JP2012509349A5 - - Google Patents
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- Publication number
- JP2012509349A5 JP2012509349A5 JP2011537627A JP2011537627A JP2012509349A5 JP 2012509349 A5 JP2012509349 A5 JP 2012509349A5 JP 2011537627 A JP2011537627 A JP 2011537627A JP 2011537627 A JP2011537627 A JP 2011537627A JP 2012509349 A5 JP2012509349 A5 JP 2012509349A5
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- JP
- Japan
- Prior art keywords
- compound
- salt
- solvate
- properly
- formula
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 16
- 239000012453 solvate Substances 0.000 claims description 14
- 229910052739 hydrogen Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 7
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 201000010099 disease Diseases 0.000 claims description 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims description 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 2
- 229940125773 compound 10 Drugs 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- ZLVXBBHTMQJRSX-VMGNSXQWSA-N jdtic Chemical compound C1([C@]2(C)CCN(C[C@@H]2C)C[C@H](C(C)C)NC(=O)[C@@H]2NCC3=CC(O)=CC=C3C2)=CC=CC(O)=C1 ZLVXBBHTMQJRSX-VMGNSXQWSA-N 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 7
- 150000001413 amino acids Chemical class 0.000 description 7
- -1 hydrate Chemical class 0.000 description 2
- GKSUUVIIAXVCBE-VIPHVISISA-N CC[C@H]([C@H](C[C@@H](CC1)O)[C@@]1(C)C(CC1)C2C(C3)[C@@]1(C)[C@@H]([C@H](C)CCC(O)=O)[C@H]3O)[C@H]2O Chemical compound CC[C@H]([C@H](C[C@@H](CC1)O)[C@@]1(C)C(CC1)C2C(C3)[C@@]1(C)[C@@H]([C@H](C)CCC(O)=O)[C@H]3O)[C@H]2O GKSUUVIIAXVCBE-VIPHVISISA-N 0.000 description 1
- 0 CC[C@]([C@](C[C@@](CC1)O)[C@@]1(C)C1C2C(C[C@](*)[C@@]3[C@](C)CCC(O)=O)[C@]3(C)C(*)C1)[C@]2O Chemical compound CC[C@]([C@](C[C@@](CC1)O)[C@@]1(C)C1C2C(C[C@](*)[C@@]3[C@](C)CCC(O)=O)[C@]3(C)C(*)C1)[C@]2O 0.000 description 1
- 208000010643 digestive system disease Diseases 0.000 description 1
- 208000016097 disease of metabolism Diseases 0.000 description 1
- 208000018685 gastrointestinal system disease Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08169460.6 | 2008-11-19 | ||
| EP08169460 | 2008-11-19 | ||
| PCT/US2009/065199 WO2010059859A1 (en) | 2008-11-19 | 2009-11-19 | Tgr5 modulators and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012509349A JP2012509349A (ja) | 2012-04-19 |
| JP2012509349A5 true JP2012509349A5 (enExample) | 2013-01-10 |
| JP5639073B2 JP5639073B2 (ja) | 2014-12-10 |
Family
ID=41666760
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011537627A Expired - Fee Related JP5639073B2 (ja) | 2008-11-19 | 2009-11-19 | Ｔｇｒ５モジュレーターおよびその使用方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US8999964B2 (enExample) |
| EP (2) | EP2373673B1 (enExample) |
| JP (1) | JP5639073B2 (enExample) |
| CN (2) | CN102282157B (enExample) |
| AU (1) | AU2009316484B2 (enExample) |
| BR (1) | BRPI0921992B1 (enExample) |
| CA (1) | CA2744135C (enExample) |
| ES (2) | ES2592452T3 (enExample) |
| IL (1) | IL212970A (enExample) |
| WO (1) | WO2010059859A1 (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201270778A1 (ru) | 2010-05-06 | 2013-04-30 | Бристол-Майерс Сквибб Компани | Бициклические гетероарильные аналоги в качестве модуляторов рецептора gpr119 |
| EP2702042A1 (en) | 2011-04-28 | 2014-03-05 | Bristol-Myers Squibb Company | Novel bicyclic nitrogen containing heteroaryl tgr5 receptor modulators |
| BR112015009395A2 (pt) * | 2012-10-26 | 2017-07-04 | Intercept Pharmaceuticals Inc | processo para preparação de derivados do ácido biliar |
| BR112015012312A2 (pt) * | 2012-11-28 | 2017-07-11 | Intercept Pharmaceuticals Inc | método de tratamento, redução do risco, prevenção ou alívio de uma afecção ou doença pulmonar em um sujeito; método de redução ou supressão de inflamação no pulmão em um sujeito; e método de promoção de reparo pulmonar em um sujeito |
| EP3008091A1 (en) | 2013-06-13 | 2016-04-20 | Fast Forward Pharmaceuticals B.V. | Cd40 signalling inhibitor and a further compound, wherein the further compound is a bile acid, a bile acid derivative, an tgr5-receptor agonist, an fxr agonist or a combination thereof, for the treatment of chronic inflammation, and the prevention of gastrointestinal cancer or fibrosis. |
| WO2015181275A1 (en) * | 2014-05-29 | 2015-12-03 | Bar Pharmaceuticals S.R.L. | Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases |
| 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) |
| 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 |
| CA2968404A1 (en) * | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| CN105348365A (zh) * | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一种胆酸衍生物及其制备方法、药物组合物和用途 |
| CN104523703A (zh) * | 2014-12-24 | 2015-04-22 | 聂飚 | 一种游离脂肪酸转运蛋白小分子抑制物的应用 |
| CN104672290B (zh) * | 2015-01-05 | 2017-06-06 | 北京普禄德医药科技有限公司 | 一种用于预防或治疗fxr‑介导的疾病的药物及其制备方法和用途 |
| CN105330554B (zh) | 2015-02-15 | 2017-07-11 | 上海迪赛诺药业股份有限公司 | 手性环丙基乙炔基叔醇类化合物的合成方法 |
| CN105985396A (zh) | 2015-02-16 | 2016-10-05 | 苏州泽璟生物制药有限公司 | 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物 |
| US10800807B2 (en) * | 2015-06-19 | 2020-10-13 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| CN106854229A (zh) * | 2015-12-08 | 2017-06-16 | 陈剑 | 一类脂肪酸盐,其制备及其在医药上的应用 |
| 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 |
| CN109641934B (zh) * | 2016-09-20 | 2021-07-02 | 江苏豪森药业集团有限公司 | 胆酸衍生物游离碱，晶型及其制备方法和应用 |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| JP2022552655A (ja) | 2019-10-07 | 2022-12-19 | キャリーオペ，インク． | Ｇｐｒ１１９アゴニスト |
| PH12022552277A1 (en) | 2020-02-28 | 2024-03-04 | Kallyope Inc | Gpr40 agonists |
| JP2023526625A (ja) | 2020-05-19 | 2023-06-22 | キャリーオペ，インク． | Ａｍｐｋアクチベーター |
| CN116390925A (zh) | 2020-06-26 | 2023-07-04 | 卡尔优普公司 | Ampk活化剂 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2696934B1 (fr) | 1992-10-20 | 1995-06-02 | Conservatoire Nal Arts Metiers | Dérivés de stéroïdes naturels 3B hydroxyles ayant des propriétés de déclenchement et de stimulation de l'immunité, composition les contenant et procédé pour les obtenir. |
| US7625887B2 (en) | 2003-01-28 | 2009-12-01 | Takeda Pharmaceutical Company Limited | Receptor agonists |
| WO2008091540A2 (en) | 2007-01-19 | 2008-07-31 | Intercept Pharmaceuticals, Inc. | 23-substituted bile acids as tgr5 modulators and methods of use thereof |
-
2009
- 2009-11-19 EP EP09759854.4A patent/EP2373673B1/en active Active
- 2009-11-19 EP EP16181337.3A patent/EP3150620B1/en active Active
- 2009-11-19 ES ES09759854.4T patent/ES2592452T3/es active Active
- 2009-11-19 WO PCT/US2009/065199 patent/WO2010059859A1/en not_active Ceased
- 2009-11-19 CA CA2744135A patent/CA2744135C/en active Active
- 2009-11-19 ES ES16181337T patent/ES2774368T3/es active Active
- 2009-11-19 CN CN200980154703.7A patent/CN102282157B/zh not_active Expired - Fee Related
- 2009-11-19 JP JP2011537627A patent/JP5639073B2/ja not_active Expired - Fee Related
- 2009-11-19 CN CN201610680498.XA patent/CN106380502A/zh active Pending
- 2009-11-19 AU AU2009316484A patent/AU2009316484B2/en not_active Ceased
- 2009-11-19 BR BRPI0921992-7A patent/BRPI0921992B1/pt not_active IP Right Cessation
- 2009-11-19 US US13/129,947 patent/US8999964B2/en active Active
-
2011
- 2011-05-18 IL IL212970A patent/IL212970A/en active IP Right Grant
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