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公开(公告)号：US4340603A
公开(公告)日：1982-07-20
申请号：US177824
申请日：1980-08-13
IPC分类号： A61K31/265 , C07C69/74 , C07C69/76 , C09F5/08
CPC分类号： C07C211/27 , C07C229/24 , C07C327/30
摘要： Novel, transient inotropic prodrug forms of the N-(2-phenylethyl)-.omega.-phenylalkylamines, notably of dobutamine, have (i) the structural formula (I): ##STR1## with the proviso that at least one R.sup.1, R.sup.2 or OR.sup.1, when R.sup.7 and/or R.sup.10 is OR.sup.1, must be R.sup.3 COXCH(R.sup.4)-- or R.sup.3 COXCH(R.sup.4)O--, respectively.
摘要翻译： 新颖的N-（2-苯基乙基） - ω-苯基烷基胺，特别是多巴酚丁胺的瞬时变性前体药物形式具有（i）结构式（I）：条件是至少一个R 1， R2或OR1，当R7和/或R10为OR1时，必须分别为R3COXCH（R4） - 或R3COXCH（R4）O-。
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公开(公告)号：US4311706A
公开(公告)日：1982-01-19
申请号：US114205
申请日：1980-01-22
IPC分类号： A61K31/165 , A61K31/22 , A61K31/235 , A61K31/245 , A61K31/25 , A61K31/26 , A61K31/265 , C07C67/02 , C07C69/00 , C07C69/74 , C07C69/76 , C09F5/08 , C07C79/46 , C07C97/16 , C07C101/20 , C07C101/44 , C07C101/72 , C07C102/00 , C07C103/20 , C07C153/00
CPC分类号： C07C233/18 , C07C217/60 , C07C229/36 , C07C327/28 , Y02P20/55
摘要： Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.3 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above; saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, containing from 1 to 3 of any one or more of the hetero atom N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8-membered; and mono- or poly-substituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, lower alkoxycarbonyl, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl and ##STR3## wherein R.sup.5 is hydrogen or alkyl having from 1 to 10 carbons; R.sup.4 is hydrogen, R.sup.3, lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, --CH.sub.2 ONO.sub.2 and --CH.sub.2 OCOR.sup.3 ; R.sup.6 is hydrogen or lower alkyl; R.sup.7 is hydrogen, lower alkyl, COCF.sub.3, COOC(CH.sub.3).sub.3, COOCH.sub.2 C.sub.6 H.sub.5, or other N-protective group conventional to amino acid acid chemistry; R.sup.8 is hydrogen, benzyl, or other conventional, cleavable carboxyl protective group; with the proviso that at least one R must be R.sup.3 COXCH(R.sup.4)--; (ii) the structural formula (I) wherein at least one R.sup.3 CO- moiety comprising at least one R group is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N,N-lower dialkyl or C.sub.4 -C.sub.7 cycloalkylamino acid; and (ii) the non-toxic, pharmaceutically acceptable salts thereof.
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公开(公告)号：US4443435A
公开(公告)日：1984-04-17
申请号：US320264
申请日：1981-11-12
IPC分类号： A61K31/095 , A61K31/10 , A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/415 , A61K31/505 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P5/12 , A61P9/12 , A61P25/04 , A61P31/04 , A61P35/00 , A61P39/02 , C07C67/00 , C07C313/00 , C07C323/12 , C07C323/52 , C07C323/59 , C07C323/60 , C07C325/00 , C07C327/22 , C07C327/24 , C07C327/26 , C07D207/16 , C07D233/84 , C07D239/38 , C07D239/42 , C07D239/56 , C07D307/88 , C07D473/38 , C07H19/16 , C07H19/167 , C07K1/00 , C07K1/113 , C07D473/24
CPC分类号： C07D239/42 , C07D207/16 , C07D233/84 , C07D239/38 , C07D307/88 , C07D473/38 , C07H19/16 , Y02P20/55 , Y10S514/863
摘要： Novel, transient prodrug forms of biologically active agents containing mercapto groups have (i) the structural formula (I): ##STR1## wherein X is O, S, or NR.sup.5 ;R.sup.1 S is the residue of any biologically active agent R.sup.1 SH;R.sup.2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweralkanoyloxyalkyl, carboxyalkyl, and lower alkanoyloxyalkyl wherein alkyl, aryl, alkenyl and alkynyl are as defined above; saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, either directly bonded to the carbonyl function or linked thereto via an alkylene bridge, containing from 1 to 3 of any one or more of the heteroatoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8- membered; and mono- or polysubstituted derivatives of the above, each of said substituents being selected from the group consisting of lower akyl, lower alkoxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl and ##STR2## wherein R.sup.4 is hydrogen or alkyl having from 1 to 10 carbons;R.sup.3 is hydrogen, R.sup.2, lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, --CH.sub.2 ONO.sub.2 and --CH.sub.2 OCOR.sup.2 ;R.sup.5 is hydrogen or lower alkyl; and further whereinR.sup.2 and R.sup.3 may be taken together to form a cyclizing moiety selected from the group consisting of ##STR3## with the proviso that when R.sup.1 S is the residue of a sulfur containing amino acid, then X cannot be NR.sup.5 ;(ii) the structural formula (I) wherein ##STR4## is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N,N-lower dialkyl of C.sub.4 -C.sub.7 cycloalkylamino acid; and(iii) the non-toxic, pharmaceutically acceptable salts thereof.
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公开(公告)号：US4313956A
公开(公告)日：1982-02-02
申请号：US108055
申请日：1979-12-28
IPC分类号： C07C233/16 , C07C149/40 , A61K31/165 , A61K31/22 , A61K31/235 , A61K31/245 , A61K31/25 , A61K31/265 , C07C67/02 , C07C69/00 , C07C69/74 , C07C69/76 , C07C79/46 , C07C97/16 , C07C101/20 , C07C101/44 , C07C101/72 , C07C102/00 , C07C103/20 , C07C153/00 , C09F5/08
CPC分类号： C07C233/16 , Y02P20/55
摘要： Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.2 is selected from the group consisting of straight or branched chain alkyl having from 1 to 20 carbon atoms; aryl having from 6 to 10 carbon atoms; cycloalkyl having from 3 to 8 carbon atoms; alkenyl having from 2 to 20 carbon atoms; cycloalkenyl having from 4 to 8 carbon atoms; alkynyl having from 2 to 20 carbon atoms; aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, loweracyloxyalkyl, and carboxyalkyl, wherein alkyl, aryl, alkenyl and alkynyl are as defined above; saturated or unsaturated monoheterocyclic or polyheterocyclic, or fused heterocyclic, containing from 1 to 3 of any one or more of the hetero atoms N, S or O in each heterocyclic ring thereof and each such ring being from 3- to 8-membered; and mono-or poly-substituted derivatives of the above, each of said substituents being selected from the group consisting of lower alkyl, lower alkoxy, lower acyl, lower acyloxy, halo, haloloweralkyl, cyano, carbethoxy, loweralkylthio, amino, nitro, loweralkylamino, diloweralkylamino, carboxyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl and ##STR2## wherein R.sup.4 is hydrogen or alkyl having from 1 to 10 carbons; R.sup.3 is hydrogen, R.sup.2, lower acyl, cyano, haloloweralkyl, carbamyl, loweralkylcarbamyl, diloweralkylcarbamyl, --CH.sub.2 ONO.sub.2 and --CH.sub.2 OCOR.sup.2 ; R.sup.5 is hydrogen or lower alkyl; (ii) the structural formula (II): ##STR3## wherein X, R.sup.2 and R.sup.3 are as defined above and R.sup.1 is the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine; (iii) either of the structural formulae (I) or (II) wherein ##STR4## is the residue of any naturally occurring protein amino acid, the residue of any N-substituted naturally occurring amino acid, which N-substituent is lower alkyl or any amino acid protective group cleavable via hydrogenolysis or hydrolysis, or the residue of an N, N-lower dialkyl or C.sub.4 -C.sub.7 cycloalkylamino acid; and (iv) the non-toxic, pharmaceutically acceptable salts thereof.
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公开(公告)号：US4677131A
公开(公告)日：1987-06-30
申请号：US793816
申请日：1985-11-01
申请人： Takeru Higuchi , Stefano A. Pogany
发明人： Takeru Higuchi , Stefano A. Pogany
IPC分类号： C07D233/34 , A61K47/22 , C07D233/32 , C07D233/70 , A61K31/415 , C07D233/30
CPC分类号： A61K9/0014 , A61K47/22 , C07D233/32 , C07D233/70
摘要： Certain novel cyclic ureas are disclosed herein as dermal penetration enhancers of drug absorption. Also disclosed herein are compositions, methods of treatment and processes for preparing said cyclic urea compounds.
摘要翻译： 本文公开了某些新颖的环脲类作为药物吸收的皮肤渗透增强剂。 本文还公开了组合物，处理方法和制备所述环状脲化合物的方法。
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6.发明授权Bioerodible poly(ortho ester) thermoplastic elastomer from diketene diacetal 失效来自双烯酮二缩醛的生物可腐蚀的聚（原酸酯）热塑性弹性体
公开(公告)号：US4549010A
公开(公告)日：1985-10-22
申请号：US625166
申请日：1984-06-27
CPC分类号： C08G65/34
摘要： The instant invention is directed to a bioerodible poly(ortho ester) thermoplastic elastomer prepared from:(A) a diketene diacetal;(B) a long-chain non-polar, flexible diol containing 4 to 22 carbon atoms; and(C) a diol selected from the group consisting of:(i) diols containing at least one functional group which produces hydrogen bonding or other association, and(ii) rigid symmetrical diols.
摘要翻译： 本发明涉及由以下物质制备的生物可腐蚀的聚（原酸酯）热塑性弹性体：（A）双烯酮二缩醛; （B）含有4-22个碳原子的长链非极性柔性二醇; 和（C）选自以下的二醇的二醇：（i）含有至少一个产生氢键或其它缔合的官能团的二醇，和（ii）刚性对称二醇。
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公开(公告)号：US5047464A
公开(公告)日：1991-09-10
申请号：US409908
申请日：1989-09-20
CPC分类号： C08G65/34 , A61K9/204 , A61K9/2072
摘要： Bioerodible, thermoset, covalently crosslinked, elastomeric poly(ortho ester)s are disclosed. These materials are comprised of polymer chains that are interlocked in a covalent, three dimensional network which imparts dimensional stability. Use of these thermoset, covalently crosslinked materials as a drug delivery device is also disclosed.
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8.发明授权Resin modulated drug delivery device for the delivery of HMG-CoA reductase inhibitor salts 失效用于递送HMG-CoA还原酶抑制剂盐的树脂调制药物递送装置
公开(公告)号：US4976967A
公开(公告)日：1990-12-11
申请号：US274172
申请日：1988-11-21
IPC分类号： A61K9/00
CPC分类号： A61K9/0004 , Y10S514/946
摘要： The instant invention relates to a drug-delivery device for the controlled release of HMG-CoA reductase inhibitor salts, as the therapeutically active ingredient, into an environment of use which comprises:(A) a core composition comprising(1) a water insoluble, non-diffusible, charged resin entity, and(2) a diffusible, water soluble ionizable therapeutically active HMG-CoA reductase inhibitor salt carrying the same charge as said resin entity; and(B) an imperforate water insoluble wall surrounding said core composition and prepared from a semipermeable material substantially impermeable to core composition and permeable to the passage of an external fluid in the environment of use, with said wall having a means for release of the therapeutic agent through the water insoluble wall; or(C) a water insoluble wall surrounding said core composition and prepared from (1) a polymer material that is permeable to water but substantially impermeable to solute and (2) 0.1 to 75% by weight, based on the total weight of (1) and (2), of at least one water leachable pore forming additive dispersed throughout said wall.
摘要翻译： 本发明涉及用于将HMG-CoA还原酶抑制剂盐作为治疗活性成分控制释放到使用环境中的药物递送装置，其包含：（A）核心组合物，其包含（1）水不溶性， 非扩散性带电树脂实体，和（2）与所述树脂实体携带相同电荷的可扩散的水溶性可离子化治疗活性HMG-CoA还原酶抑制剂盐; 和（B）围绕所述芯组合物的无孔水不溶性壁，并由基本上不渗透核心组成并且可渗透外部流体在使用环境中的半透性材料制备，所述壁具有释放治疗剂的手段 药剂通过水不溶性壁; 或（C）围绕所述芯组合物的水不溶性壁，其由（1）可渗透水但基本上不可渗透的聚合物材料制成，并且（2）基于（1）的总重量为0.1〜75重量％ ）和（2），分散在整个所述壁上的至少一种可浸出的成孔添加剂。
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公开(公告)号：US4530928A
公开(公告)日：1985-07-23
申请号：US451314
申请日：1982-12-22
申请人： John L. Haslam , Stefano A. Pogany
发明人： John L. Haslam , Stefano A. Pogany
IPC分类号： C07D215/56 , A61K31/495 , C07D401/02
CPC分类号： C07D215/56
摘要： This invention involves complexes of quinoline carboxylic acid derivatives with guanidine and guanidine carbonate. The complexes have a greater solubility and dissolution rate when compared to the parent quinoline carboxylic acid derivatives and thus are more effective anti bacterials than the parent acids.
摘要翻译： 本发明涉及喹啉羧酸衍生物与胍和碳酸胍的配合物。 当与母体喹啉羧酸衍生物相比时，络合物具有更大的溶解度和溶解速率，因此比母体酸更有效的抗细菌。
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公开(公告)号：US20130150330A1
公开(公告)日：2013-06-13
申请号：US13495772
申请日：2012-06-13
IPC分类号： A61K31/675 , A61K45/06 , C07F9/60
CPC分类号： A61K31/675 , A61K45/06 , C07F9/60
摘要： A compound can include a structure having decoquinate coupled to a prodrug moiety, or derivative or isomer or pharmaceutically acceptable salt thereof. The compound can be a decoquinate prodrug. The decoquinate prodrug can have a structure of any of the formulae described herein. The decoquinate prodrug can be synthesized in any manner, such as a synthetic method that includes Scheme 1A or Scheme 1B and Schemes 2, 3, and/or 4. The decoquinate prodrug can be prepared into a pharmaceutical composition with a pharmaceutically acceptable carrier, such as an aqueous composition. The decoquinate prodrug can be used for inhibiting or treating a parasitic infection, such as a malarial infection or a coccidian infection.
摘要翻译： 化合物可以包括具有与前药部分偶联的decoquinate或其衍生物或异构体或其药学上可接受的盐的结构。 该化合物可以是癸酸前药。 癸酸前药可以具有本文所述任何式的结构。 癸酸前药可以以任何方式合成，例如合成方法，包括方案1A或方案1B以及方案2,3和。4.癸酸前药可以制备成具有药学上可接受的载体的药物组合物，例如 作为水性组合物。 癸酸前药可用于抑制或治疗诸如疟疾感染或球虫感染的寄生虫感染。
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