C07D473/18

HDAC inhibitor solid state forms

The present disclosure relates to the crystalline mesylate Form 1 salt of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxamide and methods of making the same. The crystalline mesylate Form 1 salt of N-hydroxy 2-{6-[(6-fluoro-quinolin-2-ylmethyl)-amino]-3-aza-bicyclo[3.1.0]hex-3-yl}pyrimidine-5-carboxamide is useful in preparation of pharmaceutical compositions and dosage forms for the treatment of cancer, immune disorders and inflammation.

Synthesis of backbone modified morpholino oligonucleotides and chimeras using phosphoramidite chemistry

Amine substituted morpholino oligonucleotides, other than the classical N,N-dimethylamino PMO analogue, and methods of efficiently synthesizing these oligonucleotides with high yield are provided. Morpholino oligonucleotides having thiophosphoramidate, phosphoramidate, and alkyl phosphoramidate linkers. Chimeras containing unmodified DNA/RNA and other analogs of DNA/RNA can be prepared. These oligonucleotides form duplexes with complementary DNA or RNA that are more stable than natural DNA or DNA/RNA complexes, are active with RNAse H1, and may be transfected into cells using standard lipid reagents. These analogues are therefore useful for numerous applications.

Amino-triazolopyridine compounds and their use in treating cancer

The specification generally relates to compounds of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, where R.sup.1 and R.sup.2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Amino-triazolopyridine compounds and their use in treating cancer

The specification generally relates to compounds of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, where R.sup.1 and R.sup.2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

CARBOBICYCLIC NUCLEOSIDES FOR TREATMENT OF VIRAL INFECTION
20230357168 · 2023-11-09 ·

Carbobicyclic nucleoside compounds useful for the treatment of coronavirus disease 2019 (COVID-19), RSV and other viral infections are provided. The carbobicyclic nucleoside compound may be a compound as set forth herein. Pharmaceutical formulations useful for treatment of COVID-19 and RSV are also described.

Pyrimidine derivatives for prevention and treatment of bacterial infections

Pyrimidine derivatives of formula (I): ##STR00001##
optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. Pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. Pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.

Method of treating microbial infections

The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.

Method of treating microbial infections

The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.

WATER SOLUBLE ADJUVANT AND COMPOSITION CONTAINING SAME
20220241409 · 2022-08-04 ·

The present invention relates to a compound useful as a vaccine adjuvant for cancer vaccine, a preparation process thereof, a pharmaceutical composition comprising the compound, and use of the compound as a vaccine adjuvant for cancer vaccine.

WATER SOLUBLE ADJUVANT AND COMPOSITION CONTAINING SAME
20220241409 · 2022-08-04 ·

The present invention relates to a compound useful as a vaccine adjuvant for cancer vaccine, a preparation process thereof, a pharmaceutical composition comprising the compound, and use of the compound as a vaccine adjuvant for cancer vaccine.