Substituted Isoindoline-1, 3-diketone PDE4 Inhibitor and Pharmaceutical Application Thereof
AssigneeSuzhou Intragrand Pharma Co., Ltd
InventorsJiawang ZHU, Yao YAO
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Abstract
The present disclosure relates to a compound as shown in formula I and its racemates, stereoisomers, tantomers, isotopic labels, solvates, polymorphs, esters, prodrugs or pharmaceutically acceptable salts as well as a pharmaceutical composition containing same, and preparation methods and medical uses thereof. The structure of formula I is as follows:
Claims8
A compound as shown in formula V and its racemates, stereoisomers, tautomers, isotopic labels, solvates, polymorphs, esters, prodrugs or pharmaceutically acceptable salts:
- wherein each R refers to the following groups unsubstituted or optionally substituted with one, two or more Ra:
- hydrocarbyl groups of C4-C10;
- Ra is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo;
- R1 refers to the following groups unsubstituted or optionally substituted with one, two or more R1a:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R2 refers to the following groups unsubstituted or optionally substituted with one, two or more R2a:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R3 refers to the following groups unsubstituted or optionally substituted with one, two or more R3a:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R4 refers to the following groups unsubstituted or optionally substituted with one, two or more R4a:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R1a is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), and the following groups unsubstituted or optionally substituted with one, two or more R1b:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R2a is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), and the following groups unsubstituted or optionally substituted with one, two or more R2b:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R3a is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), and the following groups unsubstituted or optionally substituted with one, two or more R3b:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R4a is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo, and the following groups unsubstituted or optionally substituted with one, two or more R4b:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R1b is selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), as well as hydrocarbyl groups of C1-C16, and heteroalkyl groups of C1-C16;
- R2b is selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), as well as hydrocarbyl groups of C1-C16, and heteroalkyl groups of C1-C16;
- R3b is selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo (═O), as well as hydrocarbyl groups of C1-C16, and heteroalkyl groups of C1-C16;
- R4b is selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo, as well as hydrocarbyl groups of C1-C16, and heteroalkyl groups of C1-C16;
- the hydrocarbyl groups are alkanes, alkenes, and alkynes;
- and the oxo is =O.
A compound as shown in formula VI and its racemates, stereoisomers, tautomers, isotopic labels, solvates, polymorphs, esters, prodrugs or pharmaceutically acceptable salts:
- wherein R4 refers to the following groups unsubstituted or optionally substituted with one, two or more R4a:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- R4a is independently selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo, and the following groups unsubstituted or optionally substituted with one, two or more R4b:
- hydrocarbyl groups of C1-C16, heteroalkyl groups of C1-C16, and cycloalkyl groups of C3-C12;
- and
- R4b is selected from deuterium, halogen, amino, hydroxyl, cyano, nitro, oxo, as well as hydrocarbyl groups of C1-C16, and heteroalkyl groups of C1-C16;
- the hydrocarbyl groups are alkanes, alkenes, and alkynes.
Dependencies are inferred from the claim text.