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    • 45. 发明授权
    • Quinolines for the treatment of PI3K-δ mediated diseases
    • 喹诺酮用于治疗PI3K-δ介导的疾病
    • US08329910B2
    • 2012-12-11
    • US13187188
    • 2011-07-20
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • C07D215/12
    • C07D401/12C07D401/14
    • Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity. The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including nut not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
    • 取代的双环杂芳基和含有它们的组合物,用于治疗一般炎症,关节炎,风湿性疾病,骨关节炎,炎性肠病,炎症性眼病,炎症性或不稳定性膀胱病,牛皮癣,皮肤炎症成分的投诉,慢性炎性病症 不限于自身免疫性疾病如系统性红斑狼疮(SLE),重症肌无力,类风湿关节炎,急性播散性脑脊髓炎,特发性血小板减少性紫癜,多发性硬化症,Sjoegren综合征和自身免疫性溶血性贫血,包括所有形式的超敏反应的过敏症状。 本发明还使得能够治疗依赖于p110δ活性或与p110δ活性相关的癌症的方法,包括不限于白血病的坚果,例如急性骨髓性白血病(AML)Myelo-dysplastic综合征(MDS)骨髓增殖性疾病(MPD) 慢性骨髓性白血病(CML)T细胞急性淋巴细胞白血病(T-ALL)B细胞急性淋巴细胞白血病(B-ALL)非霍奇金淋巴瘤(NHL)B细胞淋巴瘤和实体瘤如乳腺癌。
    • 49. 发明申请
    • HETEROCYCLIC COMPOUNDS AND THEIR USES
    • 杂环化合物及其用途
    • US20110152277A1
    • 2011-06-23
    • US13036236
    • 2011-02-28
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • Yi ChenTimothy D. CushingXiaolin HaoXiao HeAndreas ReicheltRobert M. RzasaJennifer SeganishYoungsook ShinDawei Zhang
    • A61K31/519C07D473/34A61K31/52A61P19/02A61P17/06A61P29/00A61P35/00C07D471/04C07D487/04
    • C07D487/04C07D471/04C07D519/00
    • Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
    • 取代的双环杂芳基和含有它们的组合物,用于治疗一般炎症,关节炎,风湿性疾病,骨关节炎,炎性肠病,炎症性眼病,炎症性或不稳定性膀胱病,牛皮癣,皮肤炎症成分的投诉,慢性炎性病症 不限于自身免疫性疾病如系统性红斑狼疮(SLE),重症肌无力,类风湿性关节炎,急性播散性脑脊髓炎,特发性血小板减少性紫癜,多发性硬化症,Sjoegren综合征和自身免疫性溶血性贫血,包括所有形式的超敏反应的过敏症状 包括但不限于白血病,如急性骨髓性白血病(AML)骨髓增生异常综合征(MDS)骨髓增生性疾病(MPD)慢性骨髓性白血病(MPD),介导,依赖或与p110δ活性相关的癌症的方法 (CML)T细胞急性淋巴细胞白血病(T-ALL)B细胞急性淋巴细胞白血病(B-ALL)非霍奇金淋巴瘤(NHL)B细胞淋巴瘤和实体瘤如乳腺癌。
    • 50. 发明申请
    • PROCESS FOR THE PREPARATION OF DOCETAXEL, ITS INTERMEDIATES, AND METHODS FOR PREPARATION THEREOF
    • 制备DOCETAXEL及其中间体的方法及其制备方法
    • US20100311991A1
    • 2010-12-09
    • US12741714
    • 2009-05-22
    • Xin ShenHuaxing ZhanJidong YangXiao HeFuxing LinShaohong Wu
    • Xin ShenHuaxing ZhanJidong YangXiao HeFuxing LinShaohong Wu
    • C07D305/14C07C271/66C07C269/06
    • C07D305/14C07C269/04C07C269/06C07C271/22Y02P20/55
    • The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained from step a to prepare compound 5; c) removing one tert-butoxycarbonyl of compound 5 obtained from step b to prepare compound 6; d) removing one acetyl of compound 6 obtained from step c to prepare compound 1; wherein, R1 represents tert-butyl dimethyl silyl, triethylsilyl, ethoxyethyl, tetrahydropyranyl, trichloroethoxycarbonyl or methoxymethyl, Boc is tert-butoxycarbonyl, Ac is acetyl, and Ph is phenyl. The present invention also disclosed intermediates of docetaxel and methods for preparation thereof. In the methods for preparation of the present invention, the protective groups used are easy to be removed, the purification of the intermediates is easy, the cost is lower, the yield and the purity are higher, and the processes can be scaled to commercial implementation.
    • 本发明公开了一种制备多西紫杉醇1的方法,包括以下步骤:a)化合物2和3的羟基酰化反应得到化合物4; b)由步骤a获得的化合物4的羟基的脱保护基团R1,以制备化合物5; c)除去由步骤b获得的化合物5的一个叔丁氧基羰基,制备化合物6; d)除去由步骤c获得的化合物6的一个乙酰基,制备化合物1; 其中,R1表示叔丁基二甲基甲硅烷基,三乙基甲硅烷基,乙氧基乙基,四氢吡喃基,三氯乙氧基羰基或甲氧基甲基,Boc是叔丁氧基羰基,Ac是乙酰基,Ph是苯基。 本发明还公开了多西紫杉醇的中间体及其制备方法。 在本发明的制备方法中,所使用的保护基团易于除去,中间体的纯化容易,成本低,产率和纯度高,并且可以将其扩展到商业实施 。