Janice S Kerr

20020115612, Aug 22, 2002

Feb 8, 2002

10/071577

Ronald Zuckermann - El Cerrito CA, US
Janice Kerr - Oakland CA, US
Stephen Kent - La Jolla CA, US

Chiron Corporation

A61K038/16
C07K014/00

514/012000, 530/350000

An automated solid-phase method for the synthesis of poly (N-substituted glycines) (referred to herein as poly NSGs) taught here can be used to obtain 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 resin-bound secondary amine with an agent such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the halogen (as a resin-bound -haloacetamide) with an excess of primary amine. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology, as presented here, makes these polymers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of polymers not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.

58310053, Nov 3, 1998

May 16, 1995

8/441826

Ronald N. Zuckerman - Berkeley CA
Janice M. Kerr - Irvine CA
Stephen B. H. Kent - La Jolla CA
Walter H. Moos - Oakland CA
Reyna J. Simon - Felton CA
Dane A. Goff - Redwood City CA

Chiron Corporation - Emeryville CA

C07K 104

530333

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 is 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 resin-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.

50808842, Jan 14, 1992

Feb 22, 1991

7/660403

William J. McBride - Oakland CA
Ronald M. Baldwin - Concord CA
Janice M. Kerr - San Jose CA
Lisa M. Schultze - Oakland CA
Nilda Salazar - Hercules CA
James M. Chinitz - Oakland CA

Medi-Physics, Inc. - Arlington Heights IL

A61K 4902
C07F 1300

424 11

An agent for imaging organs using a radioactive complex of a radioactive metal with a benzene ring having two 2-mercapto-2-methylpropylamino substituents where one of these mercapto substituents is substituted with a hydrocarbyl group.

50269135, Jun 25, 1991

Aug 30, 1990

7/576163

William J. McBride - Oakland CA
Ronald M. Baldwin - Concord CA
Janice M. Kerr - San Jose CA
Lisa M. Schultze - Oakland CA
Nilda Salazar - Hercules CA

Medi-Physics, Inc. - Arlington Heights IL

C07C32100
C07C32300
C07C38100

564440

An agent for imaging organs using a radioactive complex of a radioactive metal with a benzene ring having two 2-mercapto-2-methylpropylamino substitutents where one of these mercapto substituents is substituted with a hydrocarbyl group.

59773014, Nov 2, 1999

Jun 7, 1995

8/485106

Ronald N. Zuckerman - Berkeley CA
Janice M. Kerr - Irvine CA
Stephen B. H. Kent - La Jolla CA
Walter H. Moos - Oakland CA
Reyna J. Simon - Telton CA
Dane A. Goff - Redwood City CA

Chiron Corporation - Emeryville CA

C07K 104

530334

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 resin-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.