Merck Sharp + Dohme Corp.

Oncoethix Gmbh

Maria Eugenia Riveiro

Eric Raymond

Francesco Bertoni

Kay Noel

A method of treating acute myeloid leukemia, acute lymphoblastic leukemia, high risk myelodysplastic syndrome, and/or HR-MDS/AML in a mammal by administering a solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein R1 is alkyl having a carbon number of 1-4, R2 is a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, R3 is a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; &#x2014;NR5-(CH2)m R6 wherein R5 is a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and R6 is phenyl or pyridyl optionally substituted by a halogen atom.

Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds

A method of treating non-small cell lung cancer and/or small cell lung cancer in a mammal comprises the step of administering to a patient a pharmaceutical acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1). 

Method of treating non-small cell lung cancer and/or small cell lung cancer using thienotriazolodiazepine compounds

A method of treating non-small cell lung cancer in a mammal by administering to a patient a pharmaceutically acceptable amount of a compound being a thienotriazolodiazepine compound of the Formula (1) wherein Ris alkyl having a carbon number of 1-4, Ris a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, Ris a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; &#x2014;NR&#x2014;(CH)&#x2014;Rwherein Ris a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and Ris phenyl or pyridyl optionally substituted by a halogen atom; or &#x2014;NR&#x2014;CO&#x2014;(CH)&#x2014;Rwherein Ris a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and Ris phenyl or pyridyl optionally substituted by a halogen atom, and Ris &#x2014;(CH)&#x2014;CO&#x2014;NH&#x2014;Rwherein a is an integer of 1-4, and Ris alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or &#x2014;(CH)&#x2014;COORwherein b is an integer of 1-4, and Ris alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof. 

Method of treating non-small-cell lung cancer using pharmaceutical formulation containing thienotriazolodiazepine compounds

A method of treating leukemia in a mammal by administering a solid dispersion comprising an amorphous thienotriazolodiazepine compound of the Formula (1) wherein Ris alkyl having a carbon number of 1-4, Ris a hydrogen atom; a halogen atom; or alkyl having a carbon number of 1-4 optionally substituted by a halogen atom or a hydroxyl group, Ris a halogen atom; phenyl optionally substituted by a halogen atom, alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4 or cyano; &#x2014;NR&#x2014;(CH)&#x2014;Rwherein Ris a hydrogen atom or alkyl having a carbon number of 1-4, m is an integer of 0-4, and Ris phenyl or pyridyl optionally substituted by a halogen atom; or &#x2014;NR&#x2014;CO&#x2014;(CH)&#x2014;Rwherein Ris a hydrogen atom or alkyl having a carbon number of 1-4, n is an integer of 0-2, and Ris phenyl or pyridyl optionally substituted by a halogen atom, and Ris &#x2014;(CH)&#x2014;CO&#x2014;NH&#x2014;Rwherein a is an integer of 1-4, and Ris alkyl having a carbon number of 1-4; hydroxyalkyl having a carbon number of 1-4; alkoxy having a carbon number of 1-4; or phenyl or pyridyl optionally substituted by alkyl having a carbon number of 1-4, alkoxy having a carbon number of 1-4, amino or a hydroxyl group or &#x2014;(CH)&#x2014;COORwherein b is an integer of 1-4, and Ris alkyl having a carbon number of 1-4, or a pharmaceutically acceptable salt thereof or a hydrate or solvate thereof. 

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Clichy, France

Maria Eugenia Riveiro