- Allylamine derivative as well as preparation method and application thereof
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The invention relates to an allylamine derivative as well as a preparation method and application thereof, and in particular, relates to a compound represented by a formula I, or a stereoisomer, a tautomer, a polymorphic substance, a solvate, an N-oxide, an isotope labeled compound, a metabolite, a prodrug or ester thereof, or a pharmaceutically acceptable salt thereof. The compound has a higher inhibitory activity against vascular adhesion protein 1/semicarbazide sensitive amine oxidase, a good selectivity against monoamine oxidase and diamine oxidase; and additionally, in some embodiments, the mixture has a high in vivo bioavailability as well as safety.
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- Preparation and application of aminourea sensitive amine oxidase inhibitor
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The invention provides preparation and application of an aminourea sensitive amine oxidase inhibitor. Specifically, the invention discloses a compound as shown in a formula I, or a stereoisomer, raceme or pharmaceutically acceptable salt thereof. The invention also discloses the compound capable of inhibiting the aminourea sensitive amine oxidase.
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- VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
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Disclosed herein are small molecule Vascular Adhesion Protein- 1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
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- FLUOROALLYLAMINE DERIVATIVE AND USE THEREOF
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The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity.
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- SSAO INHIBITOR
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The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof.
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- Halogenated allyl amine type SSAO/VAP-1 inhibitor and application thereof
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The invention belongs to the technical field of medicine, and particularly relates to a halogenated allyl amine type compound shown as a formula I, medically acceptable salt, ester or stereo isomers thereof, wherein R1, R2, R3, R4, R5, R6, L1, Cy1, R7 and p are defined in description. The invention also relates to a medicine preparation containing the compounds, a medicine composition containing the compounds, and application of the compounds to prevention and/or treatment on diseases relevant to SSAO/VAP 1 protein or diseases caused by SSAO/VAP 1 protein mediating. The formula I is shown in the description.
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- SSAO INHIBITORS AND USES THEREOF
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Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.
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- SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF SSAO AND USES THEREOF
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The present invention is related to the preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula (I), as defined in the specification. The invention also relates to methods of using compounds of Formula (I), or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer.
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- Synthesis and biological evaluation of novel, peripherally selective chromanyl imidazolethione-based inhibitors of dopamine β-hydroxylase
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A novel series of dopamine β-hydroxylase (DBH) inhibitors was designed and synthesized incorporating modifications to the core structure of nepicastat 3, with the principal aim of discovering potent DBH inhibitors exerting minimal effects on dopamine (DA) and noradrenaline (NA) levels in the central nervous system. This study resulted in the identification of a potent, peripherally selective DBH inhibitor, (R)-5-(2-aminoethyl)-1-(6,8-difluorochroman-3-yl)-1,3- dihydroimidazole-2-thione hydrochloride 54 (BIA 5-453). In experiments in mice and rats at Tmax (9 h after administration), 54 reduced NA levels in a dose-dependent manner in both the left atrium and the left ventricle, with the maximal inhibitory effect attained at a dose of 100 mg/kg. In contrast to that found in the heart, 54 failed to affect NA tissue levels in the brain. Compound 54 is thus presented as a candidate for clinical evaluation for the treatment of chronic heart failure and hypertension.
- Beliaev, Alexandre,Learmonth, David A.,Soares-Da-Silva, Patricio
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p. 1191 - 1197
(2007/10/03)
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- 5-hydroxypentane-2,3-dione and 3-amino-1-hydroxypropan-2-one, putative precursors of vitamin B6
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New synthesis are described of 5-hydroxypentane-2,3-dione (7) (i.e., laurencione (7 ? 8)) and of 3-amino-1-hydroxypropan-2-one (3-amino-1- hydroxyacetone) (5) hydrochloride, putative precursors of the C5 unit, C- 2',2,3,4,4', and of the C3N unit, N-1,C-6,5,5', respectively, of pyridoxine (6). The condensation of hydroxypentane dione (i.e., laurencione) and aminohydroxypropanone forms a vitamin B, pyridoxine. The two compounds incorporated structural modifications on the formation mechanism of vitamin B. These compounds were considered as putative precursors of the C5 unit and the C3N unit of pyridoxine.
- Wolf, Eckardt,Kennedy, Isaac A.,Himmeldirk, Klaus,Spenser, Ian D.
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p. 942 - 948
(2007/10/03)
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