Solid State Polymerization Process for Polyester with Phosphinic Acid Compounds
申请人:Odorisio Paul
公开号:US20130035451A1
公开(公告)日:2013-02-07
Disclosed are phosphinic acid compounds of formula I, II or III
where R
1
and R
1
′ are for instance straight or branched C
1
-C
50
alkyl, R
2
is for instance straight or branched C
22
-C
50
alkyl, R
3
and R
3
′ are for instance straight or branched C
1
-C
50
alkyl, R
4
is for instance straight or branched C
1
-C
50
alkylene and m is from 2 to 100. Also disclosed are polyester compositions comprising the compounds of formula I, II and III.
[EN] CONTROLLED-RELEASE TYROSINE KINASE INHIBITOR COMPOUNDS WITH LOCALIZED PK PROPERTIES<br/>[FR] COMPOSÉS INHIBITEURS DE TYROSINE KINASE À LIBÉRATION CONTRÔLÉE PRÉSENTANT DES PROPRIÉTÉS PHARMACOCINÉTIQUES LOCALISÉES
申请人:ASCENDIS PHARMA ONCOLOGY DIV A/S
公开号:WO2020254613A1
公开(公告)日:2020-12-24
The present invention relates to a water-insoluble controlled-release tyrosine kinase inhibitor ("TKI") compound for use in the treatment of a cell-proliferation disorder, wherein said water-insoluble controlled-release TKI compound releases one or more TKI drug, wherein the water-insoluble controlled-release TKI compound is administered by intra-tissue administration and wherein the total amount of TKI moieties and TKI drug molecules remaining locally in such tissue 3 days after said intra-tissue administration is at least 25% of the amount of TKI moieties or TKI drug molecules administered by said intra-tissue administration; and to related aspects.
[EN] MINIMIZATION OF SYSTEMIC INFLAMMATION<br/>[FR] MINIMISATION DE L'INFLAMMATION SYSTÉMIQUE
申请人:ASCENDIS PHARMA AS
公开号:WO2020141225A1
公开(公告)日:2020-07-09
The present invention relates to a water-insoluble controlled-release pattern recognition receptor agonist ("PRRA") for use in the treatment of a cell-proliferation disorder, wherein the water-insoluble controlled-release PRRA is administered by intra-tissue administration, and wherein the protein levels of at least one cytokine selected from the group consisting of IL-6, CCL2 and IL-10 in plasma has a more than 10-fold lower maximum protein level within 24 hours compared to an equivalent molar dose of the corresponding free PRRA upon intra/tissue administration; and to related aspects.
[EN] TREATMENT OF INFECTIONS<br/>[FR] TRAITEMENT D'INFECTIONS
申请人:ASCENDIS PHARMA AS
公开号:WO2020064844A1
公开(公告)日:2020-04-02
The present invention relates among other aspects to a conjugate or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising said conjugate or its pharmaceutically acceptable salt for use in a method of preventing or treating an infection, wherein said conjugate is water-insoluble and comprises a polymeric moiety -Z to which a plurality of moieties -L2-X0D-L1-D are covalently conjugated, wherein each -D is independently an antibiotic moiety; each -L1- is independently a linker moiety to which -D is covalently and reversibly conjugated; each -X0D- is independently absent or a linkage and each -L2- is independently either a chemical bond or a spacer moiety.
[EN] CONTROLLED-RELEASE TYROSINE KINASE INHIBITOR COMPOUNDS WITH LOCALIZED PD PROPERTIES<br/>[FR] COMPOSÉS INHIBITEURS DE TYROSINE KINASES À LIBÉRATION CONTRÔLÉE PRÉSENTANT DES PROPRIÉTÉS PHARMACODYNAMIQUES LOCALISÉES
申请人:ASCENDIS PHARMA ONCOLOGY DIV A/S
公开号:WO2020254612A1
公开(公告)日:2020-12-24
The present invention relates to a water-insoluble controlled-release TKI compound for use in the treatment of a cell-proliferation disorder, wherein said water-insoluble controlled-release TKI compound releases one or more TKI drug, wherein upon intra-tissue administration of a single dose of the water-insoluble controlled-release TKI compound anti-tumor activity is observed between 7 and 21 days following administration of the water-insoluble controlled-release TKI compound, and wherein the change in mean arterial blood pressure as measured in mmHg is less than 50% of the change in mean arterial blood pressure observed in the same animal species treated with a daily equimolar dose of the corresponding free TKI drug; and to related aspects.