52239-91-5

Upstream product

• 1771-65-9 2-methyl-4-oxo-4-phenylbutanoic acid 
• 928-55-2 ethyl 1-propenyl ether 
• 71094-28-5 N′-(2-chloro-1-phenylethylidene)-4-methylbenzenesulfonohydrazide 
• 4100-80-5 2-methylsuccinic anhydride 
• 71-43-2 benzene 
• 70-11-1 α-bromoacetophenone 

Downstream Products

• 103853-58-3 5-methyl-3-phenyl-1,4,5,6-tetrahydro-pyridazine 
• 13300-09-9 4-methyl-6-phenylpyridazin-3(2H)-one 
• 1450829-10-3 (+/-)-N-(4-bromophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-11-4 (+/-)-N-(4-fluorophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-12-5 (+/-)-N-(1,3-benzo-dioxol-5-yl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-14-7 (S)-(-)-N-(4-bromophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-13-6 (R)-(+)-N-(4-bromophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-18-1 (S)-(-)-N-(1,3-benzo-dioxol-5-yl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-16-9 (S)-(-)-N-(4-fluorophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-15-8 (R)-(+)-N-(4-fluorophenyl)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetamide 
• 1450829-09-0 (+/-)-2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetic acid 
• 1450829-08-9 (+/-)-ethyl 2-[5-methyl-6-oxo-3-phenyl-5,6-dihydropyridazin-1(4H)-yl]acetate 
• 924909-75-1 TT-302 
• 28657-39-8 3-chloro-4-methyl-6-phenylpyridazine 

Relevant academic research and scientific papers

FORMULATIONS CONTAINING PYRIDAZINE COMPOUNDS

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.

SALTS OF PYRIDAZINE COMPOUNDS

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 CHOLINESTERASE INHIBITORS

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

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

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.

Development of a novel therapeutic suppressor of brain proinflammatory cytokine up-regulation that attenuates synaptic dysfunction and behavioral deficits

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.

Endothelin receptor antagonists

This invention relates to pyridizinone derivatives of formula I STR1 wherein the various substituents are defined in the specification, and salts thereof, which have useful pharmacological properties, in particular endothelin receptor-antagonistic properties. The compounds are thus useful for the treatment of illnesses associated with endothelin activities, such as hypertension, cardiac insufficiency, coronary heart disease, renal, cerebral and myocardial ischaemia, renal insufficiency, cerebral infarct, subarachnoid haemorrhage, arteriosclerosis pulmonary high blood pressure, inflammations, asthma, prostate hyperplasia, endotoxic shock and in complications after the administration of immunosuppressants which produce renal vasoconstriction.

Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors

A novel series of nonsteroidal heterocycles was discovered which display cell-type selective, high-affinity (nanomolar) binding to the progesterone receptors from TE85 osteosarcoma cells but > 1 μM binding affinity to the progesterone receptors from T47D and ZR75 human breast carcinpma cells.Structure-activity relationships were developed for a set of these compounds, and a representative analog 1-(3,4-dichlorobenzoyl)-3-phenyl-1,4,5,6-tetrahydropyridazine (1i, RWJ 25333) was chosen for further evaluation.RWJ 25333 stimulated the in vitro proliferation of human osteoblast-like cells but not human breast cells.

1,4,5,6-Tetrahydropyridazines by Cycloaddition of Enol Ethers to Azoalkenes and their Aromatisation to Pyridazines.

Transient azoalkenes generated from acyl- and 4-tolylsulphonyl-hydrazones of α-haloacetophenones and of ethyl bromopyruvate are intercepted by cycloaddition to enol ethers, giving 6-alkoxy-1,4,5,6-tetrahydropyridazines (2). 6-Alkoxy-3-aryl-1,4,5,6-tetrahydropyridazines are converted by reaction with sodium ethoxide into 3-arylpyridazines (3).

Substituted 6-phenyl-3(2H)-pyridazinones useful as cardiotonic agents

Substituted 6-phenyl-3(2H)-pyridazinone compounds are useful as cardiotonic agents. Said compounds cause a significant increase in myocardial contractility in the anesthetized dog. Said compounds are produced by reacting substituted γ-oxobenzenebutanoic acids with suitably substituted hydrazines to provide 6-phenyl-4,5-dihydro-3(2H)-pyridazinones which are dehydrogenated to the desired product. The intermediate 6-phenyl-4,5-dihydro-3(2H)-pyridazinones are themselves useful as cardiotonic agents.