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公开(公告)号：US5605932A
公开(公告)日：1997-02-25
申请号：US582156
申请日：1996-01-02
IPC分类号： C07C271/24 , C07C323/32 , A61K31/185
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##
摘要翻译： 式1的化合物结合阿片受体：其结合阿片受体：
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公开(公告)号：US5481020A
公开(公告)日：1996-01-02
申请号：US366830
申请日：1994-12-30
IPC分类号： C07C271/24 , C07C323/32 , C07C271/10
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind opioid receptors: which binds to the opioid receptor: ##STR1##
摘要翻译： 式1的化合物结合阿片受体：其结合阿片受体：
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公开(公告)号：US5536868A
公开(公告)日：1996-07-16
申请号：US391132
申请日：1995-02-21
IPC分类号： C07C271/24 , C07C323/32 , C07C205/05 , C07C229/04 , C07C271/10
CPC分类号： C07C271/24 , C07C323/32 , C07C2102/42
摘要： Compounds of Formula 1 bind to the opioid receptors: ##STR1## wherein R.sub.1 is a group of the formula ##STR2## where W is --(CH.sub.2).sub.a -- (where a is 0, 1, or 2), --O--, --NH--, --S--, --SO--, or --SO.sub.2 --, and Ar is phenyl, phenyl-alkyl, phenyl substituted with 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups, and n is 0, 1, 2, 3, or 4;R.sub.2 and R.sub.3 are each independently H, lower alkyl, or ##STR3## where X is H, OH, lower alkyl, or lower alkoxy, and p is 0, 1, 2, or 3; R.sub.4 is ##STR4## where m is 0, 1, 2, or 3, and R is 1-3 halo, nitro, lower alkyl, hydroxy, amino, alkylamino, dialkylamino, and/or hydroxy-lower alkyl groups;R.sub.5 is cycloalkyl, bicycloalkyl, or tricycloalkyl; andR.sub.6, R.sub.7, R.sub.8, and R.sub.9 are each independently H or lower alkyl.
摘要翻译： 式1的化合物与阿片受体结合：其中R 1是下式的基团：其中W是 - （CH 2）a - （其中a是0,1或2），-O-， - NH - ， - S - ， - SO-或-SO 2 - ，Ar是苯基，苯基 - 烷基，被1-3个卤素，硝基，低级烷基，羟基，氨基，烷基氨基，二烷基氨基和/或羟基 - 低级烷基，n为0,1,2,3或4; R 2和R 3各自独立地为H，低级烷基或者其中X为H，OH，低级烷基或低级烷氧基，p为0,1,2或3; R4是
，其中m是0,1,2或3，R是1-3个卤素，硝基，低级烷基，羟基，氨基，烷基氨基，二烷基氨基和/或羟基 - 低级烷基; R5是环烷基，双环烷基或三环烷基; 并且R 6，R 7，R 8和R 9各自独立地为H或低级烷基。 -
公开(公告)号：US5877278A
公开(公告)日：1999-03-02
申请号：US487282
申请日：1995-06-07
申请人： Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
发明人： Ronald N. Zuckermann , Dane A. Goff , Simon Ng , Kerry Spear , Barbara O. Scott , Aaron C. Sigmund , Richard A. Goldsmith , Charles K. Marlowe , Yazhong Pei , Lutz Richter , Reyna Simon
IPC分类号： C07D243/14 , A61K38/00 , C07B61/00 , C07D217/24 , C07D221/12 , C07D487/04 , C07K1/04 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/10
CPC分类号： C40B40/04 , C07K1/04 , C07K1/047 , C07K14/001 , C07K7/06 , C07K7/08 , C08G69/10 , C40B50/14 , A61K38/00 , B01J2219/00497 , B01J2219/00596 , B01J2219/0072 , C07B2200/11 , C40B40/10
摘要： A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by --NH.sub.2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound .alpha.-haloacetamide) with a sufficient amount of a second sub-monomer comprising an --NH.sub.2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
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公开(公告)号：US5536853A
公开(公告)日：1996-07-16
申请号：US225758
申请日：1994-04-11
申请人： David C. Spellmeyer , Walter H. Moos , Eric J. Martin , Ronald N. Zuckermann , Gregory Stauber , Kevin R. Shoemaker , Dane Goff
发明人： David C. Spellmeyer , Walter H. Moos , Eric J. Martin , Ronald N. Zuckermann , Gregory Stauber , Kevin R. Shoemaker , Dane Goff
IPC分类号： A61K38/00 , C07K5/083 , C07D317/50 , C07D317/54 , C07D317/58 , C07D319/14
CPC分类号： C07K5/0806 , A61K38/00
摘要： Compounds of Formula 1 bind opioid receptors: ##STR1## wherein X and Y are each independently ##STR2##
摘要翻译： 式1的化合物结合阿片受体：其中X和Y各自独立地为“IMAGE”
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公开(公告)号：US5447916A
公开(公告)日：1995-09-05
申请号：US99908
申请日：1993-07-30
IPC分类号： C07C237/22 , C07K5/02 , C07K5/023 , C07K5/083 , G01N33/566 , G01N33/74 , G01N33/94 , A61K38/05 , A61K38/06
CPC分类号： C07C237/22 , C07K5/0202 , C07K5/0806 , G01N33/566 , G01N33/74 , G01N33/9433 , Y10S514/821 , Y10S514/824 , Y10S514/913
摘要： Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.
摘要翻译： 下式的化合物：
可用于治疗由α1-肾上腺素能受体调节的病症。 -
公开(公告)号：US5480871A
公开(公告)日：1996-01-02
申请号：US440108
申请日：1995-05-12
IPC分类号： C07C237/22 , C07K5/02 , C07K5/023 , C07K5/083 , G01N33/566 , G01N33/74 , G01N33/94 , A61K38/05 , A61K38/06
CPC分类号： C07C237/22 , C07K5/0202 , C07K5/0806 , G01N33/566 , G01N33/74 , G01N33/9433 , Y10S514/821 , Y10S514/824 , Y10S514/913
摘要： Compounds of the formula: ##STR1## are useful for treating conditions modulated by .alpha..sub.1 -adrenergic receptors.
摘要翻译： 下式的化合物：
可用于治疗由α1-肾上腺素能受体调节的病症。 -
公开(公告)号：US09073977B2
公开(公告)日：2015-07-07
申请号：US13022548
申请日：2011-02-07
申请人： Ronald N. Zuckermann , Tammy K. Chu , Ki Tae Nam
发明人： Ronald N. Zuckermann , Tammy K. Chu , Ki Tae Nam
CPC分类号： C07K14/001 , C07K1/13 , C07K7/06 , C07K7/08
摘要： The present invention provides for novel peptoid oligomers that are capable of self-assembling into two-dimensional sheet structures. The peptoid oligomers can have alternately hydrophilic or polar side-chains and hydrophobic or apolar side-chains. The peptoid oligomers, and the two-dimensional sheet structures, can be applied to biological applications where the peptoid plays a role as a biological scaffold or building block. Also, the two-dimensional sheet structures of the present invention can be used as two-dimensional nanostructures in device applications.
摘要翻译： 本发明提供了能够自组装成二维片状结构的新型拟肽低聚物。 拟肽低聚物可以具有交替的亲水或极性侧链和疏水或非极性侧链。 拟肽低聚物和二维片状结构可以应用于生物应用，其中拟肽作为生物支架或构建块起作用。 此外，本发明的二维片状结构可以用作器件应用中的二维纳米结构。
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公开(公告)号：US08952127B2
公开(公告)日：2015-02-10
申请号：US13153141
申请日：2011-06-03
CPC分类号： C01F11/183 , C01P2004/03 , C01P2004/30 , C01P2004/32 , C01P2004/39 , C01P2004/61 , C08G69/10 , Y10S930/03
摘要： The present invention provides for a bio-mimetic polymer capable of catalyzing CO2 into a carbonate.
摘要翻译： 本发明提供了能够将CO 2催化成碳酸盐的生物模拟聚合物。
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公开(公告)号：US20120258918A1
公开(公告)日：2012-10-11
申请号：US13385310
申请日：2012-02-13
CPC分类号： C07K14/785 , A61K38/1709 , Y10S930/32 , A61K31/74 , A61K31/685 , A61K31/66 , A61K31/20 , A61K31/195 , A61K2300/00
摘要： The present invention provides spreading agents based on sequence-specific oligomers comprising a peptoid, a peptide-peptoid chimera, a retropeptoid or a retro(peptoid-peptide) chimera, and methods for using the same, including for the treatment of respiratory distress of the lungs. The spreading agents are sequence-specific oligomers, including retrosequence-specific oligomers, based on a peptide backbone, that are designed as analogs of surfactant protein-B or surfactant protein-C.
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