Barbara J Scott

US Patent:

59587920, Sep 28, 1999

Filed:

Jun 7, 1995

Appl. No.:

8/485006

Inventors:

Manoi C. Desai - Pleasant Hill CA
John M. Nuss - Danville CA
Kerry L. Spear - Oakland CA
Rajinder Singh - Walnut Creek CA
Paul A. Renhowe - Danville CA
Edward G. Brown - Lafayette CA
Lutz Richter - Pacifica CA
Barbara O. Scott - San Antonio TX

Assignee:

Chiron Corporation - Emeryville CA

International Classification:

G01N 33543
G01N 33545
G01N 3353
A61K 3806

US Classification:

436518

Abstract:

The invention relates to libraries of cyclic organic compounds and method of producing and assaying such libraries. According to the invention, each cyclic organic compound is constructed from a starting material in the form of a solid surface derivatized with a starting resin. Compounds are reacted with the resin to add or to form a cyclic group. The reactions are preferable carried out using a split resin procedure so that different compounds can be reacted with a plurality of subamounts so as to increase the size of the library. For example, compounds are reacted with a solid support bound starting resin to obtain a compound which includes an aldehyde functional group wherein the aldehyde compound or compounds reacted with it have substituents which are varied such that a mixture of products is obtained. The invention further relates to methods of producing combinatorial libraries of cyclic organic compounds from substrate bound compounds by cleaving the compounds from the support after synthesizing is completed and to assaying libraries of such compounds.

US Patent:

58772782, Mar 2, 1999

Filed:

Jun 7, 1995

Appl. No.:

8/487282

Inventors:

Ronald N. Zuckermann - Berkeley CA
Dane A. Goff - Redwood City CA
Simon Ng - Walnut Creek CA
Kerry Spear - Oakland CA
Barbara O. Scott - San Antonio TX
Aaron C. Sigmund - El Sobrante CA
Richard A. Goldsmith - Daly City CA
Charles K. Marlowe - San Carlos CA
Yazhong Pei - Alisa Viejo CA
Lutz Richter - Montera CA
Reyna Simon - Felton CA

Assignee:

Chiron Corporation - Emeryville CA

International Classification:

C07K 104

US Classification:

530334

Abstract:

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.