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1. WO1996040201 - COMBINATORIAL LIBRARIES OF SUBSTRATE-BOUND CYCLIC ORGANIC COMPOUNDS

Publication Number WO/1996/040201
Publication Date 19.12.1996
International Application No. PCT/US1996/007684
International Filing Date 23.05.1996
Chapter 2 Demand Filed 05.12.1996
IPC
C07B 61/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61Other general methods
C07K 1/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General processes for the preparation of peptides
04on carriers
CPC
C07B 2200/11
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
11Compounds covalently bound to a solid support
C07C 231/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
12by reactions not involving the formation of carboxamide groups
C07K 1/047
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
KPEPTIDES
1General methods for the preparation of peptides ; , i.e. processes for the organic chemical preparation of peptides or proteins of any length
04on carriers
047Simultaneous synthesis of different peptide species; Peptide libraries
C40B 40/04
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
40Libraries per se, e.g. arrays, mixtures
04Libraries containing only organic compounds
C40B 50/14
CCHEMISTRY; METALLURGY
40COMBINATORIAL TECHNOLOGY
BCOMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES, IN SILICO LIBRARIES
50Methods of creating libraries, e.g. combinatorial synthesis
14Solid phase synthesis, i.e. wherein one or more library building blocks are bound to a solid support during library creation; Particular methods of cleavage from the solid support
Applicants
  • CHIRON CORPORATION [US]/[US]
Inventors
  • DESAI, Manoi, C.
  • NUSS, John, M.
  • SPEAR, Kerry, L.
  • SINGH, Rajinder
  • RENHOWE, Paul, A.
  • BROWN, Edward, G.
  • RICHTER, Lutz
  • SCOTT, Barbara, O.
Agents
  • BOZICEVIC, Karl
Priority Data
08/485,00607.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) COMBINATORIAL LIBRARIES OF SUBSTRATE-BOUND CYCLIC ORGANIC COMPOUNDS
(FR) BANQUES COMBINATOIRES DE COMPOSES ORGANIQUES CYCLIQUES LIES A UN SUBSTRAT
Abstract
(EN)
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 preferably 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.
(FR)
L'invention concerne des banques de composés organiques cycliques et un procédé de production et de dosage de ces banques. Selon l'invention, chaque composé organique cyclique est construit à partir d'un produit de départ sous la forme d'une surface solide dérivée à l'aide d'une résine de départ. On fait réagir lesdits composés avec la résine pour ajouter ou former un groupe cyclique. Ces réactions sont de préférence réalisées à l'aide d'un traitement séparé à la résine, de sorte que l'on puisse faire réagir différents composés avec une pluralité de sous-quantités afin d'accroître la taille de la banque. Par exemple, on fait réagir des composés avec une résine de départ liée à un support solide pour obtenir un composé incluant un groupe fonctionnel aldéhyde dans lequel le ou les composés aldéhydes que l'on a fait réagir possèdent des substituants que l'on fait varier de façon à obtenir un mélange de produits. L'invention concerne également des procédés pour produire des banques combinatoires de composés organiques cycliques à partir de composés liés au substrat, consistant à détacher les composés du support après achèvement de la synthèse, et pour effectuer un dosage desdites banques de composés.
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