Patent classifications
A61P25/00
SIGMA-1 RECEPTOR LIGANDS AND USES THEREOF
The present invention relates to the field of medicine. More specifically, the present invention relates to compounds that are sigma-1 receptor agonists and their use for the treatment of central nervous system disorders, including cognitive or neurodegenerative disorders, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis, and multiple sclerosis.
PFKFB3 INHIBITORS AND THEIR USES
- Petr Olegovich FEDICHEV ,
- Kevin GREENMAN ,
- Chang CHIH-TSUNG ,
- Maksim Nikolaevich KHOLIN ,
- Evgeny Gennadievich GETMANTSEV ,
- Tatiana Vladimirovna ZHIDKOVA ,
- Alexandr Viktorovich KADUSHKIN ,
- Timofey Vladimirovich PYRKOV ,
- Dmitry Veniaminovich SHISHOV ,
- Juan Pedro BOLANOS-HERNANDEZ ,
- Kristina Aleksandrovna ZAKURDAEVA ,
- Olga Andreevna BURMISTROVA
This disclosure relates to new phthalimide and isoindolinone derivatives and other PFKFB3 inhibitors for use in the treatment of diseases. The invention further relates to pharmaceutical compositions containing such PFKFB3 inhibitors, methods of preparation thereof, methods for their use as therapeutic agents, and methods of preparation of a medicament for use in therapy, as well as kits and other inventions comprising such PFKFB3 inhibitors. These PFKFB3 inhibitors are useful for the treatment and prophylaxis of cancer, neurodegenerative diseases, autoimmune diseases, inflammatory disorders, multiple sclerosis, metabolic diseases, inhibition of angiogenesis and other diseases and conditions, where the modulation of PFKFB3 and/or PFKFB4 has beneficial effect as well as neuroprotection.
CONFORMATION-SPECIFIC EPITOPES IN ALPHA-SYNUCLEIN, ANTIBODIES THERETO AND METHODS RELATED THEREOF
The disclosure pertains to conformational epitopes in alpha-synuclein, antibodies thereto and methods of making and using immunogens and antibodies specific thereto. In particular antibodies raised to cyclic compounds comprising at least 3 amino acids of EKTKEQ (SEQ ID NO: 1) selectively recognize misfolded oligomeric alpha-synuclein and are able to inhibit alpha-synuclein propagation and toxicity.
CONFORMATION-SPECIFIC EPITOPES IN ALPHA-SYNUCLEIN, ANTIBODIES THERETO AND METHODS RELATED THEREOF
The disclosure pertains to conformational epitopes in alpha-synuclein, antibodies thereto and methods of making and using immunogens and antibodies specific thereto. In particular antibodies raised to cyclic compounds comprising at least 3 amino acids of EKTKEQ (SEQ ID NO: 1) selectively recognize misfolded oligomeric alpha-synuclein and are able to inhibit alpha-synuclein propagation and toxicity.
PHARMACEUTICAL COMPOSITIONS COMPRISING N-[1-(5-CYANO-PYRIDIN-2-YLMETHYL)-1H-PYRAZOL-3-YL]-2-[4-(1-TRIFLUOROMETHYL-CYCLOPROPYL)-PHENYL]-ACETAMIDE
The present invention relates to solid pharmaceutical compositions comprising N-[1-(5-cyano-pyridin-2−ylmethyl)-1H-pyrazol-3-yl]-2-[4-(1-trifluoromethyl-cyclopropyl)-phenyl]-acetamide or pharmaceutically acceptable salt thereof. The invention further relates to methods for manufacturing said compositions and their uses for the treatment or prevention of diseases and disorders linked to T-type calcium channels such as epilepsy.
SALTS/COCRYSTALS OF (R)-N-(4-CHLOROPHENYL)-2-((1S,4S)-4-(6-FLUOROQUINOLIN-4-YL)CYCLOHEXYL)PROPANAMIDE
The present disclosure relates to amorphous and crystalline forms of (R)—N-(4-chlorophenyl)-2-((1S,4S)-4-(6-fluoro-quinolin-4-yl)cyclohexyl)propanamide and its salts/cocrystals, solvates, and/or hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
MUSCARINIC RECEPTOR 4 ANTAGONISTS AND METHODS OF USE
Provided herein are compounds of the following Formula (I): or a pharmaceutically acceptable salt thereof. Methods for treating a diseases, disorders, or symptom by antagonizing muscarinic receptors, including specifically antagonizing muscarinic receptor 4 (M4), are also provided.
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SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT
The present invention relates to a novel compound represented by Formula 1, functioning as a sphingosine-1-phosphate receptor agonist useful for treating autoimmune disorders, a preparation method therefor, a pharmaceutical composition containing the same as an active ingredient, and a use. The compound according to the present invention has an effect in extensive autoimmune diseases and chronic inflammatory diseases, including relapsing-remitting multiple sclerosis, and can also be used for treating or preventing immunoregulatory disorders.
PEPTIDE COMPOUNDS AND METHODS OF TREATING DISEASES USING SAME
Isolated peptides capable of reducing the amount of dexamethasone-induced spleen and/or thymus weight loss in a mouse are disclosed. Uses thereof for treating inflammatory or degenerative diseases are also disclosed.
ALLOSTERIC MODULATORS OF CANNABINOID RECEPTORS AND METHODS OF TREATING NEUROPATHIC PAIN
Provided are methods for treating neuropathic pain by administering to a subject in need thereof a compound comprising phenyl-indole scaffold, wherein the compound has a modulatory effect on cannabinoid type 1 receptor (CB.sub.1R). Pharmaceutical compositions containing compounds comprising phenyl-indole scaffolds and pharmaceutically acceptable carriers are also provided, along with methods of using the same.
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