 0.021 |
47 | 0.261 |
24 | 0.070 |
48 | 0.208 |
23 | 0.031 |
28 | 0.021 |
29 | 0.121 |
30 | 0.109 |
31 | 0.094 |
74 | 0.087 |
25 | 0.050 |
26 | 0.105 |
49 | 2.5 |
50 | 0.171 |
27 | 0.157 |
32 | 0.265 |
76 | 0.328 |
79 | 0.386 |
84 | 1.393 |
80 | 0.389 |
51 | 0.247 |
57 | 0.566 |
58 | 0.816 |
34 | 0.200 |
97 | 1.616 |
44 | 0.114 |
45 | 0.869 |
42 | D.165 |
化合物 | EC50(nM) |
A | 2.1 |
B | 13 |
115 | 172 |
C | 1.3 |
D | 0.06 |
E | 0.79 |
79 | 0.241 |
80 | 0.207 |
化合物 | EC50(nM) |
108 | 0.017 |
110 | 0.031 |
107 | 0.043 |
114 | 0.056 |
112 | 0.064 |
98 | 0.077 |
109 | 0.087 |
91 | 0.109 |
64 | 0.138 |
66 | 0.145 |
93 | 0.196 |
103 | 0.209 |
104 | 0.272 |
95 | 0.288 |
102 | 0.289 |
97 | 0.307 |
68 | 0.337 |
45 | 0.373 |
92 | 0.485 |
72 | 0.531 |
67 | 0.562 |
33 | 0.636 |
88 | 0.641 |
105 | 0.731 |
105 | 0.753 |
35 | 0.832 |
70 | 0.856 |
71 | 1.021 |
62 | 1.195 |
44 | 1.479 |
13 | 1.515 |
69 | 1.564 |
94 | 1.673 |
73 | 2.684 |
96 | 10.260 |
111 | ~0.1178 |
91 | 0.109 |
93 | 0.196 |
95 | 0.288 |
97 | 0.307 |
92 | 0.485 |
88 | 0.641 |
62 | 1.195 |
94 | 1.673 |
96 | 10.260 |
64 | 0.138 |
66 | 0.145 |
103 | 0.209 |
104 | 0.272 |
102 | 0.289 |
68 | 0.337 |
72 | 0.531 |
105 | 0.731 |
105 | 0.753 |
70 | 0.856 |
71 | 1.021 |
69 | 1.564 |
46 | - |
108 | 0.017 |
110 | 0.031 |
107 | 0.043 |
114 | 0.056 |
112 | 0.064 |
98 | 0.077 |
109 | 0.087 |
111 | 0.12 |
97 | 0.307 |
45 | 0.373 |
44 | 1.479 |
67 | 0.562 |
33 | 0.636 |
35 | 0.832 |
72 | 2.684 |
化合物 | EC50(nM) |
107 | 0.043 |
108 | 0.017 |
109 | 0.087 |
110 | 0.031 |
111 | 0.12 |
112 | 0.064 |
114 | 0.056 |
ADC | CAPAN-1 | CAPAN-2 |
T-VC-PABC-77 | 2.035 | - |
C-VC-PABC-77 | - | 0.115 |
Claims (28)
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CN201910125160.1A CN110143999B (zh) | 2013-03-15 | 2014-03-14 | 具细胞毒性和抗有丝分裂的化合物以及其使用方法 |
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US201361792066P | 2013-03-15 | 2013-03-15 | |
US61/792020 | 2013-03-15 | ||
US61/792066 | 2013-03-15 | ||
PCT/US2014/029463 WO2014144871A1 (en) | 2013-03-15 | 2014-03-14 | Cytotoxic and anti-mitotic compounds, and methods of using the same |
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AU (1) | AU2014228489B2 (zh) |
CA (1) | CA2906784C (zh) |
DK (1) | DK2968440T3 (zh) |
EA (1) | EA029818B8 (zh) |
ES (1) | ES2741207T3 (zh) |
HK (2) | HK1220140A1 (zh) |
IL (1) | IL241524B (zh) |
MX (1) | MX368258B (zh) |
MY (1) | MY174813A (zh) |
NZ (1) | NZ711982A (zh) |
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CN106255513A (zh) * | 2013-12-27 | 2016-12-21 | 酵活有限公司 | 用于药物偶联物的含磺酰胺连接系统 |
CN111032676A (zh) * | 2017-08-10 | 2020-04-17 | 大日本住友制药株式会社 | 包含哈米特林衍生物的抗体药物复合物 |
CN111051329A (zh) * | 2017-08-10 | 2020-04-21 | 大日本住友制药株式会社 | 哈米特林衍生物及它们的抗体药物复合物 |
CN113412271A (zh) * | 2019-02-13 | 2021-09-17 | 大日本住友制药株式会社 | 具有半胱氨酸残基的哈米特林衍生物 |
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ES2741207T3 (es) | 2013-03-15 | 2020-02-10 | Zymeworks Inc | Compuestos citotóxicos y antimitóticos, y métodos de uso de los mismos |
JP6615115B2 (ja) | 2013-12-27 | 2019-12-04 | ザイムワークス インコーポレイティド | Var2csa−薬物コンジュゲート |
WO2016041082A1 (en) | 2014-09-17 | 2016-03-24 | CDRD Ventures, Inc. | Cytotoxic and anti-mitotic compounds, and methods of using the same |
GB201416960D0 (en) * | 2014-09-25 | 2014-11-12 | Antikor Biopharma Ltd | Biological materials and uses thereof |
EP3598983A1 (en) | 2014-10-03 | 2020-01-29 | Synaffix B.V. | Sulfamide linker, conjugates thereof, and methods of preparation |
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US10975112B2 (en) | 2015-06-16 | 2021-04-13 | Hangzhou Dac Biotech Co., Ltd. | Linkers for conjugation of cell-binding molecules |
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CN106255513A (zh) * | 2013-12-27 | 2016-12-21 | 酵活有限公司 | 用于药物偶联物的含磺酰胺连接系统 |
CN106255513B (zh) * | 2013-12-27 | 2022-01-14 | 酵活有限公司 | 用于药物偶联物的含磺酰胺连接系统 |
CN111032676A (zh) * | 2017-08-10 | 2020-04-17 | 大日本住友制药株式会社 | 包含哈米特林衍生物的抗体药物复合物 |
CN111051329A (zh) * | 2017-08-10 | 2020-04-21 | 大日本住友制药株式会社 | 哈米特林衍生物及它们的抗体药物复合物 |
CN113412271A (zh) * | 2019-02-13 | 2021-09-17 | 大日本住友制药株式会社 | 具有半胱氨酸残基的哈米特林衍生物 |
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