Patent classifications
C07D413/00
Kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
Synthesis of tetracyclines and analogues thereof
The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
Crystal form of pyrazolyl-amino-pyrimidinyl derivative, and preparation method therefor and use thereof
Provided in the present disclosure is crystal form I of compound 1, and a preparation method thereof and the use thereof. ##STR00001##
Crystal form of pyrazolyl-amino-pyrimidinyl derivative, and preparation method therefor and use thereof
Provided in the present disclosure is crystal form I of compound 1, and a preparation method thereof and the use thereof. ##STR00001##
2-(hetero)aryl-benzimidazole and imidazopyridine derivatives as inhibitors of asparagime emethyl transferase
Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR.sup.4; A.sup.2 is selected from: a C.sub.5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are to one another; L.sup.1 is selected from: (i) .sup.A1OCH.sub.2.sup.A2; (ii) .sup.A1CH.sub.2O.sup.A2; (iii) .sup.A1C(O)NH.sup.A2; (iv) .sup.A1CH(OH).sup.A2; (v) .sup.A1CH.sub.2NHC(O).sup.A2; (vi) .sup.A1SCH.sub.2.sup.A2; (vii) .sup.A1CH.sub.2S.sup.A2; (viii) .sup.A1CH.sub.2.sup.A2; and (ix) .sup.A1CH(CH.sub.3)O.sup.A2; A1 is phenyl, optionally substituted by F or CF.sub.3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies. ##STR00001##
Composition and method for controlling pests
The present invention provides a composition for controlling pests having an excellent control efficacy on pests. A composition for controlling pests comprising a compound represented by the formula (1): ##STR00001##
wherein each of symbols are the same as defined in the Description, or N-oxide thereof; and
a compound represented by the formula (2): ##STR00002##
wherein each of symbols are the same as defined in the Description;
shows an excellent controlling efficacy on pests.
Difluoromethoxy compound with low bioactivation potential for the reduction of beta-amyloid production
The compound N2-(3-(difluoromethoxy)-4-(3-methyl-1H-1,2,4-triazol-1-yl)phenyl)-7-(4-fluorophenyl)-N4,5,5-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidine-2,4-diamine: [PLEASE INSERT CHEMICAL STRUCTURE HERE] reduces -amyloid peptide (A 42) production and has low potential for bioactivation, and may be useful in the treatment of Alzheimer's Disease and other conditions affected by -amyloid peptide (A 42) production.
Arylcyclopropylamine based demethylase inhibitors of LSD1 and their medical use
The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX). ##STR00001## ##STR00002##
Urethanes, ureas, amidines and related inhibitors of factor Xa
The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
Trisubstituted bicyclic heterocyclic compounds with kinase activities and uses thereof
Trisubstituted bicyclic heterocyclic compounds (e.g., chromenones and quinolines) and pharmaceutical compositions,that modulate kinase activity, including PI3 kinase activity, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.