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Patent
PolyTherics | Date: 2017-04-07

The invention provides compound of the general formula: in which each X independently represents a polymer chain; n represents an integer greater than 1; Q represents a linker; Y represents an amide group; and Z represents either CH.(CH_(2)L)_(2 )or C(CH_(2)L)(CH_(2)), in which each L independently represents a leaving group. The compounds are useful reagents for the conjugation of polymers to proteins, the resulting conjugates being novel and also forming part of the invention.


Patent
PolyTherics | Date: 2017-04-26

A conjugate of the general formula: (((D_(q)-Lk^(1))_(m)-P)_(p)-Lk^(2)-Lk^(3))_(n)-Ab(I)in which D represents a drug moiety;q represents an integer from 2 to 10;Lk^(1) represents a linker;m represents an integer from 1 to 10;P represents a z-valent group -P^(1)-NH- where z is from 2 to 11 and P^(1) is a polyethylene glycol group;p represents an integer from 1 to 10;Lk^(2) represents a bond or a y-valent linker where y is from 2 to 11 and which consists of from 1 to 9 aspartate and/or glutamate residues;Lk^(3) represents a linker of the general formula: -CO-Ph-X-Y-(II)in which Ph is an optionally substituted phenyl group; X represents a CO group or a CH.OH group; and Y represents a group of formula:_(1-4)alkylene or alkenylene group;Ab represents a binding protein or peptide capable of binding to a binding partner on a target, said binding protein being bonded to Lk^(3) via two sulfur atoms derived from a disulfide bond in the binding protein or peptide; andn represents an integer from 1 to s where s is the number of disulfide bonds present in the binding protein or peptide prior to conjugation to Lk^(3);the meanings of m, n, p, q, y and z being chosen such that the conjugate contains from 1 to 10 D groups.


The invention relates to novel conjugating reagents capable of reaction with at least one nucleophile present in a peptide or protein, which contain at least one leaving group which is lost on reaction with said nucleophile, in which the leaving group includes a portion -(CH2CH2O)n- in which n is a number of six or more; and novel processes for the preparation of conjugates containing peptides or proteins made using such reagents.


Patent
PolyTherics | Date: 2013-10-11

Specific conjugates containing auristatins and a binding protein or peptide, and processes for making them, are described. The conjugates use specific linker technology which gives advantages over known antibody-drug conjugates. Also described are specific conjugates of drugs and a binding protein or peptide in which more than one copy of the drug is present.


Patent
PolyTherics | Date: 2016-04-04

The present invention concerns a conjugate of a domain I 2GP1 polypeptide with a water-soluble polymer, wherein the polymer is bound via two cysteine residues derived from a disulfide bridge in the domain I 2GP1 polypeptide.


Patent
PolyTherics | Date: 2014-07-28

Novel biologically active compounds of the general formula (I) in which one of X and X represents a polymer, and the other represents a hydrogen atom; each Q independently represents a linking group; W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety; or, if X represents a polymer, X-Q-W together may represent an electron withdrawing group; and in addition, if X represents a polymer, X and electron withdrawing group W together with the interjacent atoms may form a ring; each of Z^(1 )and Z^(2 )independently represents a group derived from a biological molecule, each of which is linked to A and B via an amine group; or Z^(1 )and Z^(2 )together represent a single group derived from a biological molecule which is linked to A and B via two amine groups; A is a C_(1-5 )alkylene or alkenylene chain; and B is a bond or a C_(1-4 )alkylene or alkenylene chain; are formed by conjugating a suitable polymer to a suitable biologically active molecule via amine groups in said molecule, preferably via a disulphide bridge.


A compound of the general formula X-[Q-W(CHCH)_(n)(CH_(2))_(2)-L]_(m )(I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.


Patent
PolyTherics | Date: 2015-03-16

Novel compounds of the general formula: in which X represents a polymer, Q represents a linking group;W represents an electron-withdrawing moiety or a moiety preparable by reduction of an electron-withdrawing moiety;each of R^(1 )and R^(2 )independently represents a hydrogen atom or a C_(1-4)alkyl group; andeither Z^(1 )represents a protein or a peptide linked to CR^(2 )via a nucleophilic moiety, and Z^(2 )represents a molecule linked to CR^(2 )via a nucleophilic moiety, or Z^(1 )and Z^(2 )together represent a single group derived from a protein or peptide linked to CR^(2 )via two nucleophilic moieties.


Patent
PolyTherics | Date: 2013-10-11

Specific conjugates containing maytansines and a binding protein or peptide, and processes for making them, are described. The conjugates use specific linker technology which gives advantages over known antibody-drug conjugates.


A compound of the general formula X[NRCOArCO(CHCH)_(n)(CH_(2))_(2)-L]_(m )(I) in which X represents a polymer; R represents a hydrogen atom or an alkyl, aryl or alkyl-aryl group; Ar represents an unsubstituted or substituted heteroaryl or aryl group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represents an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.

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