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1. 发明授权

US4003997A Heart glycosides and process for preparing them 失效
标题翻译：心脏糖苷及其制备方法
公开(公告)号：US4003997A
公开(公告)日：1977-01-18
申请号：US496892
申请日：1974-08-12
申请人： Ulrich Stache , Kurt Radscheit , Werner Fritsch , Werner Haede , Ernst Lindner
发明人： Ulrich Stache , Kurt Radscheit , Werner Fritsch , Werner Haede , Ernst Lindner
IPC分类号： C07J71/00 , C07J19/00 , A61K31/70
CPC分类号： C07J19/00
摘要： 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.
摘要翻译： 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。

2. 发明授权

US3950323A Digoxigenine-3-[2',3'-didesoxy-glycosides] and a process for their manufacture 失效
标题翻译： DIGOXIGENINE-3-（2'，3'-DIDESOXY-GLYCOSIDES）+0及其制造方法
公开(公告)号：US3950323A
公开(公告)日：1976-04-13
申请号：US416656
申请日：1973-11-16
申请人： Ulrich Stache , Werner Fritsch , Werner Haede , Ernst Lindner
发明人： Ulrich Stache , Werner Fritsch , Werner Haede , Ernst Lindner
IPC分类号： C07J19/00 , A61K31/585
CPC分类号： C07J19/00 , Y10S514/869
摘要： 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.

3. 发明授权

US3937697A 12-Dehydro digoxin-4'"-and 3'"-alkyl ethers 失效
标题翻译： 12-DEHYDRO DIGOXIN-4'+ 41 -AND 3'+ 41-ALKYL ETHERS
公开(公告)号：US3937697A
公开(公告)日：1976-02-10
申请号：US554182
申请日：1975-02-28
申请人： Ulrich Stache , Werner Fritsch , Werner Haede , Ernest Lindner
发明人： Ulrich Stache , Werner Fritsch , Werner Haede , Ernest Lindner
IPC分类号： C07J19/00
CPC分类号： C07J19/005 , Y10S514/869
摘要： 12-Dehydro digoxin mono-4'" and 3'"-alkyl ethers and a process for their manufacture.The compounds have a cardiotonic and diuretic activity.

4. 发明授权

US4191765A 1-Aryloxy-2-hydroxy-3-aminopropanes 失效
标题翻译： 1-芳氧基-2-羟基-3-氨基丙烷
公开(公告)号：US4191765A
公开(公告)日：1980-03-04
申请号：US932504
申请日：1978-08-10
申请人： Werner Fritsch , Ulrich Stache , Ernst Lindner
发明人： Werner Fritsch , Ulrich Stache , Ernst Lindner
IPC分类号： C07D211/14 , C07D295/092 , C07D295/112 , A61K31/215 , A61K31/275 , C07C69/76 , C07C121/80
CPC分类号： C07D295/088 , C07D211/14 , C07D295/112
摘要： Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.1' are identical or different and represent hydrogen, an alkyl radical or alkoxy radical having 1-4 carbon atoms, the allyl group, a halogen atom or the nitro group, R.sup.2 represents an acrylic acid radical or an acrylic acid nitrile radical of the formulae ##STR2## wherein R.sup.5 represents hydrogen, an alkyl radical having 1-5 carbon atoms, an aryl radical or aryl-lower alkyl radical either unsubstituted or substituted by lower alkyl or alkoxy, R.sup.6 represents hydrogen or an alkyl radical having 1-8 carbon atoms, R.sup.7 represents hydrogen, a lower alkyl radical or an aryl-lower alkyl radical, R.sup.3 and R.sup.4 represent together with the nitrogen atom a heterocyclic ring with 5-7 members being optionally substituted by C.sub.1 -C.sub.4 alkyl, in which ring one carbon atom may be replaced by one oxygen atom, sulfur atom or one further nitrogen atom, the latter may be substituted, or wherein R.sup.3 represents hydrogen and R.sup.4 represents a phenyl-alkylene or phenyl-alkylidene radical of the formula ##STR3## in which Alk is alkyl having 1 to 3 carbon atoms, and n is a figure from 1-3, and R.sup.8 and R.sup.9 are identical or different and represent hydrogen, an alkoxy radical having 1-3 carbon atoms or the benzoyl radical or R.sup.8 and R.sup.9 represent together the bismethylene dioxy radical, as well as the physiologically compatible acid addition salts and a process for preparing these compounds.
摘要翻译：式I的化合物其中R 1和R 1'相同或不同并且表示氢，具有1-4个碳原子的烷基或烷氧基，烯丙基，卤原子或硝基，R 2表示丙烯酸酸基或丙烯酸腈基，其中R 5表示氢，具有1-5个碳原子的烷基，未取代或被低级烷基或烷氧基取代的芳基或芳基 - 低级烷基，R 6表示氢或具有1-8个碳原子的烷基，R7表示氢，低级烷基或芳基 - 低级烷基，R3和R4与氮原子一起表示与5-7个成员任选被C1取代的杂环 -C 1-4烷基，其中一个碳原子可以被一个氧原子，硫原子或一个另外的氮原子代替，后者可以被取代，或其中R3代表氢，R4代表苯基亚烷基或苯基亚烷基其中Alk是具有1至3个碳原子的烷基，n是1-3的数字，R8和R9相同或不同并表示氢，具有1-3个碳原子的烷氧基的式“IMAGE”的基团原子或苯甲酰基或R8和R9一起表示双亚乙基二氧自由基，以及生理上相容的酸加成盐和制备这些化合物的方法。

5. 发明授权

US4377575A Corticoid-17-(alkyl carbonates) and process for their manufacture 失效
标题翻译：皮质激素-17-（碳酸烷基酯）及其制造方法
公开(公告)号：US4377575A
公开(公告)日：1983-03-22
申请号：US216258
申请日：1980-12-15
申请人： Ulrich Stache , Werner Fritsch , Hans G. Alpermann , Jurgen K. Sandow
发明人： Ulrich Stache , Werner Fritsch , Hans G. Alpermann , Jurgen K. Sandow
IPC分类号： A61K31/57 , A61K31/58 , A61P29/00 , C07J7/00 , C07J21/00 , C07J31/00 , C07J71/00 , A61K31/56 , C07J5/00
CPC分类号： C07J7/0085 , C07J21/00 , C07J31/006 , C07J71/0047 , Y10S514/887
摘要： What is disclosed are steroid-21-halogeno-17-(alkyl carbonates), useful as medicaments for the treatment of inflammatory dermatoses, and a method for making them.
摘要翻译：公开的是用作治疗炎性皮肤病的药物的类固醇-21-卤代-17-（烷基碳酸酯）及其制备方法。

6. 发明授权

US4242334A Corticoid 17-(alkyl carbonates) and processes for their preparation 失效
标题翻译：皮质激素17-（碳酸烷基酯）及其制备方法
公开(公告)号：US4242334A
公开(公告)日：1980-12-30
申请号：US930194
申请日：1978-08-02
申请人： Ulrich Stache , Werner Fritsch , Hans G. Alpermann
发明人： Ulrich Stache , Werner Fritsch , Hans G. Alpermann
IPC分类号： A61K31/57 , A61P17/00 , A61P29/00 , C07J5/00 , C07J21/00 , C07J31/00 , C07J43/00 , C07J71/00 , A61K31/56 , C07J7/00
CPC分类号： C07J5/0076 , C07J21/00 , C07J31/006 , C07J43/003 , C07J5/0053 , C07J71/0047
摘要： What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.
摘要翻译：所公开的是说明书中定义的式“IMAGE”的皮质激素17-（烷基碳酸酯），该化合物可以以悬浮液，软膏，霜剂，喷雾剂等形式用于兽医治疗和人类治疗，用于治疗非常不同原因的炎性皮肤病。

7. 发明授权

US5637721A Process for the preparation of cephem prodrug esters 失效
标题翻译：头孢烯前药酯的制备方法
公开(公告)号：US5637721A
公开(公告)日：1997-06-10
申请号：US470422
申请日：1995-06-06
申请人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
发明人： Elisabeth Defossa , Gerd Fischer , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D417/12 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/34
CPC分类号： C07D277/587 , C07D417/12 , C07D501/00 , Y02P20/55
摘要： The invention relates to a process which comprises a compound of the formula II ##STR1##
摘要翻译：本发明涉及包含式II化合物的方法

8. 发明授权

US5608093A Corticosteroid 17-alkyl carbonate 21-[0]-carboxylic and carbonic esters, and pharmaceuticals containing these compounds 失效
标题翻译：皮质类固醇17-烷基碳酸酯21- [0] - 羧酸和碳酸酯，以及含有这些化合物的药物
公开(公告)号：US5608093A
公开(公告)日：1997-03-04
申请号：US294804
申请日：1994-08-25
申请人： Ulrich Stache , Hans-Georg Alpermann , Walter D urckheimer , Manfred Bohn
发明人： Ulrich Stache , Hans-Georg Alpermann , Walter D urckheimer , Manfred Bohn
IPC分类号： A61K31/57 , A61P17/00 , A61P29/00 , C07J5/00 , C07J17/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , A61K31/56
CPC分类号： C07J5/0053 , C07J17/00 , C07J31/006 , C07J33/002 , C07J41/005 , C07J43/003 , C07J5/0076
摘要： Corticoid 17-alkyl carbonate 21-carboxylic and carbonic esters of the formula I ##STR1## are described in which A is CHOH and CHCl, CH.sub.2, C.dbd.O or 9(11) double bond; Y is H, F or Cl; Z is H, F or CH.sub.3 ; R(1) is aryl or hetaryl; n and m are zero or 1; R(2) is alkyl or --(CH.sub.2).sub.2 --OCH.sub.3 ; R(3) is H or methyl. They are obtained by reacting a compound of the formula II, ##STR2## in which R(5) is OH, with an activated carboxylic acid of the formula III,R(6)--CO--(O).sub.n --(X)--R(1) III.The compounds I have a very strong local and topical antiinflammatory action and exhibit a very good ratio of local to systemic antiinflammatory effects, which ratio is often markedly superior to that of analogous corticoid 17-alkyl carbonate 21-esters which do not carry any aryl or heteraryl group in the 21-ester radical.
摘要翻译：其中A是CHOH和CHCl，CH2，C = O或9（11）双键，其中描述了式I的皮质激素17-烷基碳酸酯21-羧酸和碳酸酯。 Y为H，F或Cl; Z是H，F或CH 3; R（1）是芳基或杂芳基; n和m为零或1; R（2）是烷基或 - （CH 2）2 -OCH 3; R（3）为H或甲基。 R（6）-CO-（O）n-（X）的活化羧酸与式（Ⅶ）化合物反应，其中R（5）为OH， -R（1）III。化合物I具有非常强的局部和局部抗炎作用，并表现出非常好的局部与全身抗炎作用的比例，该比例通常明显优于不携带任何芳基或类似物的类似皮质类固醇17-烷基碳酸酯21-酯的比例 21位芳基中的杂芳基。

9. 发明授权

US5550232A Diastereomers of 1-(isopropoxycarbonyloxy) ethyl 3-cephem 4-carboxylate 失效
标题翻译： 1-（异丙氧基羰基氧基）乙基3-头孢烯-4-羧酸酯的非对映异构体
公开(公告)号：US5550232A
公开(公告)日：1996-08-27
申请号：US447229
申请日：1995-05-22
申请人： Gerd Fischer , Elisabeth Defossa , Uwe Gerlach , Rolf H orlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann , Dieter Isert
发明人： Gerd Fischer , Elisabeth Defossa , Uwe Gerlach , Rolf H orlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann , Dieter Isert
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/06 , C07D501/34 , C07D501/56 , C07D501/14
CPC分类号： C07D501/00
摘要： Enterally absorbable diastereomers of 1-(isopropoxycarbonyloxy)ethyl (6R,7R)-7-[2-(2-aminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-(methoxymethyl)-3-cephem-4-carboxylate of the formula I ##STR1## and their physiologically acceptable salts and also diastereomerically pure salts of the compounds of the formula II ##STR2## where HX is a mono- or polybasic acid and where X is an inorganic or organic physiologically acceptable anion, and a process for the preparation of these compounds of the formula I or II, which comprises first precipitating the more sparingly soluble diastereomer of the formula IV in the mixing together of 1 equivalent of a solution of the diastereomer mixture of the formula III with 0.2-2 equivalents of a solution of the acid component HY and separating it off by filtration, then precipitating the more readily soluble diastereomer of the formula IV from the filtration solution, it being possible for the acid component HY to be identical or different in the consecutive partial steps and any desired sequence of addition of different acid components HY being possible, and optionally further purifying the obtained salts by crystallization, are described.
摘要翻译： 1-（异丙氧羰基氧基）乙基（6R，7R）-7- [2-（2-氨基噻唑-4-基）-2-（Z） - （甲氧基亚氨基）乙酰氨基] -3-（甲氧基甲基）-3 式I的化合物 - 头孢烯-4-羧酸酯及其生理学上可接受的盐以及式II化合物的非对映体纯盐，其中HX是单或多元酸，其中X是无机或有机的生理学上可接受的阴离子，以及制备这些式I或II化合物的方法，其包括首先将式IV的较微溶的非对映体沉淀在1当量的式（I）的非对映体混合物的溶液中， III与0.2-2当量的酸组分HY的溶液并通过过滤分离，然后从过滤溶液中沉淀出更容易溶解的式IV的非对映异构体，酸组分HY可能相同或不同在一起描述了部分步骤和任何期望的不同酸组分HY的加入顺序是可能的，并且任选地通过结晶进一步纯化得到的盐。

10. 发明授权

US4762648A Monofunctional and bisfunctional anthraquinone-(oxy-2,3-oxidopropanes), processes for their preparation, and their use as drugs 失效
标题翻译：单功能和双功能蒽醌 - （氧-2,3-氧丙烷），其制备方法及其作为药物的用途
公开(公告)号：US4762648A
公开(公告)日：1988-08-09
申请号：US645266
申请日：1984-08-29
申请人： Ulrich Stache , Hans P. Kraemer , Hans-Harald Sedlacek
发明人： Ulrich Stache , Hans P. Kraemer , Hans-Harald Sedlacek
IPC分类号： C07D303/20 , A61K31/335 , A61K31/336 , A61P35/00 , C07D303/22 , C07D303/24 , C07D303/27 , C07C50/34 , C07D303/12
CPC分类号： C07D303/22 , C07D303/24
摘要： The present invention relates to a novel mono-functional and bis-functional anthraquinone-(oxy-2,3-oxido-propanes) and to a process for their preparation. The compounds according to the invention are useful as intermediates in the preparation of drugs possessing a .beta.-receptor blocker action and as crosslinking agents in the preparation of polymers, and moreover exhibit cytostatic activity.
摘要翻译：本发明涉及一种新的单官能和双官能蒽醌 - （氧-2,3-氧基丙烷）及其制备方法。根据本发明的化合物可用作制备具有β-受体阻滞剂作用的药物和作为聚合物制备中的交联剂的中间体，并且还表现出细胞抑制活性。

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