C07D451/02

NOVEL LXR MODULATORS WITH BICYCLIC CORE MOIETY

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRα and/or LXKβ) and act preferably as inverse agonists of LXR.

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NOVEL LXR MODULATORS WITH BICYCLIC CORE MOIETY

The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRα and/or LXKβ) and act preferably as inverse agonists of LXR.

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N-PHENYLAMINOCARBONYL PYRIDINO-, PYRIMIDINO AND BENZO-TROPANES AS MODULATORS OF GPR65

One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5 or 6 membered aromatic or heteroaromatic ring, wherein said aromatic or heteroaromatic ring is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, and aralkyl; Y is selected from C═N—OH and CR10R.sub.10′, wherein R.sub.10 and R.sub.10′, are each independently selected from H, F, alkyl, and haloalkyl; R.sub.1, R.sub.4, and R.sub.5 are each independently selected from H, F, Cl, Br, and I; R.sub.2 and R.sub.3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, and haloalkyl; and R.sub.11 and R.sub.11′ wherein R.sub.12 and R.sub.13 are both alkyl; for use as a medicament. Further aspects of the invention relate to compounds of formula (I) for use in the field of immuno-oncology, immunology, and related applications, and compounds of formula (I) per se.

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N-PHENYLAMINOCARBONYL PYRIDINO-, PYRIMIDINO AND BENZO-TROPANES AS MODULATORS OF GPR65

One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring A is a 5 or 6 membered aromatic or heteroaromatic ring, wherein said aromatic or heteroaromatic ring is optionally substituted with one or more substituents selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from F, Cl, Br, I, CN, alkoxy, NR.sub.11R.sub.11′, OH, alkyl, haloalkyl, and aralkyl; Y is selected from C═N—OH and CR10R.sub.10′, wherein R.sub.10 and R.sub.10′, are each independently selected from H, F, alkyl, and haloalkyl; R.sub.1, R.sub.4, and R.sub.5 are each independently selected from H, F, Cl, Br, and I; R.sub.2 and R.sub.3 are each independently selected from H, F, Cl, Br, I, CN, methoxy, and haloalkyl; and R.sub.11 and R.sub.11′ wherein R.sub.12 and R.sub.13 are both alkyl; for use as a medicament. Further aspects of the invention relate to compounds of formula (I) for use in the field of immuno-oncology, immunology, and related applications, and compounds of formula (I) per se.

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SUBSTITUTED BENZENECARBOXAMIDES AS IL-17A MODULATORS

The disclosure herein provides compounds and pharmaceutical compositions of the structure of Formula I:

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for the modulation of IL-17A, useful for the treatment of inflammatory conditions, such as psoriasis.

Method for preparing a non-radioactive standard β-CFT

This invention discloses method for preparing a non-radioactive standard β-CFT. Using cocaine hydrochloride as the starting material, and after a series of hydrolysis, dehydration, esterification and bonding reactions, a non-radioactive standard (2β-Carbomethoxy-3β-(4-fluoropenyl) tropane) is prepared. Furthermore, this preparation method has fewer steps, is easy to operate, and the purity of the product is as high as 97.97%. Therefore, the method for preparing a non-radioactive standard β-CFT can promote the development of positron imaging in the diagnosis of Parkinson's disease.

Method for preparing a non-radioactive standard β-CFT

This invention discloses method for preparing a non-radioactive standard β-CFT. Using cocaine hydrochloride as the starting material, and after a series of hydrolysis, dehydration, esterification and bonding reactions, a non-radioactive standard (2β-Carbomethoxy-3β-(4-fluoropenyl) tropane) is prepared. Furthermore, this preparation method has fewer steps, is easy to operate, and the purity of the product is as high as 97.97%. Therefore, the method for preparing a non-radioactive standard β-CFT can promote the development of positron imaging in the diagnosis of Parkinson's disease.

Methods and compositions for modulating splicing

Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.