- Macrocyclic compounds and methods for their production
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There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.
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Page/Page column 38
(2015/11/10)
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- Sanglifehrin Derivatives and Methods for Their Production
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There are provided inter alia compounds of formula (I) and (II) and their use in therapy, particularly for the treatment of viral infection.
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Paragraph 0152
(2014/04/03)
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- Novel Dosage Form
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There is provided inter alia a pharmaceutical dosage form for oral administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral admin
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Paragraph 0255; 0257
(2014/09/03)
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- NOVEL DOSAGE FORM
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There is provided inter alia apharmaceutical dosage form fororal administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral adminis
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Page/Page column 62
(2013/05/21)
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Disclosed herein are substantially pure forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, stereoisomer or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
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Page/Page column 61-62
(2010/11/04)
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- IMIDAZOPYRAZINE TYROSINE KINASE INHIBITORS
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Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein Q1 and R1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.
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Page/Page column 184
(2008/06/13)
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- Synthesis of high-specific-radioactivity 4- and 6-[18F]fluorometaraminol- PET tracers for the adrenergic nervous system of the heart
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Fluorine-18 (t12:109.8min)-labeled analogues of metaraminol, 4-[18F]FMR ((1R,2S)-2-amino-1-(4-[18F]fluoro-3-hydroxy phenyl)-1-propanol) and 6-[18F]FMR ((1R,2S)-2-amino-1-(2-[18F]fluoro-5-hydroxyphenyl)-1-propanol), were synthesized as new positron-emission-tomography (PET) tracers for mapping cardiac adrenergic nerve terminals. Copyright
- Langer, Oliver,Dollé, Frédéric,Valette, Héric,Halldin, Christer,Vaufrey, Fran?oise,Fuseau, Chantal,Coulon, Christine,Ottaviani, Michéle,N?gren, Kjell,Bottlaender, Michel,Maziére, Bernard,Crouzel, Christian
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p. 677 - 694
(2007/10/03)
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- Substituted alkylamine derivatives
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The substituted alkylamine derivatives represented by formula (I) STR1 wherein R1 represents (a) substituted or unsubstituted C2-6 alkenyl group, (b) substituted or unsubstituted C3-6 cycloalkenyl group, (c) substituted or unsubstituted C2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru11 -Ar wherein R11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; STR2 represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R7, X and Y are linking groups, R2 is H or lower alkyl, R3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl, R4 and R5 are independently hydrogen or halogen atoms, R6 represents (a) substituted or unsubstituted acyclic hydrocarbon group which may be unsaturated, (b) substituted or unsubstituted cycloalkyl group, or (c) substituted or unsubstituted phenyl group, or non-toxic salts thereof. (E)-N-(6-6-dimethyl-2-hepten-4-ynyl)-N-ethyl-3-[4-(3-thienyl)-2-thienyl-methyloxy]benzylamine hydrochloride is a representative example. The substituted alkylamine derivatives are useful as pharmaceuticals, particularly for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.
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- Synthesis and Adrenergic Activity of Ring-Fluorinated Phenylephrines
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2-Fluoro-, 4-fluoro-, and 6-fluorophenylephrine (6-FPE) were synthesized from the corresponding fluorinated 3-hydroxybenzaldehydes.New routes to 2-fluoro- and 6-fluoro-3-hydroxybenzaldehydes were developed based on regioselective lithiation of 2- and 4-fluorobenzene ortho to fluorine.As with norepinephrine and isoproterenol analogues, the adrenergic properties of phenylephrine were markedly altered by ring fluorination.The order of potency of the fluoro analogues as α1-adrenergic agonists in the stimulation of contraction of aorticstrips and of phosphatidylinositol turnover and potentiation of cyclic AMP accumulation in guinea pig synaptoneurosomes was 6-FPE > PE > 4-FPE > 2-FPE.The same pattern was observed for the displacement of radioligands specific for α1- and α2-adrenergic receptors on brain membranes.The order of potency for the displacement of 3H>dihydroalprenolol, a β-specific adrenergic ligand from brain membranes, was 2-FPE > 4-FPE = PE >> 6-FPE. 6-FPE was much more selective for α-adrenergic receptors compared to β-receptors than was phenylephrine.A rationale for the observed fluorine-induced alterations in potency and selectivity of the FPEs for α- and β-adrenergic systems is presented based on fluorine-induced conformations due to electrostatic repulsion of fluorine and the benzyl hydroxyl group.
- Kirk, Kenneth L.,Olubajo, Olarangbe,Buchhold, Konstantin,Lewandowski, Gail A.,Gusovsky, Fabian,et al.
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p. 1982 - 1988
(2007/10/02)
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