Patent classifications
C07D277/42
Novel Bridged Bicycloalkyl-Substituted Aminothiazoles and Their Methods of Use
The present invention includes novel bridged bicycloalkyl-substituted aminothiazole compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
Novel Bridged Bicycloalkyl-Substituted Aminothiazoles and Their Methods of Use
The present invention includes novel bridged bicycloalkyl-substituted aminothiazole compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
CRYSTALLINE FORMS OF SELECTIVE S1P1 RECEPTOR MODULATOR AND PREPARATION METHOD THEREOF
The present disclosure relates to crystalline Form 1, Form 2, Form 3 of Ponesimod, a selective S1P1 receptor modulator, and preparation methods thereof. The X-ray powder diffraction pattern of Form 1 shows characteristic peaks at 2theta values of 18.10.2, 14.60.2, 11.30.2; the X-ray powder diffraction pattern of Form 2 shows characteristic peaks at 2theta values of 3.80.2, 10.80.2, 6.10.2; the X-ray powder diffraction pattern of Form 3 shows characteristic peaks at 2theta values of 12.20.2, 6.20.2, 5.60.2. The crystalline forms in present disclosure not only have better stability but also have higher solubility compared with the prior art forms, they are more suitable for the formulation development of Ponesimod.
CRYSTALLINE FORMS OF SELECTIVE S1P1 RECEPTOR MODULATOR AND PREPARATION METHOD THEREOF
The present disclosure relates to crystalline Form 1, Form 2, Form 3 of Ponesimod, a selective S1P1 receptor modulator, and preparation methods thereof. The X-ray powder diffraction pattern of Form 1 shows characteristic peaks at 2theta values of 18.10.2, 14.60.2, 11.30.2; the X-ray powder diffraction pattern of Form 2 shows characteristic peaks at 2theta values of 3.80.2, 10.80.2, 6.10.2; the X-ray powder diffraction pattern of Form 3 shows characteristic peaks at 2theta values of 12.20.2, 6.20.2, 5.60.2. The crystalline forms in present disclosure not only have better stability but also have higher solubility compared with the prior art forms, they are more suitable for the formulation development of Ponesimod.
Substituted aminothiazoles as DGKzeta inhibitors for immune activation
The present invention covers aminothiazole compounds of general formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGK?) regulated disorders, as a sole agent or in combination with other active ingredients.
Substituted aminothiazoles as DGKzeta inhibitors for immune activation
The present invention covers aminothiazole compounds of general formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and/or prophylaxis of diseases, in particular of diacylglycerol kinase zeta (DGK?) regulated disorders, as a sole agent or in combination with other active ingredients.
BENZENE RING COMPOUND AND USE THEREOF
The present invention relates to a benzene ring compound and a use thereof. In particular, provided is a compound as shown in formula I, or an optical isomer thereof or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof. The present compound has good therapeutic effects on tumors
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PI-kinase inhibitors with anti-infective activity
Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole or a 5-hetereoaryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
PI-kinase inhibitors with anti-infective activity
Compounds and methods are provided for the treatment of pathogen infections. In some embodiments, the anti-infective compounds have broad spectrum activity against a variety of infective diseases, where the diseases are caused by pathogens containing a basic amino acid PIP-2 pincer (BAAPP) domain that interacts with phosphatidylinositol 4,5-bisphosphate (PIP-2) to mediate pathogen replication. Also provided are methods of inhibiting a PI4-kinase and methods of inhibiting viral infection. In some embodiments, the compound is a PI4-kinase inhibiting compound that is a 5-aryl-thiazole or a 5-hetereoaryl-thiazole. The subject compounds may be formulated or provided to a subject in combination with a second anti-infective agent, e.g. interferon, ribivarin, and the like.
GP130 MODULATORS
There are provided, inter alia, compounds and methods useful for the treatment of neurological conditions, such as neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.