C07D275/06

MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

Ammonium salt having saccharin anion
11512061 · 2022-11-29 · ·

An ammonium salt having a saccharin anion, which is represented by formula (1), exhibits excellent thermal stability even though no halogen atom is contained therein. ##STR00001##
(In the formula, each of R.sup.1-R.sup.4 independently represents an alkyl group having 1-4 carbon atoms or an alkoxyalkyl group that is represented by —(CH.sub.2).sub.n—OR (wherein R represents an alkyl group having 1-4 carbon atoms, and n represents an integer of 1 or 2). Incidentally, any two of the R.sup.1-R.sup.4 may combine with each other to form a ring together with a nitrogen atom.

Ammonium salt having saccharin anion
11512061 · 2022-11-29 · ·

An ammonium salt having a saccharin anion, which is represented by formula (1), exhibits excellent thermal stability even though no halogen atom is contained therein. ##STR00001##
(In the formula, each of R.sup.1-R.sup.4 independently represents an alkyl group having 1-4 carbon atoms or an alkoxyalkyl group that is represented by —(CH.sub.2).sub.n—OR (wherein R represents an alkyl group having 1-4 carbon atoms, and n represents an integer of 1 or 2). Incidentally, any two of the R.sup.1-R.sup.4 may combine with each other to form a ring together with a nitrogen atom.

Processes for making alkylated arylpiperazine and alkylated arylpiperidine compounds including novel intermediates

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively ##STR00001##
wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

Processes for making alkylated arylpiperazine and alkylated arylpiperidine compounds including novel intermediates

Novel processes, and intermediates, for making alkylated arylpiperazine and alkylated arylpiperidine compounds of the general formulas (I) and (VII), respectively ##STR00001##
wherein, R.sub.1 and R.sub.2 are individually selected from hydrogen, alkyl, substituted or alkyl; n=0, 1, or 2; Y=NR.sub.3R.sub.4, OR.sub.5, or SR.sub.5, where R.sub.3 and R.sub.4 are individually selected from acyl or sulfonyl, and where R.sub.5 is aryl or heteroaryl, or heterocyclic; and Ar is an aryl, heteroaryl, or heterocyclic compound.

STAT3 inhibitors and their anticancer use

In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

STAT3 inhibitors and their anticancer use

In one aspect, the invention relates to substituted 6-amino-5,8-dioxo-5,8-dihydronaphthalene-1-sulfonamide analogs and derivatives thereof, substituted 4-amino-5H-naphtho[1,8-cd]isothiazol-5-one 1,1-dioxide analogs and derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Crystalline forms of lenalidomide

The present invention provides for novel co-crystals of lenalidomide. The present invention particularly provides for novel cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention also provides for the processes for the production of cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention further provides for processes for the preparation of crystalline anhydrous lenalidomide Form IV.

Crystalline forms of lenalidomide

The present invention provides for novel co-crystals of lenalidomide. The present invention particularly provides for novel cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention also provides for the processes for the production of cocrystals of lenalidomide with Resorcinol, Methyl paraben and Saccharin. The present invention further provides for processes for the preparation of crystalline anhydrous lenalidomide Form IV.

INHIBITORS OF CD40-CD154 BINDING

Disclosed herein are compounds including pharmaceutically acceptable salts, esters, prodrugs, hydrates and tautomers thereof which modulate the interactions of CD-40-CD40L. The compounds are useful for treating, ameliorating or preventing an autoimmune disease, inflammatory disease, or other immune-related disease in a patient in need of treatment.