C07F9/65583

PROCESSES FOR PREPARING PHOSPHORODIAMIDATE MORPHOLINO OLIGOMERS

Provided herein are processes for preparing an oligomer (e.g., a morpholino oligomer). The synthetic processes described herein may be advantageous to scaling up oligomer synthesis while maintaining overall yield and purity of a synthesized oligomer.

NEW-TYPE OXAZOLIDINONE COMPOUNDS AND PREPARATION METHOD THEREFOR

Oxazolidinones having structures represented by structural formula I, preparation methods therefor, and pharmaceutical uses thereof, in particular an application of said compounds and salts or compositions thereof in the treatment of a bacterial infection. In the formula: R.sup.1 is a methyl group, an ethyl group, a propyl group, a cyclopropyl group, or a vinyl group; R.sup.2 is F; and R.sup.3 is F, CH.sub.3, C.sub.2H.sub.5, CF.sub.3, CHF.sub.2, CH.sub.2F, or a cyclopropyl group.

Nucleic acid-polypeptide compositions and uses thereof

Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.

PHOSPHATE DERIVATIVES OF RORGAMMA MODULATORS AND USES THEREOF

The present invention relates to phosphate derivatives of formula (I), and their therapeutic uses, preferably for treating a respiratory disease. The present invention further relates to pharmaceutical compositions and devices comprising such compounds.

TETRA- AND PENTASUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS USEFUL IN THE TREATMENT OF RESPIRATORY DISEASES
20180002312 · 2018-01-04 ·

The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z have one of the meanings as defined in the specification, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).

##STR00001##

N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamides useful as CCR6 inhibitors

The present invention relates to N-substituted-dioxocyclobutenylamino-3-hydroxy-picolinamide compounds of Formulae (IA and 1B) ##STR00001##
or a pharmaceutically acceptable salt or hydrate thereof, that inhibit CC chemokine receptor 6 (CCR6), pharmaceutical compositions containing these compounds, and the use of these compounds for treating or preventing diseases, conditions, or disorders ameliorated by inhibition of CCR6.

Aryl, heteroaryl, and heterocyclic pharmaceutical compounds for treatment of medical disorders

Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Protease inhibitors for treatment of coronavirus infections

Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4, R.sup.5, and A are defined in the present disclosure. The compounds are potent inhibitors of the main protease (M.sup.pro) of severe acute respiratory syndrome Coronavirus-2 (SARS-CoV-2), and they are useful in treating or preventing COVID-19 in a subject.

Phenylpyrrolidinone formyl peptide 2 receptor agonists

The disclosure relates to compounds of Formulae (I)-(IX), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases. ##STR00001##

NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF

Disclosed herein are compositions and pharmaceutical formulations that comprise a binding moiety conjugated to a modified polynucleic acid molecule and a polymer. Also described herein include methods for treating a cancer which utilize a composition or a pharmaceutical formulation comprising a binding moiety conjugated to a polynucleic acid molecule and a polymer.