JP2013521281A5 - - Google Patents
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- JP2013521281A5 JP2013521281A5 JP2012556056A JP2012556056A JP2013521281A5 JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5 JP 2012556056 A JP2012556056 A JP 2012556056A JP 2012556056 A JP2012556056 A JP 2012556056A JP 2013521281 A5 JP2013521281 A5 JP 2013521281A5
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- Prior art keywords
- cancer
- alkyl
- compound
- haloalkyl
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 19
- 201000011510 cancer Diseases 0.000 claims 14
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 4
- 206010025650 Malignant melanoma Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 201000001441 melanoma Diseases 0.000 claims 3
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 2
- HRYJJMQDEVGSAQ-UHFFFAOYSA-N [2-(4-bromophenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(Br)=CC=2)=C1 HRYJJMQDEVGSAQ-UHFFFAOYSA-N 0.000 claims 2
- XDODKXXXAHTIRD-UHFFFAOYSA-N [2-(4-chlorophenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(Cl)=CC=2)=C1 XDODKXXXAHTIRD-UHFFFAOYSA-N 0.000 claims 2
- NQHVDNDKHQBFKP-UHFFFAOYSA-N [2-(4-methylphenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(NC=2)C=2C=CC(C)=CC=2)=C1 NQHVDNDKHQBFKP-UHFFFAOYSA-N 0.000 claims 2
- 125000004432 carbon atoms Chemical group C* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229940079593 drugs Drugs 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 239000004215 Carbon black (E152) Substances 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010024324 Leukaemias Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- -1 O-alkyl Inorganic materials 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- AAXZBPGIFMJMRG-UHFFFAOYSA-N [1-methyl-2-(4-methylphenyl)imidazol-4-yl]-(3,4,5-trimethoxyphenyl)methanone Chemical compound COC1=C(OC)C(OC)=CC(C(=O)C=2N=C(N(C)C=2)C=2C=CC(C)=CC=2)=C1 AAXZBPGIFMJMRG-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002430 hydrocarbons Chemical class 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 201000001514 prostate carcinoma Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 0 CS1*CCC1 Chemical compound CS1*CCC1 0.000 description 1
Claims (17)
- 下記の構造式(II)で表される化合物。
R1、R2、R3、R4、R5、およびR6は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
R10およびR11は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
Xは、単結合、炭素数1〜5の炭化水素、SまたはOであり;
Yは、単結合、−C=O、−C=S、−C=N−NH2、−C=N−OH、−CH−OH、−C=CH−CN、−C=N−CN、−CH=CH−、−C=C(CH3)2、−C=N−OMe、−(C=O)−NH、−NH−(C=O)、-(C=O)−O、−O−(C=O)、−(CH2)1−5−(C=O)、(C=O)−(CH2)1−5、−(SO2)−NH−、−NH−(SO2)−、SO2、SO、またはSであり;
iは、0〜5の整数であり;
lは、1〜2の整数であり;
nは、1〜3の整数であり;
mは、1〜3の整数である。 - 請求項1に記載の化合物であって、
下記の構造式Vで表される化合物であることを特徴とする化合物。
R4、R5、およびR6は、互いに独立して、水素、O−アルキル、O−ハロアルキル、F、Cl、Br、I、ハロアルキル、CF3、CN、−CH2CN、NH2、ヒドロキシル、−(CH2)iNHCH3、−(CH2)iNH2、−(CH2)iN(CH3)2、−OC(O)CF3、炭素数1〜5の直鎖もしくは分岐鎖のアルキル、ハロアルキル、アルキルアミノ、アミノアルキル、−OCH2Ph、−NHCO−アルキル、COOH、−C(O)Ph、C(O)O−アルキル、C(O)H、−C(O)NH2、またはNO2であり;
nは、1〜3の整数である。 - 請求項3に記載の化合物であって、
前記R3が、FまたはClであることを特徴とする化合物。 - 請求項3に記載の化合物であって、
前記R4が、ClまたはOCH 3 であることを特徴とする化合物。 - 請求項3に記載の化合物であって、
前記R5が水素であることを特徴とする化合物。 - 請求項1〜7のいずれかに記載の化合物、またはその異性体、薬学的に許容される塩、医薬品、互変異性体、水和物、N−酸化物あるいはそれらの組み合わせ。
- 請求項8に記載の化合物および薬学的に許容される担体を含む医薬組成物。
- 請求項8に記載の化合物を、癌の処置に有効な条件の下で癌を患う被検体に投与することを含む、癌の処置、抑制、重症度軽減、リスク軽減、または阻害の方法。
- 請求項10に記載の方法であって、
前記癌が、前立腺癌、乳癌、卵巣癌、皮膚癌、メラノーマ、肺癌、大腸癌、白血病、腎臓癌、CNS癌、およびそれらの組み合わせからなる群から選択されることを特徴とする方法。 - 請求項11に記載の方法であって、
前記癌が、メラノーマ癌、転移性メラノーマ癌、前立腺癌または卵巣癌であることを特徴とする方法。 - 請求項10に記載の方法であって、
前記投与が別の癌治療との併用で行われることを特徴とする方法。 - 請求項8に記載の化合物を、薬剤耐性腫瘍の処置に有効な条件の下で癌を患う被検体に投与することを含む、薬剤耐性腫瘍を処置する方法。
- 請求項14に記載の方法であって、
前記腫瘍が、メラノーマ癌腫瘍、転移性メラノーマ腫瘍、前立腺癌腫または卵巣癌腫瘍であることを特徴とする方法。 - 請求項14に記載の方法であって、
前記投与が別の癌治療との併用で行われることを特徴とする方法。 - 請求項8に記載の化合物を提供すること、および癌細胞の死滅に有効な条件の下で癌細胞を化合物に接触させることを含む、癌性細胞を破壊する方法。
Applications Claiming Priority (7)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30936010P | 2010-03-01 | 2010-03-01 | |
US61/309,360 | 2010-03-01 | ||
US31579010P | 2010-03-19 | 2010-03-19 | |
US61/315,790 | 2010-03-19 | ||
US37667510P | 2010-08-24 | 2010-08-24 | |
US61/376,675 | 2010-08-24 | ||
PCT/US2010/062418 WO2011109059A1 (en) | 2010-03-01 | 2010-12-29 | Compounds for treatment of cancer |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2013521281A JP2013521281A (ja) | 2013-06-10 |
JP2013521281A5 true JP2013521281A5 (ja) | 2014-02-20 |
JP5879273B2 JP5879273B2 (ja) | 2016-03-08 |
Family
ID=44542481
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012556056A Expired - Fee Related JP5879273B2 (ja) | 2010-03-01 | 2010-12-29 | 癌を処置するための化合物 |
Country Status (11)
Country | Link |
---|---|
US (1) | US9334242B2 (ja) |
EP (2) | EP2542081A4 (ja) |
JP (1) | JP5879273B2 (ja) |
KR (2) | KR20120130777A (ja) |
CN (2) | CN104592205A (ja) |
AU (1) | AU2010347233B2 (ja) |
CA (1) | CA2791738C (ja) |
IL (3) | IL221710A (ja) |
MX (1) | MX2012010115A (ja) |
RU (1) | RU2581367C2 (ja) |
WO (1) | WO2011109059A1 (ja) |
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