C07D317/68

T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
20180003702 · 2018-01-04 ·

The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

T1R HETERO-OLIGOMERIC TASTE RECEPTORS, CELL LINES THAT EXPRESS SAID RECEPTORS, AND TASTE COMPOUNDS
20180003702 · 2018-01-04 ·

The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

LEFT-HANDED BICYCLIC MORPHOLINE AND SALT THEREOF, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USE

The invention relates to the field of pharmaceutical chemistry, and it particularly relates to a left-handed bicyclic morpholine and a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and use thereof in the preparation of medicaments for preventing and/or treating liver diseases and the like.

LEFT-HANDED BICYCLIC MORPHOLINE AND SALT THEREOF, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USE

The invention relates to the field of pharmaceutical chemistry, and it particularly relates to a left-handed bicyclic morpholine and a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and use thereof in the preparation of medicaments for preventing and/or treating liver diseases and the like.

Taste Modifying Compositions and Uses Thereof

The present disclosure generally relates to various formulations and uses of the compound: N-(heptan-4-yl)benzo[d] [1,3]dioxole-5-carboxamide, which is also referred to herein a “TM1” and comestibly acceptable salts thereof. In some aspects, the disclosure provides compositions that include TM1, or a comestibly acceptable salt thereof. In some embodiments, the compositions are ingestible compositions, including, but not limited to, packaged food and beverage products. In some other aspects, the disclosure provides methods of reducing the caloric content of a flavored article, for example, by reducing the amount of caloric sweeteners, fatty products (such as cheese). In some other aspects, the disclosure provides methods of reducing the amount of monosodium glutamate (MSG).

Taste Modifying Compositions and Uses Thereof

The present disclosure generally relates to various formulations and uses of the compound: N-(heptan-4-yl)benzo[d] [1,3]dioxole-5-carboxamide, which is also referred to herein a “TM1” and comestibly acceptable salts thereof. In some aspects, the disclosure provides compositions that include TM1, or a comestibly acceptable salt thereof. In some embodiments, the compositions are ingestible compositions, including, but not limited to, packaged food and beverage products. In some other aspects, the disclosure provides methods of reducing the caloric content of a flavored article, for example, by reducing the amount of caloric sweeteners, fatty products (such as cheese). In some other aspects, the disclosure provides methods of reducing the amount of monosodium glutamate (MSG).

AN EFFICIENT PROCESS FOR THE SYNTHESIS OF ALKOXY SUBSTITUTED BENZALDEHYDES

The present invention relates to the synthesis of alkoxy substituted benzaldehydes obtained from the corresponding alkoxy substituted benzenes. Alkoxy substituted benzaldehydes are products of broad commercial interest and are used as end products and intermediates in flavor and fragrance applications and pharmaceutical ingredients. For example, 3,4-methylendioxy-benzaldehyde (also known as heliotropin or piperonal) is used widely both as a end product and intermediate for the above mentioned applications. Other examples include 3,4-dimethoxybenzaldehyde, 3,4,5-trimethoxybenzaldehyde and 3,4-ethylenedioxybenzene which are intermediates in the synthesis of active pharmaceutical intermediates.

Alpha-cinnamide compounds and compositions as HDAC8 inhibitors

The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

Alpha-cinnamide compounds and compositions as HDAC8 inhibitors

The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.

SANGUINARINE ANALOG PP2C INHIBITORS FOR CANCER TREATMENT

Sanguinarine analogs as PP2C inhibitors are disclosed for the treatment of various cancers, as well as methods of synthesizing such analogs.