- Substituted pyridazinone compound and application thereof
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The invention provides a substituted pyridazinone compound and application thereof. The substituted pyridazinone compound is a compound shown in a general formula I, or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvent compound, a poly
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Paragraph 0044-0048
(2021/04/14)
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- ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4
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Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
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Paragraph 00212
(2021/06/22)
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- OXADIAZOLYLTHIOPHENE DERIVATIVES USEFUL AS HISTONE DEACETYLASE INHIBITORS
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A compound of Formula I : (I) or a pharmaceutically acceptable salt thereof, wherein: each R' is QR1; each Q is independently selected from a bond, -C1-C10 alkylene, -C2-C10 alkenylene, -C(O)-, -C(O)O-, -C(O)N(R1)-, -C(O)N(R1)SO2- -N(R1)C(O)-, - N(R1)-, -N(SO2(R1)), -N(R1)SO2- -C(O)NR4R5-, -N(R4R5)C(O)-, -N(R4R5)- - S-, -SO-, -SO2-, -S(O)O-, -SO2N(R1)- and -O-; each R1 is independently selected from H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C1-C10 haloalkyl, C1-C10 heteroalkyl, aryl, heteroaryl, C3-C10 cycloalkyl, -(C1-C10 alkylene)-C3-C10 cycloalkyl, halogen, cyano, C1-C10 alkylene- aryl, C1-C10 alkylene heteroaryl, C1-C10 heterocycloalkyl and -(C1-C10 alkylene)- C1-C10 heterocycloalkyl. The compounds are inhibitors of HDAC and therefore have potential utility in the therapy of a number of conditions including cancer and inflammation.
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Page/Page column 206
(2019/09/18)
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- Discovery of pyrrolopyridazines as novel DGAT1 inhibitors
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A new structural class of DGAT1 inhibitors was discovered and the structure-activity relationship was explored. The pyrrolotriazine core of the original lead molecule was changed to a pyrrolopyridazine core providing an increase in potency. Further exploration resulted in optimization of the propyl group at C7 and the discovery that the ester at C6 could be replaced by five-membered heterocyclic rings. The analogs prepared have DGAT1 IC 50 values ranging from >10 μM to 48 nM.
- Fox, Brian M.,Iio, Kiyosei,Li, Kexue,Choi, Rebeka,Inaba, Takashi,Jackson, Simon,Sagawa, Shoichi,Shan, Bei,Tanaka, Masahiro,Yoshida, Atsuhito,Kayser, Frank
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scheme or table
p. 6030 - 6033
(2010/11/05)
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- Heterocyclic Compounds Useful as RAF Kinase Inhibitors
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The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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Page/Page column 39
(2009/01/24)
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- COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
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The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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Page/Page column 84
(2009/03/07)
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- 7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy) -3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: A functionally selective γ-aminobutyric acidA (GABAA) α2/α3- subtype selective agonist that exhibits potent anxiolyti
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There is increasing evidence that compounds with selectivity for γ-aminobutyric acidA (GABAA) α2- and/or α3-subtypes may retain the desirable anxiolytic activity of nonselective benzodiazepines but possess an improved side effect pro
- Carling, Robert W.,Madin, Andrew,Guiblin, Alec,Russell, Michael G. N.,Moore, Kevin W.,Mitchinson, Andrew,Sohal, Bindi,Pike, Andrew,Cook, Susan M.,Ragan, Ian C.,McKernan, Ruth M.,Quirk, Kathleen,Ferris, Pushpinder,Marshall, George,Thompson, Sally Ann,Wafford, Keith A.,Dawson, Gerard R.,Atack, John R.,Harrison, Timothy,Castro, José L.,Street, Leslie J.
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p. 7089 - 7092
(2007/10/03)
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- Substituted triazolo-pyridazine derivative, pharmaceutical compositions made therefrom
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7-(1,1 -Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine, and pharmaceutically acceptable salts thereof are selective ligands for GABAAreceptors useful in the treatment of disorders of t
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- Fungicidal pyridazines
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Plants are protected from the damaging effects of Phycomycetous fungi by a series of pyridazines of formula STR1 wherein R3 is chloro, bromo, methyl, cyano or iodo; R is chloro, bromo, iodo, methyl, cyano or furan-2-ylmethoxy; R1 is
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- Preparation of substituted pyridazines
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A novel process is described for preparing substituted pyridazines, where a less substituted pyridazine is reacted with a carboxylic acid in the presence of a silver ion as catalyst, using peroxydisulfate ion. The reaction is run at a temperature from about 40° to 80° C. in an aqueous solvent system and mineral acid. The substituted pyridazines are useful as intermediates to herbicidal and fungicidal compounds.
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