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    51.
    发明专利
    未知

    公开(公告)号：DK127421B

    公开(公告)日：1973-11-05

    申请号：DK37072

    申请日：1972-01-27

    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 ,  C07C173/02

    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.

    52.
    发明专利
    未知

    公开(公告)号：DK127110B

    公开(公告)日：1973-09-24

    申请号：DK29671

    申请日：1971-01-22

    Applicant: HOECHST AG

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

    IPC: A61K31/585 ,  C07D20060101 ,  C07J19/00 ,  C07C173/02

    Abstract: 1327745 4 - Chlorocardenolide glycosides FARBWERKE HOECHST AG 19 Jan 1971 [26 Jan 1970] 2585/71 Heading C2U The invention comprises compounds of formula (wherein R is an unsubstituted glycopyranosyl radical and R 1 is α-H, #-H or #-OH), and their preparation from the corresponding 3-ols by reaction with an acylated 1-halo-1-deoxyglycopyranose in the presence of silver carbonate and an inert solvent (with azeotropic distillation to remove the water of reaction) followed by hydrolysis of the acyl groups). 3#-Hydroxy - 4 - chloro - 14α - carda - 4,20(22)- dienolide is prepared from 3-oxo-14α-carda- 4,20(22)-dienolide via 3-oxo-4-chloro-14α-carda- 4,20(22)-dienolide. The 14#-isomer is prepared likewise. The inventive compounds are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

    53.
    发明专利
    未知

    公开(公告)号：DK126190B

    公开(公告)日：1973-06-18

    申请号：DK243470

    申请日：1970-05-13

    Applicant: HOECHST AG

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

    IPC: A41D27/20 ,  A61K31/585 ,  C07J19/00 ,  C07C173/02

    Abstract: 1308656 4-Chloro-carda-4,20(22)-dienolides FARBWERKE HOECHST AG 14 May 1970 [14 May 1969] 23473/70 Heading C2U The invention comprises 3-oxo-4-chloro-14#- hydroxycarda-4,20(22)-dienolide (V) and 3α,14#- or 3#,14#-dihydroxy -4 - chlorocarda - 4,20(22)- dienolide (VI), and their derivatives wherein one or more of the 1, 2, 6, 7, 11, 12 and 16- positions is substituted by an alkyl, acyl, C 1-3 acyloxy or ketalized oxo group. Preparation of the above is by the route: 3 - oxo - carda - 4,14,20(22) - trienolide # 3 - oxo - 4,14,15 - trichlorocarda - 4,20(22)- dienolide # 3 - oxo - 4 - chlorocarda - 4,14,20- (22) - trienolide # 3 - oxo - 4 - chloro - 14#- hydroxy - 15α - bromocarda - 4,20(22) - dienolide # V # VI. Pharmaceutical compositions comprise an inventive compound and a carrier. Compound V and its derivatives are said to be cardioactive, but no activity is specified for compound VI and its derivatives. Routes of administration are not specified.

    57.
    发明专利
    未知

    公开(公告)号：SE352349B

    公开(公告)日：1972-12-27

    申请号：SE1282569

    申请日：1969-09-18

    Applicant: HOECHST AG

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

    IPC: C07C169/28

    Abstract: 1288414 Steroid 21-cyclobutane esters FARBWERKE HOECHST AG 22 Sept 1969 [20 Sept 1968] 46559/69 Heading C2U The invention comprises compounds of formula represents (i) a Y . . . C 9 -C 11 =X group where Y is H or F and X is H 2 , OXO, H(#-OH), H(α-OH), H(#-Cl) or H(#-F), or group; R 1 represents H 2 , H(α-Me), H(#-Me), H(α-F), H(#-F), CH 2 , CHF or CF 2 ; R 2 represents H or OH; R 3 represents a direct bond or a C 1-5 divalent aliphatic hydrocarbon group; and R 4 represents a cyclobutyl group which is substituted by at least one fluorine atom and which may be further substituted by one or more methyl groups and/or chlorine atoms. Preparation of the above compounds is from the corresponding steroid 21-ols by reaction with a compound of formula Cl-CO-R 3 -R 4 . Product interconversions specified are 1,2- and/ or 6,7-dehydrogenation; 6-, 9-, 11- and/or 16- fluorination; further fluorination of the cyclobutane ring; and reduction of 11-oxo to 11- hydroxy. The inventive compounds are stated to possess anti-inflammatory activity and may be made up with carriers into pharmaceutical and veterinary compositions for topical administration.

    59.
    发明专利
    未知

    公开(公告)号：FI45756B

    公开(公告)日：1972-05-31

    申请号：FI86169

    申请日：1969-03-24

    Applicant: HOECHST AG

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

    IPC: A61K31/70 ,  C07C173/02

    Abstract: 1,228,069. Cardenolide ethers. FARBWERKE HOECHST A.G. 2 April, 1969 [6 April, 1968], No. 17192/69. Heading C2U. The invention comprises compounds of formula wherein R 1 is x-H, #-H or #-OH; R 2 , R 3 and R 4 are each H or OH; and R 5 is C 1-3 alkyl; and their preparation by LiAlH 4 reduction of compounds of formula wherein R 6 is C 1-3 alkyl and R 7 is CH 3 , CH 2 OH or CHO. A starting material with R 7 = CHO yields a product with R 2 = OH. Compounds of Formula II are prepared from the corresponding 3-hydroxy steroids by reaction with appropriately substituted dihydropyrans. Compounds of Formula I are stated to possess inotropic, cardiovascular, diuretic and anti-diarrhoeal effects, and may be made up with carriers into pharmaceutical compositions for oral administration.

    2,3-ALKYLIDENE-RHAMNOPYRANOSIDES AND PROCESS FOR PREPARING THEM
    60.
    发明专利
    2,3-ALKYLIDENE-RHAMNOPYRANOSIDES AND PROCESS FOR PREPARING THEM 未知

    公开(公告)号：ZA712827B

    公开(公告)日：1972-01-26

    申请号：ZA712827

    申请日：1971-04-30

    Applicant: HOECHST AG

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

    IPC: C07J19/00 ,  C07G ,  A61K

    Abstract: 1345388 Convallatoxin derivatives FARBWERKE HOECHST AG 30 April 1971 [2 May 1970] 12427/71 Heading C2U The invention comprises compounds of formula (wherein R 1 and R 2 are each C 1-4 alkyl, or together with the intervening carbon atom form a carbocyclic or heterocyclic ring; and R 3 is CHO or CH 2 OH) and their preparation from convallatoxin by reaction with R 1 R 2 C(OR 4 ) 2 (where R 4 is C 1-4 alkyl), optionally followed by reduction of 19-oxo to hydroxy. The inventive compounds are said to be cardioactive, and may be made up with carriers into pharmaceutical compositions for oral and parenteral administration.

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