HETEROCYCLIC COMPOUNDS FOR PREVENTING AND TREATING DISORDERS ASSOCIATED WITH EXCESSIVE BONE LOSS
    1.
    发明申请
    HETEROCYCLIC COMPOUNDS FOR PREVENTING AND TREATING DISORDERS ASSOCIATED WITH EXCESSIVE BONE LOSS 审中-公开
    用于预防和治疗与骨质疏松相关的疾病的异种化合物

    公开(公告)号:US20100120722A1

    公开(公告)日:2010-05-13

    申请号:US12688849

    申请日:2010-01-15

    摘要: This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

    摘要翻译: 本发明涉及式(I),式(I')和式(I“)的嘧啶化合物及其药学上可接受的盐,溶剂合物,包合物和前药,其中R1,R2,R3,R4,R5,U ,V,W,X,Y,Z和n在本文中定义。 本发明还涉及包含这些化合物的组合物和使用它们的方法。 本发明的化合物和组合物可用于治疗或预防与过量骨丢失相关的疾病,包括但不限于牙周病,非恶性骨病(例如骨质疏松症,骨骼传播者疾病,成骨不全,纤维性发育异常和 原发性甲状旁腺功能亢进)雌激素缺乏,炎性骨丢失,骨恶性肿瘤,关节炎,骨硬化和某些癌症相关疾病(如恶性高钙血症(HCM),多发性骨髓瘤溶骨性骨损伤和乳腺癌和其他转移性癌症的溶骨性骨转移 )。

    Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss
    2.
    发明申请
    Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss 审中-公开
    用于预防和治疗与过度骨丢失相关的疾病的杂环化合物

    公开(公告)号:US20080058297A1

    公开(公告)日:2008-03-06

    申请号:US10561025

    申请日:2004-05-28

    摘要: This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

    摘要翻译: 本发明涉及式(I),式(I')和式(I“)的嘧啶化合物及其药学上可接受的盐,溶剂合物,包合物和前药,其中R 1, R 2,R 3,R 4,R 5,U,V,W,X,Y, Z和n在本文中定义。 本发明还涉及包含这些化合物的组合物和使用它们的方法。 本发明的化合物和组合物可用于治疗或预防与过量骨丢失相关的疾病,包括但不限于牙周病,非恶性骨病(例如骨质疏松症,骨骼传播者疾病,成骨不全,纤维性发育异常和 原发性甲状旁腺功能亢进)雌激素缺乏,炎性骨丢失,骨恶性肿瘤,关节炎,骨硬化和某些癌症相关疾病(如恶性高钙血症(HCM),多发性骨髓瘤溶骨性骨损伤和乳腺癌和其他转移性癌症的溶骨性骨转移 )。

    Process for producing fluorinated alkyl ether
    6.
    发明申请
    Process for producing fluorinated alkyl ether 有权
    制备氟化烷基醚的方法

    公开(公告)号:US20060128915A1

    公开(公告)日:2006-06-15

    申请号:US11348490

    申请日:2006-02-07

    IPC分类号: C08F16/24

    CPC分类号: C07C41/06 C07C43/123

    摘要: To provide a process for producing a fluorinated alkyl ether, whereby a sufficient reaction rate can be attained even under mild reaction conditions, and a post-process such as distillation after the reaction can be efficiently carried out. A process for producing a fluorinated alkyl ether, which comprises introducing an aprotic polar solvent, a fluorinated ether, a catalyst, a fluorinated alkyl alcohol and a fluorinated olefin into a reactor, and then, reacting the fluorinated alkyl alcohol with the fluorinated olefin, characterized in that the ratio of the two components of the aprotic polar solvent and the fluorinated ether introduced into the reactor is the aprotic polar solvent/the fluorinated ether=5/95 to 80/20 by mass ratio.

    摘要翻译: 为了提供氟化烷基醚的制造方法,即使在温和的反应条件下也能够得到充分的反应速度,能够有效地进行反应后的蒸馏等后处理。 一种制备氟化烷基醚的方法,包括将非质子极性溶剂,氟化醚,催化剂,氟化烷基醇和氟化烯烃引入反应器中,然后使氟化烷基醇与氟化烯烃反应,其特征在于 引入到反应器中的非质子极性溶剂和氟化醚的两种组分的比例是非质子极性溶剂/氟化醚= 5/95〜80/20质量比。

    Method for producing fluoroalkyl ether
    7.
    发明申请
    Method for producing fluoroalkyl ether 有权
    氟烷基醚的制备方法

    公开(公告)号:US20060094908A1

    公开(公告)日:2006-05-04

    申请号:US11293200

    申请日:2005-12-05

    IPC分类号: C07C41/06

    CPC分类号: C07C41/06 C07C43/123

    摘要: A method for producing a fluoroalkyl ether, which comprises reacting a fluoroalkyl alcohol with a fluorinated olefin in the presence of a solvent and a catalyst, wherein the fluoroalkyl alcohol and the fluorinated olefin are continuously supplied into a reactor, a reaction product containing the fluoroalkyl ether is continuously withdrawn from the reactor, and the reaction is carried out while the concentration of the fluoroalkyl alcohol present in the reactor is maintained to be at most 7 mass % based on the total organic component present in the reactor. According to the present invention, a fluoroalkyl ether having a high purity can be produced in an industrial scale and at a high reaction rate.

    摘要翻译: 一种制备氟烷基醚的方法,其包括在溶剂和催化剂存在下使氟代烷基醇与氟化烯烃反应,其中将氟代烷基醇和氟化烯烃连续地供入反应器中,将含有氟代烷基醚 从反应器中连续取出,反应进行,同时反应器中存在的氟代烷基醇的浓度维持在反应器中存在的总有机成分的7质量%以下。 根据本发明,可以以工业规模和高反应速度制备高纯度的氟烷基醚。

    Peptides and peptide compositions having osteoinductive activity
    8.
    发明授权
    Peptides and peptide compositions having osteoinductive activity 有权
    具有骨诱导活性的肽和肽组合物

    公开(公告)号:US08815807B2

    公开(公告)日:2014-08-26

    申请号:US13309734

    申请日:2011-12-02

    CPC分类号: C40B60/12

    摘要: Compositions and kits are provided having a peptide having an amino acid sequence that binds to eukaryotic cells and effects differentiation and support growth of the cells. Peptide-scaffold compositions containing at least one peptide or combinations of peptides are therapeutic agents for stimulating and promoting osteogenic activity and osteoinduction activity for cells. The scaffold is for example apatite, natural cancellous bone, demineralized natural cancellous bone, collagen, calcium phosphate, or hydroxyapatite.

    摘要翻译: 提供组合物和试剂盒,其具有具有结合真核细胞并实现分化并支持细胞生长的氨基酸序列的肽。 含有至少一种肽或肽组合的肽 - 支架组合物是用于刺激和促进细胞的成骨活性和骨诱导活性的治疗剂。 脚手架是例如磷灰石,天然松质骨,软化天然松质骨,胶原蛋白,磷酸钙或羟基磷灰石。

    BIS[THIOHYDRAZIDE AMIDE] COMPOUNDS FOR TREATING LEUKEMIA
    10.
    发明申请
    BIS[THIOHYDRAZIDE AMIDE] COMPOUNDS FOR TREATING LEUKEMIA 有权
    BIS [THIOHYDRAZIDE AMIDE]用于处理低密度脂蛋白的化合物

    公开(公告)号:US20130035386A1

    公开(公告)日:2013-02-07

    申请号:US13513449

    申请日:2010-12-06

    CPC分类号: A61K31/15 A61K31/282

    摘要: Certain bis[thio-hydrazide amide]-related compounds are found to be surprisingly effective at treating with leukemia, e.g., acute myeloid leukemia (AML). Methods of treating a subject with AML including administering bis[thio-hydrazide amide]-related compounds described herein, are disclosed.

    摘要翻译: 发现某些双[硫代 - 酰肼酰胺]相关化合物在用白血病例如急性骨髓性白血病(AML)治疗方面令人惊奇地有效。 公开了用AML治疗受试者的方法,包括施用本文所述的双[硫代 - 酰肼酰胺]相关化合物。