94477-36-8Relevant academic research and scientific papers
FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS
-
Page/Page column 29, (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.
COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND CHOLINESTERASE INHIBITORS
-
Page/Page column 93-94; 7/13, (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
-
Page/Page column 74; 7/13, (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.
COMPOSITIONS AND TREATMENTS USING PYRIDAZINE COMPOUNDS AND SECRETASES
-
Page/Page column 94, (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.
3,4,6-Substituted pyridazines for treating neuropathic pain and associated syndromes
-
Page/Page column 17, (2008/06/13)
The present invention is directed to the use of 3,4,6-substituted pyridazines such as those characterized by structure I for treating conditions such as neuropathic pain among others.
A New Synthetic Route to 4,6-Diarylpyridazinones and Some of their Derivatives
Coudert, P.,Couquelet, J.,Tronche, P.
, p. 799 - 802 (2007/10/02)
A novel approach to the titled ring system starting from conveniently available chalcones 1 is proposed.It involves a catalysed exchange of hydrogen cyanide between acetone cyanohydrin and 1.The resulting γ-ketonitriles 2 give the expected 4,6-diarylpyrid
Synthesis and Structure-Activity Relationships of Series of Aminopyridazine Derivatives of γ-Aminobutyric Acid Acting as Selective GABA-A Antagonists
Wermuth, Camille-Georges,Bourguignon, Jean-Jacques,Schlewer, Gilbert,Gies, Jean-Pierre,Schoenfelder, Angele,et al.
, p. 239 - 249 (2007/10/02)
We have recently shown that an aryloaminopyridazine derivarive of GABA, SR 95103 , is a selective and competitive GABA-A receptor antagonist.In order to further explore the structural requirements for GABA receptor affinity, we synthesized a series of 38 compounds by attaching various pyridazinic structures to GABA or GABA-like side chains.Most of the compounds displaced GABA from rat brain membranes.All the active compounds antagonized the GABA-elicited enhancement of diazepam binding, strongly suggesting that all these compounds are GABA-A receptor antagonists.None of the compounds that displaced GABA from rat brain membranes interacted with other GABA recognition sites (GABA-B receptor, GABA uptake binding site, glutamate decarboxylase, GABA-transaminase).They did not interact with the Cl- ionophore associated with the GABA-A receptor and did not interact with the benzodiazepine, strychnine, and glutamate binding sites.Thus these compounds appear to be specific GABA-A receptor antagonists.In terms of structure-activity, it can be concluded that a GABA moiety bearing a positive charge is necessary for optimal GABA-A receptor recognition.Additional binding sites are tolerated only if they are part of a charge-delocalized amidinic or guanidinic system.If this delocalization is achieved by linking a butyric acid moiety to the N(2) nitrogen of a 3-aminopyridazine, GABA-antagonistic character is produced.The highest potency (ca.250 times bicuculline) was observed when an aromatic ? system, bearing electron-donating substituents, was present on the 6-position of the pyridazine ring.
