- Preparation method of 4 -phenoxyl -3 -aminoanisole
-
The invention discloses a preparation method of 4 - phenoxyl -3 -aminoanisole, which comprises the following steps: adding 4 - phenoxyl -3 - nitroanisole, a solvent to an autoclave, adding 0.5 - 5% molecular sieve loaded 2.5% nickel as a catalyst, and rep
- -
-
Paragraph 0013; 0024-0034
(2021/11/03)
-
- COMPOUNDS COMPRISING N-METHYL-2-PYRIDONE, AND PHARMACEUTICALLY ACCEPTABLE SALTS
-
The present invention concerns compounds comprising N-methyl-2-pyridone, and pharmaceutically-acceptable salts and compositions of such compounds. Such compounds are useful in anti-inflammatory and anti-cancer therapies. Therefore, the present invention also concerns such compounds for use as medicaments, particularly for the treatment of inflammatory diseases and oncology.
- -
-
Page/Page column 51; 61
(2020/12/30)
-
- Iguratimod intermediate and synthesis method thereof
-
The invention belongs to the technical field of chemical drug synthesis, and particularly relates to an Iguratimod key intermediate and a synthesis method thereof. The synthesis method comprises the following steps: carrying out reduction on 4-methoxy-2-n
- -
-
Paragraph 0035; 0038; 0041
(2019/05/15)
-
- Synthesis and antiinflammatory activity of 7-methanesulfonylamino-6- phenoxychromones. Antiarthritic effect of the 3-formylamino compound (T-614) in chronic inflammatory disease models
-
A group of derivatives of 7-methanesulfonylamino-6-phenoxychromone (1) at the pyrone and phenoxy rings was synthesized starting with 4-chloro-3- nitroanisole and evaluated against acute and chronic inflammations in oral administration in animals. Significant potency in the rat models of carrageenin-induced edema (CPE) and adjuvant-induced arthritis (AA) was realized with 2'-fluoro and 2',4'-difluoro derivatives (9a and 9d), and 3- formylamino derivative (19a) and its 2'-fluoro and 2',4'-difluoro compounds (22a and 22d), displaying AA therapeutic effect of ED40=2.5-7.1 mg/kg/d for 7 d and AA prophylactic effect of 53-70% inhibition at the dosage of 3 mg/kg/d for 22 d. To identify a candidate for further pharmacological study, the five compounds were subjected to evaluation of their gastro-ulcerogenic liability, leading to selection of the fluorine-free compound 19a which did not cause acute ulceration at 300 mg/kg in oral administration in rats. Compound 19a (ED40=3.6 mg/kg in established AA) possessed good therapeutic efficacy against type II collagen-induced arthritis in DBA/1J mice with doses of 30 and 100 mg/kg, suggesting the development of 19a (designated T-614) as a prospective disease-modifying antirheumatic agent. In addition, a preparative-scale synthetic route to T-614 has been established.
- Inaba, Takihiro,Tanaka, Keiichi,Takeno, Ryuko,Nagaki, Hideyoshi,Yoshida, Chosaku,Takano, Shuntaro
-
p. 131 - 139
(2007/10/03)
-
- 1-,2-,3-,4-,5-,6-,7-,8- AND/OR 9 SUBSTITUTED DIBENZOXAZEPINE COMPOUDS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING PAIN
-
The present invention provides substituted dibenzoxazepine compounds of Formula I: STR1 which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
- -
-
-
- 4H-1-benzopyran-4-one derivative or its salt, process for producing the same and pharmaceutical composition comprising the same as active ingredient
-
This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: STR1 or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.
- -
-
-