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    Ammonium salts of hemoglobin allosteric effectors, and uses thereof
    6.
    发明申请
    Ammonium salts of hemoglobin allosteric effectors, and uses thereof 审中-公开
    血红蛋白变构效应物的铵盐及其用途

    公开(公告)号：US20020142995A1

    公开(公告)日：2002-10-03

    申请号：US09920310

    申请日：2001-08-01

    Inventor： Yves Claude Nicolau ,  Jaime E. Lazarte ,  Dennis R. Alford

    IPC: A61K031/663 ,  C07F009/02

    CPC classification number: C07F9/117 ,  A61K31/132 ,  A61K31/661 ,  A61K31/6615 ,  A61K31/663 ,  C07F9/093 ,  A61K2300/00

    Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering a broad range of anionic molecules to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering a ligand for the allosteric site of hemoglobin to the cytoplasm of the red blood cells.

    Abstract translation: 本发明包括化合物，其组合物和能够将广泛范围的阴离子分子递送至哺乳动物细胞的细胞质的方法。 在某些实施方案中，本发明涉及通过将血红蛋白的变构位点的配体递送至红细胞的细胞质来提高哺乳动物红细胞传递氧的能力的化合物，其组合物和方法。

    Combinations of bisphosphonates, estrogens and estrogenic agents
    7.
    发明申请
    Combinations of bisphosphonates, estrogens and estrogenic agents 审中-公开
    双膦酸盐，雌激素和雌激素剂的组合

    公开(公告)号：US20020028792A1

    公开(公告)日：2002-03-07

    申请号：US09896219

    申请日：2001-06-29

    Applicant: American Home Products Corporation

    Inventor： Simon N. Jenkins ,  Barry S. Komm ,  Christopher P. Miller

    IPC: A61K031/663 ,  A61K031/404 ,  A61K031/56

    CPC classification number: A61K45/06 ,  A61K31/404 ,  A61K31/56 ,  A61K31/663 ,  A61K2300/00

    Abstract: This invention comprises methods of treating bone disorders and lowering blood LDL levels comprising administration of a bisphosphonate, an estrogen and compound of the formulae I or II: 1 wherein Z is a moiety selected from the group of: 2 wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety: 3 R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明包括治疗骨疾病和降低血液LDL水平的方法，其包括施用二膦酸盐，雌激素和式I或II化合物：其中Z是选自以下的部分：其中：R1选自H，OH 或其C1-C12酯或其C1-C12烷基醚，苄氧基或卤素; 或包括三氟甲基醚和三氯甲基醚的C 1 -C 4卤代醚; R2，R3，R4，R5和R6是H，OH或C1-C12酯或其C1-C12烷基醚，卤素或C1-C4卤代醚，氰基，C1-C6烷基或三氟甲基，条件是 当R1为H时，R2不为OH; Y是部分：R 7和R 8是烷基或连接在一起形成任选取代的含氮环; 或其药学上可接受的盐。

    Combinations of bisphosphonates and estrogenic agents
    8.
    发明申请
    Combinations of bisphosphonates and estrogenic agents 审中-公开
    双膦酸盐和雌激素剂的组合

    公开(公告)号：US20020019373A1

    公开(公告)日：2002-02-14

    申请号：US09896154

    申请日：2001-06-29

    Applicant: American Home Products Corporation

    Inventor： Simon N. Jenkins ,  Barry S. Komm

    IPC: A61K031/663 ,  A61K031/55 ,  A61K031/454 ,  A61K031/404

    CPC classification number: A61K31/454 ,  A61K31/404 ,  A61K31/55 ,  A61K31/663 ,  A61K2300/00

    Abstract: This invention comprises methods of treating bone disorders comprising administration of a bisphosphonate and compound of the formulae I or II: 1 wherein Z is a moiety selected from the group of: 2 wherein: R1 is selected from H, OH or the C1-C12 esters or C1-C12 alkyl ethers thereof, benzyloxy, or halogen; or C1-C4 halogenated ethers including trifluoromethyl ether and trichloromethyl ether; R2, R3, R4, R5, and R6 are H, OH or C1-C12 esters or C1-C12 alkyl ethers thereof, halogens, or C1-C4 halogenated ethers, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH; Y is the moiety: 3 R7 and R8 are alkyl or concatenated together to form an optionally substituted, nitrogen-containing ring; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明包括治疗骨疾病的方法，包括施用双膦酸盐和式I或II化合物：其中Z是选自下组的部分：其中：R1选自H，OH或C1-C12酯或C1 -C 12烷基醚，苄氧基或卤素; 或包括三氟甲基醚和三氯甲基醚的C 1 -C 4卤代醚; R2，R3，R4，R5和R6是H，OH或C1-C12酯或其C1-C12烷基醚，卤素或C1-C4卤代醚，氰基，C1-C6烷基或三氟甲基，条件是 当R1为H时，R2不为OH; Y是部分：R 7和R 8是烷基或连接在一起形成任选取代的含氮环; 或其药学上可接受的盐。

    Treatment of carcinomas using squalamine in combination with other anti-cancer agents or modalities
    9.
    发明申请
    Treatment of carcinomas using squalamine in combination with other anti-cancer agents or modalities 有权
    使用角质胺与其他抗癌剂或方式联合治疗癌症

    公开(公告)号：US20010046521A1

    公开(公告)日：2001-11-29

    申请号：US09803740

    申请日：2001-03-12

    Inventor： Michael Zasloff ,  Jon Williams ,  Mitchell H. Sokoloff

    IPC: A61K033/24 ,  A61K031/663 ,  A61K031/665 ,  A61K031/337

    CPC classification number: A61K31/575 ,  A61K31/00 ,  A61K33/24 ,  A61K2300/00

    Abstract: A method for treating a tumor includes a first treatment procedure using a conventional cancer treatment technique, and a second treatment procedure which includes administering an effective amount of squalamine. Synergistically effective amounts are preferred. The first treatment procedure may be a treatment with one or more conventional cytotoxic chemical compounds. As examples, the cytotoxic chemical compound may be a nitrosourea (such as BCNU), cyclophosphamide, doxorubicin, 5-fluorouracil, paclitaxel and its derivatives, cisplatin or other platinum containing cancer treating agents. Alternatively, the first treatment may be a treatment with one or more conventional anti-hormonal agents. As examples, the anti-hormonal agents may be a LHRH (luteinizing hormone releasing hormone) agonist or an anti-androgen such as flutamide, biclutamide, nilutamide, and luprolide. These conventional cancer treatments compounds and the squalamine may be administered by any suitable route. The first treatment procedure may take place prior to the second treatment procedure, after the second treatment procedure, or the two treatment procedures may take place simultaneously. As an alternative, the first treatment procedure may be a conventional radiation treatment regimen. As a further alternative the first treatment procedure may be a combination of treatment with one or more conventional cytotoxic chemical compounds and a conventional radiation treatment regimen.

    Abstract translation: 治疗肿瘤的方法包括使用常规癌症治疗技术的第一治疗方法和包括给予有效量的角鲨胺的第二治疗方法。 协同有效量是优选的。 第一种治疗方法可以是用一种或多种常规细胞毒性化学化合物治疗。 作为实例，细胞毒性化合物可以是亚硝基脲（例如BCNU），环磷酰胺，多柔比星，5-氟尿嘧啶，紫杉醇及其衍生物，顺铂或其它含铂的癌症治疗剂。 或者，第一种治疗可以是用一种或多种常规抗激素剂治疗。 作为实例，抗激素剂可以是LHRH（黄体生成激素释放激素）激动剂或抗雄激素，例如氟他胺，双氯吡格胺，尼鲁替丁和氟洛西林。 这些常规的癌症治疗化合物和角鲨胺可以通过任何合适的途径施用。 第一处理程序可以在第二处理程序之前，第二处理程序之后进行，或者两个处理程序可以同时进行。 作为替代方案，第一种治疗方法可以是常规的放射治疗方案。 作为另一种替代方案，第一种治疗方法可以是与一种或多种常规细胞毒性化学化合物的治疗和常规放射治疗方案的组合。

    Methods for treatment of lysosomal storage diseases
    10.
    发明申请
    Methods for treatment of lysosomal storage diseases 审中-公开
    溶酶体贮积病治疗方法

    公开(公告)号：US20010031741A1

    公开(公告)日：2001-10-18

    申请号：US09777743

    申请日：2001-02-06

    Inventor： Robin Ziegler ,  Seng Cheng ,  John Marshall ,  Mark Goldberg

    IPC: A61K048/00 ,  A61K038/47 ,  A61K031/663

    CPC classification number: A61K31/66 ,  A61K31/663 ,  A61K38/465 ,  A61K38/47 ,  A61K48/00 ,  C12N9/18 ,  C12N9/2402 ,  C12N9/2465 ,  C12N2799/022 ,  C12Y302/0102 ,  C12Y302/01022 ,  C12Y302/01045 ,  A61K2300/00

    Abstract: Methods are disclosed for treatment of patients suffering from accumulation of a metabolite within macrophages, such as in lysosomal storage diseases. The methods comprise treating the patient with a macrophage depleting amount of a bisphosphonate compound, such that apoptosis of macrophages is induced and the metabolite is released into circulation so that the metabolites may be eliminated from the patient. The methods may further include administration of a gene therapy vector for the treatment of lysosomal storage diseases.

    Abstract translation: 公开了用于治疗患有巨噬细胞内的代谢物积聚的患者的方法，例如在溶酶体贮积疾病中。 所述方法包括用巨噬细胞消耗量的二膦酸盐化合物治疗患者，从而诱导巨噬细胞的凋亡并将代谢物释放到循环中，使得代谢物可以从患者中消除。 所述方法还可包括施用用于治疗溶酶体贮积病的基因治疗载体。

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