SUBSTITUTED THIAZOLES
    1.
    发明申请
    SUBSTITUTED THIAZOLES 审中-公开
    替代THIAZOLES

    公开(公告)号:WO2005012273A2

    公开(公告)日:2005-02-10

    申请号:PCT/US2004/024758

    申请日:2004-07-30

    CPC classification number: C07D277/56

    Abstract: This invention is directed to processes for making substituted thiazoles. The substituted thiazole, ethyl 2-(4-hydroxyphenyl)-4-methyl-1,3-thiazole-5-carboxylate, also known as TEI-6720, is useful for treatment of gout and hyperuricemia. This compound belongs to a class of substituted thiazoles that inhibit xanthine oxidase and thus block uric acid production.

    Abstract translation: 本发明涉及制备取代噻唑的方法。 取代的噻唑,2-(4-羟基苯基)-4-甲基-1,3-噻唑-5-羧酸乙酯,也称为TEI-6720,可用于治疗痛风和高尿酸血症。 该化合物属于一类抑制黄嘌呤氧化酶并因此阻断尿酸生产的取代噻唑类。

    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE
    2.
    发明申请
    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE 审中-公开
    制备取代的2.5-二氨基-3-羟基己烷的方法

    公开(公告)号:WO1996004232A1

    公开(公告)日:1996-02-15

    申请号:PCT/US1995009133

    申请日:1995-07-17

    CPC classification number: C07C213/00 C07C215/32

    Abstract: A process is disclosed for the preparation of the substantially pure compound of formula (I) comprising catalytic hydrogenation of a compound of formula (II) wherein R6 and R7 are independently selected from (i) wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b) wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; or an acid addition salt thereof.

    Abstract translation: 公开了制备基本上纯的式(I)化合物的方法,其包括式(II)化合物的催化氢化,其中R 6和R 7独立地选自(ⅰ)其中R a和R b独立地选自氢, 苯基和Rc,Rd和Re独立地选自氢,低级烷基,三氟甲基,烷氧基,卤素和苯基; 和(ii)其中萘基环是未取代的或被一个,两个或三个独立地选自低级烷基,三氟甲基,烷氧基和卤素的取代基取代; 或者R 6和R 7与它们所键合的氮原子一起是(a)或(b),其中R f,R g,Rh和R 1独立地选自氢,低级烷基,烷氧基,卤素和三氟甲基; 或其酸加成盐。

    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2,5-DIAMINO-3-HYDROXYHEXANE 审中-公开
    制备取代的2,5-二氨基-3-羟基己酸的方法

    公开(公告)号:WO1995011224A1

    公开(公告)日:1995-04-27

    申请号:PCT/US1994010852

    申请日:1994-09-26

    Abstract: Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R6 and R7 are each hydrogen or R6 and R7 are independently selected from (i), wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 is as defined above and R7 is R7aOC (O)-wherein R7a is loweralkyl or benzyl; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R8 is hydrogen or -C(O)R" wherein R" is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

    Abstract translation: 公开了可用于制备基本上纯的式(3)化合物的中间体和方法,其中R 6和R 7各自为氢或R 6和R 7独立地选自(ⅰ),其中R a和R b独立地选自氢 ,低级烷基和苯基,Rc,Rd和Re独立地选自氢,低级烷基,三氟甲基,烷氧基,卤素和苯基; 和(ii)其中萘基环是未取代的或被一个,两个或三个独立地选自低级烷基,三氟甲基,烷氧基和卤素的取代基取代; 或R 6如上所定义,且R 7为R 7 a OC(O) - 其中R 7a为低级烷基或苄基; 或R 6和R 7与它们所键合的氮原子一起是(a)或(b),其中R f,R g,Rh和R 1独立地选自氢,低级烷基,烷氧基,卤素和三氟甲基,并且R 8是氢或 -C(O)R“其中R”是低级烷基,烷氧基,苄氧基或苯基,其中苯环是未取代的或被一个,两个或三个独立地选自低级烷基,三氟甲基,烷氧基和卤素的取代基取代; 或其酸加成盐。

    PROCESS FOR THE PREPARATION OF SUBSTITUTED THIAZOLES
    6.
    发明公开
    PROCESS FOR THE PREPARATION OF SUBSTITUTED THIAZOLES 有权
    用于生产取代噻唑

    公开(公告)号:EP1651624A2

    公开(公告)日:2006-05-03

    申请号:EP04779726.1

    申请日:2004-07-30

    CPC classification number: C07D277/56

    Abstract: This invention is directed to processes for making substituted thiazoles. The substituted thiazole, ethyl 2-(4-hydroxyphenyl)-4-methyl-1,3-thiazole-5-carboxylate, also known as TEI-6720, is useful for treatment of gout and hyperuricemia. This compound belongs to a class of substituted thiazoles that inhibit xanthine oxidase and thus block uric acid production.

    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE
    7.
    发明授权
    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE 失效
    用于生产取代的2,5-二氨基-3-羟基己烷

    公开(公告)号:EP0773921B1

    公开(公告)日:1999-12-01

    申请号:EP95926318.7

    申请日:1995-07-17

    CPC classification number: C07C213/00 C07C215/32

    Abstract: A process is disclosed for the preparation of the substantially pure compound of formula (I) comprising catalytic hydrogenation of a compound of formula (II) wherein R6 and R7 are independently selected from (i) wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b) wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; or an acid addition salt thereof.

    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE
    9.
    发明公开
    PROCESS FOR THE PREPARATION OF A SUBSTITUTED 2.5-DIAMINO-3-HYDROXYHEXANE 失效
    用于生产取代的2,5-二氨基-3-羟基己烷

    公开(公告)号:EP0773921A1

    公开(公告)日:1997-05-21

    申请号:EP95926318.0

    申请日:1995-07-17

    CPC classification number: C07C213/00 C07C215/32

    Abstract: A process is disclosed for the preparation of the substantially pure compound of formula (I) comprising catalytic hydrogenation of a compound of formula (II) wherein R6 and R7 are independently selected from (i) wherein Ra and Rb are independently selected from hydrogen, loweralkyl and phenyl and Rc, Rd and Re are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and (ii) wherein the naphthyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R6 and R7 taken together with the nitrogen atom to which they are bonded are (a) or (b) wherein Rf, Rg, Rh and Ri are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl; or an acid addition salt thereof.

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