摘要:
Poly(alkylene glycol) derivatives of the formula :
PAG [ O - V - Hg ⊖ x ⊕ ] n
or
PAG [ O - V₁ - S - R₁ ] n
wherein
PAG is a poly(alkylene glycol), x is a counter ion, V, V₁ is a non polymeric organic group, n is 1 or 2, and R₁ is selected from the group of -SO₃ ⊕ ; -S-SO₃ ⊕ ; -SO₂CH₃; thiopyridyl; nitrosulfenyl; otherwise substituted sulfenyl; -SO-(CH₂) m -CH₃ with m = 0, 1, ...; -SO m -CH₂-CH=CH₂ with m = 1, 2; -SO₂-R where R is alkyl or aryl.
摘要:
A coating composition comprises an anhydride polymer (A) containing a least two cyclic carboxylic acid anhydride functional groups and a polymer (B) containing at least two functional groups reactive with anhydride groups and selected from hydroxyalkylamino, hydroxyalkoxyalkylamino, hydroxy-substituted acyloxyalkylamino, hydroxy-substituted polyacyloxyalkylamino, mercaptoalkylamino and oxazolidino groups. One of the polymers (A) and (B) comprises at least one flexible polymer chain selected from polyether, polyester, silicone, diene polymer, hydrogenated diene polymer, polyurethane, polyisobutylene and polyacrylate chains. The functional groups characteristic of that polymer are each present as a terminal group at the end of a flexible polymer chain.
摘要:
An intestinal anti-inflammatory preparation comprising a polymeric agent for releasing 5-aminosalicylic acid or its salts is disclosed. The polymeric agent comprises a nonabsorbable pharmacologically acceptable organic polymer backbone containing aromatic rings to which are covalently bonded via azo bonds a plurality of salicylic acid or salicylate's salt groups. The azo bonds attach to the salicylates' 5-position carbon. The polymers' azo bonds undergo bacterial cleavage in the mammalian lower bowel to release 5-aminosalicylic acid and/or its salts.
摘要:
An intestinal anti-inflammatory preparation comprising a polymeric agent for releasing 5-aminosalicylic acid or its salts is disclosed. The polymeric agent comprises a nonabsorbable pharmacologically acceptable organic polymer backbone containing aromatic rings to which are covalently bonded via azo bonds a plurality of salicylic acid or salicylate's salt groups. The azo bonds attach to the salicylates' 5-position carbon. The polymers' azo bonds undergo bacterial cleavage in the mammalian lower bowel to release 5-aminosalicylic acid and/or its salts.
摘要:
A DDS preparation of a platinum complex, which exhibits a superior antitumor effect required as a medicine and reduced side effects, that is, a clinically usable DDS preparation of a platinum complex, which is conjugated to a polymer carrier that is different from conventional carriers, is desired. Provided is a polymer conjugate of a platinum(II) complex, the polymer conjugate including: a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; a sulfoxide derivative introduced into a side-chain carboxyl group of the block copolymer; and a platinum(II) complex coordinate-bonded to a sulfoxide group of the sulfoxide derivative.
摘要:
Disclosed are an 8-arm polyethylene glycol (PEG) derivative (formula 1), manufacturing method and modified bio-related substance thereby, wherein a tetravalent group U and four trivalent groups E c form a highly symmetric octavalent central structure CORE 0 together, L c connects the octavalent center to eight PEG arms having polydiversity or monodiversity and having n 1 -n 8 as the degrees of polymerization thereof. The terminal of one PEG chain is connected to at least one functional group F (k ‰¥ 1), and said PEG chain and F can be directly connected (g = 0) or connected with a divalent linking group L 0 connected with a terminal branched group G (g = 1) therebetween. The latter provides more reacting sites to combine more pharmaceutical molecules, thereby increasing the drug loading capacity. The near-center symmetric structure of the derivative allows more precise control over the molecular weight during large-scale production, thereby facilitating acquisition of a product having a narrower molecular weight distribution. A bio-related substance modified thereby has a more uniform and controllable performance.
摘要:
Provided is a hetero type monodispersed polyethylene glycol which contains a compound represented by formula (1) ((1): NH 2 -(CH 2 CH 2 O) a -CH 2 CH 2 COOH (in formula (1), a is an integer between 6 and 40)) and in which the following each satisfy a specified relational expression: (A) a chromatogram detected by a differential refractometer when separation is carried out using reversed phase chromatography; (B) a chromatogram detected by a differential refractometer when separation is carried out using cation exchange chromatography; and (C) a chromatogram detected by a differential refractometer when the hetero type monodispersed polyethylene glycol containing a compound represented by formula (1) is derivatized and separation is carried out using anion exchange chromatography.
摘要:
It is provided a polyglycerol derivative, comprising a dendritic polyglycerol backbone and at least one substituent in the nature of a covalently bound negatively charged group chosen from the group consisting of sulfates, sulfonates, phosphates, phosphonates, bisphosphonates, carboxylates and combinations thereof. The substituent is bound to the polyglycerol backbone via a linker, the linker being chosen from the group consisting of moieties being or comprising a carbamate group, an ester group, an orthoester group, an amide group, a disulfide bridge group, an acetal group, an imine group and combinations thereof.