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1. 发明申请

WO2012037261A2 6-SUBSTITUTED DEMETHYL-ESTRADIOL DERIVATIVES AS ER-BETA AGONISTS 审中-公开
标题翻译： 6-取代的DEMETHYL-ESTRADIOL衍生物作为ER-BETA AGONISTS
公开(公告)号：WO2012037261A2
公开(公告)日：2012-03-22
申请号：PCT/US2011051608
申请日：2011-09-14
申请人： ENDECE LLC , YARGER JAMES G , NYE STEVEN H
发明人： YARGER JAMES G , NYE STEVEN H
IPC分类号： C07J1/00 , A61K31/565
CPC分类号： C07J1/007 , A61K31/56 , C07J1/0059 , C07J1/0074 , C07J17/00 , C07J31/006 , C07J41/0016 , C07J41/0044 , C07J51/00
摘要： Disclosed herein are 6-substituted 13-demethyl- estradiol derivatives as selective ERß agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.
摘要翻译：本文公开了作为选择性ERβ激动剂的6-取代的13-去甲基 - 雌二醇衍生物。还公开了通过施用这些6-取代的13-去甲基 - 雌二醇衍生物来治疗疼痛的方法。

2. 发明申请

WO2011066542A3 6-SUBSTITUTED ESTRADIOL DERIVATIVES AND METHODS OF USE 审中-公开
公开(公告)号：WO2011066542A3
公开(公告)日：2011-06-03
申请号：PCT/US2010/058342
申请日：2010-11-30
申请人： ENDECE INC. , YARGER, James, G.
发明人： YARGER, James, G.
IPC分类号： C07J1/00 , A61K31/565 , A61P35/00
摘要： Disclosed are compounds of the formula (I): where in R 1 , R 2 , R 3 and R 4 are independent l y hydrogen, C 1 -C 6 alkyl, halo, a sulfate, a glucuronide, -OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N ( CH 2 ) n ; a phosphate group, and a phosphinate group; R 9 is hydrogen, halogen or alkyl; R11 i s selected from the group consisting of H, C 1 -C 6 alkyl, halogen, a sulfate, a glucoronide, - SO 2 NH 2 , -COOH, -CN, -CH 2 CN-, -NHCN-, -CHO, =CHOCH 3 , -COO salt, -0S0 2 alkyl, -NH 2 , and -NHCO ( CH 2 ) n; R 12 is selected from the group consisting o f H, a C 1 -C 6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X i s selected from the group consisting of C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, halogen, a glucoronide, -NH 2 , - SO 2 NH 2 , -COOH, -CN, -CH 2 CN, -NHCN, -CHO, -COOsalt, -0S0 2 alkyl, - SH, - SCH 3 , -CH [ ( CH 2 ) n CH 3 ] COOCH 3 , - ( CH 2 ) mCOOCH 3 , - ( CH 2 U-O-CH 3 , - ( CH 2 ) m-0- ( CH 2 ) n CH 3 , ( CH 2 ) m - S -CH 3 , - ( CH 2 U- S - ( CH 2 ) n CH 3 , - ( CH 2 ) m -NH- ( CH 2 ) n CH 3 , -C 2 -C 8 alkenyl -0- ( CH 2 ) n CH 3 , - C 2 -C 8 alkenyl - S - ( CH 2 ) n CH 3 , -C 2 -C 8 alkenyl -N- ( CH 2 ) n CH 3 , -C 2 -C 8 alkynyl -O- ( CH 2 ) n CH 3 , -C 2 -C 8 alkynyl - S - ( CH 2 ) n CH 3 , -C 2 -C 8 alkynyl -N- ( CH 2 ) n CH 3 , - ( CH 2 U-OH, - ( CH 2 ) m -O-NH 2 , - ( CH 2 ) m - S -NH 2 , -NH ( CH 2 ) m CH 3 , -NH ( CH 2 ) m OCH 3 , -NH ( CH 2 ) m CHOH-COOH, -N ( CH 3 ) 2 , - ( CH 2 ) m (NH ) CH 2 OH, -NHCOOH, - ( CH 2 ) m NHCOOH, -NO 2 , - SCN, - S0 2 alkyl, -B ( OH ) 2 , - ( CH 2 ) m N ( CH 3 ) - SO 2 -NH 3 , - ( CH 2 ) m -NH- SO 2 -NH 2 ,-NHC ( = S) CH 3 , and -NHNH 2 ; and Y is selected from hydrogen, =0, -OCO(R 6 ) and -OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the Λ/WV symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.

3. 发明申请

WO2012129324A2 6-SUBSTITUTED ESTRADIOL DERIVATIVES FOR USE IN REMYELINATION OF NERVE AXONS 审中-公开
标题翻译：用于神经轴恢复的6-取代的雌二醇衍生物
公开(公告)号：WO2012129324A2
公开(公告)日：2012-09-27
申请号：PCT/US2012/029973
申请日：2012-03-21
申请人： ENDECE LLC , YARGER, James, G. , NYE, Steve
发明人： YARGER, James, G. , NYE, Steve
IPC分类号： A61K31/56 , A61K31/565 , A61K31/57 , A61P25/00
CPC分类号： A61K31/565 , A61K31/566 , A61K31/568 , A61K31/5685 , A61K45/06 , A61K2300/00
摘要： Disclosed is a method of remyelinating axons with 6-substituted estradiol compounds of the formula. The method can be used to treat a variety of demyelinating diseases
摘要翻译：公开了用下式的6-取代雌二醇化合物对轴突进行再髓鞘化的方法。该方法可用于治疗各种脱髓鞘疾病

4. 发明申请

WO2007041564A2 (S)-6-METHYLOXAALKYL EXEMESTANE COMPOUNDS AND RELATED METHODS OF USE 审中-公开
标题翻译：（S）-6-甲氧基亚苄基化合物及相关使用方法
公开(公告)号：WO2007041564A2
公开(公告)日：2007-04-12
申请号：PCT/US2006038583
申请日：2006-10-02
申请人： ENDECE LLC , PARIZA RICHARD J , YARGER JAMES G
发明人： PARIZA RICHARD J , YARGER JAMES G
IPC分类号： A61K31/57 , C07J1/00
CPC分类号： C07J1/0003 , A61K31/565 , A61K31/57 , C07J1/00
摘要： 6-Methyloxaalkyl exemestane compounds and related compositions, as can be used, chemotherapeutically, to inhibit growth and proliferation of cancer cells.
摘要翻译： 6-甲基恶唑烷基依西美坦化合物和可用于化学治疗抑制癌细胞生长和增殖的相关组合物。

5. 发明申请

WO2012129324A9 6-SUBSTITUTED ESTRADIOL DERIVATIVES FOR USE IN REMYELINATION OF NERVE AXONS 审中-公开
标题翻译：用于神经轴恢复的6-取代的雌二醇衍生物
公开(公告)号：WO2012129324A9
公开(公告)日：2012-11-15
申请号：PCT/US2012029973
申请日：2012-03-21
申请人： ENDECE LLC , YARGER JAMES G , NYE STEVE
发明人： YARGER JAMES G , NYE STEVE
IPC分类号： A61K31/56 , A61K31/565 , A61K31/57 , A61P25/00
CPC分类号： A61K31/565 , A61K31/566 , A61K31/568 , A61K31/5685 , A61K45/06 , A61K2300/00

6. 发明申请

WO2012037261A3 6-SUBSTITUTED DEMETHYL-ESTRADIOL DERIVATIVES AS ER-BETA AGONISTS 审中-公开
公开(公告)号：WO2012037261A3
公开(公告)日：2012-03-22
申请号：PCT/US2011/051608
申请日：2011-09-14
申请人： ENDECE, LLC , YARGER, James G. , NYE, Steven H.
发明人： YARGER, James G. , NYE, Steven H.
IPC分类号： C07J1/00 , A61K31/565
摘要： Disclosed herein are 6-substituted 13-demethyl- estradiol derivatives as selective ERβ agonists. Also disclosed is a method for treating pain by administering these 6-substituted 13-demethyl-estradiol derivatives.

7. 发明申请

WO2011066542A2 6-SUBSTITUTED ESTRADIOL DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译： 6-取代的雌二醇衍生物及其使用方法
公开(公告)号：WO2011066542A2
公开(公告)日：2011-06-03
申请号：PCT/US2010058342
申请日：2010-11-30
申请人： ENDECE INC , YARGER JAMES G
发明人： YARGER JAMES G
IPC分类号： C07J1/00 , A61K31/565 , A61P35/00
CPC分类号： C07J1/0059 , C07J1/007 , C07J1/0074 , C07J41/0044 , C12N5/0693 , C12N2501/392
摘要： Disclosed are compounds of the formula (I): where in R1, R2, R3 and R4 are independent l y hydrogen, C1 -C6 alkyl, halo, a sulfate, a glucuronide, -OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N ( CH2 ) n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 i s selected from the group consisting of H, C1 -C6 alkyl, halogen, a sulfate, a glucoronide, - SO2NH2, -COOH, -CN, -CH2CN-, -NHCN-, -CHO, =CHOCH3, -COO salt, -0S02alkyl, -NH2, and -NHCO ( CH2 ) n; R12 is selected from the group consisting o f H, a C1 -C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X i s selected from the group consisting of C1 -C12 alkyl, C2 -C12 alkenyl, C2 -C12 alkynyl, halogen, a glucoronide, -NH2, - SO2NH2, -COOH, -CN, -CH2CN, -NHCN, -CHO, -COOsalt, -0S02alkyl, - SH, - SCH3, -CH [ ( CH2 ) nCH3 ] COOCH3, - ( CH2 ) mCOOCH3, - ( CH2 U-O-CH3, - ( CH2 ) m-0- ( CH2 ) nCH3, ( CH2 ) m- S -CH3, - ( CH2 U- S - ( CH2 ) nCH3, - ( CH2 ) m-NH- ( CH2 ) nCH3, -C2 -C8 alkenyl -0- ( CH2 ) nCH3, - C2 -C8 alkenyl - S - ( CH2 ) nCH3, -C2 -C8 alkenyl -N- ( CH2 ) nCH3, -C2 -C8 alkynyl -O- ( CH2 ) nCH3, -C2 -C8 alkynyl - S - ( CH2 ) nCH3, -C2 -C8 alkynyl -N- ( CH2 ) nCH3, - ( CH2 U-OH, - ( CH2 ) m-O-NH2, - ( CH2 ) m- S -NH2 , -NH ( CH2 ) mCH3, -NH ( CH2 ) mOCH3, -NH ( CH2 ) mCHOH-COOH, -N ( CH3 ) 2, - ( CH2 ) m (NH ) CH2OH, -NHCOOH, - ( CH2 ) mNHCOOH, -NO2, - SCN, - S02alkyl, -B ( OH ) 2, - ( CH2 ) m N ( CH3 ) - SO2 -NH3, - ( CH2 ) m-NH- SO2 -NH2,-NHC ( = S) CH3, and -NHNH2; and Y is selected from hydrogen, =0, -OCO(R6) and -OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the ?/WV symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.
摘要翻译：公开了式（I）的化合物：其中R1，R2，R3和R4独立地为氢，C1-C6烷基，卤素，硫酸根，葡糖苷酸，-OH，大体积基团，芳基，环烷基，杂芳基，杂环烷基，N（CH 2）n; 磷酸酯基和次膦酸酯基; R9是氢，卤素或烷基; R 11选自H，C 1 -C 6烷基，卤素，硫酸根，葡萄糖醛酸，-SO 2 NH 2，-COOH，-CN，-CH 2 CN - ， - NHCN-， - CHO，= CHOCH 3，-COO盐， -OSO 2烷基，-NH 2和-NHCO（CH 2）n; R 12选自H，C 1 -C 6烷基，硫酸根，葡糖苷酸，大体积基团，芳基，环烷基，杂芳基和杂环烷基; X选自C 1 -C 12烷基，C 2 -C 12烯基，C 2 -C 12炔基，卤素，葡糖苷酸，-NH 2，-SO 2 NH 2，-COOH，-CN，-CH 2 CN，-NHCN，-CHO，（CH 2）n CO 3 CH 3， - （CH 2）m COOCH 3， - （CH 2 UO-CH 3， - （CH 2）m -O- m -CH 3， - （CH 2 U-S - （CH 2）n CH 3， - （CH 2）m -NH-（CH 2）n CH 3，-C 2 -C 8烯基-O-（CH 2）n CH 3，-C 2 -C 8烯基 - S - （CH 2）n CH 3，-C 2 -C 8烯基-N-（CH 2）n CH 3，-C 2 -C 8炔基-O-（CH 2）n CH 3，-C 2 -C 8炔基-S-（CH 2）n CH 3，-C 2 -C 8 炔基-N-（CH2）nCH3， - （CH2U-OH， - （CH2）mO-NH2， - （CH2）m-S -NH2，-NH（CH2）mCH3，-NH（CH2）mOCH3，（CH2）mCHOH-COOH，-N（CH3）2， - （CH2）m（NH）CH2OH，-NHCOOH， - （CH2）mNHCOOH，-NO2，-SCN，-SO2烷基，-B（OH）（CH 2）m N（CH 3）-SO 2 -NH 3， - （CH 2）m -NH-SO 2 -NH 2，-NHC（= S）CH 3和-NHNH 2; Y选自氢，= 0，-OCO R6）和-OH;其中m是0-20之间的整数，n是整数在0-8之间，符号表示能够在3或17位形成酮基的单键或双键; 和/或WV符号代表任何类型的债券，而不管立体化学; 以及所述化合物的各自的对映异构体，其它立体化学异构体，水合物，溶剂合物，互变异构体和药学上可接受的盐。该化合物可用于治疗各种类型的癌症。

8. 发明申请

WO2007041564A3 (S)-6-METHYLOXAALKYL EXEMESTANE COMPOUNDS AND RELATED METHODS OF USE 审中-公开
公开(公告)号：WO2007041564A3
公开(公告)日：2007-04-12
申请号：PCT/US2006/038583
申请日：2006-10-02
申请人： ENDECE, LLC , PARIZA, Richard, J. , YARGER, James, G.
发明人： PARIZA, Richard, J. , YARGER, James, G.
IPC分类号： A61K39/395 , C07D215/04
摘要： 6-Methyloxaalkyl exemestane compounds and related compositions, as can be used, chemotherapeutically, to inhibit growth and proliferation of cancer cells.

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