- 5-(3-(ETHYLSULFONYL)PYRIDIN-2-YL)-PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND RELATED COMPOUNDS AS PESTICIDE AND INSECTICIDE AGENTS FOR CROP PROTECTION
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The present invention discloses a fused heterocyclic compound of formula (I), wherein, Q, R1, R2, n, m and Y are as defined in the detailed description. The present invention further discloses methods for their preparation and use of
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Page/Page column 70; 71
(2021/08/27)
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- TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
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The invention provides certain bicylic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X1, X2, R1, R2, R3, R4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
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Paragraph 0628
(2015/07/07)
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- Creating an antibacterial with in vivo efficacy: Synthesis and characterization of potent inhibitors of the bacterial cell division protein FTSZ with improved pharmaceutical properties
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3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
- Haydon, David J.,Bennett, James M.,Brown, David,Collins, Ian,Galbraith, Greta,Lancett, Paul,MacDonald, Rebecca,Stokes, Neil R.,Chauhan, Pramod K.,Sutariya, Jignesh K.,Nayal, Narendra,Srivastava, Anil,Beanland, Joy,Hall, Robin,Henstock, Vincent,Noula, Caterina,Rockley, Chris,Czaplewski, Lloyd
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supporting information; experimental part
p. 3927 - 3936
(2010/09/04)
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- HETEROCYCLIC COMPOUNDS AND THEIR USES
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Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.
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Page/Page column 70
(2011/01/05)
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- COMPOUNDS
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Bicyclic nitrogen containing compounds and their use as antibacterials.
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Page/Page column 37; 73
(2008/12/08)
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- ANTIBACTERIAL AGENTS
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Compounds of formula (I) have antibacterial activity wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is =C(R1)- or =N-; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are -CH2-, -CH2CH2-, -O-, or, in either orientation, -O- CH2- Or -OCH2CH2-; R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z is -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, -N(CH2CH3)-, -C(=O)-, -O-(C=O)-, -C(=O)-O-, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by -O-, -S-, -S(O)-, -S(O2)-, -NH-, -N(CH3)-, or -N(CH2CH3)-; and Q is hydrogen, halogen, nitrile, or hydroxyl or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms.
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Page/Page column 125
(2010/11/28)
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- 3-fluoropyridines, process for their preparation, and their use in liquid-crystal mixtures
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A 3-fluoropyridine of the formula (I) STR1 in which the symbols have the following meanings: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
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- TITANIUM (O) REAGENTS; 4. A SELECTIVE AND EFFICIENT REDUCTION OF NITROPYRIDINE DERIVATIVES
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Following the successful applications of a titanium (O) slurry in the deoxygenation of aromatic N-oxides, we attempted to achieve this method for the reduction of a nitro- group in pyridine derivatives.In general, only aminopyridine derivates were formed in 85-98percent yield.The advantage of this excellent reducing agent consists in mild reaction conditions and high yields of products, as well as in the selectivity of the reaction.
- Malinowski, Marek
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