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144 records (took 0.02 seconds)

    41.
    发明专利
    未知

    公开(公告)号：ATA583871A

    公开(公告)日：1976-06-15

    申请号：AT583871

    申请日：1971-07-06

    Applicant: HOECHST AG

    Inventor： STACHE U ,  RADSCHEIT K ,  FRITSCH W ,  HAEDE W

    IPC: C07D20060101 ,  C07J19/00

    Abstract: 1362383 Cardenolides; bufadienolides FARBWERKE HOECHST AG 7 July 1971 [7 July 1970] 31974/71 Heading C2U [Also in Division A5] The invention comprises (A) the compounds 3#,14 - dihydroxy - 5α,14# - bufa - 20,22 - dienolide (Ia); 3#-hydroxy-5α,14α-card-20(22)- enolide; 3# - hydroxy - 5α - bufa - 14,20,22- trienolide; and 3#-hydroxy-5α,14α-bufa-20,22- dienolide; and (B) a process for preparing compounds of formula (wherein R 1 is the lactone ring of a 20(22)- cardenolide or 20,22-bufadienolide; R 2 is CH 3 , CH 2 OH or CH 2 OCOCH 3 ; R 3 is H, OH or acyloxy; R 4 is H; or R 3 + R 4 is epoxy or an extra C-C bond; and R 5 and R 6 are each H, OH or acyloxy) which comprises reducing the corresponding 3-oxo-# 4 compounds (wherein R 2 is alternatively CHO and R 5 and R 6 are each alternatively oxo) with a reducing agent which is more powerful than NaBH 4 , in the presence of an organic nitrogen base at - 30‹ to + 60‹ C. Any oxo groups at positions 11, 12 and 19 are reduced concomitantly. Specified reducing agents are the borohydrides of Li, Mg, Ca, Sr, Ba, Zn and Al, the trimethoxy borohydrides of Na and Li, the aluminium hydrides of Na, Li and Mg, aluminium hydride, lithium trimethoxy aluminium hydride, diborane, pyridine-borane, ethane-1,2- diamine-borane and (3-methyl-2-butyl)borane. Compound Ia supra is alternatively prepared from 3# - hydroxy - 5α - bufa - 14,20,22 - trienolide (III) by the sequence : III # III 3- formate # 15α-bromo-(Ia)-3-formate # Ia 3-formate -# Ia. 3 - Oxo - 14α - bufa - 4,20,22 - trienolide is prepared from the corresponding # 5 -3#-ol by Oppenauer oxidation. Compounds I are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    43.
    发明专利
    未知

    公开(公告)号：CH562259A5

    公开(公告)日：1975-05-30

    申请号：CH983871

    申请日：1971-07-05

    Applicant: HOECHST AG

    Inventor： STACHE U ,  RADSCHEIT K ,  FRITSCH W ,  HAEDE W

    IPC: C07D20060101 ,  C07J19/00

    Abstract: 1362383 Cardenolides; bufadienolides FARBWERKE HOECHST AG 7 July 1971 [7 July 1970] 31974/71 Heading C2U [Also in Division A5] The invention comprises (A) the compounds 3#,14 - dihydroxy - 5α,14# - bufa - 20,22 - dienolide (Ia); 3#-hydroxy-5α,14α-card-20(22)- enolide; 3# - hydroxy - 5α - bufa - 14,20,22- trienolide; and 3#-hydroxy-5α,14α-bufa-20,22- dienolide; and (B) a process for preparing compounds of formula (wherein R 1 is the lactone ring of a 20(22)- cardenolide or 20,22-bufadienolide; R 2 is CH 3 , CH 2 OH or CH 2 OCOCH 3 ; R 3 is H, OH or acyloxy; R 4 is H; or R 3 + R 4 is epoxy or an extra C-C bond; and R 5 and R 6 are each H, OH or acyloxy) which comprises reducing the corresponding 3-oxo-# 4 compounds (wherein R 2 is alternatively CHO and R 5 and R 6 are each alternatively oxo) with a reducing agent which is more powerful than NaBH 4 , in the presence of an organic nitrogen base at - 30‹ to + 60‹ C. Any oxo groups at positions 11, 12 and 19 are reduced concomitantly. Specified reducing agents are the borohydrides of Li, Mg, Ca, Sr, Ba, Zn and Al, the trimethoxy borohydrides of Na and Li, the aluminium hydrides of Na, Li and Mg, aluminium hydride, lithium trimethoxy aluminium hydride, diborane, pyridine-borane, ethane-1,2- diamine-borane and (3-methyl-2-butyl)borane. Compound Ia supra is alternatively prepared from 3# - hydroxy - 5α - bufa - 14,20,22 - trienolide (III) by the sequence : III # III 3- formate # 15α-bromo-(Ia)-3-formate # Ia 3-formate -# Ia. 3 - Oxo - 14α - bufa - 4,20,22 - trienolide is prepared from the corresponding # 5 -3#-ol by Oppenauer oxidation. Compounds I are said to be cardiotonic, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    44.
    发明专利
    未知

    公开(公告)号：NO130644B

    公开(公告)日：1974-10-07

    申请号：NO149169

    申请日：1969-04-11

    Applicant: HOECHST AG

    Inventor： RADSCHEIT K ,  STACHE U ,  FRITSCH W ,  HAEDE W

    IPC: A61K31/573 ,  A61K31/58 ,  C07C169/34

    Abstract: DELTA 14-20-KETO-21-DIALKOXY STEROIDS ARE PREPARED BY OXIDIZING 20-KETO-15 alpha ,21-DIHYDROXY STEROIDS OF THE GENERAL FORMULA IN WHICH Y is an oxo group which may be ketalized, GROUP WHICH MAY BE ETHERIFIED OR ESTERIFIED, A DELTA 3-, DELTA 2-, OR DELTA 3,5-ENOL ETHER GROUP OR A DELTA 3-, DELTA 2-, OR DELTA 3,5-ENAMINO GROUP, WHICH GROUPS MAY HAVE A DOUBLE BOND IN THE 4-POSITION, AND IS A LOWER ACYCLIC OR CYCLIC ACETAL GROUPING, ACETALIZING THE 15 alpha -HYDROXY-20-KETO-21-OXO STEROIDS OBTAINED, REACTING THE 15 alpha -HYDROXY-20-KETO-21-DIALKOXY STEROIDS THUS OBTAINED WITH SULFONIC ACID HALIDES AND TREATING THE 15-SULFONIC ACID ESTERS THUS OBTAINED WITH AGENTS SPLITTING OFF ACIDS. The products are valuable intermediates for the manufacture of medicaments.

    45.
    发明专利
    未知

    公开(公告)号：SE368570B

    公开(公告)日：1974-07-08

    申请号：SE1172170

    申请日：1970-08-28

    Applicant: HOECHST AG

    Inventor： STACHE U ,  FRITSCH W ,  HAEDE W ,  RADSCHEIT K ,  LINDER E

    IPC: A61K31/58 ,  A61K31/585 ,  A61K31/70 ,  A61K31/704 ,  A61P1/12 ,  A61P7/10 ,  A61P9/04 ,  C07J19/00 ,  C07C173/02

    Abstract: 1323775 Cardial glycosides FARBWERKE HOECHST AG 1 Sept 1970 [29 Aug 1969(2)] 41722/70 Heading C2U The invention comprises compounds of formula where R is a steroid 3-yl radical of the 20(22)- cardenolide or 20,22-bufadienolide series; the two symbols R 1 together represent an epoxy group, or, when R is a cardenolide radical, they each may alternatively represent a hydrogen atom; R 2 is H or an aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbyl or acyl group; and R 3 is H, Me or CH 2 OR 2 . Preparation of compounds (I) is from compounds of formula by catalytic hydrogenation (for products wherein R 1 = H) or by reaction with an organic peracid (for products wherein R 1 +R 1 = epoxy). Subsequently any 4 1 -acyloxy group may be hydrolysed, or any 4 1 -hydroxy group esterified or etherified. Digitoxigenin 3 - (# 2 - 2,3 - dideoxy - 4 - O- acetyl - D - arabinoside) is prepared by reacting digitoxigenin with di-O-acetyl-D-arabinal. The L-arabinoside isomer is prepared analogously and then hydrolysed to digitoxigenin 3-(# 2 - 2,3-dideoxy-L-arabinoside). Uzarigenin 3 - (# 2 - 2,3 - dideoxy - 4 - O- acetyl-α-L-rhamnoside) is prepared by reacting uzarigenin with di-O-acetyl-L-rhamnal. Other starting materials of Formula II are prepared as described in Specfications 1,268,230, 1,282,019 and 1,323,148. The steroids of Formula (I) are stated to possess cardiotonic, diuretic and antidiarrhoeal activities, and may be made up with carriers into pharmaceutical compositions for oral or parenteral administration.

    CARDENOLIDE-3-(2'-DESOXY-GLYCOSIDES)AND PROCESS FOR THEIR MANUFACTURE
    46.
    发明专利
    CARDENOLIDE-3-(2'-DESOXY-GLYCOSIDES)AND PROCESS FOR THEIR MANUFACTURE 未知

    公开(公告)号：ZA735149B

    公开(公告)日：1974-06-26

    申请号：ZA735149

    申请日：1973-07-27

    Applicant: HOECHST AG

    Inventor： STACHE U ,  FRITSCH W ,  HAEDE W ,  RADSCHEIT K ,  LINDER E

    IPC: C07J19/00 ,  A61K20060101 ,  A61K31/585 ,  A61P1/08 ,  A61P7/10 ,  A61P9/04 ,  A61P9/14 ,  C07C20060101 ,  C07D20060101 ,  C07J20060101 ,  C07C

    Abstract: 1435204 Cardenolide glycosides HOECHST AG 30 July 1973 [29 July 1972] 36141/73 Heading C2U The invention comprises cardenolide 3-(2- deoxy-α-L-glycosides) of formula wherein R 1 is a steroid-3-yl radical of the 20(22)- cardenolide series; R 2 is H, C 1-5 aliphatic carboxylic acyl or C 7-8 aromatic carboxylic acyl; and R 3 is H, Me or OH 2 OR 2 . Preparation is from the corresponding 3-(2,3-dideoxy-2(3)-dehydro - α - L - glycosides) (cf. Specification 1,268,230) by hydroxybromination to give 3-(2- bromo - 2 - deoxy - α - L - glycosides), catalytic hydrogenation of which yields compounds I which may be interconverted by saponification or acylation within the sugar moiety. Digitoxigenin 3 - (2,3 - dideoxy - 2(3) - dehydro- α-L-rhamnoside)-4 1 -acetate is prepared from digitoxigenin by reaction with diacetyl-L- rhamnal. Compounds I are said to possesss cardiotonic, diuretic, antidiarrhoeal and venous tonusimproving properties, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    47.
    发明专利
    未知

    公开(公告)号：DK128738B

    公开(公告)日：1974-06-24

    申请号：DK445070

    申请日：1970-08-28

    Applicant: HOECHST AG

    Inventor： STACHE U ,  FRITSCH W ,  HAEDE W ,  RADSCHEIT K ,  LINDNER E

    IPC: A61K31/58 ,  A61K31/585 ,  A61K31/70 ,  A61K31/704 ,  A61P1/12 ,  A61P7/10 ,  A61P9/04 ,  C07J19/00 ,  C07C173/00

    Abstract: 1323775 Cardial glycosides FARBWERKE HOECHST AG 1 Sept 1970 [29 Aug 1969(2)] 41722/70 Heading C2U The invention comprises compounds of formula where R is a steroid 3-yl radical of the 20(22)- cardenolide or 20,22-bufadienolide series; the two symbols R 1 together represent an epoxy group, or, when R is a cardenolide radical, they each may alternatively represent a hydrogen atom; R 2 is H or an aliphatic, cycloaliphatic, aromatic or araliphatic hydrocarbyl or acyl group; and R 3 is H, Me or CH 2 OR 2 . Preparation of compounds (I) is from compounds of formula by catalytic hydrogenation (for products wherein R 1 = H) or by reaction with an organic peracid (for products wherein R 1 +R 1 = epoxy). Subsequently any 4 1 -acyloxy group may be hydrolysed, or any 4 1 -hydroxy group esterified or etherified. Digitoxigenin 3 - (# 2 - 2,3 - dideoxy - 4 - O- acetyl - D - arabinoside) is prepared by reacting digitoxigenin with di-O-acetyl-D-arabinal. The L-arabinoside isomer is prepared analogously and then hydrolysed to digitoxigenin 3-(# 2 - 2,3-dideoxy-L-arabinoside). Uzarigenin 3 - (# 2 - 2,3 - dideoxy - 4 - O- acetyl-α-L-rhamnoside) is prepared by reacting uzarigenin with di-O-acetyl-L-rhamnal. Other starting materials of Formula II are prepared as described in Specfications 1,268,230, 1,282,019 and 1,323,148. The steroids of Formula (I) are stated to possess cardiotonic, diuretic and antidiarrhoeal activities, and may be made up with carriers into pharmaceutical compositions for oral or parenteral administration.

    49.
    发明专利
    未知

    公开(公告)号：FI48075B

    公开(公告)日：1974-02-28

    申请号：FI96871

    申请日：1971-04-06

    Applicant: HOECHST AG

    Inventor： RADSCHEIT K ,  STACHE U ,  FRITSCH W ,  HAEDE W ,  LINDNER E

    IPC: A61K31/70 ,  C07J71/00 ,  C07C173/04

    Abstract: 1315235 Bufapolyenolides FARBWERKE HOECHST AG 19 April 1971 [8 April 1970] 26359/71 Heading C2U The novel compound 3#-(α-L-rhamnopyranosyloxy) - 14,15# - epoxy - 14# - bufa - 4,20,22- trienolide is prepared from proscillaridin by successively acylating the three sugar hydroxy groups, dehydrating in the 14,15-position, adding hypohalous acid acoross the resulting # 14 - double bond, dehydrohalogenating the resulting 14#-hydroxy-15α-halo grouping, and lastly liberating the three sugar hydroxy groups by saponification. The novel compound is stated to be cardioactive and may be made up with carriers into pharmaceutical compositions for oral administration.

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