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1. 发明申请

WO1996001825A1 HETEROBICYCLIC DERIVATIVES 审中-公开
标题翻译：杂环衍生物
公开(公告)号：WO1996001825A1
公开(公告)日：1996-01-25
申请号：PCT/JP1995001366
申请日：1995-07-10
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , SHIMAZAKI, Norihiko , WATANABE, Shinya , SAWADA, Akihiko
发明人： FUJISAWA PHARMACEUTICAL CO., LTD. , HEMMI, Mitsue +hf , HEMMI, Keiji +di
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Heterobicyclic derivatives of formula (I) wherein R is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected carboxy(lower)alkyl, acyl(lower)alkyl, heterocyclic group or heterocyclic(lower)alkyl which may have suitable substituent(s), R is aryl which may have suitable substituent(s) or heterocyclic group, and R is hydrogen, lower alkoxy or arylthio, and a pharmaceutically acceptable salt thereof which are useful as PDE IV and TNF inhibitors.
摘要翻译：式（I）的杂双环衍生物，其中R 1为可具有合适取代基的芳基，可具有合适取代基的芳基（低级）烷基，卤代（低级）烷基，被保护的羧基（低级）烷基，可以具有合适取代基的酰基（低级）烷基，杂环基或杂环（低级）烷基，R 2是可具有合适取代基或杂环基的芳基，R 3是氢，低级烷氧基或芳硫基，及其药学上可接受的盐，可用作PDE IV和TNF抑制剂。

2. 发明申请

WO1997024355A1 PYRIDO (2,3-B) PYRAZINE DERIVATIVES 审中-公开
标题翻译：吡嗪（2,3-B）吡嗪衍生物
公开(公告)号：WO1997024355A1
公开(公告)日：1997-07-10
申请号：PCT/JP1996003666
申请日：1996-12-13
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , SHIMAZAKI, Norihiko , SAWADA, Akihiko , WATANABE, Shinya
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： Compounds of formula (I), wherein R is pyridyl(lower)alkyl, N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl; R is aminophenyl, [protected amino]phenyl, [[[halophenyl](lower)alkenoyl]amino]phenyl, [[pyridyl(lower)alkenoyl]amino]phenyl, [[[N-oxidopyridyl](lower)alkenoyl]-amino]phenyl, [[[protected aminopyridyl](lower)alkenoyl]amino]-phenyl, [thiazolylcarbonylamino]phenyl which may have pyridyl, naphthyl having lower alkoxy and halogen, [dihalophenyl](lower)alkenyl, [N-oxidopyridyl](lower)alkenyl, [aminopyridyl](lower)alkenyl, [protected aminopyridyl](lower)alkenyl, [carboxypyridyl](lower)alkenyl, [protected carboxypyridyl](lower)alkenyl, [[pyridyl(lower)alkenyl]pyridyl](lower)alkenyl, [[carboxy(lower)alkenyl]pyridyl](lower)alkenyl, [[protected carboxy(lower)alkenyl]pyridyl](lower)-alkenyl, [pyridyl(lower)alkenyl]pyridyl, lower alkylbenzothiazolyl or [halopyridylcarbonyl]amino, with proviso that when R is [[4-pyridyl(lower)alkenoyl]-amino]phenyl, aminophenyl, [lower alkanoylamino]phenyl or [dihalophenyl](lower)alkenyl, then R is N-oxidopyridyl(lower)alkyl or imidazolyl(lower)alkyl, possess a strong phosphodiesterase IV (PDE IV)-inhibitory activity and a strong inhibitory activity on the production of tumor necrosis factor (TNF).
摘要翻译：式（I）化合物，其中R 1是吡啶基（低级）烷基，N-氧化吡啶基（低级）烷基或咪唑基（低级）烷基; 苯基，[[吡啶基（低级）烯酰基]氨基]苯基，[[[N-氧化吡啶基]（低级）烯酰基 ] - 氨基]苯基，[[保护的氨基吡啶基]（低级）烯酰基]氨基] - 苯基，[噻唑基羰基氨基]苯基，其可具有吡啶基，具有低级烷氧基和卤素的萘基，[二卤苯基]（低级）烯基，[N-氧化吡啶基（低级）烯基，[氨基吡啶基]（低级）烯基，[保护的氨基吡啶基]（低级）烯基，[羧基吡啶基]（低级）烯基，[保护的羧基吡啶基] （低级）烯基，[[羧基（低级）烯基]吡啶基]（低级）链烯基，[[保护的羧基（低级）烯基]吡啶基]（低级） - 烯基，[吡啶基（低级）烯基]吡啶基，低级烷基苯并噻唑基或[ 卤代吡啶基羰基]氨基，条件是当R 2为[[4-吡啶基（低级）烯酰基] - 氨基]苯基，氨基苯基，[低级烷酰基氨基]苯基或[二卤代苯基]（低级）烯基时，则R 1为烷氧基吡啶（低级）烷基或咪唑基（低级）烷基具有强的磷酸二酯酶IV（PDE IV） - 抑制活性和对肿瘤坏死因子（TNF）产生的强抑制活性。

3. 发明申请

WO0232974A3 POLYMER AND ITS USE FOR THE TREATMENT AND/OR PREVENTION OF HYPERPHOSPHOREMIA 审中-公开
标题翻译：聚合物及其用于治疗和/或预防高磷血症的用途
公开(公告)号：WO0232974A3
公开(公告)日：2003-02-20
申请号：PCT/JP0107958
申请日：2001-09-13
申请人： FUJISAWA PHARMACEUTICAL CO , YAMADA AKIRA , SHIMAZAKI NORIHIKO , NAKAYAMA OSAMU , SHOBO MIWAKO , NAKAJIMA YOSHIMITSU , SAWADA HIDEO
发明人： YAMADA AKIRA , SHIMAZAKI NORIHIKO , NAKAYAMA OSAMU , SHOBO MIWAKO , NAKAJIMA YOSHIMITSU , SAWADA HIDEO
IPC分类号： A61K31/74 , C08F220/00 , C08F226/00 , C08F230/08 , C08F251/02 , C08F20/00 , C08F26/00 , C08F30/08
CPC分类号： C08F220/00 , A61K31/74 , C08F226/00 , C08F230/08 , C08F251/02
摘要： A polymer or its salt which is obtainable by polymerization of a monomer of the formula (I) or its salt in the presence of a radical initiator, or by polymerization of a monomer of the formula (I) or its salt with a monomer of the formula (II) or its salt in a molar ratio of (I): (II) being 1:0.1 to 1:25 in the presence of a radical initiatorwherein R1 and R3 are each hydrogen atom or lower alkyl group, R2 and R4 are each acyl group,aliphatic silyl group,amino lower alkyl group which may have one or more suitable substituent(s),heterocyclic group which may have one or more suitable substituent(s) orcarboxy group esterified by the residue of cellulose optionally substituted with one or more lower alkyl and/or lower alkenoyl.
摘要翻译：聚合物或其盐，其可以通过在自由基引发剂的存在下聚合式（I）的单体或其盐，或通过式（I）的单体或其盐与单体的聚合式（II）或其盐在自由基引发剂存在下为（I）：（II）的摩尔比为1:0.1至1:25，其中R 1和R 3各自为氢原子或低级烷基，R 2和R 4为每个酰基，脂族甲硅烷基，可具有一个或多个合适取代基的氨基低级烷基，可具有一个或多个合适的取代基的杂环基或被任选被一个或多个取代基取代的纤维素残基的羧基残基酯化的羧基，更低级烷基和/或低级烯酰基。

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