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    • 1. 发明申请
    • (Polyalkoxy)sulfonate surface modifiers
    • (聚烷氧基)磺酸盐表面改性剂
    • US20060141048A1
    • 2006-06-29
    • US11304421
    • 2005-12-15
    • James KippTon HaiBennett Melnick
    • James KippTon HaiBennett Melnick
    • A61K9/14
    • C08G65/334A61K8/90A61K9/146A61K47/34A61Q19/00C08G65/326C08L71/02
    • The present invention is directed to novel compounds, methods of manufacture and methods of use. The present invention is also directed to solid drug/active agent particles having one or more of the compounds of the present invention associated with the surface thereof. The compounds of the present invention are comprised of a non-polar polyether covalently linked to an anionic sulfonate group. The compounds have an amphipathic quality and preferably, are surface active. Such compounds are preferably useful as surface-active agents to coat and stabilize dispersions of particles in a continuous liquid medium. These surface-active agents may be applied in the stabilization of suspensions, emulsions, or liposome formulations intended for pharmaceutical, medical, cosmetic, or agricultural use. The particles that can be prepared by a variety of methods and will preferably comprise a pharmaceutical agent. Pharmaceutical compositions of the present invention can be used to treat a myriad of conditions and can be administered by many routes, including intravenous, intramuscular, subcutaneous, intrathecal, subdural, intracameral, intracerebral, intralesional, topical, oral, buccal, rectal, transcutaneous, pulmonary, and nasal.
    • 本发明涉及新化合物,制备方法和使用方法。 本发明还涉及具有一种或多种与其表面相关的本发明化合物的固体药物/活性剂颗粒。 本发明的化合物由与阴离子磺酸盐基团共价连接的非极性聚醚组成。 该化合物具有两性质量,优选表面活性。 这些化合物优选用作表面活性剂以涂覆和稳定颗粒在连续液体介质中的分散体。 这些表面活性剂可以用于稳定用于制药,医疗,化妆品或农业用途的悬浮液,乳剂或脂质体制剂。 可以通过多种方法制备并且优选包含药剂的颗粒。 本发明的药物组合物可用于治疗无数的病症,并且可以通过许多途径施用,包括静脉内,肌肉内,皮下,鞘内,硬膜下,阴道内,脑内,肠内,局部,口腔,口腔,直肠,经皮, 肺和鼻。
    • 2. 发明申请
    • Preparation and Use of a Stable Formulation of Allosteric Effector Compounds
    • 稳定配方的变构效应剂的制备和应用
    • US20070212302A1
    • 2007-09-13
    • US11749610
    • 2007-05-16
    • Douglas JohnsonMark DotyJames Kipp
    • Douglas JohnsonMark DotyJames Kipp
    • A61K31/205A61B5/055
    • A61K31/195A61K9/0019A61K47/12A61K47/18A61K47/183A61K49/10
    • A pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salts suitable for parenteral administration includes an aqueous formulation of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salt and a buffer to maintain the pH from about 6 to about 11. The composition in accordance with the invention reduces the amount of particulate matter that forms in solution after heat sterilization. The invention also includes a process for making a pharmaceutical composition of 2-[4-[2-[(3,5-dimethylphenyl)amino]-2-oxoethyl]phenoxy]-2-methyl-propionic acid or its physiologically acceptable salt that has a shelf life in excess of thirty days and is useful in parenteral administration.
    • 2- [4- [2 - [(3,5-二甲基苯基)氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其适用于胃肠外给药的生理学上可接受的盐的药物组合物包括 2- [4- [2 - [(3,5-二甲基苯基)氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其生理上可接受的盐和缓冲液,以将pH保持在约6至约11 根据本发明的组合物减少加热灭菌后在溶液中形成的颗粒物质的量。 本发明还包括制备2- [4- [2 - [(3,5-二甲基苯基)氨基] -2-氧代乙基]苯氧基] -2-甲基 - 丙酸或其生理上可接受的盐的药物组合物的方法, 保质期超过30天,可用于肠胃外给药。
    • 4. 发明申请
    • Method for delivering drugs to the brain
    • 向大脑输送药物的方法
    • US20050048002A1
    • 2005-03-03
    • US10868680
    • 2004-06-15
    • Barrett RabinowJames KippHoward Gendelman
    • Barrett RabinowJames KippHoward Gendelman
    • A61K9/00A61K9/51A61K47/48A61L9/04A61K9/14
    • A61K9/00A61K9/0085A61K9/5123A61K9/5146A61K47/6901
    • The present invention is concerned with delivering a pharmaceutical composition to the brain of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the brain of a portion of the pharmaceutical composition by cells capable of reaching the brain. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytised or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the brain.
    • 本发明涉及向哺乳动物受试者的脑中递送药物组合物以治疗脑部疾病或病症。 该方法包括以下步骤:(i)提供药物组合物的分散体作为平均粒度为约150nm至约100微米的颗粒,和(ii)向哺乳动物受试者施用分散体以递送至脑 的药物组合物的一部分能够到达脑的细胞。 例如,作为颗粒的药物组合物的分散体可以在给予哺乳动物受试者之前或之后被细胞吞噬或吸附。 药物组合物的分散体可以施用于中枢神经系统或血管系统。 给药后,负载的细胞将药物组合物作为颗粒输送到脑中。
    • 5. 发明申请
    • Method for delivering particulate drugs to tissues
    • 将颗粒药物递送至组织的方法
    • US20060280430A1
    • 2006-12-14
    • US11406986
    • 2006-04-19
    • Barrett RabinowHoward GendelmanJames Kipp
    • Barrett RabinowHoward GendelmanJames Kipp
    • G11B27/00
    • A61K9/0085A61K9/10A61K9/5123A61K9/5146A61K47/6901
    • The present invention is concerned with delivering a pharmaceutical composition to a tissue target of a mammalian subject for treating brain diseases or disorders. The process includes the steps of: (i) providing a dispersion of the pharmaceutical composition as particles having an average particle size of from about 150 nm to about 100 microns, and (ii) administering the dispersion to the mammalian subject for delivery to the tissue target of a portion of the pharmaceutical composition by cells capable of reaching the tissue target. The dispersion of the pharmaceutical composition as particles, for example, can be phagocytised or adsorbed by the cells prior or subsequent to administration into the mammalian subject. The dispersion of the pharmaceutical composition can be administered to the central nervous system or the vascular system. After administration, the loaded cells transport the pharmaceutical composition as particles into the tissue target.
    • 本发明涉及将药物组合物递送至哺乳动物受试者的组织靶以治疗脑部疾病或病症。 该方法包括以下步骤:(i)提供药物组合物的分散体作为平均粒度为约150nm至约100微米的颗粒,和(ii)向哺乳动物受试者施用分散体以递送至组织 通过能够到达组织靶的细胞的一部分药物组合物的靶标。 例如,作为颗粒的药物组合物的分散体可以在给予哺乳动物受试者之前或之后被细胞吞噬或吸附。 药物组合物的分散体可以施用于中枢神经系统或血管系统。 给药后,负载的细胞将药物组合物作为颗粒输送到组织靶中。