JP2016540738A5 - - Google Patents

Info

Publication number

JP2016540738A5

JP2016540738A5 JP2016526801A JP2016526801A JP2016540738A5 JP 2016540738 A5 JP2016540738 A5 JP 2016540738A5 JP 2016526801 A JP2016526801 A JP 2016526801A JP 2016526801 A JP2016526801 A JP 2016526801A JP 2016540738 A5 JP2016540738 A5 JP 2016540738A5

Authority

JP

Japan

Prior art keywords

inhibitor

prostate cancer

pharmaceutical composition

composition according

akr1c3

Prior art date

2014-10-27

Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• 206010060862 Prostate cancer Diseases 0.000 claims description 85
• 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 85
• 239000003112 inhibitor Substances 0.000 claims description 76
• 108091008721 AR-V7 Proteins 0.000 claims description 42
• 239000000203 mixture Substances 0.000 claims description 21
• ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 18
• 229960003668 docetaxel Drugs 0.000 claims description 18
• CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical group CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 18
• LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims description 17
• GZOSMCIZMLWJML-VJLLXTKPSA-N abiraterone Chemical compound C([C@H]1[C@H]2[C@@H]([C@]3(CC[C@H](O)CC3=CC2)C)CC[C@@]11C)C=C1C1=CC=CN=C1 GZOSMCIZMLWJML-VJLLXTKPSA-N 0.000 claims description 17
• 229960000853 abiraterone Drugs 0.000 claims description 17
• 229960000997 bicalutamide Drugs 0.000 claims description 17
• WXCXUHSOUPDCQV-UHFFFAOYSA-N enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 claims description 17
• 229960004671 enzalutamide Drugs 0.000 claims description 17
• RJMUSRYZPJIFPJ-UHFFFAOYSA-N niclosamide Chemical group OC1=CC=C(Cl)C=C1C(=O)NC1=CC=C([N+]([O-])=O)C=C1Cl RJMUSRYZPJIFPJ-UHFFFAOYSA-N 0.000 claims description 17
• 229960001920 niclosamide Drugs 0.000 claims description 17
• 150000001875 compounds Chemical class 0.000 claims description 16
• 229940079593 drug Drugs 0.000 claims description 14
• 239000003814 drug Substances 0.000 claims description 14
• 230000002280 anti-androgenic effect Effects 0.000 claims description 13
• 239000000051 antiandrogen Substances 0.000 claims description 13
• 239000003560 cancer drug Substances 0.000 claims description 10
• 229960000905 indomethacin Drugs 0.000 claims description 9
• 230000001225 therapeutic effect Effects 0.000 claims description 9
• 230000008901 benefit Effects 0.000 claims description 6
• 230000001394 metastastic effect Effects 0.000 claims description 4
• 206010061289 metastatic neoplasm Diseases 0.000 claims description 4
• 239000008194 pharmaceutical composition Substances 0.000 claims 19
• 102000004602 Aldo-Keto Reductase Family 1 Member C3 Human genes 0.000 claims 14
• 108010065942 Prostaglandin-F synthase Proteins 0.000 claims 14
• 230000002708 enhancing effect Effects 0.000 claims 1
• 238000000034 method Methods 0.000 description 43
• 108010080146 androgen receptors Proteins 0.000 description 8
• 102000001307 androgen receptors Human genes 0.000 description 8
• 230000002401 inhibitory effect Effects 0.000 description 6
• 239000003183 carcinogenic agent Substances 0.000 description 5
• 102000007066 Prostate-Specific Antigen Human genes 0.000 description 2
• 108010072866 Prostate-Specific Antigen Proteins 0.000 description 2
• 230000005764 inhibitory process Effects 0.000 description 2
• 102000005602 Aldo-Keto Reductases Human genes 0.000 description 1
• 108010084469 Aldo-Keto Reductases Proteins 0.000 description 1
• 230000015572 biosynthetic process Effects 0.000 description 1
• 230000012292 cell migration Effects 0.000 description 1
• 239000003085 diluting agent Substances 0.000 description 1
• 230000000694 effects Effects 0.000 description 1
• 230000009545 invasion Effects 0.000 description 1
• 239000000546 pharmaceutical excipient Substances 0.000 description 1
• 230000023603 positive regulation of transcription initiation, DNA-dependent Effects 0.000 description 1
• 230000007115 recruitment Effects 0.000 description 1