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1. 发明授权

US4670427A 1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes, their preparation and pharmaceutical use 失效
标题翻译： 1α，2α-亚甲基-6-亚甲基和6α-甲基孕烯，其制备和药物用途
公开(公告)号：US4670427A
公开(公告)日：1987-06-02
申请号：US692488
申请日：1985-01-18
申请人： Klaus Annen , Henry Laurent , Walter Elger , Rudolf Wiechert , Helmut Hofmeister , Michael Topert
发明人： Klaus Annen , Henry Laurent , Walter Elger , Rudolf Wiechert , Helmut Hofmeister , Michael Topert
IPC分类号： A61K31/57 , C07J7/00 , C07J51/00 , C07J53/00 , C07J1/00 , A61K31/56
CPC分类号： C07J53/005 , C07J7/0045
摘要： 1.alpha.,2.alpha.-methylene-6-methylene- and 6.alpha.-methylpregnenes of Formula I ##STR1## wherein A is ##STR2## and R is a hydrogen atom, an acyl group, or an alkoxymethyl groupare strong antiandrogens, and suitable for the topical treatment of seborrhea, acne, alopecia, and hirsutism.
摘要翻译：式Ⅰ的α，α，α，亚甲基-6-亚甲基和6α-甲基孕烯，其中A是A，而R是氢原子，酰基或烷氧基甲基是强抗雄激素，适用于皮脂溢，痤疮，脱发和多毛症的局部治疗。

2. 发明授权

US4777165A 6.alpha., 16.beta.-dimethyl corticoids and their anti-inflammatory use 失效
标题翻译： 6α，16β-二甲基皮质激素及其抗炎用途
公开(公告)号：US4777165A
公开(公告)日：1988-10-11
申请号：US64029
申请日：1987-06-17
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Michael Topert
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Rudolf Wiechert , Michael Topert
IPC分类号： A61K31/57 , A61K31/575 , A61P5/38 , C07J5/00 , C07J7/00 , C07J9/00 , C07J31/00 , C07J71/00 , A61K31/56 , C07J1/00
CPC分类号： C07J7/0055 , C07J31/006 , C07J5/0076 , C07J71/0015 , C07J9/00
摘要： 6.alpha.,16.beta.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond .sub.-------- is a single bond or a double bond, andX is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,Z is a hydrogen atom or, jointly with X, is a carbon-carbon bond,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom or a methyl group,are pharmacologically active compounds.
摘要翻译： 6α，16β-二甲基皮质类固醇通式Ⅰ（Ⅰ）其中键----是单键或双键，X是氢原子，氟原子，氯原子或溴原子，Z为氢原子，或与X一起为碳 - 碳键，R1为2-8个碳原子的甲酰基，烷酰基或烷氧基烷基，或苯甲酰基，Y为氢原子或甲基是药理活性化合物。

3. 发明授权

US4619922A 6.alpha., 16.alpha.-dimethyl corticoids 失效
标题翻译： 6α，16α-二甲基皮质激素
公开(公告)号：US4619922A
公开(公告)日：1986-10-28
申请号：US688134
申请日：1985-01-02
申请人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Michael Topert
发明人： Klaus Annen , Henry Laurent , Helmut Hofmeister , Michael Topert
IPC分类号： A61K31/57 , A61P5/38 , C07J5/00 , C07J7/00 , C07J21/00 , C07J31/00
CPC分类号： C07J7/0085 , C07J21/00 , C07J31/006 , C07J5/0076 , C07J7/0055
摘要： 6.alpha.,16.alpha.-Dimethyl corticoids of general Formula I ##STR1## wherein the bond is a single bond or a double bond,X is a hydrogen atom, a fluorine atom, a chlorine atom, or a bromine atom,R.sub.1 is a formyl group, an alkanoyl group or alkoxyalkyl group of 2-8 carbon atoms, or a benzoyl group, andY is a hydrogen atom, a chlorine atom, a hydroxy group, a formyl group, an alkanoyloxy group of 2-8 carbon atoms, or a benzoyloxy group,are pharmacologically effective compounds.
摘要翻译： 6α，16α-二甲基皮质类固醇通式Ⅰ（Ⅰ）其中键是单键或双键，X是氢原子，氟原子，氯原子或溴原子，R1 是甲酰基，2-20个碳原子的烷酰基或烷氧基烷基或苯甲酰基，Y是氢原子，氯原子，羟基，甲酰基，2-8碳的烷酰氧基原子或苯甲酰氧基是药理学上有效的化合物。

4. 发明授权

US5010071A Androstane derivatives 失效
标题翻译：雄甾烷衍生物
公开(公告)号：US5010071A
公开(公告)日：1991-04-23
申请号：US379399
申请日：1989-07-13
申请人： Dieter Bittler , Henry Laurent , Petra Rach , Michael Topert
发明人： Dieter Bittler , Henry Laurent , Petra Rach , Michael Topert
IPC分类号： A61K31/57 , A61P17/00 , C07J1/00 , C07J5/00 , C07J21/00
CPC分类号： C07J21/006 , C07J1/0033 , Y10S514/859 , Y10S514/864
摘要： Androstane derivatives of the general Formula I ##STR1## in which R.sub.1 represents a hydrogen atom or a methyl group,X and Y each mean hydrogen atoms or together a carbon-carbon bond, andR.sub.2 symbolizes a hydrogen atom or an alkyl group with 1 to 6 carbon atoms,are pharmaceutically effective substances which have a distinct antiandrogenic effectiveness in topical application.
摘要翻译：其中R 1表示氢原子或甲基的通式I的（I）的雄甾烷衍生物，X和Y各自表示氢原子或碳 - 碳键，R2表示氢原子或烷基具有1至6个碳原子的是在局部施用中具有明显的抗雄激素效力的药学有效物质。

5. 发明授权

US5616573A Glucocorticoids 失效
标题翻译：糖皮质激素
公开(公告)号：US5616573A
公开(公告)日：1997-04-01
申请号：US530352
申请日：1995-10-06
申请人： Hans J. Zentel , Michael Topert , Henry Laurent , Thomas Brumby , Peter Esperling
发明人： Hans J. Zentel , Michael Topert , Henry Laurent , Thomas Brumby , Peter Esperling
IPC分类号： A61K31/57 , A61K31/58 , A61P29/00 , C07J41/00 , C07J43/00 , C07J5/00
CPC分类号： C07J41/005 , C07J43/003
摘要： Glucocorticoids of general formula IR--Val--O--GC (II),are described,in whichO-GC is the radical of a 21-hydroxycorticoid that has an antiinflammatory action,Val represents a valine radical in the 21-position of the corticoid andR means a hydrogen atom or a hydrocarbon radical with up to 32 carbon atoms that is optionally substituted by hydroxy groups, amino groups, oxo groups and/or halogen atoms and/or interrupted by oxygen atoms, SO.sub.2 groups and/or NH groups and their salts.
摘要翻译： PCT No.PCT / EP94 / 00937 371日期1995年10月6日 102（e）日期1995年10月6日PCT 1994年3月24日PCT公布。出版物WO94 / 22898 日期：1994年10月13日描述了通式IR-Val-O-GC（II）的糖皮质激素，其中O-GC是具有抗炎作用的21-羟基皮质激素的基团，Val表示21位的缬氨酸基团皮质激素和R表示氢原子或具有多至32个碳原子的烃基，其任选被羟基，氨基，氧代基和/或卤素原子取代和/或被氧原子，SO2基团和 /或NH基及其盐。

6. 发明授权

US5089175A Hydroxyalkane carboxylic acid derivatives and their production 失效
标题翻译：羟基烷氧基羧酸衍生物及其生产
公开(公告)号：US5089175A
公开(公告)日：1992-02-18
申请号：US480497
申请日：1990-02-16
申请人： Christopher G. Earnshaw , Gerald Kirsch , Petra Rach , Ruth Thieroff-Ekerdt , Michael Topert
发明人： Christopher G. Earnshaw , Gerald Kirsch , Petra Rach , Ruth Thieroff-Ekerdt , Michael Topert
IPC分类号： A61K31/19 , A61K31/22 , A61K31/40 , A61P17/00 , A61P29/00 , A61P31/04 , C07C231/02 , C07C231/12 , C07C235/06 , C07C235/08 , C07D295/10 , C07D295/185
CPC分类号： C07D295/185 , C07C235/06
摘要： Hydroxyalkane carboxylic acid derivatives of general formula I ##STR1## in which n means the numbers 7 to 18,R.sub.1 represents a hydrogen atom or an acyl group with a maximum of 16 carbon atoms, andoptionally an alkylene group with 4 to 8 carbon atoms interrupted by an oxygen atom or a nitrogen atom, are useful for the production of pharmaceutical agents for local treatment of diseases of the skin and mucous membranes.
摘要翻译：通式I的羟基烷烃羧酸衍生物（I）其中n表示数字7至18，R 1表示氢原子或最多16个碳原子的酰基，任选具有4至8个亚烷基由氧原子或氮原子中断的碳原子可用于制备局部治疗皮肤和粘膜疾病的药剂。

7. 发明授权

US4543329A Process for the specific cleavage of protein sequences from proteins 失效
标题翻译：蛋白质序列特异性切割的方法
公开(公告)号：US4543329A
公开(公告)日：1985-09-24
申请号：US395433
申请日：1982-07-06
申请人： Joachim Daum , Gerhard Siewert , Michael Topert , Hartmut Seliger
发明人： Joachim Daum , Gerhard Siewert , Michael Topert , Hartmut Seliger
IPC分类号： C07K14/575 , C07K14/61 , C07K14/62 , C12N15/62 , C12P21/06 , C12N15/00 , C12P21/02
CPC分类号： C07K14/62 , C07K14/57554 , C07K14/61 , C12N15/62 , C12P21/06 , C07K2319/00 , C07K2319/50 , C07K2319/61 , C07K2319/75 , Y10S930/31
摘要： A process for cleavage of a protein (a) sequence from a protein containing the tetrapeptide sequence Pro-Xyz-Gly-Pro, wherein Xyz can be any desired amino acid, and reacting the protein with a collagenase whereby the Xyz-Gly bond is selectively cleaved, thereby producing a protein with the sequence Gly-Pro at its N-terminal end; or (b) containing the sequence Met-Pro; and subsequently selectively cleaving the glycine or methionine residue from the N-terminal end of the product protein with an aminoacylproline aminopeptidase and selectively cleaving the proline residue therefrom with a proline aminopeptidase; or subsequently selectively cleaving the Gly-Pro or Met-Pro residue from the N-terminal end of the produced protein using a postproline dipeptidylaminopeptidase. In a special embodiment, the protein which is split contains the sequence -Zxy-Uvw-Pro- on the carboxy end of the sequence Pro-Xyz-Gly-Pro, wherein Zxy and Uvw are independently any natural amino acid in the genetic code except Pro, whereby after the collagenase reaction, there is produced a protein with the sequence Gly-Pro-Zxy-Uvw-Pro at the N-terminal end. This is split by subsequently selectively cleaving the Pro-Zxy-bond by treating the protein with postproline dipeptidylaminopeptidase (PPDA), thereby producing protein having the sequence Zxy-Uvw-Pro at its N-terminal end, followed by cleaving the Zxy acid from the resultant protein by treating the latter with leucine aminopeptidase.
摘要翻译：从含有四肽序列Pro-Xyz-Gly-Pro的蛋白质中切割蛋白质（a）序列的方法，其中Xyz可以是任何所需的氨基酸，并使蛋白质与胶原酶反应，由此Xyz-Gly键是选择性的从而在其N-末端产生具有Gly-Pro序列的蛋白质; 或（b）含有序列Met-Pro; 并随后用氨酰脯氨酸氨基肽酶选择性地从产物蛋白的N末端切割甘氨酸或甲硫氨酸残基，并用脯氨酸氨基肽酶选择性地切割脯氨酸残基; 或随后使用后脯氨酸二肽基氨基肽酶从产生的蛋白质的N末端选择性地切割Gly-Pro或Met-Pro残基。在一个特殊的实施方案中，分裂的蛋白质包含序列Pro-Xyz-Gly-Pro的羧基末端的序列-Zxy-Uvw-Pro，其中Zxy和Uvw独立地是遗传密码中的任何天然氨基酸， Pro，由此在胶原酶反应之后，在N末端产生具有序列Gly-Pro-Zxy-Uvw-Pro的蛋白质。通过用后脯氨酸二肽基氨基肽酶（PPDA）处理蛋白质随后选择性地切割Pro-Zxy-键，从而在其N-末端产生具有序列Zxy-Uvw-Pro的蛋白质，随后将Zxy酸从通过用亮氨酸氨基肽酶处理后者产生的蛋白质。

8. 发明授权

US3987159A Stable sensitized erythrocytes and preparation means 失效
标题翻译：稳定的致敏物质和制备方法
公开(公告)号：US3987159A
公开(公告)日：1976-10-19
申请号：US447205
申请日：1974-03-01
申请人： Jurgen Spona , Michael Topert
发明人： Jurgen Spona , Michael Topert
IPC分类号： G01N33/556 , G01N33/555 , A61K35/12 , G01N1/00 , G01N31/00 , G01N33/16
CPC分类号： G01N33/555 , Y10S436/814 , Y10S436/817 , Y10S436/818 , Y10S436/826
摘要： Stable preparations of sensitized erythrocytes are provided by simultaneously admixing washed erythrocytes in a buffered aqueous solution of glutaraldehyde, antigen or antigen-protein conjugate and formaldehyde. After washing, the separated sensitized erythrocytes can be lyophilized and thereby become stable at room temperature.

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