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    Novel antimicrobial lactam-quinolones
    2.
    发明公开
    Novel antimicrobial lactam-quinolones 失效
    新型抗菌内酰胺 - 喹诺酮类

    公开(公告)号：EP0997466A1

    公开(公告)日：2000-05-03

    申请号：EP99204491.7

    申请日：1989-10-18

    申请人： PROCTER & GAMBLE PHARMACEUTICALS, INC.

    发明人： White, Ronald Eugene ,  Demuth Jr, Thomas Prosser

    IPC分类号： C07D501/20 ,  C07D499/00 ,  C07D499/88 ,  C07D401/12 ,  C07D463/16 ,  C07D477/14 ,  C07D477/20 ,  C07D503/00 ,  C07D505/00 ,  C07D513/04 ,  C07D498/04 ,  C07D487/04 ,  A61K31/546 ,  A61K31/431 ,  A61P31/04

    CPC分类号： C07D401/04 ,  C07D215/56 ,  C07D401/12 ,  C07D401/14 ,  C07D417/14 ,  C07D455/04 ,  C07D463/18 ,  C07D463/22 ,  C07D471/04 ,  C07D477/10 ,  C07D487/04 ,  C07D499/00 ,  C07D501/00 ,  C07D503/00 ,  C07D505/00 ,  C07D513/04

    摘要： Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula:
    wherein

    (1) A 1 , A 2 , A 3 , R 1 , R 4 and R 6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and
    (2) R 1 or R 3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula:
    wherein
    (3) R 10 , R 11 , R 12 , R 13 , and R 14 , together with bonds "a" and "b" form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and
    (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphono, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.

    摘要翻译： 包含与喹诺酮部分连接的含内酰胺部分的抗微生物内酰胺 - 喹诺酮化合物，其具有下式：其中（1）A1，A2，A3，R1，R4和R6通常形成多种喹诺酮，萘啶或相关环状部分中的任一种 本领域已知具有抗微生物活性; （2）R 1或R 3含有连接部分，将喹诺酮部分连接至具有下式的含内酰胺部分：其中（3）R 10，R 11，R 12，R 13和R 14连同键“a”和“b “形成本领域已知的具有抗微生物活性的各种含内酰胺部分中的任何一种; （4）连接部分包括氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异脲鎓，异硫脲鎓，胍，碳酸酯，三硫代碳酸酯，反向氨基甲酸酯，黄原酸酯，反异脲鎓，反二硫代氨基甲酸酯，反异硫脲，胺，亚胺， 杂芳基醚，醚，硫醚，膦酰基，磷酰胺，磷酸酯，磺酰胺，酯，硫酯，酰胺和酰肼基团。

    CYCLIC UREAS USEFUL AS ANTIARRHYTHMIC AND ANTIFIBRILLATORY AGENTS
    4.
    发明授权
    CYCLIC UREAS USEFUL AS ANTIARRHYTHMIC AND ANTIFIBRILLATORY AGENTS 失效
    抗心律失常及效果ANTIFIBRILLATORISCHER环脲

    公开(公告)号：EP0598046B1

    公开(公告)日：1999-03-24

    申请号：EP92917977.8

    申请日：1992-08-10

    申请人： PROCTER & GAMBLE PHARMACEUTICALS

    发明人： PELOSI, Stanford, Salvatore, Jr. ,  YU, Chia-Nien

    IPC分类号： C07D405/12 ,  A61K31/415 ,  A61K31/505 ,  A61K31/34

    CPC分类号： C07D405/12

    摘要： The novel cyclic ureas of the present invention are useful as antiarrhythmic and antifibrillatory agents and have general structure (I) wherein (a) X is a saturated or unsaturated, 5-, 6-, or 7-membered heterocycle or carbocycle; (b) R is selected from the group consisting of covalent bond, nil, heteroatom, carbonyl, heterocyclic ring, carbocyclic ring, alkyl, alkenyl, alkoxy, alkylamino, arylalkyl, aryloxy, acyl, acyloxy, and acylamino; (c) Y is a substituted or unsubstituted, saturated or unsaturated, 5-, 6-, or 7-membered heterocyclic ring or carbocyclic ring, or is nil; and wherein when R is nil, X and Y are fused ring systems; and when R is a covalent bond, X and Y are ring systems linked through a covolent bond; and when Y is nil, R is a covalent bond and X is bound to L through R; (d) R1, R2, and R3 are independently selected from the group consisting of nil, Cl, F, Br, NH2, CF3, OH, SO3H, CH3SO2NH, COOH, alkoxy, alkyl, alkoxycarbonyl, hydroxyalkyl, carboxyalkyl, aminoalkyl, acylamino, and acyloxy; (e) L is selected from the group consisting of alkylamino, alkenylamino, alkylimino, alkenylimino, and acylamino wherein the nitrogen atom thereof is bound to the nitrogen atom at the 1-position of the cyclic urea moiety; (f) R4 is selected from the group consisting of alkyl, alkenyl, alkynyl, alkylacyl, and heteroalkyl; (g) A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched, C1-C8 heteroalkyl, or a substituted or unsubstituted, saturated or unsaturated heterocycle having 5-, 6-, or 7-members; and has one nitrogen atom, which is adjacent to R4; and (h) R5 is a substituted or unsubstituted C1 or C2 alkyl; and the pharmaceutically-acceptable salts and esters thereof.

    Novel cyclic ureas useful as antiarrhythmic and antifibrillatory agents
    5.
    发明公开
    Novel cyclic ureas useful as antiarrhythmic and antifibrillatory agents 失效
    Zyklische Harnstoffe mit抗心律失常药物和抗纤维蛋白酶Wirkung

    公开(公告)号：EP0891976A1

    公开(公告)日：1999-01-20

    申请号：EP98203050.4

    申请日：1992-08-10

    申请人： PROCTER & GAMBLE PHARMACEUTICALS

    发明人： Pelosi, Stanford Salvatore, Jr. ,  Yu, Chia-Nien

    IPC分类号： C07D405/12 ,  C07D233/38 ,  A61K31/415 ,  C07D239/10 ,  A61K31/505

    CPC分类号： C07D405/12

    摘要： The novel cyclic ureas of the present invention are useful as antiarrhythmic and antifibrillatory agents and have general structure (I)
    wherein (a) X is a saturated or unsaturated, 5-, 6-, or 7-membered heterocycle or carbocycle; (b) R is selected from the group consisting of covalent bond, nil, heteroatom, carbonyl, heterocyclic ring, carbocyclic ring, alkyl, alkenyl, alkoxy, alkylamino, arylalkyl, aryloxy, acyl, acyloxy, and acylamino; (c) Y is a substituted or unsubstituted, saturated or unsaturated, 5-, 6-, or 7-membered heterocyclic ring or carbocyclic ring, or is nil; and wherein when R is nil, X and Y are fused ring systems; and when R is a covalent bond, X and Y are ring systems linked through a covalent bond; and when Y is nil, R is a covalent bond and X is bound to L through R; (d) R 1 , R 2 and R 3 are independently selected from the group consisting of nil, Cl, F, Br, NH 2 , CF 3 , OH, SO 3 H, CH 3 SO 2 NH, COOH, alkoxy, alkyl, alkoxycarbonyl, hydroxyalkyl, carboxyalkyl, aminoalkyl, acylamino, and acyloxy; (e) L is selected from the group consisting of alkylamino, alkenylamino, alkylimino, alkenylimino, and acylamino wherein the nitrogen atom thereof is bound to the nitrogen atom at the 1-position of the cyclic urea moiety; (f) R 4 is selected from the group consisting of alkyl, alkenyl, alkynyl, alkylacyl, and heteroalkyl; (g) A is a substituted or unsubstituted, saturated or unsaturated, straight-chain or branched, C 1 -C 8 heteroalkyl, or a substituted or unsubstituted, saturated or unsaturated heterocycle having 5-, 6-, or 7-members; and has one nitrogen atom, which is adjacent to R 4 ; and (h) R 5 is a substituted or unsubstituted C 2 alkylene; and pharmaceutically-acceptable salts and esters thereof.

    摘要翻译： 本发明的新型环脲可用作抗心律不齐和抗纤维化剂，并具有通式（I），其中（a）X是饱和或不饱和的，5-，6-或7-元杂环或碳环; （b）R选自共价键，无，杂原子，羰基，杂环，碳环，烷基，烯基，烷氧基，烷基氨基，芳基烷基，芳氧基，酰基，酰氧基和酰基氨基; （c）Y是取代或未取代的饱和或不饱和的5-，6-或7-元杂环或碳环，或无; 并且其中当R为零时，X和Y为稠环体系; 当R是共价键时，X和Y是通过共价键连接的环系; 当Y为零时，R为共价键，X通过R与L结合; （d）R 1，R 2和R 3独立地选自n，Cl，F，Br，NH 2，CF 3，OH，SO 3 H，CH 3 SO 2 NH，COOH，烷氧基，烷基，烷氧基羰基，羟烷基，羧基烷基，氨基烷基，酰基氨基， 和酰氧基; （e）L选自烷基氨基，烯基氨基，烷基亚氨基，烯基亚氨基和酰氨基，其中氮原子与环脲部分1位的氮原子结合; （f）R 4选自烷基，烯基，炔基，烷基酰基和杂烷基; （g）A是具有5-，6-或7-成员的取代或未取代的饱和或不饱和的直链或支链C 1 -C 8杂烷基或取代或未取代的饱和或不饱和杂环; 并具有与R4相邻的一个氮原子; 和（h）R 5是取代或未取代的C 2亚烷基; 及其药学上可接受的盐和酯。

    PROCESS FOR MAKING ANTIMICROBIAL QUINOLONYL LACTAMS
    6.
    发明授权
    PROCESS FOR MAKING ANTIMICROBIAL QUINOLONYL LACTAMS 失效
    用于生产抗菌喹诺酮内酰胺

    公开(公告)号：EP0606336B1

    公开(公告)日：1997-03-19

    申请号：EP92920743.9

    申请日：1992-09-28

    申请人： PROCTER & GAMBLE PHARMACEUTICALS, INC.

    发明人： WHITE, Ronald, Eugene ,  DEMUTH, Thomas, Prosser, Jr.

    IPC分类号： C07D499/883 ,  C07D477/14 ,  C07D463/22 ,  C07D505/24 ,  C07D519/06

    CPC分类号： C07D505/00 ,  C07D477/02 ,  C07D499/88 ,  Y02P20/55

    摘要： The present invention provides methods of making compounds of the structure [Q - L1] - L - [L2 - B], wherein Q is a quinolone moiety; B is a beta-lactam moiety; L, L?1, and L2¿ together comprise a carbamate-containing linking moiety, comprising the steps of: 1) reacting a lactam compound of the formula B-L4-H with phosgene to form an intermediate compound of the formula B-L4-C(=O)-Cl, where L4 is oxygen; and 2) coupling said intermediate compound with a quinolone compound of the formula Q-l3-R44, wherein L3 is nitrogen; R44 is hydrogen, Si(R45)3, or Sn(R45)3; and R45 is lower alkyl. Preferably, the process additionally comprises steps prior to the reacting and coupling steps where esters of the lactam and quinolone compounds are made. Also preferably, the coupling step comprises adding a solution containing the quinolone compound to a solution containing the intermediate compound. The process steps are also preferably performed at a temperature of from about -80 °C to about 0 °C. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem.

    USE OF PHOSPHONATES FOR THE TREATMENT OF OSTEOPOROSIS
    7.
    发明公开
    USE OF PHOSPHONATES FOR THE TREATMENT OF OSTEOPOROSIS 无效
    膦酸盐骨质疏松症的治疗。

    公开(公告)号：EP0648120A1

    公开(公告)日：1995-04-19

    申请号：EP93914339.0

    申请日：1993-06-04

    申请人： PROCTER & GAMBLE PHARMACEUTICALS, INC.

    发明人： FRANCIS, Marion, David ,  BOYCE, Rogely, Waite

    IPC分类号： A61K31 ,  A61P3 ,  A61P19 ,  A61P43 ,  C07F9

    CPC分类号： A61K31/675 ,  A61K31/66 ,  C07F9/582 ,  C07F9/592

    摘要： A method of increasing bone mass in a human or other mammal subject afflicted with osteoporosis, comprising a thirty (30) day treatment period, comprised of a high potency phosphonate compound administration regimen wherein a) said high potency phosphonate administration regimen comprises the systemic administration to said subject of a high potency phosphonate compound at a level of from 0.00001 mgP/kg to 0.1 mgP/kg per day that said high potency phosphonate compound is administered, provided that said high potency phosphonate compound is administered at least one day of every said thirty (30) day treatment period; and wherein b) said thirty (30) day treatment period may be followed by a rest period of at least one day.

    Composition à activité anti-agrégante plaquettaire utilisable en thérapeutique
    9.
    发明公开
    Composition à activité anti-agrégante plaquettaire utilisable en thérapeutique 失效
    In der Therapeutik anwendbare Zusammensetzung mit aggregationshemmender Wirkung aufBlutplättchen。

    公开(公告)号：EP0387140A1

    公开(公告)日：1990-09-12

    申请号：EP90400605.3

    申请日：1990-03-06

    申请人： PROCTER & GAMBLE PHARMACEUTICALS FRANCE

    发明人： Covarrubias, Jésus

    IPC分类号： A61K31/615 ,  A61K31/60

    CPC分类号： A61K31/621 ,  A61K31/60 ,  A61K31/185 ,  A61K2300/00

    摘要： L'invention concerne une composition à base d'acide acétylsalicylique et de taurine, ou de leurs sels respectifs, combinés dans un rapport en poids compris entre 1/5 et 1/50, associés le cas échéant à un ou plusieurs excipients.
    La composition est utilisable en thérapeutique pour le traitement des thromboses artérielles et artériolaires.

    摘要翻译： 本发明涉及一种牛磺酸和乙酰基水杨酸类组合物或其相应的盐，其重量比为1/5至1/50，与一种或几种赋形剂相关。 该组合物可用于治疗动脉和小动脉血栓形成。