Abstract: The present application provides deazaguaine compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.

Abstract: The present specification discloses one or more anti-oncogenic phytochemicals comprising one or more compounds of chemical formula I: wherein R1is independently selected from H, CH3 or C2H5or is not present; R2 is independently selected from H, CH3 or C2H5 or is not present; provided that when R1 is not present, R2 is selected from H, CH3 or C2H5 and when R2 is not present R1 is selected from H, CH3 or C2H5: R3 is a C4-40 straight or branched chain, alkyl or alkylene and optionally substituted with one or more groups independently selected from CH3, OH, SH, NH2, OMe, OEt, N(H)Me and NMe2; and X is independently selected from CH3, OH, SH, NH2, OMe, OEt, N(H)Me, and NMe2, as well as, extracts, pharmaceutical compositions and medicaments comprising the one or more anti-oncogenic phytochemicals disclosed herein, methods of preparing such extracts, pharmaceutical compositions, and medicaments comprising the one or more anti-oncogenic phytochemicals , and methods and uses for treating a neoplasm or a cancer usi

Abstract: The present invention relates to indoline-based compounds that inhibit Rho-associated protein kinase (ROCK) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.

Abstract: The present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (II): wherein R1, R2, R3, X and Y are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt. More particularly, the present disclosure relates to a method of preventing and/or treating non-alcoholic steatohepatitis in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a compound of Formula (I): wherein R2, R3, and X, are as defined in the specification; or a pharmaceutically acceptable salt, solvate, or solvate of such a salt.

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with inhibition of HDAC (e.g,. HDAC2).

Abstract: The present invention provides a compound of the formula (1): wherein X, R1, R2, R3, R4, R5, R6, Y1, Y2, L, and m are as defined in the description, and a pharmaceutically acceptable salt thereof, which are useful as a vaccine adjuvant.

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: 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: 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: 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: 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: 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.