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1. WO2019051222 - BENZENE FUSED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Publication Number WO/2019/051222
Publication Date 14.03.2019
International Application No. PCT/US2018/049946
International Filing Date 07.09.2018
IPC
C07C 259/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
10having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
C07C 65/21 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
65Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
21containing ether groups, groups, groups, or groups
C07C 271/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
271Derivatives of carbamic acid, i.e. compounds containing any of the groups the nitrogen atom not being part of nitro or nitroso groups
06Esters of carbamic acids
08having oxygen atoms of carbamate groups bound to acyclic carbon atoms
26with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
30to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
C07C 275/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
275Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups
28having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
30being further substituted by halogen atoms, or by nitro or nitroso groups
C07C 311/16 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
16having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
C07C 311/51 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
311Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
50Compounds containing any of the groups X being a hetero atom, Y being any atom
51Y being a hydrogen or a carbon atom
CPC
C07C 217/76
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
76having amino groups bound to carbon atoms of six-membered aromatic rings and etherified hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 233/66
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
64having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
66having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
C07C 233/67
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
64having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
67having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07C 233/69
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
64having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
67having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
68with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
69of an acyclic saturated carbon skeleton
C07C 235/42
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
235Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
42having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
C07C 259/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
259Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
04without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
10having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
Applicants
  • TAIWANJ PHARMACEUTICALS CO., LTD.
Inventors
  • YANG, Syaulan S.
  • LEE, Kuang Yuan
  • LIU, Meng Hsien
  • JIANG, Yan-Feng
  • FAN, Yu-Shiou
  • CHEN, Chi-Han
  • LIU, Sheng Hung
Agents
  • MCROBBIE, Craig A.
Priority Data
62/555,23307.09.2017US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) BENZENE FUSED HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
(FR) DÉRIVÉ HÉTÉROCYCLIQUE FUSIONNÉ DE BENZÈNE ET COMPOSITION PHARMACEUTIQUE LE COMPRENANT
Abstract
(EN)
The present disclosure provides a benzene fused heterocyclic derivative of Formula (I): --̅-̅-̅ is a single or double bond; n is an integer of 0 or 1; A is -CH2-, -CH(OH)-, or - C(O)-; G is C or N; X is -CH2-, O, or -C(O)-; Y is alkyl, aryl, or heterocyclic alkyl optionally substituted with at least one substituent independently selected from a group consisting of: H, halogen, alkyl, alkyl substituted with at least one halogen, aryl, aryl substituted with at least one halogen, -NRy1Ry2, -ORy1, -Ry1C(O)Ry3, -C(O)Ry1, -C(O)ORy2, -C(O)ORy2Ry3, - NRy1C(O)Ry2, -NRy1C(O)NRy2Ry3, -NRy1C(O)ORy2Ry3, -NRy1C(O)Ry2ORy3, C(O)NRy1(Ry2Ry3), -C(O)NRy1(Ry2ORy1), -ORy2Ry3, and -ORy2ORy3, wherein each of Ry1 and Ry2 is independently selected from a group consisting of H, oxygen, alkyl, and aryl, and Ry3 is aryl optionally substituted with at least one halogen; Z is -NRz1Rz2, -NRz1Rz3, -ORz1, -ORz1Rz3, -C(O)Rz1Rz3, -C(O)ORz1Rz3, -NRz1C(O)Rz2Rz3, -NRz1C(O)ORz2Rz3, -C(O)NRz1Rz3, or ORz2ORz3, wherein each of Rz1 and Rz2 is independently selected from a group consisting of H, oxygen, alkyl and aryl, and Rz3 is aryl optionally substituted with at least one substituent independently selected from a group consisting of halogen, OH, -RzaCOORzb, -ORzaCOORzb, -RzaSO2Rzb, -RzaSO2NRzbRzcRzd, -RzaC(O)RzbRzc, -RzaC(O)NRzbRzcRzd, -RZaC(O)NRzbSO2Rzc, wherein Rza is nil or alkyl, Rzb is H or alkyl, each of Rzb and Rzc is independently selected from a group consisting of H, OH, alkyl, aryl, alkoxyl, or NRzbRzc is a nitrogen-containing heterocyclic alkyl ring, Rzd is nil or a sulfonyl alkyl group.
(FR)
La présente invention concerne un dérivé hétérocyclique fusionné de benzène de formule (I) : --̅-̅-̅ représente une liaison simple ou double ; n est un nombre entier qui vaut 0 ou 1 ; A représente -CH2-, -CH(OH)-, ou - C(O)- ; G représente C ou N ; X représente -CH2-, O, ou -C(O)- ; Y est un alkyle, aryle, ou alkyle hétérocyclique éventuellement substitué par au moins un substituant indépendamment choisi dan un groupe constitué de : H, halogène, alkyle, alkyle substitué par au moins un halogène, aryle, aryle substitué par au moins un halogène, -NRy1Ry2, -ORy1, -Ry1C(O)Ry3, -C(O)Ry1, -C(O)ORy2, -C(O)ORy2Ry3, - NRy1C(O)Ry2, -NRy1C(O)NRy2Ry3, -NRy1C(O)ORy2Ry3, -NRy1C(O)Ry2ORy3, C(O)NRy1(Ry2Ry3), -C(O)NRy1(Ry2ORy1), -ORy2Ry3, et -ORy2ORy3, chacun de Ry1 et Ry2 est indépendamment choisi dans un groupe constitué de H, oxygène, alkyle, et aryle, et Ry3 représente un aryle éventuellement substitué par au moins un halogène ; Z représente -NRz1Rz2, -NRz1Rz3, -ORz1, -ORz1Rz3, -C(O)Rz1Rz3, -C(O)ORz1Rz3, -NRz1C(O)Rz2Rz3, -NRz1C(O)ORz2Rz3, -C(O)NRz1Rz3, ou ORz2ORz3, chacun de Rz1 et Rz2 est indépendamment choisi dans un groupe constitué de H, oxygène, alkyle et aryle, et Rz3 représente un aryle éventuellement substitué par au moins un substituant indépendamment choisi dans un groupe constitué de : halogène, OH, -RzaCOORzb, -ORzaCOORzb, -RzaSO2Rzb, -RzaSO2NRzbRzcRzd, -RzaC(O)RzbRzc, -RzaC(O)NRzbRzcRzd, -RZaC(O)NRzbSO2Rzc, Rza est nul ou représente un alkyle, Rzb représente H ou alkyle, chacun de Rzb et Rzc est indépendamment choisi dans un groupe constitué de H, OH, alkyle, aryle, alcoxyle, ou NRzbRzc représente un cycle alkyle hétérocyclique contenant de l'azote, Rzd est nul ou représente un groupe alkyle sulfonyle.
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