JP2020518580A5 - - Google Patents
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- JP2020518580A5 JP2020518580A5 JP2019559295A JP2019559295A JP2020518580A5 JP 2020518580 A5 JP2020518580 A5 JP 2020518580A5 JP 2019559295 A JP2019559295 A JP 2019559295A JP 2019559295 A JP2019559295 A JP 2019559295A JP 2020518580 A5 JP2020518580 A5 JP 2020518580A5
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- 210000003780 hair follicle Anatomy 0.000 claims description 28
- 150000001875 compounds Chemical class 0.000 claims description 18
- 210000004209 hair Anatomy 0.000 claims description 16
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 210000003491 skin Anatomy 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000024891 symptom Diseases 0.000 claims description 3
- 201000004384 Alopecia Diseases 0.000 claims 3
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 claims 2
- 231100000360 alopecia Toxicity 0.000 claims 2
- 239000011928 denatured alcohol Substances 0.000 claims 2
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- 206010020112 Hirsutism Diseases 0.000 claims 1
- 206010036049 Polycystic ovaries Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 239000003098 androgen Substances 0.000 claims 1
- 230000003412 degenerative effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000001815 facial effect Effects 0.000 claims 1
- 230000003648 hair appearance Effects 0.000 claims 1
- 230000003752 improving hair Effects 0.000 claims 1
- 239000004615 ingredient Substances 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 210000002374 sebum Anatomy 0.000 claims 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 238000005259 measurement Methods 0.000 description 6
- 210000001519 tissue Anatomy 0.000 description 5
- -1 Boc-protected amino Chemical group 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 235000001014 amino acid Nutrition 0.000 description 3
- 229940024606 amino acid Drugs 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- BRUZQRBVNRKLJG-UHFFFAOYSA-N 2-methylpropyl carbamate Chemical compound CC(C)COC(N)=O BRUZQRBVNRKLJG-UHFFFAOYSA-N 0.000 description 2
- 239000004475 Arginine Substances 0.000 description 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 2
- 239000004472 Lysine Substances 0.000 description 2
- 235000009697 arginine Nutrition 0.000 description 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 2
- 235000003704 aspartic acid Nutrition 0.000 description 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 230000003793 hair pigmentation Effects 0.000 description 2
- 235000018977 lysine Nutrition 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 229920001184 polypeptide Polymers 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 108090000765 processed proteins & peptides Proteins 0.000 description 2
- 230000037384 skin absorption Effects 0.000 description 2
- 231100000274 skin absorption Toxicity 0.000 description 2
- 239000011550 stock solution Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- XMAYWYJOQHXEEK-OZXSUGGESA-N (2R,4S)-ketoconazole Chemical compound C1CN(C(=O)C)CCN1C(C=C1)=CC=C1OC[C@@H]1O[C@@](CN2C=NC=C2)(C=2C(=CC(Cl)=CC=2)Cl)OC1 XMAYWYJOQHXEEK-OZXSUGGESA-N 0.000 description 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 description 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 description 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 description 1
- CKLJMWTZIZZHCS-UHFFFAOYSA-N Aspartic acid Chemical compound OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 description 1
- LUHPQXZCWVFCDI-UHFFFAOYSA-N CC(C)(C)OC(NC(CC(NC(OC(C)(C)C)=O)=O)C(N)=O)=O Chemical compound CC(C)(C)OC(NC(CC(NC(OC(C)(C)C)=O)=O)C(N)=O)=O LUHPQXZCWVFCDI-UHFFFAOYSA-N 0.000 description 1
- GUKVNJVXOCGBDS-UHFFFAOYSA-N CC(C)(C)OC(NC(CCC(NC(OC(C)(C)C)=O)=O)C(N)=O)=O Chemical compound CC(C)(C)OC(NC(CCC(NC(OC(C)(C)C)=O)=O)C(N)=O)=O GUKVNJVXOCGBDS-UHFFFAOYSA-N 0.000 description 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 description 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 description 1
- 125000001429 N-terminal alpha-amino-acid group Chemical group 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 235000009582 asparagine Nutrition 0.000 description 1
- 229960001230 asparagine Drugs 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 229940125807 compound 37 Drugs 0.000 description 1
- 229940125936 compound 42 Drugs 0.000 description 1
- 235000018417 cysteine Nutrition 0.000 description 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 description 1
- 230000007547 defect Effects 0.000 description 1
- 238000007865 diluting Methods 0.000 description 1
- 235000013922 glutamic acid Nutrition 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 235000004554 glutamine Nutrition 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- 210000004919 hair shaft Anatomy 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 210000002510 keratinocyte Anatomy 0.000 description 1
- 229960004125 ketoconazole Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- XBXCNNQPRYLIDE-UHFFFAOYSA-M n-tert-butylcarbamate Chemical compound CC(C)(C)NC([O-])=O XBXCNNQPRYLIDE-UHFFFAOYSA-M 0.000 description 1
- 239000013642 negative control Substances 0.000 description 1
- RJMUSRYZPJIFPJ-UHFFFAOYSA-N niclosamide Chemical compound OC1=CC=C(Cl)C=C1C(=O)NC1=CC=C([N+]([O-])=O)C=C1Cl RJMUSRYZPJIFPJ-UHFFFAOYSA-N 0.000 description 1
- 229960001920 niclosamide Drugs 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 235000008729 phenylalanine Nutrition 0.000 description 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 239000013641 positive control Substances 0.000 description 1
- 230000017854 proteolysis Effects 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- LXMSZDCAJNLERA-ZHYRCANASA-N spironolactone Chemical compound C([C@@H]1[C@]2(C)CC[C@@H]3[C@@]4(C)CCC(=O)C=C4C[C@H]([C@@H]13)SC(=O)C)C[C@@]21CCC(=O)O1 LXMSZDCAJNLERA-ZHYRCANASA-N 0.000 description 1
- 229960002256 spironolactone Drugs 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000011179 visual inspection Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762492822P | 2017-05-01 | 2017-05-01 | |
| US62/492,822 | 2017-05-01 | ||
| PCT/US2018/030538 WO2018204422A1 (en) | 2017-05-01 | 2018-05-01 | Tripartite androgen receptor eliminators, methods and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020518580A JP2020518580A (ja) | 2020-06-25 |
| JP2020518580A5 true JP2020518580A5 (https=) | 2021-06-17 |
| JP7061135B2 JP7061135B2 (ja) | 2022-04-27 |
Family
ID=64016717
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019559295A Active JP7061135B2 (ja) | 2017-05-01 | 2018-05-01 | トリパータイトアンドロゲン受容体除去剤、その方法および使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US11447483B2 (https=) |
| EP (1) | EP3618833B1 (https=) |
| JP (1) | JP7061135B2 (https=) |
| KR (1) | KR102746106B1 (https=) |
| CN (1) | CN110831601B (https=) |
| AU (1) | AU2018261331C1 (https=) |
| CA (1) | CA3062161A1 (https=) |
| ES (1) | ES2910976T3 (https=) |
| WO (1) | WO2018204422A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110506039A (zh) | 2016-10-11 | 2019-11-26 | 阿尔维纳斯股份有限公司 | 用于雄激素受体靶向降解的化合物和方法 |
| IL312367A (en) | 2017-01-31 | 2024-06-01 | Arvinas Operations Inc | Cereblon ligands and bifunctional compounds comprising the same |
| CN110746399B (zh) * | 2018-07-23 | 2022-04-22 | 上海美志医药科技有限公司 | 具有降解雄激素受体活性的化合物 |
| CN109762045A (zh) * | 2018-12-14 | 2019-05-17 | 中山大学附属第一医院 | 一种双靶点构建protac的方法及其用途 |
| AU2020405129A1 (en) | 2019-12-19 | 2022-06-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| CR20220630A (es) | 2020-05-09 | 2023-01-23 | Arvinas Operations Inc | Métodos para fabricar un compuesto bifuncional, formas ultrapuras del compuesto bifuncional y formas de dosificación que comprenden el mismo |
| TW202535392A (zh) | 2023-12-08 | 2025-09-16 | 美商亞文納營運公司 | 使用雄性素受體降解劑治療脊髓延髓性肌肉萎縮 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3013012A (en) * | 1960-12-22 | 1961-12-12 | Searle & Co | Alkanoylthio-17alpha-carboxyethyl-17beta-hydroxyandrosten-3-one lactones |
| US6790979B2 (en) | 2002-04-17 | 2004-09-14 | University Of North Carolina At Chapel Hill | Curcumin analogues and uses thereof |
| US7355081B2 (en) | 2002-04-17 | 2008-04-08 | The University Of North Carolina At Chapel Hill | Curcumin analogues and uses thereof |
| KR102668696B1 (ko) * | 2012-01-12 | 2024-05-29 | 예일 유니버시티 | E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법 |
| WO2013170147A1 (en) | 2012-05-11 | 2013-11-14 | Yale University | Compounds useful for promoting protein degradation and methods using same |
| CN107753954A (zh) * | 2012-12-13 | 2018-03-06 | 免疫医疗公司 | 功效改进且毒性降低的抗体与sn‑38的免疫缀合物的剂量 |
| WO2017004144A1 (en) * | 2015-07-01 | 2017-01-05 | Immunomedics, Inc. | Antibody-sn-38 immunoconjugates with a cl2a linker |
| JP6817962B2 (ja) | 2015-01-20 | 2021-01-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | ターゲティングされたアンドロゲン受容体分解のための化合物および方法 |
| RU2724103C2 (ru) * | 2015-04-21 | 2020-06-22 | Джи Ти Икс, ИНК. | Селективные лиганды-разрушители андрогенных рецептов (sard) и способы их применения |
| WO2016197114A1 (en) | 2015-06-05 | 2016-12-08 | Arvinas, Inc. | Tank-binding kinase-1 protacs and associated methods of use |
-
2018
- 2018-05-01 WO PCT/US2018/030538 patent/WO2018204422A1/en not_active Ceased
- 2018-05-01 JP JP2019559295A patent/JP7061135B2/ja active Active
- 2018-05-01 AU AU2018261331A patent/AU2018261331C1/en active Active
- 2018-05-01 CA CA3062161A patent/CA3062161A1/en active Pending
- 2018-05-01 CN CN201880044734.6A patent/CN110831601B/zh active Active
- 2018-05-01 ES ES18794821T patent/ES2910976T3/es active Active
- 2018-05-01 EP EP18794821.1A patent/EP3618833B1/en active Active
- 2018-05-01 KR KR1020197034692A patent/KR102746106B1/ko active Active
- 2018-05-01 US US16/608,749 patent/US11447483B2/en active Active
-
2022
- 2022-09-13 US US17/931,773 patent/US12319681B2/en active Active
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