- FE NANOPARTICLES WITH PPM CONTENTS OF PD, CU AND/OR NI, REACTIONS IN WATER CATALYZED BY THEM
-
The present application discloses a nanoparticle composition prepared from a mixture comprising: a) a transition metal salt; b) an iron salt; and c) a reducing agent; and methods for the use of such compositions, including the reduction of an organic compound comprising a nitro group to form an organic compound comprising an amine group, the Cu-catalyzed cyclization of an azide and an alkyne (click chemistry) and cross coupling reactions, notably Suzuki-Miyaura reactions. The transition metal salts are in particular Pd, Cu and Ni salts, the content of these metals being typically in the ppm range based on the major constituent Fe in the final products.
- -
-
Paragraph 0077; 0078
(2017/07/14)
-
- Design of photoaffinity labeling probes derived from 3,4,5-trimethylfuran-2(5H)-one for mode of action elucidation
-
Herein we report the synthesis of new probes for photoaffinity labeling with the aim of receptor identification and mode of action elucidation of 3,4,5-trimethylfuran-2(5H)-one (TMB), recently identified in the smoke of burning vegetation as an efficient seed germination inhibitor. These photoaffinity probes consist of an ethynyl group that acts as a tag for introduction of an optional detectable marker unit by an appropriate chemoselective ligation method after the photo-cross-linking operation.
- Po?ta, Martin,Soós, Vilmos,Beier, Petr
-
p. 3809 - 3817
(2016/07/06)
-
- Bioreduction of aryl azides during mutasynthesis of new ansamitocins
-
Supplementing a culture of a mutant strain of Actinosynnema pretiosum that is unable to biosynthesize aminohydroxy benzoic acid (AHBA), with 3-azido-5-hydroxy-benzoic acid and 3-azido-5-amino-benzoic acid, unexpectedly yielded anilino ansamitocins instead
- Mancuso, Lena,Juerjens, Gerrit,Hermane, Jekaterina,Harmrolfs, Kirsten,Eichner, Simone,Fohrer, Joerg,Collisi, Wera,Sasse, Florenz,Kirschning, Andreas
-
supporting information
p. 4442 - 4445
(2013/09/24)
-
- Zinc phthalocyanine with PEG-400 as a recyclable catalytic system for selective reduction of aromatic nitro compounds
-
Zinc phthalocyanine with PEG-400 was established as a catalytic system for chemo and regioselective reduction of aromatic nitro compounds to corresponding amines. A large range of reducible functional groups such as acid, amide, ester, halogen, lactone, nitrile, N-benzyl, O-benzyl, hydroxy and heterocycles were well tolerated. Direct synthesis of benzotriazole from O-dinitrobenzene was achieved for the first time. The present catalytic system was successfully employed for the reduction of carbonyl and ester compounds to corresponding alcohols and reductive amination of benzaldehydes with primary amines to form corresponding secondary amines. Remarkable advantages of the present catalytic method include low loading of metal, avoidance of toxic ligands and high isolated yields. The catalyst was recyclable up to four times without any loss of selectivity and activity.
- Sharma, Upendra,Kumar, Neeraj,Verma, Praveen Kumar,Kumar, Vishal,Singh, Bikram
-
supporting information; experimental part
p. 2289 - 2293
(2012/09/10)
-
- Pteridinone derivatives as PI3-kinases inhibitors
-
New compounds of formula 1 are provided which by virtue of their pharmaceutical activity as PI3-kinase modulators may be used in the therapeutic field for the treatment of inflammatory or allergic diseases. Examples of these include inflammatory and allergic respiratory complaints, inflammatory diseases of the gastro-intestinal tract and motor apparatus, inflammatory and allergic skin diseases, inflammatory eye diseases, diseases of the nasal mucosa, inflammatory or allergic conditions involving autoimmune reactions or inflammations of the kidney.
- -
-
Page/Page column 12
(2008/12/07)
-
- BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs)
-
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of pot
- Clarke, Brian,Demont, Emmanuel,Dingwall, Colin,Dunsdon, Rachel,Faller, Andrew,Hawkins, Julie,Hussain, Ishrut,MacPherson, David,Maile, Graham,Matico, Rosalie,Milner, Peter,Mosley, Julie,Naylor, Alan,O'Brien, Alistair,Redshaw, Sally,Riddell, David,Rowland, Paul,Soleil, Virginie,Smith, Kathrine J.,Stanway, Steven,Stemp, Geoffrey,Sweitzer, Sharon,Theobald, Pam,Vesey, David,Walter, Daryl S.,Ward, John,Wayne, Gareth
-
p. 1011 - 1016
(2008/12/20)
-
- Second generation of hydroxyethylamine BACE-1 inhibitors: Optimizing potency and oral bioavailability
-
BACE-1 inhibition has the potential to provide a disease-modifying therapy for the treatment of Alzheimer's disease. Optimization of a first generation of BACE-1 inhibitors led to the discovery of novel hydroxyethylamines (HEAs) bearing a tricyclic nonprime side. These derivatives have nanomolar cell potency and are orally bioavailable.
- Charrier, Nicolas,Clarke, Brian,Cutler, Leanne,Demont, Emmanuel,Dingwall, Colin,Dunsdon, Rachel,East, Philip,Hawkins, Julie,Howes, Colin,Hussain, Ishrut,Jeffrey, Phil,Maile, Graham,Matico, Rosalie,Mosley, Julie,Naylor, Alan,O'Brien, Alistair,Redshaw, Sally,Rowland, Paul,Soleil, Virginie,Smith, Kathrine J.,Sweitzer, Sharon,Theobald, Pam,Vesey, David,Walter, Daryl S.,Wayne, Gareth
-
supporting information; experimental part
p. 3313 - 3317
(2009/04/06)
-
- β SECRETASE INHIBITOR
-
Disclosed is a compound represented by the formula (1) below which is useful as a drug for treating Alzheimer's disease, or a pharmaceutically acceptable salt thereof. (1) [In the formula, R1 represents a group represented by the following formula (2): (2) (wherein X represents a nitrogen atom or a group expressed as C(R5); Y represents a nitrogen atom or a group expressed as C(R6); and R5 and R6 independently represent a hydrogen atom or the like) or the like; m represents an integer of 1-6; L1 represents a single bond or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group or the like; R3 represents a hydrogen atom or the like; L2 represents a single bond or the like; and R4 represents a hydrogen atom, a substituted or unsubstituted aryl group or the like.]
- -
-
Page/Page column 35
(2008/06/13)
-
- CONTRAST AGENTS AND DIAGNOSTIC COMPOSITIONS BASED ON IODINE-CONTAINING CYANURIC ACID DERIVATIVES
-
The present invention relates to a class of compounds of Formula (I) and to diagno stic compositions containing such compounds where the compounds are iodine conta ining compounds. More specifically the iodine containing compounds are chemical compounds containing a cyanuric acid scaffolding moiety allowing for the arrange ment of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imag ing and in particular in X-ray imaging and to contrast media containing such com pounds .
- -
-
Page/Page column 16
(2008/06/13)
-
- HYDROXYETHYLAMINE DERIVATIVES FOR THE TREATMENT OF ALZHEIMER'S DISEASE
-
The present invention relates to novel hydroxyethylamine compounds of formula (I): (I) having Asp2 (-secretase, BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated-amyloid levels or-amyloid deposits, particularly Alzheimer's disease.
- -
-
-
- PYRROLE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
-
Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein A, R1, R2a, R2b, Rx, R8, and R9 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine, in particular their use in the treatment of prostaglandin mediated diseases such as pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
- -
-
Page 142-143
(2010/02/05)
-