JP2010513288A5

JP2010513288A5 -

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Publication number: JP2010513288A5
Authority: JP; Japan
Prior art keywords: alkyl; optionally substituted; optionally; pharmaceutical composition; formula
Prior art date: 2007-12-14
Legal status : Granted

Application number

JP2009541420A

Other languages

English (en)

Japanese (ja)

Other versions

JP5311673B2 (ja

JP2010513288A (ja

Filing date

2007-12-14

Publication date

2011-04-28

2007-12-14 Application filed filed Critical

2007-12-14 Priority claimed from PCT/US2007/025751 external-priority patent/WO2008076415A1/en

2010-04-30 Publication of JP2010513288A publication Critical patent/JP2010513288A/ja

2011-04-28 Publication of JP2010513288A5 publication Critical patent/JP2010513288A5/ja

2013-10-09 Application granted granted Critical

2013-10-09 Publication of JP5311673B2 publication Critical patent/JP5311673B2/ja

Status Expired - Fee Related legal-status Critical Current

2027-12-14 Anticipated expiration legal-status Critical

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125000000217 alkyl group Chemical group 0.000 claims description 660
-1 2-fluoro-4-iodophenyl Chemical group 0.000 claims description 509
229910052739 hydrogen Inorganic materials 0.000 claims description 346
239000001257 hydrogen Substances 0.000 claims description 336
150000001875 compounds Chemical class 0.000 claims description 271
125000001072 heteroaryl group Chemical group 0.000 claims description 219
125000003342 alkenyl group Chemical group 0.000 claims description 205
125000000592 heterocycloalkyl group Chemical group 0.000 claims description 198
125000005843 halogen group Chemical group 0.000 claims description 187
125000000753 cycloalkyl group Chemical group 0.000 claims description 177
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 167
125000003118 aryl group Chemical group 0.000 claims description 124
125000004356 hydroxy functional group Chemical group O* 0.000 claims description 119
239000002246 antineoplastic agent Substances 0.000 claims description 106
125000003107 substituted aryl group Chemical group 0.000 claims description 105
229940127089 cytotoxic agent Drugs 0.000 claims description 104
125000000304 alkynyl group Chemical group 0.000 claims description 95
125000004093 cyano group Chemical group *C#N 0.000 claims description 84
XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims description 83
229910052799 carbon Inorganic materials 0.000 claims description 70
125000001188 haloalkyl group Chemical group 0.000 claims description 68
125000003545 alkoxy group Chemical group 0.000 claims description 63
OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 62
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 61
125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 60
206010028980 Neoplasm Diseases 0.000 claims description 56
239000008194 pharmaceutical composition Substances 0.000 claims description 54
150000003839 salts Chemical class 0.000 claims description 52
YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 50
125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 49
125000003710 aryl alkyl group Chemical group 0.000 claims description 42
201000011510 cancer Diseases 0.000 claims description 42
238000011282 treatment Methods 0.000 claims description 41
125000002768 hydroxyalkyl group Chemical group 0.000 claims description 34
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
125000004438 haloalkoxy group Chemical group 0.000 claims description 26
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 22
QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 21
125000004663 dialkyl amino group Chemical group 0.000 claims description 19
125000005415 substituted alkoxy group Chemical group 0.000 claims description 19
125000003282 alkyl amino group Chemical group 0.000 claims description 17
ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 17
229960002930 sirolimus Drugs 0.000 claims description 17
125000000547 substituted alkyl group Chemical group 0.000 claims description 15
125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 14
125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 14
125000004104 aryloxy group Chemical group 0.000 claims description 13
125000002102 aryl alkyloxo group Chemical group 0.000 claims description 12
125000004183 alkoxy alkyl group Chemical group 0.000 claims description 10
201000001441 melanoma Diseases 0.000 claims description 9
125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 9
150000002431 hydrogen Chemical class 0.000 claims description 8
239000012453 solvate Substances 0.000 claims description 8
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206010014733 Endometrial cancer Diseases 0.000 claims description 7
206010014759 Endometrial neoplasm Diseases 0.000 claims description 7
206010033128 Ovarian cancer Diseases 0.000 claims description 7
125000005092 alkenyloxycarbonyl group Chemical group 0.000 claims description 7
206010009944 Colon cancer Diseases 0.000 claims description 6
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206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
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208000015634 Rectal Neoplasms Diseases 0.000 claims description 5
206010041067 Small cell lung cancer Diseases 0.000 claims description 5
125000005098 aryl alkoxy carbonyl group Chemical group 0.000 claims description 5
125000005161 aryl oxy carbonyl group Chemical group 0.000 claims description 5
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125000005170 cycloalkyloxycarbonyl group Chemical group 0.000 claims description 5
208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 5
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201000001275 rectum cancer Diseases 0.000 claims description 5
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206010033701 Papillary thyroid cancer Diseases 0.000 claims description 4
239000003085 diluting agent Substances 0.000 claims description 4
239000000546 pharmaceutical excipient Substances 0.000 claims description 4
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LLAPDLPYIYKTGQ-UHFFFAOYSA-N 1-aminoethyl Chemical group C[CH]N LLAPDLPYIYKTGQ-UHFFFAOYSA-N 0.000 claims description 3
208000001446 Anaplastic Thyroid Carcinoma Diseases 0.000 claims description 3
206010002240 Anaplastic thyroid cancer Diseases 0.000 claims description 3
208000019179 thyroid gland undifferentiated (anaplastic) carcinoma Diseases 0.000 claims description 3
238000006243 chemical reaction Methods 0.000 claims description 2
GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims description 2
239000000203 mixture Substances 0.000 claims 29
GMWFCJXSQQHBPI-UHFFFAOYSA-N azetidin-3-ol Chemical compound OC1CNC1 GMWFCJXSQQHBPI-UHFFFAOYSA-N 0.000 claims 5
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125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 2
125000006306 4-iodophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1I 0.000 claims 1
239000000178 monomer Substances 0.000 claims 1
125000004435 hydrogen atom Chemical class [H]* 0.000 description 163
HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical group ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 description 80
125000000623 heterocyclic group Chemical group 0.000 description 73
238000000034 method Methods 0.000 description 67
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125000004122 cyclic group Chemical group 0.000 description 47
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AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 33
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 30
IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 30
229920006395 saturated elastomer Polymers 0.000 description 29
125000004429 atom Chemical group 0.000 description 27
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150000002367 halogens Chemical class 0.000 description 23
125000002346 iodo group Chemical group I* 0.000 description 23
RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 23
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125000005842 heteroatom Chemical group 0.000 description 22
VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 description 21
125000001309 chloro group Chemical group Cl* 0.000 description 21
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DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 description 21
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125000002619 bicyclic group Chemical group 0.000 description 19
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DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 19
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JP2009541420A 2006-12-14 2007-12-14 Ｍｅｋ阻害剤の使用方法 Expired - Fee Related JP5311673B2 (ja)