C07D239/95

QUINAZOLINE PRODRUGS FOR THE TREATMENT OF VIRAL INFECTIONS AND FURTHER DISEASES
20220324817 · 2022-10-13 ·

Provided herein are compounds of formula (I), pharmaceutical compositions comprising such compounds, and methods of using such compounds through induction of the T helper 1 (Th1) immune response to treat infections, diseases, and disorders. The compounds disclosed herein may also be considered prodrugs and vaccine adjuvants.

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SMALL MOLECULES FOR THE TREATMENT OF AUTOIMMUNE DISEASES AND CANCER

Disclosed herein are quinazolinyl compounds, compositions, and methods of use thereof. The compounds may be used in the treatment of autoimmune disorders or cancer.

COMPOSITIONS AND METHODS FOR TREATING CANCER

The present disclosure relates to compounds that are capable of penetrating the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating glioblastoma and other EGFR-mediated cancers, such as those that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.

COMPOSITIONS AND METHODS FOR TREATING CANCER

The present disclosure relates to compounds that are capable of penetrating the blood brain barrier to modulate the activity of EGFR tyrosine kinase. The disclosure further relates to methods of treating glioblastoma and other EGFR-mediated cancers, such as those that have been determined to have altered glucose metabolism in the presence of inhibitors. The present disclosure also provides methods of administering to a subject a glucose metabolism inhibitor and a cytoplasmic p53 stabilizer.

AUTOMATED MICROREACTOR FOR EFFECTIVE OPTIMIZATION OF HIGH-SPEED CHEMICAL REACTION, AND METHOD OF OPTIMIZING HIGH-SPEED CHEMICAL REACTION THEREFOR
20230110331 · 2023-04-13 ·

Proposed are an automated microreactor for effective optimization of a high-speed chemical reaction, and a method of optimizing a high-speed chemical reaction using the same. The automated microreactor includes a raw material supply unit including a plurality of flow rate controllers that supply a plurality of raw materials and control flow rates of the plurality of raw materials, an intermediate reaction unit including a plurality of micromixers for intermediate that generate a first mixture and a plurality of tubular reactors for intermediate that generate an intermediate product, an intermediate reaction control unit including a valve member, and a product reaction unit including a product micromixer that produces a second mixture and producing a product, through which optimal synthesis conditions (optimal temperature, flow rate, reaction volume and organolithium reagent type) can be achieved to obtain the highest yield in a short time.

AUTOMATED MICROREACTOR FOR EFFECTIVE OPTIMIZATION OF HIGH-SPEED CHEMICAL REACTION, AND METHOD OF OPTIMIZING HIGH-SPEED CHEMICAL REACTION THEREFOR
20230110331 · 2023-04-13 ·

Proposed are an automated microreactor for effective optimization of a high-speed chemical reaction, and a method of optimizing a high-speed chemical reaction using the same. The automated microreactor includes a raw material supply unit including a plurality of flow rate controllers that supply a plurality of raw materials and control flow rates of the plurality of raw materials, an intermediate reaction unit including a plurality of micromixers for intermediate that generate a first mixture and a plurality of tubular reactors for intermediate that generate an intermediate product, an intermediate reaction control unit including a valve member, and a product reaction unit including a product micromixer that produces a second mixture and producing a product, through which optimal synthesis conditions (optimal temperature, flow rate, reaction volume and organolithium reagent type) can be achieved to obtain the highest yield in a short time.

SELECTIVE NON-CYCLIC NUCLEOTIDE ACTIVATORS FOR THE CAMP SENSOR EPAC1

The invention relates generally to novel EPAC1 activators, such as Formula I and II and the preparation thereof as well as the use of EPAC1 activators disclosed herein as to selectively activate EPAC1 in cells.

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MASP-2 INHIBITORS AND METHODS OF USE

The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds and methods of making and using such compounds.

Substituted quinazolines as inhibitors of KRAS G12C

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R.sup.1, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Substituted quinazolines as inhibitors of KRAS G12C

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): ##STR00001##
or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R.sup.1, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, G.sup.1, G.sup.2, L.sup.1, L.sup.2, m.sup.1, m.sup.2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.