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MULTITARGET COMPOUNDS ACTIVE AT A PPAR AND CANNABINOID RECEPTOR
专利权人:
GIULIANI INTERNATIONAL LIMITED
发明人:
DESREUMAUX, PIERRE,BELLINVIA, SALVATORE,CHAVATTE, PHILIPPE,BARONI, SERGIO
申请号:
NZ58532608
公开号:
NZ585326A
申请日:
2008.12.22
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
The disclosure relates to pharmaceutical compounds which have activity of, at least one of a PPAR and a cannabinoid receptor, wherein the compound comprises: a PPAR pharmacophore and a cannabinoid pharmacophore linked together by a moiety comprising a fused bicyclic ring comprising a five membered ring fused with a six membered ring or a six membered ring fused with a six membered ring selected from the structure depicted herein wherein the cannabinoid pharmacophore comprises the fused bicyclic ring and wherein the PPAR pharmacophore comprises a salicylic acid, alkoxybenzylacetic acid or a alkoxyphenylacetic acid functionality and wherein the PPAR pharmacophore is linked to the bicyclic ring of the cannabinoid pharmacophore through a linker comprising an amine or an amide functional group. The structural representation of the compounds having said PPAR and a cannabinoid receptor activity are also depicted in the specification. These compounds are suitable for the treatment of a disease which responds to stimulation of a PPAR and a cannabinoid receptor, wherein the disease is associated with pain, inflammation, hyperactivation of the immune system including chronic inflammatory diseases, allergic diseases, autoimmune diseases, metabolic disorders, diseases with intestinal inflammation including Crohn disease, ulcerative colitis, indeterminate colitis, infections intestinal inflammation, celiac disease, microscopic colitis, irritable bowel syndrome, hepatitis, dermatitis including atopic dermatitis, contact dermatitis, acne, rosacea, Lupus Erythematosus, lichen planus, and Psoriasis , NASH, liver fibrosis, lung inflammation and fibrosis, anxiety, emesis, glaucoma, feeding disorders, obesity, movement disorders, diseases of Central Nervous System, including multiple sclerosis, traumatic brain injury, stroke, Alzheimers Disease and Peripheral Neuropathies including traumatic neuropathies, metabolic neuropathies and neuropathic pain, Atherosclerosis, Osteoporosis, alopec
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