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1. 发明申请

WO2013014569A1 QUINOLINYL GLUCAGON RECEPTOR MODULATORS 审中-公开
标题翻译：喹啉吡咯烷酮受体调节剂
公开(公告)号：WO2013014569A1
公开(公告)日：2013-01-31
申请号：PCT/IB2012/053575
申请日：2012-07-12
申请人： PFIZER INC. , DIDIUK, Mary , FILIPSKI, Kevin J. , GUZMAN-PEREZ, Angel , LEE, Esther C. , PFEFFERKORN, Jeffrey A. , STEVENS, Benjamin , TU, Meihua
发明人： DIDIUK, Mary , FILIPSKI, Kevin J. , GUZMAN-PEREZ, Angel , LEE, Esther C. , PFEFFERKORN, Jeffrey A. , STEVENS, Benjamin , TU, Meihua
IPC分类号： C07D215/38 , C07D239/94 , A61K31/47 , A61K31/502 , A61P3/10
CPC分类号： C07D239/84 , A61K31/517 , C07D215/38 , C07D217/22 , C07D239/94 , C07D241/44
摘要： The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , A 1 , A 2 , A 3 , B 1 , B 2 , B 3 and B 4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
摘要翻译：本发明提供式I化合物或其药学上可接受的盐，其中R1，R2，R3，A1，A2，A3，B1，B2，B3和B4如本文所定义。已经发现式I的化合物用作胰高血糖素拮抗剂或反向激动剂。因此，式I化合物及其药物组合物可用于治疗由胰高血糖素介导的疾病，病症或病症。

2. 发明申请

WO2004046162A3 NON-STEROIDAL FXR AGONISTS 审中-公开
公开(公告)号：WO2004046162A3
公开(公告)日：2004-06-03
申请号：PCT/US2003/036195
申请日：2003-11-14
申请人： THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, Kyriacos, C. , ROECKER, Anthony, J. , HUGHES, Robert , PFEFFERKORN, Jeffrey, A.
发明人： NICOLAOU, Kyriacos, C. , ROECKER, Anthony, J. , HUGHES, Robert , PFEFFERKORN, Jeffrey, A.
IPC分类号： C07C233/61
摘要： ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, phenyl, or NH(C1-C8)alkyl; L1 and L2 are both H, or together form a pi-bond; X1 is C(O), or CH2; Y1 is H, NHZ1, NH(Z2)Z3, or OZ4; aryl moiety A1 is selected from the group of radicals consisting of: INSERT FORMULA A2 and G1 - G11 are as defined in the specification; and T1 and T2 are each independently O, S, NH, or N(C1-C8)alkyl. The FXR agonists are useful as therapeutic agents for the treatment of diseases linked to cholesterol, bile acids, and their metabolism and homeostasis.

3. 发明申请

WO2006056845A1 7-(2H-PYRAZOL-3-YL)-3, 5-DIHYROXY-HEPTANOIC ACID DERIVATIVES AS HMG CO-A REDUCTASE INHIBITORS FOR THE TREATMENT OF LIPIDEMIA 审中-公开
标题翻译： 7-（2H-PYRAZOL-3-YL）-3,5-二羟基乙酸衍生物作为HMG CO-A还原酶抑制剂用于治疗LIPIDEMIA
公开(公告)号：WO2006056845A1
公开(公告)日：2006-06-01
申请号：PCT/IB2005/003461
申请日：2005-11-14
申请人： WARNER-LAMBERT COMPANY LLC , CHOI, Chulho , HUTCHINGS, Richard, H. , PFEFFERKORN, Jeffrey, A. , BOWLES, Daniel, Merritt , PARK, William, Keun, Chan
发明人： CHOI, Chulho , HUTCHINGS, Richard, H. , PFEFFERKORN, Jeffrey, A. , BOWLES, Daniel, Merritt , PARK, William, Keun, Chan
IPC分类号： C07D231/14 , C07D405/06 , A61P3/06 , A61P3/10
CPC分类号： C07D231/12 , C07D231/14 , C07D401/06 , C07D401/12 , C07D405/06
摘要： The present invention provides compounds of the formula (I), (IV) and (V) and intermediates of the formuale (VI) and (VII): (I), (IV), (V), (VI), (VII). wherein: R 1 is hydrogen, halogen, C 1 -C 7 alkyl, C 3 -C 8 cycloalkyl, aryl, aralkyl, heteroaryt, or heteroaralkyl; more specifically, R 1 is C 1 -C 7 alkyl or C 3 -C 8 cycloalkyl; even more specifically, R 1 is isopropyl; where alkyl, cycloalkyt, aryl, aralkyt, heteroaryl, or heteroaralkyl of R 1 is optionally substituted, R 2 is hydrogen, halogen, C 1 -C 7 alkyl, C 3 -C 8 cycloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, NC-, R 2b R 2a NCO(CH 2 ) n -, R 2b R 2a NS(O) n -, R 2c S(O) n -, R 2b R 2a N(CH 2 ) n -, R 2b -J-C(O)NR 2a (CH2) n -, R 2b -J-SO 2 NR 2a (CH 2 ) n -, R 2b -J-SONR 2a (CH 2 ) n , R 7 OOC(CH 2 ) n -, or R 7 CO(CH 2 ) n -; more specifically, R 2 is R 2b R 2a NCO(CH 2 ) n -; even more specifically, R 2 is R 2b R 2a NCO-; where alkyl, cycloalkyl, aryl , aralkyl, heteroaryl, or heteroaralkyl of R 2 is optionally substituted, R 3 is hydrogen, C 1-6 aikyl, C 3-6 necycloafkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; more specifically, R 3 is aryl; even more specifically, R 3 is phenyl or p-fluorophenyl; where alkyl, cycloalkyl, aryl, aralkyl, heteroaryt, or beteroaralkyd of A 3 is opltianally substituted and is a bond or is absent. The other substituents are defined in the claims. The present invention relates to compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents. Moree specifically, the present invention concerns certain potent inhibitors of the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A reductase ("HMG CoA reciuctase"). The compounds are useful for the treatement of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, Alzheimer's Disease, benign prostatic hypertrophy (BPH), diabetes and osteoporosis.
摘要翻译：（I），（IV），（V），（VI），（VII）所示的本发明提供式（I），（IV）和（V））。其中：R 1是氢，卤素，C 1 -C 7烷基，C 3 -C 3 环烷基，芳基，芳烷基，杂芳基或杂芳烷基; 更具体地说，R 1是C 1 -C 7烷基或C 3 -C 8烷基，环烷基; 甚至更具体地，R 1是异丙基; 其中R 1的烷基，环烷基，芳基，芳烷基，杂芳基或杂芳烷基任选被取代，R 2是氢，卤素，C 1 H 3， C 1 -C 7烷基，C 3 -C 8环烷基，芳基，芳烷基，杂芳基，杂芳烷基，NC-，R 2b， R 2 N 2 NCO（CH 2）n - ，R 2b R 2a， N（O）n - ，R 2c（O）n - ， - R 2b - N 2（CH 2）n - ，R 2b -JC（O）NR 2a，（CH 2）n - ， - R 2b - （CH 2）n N 2 - （CH 2）（CH 2）n， - - - - - - - - - - - - - - - - - （2） R 3，R 7，OOC（CH 2）n - ，或R 7 CO（ CH _{2 ）_{名词 - ; 更具体地说，R 2是R 2b R 2a NCO（CH 2）n N / N > - ; 甚至更具体地，R 2是R 2b R 2a NCO-; 其中R 2的烷基，环烷基，芳基，芳烷基，杂芳基或杂芳烷基任选被取代，R 3是氢，C 1-6 - 芳基，C 3-6亚烷基，芳基，芳烷基，杂芳基或杂芳烷基; 更具体地说，R 3是芳基; 甚至更具体地，R 3是苯基或对氟苯基; 其中A 3的烷基，环烷基，芳基，芳烷基，杂芳基或取代环烷基是被全面取代的并且是键或不存在。其它取代基在权利要求中限定。本发明涉及可用作低胆固醇血症和降血脂药物的化合物和药物组合物。特别地，本发明涉及3-羟基-3-甲基戊二酰辅酶A还原酶（“HMG CoA丝氨酸酶”）的某些有效抑制剂。这些化合物可用于治疗高脂血症，高胆固醇血症，高甘油三酯血症，动脉粥样硬化，阿尔茨海默病，良性前列腺肥大（BPH），糖尿病和骨质疏松症。}}

4. 发明申请

WO2004046162A2 NON-STEROIDAL FXR AGONISTS 审中-公开
标题翻译：非特异性FXR激素
公开(公告)号：WO2004046162A2
公开(公告)日：2004-06-03
申请号：PCT/US0336195
申请日：2003-11-14
申请人： SCRIPPS RESEARCH INST , NICOLAOU KYRIACOS C , ROECKER ANTHONY J , HUGHES ROBERT , PFEFFERKORN JEFFREY A
发明人： NICOLAOU KYRIACOS C , ROECKER ANTHONY J , HUGHES ROBERT , PFEFFERKORN JEFFREY A
IPC分类号： C07C233/54 , C07C233/63 , C07C275/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07D277/28 , C07D311/04 , C07D311/58 , C07D317/58 , C07D333/20 , C07D405/12 , C07D409/12 , C07J
CPC分类号： C07D405/12 , C07C233/54 , C07C233/63 , C07C275/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07C2601/14 , C07D277/28 , C07D311/04 , C07D311/58 , C07D317/58 , C07D333/20 , C07D409/12
摘要： ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, phenyl, or NH(C1-C8)alkyl; L1 and L2 are both H, or together form a pi-bond; X1 is C(O), or CH2; Y1 is H, NHZ1, NH(Z2)Z3, or OZ4; aryl moiety A1 is selected from the group of radicals consisting of: INSERT FORMULA A2 and G1 - G11 are as defined in the specification; and T1 and T2 are each independently O, S, NH, or N(C1-C8)alkyl. The FXR agonists are useful as therapeutic agents for the treatment of diseases linked to cholesterol, bile acids, and their metabolism and homeostasis.
摘要翻译：摘要有益的非甾体法尼醇X受体（FXR）激动剂是具有由下式（I）表示的化学结构的N-芳基-N-芳基甲基酰胺和脲基化合物：其中E1是（C1-C8）烷基，环己基，2-呋喃基，3-呋喃基，2-噻吩基，3-噻吩基，苯基或NH（C1-C8）烷基; L1和L2均为H，或一起形成π键; X1是C（O）或CH2; Y1是H，NHZ1，NH（Z2）Z3或OZ4; 芳基部分A1选自由以下组成的基团：插入物质A2和G1-G11如说明书中所定义; 且T1和T2各自独立地为O，S，NH或N（C1-C8）烷基。 FXR激动剂可用作治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗剂。

5. 发明申请

WO2004046162A8 NON-STEROIDAL FXR AGONISTS 审中-公开
标题翻译：非立体FXR激励
公开(公告)号：WO2004046162A8
公开(公告)日：2005-03-24
申请号：PCT/US0336195
申请日：2003-11-14
申请人： SCRIPPS RESEARCH INST , NICOLAOU KYRIACOS C , ROECKER ANTHONY J , HUGHES ROBERT , PFEFFERKORN JEFFREY A
发明人： NICOLAOU KYRIACOS C , ROECKER ANTHONY J , HUGHES ROBERT , PFEFFERKORN JEFFREY A
IPC分类号： C07C233/54 , C07C233/63 , C07C275/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07D277/28 , C07D311/04 , C07D311/58 , C07D317/58 , C07D333/20 , C07D405/12 , C07D409/12 , C07C233/61
CPC分类号： C07D405/12 , C07C233/54 , C07C233/63 , C07C275/42 , C07C323/40 , C07C323/41 , C07C323/44 , C07C2601/14 , C07D277/28 , C07D311/04 , C07D311/58 , C07D317/58 , C07D333/20 , C07D409/12
摘要： ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, phenyl, or NH(C1-C8)alkyl; L1 and L2 are both H, or together form a pi-bond; X1 is C(O), or CH2; Y1 is H, NHZ1, NH(Z2)Z3, or OZ4; aryl moiety A1 is selected from the group of radicals consisting of: INSERT FORMULA A2 and G1 - G11 are as defined in the specification; and T1 and T2 are each independently O, S, NH, or N(C1-C8)alkyl. The FXR agonists are useful as therapeutic agents for the treatment of diseases linked to cholesterol, bile acids, and their metabolism and homeostasis.
摘要翻译：摘要有益的非甾体法尼醇X受体（FXR）激动剂是具有由下式（I）表示的化学结构的N-芳基-N-芳基甲基酰氨基和脲基化合物：其中E1为（C1-C8）烷基，环己基，2-呋喃基，3-呋喃基，2-噻吩基，3-噻吩基，苯基或NH（C1-C8）烷基; L1和L2均为H，或一起形成π键; X1是C（O）或CH2; Y1是H，NHZ1，NH（Z2）Z3或OZ4; 芳基部分A1选自由以下组成的基团：插入物质A2和G1-G11如说明书中所定义; 并且T1和T2各自独立地为O，S，NH或N（C1-C8）烷基。 FXR激动剂可用作治疗与胆固醇，胆汁酸及其代谢和体内平衡相关的疾病的治疗剂。

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