公开(公告)号：US3682987A

公开(公告)日：1972-08-08

申请号：US3682987D

申请日：1969-04-14

Applicant: KURT RADSCHEIT ,  ULRICH STACHE ,  WERNER FRITSCH ,  WERNER HAEDE ,  HOECHST AG

Inventor： RADSCHEIT KURT ,  STACHE ULRICH ,  FRITSCH WERNER ,  HAEDE WERNER

IPC: A61K31/573 ,  A61K31/58 ,  C07C169/32

CPC classification number: A61K31/573 ,  A61K31/58

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.

Abstract translation: 通过氧化通用制剂的20-KETO-15α，21-二羟基甾体来制备DELTA 14-20-酮二十二烷氧基甾体，其中Y是可被缩合的氧代基团，其可以被醚化或被纯化， DELTA 3-，DELTA 2-或OR DELTA 3,5-ENOL ETHER GROUP或DELTA 3-，DELTA 2-或DELTA 3,5-ENAMINO集团，其组合可能在4位置有双重粘结， 并且是一种较低的ACYCLIC或循环乙酰基化，获得所获得的15α-羟基-20-酮二十一氧代甾族化合物，反应获得的15个α-羟基-20-酮二十二烷氧基异烟肼和治疗 这种15-磺基酸酯可以与分离出酸的试剂一起获得。 这些产品是制造药物的有价值的中间体。

公开(公告)号：US4003997A

公开(公告)日：1977-01-18

申请号：US496892

申请日：1974-08-12

Applicant: Ulrich Stache ,  Kurt Radscheit ,  Werner Fritsch ,  Werner Haede ,  Ernst Lindner

Inventor： Ulrich Stache ,  Kurt Radscheit ,  Werner Fritsch ,  Werner Haede ,  Ernst Lindner

IPC: C07J71/00 ,  C07J19/00 ,  A61K31/70

CPC classification number: C07J19/00

Abstract: Cyclic 2',3'-ethers of 3-hydroxy-14,15.beta.-oxido-14.beta.-bufa-4,20,22-trienolide, 3.beta.-(.alpha.-L-rhamnopyranoside) and process for preparing them. The compounds have a strongly positive inotropic activity and may be used in the therapy of cardiac insufficiency.

Abstract translation: 3-羟基-14,15β-氧代-14β-bufa-4,20,22-三烯内酯，3β-（α-L-鼠李糖吡喃糖苷）的环状2'，3'-醚及其制备方法。 该化合物具有强烈的正性肌力活性，可用于治疗心功能不全。

公开(公告)号：US3950323A

公开(公告)日：1976-04-13

申请号：US416656

申请日：1973-11-16

Applicant: Ulrich Stache ,  Werner Fritsch ,  Werner Haede ,  Ernst Lindner

Inventor： Ulrich Stache ,  Werner Fritsch ,  Werner Haede ,  Ernst Lindner

IPC: C07J19/00 ,  A61K31/585

CPC classification number: C07J19/00 ,  Y10S514/869

Abstract: Digoxigenine-3-[2', 3'-didesoxy-glycosides] of the formula ##SPC1##In which R.sup.1 is the digoxigenine radical and R.sup.2 is hydrogen, methyl or --CH.sub.2 OH, which are prepared by a reaction of a digoxigenine-12-monoacylate with an acylated 1,2-glycal, a catalytic hydrogenation of the 12-acylates obtained and a subsequent hydrolysis. The products have a cardiotonic, diuretic and especially venotonic activity.

公开(公告)号：US3937697A

公开(公告)日：1976-02-10

申请号：US554182

申请日：1975-02-28

Applicant: Ulrich Stache ,  Werner Fritsch ,  Werner Haede ,  Ernest Lindner

Inventor： Ulrich Stache ,  Werner Fritsch ,  Werner Haede ,  Ernest Lindner

IPC: C07J19/00

CPC classification number: C07J19/005 ,  Y10S514/869

Abstract: 12-Dehydro digoxin mono-4'" and 3'"-alkyl ethers and a process for their manufacture.The compounds have a cardiotonic and diuretic activity.