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1. 发明授权

US5095006A Renin inhibitors having all retro-inverted peptide bonds 失效
标题翻译：具有所有逆转肽基因的RENIN抑制剂
公开(公告)号：US5095006A
公开(公告)日：1992-03-10
申请号：US553493
申请日：1990-07-13
申请人： Wolfgang Bender , Gunther Kinast , Andreas Knorr , Johannes-Peter Stasch
发明人： Wolfgang Bender , Gunther Kinast , Andreas Knorr , Johannes-Peter Stasch
IPC分类号： A61K31/19 , A61K31/215 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C229/22 , C07C229/34 , C07C237/22 , C07C271/22 , C07C311/19 , C07D207/08 , C07D209/48 , C07D233/54 , C07D233/64 , C07D263/22 , C07D263/26 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K14/81
CPC分类号： C07D209/48 , C07C229/34 , C07C271/22 , C07C311/19 , C07D207/08 , C07D233/64 , C07D263/26 , C07K5/0205 , C07K5/06147 , A61K38/00 , C07C2101/14
摘要： Renin-inhibiting peptides of the formula ##STR1## in which X represents a group of the formula ##STR2## represents hydroxyl, alkoxy having up to 8 carbon atoms, benzyloxy or a group of the formula --NR.sup.4 R.sup.5,A, B, D and E are identical or different and in each caserepresent a direct bond,represent a radical of the formula ##STR3## in which Q1 denotes oxygen, sulphur or the methylene grouprepresent a grouping of the formula ##STR4## m represents a number 0, 1 or 2, and L represents a group of the formula --CH.sub.2 NR.sup.2 R.sup.3and physiologically acceptable salts thereof.
摘要翻译：式（I）的肾素抑制肽，其中X表示下式的基团：表示羟基，具有至多8个碳原子的烷氧基，苄氧基或式-NR4R5基团，A ，B，D和E相同或不同，并且在每种情况下代表直接键，表示式为“IMAGE”的基团，其中Q1表示氧，硫或亚甲基表示下式的基团：m表示数字0,1或2，L表示式-CH2NR2R3的基团及其生理上可接受的盐。

2. 发明授权

US5242903A Renin inhibitors 失效
标题翻译：肾素抑制剂
公开(公告)号：US5242903A
公开(公告)日：1993-09-07
申请号：US771077
申请日：1991-10-02
申请人： Wolfgang Bender , Gunther Kinast , Andreas Knorr , Johannes-Peter Stasch
发明人： Wolfgang Bender , Gunther Kinast , Andreas Knorr , Johannes-Peter Stasch
IPC分类号： A61K38/00 , C07C229/34 , C07C271/22 , C07C311/19 , C07D207/08 , C07D209/48 , C07D233/54 , C07D263/26 , C07K5/02 , C07K5/078
CPC分类号： C07D209/48 , C07C229/34 , C07C271/22 , C07C311/19 , C07D207/08 , C07D233/54 , C07D233/64 , C07D263/26 , C07K5/0205 , C07K5/06147 , A61K38/00 , C07C2101/14
摘要： Renin-inhibiting peptides of the formula ##STR1## in which X represents a group of the formula ##STR2## represents hydroxyl, alkoxy having up to 8 carbon atoms, benzyloxy or a group of the formula --NR.sup.4 R.sup.5,A, B, D and E are identical or different and in each caserepresent a direct bond,represent a radical of the formula ##STR3## in which Z denotes oxygen, sulphur or the methylene grouprepresents a grouping of the formula ##STR4## m represents a number 0, 1 or 2, and L represents a group of the formula --CH.sub.2 --NR2R.sub.3and physiologically acceptable salts thereof.
摘要翻译：式（I）的肾素抑制肽，其中X表示下式的基团：表示羟基，具有至多8个碳原子的烷氧基，苄氧基或式-NR4R5基团，A ，B，D和E相同或不同，并且在每种情况下都代表直接键，表示式为“IMAGE”的基团，其中Z表示氧，硫或亚甲基表示下式的基团：m表示数字0,1或2，L表示式-CH 2 -NR 2 R 3的基团及其生理上可接受的盐。

3. 发明授权

US4808622A Circulation active methionine-substituted 1,4-dihydropyridines 失效
标题翻译：循环活性甲硫氨酸取代的1,4-二氢吡啶类
公开(公告)号：US4808622A
公开(公告)日：1989-02-28
申请号：US1496
申请日：1987-01-07
申请人： Gunther Kinast , Eckhard Schwenner , Stanislav Kazda , Andreas Knorr , Michael Kayser
发明人： Gunther Kinast , Eckhard Schwenner , Stanislav Kazda , Andreas Knorr , Michael Kayser
IPC分类号： A61K31/455 , A61P9/10 , A61P9/12 , C07D211/90 , C07D413/04 , C07D211/86
CPC分类号： C07D413/04 , C07D211/90
摘要： Circulation active, e.g. antihypertensive novel methionine-substituted dihydropyridines of the formula ##STR1## in which R.sup.1 is phenyl or a heterocyclic radical, or a physiologically acceptable salt thereof.
摘要翻译：循环活跃，例如其中R1是苯基或杂环基的式“IMAGE”的抗高血压新型甲硫氨酸取代的二氢吡啶或其生理上可接受的盐。

4. 发明授权

US4626535A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4626535A
公开(公告)日：1986-12-02
申请号：US566975
申请日：1983-12-30
申请人： Rolf Angerbauer , Michael Boberg , Gunther Kinast , Karl G. Metzger , Wilfried Schrock , Hans-Joachim Zeiler
发明人： Rolf Angerbauer , Michael Boberg , Gunther Kinast , Karl G. Metzger , Wilfried Schrock , Hans-Joachim Zeiler
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D285/08 , C07D417/06 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/59 , C07D501/38
CPC分类号： C07D285/08 , C07D417/06
摘要： Novel antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes hydrogen, optionally substituted alkyl, a substituted or unsubstituted phenyl ring, a polycyclic aromatic ring or an optionally substituted heterocyclic 5- or 6-member ring having 1-4 heteroatoms,R.sup.2 represents hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkenyl, halogen, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, hydroxymethyl, formyloxymethyl, C.sub.1 -C.sub.4 -alkylcarbonyloxymethyl, aminocarbonyloxymethyl, pyridiniummethyl, 4-carbamoylpyridiniummethyl, 4-sulphonylethylpyridiniummethyl, 4-carboxylmethylpyridiniummethyl or heterocyclylthiomethyl, heterocyclyl representing a radical of the formula ##STR2## wherein R.sup.8 denotes hydrogen, methyl, 2-dimethylaminoethyl, carboxymethyl, sulphomethyl, carboxyethyl or sulphoethyl andR.sup.9 denotes hydrogen or methyl,or pharmaceutically tolerated salts or esters thereof.
摘要翻译：式中，R1表示氢，任选取代的烷基，取代或未取代的苯基环，多环芳环或具有1-4个杂原子的任选取代的杂环的5-或6-元环的新型抗菌活性头孢菌素，R2 表示氢，C 1 -C 4 - 烷基，C 1 -C 4 - 烯基，卤素，C 1 -C 4 - 烷氧基，C 1 -C 4 - 烷硫基，羟甲基，甲酰氧基甲基，C 1 -C 4 - 烷基羰氧基甲基，氨基羰基氧基甲基，吡啶鎓甲基，4-氨基甲酰基吡啶鎓甲基，4-磺基乙基吡啶鎓甲基，4-羧基甲基吡啶鎓甲基或杂环硫基甲基，代表下式基团的杂环基，其中R8表示氢，甲基，2-二甲基氨基乙基，羧甲基，磺基甲基，羧乙基或磺基，R9表示氢或甲基，或其药学上可耐受的盐或酯。

5. 发明授权

US4348402A 2-Hydroxyalkyl-3,4,5-trihydroxy-piperidine compounds, their production and their medicinal use 失效
标题翻译： 2-羟基烷基-3,4,5-三羟基 - 哌啶化合物，其生产及其药用
公开(公告)号：US4348402A
公开(公告)日：1982-09-07
申请号：US193498
申请日：1980-10-02
申请人： Gunther Kinast , Lutz Muller , Rudiger Sitt , Walter Puls
发明人： Gunther Kinast , Lutz Muller , Rudiger Sitt , Walter Puls
IPC分类号： A61K31/445 , A61K31/70 , A61K31/7028 , A61P1/00 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/12 , A61P43/00 , C07D211/46 , C07D498/04 , C07H7/02 , C07H9/04 , C07H13/08 , C07H15/12 , C07H15/18 , C07D211/42
CPC分类号： C07H9/04 , C07D211/46 , C07H7/02 , Y10S514/824 , Y10S514/835 , Y10S514/866
摘要： The invention relates to .alpha.-hydroxyalkyl-3,4,5-trihydroxypiperidines defined by Formula (I), infra, and pharmaceutical compositions and medicaments containing said compounds. Also included in the invention are methods for the use of said compounds, compositions and medicaments as inhibitors of .alpha.-glucoside hydrolases; and intermediates for the compounds of said Formula (I).
摘要翻译：本发明涉及由下式（I）定义的α-羟基烷基-3,4,5-三羟基哌啶以及含有所述化合物的药物组合物和药物。本发明还包括使用所述化合物，组合物和药物作为α-葡糖苷水解酶抑制剂的方法; 和所述式（I）的化合物的中间体。

6. 发明授权

US4500716A Intermediate products for the preparation of Z-cephalosporins 失效
标题翻译：用于制备Z-头孢菌素的中间产物
公开(公告)号：US4500716A
公开(公告)日：1985-02-19
申请号：US438189
申请日：1982-11-01
申请人： Gunther Kinast
发明人： Gunther Kinast
IPC分类号： C07D277/28 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/40 , C07D277/46 , C07D277/48 , C07D417/12 , C07D417/14 , C07D501/04 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/38 , C07F7/10
CPC分类号： C07D277/20
摘要： Highly active substantially pure Z-isomers of cephalosporins are produced by the following synthesis: ##STR1## in which R.sup.1, R.sup.4 and R.sup.5 ae various organic radicals,R.sup.2 is alkoxycarbonyl,Y is Cl, Br or --O--SO.sub.2 --R.sup.5, andX is a conventional cephalosporin substituent.Many of the intermediates are new, especially in pure Z-form.
摘要翻译：通过以下合成产生头孢菌素的高活性基本上纯的Z-异构体：其中R 1，R 3，R 3，R 3，R 3，R 3，R 3，R 3，，R4和R5a各种有机基团，R2是烷氧基羰基，Y是Cl，Br或-O-SO2-R5，X是常规的头孢菌素取代基。许多中间体是新的，特别是纯Z形式。

7. 发明授权

US4489076A Cephalosporins 失效
标题翻译：头孢菌素
公开(公告)号：US4489076A
公开(公告)日：1984-12-18
申请号：US542833
申请日：1983-10-17
申请人： Gunther Kinast , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
发明人： Gunther Kinast , Michael Boberg , Karl G. Metzger , Hans-Joachim Zeiler
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/46 , C07D501/38
CPC分类号： C07D277/20
摘要： Antibacterially active cephalosporins of the formula ##STR1## in which R.sup.1 denotes C.sub.1 -C.sub.6 -alkyl, phenyl or halogen-substituted phenyl, andR.sup.2 and R.sup.3, which can be identical or different, denote H, C.sub.1 -C.sub.4 -alkyl, chlorine, bromine, carbamoyl or N-C.sub.1 -C.sub.4 -alkylcarbamoyl.
摘要翻译：其中R 1表示C 1 -C 6 - 烷基，苯基或卤素取代的苯基，R 2和R 3可以相同或不同，表示H，C 1 -C 4 - 烷基，氯，溴的化学式为“IMAGE”的抗菌活性头孢菌素，氨基甲酰基或N-C 1 -C 4 - 烷基氨基甲酰基。

8. 发明授权

US4871747A 3-Amino-4,5-dihydroxypiperidines, process for their preparation and their use 失效
标题翻译： 3-氨基-4,5-二羟基哌啶，其制备及其用途
公开(公告)号：US4871747A
公开(公告)日：1989-10-03
申请号：US937645
申请日：1986-12-03
申请人： Gunther Kinast , Matthias Schuller , Theo Schroder
发明人： Gunther Kinast , Matthias Schuller , Theo Schroder
IPC分类号： C07D211/46 , C07D211/56 , C07D491/04 , C07D491/056 , C07H13/04 , C07H13/12
CPC分类号： C07D491/04 , C07D211/46 , C07D211/56 , C07H13/04 , C07H13/12
摘要： A 3-amino-4,5-dihydroxy-piperidine compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, alkyl having up to 8 carbon atoms, aralkyl having 7 to 14 carbon atoms, or represents a group of the formula ##STR2## R.sup.4 denotes straight-chain or branched alkyl having up to 8 carbon atoms, straight-chain or branched alkoxy having up to 8 carbon atoms, or aralkoxy having up to 10 carbon atoms, andR.sup.2 and R.sup.3 represent hydrogen or represent the group NHR.sup.5,R.sup.5 having the same meaning as R.sup.1 and being identical to or different from the latter,with the proviso that, in every case, one substituent of R.sup.2 or R.sup.3 represents hydrogen and the other substituent of R.sup.2 or R.sup.3 represents NHR.sup.5, and physiologically acceptable salts thereof. Such compound is useful to treat prediabetes, gastritis, constipation, caries, atherosclerosis, obesity, diabetes and hyperlipoproteinaemia.
摘要翻译：式（I）的3-氨基-4,5-二羟基 - 哌啶化合物其中R 1表示氢，具有至多8个碳原子的烷基，具有7-14个碳原子的芳烷基，或表示式的基团R4表示具有至多8个碳原子的直链或支链烷基，具有至多8个碳原子的直链或支链烷氧基或具有至多10个碳原子的芳烷氧基，R2和R3表示氢或代表NHR5基团，R 5具有与R 1相同的含义并且与后者相同或不同，条件是在每种情况下，R 2或R 3的一个取代基表示氢，R 2或R 3的其它取代基表示NHR 5 ，及其生理上可接受的盐。这种化合物可用于治疗糖尿病前期，胃炎，便秘，龋齿，动脉粥样硬化，肥胖，糖尿病和高脂蛋白血症。

9. 发明授权

US4754031A Preparation of cephalosporins 失效
标题翻译：头孢菌素的制备
公开(公告)号：US4754031A
公开(公告)日：1988-06-28
申请号：US731248
申请日：1985-05-06
申请人： Rolf Angerbauer , Gunther Kinast
发明人： Rolf Angerbauer , Gunther Kinast
IPC分类号： C07D501/06 , A61K31/545 , C07D20060101 , C07D417/00 , C07D417/12 , C07D417/14 , C07D501/04 , C07D501/22 , C07D501/46
CPC分类号： C07D501/46
摘要： A process for the preparation of a cephalosporin of the formula ##STR1## in which R.sup.1 is an aliphatic or cycloaliphatic radical with up to 6 carbon atoms, andA is a pyridinium radical or a radical of the formula ##STR2## comprising reacting an acid of the formula ##STR3## with methanesulphonyl chloride to form an anhydride of the formula ##STR4## and reacting the anhydride with a 7-aminocephalosporanate of the formula ##STR5## The reaction proceeds smoothly and in high yield.
摘要翻译：制备式“IMAGE”的头孢菌素的方法，其中R 1是具有至多6个碳原子的脂族或脂环族基团，A是吡啶鎓基团或下式的基团，其包括使式“IMAGE”与甲磺酰氯反应以形成下式的酐，并使酸酐与下式的7-氨基头孢烷酸酯反应。反应顺利进行并以高产率进行。

10. 发明授权

US4266025A Production of N-substituted derivatives of 1-desoxy-nojirimycin 失效
标题翻译： 1-脱氧 - nojirimycin的N-取代衍生物的制备
公开(公告)号：US4266025A
公开(公告)日：1981-05-05
申请号：US97099
申请日：1979-11-23
申请人： Gunther Kinast , Michael Schedel
发明人： Gunther Kinast , Michael Schedel
IPC分类号： C12P17/12 , C07C271/16 , C07D211/46 , C07H13/12 , C12P19/26 , C12P19/44 , C12R1/01 , C12R1/15 , C12R1/645
CPC分类号： C07H13/12 , C07C271/16 , C07D211/46 , C12P19/26
摘要： The invention relates to a process for the production of compounds of the formula ##STR1## in which R is hydrogen or optionally substituted alkyl, alkenyl, aralkyl or aryl, by microbiological transformation of ##STR2## follow by catalytic hydrogenation. The compounds obtained are useful for the treatment of diabetes, hyperlipoproteinaemia and adiposity which comprises aerobically cultivates, in the presence of an assimilable source of carbon nitrogen, at a temperature of 20.degree. to 45.degree. C. and pH between 2 and 10 and in the presence of an effective amount of a compound of the formula ##STR3## in which R has the above-given meaning and,R.sub.1 denotes an optionally substituted benzyl radical or an optionally substituted .beta.-alkenyl group,an aerobic microorganism or an extract of aerobic microorganism capable, in a nutrient medium containing a compound of the formula (X), or accumulating an amount of a compound of the formula ##STR4## in which R and R.sub.1 have the above-mentioned meanings andsubjecting the resulting compound of the general formula XI to catalytic hydrogenation.
摘要翻译：本发明涉及通过催化氢化随后的微生物转化制备式（I）化合物的方法，其中R是氢或任选取代的烷基，烯基，芳烷基或芳基。。所获得的化合物可用于治疗糖尿病，高脂蛋白血症和肥胖，其包括在可同化的碳氮源的存在下，在20°至45℃的温度和2至10之间的pH下进行有氧培养，并且在存在有效量的式（X）化合物，其中R具有上述含义，R 1表示任选取代的苄基或任选取代的β-链烯基，需氧微生物或提取物在含有式（X）化合物的营养培养基中，或者累积一定量的式（XI）化合物，其中R和R 1具有上述含义，并使所得的通式XI的化合物进行催化氢化。

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