JP2016531852A5 - - Google Patents
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- Publication number
- JP2016531852A5 JP2016531852A5 JP2016516578A JP2016516578A JP2016531852A5 JP 2016531852 A5 JP2016531852 A5 JP 2016531852A5 JP 2016516578 A JP2016516578 A JP 2016516578A JP 2016516578 A JP2016516578 A JP 2016516578A JP 2016531852 A5 JP2016531852 A5 JP 2016531852A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- compound
- alkyl
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims description 74
- 150000003839 salts Chemical class 0.000 claims description 35
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
- 239000001257 hydrogen Substances 0.000 claims description 23
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 15
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 11
- 150000002431 hydrogen Chemical class 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- 125000001475 halogen functional group Chemical group 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 8
- 102000003676 Glucocorticoid Receptors Human genes 0.000 claims description 6
- 108090000079 Glucocorticoid Receptors Proteins 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 5
- 206010003246 arthritis Diseases 0.000 claims description 4
- 208000006673 asthma Diseases 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 125000001188 haloalkyl group Chemical group 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 4
- -1 —OH Chemical group 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 3
- 239000012472 biological sample Substances 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 2
- 208000015943 Coeliac disease Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010000496 acne Diseases 0.000 claims description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 4
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 239000003446 ligand Substances 0.000 description 8
- SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical group OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 description 6
- 230000027455 binding Effects 0.000 description 6
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 6
- 210000004027 cell Anatomy 0.000 description 4
- 238000003556 assay Methods 0.000 description 3
- 229960000890 hydrocortisone Drugs 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 230000002103 transcriptional effect Effects 0.000 description 3
- 210000000172 cytosol Anatomy 0.000 description 2
- 231100000673 dose–response relationship Toxicity 0.000 description 2
- 239000003862 glucocorticoid Substances 0.000 description 2
- 238000000159 protein binding assay Methods 0.000 description 2
- 238000013518 transcription Methods 0.000 description 2
- 230000035897 transcription Effects 0.000 description 2
- OEDUIFSDODUDRK-UHFFFAOYSA-N 5-phenyl-1h-pyrazole Chemical group N1N=CC=C1C1=CC=CC=C1 OEDUIFSDODUDRK-UHFFFAOYSA-N 0.000 description 1
- 0 CC(CC1O)(C(CC2)C(CC3)C1C(C)(C1)C3=Cc3c1cn[n]3-c1ccccc1)C2(C(N(*)OC)=O)O Chemical compound CC(CC1O)(C(CC2)C(CC3)C1C(C)(C1)C3=Cc3c1cn[n]3-c1ccccc1)C2(C(N(*)OC)=O)O 0.000 description 1
- SHJSGBRBJAUAOI-DPYUSNRASA-N CCNC(Nc1cccc(-[n]2ncc(C3)c2C=C(CCC2C(CC4)[C@](C)(C5)C4(C(NCc4ccccc4)=O)OC(c4ccc[o]4)=O)[C@@]3(C)C2C5O)c1)=O Chemical compound CCNC(Nc1cccc(-[n]2ncc(C3)c2C=C(CCC2C(CC4)[C@](C)(C5)C4(C(NCc4ccccc4)=O)OC(c4ccc[o]4)=O)[C@@]3(C)C2C5O)c1)=O SHJSGBRBJAUAOI-DPYUSNRASA-N 0.000 description 1
- MFCLGLNXQPILRU-LPQFBKIQSA-N C[C@H](CC(C([C@]1([C@@](C)(C2)C3=Cc4c2cn[n]4-c2ccccc2)F)C=C3F)[C@]2(C)CC1O)C2(C(N(C)OC)=O)OC(c1ccc[o]1)=O Chemical compound C[C@H](CC(C([C@]1([C@@](C)(C2)C3=Cc4c2cn[n]4-c2ccccc2)F)C=C3F)[C@]2(C)CC1O)C2(C(N(C)OC)=O)OC(c1ccc[o]1)=O MFCLGLNXQPILRU-LPQFBKIQSA-N 0.000 description 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 1
- 102000008300 Mutant Proteins Human genes 0.000 description 1
- 108010021466 Mutant Proteins Proteins 0.000 description 1
- 230000004913 activation Effects 0.000 description 1
- 235000004279 alanine Nutrition 0.000 description 1
- 230000009137 competitive binding Effects 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000001718 repressive effect Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 229940037128 systemic glucocorticoids Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361882444P | 2013-09-25 | 2013-09-25 | |
| US61/882,444 | 2013-09-25 | ||
| PCT/US2014/057497 WO2015048316A1 (en) | 2013-09-25 | 2014-09-25 | Highly potent glucocorticoids |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016531852A JP2016531852A (ja) | 2016-10-13 |
| JP2016531852A5 true JP2016531852A5 (https=) | 2017-11-02 |
Family
ID=52744465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516578A Pending JP2016531852A (ja) | 2013-09-25 | 2014-09-25 | 非常に強力なグルココルチコイド |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US9975918B2 (https=) |
| EP (1) | EP3049089B1 (https=) |
| JP (1) | JP2016531852A (https=) |
| KR (1) | KR20160060688A (https=) |
| CN (2) | CN105744937A (https=) |
| AU (1) | AU2014324961A1 (https=) |
| ES (1) | ES2751457T3 (https=) |
| HK (1) | HK1222565A1 (https=) |
| WO (1) | WO2015048316A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3319611T3 (pl) | 2015-07-06 | 2021-07-12 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| MX382122B (es) | 2015-07-06 | 2025-03-13 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| EP3436022B1 (en) | 2016-04-01 | 2022-03-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| PT3519422T (pt) | 2016-09-30 | 2022-12-05 | Sage Therapeutics Inc | Oxisteróis substituídos em c7 e métodos como moduladores nmda |
| CN110382033B (zh) | 2016-10-14 | 2022-04-15 | 范安德尔研究所 | 用于设计高效力糖皮质激素的结构与机制 |
| CA3041088C (en) | 2016-10-18 | 2024-05-21 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| DK4105223T3 (da) | 2016-10-18 | 2025-07-07 | Sage Therapeutics Inc | Oxysteroler og fremgangsmåder til anvendelse deraf |
| CA3166630A1 (en) | 2020-01-03 | 2021-07-08 | Berg Llc | Polycyclic amides as ube2k modulators for treating cancer |
| CN117024499A (zh) * | 2023-07-17 | 2023-11-10 | 陕西汉江药业集团股份有限公司 | 在2位引入亚甲基羟基的甾体化合物制备方法 |
| WO2025157225A1 (zh) * | 2024-01-24 | 2025-07-31 | 浙江柏拉阿图医药科技有限公司 | 一种高效力糖皮质激素化合物及其制备和用途 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4049813A (en) | 1976-07-15 | 1977-09-20 | Sandoz, Inc. | Substituted isoxazolo pyridinones |
| CA2451057A1 (en) | 2001-06-14 | 2002-12-27 | Banyu Pharmaceutical Co., Ltd. | Novel isoxazolopyridone derivatives and use thereof |
| GB0119911D0 (en) | 2001-08-15 | 2001-10-10 | Novartis Ag | Organic Compounds |
| NZ584160A (en) * | 2007-10-04 | 2011-05-27 | Astrazeneca Ab | Steroidal [3,2-c] pyrazole compounds, with glucocorticoid activity |
| CA2749585A1 (en) | 2009-01-13 | 2010-07-22 | Van Andel Research Institute | Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids |
| UY32525A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| UY32523A (es) * | 2009-04-03 | 2010-10-29 | Astrazeneca Ab | Compuestos que tienen actividad agonista del receptor de glucocorticosteroides |
| JP2012530140A (ja) * | 2009-06-16 | 2012-11-29 | メルク・シャープ・アンド・ドーム・コーポレーション | グルココルチコイド受容体アゴニストとしての新規［３，２−ｃ］ヘテロアリールステロイド、組成物およびこの使用 |
-
2014
- 2014-09-25 JP JP2016516578A patent/JP2016531852A/ja active Pending
- 2014-09-25 US US15/024,496 patent/US9975918B2/en active Active
- 2014-09-25 CN CN201480063706.0A patent/CN105744937A/zh active Pending
- 2014-09-25 EP EP14849674.8A patent/EP3049089B1/en active Active
- 2014-09-25 CN CN202110799536.4A patent/CN113845558A/zh active Pending
- 2014-09-25 ES ES14849674T patent/ES2751457T3/es active Active
- 2014-09-25 WO PCT/US2014/057497 patent/WO2015048316A1/en not_active Ceased
- 2014-09-25 HK HK16110801.0A patent/HK1222565A1/zh unknown
- 2014-09-25 KR KR1020167010304A patent/KR20160060688A/ko not_active Withdrawn
- 2014-09-25 AU AU2014324961A patent/AU2014324961A1/en not_active Abandoned
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