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1. 发明申请

WO2004022540A2 PYRIDAZINONE COMPOUND AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：吡咯烷酮化合物及其药物用途
公开(公告)号：WO2004022540A2
公开(公告)日：2004-03-18
申请号：PCT/JP2003/011271
申请日：2003-09-03
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TABUCHI, Seiichiro , TSUTSUMI, Hideo , SATO, Yoshinari , AKAHANE, Atsushi
发明人： TABUCHI, Seiichiro , TSUTSUMI, Hideo , SATO, Yoshinari , AKAHANE, Atsushi
IPC分类号： C07D213/73
CPC分类号： C07D213/64 , C07D213/73 , C07D401/04 , C07D401/14 , C07D417/14
摘要： A pyridazinone or pyridone compound of the following formula (I). wherein',Itor a salt thereof. The pyridazinone or pyridone compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的哒嗪酮或吡啶酮化合物。其中'，它或其盐。本发明的哒嗪酮或吡啶酮化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑症，疼痛，脑血管疾病（例如中风等），心力衰竭等。

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. 发明申请

WO2004089939A1 CONDENSED FURAN DERIVATIVES AS ADENOSINE ANTAGONISTS 审中-公开
标题翻译：浓缩的呋喃衍生物作为腺苷拮抗剂
公开(公告)号：WO2004089939A1
公开(公告)日：2004-10-21
申请号：PCT/JP2004/003435
申请日：2004-03-15
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YONISHI, Satoshi , ITANI, Hiromichi , SATO, Yoshinari , TSUTSUMI, Hideo , AKAHANE, Atsushi
发明人： YONISHI, Satoshi , ITANI, Hiromichi , SATO, Yoshinari , TSUTSUMI, Hideo , AKAHANE, Atsushi
IPC分类号： C07D405/04
CPC分类号： C07D491/04 , C07D405/04
摘要： A novel compound of the following formula (I): wherein Z is a phenyl or pyridyl which condenses to a furan ring; X is CH or N; R 1 is hydrogen or optionally substituted lower alkyl; R 2 is hydrogen, halogen or lower alkoxy; and R 3 is hydrogen, hydroxy, lower alkyl, lower alkoxy or halogen, or a salt thereof. The compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的新化合物：其中Z是与呋喃环稠合的苯基或吡啶基; X是CH或N; R 1是氢或任选取代的低级烷基; R 2是氢，卤素或低级烷氧基; 和R 3是氢，羟基，低级烷基，低级烷氧基或卤素，或其盐。本发明的化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴随帕金森病的痴呆等），帕金森病，焦虑症，疼痛，脑血管疾病（例如中风等），心力衰竭等。

4. 发明申请

WO2003057689A1 AMINOPYRIMIDINE COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：氨基嘧啶化合物，其制备方法和含有它们的药物组合物
公开(公告)号：WO2003057689A1
公开(公告)日：2003-07-17
申请号：PCT/JP2002/013796
申请日：2002-12-27
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TSUTSUMI, Hideo , YONISHI, Satoshi , AKAHANE, Atsushi
发明人： TSUTSUMI, Hideo , YONISHI, Satoshi , AKAHANE, Atsushi
IPC分类号： C07D403/04
CPC分类号： C07D401/14 , C07D403/04 , C07D409/14
摘要： An aminopyrimidine compound of the following formula (I). wherein Q is (a) or (b) in which R and R' are each optionally substituted aryl or heterocyclic group,R 5 is hydrogen, halogen, lower alkyl,optionally substituted hydroxy, optionally substituted amino which may form N-containing heterocyclic group, optionally substituted mercapto, lower alkylsulfinyl or lower alkylsulfonyl, and X is oxygen or sulfur; R 1 is hydrogen, optionally substituted lower alkyl or cyclo (lower) alkyl which may be interrupted by an oxygen atom; R 2 and R 3 are each independently hydrogen, lower alkyl, acyl, aryl or heterocyclic(lower)alkyl, R 2 and R 3 may be combined together with N atom to which they are attached to form N-containing heterocyclic group; or a salt thereof. The aminopyrimidine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的氨基嘧啶化合物。其中Q为（a）或（b），其中R和R'各自为任选取代的芳基或杂环基，R 5为氢，卤素，低级烷基，任选取代的羟基，任选取代的氨基，可以形成含氮杂环基，任选取代的巯基，低级烷基亚磺酰基或低级烷基磺酰基，X是氧或硫; R 1是氢，任选取代的可被氧原子间隔的低级烷基或环（低级）烷基; R 2和R 3各自独立地为氢，低级烷基，酰基，芳基或杂环（低级）烷基，R 2和R > 3 可以与它们所连接的N原子一起形成含氮杂环基; 或其盐。本发明的氨基嘧啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴有帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

5. 发明申请

WO2005095384A1 PYRAZINE DERIVATIVES AND PHARMACEUTICAL USE THEREOF AS ADENOSINE ANTAGONISTS 审中-公开
标题翻译：吡嗪衍生物和药物用途作为腺苷拮抗剂
公开(公告)号：WO2005095384A1
公开(公告)日：2005-10-13
申请号：PCT/JP2005/005663
申请日：2005-03-22
申请人： Astellas Phama Inc. , TSUTSUMI, Hideo , TABUCHI, Seiichiro , MINAGAWA, Masatoshi , AKAHANE, Atsushi
发明人： TSUTSUMI, Hideo , TABUCHI, Seiichiro , MINAGAWA, Masatoshi , AKAHANE, Atsushi
IPC分类号： C07D403/04
CPC分类号： C07D417/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D487/04
摘要： A pyrazine derivative of the following formula (I): wherein is hydrogen or optionally substituted lower alkyl; X,is hydrogen, halogen, hydroxy, cyano, acyl, or amino, aryl, heterocyclic group or the like; Y is hydrogen, halogen, hydroxy, acyl, amino, or the like; Z is aryl . or heteroaryl, each of which is optionallysubstituted; or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease,anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物：其中是氢或任意取代的低级烷基; X是氢，卤素，羟基，氰基，酰基或氨基，芳基，杂环基等; Y是氢，卤素，羟基，酰基，氨基等; Z是芳基。或杂芳基，其各自任选被取代; 或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴随帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

6. 发明申请

WO2003004494A1 PYRIDAZINONE COMPOUND AS ADENOSINE ANTAGONISTS 审中-公开
标题翻译：吡咯烷酮化合物作为腺苷拮抗剂
公开(公告)号：WO2003004494A1
公开(公告)日：2003-01-16
申请号：PCT/JP2002/006671
申请日：2002-07-02
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TSUTSUMI, Hideo , AKAHANE, Atsushi
发明人： TSUTSUMI, Hideo , AKAHANE, Atsushi
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： A compound of the following formula (I): wherein R 1 , R 2 , R 3 and R 4 are each independently hydrogen or a suitable substituent, in which R 1 and R 2 together or R 2 and R 3 together may form -(CH 2 ) n - (wherein n is an integer of 1 to 12) which is optionally interrupted by heteroatom(s) and optionally having suitable substituent(s); andW is , or ,or a salt thereof.The compound of the above formula (I) and a salt thereof are adenosine antagonists and are useful as medicaments.
摘要翻译：下式（I）的化合物：其中R 1，R 2，R 3和R 4各自独立地为氢或适当的取代基，其中R 1和R 2为一起或R 2和R 3一起可以形成 - （CH 2）n - （其中n为1至12的整数），其任选地被杂原子中断并任选具有合适的取代基; 和W是或其盐。上式（I）的化合物及其盐是腺苷拮抗剂，可用作药物。

7. 发明申请

WO2003045950A1 PYRAZOLOPYRIDINE DERIVTIVES AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：吡咯并吡啶衍生物及其药物用途
公开(公告)号：WO2003045950A1
公开(公告)日：2003-06-05
申请号：PCT/JP2002/012381
申请日：2002-11-27
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TANAKA, Akira , MINAGAWA, Masatoshi , AKAHANE, Atsushi
发明人： TANAKA, Akira , MINAGAWA, Masatoshi , AKAHANE, Atsushi
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A pyrazolopyridine compound of the following formula (I). Wherein R 1 is hydrogen, optionally substituted lower alkyl or cyclo (lower) alkyl, R 2 is hydrogen, optionally substituted hydroxy, acyl or optionally substituted amino, R 3 is hydrogen or halogen, and at least one of R 1 , R 2 and R 3 are not hydrogen, or a salt thereof. The pyrazolopyridine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc), heart failure and the like.
摘要翻译：下式（I）的吡唑并吡啶化合物。其中R 1是氢，任选取代的低级烷基或环（低级）烷基，R 2是氢，任选取代的羟基，酰基或任选取代的氨基，R 3是氢或卤素， R 1，R 2和R 3不是氢，或其盐。本发明的吡唑并吡啶化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴随帕金森病的痴呆等），帕金森病，焦虑症，疼痛，脑血管疾病（例如中风等），心力衰竭等。

8. 发明申请

WO2002100864A1 PYRAZOLOPYRAZINE COMPOUND AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：吡咯并吡嗪化合物及其药物用途
公开(公告)号：WO2002100864A1
公开(公告)日：2002-12-19
申请号：PCT/JP2002/005453
申请日：2002-06-03
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , AKAHANE, Atsushi , TANAKA, Akira
发明人： AKAHANE, Atsushi , TANAKA, Akira
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4985
摘要： A pyrazolopyrazine compound of formula (I) wherein R 1 is hydrogen or a suitable substituent; and R 2 is hydrogen or halogen, or a salt thereof. The pyrazolopyrazine compound (I) and salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, dementia accompanying Parkinson's disease, etc.), Parkinson's disease, anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure and the like.
摘要翻译：式（I）的吡唑并吡嗪化合物，其中R 1是氢或合适的取代基; 和R 2是氢或卤素，或其盐。本发明的吡唑并吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁症，痴呆（例如阿尔茨海默氏病，脑血管性痴呆，伴随帕金森病的痴呆等），帕金森病，焦虑，疼痛，脑血管疾病（例如中风等），心力衰竭等。

9. 发明申请

WO2005040151A1 PYRAZINE DERIVATIVES AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：吡嗪衍生物及其药物用途
公开(公告)号：WO2005040151A1
公开(公告)日：2005-05-06
申请号：PCT/JP2004/016193
申请日：2004-10-25
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , YONISHI, Satoshi , AOKI, Satoshi , MATSUSHIMA, Yuji , AKAHANE, Atsushi
发明人： YONISHI, Satoshi , AOKI, Satoshi , MATSUSHIMA, Yuji , AKAHANE, Atsushi
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A pyrazine derivative of the following formula (I): or a salt thereof. The pyrazine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer’s disease, cerebrovascular dementia, dementia accompanying Parkinson’s, disease, etc.), Parkinson’s disease, anxiety, pain, cerebrovascular disease (e.g. stroke), etc.), heart failure and the like.
摘要翻译：下式（I）的吡嗪衍生物或其盐。本发明的吡嗪化合物（I）及其盐是腺苷拮抗剂，可用于预防和/或治疗抑郁，痴呆（例如阿尔茨海默病，脑血管性痴呆，伴随帕金森病，疾病等的痴呆），帕金森病疾病，焦虑，疼痛，脑血管疾病（例如中风）等），心力衰竭等。

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