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91. 发明授权

US09115127B2 Benzimidazole and azabenzimidazole compounds that inhibit anaplastic lymphoma kinase 有权
标题翻译：抑制间变性淋巴瘤激酶的苯并咪唑和氮杂苯并咪唑化合物
公开(公告)号：US09115127B2
公开(公告)日：2015-08-25
申请号：US13813813
申请日：2011-07-28
申请人： Christiane M. Boezio , Alan C. Cheng , Deborah Choquette , Richard T. Lewis , Michele H. Potashman , Karina Romero , John C. Stellwagen , Douglas A. Whittington
发明人： Christiane M. Boezio , Alan C. Cheng , Deborah Choquette , Richard T. Lewis , Michele H. Potashman , Karina Romero , John C. Stellwagen , Douglas A. Whittington
IPC分类号： C07D235/30 , C07D235/32 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/14 , C07D417/04 , C07D413/04 , A61P35/00 , C07D471/04 , C07D417/06 , C07D487/04 , C07D401/10 , C07D413/10 , C07D413/14 , C07D417/14 , C07D417/12 , C07D519/00
CPC分类号： C07D471/04 , C07D235/30 , C07D235/32 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D413/10 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D487/04 , C07D519/00
摘要： Compounds of Formula (I) are useful inhibitors of anaplastic lymphoma kinase. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
摘要翻译：式（I）的化合物是间变性淋巴瘤激酶的有用的抑制剂。式（I）的化合物具有以下结构：其中本文提供变量的定义。

92. 发明授权

US09107411B2 Indolecarboxamides and benzimidazolecarboxamides as insecticides and acaricides 有权
标题翻译：吲哚甲酰胺和苯并咪唑酰胺作为杀虫剂和杀螨剂
公开(公告)号：US09107411B2
公开(公告)日：2015-08-18
申请号：US14003778
申请日：2012-03-05
申请人： Markus Heil , Eike Kevin Heilmann , Graham Holmwood , Peter Jeschke , Michael Maue , Tobias Kapferer , Matthias Riedrich , Angela Becker , Olga Malsam , Peter Lösel , Arnd Voerste , Ulrich Görgens , Roland Andree
发明人： Markus Heil , Eike Kevin Heilmann , Graham Holmwood , Peter Jeschke , Michael Maue , Tobias Kapferer , Matthias Riedrich , Angela Becker , Olga Malsam , Peter Lösel , Arnd Voerste , Ulrich Görgens , Roland Andree
IPC分类号： C07D209/42 , C07D235/24 , A01N43/52 , A01N43/38 , C07D209/24 , C07D235/32
CPC分类号： A01N43/52 , A01N43/38 , C07D209/24 , C07D209/42 , C07D235/24 , C07D235/32
摘要： The present invention relates to compounds of the general formula (I) in which R1 to R6, A, Y, X, G, n and m are each as defined in the description—and to a process for preparation thereof and to the use thereof as insecticides and acaricides.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1至R 6，A，Y，X，G，n和m各自如说明书中所定义 - 及其制备方法及其用途作为杀虫剂和杀螨剂。

93. 发明申请

US20140228378A1 N-(Benzimimdazol-2-yl)-Cyclopropane Carboxamides as Lysophosphatidic Acid Antagonists 有权
标题翻译： N-（苯并咪唑-2-基） - 环丙烷甲酰胺作为溶血磷脂酸拮抗剂
公开(公告)号：US20140228378A1
公开(公告)日：2014-08-14
申请号：US14237446
申请日：2012-07-07
申请人： Wolfgang Staehle , Melanie Schultz , Kai Schiemann
发明人： Wolfgang Staehle , Melanie Schultz , Kai Schiemann
IPC分类号： C07D473/00 , A61K31/437 , A61K31/454 , A61K31/4184 , C07D231/56 , C07D471/04 , C07D401/12 , C07D403/12 , C07D235/32 , A61K31/52 , A61K31/416
CPC分类号： C07D473/00 , A61K31/416 , A61K31/4184 , A61K31/437 , A61K31/454 , A61K31/52 , C07D231/56 , C07D235/30 , C07D235/32 , C07D401/12 , C07D403/12 , C07D417/04 , C07D471/04
摘要： The invention provides novel substituted cyclopropane carboxamide compounds according to Formula (I), their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.
摘要翻译：本发明提供根据式（I）的新型取代的环丙烷甲酰胺化合物，其用于治疗增殖性或炎性疾病如癌症，纤维化或关节炎的制备和用途。

94. 发明申请

US20140045909A1 DENIBULIN DI-HYDROCHLORIDE 审中-公开
标题翻译：丹尼林二氢氯化物
公开(公告)号：US20140045909A1
公开(公告)日：2014-02-13
申请号：US14053289
申请日：2013-10-14
申请人： MediciNova, Inc.
发明人： Kale RUBY
IPC分类号： C07D235/32 , A61K31/4184 , A61K45/06
CPC分类号： C07D235/32 , A61K31/4184 , A61K45/06
摘要： MN-029 di-hydrochloride (MN-029.2HCl, Formula 2) is a potent vascular targeting agent. The present invention focuses on the synthesis and characterization of the di-hydrochloride salt MN-029 and the preparation of pharmaceutically acceptable formulations thereof. Methods are disclosed of using the compound and formulations thereof in the treatment of diseases that rely on the generation of neovasculature by angiogenesis for disease progression.
摘要翻译： MN-029二盐酸盐（MN-029.2HCl，式2）是有效的血管靶向剂。本发明着重于二盐酸盐MN-029的合成和表征及其药学上可接受的制剂的制备。公开了使用该化合物及其制剂治疗依赖于通过血管发生用于疾病进展的新血管生成的疾病的方法。

95. 发明申请

US20110172245A1 HETEROCYCLIC COMPOUND AND USE THEREOF 有权
标题翻译：杂环化合物及其用途
公开(公告)号：US20110172245A1
公开(公告)日：2011-07-14
申请号：US12674801
申请日：2008-08-22
申请人： Masaaki Hirose , Masanori Okaniwa , Takashi Imada
发明人： Masaaki Hirose , Masanori Okaniwa , Takashi Imada
IPC分类号： A61K31/496 , C07D235/32 , A61K31/4184 , C07D263/58 , A61K31/423 , C07D277/82 , A61K31/428 , C07D417/12 , A61P35/00
CPC分类号： C07D235/30 , C07D263/58 , C07D277/82 , C07D417/12
摘要： Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译：提供显示出强的Raf抑制活性的杂环化合物。由下式表示的化合物，其中每个符号如说明书中所定义，或其盐。

96. 发明申请

US20050288348A1 Compounds and methods for use thereof in the treatment of cancer 审中-公开
标题翻译：用于治疗癌症的化合物和方法
公开(公告)号：US20050288348A1
公开(公告)日：2005-12-29
申请号：US11204707
申请日：2005-08-16
申请人： James Camden , James Quada , Joseph Agyin
发明人： James Camden , James Quada , Joseph Agyin
IPC分类号： A61K31/4184 , C07D235/30 , C07D235/32
CPC分类号： C07D235/30 , A61K31/4184 , C07D235/32
摘要： Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
摘要翻译：公开了苯并咪唑衍生物及其盐和前药，以及通过施用这些化合物治疗温血动物中的癌症或病毒感染的方法。这样的化合物可以与化疗剂和/或增效剂组合使用。

97. 发明授权

US06930121B2 Compounds and methods for use thereof in the treatment of viral infections 失效
公开(公告)号：US06930121B2
公开(公告)日：2005-08-16
申请号：US10267051
申请日：2002-10-08
申请人： James Berger Camden , James C. Quada, Jr. , Joseph K. Agyin
发明人： James Berger Camden , James C. Quada, Jr. , Joseph K. Agyin
IPC分类号： A61K31/4184 , C07D235/30 , C07D235/32 , A61K31/415
CPC分类号： C07D235/30 , A61K31/4184 , C07D235/32
摘要： Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.

98. 发明授权

US06916836B2 Compounds and methods for use thereof in the treatment of viral infections 失效
标题翻译：用于治疗病毒感染的化合物和方法
公开(公告)号：US06916836B2
公开(公告)日：2005-07-12
申请号：US10634542
申请日：2003-08-05
申请人： James Berger Camden , James C. Quada, Jr. , Joseph K. Agyin
发明人： James Berger Camden , James C. Quada, Jr. , Joseph K. Agyin
IPC分类号： A61K31/4184 , C07D235/30 , C07D235/32 , A61K31/425 , A61K31/415
CPC分类号： C07D235/32 , A61K31/4184 , C07D235/30
摘要： Benzimidazole derivatives and salts and prodrugs thereof are disclosed, together with methods for the treatment of cancers or viral infections in warm blooded animals by administration of these compounds. Such compounds may be used in combination with a chemotherapeutic agent and/or a potentiator.
摘要翻译：公开了苯并咪唑衍生物及其盐和前药，以及通过施用这些化合物治疗温血动物中的癌症或病毒感染的方法。这样的化合物可以与化疗剂和/或增效剂组合使用。

99. 发明申请

US20050038022A1 Method for treatment of cancer and compositions for use therein 审中-公开
标题翻译：治疗癌症的方法及其中使用的组合物
公开(公告)号：US20050038022A1
公开(公告)日：2005-02-17
申请号：US10472888
申请日：2002-03-20
申请人： David Morris , Mohammad Pourgholami
发明人： David Morris , Mohammad Pourgholami
IPC分类号： C07D235/32 , A61K9/00 , A61K31/4164 , A61K31/4184 , A61K31/427 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K47/44 , A61P1/16 , A61P35/00 , A61P43/00
CPC分类号： A61K9/0019 , A61K31/4164 , A61K31/4184 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K47/44
摘要： The present invention provides a method for the treatment of a tumor in a subject. The method comprises administering to the subject a composition comprising a therapeutically effective amount of a compound of Formula (I), wherein R1 is selected from H, substituted or unsubstituted, straight or branch chain alkyl, alkenyl, alkenylalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aryl, arylalkyl, —SR7, —SOR8, —SO2R9, —SCN, B′(CH2)nBR10, —C(O)—R11 or —OR12, COOR13, —NO2, NR13aCOOR13b, isothiocyanato, or —CN where R7 to R13b are each independently selected from H, substituted or unsubstituted, straight or branch chain alkyl, alkenyl, alkenylalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aryl, arylalkyl, B and B′ are independently selected from O, S, S(O) or SO2 and n is 1 to 4; R2 is selected from H, or substituted or unsubstituted alkyl. R3 is selected from H, substituted or unsubstituted, straight or branch chain alkyl, alkenyl, alkenylalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aryl, arylalkyl, 5- or 6-membered heterocyclic ring the heteroatom(s) of which are selected from one of more of O, S and/or N, —SR14, —OR15, —SOR16, —SO2R17, —SCN, —C(O)—R18, —OR19, NR20COOR21, where R15 to R21 are each independently selected from H, substituted or unsubstituted, straight or branch chain alkyl, alkenyl, alkenylalkyl, cycloalkyl, cycloalkylalkyl, cycloalkenylalkyl, aryl or arylalkyl; or an analogue or metabolite thereof.
摘要翻译：本发明提供了治疗受试者中肿瘤的方法。该方法包括向受试者施用包含治疗有效量的式（I）化合物的组合物，其中R 1选自H，取代或未取代的直链或支链烷基，烯基，烯基烷基，环烷基，环烷基烷基，环烯基烷基，芳基，芳基烷基，-SR7，-SOR8，-SO2R9，-SCN，B'（CH2）nBR10，-C（O）-R11或-OR12，COOR13，-NO2，NR13aCOOR13b，异硫氰酸酯或-CN，其中R7至R13b 各自独立地选自H，取代或未取代的直链或支链烷基，烯基，烯基烷基，环烷基，环烷基烷基，环烯基烷基，芳基，芳基烷基，B和B'独立地选自O，S，S（O）或SO 2， n为1〜4; R2选自H或取代或未取代的烷基。 R 3选自H，取代或未取代的直链或支链烷基，烯基，烯基烷基，环烷基，环烷基烷基，环烯基烷基，芳基，芳烷基，5-或6-元杂环，杂原子选自更多的O，S和/或N，-SR 14，-OR 15，-SOR 16，-SO 2 R 17，-SCN，-C（O）-R 18，-OR 19，NR 20 COOR 21，其中R 15至R 21各自独立地选自H，或未取代的直链或支链烷基，烯基，烯基烷基，环烷基，环烷基烷基，环烯基烷基，芳基或芳基烷基; 或其类似物或代谢物。

100. 发明申请

US20050014811A1 Substituted benzimidazole compounds and their use for the treatment of cancer 失效
标题翻译：取代的苯并咪唑化合物及其用于治疗癌症的用途
公开(公告)号：US20050014811A1
公开(公告)日：2005-01-20
申请号：US10808889
申请日：2004-03-25
申请人： Francois Clerc , Francois Hamy , Isabelle Depaty , Odile Angouillant-Boniface , Stephanie Deprets , Chantal Carrez , Manfred Roesner
发明人： Francois Clerc , Francois Hamy , Isabelle Depaty , Odile Angouillant-Boniface , Stephanie Deprets , Chantal Carrez , Manfred Roesner
IPC分类号： C07D233/48 , A61K31/4184 , A61K31/422 , A61K31/4245 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/498 , A61K31/506 , A61K31/52 , A61K31/5377 , A61K31/55 , A61K31/551 , A61P35/00 , A61P43/00 , C07D235/30 , C07D235/32 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D473/34 , C07D235/16
CPC分类号： C07D235/30 , C07D235/32 , C07D401/12 , C07D403/12
摘要： The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is sleceted from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —O-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.
摘要翻译：本发明公开并要求式（I）的苯并咪唑化合物：其中A是芳基或杂芳基; R 1从任选取代的烷基，烷氧基，芳基或杂芳基，NH-低级烷基或NH-环烷基取代，或卤素，NH 2; 1-咪唑基或SO2Me; R 2选自任选取代的-CO-烷基，-CO-环烷基，-CO-芳烷基，-CO-芳基，-CO-烷氧基，芳基或芳烷基，或-O-氨基，CO-NHR3或CO-R3R4，其中R3 烷基，羟基烷基，烷氧基烷基，氟代烷基，炔基，杂烷基，烷基杂烷基，芳基，芳烷基或一起形成任选含有1至4个杂原子的亚烷基链; 其药学上可接受的盐或其前药; 使用式（I）化合物治疗癌症，以及包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物。

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