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Last Updated: April 25, 2024

Details for Patent: 9,790,226


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Title:4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as BtK inhibitors
Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) ##STR00001## or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
Inventor(s): Barf; Tjeerd A. (Ravenstein, NL), Jans; Christiaan Gerardus Johannes Maria (Cuijk, NL), de Man; Adrianus Petrus Antonius (Hurwenen, NL), Oubrie; Arthur A. (Wijchen, NL), Raaijmakers; Hans C. (Eindhoven, NL), Rewinkel; Johannes Bernardus Maria (Berghem, NL), Sterrenburg; Jan Gerard (Renkum, NL), Wijkmans; Jacobus C. H. M. (Oss, NL)
Assignee: Merck Sharp & Dohme B.V. (Haarlem, NL)
Filing Date:Feb 09, 2016
Application Number:15/019,561
Claims:1. A compound which is (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl- )-2-methoxy-N-(pyridin-2-yl)benzamide, having the structure: ##STR00187##

2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and the compound of claim 1.

3. A pharmaceutically acceptable salt of a compound, the compound being (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl- )-2-methoxy-N-(pyridin-2-yl)benzamide and having the structure: ##STR00188##

4. The pharmaceutically acceptable salt of claim 3, wherein the salt is selected from the group consisting of acetate, ascorbate, benzoate, benzenesulfonate, bisulfate, borate, butyrate, citrate, camphorate, camphorsulfonate, fumarate, hydrochloride, hydrobromide, hydroiodide, lactate, maleate, methanesulfonate, naphthalenesulfonate, nitrate, oxalate, phosphate, propionate, salicylate, succinate, sulfate, tartarate, thiocyanate, and toluenesulfonate.

5. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and the pharmaceutically acceptable salt of claim 3.

6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and the pharmaceutically acceptable salt of claim 4.

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