- ANTIDIABETIC TRICYCLIC COMPOUNDS
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Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR 40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds may be useful in the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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Page/Page column 116
(2015/12/08)
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- SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
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This invention provides compounds of formula (I): wherein R1, R1b, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
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Page/Page column 50
(2012/02/01)
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- ALKYNYL ARYL CARBOXAMIDES
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The present invention is related to alkynyl aryl carboxamides of Formula (I’) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance. insulin resistance, hyperlipidemia, hypertriglyceridemia- hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I’) to modulate, notably to inhibit the activity of PTPs. (I’) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1and R2 are independently from each other is selected from the group consisting of hydrogen or (CI-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1 -C6 alkyl, carboxy, C1-C6 alkoxy, C1 -C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
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Page/Page column 55
(2008/06/13)
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- Radiolabeled platelet GPIIb/IIIa receptor antagonists as imaging agents for the diagnosis of thromboembolic disorders
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This invention provides novel radiopharmaceuticals that are radiolabeled cyclic compounds containing carbocyclic or heterocyclic ring systems which act as antagonists of the platelet glycoprotein IIb/IIIa complex; to methods of using said radiopharmaceuticals as imaging agents for the diagnosis of arterial and venous thrombi; to novel reagents for the preparation of said radiopharmaceuticals; and to kits comprising said reagents.
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- The synthesis of novel structural analogues of sialyl Lewis(x)
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The synthesis of conformationally rigid tetralin-based mimics of the tetrasaccharide sialyl Lewis(x) are described. Palladium catalysed coupling reactions are employed in the key synthetic steps.
- Murphy, Paul V.,Hubbard, Rod E.,Manallack, David T.,Montana, John G.,Taylor, Richard J. K.
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p. 3273 - 3276
(2007/10/03)
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- The design, synthesis, and evaluation of novel conformationally rigid analogues of sialyl Lewis(x)
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The design and synthesis of a series of analogues of sialyl Lewis(x) (1) which incorporate conformationally rigid tetralin and naphthalene ring systems (2-4) has led to novel compounds which have similar potency to 1 as inhibitors of cell adhesion. Copyright (C) 1998 Elsevier Science Ltd.
- Murphy, Paul V.,Hubbard, Rod E.,Manallack, David T.,Wills, Ruth E.,Montana, John G.,Taylor, Richard J. K.
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p. 2421 - 2439
(2007/10/03)
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- Template-Assembled Synthetic Proteins (TASP). Cyclic Templates with Incorporated Turn-Inducing Mimics
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The 8-amino-5,6,7,8-tetrahydronaphth-2-oic acid (1), 8-(aminomethyl)-5,6,7,8-tetrahydronaphth-2-oic acid (2), and 8-(aminomethyl)naphth-2-oic acid (3) were synthesized in their protected forms as turn-inducing dipeptide mimics.Two of them (2 and 3) were i
- Ernest, Ivan,Kalvoda, Jaroslav,Sigel, Christoph,Rihs, Grety,Fritz, Hans,et al.
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p. 1539 - 1563
(2007/10/02)
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- Synthesis of Benzoic and Tetralone Carboxylic Acid Esters from Phenols by Palladium Catalyzed Alkoxy/Aryloxy Carbonylation
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Various phenols with an acyl group conjugated to the aromatic system were converted via trifluoromethanesulfonates into benzoic acid esters by a palladium catalyzed alkoxy/aryloxy carbonylation.
- Gerlach, Uwe,Wollmann, Theo
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p. 5499 - 5502
(2007/10/02)
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