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A compound and alkyl technology, applied in the field of regulating cannabinoid receptors, to achieve the effect of reducing lipophilicity and improving water solubility
Inactive Publication Date: 2008-02-06
UCL BUSINESS PLC
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[0016] It is an object of the present invention to provide cannabinoid receptor modulators that alleviate and / or eliminate some of the disadvantages commonly associated with prior art modulators, such as undesired psychoactive side effects
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[0234] overview
[0235] Unless noted, all starting materials were either commercially available or reported in previous literature. Solvents and reagents were used without further purification, except tetrahydrofuran (THF), which was dried over sodium. The reaction was monitored by thin layer chromatography (TCL) on precoated silica gel plates (Kieselgel 60F254, Merck). Unless otherwise noted, use Still 36 Purification was carried out by flash chromatography using a column packed with silica gel (particle size 40-63 μM, Merck). Recorded on a Bruker AMX-300 spectrometer 1 H and 13 CNMR spectrum. Chemical shifts are reported in ppm. Coupling constants are in Hz. Mass spectra were recorded on a VG ZAB SE spectrometer (ESP, FAB) or a Micromass Quattro electrospray liquid crystal mass spectrometer (LCMS). Using CEM Focused Microwave TM The Synthesis System performs certain Suzuki coupling reactions.
[0236] synthesis
[0237] Compounds of formula I were synthesized by...
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Abstract
The present invention relates to a compound of formula I or a pharmaceutically acceptable salt thereof. In formula (I), R 1 and R 2 Each independently is H or alkyl; Y is alkyl, CONR 3 R 4 、COOR 5 , SO 2 NR 16 R 17 , NHSO 2 R 18 or CN; X is aryl or heteroaryl, each of which may optionally be substituted by one or more substituents selected from (CH 2 ) m Z, where Z is halogen, OH, CN, alkyl, alkoxy, NO 2 、CF 3 、CONR 6 R 7 , CN, NR 8 R 9 、COOR 10 or NHCOR 11 , m is 0 to 3; R 3 to R 11 Each is independently H, alkyl or aryl, wherein the alkyl and aryl are optionally substituted by one or more substituents selected from halogen, OH, CN, alkyl, alkoxy , NO 2 、CF 3 、CONR 12 R 13 , CN, NH 2 、COOR 14 , NHCOR 15 and CN; R 12 to R 18 Each independently is H or alkyl, more preferably H or Me; n is 1 to 6; wherein the compound is not 3',5'-dimethyl-4-(1,1-dimethylheptyl)- 1,1'-biphenyl-2-phenol. Another aspect of the invention relates to the use of such compounds for the manufacture of a medicament for the treatment of muscular disorders, gastrointestinal disorders or for the control of spasticity or tremor.
Description
technical field [0001] The present invention relates to the ability to modulate cannabinoid receptors (cannabinoid receptors), especially peripheral CB 1 receptor compounds. Background technique [0002] There has recently been renewed interest in medical marijuana and the therapeutic use of synthetic cannabinoids, such as the active component of marijuana-Δ 9 - Tetrahydrocannabinol (THC) [1]. [0003] [0004] THC has therapeutic advantages in several major areas of medicine, including control of acute pain and especially chronic / neuropathic pain, nausea, loss of appetite, AIDS, glaucoma, asthma and multiple sclerosis [Baker, D. et al, Nature 2000, 404, 84-87; Baker, D. et al FASEB J. 2001, 15, 300-302; Schnelle, M. et al, Forsch. Komplement armed. 1999, 6 Suppl 3, 28-36]. [0005] Various cannabinoid ligands have been reported in the literature. Broadly speaking, cannabinoid ligands can be divided into three major categories including: (i) typical cannabinoids such ...
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