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 |
|---|---|---|---|---|---|---|
| 161 | Antibiotic PA-39504-X.sub.3 and production thereof | US286757 | 1981-07-27 | US4387052A | 1983-06-07 | Kentaro Tanaka; Eiji Kondo; Kouichi Matsumoto; Jun'ichi Shoji; Naoki Tsuji |
| A new antibiotic having .beta.-lactamase inhibitory activity, PA-39504-X.sub.3 of the formula: ##STR1## and the pharmaceutically acceptable slats being useful as a drug, a animal drug and a disinfectant for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces argenteolus PA-39504 or Streptomyces tokunonensis PA-31088 in a suitable medium and isolating PA-39504-X.sub.3 from the cultured broth. | ||||||
| 162 | 6-Amidocyclonocardicins | US301668 | 1981-09-14 | US4374849A | 1983-02-22 | Burton G. Christensen; James V. Heck |
| Disclosed are 6-amidocyclonocardicins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics ##STR1## wherein: R is NH.sub.2, R.sup.1 NH, R.sup.1 is acyl. Also disclosed are processes for the preparation of such compounds; pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated. | ||||||
| 163 | .beta.-Lactam antibiotics, preparation and use | US25556 | 1979-03-30 | US4366167A | 1982-12-28 | David F. Corbett |
| This invention provides the anti-bacterial compounds (III) and (IV): ##STR1## and salts and esters thereof wherein X is a --CH.sub.2 --CH.sub.2 -- or trans --CH.dbd.CH-- group and R is a group R.sup.1 or NH.R.sup.1 wherein R.sup.1 is an alkyl group of up to 6 carbon atoms, an alkenyl group of up to 6 carbon atoms, an aryl group, or an alkyl group of up to 6 carbon atoms substituted by an aryl or aryloxy group.The invention also provides processes for their preparation comprising a the acylation or carbamoylation of the corresponding 6-(1-hydroxyethyl) compounds.The invention further provides pharmaceutical compositions containing them. | ||||||
| 164 | Antibiotic PA-39504-X.sub.1 and production thereof | US211715 | 1980-12-01 | US4362665A | 1982-12-07 | Kentaro Tanaka; Eiji Kondo; Kouichi Matsumoto; Jun'ichi Shoji; Naoki Tsuji |
| A new antibiotic having .beta.-lactamase inhibitory activity, PA-39504-X.sub.1 of the formula: ##STR1## being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces argenteolus PA-39504 or Streptomyces tokunonensis PA-31088 in a suitable medium and recovering PA-39504-X.sub.1 from the cultured broth. | ||||||
| 165 | 6- and 4-Substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylates | US245005 | 1981-03-18 | US4350631A | 1982-09-21 | Burton G. Christensen; David H. Shih |
| Disclosed are 6- and 4-substituted-1-azabicyclo[3.2.0]heptan-3,7-dione-2-carboxylic acid esters and salts (I) which are useful in the preparation of 6-, 1- and 2-substituted carbapenem antibiotics. ##STR1## wherein R.sup.5 is a pharmaceutically acceptable ester moiety or a removable protecting group or an alkali or alkaline earth metal cation such as sodium or potassium and wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, aryl and aralkyl. | ||||||
| 166 | .beta.-Lactam anti-bacterial, compositions containing them and a process for their preparation | US68893 | 1979-08-23 | US4323569A | 1982-04-06 | Andrew J. G. Baxter |
| The compounds of the formula (II): ##STR1## and salts and esters thereof wherein R.sub.1 is a pyrimidyl group, or a pyrimidyl group substituted by one or two lower alkyl groups, or by a lower alkoxy group or by a lower acyloxy group; and R.sub.2 is a hydrogen atom or a group CR.sub.3 R.sub.4 R.sub.5 wherein R.sub.3 is a hydrogen atom or a hydroxy group; R.sub.4 is a hydrogen atom or a lower alkyl group; and R.sub.5 is a hydrogen atom or a lower alkyl group, a benzyl group, a phenyl group or is joined to R.sub.4 to form part of a C.sub.5-7 carbocyclic ring, have been found to be anti-bacterial-agents. Their preparation and use is described. | ||||||
| 167 | Process for the preparation of 1-carbapenems and intermediates via trithioorthoacetates | US134396 | 1980-03-27 | US4309346A | 1982-01-05 | Burton G. Christensen; Ronald W. Ratcliffe; Thomas N. Salzmann |
| Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via intermediates II and III: ##STR1## wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R.sup.6 and R.sup.7 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R.sup.1' is hydrogen or a protecting group; and R.sup.a, R.sup.b and R.sup.c are independently selected from alkyl, aryl and aralkyl. | ||||||
| 168 | Antibiotic PA-31088-IV and production thereof | US115278 | 1980-01-25 | US4292241A | 1981-09-29 | Kentaro Tanaka; Jun'ichi Shoji; Yoshimi Kawamura; Teruo Hattori; Eiji Kondo; Kouichi Matsumoto; Tadashi Yoshida; Naoki Tsuji |
| A new antibiotic having .beta.-lactamase inhibitory activity, PA-31088-IV, being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative phathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces tokunonensis sp. nov. in a suitable medium and recovering PA-31088-IV from the cultured broth. | ||||||
| 169 | Process for the preparation of thienamycin and intermediates | US59842 | 1979-07-23 | US4273709A | 1981-06-16 | Burton G. Christensen; Ronald W. Ratcliffe; Thomas N. Salzmann |
| Disclosed is a process for the total synthesis of thienamycin from 4-allylazetidinone (IIIa) via ##STR1## L-aspartic acid (III): ##STR2## R.dbd.H, blocking group or salt cation. | ||||||
| 170 | N-Alkyl-N-acyl derivatives of thienamycin | US793974 | 1977-05-05 | US4235917A | 1980-11-25 | Burton G. Christensen; William J. Leanza |
| Disclosed are N-alkyl- N-acyl derivatives of the antibiotic thienamycin having the following structural formula: ##STR1## wherein R.sup.1 is, inter alia, alkyl, alkenyl, aryl or aralkyl; and R.sup.2 is acyl. Such compounds, including their O- and carboxyl derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated. | ||||||
| 171 | Bicyclic .beta.-lactam antibiotics | US955598 | 1978-10-30 | US4223038A | 1980-09-16 | Terence C. Smale |
| Compounds of the formula (I): ##STR1## wherein G is hydrogen, alkyl, alkenyl, substituted alkyl or substituted alkenyl, R.sub.1 is alkyl or aryl, substituted alkyl or substituted aryl, and R is an organic group such that --CO.sub.2 R is an ester group are produced. The compounds are useful as antibacterial and .beta.-lactamase inhibitory agents. | ||||||
| 172 | Process for preparing 6- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids | US898591 | 1978-04-21 | US4203902A | 1980-05-20 | David H. Shih |
| A process is disclosed for preparing antibiotic 6- and 2-substituted-1-carbadethiapen-2-em-3-carboxylic acids and their pharmaceutically acceptable salts and esters (I) ##STR1## wherein: R.sup.1 and R.sup.2 are selected from hydrogen, alkyl aryl, and aralkyl; and R.sup.3 is hydrogen, --R, --OR, or --SR, wherein R is hydrogen, alkyl, aryl or aralkyl. The process comprises complexing an appropriately substituted .delta.,.omega.-unsaturated amino acid with a transition metal carbonyl complex, followed by oxidatively induced ligand transfer and ring closure: ##STR2## wherein: F.sub.p =.eta..sup.5 --C.sub.5 H.sub.5 Fe(CO).sub.2 and F.sub.p (isobutene.sup..sym. represents a cationic complex between F.sub.p and an olefin such as isobutene, which complex cation is employed in the initial ligand exchange reaction; R.sup.4 is lower alkyl or phenyl; R.sup.5 is a readily removable blocking group or pharmaceutically acceptable ester radical; and R.sup.1, R.sup.2 and R.sup.3 are as defined above. | ||||||
| 173 | Method for the preparation of carbapenam compounds | US13985478 | 2012-02-14 | US08884005B2 | 2014-11-11 | Marek Chmielewski; Bartlomiej Furman; Sebastian Stecko; Irma Panfil; Margarita Jurczak; Paulina Mikolajczyk; Magdalena Soluch |
| The subject of the present invention is a method of the preparation of compounds containing the core skeleton of carbapenem antibiotics, novel intermediate compounds used in this method, a method of the preparation of the intermediate compounds as well as the use of the intermediate compounds in the production of carbapenem antibiotics. | ||||||
| 174 | Organic nitric oxide donor salts of antimicrobial compounds, compositions and methods of use | US11883445 | 2006-02-16 | US20090042819A1 | 2009-02-12 | James L. Ellis; David S. Garvey; Chia-En Lin |
| The invention describes novel organic nitric oxide donor salts of a antimicrobial compounds, and novel compositions and kits comprising at least one organic nitric oxide donor salt of an antimicrobial compound, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating bacterial infections; (b) treating viral infections; (c) treating fungal infections; and (d) treating lesions. In one embodiment the antimicrobial compounds of the invention are aztreonam, ciprofloxacin, doripenam, duramycin and tobramycin. The organic nitric oxide donors that form salts are preferably organic nitrates, organic nitrites, nitrosothiols, thionitrites and heterocyclic nitric oxide donors. The heterocyclic nitric oxide donors are preferably furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. The methods of the invention are preferably for the treatment of bacterial infections associated with pulmonary diseases such as cystic fibrosis and for treating Bacillus anthracis infections. | ||||||
| 175 | Novel carbapenem compound | US11886949 | 2006-03-23 | US20090029964A1 | 2009-01-29 | Makoto Sunagawa; Akira Sasaki; Takashi Tsukimura |
| An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R0 represents hydrogen atom or the like; R1 represents C1-C3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH2(CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH2—, —NRaCH2— (wherein Ra represents hydrogen atom, optionally substituted C1-C4 alkyl group or the like) or the like. | ||||||
| 176 | Process for the preparation of crystalline imipenem | US10495681 | 2002-11-18 | US20050004359A1 | 2005-01-06 | Bishwa Rai; Neera Tewari; Yatendra Kumar |
| The present invention relates to a cost effective and industrially advantageous process for the preparation of imipenem of high purity. | ||||||
| 177 | 1'S, 5R, 6R-carbapenem derivatives and antimicrobial agents comprising the same | US911937 | 1997-08-15 | US6051569A | 2000-04-18 | Masaji Ishiguro; Takashi Nakatsuka; Hidekazu Inoue |
| A carbapenem derivative represented by the following formula (I), ##STR1## wherein R.sub.1 represents a hydrogen atom, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, R.sub.2 indicates a hydrogen atom or a protective group for a carboxyl group, and R.sub.3 is a methyl group or an ethyl group; or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising this carbapenem derivative or a salt thereof as an active ingredient. The carbapenem derivative exhibits a wide and strong antimicrobial activity, particularly a strong antimicrobial activity against MRSA. An intermediate compound for preparing the carbapenem derivative is also disclosed. | ||||||
| 178 | Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment | US150569 | 1998-09-10 | US5994343A | 1999-11-30 | Frank P. Dininno; Kevin D. Dykstra |
| The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a --Z--CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including cationic groups. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included. | ||||||
| 179 | .beta.-methylcarbapenem derivatives, process for the preparation thereof and pharmaceutical composition comprising same | US760431 | 1996-12-04 | US5869477A | 1999-02-09 | Cheol-Hae Lee; Dong-Ha Lee; Kyung-Sook Kim; Jae-Hak Kim; Young-Sook Kim; Yu-Sung Jun; Sung-Su Lim; Eun-Mi Bae; Bong-Jin Kim |
| A .beta.-methylcarbapenem compound of formula (I), a salt or an ester thereof, a process for the preparation thereof and a anti-bacterial composition containing same: ##STR1## wherein: R.sup.1 is a C.sub.1-6 alkyl, C.sub.2-6 alkenyl, cycloalkyl, aryl or heterocyclic aryl group. | ||||||
| 180 | Azetidinone derivatives, a process for their preparation and their use as intermediates in the preparation of carbapenem antibiotics | US35915 | 1993-03-23 | US5856556A | 1999-01-05 | Sadao Oida; Akira Yoshida; Yawara Tajima; Noriko Takeda |
| Compounds of formula (I): ##STR1## (wherein R.sup.1 represents hydrogen or a hydroxy-protecting group, R.sup.2 and R.sup.3 represent hydrogen, alkyl or aryl; R.sup.4 represents optionally substituted alkyl, alicyclic heterocyclic, aryl, aromatic heterocyclic, optionally substituted alkenyl or optionally substituted alkynyl; R.sup.5 represents hydrogen or a carboxy-protecting group; and R.sup.6 represents alkoxy, aryloxy, dialkylamino or diarylamino or two or R.sup.6 together represent o-phenylenedioxy or three together represent CH.sup.3 C(--CH.sub.2 O--).sub.3) may be prepared by reacting the corresponding carbonyl compound with a compound of formula P(R.sup.6).sub.3. Compounds (I) may be cyclised to prepare carbopenem derivatives, many of which have valuable antibiotic activity. | ||||||
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