BG107959A - Заместени производни на триазол диамин като киназни инхибитори - Google Patents

Info

Publication number

BG107959A

BG107959A BG107959A BG10795903A BG107959A BG 107959 A BG107959 A BG 107959A BG 107959 A BG107959 A BG 107959A BG 10795903 A BG10795903 A BG 10795903A BG 107959 A BG107959 A BG 107959A

Authority

BG

Bulgaria

Prior art keywords

alkyl

group

amino

substituted

independently selected

Prior art date

2000-12-22

Links

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• 229940043355 kinase inhibitor Drugs 0.000 title abstract description 14
• 239000003757 phosphotransferase inhibitor Substances 0.000 title description 4
• 108091000080 Phosphotransferase Proteins 0.000 claims abstract description 97
• 102000020233 phosphotransferase Human genes 0.000 claims abstract description 97
• 238000000034 method Methods 0.000 claims abstract description 75
• 230000001404 mediated effect Effects 0.000 claims abstract description 18
• 125000000217 alkyl group Chemical group 0.000 claims description 624
• 125000001424 substituent group Chemical group 0.000 claims description 492
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 374
• 150000001875 compounds Chemical class 0.000 claims description 292
• 229910052739 hydrogen Inorganic materials 0.000 claims description 273
• 239000001257 hydrogen Substances 0.000 claims description 270
• 125000003118 aryl group Chemical group 0.000 claims description 223
• 125000001072 heteroaryl group Chemical group 0.000 claims description 223
• 125000000623 heterocyclic group Chemical group 0.000 claims description 201
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 199
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 168
• 229910052799 carbon Inorganic materials 0.000 claims description 150
• 125000004093 cyano group Chemical group *C#N 0.000 claims description 146
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 145
• 125000001475 halogen functional group Chemical group 0.000 claims description 112
• 125000004432 carbon atom Chemical group C* 0.000 claims description 105
• 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 95
• 125000003545 alkoxy group Chemical group 0.000 claims description 80
• 125000003342 alkenyl group Chemical group 0.000 claims description 77
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 59
• 125000000304 alkynyl group Chemical group 0.000 claims description 51
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 42
• 150000001335 aliphatic alkanes Chemical class 0.000 claims description 33
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 28
• KLSJWNVTNUYHDU-UHFFFAOYSA-N Amitrole Chemical compound NC1=NC=NN1 KLSJWNVTNUYHDU-UHFFFAOYSA-N 0.000 claims description 25
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 25
• 239000008194 pharmaceutical composition Substances 0.000 claims description 25
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• 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 16
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• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 9
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• 229910052757 nitrogen Inorganic materials 0.000 claims description 8
• 125000003626 1,2,4-triazol-1-yl group Chemical group [*]N1N=C([H])N=C1[H] 0.000 claims description 7
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• YAMHXTCMCPHKLN-UHFFFAOYSA-N imidazolidin-2-one Chemical compound O=C1NCCN1 YAMHXTCMCPHKLN-UHFFFAOYSA-N 0.000 claims description 6
• 230000004614 tumor growth Effects 0.000 claims description 6
• 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 5
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• 125000001541 3-thienyl group Chemical group S1C([H])=C([*])C([H])=C1[H] 0.000 claims description 2
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• 150000002431 hydrogen Chemical group 0.000 claims 50
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• 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
• VVGOTCALTHQXFY-UHFFFAOYSA-N 4-[[5-amino-1-(2-chloro-6-fluorobenzoyl)-1,2,4-triazol-3-yl]amino]benzenesulfonamide Chemical compound N=1N(C(=O)C=2C(=CC=CC=2F)Cl)C(N)=NC=1NC1=CC=C(S(N)(=O)=O)C=C1 VVGOTCALTHQXFY-UHFFFAOYSA-N 0.000 claims 1
• JBOXDNIWQACYPW-UHFFFAOYSA-N 5-amino-n-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carboxamide Chemical compound N=1N(C(=O)NC=2C(=CC=CC=2F)F)C(N)=NC=1NC1=CC=C(S(N)(=O)=O)C=C1 JBOXDNIWQACYPW-UHFFFAOYSA-N 0.000 claims 1
• CWDWFSXUQODZGW-UHFFFAOYSA-N 5-thiazolyl Chemical group [C]1=CN=CS1 CWDWFSXUQODZGW-UHFFFAOYSA-N 0.000 claims 1
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• GVUGOAYIVIDWIO-UFWWTJHBSA-N nepidermin Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C(C)C)C(C)C)C1=CC=C(O)C=C1 GVUGOAYIVIDWIO-UFWWTJHBSA-N 0.000 claims 1
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