Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). ##STR00001##

The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.

Compounds of formula (A) are provided which are useful in the treatment of diseases or conditions modulated at least in part by CCR6:

##STR00001##

An object of the present invention is to provide a compound with an excellent JAK1 inhibitory activity. The compound of the invention has JAK1 inhibitory activity, and thus, immunosuppressive effect, anti-inflammatory effect, anti-proliferative effect and so on, and is useful in the treatment of the diseases, for example, rheumatoid arthritis, inflammatory bowel disease, psoriasis, vasculitis, bronchial asthma, chronic obstructive pulmonary disease, eosinophilic sinusitis and nasal polyp.

The present invention covers bicyclic pyrazole compounds of general formula (I): in which G, A, R.sup.1, R.sup.2, R.sup.3, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients. ##STR00001##

An organic molecule is disclosed having: a first chemical unit comprising or consisting of a structure according to formula I ##STR00001##
and two second chemical moieties, each at each occurrence independently from another comprising or consisting of a structure of formula II, ##STR00002##
wherein the first chemical moiety is linked to each of the two second chemical moieties via a single bond.

The present invention discloses a tetrahydropyrrole compound, a preparation method therefor, a pharmaceutical composition containing the same, and a use thereof. The tetrahydropyrrole compound of the present invention is represented by general formula (I). The tetrahydropyrrole compound of the present invention has better inhibitory effects on the positive symptoms of schizophrenia, and the potency thereof is equivalent to or slightly stronger than that of the positive drug olanzapine. In addition, the compound of the present invention has dual inhibitory effects on D2 receptors and DAT receptors, and is effective for treating schizophrenia and improving negative symptoms and cognitive functions, while also reducing vertebral side effects and prolactin secretion.

##STR00001##

Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound IA, wherein R.sup.1 is described herein. Compound IA can be useful in synthesizing compound A1, or a salt or solvate thereof, and compound A2, or a salt of solvate thereof.

##STR00001##

Provided herein are processes for synthesizing intermediates useful in preparing Mcl-1 inhibitors. In particular, provided herein are processes for synthesizing compound IA, wherein R.sup.1 is described herein. Compound IA can be useful in synthesizing compound A1, or a salt or solvate thereof, and compound A2, or a salt of solvate thereof.

##STR00001##

The present invention covers bicyclic pyrazole compounds of general formula (I): in which G, A, R.sup.1, R.sup.2, R.sup.3, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

##STR00001##