/pdf/aryl-aryl-bond-formation-one-century-after-the-discovery-of-1jdyxlkwix.pdf

Aryl-aryl bond formation one century after the discovery of the Ullmann reaction.

The mammalian ionotropic glutamate receptor family encodes 18 gene products that coassemble to form ligand-gated ion channels containing an agonist recognition site, a transmembrane ion permeation pathway, and gating elements that couple agonist-induced conformational changes to the opening or closing of the permeation pore. Glutamate receptors mediate fast excitatory synaptic transmission in the central nervous system and are localized on neuronal and non-neuronal cells. These receptors regulate a broad spectrum of processes in the brain, spinal cord, retina, and peripheral nervous system. Glutamate receptors are postulated to play important roles in numerous neurological diseases and have attracted intense scrutiny. The description of glutamate receptor structure, including its transmembrane elements, reveals a complex assembly of multiple semiautonomous extracellular domains linked to a pore-forming element with striking resemblance to an inverted potassium channel. In this review we discuss International Union of Basic and Clinical Pharmacology glutamate receptor nomenclature, structure, assembly, accessory subunits, interacting proteins, gene expression and translation, post-translational modifications, agonist and antagonist pharmacology, allosteric modulation, mechanisms of gating and permeation, roles in normal physiological function, as well as the potential therapeutic use of pharmacological agents acting at glutamate receptors.

/pdf/glutamate-receptor-ion-channels-structure-regulation-and-148yts0p6h.pdf

Glutamate Receptor Ion Channels: Structure, Regulation, and Function

Nickel-Catalyzed Cross-Couplings Involving Carbon-Oxygen Bonds Brad M. Rosen, Kyle W. Quasdorf, Daniella A. Wilson, Na Zhang, Ana-Maria Resmerita, Neil K. Garg,* and Virgil Percec* Roy & Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States Department of Chemistry and Biochemistry, University of California, Los Angeles, California 90095, United States

/pdf/nickel-catalyzed-cross-couplings-involving-carbon-oxygen-1zs88el3fl.pdf

Nickel-Catalyzed Cross-Couplings Involving Carbon-Oxygen Bonds

Catalytic cross-coupling reactions in biaryl synthesis

https://chemistry.mdma.ch/hiveboard/rhodium/pdf/indole.synth.review.1994-99.pdf

Recent developments in indole ring synthesis—methodology and applications

Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y = SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.

N-aryl(thio)anthranilic acid amide derivatives, their preparation and their use as vegf receptor tyrosine kinase inhibitors

Synthesis of diarylic compounds by palladium catalyzed reaction of aromatic triflates with boronic acids

VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridinamides, their production and use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis, as well as intermediate products for the production of the compounds are described. The compounds according to the invention can be used as or in the case of tumor or metastasis growth, psoriasis, Kaposi's sarcoma, restenosis, such as, e.g., stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukemia; arthritis, such as rheumatoid arthritis, hemangioma, angiofibroma; eye diseases, such as diabetic retinopathy, neovascular glaucoma; renal diseases, such as glomerulonephritis, diabetic nephropathy, malignant nephrosclerosis, thrombic microangiopathic syndrome, transplant rejections and glomerulopathy; fibrotic diseases, such as cirrhosis of the liver, mesangial cell proliferative diseases, arteriosclerosis, injuries to nerve tissue, and inhibition of the reocclusion of vessels after balloon catheter treatment, in vascular prosthetics or after mechanical devices are used to keep vessels open, such as, e.g., stents, as immunosuppressive agents, as a support in scar-free healing, senile keratosis and contact dermatitis. The compounds according to the invention can also be used as VEGFR-3 inhibitors in the case of lymphangiogenesis.

VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines

The invention relates to aza- and polyazanthranyl amides, to their use as medicaments for treating diseases caused by persistent angiogenesis and to their intermediate products for producing the aza- and polyazanthranyl amides.

Aza- and polyazanthranyl amides and their use as medicaments

The invention relates to selective anthranilamide pyridine amides as inhibitors of VEGFR-2 and VEGFR-3 and to their production and use as medicaments for treating diseases that are caused by persistent angiogenesis. The inventive compounds can be used for example in cases of psoriasis, Kaposi's sarcoma, restenosis, such as e.g. stent-induced restenosis, endometriosis, Crohn's disease, Hodgkin's disease, leukaemia, arthritis, such as rheumatoid arthritis, haemangioma, angiofibromatosis, in eye diseases such as diabetic retinopathy, neovascular glaucoma, in kidney diseases such as glomerulonephritis, diabetic nephropathy, malign nephrosclerosis, thrombic micro-angiopathic syndrome, transplant rejection and glomerulopathy, in fibrotic diseases such as hepatic cirrhosis, mesangial-cell proliferative diseases, arteriosclerosis, damage to the nerve tissue and inhibition of the re-occlusion of vessels after balloon catheter treatment, in vessel prosthetics or after the use of mechanical devices for keeping vessels open, e.g. stents, as immunosuppressants, to support wound healing without scars and in cases of age spots and contact dermatitis. The inventive compounds can also be used as inhibitors of VEGFR-3 in lymphangiogenesis for hyperplastic and dysplastic changes in the lymphatic system.

Andreas Huth

Papers

N-aryl(thio)anthranilic acid amide derivatives, their preparation and their use as vegf receptor tyrosine kinase inhibitors

Synthesis of diarylic compounds by palladium catalyzed reaction of aromatic triflates with boronic acids

VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridines

Aza- and polyazanthranyl amides and their use as medicaments

Selective anthranilamide pyridine amides as inhibitors of vegfr-2 and vegfr-3