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1. 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

2. 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.

3. 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.

4. 发明申请

WO2015143201A2 6-SUBSTITUTED ESTRADIOL DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的6-替代的雌二醇衍生物
公开(公告)号：WO2015143201A2
公开(公告)日：2015-09-24
申请号：PCT/US2015/021538
申请日：2015-03-19
申请人： ENDECE LLC
发明人： YARGER, James, G. , NYE, Steven, H.
IPC分类号： A61K31/565 , A61K31/56 , A61P25/28 , A61P25/00
CPC分类号： A61K31/565

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