公开(公告)号：US3400155A

公开(公告)日：1968-09-03

申请号：US64727167

申请日：1967-04-25

Applicant: HOECHST AG

Inventor： EHRHART GUSTAV ,  LINDNER ERNST ,  OTT HEINRICH

IPC: C07D209/86 ,  C07D219/14 ,  C07D223/28 ,  C07D265/38 ,  C07D279/18

CPC classification number: C07D279/18 ,  C07D209/86 ,  C07D219/14 ,  C07D223/28 ,  C07D265/38

公开(公告)号：US3919191A

公开(公告)日：1975-11-11

申请号：US27410672

申请日：1972-07-21

Applicant: HOECHST AG

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

IPC: A61K20060101 ,  A61K31/585 ,  C07C20060101 ,  C07D20060101 ,  C07J19/00 ,  C07J63/00 ,  C07J71/00

CPC classification number: C07J19/00

Abstract: Cardioactive 3 Beta -hydroxy-14,15 Beta -epoxy-5 Beta cardenolide-or -5 Beta -bufadienolide-glucosides and rhamnosides. A method for making these compounds by reacting the corresponding 14-anhydrocardenolides or 14-anhydrobufadienolides with an acylhalopyranose, reacting the resultant acylated pyranoside with a hypohalous acid to form the corresponding halohydrin, and epoxidizing the halohydrin with a base.

Abstract translation: 心脏活性3β-羟基-14,15β-环氧-5β-硬脑苷脂或-5β-布非那内苷 - 糖苷和鼠李糖苷。 通过使相应的14-脱水卡非德内酯或14-脱水布非内酯与酰基吡喃吡喃糖反应制备这些化合物的方法，使得到的酰化吡喃糖苷与次卤酸反应形成相应的卤代醇，并用卤代醇环氧化。

公开(公告)号：US3872081A

公开(公告)日：1975-03-18

申请号：US37068573

申请日：1973-06-18

Applicant: HOECHST AG

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

IPC: C07J19/00 ,  A61K31/585 ,  A61K31/704 ,  A61P9/04 ,  C07D20060101 ,  C07C173/02

Abstract: wherein R is hydrogen or alkanoyl or alkyl having 1 to 5 carbon atoms are described as well as two processes for their preparation. The compounds show positive inotropic action and are suitable for treating heart diseases.

Digitoxigenin-3- Alpha -(L-rhamnopyranoside-2'',3''cyclocarbonates) of the general formula I

Abstract translation: 对其中R是氢或烷酰基或具有1-5个碳原子的烷基的通式I的二氧化硫脲-3α-[L-鼠李糖吡喃糖苷-2'，3'-环状碳酸酯]以及它们的制备方法进行了描述。 这些化合物显示正性肌力作用，适用于治疗心脏病。

公开(公告)号：US3682891A

公开(公告)日：1972-08-08

申请号：US3682891D

申请日：1970-01-09

Applicant: HOECHST AG

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

IPC: A61K20060101 ,  A61K36/00 ,  C07C20060101 ,  C07J19/00 ,  C07C173/00

CPC classification number: C07J19/005

Abstract: A METHOD FOR SYNTHESIZING ESTERS IN WHICH THE ACID MOIETY IS THAT OF A HYDROXY ACID AND THE ALCOHOL MOIETY IS A 3-HYDROXY-CARDENOLIDE OR 3-HYDOXY-BUFADIENOLIDE, BY ESTERIFYING THE STEROL WITH AN ACID ANHYDRIDE OR AN ACID CHLORIDE OF THE HYDROXY ACID, THE HYDROXY GROUPS OF WHICH HAVE BEEN ACETALIZED OR KETALIZED, AND THEN SELECTIVELY REMOVING SAID ACETAL OR KETAL GROUPS BY ACID HYDROLYSIS. CARDI-ACTIVE OXY-ESTERS PRODUCED BY THIS METHOD.

公开(公告)号：US3879379A

公开(公告)日：1975-04-22

申请号：US12542571

申请日：1971-03-17

Applicant: HOECHST AG

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

IPC: A61K31/585 ,  C07D20060101 ,  C07J41/00 ,  C07C173/00

CPC classification number: C07J19/00

Abstract: Cardioactive 3-amino-cardenolides and a method for preparing them by reacting a 3-oxo-cardenolide with hydroxylamine or its salts to form a cardenolide-3-oxime and then catalytically hydrogenating this intermediate.

Abstract translation: 心脏活性3-氨基 - 己烯酸烯诺酯及其制备方法是通过使3-氧代 - 己烯酸烯醇与羟胺或其盐反应形成己内酰胺-3-肟，然后催化氢化该中间体。

公开(公告)号：US3873699A

公开(公告)日：1975-03-25

申请号：US39153473

申请日：1973-08-27

Applicant: HOECHST AG

Inventor： GROEBEL ALFRED ,  LINDNER ERNST

IPC: A61K36/00 ,  A61K36/48 ,  C07G5/00 ,  C07G99/00 ,  A61K27/14

CPC classification number: A61K36/48 ,  Y10S514/821

Abstract: Method for isolating a pharmacologically active fraction from Cadia ellisiana by extraction of dried plant material. A first crystalline substance, found in said active fraction, having a hypotensive and anti-arrhythmic action. A second crystalline substance, found in said active fraction, having a hypotensive action. Pharmaceutical dosage unit forms containing these compounds. Methods of treating hypertonia and/or arrhythmia with these compouds.

Abstract translation: 通过提取干燥的植物材料分离来自茜草属的药理活性级分的方法。 在所述活性部分中发现的具有降血压和抗心律失常作用的第一结晶物质。 在所述活性级分中发现的具有降血压作用的第二结晶物质。 含有这些化合物的药物剂量单位形式。 用这些方法治疗高血压和/或心律失常的方法。

公开(公告)号：US3639392A

公开(公告)日：1972-02-01

申请号：US3639392D

申请日：1969-12-02

Applicant: HOECHST AG

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

IPC: A47F5/11 ,  A61K31/58 ,  A61K31/585 ,  C07J19/00 ,  C07J71/00 ,  C07C173/04

CPC classification number: A61K31/58 ,  A61K31/585 ,  C07J19/00 ,  C07J71/00

Abstract: CARDIOACTIVE OXIDO-CARDADIENOLIDES AND OXIDO-BUFATRIENOLIDES OF THE FORMULA

3-R1,14,15-(-O-),17-R-4-GONENE

WHEREIN R IS A CARDENOLIDE OR BUFADIENOLIDE RING AND R1 IS -OH IN THE B-POSITION OR KETO. METHODS OF MAKING SUCH COMPOUNDS. AS SPECIFIC OXIDO-BUFATRIENOLIDES: 3-OXO14,15B-OXIDO-BUFA-4,20(21),22(23)-TRIENOLIDE; 3BHYDROXY-14,15B-OXIDO-BUFA-4,20(21),22(23)-TRIENOLIDE.

公开(公告)号：US3475482A

公开(公告)日：1969-10-28

申请号：US3475482D

申请日：1966-05-24

Applicant: HOECHST AG

Inventor： EHRHART GUSTAV ,  LINDNER ERNST ,  OTT HEINRICH

IPC: A61K31/195 ,  C07C101/04 ,  A61K27/00

CPC classification number: A61K31/195

公开(公告)号：US3920627A

公开(公告)日：1975-11-18

申请号：US46783274

申请日：1974-05-07

Applicant: HOECHST AG

Inventor： WISSMANN HANS ,  GEIGER ROLF ,  LINDNER ERNST ,  SCHOLKENS BERNWARD

IPC: C07K7/06 ,  A61K38/00 ,  A61P5/00 ,  C07C231/00 ,  C07K1/113 ,  C07K7/14 ,  C07C103/52 ,  A61K37/26

CPC classification number: C07K7/14 ,  A61K38/00 ,  Y02P20/55

Abstract: Peptides of the formula I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH (I) in which X represents the radical of an aliphatic carboxylic acid of up to 5 carbon atoms or the phthalic acid radical, and Phegly-OH represents L-C-phenylglycine, and a process of preparing them by condensing the O-tert. butyl ester of compound I, in which tyrosine is protected by tert. butyl, and X represents hydrogen, with carboxylic acids of the formula X-OH, in which X has the first mentioned meaning, according to the condensation methods usually employed in peptide chemistry.

Abstract translation: 式I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH（I）的肽，其中X表示至多5个碳原子的脂肪族羧酸基团或邻苯二甲酸基团，Phegly -OH表示LC-苯基甘氨酸，以及通过将O-叔丁基缩合制备它们的方法。 化合物I的丁酯，其中酪氨酸被叔保护。 丁基，X表示氢，根据肽化学中通常使用的缩合方法，具有式X-OH的羧酸，其中X具有第一个提及的含义。

公开(公告)号：US3910882A

公开(公告)日：1975-10-07

申请号：US38266273

申请日：1973-07-26

Applicant: HOECHST AG

Inventor： HAEDE WERNER ,  FRITSCH WERNER ,  STACHE ULRICH ,  LINDNER ERNST

IPC: C07J19/00 ,  A61K20060101 ,  A61K31/585 ,  A61K31/704 ,  A61P7/10 ,  A61P9/04 ,  C07C20060101 ,  C07D20060101

CPC classification number: C07J19/00

Abstract: The invention relates to 3'', 4''-anhydro- Beta , Ltalomethylosides of the general formula I

wherein R1 is methyl or formyl and R2 stands for Beta -H or Beta -OH, if there is no double bond in 4,5-position, and R3 is a butenolide or cumalin ring, a process for preparing them and their use in the treatment of cardiac and circulatory disturbances. The compounds are especially suitable for treating cardiac insufficiency, tachycardia and conduction defects.

Abstract translation: 本发明涉及通式Ⅰ的3'，4'-脱氢-β，L-天门冬氨酸盐，其中R1是甲基或甲酰基，R2代表β-H或β--OH，如果4,5中没有双键 - 位，R3是丁烯内酯或坎加林环，其制备方法及其在治疗心脏和循环障碍中的应用。 该化合物特别适用于治疗心功能不全，心动过速和传导缺陷。