23-yne-vitamin D3 derivative
    1.
    发明授权
    23-yne-vitamin D3 derivative 有权
    23-维生素D3衍生物

    公开(公告)号:US09006220B2

    公开(公告)日:2015-04-14

    申请号:US13880637

    申请日:2011-10-24

    IPC分类号: C07C401/00 C07F7/18

    摘要: To provide a novel vitamin D3 derivative useful as a therapeutic agent for osteoporosis.Provided is a vitamin D3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.

    摘要翻译: 提供可用作骨质疏松症治疗剂的新型维生素D3衍生物。 本发明提供由下式(1)表示的维生素D3衍生物或其药学上可接受的溶剂合物:其中,R1表示氢原子,碳原子数1〜6的烷基,碳原子数1〜6的烷基的烷基羰氧基烷基 或芳基具有6至10个碳原子的芳基羰氧基烷基和具有1至6个碳原子的烷基; R 2表示氢原子或碳原子数1〜6的烷基,或者与其它的R 2和与它们相连的碳原子一起形成可以形成碳原子数为3〜6的环状烷基。 R 3表示碳原子数为1〜6的烷基,或者与另外的R 3及与它们相连的碳原子一起形成碳原子数为3〜6的环状烷基。 X表示氧原子或亚甲基; n表示1或2的整数。

    Process for producing phenyl-substituted heterocyclic derivative through coupling using transition metal catalyst
    3.
    发明授权
    Process for producing phenyl-substituted heterocyclic derivative through coupling using transition metal catalyst 有权
    使用过渡金属催化剂通过偶联生产苯基取代的杂环衍生物的方法

    公开(公告)号:US08952174B2

    公开(公告)日:2015-02-10

    申请号:US13148820

    申请日:2010-02-26

    IPC分类号: C07D277/56 C07D277/20

    摘要: A process for efficiently producing, through few steps either a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or an intermediate therefore. The process is a novel coupling process which comprises subjecting a compound represented by formula (1) to coupling reaction with a compound represented by formula (2) in the presence of a transition metal compound to thereby obtain a compound represented by formula (3).

    摘要翻译: 通过几步来高效地产生作为高尿酸血症的治疗剂的黄嘌呤氧化酶抑制剂或其中间体的方法。 该方法是一种新颖的偶联方法,其包括使式(1)表示的化合物在过渡金属化合物的存在下与式(2)表示的化合物进行偶联反应,从而得到由式(3)表示的化合物。

    PROCESS FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE THROUGH COUPLING USING TRANSITION METAL CATALYST
    4.
    发明申请
    PROCESS FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE THROUGH COUPLING USING TRANSITION METAL CATALYST 有权
    通过使用过渡金属催化剂的偶联生产苯基取代的杂环衍生物的方法

    公开(公告)号:US20110313169A1

    公开(公告)日:2011-12-22

    申请号:US13148820

    申请日:2010-02-26

    IPC分类号: C07D277/56

    摘要: A process for efficiently producing, through few steps either a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or an intermediate therefore. The process is a novel coupling process which comprises subjecting a compound represented by formula (1) to coupling reaction with a compound represented by formula (2) in the presence of a transition metal compound to thereby obtain a compound represented by formula (3).

    摘要翻译: 通过几步来高效地产生作为高尿酸血症的治疗剂的黄嘌呤氧化酶抑制剂或其中间体的方法。 该方法是一种新颖的偶联方法,其包括使式(1)表示的化合物在过渡金属化合物的存在下与式(2)表示的化合物进行偶联反应,从而得到由式(3)表示的化合物。

    METHOD FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE BY MEANS OF COUPLING METHOD USING PALLADIUM COMPOUND
    5.
    发明申请
    METHOD FOR PRODUCING PHENYL-SUBSTITUTED HETEROCYCLIC DERIVATIVE BY MEANS OF COUPLING METHOD USING PALLADIUM COMPOUND 有权
    通过使用钯化合物的联合方法生产苯基取代的杂环衍生物的方法

    公开(公告)号:US20130158272A1

    公开(公告)日:2013-06-20

    申请号:US13818538

    申请日:2011-08-26

    申请人: Masato Komiyama

    发明人: Masato Komiyama

    摘要: The present invention provides a method for producing a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or intermediates of the same, said method being efficient and using a short process. The present invention is a novel coupling method for obtaining a compound represented by formula (3) by bringing about a coupling reaction between a compound represented by formula (1) and a compound represented by formula (2), in the presence of a palladium compound, a ligand capable of coordinating to the palladium compound, a base, a C1-C40 carboxylic acid, and at least one kind of additive.

    摘要翻译: 本发明提供一种黄嘌呤氧化酶抑制剂的制造方法,所述黄嘌呤氧化酶抑制剂是高尿酸血症的治疗剂或其中间体,所述方法是有效的并且使用短的方法。 本发明是一种新型的通过在式(3)表示的化合物在钯化合物存在下引起由式(1)表示的化合物与式(2)表示的化合物的偶联反应而获得的化合物的偶联方法, ,能与钯化合物配位的配体,碱,C1-C40羧酸和至少一种添加剂。

    Method for producing phenyl-substituted heterocyclic derivative by means of coupling method using palladium compound
    6.
    发明授权
    Method for producing phenyl-substituted heterocyclic derivative by means of coupling method using palladium compound 有权
    通过使用钯化合物的偶联方法制备苯基取代的杂环衍生物的方法

    公开(公告)号:US08916714B2

    公开(公告)日:2014-12-23

    申请号:US13818538

    申请日:2011-08-26

    申请人: Masato Komiyama

    发明人: Masato Komiyama

    摘要: The present invention provides a method for producing a xanthine oxidase inhibitor, which is a therapeutic agent for hyperuricemia, or intermediates of the same, said method being efficient and using a short process. The present invention is a novel coupling method for obtaining a compound represented by formula (3) by bringing about a coupling reaction between a compound represented by formula (1) and a compound represented by formula (2), in the presence of a palladium compound, a ligand capable of coordinating to the palladium compound, a base, a C1-C40 carboxylic acid, and at least one kind of additive.

    摘要翻译: 本发明提供一种黄嘌呤氧化酶抑制剂的制造方法,所述黄嘌呤氧化酶抑制剂是高尿酸血症的治疗剂或其中间体,所述方法是有效的并且使用短的方法。 本发明是一种新型的通过在式(3)表示的化合物在钯化合物存在下引起由式(1)表示的化合物与式(2)表示的化合物的偶联反应而获得的化合物的偶联方法, ,能与钯化合物配位的配体,碱,C1-C40羧酸和至少一种添加剂。