- SUBSTITUTED PYRAZOLES FFA4/GPR120 RECEPTOR AGONISTS
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The present invention refers to compounds of formula (I) or a pharmaceutically acceptable salt thereof: Formula (I). These compounds have FFA4/GPR120 receptor (FFA4) agonistic properties. The invention refers also to pharmaceutical compositions comprising these compounds, chemical processes for preparing them and their use in the treatment or prophylaxis of diseases associated with FFA4 receptor activity in animals, in particular humans.
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Page/Page column 46; 88
(2019/10/04)
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- Fibrinogen receptor antagonists and their use
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This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.
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Page/Page column 65
(2010/08/04)
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- A new and efficient route for the synthesis of naturally occurring catecholamines
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Catecholamines, sympathomimetic drugs and adrenergic receptor antagonists, have been prepared by a regioselective oxidation of the corresponding 4-hydroxyphenethylamine derivatives by 2-iodoxybenzoic acid (IBX) in homogeneous as well as in heterogeneous conditions and followed by cleavage of the amino protective group. By using polymer-supported IBX, after the first oxidation, the oxidant can be recovered, regenerated, and efficiently reused for several additional times. An efficient, easy and green procedure for the synthesis of N-(methoxycarbonyl)dopamine, key component of many pharmaceuticals, has also been reported. Georg Thieme Verlag Stuttgart.
- Bernini, Roberta,Crisante, Fernanda,Barontini, Maurizio,Fabrizi, Giancarlo
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experimental part
p. 3838 - 3842
(2010/03/30)
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- Phenethanolamine-derived haptens, immunogens and conjugates comprising them and antibodies recognising said immunogenes and conjugates
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The present invention relates to a method for preparing haptens of formulae I and II that are useful in the preparation of immunogens, antibodies and conjugates, for use in competitive immunoassays for the detection of ractopamine, isoxsuprine and ritodrine. The haptens are prepared by reacting a phenylethanolamine derivative of formula D with a phenylalkylcarbonyl derivative of formula E: in which, in formula I, Z1 is a crosslinker and Z2 is H and, in formula II, Z1 is H and Z2 is a crosslinker.
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Page/Page column 10; 24
(2010/11/08)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 158
(2008/06/13)
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- FIBRINOGEN RECEPTOR ANTAGONISTS AND THEIR USE
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This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.
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Page/Page column 79
(2010/02/11)
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- Enantiomers of adrenaline-type amino alcohols by Burkholderia cepacia lipase-catalyzed asymmetric acylation
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The enantiomers of norphenylephrine and octopamine were prepared using lipase PS-catalyzed enantioselective acylation with butanoic anhydride. Burkholderia cepacia lipase-catalyzed acylation with butanoic anhydride was used for the preparation of pharmaceutically important norphenylephrine and octopamine enantiomers, all in 98% ee. Reactivity of the phenolic OH groups and easy racemization, especially in the case of octopamine, complicated optimization. For norphenylephrine, chemical N-acylation was fast and allowed the subsequent enzymatic benzylic acylation in situ. The preparation of the octopamine enantiomers became possible by using the N-Fmoc protected substrate and by the Candida antarctica lipase B-catalyzed deprotection of the OH groups before the N-deprotection was performed.
- Lundell, Katri,Katainen, Erja,Kiviniemi, Anu,Kanerva, Liisa T.
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p. 3723 - 3729
(2007/10/03)
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