ZA200603938B - Pyrazole derivatives as inhibitors of receptor tyroyne kinases - Google Patents
Pyrazole derivatives as inhibitors of receptor tyroyne kinases Download PDFInfo
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- ZA200603938B ZA200603938B ZA200603938A ZA200603938A ZA200603938B ZA 200603938 B ZA200603938 B ZA 200603938B ZA 200603938 A ZA200603938 A ZA 200603938A ZA 200603938 A ZA200603938 A ZA 200603938A ZA 200603938 B ZA200603938 B ZA 200603938B
- Authority
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- South Africa
- Prior art keywords
- amino
- optionally substituted
- alkyl
- methyl
- formula
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- 239000003112 inhibitor Substances 0.000 title description 8
- 150000003217 pyrazoles Chemical class 0.000 title description 8
- 108091000080 Phosphotransferase Proteins 0.000 title description 4
- 102000020233 phosphotransferase Human genes 0.000 title description 4
- -1 nitro, cyano, hydroxy, trifluoromethoxy, amino, carboxy, carbamoyl Chemical group 0.000 claims description 97
- 125000000217 alkyl group Chemical group 0.000 claims description 69
- 125000000623 heterocyclic group Chemical group 0.000 claims description 41
- 150000001875 compounds Chemical class 0.000 claims description 39
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 30
- 229910052757 nitrogen Inorganic materials 0.000 claims description 29
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 29
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 28
- 229910052799 carbon Inorganic materials 0.000 claims description 28
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 28
- 125000005843 halogen group Chemical group 0.000 claims description 22
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 19
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 17
- 229910052739 hydrogen Inorganic materials 0.000 claims description 17
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- 239000001257 hydrogen Substances 0.000 claims description 14
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 11
- 238000004519 manufacturing process Methods 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 11
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- 125000003342 alkenyl group Chemical group 0.000 claims description 5
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- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims description 4
- 125000001584 benzyloxycarbonyl group Chemical group C(=O)(OCC1=CC=CC=C1)* 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 claims description 4
- 238000011321 prophylaxis Methods 0.000 claims description 4
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 3
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 3
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- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims description 3
- 125000001424 substituent group Chemical group 0.000 claims description 3
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- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims description 2
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
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- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 2
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 2
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- 239000000203 mixture Substances 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- YPFDHNVEDLHUCE-UHFFFAOYSA-N propane-1,3-diol Chemical compound OCCCO YPFDHNVEDLHUCE-UHFFFAOYSA-N 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- MAYHUFQBMJUHBX-HNNXBMFYSA-N (2r)-2-[[4-[(5-cyclopropyl-1h-pyrazol-3-yl)amino]-5-fluoropyrimidin-2-yl]amino]-2-(4-fluorophenyl)ethanol Chemical compound N([C@@H](CO)C=1C=CC(F)=CC=1)C(N=1)=NC=C(F)C=1NC(=NN1)C=C1C1CC1 MAYHUFQBMJUHBX-HNNXBMFYSA-N 0.000 claims 1
- ODABQTDWBANHOR-IBGZPJMESA-N (2r)-2-[[4-[(5-cyclopropyl-1h-pyrazol-3-yl)amino]-7-fluoroquinazolin-2-yl]amino]-2-(4-fluorophenyl)ethanol Chemical compound N([C@@H](CO)C=1C=CC(F)=CC=1)C(N=C1C=C(F)C=CC1=1)=NC=1NC(=NN1)C=C1C1CC1 ODABQTDWBANHOR-IBGZPJMESA-N 0.000 claims 1
- FXSOVNSBVDXYOV-HNNXBMFYSA-N (2r)-2-[[5-chloro-4-[(5-cyclopropyl-1h-pyrazol-3-yl)amino]pyrimidin-2-yl]amino]-2-(4-fluorophenyl)ethanol Chemical compound N([C@@H](CO)C=1C=CC(F)=CC=1)C(N=1)=NC=C(Cl)C=1NC(NN=1)=CC=1C1CC1 FXSOVNSBVDXYOV-HNNXBMFYSA-N 0.000 claims 1
- ILROLYQPRYHHFG-UHFFFAOYSA-N 1-$l^{1}-oxidanylprop-2-en-1-one Chemical group [O]C(=O)C=C ILROLYQPRYHHFG-UHFFFAOYSA-N 0.000 claims 1
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 1
- XFGQQCZWCNSYOC-LBPRGKRZSA-N 2-[[5-chloro-2-[[(1s)-1-(4-fluorophenyl)ethyl]amino]-6-[(3-propan-2-yloxy-1h-pyrazol-5-yl)amino]pyrimidin-4-yl]amino]propane-1,3-diol Chemical compound N1C(OC(C)C)=CC(NC=2C(=C(NC(CO)CO)N=C(N[C@@H](C)C=3C=CC(F)=CC=3)N=2)Cl)=N1 XFGQQCZWCNSYOC-LBPRGKRZSA-N 0.000 claims 1
- SWQAOASNZJKPPA-INIZCTEOSA-N 2-[[5-chloro-6-[(5-cyclopropyl-1h-pyrazol-3-yl)amino]-2-[[(1r)-1-(4-fluorophenyl)-2-hydroxyethyl]amino]pyrimidin-4-yl]amino]propane-1,3-diol Chemical compound C1([C@H](CO)NC=2N=C(C(=C(NC3=NNC(=C3)C3CC3)N=2)Cl)NC(CO)CO)=CC=C(F)C=C1 SWQAOASNZJKPPA-INIZCTEOSA-N 0.000 claims 1
- 125000003006 2-dimethylaminoethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims 1
- GMMWNTHAIOJBSD-UHFFFAOYSA-N 6-chloro-4-n-(2,3-dimethylphenyl)-2-n,2-n-dimethylpyrimidine-2,4-diamine Chemical compound CN(C)C1=NC(Cl)=CC(NC=2C(=C(C)C=CC=2)C)=N1 GMMWNTHAIOJBSD-UHFFFAOYSA-N 0.000 claims 1
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Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US52058103P | 2003-11-17 | 2003-11-17 |
Publications (1)
Publication Number | Publication Date |
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ZA200603938B true ZA200603938B (en) | 2007-11-28 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ZA200603938A ZA200603938B (en) | 2003-11-17 | 2006-05-16 | Pyrazole derivatives as inhibitors of receptor tyroyne kinases |
Country Status (3)
Country | Link |
---|---|
CN (1) | CN1905884A (ru) |
UA (1) | UA90254C2 (ru) |
ZA (1) | ZA200603938B (ru) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103242341B (zh) * | 2013-04-19 | 2015-12-09 | 中国科学院广州生物医药与健康研究院 | 噻吩并2,4取代嘧啶类化合物及其药物组合物与应用 |
CN116023380B (zh) * | 2021-10-26 | 2024-01-23 | 沈阳药科大学 | 一类吡唑并嘧啶衍生物及制备方法和应用 |
-
2004
- 2004-11-15 UA UAA200606736A patent/UA90254C2/ru unknown
- 2004-11-15 CN CN 200480040487 patent/CN1905884A/zh active Pending
-
2006
- 2006-05-16 ZA ZA200603938A patent/ZA200603938B/en unknown
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Publication number | Publication date |
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UA90254C2 (ru) | 2010-04-26 |
CN1905884A (zh) | 2007-01-31 |
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