摘要:
Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.
摘要:
Disclosed are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of formula (I), methods for inhibiting tumor necrosis factor-α and methods for treating septic shock, inflammation, or allergic disease.
摘要:
Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.
摘要:
The invention provides a compound of formula (I), wherein R?1, R2, R3¿, and Y have any of the meanings defined in the specification; as well as a pharmaceutical composition comprising a compound of formula (I); intermediates and methods useful for preparing a compound of formula (I); and therapeutic methods for treating drug addiction, Parkinson's disease or depression comprising administering a compound of formula (I), to a mammal in need of such treatment.
摘要:
Arylpiperidinol or arylpiperidine derivatives represented by general formula (I) and drugs containing the same, in particular, those for improving or treating symptoms on the basis of ischemic diseases, convulsion, epilepsy and symptoms originating in hemicrania and calcium ion superloading inhibitors. In said formula (I) R represents H, optionally substituted phenyl, optionally substituted phenoxy or optionally substituted benzoyl; A represents a bond, cycloalkylene or alkenylene optionally substituted by lower alkyl; B represents alkylene optionally substituted by OH or alcoxy or -NHCO(CH2)n- (wherein n is an integer of 1 to 5); E represents a bond, O or methylene; X represents OH or H, provided that X is not H when E is O or methylene; and Y and Z independently represent each H, halogeno, alkoxy or optionally halogenated alkyl.
摘要:
In a process for preparing 3-methylpiperidine or 3-methylpyridine from 2-methyl-1,5-diaminopentane in the gaseous phase, the initial product is made to flow over catalysts. In the first step, 3-methylpiperidine is produced, and if required 3-methylpyridine is produced in a second step.
摘要:
Disclosed are compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of formula (I), methods for inhibiting tumor necrosis factor-α and methods for treating septic shock, inflammation, or allergic disease.
摘要:
Herstellung von in 3- und/oder 4-Stellung substituierten Piperidinen durch Umsetzung von in 2- und/oder 3-Stellung substituierten Glutardialdehyden mit Ammoniak oder einem primären Amin und Wasserstoff bei erhöhter Temperatur und erhöhtem Druck in Gegenwart eines Hydrierkatalysators.
摘要:
Procédé de transformation des composés de formule: dans laquelle R est un atome d'hydrogène ou un substituant et pour lesquels le carbone porteur du groupe vinyle possède la configuration rectus en les composés correspondants de formule (I) pour lesquels le carbone porteur du groupe vinyle possède la configuration sinister, et vice versa, caractérisé en ce que l'on chauffe à température supérieure à 50°C, au sein d'un solvant protique ou d'un mélange de solvants protiques, en présence ou en l'absence de formaldéhyde, un composé de formule (1) pour lequel le carbone porteur du groupe vinyle a la configuration rectus ou sinister,. partiellement ou totalement salifié, et isole le composé de formule (I) pour lequel le carbone porteur du groupe vinyle a la configuration sinister ou rectus ainsi formé. Les composés obtenus sont utilisables en particulier comme produits intermédiaires pour la préparation de médicaments.