Pharmacyclics, Inc.

Leo-Pharma A/s

Libra Therapeutics, Inc.

Maria Pia Catalani

Wei Yu Chen

Jeremy Robert Greenwood

David J Loury

Zhaozhong Jon Jia

Romano Di Fabio

Jakob Felding

Shunqi Yan

Morten Dahl Sørensen

Leah Lynn Frye

Mee Shelley

Longcheng Wang

Luca Francesco Raveglia

Alfonso Pozzan

Gordana Babic Atallah

Haakon Bladh

Riccardo Zanaletti

Ali Munaim Yousif

Morten Dahl SØRENSEN

Described herein are oxazole TRPML1 agonists and pharmaceutical compositions comprising said agonists. The subject compounds and compositions are useful for the treatment of TRPML1-mediated disorders or diseases.

Oxazole TRPML1 agonists and uses thereof

Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk) having the structure of Formula (B):  Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Inhibitors of Bruton's tyrosine kinase

The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, Calkyl, Chaloalkyl, Calkoxy, CD3 or halogen; R3 is hydrogen, C(&#x2550;O)OR7 or Calkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(&#x2550;O)R7, C(&#x2550;O)OR7, C(&#x2550;O)NR8R9, Calkyl, wherein said Calkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with Calkyl or C(&#x2550;O)R7; or R5 and R6, together with the carbon atom to which they are attached, form &#x2550;CHor a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with Calkyl; R7 is hydrogen or Calkyl; R8 and R9 are independently hydrogen or Calkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically acceptable salt or solvate thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating or ameliorating pruritic dermal diseases or conditions with said compounds, and to the use of said compounds in the manufacture of medicaments. 

Substituted pyrrolo[1,2-a]piperazines and pyrrolo[1,2-a][1,4]diazepines as neurokinin 1 receptor antagonists

Growing community of inventors

Verona, Italy

Maria Pia Catalani