Patent classifications
C07D217/24
FUSED RING COMPOUND AND APPLICATION THEREOF
Disclosed is a fused ring compound and an application thereof. Disclosed is a fused ring compound represented by formula I, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, an isotope compound, a crystal form, a nitrogen oxide, a solvate, or a solvate of the pharmaceutically acceptable salt thereof. The fused ring compound of the present invention has high P2X4 antagonistic activity, excellent selectivity, low toxicity and excellent metabolic stability.
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MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I′): where the substituents R.sup.1, R.sup.2, R.sup.2′, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein and where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R′, R″, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
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BICYCLIC COMPOUNDS
Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
7- OR 8-HYDROXY-ISOQUINOLINE AND 7- OR 8-HYDROXY-QUINOLINE DERIVATIVES AS ALPHA-1-ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1-ANTITRYPSIN DEFICIENCY (AATD)
- Simon Giroux ,
- Michael Philip CLARK ,
- Michael Aaron Brodney ,
- Peter Jones ,
- Michael Paul DENINNO ,
- Wenxin Gu ,
- Qing TANG ,
- Steven David STONE ,
- Timothy J. Senter ,
- Zachary GALE-DAY ,
- 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
7- or 8-hydroxy-isoquinoline and 7- or 8-hydroxy-quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD).
7- OR 8-HYDROXY-ISOQUINOLINE AND 7- OR 8-HYDROXY-QUINOLINE DERIVATIVES AS ALPHA-1-ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1-ANTITRYPSIN DEFICIENCY (AATD)
- Simon Giroux ,
- Michael Philip CLARK ,
- Michael Aaron Brodney ,
- Peter Jones ,
- Michael Paul DENINNO ,
- Wenxin Gu ,
- Qing TANG ,
- Steven David STONE ,
- Timothy J. Senter ,
- Zachary GALE-DAY ,
- 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
7- or 8-hydroxy-isoquinoline and 7- or 8-hydroxy-quinoline derivatives as alpha-1-antitrypsin modulators for treating alpha-1-antitrypsin deficiency (AATD).
Methods and Compositions for Targeting Tregs using CCR8 Inhibitors
The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.
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Tetrahydroisoquinoline compounds
The present invention relates to a novel class of tetrahydroisoquinoline compounds of formula I and to compositions comprising the same. The compounds and compositions of the present invention can be used as medicaments in the treatment of cancer. ##STR00001##
BROMODOMAIN INHIBITORS
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
BROMODOMAIN INHIBITORS
The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.
ISOQUINOLINONE COMPOUND FOR INHIBITING SSAO/VAP-1, AND USE THEREOF
An isoquinolinone compound acts as an inhibitor of semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1), and the use thereof, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be used to prepare a drug for preventing, treating or ameliorating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases in patients, and especially can be used to prepare a drug for preventing, treating or ameliorating non-alcoholic fatty liver diseases in patients.