Applied Research Systems Ars Holding N.v.

Iksuda Therapeutics Limited

Anthony David Baxter

Anna Quattropani

Serge Halazy

Matthias Schwarz

Agnes Bombrun

Russell Thomas

Alexander Scheer

Christopher Michael Birchall

David James Mansell

Justyna Helena Mysliwy

Jenny Thirlway

Mattias Schwarz

Russel Thomas

The present invention relates to protein drug conjugates, methods of manufacturing the same and their use in therapy. In particular, the present invention relates to protein drug conjugates comprising a globular protein, an improved linker and a drug for use in targeted drug delivery applications.

Materials and methods relating to linkers for use in protein drug conjugates

The present invention is related to pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of &#x2014;(C&#x2550;O)&#x2014;, &#x2014;(C&#x2550;O)&#x2014;O&#x2014;, &#x2014;C(&#x2550;NH)&#x2014;, &#x2014;(C&#x2550;O)&#x2014;NH&#x2014;, &#x2014;(C&#x2550;S)&#x2014;NH, &#x2014;SO22-, &#x2014;SO2NH&#x2014;, &#x2014;CH2-, B is either a group &#x2014;(C&#x2550;O)&#x2014;NR8R9 or represents a heterocyclic residue having the formula (a) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5&#x2013;6 membered aryl or heteroaryl ring.

Pharmaceutically active pyrrolidine derivatives

The present invention is related to new substituted pyrrolidine derivatives of formula (I). Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula (I) are useful in the treatment and/or prevention of neurodegenerative disorders, diseases associated with polygultamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders renal hypoxia, hepatitis and AIDS. Said pyrrolidine derivatives display a modulatory and most notably a down-regulating-up to an inhibitory-activity with respect to the cellular death agonist Bax and/or the activation pathways leading to Bax and allows therefore to block the release of cytochrome (c). The present invention is furthermore related to novel pharmaceutically activity substituted pyrrolidine derivatives as well as to methods of their preparation, wherein X is selected from the group consisting of O, S, CR&#x3c;6&#x3e;R&#x3c;7&#x3e;, NOR&#x3c;6&#x3e;, NNR&#x3c;6&#x3e;R&#x3c;7&#x3e;; A is selected from the group consisting of &#x2014;(C&#x2550;O)&#x2014;, &#x2014;(C&#x2550;O)&#x2014;O&#x2014;, &#x2014;C(&#x2550;NH)&#x2014;, &#x2014;(C&#x2550;O)&#x2014;NH&#x2014;, &#x2014;(C&#x2550;S)&#x2014;NH, &#x2014;SO2&#x2014;, &#x2014;SO2NH&#x2014;; &#x2014;CH2&#x2014;; B is either a group &#x2014;(C&#x2550;O)&#x2014;NR&#x3c;8&#x3e;R&#x3c;9&#x3e; or represents a heterocyclic residue having the formula (II) wherein Q is NR&#x3c;10&#x3e;, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5&#x2013;6 membered aryl or heteroaryl ring.

Pharmaceutically active pyrrolidine derivatives as Bax inhibitors

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Much Hadham, United Kingdom

Anthony David Baxter