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Last Updated: March 29, 2024

Claims for Patent: 9,758,524


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Summary for Patent: 9,758,524
Title:4-imidazopyridazin-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. A. (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)
Application Number:15/019,543
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 9,758,524
Patent Claims: 1. A method of treating Mantle Cell Lymphoma (MCL) in a human subject, the method comprising administering to the human subject a compound which is (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1- -yl)-N-(pyridin-2-yl)benzamide, having the structure: ##STR00187## or a pharmaceutically acceptable salt thereof, in an amount effective to treat the MCL in the human subject.

2. The method of claim 1, wherein the compound is present in a pharmaceutical composition.

3. The method of claim 2, wherein the pharmaceutical composition comprises one or more pharmaceutically acceptable auxiliaries.

4. The method of claim 2, wherein the pharmaceutical composition is administered to the human subject by oral administration.

5. The method of claim 3, wherein the pharmaceutical composition is administered to the human subject by oral administration.

6. The method of claim 4, wherein the pharmaceutical composition is a tablet.

7. The method of claim 5, wherein the pharmaceutical composition is a tablet.

8. The method of claim 4, wherein the pharmaceutical composition is a capsule.

9. The method of claim 5, wherein the pharmaceutical composition is a capsule.

10. The method of claim 4, wherein the pharmaceutical composition is a suspension.

11. The method of claim 5, wherein the pharmaceutical composition is a suspension.

12. The method of claim 1, wherein the amount administered to the human subject is 0.0001-25 mg per kg body weight.

13. The method of claim 1, wherein the compound (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl- )-N-(pyridin-2-yl)benzamide is administered to the human subject.

14. The method of claim 1, wherein a pharmaceutically acceptable salt of the compound (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl- )-N-(pyridin-2-yl)benzamide is administered to the human subject.

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