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1. 发明授权

US6013768A Kainate-binding human CNS receptors of the EAA1 family 失效
标题翻译： EAA家族的Kainate结合人CNS受体
公开(公告)号：US6013768A
公开(公告)日：2000-01-11
申请号：US789478
申请日：1997-01-27
申请人： Rajender Kamboj , Stephen L. Nutt , Lee Shekter , Michael A. Wosnick
发明人： Rajender Kamboj , Stephen L. Nutt , Lee Shekter , Michael A. Wosnick
IPC分类号： C07K16/00 , C07K14/00 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12R1/91 , G01N33/53
CPC分类号： C07K14/70571
摘要： Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described art recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.
摘要翻译：兴奋性氨基酸（EAAs）如谷氨酸的神经传递通过膜结合表面受体介导。已经分离了编码这些受体的一个家族的类红景天结合型EAA受体的DNA，并且以受体蛋白为特征。本文描述了产生EAA受体作为异源膜结合产物的重组细胞系。还描述了具有商业意义的本发明的相关方面。包括使用细胞系作为发现调节EAA受体刺激的化合物的工具。

2. 发明授权

US5798350A Dopamine receptor ligands 失效
标题翻译：多巴胺受体配体
公开(公告)号：US5798350A
公开(公告)日：1998-08-25
申请号：US642264
申请日：1996-05-03
申请人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
发明人： Ashok Tehim , Jian-Min Fu , Sumanas Rakhit
IPC分类号： A61K31/00 , A61K31/55 , A61P25/18 , A61P25/20 , C07D243/10 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/12 , C07D491/00 , A61K31/495 , A61K31/435 , C07D401/14 , C07D403/14
CPC分类号： C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO; X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--; R.sub.1 represents C.sub.1-4 alkyl; Y is selected from CH and N; n is 0, 1 or 2; q is 1 or 2; R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S; D is cyclohexane or benzene; and E is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是具有以下通式的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元，杂环或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-N（C 1-4烷基）2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，所以; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; R 1表示C 1-4烷基; Y选自CH和N; n为0,1或2; q为1或2; R2是任选地加入选自N，O和S的杂原子的C 1-6烷基; D是环己烷或苯; 并且E是掺杂有1,2或3个选自O，N和S的杂原子的饱和或不饱和的5-或6-元杂环，其中E任选被1或2个选自卤素，C 1-4烷基和卤素 - 取代的C 1-4烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗其中涉及D4受体的适应症的药物，例如精神分裂症。

3. 发明授权

US5561127A Muscarinic receptor ligands 失效
标题翻译：毒蕈碱受体配体
公开(公告)号：US5561127A
公开(公告)日：1996-10-01
申请号：US358471
申请日：1994-12-19
申请人： Ashok Tehim , Sumanas Rakhit
发明人： Ashok Tehim , Sumanas Rakhit
IPC分类号： C07D487/08 , A61K31/55 , C07D403/04 , C07D413/04 , C07D417/00
CPC分类号： C07D487/08
摘要： Described herein are D4 receptor-selective compounds of the general formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--NEt.sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 --is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;n is 1 or 2; andZ is selected from C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
摘要翻译：本文描述的是通式I的D4受体选择性化合物：其中：A和B独立选择，任选取代的饱和或不饱和的5-或6-元的同或杂环; X 1选自CH 2，O，NH，S，C = O，CH-OH，CH-NEt 2，C = CHCl，C = CHCN，N-C 1-4烷基，N-乙酰基，SO 2和SO; X2-选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; Z选自任选被选自OH，卤素，C 1-4烷基和C 1-4烷氧基的取代基取代的C 1-6烷基; 及其酸加成盐，溶剂化物和水合物。还描述了它们作为多巴胺受体鉴定和药物筛选程序的配体的用途，以及用于治疗M1 / M2受体涉及的指征的药物，例如精神分裂症。

4. 发明授权

US5504101A 5-HT-1D receptor ligands 失效
标题翻译： 5-HT-1D受体配体
公开(公告)号：US5504101A
公开(公告)日：1996-04-02
申请号：US238823
申请日：1994-05-06
申请人： Richard A. Glennon
发明人： Richard A. Glennon
IPC分类号： C07D209/16 , C07D209/04 , A61K31/40
CPC分类号： C07D209/16
摘要： Described herein are tryptamine analogs that display high binding affinity and selectivity for the 5-HT1D.beta. receptor, of the formula: ##STR1## wherein R.sup.1 is a group selected from aryl-C.sub.1-7 alkyl; aryl-C.sub.2-7 alkoxy; aryl-C.sub.2-7 alkanoyl and aryl-C.sub.1-7 alkanoyloxy, wherein said alkyl, alkoxy, alkanoyl and alkanoyloxy groups are optionally substituted by a C.sub.1-4 alkyl substituent and wherein said aryl group is optionally substituted by one or more substituent selected from hydroxyl, halogen, mercapto, linear or branched C.sub.1-4 alkyl, linear or branched C.sub.1-4 alkoxy, linear or branched C.sub.1-4 alkylthio, thiol substituted C.sub.1-4 alkyl and nitro substituted C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected independently from H and C.sub.1-4 alkyl; andR.sup.4 is selected from H, C.sub.1-4 alkyl, aryl and arylC.sub.1-4 alkyl. The compounds are useful as reagents for receptor identification and in receptor-based drug screening programs, and can also be used therapeutically to treat conditions for which administration of a 5-HT1D ligand is indicated, for example in the treatment of migraine.
摘要翻译：本文描述了对5-HT1Dβ受体显示出高结合亲和力和选择性的色胺类似物，其具有下式：其中R 1是选自芳基-C 1-7烷基的基团; 芳基-C 2-7烷氧基; 芳基-C 2-7烷酰基和芳基-C 1-7烷酰氧基，其中所述烷基，烷氧基，烷酰基和烷酰氧基任选被C 1-4烷基取代基取代，并且其中所述芳基任选被一个或多个选自羟基，卤素直链或支链C 1-4烷氧基，直链或支链C 1-4烷硫基，硫醇取代的C 1-4烷基和硝基取代的C 1-4烷基; R2和R3独立地选自H和C1-4烷基; 并且R 4选自H，C 1-4烷基，芳基和芳基C 1-4烷基。该化合物可用作受体鉴定试剂和基于受体的药物筛选程序，并且也可用于治疗性治疗指示施用5-HT1D配体的病症，例如用于治疗偏头痛。

5. 发明授权

US5494792A Kainate-binding, human CNS receptors of the EAA2 family 失效
标题翻译：凯赛汀结合，EAA2家族的人类CNS受体
公开(公告)号：US5494792A
公开(公告)日：1996-02-27
申请号：US91569
申请日：1993-07-15
申请人： Rajender Kamboj , Stephen L. Nutt , Lee Shekter , Michael A. Wosnick
发明人： Rajender Kamboj , Stephen L. Nutt , Lee Shekter , Michael A. Wosnick
IPC分类号： G01N33/53 , A61K38/00 , C07K14/705 , C07K16/28 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , C12R1/91 , C12N15/10 , C12Q1/00 , G01N33/50
CPC分类号： C07K14/70571 , A61K38/00 , Y10S530/839
摘要： Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commerical significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.
摘要翻译：兴奋性氨基酸（EAAs）如谷氨酸的神经传递通过膜结合表面受体介导。已经分离了编码这些受体的一个家族的类红景天结合型EAA受体的DNA，并且以受体蛋白为特征。本文描述了产生作为异源膜结合产物的EAA受体的重组细胞系。还描述了具有商业意义的本发明的相关方面。包括使用细胞系作为发现调节EAA受体刺激的化合物的工具。

6. 发明授权

US5432080A DNA encoding variants of human corticosteroid binding globulin 失效
标题翻译：编码人类皮质类固醇结合球蛋白变体的DNA
公开(公告)号：US5432080A
公开(公告)日：1995-07-11
申请号：US994423
申请日：1992-12-16
申请人： Geoffrey L. Hammond , George V. Avvakumov
发明人： Geoffrey L. Hammond , George V. Avvakumov
IPC分类号： A61K38/00 , C07K14/47 , C12N5/10 , C12N15/00
CPC分类号： C07K14/4717 , A61K38/00
摘要： A novel steroid-binding variant of human corticosteroid binding globulin in which one or more of the glycosylation sites, other than the glycosylation site at amino acid position 238, has been functionally disrupted is complexed with an anti-inflammatory ligand in the treatment of inflammation in mammals.
摘要翻译：人类皮质类固醇结合球蛋白的新型类固醇结合变体，其中在氨基酸位置238处的除糖基化位点之外的一个或多个糖基化位点已经被功能性地破坏，其与抗炎配体在治疗炎症中是复合的哺乳动物。

7. 发明授权

US4918011A Enzymatic preparation of 3',4'-anhydrovinblastine 失效
标题翻译： 3'，4'-脱氢长春花碱的酶制剂
公开(公告)号：US4918011A
公开(公告)日：1990-04-17
申请号：US893018
申请日：1986-08-04
申请人： Anne E. Goodbody , Endo Tsuyoshi , John Vukovic , Masanaru Misawa
发明人： Anne E. Goodbody , Endo Tsuyoshi , John Vukovic , Masanaru Misawa
IPC分类号： C07D519/04 , C12N9/08 , C12P17/18
CPC分类号： C07D519/04 , C12P17/182
摘要： 3',4'-anhydrovinblastine, a precursor of the anti-tumor alkaloids vincristine and vinblastine, is prepared by the enzymatic coupling of catharanthine and vindoline using an iron-containing compound such as peroxidase optionally in the presence of a peroxide. Substantially enhanced yields are obtained.
摘要翻译： 3'，4'-脱氢长春花碱，抗肿瘤生物碱长春新碱和长春花碱的前体，通过使用含铁化合物如过氧化物酶任选在过氧化物存在下酶联偶联衣原体和维林达诺来制备。获得了显着提高的产率。

8. 发明授权

US2882516A Record sensing system 失效
标题翻译：记录传感系统
公开(公告)号：US2882516A
公开(公告)日：1959-04-14
申请号：US31746752
申请日：1952-10-29
申请人： FREDERIC W OLMSTEAD , HANS W TRECHSEL , DERYCK A GERARD , JOHN J KOJIS , NORMAN S PARKER , MALCOLM S BRADWAY , NORTHERN TRUST CO
发明人： DE NEERGAARD LEIF ERIC
IPC分类号： B23Q35/12
CPC分类号： B23Q35/12

9. 发明授权

US6057126A Mammalian EDG-5 receptor homologs 失效
标题翻译：哺乳动物EDG-5受体同系物
公开(公告)号：US6057126A
公开(公告)日：2000-05-02
申请号：US997803
申请日：1997-12-24
申请人： Donald G. Munroe , Ashwani K. Gupta , Tejal B. Vyas , Jerold J. M. Chun
发明人： Donald G. Munroe , Ashwani K. Gupta , Tejal B. Vyas , Jerold J. M. Chun
IPC分类号： G01N33/50 , C07K14/705 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/12 , C12Q1/02 , C12Q1/68 , G01N33/15 , G01N33/68 , C07H21/04 , C12N15/85
CPC分类号： C07K14/705 , A01K2217/05 , A01K2217/075 , C07K2319/00
摘要： The present invention describes a nucleic acid sequence and an amino acid sequence for novel mammalian, including human, EDG-5 receptor homologs.
摘要翻译：本发明描述了新型哺乳动物，包括人EDG-5受体同系物的核酸序列和氨基酸序列。

10. 发明授权

US5998462A 5-alkyl indole compounds 失效
标题翻译： 5-烷基吲哚化合物
公开(公告)号：US5998462A
公开(公告)日：1999-12-07
申请号：US767323
申请日：1996-12-16
申请人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
发明人： Abdelmalik Slassi , Louise Edwards , Qingchang Meng , Sumanas Rakhit
IPC分类号： C07D209/16 , C07D403/06 , A61K31/40
CPC分类号： C07D403/06 , C07D209/16
摘要： Described herein are compounds selective for the 5-HT.sub.1D -like receptor, which have the general formula: ##STR1## wherein: R.sup.1 is linear or branched loweralkyl;R.sup.2 is selected from a group of Formula II, III, IV and V: ##STR2## R.sup.3 is selected from H and loweralkyl; R.sup.4 is selected from H and loweralkyl;One of R.sup.5 and R.sup.6 is H and the other is independently selected from H, loweralkoxy, loweralkyl and hydroxy; andn is 1-3;or a salt, solvate or hydrate thereof.Also described is the use of these compounds as pharmaceuticals to treat indications where stimulation of the 5-HT.sub.1D -like receptor is implicated, such as migraine.
摘要翻译：本文描述的是对具有以下通式的5-HT1D样受体有选择性的化合物：其中：R1是直链或支链的低级烷基; R2选自式II，III，IV和V的基团：R3选自H和低级烷基; R4选自H和低级烷基; R5和R6之一是H，另一个独立地选自H，低级烷氧基，低级烷基和羟基; n为1-3; 或其盐，溶剂合物或水合物。还描述了这些化合物作为药物用于治疗涉及5-HT1D样受体的刺激的指征，例如偏头痛。

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