C07D409/02

Oxa spiro derivative, preparation method therefor, and applications thereof in medicines

The present invention relates to an oxa spiro derivative, a preparation method therefor, and applications thereof in medicines. Particularly, the present invention relates to an oxa spiro derivative represented by formula (I), a preparation method therefor, and a pharmaceutical composition comprising the derivative, applications thereof as an MOR receptor agonist, and applications in the preparation of drugs for treating and/or preventing pains and pains-related diseases. Substituent groups in the formula (I) are same as definitions in the specification. ##STR00001##

TRICYCLIC HETEROCYCLIC DERIVATIVES AND USES THEREOF

Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.

TRICYCLIC HETEROCYCLIC DERIVATIVES AND USES THEREOF

Disclosed are tricyclic heterocyclic compounds having kinase inhibitory activity, pharmaceutical compositions and kits comprising the compounds, and use of the compounds in the treatment of or in medicaments for the treatment of various diseases and conditions. In particular, disclosed are tricyclic heterocyclic compounds of the formula (I) having CSF-1R (c-FMS kinase) inhibitory activity and their use in the treatment of various diseases and conditions, such as those mediated by CSF-1R, including proliferative or neoplastic diseases and conditions, including cancers, and bone, inflammatory, and autoimmune diseases and conditions.

4-METHYLSULFONYL-SUBSTITUTED PIPERIDINE UREA COMPOUNDS

The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

4-METHYLSULFONYL-SUBSTITUTED PIPERIDINE UREA COMPOUNDS

The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

SUBSTITUTED BENZOTHIOPHENYL DERIVATIVES AS GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows:

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, W, and A are defined herein.

SUBSTITUTED BENZOTHIOPHENYL DERIVATIVES AS GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows:

##STR00001##

wherein R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, W, and A are defined herein.

METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.

Substituted benzothiophenyl derivatives as GPR40 agonists for the treatment of type II diabetes

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: ##STR00001##
wherein R.sub.1, R.sub.2, R.sub.3, R.sub.5, R.sub.6, W, and A are defined herein.