摘要:
The invention relates to a method for carrying out the highly regioselective aromatic nitration of 4-alkanoylamino-3-alkyl-benzoic acid alkyl esters at the 5-position in a mixture containing nitric acid. The invention also relates to the use of the products obtained using said method and to the production of benzimidazole derivatives which are, in particular, pharmaceutically active.
摘要:
Aryloxyaniline derivatives represented by the general formula (I), wherein Ar and Ar represent each a substituted or unsubstituted phenyl, pyridyl, or naphthyl group; R represents a hydrogen atom, an alkyl group or the like; X represents a hydrogen atom, an alkyl group or the like; and Y represents a branched or unbranched 1-6 C alkylene group or a single bond, or pharmaceutically acceptable salts thereof. The derivatives can provide medicines having high affinity for MDR exhibiting therapeutic and prophylactic effects on anxiety and associated diseases, depression, and the like.
摘要翻译:由通式(I)表示的芳氧基苯胺衍生物,其中Ar 1和Ar 2各自表示取代或未取代的苯基,吡啶基或萘基; R 1表示氢原子,烷基等; X 1表示氢原子,烷基等; Y 1表示支链或非支链的1-6C亚烷基或单键,或其药学上可接受的盐。 该衍生物可以提供对MDR具有高亲和力的药物,其表现出对焦虑和相关疾病,抑郁症等的治疗和预防作用。
摘要:
Methods and compounds useful for the inhibition of convulsive disorders, including epilepsy, are disclosed. The methods and compounds of the invention inhibit or prevent ictogenesis and epileptogenesis. Methods for preparing the compounds of the invention are also described.
摘要:
Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
摘要:
The invention concerns compounds of formula (I), wherein the substituents have various meanings, and their use in the prevention or treatment of inflammatory and proliferative skin diseases and cancer.
摘要:
Novel substituted alicyclic fused ring 2,3-quinoxalinediones, pharmaceutical compositions containing the same and the method of using the same, for the blockade of glutamate receptors, including either or both N-methyl-D-aspartate (NMDA) receptors and non-NMDA receptors such as the alpha -amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor and the kainate receptor, are described. Methods of preparing the substituted alicyclic fused ring 2,3-quinoxalinediones are also described. Novel intermediates of the inventive quinoxalinediones are disclosed. The novel substituted alicyclic fused ring 2,3-quinoxalinediones may be used, for example, as neuroprotective agents, for treatment of chronic neurodegenerative disorders, as anticonvulsants and in the treatment of schizophrenia, epilepsy, anxiety, pain and drug addiction.
摘要:
Compounds having structure (I) wherein Q is (II); n is an integer from 0 to 20; R is H, alkyl, fluoroalkyl, cycloalkyl, aryl, aralkyl, alkoxyalkyl or acetamidoalkyl; R , R , R and R are independently H, alkyl, fluoroalkyl, halogen, hydroxy, acylamino, acetamidoalkyl, cyano, sulfonyl, carboxamido or sulfonamido; R is alkyl, cycloalkyl, aryl or aralkyl; and R is H or -COR are useful as contrast agents in medical diagnostic x-ray imaging compositions and methods.
摘要翻译:具有结构(I)的化合物,其中Q是(II); n为0〜20的整数, R 1是H,烷基,氟代烷基,环烷基,芳基,芳烷基,烷氧基烷基或乙酰氨基烷基; R 2,R 3,R 4和R 5独立地是H,烷基,氟烷基,卤素,羟基,酰氨基,乙酰氨基烷基,氰基,磺酰基,甲酰氨基或亚磺酰氨基; R 6是烷基,环烷基,芳基或芳烷基; 和R 7是H或-COR 6可用作医学诊断x射线成像组合物和方法中的造影剂。
摘要:
Substituted N-phenylglutarimides (I), wherein X , X = O, S; R = halogen, NO2, CN, CF3; R = H, halogen; R , R , R = H, halogen, CN, alkyl, cycloalkyl, alkenyl, alkinyl, alkyl halide, alkoxy, alkoxy halide, alkyl thio, alkyl thio halide, cyanoalkyl, alkoxy carbonyl, possibly substituted phenyl or benzyl, or 2 substituents of a C atom of the glutarimide ring are linked via a possibly substituted chain, or 2 substituents of adjacent C atoms of the glutarimide ring are linked via a possibly substituted chain; A = CHR -CHR -CO-B or CR =CR -CO-B; R = H, C1-C6-alkyl or C1-C6-alkyl halide; R = halogen, alkyl halide, OH, alkoxy or alkyl carbonyl alkoxy; R = H, halogen, CN, alkyl, alkyl halide, OH, alkoxy, alkyl carbonyl, alkoxy carbonyl or alkyl carbonyloxy; B = H, alkyl, alkenyl, alkinyl, alkyl halide, cycloalkyl, alkoxy alkyl, dialkoxy alkyl, alkyl thioalkyl, OR , SR , NR , R ; R = H, alkyl, alkenyl, alkinyl, cycloalkyl, alkyl halide, cyanoalkyl, alkenyl halide, alkoxy carbonyl alkyl, alkoxyalkyl, alkyl thioalkyl, alkylimino, alkylimino alkyl, possibly substituted phenyl or benzyl; R , R = H, alkyl, alkenyl, alkinyl, cycloalkyl, alkyl halide, alkyl carbonyl, alkoxy carbonyl, alkoxy alkyl, possibly substituted phenyl, or R und R together with the common N atom = saturated or unsaturated 4- to 7- membered heterocycle with 1-2 other heteroatoms, as well as salts of (I) that are tolerable to plants; their preparation and use as herbicides and desiccants/defoliants, as well as preproducts for preparing the N-phenylglutarimides (I).
摘要:
The present invention includes methods and compositions that inhibit AKR1C3 enzymatic activity and consequently reduces androgen receptor (AR) transactivation, AR and prostate specific antigen (PSA) expression levels in, for example, prostate cancer, castration-resistant prostate cancer, breast cancer, acute myeloid leukemia (AML), T-cell acute lymphoblastic leukemia (T-ALL), or a leukemia.
摘要:
The present invention provides novel compounds and pharmaceutical compositions suitable for administration to mammals, for the prevention and/or treatment of cancer, precancerous conditions, pain, fever, skin disorders, inflammation-related diseases and/or cardiovascular diseases. The compounds of the invention have improved efficacy and safety, including higher potency and/or fewer or less severe side effects, than conventional therapies. These comprise a biologically active moiety or portion (A) preferably derived from a non-steroidal anti-inflammatory drug or NSAID (A), bound via a linker moiety (B) to functional moiety Z, which facilitates access of the compound into cells. The moiety Z can comprise, for example, a phosphorous-containing group, a nitrogen-containing group, or a folic acid residue.