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1. 发明申请

WO2004099130A3 1,2-DIARYLIMIDAZOLES USEFUL AS INHIBITORS OF COX 审中-公开
标题翻译：作为COX的抑制剂的1,2-二氨基嘧啶有用
公开(公告)号：WO2004099130A3
公开(公告)日：2005-01-27
申请号：PCT/JP2004005987
申请日：2004-04-26
申请人： FUJISAWA PHARMACEUTICAL CO , TAKAHASHI FUMIE , TERASAKA TADASHI , MORITA MASATAKA , KONISHI NOBUKIYO , NAKAMURA KATSUYA
发明人： TAKAHASHI FUMIE , TERASAKA TADASHI , MORITA MASATAKA , KONISHI NOBUKIYO , NAKAMURA KATSUYA
IPC分类号： A61K31/4164 , A61K31/4178 , A61K31/4427 , A61P29/00 , C07D20060101 , C07D233/54 , C07D233/90 , C07D401/04
CPC分类号： C07D401/12 , C07D233/90 , C07D417/12
摘要： A compound of the formula (I) : wherein R is cyano, and the like; R is hydroxy, and the like; R is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译：式（I）的化合物：其中R 1是氰基等; R 2是羟基等; R 3为（低级）烷氧基等; X和Y各自为CH或N; 或其药学上可接受的盐，其可用作药物。

2. 发明申请

WO2004050632A1 PYRAZOLE DERIVATIVES USEFUL AS COX-I INHIBITORS 审中-公开
标题翻译：有用的吡唑衍生物作为COX-I抑制剂
公开(公告)号：WO2004050632A1
公开(公告)日：2004-06-17
申请号：PCT/JP2003/014489
申请日：2003-11-14
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , SHIRAI, Fumiyuki , AZAMI, Hidenori , KAYAKIRI, Natsuko , OKUMURA, Kazuo , NAKAMURA, Katsuya
发明人： SHIRAI, Fumiyuki , AZAMI, Hidenori , KAYAKIRI, Natsuko , OKUMURA, Kazuo , NAKAMURA, Katsuya
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D231/14 , C07D231/22 , C07D231/24 , C07D401/04 , C07D403/10 , C07D403/14 , C07D413/04
摘要： A compound of the formula (I): (1) wherein R 1 is hydrogen or lower alkyl; R 2 is lower alkyl, etc.; R 3 is lower alkoxy, etc. ; R 4 is hydroxy, etc.; X is 0, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.
摘要翻译：式（I）的化合物：（1）其中R 1是氢或低级烷基; R 2是低级烷基等; R 3是低级烷氧基等; R 4是羟基等; X为0，S等; Y是CH或N; Z是低级亚烷基或低级亚烯基; m为0或1; 或其盐，其可用作药物。

3. 发明申请

WO2003068768A1 IMIDAZOLE 4-CARBOXAMIDE COMPOUNDS WITH ADENOSINE DEAMINASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有腺苷脱氨酶抑制活性的咪达唑-4-羧酰胺化合物
公开(公告)号：WO2003068768A1
公开(公告)日：2003-08-21
申请号：PCT/JP2003/001459
申请日：2003-02-12
申请人： FUJISAWA PHARMACEUTICAL Co., Ltd. , TSUJI, Kiyoshi , TERASAKA, Tadashi , KONISHI, Nobukiyo , KATO,Takeshi , NAKAMURA, Katsuya
发明人： TSUJI, Kiyoshi , TERASAKA, Tadashi , KONISHI, Nobukiyo , KATO,Takeshi , NAKAMURA, Katsuya
IPC分类号： C07D405/06
CPC分类号： C07D403/06 , C07D417/06
摘要： Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I): wherein R 1 is optionally substituted aryl or optionally substituted heteroaryl, R 2 is lower alkyl; R 3 is hydroxy or protected hydroxy; X is 0 or S; and - A - is lower alkylene, its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
摘要翻译：具有由式（I）表示的腺苷脱氨酶抑制活性的咪唑化合物：其中R 1为任选取代的芳基或任选取代的杂芳基，R 2为低级烷基; R3是羟基或被保护的羟基; X为0或S; 和 - A - 是低级亚烷基，其前药或其盐。该化合物可用于治疗和/或预防腺苷有效的疾病。

4. 发明申请

WO1997013755A1 1,3,5-TRISUBSTITUTED PYRAZOLES FOR TREAMENT OF INFLAMMATION 审中-公开
标题翻译： 1,3,5-三唑基吡唑类化合物
公开(公告)号：WO1997013755A1
公开(公告)日：1997-04-17
申请号：PCT/JP1996002919
申请日：1996-10-08
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , MATSUO, Masaaki , OKUMURA, Kazuo , OGINO, Takashi , NAKAMURA, Katsuya , NISHIMURA, Hiroaki , HARADA, Keiko , HOTTA, Yuka , TSUJI, Kiyoshi
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D231/12
CPC分类号： C07D231/14 , C07D231/12 , C07D231/16
摘要： A compound of the formula (I) wherein R is hydroxyethyl, 1-hydroxy-1-methylethyl, hydrogen, halogen, nitro, or cyano, R is chloro, cyano, or lower alkyl optionally substituted with halogen, and R is lower alkylthio, lower alkylsulfinyl, or lower alkylsulfonyl, provided that when R is hydrogen, halogen, nitro, or cyano, then R is chloro, and a pharmaceutically acceptable salt thereof, processes for their preparation and pharmaceutical compositions.
摘要翻译：式（I）的化合物，其中R 1是羟乙基，1-羟基-1-甲基乙基，氢，卤素，硝基或氰基，R 2是氯，氰基或任选被卤素取代的低级烷基， R 3为低级烷硫基，低级烷基亚磺酰基或低级烷基磺酰基，条件是当R 1为氢，卤素，硝基或氰基时，则R 2为氯，并且其药学上可接受的盐为其制剂和药物组合物。

5. 发明申请

WO1994029295A1 HETEROCYCLIC DERIVATIVES WITH IMMUNOMODULATING ACTIVITY 审中-公开
标题翻译：具有免疫调节活性的杂环衍生物
公开(公告)号：WO1994029295A1
公开(公告)日：1994-12-22
申请号：PCT/JP1994000824
申请日：1994-05-24
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , MATSUO, Masaaki , TSUJI, Kiyoshi , NAKAMURA, Katsuya , SPEARS, Glen, W.
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , C07D215/56 , C07D401/14 , C07D413/06 , C07D471/06 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Heterocyclic derivatives of formula (I) wherein R is lower alkyl; R is hydroxy, protected hydroxy or halogen; (a) is bicyclic heterocyclic group containing at least one nitrogen atom, which may have suitable substituent(s); and Y is a bivalent radical of (b) (in which R is hydrogen or lower alkoxy; R is hydrogen, lower alkyl, lower alkoxy, halogen, etc.; R is hydrogen, halogen or lower alkoxy, etc.; R is hydrogen or lower alkoxy, etc.), etc. and a pharmaceutically acceptable salt thereof which are useful as a medicament.
摘要翻译：式（I）的杂环衍生物，其中R 5为低级烷基; R 6是羟基，保护的羟基或卤素; （a）是含有至少一个氮原子的二环杂环基，其可以具有合适的取代基; 并且Y是（b）的二价基团（其中R 1是氢或低级烷氧基; R 2是氢，低级烷基，低级烷氧基，卤素等; R 3是氢，卤素或低级烷氧基等; R 4为氢或低级烷氧基等）等及其药学上可接受的盐，其可用作药物。

6. 发明申请

WO2004060367A1 IMIDAZOLE AND TRIAZOLE DERIVATIVES USEFUL AS SELECTIVE COX-1 INHIBITORS 审中-公开
标题翻译：作为选择性COX-1抑制剂有用的咪唑和三唑衍生物
公开(公告)号：WO2004060367A1
公开(公告)日：2004-07-22
申请号：PCT/JP2003/015921
申请日：2003-12-12
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TAKAHASHI, Fumie , NAKAGAWA, Toshiya , MATSUSHIMA, Yuji , NAKAMURA, Katsuya
发明人： TAKAHASHI, Fumie , NAKAGAWA, Toshiya , MATSUSHIMA, Yuji , NAKAMURA, Katsuya
IPC分类号： A61K31/4164
CPC分类号： A61K31/4164 , A61K31/4196 , C07D233/54 , C07D233/90 , C07D249/08 , C07D401/04 , C07D403/12
摘要： A compound of the formula (I): or salts thereof, which are useful for treatment and/or prevention of inflammatory conditions, various pains, collagen diseases, autoimmune diseases, thrombosis, cancer or neurodengenerative diseases.
摘要翻译：用于治疗和/或预防炎性病症，各种疼痛，胶原病，自身免疫疾病，血栓形成，癌症或神经再生疾病的式（I）化合物或其盐。

7. 发明申请

WO0055155A3 HETEROCYCLIC COMPOUNDS AS ADENOSINE DEAMINASE INHIBITORS 审中-公开
标题翻译：作为腺苷类杀虫剂抑制剂的杂环化合物
公开(公告)号：WO0055155A3
公开(公告)日：2001-03-22
申请号：PCT/JP0001316
申请日：2000-03-03
申请人： FUJISAWA PHARMACEUTICAL CO , TERASAKA TADASHI , SEKI NOBUO , TSUJI KIYOSHI , NAKANISHI ISAO , KINOSHITA TAKAYOSHI , NAKAMURA KATSUYA
发明人： TERASAKA TADASHI , SEKI NOBUO , TSUJI KIYOSHI , NAKANISHI ISAO , KINOSHITA TAKAYOSHI , NAKAMURA KATSUYA
IPC分类号： C07D249/08 , A61K31/4174 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/695 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P5/14 , A61P7/04 , A61P7/06 , A61P9/10 , A61P9/14 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P17/16 , A61P19/02 , A61P19/04 , A61P19/06 , A61P19/08 , A61P21/00 , A61P21/04 , A61P25/06 , A61P27/02 , A61P29/00 , A61P35/02 , A61P37/02 , A61P37/06 , A61P43/00 , C07D233/90 , C07D249/10 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04 , C07D521/00 , C07F7/18 , A61K31/395
CPC分类号： C07D249/08 , C07D231/12 , C07D233/56 , C07D233/90 , C07D249/10 , C07D401/14 , C07D403/06 , C07D403/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/04 , C07F7/1852 , C07F7/1856 , Y02P20/55
摘要： Heterocyclic compounds of formula (I) wherein B is (1) [wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino (lower) alkyl; A is lower alkylene; W is heterocyclic or carbocyclic group, each of which may have one or more substituent(s); Z is heterocyclic group selected from the group consisting of imidazolyl, triazolyl, imidazopyridyl and adenyl, each of which may have one or more subtituent (s); or a salt thereof, provided that when W is aryl which may have one or more substituent(s), then (i) Z is triazolyl, imidazopyridyl or adenyl, each of which may have one or more substituent(s); (ii) Z is imidazolyl which may have one or more substituent(s) and B is lower alkanoyl or hydroxyimino(lower) alkyl; or (iii) Z is imidazolyl which may have one or more substituent(s) and R1 and R2 are both lower alkyl; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译：式（I）的杂环化合物，其中B是（1）[其中R 1是氢或低级烷基; R2是氢或低级烷基; 和X为氢或羟基保护基]，低级烷酰基或羟基亚氨基（低级）烷基; A是低级亚烷基; W是杂环或碳环基，其各自可以具有一个或多个取代基; Z是选自咪唑基，三唑基，咪唑并吡啶基和腺苷酸的杂环基，其各自可以具有一个或多个取代基; 条件是当W是可具有一个或多个取代基的芳基时，则（i）Z是三唑基，咪唑并吡啶基或腺苷酸，它们各自可以具有一个或多个取代基; （ii）Z是可以具有一个或多个取代基的咪唑基，B是低级烷酰基或羟基亚氨基（低级）烷基; 或（iii）Z是可具有一个或多个取代基的咪唑基，并且R 1和R 2均为低级烷基; 或其药学上可接受的盐，其可用作药物。

8. 发明申请

WO1991019708A1 NEW THIOPHENE DERIVATIVES 审中-公开
标题翻译：新的噻吩衍生物
公开(公告)号：WO1991019708A1
公开(公告)日：1991-12-26
申请号：PCT/JP1991000744
申请日：1991-05-31
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , MATSUO, Masaaki , TSUJI, Kiyoshi , KONISHI, Nobukiyo , NAKAMURA, Katsuya
发明人： FUJISAWA PHARMACEUTICAL CO., LTD.
IPC分类号： C07D333/38
CPC分类号： C07D409/12 , C07D333/12 , C07D333/22 , C07D333/24 , C07D333/32 , C07D333/34 , C07D333/36 , C07D333/38
摘要： This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by general formula (I), wherein R is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclic sulfonyl, hydroxy, substituted or unsubstituted heterocyclic group, R is substituted or unsubstituted aryl, and R is substituted or unsubstituted aryl, provided that R is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.
摘要翻译：本发明涉及具有抗炎和止痛活性并由通式（I）表示的新噻吩衍生物，其中R 1是氢，卤素，氰基，取代的低级烷基，取代或未取代的低级烯基，酰基，硝基，取代或未取代的氨基，磺基，取代或未取代的氨磺酰基，含N的杂环磺酰基，羟基，取代或未取代的杂环基，R 2是取代或未取代的芳基，R 3是取代或未取代的芳基，条件是R 3，是当R 1是氢，卤素或氰基时，被选自氨基，单（低级） - 烷基氨基，酰氨基，低级烷基（酰基）氨基和氨磺酰基的取代基取代的芳基及其药学上可接受的盐，其制备方法和包含其的药物组合物。

9. 发明申请

WO2004099130A2 INHIBITOR OF COX 审中-公开
标题翻译： COX抑制剂
公开(公告)号：WO2004099130A2
公开(公告)日：2004-11-18
申请号：PCT/JP2004/005987
申请日：2004-04-26
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TAKAHASHI, Fumie , TERASAKA, Tadashi , MORITA, Masataka , KONISHI, Nobukiyo , NAKAMURA, Katsuya
发明人： TAKAHASHI, Fumie , TERASAKA, Tadashi , MORITA, Masataka , KONISHI, Nobukiyo , NAKAMURA, Katsuya
IPC分类号： C07D
CPC分类号： C07D401/12 , C07D233/90 , C07D417/12
摘要： A compound of the formula (I) : wherein R 1 is cyano, and the like; R 2 is hydroxy, and the like; R 3 is (lower)alkoxy, and the like; X and Y are each CH or N; or pharmaceutically acceptable salts thereof, which are useful as a medicament.
摘要翻译：式（I）的化合物：其中R 1为氰基等; R 2是羟基等; R 3为（低级）烷氧基等; X和Y各自为CH或N; 或其药学上可接受的盐，其可用作药物。

10. 发明申请

WO2003006437A1 IMIDAZOLE DERIVATIVES AS ADENOSINE DEAMINASE INHIBITORS 审中-公开
标题翻译：咪唑衍生物作为腺苷类杀虫剂抑制剂
公开(公告)号：WO2003006437A1
公开(公告)日：2003-01-23
申请号：PCT/JP2002/006983
申请日：2002-07-10
申请人： FUJISAWA PHARMACEUTICAL CO., LTD. , TERASAKA, Tadashi , KATO, Takeshi , TSUJI, Kiyoshi , NAKAMURA, Katsuya
发明人： TERASAKA, Tadashi , KATO, Takeshi , TSUJI, Kiyoshi , NAKAMURA, Katsuya
IPC分类号： C07D233/90
CPC分类号： C07D401/12 , C07D233/90 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I)wherein R1 is aryl or heterocyclic group which is optionally substituted with substituent(s);R 2 is lower alkyl;R 3 is hydroxy or protected hydroxy;- A - is lower alkylene; and- X - is - O - or - S -;provided that when - X - is - O -, then R 1 is aryl which is substituted with substituent(s), or heterocyclic group which is optionally substituted with substituent(s),its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.
摘要翻译：具有式（I）表示的腺苷脱氨酶抑制活性的咪唑化合物，其中R 1为任选被取代基取代的芳基或杂环基; R 2为低级烷基; R 3为羟基或被保护的羟基; -A-为低级亚烷基; X - 为-O-或-S-;条件是当-X - 为-O-时，R 1为被取代基取代的芳基或任选被取代基取代的杂环基，其前药或其盐。该化合物可用于治疗和/或预防腺苷有效的疾病。

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