Abstract: The present invention relates to protein-inhibitory substituted pyrrolopyridine derivatives of formula (I), in which A, X, R1, R2a, R2b, R3a, R3b, R4a and R4b are as defined herein, to pharmaceutical compositions and combinations comprising the compounds according to the invention, and to the prophylactic and therapeutic use of the inventive compounds, respectively to the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular for neoplastic disorders, respectively cancer or conditions with dysregulated immune responses or other disorders associated with aberrant MAP4K1 signaling, as a sole agent or in combination with other active ingredients.

Abstract: The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.

Abstract: A method is provided to prevent and to treat Macular Degeneration by using Calcium Channel Blockers, Angiotensin-Converting Enzyme (ACE) Inhibitors, or Angiotensin Receptor Blockers (ARB), and more particularly, to a method to prevent and treat Macular Degeneration by using Calcium Channel Blockers, Angiotensin-Converting Enzyme Inhibitors, or Angiotensin Receptor Blockers that are not taken orally, but administered by ophthalmic preparation directly onto or into the eye where Macular Degeneration is formed, to increase the capillary network and blood supply to the retinal macula.

Abstract: The present disclosure relates to novel compounds, pharmaceutical compositions containing such compounds, and their use in prevention and treatment of cancer and related diseases and conditions. In some embodiments, the compounds disclosed herein exhibit androgen receptor degradation activity.

Abstract: The present invention provides methods of treating hematological disorders, such as acute myeloid leukemia, using substituted heterocyclic compounds and pharmaceutically acceptable salts thereof. The compounds inhibit IRAK4 and FLT-3 kinases.

Abstract: Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

Abstract: This invention is in the field of fluorescence imaging and relates to a new near infrared (NIR) reactive oxygen species (ROS) sensor designed with controlled fluorescence on-off switching mechanism.

Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Abstract: Resolution of a pathological condition is promoted via the application, e.g., via injection, of a potassium osmolyte such as hyperosmolar potassium gluconate, potassium aspartate, another potassium-based salt, or combinations thereof to the condition site. The application of the potassium osmolyte increases the extracellular concentration of potassium ions, reducing the membrane potential of the cells at the condition site and including immune cell quiescence. As a result, the inflammatory response in the patient to the pathological condition is reduced or eliminated. Reducing the inflammatory response is useful in treatment of myriad conditions including arthritis, auto-immune conditions, inflammatory disorders, neurodegenerative disorders, neurodevelopmental disorders, tissue breakdown, etc.

Abstract: Provided is a preparation method for a tyrosine kinase inhibitor and an intermediate thereof. Specifically, a preparation method for a cyanoquinoline compound is provided. The method has a high yield, good product purity, and mild reaction conditions.

Abstract: Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.

Abstract: The present invention provides dihydroquinolinone compounds which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

Abstract: Provided is a 2-heteroaryl aminoquinazolinone derivative, which is a compound represented by formula (1): or a pharmaceutically acceptable salt thereof wherein X1 represents CR1 or N, X2 represents CR2 or N, X3 represents CR3 or N, X4 represents CR4 or N, Y represents optionally substituted C1-6 alkyl, an optionally substituted C3-10 alicyclic group, an optionally substituted 4- to 10-membered nitrogen-containing non-aryl heterocycle, optionally substituted C6-10 aryl, or optionally substituted 5- to 10-membered heteroaryl, Z represents optionally substituted 6- to 10-membered heteroaryl, and R1, R2, R3, and R4 each independently represent a hydrogen atom, halogen, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-6 alkoxy, or the like.

Abstract: Disclosed herein are compounds and compositions for modulating glycolate oxidase, useful for treating oxalate-related diseases, such as hyperoxaluria, where modulating glycolate oxidase is expected to be therapeutic to a patent in need thereof. Methods of modulating glycolate oxidase activity in a human or animal subject is also provided.

Abstract: The present invention relates to a novel pentafluorosulfanyl-substituted amide compound that regulates or inhibits indoleamine 2,3-dioxygenase (IDO) activity, its preparation method and its application in medicine. Specifically, the present invention relates to a compound represented by general formula (I) and pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof, application of the compound or pharmaceutically acceptable salt thereof for treating and/or preventing related disorders mediated by IDO, especially tumors, and a method for preparing the compound or pharmaceutically acceptable salt thereof. The present invention also relates to the preparation of the compound or pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof for the treatment and/or prevention of IDO-mediated related disorders, especially for use in tumor treatment.

Abstract: The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, Z, Y and m are as defined herein.

Abstract: The disclosure relates to benzoimidazole derivatives, acting as anticancer drugs, as well as pharmaceutical composition containing said compounds. These compounds are able to firstly inhibit the protein/protein interactions of the MAP Kinase Erk, leading to inhibition of proliferation and secondly to induce apoptosis in human cancer cell lines.

Abstract: The invention provides a compound, namely acetylsalicylic acid (ASA) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising ASA or a pharmaceutically acceptable salt thereof, for use in the treatment of a patient, e.g. a human being, suffering from a severe influenza virus infection and/or a symptom or condition associated therewith (namely, nasal congestion, sore throat, cough, fever, fatigue, headache and myalgias), wherein said use comprises the administration of a composition comprising ASA or a pharmaceutically acceptable salt thereof to the patient by inhalation.

Abstract: The present invention relates to a pharmaceutical composition, containing sarpogrelate or a pharmaceutically acceptable salt thereof as an active ingredient, for preventing, alleviating, or treating sensorineural hearing loss. The sarporgrelate according to the present invention protects against hearing loss caused by noise through the suppression of auditory cell apoptosis and the expression increase of antioxidant enzyme in auditory cells, and thus can be advantageously used in the prevention and alleviation of sensorineural hearing loss.

Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X and mare as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.