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    Amorphous paroxetine composition
    1.
    发明授权
    Amorphous paroxetine composition 失效
    无定形帕罗西汀组成

    公开(公告)号：US5672612A

    公开(公告)日：1997-09-30

    申请号：US708802

    申请日：1996-09-09

    申请人： Bruce Ronsen ,  Ragab El-Rashidy

    发明人： Bruce Ronsen ,  Ragab El-Rashidy

    IPC分类号： C07D405/12 ,  A61K31/435 ,  A61K31/4525 ,  A61P15/10 ,  C07D401/12 ,  A61K31/44

    CPC分类号： C07D401/12 ,  A61K31/4525

    摘要： A free-flowing, amorphous paroxetine hydrochloride-ethanol composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. In a preferred embodiment, the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.

    摘要翻译： 适合作为早泄治疗剂的自由流动的无定形帕罗西汀盐酸盐 - 乙醇组合物可以通过将帕罗西汀游离碱溶解在盐酸 - 乙醇溶液中然后干燥来制备。 在优选的实施方案中，基于帕罗西汀盐酸盐，存在于无定形产物中的乙醇的量在1至4重量％的范围内。 无定形产物是稳定的并且基本上不吸湿。

    Preparation of ethers of monosaccharides
    3.
    发明授权
    Preparation of ethers of monosaccharides 失效
    单糖醚的制备

    公开(公告)号：US4056322A

    公开(公告)日：1977-11-01

    申请号：US563080

    申请日：1975-03-28

    申请人： Paul Gordon ,  Bruce Ronsen ,  Shrikant V. Kulkarni

    发明人： Paul Gordon ,  Bruce Ronsen ,  Shrikant V. Kulkarni

    IPC分类号： C07H9/04 ,  C07H15/04 ,  C07H17/02 ,  G03C1/73 ,  C07H5/06

    CPC分类号： C07H9/04 ,  C07H15/04 ,  C07H17/02 ,  G03C1/73

    摘要： Ethereally substituted monosaccharides are prepared from certain selectively derivatized monosaccharides. In practicing the method:1. a monosaccharide derivative having the general formula A.sub.1 -O-H, wherein O is oxygen, H is hydrogen and A.sub.1 is the residue of a monosaccharide selected from the group consisting of pentoses, hexoses and heptoses which has been derivatized with at least one substance selected from the group consisting of (1-a) at least one aliphatic alcohol containing 1-18 carbon atoms to produce an hydrolyzable acetal group at the site of at least one available hydroxyl residue, (1-b) at least one aldehyde containing 1-18 carbon atoms to produce at least one hydrolyzable acetal group at the site of at least one available hydroxyl residue, (1-c) at least one ketone containing 1-18 carbon atoms to produce at least one hydrolyzable ketal group at the site of at least one available hydroxyl residue, and (1-d) at least one organic acid residue containing 1-18 carbon atoms to produce an hydrolyzable ester group at the site of at least one available hydroxyl residue; is reacted with2. an organic halide having the general formula Y - X, wherein X is selected from the group consisting of chlorine, bromine and iodine and Y is selected from the group consisting of (2-a) cyclic monovalent nitrogen containing organic radicals and residua, and (2-b) monovalent organic radicals and residue having the general formula -R.sub.1 B wherein B is selected from the group consisting of ##STR1## --O--R.sub.4 and --S--R.sub.4, R.sub.1 is a divalent organic radical having a linear carbon chain length of about 1-7 carbon atoms, R.sub.2 and R.sub.3 are selected from the group consisting of --H,--OH, --SH, halogen and monovalent organic radicals and residua having a linear carbon chain length of about 1-7 carbon atoms, R.sub.4 is selected from the group consisting of --H and monovalent organic radicals and residua having a linear carbon chain length of about 1-7 carbon atoms, N is nitrogen, O is oxygen, S is sulfur and H is hydrogen;To produce an ethereally substituted monosaccharide derivative having the general formula A-O-Y wherein A, Y and O are as above defined. The monosaccharide derivative (1) and the organic halide (2) are reacted at an elevated reaction temperature while dissolved in a substantially anhydrous organic solvent in the presence of a solid substantially anhydrous strong inorganic base of a metal selected from the group consisting of the alkali metals and the alkaline earth metals. The resultant ethereally substituted monosaccharides may be partially or fully hydrolyzed in an aqueous acidic medium. In one preferred variant, 1,2:5,6-di-O-isopropylidene 3-O-3'-(N',N'-dimethylamino-n-propyl)-D-glucofuranose is prepared and, when desired, thereafter partially or fully hydrolyzed to produce 1,2-O-isopropylidene-3-O-3'-(N',N'-dimethylamino-n-propyl)-D-glucofuranose or 3-O-3'-(N'-N'-dimethylamino-n-propyl-D-glucose in the free amine and/or salt forms. The method is capable of preparing the ethereally substituted monosaccharides in high yield and purity with a minimum of side products. The resultant compounds exhibit striking antiviral activity and/or have other therapeutically valuable properties and are useful in the treatment of warm-blooded animals.

    摘要翻译： 从某些选择性衍生的单糖中制备取代的单糖。 练习方法：

    Amorphous paroxetine composition
    4.
    发明授权
    Amorphous paroxetine composition 失效
    无定形帕罗西汀组成

    公开(公告)号：US06503927B1

    公开(公告)日：2003-01-07

    申请号：US09428812

    申请日：1999-10-28

    申请人： Bruce Ronsen ,  Yogesh D. Sadhale ,  Ragab El-Rashidy

    发明人： Bruce Ronsen ,  Yogesh D. Sadhale ,  Ragab El-Rashidy

    IPC分类号： A61K31445

    CPC分类号： C07D405/12 ,  A61K9/145 ,  A61K9/146 ,  A61K31/445 ,  Y10S514/937

    摘要： A stable amorphous paroxetine hydrochloride composition suitable as a therapeutic agent is prepared employing an aqueous solvent medium containing an acidulant and polyvinylpyrrolidone and drying the resulting solid dispersion. The preferred compositions include amorphous paroxetine hydrochloride, polyvinylpyrrolidone and citric acid.

    摘要翻译： 使用含有酸性剂和聚乙烯吡咯烷酮的水性溶剂介质并干燥所得的固体分散体制备适合作为治疗剂的稳定的无定形帕罗西汀盐酸盐组合物。 优选的组合物包括无定形帕洛西汀盐酸盐，聚乙烯吡咯烷酮和柠檬酸。

    Amelioration of apomorphine adverse effects
    5.
    发明授权
    Amelioration of apomorphine adverse effects 失效
    改善阿扑吗啡的不良反应

    公开(公告)号：US5994363A

    公开(公告)日：1999-11-30

    申请号：US138982

    申请日：1998-08-24

    申请人： Ragab El-Rashidy ,  Bruce Ronsen

    发明人： Ragab El-Rashidy ,  Bruce Ronsen

    IPC分类号： A61K31/435 ,  A61K31/473 ,  A61P15/10 ,  A61P25/16 ,  A61P25/22 ,  A61K31/44

    CPC分类号： A61K31/473

    摘要： Symptoms of Parkinson's disease and psychogenic male erectile dysfunction (MED) can be ameliorated through the use of apomorphine. The adverse side effects of apomorphine administration, such as nausea, vomiting, yawning, and cardiovascular effects, can be significantly reduced by a dose escalating method of acclimatization. An initial dose of apomorphine is administered to the patient, and subsequently increased over a period of time until a final apomorphine dose in excess of a desired therapeutic dose has been received by the patient. Thereafter a therapeutic dose of apomorphine, less than the final apomorphine dose, is administered to the patient with attendant reduced side effects.

    摘要翻译： 可以通过使用阿扑吗啡来改善帕金森病和精神性男性勃起功能障碍（MED）的症状。 阿扑吗啡给药的不良副作用，如恶心，呕吐，打呵欠和心血管作用，可以通过剂量不断升高的驯化方法显着降低。 将阿扑吗啡的初始剂量施用于患者，随后在一段时间内增加，直到患者已经接受超过所需治疗剂量的最终阿扑吗啡剂量。 此后，给患者施用小于最终阿扑吗啡剂量的阿扑吗啡的治疗剂量，伴随着降低的副作用。

    Amorphous paroxetine composition
    7.
    发明授权
    Amorphous paroxetine composition 失效
    无定形帕罗西汀组成

    公开(公告)号：US06638948B1

    公开(公告)日：2003-10-28

    申请号：US08940058

    申请日：1997-09-30

    申请人： Bruce Ronsen ,  Ragab El-Rashidy

    发明人： Bruce Ronsen ,  Ragab El-Rashidy

    IPC分类号： A61K31445

    CPC分类号： A61K31/4525 ,  A61K9/145 ,  A61K9/146 ,  C07D401/12

    摘要： A free-flowing, amorphous paroxetine hydrochloride composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. The present compositions comprise amorphous paroxetine hydrochloride and at least one hydroxyl-bearing compound. In one preferred embodiment, the hydroxyl-bearing compound is ethanol and the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.

    摘要翻译： 适合作为早泄治疗剂的自由流动的无定形帕罗西汀盐酸盐组合物可以通过将帕罗西汀游离碱溶解在盐酸 - 乙醇溶液中然后干燥来制备。 本发明组合物包含无定形帕罗西汀盐酸盐和至少一种含羟基化合物。 在一个优选的实施方案中，含羟基化合物是乙醇，基于帕罗西汀盐酸盐，存在于无定形产物中的乙醇的量在1至4重量％的范围内。 无定形产物是稳定的并且基本上不吸湿。

    Treatment of female sexual dysfunction
    10.
    发明授权
    Treatment of female sexual dysfunction 失效
    治疗女性性功能障碍

    公开(公告)号：US5945117A

    公开(公告)日：1999-08-31

    申请号：US16252

    申请日：1998-01-30

    申请人： Ragab El-Rashidy ,  Bruce Ronsen

    发明人： Ragab El-Rashidy ,  Bruce Ronsen

    IPC分类号： C07D221/18 ,  A61K31/473 ,  A61K31/485 ,  A61K47/40 ,  A61P15/00 ,  A61F6/06 ,  A61K9/20 ,  A61K47/32

    CPC分类号： A61K31/485

    摘要： Sexual dysfunction in human females can be ameliorated, without substantial undesirable side effects, by sublingual administration of apomorphine dosage forms. Administration of apomorphine increases nerve stimulated clitoral intracavernosal blood flow and vaginal wall blood flow for enhanced clitoral erection and vaginal engorgement in a female. A plasma concentration of apomorphine of no more than about 5.5 nanograms per milliliter is preferably maintained.

    摘要翻译： 通过舌下施用阿扑吗啡剂型，可以改善人类女性的性功能障碍，无明显不良副作用。 阿扑吗啡的施用增加神经刺激的阴蒂海绵体内血流量和阴道壁血流量，以增强女性的阴蒂勃起和阴道充盈。 优选维持阿扑吗啡的血药浓度不超过约5.5纳克每毫升。