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公开(公告)号：US5001115A
公开(公告)日：1991-03-19
申请号：US352919
申请日：1989-05-17
申请人： Kenneth B. Sloan
发明人： Kenneth B. Sloan
IPC分类号： A61K45/08 , C07D207/40 , C07D207/404 , C07D207/416 , C07D207/42 , C07D209/48 , C07D275/06 , C07D417/12
CPC分类号： C07D207/404 , A61K47/4813 , C07D207/416 , C07D207/42 , C07D209/48 , C07D275/06 , C07D417/12
摘要： Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.
摘要翻译： 具有以下结构式的生物活性羟基芳族药物的前药：生物活性的治疗有效的羟基芳族药物的药学上可接受的前药，所述前药选自：（A）具有以下结构式的化合物：DRUG-O-CR R“Z] n其中：DRUG -O-是所述药物的羟基芳族O-脱氢残基; R'和R'可以相同或不同，可以是H，烷基，芳基或吸电子基团; Z是可置换的离去基团; 和n是1至3的整数，和（B）其药学上可接受的盐。
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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：US4117232A
公开(公告)日：1978-09-26
申请号：US777074
申请日：1977-03-14
申请人： Nicolae S. Bodor , Kenneth B. Sloan
发明人： Nicolae S. Bodor , Kenneth B. Sloan
IPC分类号： C07D231/34
CPC分类号： C07D231/34
摘要： Novel, transient pro-drug forms of the anti-inflammatories phenylbutazone and oxyphenbutazone are disclosed, the same having the structural formulae: ##STR1## wherein R is a member selected from the group consisting of C.sub.1 -C.sub.2 alkylsulfonyl, phenylsulfonyl, p-tolylsulfonyl and naphthylsulfonyl, and ##STR2## wherein X and Y each represent a member selected from the group consisting of a hydrogen atom and ##STR3## with the proviso that either X or Y is a hydrogen atom, R.sub.1 is selected from the group consisting of C.sub.1 -C.sub.2 alkylsulfonyl, phenylsulfonyl, p-tolylsulfonyl and naphthylsulfonyl, and R.sub.2 is selected from the group consisting of straight or branched chain C.sub.1 -C.sub.5 alkyl and phenyl.
摘要翻译： 公开了化合物1,2-二苯基-3,5-二氟乙酰氧基-4-丁基-5-羟基-3-吡唑啉作为制备所选择的保泰松酮衍生物的中间体。
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公开(公告)号：US4061753A
公开(公告)日：1977-12-06
申请号：US655786
申请日：1976-02-06
申请人： Nicolae S. Bodor , Kenneth B. Sloan
发明人： Nicolae S. Bodor , Kenneth B. Sloan
IPC分类号： C07D473/06 , C07D473/08 , A61K31/52
CPC分类号： C07D473/08 , C07D473/06 , Y02P20/55 , Y10S514/863
摘要： Compounds of the formula: ##STR1## wherein R, which may be the same or different, represents a member selected from the group consisting of --CH.sub.3, --C.sub.2 H.sub.5, --C.sub.3 H.sub.7, iso--C.sub.3 H.sub.7, --C.sub.4 H.sub.9, iso--C.sub.4 H.sub.9, pentyl, benzyl, allyl, 2-hydroxyethyl, cyclohexyl, 2-isobutenyl, hydroxymethyl, 2-phenylethyl and -CH.sub.2 O-R.sub.2, wherein R.sub.2 is defined infra; wherein R.sub.1 represents a member selected from the group consisting of H, C.sub.1 -C.sub.7 straight or branched alkyl, CCl.sub.3, CBr.sub.3, CI.sub.3, ##STR2## CH.sub.3 O--CH.sub.2 --, (CH.sub.3).sub.2 NCH.sub.2 --, ##STR3## wherein R.sub.3 represents a member selected from the group consisting of -OH, halogen (Cl, Br, I), --OCH.sub.3, -COOCH.sub.3, -NO.sub.2 and -OCOCH.sub.3 ; wherein ##STR4## and wherein R.sub.2 represents a member selected from the group consisting of ##STR5## wherein R.sub.4 is a member selected from the group consisting of C.sub.2 -C.sub.20 straight or branched alkyl (C.sub.3 -C.sub.7 preferred), --[--(CH.sub.2).sub.m --], wherein m represents an integer of from 0 to 10, ##STR6## wherein R.sub.3 is defined as above, ##STR7## the residue of any naturally occurring amino acid, the residue of any N- substituted amino acid, wherein said substituent is any amino acid protective group cleavable via hydrogenolysis or hydrolysis (e.g., formyl, benzyloxy, carbonyl, t-butyloxycarbonyl), the residue of an N,N-C.sub.1 -C.sub.5 -dialkyl or cycloalkylamino acid, ##STR8## wherein n represents an integer of from 1-5 and R.sub.5 and R.sub.6 which may be the same or different represent C.sub.1 -C.sub.5 alkyl or together form a heterocyclic ring with the N atom to which they are attached (e.g., pyrolidine, piperidine, morpholine, piperazine, imidazoline, thiazolidine, isoxazolidine), imidazolyl, O-C.sub.1 -C.sub.8 alkyl, O-benzyl, O-phenyl and ##STR9## wherein n, R.sub.5 and R.sub.6 are defined as above; and wherein R.sup.2 further represents a member selected from the group consisting of straight or branched C.sub.1 -C.sub.20 alkyl, ##STR10## wherein n, R.sub.5 and R.sub.6 are defined as above, phenyl, tolyl, xylyl, and --SO.sub.2 --R.sub.7, wherein R.sub.7 is a straight or branched C.sub.1 -C.sub.20 alkyl useful in treating psoriasis in warm-blooded animals are provided.
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公开(公告)号：US3998799A
公开(公告)日：1976-12-21
申请号：US569009
申请日：1975-04-17
IPC分类号： A61K31/195 , A61K38/00 , C07D213/55 , C07D213/56 , C07K5/06 , C07C103/52 , A61K37/00
CPC分类号： C07D213/56 , A61K31/195 , C07D213/55 , C07K5/06 , A61K38/00 , Y10S930/29
摘要： There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##STR1## wherein n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B);R represents a hydrogen atom, an acyl group, ##STR2## --CO-pyridyl, or --CO--R.sub.3, wherein R.sub.3 is the residue of any N,N-C.sub.1 -C.sub.2 dialkylamino acid or a C.sub.4 -C.sub.6 cycloalkylamino acid; R.sub.1 represents --OH, --O-lower alkyl, --O-benzyl, or a naturally occurring protein amino acid; and R.sub.2 represents ##STR3## --CO-pyridyl, a naturally occurring protein amino acid, 3',4'-L-diacyloxy phenylalanine, or --CO-R.sub.3.These compounds are all useful in the treatment of Parkinson's Disease.
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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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8.发明授权
公开(公告)号：US4279900A
公开(公告)日：1981-07-21
申请号：US61177
申请日：1979-07-27
CPC分类号： C07J33/005 , C07J71/0031 , Y10S514/887
摘要： Novel 3,2'-spiro(1',3'-thiazolidine) compounds which are transient prodrug forms of known 6- and/or 9-haloglucocorticosteroids are described. The subject prodrugs provide improved delivery of the prior art steroids for therapeutic purposes, particularly in alleviating inflammation, and can be prepared by known methods, for example, by reacting the corresponding 3-keto steroids with a thiazolidine forming reagent such as an L-cysteine alkyl ester.
摘要翻译： 描述了已知的6-和/或9-卤素糖皮质激素的瞬时前药形式的新型3,2'-螺（1'，3'-噻唑烷）化合物。 本发明的前药提供了用于治疗目的的现有技术类固醇的改进递送，特别是在减轻炎症中，并且可以通过已知方法制备，例如通过使相应的3-酮类固醇与形成噻唑烷的试剂例如L-半胱氨酸 烷基酯。
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公开(公告)号：US4169147A
公开(公告)日：1979-09-25
申请号：US840291
申请日：1977-10-07
IPC分类号： C07D231/34 , A61K31/44 , A61K31/415 , A61K31/455
CPC分类号： C07D231/34 , Y02P20/55 , Y10S514/87
摘要： There is provided, novel, transient, pro-drug forms of phenylbutazone and oxyphenbutazone having the following formula: ##STR1## wherein R represents a member selected from the group consisting of a C.sub.1 -C.sub.2 O-alkylsulfonyl group, an aryl(phenyl, p-tolyl, naphthyl)sulfonyl group, a nicotinoyl group, an iso-nicotinoyl group, a picolinoyl group, an N-protected naturally occurring amino acid residue, wherein the protective group on the amino group of the amino acid residue is removable via hydrogenolysis or hydrolysis, and an amino acid residue containing a C.sub.1 -C.sub.2 N,N-dialkylamino or a C.sub.4 -C.sub.6 cycloalkylamino group. ##STR2## wherein X and Y each represent a member selected from the group consisting of a hydrogen atom and a --OR.sub.1 group, with the proviso that either X or Y is a hydrogen atom and that R.sub.2 is a member selected from the same or different groups represented by R.sub.1 ; and wherein R.sub.1 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.2 O-alkylsulfonyl group, an aryl(phenyl, p-tolyl, naphthyl)sulfonyl group, a --CH.sub.2 COOM group, wherein M represents an alkali or alkaline earth metal (Na, K, Ca, Mg), a --CO-R.sub.3 group, wherein R.sub.3 represents a member selected from the group consisting of a straight or branched C.sub.1 -C.sub.5 alkyl group, a C.sub.1 -C.sub.2 alkoxy group, a phenyl group, a substituted phenyl group, whose substituents are selected from the group consisting of a 2,3, or 4-hydroxy group, a 2,3, or 4-acetyloxy group, and a 2,3, or 4-acetylamino group, a 2,3, or 4-pyridyl group, a 1,2, or 5-imidazolyl group, a residue of an N-protected naturally occurring amino acid, wherein the protective group on the amino group of the amino acid is removable via hydrogenolysis or hydrolysis, and an amino acid residue containing a C.sub.1 -C.sub.2 N, N-dialkylamino or C.sub.4 -C.sub.5 cycloalkylamino group. ##STR3## wherein X or Y represents a member selected from the group consisting of a hydrogen atom and a -OR.sub.1 group, wherein R.sub.1 is as defined above with the proviso that either X or Y is a hydrogen atom, wherein R.sub.4 represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, an aryl group (phenyl, styryl), a 2,3, or 4-methoxyphenyl group, and a -CH.dbd.CH.sub.2 group; and wherein R.sub.5 represents a member selected from the group consisting of a --OOC- R.sub.6 group, a ##STR4## group, and a -COOM group, wherein M represents an alkali or alkaline earth metal (Na, K, Ca, Mg), wherein R.sub.6 represents a member selected from the group consisting of R.sub.4 as defined above, with the proviso that R.sub.6 cannot be a hydrogen atom, and wherein R.sub.7 and R.sub.8 each represent a C.sub.1 -C.sub.3 alkyl group.The above-identified compounds exhibit anti-inflammatory activity in warm-blooded animals. Upon administration to warm-blooded animals, these compounds pass through the gastrointestinal tract and "cleave" in the bloodstream, thus releasing phenylbutazone or oxyphenbutazone in an anti-inflammatory effective amount at their therapeutic site or sites of activity.
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公开(公告)号：US5610160A
公开(公告)日：1997-03-11
申请号：US347108
申请日：1994-11-22
申请人： Kenneth B. Sloan , Howard D. Beall
发明人： Kenneth B. Sloan , Howard D. Beall
IPC分类号： A61K31/505
CPC分类号： A61K31/505
摘要： A pharmaceutical composition in unit dosage form adapted for topical administration to a human or non-human animal in need thereof comprising a pharmacologically effective amount of a prodrug of 5-fluorouracil having the formula: ##STR1## wherein R.sub.3 is bonded to C=O by a carbon-to-carbon bond and is a group such that the prodrug (1) has an enhanced delivery across topical membranes and (2) hydrolyzes after delivery to 5-fluorouracil.
摘要翻译： 适于局部施用于有需要的人或非人动物的单位剂量形式的药物组合物，其包含药理学有效量的具有下式的5-氟尿嘧啶的前体药物：其中R 3通过 碳 - 碳键，并且是使得前药（1）在局部膜上具有增强的递送和（2）在递送至5-氟尿嘧啶之后水解的基团。
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