US 2022/0175682 A1 · Siremadlin Succinate

Siremadlin Succinate

AssigneeNovartis AG

InventorsNicole BIERI, Elodia DI RENZO, David HOOK, Jennifer Claire HOOTON, Markus KRUMME, Steffen LANG, Franck MALLET, Massimo MORATTO, Joerg OGORKA, Jim PARKS, Dale W. PLOEGER, Norbert RASENACK, Hendrik SCHNEIDER, Lipa SHAH, Stefan STEIGMILLER, Gordon STOUT, Patrick TRITSCHLER, Fabian WEBER

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Abstract

The present invention relates to methods of preparing pharmaceutical products, involving filling active pharmaceutical ingredient powders into pharmaceutical carriers with a vacuum assisted metering and filling device. The methods disclosed herein can be used in a continuous process, such as in a high-throughput process for producing a pharmaceutical product. The present invention further relates to a particular quality of the neat active pharmaceutical ingredient (API) HDM201, i.e. siremadlin, present as succinic acid co-crystal, which can be used in the methods of preparation of the present invention.

Claims22

Dependent claims

The neat active pharmaceutical ingredient (API) HDM201 (siremadlin) present as succinic acid co-crystal in a quality which complies with at least five of the following parameters (i)-(viii) as determined by using a FT4 powder rheometer:

(i) specific basic flow energy (sBFE) of at most 60 mJ/g;
(ii) stability index (SI) of 0.75 to 1.25;
(iii) specific energy (SE) of at most 10 mJ/g;
(iv) major principle stress at 15 kPa (MPS-15) of at most 40;
(v) flow function at 15 kPa (FF-15) of at least 1.3;
(vi) consolidated bulk density at 15 kPa (CBD-15) of at least 0.26 g/mL;
(vii) compressibility of at most 47%;
and
(viii) wall friction angle (WFA) of at most 40°.

6 more elements

Dependencies are inferred from the claim text.

Facts

Application

17/600,203Filed 2 Apr 2020

Priority

4 Apr 2019

Published

9 Jun 2022

Term ends

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Classification8 codes

A61K 9/4833
Preparations in capsules, e.g. of gelatin, of chocolate: encapsulating processes; Filling of capsules
C07D 487/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61K 9/1682
Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,…:…
A61K 31/506
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: not condensed and containing further heterocyclic rings