- A Heteroditopic Hexa-imidazole 'Encapsulating' Podand and a Facially Differentiated Hexadentate Ligand
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Syntheses of the facially differentiated tris-imidazole triamine (10) and of the novel 'hetero'-ditopic hexa-imidazole ligand (11), from histamine (3), are described.
- Potvin, Pierre G.,Wong, Man Hung
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- Synthesis, anti-proliferative activity, and toxicity of C4(C5) substituted N,N′-bis(arylmethyl)imidazolium salts
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The syntheses and characterization of C4and C5substituted N,N′-bis(arylmethyl)imidazolium salts with hydrophilic or lipophilic substituents on the imidazole ring are reported. A structure-activity relationship study revealed that the
- Shelton, Kerri L.,DeBord, Michael A.,Wagers, Patrick O.,Southerland, Marie R.,Taraboletti, Alexandra,Robishaw, Nikki K.,Jackson, Daniel P.,Tosanovic, Radisa,Kofron, William G.,Tessier, Claire A.,Paruchuri, Sailaja,Shriver, Leah P.,Panzner, Matthew J.,Youngs, Wiley J.
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- 2-(1H-Imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chain variants of the IGF-1R inhibitor BMS-536924
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A series of IGF-1R inhibitors is disclosed, wherein the (m-chlorophenyl)ethanol side chain of BMS-536924 (1) is replaced with a series of 2-(1H-imidazol-4-yl)ethanamine and 2-(1H-pyrazol-1-yl)ethanamine side chains. Some analogs show improved IGF-1R poten
- Saulnier, Mark G.,Frennesson, David B.,Wittman, Mark D.,Zimmermann, Kurt,Velaparthi, Upender,Langley, David R.,Struzynski, Charles,Sang, Xiaopeng,Carboni, Joan,Li, Aixin,Greer, Ann,Yang, Zheng,Balimane, Praveen,Gottardis, Marco,Attar, Ricardo,Vyas, Dolatrai
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- Bistellettazines A-C and bistellettazole A: new terpenyl-pyrrolizidine and terpenyl-imidazole alkaloids from a southern Australian marine sponge, Stelletta sp
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(Chemical Equation Presented) Four new alkaloids have been isolated during chemical investigations into a southern Australian marine sponge, Stelletta p. Detailed spectroscopic analysis, supported by chemical degradation and partial synthesis, permitted structure elucidation of bistellettazines A-C (1-3), the first reported examples of terpenyl-pyrrolizidine conjugates, and bistellettazole A (4), a unique cyclic terpenyl-imidazole conjugate. The alkaloids 1-4 feature unprecedented carbon skeletons that are proposed to share a common convergent biosynthetic origin, arising via the biogenic equivalent of a Diels-Alder addition between two hypothetical polyenyl norsesquiterpene precursors.
- El-Naggar, Mohamed,Piggott, Andrew M.,Capon, Robert J.
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- FUSED BICYCLIC COMPOUNDS AS INHIBITORS FOR PI3 KINASE
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The invention relates to compounds of formula (I) for the regulation of phosphoinositides 3-kinases activity and related diseases.
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Page/Page column 123
(2010/09/18)
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- THIAZOLYL-DIHYDRO-CYCLOPENTAPYRAZOLE
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Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures
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Page/Page column 17
(2008/06/13)
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- THIAZOLYL-DIHYDRO-CHINAZOLINE
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Disclosed are compounds of general formula (I), wherein the groups A, R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-quinazolines and the use thereof as pharmaceutical compositions.
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Page/Page column 21
(2008/06/13)
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- THIAZOLYL-DIHYDRO-INDAZOLE
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Disclosed are compounds of general formula (I), wherein the groups R1, R2, Ra and Rb have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers and the mixtures thereof, and optionally the pharmacologically acceptable acid addition salts, solvates and hydrates thereof, and processes for preparing these thiazolyl-dihydro-indazoles and the use thereof as pharmaceutical compositions.
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Page/Page column 20
(2008/06/13)
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- PURINE DERIVATIVES AS AGONISTS OF THE ADENOSINE A2A RECEPTOR
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The invention relates to novel adenosine receptor agonists of formula (I), methods for their manufacture and their use as medicaments.
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Page/Page column 39
(2010/11/25)
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- THIAZOLE DERIVATIVES AND USE THEREOF
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The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
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Page/Page column 68; 69
(2010/11/25)
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- PURINE DERIVATIVES ACTING AS A2A RECEPTOR AGONISTS
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Compounds of formula (I) in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
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Page/Page column 49
(2008/06/13)
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- METAL COMPLEXES OF N-HETEROCYCLIC CARBENES AS RADIOPHARMACEUTICALS AND ANTIBIOTICS
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A method for inhibiting microbial growth comprises administering an effective amount of a silver complex of a N-heterocyclic amine. A method for treating cancer cells or a method for imaging one or more tissues of a patient includes administering an effective amount of a complex of a N-heterocyclic amine and a radioactive metal. N-heterocyclic carbenes of the present invention may be represented by formula (I) wherein Z is a heterocyclic group, and R1 and R2 are, independently or in combination, hydrogen or a C1-C12 organic group selected from the group consisting of alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, aryl, arylalkyl, alkylaryl, heterocyclic, and alkoxy groups and substituted derivatives thereof.
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Page/Page column 12-13
(2010/02/11)
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- The selective synthesis of 1-methyl-1H-histamines
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The selective synthesis of 1-methyl-1H-4-histamine (1) and 1-methyl-1H-5-histamine (2) via 5-oxo-5,6,7,8-tetrahydroimidazo[1,5-c]pyrimidine (3) from commercially available histamine hydrochloride salt is described.
- Collman,Zhong,Costanzo
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p. 195 - 197
(2007/10/03)
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- Regiospecific synthesis of 2,3-disubstituted-L-histidines and histamines
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Regiospecific synthesis of 2,3-disubstituted-L-histidines and 2,3-disubstituted histamines starting from L-histidine methyl ester and histamine is reported. The key step involves homolytic free radical alkylation via silver catalyzed oxidative decarboxyla
- Narayanan, Sanju,Vangapandu, Suryanarayana,Jain, Rahul
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p. 1133 - 1136
(2007/10/03)
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- Regiospecific alkylation of histidine and histamine at N-1 (τ)
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Series of 1-alkyl histidines and histamines have been synthesized by the alkylation of the corresponding 5,6,7,8-tetrahydro-5-oxomidazo[1,5-c]pyrimidines with alkyl halides in aprotic solvents. The method of conversion of the intermediate quaternary salt to the amino acid or amino depends on the nature of the alkyl group.
- Jain, Rahul,Cohen, Louis A.
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p. 5363 - 5370
(2007/10/03)
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- Zn(2+) Inclusion Complexes of Endodentate Tripodands as Carbonic Anhydrase-Inspired Artificial Esterases
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Facile syntheses are reported for three endo-tridentate tris-imidazole podands 1 - 3, two of which also bear basic amino residues, designed to reproduce the active site of carbonic anhydrase.The architecture was tested for the ability to bind Zn(2+) in a
- Jairam, Rick,Potvin, Pierre G.
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p. 4136 - 4141
(2007/10/02)
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- Anti-ulcer and antisecretory activity of selected imidazopiperidines
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New thioureas and ureas with an interesting anti-ulcer and antisecretory activity are presented. The chemical synthesis, determination of the structure, and structure-activity relationships of the compounds are discussed.
- Arcari,Bernardi,Cimaschi,Falconi,Luini,Scarponi
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p. 1467 - 1471
(2007/10/02)
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