Patent classifications
A61K31/40
5-membered heteroaryl carboxamide compounds for treatment of HBV
The present disclosure provides, in part, 5-membered heteroaryl carboxamide compounds, and pharmaceutical compositions thereof, useful for disruption of HBV core protein assembly, and methods of treating Hepatitis B (HBV) infection.
Bicyclic-fused heteroaryl or aryl compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Bicyclic-fused heteroaryl or aryl compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, ##STR00001##
as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1-AMINOSULFONYL-2-CARBOXYPYRROLE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS
This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.
##STR00001##
1-AMINOSULFONYL-2-CARBOXYPYRROLE DERIVATIVES AS METALLO-BETA-LACTAMASE INHIBITORS
This invention relates to compounds of formula (I) and methods of treatment using the compounds. The compounds of the invention can be used in combination with antibacterial agents to treat bacterial infections. More specifically, the compounds of formula (I) can be used in combination with a class of antibacterial agents known as carbapenems. The novel compounds of the present invention are enzyme inhibitors and more particularly are metallo-β-lactamase inhibitors.
##STR00001##
Method of determining composition effective for treating diabetes
The treatment of diabetes mellitus with excellent hypoglycemic effect that suppresses lactic acidosis without substantially increasing the blood lactate concentration. A composition for treating diabetes mellitus with hypoglycemic effect that suppresses lactic acidosis without substantially increasing the blood lactate concentration, and the composition has branched-chain amino acids and salts of biguanide derivatives and derivatives of biguanide derivatives or branched-chain amino acids as the active components. The composition will be more effective when leucine, isoleucine, or valine is included as branched-chain amino acids, and metformin as the biguanide derivative.
Method of determining composition effective for treating diabetes
The treatment of diabetes mellitus with excellent hypoglycemic effect that suppresses lactic acidosis without substantially increasing the blood lactate concentration. A composition for treating diabetes mellitus with hypoglycemic effect that suppresses lactic acidosis without substantially increasing the blood lactate concentration, and the composition has branched-chain amino acids and salts of biguanide derivatives and derivatives of biguanide derivatives or branched-chain amino acids as the active components. The composition will be more effective when leucine, isoleucine, or valine is included as branched-chain amino acids, and metformin as the biguanide derivative.
ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V). wherein, X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, R.sup.2a, R.sup.13, R.sup.13a, R.sup.23, R.sup.23a, R.sup.23b, R.sup.33, R.sup.33a, R.sup.33b, R.sup.43, R.sup.43a, R.sup.51, R.sup.53, R.sup.53a, R.sup.53b, bond “a”, and subscript n are described herein.
ARYL-ANILINE AND HETEROARYL-ANILINE COMPOUNDS FOR TREATMENT OF BIRTHMARKS
Provided herein are compounds and pharmaceutical compositions thereof for treating a birthmark in a subject in need thereof, wherein the compound is according to any one of formula (I), (II), (III), (IV), and (V). wherein, X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2, R.sup.2a, R.sup.13, R.sup.13a, R.sup.23, R.sup.23a, R.sup.23b, R.sup.33, R.sup.33a, R.sup.33b, R.sup.43, R.sup.43a, R.sup.51, R.sup.53, R.sup.53a, R.sup.53b, bond “a”, and subscript n are described herein.
INHALED STATINS AS BRONCHODILATORS TO IMPROVE LUNG FUNCTION IN RESPIRATORY DISEASES
present disclosure relates to methods for relaxing airway smooth muscle tissue, alleviating or preventing bronchospasm, and treating lung diseases by administering an HMG-CoA reductase inhibitor (statin) directly to lung tissue by inhalation. The disclosure also relates to formulations and compositions useful for the practice of methods of the disclosure.