该化合物是一种微酸衍生物,具体来说是一种胆碱酯酶合成的丙氧基酸,一种在水中溶解的白色至非白粉粉粉,由于其缺水类类类固醇核和嗜血性厌氨酸,具有很强的非对症性质.TDCA在肠中饮食脂肪和脂肪溶解维生素的乳化和吸收方面发挥着关键作用.它参与了胆固醇新陈代谢的调控工作,并且已经就其在肝脏疾病和代谢紊乱中的潜在治疗作用进行了研究.该化合物具有相对高的pKA,表明其主要存在于生理pH的厌离形式中.此外,TECA可以影响各种细胞信号路径,包括与炎症和流行有关的路径.其生物活动和与特定受体的相互作用,如远nesidy X 受体(FXR),使其成为对物理和临床应用的兴趣对象.
专利号:US-2009264300-A1 优先权日:2005-12-01 标题 :Enzymatic encoding methods for efficient synthesis of large libraries
专利号:EP-1957644-B1 优先权日:2005-12-01 标 题 :Enzymatic encoding methods for efficient synthesis of large libraries
专利号:US-9295677-B2 优先权日:2008-02-26 标题 :Polyhydroxylated bile acids for treatment of biliary disorders 发明人:LING VICTOR; WANG RENXUE; SHEPS JONATHAN AHAB 权利人:LING VICTOR; WANG RENXUE; SHEPS JONATHAN AHAB; QING BILE THERAPEUTICS INC 摘要:The invention provides, in part, polyhydroxylated bile acids for treating biliary disorders, for example, biliary disorders arising out of cholestasis of portal hypertension. The invention also provides, in part, polyhydroxylated bile acids for stimulating bile flow. New compounds 2α,3α,7α,12α-tetrahydroxy-5β-cholanoic acid and 3α.4α,7α,12α-tetrahydroxy-5β-cholanoic acid are disclosed, uses thereof and synthesis thereof.
专利号:EP-1957644-A2 优先权日:2005-12-01 标题 :Enzymatic encoding methods for efficient synthesis of large libraries
专利号:US-7064122-B2 优先权日:2001-12-20 标题:Pancreatic lipase inhibitor compounds, their synthesis and use 发明人:WITTER DAVID; CASTELHANO ARLINDO 权利人:OSI PHARM INC 摘要:The subject invention features compounds having the structure: n n nwherein X is O, S, CH 2 or NR 5 ; Y is O or S; R 1 is H, substituted or unsubstituted C 1 -C 15 alkyl, C 1 -C 8 alkylaryl, —C(O)OR 4 , —C(O)NR 4 R 5 , —CR 6 R 6′ OR 4 , —CR 6 R 6′ OC(O)R 4 , —CR 6 R 6′ OC(O)NHR 7 , —C(O)NR 10 R 11 , —C(O)NR 8 R 9 NR 8 R 9 , —N(R 5 )C(O)NHR 5 , or CH 2 R 4 ; R 2 is a substituted or unsubstituted, straight chain C 1 —C 30 alkyl or branched C 3 -C 30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R 3 is H or substituted or unsubstituted C 1 -C 6 alkyl or C 3 -C 10 cycloalkyl; R 4 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl, —CH 2 -aryl, aryl —C 1 -C 15 alkyl, heteroaryl-C 1 -C 15 alkyl or C 3 -C 10 cycloalkyl; R 5 is H or a substituted or unsubstituted, straight chain or branched, C 6 -C 30 alkyl, aryl C 1 -C 30 alkyl, heteroarylalkyl or cycloalkyl; R 6 and R 6′ are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, dialkyl or C 3 -C 10 cycloalkyl or together form a 3-7 membered ring system; R 7 is H or substituted or unsubstituted C 1 -C 12 alkyl or C 3 -C 10 cycloalkyl; R 8 and R 9 are each independently H, substituted or unsubstituted C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkylaryl, or NR 8 R 9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
专利号:EP-2341140-A1 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries