Abstract: Provided herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, useful as RIPK1 inhibitors, and pharmaceutical compositions comprising same. Further provided are methods of use and preparation. Also provided are methods of treating Ulcerative Colitis using a compound of Formula (I).

Abstract: Disclosed herein are serotonin (5-hydroxytryptamine) 5-HT2A receptor and/or 5-HT2C receptor allosteric modulators, the preparation thereof and use thereof.

Abstract: The invention provides a pharmaceutically acceptable salt of 5-[[5-[4-(4-fluoro-1-methyl-4-piperidyl)-2-methoxy-phenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile which is selected from maleate, tosylate, besylate and malonate salts. Also provided are particular crystalline forms of the salts, methods for the preparation of the salts, pharmaceutical compositions containing the salts and their therapeutic uses.

Abstract: The present invention relates to a pyrimidine-4,6-diamine derivative, a preparation method therefor, and a pharmaceutical application thereof. Particularly, the present invention relates to a pyrimidine-4,6-diamine derivative having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, and a use of same as an EGFR inhibitor and a use of same in the preparation of drugs for the treatment and/or prevention of cancers, tumors, or metastatic diseases at least partially related to EGFR Del19 mutation, EGFR L858R mutation, EGFR L858R/C797S double mutation or EGFRDel19/C797S double mutation, in particular a use of same in the preparation of drugs for the treatment and/or prevention of hyperproliferative diseases and induced cell death disorders. The definition of each substituent in formula (I) is the same as that in the description.

Abstract: Among other things, the present disclosure provides technologies for modulating complement activation. In some embodiments, the present disclosure provides compounds that inhibit C3 convertase activity. In some embodiments, the present disclosure provides methods for treating complement-mediated conditions, disorders or diseases. In some embodiments, the present disclosure provides methods for treating conditions, disorders or diseases mediated by C3 convertase.

Abstract: Provided herein are compounds of Formula (I?), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), or Formula (VIII) and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, or prodrugs thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

Abstract: The disclosure relates to synthetic methods for producing polyamides, for example pyrrole and imidazole containing polyamides of Formula (I) or (II), or a pharmaceutically acceptable salts thereof. These polyamides bind genes having expanded oligonucleotide repeat sequences, which thereby modulates transcription. The disclosure further provides methods of modulation of the transcription of such DNA, and the use of polyamides as therapeutic agents to treat diseases associated with such DNA.

Abstract: Described herein are methods and compositions for the treatment of conditions, diseases, or disorders associated with thyroid hormone receptor activity. The methods and compositions disclosed herein include the use of at least one thyroid hormone receptor agonist.

Abstract: The present invention features inhibitors of the eIF4A enzyme. These inhibitors have a novel mechanism for inhibiting the eIF4A enzyme by occupying a binding pocket within the eIF4A RNA-binding groove, thereby perturbing RNA binding, blocking ATP hydrolysis, and, consequently, inhibiting RNA helicase activity. Thus, the compounds of the present invention are RNA-competitive, ATP-uncompetitive elF4A inhibitors that directly bind elF4A and inhibit the protein.

Abstract: Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

Abstract: Provided are a polycyclic derivative regulator, a preparation method therefor, and an application thereof. In particular, provided are a compound represented by general formula (I?), a preparation method therefor, a pharmaceutical composition comprising the compound, and an application thereof as a regulator in the preparation of a drug for treating metabolic diseases and related diseases; the substituents in general formula (I?) are the same as those defined in the description.

Abstract: Provided are a GLP-1 receptor agonist compound and a composition and use thereof. The compound can be used for treating or preventing GLP-1 receptor-mediated diseases or disorders and related diseases or disorders.

Abstract: Itraconazole, a widely used antifungal drug, has been found to possess potent anti-angiogenic and anti-hedgehog activities, exhibiting promising antitumor activity in several human clinical studies. The wider use of itraconazole in the treatment of cancer, however, has been limited by its potent inhibition of the drug metabolic enzyme CYP3A4 which causes drug-drug interactions. In an effort to eliminate the CYP3A4 inhibition of itraconazole while retaining its anti-angiogenic activity, we synthesized a series of itraconazole derivatives. The newly synthesized analogs of itraconazole were evaluated for their cytotoxicity against human umbilical vein endothelial cells (HUVEC) and their inhibitory activity against CYP3A4 enzyme.

Abstract: The invention relates to a series of compounds with heterocycloalkyl, or isomers or pharmaceutically acceptable salts thereof, and to a use thereof in manufacturing a medicine of treatment CCR2/CCR5 antagonist-related diseases, specifically to a compound of Formula ( ), or an isomer or pharmaceutically acceptable salt thereof.

Abstract: N,N-disubstituted arylamine compounds and to their use as integrin agonists for enhancing binding of integrin-expressing cells to integrin-binding ligands or receptors.

Abstract: This disclosure provides compounds of Formula I, compositions comprising the same, and methods of using the same, including use in treating various diseases and conditions, e.g., those involving ferroptosis.

Abstract: Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

Abstract: The present invention provides compounds of formula (I?): which are useful in the control of endoparasites, for example heartworms, in warm-blooded animals.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The present invention provides a compound, or a pharmaceutically acceptable salt thereof, of formula (I): wherein R1, R2, R3, R4, R5, R26, R27, y, R, M, W, L, V, T, Y, J, K and A are as described herein, therapeutic uses of said compounds, uses of said compounds as research chemicals, a pharmaceutical composition and combinations comprising said compounds, and methods for manufacturing the compounds of the invention.

Abstract: The present invention relates to compounds of formula (I). The compounds may be used to antagonise the Stimulator of Interferon Genes (STING) protein and may thereby treat liver fibrosis, fatty liver disease, non-alcoholic steatohepatitis (NASH), pulmonary fibrosis, lupus, sepsis, rheumatoid arthritis (RA), type I diabetes, STING-associated vasculopathy with onset in infancy (SAVI), Aicardi-Goutieres syndrome (AGS), familial chilblain lupus (FCL), systemic lupus erythematosus (SLE), retinal vasculopathy, neuroinflammation, systemic inflammatory response syndrome, pancreatitis, cardiovascular disease, renal fibrosis, stroke and age-related macular degeneration (AMD).

Abstract: This application is directed to inhibitors of RAD51 represented by the following structural formula, and methods for their use, such as to treat cancer, autoimmune diseases, immune deficiencies, or neurodegenerative diseases.

Abstract: Disclosed herein are compounds and compositions useful in the treatment of GLS1 mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibition GLS1 activity in a human or animal subject are also provided.

Abstract: The disclosure relates to solid forms of 2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(thiazol-5-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid (Compound 1), including solid forms of Compound 1, salts of Compound 1 and solid forms thereof, including crystalline forms of Compound 1 and salts thereof, as well as polymorphs of Compound 1 and salts of Compound 1.

Abstract: The present disclosure provides anti-CD25 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.

Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R6, X1, and X2 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising compounds of formula (I).

Abstract: Provided herein are 2-substituted bicyclo[1.1.1]pentane (BCP) compounds, as well as methods of making the 2-substituted BCP compounds and methods of derivatizing the 2-substituted BCP compounds, particularly at the 2-position. The 2-substituted BCP compounds described herein are useful building blocks in the synthesis of a variety of products, including pharmaceuticals, polymers, liquid crystals, monolayers and supramolecular structures.

Abstract: The present invention relates to compounds of formula (I), wherein R1 to R3, A, M, W and Q are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein.

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

Abstract: The present disclosure relates to inhibitors of NLRP3 useful in the treatment of diseases and disorders inhibited by said protein and having the Formula (I):

Abstract: The present disclosure relates to inhibitors of NLRP3 of Formula (I) or a pharmaceutically acceptable salt, solvate, clathrate, hydrate, stereoisomer, tautomer, isotopically labeled compound, or prodrug thereof, wherein Ring A is a 5- to 8-membered monocyclic heterocycloalkyl comprising at least one O ring atom, p is 0 or 1, and R1, R2, R3, R4, and X are as defined herein, useful in the treatment of diseases and disorders inhibited by said protein.

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract: The present disclosure provides compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The provided compounds may be kinase (e.g., Janus kinase (JAK) (e.g., Janus kinase 2 (JAK2)) and/or cyclin-dependent kinase (CDK) (e.g., cyclin-dependent kinase 11 (CDK11)) inhibitors. Also provided are pharmaceutical compositions and kits including the provided compounds. Further provided are methods of using the provided compounds, pharmaceutical compositions, and kits (e.g., for treating a disease (e.g., proliferative disease) in a subject in need thereof).

Abstract: The present invention relates to a fused tricyclic compound, a preparation method therefor, and an application thereof in medicine. Specifically, the present invention relates to a fused tricyclic compound represented by general formula (1), a preparation method therefor, a pharmaceutical composition containing the compound, and a use thereof as a therapeutic agent, particularly a use as a TLR7/8/9 inhibitor and a use in preparing a drug for the treatment and/or prevention of inflammatory and autoimmune diseases. The definition of each group in general formula (1) is as defined in the description.

Abstract: The disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprising compounds of formula (I), as well as methods of their use and preparation, are also described.

Abstract: Provided herein are compounds of the following structural formula: or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., R1, R2 n) are as described herein. Compounds of Structural Formula I and pharmaceutically acceptable salts thereof, pharmaceutical compositions of either of the foregoing, and pharmaceutical combinations of any of the foregoing can be used, e.g., to treat a disease, disorder or condition described herein, such as cancer, fibrosis or inflammation.

Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.

Abstract: The invention relates to compounds which inhibit CDK2 (Cyclin-Dependent Kinase 2 or Cell Division protein Kinase 2), and to processes for the preparation of said compounds, pharmaceutical compositions comprising said compounds, and use of said compounds in the treatment of conditions, diseases and disorders mediated by CDK2.

Abstract: Provided herein are, inter alia, compositions that bind to a PDZI domain of MDA-9/Syntenin (syndecan binding protein: SDCBP), thereby inhibiting MDA-9/Syntenin activity, and methods of use of same. The compositions and methods provided herein are useful for treating cancer and preventing cancer metastasis, particularly in cancers that have increased MDA-9/Syntenin expression.

Abstract: The present invention relates to novel blood-brain barrier (BBB) penetrable substituted bicyclic derivatives that can selectively inhibit ROCK2 and/or Rho-kinase mediated phosphorylation of myosin light chain phosphates, compositions comprising the derivatives, methods for preparing the derivatives and/or compositions, and methods for using the derivatives and/or compositions.

Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.

Abstract: Provided herein are compounds of Formula I, or a pharmaceutically acceptable form thereof, and pharmaceutical compositions comprising the same. Also provided herein methods of modulating the activity of cellular targets by administering to a subject a compound of Formula I, or a pharmaceutically acceptable form thereof. Further provided herein are methods of treating cancer, fibrotic diseases, and inflammatory diseases by administering to a subject a compound of or a pharmaceutically acceptable form thereof.

Abstract: A compound having the structure of AGN5 or AGN11 is provided. A composition comprising either AGN5 or AGN11 and a pharmaceutically acceptable carrier is provided. A method of treating a patient having dementia with Lewy Bodies, Parkinson's Disease, and Alzheimer Disease with Lewy Bodies comprising administering to said patient a therapeutically effective amount of the compound AGN5, AGN11, or the composition comprising AGN5 or AGN11 and a pharmaceutically acceptable carrier.

Abstract: The present invention is related to compounds, methods, compositions and uses that are able to inhibit mitochondrial pyruvate carrier (MPC) activity and which are useful for immunotherapy, in particular T-cell therapies, immune check point inhibitors or anti-cancer vaccine.

Abstract: The present invention provides a pyrazolopyrimidine ester compound of the following general structural formula: The present invention also provides a method of preparing the pyrazolopyrimidine ester compound and use thereof for preparation of a drug for treating blood disease such as lymphoma and lymphocytic leukemia. The pyrazolopyrimidine ester compound of the present invention undergoes a mild first-pass effect, and once orally absorbed, can rapidly enter the blood plasma to deliver the intended therapeutic effect. It produces a flat plasma drug concentration peak, but has a great AUC. It can provide high bioavailability, a steady plasma drug concentration profile and a sustained duration of action. Compared with the existing BTK inhibitors, it can better address clinical needs.

Abstract: Provided are pyrimidine-2,4-diamine derivatives and use thereof.

Abstract: Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof; or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.

Abstract: The disclosure provides processes for preparing Compound A, Compound E, Compound I, salts thereof, and/or stereoisomers thereof, as described herein.

Abstract: The present invention relates to cyano-containing compounds and compositions capable of acting as inhibitors of small ubiquitin-like modifier (SUMO) family of proteins. The compounds and compositions may be used in the treatment of cancer. There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme.