Aminoalkylenephosphonates for treatment of bone disorders
    1.
    发明授权
    Aminoalkylenephosphonates for treatment of bone disorders 失效
    用于治疗骨骼疾病的氨基亚烷基膦酸盐

    公开(公告)号:US06794371B1

    公开(公告)日:2004-09-21

    申请号:US10088884

    申请日:2002-03-21

    申请人: R. Keith Frank

    发明人: R. Keith Frank

    IPC分类号: A61K31675

    摘要: A method for preventing loss of bone mineral in mammals which method comprises administering to a mammal an amount of an aminoalkylenephosphonate which is effective to prevent or minimize loss of bone material density. The aminoalkylenephophonates of the present invention should have at least one R-N(Alk-PO3H2)2 group or at least two RRN-Alk-PO3H2 groups wherein R and R can be, same or different, aliphatic or cyclic moiety, and Alk is an alkylene group having from 1 to 4 carbon atoms.

    摘要翻译: 一种用于防止哺乳动物骨矿物质损失的方法,该方法包括向哺乳动物施用一定量的有效预防或最小化骨材料密度损失的氨基亚烷基膦酸盐。 本发明的氨基亚烷基突磷酸盐应具有至少一个RN(Alk-PO3H2)2基团或至少两个RRN-Alk-PO3H2基团,其中R和R可以相同或不同,为脂族或环状部分,Alk为亚烷基 具有1至4个碳原子的基团。

    Process for increasing the egg production and strengthening the eggshells of poultry
    2.
    发明授权
    Process for increasing the egg production and strengthening the eggshells of poultry 失效
    增加鸡蛋生产和加强家禽蛋壳的过程

    公开(公告)号:US06649601B2

    公开(公告)日:2003-11-18

    申请号:US09506032

    申请日:2000-02-17

    IPC分类号: A61K31675

    CPC分类号: A61K31/663

    摘要: The present invention relates to a process for increasing the egg production and strengthening the eggshells of poultry, which comprises the administration to the animal of at least one bisphosphonic compound chosen from a bisphosphonic acid, a physiologically acceptable salt thereof, hydrates thereof and mixtures thereof.

    摘要翻译: 本发明涉及增加鸡蛋生产和加强家禽蛋壳的方法,其包括向动物施用选自双膦酸,其生理学上可接受的盐,其水合物及其混合物的至少一种双膦酸化合物。

    Method of modulating NF-kB activity
    3.
    发明授权
    Method of modulating NF-kB activity 失效
    调节NF-kB活性的方法

    公开(公告)号:US06642215B2

    公开(公告)日:2003-11-04

    申请号:US10153800

    申请日:2002-05-24

    IPC分类号: A61K31675

    CPC分类号: C07D213/89 C07D401/12

    摘要: A method of modulating the level of activated, NF-&kgr;B in cells by contacting cells with a cyanoguanidine compound of general formula I wherein n is 0, 1 or 2; each R independently represents halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, cyano, amino, sulfo or carboxy groups; Q is a straight or branched, saturated or unsaturated C4-20 divalent hydrocarbon radical; X is a bond, O, S, amino, carbonyl, carbonylamino, aminocarbonyl, oxycarbonyloxy, oxycarbonyl, carbonyloxy, aminocarbonyloxy, aminothiocarbonyloxy, oxycarbonylamino or oxythiocarbonylamino; A is di-(C1-4 alkoxy)phosphinoyloxy, C1-4 alkoxycarbonyl, C1-4 alkoxycarbonylamino, saturated or unsaturated C3-12 carbocyclic ring or C3-12 heterocarbocyclic ring optionally substituted with one or more R1; R1 being independently selected from the group consisting of halogen, trifluoromethyl, hydroxy, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxycarbonyl, nitro, cyano, amino, carboxy, sulfo, carboxamido, sulfamoyl or C1-4 hydroxyalkyl; or a pharmaceutically acceptable salt, N-oxide or N-substituted prodrug thereof, in an amount effective to modulate the activity of IKK.

    摘要翻译: 通过使细胞与通式I的氰基胍化合物接触,调节细胞中活化的NF-κB的水平的方法,其中n为0,1或2;每个R独立地表示卤素,三氟甲基,羟基,C 1-4烷基,C 1-4 烷氧基,C 1-4烷氧基羰基,硝基,氰基,氨基,磺基或羧基; Q是直链或支链饱和或不饱和的C 4-20二价烃基; X是键,O,S,氨基,羰基,羰基氨基, 氨基羰基,氧羰基氧基,氧羰基,羰氧基,氨基羰基氧基,氨基硫代羰氧基,氧羰基氨基或氧硫代羰基氨基; A是二 - (C1-4烷氧基)膦酰氧基,C1-4烷氧基羰基,C1-4烷氧基羰基氨基,饱和或不饱和C3-12碳环或C3-12 任选被一个或多个R 1取代的杂碳环; R 1独立地选自卤素,三氟甲基,羟基,C 1-4烷基,C 1-4烷氧基,C 1-4烷氧基羰基,硝基,氰基,氨基,羧基,磺基,甲酰氨基,氨磺酰基或C 1-4羟基烷基;或 其药学上可接受的盐,N-氧化物或N-取代的前药,其量有效调节IKK的活性。

    Dosage forms of risedronate
    8.
    发明授权
    Dosage forms of risedronate 有权
    利塞膦酸盐的剂型

    公开(公告)号:US06596710B1

    公开(公告)日:2003-07-22

    申请号:US09591911

    申请日:2000-06-09

    IPC分类号: A61K31675

    摘要: The present invention is directed to a novel enteric-coated oral dosage form of a risedronate active ingredient comprised of a safe and effective amount of a pharmaceutical compostion which is comprised of a risedronate active ingredient and pharmaceutically-acceptable excipients. Said dosage forms prohibit the exposure of the risedronate active ingredient to the epithelial and mucosal tissues of the buccal cavity, pharynx, esophagus, and stomach and thereby protects said tissues from erosion, ulceration or other like irritation. Accordingly, the said dosage forms effect the delivery to the lower intestinal tract of said human or other mammal of a safe and effective amount of the risedronate active ingredient, and substantially alleviate the esophagitis or esophageal irritation which sometimes accompanies the oral administration of risedronate active ingredients.

    摘要翻译: 本发明涉及由利塞膦酸酯活性成分组成的新型肠溶衣口服剂型,其包含由利塞膦酸盐活性成分和药学上可接受的赋形剂组成的安全有效量的药物组合物。 所述剂型禁止将利塞膦酸盐活性成分暴露于颊腔,咽,食管和胃的上皮和粘膜组织,从而保护所述组织免受侵蚀,溃疡或其它类似的刺激。 因此,所述剂型影响将所述人或其他哺乳动物的下肠道递送至安全有效量的利塞膦酸盐活性成分,并且基本上减轻了有时伴随利塞膦酸盐活性成分口服的食管炎或食管刺激 。

    6-amino- or 6-hydrazino-sulphonyl-3-quinolynyl-phosphonic acid compounds
    9.
    发明授权
    6-amino- or 6-hydrazino-sulphonyl-3-quinolynyl-phosphonic acid compounds 失效
    6-氨基或6-肼基磺酰基-3-喹啉基 - 膦酸化合物

    公开(公告)号:US06486143B2

    公开(公告)日:2002-11-26

    申请号:US09784632

    申请日:2001-02-15

    IPC分类号: A61K31675

    CPC分类号: C07F9/60

    摘要: The invention relates to a compound of formula (I): wherein: R1 represents halogen or a group CF3, R2 represents hydrogen or alkyl or cycloalkyl, R3 is as defined in the description, R4 and R5 represent hydrogen or alkyl, cycloalkyl, aryl or arylalkyl a group Medicaments.

    摘要翻译: 本发明涉及式(I)化合物:其中:R 1表示卤素或基团CF 3,R 2表示氢或烷基或环烷基,R 3如说明书中所定义,R 4和R 5表示氢或烷基,环烷基,芳基或 芳基烷基一个基团。

    (-)-phosphonorisperidone and (-)-sulforisperidone compositions and methods
    10.
    发明授权
    (-)-phosphonorisperidone and (-)-sulforisperidone compositions and methods 有权
    ( - ) - 膦酰哌啶酮和( - ) - 硫代赖吡酮组合物和方法

    公开(公告)号:US06326362B1

    公开(公告)日:2001-12-04

    申请号:US09700621

    申请日:2000-11-17

    申请人: William E. Yelle

    发明人: William E. Yelle

    IPC分类号: A61K31675

    CPC分类号: A61K31/505 A61K31/675

    摘要: Methods and compositions utilizing a compound represented by Formula III, wherein R is chosen from —P(O)(OH)2 and —SO3H, or pharmaceutically acceptable salts thereof, for the treatment of psychoses in humans are disclosed. The compounds of the present invention exhibit fewer side effects than risperidone, a lessened liability toward drug-drug interactions than risperidone and a more predictable dosing regimen than risperidone. The compounds of the invention are also useful for the treatment of emesis and withdrawal syndromes.

    摘要翻译: 公开了利用式III表示的化合物的方法和组合物,其中R选自-P(O)(OH)2和-SO 3 H或其药学上可接受的盐,用于治疗人类的精神病。 与利培酮相比,本发明的化合物表现出比利培酮更少的副作用,比利培酮减轻了药物相互作用的责任,而且比利培酮具有更可预测的给药方案。 本发明的化合物也可用于治疗呕吐和戒断综合征。