C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 16/00 (2006.01) A61K 39/44 (2006.01) A61K 47/48 (2006.01) C07C 43/178 (2006.01) C07C 69/708 (2006.01) C07C 217/08 (2006.01) C07C 229/22 (2006.01) C07C 233/18 (2006.01) C07C 233/47 (2006.01) C07C 271/16 (2006.01) C07C 271/22 (2006.01) C07D 207/46 (2006.01) C07D 209/48 (2006.01) C07D 213/71 (2006.01) C07D 401/12 (2006.01) C07K 16/28 (2006.01) C07K 16/44 (2006.01) C08G 65/04 (2006.01) C08G 65/32 (2006.01)
Patent
CA 2087163
2087163 9201474 PCTABS00010 A conjugate substance (A-B-A'), where A and A' are residues from organic compounds F and F'; at least one of which being a polymer (carrier) and said compounds having properties that are retained in the conjugate and -B- being a bridge that covalently binds A to A'. The bridge -B- comprises the structure -SrRCONHCH2CH2(OCH2CH2)nO(CH2)mCOY- (I); (i) n is often an integer 1-20 that is uniform for bridges linking identically located positions in individual molecules of the substance; (ii) m = 1 or 2; (iii) R = an alkylene group (1-4 carbon atoms) that possibly is substituted with one or more (1-3) hydroxy(OH) groups; (iv) = sulfur in the form of a thioether (r = 1) or disulfide (r = 2), and Sr binding to saturated carbon atoms in both directions; (v) Y is -NH-, -NHNH- or -NHN=CH- that in their left ends bind to CO and in their right ends to saturated carbon atom or to a carbonyl group (only -NHNH-). A bifunctional coupling reagent complying with the formula Z1RCONHCH2CH2(OCH2CH2)nO(CH2)mZ'1 (III); (i) n is an integer, often 1-20; (ii) m is an integer 1 or 2, preferably 1; (iii) Z1 = a SH-reactive electrophile or thiol (SH-) or protected thiol; (iv) R = an alkylene group (1-4 carbon atoms, that possibly is substituted with one or more (1-3) hydroxy(OH) groups; and (v) Z'1 is activated carboxy. A polyether complying with the formula XCH2CH2(OCH2CH2-)nOCH2Y (IV) where n is an integer 2-20, preferably 3-10. X is H2N- or substituted H2N- that is transformable to H2N-, preferably by hydrolysis or reduction. Y is carboxy or a group that is transformable to carboxy.
Agback Hubert
Ahrgren Leif
Akerblom Eva
Haraldsson Martin
Gowling Lafleur Henderson Llp
Pharmacia Aktiebolag
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