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公开(公告)号：US07678790B2
公开(公告)日：2010-03-16
申请号：US11286259
申请日：2005-11-23
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D417/12 , C07D411/12 , C07D417/14 , C07D401/04 , A61K31/40 , A61K31/38 , A61K31/44 , A61K31/425 , A61K31/495 , A61K31/55
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
摘要翻译： 式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。
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公开(公告)号：US07022731B2
公开(公告)日：2006-04-04
申请号：US10759396
申请日：2004-01-15
申请人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
发明人： Robert M. Scarborough , Hans-Michael Jantzen , Wolin Huang , David M. Sedlock , Charles Marlowe
IPC分类号： C07D409/12 , A61K31/4025 , A61P7/02
CPC分类号： C07D239/22 , C07D239/48 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D495/04
摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)–(VI), or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20050113399A1
公开(公告)日：2005-05-26
申请号：US10956006
申请日：2004-09-29
IPC分类号： A61K31/4709 , A61K31/506 , C07D217/24 , C07D401/04 , C07D409/12 , C07D49/14
CPC分类号： C07D409/14 , C07D217/24 , C07D401/04 , C07D409/12
摘要： Isoquinolinone compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
摘要翻译： 提供了可用于抑制ADP-血小板聚集的异喹啉酮化合物，特别是在治疗血栓形成和血栓形成相关病症或病症中。
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4.发明授权Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof 失效腺嘌呤环腺苷酸腺嘌呤抑制剂，药物组合物及其使用方法公开(公告)号：US06887880B2
公开(公告)日：2005-05-03
申请号：US09989348
申请日：2001-11-20
IPC分类号： C07D473/34 , A61K31/52 , A61P9/04
CPC分类号： C07D473/34
摘要： The present invention relates to derivatives and analogues of adenine of the formula: wherein L, A, Y and Z are those defined herein. Compounds of the present invention are useful in inhibiting adenylyl cyclase activity. The present invention also relates to a method of preventing and inhibiting a patient's fibroproliferative vasculopathy following vascular injury or a vascular surgical operation which includes administering to the patient, an effective amount of a compound according to the invention subsequent to a vascular injury, or subsequent to a vascular surgical operation, for one to two weeks after the injury or surgical operation, effective to treat or prevent a patient's fibroproliferative vasculopathy such as chronic allograft rejection or vascular restenosis following vascular trauma. The present invention also relates to a method for measuring the inhibition of adenylyl cyclase activity and a method for treating congestive heart failure.
摘要翻译： 本发明涉及下式的腺嘌呤的衍生物和类似物：其中L，A，Y和Z是本文定义的那些。 本发明的化合物可用于抑制腺苷酸环化酶活性。 本发明还涉及在血管损伤或血管外科手术之后预防和抑制患者的纤维增生性血管病变的方法，其包括向患者施用有效量的血管损伤后的本发明化合物或随后的 在损伤或外科手术后一至两周进行血管外科手术，有效治疗或预防患者的纤维增生性血管病变，如血管创伤后的慢性同种异体移植排斥或血管再狭窄。 本发明还涉及测定腺苷酸环化酶活性抑制的方法和治疗充血性心力衰竭的方法。
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公开(公告)号：US06534535B1
公开(公告)日：2003-03-18
申请号：US09636804
申请日：2000-08-10
申请人： Bing-Yan Zhu , Robert M. Scarborough , Lane Clizbe , Brandon Doughan , Zhaozhong Jon Jia , Kim Kane-Maguire , Charles Marlowe , Yonghong Song , Ting Su , Willy Teng , Penglie Zhang
发明人： Bing-Yan Zhu , Robert M. Scarborough , Lane Clizbe , Brandon Doughan , Zhaozhong Jon Jia , Kim Kane-Maguire , Charles Marlowe , Yonghong Song , Ting Su , Willy Teng , Penglie Zhang
IPC分类号： A61K3140
CPC分类号： C07D215/227 , C07D209/08 , C07D209/34 , C07D209/38 , C07D215/08 , C07D231/56 , C07D235/06 , C07D235/26 , C07D241/38 , C07D241/44 , C07D243/24 , C07D265/36 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D409/06 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.
摘要翻译： 公开了与哺乳动物因子Xa具有活性的新型化合物，其盐和与其相关的组合物。 以下式（I）的化合物：在体外或体内可用于预防或治疗凝血障碍。
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6.发明授权Herbicidal 12-substituted 12H-dibenzo(D,G)(1,3)dioxocin-6-carboxylic acids 失效除草12-取代的12H-二苯并（D，G）（1,3）二氧杂环己烯-6-羧酸
公开(公告)号：US4938790A
公开(公告)日：1990-07-03
申请号：US366382
申请日：1989-06-15
IPC分类号： A01N43/24 , C07C39/17 , C07C41/30 , C07C43/205 , C07C43/21 , C07C43/215 , C07C43/23 , C07C43/315 , C07C49/84 , C07D321/12
CPC分类号： C07D321/12 , A01N43/24
摘要： Dibenzo[d,g][1,3]dioxocin-6-carboxylic acids substituted by methyl or ethyl or a moiety --CH.sub.2 CH.sub.2 -- at the 12-position and optionally substituted at other positions, such as methyl 4'-chlorospiro(cyclopropane-1,12'(12'H)-dibenzo[d,g][1,3]dioxocin)-6'-carboxylic acid, and their agriculturally acceptable esters, amides, and salts are useful for the control of undesirable vegetation. The 1,1-diarylcyclopropane intermediates required for the spirocyclopropane compounds can be prepared from appropriately substituted 1,1-diarylethene procursors by reaction with phenylthiomethyl lithium reagent.
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7.发明授权Herbicidal 12-substituted 12H-dibenzo[d,g]dioxocin-6-carboxylic acids 失效除草12-取代的12H-二苯并[d，g]二氧杂环己烯-6-羧酸
公开(公告)号：US5158597A
公开(公告)日：1992-10-27
申请号：US586165
申请日：1990-09-21
IPC分类号： A01N43/24 , C07D321/12
CPC分类号： A01N43/24 , C07D321/12
摘要： Dibenzo[d,g][1,3]dioxocin-6-carboxylic acids substituted by methyl or ethyl or a moiety --CH.sub.2 CH.sub.2 -- at the 12-position and optionally substituted at other positions, such as methyl 4'-chlorospiro(cyclopropane-1,12'(12'H)-dibenzo[d,g][1,3]dioxocin)-6'-carboxylic acid, and their agriculturally acceptable esters, amides, and salts are useful for the control of undesirable vegetation. The 1,1-diarylcyclopropane intermediates required for the spirocyclopropane compounds can be prepared from appropriately substituted 1,1-diarylethene procursors by reaction with phenylthiomethyl lithium reagent.
摘要翻译： 被甲基或乙基取代的二苯并[d，g] [1,3]二氧杂环己烯-6-羧酸或在12位被-CH 2 CH 2 - 部分取代的任选取代基，例如甲基4'-氯螺（环丙烷 - 1,12'（12'H） - 二苯并[d，g] [1,3]二氧杂环己烯）-6'-羧酸，它们的农业上可接受的酯，酰胺和盐可用于控制不期望的植被。 螺环丙烷化合物所需的1,1-二芳基环丙烷中间体可以通过与苯基硫代甲基锂试剂的反应从适当取代的1,1-二芳基乙前体制备。
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8.发明授权Herbicidal 12-substituted 12H-dibenzo[d,g][1,3]dioxocin-6-carboxylic acids 失效除草12-取代的12H-二苯并[d，g] [1,3]二氧杂环己烯-6-羧酸
公开(公告)号：US5071465A
公开(公告)日：1991-12-10
申请号：US508371
申请日：1990-04-12
IPC分类号： A01N43/24 , C07D321/12
CPC分类号： C07D321/12 , A01N43/24
摘要： Dibenzo[d,g][1,3]dioxocin-6-carboxylic acids substituted by methyl or ethyl or a moiety --CH.sub.2 CH.sub.2 -- at the 12-position and optionally substituted at other positions, such as methyl 4'-chlorospiro(cyclopropane-1,12'(12'H)-dibenzo[d,g][1,3]dioxocin)-6'-carboxylic acid, and their agriculturally acceptable esters, amides, and salts are useful for the control of undesirable vegetation. The 1,1-diarylcyclopropane intermediates required for the spirocyclopropane compounds can be prepared from appropriately substituted 1,1-diarylethene procursors by reaction with phenylthiomethyl lithium reagent.
摘要翻译： 被甲基或乙基取代的二苯并[d，g] [1,3]二氧杂环己烯-6-羧酸或在12位被-CH 2 CH 2 - 部分取代的任选取代基，例如甲基4'-氯螺（环丙烷 - 1,12'（12'H） - 二苯并[d，g] [1,3]二氧杂环己烯）-6'-羧酸，其农业上可接受的酯，酰胺和盐可用于控制不希望的植被。 螺环丙烷化合物所需的1,1-二芳基环丙烷中间体可以通过与苯基硫代甲基锂试剂的反应由适当取代的1,1-二芳基乙前体制备。
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公开(公告)号：US4999448A
公开(公告)日：1991-03-12
申请号：US508208
申请日：1990-04-12
IPC分类号： A01N43/24 , C07C43/205 , C07C43/21 , C07C43/215 , C07C43/23 , C07C43/313 , C07C43/315 , C07C45/29 , C07C49/84 , C07C205/37 , C07C205/38 , C07D321/12
CPC分类号： C07D321/12 , A01N43/24 , C07C41/30 , C07C45/29 , C07C45/292 , C07C2101/02
摘要： A method of preparing a compound of Formula XII ##STR1## wherein R.sub.1 and R.sub.2 together represent the fragment --Ch.sub.2 CH.sub.2 --;each R.sup.4 independently represents C.sub.1 -C.sub.4 alkyl optionally substituted with 1 to 2 C.sub.1 -C.sub.4 alkoxy groups; andX, X', Y, Y', Z, and Z' each, independently represent H, F, Cl, Br, I, CN, NO.sub.2, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenoxy, C.sub.1 -C.sub.4 alkylthio, phenylthio, or C.sub.1 -C.sub.4 dialkylamino, wherein each alkyl, alkoxy, and alkylthio group is optionally substituted with one or more compatible groups selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, F, Cl, Br, CN, and phenyl and wherein each phenyl group is optionally substituted with up to 3 groups selected from F, Cl, Br, CN, CF.sub.3, C.sub.1 -C.sub.4 alkyl, and C.sub.1 -C.sub.4 alkoxy.
摘要翻译： 制备式XII化合物的方法其中R1和R2一起表示片段-Ch2CH2-; 每个R 4独立地表示任选被1至2个C 1 -C 4烷氧基取代的C 1 -C 4烷基; 并且X，X'，Y，Y'，Z和Z'各自独立地表示H，F，Cl，Br，I，CN，NO 2，C 1 -C 4烷基，C 1 -C 4烷氧基，苯氧基，C 1 -C 4烷硫基 ，苯硫基或C 1 -C 4二烷基氨基，其中每个烷基，烷氧基和烷硫基任选地被一个或多个选自C 1 -C 4烷氧基，C 1 -C 4烷硫基，F，Cl，Br，CN和苯基的相容基取代;以及 其中每个苯基任选被至多3个选自F，Cl，Br，CN，CF 3，C 1 -C 4烷基和C 1 -C 4烷氧基的基团取代。
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公开(公告)号：US20050228029A1
公开(公告)日：2005-10-13
申请号：US10941053
申请日：2004-09-13
IPC分类号： C07D239/96 , A61K31/16 , A61K31/175 , A61K31/381 , A61K31/4196 , A61K31/4725 , A61K31/519 , A61K31/54 , A61K31/64 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/14 , A61P43/00 , C07D209/48 , C07D213/70 , C07D239/22 , C07D239/50 , C07D333/34 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12 , C07D487/04 , C07D495/04 , C07D521/00
CPC分类号： C07D487/04 , C07D209/48 , C07D239/22 , C07D239/48 , C07D239/50 , C07D239/96 , C07D333/34 , C07D333/62 , C07D401/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D495/04 , C07D521/00
摘要： Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.
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