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11. 发明专利

CA1187483A D-HOMO STEROIDS 未知
公开(公告)号：CA1187483A
公开(公告)日：1985-05-21
申请号：CA388479
申请日：1981-10-22
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , KELLER PETER , MUELLER MARCEL , KERB ULRICH , WIECHERT RUDOLF
IPC分类号： A61K31/16 , A61K31/19 , A61K31/215 , A61K31/275 , A61K31/34 , A61K31/56 , A61P13/02 , A61P15/00 , C07J63/00
摘要： D-Homosteroids of the formula I wherein R4 signifies hydrogen, methyl, chlorine or hydroxy; R6 signifies hydrogen or methylene; R17a.alpha. signifies hydrogen, methyl or chlorine and R17a.beta. signifies carboxy, esterified carboxy, cyano, formyl, carbamoyl, mono(lower alkyl)carbamoyl or di(lower alkyl -carbamoyl; or R17a.alpha. and R17a.beta. together signify a spiroether ring of the formula and wherein the dotted bonds in the D-ring represent an optional 16(17)- or 17(17a)-double bond, have anti-androgenic activity. They can be manufactured in various ways by the molecular transformation of other D-homosteroids.

12. 发明专利

AU537302B2 D-HOMOPREGNA-3,,20-DIONES 未知
公开(公告)号：AU537302B2
公开(公告)日：1984-06-14
申请号：AU5814880
申请日：1980-05-06
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FURST ANDOR , MULLER MARCEL , KERB ULRICH , KIESLICH KLAUS , WIECHERT RUDOLF
IPC分类号： C07J63/00 , C12P33/08

13. 发明专利

DK23984D0 未知
公开(公告)号：DK23984D0
公开(公告)日：1984-01-19
申请号：DK23984
申请日：1984-01-19
申请人： HOFFMANN LA ROCHE
发明人： FUERST ANDOR , MUELLER MARCEL , KERB ULRICH , WIECHERT RUDOLF
IPC分类号： A61K31/15 , A61K31/275 , C07J63/00 , C07J71/00 , C07J
摘要： The novel D-homosteroids of the formula I wherein R1 represents a -CN, =NOH or =CH-NHOH group; R2 represents oxo or, where R1 represents a -CN group, R2 represents oxo or a -OAc group; or R1 and R2 together with carbon atoms 2 and 3 of the steroid skeleton represents a [2,3-d]-fused isoxazole ring, a [3,2-c]-fused pyrazole ring, a [3,2-c]-fused N-acylated pyrazole ring or a [2,3-c]-fused furazan ring; Ac represents an acyl group; R3 and R4 represent methyl and R5 and R6 together represent an additional bond between carbon atoms 5 and 6 of the steroid skeleton; or R4 and R5 together represent -O-, R3 represents hydrogen or methyl, and R6 represents hydrogen; R7 represents hydrogen, lower-alkyl or ethynyl; R8 represents hydroxy or acyloxy; or R7 and R8 together represent a spiroether group of the formula 17a or a spirolactone group of the formula 17a the dotted 16,17-bond is an optional additional carbon-carbon bond; and the dotted 2,3-bond is an additional carbon-carbon bond when R1 and R2 together with carbon atoms 2 and 3 form the isoxazole or pyrazole ring or when R2 represents a -OAc group, inhibit the synthesis of progesterone in organisms and can be used for fertility control. The novel D-homosteroids can be manufactured by molecular modifications of other D-homosteroids.

14. 发明专利

CA1138857A D-HOMOSTEROIDS 未知
公开(公告)号：CA1138857A
公开(公告)日：1983-01-04
申请号：CA341528
申请日：1979-12-10
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , MUELLER MARCEL , KERB ULRICH , KIESLICH KLAUS , WIECHERT RUDOLF
IPC分类号： A61K31/19 , A61K31/215 , C07J63/00 , C12P33/02 , C12P33/08
摘要： Novel D-homosteroids with endocrinal, especially antiinflammatory, activity and having the formula I wherein R6 represents a hydrogen, fluorine or chlorine atom or a methyl group; R9 represents a hydrogen, fluorine, chlorine of bromino atom; R11 represents an oxo or (.alpha.-H,.beta.-OH) group when R9 represents a hydrogen atom or an oxo, (.alpha.-H,.beta.-OH), (.alpha.-H,.beta.-fluoro) or (.alpha.-H,.beta.-chloro) group when R9 represents a fluorine, chlorine or bromine atom, with the proviso that, in the case of 9,11-dihalo compounds, the atomic number of the halogen atom in the 9-position is not less than the atomic number of the halogen atom in the 11 -position; R17a represents an acyloxy group and R20 represents a lower alkyl or halo-(lower alkyl) group and wherein the broken line in the 1,2-position denotes an optional carbon-carbon bond, a process for their manufacture and medicaments containing said D-homosteroids.

15. 发明专利

NO147275B 未知
公开(公告)号：NO147275B
公开(公告)日：1982-11-29
申请号：NO781390
申请日：1978-04-20
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , MUELLER MARCLE , KERB ULRICH , WIECHERT RUDOLF
IPC分类号： A61K31/12 , A61K31/215 , A61K31/22 , A61K31/57 , A61P29/00 , C07J63/00
摘要： D-homopregnanes of the formula I wherein R6 is hydrogen, chloro, fluoro or methyl; X is beta -hydroxymethylene or carbonyl; R17a is hydroxy, lower alkanoyloxy or aroyloxy; R21 is hydrogen, chloro, fluoro, hydroxy, lower alkanoyloxy, aroyloxy, sulfate or phosphate; and the dotted line in the 1,2-position of the A-ring denotes an additional carbon-carbon bond AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PROCESSES FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AS THE ACTIVE INGREDIENT ARE DISCLOSED. The D-homopregnanes of the present invention exhibit hormonal activity and are useful for the treatment of inflammation.

16. 发明专利

ZA8107896B NOVEL D-HOMOSTEROIDS 未知
公开(公告)号：ZA8107896B
公开(公告)日：1982-10-27
申请号：ZA8107896
申请日：1981-11-13
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , KELLER PETER , MUELLER MARCEL , WIECHERT RUDOLF , KERB ULRICH
IPC分类号： A61K31/56 , A61P13/02 , A61P15/00 , C07J63/00 , C07J , A61K
CPC分类号： C07J63/008

17. 发明专利

CH629830A5 未知
公开(公告)号：CH629830A5
公开(公告)日：1982-05-14
申请号：CH598481
申请日：1981-09-16
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , MUELLER MARCEL , KERB ULRICH , KIESLICH KLAUS , WIECHERT RUDOLF
IPC分类号： A61K31/12 , A61K31/57 , A61P29/00 , C07J63/00 , C12P33/08

18. 发明专利

NO145621B 未知
公开(公告)号：NO145621B
公开(公告)日：1982-01-18
申请号：NO773057
申请日：1977-09-02
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , MUELLER MARCEL , KERB ULRICH , KIESLICH KLAUS , WIECHERT RUDOLF
IPC分类号： A61K31/12 , A61K31/57 , A61P29/00 , C07J63/00 , C12P33/08

19. 发明专利

NO143428C 未知
公开(公告)号：NO143428C
公开(公告)日：1981-02-11
申请号：NO790890
申请日：1979-03-15
申请人： HOFFMANN LA ROCHE
发明人： ALIG LEO , FUERST ANDOR , MUELLER MARCEL , KERB ULRICH , WIECHERT RUDOLF
IPC分类号： C07J63/00 , A61K31/56 , A61K31/57 , C07J20060101

20. 发明专利

NO142349C 未知
公开(公告)号：NO142349C
公开(公告)日：1980-08-06
申请号：NO753505
申请日：1975-10-17
申请人： HOFFMANN LA ROCHE
发明人： FUERST ANDOR , MUELLER MARCEL , GUTZWILLER JUERG ALBERT WALTER , WIECHERT RUDOLF , KERB ULRICH
IPC分类号： A61K31/12 , A61K31/21 , A61K31/56 , C07J63/00

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