13300-09-9Relevant articles and documents
Development of a novel therapeutic suppressor of brain proinflammatory cytokine up-regulation that attenuates synaptic dysfunction and behavioral deficits
Hu, Wenhui,Ralay Ranaivo, Hantamalala,Roy, Saktimayee M.,Behanna, Heather A.,Wing, Laura K.,Munoz, Lenka,Guo, Ling,Van Eldik, Linda J.,Watterson, D. Martin
, p. 414 - 418 (2007)
We report the development of a novel, aqueous-soluble, safe, small molecule, experimental therapeutic that suppresses injury-induced, proinflammatory cytokine increases in the brain, with resultant attenuation of synaptic protein biomarker loss and improvement in hippocampus-dependent behavioral deficits. A GMP production scheme for the active pharmaceutical ingredient, compound 17, is presented. The development and large-scale availability of this novel compound allow exploration of new, potentially disease-modifying, therapeutic approaches to CNS disorders.
FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS
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Page/Page column 27-28, (2010/01/31)
The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfenyl, sulfinyl, sulfonyl, sulfonate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, ═O, ═S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof. The invention additional relates to compositions comprising the compounds, and methods of using the compounds and compositions for modulation of cellular pathways, for treatment or prevention of inflammatory diseases, for research, drug screening, and therapeutic applications.
New, simple and versatile synthesis of 4,6-disubstituted pyridazin-3(2H)-ones
Albrecht, Anna,Koszuk, Jacek,Kobucinski, Michal,Janecki, Tomasz
experimental part, p. 1197 - 1200 (2008/10/09)
A simple, two-step synthesis of 4,6-disubstituted pyridazin-3(2H)-ones starting from 2-diethoxyphosphoryl-4-oxoalkanoates and hydrazines is described. The intermediate 4-diethoxyphosphoryl-4,5-dihydropyridazin-3(2H)-ones obtained in this way are used in a
Synthesis of regiospecifically polysubstituted pyridazinones
de Araújo-Júnior, Jo?o X.,Schmitt, Martine,Antheaume, Cyril,Bourguignon, Jean-Jacques
, p. 7817 - 7820 (2008/03/11)
Desymmetrization of pyridazine-3,6-diones by the use of N-benzyl protective groups leads to useful starting materials for building polysubstituted pyridazine libraries in a regioselective manner.
COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND CHOLINESTERASE INHIBITORS
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Page/Page column 85-87; 89-90; 2/13; 5/13, (2008/06/13)
The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
COMPOSITIONS AND TREATMENTS FOR DEMYELINATING DISEASES AND PAIN DISORDERS
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Page/Page column 67; 70-71; 2/13; 5/13, (2008/06/13)
The invention relates to compositions and methods for treating patients with Demyelinating Diseases and Conditions including Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compositions and methods may also be used for Stroke Rehabilitation and the treatment of pain disorders including Neuropathic Pain and Chemokine-Induced Pain. The compositions comprise one or more pyridazine compounds having a pyridazinyl radical pendant with an aryl or substituted aryl, a heteroaryl or substituted heteroaryl.
SALTS OF PYRIDAZINE COMPOUNDS
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Page/Page column 57-58, (2008/06/13)
The invention relates to stable and substantially purified synthetic pharmaceutically acceptable acid addition salts of pyridazine compounds of the formula I wherein R10 is hydrogen, hydroxyl, alkyl, alkoxy, alkenyl, alkynyl, alkylene, aryl, heteroaryl, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, carboxyl, carbonyl, carbamoyl, carboxamide, or phosphonate, and R11 is alkyl, alkoxy, alkenyl, alkynyl, alkylene, alkenylene, alkenyloxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, sulfonyl, sulfinyl, sulfenyl, amino, imino, azido, thiol, thioalkyl, thioalkoxy, thioaryl, nitro, cyano, halo, =0, =S, phosphonate, carboxyl, carbonyl, carbamoyl, carboxamide, or ureido. The invention also relates to formulations, dosage forms and compositions comprising the salts, and methods of using the salts, formulations, dosage forms and compositions.
COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND SECRETASES
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Page/Page column 86-87; 90, (2010/11/29)
The invention relates to compositions, conjugates and methods comprising pyridazine compounds and secretase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.
Bicyclic heterocycles as cannabinoid receptor modulators
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Page/Page column 13-14, (2008/06/13)
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the general Formula I: including all prodrugs, pharmaceutically acceptable salts and stereoisomers, R1, R2, R3, R3a, R4, A, B, n, Y and Z are described herein.
Sequential regio and chemoselective cross-coupling reactions by means of O6-tri-isopropylsulfonate of 4-bromo-pyridazine 3,6-dione
de Araújo-Júnior, Jo?o X.,Schmitt, Martine,Benderitter, Pascal,Bourguignon, Jean-Jacques
, p. 6125 - 6128 (2007/10/03)
Regioselective desymmetrization of 4-substituted pyridazin-3,6-diones using sterically hindered 2,4,6-triisopropylphenyl-sulfonylchloride allowed efficient sequential palladium cross-coupling reactions.