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) | CN113845558A (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 |
|---|---|---|---|---|
| HUE071964T2 (hu) | 2015-07-06 | 2025-10-28 | Sage Therapeutics Inc | Oxiszterolok és alkalmazási eljárásaik |
| EP3828194B1 (en) | 2015-07-06 | 2025-04-16 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| SMT202200300T1 (it) | 2016-04-01 | 2022-09-14 | Sage Therapeutics Inc | Ossisteroli e relativi metodi d'uso |
| WO2017193046A1 (en) | 2016-05-06 | 2017-11-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| ES2935057T3 (es) | 2016-09-30 | 2023-03-01 | Sage Therapeutics Inc | C7 oxisteroles sustituidos y estos compuestos para su uso como moduladores de la NMDA |
| EP3525870B1 (en) * | 2016-10-14 | 2023-05-10 | Van Andel Research Institute | Highly potent glucocorticoids |
| KR20230051723A (ko) | 2016-10-18 | 2023-04-18 | 세이지 테라퓨틱스, 인크. | 옥시스테롤 및 그의 사용 방법 |
| RU2019115113A (ru) | 2016-10-18 | 2020-11-24 | Сейдж Терапьютикс, Инк. | Оксистеролы и способы их применения |
| CN115210229A (zh) | 2020-01-03 | 2022-10-18 | 博格有限责任公司 | 多环酰胺作为治疗癌症的ube2k调节剂 |
| 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 |
| CN120365344A (zh) * | 2024-01-24 | 2025-07-25 | 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 |
| WO2002102807A1 (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 |
| EA201000436A1 (ru) | 2007-10-04 | 2010-10-29 | Астразенека Аб | Стероидные [3,2-с]пиразольные соединения, обладающие глюкокортикоидной активностью |
| CN102361640B (zh) | 2009-01-13 | 2016-10-19 | 范安德尔研究所 | 异噁唑吡啶酮在制备用于缓解或减轻温血哺乳动物关节炎和哮喘的症状的药物中的用途 |
| 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 |
| CN102834406A (zh) * | 2009-06-16 | 2012-12-19 | 默沙东公司 | 作为糖皮质激素受体激动剂的新的[3.2-c]杂芳基甾体、其组合物和用途 |
-
2014
- 2014-09-25 JP JP2016516578A patent/JP2016531852A/ja active Pending
- 2014-09-25 HK HK16110801.0A patent/HK1222565A1/zh unknown
- 2014-09-25 CN CN202110799536.4A patent/CN113845558A/zh active Pending
- 2014-09-25 ES ES14849674T patent/ES2751457T3/es active Active
- 2014-09-25 KR KR1020167010304A patent/KR20160060688A/ko not_active Withdrawn
- 2014-09-25 AU AU2014324961A patent/AU2014324961A1/en not_active Abandoned
- 2014-09-25 CN CN201480063706.0A patent/CN105744937A/zh active Pending
- 2014-09-25 WO PCT/US2014/057497 patent/WO2015048316A1/en not_active Ceased
- 2014-09-25 US US15/024,496 patent/US9975918B2/en active Active
- 2014-09-25 EP EP14849674.8A patent/EP3049089B1/en active Active
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