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1. 发明授权

EP1062201B1 HALOGENATED AMIDINO AMINO ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 有权
标题翻译：致癌氨基酸衍生物ALS HEMMSTOFFE DER STICKSTOFFMONOXID-SYNTHASE
公开(公告)号：EP1062201B1
公开(公告)日：2004-09-29
申请号：EP99908324.9
申请日：1999-03-04
申请人： G.D. SEARLE & CO.
发明人： HALLINAN, E., Ann , PITZEL, Barnett, S. , SPANGLER, Dale, P. , BERGMANIS, Arija, A. , HAGEN, Timothy, J. , TSYMBALOV, Sofya , TOTH, Mihaly, V. , WEBBER, R., Keith , HANSEN, Donald, W., Jr. , AWASTHI, Alik, K.
IPC分类号： C07C257/14 , C07C323/58 , C07D333/24 , A61K31/38 , A61K31/55
CPC分类号： C07D333/24 , C07C257/14 , C07C323/58 , C07C2601/02
摘要： Halogenated amidino aminoacid derivatives (I) are new. Aminoacid derivatives of formula (I) and their salts are new. [Image] R1H, alkyl, alkenyl or alkynyl; R2as R1 or R- or S-alpha -aminoacid; R3, R4as R1 or NO2; R1-R4 are optionally substituted by T; T : lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, OH, lower alkoxy, aryloxy, SH, lower thioalkoxy, halo, CN, NO2, NH2, COOH, carboxyalkyl, carboxyaryl, amidino or guanidino; R11OH or R- or S-alpha -aminoacid; G : (i) 1-10C alkylene, 2-10C alkenylene or 2-10C alkynylene (all optionally substituted by one or more of halo, OH, CF3, NO2, CN, NH2, =CH2, alkyl, alkenyl, alkynyl or alkoxy (all optionally substituted by T or CF3)); (ii) (CH2)p(CX1X2)r(CH2)sQ(CH2)t(CX3X4)u(CH2)v; or (iii) (CH2)q(CX5X6)y(CH2)zA(CH2)k(CX7X8)j(CH2)h; p, r, s, t, u, v, w, y, z, k, j, h : 0-3; Q : Q = O, CO, S(O)a or NR12; a : 0-2, provided that if a = 1-2 then G must contain halo; R12H or alkyl (optionally substituted by alkyl, alkoxy, OH, CF3, NO2, CN, NH2 or halo); A : 3-6-membered carbocyclic or heterocyclic residue (optionally substituted by one or more of halo, alkyl, alkoxy, OH, CF3, NO2, CN or NH2); X1-X8H or halo; or alkyl, CH2, alkenyl or alkynyl (all optionally substituted by T or CF3); Y : heterocycle, mono-, di- or tri-haloalkyl, alkyl, cycloalkyl, alkenyl or alkynyl (all optionally substituted by one or more of halo, OH, CF3, NO2, CN, NH2, alkyl, alkenyl, alkynyl and alkoxy); or NR9R10; R9, R10H, alkyl, cycloalkyl, alkenyl, alkynyl, NO2, NH2, aryl or alkaryl; unless specified otherwise alkyl moieties have 1-10C, alkenyl or alkynyl moieties 2-10C and cycloalkyl moieties 3-10C; provided that at least one of G and Y contains a halogen; and that if G = (iii) then Y must contain halogen. ACTIVITY : Hypertensive; antiinflammatory; immunomodulatory; antidiabetic; cardiovascular; gastrointestinal; dermatological; bronchodilatory; anticancer; analgesic. MECHANISM OF ACTION : Inducible nitric oxide synthase (iNOS) inhibitor.
摘要翻译：卤代脒基氨基酸衍生物（I）是新的。式（I）的氨基酸衍生物及其盐是新的。 R1H，烷基，烯基或炔基; R2as R1或R-或S-α-氨基酸; R3，R4as R1或NO2; R1-R4任选被T取代; 低级烷基，低级烯基，低级炔基，环烷基，杂环基，芳基，杂芳基，OH，低级烷氧基，芳氧基，SH，低级硫代烷氧基，卤素，CN，NO2，NH2，COOH，羧基烷基，羧基芳基，脒基或胍基; R11OH或R-或S-α-氨基酸; G：（i）1-10C亚烷基，2-10C亚烯基或2-10C亚炔基（全部任选被一个或多个卤素，OH，CF 3，NO 2，CN，NH 2，= CH 2，烷基，烯基，炔基或烷氧基取代（全部由T或CF 3取代））; （ⅱ）（CH2）p（CX1X2）r（CH2）sQ（CH2）t（CX3X4）u（CH2）v; 或（iii）（CH 2）q（CX 5 X 6）y（CH 2）z A（CH 2）k（CX 7 X 8）j（CH 2）h; p，r，s，t，u，v，w，y，z，k，j，h：0-3; Q：Q = O，CO，S（O）a或NR12; a：0-2，条件是如果a = 1-2，那么G必须包含光环; R12H或烷基（任选被烷基，烷氧基，OH，CF 3，NO 2，CN，NH 2或卤素取代）; A：3-6元碳环或杂环残基（任选被卤素，烷基，烷氧基，OH，CF 3，NO 2，CN或NH 2中的一个或多个取代）; X1-X8H或卤素; 或烷基，CH 2，烯基或炔基（全部被T或CF 3取代）; Y：杂环，单 - ，二 - 或三 - 卤代烷基，烷基，环烷基，烯基或炔基（全部被卤素，OH，CF 3，NO 2，CN，NH 2，烷基，烯基，炔基和烷氧基中的一个或多个取代） ; 或NR9R10; R9，R10H，烷基，环烷基，烯基，炔基，NO2，NH2，芳基或烷芳基; 除非另有说明，烷基部分具有1-10C，链烯基或炔基部分2-10C和环烷基部分3-10C; G和Y中的至少一个含有卤素; 并且如果G =（iii）则Y必须含有卤素。活动：高血压; 抗炎; 免疫调节; 降糖; 心血管疾病; 胃肠道; 皮肤; 支气管扩张; 抗癌; 镇痛药。作用机制：诱导型一氧化氮合酶（iNOS）抑制剂。

3. 发明公开

EP0724570A1 AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 失效
标题翻译：脒衍生物作为NO合成酶抑制剂
公开(公告)号：EP0724570A1
公开(公告)日：1996-08-07
申请号：EP94931893.0
申请日：1994-10-20
申请人： G.D. SEARLE & CO.
发明人： HANSEN, Donald, W., Jr. , CURRIE, Mark, G. , HALLINAN, E., Ann , FOK, Kam, F. , HAGEN, Timothy, J. , BERGMANIS, Arija, A. , KRAMER, Steven, W. , LEE, Len, F. , METZ, Suzanne , MOORE, William, M. , PETERSON, Karen, B. , PITZELE, Barnett, S. , SPANGLER, Dale, P. , WEBBER, R., Keith , TOTH, Mihaly, V. , TRIVEDI, Mahima , TJOENG, Foe, S.
IPC分类号： C07D207 , A61K31 , A61P3 , A61P9 , A61P29 , A61P31 , A61P35 , A61P37 , A61P43 , C07C251 , C07D209 , C07D211 , C07D213 , C07D215 , C07D217 , C07D221 , C07D223 , C07D225 , C07D233 , C07D239 , C07D263 , C07D265 , C07D277 , C07D279 , C07D405 , C07D471 , C07D498 , C07D513
CPC分类号： C07D213/06 , A61K31/395 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/505 , A61K31/535 , A61K31/54 , A61K31/55 , C07D207/22 , C07D209/44 , C07D211/72 , C07D211/74 , C07D215/38 , C07D217/22 , C07D221/22 , C07D221/24 , C07D223/12 , C07D225/02 , C07D233/46 , C07D239/12 , C07D239/14 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D405/06
摘要： The current invention discloses useful pharmaceutical compositions containing amidino derivatives of formula (I) as nitric oxide synthase inhibitors.

4. 发明公开

EP1062201A2 HALOGENATED AMIDINO AMINO ACID DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 有权
标题翻译：卤化氨基衍生物硝酸合酶抑制剂的
公开(公告)号：EP1062201A2
公开(公告)日：2000-12-27
申请号：EP99908324.9
申请日：1999-03-04
申请人： G.D. SEARLE & CO.
发明人： HALLINAN, E., Ann , PITZEL, Barnett, S. , SPANGLER, Dale, P. , BERGMANIS, Arija, A. , HAGEN, Timothy, J. , TSYMBALOV, Sofya , TOTH, Mihaly, V. , WEBBER, R., Keith , HANSEN, Donald, W., Jr. , AWASTHI, Alik, K.
IPC分类号： C07C257/14 , C07C323/58 , C07D333/24 , A61K31/38 , A61K31/55
CPC分类号： C07D333/24 , C07C257/14 , C07C323/58 , C07C2601/02
摘要： Halogenated amidino aminoacid derivatives (I) are new. Aminoacid derivatives of formula (I) and their salts are new. [Image] R1H, alkyl, alkenyl or alkynyl; R2as R1 or R- or S-alpha -aminoacid; R3, R4as R1 or NO2; R1-R4 are optionally substituted by T; T : lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, OH, lower alkoxy, aryloxy, SH, lower thioalkoxy, halo, CN, NO2, NH2, COOH, carboxyalkyl, carboxyaryl, amidino or guanidino; R11OH or R- or S-alpha -aminoacid; G : (i) 1-10C alkylene, 2-10C alkenylene or 2-10C alkynylene (all optionally substituted by one or more of halo, OH, CF3, NO2, CN, NH2, =CH2, alkyl, alkenyl, alkynyl or alkoxy (all optionally substituted by T or CF3)); (ii) (CH2)p(CX1X2)r(CH2)sQ(CH2)t(CX3X4)u(CH2)v; or (iii) (CH2)q(CX5X6)y(CH2)zA(CH2)k(CX7X8)j(CH2)h; p, r, s, t, u, v, w, y, z, k, j, h : 0-3; Q : Q = O, CO, S(O)a or NR12; a : 0-2, provided that if a = 1-2 then G must contain halo; R12H or alkyl (optionally substituted by alkyl, alkoxy, OH, CF3, NO2, CN, NH2 or halo); A : 3-6-membered carbocyclic or heterocyclic residue (optionally substituted by one or more of halo, alkyl, alkoxy, OH, CF3, NO2, CN or NH2); X1-X8H or halo; or alkyl, CH2, alkenyl or alkynyl (all optionally substituted by T or CF3); Y : heterocycle, mono-, di- or tri-haloalkyl, alkyl, cycloalkyl, alkenyl or alkynyl (all optionally substituted by one or more of halo, OH, CF3, NO2, CN, NH2, alkyl, alkenyl, alkynyl and alkoxy); or NR9R10; R9, R10H, alkyl, cycloalkyl, alkenyl, alkynyl, NO2, NH2, aryl or alkaryl; unless specified otherwise alkyl moieties have 1-10C, alkenyl or alkynyl moieties 2-10C and cycloalkyl moieties 3-10C; provided that at least one of G and Y contains a halogen; and that if G = (iii) then Y must contain halogen. ACTIVITY : Hypertensive; antiinflammatory; immunomodulatory; antidiabetic; cardiovascular; gastrointestinal; dermatological; bronchodilatory; anticancer; analgesic. MECHANISM OF ACTION : Inducible nitric oxide synthase (iNOS) inhibitor.

5. 发明公开

EP0821674A1 CYCLIC AMIDINO AGENTS USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 失效
标题翻译： ZYCLISCHE脒MEDIUM硝酸合酶抑制剂
公开(公告)号：EP0821674A1
公开(公告)日：1998-02-04
申请号：EP96910833.0
申请日：1996-04-19
申请人： G.D. SEARLE & CO.
发明人： HANSEN, Donald, W., Jr. , HALLINAN, E., Ann , HAGEN, Timothy, J. , KRAMER, Steven, W. , METZ, Suzanne , PETERSON, Karen, B. , SPANGLER, Dale, P. , TOTH, Mihaly, V. , FOK, Kam, F. , BERGMANIS, Arija, A. , WEBBER, R., Keith , TRIVEDI, Mahima , TJOENG, Foe, S. , PITZELE, Barnett, S.
IPC分类号： C07D319 , A61K31 , A61P9 , A61P25 , A61P29 , A61P43 , C07C251 , C07D207 , C07D211 , C07D223 , C07D225 , C07D309 , C07D333 , C07D401 , C07D403 , C07D405 , C07D409 , C07D413 , C07D417 , C07D521
CPC分类号： C07D249/08 , C07D207/22 , C07D211/72 , C07D223/12 , C07D225/02 , C07D231/12 , C07D233/56 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The current invention discloses amidino derivatives of formula (I) useful as nitric oxide synthase inhibitors wherein R1 is selected from the group consisting of cycloalkyl, heterocyclyl and aryl, which may optionally be substituted; L is selected from the group consisting of lower alkynylene, and (CH2)m-D-(CH2)n-; D is selected from the group consisting of O, S, SO, SO2, SO2NR7, NR7SO2, NR8, POOR7, PON(R7)2, POOR7NR7, NR7POOR7, C(O), C(O)O; B is selected from the group consisting of (CH2)v, CH=CH; A is selected from the group consisting of O, NR7, (CH2)q, CH=CH; X is selected from the group consisting of NH, O, S, (CH2)p and CH=CH.

6. 发明授权

EP0821674B1 CYCLIC AMIDINO AGENTS USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 失效
标题翻译： ZYCLISCHE脒MEDIUM硝酸合酶抑制剂
公开(公告)号：EP0821674B1
公开(公告)日：2003-08-06
申请号：EP96910833.1
申请日：1996-04-19
申请人： G.D. SEARLE & CO.
发明人： HANSEN, Donald, W., Jr. , HALLINAN, E., Ann , HAGEN, Timothy, J. , KRAMER, Steven, W. , METZ, Suzanne , PETERSON, Karen, B. , SPANGLER, Dale, P. , TOTH, Mihaly, V. , FOK, Kam, F. , BERGMANIS, Arija, A. , WEBBER, R., Keith , TRIVEDI, Mahima , TJOENG, Foe, S. , PITZELE, Barnett, S.
IPC分类号： C07D223/12 , A61K31/55 , C07D405/06 , C07D409/06 , C07D207/14 , C07D225/02 , C07D211/72 , C07D413/06 , C07D403/06 , C07D401/12
CPC分类号： C07D249/08 , C07D207/22 , C07D211/72 , C07D223/12 , C07D225/02 , C07D231/12 , C07D233/56 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D417/06
摘要： The current invention discloses amidino derivatives of formula (I) useful as nitric oxide synthase inhibitors wherein R1 is selected from the group consisting of cycloalkyl, heterocyclyl and aryl, which may optionally be substituted; L is selected from the group consisting of lower alkynylene, and (CH2)m-D-(CH2)n-; D is selected from the group consisting of O, S, SO, SO2, SO2NR7, NR7SO2, NR8, POOR7, PON(R7)2, POOR7NR7, NR7POOR7, C(O), C(O)O; B is selected from the group consisting of (CH2)v, CH=CH; A is selected from the group consisting of O, NR7, (CH2)q, CH=CH; X is selected from the group consisting of NH, O, S, (CH2)p and CH=CH.

7. 发明公开

EP1000041A1 1,3-DIAZA- HETEROCYCLES AND THEIR USE AS NITRIC OXIDE SYNTHASE INHIBITORS 失效
标题翻译： 1.3二氮杂 - 杂环及其使用硝酸合成酶抑制剂
公开(公告)号：EP1000041A1
公开(公告)日：2000-05-17
申请号：EP98935498.0
申请日：1998-07-08
申请人： G.D. SEARLE & CO.
发明人： HANSEN, Donald, W., Jr. , BERGMANIS, Arija, A. , HAGEN, Timothy, J. , HALLINAN, E., Ann , KRAMER, Steven, W. , METZ, Suzanne , PETERSON, Karen, B. , PITZELE, Barnett, S. , TJOENG, Foe, S. , TOTH, Mihaly , TRIVEDI, Mahima , WEBBER, R., Keith , TSYMBALOV, Sofya , GAPUD, Rolando, E.
IPC分类号： C07D271/07 , C07D285/125 , C07D291/04 , C07D233/96 , C07D273/04 , A61K31/41 , A61K31/535
CPC分类号： C07D291/04 , C07D233/96 , C07D271/07 , C07D273/04 , C07D285/08
摘要： Compounds of formula (I) are useful as nitric oxide synthase inhibitors.

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