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51. 发明授权

US4354023A Cefadroxil acetylcysteinate salt 失效
标题翻译：头孢羟氨苄乙酰半胱氨酸盐
公开(公告)号：US4354023A
公开(公告)日：1982-10-12
申请号：US240310
申请日：1981-03-04
申请人： Marco Falciani , Renato Broggi
发明人： Marco Falciani , Renato Broggi
IPC分类号： C07D501/22
CPC分类号： C07D501/22
摘要： Salts of cefadroxil with an amino acid selected from the group consisting of L-lysine, L-arginine and acetylcysteine. Said salts are obtained by reacting an aqueous suspension of cefadroxil with an aqueous solution of an amino acid or its derivative, selected from the group consisting of L-lysine, L-arginine and acetylcysteine. To isolate the salt, the aqueous solution is submitted to lyophilization.
摘要翻译：头孢羟氨苄与选自L-赖氨酸，L-精氨酸和乙酰半胱氨酸的氨基酸的盐。所述盐通过将头孢羟氨苄的水悬浮液与选自L-赖氨酸，L-精氨酸和乙酰半胱氨酸的氨基酸或其衍生物的水溶液反应而获得。为了分离盐，将水溶液冷冻干燥。

52. 发明授权

US4304717A Process for the preparation of reactive penicillanic acid and cephalosporanic acid derivatives 失效
标题翻译：反应性青霉烷酸和头孢烷酸衍生物的制备方法
公开(公告)号：US4304717A
公开(公告)日：1981-12-08
申请号：US36756
申请日：1979-05-07
申请人： Magda Huhn , Gabor Szabo , Gabor Resofszki , Eva Somfai
发明人： Magda Huhn , Gabor Szabo , Gabor Resofszki , Eva Somfai
IPC分类号： C07C69/353 , A61K31/43 , A61K31/545 , A61K31/546 , A61P31/04 , C07D333/24 , C07D499/00 , C07D499/12 , C07D499/72 , C07D501/06 , C07D501/20 , C07D501/22 , C07D501/26 , C07D501/28 , C07D501/32 , C07D501/34 , C07D501/60
CPC分类号： C07D499/00
摘要： This invention relates to a process for the preparation of acid amides having the formula (I) or their salts ##STR1## wherein R.sup.1 is hydrogen or an easily removable ester-forming or salt-forming group, preferably a trialkylamine, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group,R.sup.2 is hydrogen, alkyl group, alkenyl group, alkyl group having an aryl or heterocyclic (preferably furyl or thienyl) - substituent, an aryl group having an alkyl substituent (preferably xylyl), or an aryl, aralkyl or heterocyclic group (preferably a phenyl, thienyl, or furyl group) which can have one or more substituents,R.sup.3 is hydrogen, or substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, andX is a group of one of the formulae ##STR2## according to the invention an amine of the formula (II), ##STR3## wherein R.sup.4 is an easily removable ester-forming group, preferably a trialkylamino, trialkylsilyl, trichloroethyl, acetoxymethyl, phenacyl, substituted phenacyl, substituted phenyl or benzyl group, or a salt formed preferably with an alkali metal or a trialkylamine, is acylated with an ester of the formula (III), ##STR4## wherein R.sup.5 is a substituted or unsubstituted aryl, alkyl, cycloalkyl or aralkyl group, and, if desired, substituents R.sup.4 and/or R.sup.5 of the obtained product can be split off, and/or, if desired, the obtained product is converted into its salt or a salt is converted into the free acid.
摘要翻译：本发明涉及一种制备具有式（I）的酸酰胺或其盐（Ⅰ）的方法，其中R1是氢或易于除去的形成酯或成盐基团，优选三烷基胺，三烷基甲硅烷基，三氯乙基，乙酰氧基甲基，苯甲酰甲基，取代的苯甲酰甲基，取代的苯基或苄基，R2是氢，烷基，烯基，具有芳基或杂环（优选呋喃基或噻吩基） - 取代基的烷基，具有烷基取代基的芳基二甲苯基）或可具有一个或多个取代基的芳基，芳烷基或杂环基（优选苯基，噻吩基或呋喃基），R 3为氢或取代或未取代的芳基，烷基，环烷基或芳烷基，X为根据本发明的一组式（IMAGE），式（II）的胺，其中R 4是易于除去的酯形成基团，优选三烷基氨基，三烷基甲硅烷基，三氯乙基，乙酰氧基乙基，苯甲酰甲基，取代的苯甲酰甲基，取代的苯基或苄基，或优选与碱金属或三烷基胺形成的盐，用式（III）的酯，其中R5是取代或未取代的芳基，烷基，环烷基或芳烷基，并且如果需要，所得产物的取代基R 4和/或R 5可以被分离，和/或如果需要，将得到的产物转化为其盐或盐被转化进入游离酸。

53. 发明授权

US4299955A Process for preparing derivatives of 7-amino-desacetoxy cephalosporanic acid 失效
标题翻译：制备7-氨基去乙酸基头孢烷酸衍生物的方法
公开(公告)号：US4299955A
公开(公告)日：1981-11-10
申请号：US132761
申请日：1980-03-24
申请人： Marco Falciani , Renato Broggi
发明人： Marco Falciani , Renato Broggi
IPC分类号： A61K20060101 , A61K31/545 , C07D501/00 , C07D501/04 , C07D501/06 , C07D501/20 , C07D501/22
CPC分类号： C07D501/22
摘要： Process for preparing cephalexine monohydrate and cephadroxyl monohydrate, according to which a reaction is carried out of a mixed anhydride prepared from a Dane salt of phenylglycine or p-hydroxyphenyl-glycine with a chloroformiate, with an aqueous solution of 7-ADCA in a solvent selected from the group comprising dimethyl sulphoxide, dimethylacetamide, formamide, dimethylformamide and dioxane.
摘要翻译：制备头孢氨苄一水合物和甲肾上腺素一水合物的方法，根据该方法，将由苯基甘氨酸或对羟基苯基 - 甘氨酸的丹烷盐与氯甲酸酯制备的混合酸酐与选自下列溶剂的7-ADCA水溶液进行反应由二甲基亚砜，二甲基乙酰胺，甲酰胺，二甲基甲酰胺和二恶烷组成。

54. 发明授权

US4294827A Antibacterial and growth promoting .beta.-lactam antibiotics carrying an -ylidene-2-pyrrolidinon-1-yl radical 失效
标题翻译：携带亚基-2-吡咯烷酮-1-基的抗菌和生长促进β-内酰胺抗生素
公开(公告)号：US4294827A
公开(公告)日：1981-10-13
申请号：US862452
申请日：1977-12-20
申请人： Michael Preiss , Karl G. Metzger
发明人： Michael Preiss , Karl G. Metzger
IPC分类号： C07D499/66 , A61K31/40 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/535 , A61K31/54 , A61P31/04 , C07D207/36 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70 , C07D501/20 , A61K31/655 , C07D501/22 , C07D501/34
CPC分类号： C07D207/36 , C07D499/00
摘要： New .beta.-lactam antibiotics carrying a terminal -ylidene-2-pyrrolidinon-1-yl radical and of the formula ##STR1## in which A and A' represent hydrogen, optionally substituted alkyl, aryl or a group of the formula R.sub.1 --X'in whichX' denotes a --CO-- or --SO.sub.2 -- group andR.sub.1 denotes hydrogen, optionally substituted alkyl, aryl, thienyl, furyl, amino, monoalkylamino, dialkylamino, pyrrolidyl or piperidyl, it being furthermore possible for R.sub.1 to denote alkoxy if X' represents the --CO-- group;R represents H or OCH.sub.3B represents phenyl, methylphenyl, chlorophenyl, hydroxyphenyl, furyl or the radical ##STR2## X represents S, O, SO, SO.sub.2 or --CH.sub.2 --; and Y represents the group ##STR3## in which the carbon atom which carries the carboxyl group is bonded to the nitrogen atom of the .beta.-lactam ring and T denotes hydrogen, alkyl-CO-O, pyridinium, amino-pyridinium, carbamoyloxy, azido, cyano, hydroxyl, the group -S-phenyl, which can be substituted, or the group --S--Het, in whichHet represents an optionally substituted heterocyclic5-membered or 6-membered ring;or a salt thereof, exhibit antibacterial and animal growth promoting activity.
摘要翻译：带有末端亚烷基-2-吡咯烷酮-1-基和式（I）的新的β-内酰胺抗生素，其中A和A'代表氢，任选取代的烷基，芳基或式R1的基团 -X'，其中X'表示-CO-或-SO 2 - 基，R 1表示氢，任选取代的烷基，芳基，噻吩基，呋喃基，氨基，单烷基氨基，二烷基氨基，吡咯烷基或哌啶基，此外R1可以表示如果X'代表-CO-基团，则为烷氧基; R表示H或OCH 3 B表示苯基，甲基苯基，氯苯基，羟基苯基，呋喃基或基团X表示S，O，SO，SO 2或-CH 2 - ; Y代表携带羧基的碳原子与β-内酰胺环的氮原子键合的基团，T表示氢，烷基-CO-O，吡啶鎓，氨基 - 吡啶鎓，氨基甲酰氧基，叠氮基，氰基，羟基，可被取代的基团-S-苯基或基团-S-Het，其中Het表示任选取代的杂环5元或6元环; 或其盐表现出抗菌和动物生长促进活性。

55. 发明授权

US4284631A 7-Substituted cephem compounds and pharmaceutical antibacterial compositions containing them 失效
标题翻译： 7-取代的头孢烯化合物和含有它们的药物抗菌组合物
公开(公告)号：US4284631A
公开(公告)日：1981-08-18
申请号：US59893
申请日：1979-07-23
申请人： Takao Takaya , Hisashi Takasugi , Toshiyuki Chiba , Kiyoshi Tsuji
发明人： Takao Takaya , Hisashi Takasugi , Toshiyuki Chiba , Kiyoshi Tsuji
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D209/48 , C07D277/20 , C07D277/38 , C07D277/40 , C07D417/12 , C07D501/04 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/59
CPC分类号： C07D209/48 , C07D277/20 , C07D277/587
摘要： This invention relates to new cephem compounds. More particularly, it relates to new 7-substituted-3-cephem-4-carboxylic acid, its pharmaceutically acceptable salt and pharmaceutically acceptable bioprecursor thereof, which have antimicrobial activities, and processes for preparation thereof, to intermediate for preparing the same and processes for preparation thereof, and to pharmaceutical composition comprising the same and methods of using the same prophylactically and therapeutically for treatment of infectious diseases in human beings and animals.The cephem compounds of this invention include the compound represented by the formula (I): ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is lower alkyl substituted with a substituent selected from the groups consisting of cyano, carbamoyl, hydroxy, protected hydroxy, amino, protected amino, lower alkoxy, lower alkylthio, lower alkenylthio, aryl which may have one or more suitable substituent(s), and heterocyclic group which may have one or more suitable substituent(s),R.sup.3 is carboxy or protected carboxy, andR.sup.4 is hydrogen or halogen,and their pharmaceutically acceptable salts or pharmaceutically acceptable bioprecursors thereof.
摘要翻译：本发明涉及新的头孢烯化合物。更特别地，本发明涉及具有抗微生物活性的新的7-取代-3-头孢烯-4-羧酸，其药学上可接受的盐和药学上可接受的生物前体，及其制备方法，以及包含其的药物组合物以及在预防和治疗上用于治疗人类和动物中的感染性疾病的方法。本发明的头孢烯化合物包括由式（I）表示的化合物：其中R1是氨基或被保护的氨基，R2是被选自氰基，氨基甲酰基，羟基的取代基取代的低级烷基，保护的羟基，氨基，被保护的氨基，低级烷氧基，低级烷硫基，低级链烯硫基，可具有一个或多个合适取代基的芳基，以及可具有一个或多个合适取代基的杂环基，R 3是羧基或保护的羧基，R4是氢或卤素，以及它们的药学上可接受的盐或其药学上可接受的生物前体。

56. 发明授权

US4275062A Aminothiazolyl ureido sulfoxide cephalosporins 失效
标题翻译：氨基噻唑基脲基亚砜头孢菌素
公开(公告)号：US4275062A
公开(公告)日：1981-06-23
申请号：US77056
申请日：1979-09-19
申请人： Hermann Breuer , Theodore Denzel , Uwe D. Treuner
发明人： Hermann Breuer , Theodore Denzel , Uwe D. Treuner
IPC分类号： C07D501/22 , A61K20060101 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/46 , C07D501/57
CPC分类号： C07D501/20
摘要： Cephalosporins of the formula ##STR1## R represents hydrogen, sodium, potassium, or certain ester groups, R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy, X represents hydrogen ##STR2## R.sub.3 represents hydrogen or lower alkyl, R.sub.4 is hydrogen, lower alkyl, ##STR3## or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2, R.sub.5 represents hydrogen, sodium or potassium, and n represents an integer from 1 to 4. These compounds are useful as antibacterial agents.
摘要翻译：下式的头孢菌素R代表氢，钠，钾或某些酯基，R1是α构型，是氢或甲氧基，X代表氢。或低级烷基，R 4为氢，低级烷基，或 - （CH 2）n N-（低级烷基）2，R 5表示氢，钠或钾，n表示1〜4的整数。抗菌剂。

57. 发明授权

US4248868A Cephem carbonylmethyl derivatives 失效
公开(公告)号：US4248868A
公开(公告)日：1981-02-03
申请号：US14454
申请日：1979-02-23
申请人： Riccardo Scartazzini , Hans Bickel
发明人： Riccardo Scartazzini , Hans Bickel
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D501/04 , C07D501/06 , C07D501/14 , C07D501/16 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/26 , C07D501/60
CPC分类号： C07D501/04 , C07D501/14
摘要： The invention comprises carbonylmethyl derivatives of the formula IA and corresponding carbonylmethylene derivatives of the formula IB ##STR1## in which R.sub.1.sup.a represents a member of the group comrising hydrogen and an acyl radical of the formula AR.sub.a --C(R.sub.b)(R.sub.c)--C(.dbd.O)-- (A)in which R.sub.a represents a member of the group comprising optionally substituted phenyl, thienyl, furyl, cyclohexadienyl and cyclohexenyl, R.sub.b represents hydrogen and R.sub.c represents a member of the group comprising hydrogen, optionally protected hydroxyl, optionally protected amino and phenyl-lower protected sulpho, or in which R.sub.a represents a member of the group comprising cyano, optionally substituted phenoxy, pyridylthio, and tetrazolyl, and R.sub.b and R.sub.c each represent hydrogen, or in which R.sub.a represents a member of the group comprising phenyl, thienyl, furyl, and R.sub.b and R.sub.c together denote a member of the group comprising lower alkoxyimino, cycloalkoxyimino and phenyl-lower alkoxyimino in the syn-configuration, and such a group of the formula (A) contains at most one free amino group, R.sub.1.sup.b represents hydrogen, R.sub.2 represents a member of the group comprising hydroxyl, .alpha.-poly-branched lower alkoxy and 2-halogeno-lower alkoxy, which can easily be converted into the latter, and also phenacyloxy, 1-phenyl-lower alkoxy which has 1-3 phenyl radicals which are optionally substituted by lower alkoxy or nitro, lower alkanoyloxymethoxy, .alpha.-amino-lower alkanoyloxymethoxy, or 2-phthalidyloxy, and also tris-lower alkylsilyloxy, and R.sub.3 represents a member of the group comprising hydrogen, lower alkyl, cycloalkyl, phenyl which is optionally substituted by lower alkyl, lower alkoxy or halogen, phenyllower alkyl which is optionally substituted by nitro, lower alkyl, lower alkoxy or halogen, hydroxyl, etherified hydroxyl, especially lower alkoxy, above all methoxy, amino, lower alkylamino, di-lower alkylamino, lower alkyleneamino, oxa-lower alkylenamino, phenylamino, hydroxylamino, lower alkoxyamino, hydrazino, 2-lower alkylhydrazino, 2-phenylhydrazino, 4-lower alkylpiperazin-1-ylamino, lower alkylamino which is substituted by amino and/or carboxyl, and heterocyclylamino which is optionally substituted by lower alkyl, and wherein the heterocyclyl radical preferably contains 5-6 rings members and contains, as hetero-atoms, nitrogen, which is optionally also in the N-oxidized form, oxygen or sulphur and 1-oxides and salts of such compounds, which compounds are active against microorganisms, such as Gram-positive and Gram-negative bacteria, and pharmaceutical preparations containing these compounds.

58. 发明授权

US4243810A Pyridone-acetic acid derivative 失效
标题翻译：吡啶酮 - 乙酸衍生物
公开(公告)号：US4243810A
公开(公告)日：1981-01-06
申请号：US8893
申请日：1979-02-01
申请人： Rolf Gericke , Werner Rogalski , Rolf Bergmann , Walter Hameister , Helmut Wahlig
发明人： Rolf Gericke , Werner Rogalski , Rolf Bergmann , Walter Hameister , Helmut Wahlig
IPC分类号： A61K31/545 , C07D20060101 , C07D213/61 , C07D213/68 , C07D213/78 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/60
CPC分类号： A61K31/545 , C07D213/68 , C07D213/78 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/60 , C07D213/61
摘要： Novel pyridone-acetic acid derivative, viz. 3,5-dichloro-4-pyridone-1-acetic acid (I) is used as an intermediate in the production of certain cephem derivatives having anti-bacterial activity against gram-negative and gram-positive bacteria. The acid (I) is prepared by methods generally known in the art, e.g. by reacting 3,5-dichloro-4-pyridone with chloracetic acid or bromoacetic acid.
摘要翻译：新型吡啶酮 - 乙酸衍生物， 3,5-二氯-4-吡啶酮-1-乙酸（I）用作制备具有抗革兰氏阴性和革兰氏阳性菌抗细菌活性的某些头孢烯衍生物的中间体。酸（I）通过本领域通常已知的方法制备，例如，通过使3,5-二氯-4-吡啶酮与氯乙酸或溴乙酸反应。

59. 发明授权

US4200575A 7[(2-Thiazolyl)-2-(oxoimino)acetamido]cephalosporin derivatives 失效
标题翻译： 7 [（2-噻唑基）-2-（氧代亚氨基）乙酰氨基]头孢菌素衍生物
公开(公告)号：US4200575A
公开(公告)日：1980-04-29
申请号：US930041
申请日：1978-08-01
申请人： Mitsuo Numata , Tatsuo Nishimura
发明人： Mitsuo Numata , Tatsuo Nishimura
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46
CPC分类号： C07D501/20
摘要： Novel [2-(syn)-carbamoyloximinoacetamido]cephalosporins of the formula: ##STR1## [wherein, Y.sup.1 is hydrogen, hydroxyl, carbamoyloxy, acyloxy, quaternary ammonium or nitrogen-containing heterocyclic thio; R.sup.1 is alkyl, aralkyl or aryl; R.sup.2 is hydrogen or an ester residue; k is 0 or 1] and a salt thereof show strong antibacterial activities particularly against Gram-negative bacteria and they are useful as antibacterial agents.
摘要翻译：具有下式的新型[2-（顺式） - 氨基甲酰亚氨基乙酰胺基]头孢菌素其中Y1是氢，羟基，氨基甲酰氧基，酰氧基，季铵或含氮杂环硫基; R1是烷基，芳烷基或芳基; R2是氢或酯残基; k为0或1]，其盐对革兰氏阴性菌具有强的抗菌活性，可用作抗菌剂。

60. 发明授权

US4175076A Azetidinone mercury sulfides and process therefor 失效
标题翻译：氮杂环丁酮汞硫化物及其工艺
公开(公告)号：US4175076A
公开(公告)日：1979-11-20
申请号：US853064
申请日：1977-11-21
申请人： Lowell D. Hatfield
发明人： Lowell D. Hatfield
IPC分类号： C07D205/08 , C07D205/095 , C07D501/08 , C07D501/22 , C07F3/14
CPC分类号： C07F3/14 , Y02P20/55
摘要： Novel azetidinone mercury sulfides are prepared by the reaction of penicillin derived thiazolineazetidinones with a mercuric halide in the presence of an alcohol or glycol. They are useful intermediates in the preparation of cephalosporin compounds.
摘要翻译：通过青霉素衍生的噻唑啉氮杂环丁酮与卤化汞在醇或二醇的存在下反应制备新的氮杂环丁酮汞硫化物。它们是制备头孢菌素化合物的有用中间体。

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