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1. 发明授权

US5665738A Imidazole derivatives and processes for the preparation thereof 失效
标题翻译：咪唑衍生物及其制备方法
公开(公告)号：US5665738A
公开(公告)日：1997-09-09
申请号：US737563
申请日：1996-11-13
申请人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo , Hye-Suk Lee
发明人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo , Hye-Suk Lee
IPC分类号： A61K31/44 , A61K31/4427 , A61P9/12 , A61P43/00 , C07D401/14 , A61K31/415 , C07D403/14
CPC分类号： C07D401/14
摘要： Novel imidazole derivatives of formula(I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity: ##STR1## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl group, or OR.sub.1 wherein R.sub.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical; B is a halogen, CF.sub.3 or CF.sub.2 CF.sub.3 ; X is N or N-oxide; Y is --CH.sub.2 --, --CH(OR.sub.1)-- wherein R.sub.1 is the same as defined above, or --C(.dbd.O)--; n is 0 or an integer of 1 to 4; Z is a halogen, --OH, --OR.sub.1, --NR.sub.1 R.sub.2, --N(.dbd.O)R.sub.3 R.sub.4, --C(.dbd.O)R.sub.1, --C(.dbd.O)OR.sub.1, --CH(OR.sub.1).sub.2 or --C(.dbd.O)N.sub.1 N.sub.2 wherein R.sub.1 is the same as defined above, R.sub.2 is, independently of R.sub.1, a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical, and R.sub.3 and R.sub.4 are independently a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical; and D is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical.
摘要翻译： PCT No.PCT / KR95 / 00058 Sec。 371日期：1996年11月13日 102（e）1996年11月13日PCT PCT 1995年5月19日PCT公布。公开号WO95 / 32198 日期：1995年11月30日公式（I）的新型咪唑衍生物有效抑制血管紧张素II的作用并具有优异的抗高血压活性：其中：A是直链，支链或环状的C 1 -C 6烷基，或 OR1，其中R1是氢或直链，支链或环状的C1-C6烷基; B是卤素，CF 3或CF 2 CF 3; X是N或N-氧化物; Y是-CH 2 - ， - CH（OR 1） - ，其中R 1与上述定义相同，或-C（= O） - ; n为0或1〜4的整数， Z是卤素，-OH，-OR1，-NR1R2，-N（= O）R3R4，-C（= O）R1，-C（= O）OR1，-CH（OR1）2或-C ）N1N2其中R1与上述定义相同，R2独立地为R1，氢或直链，支链或环状的C1-C6烷基，R3和R4独立地为直链，支链或环状的C 1 -C 6烷基激进; 并且D是氢或直链，支链或环状的C 1 -C 6烷基。

2. 发明授权

US5849753A Pyridyl imidazole derivatives and processes for the preparation thereof 失效
标题翻译：吡啶基咪唑衍生物及其制备方法
公开(公告)号：US5849753A
公开(公告)日：1998-12-15
申请号：US682684
申请日：1996-07-25
申请人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo
发明人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo
IPC分类号： A61K31/415 , A61K31/435 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/505 , A61P9/12 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Substituted pyridyl imidazole derivatives of formula (I) inhibit effectively the action of angiotensin II and have a superior anti-hypertensive activity. ##STR1##
摘要翻译： PCT No.PCT / KR95 / 00009 Sec。 371日期：1996年7月25日 102（e）日期1996年7月25日PCT提交1995年2月8日PCT公布。公开号WO95 / 21838 日期1995年8月17日式（I）的取代吡啶基咪唑衍生物有效抑制血管紧张素II的作用并具有优异的抗高血压活性。（一）

3. 发明授权

US5691348A Pyridyl imidazole derivatives and processes for the preparation thereof 失效
标题翻译：吡啶基咪唑衍生物及其制备方法
公开(公告)号：US5691348A
公开(公告)日：1997-11-25
申请号：US750460
申请日：1996-12-08
申请人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo , Hye-Suk Lee
发明人： Sung-Eun Yoo , Kyu-Yang Yi , Sang-Hee Lee , Hye-Ryung Kim , Jee-Hee Suh , Nak-Jeong Kim , Seon-Ju Kim , Ok-Ja Cha , Young-Ah Shin , Wha-Sup Shin , Sung-Hou Lee , Yi-Sook Jung , Byung-Ho Lee , Ho-Won Seo , Hye-Suk Lee
IPC分类号： A61K31/435 , A61K31/44 , A61P9/12 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： Novel pyridyl imidazole derivatives of formula(I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity: ##STR1## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl group, OR.sup.1 (wherein R.sup.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl radical), or NR.sup.2 R.sup.3 (wherein R.sup.2 and R.sup.3 are independently a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical); B is a group of the following formula ##STR2## D is a hydrogen; a halogen; a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; tetrazol-5-yl; a perfluoro-C.sub.1 -C.sub.4 alkyl group; or N(R.sup.1).sub.2, OR.sup.1, CO.sub.2 R.sup.1 or CON(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; E is a hydrogen; a halogen; a straight or branched C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; a perfluoro-C.sub.1 -C.sub.4 alkyl group; NO.sub.2 ; or N(R.sup.1).sub.2 or OR.sup.1, wherein R.sup.1 is the same as defined above; and n is 0 or an integer of 1 to 4.
摘要翻译： PCT No.PCT / KR95 / 00075 Sec。 371日期1996年12月6日第 102（e）日期1996年12月6日PCT归档1995年6月7日PCT公布。出版物WO95 / 34564 日期：1995年12月21日新型式（I）吡啶基咪唑衍生物有效抑制血管紧张素II的作用，具有优异的抗高血压活性：d或环状C 1 -C 6烷基或链烯基，OR 1（其中R 1为氢或直链，支链或环状的C 1 -C 6烷基或链烯基）或NR 2 R 3（其中R 2和R 3独立地是氢或直链，支链或环状的C 1 -C 6烷基）; B是一组下列公式： D是氢; 卤素任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链，支链或环状C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基其中R1与上述相同; 四唑-5-基; 全氟-C 1 -C 4烷基; 或N（R1）2，OR1，CO2R1或CON（R1）2，其中R1与上述定义相同; E是氢; 卤素任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链或支链C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，其中 R1与上述定义相同; 全氟-C 1 -C 4烷基; NO2; 或N（R1）2或OR1，其中R1与上述定义相同; n为0或1〜4的整数。

4. 发明授权

US5300511A Spiro-benzopyran derivatives and useful for treating asthma and hypertension 失效
标题翻译：螺 - 苯并吡喃衍生物，可用于治疗哮喘和高血压
公开(公告)号：US5300511A
公开(公告)日：1994-04-05
申请号：US887189
申请日：1992-05-21
申请人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
发明人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
IPC分类号： A61K31/35 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/10
CPC分类号： C07D405/04 , C07D405/14
摘要： The present invention relates to novel benzopyran derivatives of formula(I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.1-4 straight or branched alkyl group, ##STR3## wherein R.sup.G and R.sup.H are, each independently, a C.sub.1-6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group, A and B are, each independently, S or O; and Z is a C.sub.1-3 straight or branched alkyl group;X is N or N.fwdarw.O.
摘要翻译：本发明涉及式（I）的新型苯并吡喃衍生物，其在治疗哮喘以及高血压方面具有显着的效果。（*化学结构*）（I）其中R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，（*化学结构*）-SO 2RC或-SO 2 NRCRD，其中X1，X2和X3各自独立地为F ，Cl或H，除了X1，X2和X3可能不是氢原子同时; RA和RB各自独立地为氢原子或具有卤素原子的C 1-6烷基或任选取代的苯基，或直链或支链C 1-3烷基; 和RC和RD各自独立地为氢原子或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是C1-4直链或支链烷基; R3是C1-4直链或支链烷基，（*化学结构*）其中RG和RH各自独立地为C1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C1- 3个烷基，A和B各自独立地为S或O; Z为直链或支链的C1-3烷基; X是N或N-> O。

5. 发明授权

US5493029A Certain pyridyl-benzopyran derivatives 失效
标题翻译：某些吡啶基 - 苯并吡喃衍生物
公开(公告)号：US5493029A
公开(公告)日：1996-02-20
申请号：US164392
申请日：1993-12-09
申请人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
发明人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
IPC分类号： A61K31/35 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04
CPC分类号： C07D405/04 , C07D405/14
摘要： The present invention relates to novel benzopyran derivatives of formula (I) which have exellent effectiveness in the treatment of asthma as well as hypertension. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, F, Cl or H, except for that X.sub.1, X.sub.2 and X.sub.3 may not be hydrogen atom simulaneously; R.sup.A and R.sup.B are, each independently, a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group; and R.sup.C and R.sup.D are, each independently, a hydrogen atom or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is a C.sub.1-4 straight or branched alkyl group;R.sub.3 is a C.sub.1-4 straight or branched alkyl group, ##STR3## wherein R.sup.G and R.sup.H are, each independently, a C.sub.1-6 alkyl group or optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group, A and B are, each independently, S or O;X is N or N.fwdarw.O;Y is a hydrogen or halogen atom, or an amino, hydroxy, a lower alkoxy or lower alkyl group.
摘要翻译：本发明涉及式（I）的新型苯并吡喃衍生物，其在治疗哮喘以及高血压方面具有显着的效果。（I）其中：R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，-SO2RC或-SO2NRCRD，其中X1，X2和X3各自独立地是F，Cl或H，除了X1，X2和X3可能不是同时是氢原子; RA和RB各自独立地为氢原子或具有卤素原子的C 1-6烷基或任选取代的苯基，或直链或支链C 1-3烷基; 和RC和RD各自独立地为氢原子或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是C1-4直链或支链烷基; R3是C1-4直链或支链烷基，其中RG和RH各自独立地是C1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基 A和B各自独立地为S或O; X是N或N-> O; Y是氢或卤素原子，或氨基，羟基，低级烷氧基或低级烷基。

6. 发明授权

US5236935A Benzopyran derivatives and processes for the preparation thereof 失效
标题翻译：苯并吡喃衍生物及其制备方法
公开(公告)号：US5236935A
公开(公告)日：1993-08-17
申请号：US886986
申请日：1992-05-21
申请人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
发明人： Sung-Eun Yoo , Kyu Y. Yi , Nak C. Jeong , Jee H. Suh , Seon-Ju Kim , Hwa-Sup Shin , Byung H. Lee , Kyu S. Jung
IPC分类号： C07D405/04
CPC分类号： C07D405/04
摘要： The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.E is a hydrogen atom, or a C.sub.1-6 alkyl, cyclopropyl, cyclopropylmethyl or benzyl group; R.sup.F is --COR.sup.A or --CSR.sup.A ; X is O, S or NR.sup.C, and n is an integer from 0 to 3, wherein R.sup.A and R.sup.C have the same meanings as defined above;R.sub.3 is a C.sub.1-4 straight or branched alkyl group; andR.sub.4 is ##STR4## wherein R.sup.G and R.sup.H are, each independently, a C.sub.-16 alkyl group or an optionally substituted phenyl group; A and B are, each independently, S or O; and Z is a C.sub.1-3 straight or branched alkyl group.
摘要翻译：本发明涉及新型的式（I）的苯并吡喃衍生物，其通过降低血压以及对血管平滑肌的松弛活性而在治疗高血压方面具有优异的选择性。本发明还涉及制备这些化合物的方法; 以及含有这些化合物作为活性成分的药物组合物。（I）其中：R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，-SO2RC或-SO2NRCRD，其中X1，X2和X3各自独立地是氟，氯或氢原子; RA和RB各自独立地为氨基，C 1-6烷氧基，C 1-6烷基或任选取代的苯基; 和RC和RD是氢原子，或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是其中RE是氢原子或C1-6烷基，环丙基，环丙基甲基或苄基; RF是-CORA或-CSRA; X是O，S或NRC，n是0-3的整数，其中RA和RC具有与上述相同的含义; R3是C1-4直链或支链烷基; 并且R 4是，其中RG和RH各自独立地是C 16-16烷基或任选取代的苯基; A和B各自独立地为S或O; Z为直链或支链的C1-3烷基。

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