CN104024228B - 咪唑二酮类化合物及其用途 - Google Patents
咪唑二酮类化合物及其用途 Download PDFInfo
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- CN104024228B CN104024228B CN201280052853.9A CN201280052853A CN104024228B CN 104024228 B CN104024228 B CN 104024228B CN 201280052853 A CN201280052853 A CN 201280052853A CN 104024228 B CN104024228 B CN 104024228B
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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- A61K31/4164—1,3-Diazoles
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
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- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
- C07D233/72—Two oxygen atoms, e.g. hydantoin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members 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
- C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin
Abstract
Description
LNCaP(IC50,uM) | 22RV1(IC50,uM) | |
比卡鲁胺 | 18.45 | 30.88 |
实施例1(对照化合物1,即化合物7) | 4.09 | 25.99 |
实施例4(对照化合物2,即化合物17) | 8.93 | 30.56 |
实施例2(化合物11) | 1.37 | 20.76 |
实施例3(化合物15) | 0.36 | 14.96 |
实施例5(化合物19) | 2.07 | 23.37 |
实施例6(化合物21) | 0.99 | 13.43 |
实施例7(化合物24) | 2.20 | 19.72 |
实施例13(化合物44) | 2.74 | 15.55 |
实施例9(化合物29) | 1.86 | 26.51 |
实施例11(化合物36) | 1.75 | 18.93 |
实施例8(化合物27) | 1.01 | 18.69 |
实施例14(化合物45) | 1.50 | 26.92 |
实施例10(化合物31) | 1.49 | 26.71 |
实施例12(化合物41) | 2.42 | 25.82 |
实施例 | LNCaP(IC50,nM) | 22RV1(IC50,nM) |
实施例1(对照化合物1) | <1000 | <2000 |
实施例4(对照化合物2) | <1000 | <2000 |
实施例2(化合物11) | <800 | <1600 |
实施例3(化合物15) | <400 | <1000 |
实施例5(化合物19) | <800 | <1600 |
实施例6(化合物21) | <400 | <1000 |
实施例7(化合物24) | <600 | <1000 |
实施例8(化合物27) | <600 | <1000 |
化合物 | Tmax(h) | Cmax(μg/ml) |
21 | 6.0 | 10.4 |
17 | 6.0 | 8.45 |
Claims (13)
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CN201110418859.0 | 2011-12-14 | ||
CN201280052853.9A CN104024228B (zh) | 2011-12-14 | 2012-12-13 | 咪唑二酮类化合物及其用途 |
PCT/CN2012/086573 WO2013087004A1 (zh) | 2011-12-14 | 2012-12-13 | 咪唑二酮类化合物及其用途 |
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WO2019218979A1 (zh) * | 2018-05-14 | 2019-11-21 | 成都海创药业有限公司 | 一种hc-1119制剂及其制备方法和用途 |
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PL2792674T3 (pl) | 2016-12-30 |
US9346764B2 (en) | 2016-05-24 |
CN104024228A (zh) | 2014-09-03 |
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CN103159680A (zh) | 2013-06-19 |
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CA2859224A1 (en) | 2013-06-20 |
JP2015501820A (ja) | 2015-01-19 |
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CA2859224C (en) | 2019-03-19 |
EP2792674A1 (en) | 2014-10-22 |
JP5933746B2 (ja) | 2016-06-15 |
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EP2792674B1 (en) | 2016-05-25 |
WO2013087004A1 (zh) | 2013-06-20 |
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AU2012350482A1 (en) | 2014-07-10 |
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