- Desymmetrization of dichloroazaheterocycles
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3,6-Dichloropyridizine 1a was converted in good yield into its mono-iodo derivative 1b when treated with a mixture of hydriodic acid and sodium iodide. Pure samples of the mono-iodo derivatives 2b, 3b and 4b could not be obtained from their corresponding dichlorinated precursors with these reagents. Compounds 1b and 4b underwent palladium catalysed Suzuki, Sonogashira and other coupling reactions.
- Goodman, Allan J.,Stanforth, Stephen P.,Tarbit, Brian
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Read Online
- Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB2 agonists for the treatment of inflammatory pain
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A series of 3-amino-6-aryl-pyridazines have been identified as CB2 agonists with high efficacy and selectivity against the CB1 receptor. Details of the investigation of structure-activity relationships (SAR) are disclosed, which led to the identification of pyridazine analogue 35, a compound with high potency in an in vivo model of inflammatory pain.
- Gleave, Robert J.,Beswick, Paul J.,Brown, Andrew J.,Giblin, Gerard M.P.,Goldsmith, Paul,Haslam, Carl P.,Mitchell, William L.,Nicholson, Neville H.,Page, Lee W.,Patel, Sadhana,Roomans, Susan,Slingsby, Brian P.,Swarbrick, Martin E.
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- COMPOUNDS AND COMPOSITIONS FOR USE IN TREATING SKIN DISORDERS
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Provided herein is a compound of formula (XXXII) or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer thereof or a physiologically functional derivative thereof, wherein R1, R2, R3, G, A, E, n, p, and q are defined herein. Also provided herein are compositions comprising a compound of formula (XXXII), and methods of using a compound of formula (XXXII), e.g., in the treatment or prevention of skin disorders.
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Paragraph 1849-1851
(2021/08/06)
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- PESTICIDALLY ACTIVE TETRACYCLIC HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS
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Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
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Page/Page column 55
(2016/05/24)
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- PESTICIDALLY ACTIVE POLYCYCLIC DERIVATIVES WITH SULFUR SUBSTITUTED FIVE-MEMBERED RING HETEROCYLES
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Polycyclic derivatives of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
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Page/Page column 85
(2016/11/14)
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- PESTICIDALLY ACTIVE POLYCYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS
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Polycyclic derivatives of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.
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Page/Page column 89
(2016/12/22)
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- NOVEL TRIFLUOROMETHYL-OXADIAZOLE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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The invention relates to novel trifluoromethyl-oxadiazole derivatives of formula (I), and pharmaceutically acceptable salts thereof, in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, pharmaceutical com
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Page/Page column 68
(2013/06/27)
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- THERAPEUTIC COMPOUNDS
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The invention provides compounds of formula I or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for prepa
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Page/Page column 41
(2011/07/09)
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- Heteroatom-substituted analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-adamantyl)-4- hydroxyphenyl]-3-chlorocinnamic acid
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(E)-4-[3'-(1-Adamantyl)-4'-hydroxyphenyl]-3-chlorocinnamic acid (3-Cl-AHPC) induces the cell cycle arrest and apoptosis of cancer cells. Because its pharmacologic properties-solubility, bioavailability, and toxicity-required improvement for translation, s
- Xia, Zebin,Farhana, Lulu,Correa, Ricardo G.,Das, Jayanta K.,Castro, David J.,Yu, Jinghua,Oshima, Robert G.,Reed, John C.,Fontana, Joseph A.,Dawson, Marcia I.
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experimental part
p. 3793 - 3816
(2011/08/06)
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- 3-(3-PYRIMIDIN-2-YLBENZYL)-1,2,4-TRIAZOLO[4,3-B]PYRIDAZINE DERIVATIVES AS MET KINASE INHIBITORS
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Compounds of the formula (I), in which R1, R2, R3, R3′, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
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Page/Page column 19
(2011/05/03)
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- PYRIDAZINONE DERIVATIVES
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Compounds of the formula (I), in which Y, R1, R2, R3 and R3′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.
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(2011/10/31)
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- Copper-mediated trifluoromethylation of heteroaromatic compounds by trifluoromethyl sulfonium salts
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Copper is king! A convenient method for the synthesis of trifluoromethylated heteroaromatic compounds under mild conditions has been developed based on the observation that 1 can be reduced by certain metals (see scheme). Substrate 1 is assumed to be reduced by copper via a single-electron transfer mechanism, and CuCF3 is the most probable intermediate in this reaction. DMF=N,N-dimethylformamide, Tf=triflate.
- Zhang, Cheng-Pan,Wang, Zong-Ling,Chen, Qing-Yun,Zhang, Chun-Tao,Gu, Yu-Cheng,Xiao, Ji-Chang
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supporting information; experimental part
p. 1896 - 1900
(2011/04/16)
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- LINEAR PYRIDAZINE AND PYRROLE COMPOUNDS, METHOD FOR OBTAINING THEM AND APPLICATIONS
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The present invention relates to linear pyridazine compounds, and more particularly to those of these compounds which are oligopyridazine compounds, to processes for obtaining them, to their uses, and also to their reduction to pyrroles and to the uses of the pyrrole, pyridazinylpyrrole and oligopyrrole compounds obtained. The invention relates in particular to the uses as medicaments, in particular for treating pathologies such as cancer, bacterial infections or parasitic infections, and also the applications in the materials, environmental, electronics and optics field.
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Page/Page column 34
(2010/02/16)
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- COMBINATION OF CB2 LIGAND AND PARACETAMOL
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Combination of one or more CB2 modulators and paracetamol are useful of treating conditions which are mediated by the activity of CB2 receptors such as an immune disorder, an inflammatory disorder, pain, rheumatoid arthritis, multiple sclerosis, osteoarthritis, and osteoporosis.
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Page/Page column 167-168
(2008/12/04)
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- PYRIDAZINE DERIVATIVES WITH ANTIINFLAMMATORY ACTIVITY
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The present invention relates to novel pyridazinyl derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of diseases, particularly pain, which diseases are caused directly or indirectly by an increase or decrea
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Page/Page column 26
(2008/06/13)
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- Aryl sulfonamide and sulfonyl compounds as modulators of PPAR and methods of treating metabolic disorders
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Aryl sulfonamide and sulfonyl compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.
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Page/Page column 66
(2010/02/14)
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- Novel diazine derivatives
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The present invention provides compounds of formula (I): their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
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(2010/02/14)
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