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1.发明授权
公开(公告)号：US5958906A
公开(公告)日：1999-09-28
申请号：US852492
申请日：1997-05-07
CPC分类号： C07F9/723
摘要： Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.
摘要翻译： 含有Th2主要组分（P，As，Sb，Bi）的更高元素的磷脂衍生物，它们的制备方法以及可从磷脂衍生物制备的抗肿瘤和抗微生物活性药物。
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公开(公告)号：US5449798A
公开(公告)日：1995-09-12
申请号：US124492
申请日：1993-09-22
IPC分类号： A61K31/66 , A61K31/285 , A61K31/665 , A61K31/67 , A61K31/675 , A61K38/00 , A61P3/00 , A61P7/02 , A61P19/10 , A61P31/04 , A61P31/12 , A61P33/02 , A61P35/00 , A61P37/00 , A61P43/00 , C07F9/09 , C07F9/10 , C07F9/54 , C07F9/655 , C07F9/6564 , C07F9/66 , C07F9/68 , C07F9/72 , C07F9/90 , C07F9/94 , C07F9/70
CPC分类号： C07F9/723 , C07F9/5407
摘要： Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.
摘要翻译： 含有Th2主要组分（P，As，Sb，Bi）的更高元素的磷脂衍生物，它们的制备方法以及可从磷脂衍生物制备的抗肿瘤和抗微生物活性药物。
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公开(公告)号：US5637577A
公开(公告)日：1997-06-10
申请号：US421920
申请日：1995-04-14
IPC分类号： A61K31/66 , A61K31/285 , A61K31/665 , A61K31/67 , A61K31/675 , A61K38/00 , A61P3/00 , A61P7/02 , A61P19/10 , A61P31/04 , A61P31/12 , A61P33/02 , A61P35/00 , A61P37/00 , A61P43/00 , C07F9/09 , C07F9/10 , C07F9/54 , C07F9/655 , C07F9/6564 , C07F9/66 , C07F9/68 , C07F9/72 , C07F9/90 , C07F9/94 , A61K31/555 , A61K31/34
CPC分类号： C07F9/723 , C07F9/5407
摘要： Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.
摘要翻译： 含有Th2主要组分（P，As，Sb，Bi）的更高元素的磷脂衍生物，它们的制备方法以及可从磷脂衍生物制备的抗肿瘤和抗微生物活性药物。
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4.发明授权Octadecyl-[2-(N-methylpiperidino)-ethyl]-phosphate and a process for its preparation 失效十八烷基 - （2-（N-甲基哌啶） - 乙基） - 磷酸酯及其制备方法
公开(公告)号：US5219866A
公开(公告)日：1993-06-15
申请号：US907025
申请日：1992-07-01
申请人： Wolfgang Schumacher , Jurgen Engel , Gerhard Nossner , Bernhard Kutscher , Jurij Stekar , Peter Hilgard
发明人： Wolfgang Schumacher , Jurgen Engel , Gerhard Nossner , Bernhard Kutscher , Jurij Stekar , Peter Hilgard
IPC分类号： A61K31/675 , A61P35/00 , C07F9/59
CPC分类号： A61K31/685 , C07F9/591
摘要： Octadecyl-[2-(N-methylpiperidino)-ethyl]-phosphate and a process for its preparation. This compound is useful for the treatment of cancer.
摘要翻译： 十八烷基 - [2-（N-甲基哌啶子基） - 乙基] - 磷酸酯及其制备方法。 该化合物可用于治疗癌症。
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公开(公告)号：US06479472B1
公开(公告)日：2002-11-12
申请号：US09672497
申请日：2000-09-29
申请人： Gerhard Nössner , Bernhard Kutscher , Jürgen Engel , Wolfgang Schumacher , Jurij Stekar , Peter Hilgard
发明人： Gerhard Nössner , Bernhard Kutscher , Jürgen Engel , Wolfgang Schumacher , Jurij Stekar , Peter Hilgard
IPC分类号： C07D21122
CPC分类号： A61K31/675 , A61K31/452 , C07F9/5532 , C07F9/572 , C07F9/59 , C07F9/6561 , Y02A50/409
摘要： A method of treating protozoal and fungal diseases is described, in which an effective amount of a compound of formula I is administered to a host having a protozoal or fungal disease. Also described are methods of treating bone marrow damage composed of administering, to a host having bone marrow damage due to treatment with cytostatic agents or other myelotoxic active ingredients, an effective amount of a compound of formula I
摘要翻译： 描述了治疗原生动物和真菌疾病的方法，其中将有效量的式I化合物施用于具有原生动物或真菌病的宿主。 还描述了治疗骨髓损伤的方法，其包括给予由于用细胞生长抑制剂或其它骨髓毒性活性成分治疗而造成的骨髓损伤的宿主，有效量的式I化合物
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公开(公告)号：US06172050B2
公开(公告)日：2001-01-09
申请号：US08905333
申请日：1997-08-04
申请人： Gerhard Nössner , Bernhard Kutscher , J{umlaut over (u)}rgen Engel , Wolfgang Schumacher , Jurij Stekar , Peter Hilgard
发明人： Gerhard Nössner , Bernhard Kutscher , J{umlaut over (u)}rgen Engel , Wolfgang Schumacher , Jurij Stekar , Peter Hilgard
IPC分类号： A61K31675
CPC分类号： A61K31/675 , A61K31/452 , C07F9/5532 , C07F9/572 , C07F9/59 , C07F9/6561 , Y02A50/409
摘要： Phospholipid derivatives of Formula X: wherein A is the ring system in which R is a linear or branched alkyl radical having 10 to 24 carbon atoms which may contain one or more double or triple bonds; R1 and R2 are independently hydrogen or linear alkyl radicals having 1 to 3 carbon atoms; y is 0, 1, 2 or 3; m and n are independently 0 or in an integer, with the proviso that m+n is between 2 and 8; or A is a tropanio or quinuclidinio ring system, which is linked via a carbon-carbon bond and is optionally substituted by one or more methyl groups; processes for the preparation of the derivatives, and methods for treating tumors therewith.
摘要翻译： 式X的磷脂衍生物：其中A是环系，其中R是具有10至24个碳原子的直链或支链烷基，其可以含有一个或多个双键或三键; R1和R2独立地是氢或具有1至3个碳原子的直链烷基; y为0,1,2或3; m和n独立地为0或整数，条件是m + n在2和8之间; 或A是通过碳 - 碳键连接并且任选地被一个或多个甲基取代的托普拉尼或奎宁环系统; 衍生物的制备方法，以及用于治疗肿瘤的方法。
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7.发明授权Pharmaceutically active 1,2,4-triamino-benzene derivatives, processes for their preparation and pharmaceutical compositions containing them 失效药学活性的1,2,4-三氨基 - 苯衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5384330A
公开(公告)日：1995-01-24
申请号：US2458
申请日：1993-01-08
申请人： Hans-Reinhold Dieter , Jurgen Engel , Bernhard Kutscher , Emanuel Polymeropoulos , Stefan Szelenyi , Bernd Nickel
发明人： Hans-Reinhold Dieter , Jurgen Engel , Bernhard Kutscher , Emanuel Polymeropoulos , Stefan Szelenyi , Bernd Nickel
IPC分类号： A61K31/165 , A61K31/167 , A61K31/17 , A61K31/18 , A61K31/185 , A61K31/235 , A61K31/27 , A61P21/02 , A61P25/02 , A61P25/08 , A61P25/26 , C07C233/43 , C07C233/44 , C07C235/38 , C07C237/20 , C07C271/28 , C07C271/58 , C07C275/40 , C07C309/45 , C07C311/12 , C07C311/35 , C07C317/32 , A61K31/24
CPC分类号： C07C233/43 , C07C271/28 , C07C275/40
摘要： Pharmacologically active 1,2,4-triaminobenzene derivatives of the General Formula I: ##STR1## where the symbols R1' R2' R3' R4' R5' Ar and Alk have the following meanings:where the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Ar and Alk have the following meanings:R.sub.1 : hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or the radical Ar;R.sub.2 : hydrogen or C.sub.1 -C.sub.6 -alkyl;R.sub.3 : C.sub.1 -C.sub.6 -alkoxy, NH.sub.2, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -dialkylamino, amino substituted by the radical Ar, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, the radical Ar or the radical ArO--;R.sub.4 : hydrogen, C.sub.1 -C.sub.6 -alkyl or the radical Ar;R.sub.5 : hydrogen or C.sub.1 -C.sub.6 -alkyl or the radical Ar;Alk: a straight or branched alkylene group containing 1-9 carbon atoms, which can also be substituted by the radical Ar.
摘要翻译： 通式I的药理活性的1,2,4-三氨基苯衍生物：其中符号R1'R2'R3'R4'R5'Ar和Alk具有以下含义：其中符号R1，R2，R3，R4 ，R 5，Ar和Alk具有以下含义：R 1：氢，C 1 -C 6 - 烷基，C 2 -C 6 - 烷酰基或基团Ar; R2：氢或C1-C6-烷基; R3：C1-C6-烷氧基，NH2，C1-C6-烷基氨基，C1-C6-二烷基氨基，被Ar，C1-C6-烷基，C2-C6-烯基，C2-C6-炔基取代的氨基，基团Ar 或激进的ArO-; R4：氢，C1-C6烷基或基团Ar; R5：氢或C1-C6-烷基或基团Ar; Alk：含有1-9个碳原子的直链或支链亚烷基，也可以被基团Ar取代。
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8.发明授权Long-chain alkylamides of amino acids and peptides with anti-proliferative and anti-inflammatory properties 失效具有抗增殖和抗炎特性的氨基酸和肽的长链烷基酰胺
公开(公告)号：US5770574A
公开(公告)日：1998-06-23
申请号：US878842
申请日：1997-06-19
申请人： Bernhard Kutscher , Michael Bernd , Heinz Grossmann , Maria Kick , Jurgen Arp , Manfred Lieflander , Jurgen Engel , Rainer Voegeli
发明人： Bernhard Kutscher , Michael Bernd , Heinz Grossmann , Maria Kick , Jurgen Arp , Manfred Lieflander , Jurgen Engel , Rainer Voegeli
IPC分类号： A61K38/00 , A61K31/16 , A61K31/195 , A61K31/40 , A61P29/00 , A61P43/00 , C07K5/068 , C07K5/09 , A61K38/05 , A61K38/06 , C07K5/00
CPC分类号： C07K5/0815 , A61K31/195 , A61K31/40 , C07K5/06086 , A61K38/00 , Y02P20/55
摘要： Long-chain, unbranched alkylamides of the general formula CH.sub.3 --(CH.sub.2).sub.n N--NH--R in which n=11-20 and R=amino acid, its D- and L-enantiomers, di- and tripeptides, forms derived by N-protective groups, and terminal ethyl esters as well as its physiologically compatible salt forms as active pharmaceutical substances with anti-proliferative and anti-inflammatory properties.
摘要翻译： n = 11-20的通式CH 3 - （CH 2）n N-NH-Rin的长链，无支链的烷基酰胺，R =氨基酸，其D-和L-对映异构体，二肽和三肽，由N-保护性 基团和末端乙酯以及其与生理上相容的盐形式作为具有抗增殖和抗炎特性的活性药物。
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公开(公告)号：US5747534A
公开(公告)日：1998-05-05
申请号：US714456
申请日：1996-09-16
IPC分类号： A61K31/555 , A61P35/00 , C07C211/65 , C07F15/00 , A61K31/295
CPC分类号： C07F15/0093
摘要： Cis-�trans-1,2-cyclobutanebis (methylamine)-N,N'!-�(2S)-lactate-O.sup.1,O.sup.2)-platinum (II) trihydrate (lobaplatin trihydrate) and its preparation.
摘要翻译： 顺式 - [反式-1,2-环丁烷双（甲胺）-N，N'] - [（2S） - 乳酸酯-O1，O2） - 三水合铂（II）三水合物及其制备。
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10.发明授权4,5-dihydro-4-oxo-pyrrolo[1,2-a]quinoxalinones and corresponding aza analogs and a process for their preparation 失效4,5-二氢-4-氧代 - 吡咯并[1,2-a]喹喔啉酮和相应的氮杂类似物及其制备方法
公开(公告)号：US5405847A
公开(公告)日：1995-04-11
申请号：US110957
申请日：1993-08-24
申请人： Hans-Reinhold Dieter , Jurgen Engel , Karl-Heinz Klingler , Bernhard Kutscher , Stefan Szelenyi , Ute Achterath-Tuckermann , Jurgen Schmidt , Peter Metzenauer
发明人： Hans-Reinhold Dieter , Jurgen Engel , Karl-Heinz Klingler , Bernhard Kutscher , Stefan Szelenyi , Ute Achterath-Tuckermann , Jurgen Schmidt , Peter Metzenauer
IPC分类号： A61K31/495 , A61K31/505 , A61K31/535 , A61P9/08 , A61P9/12 , A61P11/00 , A61P25/20 , A61P37/08 , C07D471/14 , C07D487/04 , C07D487/14
CPC分类号： C07D471/14 , C07D487/04
摘要： Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R.sub.1 is C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.3 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkanoyloxy, benzoyloxy, morpholinocarbonyloxy, C.sub.1 -C.sub.6 -alkyloxycarbonyloxy, C.sub.1 -C.sub.6 -alkylaminocarbonyloxy, C.sub.1 -C.sub.6 -dialkylaminocarbonyloxy or the group -Alk-A, where Alk represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -hydroxyalkyl or C.sub.3 -C.sub.6 -cycloalkyl and the symbol A represents hydrogen or other substituents.R.sub.2, R.sub.3 and R.sub.4 represent various substituents, where R.sub.1 may also be hydrogen, when R.sub.2 is the group ##STR2## and R.sub.5 represents phenyl, C.sub.1 -C.sub.4 -alkoxyphenyl or diphenylmethyl and R.sub.3 and R.sub.4 are hydrogen and their salts. The compounds provide anti-allergic, anti-asthmatic, anxiolytic and hypotensive effects.
摘要翻译： 式新颖的化合物，其中苯环也可以含有氮原子而不是CH基团，R 1是C 2 -C 6 - 烯基，C 2 -C 6炔基，羟基，C 1 -C 6 - 烷氧基，C 3 -C 6 - 烯氧基，C 3 -C 6 - 炔氧基，C 2 -C 6 - 烷酰氧基，苯甲酰氧基，吗啉代羰基氧基，C 1 -C 6烷氧基羰基氧基，C 1 -C 6烷基氨基羰氧基，C 1 -C 6 - 二烷基氨基羰氧基或-Alk-A，其中Alk表示C1-C6 - 烷基，C 2 -C 6 - 羟基烷基或C 3 -C 6 - 环烷基，符号A表示氢或其它取代基。 R 2，R 3和R 4表示各种取代基，其中R 1也可以是氢，当R 2是基团时，R 5表示苯基，C 1 -C 4烷氧基苯基或二苯甲基，R 3和R 4是氢。 该化合物提供抗过敏，抗哮喘，抗焦虑和降压作用。
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