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1. 发明申请

WO1995025717A1 AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：氨氮衍生物作为氮氧化物合成酶抑制剂有用
公开(公告)号：WO1995025717A1
公开(公告)日：1995-09-28
申请号：PCT/US1995003589
申请日：1995-03-24
申请人： G.D. SEARLE & CO. , CURRIE, Mark, G. , WEBBER, Keith , TJOENG, Foe, S. , FOK, Kam, F.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C257/14
CPC分类号： C07C257/14 , C07C391/00
摘要： There is disclosed amidino derivatives of formula (I), pharmaceutical compositions containing these derivatives, and their use in therapy, in particular their use as nitric oxide synthase inhibitors wherein: X is alkyl, alkenyl, alkynyl, -(CH2)kQ(CH2)l- where k is 2 or 3, l is 1 or 2 and Q is 0, Se SiY2 where Y is alkyl, S(O)z where z is 0, 1 or 2, NR where R is hydrogen or alkyl, or -(CH2)mA(CH2)n- where m is 0, 1 or 2, n is 0, 1 or 2, A is 3 to 6 membered aromatic hydrocarbon radical or 3 to 6 membered heterocyclic radical wherein 1 to 3 hetero atoms are oxygen, sulfur or nitrogen and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; R1 may be a bond to X or hydrogen (when Q is Se), hydroxyalkyl, alkyl, alkenyl, alkynyl or haloalkyl and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; R2 is alkyl, alkenyl, alkynyl, aromatic hydrocarbon radical, haloalkyl, hydroxylamine or heterocyclic radical wherein 1 to 3 hetero atoms are oxygen, sulfur or nitrogen and wherein all said radicals may optionally be substituted by one or more substituents such as alkyl, alkoxy, hydroxy, halogen, nitro, cyano, trifluoroalkyl and amino; and R3 is amino, alkylamine, amino acid, hydroxy, alkoxy, tetrazole or tetrazoloamine.
摘要翻译：公开了式（I）的脒基衍生物，含有这些衍生物的药物组合物及其在治疗中的用途，特别是其用作一氧化氮合酶抑制剂，其中：X为烷基，烯基，炔基， - （CH2）kQ（CH2）其中k是2或3，l是1或2，Q是0，Se SiY2其中Y是烷基，S（O）z，其中z是0,1或2，NR，其中R是氢或烷基，或 - （CH2）mA（CH2）n-，其中m为0,1或2，n为0,1或2，A为3至6元芳族烃基或3至6元杂环基，其中1至3个杂原子为氧，硫或氮，并且其中所有所述基团可任选被一个或多个取代基如烷基，烷氧基，羟基，卤素，硝基，氰基，三氟烷基和氨基取代; R 1可以是与X或氢的键（当Q是Se时），羟基烷基，烷基，烯基，炔基或卤代烷基，并且其中所有所述基团可任选地被一个或多个取代基例如烷基，烷氧基，羟基，卤素，硝基，氰基，三氟烷基和氨基; R 2是烷基，烯基，炔基，芳族烃基，卤代烷基，羟胺或杂环基，其中1至3个杂原子是氧，硫或氮，并且其中所有所述基团可以任选地被一个或多个取代基取代，例如烷基，烷氧基，羟基，卤素，硝基，氰基，三氟烷基和氨基; 和R3是氨基，烷基胺，氨基酸，羟基，烷氧基，四唑或四唑胺。

2. 发明申请

WO1996033175A1 CYCLIC AMIDINO AGENTS USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：循环氨基酸代谢物作为氮氧化物合成酶抑制剂有用
公开(公告)号：WO1996033175A1
公开(公告)日：1996-10-24
申请号：PCT/US1996005315
申请日：1996-04-19
申请人： G.D. SEARLE & CO. , 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.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D223/12
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.
摘要翻译：本发明公开了用作一氧化氮合酶抑制剂的式（I）的脒基衍生物，其中R 1选自环烷基，杂环基和芳基，其可任选被取代; L选自低级亚炔基和（CH 2）m -D-（CH 2）n - ; D选自O，S，SO，SO2，SO2NR7，NR7SO2，NR8，POOR7，PON（R7）2，POOR7NR7，NR7POOR7，C（O），C（O） B选自（CH 2）v，CH = CH; A选自O，NR 7，（CH 2）q，CH = CH; X选自NH，O，S，（CH 2）p和CH = CH。

3. 发明申请

WO1996035677A1 NITRIC OXIDE SYNTHASE INHIBITORS DERIVED FROM CYCLIC AMIDINES 审中-公开
标题翻译：从循环载体衍生的氮氧化物合成酶抑制剂
公开(公告)号：WO1996035677A1
公开(公告)日：1996-11-14
申请号：PCT/US1996006831
申请日：1996-05-09
申请人： G.D. SEARLE & CO. , HANSEN, Donald, W., Jr. , HAGEN, Timothy, J. , KRAMER, Steven, W. , METZ, Suzanne , PETERSON, Karen, B. , SPANGLER, Dale, P. , TOTH, Mihaly, V. , FOK, Kam, F. , WEBBER, R., Keith , TJOENG, Foe, S. , PITZELE, Barnett, S. , HALLINAN, E., Ann
发明人： G.D. SEARLE & CO.
IPC分类号： C07D223/12
CPC分类号： C07D403/06 , C07D207/22 , C07D207/24 , C07D211/72 , C07D211/74 , C07D223/12 , C07D243/08 , C07D267/10 , C07D413/06 , C07D413/12 , C07D471/10
摘要： Compounds having formula (I) wherein R , R , R and R are hydrogen or certain specified substituents; R and R are independently hydrogen, hydroxy or alkoxy; and X, A and B are independently NR , O, S, SO, SO2, CH=CH or (CH2)p, p being 0-6; are useful as nitric oxide synthase inhibitors.
摘要翻译：具有式（I）的化合物，其中R 1，R 5，R 6和R 7是氢或某些特定的取代基; R 8和R 9独立地是氢，羟基或烷氧基; 并且X，A和B独立地为NR 2，O，S，SO，SO 2，CH = CH或（CH 2）p，p为0-6; 可用作一氧化氮合酶抑制剂。

4. 发明申请

WO1995011014A1 AMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：氨氮衍生物作为氮氧化物合成酶抑制剂有用
公开(公告)号：WO1995011014A1
公开(公告)日：1995-04-27
申请号：PCT/US1994011724
申请日：1994-10-18
申请人： G.D. SEARLE & CO. , TJOENG, Foe, S. , FOK, Kam, F. , WEBBER, R., Keith
发明人： G.D. SEARLE & CO.
IPC分类号： A61K31/00
CPC分类号： A61K31/38 , A61K31/155 , A61K31/34 , A61K31/42 , A61K31/44
摘要： The current invention discloses amidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了用作一氧化氮合酶抑制剂的脒衍生物。

5. 发明申请

WO1995024382A1 L-N6-(1-IMINOETHYL)LYSINE DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：用作氮氧化物合成酶抑制剂的L-N 6 - （1-甲基乙基）赖氨酸衍生物
公开(公告)号：WO1995024382A1
公开(公告)日：1995-09-14
申请号：PCT/US1995002669
申请日：1995-03-08
申请人： G.D. SEARLE & CO. , HALLINAN, E., Ann , TJOENG, Foe, S. , FOK, Kam, F. , HAGEN, Timothy, J. , TOTH, Mihaly, V. , TSYMBALOV, Sofya , PITZELE, Barnett, S.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C257/14
CPC分类号： C07D233/64 , A61K31/155 , C07C257/14 , C07C259/06 , C07C279/18 , C07C317/40 , C07C323/41 , C07D257/04 , C07D263/32 , C07D307/14 , C07D317/28 , C07D317/38 , C07D319/12 , C07D333/20 , C07D333/22 , Y10S514/825 , Y10S514/866 , Y10S514/921
摘要： There is disclosed a novel amino glycol derivatives of L-N -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
摘要翻译：公开了L-N 6 - （1-亚氨基乙基）赖氨酸的新型氨基二醇衍生物，含有这些新化合物的药物组合物及其在治疗中的用途，特别是其用作一氧化氮合酶抑制剂。

6. 发明申请

WO1997041144A1 NOVEL STEROID NITRITE AND NITRATE ESTER DERIVATIVES USEFUL AS ANTI-INFLAMMATORY DRUGS 审中-公开
标题翻译：新型西妥昔单抗和硝酸酯衍生物作为抗炎药物有用
公开(公告)号：WO1997041144A1
公开(公告)日：1997-11-06
申请号：PCT/US1997006373
申请日：1997-04-28
申请人： G.D. SEARLE & CO. , TJOENG, Foe, S. , CURRIE, Mark, G. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07J41/00
CPC分类号： C07J71/0031 , C07J41/005
摘要： The present invention relates to a compound having the formula A-B-C, wherein A is a hydroxyl containing steroidal hormone; C is a nitrite or nitrate containing compound; and B is lower alkyl, lower alkenyl, lower alkynyl, and to pharmaceutical compositions thereof. These compounds are anti-inflammatory and vasodilation agents.
摘要翻译：本发明涉及具有式A-B-C的化合物，其中A是含羟基的甾体激素; C是含亚硝酸盐或含硝酸盐的化合物; 和B是低级烷基，低级烯基，低级炔基，及其药物组合物。这些化合物是抗炎和血管舒张剂。

7. 发明申请

WO1997040836A1 NOVEL PHARMACEUTICAL COMPOSITIONS HAVING STEROID NITRATE ESTER DERIVATIVES USEFUL AS ANTI-INFLAMMATORY DRUGS 审中-公开
标题翻译：具有非甾体类硝酸酯衍生物的新型药物组合物作为抗炎药物有用
公开(公告)号：WO1997040836A1
公开(公告)日：1997-11-06
申请号：PCT/US1997006374
申请日：1997-04-28
申请人： G.D. SEARLE & CO. , TJOENG, Foe, S. , CURRIE, Mark, G. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO.
IPC分类号： A61K31/57
CPC分类号： A61K31/573
摘要： The present invention discloses novel pharmaceutical compositions having steroid nitrate ester(ONO2) derivatives, and to their use treating undesired smooth muscle contractions and inflammatory diseases.
摘要翻译：本发明公开了具有类固醇硝酸酯（ONO 2）衍生物的新型药物组合物及其治疗不希望的平滑肌收缩和炎性疾病的用途。

8. 发明申请

WO1997021724A1 STEROID NITRITE ESTER DERIVATIVES USEFUL AS ANTI-INFLAMMATORY DRUGS 审中-公开
标题翻译：有效用作抗炎药物的甾体硝酸酯衍生物
公开(公告)号：WO1997021724A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019220
申请日：1996-12-06
申请人： G.D. SEARLE & CO. , TJOENG, Foe, S. , CURRIE, Mark, G. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07J71/00
CPC分类号： C07J71/0031
摘要： The present invention discloses novel steroid nitrite ester derivatives, and to their use treating inflammatory diseases.
摘要翻译：本发明公开了新型类固醇亚硝酸酯衍生物及其治疗炎性疾病的用途。

9. 发明申请

WO1997021721A1 NOVEL STEROID NITRITE/NITRATE ESTER DERIVATIVES USEFUL AS ANTI-INFLAMMATORY DRUGS 审中-公开
标题翻译：新西兰硝酸盐/硝酸盐衍生物有效地作为抗炎药物
公开(公告)号：WO1997021721A1
公开(公告)日：1997-06-19
申请号：PCT/US1996019219
申请日：1996-12-06
申请人： G.D. SEARLE & CO. , TJOENG, Foe, S. , CURRIE, Mark, G. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07J41/00
CPC分类号： C07J41/005
摘要： The present invention discloses novel steroid nitrite/nitrate ester derivatives, and their use for treating inflammatory diseases.
摘要翻译：本发明公开了新型类固醇亚硝酸酯/硝酸酯衍生物及其用于治疗炎性疾病的用途。

10. 发明申请

WO1996036639A1 AMIDINE DERIVATIVES USEFUL AS ANTI-PLATELET AGGREGATION INHIBITORS AND VASODILATORS 审中-公开
标题翻译：有用的氨基衍生物作为抗肿瘤抑制剂和血管扩张剂
公开(公告)号：WO1996036639A1
公开(公告)日：1996-11-21
申请号：PCT/US1996006551
申请日：1996-05-15
申请人： G.D. SEARLE & CO. , CURRIE, Mark, G. , TJOENG, Foe, S. , ZUPEC, Mark, E.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound, having formula (I).
摘要翻译：本发明公开了具有一氧化氮赋予特性的新颖的脒衍生物，其可以抑制具有式（I）的单一化合物中的血小板聚集和促进血管舒张。

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