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1. 发明专利

AU5852673A CARDIOACTIVE ANHYDROTALOMETHYLOSIDES 未知
公开(公告)号：AU5852673A
公开(公告)日：1975-02-20
申请号：AU5852673
申请日：1973-07-26
申请人： ULRICH STACHE , ERNST LINDNER , WERNER HAEDE , WERNER FRITSCH
发明人： STACHE ULRICH , LINDNER ERNST , HAEDE WERNER , FRITSCH WERNER
IPC分类号： C07J19/00 , A61K20060101 , A61K31/585 , A61K31/704 , A61P7/10 , A61P9/04 , C07C20060101 , C07D20060101 , A61K27/00 , C07C173/02
摘要： The invention relates to 3', 4'-anhydro- beta , L-talomethylosides 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.

2. 发明授权

US6152404A Apparatus for influencing a wing root airflow in an aircraft 失效
标题翻译：影响飞机机翼根部气流的装置
公开(公告)号：US6152404A
公开(公告)日：2000-11-28
申请号：US78292
申请日：1998-05-13
申请人： Axel Flaig , Detlev Schwetzler , Ulrich Stache, deceased
发明人： Axel Flaig , Detlev Schwetzler , Ulrich Stache, deceased
IPC分类号： B64C9/24 , B64C21/00 , B64C23/06
CPC分类号： B64C23/06 , B64C9/24 , Y02T50/162 , Y02T50/44
摘要： An apparatus advantageously influences the wing root airflow along the wing root of an aircraft having a high lift system including leading edge slats provided on the main wings. The apparatus includes a respective vortex generator arranged on the inboard end of each leading edge slat in the area of the wing root, and further includes a respective transition fairing arranged on a separation edge that is let into the leading edge of the wing root and that borders along the inboard edge of the respective slat. The vortex generator is a rigid member fixed to the leading edge slat and may be in the shape of a horn, a disk, or a winglet. The transition fairing may be a rigid member fixed to the wing root along the separation edge, or may be a flexible elastic member that can be inflated to have a variable outer contour. The present system avoids the need of additional independently movable auxiliary flaps, and thus achieves a reduced weight, complexity, and maintenance requirement.
摘要翻译：装置有利地影响沿着具有高提升系统的飞机的翼根的翼根气流，包括设置在主翼上的前缘板条。该装置包括设置在翼根区域中每个前缘板条的内侧端部的相应的涡流发生器，并且还包括布置在分离边缘上的相应的过渡整流装置，该分离边缘进入翼根的前缘，并且其中，沿着相应板条的内侧边缘边界。涡流发生器是固定到前缘板条的刚性构件，并且可以是喇叭，盘或小翼的形状。过渡整流罩可以是沿着分离边缘固定到翼根的刚性构件，或者可以是可膨胀以具有可变外轮廓的柔性弹性构件。本系统避免了额外的独立移动的辅助翼片的需要，从而实现了减轻的重量，复杂性和维护要求。

3. 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

4. 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。

5. 发明专利

AU5852873A CARDENOLIDE-3-%2@-DESOXY-GLYCOSIDES< 未知
公开(公告)号：AU5852873A
公开(公告)日：1975-01-30
申请号：AU5852873
申请日：1973-07-26
申请人： KURT RADSCHEIT , ERNST LINDNER , ULRICH STACHE , WERNER FRITSCH , WERNER HAEDE
发明人： RADSCHEIT KURT , LINDNER ERNST , STACHE ULRICH , FRITSCH WERNER , HAEDE WERNER
IPC分类号： C07J19/00 , A61K20060101 , A61K31/585 , A61P1/08 , A61P7/10 , A61P9/04 , A61P9/14 , C07C20060101 , C07D20060101 , C07J20060101 , C07C173/02 , A61K27/00
摘要： 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.

6. 发明授权

US5614623A Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate and processes for their preparation 失效
标题翻译： 3-头孢烯-4-羧酸1-（异丙氧基羰基氧基）乙酯的非对映异构体及其制备方法
公开(公告)号：US5614623A
公开(公告)日：1997-03-25
申请号：US447249
申请日：1995-05-22
申请人： Gerd Fischer , Elisabeth Defo.beta.a , Uwe Gerlach , Rolf H orlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann , Dieter Isert
发明人： Gerd Fischer , Elisabeth Defo.beta.a , 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 , C07D501/22
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 steps.
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consecu 有步骤。

7. 发明授权

US5461043A Diastereomers of 1-(isopropoxycarbonyloxy)ethyl 3-cephem-4-carboxylate 失效
标题翻译： 3-头孢烯-4-羧酸1-（异丙氧基羰基氧基）乙酯的非对映异构体
公开(公告)号：US5461043A
公开(公告)日：1995-10-24
申请号：US940367
申请日：1992-09-03
申请人： Gerd Fischer , Elisabeth Defossa , Uwe Gerlach , Rolf Horlein , Norbert Krass , Rudolf Lattrell , Ulrich Stache , Theodor Wollmann , Dieter Isert
发明人： Gerd Fischer , Elisabeth Defossa , Uwe Gerlach , Rolf Horlein , 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 , C07D501/22
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。

8. 发明授权

US5362721A Corticoid-17-alkyl-carbonates substituted in the 17-position, process for their preparation and pharmaceuticals containing them 失效
标题翻译：在17位取代的皮质类固醇-17-烷基 - 碳酸酯，其制备方法和含有它们的药物
公开(公告)号：US5362721A
公开(公告)日：1994-11-08
申请号：US015041
申请日：1993-02-08
申请人： Ulrich Stache , Walter Durckheimer , Hans G. Alpermann , Walter Petri
发明人： Ulrich Stache , Walter Durckheimer , Hans G. Alpermann , Walter Petri
IPC分类号： A61K31/57 , A61P29/00 , A61P37/08 , C07J5/00 , C07J7/00 , C07J21/00 , C07J31/00 , C07J9/00
CPC分类号： C07J7/0085 , C07J21/00 , C07J31/006 , C07J5/0053 , C07J5/0076
摘要： The disclosed invention includes corticoid-17-alkylcarbonates substituted in the 17-position, a process for their preparation and pharmaceuticals containing them. These corticoid-17-alkylcarbonates have the following formula I ##STR1## where A is CHOH in any desired steric arrangement, C.dbd.O or CH.sub.2 ; Y is H, F, or Cl; Z is H, F or CH.sub.3 ; R(1) is O-acyl, carbonylalkyl, alkylsulfonate or arylsulfonate;R(2) is branched alkyl or (CH.sub.2).sub.2-4 --OCH.sub.3 andR(3) is H or methyl. They have excellent local and topical antiinflammatory action. They are distinguished by a particularly good ratio of local to systemic antiinflammatory activity and in some cases also show stronger local antiinflammatory activities than their isomeric corticoid-17-alkylcarbonates having a linear alkyl group in the 17-alkylcarbonate moiety.
摘要翻译：所公开的发明包括在17位取代的皮质类固醇-17-烷基碳酸酯，其制备方法和含有它们的药物。这些皮质激素-17-烷基碳酸酯具有以下分子式I，其中A是任何所需空间排列中的CHOH，C = O或CH 2; Y是H，F或Cl; Z是H，F或CH 3; R（1）是O-酰基，羰基烷基，烷基磺酸酯或芳基磺酸酯; R（2）是支链烷基或（CH2）2-4-OCH3，R（3）是H或甲基。他们具有优异的局部和局部抗炎作用。它们的区别在于局部与系统性抗炎活性的比例特别好，并且在某些情况下也显示出比其在17-烷基碳酸酯部分具有直链烷基的异构的类皮质激素-17-烷基碳酸酯更强的局部抗炎活性。

9. 发明授权

US5260425A Anthracycline derivatives having cytostatic activity 失效
标题翻译：具有细胞抑制活性的蒽环类衍生物
公开(公告)号：US5260425A
公开(公告)日：1993-11-09
申请号：US360807
申请日：1989-06-02
申请人： Peter Hermentin , Ernst Raab , Cenek Kolar , Manfred Gerken , Dieter Hoffmann , Hans P. Kraemer , Ulrich Stache
发明人： Peter Hermentin , Ernst Raab , Cenek Kolar , Manfred Gerken , Dieter Hoffmann , Hans P. Kraemer , Ulrich Stache
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/26 , C07H15/24
CPC分类号： C07H15/252 , C07H15/26
摘要： The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, ##STR1## which can optionally also be in the form of an acid addition salt of physiologically acceptable inorganic or organic acids, where R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen, a hydroxyl or a methoxy group, R.sup.3 is hydrogen or a hydroxyl group, R.sup.4 is hydrogen or a hydroxyl group, R.sup.5 hydrogen, a hydroxyl or a methoxycarbonyl group, R.sup.6 is CH.sub.2 CH.sub.3, COCH.sub.3, COCH.sub.2 OH, CHOHCH.sub.3 or CHOHCH.sub.2 OH and R.sup.7 is an organic substituent which has 2 to 6 carbon atoms and which contains at least one oxygen, nitrogen or sulfur atom or a C--C double bond or a C--C triple bond, it being possible for the double bond also to be a constituent of a heteroaromatic system and for the oxygen, nitrogen or sulfur atom to be a constituent of an open-chain or heterocyclic system, to a process for the preparation thereof and to the use thereof in a pharmaceutical.
摘要翻译：本发明涉及具有细胞抑制活性的新型蒽环类衍生物和通式I，其也可以是生理上可接受的无机或有机酸的酸加成盐形式，其中R 1是氢或羟基， R2是氢，羟基或甲氧基，R3是氢或羟基，R4是氢或羟基，R5是氢，羟基或甲氧基羰基，R6是CH2CH3，COCH3，COCH2OH，CHOHCH3或CHOHCH2OH和R7 是具有2至6个碳原子并且含有至少一个氧，氮或硫原子或CC双键或CC三键的有机取代基，双键也可以是杂芳族体系的组分以及氧，氮或硫原子作为开链或杂环体系的组分，其制备方法及其在药物中的用途。

10. 发明授权

US3682987A PROCESS FOR THE MANUFACTURE OF {66 {11 {11 14-20-KETO-21-DIALKOXY STEROIDS 失效
标题翻译：制备{66 {11 {11-14-20-酮二十二烷氧基甾体的方法
公开(公告)号：US3682987A
公开(公告)日：1972-08-08
申请号：US3682987D
申请日：1969-04-14
申请人： KURT RADSCHEIT , ULRICH STACHE , WERNER FRITSCH , WERNER HAEDE , HOECHST AG
发明人： RADSCHEIT KURT , STACHE ULRICH , FRITSCH WERNER , HAEDE WERNER
IPC分类号： A61K31/573 , A61K31/58 , C07C169/32
CPC分类号： A61K31/573 , A61K31/58
摘要： 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.
摘要翻译：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。

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