The invention provides a novel class of propiolylamide-based irreversible inhibitors of PKM2 compounds of the general formula I, pharmaceutical compositions, and methods of inducing an anti-tumor effect in a subject suffering from tumor comprising administering to the subject a pharmaceutical composition comprising an effective amount of compound of formula I.

The invention provides a novel class of propiolylamide-based irreversible inhibitors of PKM2 compounds of the general formula I, pharmaceutical compositions, and methods of inducing an anti-tumor effect in a subject suffering from tumor comprising administering to the subject a pharmaceutical composition comprising an effective amount of compound of formula I.

The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.

The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.

The present invention relates to pyrazole derivatives of formula (X)

##STR00001## wherein ring A is a pyrazole and substituents R.sup.B1, R.sup.B2, n, R.sup.Q1, R.sup.Q2, R.sup.Q3, and R.sup.Q4 are as defined in claim 1, their manufacture, and their use in the manufacture of agrochemicals and pharmaceuticals.

Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.

A process A for the production of compounds of formula I is provided.

##STR00001##

Process A includes Step A of reacting compounds of formula II

##STR00002##

with 2,3-dihalopropionitrile or 2-haloacrylonitrile in the presence of DIPEA. A process B for the production of compounds of formula III is also provided.

##STR00003##

Process B includes Step B of reacting compounds of formula I with Br.sub.2 in the presence of DIPEA. A process C for the production of compounds of formula IV is further provided.

##STR00004##

Process C includes Step C of reacting compounds of formula III with di(C.sub.1-C.sub.4-alkoxy)methane and either POCl.sub.3, or a mixture comprising POCl.sub.3 and DMF, in the presence of DIPEA. Additionally, the use of DIPEA as a base in the production of compounds of formula I, compounds of formula III, or compounds of formula IV is provided.

A process A for the production of compounds of formula I is provided.

##STR00001##

Process A includes Step A of reacting compounds of formula II

##STR00002##

with 2,3-dihalopropionitrile or 2-haloacrylonitrile in the presence of DIPEA. A process B for the production of compounds of formula III is also provided.

##STR00003##

Process B includes Step B of reacting compounds of formula I with Br.sub.2 in the presence of DIPEA. A process C for the production of compounds of formula IV is further provided.

##STR00004##

Process C includes Step C of reacting compounds of formula III with di(C.sub.1-C.sub.4-alkoxy)methane and either POCl.sub.3, or a mixture comprising POCl.sub.3 and DMF, in the presence of DIPEA. Additionally, the use of DIPEA as a base in the production of compounds of formula I, compounds of formula III, or compounds of formula IV is provided.

Disclosed are compounds, for example, compounds of formula I, ##STR00001##
wherein R, R.sub.0, R.sub.1-R.sub.8, n, X, Y, Y′, and E are as described herein, pharmaceutical compositions containing such compounds, and methods of treating or preventing a disease or condition, for example, cancer.