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1. 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。

2. 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。

3. 发明申请

WO1997032844A1 HYDROXYAMIDINO DERIVATIVES USEFUL AS NITRIC OXIDE SYNTHASE INHIBITORS 审中-公开
标题翻译：用作氧化氮合酶抑制剂的羟基氨基衍生物
公开(公告)号：WO1997032844A1
公开(公告)日：1997-09-12
申请号：PCT/US1997003282
申请日：1997-03-05
申请人： G.D. SEARLE & CO. , GAPUD, Rolando, E. , HAGEN, Timothy, J. , HALLINAN, E., Ann , HANSEN, Donald, W., Jr. , MANNING, Robert, E. , METZ, Suzanne, S. , PITZELE, Barnett, S. , TJOENG, Foe, S. , TOTH, Mihaly, V. , WEBBER, Keith, R.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C259/14
CPC分类号： C07D261/08 , C07C257/14 , C07C259/14 , C07C275/16 , C07C313/28 , C07C323/60 , C07C327/22 , C07C329/02 , C07C329/06 , C07C333/04 , C07C391/00 , C07D223/12 , C07F7/081
摘要： The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.
摘要翻译：本发明公开了可用作一氧化氮合酶抑制剂的羟基脒基衍生物。

4. 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。

5. 发明申请

WO1997003947A1 PROCESS FOR THE PREPARATION OF ETHYL 3S-[[4-[[4-(AMINOIMINOMETHYL)PHENYL]AMINO]-1,4-DIOXOBUTYL]AMINO]-4-PENTYNOATE 审中-公开
标题翻译：乙基3S- [[4 - [[4-（氨基亚氨基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸的制备方法
公开(公告)号：WO1997003947A1
公开(公告)日：1997-02-06
申请号：PCT/US1996010658
申请日：1996-07-12
申请人： G.D. SEARLE & CO. , BABIAK, Kevin, A. , BABU, Srinivasan , BEHLING, James, R. , BOYS, Mark, L. , CAIN-JANICKI, Kimberly, J. , DOUBLEDAY, Wendell, W. , FARID, Payman , HAGEN, Timothy, J. , HALLINAN, E., Ann , HANSEN, Donald, W., Jr. , KORTE, Donald, E. , MC LAUGHLIN, Kathleen, T. , MEDICH, John, R. , NUGENT, Sean, T. , ORLOVSKI, Vlasdislav , PARK, Jung, M. , PETERSON, Karen, B. , PILIPAUSKAS, Daniel, R. , PITZELE, Barnett, S. , TSYMBALOV, Sofya , STAHL, Glenn, L.
发明人： G.D. SEARLE & CO.
IPC分类号： C07C249/12
CPC分类号： C07C227/12 , C07C227/34 , C07C257/18
摘要： The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)-phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate and pharmaceutically acceptable acid addition salt thereof which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllitium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (+/-)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (+/-)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (+/-)1,1-dimethylethyl 3-amin-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (+/-)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; desilylation of (+/-)ethyl 3-amino-5-(trimethylsilyl)-4-pentynoate to give in situ (+/-)ethyl 3-amino-4-pentynoate; resolution of (+/-)ethyl 3-amino-4-pentynoate using (R)-(-)-mandelic acid and treatment of the resolved product with gaseous hydrochloric acid to give ethyl 3S-amino-4-pentynoate, monohydrochloride; coupling the ethyl 3S-amino-4-pentynoate, monohydrochloride to 4-[[4-(aminoiminomethyl)phenyl]amino]-4-oxobutanoic acid, monohydrochloride in the presence of isobutyl chloroformate and N-methylmorpholine to give ethyl 3S-[[4-[[4-(aminoiminomehtyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentynoate, monohydrochloride.
摘要翻译：本发明涉及制备3S - [[4 - [[4-（氨基亚氨基甲基） - 苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯和药学上可接受的酸加成盐的新方法其包括依次用正丁基鎓和4-甲酰基吗啉处理（三甲基甲硅烷基）乙炔，然后酸水解，得到3-（三甲基甲硅烷基）-2-丙炔醛; 用双（三甲基甲硅烷基）氨基锂处理3-（三甲基甲硅烷基）-2-丙炔醛，得到原位N，3-二（三甲基甲硅烷基）-2-丙炔-1-亚胺; N，3-二（三甲基甲硅烷基）-2-丙炔-1-亚胺与乙酸叔丁酯的缩合得到3-氨基-5-（三甲基甲硅烷基）-4-戊炔酸（+/-）1,1-二甲基乙酯; 用对甲苯磺酸处理（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯（+/-）1,1-二甲基乙基酯，得到3-氨基-5-（三甲基甲硅烷基）-4-戊酸酯，单对甲苯磺酸盐，在对甲苯磺酸存在下用乙醇处理所得的盐，得到（+/-）3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯; （+/-）乙基3-氨基-5-（三甲基甲硅烷基）-4-戊酸乙酯脱甲硅烷基，得到原位（+/-）3-氨基-4-戊酸乙酯; 使用（R） - （ - ） - 扁桃酸分解（+/-）乙基3-氨基-4-戊炔酸，并用气态盐酸处理分离产物，得到3S-氨基-4-戊酸乙酯，一盐酸盐; 将3S-氨基-4-戊酸乙酯，一盐酸盐在氯甲酸异丁酯和N-甲基吗啉存在下，将4 - [[4-（氨基亚氨基甲基）苯基]氨基] -4-氧代丁酸单盐酸盐偶合，得到3S- [ 4 - [[4-（氨基亚氨基甲基）苯基]氨基] -1,4-二氧代丁基]氨基] -4-戊酸乙酯，一盐酸盐。

6. 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。

7. 发明申请

WO1994020457A1 N-ACYL BETA AMINO ACID DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译： N-乙酰氨基甲酸衍生物作为片剂聚集抑制剂有用
公开(公告)号：WO1994020457A1
公开(公告)日：1994-09-15
申请号：PCT/US1994001594
申请日：1994-02-22
申请人： G.D. SEARLE & CO. , MONSANTO COMPANY , TJOENG, Foe, S. , TOTH, Mihaly, V.
发明人： G.D. SEARLE & CO. , MONSANTO COMPANY
IPC分类号： C07C257/18
CPC分类号： C07D401/12 , C07C257/18 , C07D213/55
摘要： Novel N-acyl beta amino acid derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
摘要翻译：提供抑制血小板聚集的新型N-酰基β氨基酸衍生物。本发明还涉及使用这些衍生物的药物组合物和方法。

8. 发明申请

WO1994019341A1 UREA DERIVATIVES USEFUL AS PLATELET AGGREGATION INHIBITORS 审中-公开
标题翻译：尿素衍生物作为抗肿瘤抑制剂有用
公开(公告)号：WO1994019341A1
公开(公告)日：1994-09-01
申请号：PCT/US1994000513
申请日：1994-01-25
申请人： G.D. SEARLE & CO. , THE MONSANTO COMPANY , TJOENG, Foe, S. , TOTH, Mihaly, V.
发明人： G.D. SEARLE & CO. , THE MONSANTO COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Novel urea derivatives of formula (I) are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives. In formula (I) R, Z, Z', W, n, n' and m are as defined in the application.
摘要翻译：提供抑制血小板聚集的式（I）的新型尿素衍生物。本发明还涉及使用这些衍生物的药物组合物和方法。在式（I）中，R，Z，Z'，W，n，n'和m如申请中所定义。

9. 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。

10. 发明申请

WO1996015120A1 AMINOTETRAZOLE 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氨基三唑衍生物
公开(公告)号：WO1996015120A1
公开(公告)日：1996-05-23
申请号：PCT/US1995014001
申请日：1995-11-08
申请人： G.D. SEARLE & CO. , HALLINAN, E., Ann , HANSEN, Donald, W., Jr. , TSYMBALOV, Sofya
发明人： G.D. SEARLE & CO.
IPC分类号： C07D257/06
CPC分类号： C07D239/42 , C07D231/40 , C07D233/88 , C07D249/14 , C07D257/06 , C07D277/18 , C07D277/46
摘要： Compounds having formula (I) and pharmaceutically acceptable salts thereof, wherein B is NR R , wherein R is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, lower alkynyl and aryl, and R is selected from a 3 to 8 member heterocyclyl radical in which at least one member of the ring is carbon and in which 1 to about 4 members are heteroatoms independently selected from oxygen, nitrogen and sulfur and said heterocyclyl radical may be optionally substituted, useful as nitric oxide synthase inhibitors.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，其中B为NR 5 R 11，其中R 5选自氢，低级烷基，低级烯基，低级炔基和芳基，和 R 11选自3至8个杂环基，其中至少一个环的成员是碳，并且其中1至约4个成员是独立地选自氧，氮和硫的杂原子，并且所述杂环基可以是任选的取代，可用作一氧化氮合酶抑制剂。

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