- NEW BRADYKININ B1 ANTAGONISTS
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The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 202
(2010/04/03)
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- Continuous flow hydrogenation of functionalized pyridines
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The heterogeneous hydrogenation of substituted pyridines has been accomplished by employing a continuous flow hydrogenation device that incorporates in situ hydrogen generation by electrolysis of H20 and pre-packed catalyst cartridges. In general, the hydrogenation reactions proceeded smoothly regardless of the supported precious metal catalyst (Pd/C, Pt/C, or Rh/C). By using 30-80 bar of hydrogen pressure at 60-80 °C full conversion was typically achieved in all cases at a flow rate of 0.5 mL min -1, providing the corresponding piperidines in high yields. For disubstituted pyr idines, variations in stereoselectivity were observed depending on both the metal catalyst and the temperature/ pressure of the hydrogenation reaction. For ethyl nicotinate the selectivity between partial and full hydrogenation could be tuned depending on the hydrogen pressure, solvent, and the choice of supported metal catalyst. Changing the hydrogen source from H20 to D2C) allowed the preparation of de-uteriated derivatives. Wiley-VCH Verlag GmbH & Co. KGaA.
- Irfan, Muhammed,Petricci, Elena,Glasnov, Toma N.,Taddei, Maurizio,Kappe, C. Oliver
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experimental part
p. 1327 - 1334
(2009/07/19)
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- PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY
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The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: -N(R7)-, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: -N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
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Page/Page column 116-117
(2008/06/13)
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- TRICYCLIC 1,2,4-TRIAZINE OXIDES AND COMPOSITIONS THEREFROM FOR THERAPEUTIC USE IN CANCER TREATMENTS
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The invention relates to novel tricyclic 1,2,4-triazine-1-oxides and novel tricyclic 1,2,4-triazine-1,4-dioxides of formula: (I); and to related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
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Page/Page column 167
(2008/06/13)
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- 4-Amino-thieno[3,2-c]pyridine-7-carboxylic acid amides
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Disclosed are novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides, and their pharmaceutically acceptable salts and esters, that are selective inhibitors of KDR and/or FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular solid cancerous tumors of the breast, colon, lung and prostate. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer using these compounds.
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Page/Page column 16
(2010/02/14)
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- Cyclohexane derivatives and their use as therapeutic agents
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The present invention relates compounds of formula (I), wherein ring A is a phenyl or pyridyl ring; X represents a linker selected from the group consisting of formulae: (a), (b), (c), (d), and (e); and R1, R2, R3, R4, R5, R6, R7, R13, R14, R15, R16, R17, R21a and R21b are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
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- Benzothiazole derivatives with activity as adenosine receptor ligands
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The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
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- RING INVERSION EQUILIBRIA IN 4-CHLORO-, 4-BROMO-, AND 4-METHOXY-1-ALKYLPIPERIDINES IN A NON-POLAR SOLVENT
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The position of ring inversion equilibrium (axial Requuatorial R) in 4-R-N-alkylpiperidines (R = Cl, Br, or OMe), dissolved in CFCl3-CDCl3, has been determined by (13)C n.m.r. spectroscopy at low temperatures.In all three series, change of NH to NMe produces a marked increase in the proportion of conformation with axial R.When R is OMe, further alterations in the N-substituent from Me to Et, Pri, and CH2CF3 do not affect the equilibrium significantly, but the signifficant changes observed when R is halogen can be related to the inductive effect of the N-substituent. (13)C Chemical shifts, proportions of conformations, and conformational free energy differences are recorded for all systems studied.
- Bailey, Judith M.,Booth, Harold,Al-Shirayda, Hatif A.R.Y.,Trimble, Mary L.
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p. 737 - 744
(2007/10/02)
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