摘要:
The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3β(glycogen synthase kinase-3β).
摘要:
The present invention relates to kinase inhibitor compounds and derivatives thereof as well as compositions comprising them consisting of the structure of formula I: Wherein R1, R2, A, B, D and E are defined herein. These 4-benzimidazol-2-ylpyridazin-3-ones and their derivatives and compositions comprising them are useful in the treatment of neurological disorders such as Alzheimers' disease, Parkinsons' disease, obesity, hypertension and the like. These pyridazinone derivatives particularly inhibit the metabolic activity of glycogen synthase kinase-3 β (GSK-3β) which is believed to cause the neurodegeneration that results in these diseases.
摘要:
The present invention relates to pyridazinone compounds and their derivatives according to the general formula (I), with the substituents X, R1 and R2 defined herein, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-3β (glycogen synthase kinase-3β) which are useful in the treatment of neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovary syndrome and syndrome X or immunodeficiency.
摘要:
The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
摘要:
The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydrobenzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
摘要:
The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo[c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.
摘要:
Disclosed are compounds of the general formula (I), with the definitions of the substituents R1 to R5, A and X being detailed in the text, and to their physiologically tolerated salts, to processes for preparing these compounds and to the use thereof as inhibitors of hormone-sensitive lipase (HSL).
摘要:
Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 in any optically isomeric form, and their physiologically acceptable salts, where R1 is C1-C6-alkyl, C3-C9-cycloalkyl, both of which may be unsubstituted or substituted, and R2 and R3 independently of one another are hydrogen, C6-C10-aryl, C3-C8-cycloalkyl, C6-C10-aryloxymethyl, O-benzyl, O—C6-C10-aryl, O—C3-C8-cycloalkyl, O—C1-C6-alkyl, SO2—NH—C1-C6-alkyl, SO2—NH-(2,2,6,6-tetramethylpiperidin-4-yl), SO2—NH—C3-C8-cycloalkyl, SO2—N(C1-C6-alkyl)2 or COX, where X is O—C1-C6-alkyl, NH—C1-C6-alkyl, NH—C3-C8-cycloalkyl or N(C1-C6-alkyl)2, with the proviso that the substitutents R2 and R3 may in some instances be unsubstituted or substituted and are not both simultaneously hydrogen. A process for their preparation, and their inhibitory effect on the hormone-sensitive lipase, HSL.
摘要:
Substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula 1 are described, in which R1 is substituted C1-C6-alkyl and C3-C9-cycloalkyl, R2, R3, R4 and R5 are hydrogen, halogen, nitro, C1-C4-alkyl, C1-C9-alkyloxy, substituted C6-C10-aryl-C1-C4-alkyloxy, C6-C10-aryloxy, C6-C10-aryl, C3-C8-cycloalkyl or O—C3—C8-cycloalkyl, or 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, with the proviso that R2, R3, R4 and R5 are not simultaneously hydrogen, and at least one of the radicals R2, R3, R4 or R5 is the radical 2-oxopyrrolidin-1-yl, 2,5-dimethylpyrrol-1-yl or NR6-A-R7, wherein R6=hydrogen, C1-C4-alkyl or substituted C6-C10-aryl-C1-C4-alkyl, A=a single bond, COn, SOn or CONH, n=1 or 2, R7=hydrogen, substituted C1-C18-alkyl, C2-C18-alkenyl, C6-C10-aryl-C1-C4-alkyl, C5-C8-cycloalkyl-C1-C4-alkyl, C5-C8-cycloalkyl, C6-C10-aryl-C2-C6-alkenyl, C6-C10-aryl, biphenylyl, biphenylyl-C1-C4-alkyl, indanyl, or the group Het-(CH2)r—, wherein r=0, 1, 2 or 3 and Het=a saturated or unsaturated 5-7-membered heterocycle, which may be optionally benzo-fused and optionally substituted, and proceses for their preparation. The compounds of formula 1 show an inhibitory effect on hormone-sensitive lipase, HSL.
摘要:
The invention relates to isolated nucleic acid molecules and to host cells comprising such nucleic acid molecules. Moreover, the invention relates to a polypeptide having PIM-3 activity and having a definite amino acid sequence, as well as to the use of PIM-3 as a screening agent for identifying anti-type 2 diabetes mellitus drugs and for preparing a medicament for the treatment of insulin resistance or type 2 diabetes mellitus.