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1. 发明申请

WO2003040110A1 TRIAZOLE DERIVATIVES AS CYCLOOXYGENASE (COX) INHIBITORS 审中-公开
标题翻译：三唑衍生物作为CYCLOOXYGENASE（COX）抑制剂
公开(公告)号：WO2003040110A1
公开(公告)日：2003-05-15
申请号：PCT/JP2002/011314
申请日：2002-10-30
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , AOKI, Satoshi , NAKAGAWA, Toshiya , KONISHI, Nobukiyo , NAKAMURA, Katsuya , OMORI, Hiroki , KUBOTA, Ariyoshi , HASHIMOTO, Norio
发明人： AOKI, Satoshi , NAKAGAWA, Toshiya , KONISHI, Nobukiyo , NAKAMURA, Katsuya , OMORI, Hiroki , KUBOTA, Ariyoshi , HASHIMOTO, Norio
IPC分类号： C07D249/08
CPC分类号： C07D249/08 , C07D401/04 , C07D401/14 , C07D403/10 , C07D413/10 , C07D413/12 , C07D417/10 , C07D417/12
摘要： Compound of formula (I) wherein R 1 is lower alkyl which is optionally substituted with halogen, cyano, N,N-di(lower)alkylcarbamoyl, phenyl optionally substituted with halogen, or heterocyclic group, cyclo(lower)alkyl, lower alkynyl, or N,N-di(lower) alkylcarbamoyl; R 2 is lower alkyl, lower alkoxy amino, cyano, or 1H-pyrrol-1-yl; R 3 is lower alkyl, lower alkoxy, or cyano; X is O, S, SO or SO 2 ; Y and Z are each CH or N; and m is 0 or 1; or salts thereof, which are useful as a medicament.
摘要翻译：氰基，N，N-二（低级）烷基氨基甲酰基，任选被卤素取代的苯基或杂环基，低级（低级）烷基，低级炔基或N，N-二（低级）烷基氨基甲酰基; R 2是低级烷基，低级烷氧基氨基，氰基或1H-吡咯-1-基; R 3是低级烷基，低级烷氧基或氰基; X是O，S，SO或SO 2; Y和Z各自为CH或N; m为0或1; 或其盐，其可用作药物。

2. 发明申请

WO2003039451A3 THIAZOLE PYRIDAZINONES AS ADENOSINE ANTAGONISTS 审中-公开
公开(公告)号：WO2003039451A3
公开(公告)日：2003-05-15
申请号：PCT/JP2002/011639
申请日：2002-11-08
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TSUTSUMI, Hideo , TABUCHI, Seiichiro , AKAHANE, Atsushi , YASUDA, Hironobu , OMORI, Hiroki , TEMMARU, Kiyoshi , ZANKA, Atsuhiko
发明人： TSUTSUMI, Hideo , TABUCHI, Seiichiro , AKAHANE, Atsushi , YASUDA, Hironobu , OMORI, Hiroki , TEMMARU, Kiyoshi , ZANKA, Atsuhiko
IPC分类号： A61K31/501
摘要： A thiazole derivative of the formula (I):wherein R is 1-optionally substituted-6-oxo-1,6-dihydro-3-pyridazinyl, R' is an optionally substituted phenyl, and R 2 is hydrogen, a group of the formula (i): wherein R 4 is hydrogen, lower alkyl or lower alkenyl, and R 5 is hydrogen, optionally substituted lower alkyl, acyl, cyclo(lower)alkyl, lower alkenyl, optionally substituted aryl or heterocyclic, or a group of the formula (ii): wherein X is oxygen or sulfur, R 8 is hydrogen or lower alkyl, R 9 is hydrogen, optionally substituted lower alkyl, cyclo(lower)alkyl, lower alkoxy or mono- or di-lower alkylamino or R 8 and R 9 may be combine together to form optionally substituted saturated N-containing heterocyclic, or a salt thereof._The compounds are useful as Adenosine antagonists. The application also discloses an improved process for the preparation of pyridazinones (XII-1)

3. 发明公开

EP1010695A1 PROCESS FOR PRODUCING QUINAZOLINE DERIVATIVES 失效
标题翻译：生产喹唑啉衍生物的方法
公开(公告)号：EP1010695A1
公开(公告)日：2000-06-21
申请号：EP98907257.4
申请日：1998-03-17
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： OMORI, Hiroki , GOTO, Shunsuke , TSUBOI, Hiroyuki , FUKAGAWA, Masayasu , KAGARA, Kooji
IPC分类号： C07D239/96
CPC分类号： C07D239/96
摘要： This invention provides an industrially useful process for producing a quinazoline derivative (I) of the general formula:
[wherein R 1 is hydrogen or halogen; R 2 is carboxy or protected carboxy; A is lower alkylene] or its salt on a commercial scale which comprises reacting a compound of the general formula:
[wherein R 1 is hydrogen or halogen] or its salt with a silylating agent and then with a compound of the general formula:

Cl-A-R 2 (III)

[wherein R2 is carboxy or protected carboxy; A is lower alkylene] or its salt, optionally followed by desilylation.
摘要翻译：本发明提供了一种工业上有用的制备下列通式的喹唑啉衍生物（Ⅰ）的方法：[其中R1是氢或卤素; R2是羧基或保护的羧基; A为商业规模的低级亚烷基]或其盐，该方法包括使以下通式的化合物[其中R1为氢或卤素]或其盐与甲硅烷基化剂反应，然后与下列通式的化合物反应：C1-A -R2（III）[其中R2是羧基或被保护的羧基; A是低级亚烷基]或其盐，任选接着脱甲硅烷基化。

4. 发明公开

EP0648747A1 NOVEL INTERMEDIATE FOR SYNTHESIS AND PRODUCTION OF AMINO ACID DERIVATIVE 失效
标题翻译： NEUE ZWISCHENPRODUKTE ZUR SYNTHESE UND PRODUKTION VONAMINOSÄUREDERIVATEN。
公开(公告)号：EP0648747A1
公开(公告)日：1995-04-19
申请号：EP93913599.2
申请日：1993-06-28
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： KAGARA, Kooji , KAWAI, Nobutaka , MACHIYA, Koji , FURUTERA, Tetsuo , NAKAMURA, Takashi , OMORI, Hiroki
IPC分类号： C07D233/64
CPC分类号： C07D233/64 , C07D233/54 , Y02P20/55
摘要： A novel intermediate (II) for use in synthesis which is useful for the production of an amino acid derivative (I) having a renin-inhibiting activity, and a process for producing the derivative (I) which involves the reaction step represented by the figure, wherein R¹ represents lower alkyl, etc., which may be substituted by -NR⁷-CO-NR⁸R⁹ (wherein R⁷ represents hydrogen or lower alkyl, and R⁸ and R⁹ may be combined together with the adjacent nitrogen atom to represent an optionally substituted heterocyclic group), etc.; R² represents hydrogen, lower alkyl, etc., R³ represents hydrogen or lower alkyl; R⁴ represents hydrogen or an N-protecting group; R⁵ represents hydrogen or a carboxyl-protecting group; and R¹⁰ represents lower alkyl. This process, proceeding via the intermediate (II), is industrially advantageous because the final product (I) can be obtained in a high yield from an inexpensive starting material as compared with the conventional processes and hence the production cost can be reduced remarkably.
摘要翻译：用于制备具有肾素抑制活性的氨基酸衍生物（I）的合成用新型中间体（II）及其制造方法，该方法涉及由图所示的反应步骤其中R 1表示低级烷基等，其可以被-NR 7 -CO-NR 8 R 9取代（其中R 7表示氢或低级烷基，R 8 >和R 9可以与相邻的氮原子一起组合以代表任选取代的杂环基）等; R 2表示氢，低级烷基等，R 3表示氢或低级烷基; R 4表示氢或N-保护基; R 5表示氢或羧基保护基; R 1表示低级烷基。通过中间体（II）进行的该方法在工业上是有利的，因为与常规方法相比，可以从廉价的原料获得最终产物（I），因此可以显着降低生产成本。

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