Patent classifications
C07D209/18
HETEROCYCLIC COMPOUND, INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound has a high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
##STR00001##
HETEROCYCLIC COMPOUND, INTERMEDIATE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Disclosed by the invention is a heterocyclic compound, an intermediate, and a preparation method therefor and an application thereof. Provided by the invention are a heterocyclic compound as shown in formula I, and a stereoisomer, a geometric isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, an ester, a pharmaceutically acceptable salt or a prodrug thereof. The heterocyclic compound has a high P2X3 antagonistic activity, and has good selectivity, low toxicity, good metabolic stability and little taste influence.
##STR00001##
INDOLE DERIVATIVES AS ALPHA-1-ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1-ANTITRYPSIN DEFICIENCY (AATD)
- Simon Giroux ,
- Michael Philip CLARK ,
- Michael Aaron Brodney ,
- Philippe Marcel Nuhant ,
- Emily Elizabeth ALLEN ,
- Robert Francis FIMOGNARI, Jr. ,
- Mariam ZAKY ,
- Michael John BOYD ,
- David D. DEININGER ,
- Hu ZHANG ,
- Hongbo DENG ,
- Philip Noel COLLIER ,
- Brad MAXWELL ,
- Nathan D. WAAL ,
- Steven M. RONKIN ,
- Jian Wang ,
- Qing TANG ,
- Gabrielle Simone FLEMING ,
- Peter Jones ,
- Diane Marie BOUCHER ,
- Lev T.D. FANNING ,
- Amy B. HALL ,
- Dennis James HURLEY ,
- Mac Arthur Johnson, Jr. ,
- John Patrick Maxwell ,
- Rebecca Jane SWETT ,
- Timothy Lewis TAPLEY ,
- Stephen A. THOMSON ,
- Veronique DAMAGNEZ ,
- Kevin Michael Cottrell ,
- Upul Keerthi BANDARAGE
Indole derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD).
INDOLE DERIVATIVES AS ALPHA-1-ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1-ANTITRYPSIN DEFICIENCY (AATD)
- Simon Giroux ,
- Michael Philip CLARK ,
- Michael Aaron Brodney ,
- Philippe Marcel Nuhant ,
- Emily Elizabeth ALLEN ,
- Robert Francis FIMOGNARI, Jr. ,
- Mariam ZAKY ,
- Michael John BOYD ,
- David D. DEININGER ,
- Hu ZHANG ,
- Hongbo DENG ,
- Philip Noel COLLIER ,
- Brad MAXWELL ,
- Nathan D. WAAL ,
- Steven M. RONKIN ,
- Jian Wang ,
- Qing TANG ,
- Gabrielle Simone FLEMING ,
- Peter Jones ,
- Diane Marie BOUCHER ,
- Lev T.D. FANNING ,
- Amy B. HALL ,
- Dennis James HURLEY ,
- Mac Arthur Johnson, Jr. ,
- John Patrick Maxwell ,
- Rebecca Jane SWETT ,
- Timothy Lewis TAPLEY ,
- Stephen A. THOMSON ,
- Veronique DAMAGNEZ ,
- Kevin Michael Cottrell ,
- Upul Keerthi BANDARAGE
Indole derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD).
COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH
The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia.
Water soluble novel cyanine fluorophore with tunable properties between near IR and SWIR region for in vivo imaging
Cyanine fluorophores including a nine-carbon polymethine bridge are disclosed. The cyanine fluorophores have absorbance and/or emission maxima in the near-infrared (NIR) and short-wave infrared (SWIR) wavelength ranges. Methods of making and using the cyanine fluorophores are also disclosed. The compounds are useful in fluorescence imaging, more particularly in cancer treatment. The compounds have generic formula (I): ##STR00001##
Water soluble novel cyanine fluorophore with tunable properties between near IR and SWIR region for in vivo imaging
Cyanine fluorophores including a nine-carbon polymethine bridge are disclosed. The cyanine fluorophores have absorbance and/or emission maxima in the near-infrared (NIR) and short-wave infrared (SWIR) wavelength ranges. Methods of making and using the cyanine fluorophores are also disclosed. The compounds are useful in fluorescence imaging, more particularly in cancer treatment. The compounds have generic formula (I): ##STR00001##
Indole carboxamide compounds
Disclosed are compounds of Formula (I): ##STR00001##
or a salt thereof, wherein: X is CR.sub.4 or N; R.sub.1, R.sub.2, R.sub.3, R.sub.4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Indole carboxamide compounds
Disclosed are compounds of Formula (I): ##STR00001##
or a salt thereof, wherein: X is CR.sub.4 or N; R.sub.1, R.sub.2, R.sub.3, R.sub.4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
PPARG Modulators for the Treatment of Osteoporosis
The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.