公开(公告)号：EP0916646A2

公开(公告)日：1999-05-19

申请号：EP99101692.4

申请日：1994-09-26

Applicant: ABBOTT LABORATORIES

Inventor： Stuk, Timothy, L ,  Kerdesky, Francis, A., J. ,  Lijewski, Linda, M ,  Norbeck, Daniel, W ,  Scarpetti, David ,  Tien, Jien-Heh, J ,  Allen, Michael, S ,  Langridge, Denton, C ,  Melcher, Laura ,  Reno, Daniel, S ,  Sham, Hing, Leung ,  Zhao, Chen ,  Haight, Anthony, R. ,  Leanna, M., Robert ,  Morton, Howard, E. ,  Robbins, Timothy, A. ,  Sowin, Thomas, J.

IPC: C07C225/16 ,  C07C213/00 ,  C07C255/42 ,  C07C271/20 ,  C07C269/06 ,  C07C215/28 ,  C07C251/40

CPC classification number: C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08

Abstract: Processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R 6 and R 7 are each hydrogen or R 6 and R 7 are independently selected from (i), wherein R a and R b are independently selected from hydrogen, loweralkyl and phenyl and R c , R d and R e 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 R 6 is as defined above and R 7 is R 7a OC (O)- wherein R 7a is loweralkyl or benzyl; or R 6 and R 7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein R f , R g , R h and R i are independently selected from hydrogen, loweralkyl, alkoxy, halogen, and trifluoromethyl and R 8 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 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R 6如上所定义，且R 7为R 7aOC（O） - ，其中R 7a为低级烷基或苄基; 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，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。

公开(公告)号：EP0916646A3

公开(公告)日：1999-08-18

申请号：EP99101692.4

申请日：1994-09-26

Applicant: ABBOTT LABORATORIES

Inventor： Stuk, Timothy, L ,  Kerdesky, Francis, A., J. ,  Lijewski, Linda, M ,  Norbeck, Daniel, W ,  Scarpetti, David ,  Tien, Jien-Heh, J ,  Allen, Michael, S ,  Langridge, Denton, C ,  Melcher, Laura ,  Reno, Daniel, S ,  Sham, Hing, Leung ,  Zhao, Chen ,  Haight, Anthony, R. ,  Leanna, M., Robert ,  Morton, Howard, E. ,  Robbins, Timothy, A. ,  Sowin, Thomas, J.

IPC: C07C225/16 ,  C07C213/00 ,  C07C255/42 ,  C07C271/20 ,  C07C269/06 ,  C07C215/28 ,  C07C251/40

CPC classification number: C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08

Abstract: Processes are disclosed which are useful for the preparation of a substantially pure compound of formula (3), wherein R 6 and R 7 are each hydrogen or R 6 and R 7 are independently selected from (i), wherein R a and R b are independently selected from hydrogen, loweralkyl and phenyl and R c , R d and R e 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 R 6 is as defined above and R 7 is R 7a OC (O)- wherein R 7a is loweralkyl or benzyl; or R 6 and R 7 taken together with the nitrogen atom to which they are bonded are (a) or (b), wherein R f , R g , R h and R i are independently selected from hydrogen, loweralkyl, alkoxy, halogen, and trifluoromethyl and R 8 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.

公开(公告)号：EP2386548A2

公开(公告)日：2011-11-16

申请号：EP11170183.5

申请日：2004-07-30

Applicant: Abbott Laboratories

Inventor： Robbins, Timothy, A. ,  Zhu, Helen ,  Shao, Jun

IPC: C07D277/56

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。 取代的噻唑乙基2-（4-羟基苯基）-4-甲基-1,3-噻唑-5-羧酸酯也被称为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从而阻断尿酸生成的取代噻唑。

公开(公告)号：EP0916646B1

公开(公告)日：2003-05-02

申请号：EP99101692.4

申请日：1994-09-26

Applicant: ABBOTT LABORATORIES

Inventor： Stuk, Timothy, L ,  Kerdesky, Francis, A., J. ,  Lijewski-Linch, Linda, M ,  Norbeck, Daniel, W ,  Scarpetti, David ,  Tien, Jien-Heh, J ,  Allen, Michael, S ,  Langridge, Denton, C ,  Melcher, Laura ,  Reno, Daniel, S ,  Sham, Hing, Leung ,  Zhao, Chen ,  Haight, Anthony, R. ,  Leanna, M., Robert ,  Morton, Howard, E. ,  Robbins, Timothy, A. ,  Sowin, Thomas, J.

IPC: C07C225/16 ,  C07C213/00 ,  C07C255/42 ,  C07C271/20 ,  C07C269/06 ,  C07C215/28 ,  C07C251/40

CPC classification number: C07D221/14 ,  C07B2200/07 ,  C07C213/00 ,  C07C215/28 ,  C07C225/16 ,  C07C251/40 ,  C07C255/42 ,  C07C269/06 ,  C07C271/20 ,  C07D209/44 ,  C07C215/08