专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-10766921-B2 优先权日:2016-05-18 标 题 :Process and intermediates for the 6,7-alpha-epoxidation of steroid 4,6-dienes 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY 权利人:NZP UK LTD 摘要:The invention relates to a process for preparing a compound of general formula (Ia): wherein R2, Y, R4 and R5 are as defined herein, wherein the epoxidation is conducted using an oxidant and methyltrioxorhenium as a catalyst (MeReO3). The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.
专利号:US-10301350-B2 优先权日:2014-11-19 标题 :6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal FXR modulators 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; BOYDELL JAMES; OTTER CARL; WALLIS LAURA; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The invention relates to compounds of formula (I) and related methods, wherein R 1 , R 2 , Y, R 4 and R 5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids with pharmacological activity. The invention futher provides intermediated in the systhesis of obeticholic acid and its analogues. The invention also provides methods related to the synthesizing of these intermediates and methods of preparing obeticholic acid and obeticholic acid analogues from the compound of the invention.
专利号:US-10597423-B2 优先权日:2014-11-19 标题 :6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal FXR modulators 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; BOYDELL JAMES; WALLIS LAURA; OTTER CARL; DAVIES IEUAN; CLARKSON ROB 权利人:NZP UK LTD 摘要:Disclosed herein is a process for the preparation of a compound of formula (I) and related methods. The compounds of formula (I) are intermediates in the synthesis of synthetic bile acids and its analogues, and the compounds of formula (I) have pharmacological activity. Methods include the synthesizing of these intermediates, and methods of preparing obeticholic acid and obeticholic acid analogues from the prepared compounds.
专利号:US-10538550-B2 优先权日:2014-11-19 标 题:6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal FXR modulators 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; BOYDELL JAMES; WALLIS LAURA; BATCHELOR RHYS; OTTER CARL; DAVIES IEUAN 权利人:NZP UK LTD 摘要:The invention relates to compounds of formula (I) wherein R 1 , R 2 , Y 1 , R 4 and R 5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acid derivatives with pharmacological activity. The invention further provides methods related to the synthesizing of these intermediates, and methods of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-10131688-B2 优先权日:2014-11-19 标题:5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal FXR modulators 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; BOYDELL JAMES; WALLIS LAURA; BARTLETT NATHAN; SHELBOURNE MONTSERRAT 权利人:NZP UK LTD 摘要:The invention relates to compounds of formula (I): wherein R 1 , R 2 , Y, R 4 and R 5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.
参考标题: Intermediates For The Synthesis Of Bile Acid Derivatives, In Particular Of Obeticholic Acid Intermédiaires Pour La Synthèse De Dérivés De L'Acide Biliaire, En Particulier De L'Acide Obéticholique 摘要:The Invention Relates To Compounds Of General Formula (I): Wherein: R1,R2, R3, R4, R5, R6 And Y Are As Defined Herein. The Compounds Are Intermediates In The Synthesis Of Synthetic Bile Acids Which Are Useful In The Treatment Of Conditions Such As Liver Disease.
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198