JP2016523253A5 - - Google Patents
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- Publication number
- JP2016523253A5 JP2016523253A5 JP2016521557A JP2016521557A JP2016523253A5 JP 2016523253 A5 JP2016523253 A5 JP 2016523253A5 JP 2016521557 A JP2016521557 A JP 2016521557A JP 2016521557 A JP2016521557 A JP 2016521557A JP 2016523253 A5 JP2016523253 A5 JP 2016523253A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- salt
- cancer
- compound
- 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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- 150000003839 salts Chemical class 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 239000007788 liquid Substances 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 1
- AMMPLVWPWSYRDR-UHFFFAOYSA-N 1-methylbicyclo[2.2.2]oct-2-ene-4-carboxylic acid Chemical compound C1CC2(C(O)=O)CCC1(C)C=C2 AMMPLVWPWSYRDR-UHFFFAOYSA-N 0.000 claims 1
- LBLYYCQCTBFVLH-UHFFFAOYSA-M 2-methylbenzenesulfonate Chemical compound CC1=CC=CC=C1S([O-])(=O)=O LBLYYCQCTBFVLH-UHFFFAOYSA-M 0.000 claims 1
- 229940080296 2-naphthalenesulfonate Drugs 0.000 claims 1
- ALKYHXVLJMQRLQ-UHFFFAOYSA-M 3-carboxynaphthalen-2-olate Chemical compound C1=CC=C2C=C(C([O-])=O)C(O)=CC2=C1 ALKYHXVLJMQRLQ-UHFFFAOYSA-M 0.000 claims 1
- ZRPLANDPDWYOMZ-UHFFFAOYSA-N 3-cyclopentylpropionic acid Chemical compound OC(=O)CCC1CCCC1 ZRPLANDPDWYOMZ-UHFFFAOYSA-N 0.000 claims 1
- XMIIGOLPHOKFCH-UHFFFAOYSA-N 3-phenylpropionic acid Chemical class OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
- OBKXEAXTFZPCHS-UHFFFAOYSA-N 4-phenylbutyric acid Chemical compound OC(=O)CCCC1=CC=CC=C1 OBKXEAXTFZPCHS-UHFFFAOYSA-N 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 claims 1
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 claims 1
- IPDWABJNXLNLRA-LREBCSMRSA-N C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C([C@H](O)[C@@H](O)C(=O)O)(=O)O Chemical compound C(CC(O)(C(=O)O)CC(=O)O)(=O)O.C([C@H](O)[C@@H](O)C(=O)O)(=O)O IPDWABJNXLNLRA-LREBCSMRSA-N 0.000 claims 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims 1
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 1
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- OFOBLEOULBTSOW-UHFFFAOYSA-L Malonate Chemical compound [O-]C(=O)CC([O-])=O OFOBLEOULBTSOW-UHFFFAOYSA-L 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- LCTONWCANYUPML-UHFFFAOYSA-M Pyruvate Chemical compound CC(=O)C([O-])=O LCTONWCANYUPML-UHFFFAOYSA-M 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- IPBVNPXQWQGGJP-UHFFFAOYSA-N acetic acid phenyl ester Natural products CC(=O)OC1=CC=CC=C1 IPBVNPXQWQGGJP-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 229940077388 benzenesulfonate Drugs 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 claims 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 229940114081 cinnamate Drugs 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- MOTZDAYCYVMXPC-UHFFFAOYSA-N dodecyl hydrogen sulfate Chemical compound CCCCCCCCCCCCOS(O)(=O)=O MOTZDAYCYVMXPC-UHFFFAOYSA-N 0.000 claims 1
- 229940043264 dodecyl sulfate Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 239000002834 estrogen receptor modulator Substances 0.000 claims 1
- AFAXGSQYZLGZPG-UHFFFAOYSA-N ethanedisulfonic acid Chemical compound OS(=O)(=O)CCS(O)(=O)=O AFAXGSQYZLGZPG-UHFFFAOYSA-N 0.000 claims 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- -1 glu Heptonic acid salt Chemical class 0.000 claims 1
- 235000012208 gluconic acid Nutrition 0.000 claims 1
- 239000000174 gluconic acid Substances 0.000 claims 1
- 229930195712 glutamate Natural products 0.000 claims 1
- FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims 1
- 238000010253 intravenous injection Methods 0.000 claims 1
- SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 229940049920 malate Drugs 0.000 claims 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 claims 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims 1
- IWYDHOAUDWTVEP-UHFFFAOYSA-M mandelate Chemical compound [O-]C(=O)C(O)C1=CC=CC=C1 IWYDHOAUDWTVEP-UHFFFAOYSA-M 0.000 claims 1
- 125000005341 metaphosphate group Chemical group 0.000 claims 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 229940049953 phenylacetate Drugs 0.000 claims 1
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 claims 1
- 229950009215 phenylbutanoic acid Drugs 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- IUGYQRQAERSCNH-UHFFFAOYSA-M pivalate Chemical compound CC(C)(C)C([O-])=O IUGYQRQAERSCNH-UHFFFAOYSA-M 0.000 claims 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 claims 1
- 229960001860 salicylate Drugs 0.000 claims 1
- AEQFSUDEHCCHBT-UHFFFAOYSA-M sodium valproate Chemical compound [Na+].CCCC(C([O-])=O)CCC AEQFSUDEHCCHBT-UHFFFAOYSA-M 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 238000010254 subcutaneous injection Methods 0.000 claims 1
- 239000007929 subcutaneous injection Substances 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 229940095064 tartrate Drugs 0.000 claims 1
- WMOVHXAZOJBABW-UHFFFAOYSA-N tert-butyl acetate Chemical compound CC(=O)OC(C)(C)C WMOVHXAZOJBABW-UHFFFAOYSA-N 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 229940102566 valproate Drugs 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361836901P | 2013-06-19 | 2013-06-19 | |
| US61/836,901 | 2013-06-19 | ||
| US201461952430P | 2014-03-13 | 2014-03-13 | |
| US61/952,430 | 2014-03-13 | ||
| PCT/US2014/043040 WO2014205138A1 (en) | 2013-06-19 | 2014-06-18 | Estrogen receptor modulator and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019045520A Division JP2019142871A (ja) | 2013-06-19 | 2019-03-13 | エストロゲン受容体モジュレーター及びその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016523253A JP2016523253A (ja) | 2016-08-08 |
| JP2016523253A5 true JP2016523253A5 (https=) | 2017-08-03 |
| JP6576916B2 JP6576916B2 (ja) | 2019-09-18 |
Family
ID=52105249
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016521557A Active JP6576916B2 (ja) | 2013-06-19 | 2014-06-18 | エストロゲン受容体モジュレーター及びその使用 |
| JP2019045520A Pending JP2019142871A (ja) | 2013-06-19 | 2019-03-13 | エストロゲン受容体モジュレーター及びその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019045520A Pending JP2019142871A (ja) | 2013-06-19 | 2019-03-13 | エストロゲン受容体モジュレーター及びその使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9873684B2 (https=) |
| EP (1) | EP3010501B1 (https=) |
| JP (2) | JP6576916B2 (https=) |
| KR (1) | KR20160021277A (https=) |
| CN (1) | CN105324115B (https=) |
| AU (1) | AU2014281511A1 (https=) |
| BR (1) | BR112015031903A8 (https=) |
| CA (1) | CA2912853A1 (https=) |
| CL (1) | CL2015003456A1 (https=) |
| CR (1) | CR20150664A (https=) |
| EA (1) | EA031077B1 (https=) |
| IL (1) | IL242611B (https=) |
| MX (1) | MX2015017655A (https=) |
| PE (1) | PE20160157A1 (https=) |
| PH (1) | PH12015502621A1 (https=) |
| SG (1) | SG11201509508YA (https=) |
| TW (1) | TW201501710A (https=) |
| UA (1) | UA117249C2 (https=) |
| WO (1) | WO2014205138A1 (https=) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| EA031077B1 (ru) * | 2013-06-19 | 2018-11-30 | Серагон Фармасьютикалз, Инк. | Модулятор рецептора эстрогена и его применения |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| EP2862880A1 (en) | 2013-10-16 | 2015-04-22 | Solvay Acetow GmbH | Acylation process |
| PT3116316T (pt) | 2014-03-13 | 2019-09-30 | Assembly Biosciences Inc | Moduladores alostéricos da proteína do núcleo da hepatite b |
| JP2017507964A (ja) * | 2014-03-13 | 2017-03-23 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | エストロゲン受容体モジュレーターを用いた治療的組合せ |
| CA2941161A1 (en) | 2014-03-13 | 2015-09-17 | F.Hoffmann-La Roche Ag | Methods and compositions for modulating estrogen receptor mutants |
| CN107406424B (zh) | 2014-12-18 | 2020-08-25 | 豪夫迈·罗氏有限公司 | 雌激素受体调节剂及其用途 |
| KR102785474B1 (ko) | 2014-12-18 | 2025-03-26 | 에프. 호프만-라 로슈 아게 | 테트라하이드로-피리도[3,4-b]인돌 에스트로겐 수용체 조절제 및 이의 용도 |
| EP3233818A1 (en) * | 2014-12-18 | 2017-10-25 | F. Hoffmann-La Roche AG | Derivatives of 2,3-diphenylchromene useful for the treatment of cancer |
| CN107847498B (zh) | 2015-05-29 | 2021-04-13 | 卫材R&D管理有限公司 | 四取代的烯烃化合物及其用途 |
| WO2017024318A1 (en) | 2015-08-06 | 2017-02-09 | Dana-Farber Cancer Institute, Inc. | Targeted protein degradation to attenuate adoptive t-cell therapy associated adverse inflammatory responses |
| TWI730985B (zh) | 2015-09-15 | 2021-06-21 | 美商艾森伯利生物科學公司 | B型肝炎核心蛋白質調節劑 |
| KR102710603B1 (ko) * | 2015-10-01 | 2024-09-27 | 올레마 파마슈티컬스 인코포레이티드 | 테트라히드로-1H-피리도[3,4-b]인돌 항에스트로겐 약물 |
| MX385940B (es) | 2015-10-27 | 2025-03-18 | Sun Pharma Advanced Res Co Ltd | Nuevos antiestrógenos heterocíclicos. |
| SMT202300018T1 (it) | 2015-12-09 | 2023-03-17 | Univ Illinois | Downregolatori del recettore degli estrogeni a base di benzotiofene |
| US10125135B2 (en) | 2016-04-20 | 2018-11-13 | Astrazeneca Ab | Chemical compounds |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| EP4491236A3 (en) | 2016-05-10 | 2025-04-02 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| TWI794171B (zh) | 2016-05-11 | 2023-03-01 | 美商滬亞生物國際有限公司 | Hdac抑制劑與pd-l1抑制劑之組合治療 |
| TWI808055B (zh) | 2016-05-11 | 2023-07-11 | 美商滬亞生物國際有限公司 | Hdac 抑制劑與 pd-1 抑制劑之組合治療 |
| US20180002344A1 (en) | 2016-06-16 | 2018-01-04 | Genentech, Inc. | Heteroaryl estrogen receptor modulators and uses thereof |
| EP3858835A1 (en) | 2016-07-01 | 2021-08-04 | G1 Therapeutics, Inc. | Pyrimidine-based antiproliferative agents |
| WO2018019793A1 (en) | 2016-07-25 | 2018-02-01 | Astrazeneca Ab | N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer |
| AU2017326356A1 (en) | 2016-09-15 | 2019-04-11 | Assembly Biosciences, Inc. | Hepatitis B core protein modulators |
| JP2020011901A (ja) * | 2016-10-20 | 2020-01-23 | 協和キリン株式会社 | ピロリジン化合物の製造方法 |
| TWI735681B (zh) | 2016-10-24 | 2021-08-11 | 瑞典商阿斯特捷利康公司 | 化合物 |
| WO2018081168A2 (en) | 2016-10-24 | 2018-05-03 | The Board Of Trustees Of The University Of Illinois | Benzothiophene-based selective mixed estrogen receptor downregulators |
| AU2017355432A1 (en) * | 2016-11-04 | 2019-05-16 | F. Hoffmann-La Roche Ag | Treatment of HER2-positive breast cancer |
| CA3041986A1 (en) | 2016-11-28 | 2018-05-31 | Eisai R&D Management Co., Ltd. | Salts of indazole derivative and crystals thereof |
| WO2018108954A1 (en) | 2016-12-12 | 2018-06-21 | F. Hoffmann-La Roche Ag | Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol |
| EP3565558B1 (en) | 2017-01-06 | 2023-12-06 | G1 Therapeutics, Inc. | Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer |
| PT3494116T (pt) | 2017-01-30 | 2020-01-28 | Astrazeneca Ab | Moduladores de recetores de estrogénio |
| EP3580212A4 (en) | 2017-02-08 | 2021-03-17 | Dana Farber Cancer Institute, Inc. | REGULATION OF CHEMERIC ANTIGEN RECEPTORS |
| KR20190117582A (ko) | 2017-02-10 | 2019-10-16 | 쥐원 쎄라퓨틱스, 인크. | 벤조티오펜 에스트로겐 수용체 조정제 |
| SG11201908012SA (en) | 2017-03-02 | 2019-09-27 | Assembly Biosciences Inc | Cyclic sulfamide compounds and methods of using same |
| EP3596070A1 (en) | 2017-03-13 | 2020-01-22 | Assembly Biosciences, Inc. | Process for making hepatitis b core protein modulators |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| FI3645001T3 (fi) | 2017-06-29 | 2024-09-25 | G1 Therapeutics Inc | Git38:n morfisia muotoja ja niiden valmistusmenetelmiä |
| JP7585034B2 (ja) | 2017-10-18 | 2024-11-18 | ノバルティス アーゲー | 選択的タンパク質分解のための組成物及び方法 |
| CN111315378A (zh) | 2017-11-16 | 2020-06-19 | 诺华股份有限公司 | 包含lsz102和瑞博西尼的药物组合 |
| WO2019106604A1 (en) * | 2017-12-01 | 2019-06-06 | Novartis Ag | Pharmaceutical combination comprising lsz102 and alpelisib |
| WO2019192533A1 (zh) * | 2018-04-04 | 2019-10-10 | 深圳福沃药业有限公司 | 用于治疗乳腺癌的雌激素受体降解剂 |
| LT3810283T (lt) | 2018-06-21 | 2023-08-25 | F. Hoffmann-La Roche Ag | 3-((1r,3r)-1-(2,6-difluor-4-((1-(3-fluorpropil)azetidin-3- il)amino) fenil)-3-metil-1,3,4,9-tetrahidro-2h-pirido[3,4-b]indol-2-il)- 2,2- difluorpropan-1-olio tartrato druskos kietosios formos, jų paruošimo procesas ir jų naudojimo būdai vėžiui gydyti |
| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
| US20220251152A1 (en) | 2019-04-24 | 2022-08-11 | Novartis Ag | Compositions and methods for selective protein degradation |
| MX2022000279A (es) | 2019-07-07 | 2022-02-03 | Olema Pharmaceuticals Inc | Regimenes de antagonistas del receptor de estrogeno. |
| US11014915B2 (en) | 2019-07-22 | 2021-05-25 | Sun Pharma Advanced Research Company Limited | Selective estrogen receptor degrader |
| BR112022011827A2 (pt) | 2019-12-20 | 2022-08-30 | C4 Therapeutics Inc | Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| EP4117718A4 (en) * | 2020-03-09 | 2024-05-08 | University of Houston System | INFLAMMATORY BOWEL DISEASE (IBD)-ASSOCIATED STEM CELLS, AGENTS TARGETING IBD-ASSOCIATED STEM CELLS AND RELATED USES THEREOF |
| WO2021214253A1 (en) | 2020-04-24 | 2021-10-28 | Astrazeneca Ab | Dosage regimen for the treatment of cancer |
| PE20221838A1 (es) | 2020-04-24 | 2022-11-29 | Astrazeneca Ab | Formulaciones farmaceuticas |
| ES3048084T3 (en) | 2020-05-19 | 2025-12-09 | Pharmacosmos Holding As | Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| WO2022066774A1 (en) | 2020-09-23 | 2022-03-31 | Achillion Pharmaceuticals, Inc. | Pharmaceutical compounds for the treatment of complement mediated disorders |
| WO2022261250A1 (en) | 2021-06-08 | 2022-12-15 | C4 Therapeutics, Inc. | Therapeutics for the degradation of mutant braf |
| JP2025525917A (ja) | 2022-08-03 | 2025-08-07 | ブリストル-マイヤーズ スクイブ カンパニー | Retタンパク質を調節するための化合物 |
| CN120569388A (zh) | 2022-11-04 | 2025-08-29 | 百时美施贵宝公司 | Ret-ldd蛋白降解剂 |
| CN120530116A (zh) | 2022-11-04 | 2025-08-22 | 百时美施贵宝公司 | Ret-ldd蛋白抑制剂 |
| CN115872996B (zh) * | 2023-02-21 | 2023-05-05 | 山东绿叶制药有限公司 | 一种雌激素受体降解剂化合物及其制备方法和应用 |
| WO2025006753A2 (en) | 2023-06-30 | 2025-01-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| CN121646481A (zh) * | 2024-07-04 | 2026-03-10 | 海创药业股份有限公司 | 一种雌激素受体降解剂和akt抑制剂联合用药物及其用途 |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4229447A (en) | 1979-06-04 | 1980-10-21 | American Home Products Corporation | Intraoral methods of using benzodiazepines |
| US4596795A (en) | 1984-04-25 | 1986-06-24 | The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services | Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives |
| US5011692A (en) | 1985-12-28 | 1991-04-30 | Sumitomo Pharmaceuticals Company, Limited | Sustained pulsewise release pharmaceutical preparation |
| US4755386A (en) | 1986-01-22 | 1988-07-05 | Schering Corporation | Buccal formulation |
| US5395842A (en) * | 1988-10-31 | 1995-03-07 | Endorecherche Inc. | Anti-estrogenic compounds and compositions |
| US5739136A (en) | 1989-10-17 | 1998-04-14 | Ellinwood, Jr.; Everett H. | Intraoral dosing method of administering medicaments |
| US5017381A (en) | 1990-05-02 | 1991-05-21 | Alza Corporation | Multi-unit pulsatile delivery system |
| US5229135A (en) | 1991-11-22 | 1993-07-20 | Prographarm Laboratories | Sustained release diltiazem formulation |
| US6060503A (en) | 1991-12-02 | 2000-05-09 | Endorecherche, Inc. | Benzopyran-containing compounds and method for their use |
| US5407947A (en) * | 1993-11-05 | 1995-04-18 | Eli Lilly And Company | Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans |
| US5837284A (en) | 1995-12-04 | 1998-11-17 | Mehta; Atul M. | Delivery of multiple doses of medications |
| US5840329A (en) | 1997-05-15 | 1998-11-24 | Bioadvances Llc | Pulsatile drug delivery system |
| US6262270B1 (en) * | 1998-08-14 | 2001-07-17 | Schering Corporation | Enantioselective synthesis |
| US7582476B2 (en) | 1999-12-07 | 2009-09-01 | Sumitomo Chemical Company, Limited | Artificial cell comprising mutant estrogen receptor |
| DE10013782A1 (de) | 2000-03-15 | 2001-10-18 | Schering Ag | 4-Fluoralkyl-2H-benzopyrane mit antiestrogener Wirksamkeit, Verfahren zu ihrer Herstellung, pharmazeutische Präparate, die diese enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln |
| SK287086B6 (sk) | 2001-01-24 | 2009-11-05 | Chiesi Farmaceutici S.P.A. | 2H-1-Benzopyránové deriváty, farmaceutické prostriedky s ich obsahom a ich použitie |
| US7105679B2 (en) | 2001-12-19 | 2006-09-12 | Kanojia Ramesh M | Heteroatom containing tetracyclic derivatives as selective estrogen receptor modulators |
| WO2004091488A2 (en) * | 2003-04-14 | 2004-10-28 | Merck & Co., Inc. | Estrogen receptor modulators |
| HUE033581T2 (hu) * | 2010-06-10 | 2017-12-28 | Seragon Pharmaceuticals Inc | Ösztrogén receptor modulátorok és alkalmazásaik |
| GB2483736B (en) | 2010-09-16 | 2012-08-29 | Aragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| WO2013056178A2 (en) | 2011-10-14 | 2013-04-18 | Foundation Medicine, Inc. | Novel estrogen receptor mutations and uses thereof |
| WO2013055874A2 (en) * | 2011-10-14 | 2013-04-18 | Genentech, Inc. | Uses for and article of manufacture including her2 dimerization inhibitor pertuzumab |
| JP6112625B2 (ja) * | 2011-12-14 | 2017-04-12 | セラゴン ファーマシューティカルズ,インク. | フッ素化したエストロゲン受容体モジュレーターおよびその使用 |
| SG11201405918XA (en) | 2012-03-20 | 2014-10-30 | Seragon Pharmaceuticals Inc | Estrogen receptor modulators and uses thereof |
| EP2855479B1 (en) * | 2012-04-05 | 2016-03-30 | Boehringer Ingelheim International GmbH | 1,8-naphthyridin-2(1h)-one derivatives as cytomegalovirus inhibitors |
| JP2016517420A (ja) | 2013-03-14 | 2016-06-16 | セラゴン ファーマシューティカルズ, インク. | 多環式エストロゲン受容体モジュレーター及びその使用 |
| EA031077B1 (ru) * | 2013-06-19 | 2018-11-30 | Серагон Фармасьютикалз, Инк. | Модулятор рецептора эстрогена и его применения |
| BR112015030595A2 (pt) | 2013-06-19 | 2017-07-25 | Seragon Pharmaceuticals Inc | moduladores de receptor de estrogênio de azetidina e usos dos mesmos |
| WO2015082990A1 (en) | 2013-12-06 | 2015-06-11 | Seragon Pharmaceuticals, Inc. | Estrogen receptor modulator for the treatment of locally advanced or metastatic estrogen receptor positive breast cancer |
| CA2941161A1 (en) | 2014-03-13 | 2015-09-17 | F.Hoffmann-La Roche Ag | Methods and compositions for modulating estrogen receptor mutants |
| JP2017507964A (ja) | 2014-03-13 | 2017-03-23 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | エストロゲン受容体モジュレーターを用いた治療的組合せ |
| US9493945B2 (en) | 2014-07-18 | 2016-11-15 | Williams Scotsman, Inc. | Wall panel connecting system for modular building units |
| CN107406424B (zh) | 2014-12-18 | 2020-08-25 | 豪夫迈·罗氏有限公司 | 雌激素受体调节剂及其用途 |
| EP3233818A1 (en) | 2014-12-18 | 2017-10-25 | F. Hoffmann-La Roche AG | Derivatives of 2,3-diphenylchromene useful for the treatment of cancer |
-
2014
- 2014-06-18 EA EA201592214A patent/EA031077B1/ru not_active IP Right Cessation
- 2014-06-18 JP JP2016521557A patent/JP6576916B2/ja active Active
- 2014-06-18 PE PE2015002634A patent/PE20160157A1/es unknown
- 2014-06-18 BR BR112015031903A patent/BR112015031903A8/pt not_active Application Discontinuation
- 2014-06-18 CA CA2912853A patent/CA2912853A1/en not_active Abandoned
- 2014-06-18 SG SG11201509508YA patent/SG11201509508YA/en unknown
- 2014-06-18 EP EP14812952.1A patent/EP3010501B1/en active Active
- 2014-06-18 WO PCT/US2014/043040 patent/WO2014205138A1/en not_active Ceased
- 2014-06-18 UA UAA201600246A patent/UA117249C2/uk unknown
- 2014-06-18 KR KR1020167001338A patent/KR20160021277A/ko not_active Withdrawn
- 2014-06-18 CN CN201480035316.2A patent/CN105324115B/zh active Active
- 2014-06-18 AU AU2014281511A patent/AU2014281511A1/en not_active Abandoned
- 2014-06-18 MX MX2015017655A patent/MX2015017655A/es unknown
- 2014-06-19 TW TW103121277A patent/TW201501710A/zh unknown
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2015
- 2015-11-16 IL IL242611A patent/IL242611B/en not_active IP Right Cessation
- 2015-11-24 CL CL2015003456A patent/CL2015003456A1/es unknown
- 2015-11-24 PH PH12015502621A patent/PH12015502621A1/en unknown
- 2015-12-09 US US14/963,658 patent/US9873684B2/en active Active
- 2015-12-16 CR CR20150664A patent/CR20150664A/es unknown
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2017
- 2017-06-12 US US15/620,304 patent/US10227334B2/en active Active
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- 2019-03-13 JP JP2019045520A patent/JP2019142871A/ja active Pending
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