子分类：
| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 181 | Chemical process | US967723 | 1997-11-07 | US5849907A | 1998-12-15 | Garfield Cecil Tughan |
| A process for the preparation of the antibacterial compound ##STR1## or a salt thereof which comprises hydrogenolysis of the novel compound of formula (II) ##STR2## and if necessary or desired isolating the resultant carboxylic acid as a salt thereof. | ||||||
| 182 | Process for making quinolonyl lactam antimicrobials and novel intermediate compounds | US968987 | 1997-11-12 | US5801242A | 1998-09-01 | Jared Lynn Randall; Jane Ellen Godlewski |
| The present invention provides processes for making compounds of the structure (Q--L.sup.1)--L--(L.sup.2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L.sup.1, and L.sup.2 together comprise a linking moiety; comprising the steps of: (1) coupling a compound of Formula (III) with a lactam-containing compound to form an intermediate compound; and (2) cyclizing the intermediate by reaction with an organosilicon compound to give a compound of the formula (Q--L.sup.1)--L--(L.sup.2 --B). Preferably, the process additionally comprises a step prior to the coupling step, wherein protected forms of the compound of Formula (III) and the lactam compound are formed; and deprotection steps after the cyclization step, wherein the protecting groups are removed. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem, a carbapenem, a cephem, or a carbacephem. Also preferred are those compounds where L.sup.1, L, and L.sup.2 form a carbamate moiety, or a secondary or tertiary amine moiety. The present invention also provides novel intermediate compounds of the formula (M--L.sup.1)--L--(L.sup.2 --B), where (I) M has a structure according to formula (IV) ##STR1## (II) B is a lactam moiety; and (III) L, L.sup.1, and L.sup.2 together comprise a linking moiety. | ||||||
| 183 | 2- (2-Substituted pyrrolidin-4-yl) thio-carbapenem derivatives | US818233 | 1997-03-14 | US5756765A | 1998-05-26 | Hyo Sung Kwak; Chong Ryul Lee; Sang Choon Lee; Hong Woo Lee; Hoi Choo Son; Eung Nam Kim; Kyeong Bok Min |
| The present invention relates to a mercaptopyrrolidinyl derivative of the following formula ##STR1## suitable for the preparation of carbapenem compounds. | ||||||
| 184 | Intermediates for pyrrolidylthiocarbapenem derivative | US574863 | 1995-12-19 | US5703243A | 1997-12-30 | Yasuhiro Nishitani; Tadashi Irie; Yutaka Nishino |
| A pyrrolidylthiocarbapenem derivative represented by Formula I is provided: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; R.sup.2, R.sup.3 and R.sup.4 are hydrogen, lower alkyl which can be substituted or an amino protecting group independently, or R.sup.2 and R.sup.3 together with a nitrogen atom to which R.sup.2 and R.sup.3 are bonded form a saturated or unsaturated cyclic group, or R.sup.2 and R.sup.4, or R.sup.3 and R.sup.4 together with two nitrogen atoms and one sulfur atom in the sufamide group form a saturated or unsaturated cyclic group; each cyclic group can further include at least one atom selected from the group consisting of oxygen, sulfur and nitrogen, and each cyclic group can be substituted; X.sup.1 is hydrogen or a hydroxy protecting group; X.sup.2 is hydrogen, a carboxy protecting group, an ammonio group, an alkali metal or an alkaline-earth metal; and Y.sup.2 is hydrogen or an amino protecting group. | ||||||
| 185 | 4-substituted azetidinones as precursors to 2-substituted-3-carboxy carbapenem antibiotics and a method of producing them | US420955 | 1995-04-12 | US5700930A | 1997-12-23 | Gregg Brian Feigelson; William V. Curran; Carl Bernard Ziegler |
| New 4-substituted azetidinones having the formulae I and II: ##STR1## wherein X is oxygen, sulfur or a moiety of the formula NR.sup.6 where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are defined hereafter, which are intermediates for the preparation of carbapenem and carbacephem antibacterials and processes for producing such antibacterials through the utilization of an acid mediated ring closure reaction. | ||||||
| 186 | 2-�1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-carbapenem derivatives | US631224 | 1996-04-12 | US5679790A | 1997-10-21 | Takao Abe; Takeshi Isoda; Chisato Sato; Ado Mihira; Satoshi Tamai; Toshio Kumagai |
| Novel carbapenem compounds, (1R,5S,6S)-2-�1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio-6-�(R)-1-hydroxyethyl!-1-methyl-carbapen-2-em-3-carboxyic acid derivatives. These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a �1-(1,3-thiazolin-2-yl)azetidin-3-yl!thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), and Y is carboxy, --COO.sup..crclbar. or protected carboxy. These compounds are useful antibiotics for prevention and treatment of bacterial infections. | ||||||
| 187 | Antibiotic compounds | US462037 | 1995-06-05 | US5652233A | 1997-07-29 | Michael John Betts; Gareth Morse Davies; Michael Lingard Swain |
| The present invention relates to carbapenems and provides a compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;R.sup.4 and R.sup.5 are the same or different and are selected from hydrogen, halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, C.sub.1-4 alkylaminosulphonyl, di-C.sub.1-4 -alkylaminosulphonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.1-4 alkanoylamino, C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino, C.sub.1-4 alkanesulphonamido and C.sub.1-4 alkylS(O)n- wherein n is zero, one or two:with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to --NR.sup.3 --. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. | ||||||
| 188 | Substituted 3-pyrrolidinylthio-carbapenems as antimicrobial agents | US302780 | 1994-09-21 | US5608056A | 1997-03-04 | Masayoshi Murata; Hideo Tsutsumi; Keiji Matsuda; Kohji Hattori; Takashi Nakajima |
| A compound of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,R.sup.2 is 1-hydroxyethyl,R.sup.3 is methyl,R.sup.4 is optionally substituted pyridyl(lower)alkyl, optionally N-substituted 2-oxopiperazin-1-yl-(lower)alkyl, optionally substituted imidazol-1-yl(C.sub.2 -C.sub.3)alkyl, optionally substituted imidazol-5-yl-(lower)alkyl, optionally substituted imidazol-2-yl-(lower)alkyl, optionally substituted pyrazol-4-(or 5-)yl(lower)alkyl, optionally substituted pyrazol-1-ylethyl, optionally substituted triazolyl(lower)alkyl, optionally substituted pyrimidinyl(lower)alkyl, optionally substituted dihydropyrimidinyl(lower)alkyl, or optionally substituted (2,3-dihydroimidazo-[1,2-b]pyrazol-1-yl)ethyl, andR.sup.5 is hydrogen or imino-protective group,and pharmaceutically acceptable salts thereof, which have antimicrobial activity. | ||||||
| 189 | Cephalosporin antibiotics | US415069 | 1995-03-29 | US5593986A | 1997-01-14 | Burton G. Christensen; In-Seop Cho; Tomasz W. Glinka; Scott J. Hecker |
| The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds. | ||||||
| 190 | 10(1-hydroxyethyl)-11-oxo-1-azatricyclo/7.2.0.0..sup.3.8/ undec-2-ene-2-carboxylic acid esters and a process for preparing thereof | US388515 | 1995-02-14 | US5587374A | 1996-12-24 | Alcide Perboni; Tino Rossi; Giovanni Gaviraghi; Giorgio Tarzia; Antonella Ursini |
| A compound of the formula 1-cyclohexyloxycarbonyloxethyl (4S, 8S, 9R 10S, 12R)-4-methoxy-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo[7.2.0.0..sup.3,8 ]undec-2-ene-2-carboxylate which is useful as a pharmaceutical composition to treat bacterial infection. | ||||||
| 191 | Carbapenem antibiotic compounds | US129167 | 1993-10-06 | US5541178A | 1996-07-30 | Michael J. Betts; Michael L. Swain |
| A carbapenem compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 is hydrogen or C.sub.1-4 alkyl;R.sup.4 is hydroxy or carboxy;and the phenyl ring is optionally further substituted by one or two substituents selected from halo, cyano, C.sub.1-4 alkyl, nitro, hydroxy, carboxy, C.sub.1-4 alkoxy, trifluoromethyl, C.sub.1-4 alkoxycarbonyl, carbamoyl, C.sub.1-4 alkylcarbamoyl, di-C.sub.1-4 alkylcarbamoyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino sulphonic acid, C.sub.1-4 alkylS(O).sub.n --(wherein n is 0-2), N-C.sub.1-4 alkanesulphonamido, C.sub.1-4 alkanoylamino and C.sub.1-4 alkanoyl(N-C.sub.1-4 alkyl)amino:provided that the phenyl ring is substituted by at least one carboxy; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. | ||||||
| 192 | 2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-carbapenem derivatives | US267397 | 1994-06-29 | US5534510A | 1996-07-09 | Takao Abe; Takeshi Isoda; Chisato Sato; Ado Mihira; Satoshi Tamai; Toshio Kumagai |
| Novel carbapenem compounds, (1R,5S,6S)-2-[1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapen-2-em-3 -carboxyic acid derivatives.These carbapenem compounds are represented by the following formula having a beta-coordinated methyl group introduced at the 1-position and a [1-(1,3-thiazolin-2-yl)azetidin-3-yl]thio group introduced at the 2-position. ##STR1## In the formula, R is hydrogen; lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy or lower alkoxy-lower alkoxy group; group --COOR.sup.1 (R.sup.1 is hydrogen or lower alkyl group); or group --CONR.sup.2 R.sup.3 (R.sup.2 and R.sup.3 are, independently each other, hydrogen or lower alkyl), andY is carboxy, --COO.sup..crclbar. or protected carboxy.These compounds are useful antibiotics for prevention and treatment of bacterial infections. | ||||||
| 193 | Antimicrobial quinolonyl lactams | US361919 | 1994-12-22 | US5530116A | 1996-06-25 | Thomas P. Demuth, Jr.; Ronald E. White |
| Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, and R.sup.4 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and(2) R.sup.6 is part of a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: ##STR2## wherein (3) R.sup.10, R.sup.11, R.sup.12, R.sup.13, and R.sup.14, together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and(4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, ester, thioester, amide, and hydrazide groups. | ||||||
| 194 | Intermediaties for aminooxypyrrolidinylthiocarbapenem compounds | US273979 | 1994-07-12 | US5523415A | 1996-06-04 | Yuji Sendo; Makoto Kii |
| An antibacterial aminooxypyrrolidinylthiocarbapenem I, its production from the corresponding carbapenem V and thiol VI, its pharmaceutical formulation, and its use for combating bacteria are presented. ##STR1## (wherein R is optionally substituted amino; R.sup.1 is hydrogen or 1C to 5C alkyl; R.sup.2 is hydrogen or a conventional hydroxy protective group; R.sup.3 is hydrogen or an imino protective group or imino substituent; R.sup.4 is 1C to 5C alkylene; and R.sup.5 is hydrogen or a conventional carboxy protective group; X is a leaving group; R.sup.6 is hydrogen or a thiol protective group; and wavy lines each shows a bond in R or S configuration). | ||||||
| 195 | 2-substituted alkyl-3-carboxy carbapenems as antibiotics and a method of producing them | US234905 | 1994-04-28 | US5480987A | 1996-01-02 | Carl B. Ziegler, Jr.; William V. Curran; Gregg Feigelson |
| The invention provides substituted allylazetidinone compounds having the formula: ##STR1## and propargyl azetidinone compounds having the formula: ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.30, X, Y and Q are defined in the specification. | ||||||
| 196 | Quinolonecarboxylic acids | US131253 | 1993-10-01 | US5480879A | 1996-01-02 | Uwe Petersen; Wilfried Schrock; Dieter Habich; Andreas Krebs; Thomas Schenke; Thomas Philipps; Klaus Grohe; Rainer Endermann; Klaus-Dieter Bremm; Karl-Georg Metzger |
| The invention relates to novel derivatives of quinolonecarboxylic acid and naphthyridonecarboxylic acid which are linked to a .beta.-lactam antibiotic, to their salts, to processes for their preparation and to antibacterial agents containing these derivatives. | ||||||
| 197 | Alkylaminoalkylpyrrolidinylthiocarbapenem derivatives | US289547 | 1994-08-12 | US5449672A | 1995-09-12 | Susumu Nakagawa; Shinji Kato; Satoshi Murase; Osamu Okamoto; Ryuji Mitomo; Katsumi Yamamoto; Koji Yamada; Hiroshi Fukatsu |
| A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or a negative charge, X is a group of --N(R.sup.3)R.sup.4 (wherein R.sup.3 is a lower alkyl group, and R.sup.4 is a hydrogen atom or a lower alkyl group) or a group of --N.sup.+ (R.sup.5)(R.sup.6)R.sup.7 (wherein each of R.sup.5, R.sup.6 and R.sup.7 which may be the same or different, is a lower alkyl group), and n is an integer of from 2 to 4; or a pharmaceutically acceptable salt or ester thereof. | ||||||
| 198 | Antibiotic compounds | US129148 | 1993-10-06 | US5447925A | 1995-09-05 | Michael J. Betts; Gloria A. Breault |
| The present invention provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;n is zero or an integer 1 to 4; andP is a benzene ring substituted by groups R.sup.3 and R.sup.4 which are ortho with respect to one another wherein R.sup.3 and R.sup.4 are independently hydroxy or in vivo hydrolysable esters thereof;or P is a group of the formula (II) or (III) ##STR2## wherein M is oxygen or a group NR.sup.5 wherein R.sup.5 is hydrogen or C.sub.1-4 alkyl;ring P being optionally further substituted;or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. | ||||||
| 199 | Bridged carbapenem compounds, compositions containing such compounds and methods of use | US74905 | 1993-06-10 | US5372993A | 1994-12-13 | Frank P. DiNinno |
| Carbapenems of the formula ##STR1## are useful antibacterial agents. Compositions containing such compounds and methods of use are also disclosed. | ||||||
| 200 | 2-substituted alkyl-3-carboxy carbopenems as antibiotics and a method of producing them | US87944 | 1993-07-06 | US5369102A | 1994-11-29 | Carl B. Ziegler, Jr.; William V. Curran; Gregg Feigelson |
| The invention relates to new 2-substituted alkyl-3-carboxy carbapenems having the formula: ##STR1## with R.sup.1, R.sup.2, R.sup.3, X and Y defined hereafter as antibiotics and beta lactamase inhibitors produced by a novel Michael addition-elimination reaction of a substituted allyl azetidinone in the reaction shown: ##STR2## with R.sup.1, R.sup.2, Q, X and Y defined hereafter. | ||||||
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