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公开(公告)号：US08501687B2
公开(公告)日：2013-08-06
申请号：US13159020
申请日：2011-06-13
CPC分类号： C07K14/655 , A61K38/00
摘要： SRIF peptide antagonists, which are selective for SSTR2 in contrast to the other cloned SRIF receptors and which bind with high affinity to the cloned human receptor SSTR2 but do not activate the receptor, have many useful functions. Because they do not bind with significant affinity to SSTR1, SSTR3, SSTR4 or SSTR5, their administration avoids potential undesirable side effects. By incorporating radioiodine or the like in these SSTR2-selective SRIF antagonists, a labeled compound useful in drug-screening methods is provided. Alternatively, for use in therapy, highly radioactive moieties can be N-terminally coupled, complexed or chelated thereto. Because they block the receptor function, they can be used therapeutically to block certain physiological effects which SSTR2 mediates.
摘要翻译： 与其他克隆的SRIF受体相比，SRIF肽拮抗剂对于SSTR2是选择性的，并且与克隆的人受体SSTR2以高亲和力结合但不激活受体具有许多有用的功能。 因为它们不与SSTR1，SSTR3，SSTR4或SSTR5具有显着的亲合力结合，所以它们的给药避免了潜在的不良副作用。 通过在这些SSTR2选择性SRIF拮抗剂中引入放射性碘等，提供了可用于药物筛选方法的标记化合物。 或者，为了在治疗中使用，高度放射性的部分可以与其N-末端偶联，复合或螯合。 因为它们阻断受体功能，它们可以用于治疗性地阻断SSTR2介导的某些生理作用。
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公开(公告)号：US07235538B2
公开(公告)日：2007-06-26
申请号：US10621302
申请日：2003-07-17
申请人： Anders Bendtz Kanstrup , Lise Brown Christiansen , Jane Marie Lundbeck , Christian K. Sams , Marit Kristiansen
发明人： Anders Bendtz Kanstrup , Lise Brown Christiansen , Jane Marie Lundbeck , Christian K. Sams , Marit Kristiansen
IPC分类号： A61K31/522 , A61K3/10 , A61K3/04 , C07D473/08 , C07D473/06
CPC分类号： C07D473/04 , C07D473/08
摘要： The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, which are of formula I wherein each n is one or two independently and R1, R2, R3, R6, R7, R9, and R10 are defined herein. The present invention also relates to pharmaceutical compositions comprising the compounds of formula I and the use of the compounds for treating diseases that are associated with proteins that are subject to inactivation by DPP-IV, such as type-2 diabetes and obesity.
摘要翻译： 本发明涉及酶DPP-IV的治疗活性和选择性抑制剂，其具有式I，其中每个n独立地为一个或两个，R 1，R 2， R 3，R 6，R 7，R 9，R 9和R 10， >在本文中定义。 本发明还涉及包含式I化合物的药物组合物和该化合物用于治疗与通过DPP-IV失活的蛋白质例如2型糖尿病和肥胖相关的疾病的用途。
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公开(公告)号：US07064122B2
公开(公告)日：2006-06-20
申请号：US10326302
申请日：2002-12-20
申请人： David Witter , Arlindo Castelhano
发明人： David Witter , Arlindo Castelhano
IPC分类号： C07D498/04 , A61K31/5365 , A61K1/18 , A61K3/10
CPC分类号： C07D513/04 , A61K31/5365 , A61K31/542 , C07D333/38 , C07D409/12 , C07D498/02 , C07D513/02
摘要： The subject invention features compounds having the structure: wherein X is O, S, CH2 or NR5; Y is O or S; R1 is H, substituted or unsubstituted C1-C15 alkyl, C1-C8 alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6′OR4, —CR6R6′OC(O)R4, —CR6R6′OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2 is a substituted or unsubstituted, straight chain C1—C30 alkyl or branched C3-C30 alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3 is H or substituted or unsubstituted C1-C6 alkyl or C3-C10 cycloalkyl; R4 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl, —CH2-aryl, aryl —C1-C15 alkyl, heteroaryl-C1-C15alkyl or C3-C10 cycloalkyl; R5 is H or a substituted or unsubstituted, straight chain or branched, C6-C30 alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6 and R6′ are each independently H, substituted or unsubstituted C1-C6 alkyl, dialkyl or C3-C10 cycloalkyl or together form a 3-7 membered ring system; R7 is H or substituted or unsubstituted C1-C12 alkyl or C3-C10 cycloalkyl; R8 and R9 are each independently H, substituted or unsubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylaryl, or NR8R9 together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
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