- IAP ANTAGONISTS AND THEIR THERAPEUTIC APPLICATIONS
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The present invention relates to Formula I. compounds including their isomers, tautomeric forms and rotamers, salts together with their manufacturing process and their pharmacological use alone or in combination with other active ingredients for the treatment of cell and tissue malignances caused diseases, including uncontrolled cell or tissue growth, proliferation and cancer.
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Page/Page column 34-35
(2021/11/06)
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- Heterocyclic acylamide derivative and preparation method and pharmaceutical application thereof
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The invention relates to a heterocyclic acylamide derivative and a preparation method and pharmaceutical application thereof, in particular to a heterocyclic acylamide derivative shown as a general formula (I) or a stereoisomer and a pharmaceutically-acce
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Paragraph 0668; 0669; 0670; 0671; 0672; 0673
(2017/07/19)
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- Remarkable configurational stability of magnesiated nitriles
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Quaternary stereocenters: Chiral α-magnesiated nitriles can be formed by deprotonation and are configurationally stable at low temperature, even for acyclic examples. These can be trapped with electrophiles to give enantiomerically enriched quaternary substituted products (see scheme; TMP=2,2,6,6-tetramethylpiperidine). Copyright
- Barker, Graeme,Alshawish, Madeha R.,Skilbeck, Melanie C.,Coldham, Iain
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p. 7700 - 7703
(2013/08/23)
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- THERAPEUTIC COMPOUNDS: PYRIDINE AS SCAFFOLD
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Compounds of formulas I, IA, and IB or IC or pharmaceutically acceptable salts thereof: wherein A, A1, A2, A3, A4, R2, R3, R4 and n are as defined in the specifications well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
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Page/Page column 105
(2010/02/14)
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- PYRROLOPYRIDINE-2-CARBOXYLIC ACID AMIDE INHIBITORS OF GLYCOGEN PHOSHORYLASE
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Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.
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- Thiazole benzamide derivatives and pharmaceutical compositions for inhibiting cell proliferation, and methods for their use
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Aminothiazole compounds with mono-/di-substituted benzamide are represented by the Formula (I), and their pharmaceutically acceptable salts, pharmaceutically acceptable prodrugs, pharmaceutically active metabolites, and pharmaceutically acceptable salts of said metabolites are described. These agents modulate and/or inhibit the cell proliferation and activity of protein kinases and are useful as pharmaceuticals for treating malignancies and other disorders.
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- Heterocyclic compounds as inhibitors of rotomase enzymes
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Compounds of the formula: wherein R1, Y, W, A and R2are as defined above are inhibitors of rotamase enzymes in particular FKBP-12 and FKBP-52. The compounds therefore moderate neuronal regeneration and outgrowth and can be used for treating neurological disorders arising from neurodegenerative diseases and nerve damage.
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- Dopamine Receptor Modulation by Pro-Leu-Gly-NH2 Analogues Possessing Cyclic Amino Acid Residues at the C-Terminal Position
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The synthesis of several analogues of L-prolyl-L-leucylglycinamide (PLG) was carried out in which the glycinamide residue was replaced with the following cyclic amino acid residues: L- and D-prolinamide, (+)- and (-)-thiazolidine-2-carboxamide, L- and D-3
- Johnson, Rodney L.,Rajakumar, G.,Mishra, Ram K.
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p. 2100 - 2104
(2007/10/02)
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- Tripeptides acting on the central nervous system and a process for the preparation thereof
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The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I), wherein X is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group, Y is L-leucyl, L-norvalyl or L-histidyl group, and W is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, or the W-NH2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof. These compounds are prepared by methods commonly applied in the peptide chemistry.
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- Tripeptides acting on the central nervous system and a process for the preparation thereof
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The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I), wherein X is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleu
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