PRODRUGS WITH 1-(DISULFANYL)ALKYLOXY-CARBONYL UNITS

    公开(公告)号:US20240299554A1

    公开(公告)日:2024-09-12

    申请号:US18572705

    申请日:2022-06-21

    申请人: PHARMACYTICS B.V.

    IPC分类号: A61K47/54 C07C381/04

    摘要: The invention is in the field of medical sciences. It provides new pharmaceutical methods and preparations. The invention relates to methods for improving the pharmacokinetic, physicochemical or pharmaceutical properties of drugs by converting the drug into a promoiety-containing 1-substituted disulfanylalkyl carbonate, thiocarbamate or carbamate prodrug. In particular, the invention relates to methods for improving the solubility, permeability, stability and/or oral bioavailability of a drug by converting the drug into a promoiety-containing 1-(disulfanylalkyl) carbonate, thiocarbonate or carbamate prodrug. The invention also provides new compositions comprising a drug covalently attached to a promoiety-containing 1-(disulfanylalkyl) carbonate, thiocarbonate or carbamate. More in particular, the invention relates to a method for increasing the oral bioavailability of a drug by covalently attaching a promoiety-containing 1-disulfanylalkyloxycarbonyl unit to a hydroxyl or amine containing drug in which the promoiety contains a 1-O—, 1-S—, 6-O— or 6-S-linked monosaccharide.

    Methods for the formation of hydrogels using thiosulfonate compositions and uses thereof
    3.
    发明授权
    Methods for the formation of hydrogels using thiosulfonate compositions and uses thereof 有权
    使用硫代磺酸盐组合物形成水凝胶的方法及其用途

    公开(公告)号:US08247598B2

    公开(公告)日:2012-08-21

    申请号:US13325936

    申请日:2011-12-14

    IPC分类号: C09K5/06 C07C381/04

    摘要: The present invention provides both crosslinked polymer compositions capable of forming hydrogels upon exposure to an aqueous environment and thiosulfonate hydrogel-forming components. The thiosulfonate hydrogel-forming components of the invention are preferably multi-arm thiosulfonate polymer derivatives that form a crosslinked polymer composition when exposed to a base without requiring the presence of a second cross-linking reagent, redox catalyst, or radiation. Methods for forming hydrogel compositions, as well as methods for using the hydrogels, are also provided.

    摘要翻译: 本发明提供了能够在暴露于水性环境中形成水凝胶的交联聚合物组合物和形成硫代磺酸盐的水凝胶组分的交联聚合物组合物。 本发明的硫代磺酸盐水凝胶形成成分优选为在不需要存在第二交联剂,氧化还原催化剂或辐射的情况下暴露于碱而形成交联聚合物组合物的多臂硫代磺酸盐聚合物衍生物。 还提供了形成水凝胶组合物的方法以及使用水凝胶的方法。

    Process and producing taurine analogues
    5.
    发明授权
    Process and producing taurine analogues 失效
    牛磺酸类似物的制备和生产

    公开(公告)号:US5856563A

    公开(公告)日:1999-01-05

    申请号:US838924

    申请日:1997-04-23

    IPC分类号: C07C381/04 C07F11/00

    CPC分类号: C07C381/04

    摘要: The present invention relates to a process for producing amino/guanidinothiosulfonic acid, which comprises treating a styrenedivinylbenzene copolymer sulfonate of amino/guanidinoethyl disulfoxide into contact with an alkali, selectively eluting amino/guanidinosulfinic acid, then reacting this product in a non-aqueous solvent in the presence of a base, and passing the reaction product through a weakly acidic cation exchange resin column; in accordance with the present invention, hypotaurine, thiotaurine and the like having a high purity can industrially be produced.

    摘要翻译: 本发明涉及一种生产氨基/胍基硫代磺酸的方法,其包括将氨基/胍基乙基二亚砜的苯乙烯二乙烯基苯共聚物磺酸盐与碱接触,选择性洗脱氨基/胍基亚磺酸,然后使该产物在非水溶剂中反应 碱的存在,并使反应产物通过弱酸性阳离子交换树脂柱; 根据本发明,可以在工业上生产具有高纯度的海牛磺酸,硫代牛磺酸等。

    Thioalkanal-s-oxides
    8.
    发明授权
    Thioalkanal-s-oxides 失效
    硫代硫氧化物

    公开(公告)号:US3686323A

    公开(公告)日:1972-08-22

    申请号:US3686323D

    申请日:1970-02-24

    摘要: This invention relates to novel thio-alkanal-S-oxides of the formula R=S=O wherein R is a straight-chain alkylidene group having from two to six carbon atoms. These novel compounds are useful to alter the flavor of consumable products. They may be prepared by reacting an alkyl sulfinyl chloride and a lower tertiary amine at a temperature below about -50* C.

    摘要翻译: 本发明涉及式R = S = O的新的硫代 - 链烷醛S-氧化物,其中R是具有2-6个碳原子的直链亚烷基。 这些新型化合物可用于改变消费品的味道。 它们可以通过在低于约-50℃的温度下使烷基亚磺酰氯和低级叔胺反应来制备。