Patent classifications
C07D217/24
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.
Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, 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.
Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, 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.
Ion Channel Antagonists/Blockers and Uses Thereof
Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.
##STR00001##
Ion Channel Antagonists/Blockers and Uses Thereof
Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.
##STR00001##
MRGPRX2 ANTAGONIST FOR THE TREATMENT OF PSEUDO ALLERGIC REACTIONS
Compounds that have antiallergic and/or anti-inflammatory properties and methods of making thereof are disclosed. These compounds can block MMRGPRX2 and prevent or reduce mast cells activation. Pharmaceutical formulations in a unit dosage form suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical formulations may include one or more active agents in addition to the compounds, such as one or more additional antiallergic and/or anti-inflammatory agents. The pharmaceutical formulation can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. Methods for preventing or treating pseudo allergic reactions, pseudo allergic diseases, and/or pseudo inflammatory diseases, or treating or ameliorating one or more symptoms associated with a pseudo allergic reaction, a pseudo allergic disease, and/or a pseudo inflammatory disease in a subject are also disclosed.
MRGPRX2 ANTAGONIST FOR THE TREATMENT OF PSEUDO ALLERGIC REACTIONS
Compounds that have antiallergic and/or anti-inflammatory properties and methods of making thereof are disclosed. These compounds can block MMRGPRX2 and prevent or reduce mast cells activation. Pharmaceutical formulations in a unit dosage form suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical formulations may include one or more active agents in addition to the compounds, such as one or more additional antiallergic and/or anti-inflammatory agents. The pharmaceutical formulation can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. Methods for preventing or treating pseudo allergic reactions, pseudo allergic diseases, and/or pseudo inflammatory diseases, or treating or ameliorating one or more symptoms associated with a pseudo allergic reaction, a pseudo allergic disease, and/or a pseudo inflammatory disease in a subject are also disclosed.
INHIBITORS OF ALPHA 2 BETA 1 INTEGRIN AND METHODS OF USE THEREOF
Disclosed herein, inter alia, are inhibitors of alpha 2 beta 1 integrin and methods of using the same.
COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).
COMPOUNDS FOR THE TREATMENT OF PARAMYXOVIRUS VIRAL INFECTIONS
Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).