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1. WO2022204902 - BENZOTHIAZINONE DERIVATIVE SUBSTITUTED WITH TRIFLUOROMETHYL AT 6-POSITION, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Publication Number WO/2022/204902
Publication Date 06.10.2022
International Application No. PCT/CN2021/083695
International Filing Date 29.03.2021
IPC
C07D 279/08 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
279Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
041,3-Thiazines; Hydrogenated 1,3-thiazines
08condensed with carbocyclic rings or ring systems
C07D 417/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
A61K 31/5415 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
5415ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61P 31/06 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
06for tuberculosis
CPC
A61K 31/5415
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
5415ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
A61P 31/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04Antibacterial agents
06for tuberculosis
C07D 279/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
279Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
041,3-Thiazines; Hydrogenated 1,3-thiazines
08condensed with carbocyclic rings or ring systems
C07D 417/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • 苏州大学 SOOCHOW UNIVERSITY [CN]/[CN]
Inventors
  • 乔春华 QIAO, Chunhua
  • 范东光 FAN, Dongguang
Agents
  • 苏州创元专利商标事务所有限公司 SUZHOU CREATOR PATENT AND TRADEMARK AGENCY, LTD
Priority Data
Publication Language Chinese (zh)
Filing Language Chinese (ZH)
Designated States
Title
(EN) BENZOTHIAZINONE DERIVATIVE SUBSTITUTED WITH TRIFLUOROMETHYL AT 6-POSITION, AND PREPARATION METHOD THEREFOR AND USE THEREOF
(FR) DÉRIVÉ DE BENZOTHIAZINONE SUBSTITUÉ PAR DU TRIFLUOROMÉTHYLE EN POSITION 6, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 6- 位三氟甲基取代的苯并噻嗪酮衍生物及其制备方法与应用
Abstract
(EN) A benzothiazinone derivative substituted with trifluoromethyl at 6-position, and a preparation method therefor and the use thereof. A series of compounds are obtained by means of changing the benzene ring of the benzothiazinone backbone, especially by means of changing a substituent thereof. Compared with other benzothiazinone derivatives, the benzothiazinone derivative substituted with trifluoromethyl at 6-position is more stable with regard to hepatic microsomal enzymes, and has longer metabolic half-life T1/2 and better water solubility.
(FR) L'invention concerne un dérivé de benzothiazinone substitué par du trifluorométhyle en position 6, son procédé de préparation et son utilisation. Une série de composés est obtenue en modifiant le cycle benzénique de la chaîne principale benzothiazinone, en particulier en modifiant un substituant de celle-ci. En comparaison des autres dérivés de benzothiazinone, le dérivé de benzothiazinone substitué par du trifluorométhyle en position 6 est plus stable vis-à-vis des enzymes microsomales hépatiques, et présente une demi-vie métabolique T1/2 plus longue et une meilleure solubilité dans l'eau.
(ZH) 一种6-位三氟甲基取代的苯并噻嗪酮衍生物及其制备方法与应用,对苯并噻嗪酮骨架苯环进行改变,尤其对取代基进行变化,得到的一系列的化合物,与其他苯并噻嗪酮衍生物相比,6-位三氟甲基取代的苯并噻嗪酮衍生物对肝微粒体酶更稳定,代谢半衰期T 1/2更长、水溶性更好。
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