JPWO2021229152A5

JPWO2021229152A5 -

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Publication number: JPWO2021229152A5
Authority: JP; Japan
Prior art keywords: compound; methylsulfonyl; methyl; alkyl; pyran
Prior art date: 2024-05-22
Legal status : Pending

Application number

JP2022568879A

Other languages

English (en)

Japanese (ja)

Other versions

JP2023525137A (ja

Publication date

2024-05-22

2021-05-12 Application filed filed Critical

2021-05-12 Priority claimed from PCT/FI2021/050353 external-priority patent/WO2021229152A1/en

2023-06-14 Publication of JP2023525137A publication Critical patent/JP2023525137A/ja

2024-05-22 Publication of JPWO2021229152A5 publication Critical patent/JPWO2021229152A5/ja

Status Pending legal-status Critical Current

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150000001875 compounds Chemical class 0.000 claims 89
125000000217 alkyl group Chemical group 0.000 claims 87
229910052739 hydrogen Inorganic materials 0.000 claims 28
239000001257 hydrogen Substances 0.000 claims 28
125000000623 heterocyclic group Chemical group 0.000 claims 19
150000002431 hydrogen Chemical class 0.000 claims 17
125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 14
125000004448 alkyl carbonyl group Chemical group 0.000 claims 13
229910052736 halogen Inorganic materials 0.000 claims 13
150000002367 halogens Chemical class 0.000 claims 13
150000003839 salts Chemical class 0.000 claims 13
125000004093 cyano group Chemical group *C#N 0.000 claims 12
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
125000003545 alkoxy group Chemical group 0.000 claims 10
-1 hydroxyimino Chemical group 0.000 claims 10
125000005842 heteroatom Chemical group 0.000 claims 9
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
229910052760 oxygen Inorganic materials 0.000 claims 9
229910052717 sulfur Inorganic materials 0.000 claims 9
125000003342 alkenyl group Chemical group 0.000 claims 8
125000001424 substituent group Chemical group 0.000 claims 8
125000004452 carbocyclyl group Chemical group 0.000 claims 6
125000004043 oxo group Chemical group O=* 0.000 claims 6
125000004453 alkoxycarbonyl group Chemical group 0.000 claims 5
229910052799 carbon Inorganic materials 0.000 claims 5
125000004432 carbon atom Chemical group C* 0.000 claims 5
125000005843 halogen group Chemical group 0.000 claims 5
229940123407 Androgen receptor antagonist Drugs 0.000 claims 3
IHSDBSSFCOCMJA-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN(CC34CC3)CC3=C4C=CC=C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN(CC34CC3)CC3=C4C=CC=C3)=CC2=O)CC1)(=O)=O IHSDBSSFCOCMJA-UHFFFAOYSA-N 0.000 claims 3
206010060862 Prostate cancer Diseases 0.000 claims 3
208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
125000004414 alkyl thio group Chemical group 0.000 claims 3
239000003936 androgen receptor antagonist Substances 0.000 claims 3
239000002246 antineoplastic agent Substances 0.000 claims 3
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
238000006467 substitution reaction Methods 0.000 claims 3
RWRDJVNMSZYMDV-SIUYXFDKSA-L (223)RaCl2 Chemical compound Cl[223Ra]Cl RWRDJVNMSZYMDV-SIUYXFDKSA-L 0.000 claims 2
KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
ZYYCRSCMXUBHEB-LFVJCYFKSA-N C/C(/C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=N\O Chemical compound C/C(/C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=N\O ZYYCRSCMXUBHEB-LFVJCYFKSA-N 0.000 claims 2
GARZUKNJHDTIBT-KOEQRZSOSA-N C/C(/C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=N\OC Chemical compound C/C(/C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=N\OC GARZUKNJHDTIBT-KOEQRZSOSA-N 0.000 claims 2
ACLAJZGRFRWAEF-UHFFFAOYSA-N CC(C)(C1=CC=C(COC2=COC(CN3CC4=CC=CC=C4C4(CCCC4)C3)=CC2=O)C=C1)O Chemical compound CC(C)(C1=CC=C(COC2=COC(CN3CC4=CC=CC=C4C4(CCCC4)C3)=CC2=O)C=C1)O ACLAJZGRFRWAEF-UHFFFAOYSA-N 0.000 claims 2
OEWRRAQKDMWOBH-UHFFFAOYSA-N CC(C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=O Chemical compound CC(C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)=O OEWRRAQKDMWOBH-UHFFFAOYSA-N 0.000 claims 2
WSKOWENJNHVKGD-UHFFFAOYSA-N CC(C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)O Chemical compound CC(C1=CC=C(CN(CC(OC=C2OCC(CC3)CCN3S(C)(=O)=O)=CC2=O)C2)C2=C1)O WSKOWENJNHVKGD-UHFFFAOYSA-N 0.000 claims 2
HGMMIAOBWBDUOM-UHFFFAOYSA-N CC(C1=CC=C(COC(C=CC(CN2CC3=CC=CC=C3C2)=C2)=C2S(C)(=O)=O)C=C1)O Chemical compound CC(C1=CC=C(COC(C=CC(CN2CC3=CC=CC=C3C2)=C2)=C2S(C)(=O)=O)C=C1)O HGMMIAOBWBDUOM-UHFFFAOYSA-N 0.000 claims 2
FCUAWCNBHUROAI-UHFFFAOYSA-N CC(C1CCC(COC(C=CC(CN(C2)CC3=C2C=CC=C3)=C2)=C2S(C)(=O)=O)CC1)O Chemical compound CC(C1CCC(COC(C=CC(CN(C2)CC3=C2C=CC=C3)=C2)=C2S(C)(=O)=O)CC1)O FCUAWCNBHUROAI-UHFFFAOYSA-N 0.000 claims 2
229940124297 CDK 4/6 inhibitor Drugs 0.000 claims 2
VWOOTEYAZNLYMC-UHFFFAOYSA-N CS(C(C=C(CN1CC2=CC(C(NO)=N)=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O Chemical compound CS(C(C=C(CN1CC2=CC(C(NO)=N)=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O VWOOTEYAZNLYMC-UHFFFAOYSA-N 0.000 claims 2
PWCOQNFUOHQNED-UHFFFAOYSA-N CS(C(C=C(CN1CC2=CC(C3=NOC=N3)=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O Chemical compound CS(C(C=C(CN1CC2=CC(C3=NOC=N3)=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O PWCOQNFUOHQNED-UHFFFAOYSA-N 0.000 claims 2
NCDSRLYUFHTBGC-UHFFFAOYSA-N CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCC1C(N1CCC1)=O)(=O)=O Chemical compound CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCC1C(N1CCC1)=O)(=O)=O NCDSRLYUFHTBGC-UHFFFAOYSA-N 0.000 claims 2
ARZFKMWMFUFARW-UHFFFAOYSA-N CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O Chemical compound CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O ARZFKMWMFUFARW-UHFFFAOYSA-N 0.000 claims 2
OYMMOSOVTNCBFO-UHFFFAOYSA-N CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C1COC1)(=O)=O)(=O)=O Chemical compound CS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C1COC1)(=O)=O)(=O)=O OYMMOSOVTNCBFO-UHFFFAOYSA-N 0.000 claims 2
LFLJZHQCDNERAQ-UHFFFAOYSA-N CS(C(C=CC(COC(C=CC(CN1CC2=CC=CC=C2C1)=C1)=C1S(C)(=O)=O)=C1)=C1F)(=O)=O Chemical compound CS(C(C=CC(COC(C=CC(CN1CC2=CC=CC=C2C1)=C1)=C1S(C)(=O)=O)=C1)=C1F)(=O)=O LFLJZHQCDNERAQ-UHFFFAOYSA-N 0.000 claims 2
PXFKKUOUTCMVSI-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN(CC3)CC(C=C4)=C3C=C4N3N=CC=C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN(CC3)CC(C=C4)=C3C=C4N3N=CC=C3)=CC2=O)CC1)(=O)=O PXFKKUOUTCMVSI-UHFFFAOYSA-N 0.000 claims 2
SNGMOAXWHNXWTQ-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN3CC4=CC(C(C(F)(F)F)O)=CC=C4C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN3CC4=CC(C(C(F)(F)F)O)=CC=C4C3)=CC2=O)CC1)(=O)=O SNGMOAXWHNXWTQ-UHFFFAOYSA-N 0.000 claims 2
APYUAGDWCLZWRD-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN3CC4=CC(C5=CC=NO5)=CC=C4C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN3CC4=CC(C5=CC=NO5)=CC=C4C3)=CC2=O)CC1)(=O)=O APYUAGDWCLZWRD-UHFFFAOYSA-N 0.000 claims 2
UVVUOQDVSNRHHJ-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN3CC4=CC(C5=NN=CS5)=CC=C4C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN3CC4=CC(C5=NN=CS5)=CC=C4C3)=CC2=O)CC1)(=O)=O UVVUOQDVSNRHHJ-UHFFFAOYSA-N 0.000 claims 2
CQKTUYIKJNOTQO-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN3CC4=CC(C5=NOC=N5)=CC=C4C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN3CC4=CC(C5=NOC=N5)=CC=C4C3)=CC2=O)CC1)(=O)=O CQKTUYIKJNOTQO-UHFFFAOYSA-N 0.000 claims 2
STQMXOLNXHKDAC-UHFFFAOYSA-N CS(N1CCC(COC2=COC(CN3CC4=CC(N5N=CC=C5)=CC=C4C3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC(CN3CC4=CC(N5N=CC=C5)=CC=C4C3)=CC2=O)CC1)(=O)=O STQMXOLNXHKDAC-UHFFFAOYSA-N 0.000 claims 2
ZKSRBKCIKPOFLS-QFIPXVFZSA-N CS(N1CCC(COC2=COC([C@@H](C(F)(F)F)N3CC4=CC=CC=C4CC3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC([C@@H](C(F)(F)F)N3CC4=CC=CC=C4CC3)=CC2=O)CC1)(=O)=O ZKSRBKCIKPOFLS-QFIPXVFZSA-N 0.000 claims 2
HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[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 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 2
108010000817 Leuprolide Proteins 0.000 claims 2
VDCAWELTQHDNAW-UHFFFAOYSA-N N#CC(C=C1)=CN=C1N1CC(COC2=COC(CN3CC4=CC=CC=C4CC3)=CC2=O)C1 Chemical compound N#CC(C=C1)=CN=C1N1CC(COC2=COC(CN3CC4=CC=CC=C4CC3)=CC2=O)C1 VDCAWELTQHDNAW-UHFFFAOYSA-N 0.000 claims 2
206010028980 Neoplasm Diseases 0.000 claims 2
BXKGJOXMCPYETK-UHFFFAOYSA-N O=C1C(OC(C2)CC2(C2)CN2S(C2=CC=CN=C2)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OC(C2)CC2(C2)CN2S(C2=CC=CN=C2)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 BXKGJOXMCPYETK-UHFFFAOYSA-N 0.000 claims 2
FAUZNZJMHGIESQ-UHFFFAOYSA-N O=C1C(OCC2CCN(CC3=NC=CC=N3)CC2)=COC(CN2CC3=CC(C4=NN=CO4)=CC=C3C2)=C1 Chemical compound O=C1C(OCC2CCN(CC3=NC=CC=N3)CC2)=COC(CN2CC3=CC(C4=NN=CO4)=CC=C3C2)=C1 FAUZNZJMHGIESQ-UHFFFAOYSA-N 0.000 claims 2
239000012828 PI3K inhibitor Substances 0.000 claims 2
108010085012 Steroid Receptors Proteins 0.000 claims 2
229940046836 anti-estrogen Drugs 0.000 claims 2
230000001833 anti-estrogenic effect Effects 0.000 claims 2
201000011510 cancer Diseases 0.000 claims 2
201000010099 disease Diseases 0.000 claims 2
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
230000001973 epigenetic effect Effects 0.000 claims 2
239000000328 estrogen antagonist Substances 0.000 claims 2
229960005167 everolimus Drugs 0.000 claims 2
239000003862 glucocorticoid Substances 0.000 claims 2
125000001841 imino group Chemical group [H]N=* 0.000 claims 2
239000003112 inhibitor Substances 0.000 claims 2
GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 claims 2
229960004338 leuprorelin Drugs 0.000 claims 2
229940124302 mTOR inhibitor Drugs 0.000 claims 2
239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
239000002395 mineralocorticoid Substances 0.000 claims 2
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 2
239000003197 protein kinase B inhibitor Substances 0.000 claims 2
229940121896 radiopharmaceutical Drugs 0.000 claims 2
239000012217 radiopharmaceutical Substances 0.000 claims 2
230000002799 radiopharmaceutical effect Effects 0.000 claims 2
229940092814 radium (223ra) dichloride Drugs 0.000 claims 2
102000005969 steroid hormone receptors Human genes 0.000 claims 2
230000010009 steroidogenesis Effects 0.000 claims 2
ASGMFNBUXDJWJJ-JLCFBVMHSA-N (1R,3R)-3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethylcyclopentane-1-carboxamide Chemical compound BrC1=NN(C2=NC(=NC=C21)N[C@H]1C[C@@](CC1)(C(=O)NC)C)C1=CC=C(C=C1)C=1SC(=NN=1)C ASGMFNBUXDJWJJ-JLCFBVMHSA-N 0.000 claims 1
UAOUIVVJBYDFKD-XKCDOFEDSA-N (1R,9R,10S,11R,12R,15S,18S,21R)-10,11,21-trihydroxy-8,8-dimethyl-14-methylidene-4-(prop-2-enylamino)-20-oxa-5-thia-3-azahexacyclo[9.7.2.112,15.01,9.02,6.012,18]henicosa-2(6),3-dien-13-one Chemical compound C([C@@H]1[C@@H](O)[C@@]23C(C1=C)=O)C[C@H]2[C@]12C(N=C(NCC=C)S4)=C4CC(C)(C)[C@H]1[C@H](O)[C@]3(O)OC2 UAOUIVVJBYDFKD-XKCDOFEDSA-N 0.000 claims 1
ABJSOROVZZKJGI-OCYUSGCXSA-N (1r,2r,4r)-2-(4-bromophenyl)-n-[(4-chlorophenyl)-(2-fluoropyridin-4-yl)methyl]-4-morpholin-4-ylcyclohexane-1-carboxamide Chemical compound C1=NC(F)=CC(C(NC(=O)[C@H]2[C@@H](C[C@@H](CC2)N2CCOCC2)C=2C=CC(Br)=CC=2)C=2C=CC(Cl)=CC=2)=C1 ABJSOROVZZKJGI-OCYUSGCXSA-N 0.000 claims 1
SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
GCTFTMWXZFLTRR-GFCCVEGCSA-N (2r)-2-amino-n-[3-(difluoromethoxy)-4-(1,3-oxazol-5-yl)phenyl]-4-methylpentanamide Chemical compound FC(F)OC1=CC(NC(=O)[C@H](N)CC(C)C)=CC=C1C1=CN=CO1 GCTFTMWXZFLTRR-GFCCVEGCSA-N 0.000 claims 1
IUSARDYWEPUTPN-OZBXUNDUSA-N (2r)-n-[(2s,3r)-4-[[(4s)-6-(2,2-dimethylpropyl)spiro[3,4-dihydropyrano[2,3-b]pyridine-2,1'-cyclobutane]-4-yl]amino]-3-hydroxy-1-[3-(1,3-thiazol-2-yl)phenyl]butan-2-yl]-2-methoxypropanamide Chemical compound C([C@H](NC(=O)[C@@H](C)OC)[C@H](O)CN[C@@H]1C2=CC(CC(C)(C)C)=CN=C2OC2(CCC2)C1)C(C=1)=CC=CC=1C1=NC=CS1 IUSARDYWEPUTPN-OZBXUNDUSA-N 0.000 claims 1
YJLIKUSWRSEPSM-WGQQHEPDSA-N (2r,3r,4s,5r)-2-[6-amino-8-[(4-phenylphenyl)methylamino]purin-9-yl]-5-(hydroxymethyl)oxolane-3,4-diol Chemical compound C=1C=C(C=2C=CC=CC=2)C=CC=1CNC1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O YJLIKUSWRSEPSM-WGQQHEPDSA-N 0.000 claims 1
VIJSPAIQWVPKQZ-BLECARSGSA-N (2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-[[(2s)-2-acetamido-5-(diaminomethylideneamino)pentanoyl]amino]-4-methylpentanoyl]amino]-4,4-dimethylpentanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid Chemical compound NC(=N)NCCC[C@@H](C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(C)=O VIJSPAIQWVPKQZ-BLECARSGSA-N 0.000 claims 1
ITOFPJRDSCGOSA-KZLRUDJFSA-N (2s)-2-[[(4r)-4-[(3r,5r,8r,9s,10s,13r,14s,17r)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H](CC[C@]13C)[C@@H]2[C@@H]3CC[C@@H]1[C@H](C)CCC(=O)N[C@H](C(O)=O)CC1=CNC2=CC=CC=C12 ITOFPJRDSCGOSA-KZLRUDJFSA-N 0.000 claims 1
WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
STBLNCCBQMHSRC-BATDWUPUSA-N (2s)-n-[(3s,4s)-5-acetyl-7-cyano-4-methyl-1-[(2-methylnaphthalen-1-yl)methyl]-2-oxo-3,4-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)[C@H](C)N(C(C)=O)C2=CC(C#N)=CC=C2N1CC1=C(C)C=CC2=CC=CC=C12 STBLNCCBQMHSRC-BATDWUPUSA-N 0.000 claims 1
TWYYFYNJOJGNFP-CUXYNZQBSA-N (2s,4r,5s,6s)-2-[(4s,5r)-4-acetyloxy-5-methyl-3-methylidene-6-phenylhexyl]-2-carbamoyl-4-[[(e,4s,6s)-4,6-dimethyloct-2-enoyl]oxymethyl]-5-hydroxy-1,3-dioxane-4,5,6-tricarboxylic acid Chemical compound O1[C@H](C(O)=O)[C@](C(O)=O)(O)[C@](COC(=O)/C=C/[C@@H](C)C[C@@H](C)CC)(C(O)=O)O[C@]1(C(N)=O)CCC(=C)[C@@H](OC(C)=O)[C@H](C)CC1=CC=CC=C1 TWYYFYNJOJGNFP-CUXYNZQBSA-N 0.000 claims 1
QFLWZFQWSBQYPS-AWRAUJHKSA-N (3S)-3-[[(2S)-2-[[(2S)-2-[5-[(3aS,6aR)-2-oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-4-yl]pentanoylamino]-3-methylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-[1-bis(4-chlorophenoxy)phosphorylbutylamino]-4-oxobutanoic acid Chemical compound CCCC(NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CCCCC1SC[C@@H]2NC(=O)N[C@H]12)C(C)C)P(=O)(Oc1ccc(Cl)cc1)Oc1ccc(Cl)cc1 QFLWZFQWSBQYPS-AWRAUJHKSA-N 0.000 claims 1
FNHHVPPSBFQMEL-KQHDFZBMSA-N (3S)-5-N-[(1S,5R)-3-hydroxy-6-bicyclo[3.1.0]hexanyl]-7-N,3-dimethyl-3-phenyl-2H-1-benzofuran-5,7-dicarboxamide Chemical compound CNC(=O)c1cc(cc2c1OC[C@@]2(C)c1ccccc1)C(=O)NC1[C@H]2CC(O)C[C@@H]12 FNHHVPPSBFQMEL-KQHDFZBMSA-N 0.000 claims 1
IWZSHWBGHQBIML-ZGGLMWTQSA-N (3S,8S,10R,13S,14S,17S)-17-isoquinolin-7-yl-N,N,10,13-tetramethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-amine Chemical compound CN(C)[C@H]1CC[C@]2(C)C3CC[C@@]4(C)[C@@H](CC[C@@H]4c4ccc5ccncc5c4)[C@@H]3CC=C2C1 IWZSHWBGHQBIML-ZGGLMWTQSA-N 0.000 claims 1
UDQTXCHQKHIQMH-KYGLGHNPSA-N (3ar,5s,6s,7r,7ar)-5-(difluoromethyl)-2-(ethylamino)-5,6,7,7a-tetrahydro-3ah-pyrano[3,2-d][1,3]thiazole-6,7-diol Chemical compound S1C(NCC)=N[C@H]2[C@@H]1O[C@H](C(F)F)[C@@H](O)[C@@H]2O UDQTXCHQKHIQMH-KYGLGHNPSA-N 0.000 claims 1
OOKAZRDERJMRCJ-KOUAFAAESA-N (3r)-7-[(1s,2s,4ar,6s,8s)-2,6-dimethyl-8-[(2s)-2-methylbutanoyl]oxy-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]-3-hydroxy-5-oxoheptanoic acid Chemical compound C1=C[C@H](C)[C@H](CCC(=O)C[C@@H](O)CC(O)=O)C2[C@@H](OC(=O)[C@@H](C)CC)C[C@@H](C)C[C@@H]21 OOKAZRDERJMRCJ-KOUAFAAESA-N 0.000 claims 1
HUWSZNZAROKDRZ-RRLWZMAJSA-N (3r,4r)-3-azaniumyl-5-[[(2s,3r)-1-[(2s)-2,3-dicarboxypyrrolidin-1-yl]-3-methyl-1-oxopentan-2-yl]amino]-5-oxo-4-sulfanylpentane-1-sulfonate Chemical compound OS(=O)(=O)CC[C@@H](N)[C@@H](S)C(=O)N[C@@H]([C@H](C)CC)C(=O)N1CCC(C(O)=O)[C@H]1C(O)=O HUWSZNZAROKDRZ-RRLWZMAJSA-N 0.000 claims 1
MPDDTAJMJCESGV-CTUHWIOQSA-M (3r,5r)-7-[2-(4-fluorophenyl)-5-[methyl-[(1r)-1-phenylethyl]carbamoyl]-4-propan-2-ylpyrazol-3-yl]-3,5-dihydroxyheptanoate Chemical compound C1([C@@H](C)N(C)C(=O)C2=NN(C(CC[C@@H](O)C[C@@H](O)CC([O-])=O)=C2C(C)C)C=2C=CC(F)=CC=2)=CC=CC=C1 MPDDTAJMJCESGV-CTUHWIOQSA-M 0.000 claims 1
OMBVEVHRIQULKW-DNQXCXABSA-M (3r,5r)-7-[3-(4-fluorophenyl)-8-oxo-7-phenyl-1-propan-2-yl-5,6-dihydro-4h-pyrrolo[2,3-c]azepin-2-yl]-3,5-dihydroxyheptanoate Chemical compound O=C1C=2N(C(C)C)C(CC[C@@H](O)C[C@@H](O)CC([O-])=O)=C(C=3C=CC(F)=CC=3)C=2CCCN1C1=CC=CC=C1 OMBVEVHRIQULKW-DNQXCXABSA-M 0.000 claims 1
YQOLEILXOBUDMU-KRWDZBQOSA-N (4R)-5-[(6-bromo-3-methyl-2-pyrrolidin-1-ylquinoline-4-carbonyl)amino]-4-(2-chlorophenyl)pentanoic acid Chemical compound CC1=C(C2=C(C=CC(=C2)Br)N=C1N3CCCC3)C(=O)NC[C@H](CCC(=O)O)C4=CC=CC=C4Cl YQOLEILXOBUDMU-KRWDZBQOSA-N 0.000 claims 1
STPKWKPURVSAJF-LJEWAXOPSA-N (4r,5r)-5-[4-[[4-(1-aza-4-azoniabicyclo[2.2.2]octan-4-ylmethyl)phenyl]methoxy]phenyl]-3,3-dibutyl-7-(dimethylamino)-1,1-dioxo-4,5-dihydro-2h-1$l^{6}-benzothiepin-4-ol Chemical compound O[C@H]1C(CCCC)(CCCC)CS(=O)(=O)C2=CC=C(N(C)C)C=C2[C@H]1C(C=C1)=CC=C1OCC(C=C1)=CC=C1C[N+]1(CC2)CCN2CC1 STPKWKPURVSAJF-LJEWAXOPSA-N 0.000 claims 1
DEVSOMFAQLZNKR-RJRFIUFISA-N (z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-n'-pyrazin-2-ylprop-2-enehydrazide Chemical compound FC(F)(F)C1=CC(C(F)(F)F)=CC(C2=NN(\C=C/C(=O)NNC=3N=CC=NC=3)C=N2)=C1 DEVSOMFAQLZNKR-RJRFIUFISA-N 0.000 claims 1
KKHFRAFPESRGGD-UHFFFAOYSA-N 1,3-dimethyl-7-[3-(n-methylanilino)propyl]purine-2,6-dione Chemical compound C1=NC=2N(C)C(=O)N(C)C(=O)C=2N1CCCN(C)C1=CC=CC=C1 KKHFRAFPESRGGD-UHFFFAOYSA-N 0.000 claims 1
MHSLDASSAFCCDO-UHFFFAOYSA-N 1-(5-tert-butyl-2-methylpyrazol-3-yl)-3-(4-pyridin-4-yloxyphenyl)urea Chemical compound CN1N=C(C(C)(C)C)C=C1NC(=O)NC(C=C1)=CC=C1OC1=CC=NC=C1 MHSLDASSAFCCDO-UHFFFAOYSA-N 0.000 claims 1
KQZLRWGGWXJPOS-NLFPWZOASA-N 1-[(1R)-1-(2,4-dichlorophenyl)ethyl]-6-[(4S,5R)-4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-5-methylcyclohexen-1-yl]pyrazolo[3,4-b]pyrazine-3-carbonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)[C@@H](C)N1N=C(C=2C1=NC(=CN=2)C1=CC[C@@H]([C@@H](C1)C)N1[C@@H](CCC1)CO)C#N KQZLRWGGWXJPOS-NLFPWZOASA-N 0.000 claims 1
WZZBNLYBHUDSHF-DHLKQENFSA-N 1-[(3s,4s)-4-[8-(2-chloro-4-pyrimidin-2-yloxyphenyl)-7-fluoro-2-methylimidazo[4,5-c]quinolin-1-yl]-3-fluoropiperidin-1-yl]-2-hydroxyethanone Chemical compound CC1=NC2=CN=C3C=C(F)C(C=4C(=CC(OC=5N=CC=CN=5)=CC=4)Cl)=CC3=C2N1[C@H]1CCN(C(=O)CO)C[C@@H]1F WZZBNLYBHUDSHF-DHLKQENFSA-N 0.000 claims 1
YCGQPIRMLGEWMW-UHFFFAOYSA-N 1-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,8-naphthyridin-3-yl]-3-[4-[(dimethylamino)methyl]-2,6-di(propan-2-yl)phenyl]urea;hydrochloride Chemical compound Cl.CC(C)C=1C=C(CN(C)C)C=C(C(C)C)C=1NC(=O)NC=1C(=O)N(CCCC)C2=NC=CC=C2C=1C1=CC=CC(OC)=C1 YCGQPIRMLGEWMW-UHFFFAOYSA-N 0.000 claims 1
SZCBDIVMCGFVPW-UHFFFAOYSA-N 1-[4-(aminomethyl)-2,6-di(propan-2-yl)phenyl]-3-[1-butyl-4-(3-methoxyphenyl)-2-oxo-1,8-naphthyridin-3-yl]urea;hydrochloride Chemical compound Cl.CC(C)C=1C=C(CN)C=C(C(C)C)C=1NC(=O)NC=1C(=O)N(CCCC)C2=NC=CC=C2C=1C1=CC=CC(OC)=C1 SZCBDIVMCGFVPW-UHFFFAOYSA-N 0.000 claims 1
WGFNXGPBPIJYLI-UHFFFAOYSA-N 2,6-difluoro-3-[(3-fluorophenyl)sulfonylamino]-n-(3-methoxy-1h-pyrazolo[3,4-b]pyridin-5-yl)benzamide Chemical compound C1=C2C(OC)=NNC2=NC=C1NC(=O)C(C=1F)=C(F)C=CC=1NS(=O)(=O)C1=CC=CC(F)=C1 WGFNXGPBPIJYLI-UHFFFAOYSA-N 0.000 claims 1
FQMZXMVHHKXGTM-UHFFFAOYSA-N 2-(1-adamantyl)-n-[2-[2-(2-hydroxyethylamino)ethylamino]quinolin-5-yl]acetamide Chemical compound C1C(C2)CC(C3)CC2CC13CC(=O)NC1=CC=CC2=NC(NCCNCCO)=CC=C21 FQMZXMVHHKXGTM-UHFFFAOYSA-N 0.000 claims 1
VCUXVXLUOHDHKK-UHFFFAOYSA-N 2-(2-aminopyrimidin-4-yl)-4-(2-chloro-4-methoxyphenyl)-1,3-thiazole-5-carboxamide Chemical compound ClC1=CC(OC)=CC=C1C1=C(C(N)=O)SC(C=2N=C(N)N=CC=2)=N1 VCUXVXLUOHDHKK-UHFFFAOYSA-N 0.000 claims 1
QEBYEVQKHRUYPE-UHFFFAOYSA-N 2-(2-chlorophenyl)-5-[(1-methylpyrazol-3-yl)methyl]-4-[[methyl(pyridin-3-ylmethyl)amino]methyl]-1h-pyrazolo[4,3-c]pyridine-3,6-dione Chemical compound C1=CN(C)N=C1CN1C(=O)C=C2NN(C=3C(=CC=CC=3)Cl)C(=O)C2=C1CN(C)CC1=CC=CN=C1 QEBYEVQKHRUYPE-UHFFFAOYSA-N 0.000 claims 1
MSSQOQPKGAMUSY-LEAFIULHSA-N 2-[1-[2-[(4r,6s)-8-chloro-6-(2,3-dimethoxyphenyl)-4,6-dihydropyrrolo[1,2-a][4,1]benzoxazepin-4-yl]acetyl]piperidin-4-yl]acetic acid Chemical compound COC1=CC=CC([C@@H]2C3=CC(Cl)=CC=C3N3C=CC=C3[C@@H](CC(=O)N3CCC(CC(O)=O)CC3)O2)=C1OC MSSQOQPKGAMUSY-LEAFIULHSA-N 0.000 claims 1
WGABOZPQOOZAOI-UHFFFAOYSA-N 2-[4-[[(3,5-dimethoxy-4-methylbenzoyl)-(3-phenylpropyl)amino]methyl]phenyl]acetic acid Chemical compound COC1=C(C)C(OC)=CC(C(=O)N(CCCC=2C=CC=CC=2)CC=2C=CC(CC(O)=O)=CC=2)=C1 WGABOZPQOOZAOI-UHFFFAOYSA-N 0.000 claims 1
PYRKKGOKRMZEIT-UHFFFAOYSA-N 2-[6-(2-cyclopropylethoxy)-9-(2-hydroxy-2-methylpropyl)-1h-phenanthro[9,10-d]imidazol-2-yl]-5-fluorobenzene-1,3-dicarbonitrile Chemical compound C1=C2C3=CC(CC(C)(O)C)=CC=C3C=3NC(C=4C(=CC(F)=CC=4C#N)C#N)=NC=3C2=CC=C1OCCC1CC1 PYRKKGOKRMZEIT-UHFFFAOYSA-N 0.000 claims 1
FUYOHIFTPJCYBW-UHFFFAOYSA-N 2-[[3-butylsulfonyl-4-[(1-methylsulfonylpiperidin-4-yl)methoxy]phenyl]methyl]-1,3-dihydroisoindole Chemical compound CCCCS(C(C=C(CN1CC2=CC=CC=C2C1)C=C1)=C1OCC(CC1)CCN1S(C)(=O)=O)(=O)=O FUYOHIFTPJCYBW-UHFFFAOYSA-N 0.000 claims 1
FMKGJQHNYMWDFJ-CVEARBPZSA-N 2-[[4-(2,2-difluoropropoxy)pyrimidin-5-yl]methylamino]-4-[[(1R,4S)-4-hydroxy-3,3-dimethylcyclohexyl]amino]pyrimidine-5-carbonitrile Chemical compound FC(COC1=NC=NC=C1CNC1=NC=C(C(=N1)N[C@H]1CC([C@H](CC1)O)(C)C)C#N)(C)F FMKGJQHNYMWDFJ-CVEARBPZSA-N 0.000 claims 1
VVCMGAUPZIKYTH-VGHSCWAPSA-N 2-acetyloxybenzoic acid;[(2s,3r)-4-(dimethylamino)-3-methyl-1,2-diphenylbutan-2-yl] propanoate;1,3,7-trimethylpurine-2,6-dione Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O.CN1C(=O)N(C)C(=O)C2=C1N=CN2C.C([C@](OC(=O)CC)([C@H](C)CN(C)C)C=1C=CC=CC=1)C1=CC=CC=C1 VVCMGAUPZIKYTH-VGHSCWAPSA-N 0.000 claims 1
YSUIQYOGTINQIN-UZFYAQMZSA-N 2-amino-9-[(1S,6R,8R,9S,10R,15R,17R,18R)-8-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-bis(sulfanylidene)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one Chemical compound NC1=NC2=C(N=CN2[C@@H]2O[C@@H]3COP(S)(=O)O[C@@H]4[C@@H](COP(S)(=O)O[C@@H]2[C@@H]3F)O[C@H]([C@H]4F)N2C=NC3=C2N=CN=C3N)C(=O)N1 YSUIQYOGTINQIN-UZFYAQMZSA-N 0.000 claims 1
TVTJUIAKQFIXCE-HUKYDQBMSA-N 2-amino-9-[(2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-ynyl-1H-purine-6,8-dione Chemical compound NC=1NC(C=2N(C(N(C=2N=1)[C@@H]1O[C@@H]([C@H]([C@H]1O)F)CO)=O)CC#C)=O TVTJUIAKQFIXCE-HUKYDQBMSA-N 0.000 claims 1
LFOIDLOIBZFWDO-UHFFFAOYSA-N 2-methoxy-6-[6-methoxy-4-[(3-phenylmethoxyphenyl)methoxy]-1-benzofuran-2-yl]imidazo[2,1-b][1,3,4]thiadiazole Chemical compound N1=C2SC(OC)=NN2C=C1C(OC1=CC(OC)=C2)=CC1=C2OCC(C=1)=CC=CC=1OCC1=CC=CC=C1 LFOIDLOIBZFWDO-UHFFFAOYSA-N 0.000 claims 1
DFRAKBCRUYUFNT-UHFFFAOYSA-N 3,8-dicyclohexyl-2,4,7,9-tetrahydro-[1,3]oxazino[5,6-h][1,3]benzoxazine Chemical compound C1CCCCC1N1CC(C=CC2=C3OCN(C2)C2CCCCC2)=C3OC1 DFRAKBCRUYUFNT-UHFFFAOYSA-N 0.000 claims 1
QBWKPGNFQQJGFY-QLFBSQMISA-N 3-[(1r)-1-[(2r,6s)-2,6-dimethylmorpholin-4-yl]ethyl]-n-[6-methyl-3-(1h-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine Chemical compound N1([C@H](C)C2=NSC(NC=3C4=NC=C(N4C=C(C)N=3)C3=CNN=C3)=C2)C[C@H](C)O[C@H](C)C1 QBWKPGNFQQJGFY-QLFBSQMISA-N 0.000 claims 1
WFOVEDJTASPCIR-UHFFFAOYSA-N 3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-n-[[2-(trifluoromethyl)phenyl]methyl]benzamide Chemical compound N=1N=C(C=2C=CN=CC=2)N(C)C=1CNC(C=1)=CC=CC=1C(=O)NCC1=CC=CC=C1C(F)(F)F WFOVEDJTASPCIR-UHFFFAOYSA-N 0.000 claims 1
WCDLCPLAAKUJNY-UHFFFAOYSA-N 4-[4-[3-(1h-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidin-6-yl]phenyl]morpholine Chemical compound C1COCCN1C1=CC=C(C2=CN3N=CC(=C3N=C2)C2=CNN=C2)C=C1 WCDLCPLAAKUJNY-UHFFFAOYSA-N 0.000 claims 1
WYFCZWSWFGJODV-MIANJLSGSA-N 4-[[(1s)-2-[(e)-3-[3-chloro-2-fluoro-6-(tetrazol-1-yl)phenyl]prop-2-enoyl]-5-(4-methyl-2-oxopiperazin-1-yl)-3,4-dihydro-1h-isoquinoline-1-carbonyl]amino]benzoic acid Chemical compound O=C1CN(C)CCN1C1=CC=CC2=C1CCN(C(=O)\C=C\C=1C(=CC=C(Cl)C=1F)N1N=NN=C1)[C@@H]2C(=O)NC1=CC=C(C(O)=O)C=C1 WYFCZWSWFGJODV-MIANJLSGSA-N 0.000 claims 1
MPMKMQHJHDHPBE-RUZDIDTESA-N 4-[[(2r)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid Chemical compound O=C([C@@]1(N(CC1)C(=O)C=1C2=CC=CC=C2SC=1)C)N(CCCC(O)=O)CC1=CC=CC(Cl)=C1 MPMKMQHJHDHPBE-RUZDIDTESA-N 0.000 claims 1
RXCVUHMIWHRLDF-HXUWFJFHSA-N 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one Chemical compound ClC1=C2CCN(C(C2=C(C(=C1)[C@@H](C1COC1)OC)Cl)=O)CC=1C(NC(=CC=1OC)C)=O RXCVUHMIWHRLDF-HXUWFJFHSA-N 0.000 claims 1
KUZSBKJSGSKPJH-VXGBXAGGSA-N 5-[(9R)-6-[(3R)-3-methylmorpholin-4-yl]-11-oxa-1,3,5-triazatricyclo[7.4.0.02,7]trideca-2,4,6-trien-4-yl]pyrazin-2-amine Chemical compound C[C@@H]1COCCN1c1nc(nc2N3CCOC[C@H]3Cc12)-c1cnc(N)cn1 KUZSBKJSGSKPJH-VXGBXAGGSA-N 0.000 claims 1
VKLKXFOZNHEBSW-UHFFFAOYSA-N 5-[[3-[(4-morpholin-4-ylbenzoyl)amino]phenyl]methoxy]pyridine-3-carboxamide Chemical compound O1CCN(CC1)C1=CC=C(C(=O)NC=2C=C(COC=3C=NC=C(C(=O)N)C=3)C=CC=2)C=C1 VKLKXFOZNHEBSW-UHFFFAOYSA-N 0.000 claims 1
XFJBGINZIMNZBW-CRAIPNDOSA-N 5-chloro-2-[4-[(1r,2s)-2-[2-(5-methylsulfonylpyridin-2-yl)oxyethyl]cyclopropyl]piperidin-1-yl]pyrimidine Chemical compound N1=CC(S(=O)(=O)C)=CC=C1OCC[C@H]1[C@@H](C2CCN(CC2)C=2N=CC(Cl)=CN=2)C1 XFJBGINZIMNZBW-CRAIPNDOSA-N 0.000 claims 1
RSIWALKZYXPAGW-NSHDSACASA-N 6-(3-fluorophenyl)-3-methyl-7-[(1s)-1-(7h-purin-6-ylamino)ethyl]-[1,3]thiazolo[3,2-a]pyrimidin-5-one Chemical compound C=1([C@@H](NC=2C=3N=CNC=3N=CN=2)C)N=C2SC=C(C)N2C(=O)C=1C1=CC=CC(F)=C1 RSIWALKZYXPAGW-NSHDSACASA-N 0.000 claims 1
FCBOUJYKAGWYQM-DEOSSOPVSA-N 6-[[(2s)-1-hydroxy-3-phenylpropan-2-yl]amino]-n-(2-phenoxyethyl)-2-(3,4,5-trimethoxyphenyl)pyridine-3-carboxamide Chemical compound COC1=C(OC)C(OC)=CC(C=2C(=CC=C(N[C@H](CO)CC=3C=CC=CC=3)N=2)C(=O)NCCOC=2C=CC=CC=2)=C1 FCBOUJYKAGWYQM-DEOSSOPVSA-N 0.000 claims 1
GDUANFXPOZTYKS-UHFFFAOYSA-N 6-bromo-8-[(2,6-difluoro-4-methoxybenzoyl)amino]-4-oxochromene-2-carboxylic acid Chemical compound FC1=CC(OC)=CC(F)=C1C(=O)NC1=CC(Br)=CC2=C1OC(C(O)=O)=CC2=O GDUANFXPOZTYKS-UHFFFAOYSA-N 0.000 claims 1
XASOHFCUIQARJT-UHFFFAOYSA-N 8-methoxy-6-[7-(2-morpholin-4-ylethoxy)imidazo[1,2-a]pyridin-3-yl]-2-(2,2,2-trifluoroethyl)-3,4-dihydroisoquinolin-1-one Chemical compound C(N1C(=O)C2=C(OC)C=C(C=3N4C(=NC=3)C=C(C=C4)OCCN3CCOCC3)C=C2CC1)C(F)(F)F XASOHFCUIQARJT-UHFFFAOYSA-N 0.000 claims 1
MITGKKFYIJJQGL-UHFFFAOYSA-N 9-(4-chlorobenzoyl)-6-methylsulfonyl-2,3-dihydro-1H-carbazol-4-one Chemical compound ClC1=CC=C(C(=O)N2C3=CC=C(C=C3C=3C(CCCC2=3)=O)S(=O)(=O)C)C=C1 MITGKKFYIJJQGL-UHFFFAOYSA-N 0.000 claims 1
IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 1
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ZKSRBKCIKPOFLS-JOCHJYFZSA-N CS(N1CCC(COC2=COC([C@H](C(F)(F)F)N3CC4=CC=CC=C4CC3)=CC2=O)CC1)(=O)=O Chemical compound CS(N1CCC(COC2=COC([C@H](C(F)(F)F)N3CC4=CC=CC=C4CC3)=CC2=O)CC1)(=O)=O ZKSRBKCIKPOFLS-JOCHJYFZSA-N 0.000 claims 1
PKMUHQIDVVOXHQ-HXUWFJFHSA-N C[C@H](C1=CC(C2=CC=C(CNC3CCCC3)S2)=CC=C1)NC(C1=C(C)C=CC(NC2CNC2)=C1)=O Chemical compound C[C@H](C1=CC(C2=CC=C(CNC3CCCC3)S2)=CC=C1)NC(C1=C(C)C=CC(NC2CNC2)=C1)=O PKMUHQIDVVOXHQ-HXUWFJFHSA-N 0.000 claims 1
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LVDRREOUMKACNJ-BKMJKUGQSA-N N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,4-dimethyl-2-oxoquinolin-7-yl)-6-oxopiperidin-3-yl]-2-methylpropane-1-sulfonamide Chemical compound CC(C)CS(=O)(=O)N[C@H]1CCC(=O)N([C@@H]1c1ccc(Cl)cc1)c1ccc2c(C)cc(=O)n(C)c2c1 LVDRREOUMKACNJ-BKMJKUGQSA-N 0.000 claims 1
OPFJDXRVMFKJJO-ZHHKINOHSA-N N-{[3-(2-benzamido-4-methyl-1,3-thiazol-5-yl)-pyrazol-5-yl]carbonyl}-G-dR-G-dD-dD-dD-NH2 Chemical compound S1C(C=2NN=C(C=2)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)NCC(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC(O)=O)C(N)=O)=C(C)N=C1NC(=O)C1=CC=CC=C1 OPFJDXRVMFKJJO-ZHHKINOHSA-N 0.000 claims 1
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UFQYAJNFIAELBT-UHFFFAOYSA-N O=C1C(OC(C2)CC2(CC2)CCN2S(C2=CC=CN=C2)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OC(C2)CC2(CC2)CCN2S(C2=CC=CN=C2)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 UFQYAJNFIAELBT-UHFFFAOYSA-N 0.000 claims 1
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ILHACGIPDRCBIF-UHFFFAOYSA-N O=C1C(OC(C2)CC22CCN(CC3=NC=CC=N3)CC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OC(C2)CC22CCN(CC3=NC=CC=N3)CC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 ILHACGIPDRCBIF-UHFFFAOYSA-N 0.000 claims 1
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UNLMBEVQLBWCHQ-UHFFFAOYSA-N O=C1C(OCC(C2)CC2(C2)CN2C2=NC=CC=N2)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OCC(C2)CC2(C2)CN2C2=NC=CC=N2)=COC(CN2CC3=CC=CC=C3CC2)=C1 UNLMBEVQLBWCHQ-UHFFFAOYSA-N 0.000 claims 1
CAJGGPRXAPEUEV-UHFFFAOYSA-N O=C1C(OCC(C2)CC2(C2)CN2S(C(C=C2)=CC=C2F)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OCC(C2)CC2(C2)CN2S(C(C=C2)=CC=C2F)(=O)=O)=COC(CN2CC3=CC=CC=C3CC2)=C1 CAJGGPRXAPEUEV-UHFFFAOYSA-N 0.000 claims 1
YGGVWOBSULBJLM-UHFFFAOYSA-N O=C1C(OCC(C2)CC2(CC2)CCN2C2=NC=CC=N2)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OCC(C2)CC2(CC2)CCN2C2=NC=CC=N2)=COC(CN2CC3=CC=CC=C3CC2)=C1 YGGVWOBSULBJLM-UHFFFAOYSA-N 0.000 claims 1
LYURXAFKTQDKNA-UHFFFAOYSA-N O=C1C(OCC(C2)CC22CCNCC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OCC(C2)CC22CCNCC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 LYURXAFKTQDKNA-UHFFFAOYSA-N 0.000 claims 1
PIHHUXPREGQUFD-UHFFFAOYSA-N O=C1C(OCC(C2)CC22CNC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 Chemical compound O=C1C(OCC(C2)CC22CNC2)=COC(CN2CC3=CC=CC=C3CC2)=C1 PIHHUXPREGQUFD-UHFFFAOYSA-N 0.000 claims 1
PSUZUBSXHUKJKE-UHFFFAOYSA-N O=C1C(OCC2CCN(CC3=NC=CC=N3)CC2)=COC(CN2C=C(C=C(C=C3)C4=NN=CO4)C3=C2)=C1 Chemical compound O=C1C(OCC2CCN(CC3=NC=CC=N3)CC2)=COC(CN2C=C(C=C(C=C3)C4=NN=CO4)C3=C2)=C1 PSUZUBSXHUKJKE-UHFFFAOYSA-N 0.000 claims 1
VYCPANTWXWVNLQ-UHFFFAOYSA-N O=C1C(OCC2CCNCC2)=COC(CN2CC3=CC(C4=NN=CO4)=CC=C3C2)=C1 Chemical compound O=C1C(OCC2CCNCC2)=COC(CN2CC3=CC(C4=NN=CO4)=CC=C3C2)=C1 VYCPANTWXWVNLQ-UHFFFAOYSA-N 0.000 claims 1
LJOOWESTVASNOG-UFJKPHDISA-N [(1s,3r,4ar,7s,8s,8as)-3-hydroxy-8-[2-[(4r)-4-hydroxy-6-oxooxan-2-yl]ethyl]-7-methyl-1,2,3,4,4a,7,8,8a-octahydronaphthalen-1-yl] (2s)-2-methylbutanoate Chemical compound C([C@H]1[C@@H](C)C=C[C@H]2C[C@@H](O)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)CC1C[C@@H](O)CC(=O)O1 LJOOWESTVASNOG-UFJKPHDISA-N 0.000 claims 1
SPXSEZMVRJLHQG-XMMPIXPASA-N [(2R)-1-[[4-[(3-phenylmethoxyphenoxy)methyl]phenyl]methyl]pyrrolidin-2-yl]methanol Chemical compound C(C1=CC=CC=C1)OC=1C=C(OCC2=CC=C(CN3[C@H](CCC3)CO)C=C2)C=CC=1 SPXSEZMVRJLHQG-XMMPIXPASA-N 0.000 claims 1
PSLUFJFHTBIXMW-WYEYVKMPSA-N [(3r,4ar,5s,6s,6as,10s,10ar,10bs)-3-ethenyl-10,10b-dihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-6-(2-pyridin-2-ylethylcarbamoyloxy)-5,6,6a,8,9,10-hexahydro-2h-benzo[f]chromen-5-yl] acetate Chemical compound O([C@@H]1[C@@H]([C@]2(O[C@](C)(CC(=O)[C@]2(O)[C@@]2(C)[C@@H](O)CCC(C)(C)[C@@H]21)C=C)C)OC(=O)C)C(=O)NCCC1=CC=CC=N1 PSLUFJFHTBIXMW-WYEYVKMPSA-N 0.000 claims 1
SMNRFWMNPDABKZ-WVALLCKVSA-N [[(2R,3S,4R,5S)-5-(2,6-dioxo-3H-pyridin-3-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [[[(2R,3S,4S,5R,6R)-4-fluoro-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-hydroxyphosphoryl]oxy-hydroxyphosphoryl] hydrogen phosphate Chemical compound OC[C@H]1O[C@H](OP(O)(=O)OP(O)(=O)OP(O)(=O)OP(O)(=O)OC[C@H]2O[C@H]([C@H](O)[C@@H]2O)C2C=CC(=O)NC2=O)[C@H](O)[C@@H](F)[C@@H]1O SMNRFWMNPDABKZ-WVALLCKVSA-N 0.000 claims 1
239000004480 active ingredient Substances 0.000 claims 1
125000000676 alkoxyimino group Chemical group 0.000 claims 1
102000001307 androgen receptors Human genes 0.000 claims 1
108010080146 androgen receptors Proteins 0.000 claims 1
125000002619 bicyclic group Chemical group 0.000 claims 1
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
239000012829 chemotherapy agent Substances 0.000 claims 1
229940125904 compound 1 Drugs 0.000 claims 1
229940125773 compound 10 Drugs 0.000 claims 1
229940126543 compound 14 Drugs 0.000 claims 1
229940125876 compound 15a Drugs 0.000 claims 1
229940126212 compound 17a Drugs 0.000 claims 1
229940125782 compound 2 Drugs 0.000 claims 1
229940125810 compound 20 Drugs 0.000 claims 1
229940126086 compound 21 Drugs 0.000 claims 1
229940126208 compound 22 Drugs 0.000 claims 1
229940125846 compound 25 Drugs 0.000 claims 1
229940125851 compound 27 Drugs 0.000 claims 1
229940127204 compound 29 Drugs 0.000 claims 1
229940126214 compound 3 Drugs 0.000 claims 1
229940125877 compound 31 Drugs 0.000 claims 1
229940125878 compound 36 Drugs 0.000 claims 1
229940125807 compound 37 Drugs 0.000 claims 1
229940127573 compound 38 Drugs 0.000 claims 1
229940126540 compound 41 Drugs 0.000 claims 1
229940125936 compound 42 Drugs 0.000 claims 1
229940125844 compound 46 Drugs 0.000 claims 1
229940127271 compound 49 Drugs 0.000 claims 1
229940125898 compound 5 Drugs 0.000 claims 1
229940126545 compound 53 Drugs 0.000 claims 1
229940127113 compound 57 Drugs 0.000 claims 1
229940125900 compound 59 Drugs 0.000 claims 1
229940126179 compound 72 Drugs 0.000 claims 1
229940126082 compound 92a Drugs 0.000 claims 1
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 1
229940127089 cytotoxic agent Drugs 0.000 claims 1
230000001419 dependent effect Effects 0.000 claims 1
BJXYHBKEQFQVES-NWDGAFQWSA-N enpatoran Chemical compound N[C@H]1CN(C[C@H](C1)C(F)(F)F)C1=C2C=CC=NC2=C(C=C1)C#N BJXYHBKEQFQVES-NWDGAFQWSA-N 0.000 claims 1
GWNFQAKCJYEJEW-UHFFFAOYSA-N ethyl 3-[8-[[4-methyl-5-[(3-methyl-4-oxophthalazin-1-yl)methyl]-1,2,4-triazol-3-yl]sulfanyl]octanoylamino]benzoate Chemical compound CCOC(=O)C1=CC(NC(=O)CCCCCCCSC2=NN=C(CC3=NN(C)C(=O)C4=CC=CC=C34)N2C)=CC=C1 GWNFQAKCJYEJEW-UHFFFAOYSA-N 0.000 claims 1
RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
KUCDOJMOTMEEOF-UHFFFAOYSA-N gtpl6345 Chemical compound C1=CC(OC)=CC=C1N1C(=O)C(SC=2C3=C4NCCOC4=CN=2)=C3N=C1 KUCDOJMOTMEEOF-UHFFFAOYSA-N 0.000 claims 1
ZLVXBBHTMQJRSX-VMGNSXQWSA-N jdtic Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@H](C(C)C)NC(=O)[C@@H]2NCC3=CC(O)=CC=C3C2)=CC=CC(O)=C1 ZLVXBBHTMQJRSX-VMGNSXQWSA-N 0.000 claims 1
ZBELDPMWYXDLNY-UHFFFAOYSA-N methyl 9-(4-bromo-2-fluoroanilino)-[1,3]thiazolo[5,4-f]quinazoline-2-carboximidate Chemical compound C12=C3SC(C(=N)OC)=NC3=CC=C2N=CN=C1NC1=CC=C(Br)C=C1F ZBELDPMWYXDLNY-UHFFFAOYSA-N 0.000 claims 1
125000002950 monocyclic group Chemical group 0.000 claims 1
YCJZWBZJSYLMPB-UHFFFAOYSA-N n-(2-chloropyrimidin-4-yl)-2,5-dimethyl-1-phenylimidazole-4-carboxamide Chemical compound CC=1N(C=2C=CC=CC=2)C(C)=NC=1C(=O)NC1=CC=NC(Cl)=N1 YCJZWBZJSYLMPB-UHFFFAOYSA-N 0.000 claims 1
YGBMCLDVRUGXOV-UHFFFAOYSA-N n-[6-[6-chloro-5-[(4-fluorophenyl)sulfonylamino]pyridin-3-yl]-1,3-benzothiazol-2-yl]acetamide Chemical compound C1=C2SC(NC(=O)C)=NC2=CC=C1C(C=1)=CN=C(Cl)C=1NS(=O)(=O)C1=CC=C(F)C=C1 YGBMCLDVRUGXOV-UHFFFAOYSA-N 0.000 claims 1
IOMMMLWIABWRKL-WUTDNEBXSA-N nazartinib Chemical compound C1N(C(=O)/C=C/CN(C)C)CCCC[C@H]1N1C2=C(Cl)C=CC=C2N=C1NC(=O)C1=CC=NC(C)=C1 IOMMMLWIABWRKL-WUTDNEBXSA-N 0.000 claims 1
PIDFDZJZLOTZTM-KHVQSSSXSA-N ombitasvir Chemical compound COC(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)NC1=CC=C([C@H]2N([C@@H](CC2)C=2C=CC(NC(=O)[C@H]3N(CCC3)C(=O)[C@@H](NC(=O)OC)C(C)C)=CC=2)C=2C=CC(=CC=2)C(C)(C)C)C=C1 PIDFDZJZLOTZTM-KHVQSSSXSA-N 0.000 claims 1
239000008194 pharmaceutical composition Substances 0.000 claims 1
229940037129 plain mineralocorticoids for systemic use Drugs 0.000 claims 1
UFUASNAHBMBJIX-UHFFFAOYSA-N propan-1-one Chemical compound CC[C]=O UFUASNAHBMBJIX-UHFFFAOYSA-N 0.000 claims 1
TZSZZENYCISATO-WIOPSUGQSA-N rodatristat Chemical compound CCOC(=O)[C@@H]1CC2(CN1)CCN(CC2)c1cc(O[C@H](c2ccc(Cl)cc2-c2ccccc2)C(F)(F)F)nc(N)n1 TZSZZENYCISATO-WIOPSUGQSA-N 0.000 claims 1
DVWOYOSIEJRHKW-UIRZNSHLSA-M sodium (2S)-2-[[(2S)-2-[[(4,4-difluorocyclohexyl)-phenylmethoxy]carbonylamino]-4-methylpentanoyl]amino]-1-hydroxy-3-[(3S)-2-oxopyrrolidin-3-yl]propane-1-sulfonate Chemical compound FC1(CCC(CC1)C(OC(=O)N[C@H](C(=O)N[C@H](C(S(=O)(=O)[O-])O)C[C@H]1C(NCC1)=O)CC(C)C)C1=CC=CC=C1)F.[Na+] DVWOYOSIEJRHKW-UIRZNSHLSA-M 0.000 claims 1
KSAVQLQVUXSOCR-UHFFFAOYSA-M sodium lauroyl sarcosinate Chemical compound [Na+].CCCCCCCCCCCC(=O)N(C)CC([O-])=O KSAVQLQVUXSOCR-UHFFFAOYSA-M 0.000 claims 1
230000003637 steroidlike Effects 0.000 claims 1
229940037128 systemic glucocorticoids Drugs 0.000 claims 1
FRACPXUHUTXLCX-BELIEFIBSA-N tert-butyl N-{1-[(1S)-1-{[(1R,2S)-1-(benzylcarbamoyl)-1-hydroxy-3-[(3S)-2-oxopyrrolidin-3-yl]propan-2-yl]carbamoyl}-2-cyclopropylethyl]-2-oxopyridin-3-yl}carbamate Chemical compound CC(C)(C)OC(=O)NC1=CC=CN(C1=O)[C@@H](CC2CC2)C(=O)N[C@@H](C[C@@H]3CCNC3=O)[C@H](C(=O)NCC4=CC=CC=C4)O FRACPXUHUTXLCX-BELIEFIBSA-N 0.000 claims 1

JP2022568879A 2020-05-14 2021-05-12 Ｃｙｐ１１ａ１阻害剤 Pending JP2023525137A (ja)