Abstract: The present disclosure relates to a novel PLK1 degradation inducing compound having a structure according to Formula I, a method for preparing the same, and the use thereof. The compounds of the present disclosure exhibit an effect of inducing PLK1 degradation. Therefore, the compounds of the present disclosure may be effectively utilized for preventing or treating PLK1-related diseases.

Abstract: The invention relates to substituted pyrridinobenzodiazepines (PDDs) of formula (XV) and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.

Abstract: Disclosed herein are salt and solid forms of tabernanthalog. Disclosed solid forms may be a polymorph of tabernanthalog fumarate, and/or may have improved properties, such as improved physical, chemical and/or pharmacokinetic properties. Disclosed salts include pharmaceutically acceptable salts of tabernanthalog. Disclosed solid forms include free base and salt forms of tabernanthalog, including amorphous and crystalline forms of tabernanthalog, such as tabernanthalog free base or a salt thereof. Also disclosed are methods for making the salts and solid forms and methods for administering the same. The salt and solid forms of tabernanthalog and salts thereof are useful for treating neurological disease and/or a psychiatric disorder in a subject.

Abstract: Pyrido[3,4-b]indole-3-carboxylic acid compounds are provided. The pyrido[3,4-b]indole-3-carboxylic acid compounds have the formula I: wherein Ring A, R1, R2, R3, and R4 are as described herein. The pyrido[3,4-b]indole-3-carboxylic acid compounds inhibit protein kinase CK2 activity and may be used as anticancer and/or antitumor agents, as well as agents for treating inflammation, pain, immunological disorders, diabetes, viral infections, and neurodegenerative diseases.

Abstract: Pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds are provided. The pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds have the general formula: where R1 is H, C1-C6 alkyl, or C3-C6 cycloalkyl, and R2 is C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 cyanoalkyl, (CH2)2-3NR3R4, (CH2)1-2aryl, (CH2)1-2heteroaryl, C(O)—(CH2)2-3NR3R4, C(O)aryl, C(O)heteroaryl, S(O)2—(CH2)2-3NR3R4, S(O)2aryl, S(O)2heteroaryl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C3-C6 cyanocycloalkyl, aryl, or 5- or 6-membered heteroaryl. The pyrrolo[2,3-c[2,7]naphthyridine-2-carboxylic acid compounds inhibit protein kinase CK2 activity and may be used as anticancer agents, as well as agents for treating inflammation, pain, immunological disorders, diabetes, viral infections, and neurodegenerative diseases.

Abstract: Pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds are provided. The pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds have the general formula: where R1 is H, C1-C6 alkyl, or C3-C6 cycloalkyl, and R2 is C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 cyanoalkyl, (CH2)2-3NR3R4, (CH2)1-2aryl, (CH2)1-2heteroaryl, C(O)—(CH2)2-3NR3R4, C(O)aryl, C(O)heteroaryl, S(O)2—(CH2)2-3NR3R4, S(O)2aryl, S(O)2heteroaryl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C3-C6 cyanocycloalkyl, aryl, or 5- or 6-membered heteroaryl. The pyrrolo[2,3-c][2,7]naphthyridine-2-carboxylic acid compounds inhibit protein kinase CK2 activity and may be used as anticancer agents, as well as agents for treating inflammation, pain, immunological disorders, diabetes, viral infections, and neurodegenerative diseases.

Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Disclosed herein are analogues of 6-(4-((2,3-dihydrobenzo[b][1,4]dioxin-6-yl)oxy)piperidin-1 -yl)-[1,2,4]triazolo[4,3-b]pyridazine of formula (Ib), which may be useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

Abstract: Pyrido[3?,4?:4,5]pyrrolo[2,3-c]quinolone compounds are provided. The pyrido[3?,4?:4,5]pyrrolo[2,3-c]quinolone compounds have the general formula: where R1 is H, C(O)OH4, O or OH: R2 is H, C(O)OH, C(O)OR4, or OH: and R3 is C—C6 alkyl, C1-C6 haloalkyl, C1-C6 cyanoalkyl, (CH2)2-3NR7R8, (CH2)1-2aryl, (CH2)1-2heteroaryl, C(O)—(CH2)2-3NR7R8, C(O)aryl, C(O)heteroaryl, NH(CH2)2-3NR7R8, NH(CH2)0-1aryl, NH(CH2)0-1heteroaryl, NHC(O)—(CH2)2-3NR7R sNHC(O)aryl, NHC(O)heteroaryl, NHS(o)2-(CH2)2-3NR7R8, NHS(O)2aryl, NHS(O)2heteroaryl, S(O)2—(CH2)2-3NR7R8, S(O)2aryl, S(O)2heteroaryl, C3-C6 cycloalyl, C3-C6 halocycloalyl, C3-C6 cyanoccloalyl, aryl, or 5- or 6-membered heteroaryl. The compounds are inhibitors of protein kinase CK2 activity.

Abstract: The present disclosure provides certain substituted 1,2,4-oxadiazole derivatives of the below formula (I) that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, 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.

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

Abstract: Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

Abstract: The present invention relates to novel solid forms of compound (I), 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methyl-phenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethyl-propanoic acid and pharmaceutical compositions comprising solid forms thereof disclosed herein, which can be used as a HBV capsid inhibitor (or HBV Core Protein Allosteric Modifier), or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

Abstract: The present application relates to chemical compounds of Formula (A): and pharmaceutically acceptable salts thereof, wherein X, R1, and R2 are as defined herein. The chemical compounds of Formula (A) inhibit IRAK4 and consequently have potential utility in medicine.

Abstract: Pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds are provided. The pyrido[4?,3?:5,6]pyrimido[1,2-a]indole compounds have the general formula: where R1 represents aryl, heteroaryl, aminoaryl, aminoheteroaryl, aminoalkyl, aminocycloalkyl, aryloxy, heteroaryloxy, or alkoxy; and R2 and R3 represent hydrogen, carboxyl, ester, amide, halogen, alkyl, aryl, hydroxyl, alkoxy, aryloxy, aminoalkyl, aminocycloalkyl, aminoaryl, or aminoheteroaryl. The compounds show inhibitory activity against CK2 enzyme, and may be used as anticancer agents.

Abstract: The present invention relates to pyrazolo [1,5-a][1,3,5]triazine and pyrazolo [1,5-a]pyrimidine derivatives having Formula I: and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferative diseases, inflammatory diseases, immunological diseases, cardiovascular diseases and infectious diseases. Furthermore, the present invention is directed towards pharmaceutical compositions containing at least one of the pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives and/or pharmaceutically acceptable salts thereof.

Abstract: The application relates to a compound of Formula (I): which modulates the activity of ALK or SRPK, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which ALK or SRPK plays a role.

Abstract: This disclosure relates therapeutic compositions containing a compound of Formula Im: or a pharmaceutically acceptable salt thereof, wherein R1 is as defined herein.

Abstract: 1?-Cyano nucleoside analogs of Formula I and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.