- Urea substituted aromatic ring connected dioxane and quinazoline or quinoline compound, composition and application thereof (by machine translation)
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The invention relates to a novel compound VEGFR - 2 composition as CSF1R and, inhibitors and application. thereof in particular, and provides a compound VEGFR - 2 with potent inhibition CSF1R and (and a pharmaceutical composition (1) containing the compound as shown) or an isomer, solvate, hydrate, of the compound in preparation of a medicament, of the compound or a pharmaceutical composition containing the compound. A compound or a pharmaceutical composition containing the compound in a pharmaceutically acceptable salt, comprises . g of a compound or, a pharmaceutical composition containing the. above compound in a pharmaceutically acceptable form. (by machine translation)
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Paragraph 0095-0097
(2020/03/17)
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- Aromatic ring dioxane quinazoline or quinoline compound, composition and application of aromatic ring dioxane quinazoline or quinoline compound
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The invention relates to a novel compound serving as an inhibitor of kinase such as TRK, c-MET, AXL, MER and/or VEGFR2, a composition and application of the novel compound. Specifically, the inventionprovides a compound (as shown in formula (1)) or an isomer, a solvate, a hydrate, a pharmaceutically acceptable salt and a prodrug thereof, and a pharmaceutical composition containing the compound, wherein the compound has the activity of strongly inhibiting kinase such as TRK, c-MET, AXL, MER and/or VEGFR2. The invention further discloses application of the compound or the pharmaceutical composition in preparation of a medicine. The medicine is used for treating autoimmune diseases or cancers.
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Paragraph 0086-0087
(2020/06/09)
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- A practical synthesis of the PDE4 inhibitor, KW-4490
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A practical and scalable synthesis of a PDE4 inhibitor KW-4490 (1) was developed. This improved synthesis features the construction of the 1-arylcyclohexene (9) by the Diels-Alder reaction followed by a newly established Brnsted acid-promoted hydrocyanation. Subsequent crystallization-induced dynamic resolution enabled the high-yield production of the desired cis-isomer (cis-8). The synthesis was achieved in seven steps in 37% overall yield.
- Yanagisawa, Arata,Nishimura, Koichiro,Ando, Kyoji,Nezu, Tetsuya,Maki, Ayako,Kato, Sachiko,Tamaki, Wakako,Imai, Eiichiro,Mohri, Shin-Ichiro
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experimental part
p. 1182 - 1187
(2011/04/17)
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- Derivatives of benzofuran or benzodioxole
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An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1and R2independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1(wherein E1represents a bond, O, or NH; and G1represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1and R2are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11or R13described below are combined to form a single bond; R3represents hydrogen, phenyl, or halogen; R4represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.
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- DERIVATIVES OF BENZOFURAN OR BENZODIOXOLE
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An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents CONH, CONHCH2, or a bond), or N], or (iii) a bond; and R5 represents aryl, an aromatic heterocyclic group, cycloalkyl, pyridine-N-oxide, cyano, or lower alkoxycarbonyl; or pharmaceutically acceptable salts thereof.
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- OXYGENIC HETEROCYCLIC COMPOUNDS
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Oxygen-containing heterocyclic compounds represented by following Formula (I): wherein n represents an integer of 1 to 4; R1, R2, R3and R4are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, or the like; R5represents hydrogen or halogen; R6represents hydroxy or substituted or unsubstituted lower alkoxy; D represents (1) -C(R8)(R9)-X- or (2) a bond; R7represents (1) substituted or unsubstituted lower alkyl, substituted or unsubstituted cycloalkyl, polycycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted heterocyclic group, or pyridine-N-oxide, (2) -Y-ZR14, (3) -Y-Z-(CH2)m-N(R16a)R16b, or (4) -Y-CON(R17a)R17b, or pharmaceutically acceptable salts thereof.
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- New benzodioxane compounds
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A compound of formula (I): STR1 in which: X represents oxygen or methylene, n represents 1, 2 or 3, R1 represents hydrogen, aminocarbonyl or hydroxymethyl, R2 represents: STR2 in which R3 and R4 are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same are useful in the treatment of schizophrenia.
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- Synthese de dioxinocoumarines angulaires
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The synthesis of angular dioxinocoumarins 1 and 2 connected with angelicins are described.These syntheses are respectively realized in eight and ten steps from 6-amino-1,4-benzodioxane and 3-methoxycatechol.
- Guillaumet, Gerald,Hretani, Mohamed,Coudert, Gerard
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p. 193 - 197
(2007/10/02)
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