TWI510486B - Ｅ１活化酶之抑制劑 - Google Patents

Info

Publication number

TWI510486B

TWI510486B TW096103917A TW96103917A TWI510486B TW I510486 B TWI510486 B TW I510486B TW 096103917 A TW096103917 A TW 096103917A TW 96103917 A TW96103917 A TW 96103917A TW I510486 B TWI510486 B TW I510486B

Authority

TW

Taiwan

Prior art keywords

hydrogen

aliphatic

compound

group

optionally substituted

Prior art date

2006-02-02

Links

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• 108090000790 Enzymes Proteins 0.000 title claims description 61
• 230000003213 activating effect Effects 0.000 title claims description 18
• 239000003112 inhibitor Substances 0.000 title description 21
• 150000001875 compounds Chemical class 0.000 claims description 385
• 125000001931 aliphatic group Chemical group 0.000 claims description 199
• 239000001257 hydrogen Substances 0.000 claims description 187
• 229910052739 hydrogen Inorganic materials 0.000 claims description 187
• 238000000034 method Methods 0.000 claims description 145
• -1 substituted Chemical class 0.000 claims description 134
• 125000003118 aryl group Chemical group 0.000 claims description 102
• 125000001424 substituent group Chemical group 0.000 claims description 91
• 125000001153 fluoro group Chemical group F* 0.000 claims description 90
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 88
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 87
• 125000001072 heteroaryl group Chemical group 0.000 claims description 72
• 125000000217 alkyl group Chemical group 0.000 claims description 68
• 125000000623 heterocyclic group Chemical group 0.000 claims description 64
• 229910052799 carbon Inorganic materials 0.000 claims description 62
• 229910052757 nitrogen Inorganic materials 0.000 claims description 57
• 206010028980 Neoplasm Diseases 0.000 claims description 47
• 150000003839 salts Chemical class 0.000 claims description 46
• 230000000694 effects Effects 0.000 claims description 39
• 125000004433 nitrogen atom Chemical group N* 0.000 claims description 38
• 229920006395 saturated elastomer Polymers 0.000 claims description 35
• 125000005843 halogen group Chemical group 0.000 claims description 33
• 201000011510 cancer Diseases 0.000 claims description 32
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• 238000011282 treatment Methods 0.000 claims description 27
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 26
• 125000004432 carbon atom Chemical group C* 0.000 claims description 25
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• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
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• JWZZKOKVBUJMES-UHFFFAOYSA-N (+-)-Isoprenaline Chemical compound CC(C)NCC(O)C1=CC=C(O)C(O)=C1 JWZZKOKVBUJMES-UHFFFAOYSA-N 0.000 claims description 4
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• HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 claims description 4
• 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims description 4
• 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 4
• 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 4
• 201000011549 stomach cancer Diseases 0.000 claims description 4
• 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 4
• 125000001544 thienyl group Chemical group 0.000 claims description 4
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 3
• 150000005208 1,4-dihydroxybenzenes Chemical class 0.000 claims description 3
• 206010025323 Lymphomas Diseases 0.000 claims description 3
• 208000034578 Multiple myelomas Diseases 0.000 claims description 3
• 125000000609 carbazolyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3NC12)* 0.000 claims description 3
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 3
• 125000001162 cycloheptenyl group Chemical group C1(=CCCCCC1)* 0.000 claims description 3
• 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
• 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims description 3
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
• 125000000522 cyclooctenyl group Chemical group C1(=CCCCCCC1)* 0.000 claims description 3
• 125000000640 cyclooctyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 3
• 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 claims description 3
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• NLUNLVTVUDIHFE-UHFFFAOYSA-N cyclooctylcyclooctane Chemical group C1CCCCCCC1C1CCCCCCC1 NLUNLVTVUDIHFE-UHFFFAOYSA-N 0.000 claims description 2
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