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21. 发明授权

US4447360A Intermediates for thia-aza compounds with a .beta.-lactam ring 失效
标题翻译：具有β-内酰胺环的噻唑化合物的中间体
公开(公告)号：US4447360A
公开(公告)日：1984-05-08
申请号：US214316
申请日：1980-12-08
申请人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
发明人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
IPC分类号： C07D499/897 , C07D205/08 , C07D205/09 , C07D499/04 , C07D499/06 , C07D499/86 , C07D499/87 , C07D499/88 , C07F9/568 , C07D401/12 , C07D405/12 , C07D409/12
CPC分类号： C07F9/5683 , C07D205/09 , C07D499/88
摘要： 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group,1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.
摘要翻译：其中R 1表示氢，通过碳原子键合到环碳原子上的有机基团或醚化的巯基，R 2表示羟基或基团R 2 A的2-蒎烯-3-羧酸化合物与羰基-C（= O） - 被保护的羧基，其1-氧化物以及具有成盐基团的化合物的盐以外消旋和旋光形式一起形成，其制备方法，药物组合物含有这些化合物及其作为抗生素的用途，以及可用于制备式I化合物的中间体及其方法。

22. 发明授权

US4364865A Bicyclic unsaturated thia-aza compounds and 4-acylthio azetidinone intermediates 失效
标题翻译：双环不饱和硫杂氮杂环化合物和4-酰硫基氮杂环丁酮中间体
公开(公告)号：US4364865A
公开(公告)日：1982-12-21
申请号：US158430
申请日：1980-06-11
申请人： Ivan Ernest , Jacques Gosteli , Robert B. Woodward
发明人： Ivan Ernest , Jacques Gosteli , Robert B. Woodward
IPC分类号： C07D205/095 , C07D499/88 , C07F9/568 , C07D205/08
CPC分类号： C07D205/095 , C07D499/88 , C07F9/5683 , Y02P20/55
摘要： The invention relates to 6-amino-2-penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1.sup.a denotes hydrogen or an amino protective group R.sub.1.sup.A and R.sub.1.sup.b represents hydrogen or an acyl radical Ac, or in which R.sub.1.sup.a and R.sub.1.sup.b conjointly form a bivalent amino protective group, R.sub.2 denotes hydroxyl or a radical R.sub.2.sup.A which, together with the carbonyl grouping --C(.dbd.O)--, forms a protected carboxyl group, and R.sub.3 represents hydrogen or an organic radical which is linked via a carbon atom to the ring carbon atom, and 1-oxides thereof, as well as salts of such compounds having salt-forming groups, which compounds possess antibiotic properties, processes for the manufacture of such compounds, and also pharmaceutical formulations containing compounds of the formula I with pharmacological properties, and the use thereof, either as antibiotics, preferably in the form of pharmaceutical formulations, or as intermediate products.
摘要翻译：本发明涉及式（I）的6-氨基-2-青霉烯-3-羧酸化合物，其中R 1a表示氢或氨基保护基R 1A和R 1b表示氢或酰基Ac，或其中 R1a和R1b共同形成二价氨基保护基，R2表示羟基或基团R2A，其与羰基-C（= O） - 一起形成被保护的羧基，R 3表示氢或连接的有机基团通过碳原子与环碳原子及其1-氧化物，以及具有成盐基团的化合物的盐，该化合物具有抗生素性质，制备这些化合物的方法，以及含有化合物的化合物的药物制剂具有药理学性质的式I及其用途，优选为药物制剂形式的抗生素或作为中间产物。

23. 发明授权

US4165268A Process for the production of substituted toluene compounds 失效
标题翻译：生产取代甲苯化合物的方法
公开(公告)号：US4165268A
公开(公告)日：1979-08-21
申请号：US846876
申请日：1977-10-31
申请人： Franz Marti , Tibor Somlo , Jacques Gosteli
发明人： Franz Marti , Tibor Somlo , Jacques Gosteli
IPC分类号： C07B39/00 , C07C17/14 , C07C205/11 , C07C121/52
CPC分类号： C07C205/11 , C07B39/00 , C07C17/14
摘要： A process for the production of benzal bromides which contain an electrophilic substituent in the ortho- and/or para-position of the formula (Ia), or of mixtures thereof with the corresponding benzyl bromides of the formula (Ib), ##STR1## IN WHICH R represents an electrophilic substituent in the ortho- and/or para position, by treating correspondingly substituted toluenes with elementary bromine under irradiation with visible light in a two-phase system which consists of an aqueous and an organic phase, which process comprises carrying out the reaction in the presence of a base.
摘要翻译：制备在式（Ia）的邻位和/或对位含有亲电子取代基的苄基溴的方法，或其与式（Ib）的相应的苄基溴，（IMA）（Ib）其中R表示邻位和/或对位的亲电子取代基，通过在两相体系中用可见光照射下用基本溴处理相应的取代的甲苯，该两相体系由水和有机相，该方法包括在碱的存在下进行反应。

24. 发明授权

US4020098A Process for the preparation of 5-substituted resorcinols and related intermediates 失效
标题翻译： 5-取代的间苯二酚和相关中间体的制备方法
公开(公告)号：US4020098A
公开(公告)日：1977-04-26
申请号：US594412
申请日：1975-07-09
申请人： Jacques Gosteli
发明人： Jacques Gosteli
IPC分类号： C07C37/50 , C07C39/08 , C07C69/76
CPC分类号： C07C37/50 , C07C67/343 , C07C69/88 , C07C69/94
摘要： According to the present invention, 5-substituted resorcinols of the formula I ##STR1## wherein R.sub.1 represents a hydrocarbon radical, optionally unsubstituted or substituted by inert substituents, are prepared by reacting a carboxylic acid ester of the formula IIr.sub.1 -- c .tbd. c -- co -- o -- r.sub.2 (ii)wherein R.sub.2 represents a non-aromatically bound lower hydrocarbon radical, in the presence of an alkaline condensation agent, with a diester of 3-oxoglutaric acid of the formula IIIr.sub.3 --o--co--ch.sub.2 --co--ch.sub.2 --co--o--r.sub.4 (iii)wherein R.sub.3 and R.sub.4 represent non-aromatically bound lower hydrocarbon radicals; hydrolyzing the resulting dihydroxyisophthalic acid acid ester of the formula IV ##STR2## and decarboxylating the hydrolyzed product, a specific embodiment is the preparation of 5-pentylresorcinol.
摘要翻译：根据本发明，式I的5-取代间苯二酚（I）其中R 1表示任选未取代或被惰性取代基取代的烃基，其通过使式II的羧酸酯R 1 -C 其中R 2表示非芳香结合的低级烃基，在碱性缩合剂的存在下，与式III的3-氧代戊二酸的二酯R 3 -O-CO- CH2-CO-CH2-CO-O-R4（Ⅲ）其中R3和R4代表非芳香结合的低级烃基; 水解所得的式IV（IV）的二羟基间苯二酸酸酯并使水解产物脱羧，具体实施方案是5-戊基间苯二酚的制备。

25. 发明授权

US5484939A 2-substituted 5-chlorimidazoles 失效
标题翻译： 2-取代的5-氯咪唑
公开(公告)号：US5484939A
公开(公告)日：1996-01-16
申请号：US208956
申请日：1994-03-11
申请人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
发明人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
IPC分类号： C07D233/68 , C07D233/08
CPC分类号： C07D233/68
摘要： The 2-substituted 5-chlorimidazoles of general formula: ##STR1## are new intermediate products for the production of antihypertensive pharmaceutical agents or of herbicidal compounds. A process for the production of these intermediate products as well as a new process for the further reaction of 2-substituted 5-chlorimidazoles of general formula I, wherein R.sub.1 is hydrogen, to the 2-substituted 5-chlorimidazole-4-carbaldehydes of general formula: ##STR2##
摘要翻译： 2-取代的5-氯咪唑，其通式如下：图1是生产抗高血压药剂或除草化合物的新中间产物。制备这些中间体产物的方法以及通式I的其它R 1为氢的2-取代的5-氯咪唑与2-取代的5-取代的5-氯咪唑-4-碳醛进一步反应的新方法公式： II

26. 发明授权

US5442075A Process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes 失效
标题翻译： 2-取代的5-氯咪唑-4-碳醛的制备方法
公开(公告)号：US5442075A
公开(公告)日：1995-08-15
申请号：US208955
申请日：1994-03-11
申请人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
发明人： Gareth Griffiths , Rene Imwinkelried , Jacques Gosteli
IPC分类号： C07D233/68 , C07D233/70 , C07D233/96
CPC分类号： C07D233/68 , C07D233/70
摘要： A process for the production of 2-substituted 5-chlorimidazole-4-carbaldehydes of the general formula: ##STR1## wherein R is hydrogen, an alkyl group, and alkenyl group, a cycloalkyl group, a benzyl group, a phenyl group or an aryl group. These compounds form important intermediate products for the production of antihypertensive pharmaceutical agents or herbicidal compounds.
摘要翻译：制备以下通式的2-取代的5-氯咪唑-4-碳醛的方法：其中R是氢，烷基和烯基，环烷基，苄基，苯基或芳基。这些化合物形成用于生产抗高血压药剂或除草化合物的重要中间产物。

27. 发明授权

US4965359A Process for the production of 4,5,6,7-tetrahydrothieno-[3,2-C]-pyridines 失效
标题翻译：制备4,5,6,7-四氢噻吩并[3,2-C] - 吡啶的方法
公开(公告)号：US4965359A
公开(公告)日：1990-10-23
申请号：US409743
申请日：1989-09-20
申请人： Jacques Gosteli , Aleksander Warm
发明人： Jacques Gosteli , Aleksander Warm
IPC分类号： C07D211/44 , C07D211/74 , C07D495/04 , C07D513/04
CPC分类号： C07D513/04 , C07D211/74
摘要： A process for the production of 4,5,6,7-tetrahydrothieno-[3,2-c]-pyridines of the formula: ##STR1## Thus, in the case of a 4-oxo-3-piperidine-3-carboxylic acid ester of the formula: ##STR2## an allyl group is introduced in the 3 position, the ester function in the 3 position is removed, the resultant compound of the formula: ##STR3## is ionized, reduced to the corresponding aldehyde of the formula: ##STR4## and with H.sub.2 S/HCl in the presence of a metal halide is cyclized to the end product. The synthesized compounds have antithrombotic action.
摘要翻译：制备下式的4,5,6,7-四氢噻吩并[3,2-c] - 吡啶的方法：因此，在4-氧代-3-哌啶-3-甲酸将下式的酸酯引入3位，除去3位的酯官能团，将所得的下式化合物离子化，还原成相应的式：在金属卤化物的存在下，使用H 2 S / HCl环化至最终产物。合成的化合物具有抗血栓作用。

28. 发明授权

US4831084A Resin-linker combination for the solid-phase synthesis of peptides and intermediates 失效
标题翻译：用于肽和中间体的固相合成的树脂 - 连接体组合
公开(公告)号：US4831084A
公开(公告)日：1989-05-16
申请号：US189294
申请日：1988-05-02
申请人： Monika Mergler , Jacques Gosteli , Peter Grogg
发明人： Monika Mergler , Jacques Gosteli , Peter Grogg
IPC分类号： C07C43/23 , C07C215/78 , C07C323/20 , C07K1/04 , C07K1/113 , C07K17/08 , C08F8/00 , C08F8/26
CPC分类号： C08F8/00 , C07K1/042 , C08F8/26 , C08F8/30 , C08F2800/20 , Y10S530/815
摘要： The present invention relates to a novel polymeric carrier, a process for its production and its use for the preparation of peptides and their intermediates. The process comprises reacting chloromethylated polystyrene (cross-linked with divinylbenzene) with a 4-hydroxy-2-substituted-benzyl alcohol (linker), attaching .alpha.-amino acids with amino and side-chain protection to the carrier thus obtained, and building up a peptide according to the method known in the field of solid phase peptide synthesis (SPPS). The method allows removal of intermediates or final products under extremely mild acidic conditions giving products in high state of purity and yield. The 2-substituent consists of an electron donating group, such as methoxy.
摘要翻译：本发明涉及一种新的聚合物载体，其制备方法及其用于制备肽及其中间体的方法。该方法包括使氯甲基化聚苯乙烯（与二乙烯基苯交联）与4-羟基-2-取代的苯甲醇（接头）反应，将α-氨基酸与氨基和侧链保护连接到由此获得的载体上，并建立根据固相肽合成领域已知的方法（SPPS）的肽。该方法允许在非常温和的酸性条件下除去中间体或最终产物，产生高纯度和高产率的产物。 2-取代基由给电子基团组成，例如甲氧基。

29. 发明授权

US4331676A Thia-aza compounds with a .beta.-lactam ring 失效
公开(公告)号：US4331676A
公开(公告)日：1982-05-25
申请号：US902639
申请日：1978-05-04
申请人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
发明人： Jacques Gosteli , Ivan Ernest , Robert B. Woodward
IPC分类号： C07D499/897 , C07D205/08 , C07D205/09 , C07D499/04 , C07D499/06 , C07D499/86 , C07D499/87 , C07D499/88 , C07F9/568 , C07D499/00
CPC分类号： C07F9/5683 , C07D205/09 , C07D499/88
摘要： 2-Penem-3-carboxylic acid compounds of the formula ##STR1## in which R.sub.1 represents hydrogen, an organic radical bonded by a carbon atom to the ring carbon atom or an etherified mercapto group andR.sub.2 represents hydroxy or a radical R.sub.2.sup.A forming together with the carbonyl grouping --C(.dbd.O)-- a protected carboxyl group, 1-oxides thereof, as well as salts of such compounds having salt-forming groups, in racemic and optically active form, processes for their preparation, pharmaceutical compositions containing such compounds, and their use as antibiotics, and intermediates and their processes which are useful in the production of the compounds of the formula I.

30. 发明授权

US4260779A Oxothia compounds 失效
标题翻译： Oxothia化合物
公开(公告)号：US4260779A
公开(公告)日：1981-04-07
申请号：US92821
申请日：1979-11-09
申请人： Raymond Bernasconi , Pier G. Ferrini , Richard Goschke , Jacques Gosteli
发明人： Raymond Bernasconi , Pier G. Ferrini , Richard Goschke , Jacques Gosteli
IPC分类号： C07D333/64 , C07D333/68 , C07D333/70
CPC分类号： C07D333/68 , C07D333/64 , C07D333/70 , Y10S514/822
摘要： Oxothia compounds, especially 2-oxo-2,3-dihydro-benzo[b]thiophene compounds of the formula ##STR1## in which Ph represents an optionally substituted 1,2-phenylene radical, X represents oxygen or sulphur, R.sub.1 represents an organic radical bonded via a carbon atom and R.sub.2 denotes hydrogen or an optionally substituted hydrocarbon radical of aliphatic character, and their salts are useful as peripheral analgetics and/or as antiphlogistic uricosuric and/or thrombolytic agents.
摘要翻译：其中Ph代表任选取代的1,2-亚苯基，X表示氧或硫，R 1，R 2，R 3，R 4，R 4，R 4，表示通过碳原子键合的有机基团，R 2表示氢或任选取代的脂肪族特征的烃基，其盐可用作外周止痛剂和/或作为消炎性尿酸和/或溶栓剂。

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