- Synthesis of the β2-Agonist Tulobuterol and Its Metabolite 4-Hydroxytulobuterol
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Abstract: Alternative methods have been developed for the synthesis of theβ2-agonist tulobuterol and its metabolite4-hydroxytulobuterol with a similar activity. The proposed procedures utilizeavailable reagents, and the key stage in the synthesis is the formation ofintermediate oxirane according to the Corey–Chaykovsky reaction, followed byopening of the oxirane ring by the action of excess tert-butylamine. In the synthesis of 4-hydroxytulobuterol, thehydroxy group was protected by benzylation, and the protecting group was removedin the final stage by hydrogenation over carbon-supported palladium.
- Burdeinyi, M. L.,Glushkova, M. A.,Popkov, S. V.
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p. 390 - 394
(2020/04/27)
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- THIOARYL DERIVATIVES AS GPR120 AGONISTS
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The present invention relates to thioaryl derivatives of Formula 1 as defined in the specification, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The thioaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in macrophages, pancreas cells, etc. due to anti-inflammatory action, and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, inflammation, obesity, non-alcoholic fatty liver, steatohepatitis or osteoporosis.
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Paragraph 885-886
(2014/05/24)
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- NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS
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The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
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Page/Page column 45; 47; 48
(2011/04/13)
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- Novel FXR (NR1H4) binding and activity modulating compounds
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The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
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Page/Page column 19
(2011/04/14)
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- C-PHENYL GLYCITOL COMPOUND
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Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, -O-(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is NHC(= NH)NH2 or -NHCON(RB)RC, n is not 1, Z is -CONHRA, -NHC(=NH)NH2 or -NHCON(RB)RC, Formula (A) or Formula (B).
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Page/Page column 83-85
(2008/06/13)
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- HISTAMINE-3 RECEPTOR ANTAGONISTS
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This invention is directed to a compound of the formula Ia or Ib. as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit disorder (ADD), attention-deficit hyperactivity disorder (ADHD), psychotic disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy- induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the Gl tract, hyper and hypo motility and acidic secretion of the gastro- intestinal tract, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above.
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Page/Page column 98
(2008/06/13)
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- Triazolopyridinylsulfanyl derivatives as p38 MAP kinase inhibitors
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A compound of formula (I), or a pharmaceutically acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
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Page/Page column 31
(2008/06/13)
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- Synthesis and Spectroscopic Data of Chlorinated 4-Hydroxybenzaldehydes
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All chlorinated 4-hydroxybenzaldehydes including three hitherto unknown compounds have been synthesized from chlorinated phenols by applying the Reimer-Tiemann method. (1)H NMR, (13)C NMR, and mass-spectral data on all compounds are reported.
- Knuutinen, Juha S.,Kolehmainen, Erkki T.
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p. 139 - 141
(2007/10/02)
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