Astrazeneca Ab

Albireo Ab

Elobix Ab

Mimetogen Pharmaceuticals, Inc

Nektar Therapeutics

Targacept, Inc.

Martin Hans Bohlin

Ingvar Ymen

Per-Göran Gillberg

Nils Ove Gustafsson

Jessica Elversson

Anna-Maria Tivert

Eva Byröd

Rikard Bryland

Ann-Charlotte Dahlquist

Robert Lundqvist

Wei Tian

Chantal Devin

Sébastien Rocchi

Tesfai Sebhatu

Andreas Vestermark

Erica Tjerneld

Stephan D Parent

David Thomas Jonaitis

Carl-Johan Aurell

Tord Bertil Inghardt

Anita Lundblad

Thomas Larsson

Ingvar Ymén

Rhony Aufdenblatten

Helena Nicklasson

Eric Thomas Healy

David Richard Jensen

Matti Ahlqvist

Carl-Gustaf Sigfridsson

Gary Maurice Dull

Craig Harrison Miller

Julio A Munoz

Per Lennart Lindberg

Anders Mattson

Ulf G Larsson

Karol Horvath

Laurent Ducry

Craig Robert Stewart

Mattias Magnusson

Anders Kronstr&ouml;m

John Peter Gilday

Bo Ingvar Ymén

Eva Leander

Bengt Leonard Åslund

Peter W Johansson

Bengt Aslund

Bo Ingvar Ymen

Karin Jansson

Bo Lassen

Ulrika Lindblad

Caroline Ericsson

Andreas Weiss

Ursula Noreland

Mikaela Recknagel

Helena Hellström

Steve Cosgrove

Anthony Stephen Graham

John Peter Astrazeneca Pharmaceuticals Gilday

Bengt Leonard ÅSlund

Bo Ingvar YMÉN

Bengt Leonard Aslund

Andreas (deceased) Weiss

Helena Hellstroem

Stephan Parent

The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I: where R, R, R, R, R, R, R, R, R, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of a β-turn cyclic peptidomimetic compounds and salts thereof.

Solution phase synthesis of β-turn peptidomimetic cyclic salts

The present invention relates to crystal modifications of 1,1-dioxo-3,3-dibutyl-5-phenyl-7-methylthio-8-(N—{(R)-α-[N—((S)-1-carboxypropyl)carbamoyl]-4-hydroxybenzyl}carbamoylmethoxy)-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine (odevixibat), more specifically crystal modifications 1 and 2 of odevixibat. The invention also relates to a process for the preparation of crystal modification 1 of odevixibat, to a pharmaceutical composition comprising crystal modification 1, and to the use of this crystal modification in the treatment of various conditions as described herein.

Crystal modifications of odevixibat

The invention relates to a pharmaceutical formulation, e.g. a paediatric formulation, of odevixibat, which comprises a plurality of small particles. The formulation may be used in the treatment of liver diseases such as bile acid-dependent liver diseases, and particularly cholestatic liver diseases such as biliary atresia, progressive familial intrahepatic cholestasis (PFIC), Alagille syndrome (ALGS) and paediatric cholestatic pruritus. The invention also relates to a process for the preparation of the pharmaceutical formulation.

Pharmaceutical formulation of odevixibat

The present disclosure relates to methods of preparing and crystallizing &#x3b2;-turn cyclic peptidomimetic salts of formula I: where R, R, R, R, R, R, R, R, R, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of a &#x3b2;-turn cyclic peptidomimetic compounds and salts thereof.

Solution phase synthesis of beta-turn peptidomimetic cyclic salts

The present invention relates to crystal modifications of 1,1-dioxo-3,3-dibutyl-5-phenyl-7-methylthio-8-(N&#x2014;{(R)-&#x3b1;-[N&#x2014;((S)-1-carboxypropyl)carbamoyl]-4-hydroxybenzyl}carbamoylmethoxy)-2,3,4,5-tetrahydro-1,2,5-benzothiadiazepine (odevixibat), more specifically crystal modifications 1 and 2 of odevixibat. The invention also relates to a process for the preparation of crystal modification 1 of odevixibat, to a pharmaceutical composition comprising crystal modification 1, and to the use of this crystal modification in the treatment of various conditions as described herein.

The present disclosure relates to methods of preparing and crystallizing &#x3b2;-turn cyclic peptidomimetic salts of formula I: where R, R, R, R, R, R, R, R, R, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of &#x3b2;-turn cyclic peptidomimetic compounds and salts thereof.

Solution phase synthesis and crystallization of beta-turn peptidomimetic cyclic salts

A camsylate salt of (1r,1'R,4R)-4-methoxy-5&#x2033;-methyl-6&#x2032;-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3&#x2032;H-dispiro[cyclohexane-1,2&#x2032;-inden-1&#x2032;2&#x2032;-imidazole]-4&#x2033;-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating A&#x3b2;-related pathologies such as Alzheimer's Disease, Down's syndrome, &#x3b2;-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

Camsylate salt

The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat).

Crystal modifications of elobixibat

The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.

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Sodertalje, Sweden

Martin Hans Bohlin