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1. 发明申请

US20030236243A1 Sterically-awkward beta-lactamase inhibitors 审中-公开
标题翻译：异位笨拙的β-内酰胺酶抑制剂
公开(公告)号：US20030236243A1
公开(公告)日：2003-12-25
申请号：US10438280
申请日：2003-05-14
发明人： Brian K. Shoichet , Larry C. Blaszczak
IPC分类号： A61K031/545 , A61K031/43 , C07D501/14 , C07D499/80
CPC分类号： C07D499/00 , A61K31/397 , A61K31/43 , C07D463/22
摘要： 6(7)-null-substituted null-lactam compounds as inhibitors of null-lactamase activity.
摘要翻译： 6（7）β-取代的β-内酰胺化合物作为β-内酰胺酶活性的抑制剂。

2. 发明授权

US4439363A Acetylmethyl ester of hetacyllin and/or salts of this ester 失效
标题翻译： hetacyllin的乙酰基甲酯和/或该酯的盐
公开(公告)号：US4439363A
公开(公告)日：1984-03-27
申请号：US352118
申请日：1982-02-25
申请人： Wojciech A. Gruszecki , Irena M. Busko-Oszczopowicz , Maria Gdulewicz-Gruszecka , Jerzy J. Cieslak , Edward Borowski , Teresa Gumiezna
发明人： Wojciech A. Gruszecki , Irena M. Busko-Oszczopowicz , Maria Gdulewicz-Gruszecka , Jerzy J. Cieslak , Edward Borowski , Teresa Gumiezna
IPC分类号： C07D499/08 , A61K31/415 , A61K31/43 , A61P31/04 , C07D20060101 , C07D499/46 , C07D499/64 , C07D499/68 , C07D499/80
CPC分类号： C07D499/80
摘要： The acetylmethyl ester of hetacyllin and/or its salts of an organic or inorganic acid are described and methods for their synthesis wherein a tertiary amine and chloroacetone are introduced to hetacyllin in an organic solvent or chloroacetone is introduced to hetacyllin in the form of a salt with an alkali metal in an organic solvent, and then from the reaction mixture, the acetylmethyl ester of hetacyllin is isolated in free form and, if desired, a salt of the ester is obtained by reaction with an organic or inorganic acid in an organic solvent.As tertiary amines, trialkylamine, N-methylpiperidine, N-ethylpiperidine or N-methylmorpholine are used; as organic solvents in obtaining the ester, dimethylformamide, dimethylacetamide or dimethylsulfoxide are used. In obtaining salts of the ester the organic solvents used are aliphatic alcohols of a chain length C.sub.2 -C.sub.5 ; ketones, preferably acetone; ethers, such as diethyl, dipropyl, diisopropyl, dibutyl ethers, or their mixtures.The obtained compounds show an antibacterial action like ampicillin but after administration per os they show a considerably higher level of the antibiotic than that after administration of free ampicillin or its esters.
摘要翻译：描述了hetacyllin的乙酰甲基酯和/或其有机或无机酸的盐，并将其合成方法，其中叔胺和氯丙酮在有机溶剂或氯丙酮中引入hetacyllin，以盐的形式引入到hetacyllin中，在有机溶剂中的碱金属，然后从反应混合物中分离出游离形式的海参酰基乙酰甲基酯，如果需要，通过在有机溶剂中与有机或无机酸反应获得酯的盐。作为叔胺，使用三烷基胺，N-甲基哌啶，N-乙基哌啶或N-甲基吗啉; 作为获得酯的有机溶剂，使用二甲基甲酰胺，二甲基乙酰胺或二甲基亚砜。在获得酯的盐时，使用的有机溶剂是链长C 2 -C 5的脂族醇; 酮，优选丙酮; 醚，如二乙基，二丙基，二异丙基，二丁基醚或它们的混合物。所得化合物显示出抗菌作用，如氨苄青霉素，但是在施用之后，它们显示比施用游离氨苄青霉素或其酯后显着高得多的抗生素水平。

3. 发明授权

US4381307A Soft tertiary amine esters of bio-affecting carboxylic acids 失效
标题翻译：生物影响羧酸的软叔胺酯
公开(公告)号：US4381307A
公开(公告)日：1983-04-26
申请号：US202750
申请日：1980-10-31
申请人： Kenneth B. Sloan
发明人： Kenneth B. Sloan
IPC分类号： A61K31/19 , A61K31/215 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/43 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61K31/545 , A61K31/57 , A61P9/12 , A61P25/04 , A61P29/00 , A61P31/04 , A61P35/00 , C07C67/00 , C07C219/00 , C07C219/10 , C07C219/14 , C07C219/28 , C07C223/02 , C07C227/00 , C07C227/08 , C07C227/16 , C07C227/18 , C07C229/00 , C07C237/20 , C07C291/02 , C07C291/04 , C07C313/00 , C07C323/24 , C07C401/00 , C07C405/00 , C07D207/16 , C07D207/20 , C07D209/18 , C07D209/28 , C07D213/80 , C07D231/12 , C07D231/56 , C07D233/60 , C07D403/12 , C07D473/08 , C07D475/04 , C07D499/00 , C07D499/32 , C07D499/44 , C07D499/46 , C07D499/60 , C07D499/62 , C07D499/68 , C07D499/72 , C07D499/74 , C07D499/76 , C07D499/80 , C07D501/20 , C07D521/00 , C07J7/00 , C07J41/00 , C07J43/00 , A61K31/56
CPC分类号： C07D231/12 , C07D209/28 , C07D233/56 , C07D249/08 , C07D499/00 , C07J41/005 , C07J43/003
摘要： Novel derivatives of known bio-affecting carboxylic acids R-COOH are disclosed, said derivatives having the structural formula ##STR1## wherein Y and Y' are each H or C.sub.1 -C.sub.4 alkyl; n is 0 or 1; R.sub.1 and R.sub.2 are each selected from a variety of unsubstituted or substituted hydrocarbon radicals, or are combined so that --NR.sub.1 R.sub.2 represents the residue of a saturated or unsaturated heterocyclic compound containing one secondary nitrogen atom; and R.sub.3 is H or one of a variety of other substituents. Salts and N-oxides of compounds of formula (I) and the corresponding diacyloxy derivatives of known bio-affecting carboxylic acids HOOC-R'-COOH are disclosed also. The parent acids from which the subject soft tertiary amine esters can be derived include such bio-affecting agents as cephalosporin and penicillin antibiotics, amino acids and structurally related compounds, prostaglandins and their metabolites, steroidal anti-inflammatory agents, and non-steroidal anti-inflammatory/non-narcotic analgesic/antipyretic agents.
摘要翻译：公开了已知的生物影响羧酸R-COOH的新衍生物，所述具有结构式（I）的衍生物，其中Y和Y'各自为H或C 1 -C 4烷基; n为0或1; R 1和R 2各自选自多个未取代或取代的烃基，或者组合使得-NR 1 R 2表示含有一个仲氮原子的饱和或不饱和杂环化合物的残基; 并且R 3是H或各种其它取代基之一。还公开了式（I）化合物的盐和N-氧化物和已知的生物影响羧酸HOOC-R'-COOH的相应的二酰氧基衍生物。可以得到本发明的软叔胺酯的母体酸包括诸如头孢菌素和青霉素抗生素的生物影响剂，氨基酸和结构相关化合物，前列腺素及其代谢物，甾体抗炎剂和非甾体抗炎药，炎症/非麻醉性镇痛/解热剂。

4. 发明授权

US4035381A Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US4035381A
公开(公告)日：1977-07-12
申请号：US735552
申请日：1976-10-26
申请人： Murray Arthur Kaplan , William Joseph Gottstein , Alphonse P. Granatek
发明人： Murray Arthur Kaplan , William Joseph Gottstein , Alphonse P. Granatek
IPC分类号： C07D499/00 , C07D499/80
CPC分类号： C07D499/00
摘要： The alkali metal salts of the reaction products of ampicillin or amoxicillin with 5-formyl-2-furansulfonic acid are found to be stable, useful water-soluble forms of the penicillin antibiotics especially advantageous for parenteral administration.
摘要翻译：发现氨苄西林或阿莫西林与5-甲酰基-2-呋喃磺酸的反应产物的碱金属盐是稳定的，有用的青霉素抗生素的水溶性形式，对肠胃外给药尤为有利。

5. 发明授权

US3652547A 3-quinazolinylpenicillanic acid 失效
标题翻译： 3-喹唑啉氨基丙酸
公开(公告)号：US3652547A
公开(公告)日：1972-03-28
申请号：US3652547D
申请日：1969-12-17
申请人： AMERICAN HOME PROD
发明人： WOLF MILTON , DIEBOLD JAMES L , BELL STANLEY C
IPC分类号： C07D499/00 , C07D499/80 , C07D99/16
CPC分类号： C07D499/00
摘要： THIS INVENTION IS CONCERNED WITH NOVEL 3-QUINAZOLINYLPENICILLANIC ACIDS.

6. 发明授权

US10730835B2 Thalidomide analogs and methods of use 有权
公开(公告)号：US10730835B2
公开(公告)日：2020-08-04
申请号：US15764193
申请日：2016-09-29
申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , University Court of the University of Aberdeen
发明人： Nigel H. Greig , Weiming Luo , David Tweedie , Neil Vargesson , Shaunna Beedie , William Douglas Figg
IPC分类号： C07D209/44 , A61P29/00 , A61P35/00 , A61K45/06 , C07D401/04 , A61K31/454 , C07D401/14 , C07D401/12 , A61K31/4035 , C07D417/04 , A61K31/428 , C07D413/04 , A61K31/4545 , C07D499/80 , A61K31/431 , C07D471/04 , A61K31/536 , C07D209/48 , C07D209/52 , C07D209/46
摘要： Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.

7. 发明申请

US20100063273A1 NOVEL CRYSTAL OF PIPERACILLIN SODIUM 审中-公开
标题翻译： PIPERACILLIN SODIUM的新型水晶
公开(公告)号：US20100063273A1
公开(公告)日：2010-03-11
申请号：US12524875
申请日：2008-01-29
申请人： Masaru Mouri , Dai Nishikawa
发明人： Masaru Mouri , Dai Nishikawa
IPC分类号： C07D499/80
CPC分类号： C07D499/68 , A61K9/0019
摘要： Disclosed are a novel crystal of piperacillin sodium which has diffraction angles of 3.7°, 5.5°, 7.3°, 11.6°, 14.5° and 18.0° and a novel crystal of piperacillin sodium which has diffraction angles of 5.6°, 7.8°, 12.3°, 15.5°, 17.5°, 23.3°, 24.8° and 28.5° expressed by 2θ in the powder X-ray diffraction analysis. The crystals have excellent stability and solubility and a low water-absorbing property, is extremely easy to be handled in the manufacturing process for a medicinal substance and in the packing during the preparation process for a pharmaceutical product. A pharmaceutical preparation for injection comprising any one of the crystals is useful.
摘要翻译：公开了一种新颖的哌拉西林钠结晶，其衍射角为3.7°，5.5°，7.3°，11.6°，14.5°和18.0°，新颖的哌拉西林钠晶体为衍射角为5.6°，7.8°，12.3° ，15.5°，17.5°，23.3°，24.8°和28.5°，由2表示; 在粉末X射线衍射分析中。晶体具有优异的稳定性和溶解性以及低吸水性，在制药过程中对于药物的制造过程和包装中的处理非常容易。包含任何一种晶体的用于注射的药物制剂是有用的。

8. 发明授权

US5856475A 4-thia-1-azabicyclo/3.2.0/Heptane-3-Imino-2-isopropylidene-7-oxo-analogon s of beta-lactams, processes for their preparation and the use thereof 失效
标题翻译： β-内酰胺的4-硫杂-1-氮杂双环/ 3.2.0 /庚烷-3-亚氨基-2-异亚丙基-7-氧代 - 类似物，其制备方法及其用途
公开(公告)号：US5856475A
公开(公告)日：1999-01-05
申请号：US828267
申请日：1997-03-21
申请人： Jure J. Herak
发明人： Jure J. Herak
IPC分类号： C07D499/87 , A61K31/00 , C07D499/00 , C07D499/86 , C07D499/897 , C07D513/04 , C07D499/80 , C07D499/861 , C07D499/865
CPC分类号： C07D499/00
摘要： The object of the present invention are 4-thia-1-azabicyclo�3.2.0!heptane-3-imino-2-isopropylidene-7-oxo beta-lactamic analogons of general formula I ##STR1## wherein the radicals have the following meanings: R.sup.1 is hydrogen or halogen,R.sup.2 is hydrogen, halogen, phthalimide,R.sup.3 is hydrogen, alkyl, benzyl, heterocycle e.g. isoxazole, pyrazole, 5-methyl-isoxazole-3-yl, 3,4-dimethyl-isoxazole-5-yl, 2-phenyl-pyrazole-3-yl, etc.These compounds are useful as intermediates in the preparation of novel beta-lactamic analogons or of active substances in preparations for antimicrobial therapy.
摘要翻译：本发明的目的是通式I的4-硫杂-1-氮杂双环[3.2.0]庚烷-3-亚氨基-2-异丙基-7-氧代β-内酰胺类似物，其含义为：R1是氢或卤素，R2 是氢，卤素，邻苯二甲酰亚胺，R3是氢，烷基，苄基，杂环异恶唑，吡唑，5-甲基 - 异恶唑-3-基，3,4-二甲基 - 异恶唑-5-基，2-苯基 - 吡唑-3-基等。这些化合物可用作制备新型β的中间体活性类似物或活性物质用于抗微生物治疗的制剂。

9. 发明授权

US4325960A 6-Amidinopenicillanic acid derivatives including the radical of a .beta.-lactamase inhibitor 失效
标题翻译：包括β-内酰胺酶抑制剂基团的6-脒基青霉烷酸衍生物
公开(公告)号：US4325960A
公开(公告)日：1982-04-20
申请号：US116651
申请日：1980-01-29
申请人： Wagn O. Godtfredsen , Welf von Daehne
发明人： Wagn O. Godtfredsen , Welf von Daehne
IPC分类号： C07D499/80 , A61K31/431 , A61P31/04 , C07D499/00 , C07D499/21 , C07D499/32 , C07D499/42 , C07D503/00 , C07D519/00
CPC分类号： C07D503/00 , C07D499/00
摘要： The present invention relates to hitherto unknown compounds of the general formula I: ##STR1## in which R.sub.1 stands for a five- to ten-membered azacycloalkyl or azabicycloalkyl residue attached via the nitrogen atom and optionally being substituted by one or two, the same or different, lower alkyl groups; R.sub.2 represents a hydrogen atom or a lower alkyl, aryl, or aralkyl radical; and A represents a radical of a .beta.-lactamase inhibitor containing a .beta.-lactam ring as well as a carboxy group, A being connected via the carboxy group.The present compounds are useful in the treatment of bacterial infections. The new compounds are in particular strongly active against .beta.-lactamase producing bacteria.
摘要翻译：本发明涉及迄今为止未知的通式I化合物：其中R1代表通过氮原子连接并任选被一个或两个相同的5至10元氮杂环烷基或氮杂双环烷基取代的相同或不同的低级烷基; R2表示氢原子或低级烷基，芳基或芳烷基; 而A代表含有β-内酰胺环以及羧基的β-内酰胺酶抑制剂的基团，A通过羧基连接。

10. 发明授权

US4064137A Penicillin and cephalosporin derivatives and process for preparing the same 失效
标题翻译：青霉素和头孢菌素衍生物及其制备方法
公开(公告)号：US4064137A
公开(公告)日：1977-12-20
申请号：US759640
申请日：1977-01-17
申请人： Koichi Hirai , Yuji Iwano , Tokio Saito , Tetsuo Hiraoka , Yukichi Kishida , Takuzo Nishimura
发明人： Koichi Hirai , Yuji Iwano , Tokio Saito , Tetsuo Hiraoka , Yukichi Kishida , Takuzo Nishimura
IPC分类号： C07D513/20 , A61K31/43 , A61K31/545 , A61P31/12 , C07D499/00 , C07D499/80 , C07D501/58 , C07D499/02
CPC分类号： C07D499/00 , Y02P20/55 , Y10S514/889
摘要： Novel penicillin and cephalosporin derivatives possessing interferon inducibility and represented by the formula ##STR1## wherein Y represents a hydrogen atom, a halogen atom a nitro group, an alkoxy group or an alkyl group; M represents a protective group for a hydroxyl or carboxyl group; Z represents a group ##STR2## or a group ##STR3## in which D is a hydrogen atom, an acyloxy group, a carbamoyloxy group or a substituted or unsubstituted heterocyclic thio group; A represents a cyano group, a carboalkoxy group or a nitro group; and B represents a hydrogen atom, a cyano group, a carboalkoxy group or a nitro groupAnd process for preparing the same.
摘要翻译：新型的具有干扰素诱导性的青霉素和头孢菌素衍生物，其由Y表示氢原子，卤素原子，硝基，烷氧基或烷基的式“IMAGE”表示。 M表示羟基或羧基的保护基; Z表示其中D为氢原子，酰氧基，氨基甲酰氧基或取代或未取代的杂环硫基的基团或基团; A表示氰基，碳烷氧基或硝基; 和B表示氢原子，氰基，烷氧羰基或硝基及其制备方法。

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