JP2013500986A5 - - Google Patents
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- JP2013500986A5 JP2013500986A5 JP2012523043A JP2012523043A JP2013500986A5 JP 2013500986 A5 JP2013500986 A5 JP 2013500986A5 JP 2012523043 A JP2012523043 A JP 2012523043A JP 2012523043 A JP2012523043 A JP 2012523043A JP 2013500986 A5 JP2013500986 A5 JP 2013500986A5
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- JP
- Japan
- Prior art keywords
- compound according
- group
- compound
- deleted
- independently
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 24
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 125000003277 amino group Chemical group 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 125000000542 sulfonic acid group Chemical group 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US22938609P | 2009-07-29 | 2009-07-29 | |
| US61/229,386 | 2009-07-29 | ||
| PCT/US2010/043719 WO2011014661A2 (en) | 2009-07-29 | 2010-07-29 | Liver x receptor agonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013500986A JP2013500986A (ja) | 2013-01-10 |
| JP2013500986A5 true JP2013500986A5 (enExample) | 2013-08-15 |
Family
ID=43529941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012523043A Pending JP2013500986A (ja) | 2009-07-29 | 2010-07-29 | 肝臓x受容体アゴニスト |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8829213B2 (enExample) |
| EP (1) | EP2459581A4 (enExample) |
| JP (1) | JP2013500986A (enExample) |
| CN (1) | CN102482315A (enExample) |
| CA (1) | CA2769203A1 (enExample) |
| WO (1) | WO2011014661A2 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150158903A1 (en) | 2011-09-08 | 2015-06-11 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| CN103360453B (zh) * | 2012-04-04 | 2015-10-07 | 浙江大学 | 四环三萜类化合物的制备和抗衰老应用 |
| CN103360456B (zh) * | 2012-04-04 | 2015-07-29 | 浙江大学 | 三萜类化合物及制备和应用 |
| EP2759295A1 (en) | 2013-01-29 | 2014-07-30 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Foam cell specific Liver X Receptor (LXR) alpha agonist, SIRT1 inhibitors as well as p300 inhibitors as pharmaceutically active agents |
| LT2968369T (lt) | 2013-03-13 | 2018-12-27 | Sage Therapeutics, Inc. | Neuroaktyvūs steroidai ir jų panaudojimo būdai |
| CN104072564B (zh) * | 2013-03-28 | 2016-08-17 | 广州市赛普特医药科技股份有限公司 | 2β,3α,5α-三羟基-雄甾-6-酮及其制备方法与用途 |
| JP6320861B2 (ja) * | 2013-10-16 | 2018-05-09 | 株式会社ファンケル | コレステロール吸収阻害剤 |
| CA2939120A1 (en) | 2014-01-10 | 2015-07-16 | Rgenix, Inc. | Lxr agonists and uses thereof |
| ES2970222T3 (es) | 2014-06-18 | 2024-05-27 | Sage Therapeutics Inc | Oxiesteroles y procedimientos de uso de los mismos |
| WO2016079520A1 (en) | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| CN107108688B (zh) | 2014-11-19 | 2019-10-29 | Nzp英国有限公司 | 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇 |
| KR102526631B1 (ko) | 2014-11-19 | 2023-04-27 | 엔제트피 유케이 리미티드 | 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드 |
| MX375864B (es) | 2014-11-19 | 2025-03-07 | Nzp Uk Ltd | Esteroides de 5.beta-6-alquil-7-hidroxi-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr) |
| RS62220B1 (sr) | 2015-07-06 | 2021-09-30 | Sage Therapeutics Inc | Oksisteroli i postupci njihovog korišćenja |
| MX376833B (es) | 2015-07-06 | 2025-03-07 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| MA42409A (fr) | 2015-07-06 | 2018-05-16 | Sage Therapeutics Inc | Oxystérols et leurs procédés d'utilisation |
| EP3397258A2 (en) * | 2015-12-30 | 2018-11-07 | Consejo Nacional De Investigaciones Cientificas Y Tecnicas (CONICET) | Use of brassinosteroid analogs for the treatment of dermal disorders by selectively modulating liver x receptors (lxr) and dermal disease treatment by brassinosteroid analogs acting as selective liver x receptor (lxr) modulators |
| CA3010883A1 (en) | 2016-01-11 | 2017-07-20 | The Rockefeller University | Methods for the treatment of myeloid derived suppressor cells related disorders |
| CN114272249A (zh) | 2016-04-01 | 2022-04-05 | 萨奇治疗股份有限公司 | 氧甾醇及其使用方法 |
| CN106188205B (zh) * | 2016-05-06 | 2017-08-25 | 深圳以诺生物制药有限公司 | 一种罗汉果醇衍生物单体及其组合物的用途 |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| GB201608777D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Compounds |
| GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
| IT201600068742A1 (it) * | 2016-07-01 | 2018-01-01 | Bar Pharmaceuticals Soc A Responsabilita Limitata | Derivati dell'acido iodesossicolico e loro uso |
| AU2017292870B2 (en) | 2016-07-07 | 2021-10-07 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| EP3519422B1 (en) | 2016-09-30 | 2022-08-31 | Sage Therapeutics, Inc. | C7 substituted oxysterols and these compounds for use as nmda modulators |
| KR20250054838A (ko) | 2016-10-18 | 2025-04-23 | 세이지 테라퓨틱스, 인크. | 옥시스테롤 및 그의 사용 방법 |
| ES2952106T3 (es) | 2016-10-18 | 2023-10-27 | Sage Therapeutics Inc | Oxisteroles y procedimientos de utilización de los mismos |
| EP3713575A4 (en) | 2017-11-21 | 2021-08-25 | Rgenix, Inc. | POLYMORPHS AND THEIR USES |
| WO2020041673A1 (en) | 2018-08-23 | 2020-02-27 | President And Fellows Of Harvard College | Compositions and methods related to cholic acid-7-sulfate as a treatment for diabetes |
| EP3890745B1 (en) | 2018-12-04 | 2025-11-19 | President and Fellows of Harvard College | Synthetic derivatives of cholic acid 7-sulfate and uses thereof |
| EP3893887A4 (en) * | 2018-12-13 | 2023-01-04 | Eyenos, Inc. | LXR AGONIST IN TOPICAL OPHTHALMIC FORMULATION FOR THE TREATMENT OF DRY EYE |
| WO2020231776A1 (en) | 2019-05-10 | 2020-11-19 | President And Fellows Of Harvard College | Small molecule modulators of gut bacterial bile acid metabolism |
| JP7689964B2 (ja) | 2019-12-13 | 2025-06-09 | インスピルナ,インコーポレーテッド | 金属塩及びその使用 |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2698853A (en) * | 1951-08-11 | 1955-01-04 | Monsanto Chemicals | Oxidation of steroids |
| FR1482102A (fr) * | 1966-03-31 | 1967-05-26 | Centre Nat Rech Scient | Nouveaux dérivés de stéroïdes et procédé de préparation |
| US3784598A (en) * | 1972-01-20 | 1974-01-08 | Ciba Geigy Corp | Process for the conversion of a 3-hydroxy-5,6-oxido group of a steroid into a delta4-3-oxo group |
| JPS4976857A (enExample) | 1972-12-06 | 1974-07-24 | ||
| US3963765A (en) * | 1973-04-01 | 1976-06-15 | Yehuda Mazur | Preparation of derivatives of cholesterol |
| US3887545A (en) * | 1973-11-12 | 1975-06-03 | Hoffmann La Roche | Synthesis of 1{60 -hydroxylated cholesterol derivatives |
| US4006172A (en) * | 1976-04-26 | 1977-02-01 | The Upjohn Company | Process for 7-keto-Δ5 -steroids |
| US4125544A (en) * | 1977-06-09 | 1978-11-14 | G. D. Searle | 20/22/23/24-Oxa-7-oxocholesterols and esters thereof |
| DE2837414A1 (de) | 1977-08-29 | 1979-03-08 | Searle & Co | 25-alkylcholesterin-derivate |
| US4193930A (en) * | 1977-08-29 | 1980-03-18 | G. D. Searle & Co. | 25-Alkyl-3β-hydroxycholest-5-en-7-ones and esters thereof |
| JPS563000A (en) * | 1979-06-20 | 1981-01-13 | Green Cross Corp:The | Water-soluble cholesterol derivative |
| US4639420A (en) * | 1984-11-21 | 1987-01-27 | Schaffner Carl P | Method for the immunoanalysis of cholesterol epoxides |
| US4917998A (en) * | 1986-05-06 | 1990-04-17 | Epitope, Inc. | Method of detecting AIDS virus infection |
| IT1212141B (it) * | 1987-06-03 | 1989-11-08 | So Ri Far S R L | Composizioni farmaceutiche per la prevenzione e terapia della calcolosi delle vie biliari e della dispepsia biliare. |
| FI901659A7 (fi) * | 1987-10-13 | 1990-04-02 | Pfizer | 3,5-dihydroksi-6,8-nonadieenihapot ja johdannaiset kolesterolia alenta vina aineina |
| US5562910A (en) * | 1989-09-25 | 1996-10-08 | University Of Utah Research Foundation | Vaccine compositions and method for enhancing an immune response |
| US5506223A (en) * | 1990-08-29 | 1996-04-09 | Humanetics Corporation | Δ5-androstenes useful for promoting weight maintenance or weight loss and treatment process |
| JPH0749438B2 (ja) | 1990-10-31 | 1995-05-31 | 東京田辺製薬株式会社 | タウリン抱合型胆汁酸の精製方法 |
| IL105050A0 (en) | 1992-03-27 | 1993-07-08 | Lilly Co Eli | Steroid derivatives |
| IT1255241B (it) | 1992-07-22 | 1995-10-20 | Simos Contos | Derivato di acido biliare e suo uso in terapia |
| IT1255486B (it) * | 1992-08-04 | 1995-11-06 | Erregierre Ind Chim | Processo per preparare gli acidi biliari coniugati con la taurina |
| US5482935A (en) * | 1993-01-05 | 1996-01-09 | American Home Product Corporation | Anti-atherosclerotic use of 17 alpha-dihydroequilin |
| TW289757B (enExample) * | 1993-05-08 | 1996-11-01 | Hoechst Ag | |
| IT1270853B (it) * | 1993-05-20 | 1997-05-13 | Sanofi Elf | Procedimento per la preparazione di derivati taurocolanici |
| CN1055929C (zh) | 1993-09-20 | 2000-08-30 | 中国科学院上海有机化学研究所 | 三氟甲基甾体化合物及其制备方法 |
| IT1274000B (it) * | 1994-04-06 | 1997-07-14 | Alfa Wassermann Spa | Derivati di acidi biliari utili nella terapia della calcolosi biliare da colesterolo e nelle patologie indotte da colestasi |
| WO1995032215A1 (en) * | 1994-05-19 | 1995-11-30 | Merck & Co., Inc. | Oxidation of steroids having allylic groups |
| US5583239A (en) * | 1995-05-30 | 1996-12-10 | Lehigh University | Antimicrobial sterol conjugates |
| PL334840A1 (en) | 1997-01-24 | 2000-03-27 | Univ California | Application of fxr, pparalpha and lxralpha activators in order to restore the barrier function, to stimulate epithelium differentation and to inhibit proliferation |
| US6060465A (en) * | 1997-02-06 | 2000-05-09 | Miljkovic; Dusan | Bile acids and their derivatives as glycoregulatory agents |
| JP2002532729A (ja) * | 1998-12-23 | 2002-10-02 | グラクソ グループ リミテッド | 核内受容体のリガンドのアッセイ |
| US6465258B1 (en) * | 1999-01-07 | 2002-10-15 | Tularik, Inc. | FXR receptor-mediated modulation cholesterol metabolism |
| IL146223A0 (en) | 1999-04-30 | 2002-07-25 | Arch Dev Corp | Steroid derivatives |
| JP2002030097A (ja) * | 2000-07-11 | 2002-01-29 | Kyorin Pharmaceut Co Ltd | ステロイド誘導体の製造方法 |
| JP2002030096A (ja) * | 2000-07-11 | 2002-01-29 | Kyorin Pharmaceut Co Ltd | 神経細胞突起再生剤及びその製造方法 |
| DE10105041A1 (de) | 2001-02-05 | 2002-08-14 | Tell Pharm Ag Hergiswil | Tripeptide und Tripeptid-Derivate für die Behandlung neurodegenerativer Krankheiten |
| CN1498222A (zh) * | 2001-02-08 | 2004-05-19 | 芝加哥大学 | 类固醇衍生物 |
| DK1392713T3 (da) * | 2001-05-03 | 2008-02-18 | Univ Chicago | Lever-X-receptoragonister |
| US7078396B2 (en) * | 2001-05-03 | 2006-07-18 | Arch Development Corporation | Method of treating disorder related to high cholesterol concentration |
| EP1450816A4 (en) | 2001-11-08 | 2008-02-13 | Univ Chicago | METHOD OF TREATING DISORDERS RELATED TO HIGH CHOLESTEROL RATE |
| CA2482195A1 (en) | 2002-04-12 | 2003-10-23 | The University Of Chicago | Farnesoid x-activated receptor agonists |
| US20070032464A1 (en) * | 2004-10-08 | 2007-02-08 | Shutsung Liao | Methods of treating cancers |
-
2010
- 2010-07-29 EP EP10805047A patent/EP2459581A4/en not_active Withdrawn
- 2010-07-29 US US12/846,326 patent/US8829213B2/en not_active Expired - Fee Related
- 2010-07-29 WO PCT/US2010/043719 patent/WO2011014661A2/en not_active Ceased
- 2010-07-29 CN CN2010800336173A patent/CN102482315A/zh active Pending
- 2010-07-29 CA CA2769203A patent/CA2769203A1/en not_active Abandoned
- 2010-07-29 JP JP2012523043A patent/JP2013500986A/ja active Pending
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