C07C279/18

Pharmaceutical composition for preventing or treating immune diseases or inflammatory diseases, containing biguanide derivative compound as active ingredient

The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.

LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME
20190209548 · 2019-07-11 ·

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

LINKED DIARYL COMPOUNDS WITH ANTICANCER PROPERTIES AND METHODS OF USING THE SAME
20190209548 · 2019-07-11 ·

Provided are compositions comprising linked diaryl compounds that possess anticancer properties. Methods of use are also disclosed herein. The method comprises administering an effective amount of a compound described herein to an individual in need thereof.

Process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine
10343984 · 2019-07-09 · ·

The present invention relates to a process for the preparation of the compound N-(3,5-dimethylphenyl)-N-(2-trifluoromethylphenyl) guanidine of formula (I) which comprises reacting a salt of a compound of formula (II) or a mixture of the salt of the compound of formula (II) and a compound of formula (II) with a compound of formula (III), in the presence of a polar organic solvent; a crystalline solid form of the compound of formula (I), in particular crystalline solid form A; to a pharmaceutical composition comprising them; and to their use as a medicament, in particular to the treatment of a condition mediated by Rho-GTPase cell proteins. ##STR00001##

Process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine
10343984 · 2019-07-09 · ·

The present invention relates to a process for the preparation of the compound N-(3,5-dimethylphenyl)-N-(2-trifluoromethylphenyl) guanidine of formula (I) which comprises reacting a salt of a compound of formula (II) or a mixture of the salt of the compound of formula (II) and a compound of formula (II) with a compound of formula (III), in the presence of a polar organic solvent; a crystalline solid form of the compound of formula (I), in particular crystalline solid form A; to a pharmaceutical composition comprising them; and to their use as a medicament, in particular to the treatment of a condition mediated by Rho-GTPase cell proteins. ##STR00001##

Process for the preparation of the compound N-(3,5-dimethylphenyl)-N′-(2-trifluoromethylphenyl) guanidine
10343984 · 2019-07-09 · ·

The present invention relates to a process for the preparation of the compound N-(3,5-dimethylphenyl)-N-(2-trifluoromethylphenyl) guanidine of formula (I) which comprises reacting a salt of a compound of formula (II) or a mixture of the salt of the compound of formula (II) and a compound of formula (II) with a compound of formula (III), in the presence of a polar organic solvent; a crystalline solid form of the compound of formula (I), in particular crystalline solid form A; to a pharmaceutical composition comprising them; and to their use as a medicament, in particular to the treatment of a condition mediated by Rho-GTPase cell proteins. ##STR00001##

Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
10314795 · 2019-06-11 · ·

The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.

Sigma receptor ligands and methods of modulating cellular protein homeostasis using same
10314795 · 2019-06-11 · ·

The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.

ANTIBACTERIAL COMPOUNDS

An antibacterial compound of formula I, wherein X is selected from fluoro or bromo, effective against Gram negative and Gram positive bacteria, and in particular against non-fermenting multiresistant bacteria affecting patients suffering from cystic fibrosis and which are responsible of severe hospital-acquired infections in immunodepressed patients; its preparation process and pharmaceutical composition comprising said compound.

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Novel Chlorhexidine Salts and Related Compositions and Methods

This application relates to a novel chlorhexidine lauryl sulfate salt, which provides enhanced chlorhexidine stability and enhanced anti-bacterial activity, and to formulations and methods utilizing the novel salt.