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1. 发明授权

US5700822A Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US5700822A
公开(公告)日：1997-12-23
申请号：US457047
申请日：1995-06-01
申请人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
发明人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。以下描述特征化合物A10（参见图1a）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

2. 发明授权

US5990141A Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US5990141A
公开(公告)日：1999-11-23
申请号：US370574
申请日：1995-01-06
申请人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
发明人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers , Fairooz F. Kabbinavar , Dennis Slamon , Peng Cho Tang
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。下面描述特征化合物A10（参见图1a）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

3. 发明授权

US5932602A Treatment of platelet derived growth factor related disorders such as cancers 失效
公开(公告)号：US5932602A
公开(公告)日：1999-08-03
申请号：US456735
申请日：1995-06-01
申请人： Klaus Peter Hirth , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Janis Haimichael , Axel Ullrich , Reiner Lammers
发明人： Klaus Peter Hirth , Laura Kay Shawver , Gyorgi Keri , Istvan Szekely , Janis Haimichael , Axel Ullrich , Reiner Lammers
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50 , A61K31/175
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.

4. 发明授权

US5700823A Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US5700823A
公开(公告)日：1997-12-23
申请号：US179570
申请日：1994-01-07
申请人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgy Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers
发明人： Klaus Peter Hirth , Donna Pruess Schwartz , Elaina Mann , Laura Kay Shawver , Gyorgy Keri , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Axel Ullrich , Reiner Lammers
IPC分类号： A61K9/00 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , C07C255/23 , C07D231/38 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , C07D498/04 , G01N33/50 , A61K31/175
CPC分类号： C07D231/38 , A61K31/165 , A61K31/167 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , A61K45/06 , A61K47/10 , A61K47/26 , A61K9/0019 , C07C255/23 , C07D239/91 , C07D241/38 , C07D241/42 , C07D487/04 , G01N33/5011 , Y10S977/904 , Y10S977/911 , Y10S977/912 , Y10S977/915
摘要： Method for treating a patient inflicted with a cell proliferation disorder, such as a cancer, characterized by inappropriate PDGF-R activity. The method involves the step of administering to the patient a therapeutically effective amount of a composition described in application.
摘要翻译：用于治疗患有细胞增殖病症（例如癌症）的患者的方法，其特征在于不适当的PDGF-R活性。该方法包括向患者施用治疗有效量的应用中描述的组合物的步骤。

5. 发明授权

US06331555B1 Treatment of platelet derived growth factor related disorders such as cancers 失效
标题翻译：治疗血小板衍生生长因子相关疾病如癌症
公开(公告)号：US06331555B1
公开(公告)日：2001-12-18
申请号：US09363237
申请日：1999-07-27
申请人： Klaus P. Hirth , Elaina Mann , Laura K. Shawyer , Axel Ullrich , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Peng Cho Tang , Reiner Lammers
发明人： Klaus P. Hirth , Elaina Mann , Laura K. Shawyer , Axel Ullrich , Istvan Szekely , Tamas Bajor , Janis Haimichael , Laszlo Orfi , Alex Levitzki , Aviv Gazit , Peng Cho Tang , Reiner Lammers
IPC分类号： A61K3142
CPC分类号： A61K31/135 , A61K31/12 , A61K31/13 , A61K31/415 , A61K31/42
摘要： The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.
摘要翻译：本发明涉及可以抑制血小板衍生生长因子受体（PDGF-R）活性的化合物，优选地，这些化合物也抑制PDGF-R超家族的其他成员的活性，并且对PDGF-R超家族的成员是选择性的。 PDGF-R超家族包括PDGF-R和PDGF-R相关的激酶Flt和KDR。特征化合物在细胞培养物中是有活性的，以降低PDGF-R，优选一种或多种PDGF-R相关激酶的活性。以下描述特征化合物A10（参见图1a）及其抑制体内肿瘤细胞生长的能力的实例。使用本申请作为指导，可以获得能够抑制PDGF-R，优选Flt和/或KDR的其它化合物。这些化合物优选用于治疗患有以不适当的PDGF-R活性为特征的细胞增殖性疾病的患者。

6. 发明授权

US4638002A 2,3,4-trinor-1,5-inter-meta-phenylene-prostacyclin compounds useful in inhibiting thrombocyte aggregation 失效
公开(公告)号：US4638002A
公开(公告)日：1987-01-20
申请号：US576399
申请日：1983-12-30
申请人： Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
发明人： Istvan Szekely , Sandor Botar , Krisztina Dolgos nee Kekesi , Bela Bertok , Antal Gajary , Tamas Szabolcsi , Gabor Kovacs , Marianna Lovasz nee Gaspar
IPC分类号： C07C69/76 , A61K31/343 , A61K31/5585 , A61P1/04 , A61P39/00 , C07C51/363 , C07C51/367 , C07C63/04 , C07C63/70 , C07C65/03 , C07C65/21 , C07C67/00 , C07C69/88 , C07C201/00 , C07C205/58 , C07C231/00 , C07C231/12 , C07C253/00 , C07C405/00 , C07D209/42 , C07D257/04 , C07D307/00 , C07D307/935 , C07D307/937 , C07D405/00 , C07D405/10 , C07F9/40 , C07F9/535 , C07F9/54 , A61K31/44
CPC分类号： C07D257/04 , C07C205/58 , C07C255/00 , C07C405/00 , C07C405/0041 , C07C405/0083 , C07C65/03 , C07C65/21 , C07D307/935 , C07D307/937 , C07D405/10 , C07F9/4015 , C07F9/5352 , C07F9/5456
摘要： The invention relates to new 2,3,4-trinor-1,5-inter-m-phenylene-PGI.sub.2 derivatives of the formula (I) ##STR1## wherein A stands for carboxy, cyano, tetrazolyl or --COOR.sup.3 or --CONR.sup.1 R.sup.2 ;R.sup.3 is C.sub.1-4 alkyl or an equivalent of a pharmacologically acceptable cation:R.sup.1 and R.sup.2 each stands for hydrogen, phenyl; C.sub.1-5 alkyl, optionally substituted by carboxy, hydroxy, phenyl or C.sub.2-5 alkoxycarbonyl; or C.sub.1-4 alkylsulfonyl; orR.sup.1 and R.sup.2 together form an .alpha.,.omega.-alkylene chain containing 3-6 carbon atoms;B stands for oxygen or methylene;Y is optionally bromo-substituted vinylene or a --C.tbd.C-- group:R.sup.4 stands for hydrogen or tetrahydro-pyran-2-yl;R.sup.5 represents an alkyl group containing 5-9 carbon atoms, which can be optionally interrupted by one or more oxygen atom(s) or --CH.dbd.CH-- or --C.tbd.C-- group(s) and/or optionally substituted by halogen; or a phenyoxymethyl group optionally substituted by halogen or trifluoromethyl; or an alkenoyloxymethyl group containing 3-5 carbon atoms;R.sup.6 is hydrogen or C.sub.1-4 alkyl;R.sup.7 stands for hydrogen, halogen, cyano, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sup.8 is hydrogen, halogen, cyano, nitro, hydroxy or C.sub.2-5 alkanoylamido;with the proviso that ifR.sup.5 stands for an alkyl group containing 5-9 carbon atoms which is unsubstituted or not interrupted by an oxygen atom or a --CH.dbd.CH-- or --C.tbd.C-- group; or a phenyoxymethyl group optionally substituted by halogen or trifluoromethyl, theneither R.sup.7 or R.sup.8 is other than hydrogen, or A is other than carboxy or --COOR.sup.3 and a process for the preparation thereof.The new compounds of the Formula I exhibit prolonged cytoprotecting and aggregation inhibiting and a low hypotensive effect and are superior to prostacycline in the prolonged duration of their activity.

7. 发明授权

US4429123A Preparation of 6-keto-7-oxo-PGF.sub.1.alpha. -derivatives 失效
标题翻译： 6-酮-7-氧代-PGF1 + 60 + B衍生物的制备
公开(公告)号：US4429123A
公开(公告)日：1984-01-31
申请号：US368016
申请日：1982-04-13
申请人： Istvan Tomoskozi , Istvan Szekely , Karoly Kanai , Peter Gyori , Gabor Kovacs
发明人： Istvan Tomoskozi , Istvan Szekely , Karoly Kanai , Peter Gyori , Gabor Kovacs
IPC分类号： C07D307/935 , A61K31/557 , A61P1/12 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07D307/937
CPC分类号： C07D307/937
摘要： The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## (wherein A is a straight or branched chain alkylene group having 1-5 carbon atoms;B is ethylene, Z or E vinylene, or ethynylene;R.sup.1 stands for hydrogen, an alkyl group having 1-5 carbon atoms or a pharmaceutically acceptable cation;R.sup.2 is hydrogen, an alkanoyl group having 1-5 carbon atoms or aroyl;R.sup.3 is hydrogen or methyl;R.sup.4 is a straight or branched chain alkyl group having 1-8 carbon atoms or an optionally monosubstituted aryloxymethyl group;R.sup.5 stands for hydrogen or an alkyl group having 1-5 carbon atoms)which comprises oxidizing a compound of the Formula III, IV or V ##STR2## or a mixture thereof R.sup.6 is hydrogen or an alkyl or alkanoyl group having 1-5 carbon atoms with a mild electrophilic oxidizing agent and if desired reacting the compound of the Formula I thus obtained wherein R.sup.5 is hydrogen with an alkanol containing 1-5 carbon atoms in the presence of boron trifluoride etherate in a manner known per se to yield the corresponding compound of the Formula I in which R.sup.5 is an alkyl group having 1-5 carbon atoms.
摘要翻译：本发明涉及制备通式Ⅰ（I）化合物的方法（其中A是具有1-5个碳原子的直链或支链亚烷基; B是乙烯，Z或E亚乙烯基，或亚乙炔基; R 1表示氢，具有1-5个碳原子的烷基或药学上可接受的阳离子; R 2是氢，具有1-5个碳原子的烷酰基或芳酰基; R 3是氢或甲基; R 4是直链或具有1-8个碳原子的支链烷基或任选的单取代的芳氧基甲基; R 5代表氢或具有1-5个碳原子的烷基），其包括将式III，IV或V的化合物（III （V）或其混合物R6是氢或具有1-5个碳原子的烷基或烷酰基，具有温和的亲电氧化剂，如果需要，则使式I的化合物反应其中R5是含有1-5个碳原子的链烷醇原子在三氟化硼乙醚合物存在下，以本身已知的方式得到相应的式I化合物，其中R 5为具有1-5个碳原子的烷基。

8. 发明授权

US4176122A Process for the preparation of bicyclic enone compounds 失效
标题翻译：双环烯酮化合物的制备方法
公开(公告)号：US4176122A
公开(公告)日：1979-11-27
申请号：US770997
申请日：1977-02-22
申请人： Istvan Szekely , Istvan Tomoskozi , Gabor Kovacs , Vilmos Simonidesz , Marianna Lovasz nee Gaspar , Borbala nee Ordog Keresztes , Julia nee Radoczi Remport , Istvan Stadler , Zsuzsa nee Gombos Visky , Csaba Szantay
发明人： Istvan Szekely , Istvan Tomoskozi , Gabor Kovacs , Vilmos Simonidesz , Marianna Lovasz nee Gaspar , Borbala nee Ordog Keresztes , Julia nee Radoczi Remport , Istvan Stadler , Zsuzsa nee Gombos Visky , Csaba Szantay
IPC分类号： A61K31/34 , A61K31/343 , A61P43/00 , C07D307/935 , C07D307/93
CPC分类号： C07D307/935
摘要： A process for the preparation of bicyclic enon compounds in which a lactone diol is selectively oxidized to obtain a hydroxy-aldehyde with one hydroxyl group and, without isolation, the hydroxy-aldehyde is reacted with a phosphorus compound. The reaction product can be acylated or silylated.
摘要翻译：制备双环烯酮化合物的方法，其中内酯二醇被选择性氧化以获得具有一个羟基的羟基醛，并且在不分离的情况下，羟基醛与磷化合物反应。反应产物可以被酰化或甲硅烷基化。

9. 发明申请

US20050171176A1 Pharmaceutically active aromatic guanylhydrazones 审中-公开
标题翻译：药用活性芳香脒腙
公开(公告)号：US20050171176A1
公开(公告)日：2005-08-04
申请号：US11052325
申请日：2005-02-07
申请人： Dorian Bevec , Joachim Hauber , Sabine Obert , Gyorgy Keri , Laszlo Orfi , Istvan Szekely , Axel Choidas , Gerald Bacher
发明人： Dorian Bevec , Joachim Hauber , Sabine Obert , Gyorgy Keri , Laszlo Orfi , Istvan Szekely , Axel Choidas , Gerald Bacher
IPC分类号： A61K31/155 , A61K31/17 , A61K31/22 , A61K31/4164 , A61K45/06 , A61P31/04 , A61P31/18 , C07C281/18 , A61K31/4172 , A61K31/165
CPC分类号： A61K45/06 , A61K31/155 , A61K31/17 , A61K31/4164 , C07C281/18 , Y02A50/402 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/479 , Y02A50/481
摘要： The present invention relates to aromatic guanylhydrazone compounds and their use as pharmaceutically active agents, especially for prophylaxis and treatment of virally caused diseases and infections, including opportunistic infections. The inventive guanylhydrazone compounds are also useful as inhibitors of deoxyhypusine synthase and as inhibitors for nuclear export in infectious diseases and may be used to regulate bacterially induced TNF-α production. Furthermore, the aromatic guanylhydrazones exhibit antibacterial activity against Gram positive and Gram negative bacteria and can be regarded as a novel class of antibiotics. In addition, methods for prophylaxis and treatment of virally or bacterially induced infections and diseases are disclosed together with pharmaceutical compositions useful within said methods containing at least one aromatic guanylhydrazone of the present invention as active ingredient.
摘要翻译：本发明涉及芳香脒腙化合物及其作为药物活性剂的用途，特别是用于预防和治疗病毒引起的疾病和感染，包括机会性感染。本发明的脒腙化合物也可用作脱氧酪氨酸合成酶的抑制剂，并且可用作感染性疾病中核出口的抑制剂，并可用于调节细菌诱导的TNF-α产生。此外，芳香脒腙对革兰氏阳性和革兰氏阴性细菌具有抗菌活性，可被认为是一类新型抗生素。此外，还公开了用于预防和治疗病毒或细菌诱导的感染和疾病的方法以及在含有本发明的至少一种芳香脒腙作为活性成分的所述方法中有用的药物组合物。

10. 发明授权

US5587370A Acaricidally active tetrazine derivatives 失效
标题翻译：杀螨活性四嗪衍生物
公开(公告)号：US5587370A
公开(公告)日：1996-12-24
申请号：US521253
申请日：1995-08-30
申请人： Janis Hajimichael , Sandor Botar , Edit Bleicher , Laszlo Pap , Istvan Szekely , Katalin Marmarosi n ee Kellner , Janos Ori
发明人： Janis Hajimichael , Sandor Botar , Edit Bleicher , Laszlo Pap , Istvan Szekely , Katalin Marmarosi n ee Kellner , Janos Ori
IPC分类号： A01N43/713 , A01P7/02 , C07D257/08
CPC分类号： C07D257/08 , A01N43/713
摘要： The invention relates to novel 1,2-dihydro-1,2,4,5-tetrazine derivatives of the formula (IV) ##STR1## wherein means fluorine, chlorine or bromine; andY stands for hydrogen or fluorine,as well as to a process for the preparation thereof. The compounds according to the invention have acaricidal, larvicidal and ovicidal effects.
摘要翻译：本发明涉及新的式（Ⅳ）的1,2-二氢-1,2,4,5-四嗪衍生物，其中意指氟，氯或溴; 和Y代表氢或氟，以及其制备方法。根据本发明的化合物具有杀螨，杀幼体和杀卵作用。

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