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1. 发明授权

EP0036534B1 An orally administrable drug form comprising a beta-lactam antibiotic and an adjuvant 有权
标题翻译：含有BETA-LACTAM抗生素和调节剂的ORALY管理药物
公开(公告)号：EP0036534B1
公开(公告)日：1987-09-23
申请号：EP81101642.7
申请日：1981-03-06
申请人： INTERx RESEARCH CORPORATION
发明人： Higuchi, Takeru , Nishihata, Toshiaki
IPC分类号： A61K31/62 , A61K31/60 , A61K31/66 , A61K31/43 , A61K31/545 , A61K45/06 , A61K47/00
CPC分类号： A61K47/20 , A61K9/2013 , A61K31/43 , A61K31/545 , A61K31/60 , A61K31/66 , A61K45/06 , A61K47/12 , A61K2300/00

2. 发明授权

EP0036145B1 An orally administered drug form comprising a polar bioactive agent and an adjuvant 有权
标题翻译：一种包含极性生物活性剂和补充剂的ORACLE管理药物
公开(公告)号：EP0036145B1
公开(公告)日：1985-05-29
申请号：EP81101644.3
申请日：1981-03-06
申请人： INTERx RESEARCH CORPORATION
发明人： Higuchi, Takeru , Nishihata, Toshiaki
IPC分类号： A61K31/62 , A61K31/60 , A61K31/66 , A61K31/52 , A61K31/71 , A61K45/06 , A61K47/00
CPC分类号： A61K31/70 , A61K9/2013 , A61K31/52 , A61K31/60 , A61K31/66 , A61K45/06 , A61K47/12 , A61K47/20 , Y10S930/27 , A61K2300/00

3. 发明公开

EP0046270A1 Novel derivatives of bio-affecting phenolic compounds and pharmaceutical composition containing them 有权
标题翻译：引导冯生物生物化学（Phenolverbindungen und diese enthaltende pharmazeutische Komposition）。
公开(公告)号：EP0046270A1
公开(公告)日：1982-02-24
申请号：EP81106277.7
申请日：1981-08-12
申请人： INTERx RESEARCH CORPORATION
发明人： Bodor, Nicholas S. , Sloan, Kenneth B. , Pogany, Stefano A.
IPC分类号： C07C103/78 , C07C93/26 , C07C69/24 , C07C153/07 , C07C69/28
CPC分类号： C07C327/00
摘要： Novel transient prodrug forms of bio-affecting phenolic compounds are selected from the group consisting of those having the structural formula (I):
wherein X is O, S or NR 5 wherein R 5 is hydrogen or lower alkyl; R 1 is the mono- or polydehydroxylated residue of a non-steroidal bio-affecting phenol, with the proviso that R' is other than a monohydroxylated or didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine; R 2 is selected from the group consisting of straight or branched chain alkyl, aryl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aralkyl, alkaryl, aralkenyl, aralkynyl, alkenylaryl, alkynylaryl, (lower acyloxy)alkyl, and carboxyalkyl; 3- to 8-membered, saturated or unsaturated mono-heterocyclic or polyheterocyclic containing from 1 to 3 of any one or more of the heteroatoms N, S or O; and mono- or polysubstituted derivatives of the above; R 3 is hydrogen, lower acyl, cyano, halo(lower alkyl), carbamyl, lower alkylcarbamyl, di(lower alkyl)carbamyl, CH 2 ONO 2 , -CH 2 OCOR 2 or any non-heterocyclic member of the group defined by R 2 above; and n is at least one and equals the total number of phenolic hydroxyl functions comprising the non-steroidal bioaffecting phenol etherified via a R2COXCH(R3)0-moiety; those having the structural formula (II):
wherein X, R', R 2 and R 3 are as defined above, and n and m are each at least one and the sum of n+m equals the total number of phenolic hydroxyl functions comprising the non-steroidal bioaffecting phenol either etherified via a R 2 COXCH(R 3 )0-moiety or esterified via a R 2 COO-moiety; and the pharmaceutically acceptable acid addition salts, quaternary ammonium salts and N-oxides thereof.
摘要翻译：生物影响酚类化合物的新型瞬时前药形式选自具有结构式（I）的那些：其中X是O，S或NR 5，其中R 5是氢或低级烷基 ; R 1是非甾体生物影响性苯酚的单或多羟基化残基，条件是R 1不是酚，核二羟基天然交感神经或拟交配胺的单羟基化或二脱羟基化残基; R 2选自直链或支链烷基，芳基，环烷基，烯基，环烯基，炔基，芳烷基，烷芳基，芳烯基，芳炔基，烯基芳基，炔基芳基，（低级酰氧基）烷基和羧基烷基。含有1至3个任何一个或多个杂原子N，S或O的3-至8-元饱和或不饱和单杂环或多杂环，以及上述的一或多取代的衍生物; R 3是氢，低级酰基，氰基，卤代（低级烷基），氨基甲酰基，低级烷基氨基甲酰基，二（低级烷基）氨基甲酰基，CH 2 ONO 2，-CH 2 OCOR 2或由R 1定义的基团的任何非杂环成员， 2>以上; 并且n是至少一个，并且等于包含通过R 2 COXCH（R 3）O-部分醚化的非甾体生物影响苯酚的酚羟基官能团的总数; 具有结构式（II）的化合物：其中X，R 1，R 2和R 3如上所定义，并且n和m各自为至少一个，并且n + m 等于包含通过R 2 COXCH（R 3） - 部分醚化或通过R 2 COO部分酯化的非甾体生物影响苯酚的酚羟基官能团的总数; 和其药学上可接受的酸加成盐，季铵盐和N-氧化物。

4. 发明授权

EP0035770B1 AN ORALLY ADMINISTERED DRUG FORM COMPRISING A GLYCOSIDIC ANTIBIOTIC AND AN ADJUVANT 有权
标题翻译：一种包含糖尿病抗生素和调节剂的口服药物
公开(公告)号：EP0035770B1
公开(公告)日：1986-12-30
申请号：EP81101645
申请日：1981-03-06
申请人： INTERX RESEARCH CORPORATION
发明人： HIGUCHI, TAKERU , NISHIHATA, TOSHIAKI
IPC分类号： A61K9/20 , A61K9/28 , A61K9/48 , A61K45/06 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/16 , A61K47/18 , A61P31/04 , A61K31/71 , A61K31/73
CPC分类号： A61K9/4858 , A61K9/2013 , A61K9/2866 , A61K9/2886 , A61K9/4891 , A61K31/70 , A61K45/06 , A61K47/12 , A61K47/14 , A61K47/18

5. 发明公开

EP0036426A1 NOVEL PROCESS AND INTERMEDIATES USEFUL IN THE PREPARATION OF SYMPATHOMIMETIC AMINES 失效
标题翻译：新工艺，用以进行拟交感胺类的中间产品生产。
公开(公告)号：EP0036426A1
公开(公告)日：1981-09-30
申请号：EP80902012.0
申请日：1980-09-24
申请人： INTERx RESEARCH CORPORATION
发明人： ZUPAN, Jacob A.
IPC分类号： C07C271 , C07C67 , C07C239 , C07C309
CPC分类号： C07C271/06 , C07C309/63 , Y02P20/55
摘要： Nouveaux procedes et nouveaux produits intermediaires utiles dans la preparation d'amines sympathomimetiques. Les produits finals utiles en pharmacologie, qui sont des derives acyles d'amines aromatiques mono- et di-hydroxy (p. ex. des amines catecholes) peuvent etre prepares sous forme racemiques ou optiquement actives en faisant reagir l'amine aromatique de mono- ou di-hydroxy correspondante avec un agent de reaction capable de former son derive N-tertio-butoxycarbonyle; en faisant reagir le nouvel intermediaire ainsi obtenu avec un chlorure d'acyloxymethyle pour obtenir l'amine aromatique correspondante nouvelle N-mono ou diacylee; puis en extrayant le groupe de protection N.

6. 发明公开

EP0036145A1 An orally administered drug form comprising a polar bioactive agent and an adjuvant 有权
标题翻译：药物制剂用于与极性生物活性剂和佐剂的含量经口给药。
公开(公告)号：EP0036145A1
公开(公告)日：1981-09-23
申请号：EP81101644.3
申请日：1981-03-06
申请人： INTERx RESEARCH CORPORATION
发明人： Higuchi, Takeru , Nishihata, Toshiaki
IPC分类号： A61K31/62 , A61K31/60 , A61K31/66 , A61K31/52 , A61K31/71 , A61K45/06 , A61K47/00
CPC分类号： A61K31/70 , A61K9/2013 , A61K31/52 , A61K31/60 , A61K31/66 , A61K45/06 , A61K47/12 , A61K47/20 , Y10S930/27 , A61K2300/00
摘要： A drug form is provided for increasing the oral absorption of polar bioactive agents such as xanthines, polyhydroxylic substances, zwitterions, polypeptides and organic anions and related chemical species by the oral administration of said polar bioactive agents in a suitable pharmaceutically accepted excipientto which has been added a hydroxyaromatic, hydroxyaryl or hydroxy aralkyl acid or salt amide or ester thereof. The hydroxy aryl or hydroxy aralkyl acid or salt amide or ester thereof is present in the drug form in quantities suffi- cientto be effective in enhancing the rate of oral absorption of the polar bioactive agents.
摘要翻译：提供了用于增加极性的生物活性剂的口服吸收的药物形式：如黄嘌呤，多羟基物质，两性离子，多肽和有机阴离子和相关的化学物质通过所述极性的生物活性剂的口服给药在合适的药学上可接受的赋形剂，以一直哪加入羟基，羟基芳基或羟基芳烷基的酸或盐的酰胺或酯。所述羟基芳基或羟基芳烷基酸或其盐酰胺或其酯的存在的量足以能有效地提高极性的生物活性剂的口服吸收率的药物形式。

7. 发明公开

EP0036534A1 An orally administrable drug form comprising a beta-lactam antibiotic and an adjuvant 有权
标题翻译：用于口服给药的药物制剂与β-内酰胺抗生素和佐剂的内容。
公开(公告)号：EP0036534A1
公开(公告)日：1981-09-30
申请号：EP81101642.7
申请日：1981-03-06
申请人： INTERx RESEARCH CORPORATION
发明人： Higuchi, Takeru , Nishihata, Toshiaki
IPC分类号： A61K31/62 , A61K31/60 , A61K31/66 , A61K31/43 , A61K31/545 , A61K45/06 , A61K47/00
CPC分类号： A61K47/20 , A61K9/2013 , A61K31/43 , A61K31/545 , A61K31/60 , A61K31/66 , A61K45/06 , A61K47/12 , A61K2300/00
摘要： A drug form is provided for increasing the oral absorption of β-lactam antibiotics such as the penicillins, cephalosporins and related chemical species by the oral administration of said β-lactam antibiotics in a suitable pharmaceutically accepted excipient to which has been added a hydroxy aryl or hydroxy aralkyl acid or salt, amide or ester thereof. The hydroxyaryl or hydroxyaralkyl acid or salt, amide or ester thereof is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of the β-lactam antibiotic.
摘要翻译：提供了用于提高的β-内酰胺抗生素的口服吸收的药物形式：如青霉素，头孢菌素和相关的化学物质通过的β-内酰胺抗生素的口服给药在接受赋形剂的合适的药学据说已加入一个羟基的芳基或羟基芳酸或盐，酰胺或酯。所述羟基芳基或羟基芳烷基酸或盐，酰胺或酯的存在的量足以能有效地增强β-内酰胺抗生素的口服吸收率的药物形式。

8. 发明公开

EP0035770A3 An orally administered drug form comprising a glycosidic or related antibiotic and an adjuvant 有权
标题翻译：一种包含糖皮质激素或相关抗生素和调节剂的口服药物
公开(公告)号：EP0035770A3
公开(公告)日：1981-09-23
申请号：EP81101645
申请日：1981-03-06
申请人： INTERx RESEARCH CORPORATION
发明人： Higuchi, Takeru , Nishihata, Toshiaki
IPC分类号： A61K31/71 , A61K31/73 , A61K45/06 , A61K47/00 , A61K31/66 , A61K31/60 , A61K31/19
CPC分类号： A61K9/4858 , A61K9/2013 , A61K9/2866 , A61K9/2886 , A61K9/4891 , A61K31/70 , A61K45/06 , A61K47/12 , A61K47/14 , A61K47/18
摘要： A drug form is provided for increasing the oral absorption of glycosidic and related antibiotics such as marcrolide, aminoglycoside, lincomycin and anthracycline antibiotics and related chemical species by the oral administration of said glycosidic and related antibiotics in a suitable pharmaceutically accepted excipient to which has been added a hydroxyaryl or hydroxyaralkyl acid or salt amide or ester thereof. The hydroxyaryl, a hydroxyaralkyl or salt amide or ester thereof is present in the drug form in quantities sufficient to be effective in enhancing the rate of oral absorption of glycosidic and related antibiotic.

9. 发明授权

EP0046270B1 Novel derivatives of bio-affecting phenolic compounds and pharmaceutical composition containing them 有权
标题翻译：生物影响酚醛化合物的新型衍生物和含有它们的药物组合物
公开(公告)号：EP0046270B1
公开(公告)日：1986-05-21
申请号：EP81106277.7
申请日：1981-08-12
申请人： INTERx RESEARCH CORPORATION
发明人： Bodor, Nicholas S. , Sloan, Kenneth B. , Pogany, Stefano A.
IPC分类号： C07C103/78 , C07C93/26 , C07C69/24 , C07C153/07 , C07C69/28
CPC分类号： C07C327/00

10. 发明授权

EP0036426B1 NOVEL PROCESS AND INTERMEDIATES USEFUL IN THE PREPARATION OF SYMPATHOMIMETIC AMINES 失效
标题翻译：新方法和中间体在制备对称性氨基酸中的应用
公开(公告)号：EP0036426B1
公开(公告)日：1986-04-23
申请号：EP80902012.6
申请日：1980-09-24
申请人： INTERx RESEARCH CORPORATION
发明人： ZUPAN, Jacob A.
IPC分类号： C07D307/62 , C07C143/68 , C07D401/12 , C07D213/79 , C07D213/80 , C07D213/46 , C07C69/75 , C07C125/065 , C07C101/62 , C07C69/78 , C07C69/035
CPC分类号： C07C271/06 , C07C309/63 , Y02P20/55
摘要： Novel process and novel intermediates useful in the preparation of sympathomimetic amines. The pharmacologically useful final products, which are acyl derivatives of mono- and dihydroxy aromatic amines (e.g., catechol amines) can be prepared in optically active or racemic form by reacting the corresponding mono- or dihydroxy aromatic amine with a reagent capable of forming the N-tert-butoxycarbonyl derivative thereof; reacting the novel intermediate thus obtained with an acyloxymethyl chloride to afford the corresponding novel mono- or diacylated N-protecting aromatic amine; and removing the N-protecting group therefrom.

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