Patent classifications
A61P11/14
CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES AS DIPEPTIDYL PEPTIDASE 1 INHIBITORS
The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),
##STR(I)##
that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD) , to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
AMINO QUINAZOLINE DERIVATIVES AS P2X3 INHIBITORS
The present invention relates to compounds of formula I inhibiting P2X purinoceptor 3; particularly the invention relates to compounds that are amino quinazoline derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. The compounds of the invention may be useful in the treatment of many disorders associated with P2X.sub.3 receptors mechanisms, such as respiratory diseases including cough, asthma, idiopathic pulmonary fibrosis (IPF) and chronic obstructive pulmonary disease (COPD).
URACIL DERIVATIVES AS TRPA1 INHIBITORS
The present disclosure provides certain uracil derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
IMIDAZO[4,5-D]PYRIDAZINONYL DERIVATIVES AS TRPA1 INHIBITORS
The present disclosure provides certain imidazo[4,5-d]pyridazinonyl derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
3H,4H-THIENO[2,3-D]PYRIMIDIN-4-ONE DERIVATIVES AS TRPA1 INHIBITORS
The present disclosure provides certain 3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
3H,4H,5H,6H,7H-PYRIMIDO[4,5-B][1,4]OXAZINE-4,6-DIONE DERIVATIVES AS TRPA1 INHIBITORS
The present disclosure provides certain 3H,4H,5H,6H,7H-pyrimido[4,5-b][1,4]oxazine-4,6-dione derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
Compounds, compositions and methods
The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II. ##STR00001##
Compounds, compositions and methods
The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One particular crystalline form, Form II, has been found to be more thermodynamically stable and, thus, likely more suitable for bulk preparation and handling than other polymorphic forms. Efficient and economic methods have been developed to prepare Compound (I) and Form II in high purity on a large scale. In animal studies, Form II has demonstrated safety and efficacy in treating depressive disorders and, when micronized, improved absorption compared to non-micronized Form II. ##STR00001##
APPLICATION OF TRADITIONAL CHINESE MEDICINE COMPOSITION IN PREPARATION OF DRUGS FOR TREATING OR PREVENTING CORONAVIRUS INFECTION
An application of a traditional Chinese medicine composition in preparing a medicine for treating or preventing coronavirus infection. The traditional Chinese medicine composition is characterized by being prepared from the following raw materials in parts by weight: 5-15 parts of Cornu saigae tataricae or 50-150 parts of goral horns, 10-60 parts of Bulbus Fritillariae Ussuriensis, 15-60 parts of Radix et Rhizoma Rhei, 7-30 parts of Radix scutellariae, 7-30 parts of Lapis Chloriti, 10-50 parts of gypsum fibrosum, 5-20 parts of calculus bovis artifactus, and 15-60 parts of radix glycyrrhizae. The traditional Chinese medicine composition can inhibit 2019-nCoV replication in cells, so that cells infected by 2019-nCoV viruses have no lesion. Therefore, the traditional Chinese medicine composition can treat or prevent coronavirus related diseases.
PHARMACEUTICAL SYRUP FORMULATION OR SUSPENSION
A stable pharmaceutical formulation or suspension has a pharmaceutical active agent, agave, and a dilutant. The formulation or suspension has viscosity suitable for drinking.