Ucb S.a.

Kemotech S.r.l.

Kemtech S.r.l.

Matteo Zanda

Paolo Lazzari

Monica Sani

Alain Wagner

Charles Mioskowski

Luc Quere

Patrice Talaga

Jean-Philippe Starck

Michel Guyaux

Chimmanamada U Dinesh

Pharmaceutical compounds

Tubulysine compounds of formula (A) having a high cytotoxicity wherein:B is selected from CH, CH&#x2014;CHor CH&#x2014;CH&#x2014;CH,D is an aromatic linker,Xis alkyl or alkenyl,Xis selected from the X, substituted or non substituted, selected from: aryl, heteroaryl, arylalkyl, cycloalkylalkyl, heterocycloalkylalkyl, or heteroarylalkyl,X: alkylene-O-alkyl, wherein alkylene is C-C,X: CH&#x2014;O-alkyl,Xis selected from H, or together with Xforms the group &#x2550;O,Xis selected from H, halogen, OH, SH, alkyl, alkenyl, (OR)&#x2014;OR, OC(O)R, NRR, or together with Xforms the group &#x2550;O,Ris an alkylene,n is zero or an integer from 1 to 10,Rand R, equal to or different from each other, have the following meanings:

Tubulysin compounds with high cytotoxicity, pharmaceutical compositions thereof, and method of use thereof

The invention concerns quinuclidine derivatives of formula I or II wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention show high affinities for m3 and/or m2 muscarinic receptors and are particularly suited for treating urinary incontinence.

Quinuclidine derivatives processes for preparing them and their uses as m2 and/or m3 muscarinic receptor inhibitors

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Gandino, Italy

Matteo Zanda