Hindered linking agents and methods

Details Hindered linking agents and methods Hindered linking agents and methods

C - Chemistry, Metallurgy

07

D

167/129, 260/328

C07D 333/36 (2006.01) A61K 47/48 (2006.01) C07D 333/50 (2006.01) C07D 333/66 (2006.01) C07D 409/04 (2006.01)

Patent

CA 2006629

HINDERED LINKING AGENTS AND METHODS ABSTRACT OF THE DISCLOSURE Novel compounds and methods for the formation of disulfide linkages are presented. The novel compounds employed are substituted 2-iminothiolane hydrohalide linking agents of the following formula (I): Image wherein, (I) x is halogen; R1 is COOR5; halogen; nitro; unsubstituted or halogenated C1-8 alkyl; unsubstituted or halogenated C1- 8alkoxy; unsubstituted or halogenated C2-8alkynyl; unsubstituted C3-8cycloalkyl; unsubstituted aryl; aryl substituted with 1 to 3 substituents selected from halogen, amino, unsubstituted or halogenated C1-8alkyl, or unsubstituted or halogenated C1-8alkoxy; unsubstituted heterocycle; or heterocycle substituted with 1 to 3 substitutents selected from amino, halogen, unsubstituted or halogenated C1- 8alkyl, or unsubstituted or halogenated C1-8alkoxy; each of R2, R3, and R4 is independently hydrogen or selected from the values of R1; or R1 and R2 together form a C2-5alkylene bridge, unsubstituted or substituted with one to five C1-4alkyl groups; or R1 and R2 together with R3 form a C1-5alkylene bridge, unsubstituted or substituted with one to five C1- 4alkyl groups; and 41 R5 is hydrogen or C1-8alkyl. Also included in the invention are methods for covalently linking two species, which methods comprise reacting one or both of the two species with a crosslinking agent of the above formula (I) and mixing the two species together. The resulting conjugated species containing the linking group are also included in the invention. Further included in the invention is the use of a quenching agent which allows direct measurement of the reaction of 2-iminothiolanes with nucleophilic groups. WMS\JHM\08586\072-l.APP

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