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41. 发明授权

US5646120A Peptide-based inhibitors of HIV replication 失效
标题翻译：基于肽的HIV复制抑制剂
公开(公告)号：US5646120A
公开(公告)日：1997-07-08
申请号：US357056
申请日：1994-12-14
申请人： Martin Sumner-Smith , Richard W. Barnett , Lorne S. Reid , Nahum Sonenberg
发明人： Martin Sumner-Smith , Richard W. Barnett , Lorne S. Reid , Nahum Sonenberg
IPC分类号： A61K38/00 , A61K38/08 , C07K7/06 , C07K7/08 , C07K5/00
CPC分类号： C07K7/06 , A61K38/08 , C07K7/08 , Y02P20/55
摘要： Described herein are oligopeptides useful to inhibit replication in virally infected individuals. In a preferred embodiment of the invention, the oligopeptide is a D-arginine nonamer having N- and C-terminal protecting groups, which, at a 5 uM concentration, exhibits greater than 95% inhibition of HIV replication, in a standard assay.
摘要翻译：本文描述的是可用于抑制病毒感染个体复制的寡肽。在本发明的优选实施方案中，寡肽是具有N-和C-末端保护基团的D-精氨酸非对映体，其在5uM浓度下在标准测定中显示出大于95％的HIV复制抑制。

42. 发明授权

US5643785A Polynucleotides encoding AMPA-binding human GluR4 receptors 失效
标题翻译：编码AMPA结合人类GluR4受体的多核苷酸
公开(公告)号：US5643785A
公开(公告)日：1997-07-01
申请号：US259164
申请日：1994-06-13
申请人： Rajender Kamboj , Candace E. Elliott , Stephen L. Nutt
发明人： Rajender Kamboj , Candace E. Elliott , Stephen L. Nutt
IPC分类号： A61K38/00 , A61K48/00 , C07K14/00 , C07K14/705 , C07K16/00 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12P21/08 , G01N33/53 , G01N33/566 , C07H21/04 , C12N15/63 , C12N15/85
CPC分类号： C07K14/70571 , A61K48/00
摘要： Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR4B receptor. The receptor is characterized structurally and the construction and use of cell lines expressing the receptor is disclosed.
摘要翻译：本文描述了编码AMPA型人CNS受体的分离的多核苷酸，其命名为人GluR4B受体。该受体的结构特征在于，公开了表达受体的细胞系的构建和用途。

43. 发明授权

US5627194A Anti-viral guanidino-substituted compounds 失效
标题翻译：抗病毒胍基取代的化合物
公开(公告)号：US5627194A
公开(公告)日：1997-05-06
申请号：US322492
申请日：1994-10-14
申请人： Sumanas Rakhit , Abdelmalik Slassi
发明人： Sumanas Rakhit , Abdelmalik Slassi
IPC分类号： C07C279/16 , C07D211/06 , C07H15/04 , C07H15/08 , A61K31/35 , A61K31/17 , A61K31/38 , A61K31/445
CPC分类号： C07H15/04 , C07C279/16 , C07D211/06 , C07H15/08
摘要： Novel guanidino-substituted compounds are described having the following general formula (I): ##STR1## in which X may be carbon, oxygen, nitrogen or sulfur; R.sub.1 may be H, OH, linear or branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine, lower alkyl-thio, hydroxy substituted lower alkoxy, lower alkoxy-alkoxy substituted lower alkoxy, hydroxy substituted lower alkyl-amine, alkoxy substituted lower alkyl-amine and terminally guanidino-substituted linear of branched lower alkyl, lower alkoxy, lower (alkyl-substituted alkoxy), lower alkyl-amine or lower alkyl-thio; and R.sub.2 and R.sub.3 are independently one of linear or branched lower alkyl, alkoxy, alkyl-substituted alkoxy and alkylamine.These compounds have been found to inhibit effectively herpesvirus replication. Particularly preferred compounds in accordance with formula (I) for this purpose are guanidino-substituted sugar derivatives.
摘要翻译：描述了新的胍基取代的化合物，其具有以下通式（I）：其中X可以是碳，氧，氮或硫; R 1可以是H，OH，直链或支链的低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺，低级烷基 - 硫代，羟基取代的低级烷氧基，低级烷氧基 - 烷氧基取代的低级烷氧基，烷基胺，烷氧基取代的低级烷基胺和末端胍基取代的直链的支链低级烷基，低级烷氧基，低级（烷基取代的烷氧基），低级烷基 - 胺或低级烷基 - 硫代; R2和R3独立地为直链或支链的低级烷基，烷氧基，烷基取代的烷氧基和烷基胺之一。已经发现这些化合物有效地抑制疱疹病毒复制。特别优选的根据式（I）的化合物是胍基取代的糖衍生物。

44. 发明授权

US5614406A Kainate-binding human CNS receptors of the EAA2 family 失效
标题翻译： EAA家族的Kainate结合人CNS受体
公开(公告)号：US5614406A
公开(公告)日：1997-03-25
申请号：US203676
申请日：1994-02-28
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 , C12N1/21 , C12N15/79
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 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。

45. 发明授权

US5602120A Benzyl-substituted compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的苄基取代的化合物
公开(公告)号：US5602120A
公开(公告)日：1997-02-11
申请号：US354766
申请日：1994-12-12
申请人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
发明人： Jian-Min Fu , Ashok Tehim , Robert A. Kirby
IPC分类号： C07D267/20 , A61K31/55 , C07D413/04 , C07D417/04
CPC分类号： C07D267/20
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--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; 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-; Y选自CH和N; Z是氰基，R 1表示C 1-4烷基; m为0,1,2或3; n为0,1或2; q为1或2; 且D为5,6或7元饱和或不饱和的均聚或杂环; 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。

46. 发明授权

US5576314A Bicyclic nonane and decane compounds having dopamine receptor affinity 失效
标题翻译：具有多巴胺受体亲和力的双环壬烷和癸烷化合物
公开(公告)号：US5576314A
公开(公告)日：1996-11-19
申请号：US354906
申请日：1994-12-12
申请人： Patricia L. Power , Sumanas Rakhit
发明人： Patricia L. Power , Sumanas Rakhit
IPC分类号： C07D471/04 , C07D487/04 , C07D513/00 , A61K31/55 , C07D487/00 , C07D498/00
CPC分类号： C07D471/04 , C07D487/04
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--;n is 1 or 2;R.sub.1 is selected from H and an amino acid side chain;R.sub.2 is selected from H, OH, C.sub.1-9 alkyl, C.sub.1-9 alkoxy, and benzyloxy; andR.sub.3 is selected from H, OH, halo, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, phenoxy, benzyloxy, .dbd.O, .dbd.S, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylthio, amino, and aminocarbonyl;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，SO 2和SO ; X2 - - - 选自N =，CH 2 - ，CH =，C（O） - ，O-和S-; n为1或2; R1选自H和氨基酸侧链; R2选自H，OH，C1-9烷基，C1-9烷氧基和苄氧基; 并且R 3选自H，OH，卤素，氰基，C 1-4烷基，C 1-4烷氧基，苯氧基，苄氧基，= O，= S，C 1-4烷基磺酰基，C 1-4烷基磺酰基，C 1-4烷硫基，氨基和氨基羰基; 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。

47. 发明授权

US5344819A Pharmaceutical compositions for use in treating inflammation 失效
标题翻译：用于治疗炎症的药物组合物
公开(公告)号：US5344819A
公开(公告)日：1994-09-06
申请号：US829954
申请日：1992-02-03
申请人： Geoffrey L. Hammond
发明人： Geoffrey L. Hammond
IPC分类号： A61K38/00 , A61K31/57 , A61K35/74 , A61P29/00 , C07K14/575 , A61K37/04
CPC分类号： C07K14/575 , A61K38/00
摘要： Inflammation in mammals is treated by administering anti-inflammatory agent complexed with corticosteroid binding globulin (CBG) that is produced by recombinant DNA-based techniques.
摘要翻译：通过施用与通过重组DNA技术产生的皮质类固醇结合球蛋白（CBG）复合的抗炎剂来治疗哺乳动物的炎症。

48. 发明授权

US4997814A Pharmaceutical compositions and use thereof in treating inflammation 失效
标题翻译：药物组合物及其在治疗炎症中的用途
公开(公告)号：US4997814A
公开(公告)日：1991-03-05
申请号：US204356
申请日：1988-06-09
申请人： Geoffrey L. Hammond
发明人： Geoffrey L. Hammond
IPC分类号： A61K38/00 , A61K31/57 , A61K35/74 , A61P29/00 , C07K14/575
CPC分类号： C07K14/575 , A61K38/00
摘要： Inflammation in mammals is treated by administering anti-inflammatory agent complexed with corticosteroid binding globulin (CBG).
摘要翻译：通过施用与皮质类固醇结合球蛋白（CBG）复合的抗炎药来治疗哺乳动物的炎症。

49. 发明授权

US2361451A Variable density sound recording method and system 失效
标题翻译：可变密度录音方法和系统
公开(公告)号：US2361451A
公开(公告)日：1944-10-31
申请号：US47558343
申请日：1943-02-11
申请人： RCA CORP
发明人： BLANEY ARTHUR C
IPC分类号： G11B7/003
CPC分类号： G11B7/0032

50. 发明申请

US20040167158A1 Heterocyclic compounds for the treatment of migraine 审中-公开
公开(公告)号：US20040167158A1
公开(公告)日：2004-08-26
申请号：US10784673
申请日：2004-02-24
申请人： NPS ALLELIX BIOPHARMACEUTICALS, INC.
发明人： Louise Edwards , Methvin Isaac , Shawn Maddaford , Abdelmalik Slassi , Tao Xin
IPC分类号： C07D471/02 , A61K031/4745
CPC分类号： C07F7/0814 , C07D209/08 , C07D231/56 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/04 , C07D417/14 , C07D471/04
摘要： Described herein are compounds useful in the treatment of migraine, which have the general formula: 1 wherein: W is a CH group or a N atom; Z is N or C-R4; B and D are selected independently from CH and N, with the proviso that at least one of B and D is CH and with the further proviso that one of B and D can represent N only when W and Z are both other than N; A is a group of Formula II, III or IV, such that group A contains at least 1 N atom; NR7 is either nullNHnull or nullNnull is a single or double bond; X is a N atom, a CH group or a C(OH) group when is a single bond; or, when is a double bond, a C atom; Y is an NH, N-alkyl, N-benzyl or CH2 group; U and V each represent a N atom or a CH group, with the proviso that both cannot be N; a and b are, independently, 0 or 1; c is an integer from 0 to 3; d is an integer from 1 to 3; e is an integer from 1 to 2; f is an integer from 0 to 3; g is an integer from 3 to 6 and h is an integer from 2 to 3; such that the sum of c and d is at least 2 and the sum of e and f is at least 2; R1 is selected from the group consisting of H, alkyl, alkyloxy, alkanoyl, aminoalkylenyl, alkylaminoalkylenyl, a hydroxyalkylenyl group, an alkyloxyalkylenyl group, a cycloalkyl group, a cycloalkylalkylenyl group, a heterocycloalkyl group, a heterocycloalkylalkylenyl group, an aryl group, a heterocycloaryl group, an amido group, a thioamido group, an arylcarbonyl group and an arylsulfonyl group; R2 and R3 are independently selected from the group consisting of H, alkyl, cycloalkyl, alkenyl and optionally-substituted benzyl; or R2 and R3, together with the nitrogen atom to which they are attached, may form a mono- or bi-cyclic group containing up to 10 carbon atoms and which, in addition, may contain a second heteroatom selected from the group consisting of N, S and O, and which may contain one or more substituents selected from the group consisting of alkyl, hydroxy, hydroxymethyl, alkyloxymethyl, amino and substituted amino; R4is selected from the group consisting of H, alkyl and cycloalkyl; CR5 represents a group selected from nullCH2null, CH(OH)null, nullC(O)null, nullCH(alkyl)- and nullCH(alkyloxy)-; R6 is selected from the group consisting of H, alkyl, aryl, halogen, hydroxy, alkyloxy, amino, monoalkylamino and di-substitutedalkylamino; and salts and solvates thereof

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