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71. 发明专利

AT234268T 未知
公开(公告)号：AT234268T
公开(公告)日：2003-03-15
申请号：AT96921278
申请日：1996-06-04
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , GOFF DANE A , NG SIMON , SPEAR KERRY , SCOTT BARBARA O , SIGMUND AARON C , GOLDSMITH RICHARD A , MARLOWE CHARLES K , PEI YAZHONG , RICHTER LUTZ , SIMON REYNA
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 , C07K1/36
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 -NH2, 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 -NH2 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.

72. 发明专利

BR9307092A 未知
公开(公告)号：BR9307092A
公开(公告)日：1999-03-30
申请号：BR9307092
申请日：1993-09-24
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , KERR JANICE M , KENT STEPHEN BRIAN HENRY , MOOS WALTER H , SIMON REYNA J , GOFF DANE A
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10
摘要： Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R ) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method 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 -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 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 the 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.

73. 发明专利

NZ256952A SYNTHESIS OF N-SUBSTITUTED POLYAMIDES AND PHARMACEUTICAL COMPOSITIONS 未知
公开(公告)号：NZ256952A
公开(公告)日：1997-07-27
申请号：NZ25695293
申请日：1993-09-24
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , KERR JANICE M , KENT STEPHEN BRIAN HENRY , MOOS WALTER H , SIMON REYNA J , GOFF DANE A
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10 , C07K1/00 , C07K1/107 , C07K5/00 , C07K7/00 , A61K38/02
摘要： Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R ) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method 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 -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 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 the 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.

74. 发明专利

AU4159396A Synthesis of peptide nucleic acids (pnas) and analogues via submonomer approach 未知
公开(公告)号：AU4159396A
公开(公告)日：1996-06-06
申请号：AU4159396
申请日：1995-11-13
申请人： CHIRON CORP
发明人： RICHTER LUTZ S , ZUCKERMANN RONALD N , HORN THOMAS
IPC分类号： C07D239/54 , A61K38/16 , A61K48/00 , A61P31/12 , A61P35/00 , C07D473/18 , C07D473/34 , C07K14/00

75. 发明专利

HUT72614A SYNTHESIS OF N-SUBSTITUTED OLIGOMERS 未知
公开(公告)号：HUT72614A
公开(公告)日：1996-05-28
申请号：HU9500855
申请日：1993-09-24
申请人： CHIRON CORP
发明人： GOFF DANE A , KENT STEPHEN BRIAN HENRY , KERR JANICE M , MOOS WALTER H , SIMON REYNA J , ZUCKERMANN RONALD N
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10
摘要： Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R ) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method 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 -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 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 the 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.

76. 发明专利

CA2203565A1 SYNTHESIS OF PEPTIDE NUCLEIC ACIDS (PNAS) AND ANALOGUES VIA SUBMONOMER APPROACH 未知
公开(公告)号：CA2203565A1
公开(公告)日：1996-05-23
申请号：CA2203565
申请日：1995-11-13
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , RICHTER LUTZ S , HORN THOMAS
IPC分类号： C07D239/54 , A61K38/16 , A61K48/00 , A61P31/12 , A61P35/00 , C07D473/18 , C07D473/34 , C07K14/00 , C07D473/00 , C07D239/00 , C08G69/00
摘要： Method of synthesizing peptide nucleic acids and such analogues are disclosed.

77. 发明专利

GR3017793T3 METHOD AND APPARATUS FOR BIOPOLYMER SYNTHESIS. 未知
公开(公告)号：GR3017793T3
公开(公告)日：1996-01-31
申请号：GR950402896
申请日：1995-10-18
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , HEUBNER VERENA D , SANTI DANIEL V , SIANI MICHAEL A
IPC分类号： B01J19/00 , C07H21/00 , C07K1/04 , C07K7/08 , C07K14/575 , C07K16/00 , C40B40/06 , C40B40/10 , C40B60/14

78. 发明专利

BG99521A PREPARATION OF N-SUBSTITUTED OLIGOMERS 未知
公开(公告)号：BG99521A
公开(公告)日：1996-01-31
申请号：BG9952195
申请日：1995-03-23
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , KERR JANICE M , KENT STEPHEN B , MOOS WALTER H , SIMON REYNA J , GOFF DANE A
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10
摘要： The N-substituted oligomers such as poly/N-substituted glycines//poly NSGS/ having potentiol therapeutical properties are produced by solid phase method. They can have different substituents in the side chain. Every N-substituted glycine monomer is priduced from two submonomers directly on a solid carrier. Each cycie of adjunction of monomer consists of two stages: (1) acylation of secondary amine bound to the carrier of an acylation agent containing a splitting group capable of nucleophilic substitution by -NH2 such as haloacetic acid, and (2) introduction of the side chain by nucleophilic substitution of the splitting group such as halogen (as -haloacetamide bound to a resin) with sufficient quantity of a second submonomer containing -NH2 group as a primary amine, alkoxyamine, semicarbamide, acylhydrazide, carbazate or other. The desired oligomers are produced by repetition of the two-stage cycle of acylation and substitution. The N-substituted glycine oligomers produced by an automated method for synthesis are suitable for the production and quick screening of peptido-like banks. a new class of peptido-like compounds is ensured which do not occur in nature but can be synthetized and have significant biologicall activity and proteolytic stability.

79. 发明专利

FI951356A 未知
公开(公告)号：FI951356A
公开(公告)日：1995-04-26
申请号：FI951356
申请日：1995-03-22
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , KERR JANICE M , KENT STEPHEN BRIAN HENRY , MOOS WALTER H , SIMON REYNA J , GOFF DANE A
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10 , C07K
摘要： Poly N-substituted Glycines (poly NSGs), wherein the substituents bear purine or pyrimidine bases (R ) every second glycine: In addition, a solid phase method for the synthesis of N-substituted oligomers of more general structures is disclosed.The poly NSGs obtainable by this method 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 -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 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 the 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.

80. 发明专利

NO950682A 未知
公开(公告)号：NO950682A
公开(公告)日：1995-04-18
申请号：NO950682
申请日：1995-02-23
申请人： CHIRON CORP
发明人： ZUCKERMANN RONALD N , KERR JANICE M , KENT STEPHEN BRIAN HENRY , MOOS WALTER H , SIMON REYNA J , GOFF DANE A
IPC分类号： C07C231/12 , A61K31/708 , A61K31/785 , A61K38/00 , A61K38/16 , A61K39/00 , A61K39/395 , A61K48/00 , C07B43/06 , C07C231/02 , C07C237/22 , C07C237/42 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K7/08 , C07K14/00 , C08G69/08 , C08G69/10
CPC分类号： C07K7/06 , A61K38/00 , B01J2219/00497 , B01J2219/00596 , B01J2219/0072 , C07K1/04 , C07K7/08 , C07K14/001 , C08G69/10

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