JP2019512515A5 - - Google Patents
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- JP2019512515A5 JP2019512515A5 JP2018549435A JP2018549435A JP2019512515A5 JP 2019512515 A5 JP2019512515 A5 JP 2019512515A5 JP 2018549435 A JP2018549435 A JP 2018549435A JP 2018549435 A JP2018549435 A JP 2018549435A JP 2019512515 A5 JP2019512515 A5 JP 2019512515A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- ester
- pharmaceutically acceptable
- compound
- acceptable salt
- Prior art date
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 42
- 239000000203 mixture Substances 0.000 claims description 15
- 150000002148 esters Chemical class 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 13
- -1 pentafluorosulfanyl Chemical group 0.000 claims description 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 5
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 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 4
- 229910052805 deuterium Inorganic materials 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000001424 substituent group Chemical group 0.000 claims description 3
- 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 2
- 229960000853 abiraterone Drugs 0.000 claims description 2
- 238000010317 ablation therapy Methods 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 239000003098 androgen Substances 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 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 2
- 229960004671 enzalutamide Drugs 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000001475 halogen functional group Chemical group 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 14
- 125000005843 halogen group Chemical group 0.000 description 9
- 0 *=C([C@@](C1)[C@]1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1c1c(C(F)(F)F)ccc(C(F)(F)F)c1 Chemical compound *=C([C@@](C1)[C@]1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1c1c(C(F)(F)F)ccc(C(F)(F)F)c1 0.000 description 7
- 125000005010 perfluoroalkyl group Chemical group 0.000 description 3
- WAOCUQIXUIXXFL-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1C(C(C1)C1c1ccc(C(F)(F)F)cc1)=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1C(C(C1)C1c1ccc(C(F)(F)F)cc1)=O)=O WAOCUQIXUIXXFL-UHFFFAOYSA-N 0.000 description 2
- GWBVLEFRNSCGRF-UHFFFAOYSA-N C[n](c(C(N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1)=O)c1)c2c1cc(C(F)(F)F)cc2 Chemical compound C[n](c(C(N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1)=O)c1)c2c1cc(C(F)(F)F)cc2 GWBVLEFRNSCGRF-UHFFFAOYSA-N 0.000 description 2
- XVNZEPIQPHHZRJ-UHFFFAOYSA-N Cc(ccc(C(F)(F)F)c1)c1N(CC1)C=CN1C(C(C1)(C2)C12c1ccc(C(F)(F)F)cc1)=O Chemical compound Cc(ccc(C(F)(F)F)c1)c1N(CC1)C=CN1C(C(C1)(C2)C12c1ccc(C(F)(F)F)cc1)=O XVNZEPIQPHHZRJ-UHFFFAOYSA-N 0.000 description 2
- XUKBRMWFIRMPME-UHFFFAOYSA-N Cc(ccc(C(F)(F)F)c1)c1N(CC1)CCN1C(C(C1)C1c1cnc(C(F)(F)F)cc1)=O Chemical compound Cc(ccc(C(F)(F)F)c1)c1N(CC1)CCN1C(C(C1)C1c1cnc(C(F)(F)F)cc1)=O XUKBRMWFIRMPME-UHFFFAOYSA-N 0.000 description 2
- DSEPTVUXFQAIJN-HDICACEKSA-N Cc1ccc(C(F)(F)F)cc1N(CC1)CCN1C([C@H](C1)C[C@H]1c1ccc(C(F)(F)F)cc1)=O Chemical compound Cc1ccc(C(F)(F)F)cc1N(CC1)CCN1C([C@H](C1)C[C@H]1c1ccc(C(F)(F)F)cc1)=O DSEPTVUXFQAIJN-HDICACEKSA-N 0.000 description 2
- IZFBODIPCXHJIZ-UHFFFAOYSA-N N#Cc(ccc(Br)c1)c1N(CC1)CCN1C(C(C1)C1c1ccc(C(F)(F)F)cc1)=O Chemical compound N#Cc(ccc(Br)c1)c1N(CC1)CCN1C(C(C1)C1c1ccc(C(F)(F)F)cc1)=O IZFBODIPCXHJIZ-UHFFFAOYSA-N 0.000 description 2
- VYRWGHUYRNQBCE-UHFFFAOYSA-N O=C(C(C1)(C2)C12c1ccc(C(F)(F)F)cc1)N(CC1)CCN1c1c(C(F)(F)F)ccc(C2CC2)c1 Chemical compound O=C(C(C1)(C2)C12c1ccc(C(F)(F)F)cc1)N(CC1)CCN1c1c(C(F)(F)F)ccc(C2CC2)c1 VYRWGHUYRNQBCE-UHFFFAOYSA-N 0.000 description 2
- LLLUJYMVANTQQP-UHFFFAOYSA-N O=C(C(C1)C1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1C(c1cc(Cl)ccc1F)=O Chemical compound O=C(C(C1)C1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1C(c1cc(Cl)ccc1F)=O LLLUJYMVANTQQP-UHFFFAOYSA-N 0.000 description 2
- CTWMSQIXAUAEGK-IRXDYDNUSA-N O=C([C@@H](C1)[C@@H]1c(cc1)ccc1F)N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1 Chemical compound O=C([C@@H](C1)[C@@H]1c(cc1)ccc1F)N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1 CTWMSQIXAUAEGK-IRXDYDNUSA-N 0.000 description 2
- QJPLOCHQGQQAEH-OZBJMMHXSA-N O=C([C@](C1)(C1c1ccc(C(F)(F)F)cc1)C(F)(F)F)N(CC1)CCN1c1c(C(F)(F)F)ccc(C(F)(F)F)c1 Chemical compound O=C([C@](C1)(C1c1ccc(C(F)(F)F)cc1)C(F)(F)F)N(CC1)CCN1c1c(C(F)(F)F)ccc(C(F)(F)F)c1 QJPLOCHQGQQAEH-OZBJMMHXSA-N 0.000 description 2
- IZRTXHQGMQIXQU-YKBQRGLWSA-N O[C@H](C(C1)[C@@H]1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1Sc(cc(cc1)Cl)c1F Chemical compound O[C@H](C(C1)[C@@H]1c1ccc(C(F)(F)F)cc1)N(CC1)CCN1Sc(cc(cc1)Cl)c1F IZRTXHQGMQIXQU-YKBQRGLWSA-N 0.000 description 2
- ITRMZYSEZBCBEC-UHFFFAOYSA-N Cc(ccc(Cl)c1)c1N(CC1)CCN1C(C(C1)C1c(cc1)ccc1F)=O Chemical compound Cc(ccc(Cl)c1)c1N(CC1)CCN1C(C(C1)C1c(cc1)ccc1F)=O ITRMZYSEZBCBEC-UHFFFAOYSA-N 0.000 description 1
- SNQFFFFYPKJVHY-UHFFFAOYSA-N Cc(ccc(Cl)c1)c1N(CC1)CCN1C(Oc1cc(C(F)(F)F)ccc1)=O Chemical compound Cc(ccc(Cl)c1)c1N(CC1)CCN1C(Oc1cc(C(F)(F)F)ccc1)=O SNQFFFFYPKJVHY-UHFFFAOYSA-N 0.000 description 1
- MSIGGNNTTPMAPN-WIYYLYMNSA-N Cc(ccc(Cl)c1)c1N(CC1)CCN1C([C@@H](C1)[C@@]1(c(cc1)ccc1F)F)=O Chemical compound Cc(ccc(Cl)c1)c1N(CC1)CCN1C([C@@H](C1)[C@@]1(c(cc1)ccc1F)F)=O MSIGGNNTTPMAPN-WIYYLYMNSA-N 0.000 description 1
- VASXUFXSDSZPAS-UHFFFAOYSA-N O=C(N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1)Oc1ccc(C(F)(F)F)cc1 Chemical compound O=C(N(CC1)CCN1c1c(C(F)(F)F)ccc(Cl)c1)Oc1ccc(C(F)(F)F)cc1 VASXUFXSDSZPAS-UHFFFAOYSA-N 0.000 description 1
- 125000004802 cyanophenyl group Chemical group 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021096497A JP7125801B2 (ja) | 2016-03-24 | 2021-06-09 | 去勢抵抗性前立腺がんの処置のためのアンドロゲン受容体の核移行の低分子阻害剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15/080,237 | 2016-03-24 | ||
| US15/080,237 US20160257657A1 (en) | 2013-09-20 | 2016-03-24 | Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer |
| PCT/US2017/024105 WO2017165822A1 (en) | 2016-03-24 | 2017-03-24 | Small molecule inhibitor of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021096497A Division JP7125801B2 (ja) | 2016-03-24 | 2021-06-09 | 去勢抵抗性前立腺がんの処置のためのアンドロゲン受容体の核移行の低分子阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019512515A JP2019512515A (ja) | 2019-05-16 |
| JP2019512515A5 true JP2019512515A5 (enExample) | 2019-06-27 |
| JP6900050B2 JP6900050B2 (ja) | 2021-07-07 |
Family
ID=59899782
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018549435A Active JP6900050B2 (ja) | 2016-03-24 | 2017-03-24 | 去勢抵抗性前立腺がんの処置のためのアンドロゲン受容体の核移行の低分子阻害剤 |
| JP2021096497A Active JP7125801B2 (ja) | 2016-03-24 | 2021-06-09 | 去勢抵抗性前立腺がんの処置のためのアンドロゲン受容体の核移行の低分子阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021096497A Active JP7125801B2 (ja) | 2016-03-24 | 2021-06-09 | 去勢抵抗性前立腺がんの処置のためのアンドロゲン受容体の核移行の低分子阻害剤 |
Country Status (3)
| Country | Link |
|---|---|
| EP (1) | EP3433239B1 (enExample) |
| JP (2) | JP6900050B2 (enExample) |
| WO (1) | WO2017165822A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111902401B (zh) * | 2018-02-23 | 2023-06-13 | 北京泰德制药股份有限公司 | 受体抑制剂、包含其的药物组合物及其用途 |
| CA3099739A1 (en) * | 2018-05-14 | 2019-11-21 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer |
| CN109438297B (zh) * | 2018-12-03 | 2021-05-14 | 昆明积大制药股份有限公司 | 雄激素受体拮抗剂、其制备方法及其应用 |
| WO2020123670A1 (en) * | 2018-12-11 | 2020-06-18 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of the androgen receptor activity and/or expression and uses thereof |
| IL326597A (en) | 2019-10-07 | 2026-04-01 | Contineum Therapeutics Inc | Muscarinic acetylcholine m1 receptor antagonists |
| US11752149B2 (en) | 2019-12-02 | 2023-09-12 | Pipeline Therapeutics, Inc. | Muscarinic acetylcholine M1 receptor antagonists |
| US11945790B2 (en) * | 2020-12-22 | 2024-04-02 | Immunomolecular Therapeutics, Inc. | Compounds and methods for treating autoimmune disorders by targeting HLA-DQ2 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4675189A (en) | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| JPS60100516A (ja) | 1983-11-04 | 1985-06-04 | Takeda Chem Ind Ltd | 徐放型マイクロカプセルの製造法 |
| CA1256638A (en) | 1984-07-06 | 1989-06-27 | Motoaki Tanaka | Polymer and its production |
| JP2551756B2 (ja) | 1985-05-07 | 1996-11-06 | 武田薬品工業株式会社 | ポリオキシカルボン酸エステルおよびその製造法 |
| WO2000017163A1 (en) * | 1998-09-22 | 2000-03-30 | Yamanouchi Pharmaceutical Co., Ltd. | Cyanophenyl derivatives |
| CN1950393A (zh) | 2004-02-27 | 2007-04-18 | 先灵公司 | 丙型肝炎病毒ns3蛋白酶的抑制剂 |
| WO2012152854A1 (en) | 2011-05-12 | 2012-11-15 | Merz Pharma Gmbh & Co. Kgaa | Metabotropic glutamate receptor modulators |
| US9708276B2 (en) | 2011-10-12 | 2017-07-18 | University of Pittsburgh—of the Commonwealth System of Higher Education | Small molecules targeting androgen receptor nuclear localization and/or level in prostate cancer |
| US20160257657A1 (en) * | 2013-09-20 | 2016-09-08 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer |
| CA2924527C (en) | 2013-09-20 | 2022-07-12 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Compounds for treating prostate cancer |
-
2017
- 2017-03-24 JP JP2018549435A patent/JP6900050B2/ja active Active
- 2017-03-24 WO PCT/US2017/024105 patent/WO2017165822A1/en not_active Ceased
- 2017-03-24 EP EP17771272.6A patent/EP3433239B1/en active Active
-
2021
- 2021-06-09 JP JP2021096497A patent/JP7125801B2/ja active Active
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