| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | JPH0215552B2 - | JP12792778 | 1978-10-19 | JPH0215552B2 | 1990-04-12 | BAATON JII KURISUTENSEN; DEIUITSUDO BII AARU JONSUTON; SUUZAN EMU SHUMITSUTO |
| 2 | Carbapenems | JP14068185 | 1985-06-28 | JPS6118779A | 1986-01-27 | ANDORE FURENMAIAA; ERUBIN GETSUCHI |
| 3 | Carba-2-penem compound and its preparation | JP11498681 | 1981-07-21 | JPS5793981A | 1982-06-11 | MORIMOTO AKIRA; MIYAWAKI TOSHIO; YOSHIOKA KOUICHI |
| NEW MATERIAL:The compound of formulaI(R 1 is alkyl, aryl, alkylthio, arylthio or acylaminoalkylthio; R 2 and R 3 are alkoxycarbonyl, cyano or COR 1; R 3 may be alkyl or aryl; R 4 is H, alkyl, hydroxyalkyl, aryl, or amino), its salt and ester. EXAMPLE: 1-Acetyl-1, 2-dimethyl-6-( 1-hydroxy-1-methylethyl )-carba-2-penem-3-carboxilic acid. USE: Antibacterial agent. It is added to an animal feed, industrial water, etc. as a disinfectant. PROCESS: The compound of formulaIcan be prepared by the cyclization of the compound of formula II (Z is phosphonio or phosphono) which is obtained from a novel compound of formula III. The compound of formula III is prepared by reacting the compound of formula IV with the compound of formula V. COPYRIGHT: (C)1982,JPO&Japio | ||||||
| 4 | JPH0367068B2 - | JP5927984 | 1984-03-27 | JPH0367068B2 | 1991-10-21 | SUGIMURA MASAO; HASHIMOTO TOSHIHIKO; TANAKA TERUO; IINO KIMIO; SHIBATA TOMOYUKI; IWATA MASAYUKI |
| 5 | 1-hetero-6-(1-hydroxyethyl)-2-sr8-1- carbadethiapen-2-em-3-carboxylic acid | JP8560985 | 1985-04-23 | JPS60233077A | 1985-11-19 | ROBUJI DEE KAMA; BAATON JII KURISUTENSEN; DEIBUITSUDO ETSUCHI SHIII |
| 6 | 1-substituted carbapenem-3-carboxylic acid derivative and its preparation | JP5927984 | 1984-03-27 | JPS60202886A | 1985-10-14 | SUGIMURA MASAO; HASHIMOTO TOSHIHIKO; TANAKA TERUO; IINO KIMIO; SHIBATA TOMOYUKI; IWATA MASAYUKI |
| NEW MATERIAL:A carbapenem derivative of formula I [R 1, R 2 are H where they are not Hs at a time, 1W10C alkyl which may be substituted, alkenyl, alkoxy or they incorporate to form a 3W6-membered ring, halogen; R 3 is (substituted) 4W8-membered ring of carbon atoms which may be interrupted with N, S, O, sulfinyl or sulfonyl; R 4 is H, COOH-protecting group; R 5 is H, 1W6C alkyl which may be substituted, alkoxy] and its salt. EXAMPLE: p-Nitrobenzyl (1S, 5R, 6S, 8R)-1-methyl-2-[(R)-1-(N-p-nitrobenzyloxycarbonylacetimidoyl)pyrrolidin-3-ylthio]-6-( 1-hydroxyethyl )-2-carbapenem-3-carboxylate. USE: Antibacterial or its synthetic intermediate. PREPARATION: A compound of formula III is converted into a compound of formula IV (R 6 is alkanesulfonyl) which is allowed to react with R 3SH. COPYRIGHT: (C)1985,JPO&Japio | ||||||
| 7 | 33substitutedd66substitutedd77oxoo11 azabicyclo*3*2*0**heptaa22enee22carboxylic acid | JP12792778 | 1978-10-19 | JPS5466697A | 1979-05-29 | BAATON JII KURISUTENSEN; DEIBUITSUDO BII AARU JIYONSUTO; SUUZAN EMU SHIYUMITSUTO |
| 8 | 33substitutedd66*1**hydroxyethyl**77oxoo11 azabicyclo*3*2*0**heptoo22enee22carboxylic acid | JP12792678 | 1978-10-19 | JPS5466696A | 1979-05-29 | BAATON JII KURISUTENSEN; DEIBUITSUDO BII AARU SHIYONSUT; SUUZAN EMU SHIYUMITSUTO |
| 9 | Carbapenem compound | JP9975091 | 1991-04-05 | JPH04234884A | 1992-08-24 | SUKOTSUTO RUISU DATSUKUSU; DENISU DORUTON KIISU; PAMERA RORIIN ROSUMAN |
| PURPOSE: To provide the novel compd. useful as an antibacterial agent. CONSTITUTION: This compd. is expressed by formula I (R is H, carboxylic acid protective group; R 1 is H lower alkyl, etc.; R 2, R 3 are each H, lower alkoxy, etc.; Y is ester, piperadinyl, etc.; where this ester is bonded to substd. quinolonyl, etc., and further, the piperadinyl includes a piperadinyl nucleus having an N atom to be bonded to naphthylidony, etc.), its ester, its salt and its hydrate; for example, raceme-[5R,6S(R)]-3-[[[6,8-difluoro-1-(2-fluoroethyl)-1, 4-dihydro-4-oxo-7-(4-methyl-1-piperadinyl-3-quinolonyl]carbonyl]oxy]methyl-6-(1- hydroxyethyl)-7-oxo-1-azabicyclo-[3,2,0]hep-2-ten-carboxylic acid. The compd. is obtd. by bringing, for example, the compd. of formula II (R 6 is an ester residue; X is H) into reaction with substd. isothiazoloquinolone. COPYRIGHT: (C)1992,JPO | ||||||
| 10 | JPH0438753B2 - | JP12792678 | 1978-10-19 | JPH0438753B2 | 1992-06-25 | |
| 11 | JPH0419230B2 - | JP13651479 | 1979-10-24 | JPH0419230B2 | 1992-03-30 | BAATON JII KURISUTENSEN; DEIUITSUDO ETSUCHI SHIII |
| 12 | JPS6319514B2 - | JP13735777 | 1977-11-17 | JPS6319514B2 | 1988-04-22 | BAATON JII KURISUTENSEN; DEIUITSUDO BII AARU JONSUTON; SUUZAN EMU SHUMITSUTO |
| 13 | 66*11 and 22substitutedd11carbadethiapenee22 emm33carboxylic acids | JP13651479 | 1979-10-24 | JPS5589285A | 1980-07-05 | BAATON JII KURISUTENSEN; DEIBUITSUDO ETSUCHI SHIII |
| 14 | 33*22aminoethylthio**66*11hydroxyethyl* 77oxoo11azabicyclo*3*2*0*heptt22 enee22carboxylate | JP13735777 | 1977-11-17 | JPS5365892A | 1978-06-12 | BAATON JII KURISUTENSEN; DEIBUITSUDO BII AARU JIYONSUTO; SUUZAN EMU SHIYUMITSUTO |
| 15 | 고정상 연속흐름반응을 이용한 페넴계 유도체의 제조 방법 | KR1020180111070 | 2018-09-17 | KR1020200031934A | 2020-03-25 | |
| 16 | Atypical Carbapenem Antibiotics with Improved Activity Against Carbapenemase-Producing Acinetobacter baumannii | US16839049 | 2020-04-02 | US20200339582A1 | 2020-10-29 | John Buynak; Sergei Vakulenko; Maha Alqurafi; Noora Al-Kharji; Marta Toth; Nichole Stewart |
| The following invention deals with the design, preparation, evaluation, and use of carbapenem antibiotics with improved activity, relative to current commercially available carbapenem antibiotics, against infections involving multidrug resistant, carbapenemase-producing Acinetobacter baumannii. The new carbapenem antibiotics are demonstrated to possess not only inherent antimicrobial activity, but also the ability to inhibit OXA-23, the most commonly produced serine carbapenemase in this species. This unusual carbapenemase-inhibitory activity also indicates that the compounds may be used synergistically, in combination with current commercial carbapenem antibiotics, to inhibit key class D carbapenemases, such as OXA-23. Additionally, one of the newly reported carbapenems is active against metallo-beta-lactamase producing A. baumannii. This is the first report of a metallo-beta-lactamase stable carbapenem antibiotic. Structurally, the present invention describes carbapenem antibiotics which are modified in unusual ways, thus differentiating them from the common scaffold of all current commercial carbapenem antibiotics. In particular, these carbapenems have either an unusual C6 substituent, a hydroxymethyl group, replacing the common hydroxyethyl group, or they have an unusual C5 substituent, an alkyl group, replacing the common hydrogen atom at this position. Such atypical carbapenem antibiotics have not previously been investigated against resistant A. baumannii, nor have they been evaluated for stability to the class D carbapenemase, or the class B metallo-beta-lactamases. | ||||||
| 17 | 2,5-DISUBSTITUTED 3-METHYL PYRAZINES AND 2,5,6-TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS | US16228324 | 2018-12-20 | US20190210977A1 | 2019-07-11 | Ashutosh JOGALEKAR; Walter WON; Elena S. KOLTUN; Adrian GILL; Kevin MELLEM; Naing AAY; Andreas BUCKL; Christopher SEMKO; Gert KISS |
| The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same. | ||||||
| 18 | METHOD FOR THE PREPARATION OF CARBAPENAM COMPOUNDS | US13985478 | 2012-02-14 | US20140148595A1 | 2014-05-29 | Marek Chmielewski; Bartlomiej Furman; Sebastian Stecko; Irma Panfil; Margarita Jurezak; Paulina Mikolajezyk; 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. | ||||||
| 19 | 6- (spirocyclopropyl) penicillanic acid 4, 4-dioxides | US09771440 | 2001-01-26 | US20020147178A1 | 2002-10-10 | Vincent P. Sandanayaka; Amarnauth S. Prashad |
| The 6-(spirocyclopropyl)-penicillanic acid 4,4-dioxides of the general Formula (I): 1 as defined herein above which exhibit beta-lactamase inhibiting activity, use of such compounds in combination with beta-lactam antibiotics for inhibiting beta-lactamases, pharmaceutical compositions and processes for preparing such compounds. | ||||||
| 20 | 2-(1-aceti midoyl-5-carbamoylpyrrolidin-3-ylthio-6-(1-hydroxyethyl)-1-methylcarbapen -2-em-3-carboxylic acid | US463773 | 1990-01-05 | US5102997A | 1992-04-07 | Yukio Sugimura; Toshihiko Hashimoto; Teruo Tanaka; Kimio Iino; Tomoyuki Shibata; Masayuki Iwata |
| Compounds of formula (I): ##STR1## wherein: one or both of R.sup.1 and R.sup.2 are selected from a variety of organic groups;R.sup.3 is an optionally substituted heterocycle; andR.sup.4 is hydrogen or optionally substituted alkyl or alkoxy.and salts and esters thereof have valuable antibiotic activity. | ||||||
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