TWI620749B - 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途 - Google Patents

Info

Publication number

TWI620749B

TWI620749B TW103105349A TW103105349A TWI620749B TW I620749 B TWI620749 B TW I620749B TW 103105349 A TW103105349 A TW 103105349A TW 103105349 A TW103105349 A TW 103105349A TW I620749 B TWI620749 B TW I620749B

Authority

TW

Taiwan

Prior art keywords

alkyl

compound

group

cycloalkyl

alkylene

Prior art date

2013-02-21

Links

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• 238000000034 method Methods 0.000 title abstract description 63
• 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title description 61
• 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title description 61
• 150000002390 heteroarenes Chemical class 0.000 title description 2
• 150000001875 compounds Chemical class 0.000 claims abstract description 307
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• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 39
• 201000010099 disease Diseases 0.000 claims abstract description 33
• 230000000694 effects Effects 0.000 claims abstract description 30
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 29
• 102000001253 Protein Kinase Human genes 0.000 claims abstract description 15
• 230000002401 inhibitory effect Effects 0.000 claims abstract description 15
• 108060006633 protein kinase Proteins 0.000 claims abstract description 15
• 230000002062 proliferating effect Effects 0.000 claims abstract description 12
• 230000001105 regulatory effect Effects 0.000 claims abstract description 7
• -1 C 3-6 heterocyclo Chemical group 0.000 claims description 152
• 125000000217 alkyl group Chemical group 0.000 claims description 91
• 229910052757 nitrogen Inorganic materials 0.000 claims description 90
• 125000002947 alkylene group Chemical group 0.000 claims description 71
• 125000001424 substituent group Chemical group 0.000 claims description 66
• 125000003118 aryl group Chemical group 0.000 claims description 63
• 108091007960 PI3Ks Proteins 0.000 claims description 58
• 125000000623 heterocyclic group Chemical group 0.000 claims description 56
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 53
• 150000003839 salts Chemical class 0.000 claims description 45
• 125000004429 atom Chemical group 0.000 claims description 37
• 229910052805 deuterium Inorganic materials 0.000 claims description 36
• 229910052731 fluorine Inorganic materials 0.000 claims description 34
• 229910052801 chlorine Inorganic materials 0.000 claims description 32
• 125000001072 heteroaryl group Chemical group 0.000 claims description 30
• 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims description 27
• 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims description 27
• 125000003545 alkoxy group Chemical group 0.000 claims description 27
• 125000005842 heteroatom Chemical group 0.000 claims description 27
• 229910052717 sulfur Inorganic materials 0.000 claims description 26
• 229910052739 hydrogen Inorganic materials 0.000 claims description 25
• 229940124597 therapeutic agent Drugs 0.000 claims description 25
• 229940079593 drug Drugs 0.000 claims description 24
• 229910052760 oxygen Inorganic materials 0.000 claims description 23
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 20
• 125000001931 aliphatic group Chemical group 0.000 claims description 19
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 18
• MWUXSHHQAYIFBG-UHFFFAOYSA-N Nitric oxide Chemical compound O=[N] MWUXSHHQAYIFBG-UHFFFAOYSA-N 0.000 claims description 18
• 229910052794 bromium Inorganic materials 0.000 claims description 18
• 238000011282 treatment Methods 0.000 claims description 17
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• 239000003795 chemical substances by application Substances 0.000 claims description 14
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 13
• 125000000304 alkynyl group Chemical group 0.000 claims description 13
• 239000000546 pharmaceutical excipient Substances 0.000 claims description 13
• 125000003342 alkenyl group Chemical group 0.000 claims description 11
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 10
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• 229910052799 carbon Inorganic materials 0.000 claims description 10
• 239000003937 drug carrier Substances 0.000 claims description 10
• 239000002671 adjuvant Substances 0.000 claims description 9
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• NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 6
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