Jiangsu Nhwaluokang Pharmceutical Research and Development Co., Ltd.

Other

Jiangsu Nhwaluokang Pharmaceutical Research and Development Co., Ltd.

Qingeng Li

Tao Wang

Lingguo Zeng

Tong Wu

Gang Chen

Yuanzhong Wang

Wei Mao

Xiangqing Xu

Guisheng Zhang

Changwen Li

Liang Ren

Jianyong Xie

Dahai Chen

Chen Duan

Chao Hao

Jian Liao

The present invention provides a crystalline form of a benzodiazepine derivative hydrochloride of Formula I or its ethanolate, wherein R is methyl or ethyl. The present invention also provides a method of preparing the crystal form of the compound of Formula I and a pharmaceutical composition comprising the crystal form.

Crystal form of ethyl (S)-3-(8-bromo-1-methyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,2-a][1,4]diazepin-4-yl)propanoate hydrochloride

The present invention discloses an etomidate derivative of Formula 1, or a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, a pharmaceutical composition and a kit comprising the same, as well as intermediates and methods for preparing the same, and use thereof. The etomidate derivative of the present invention not only has good anesthetic activity, rapid onset, and short duration of action, but also shows little inhibition to the secretion of corticosteroids in animals, and therefore has both favorable anesthetic effect and safety profiles. 

Etomidate derivative and intermediate, preparation method and use thereof

The present invention discloses a class of carboxylic acid derivatives and use thereof in preparation of prodrugs. The carboxylic acid derivatives have the general formula (I), wherein Ris H or alkyl; X is H or F; Y is F or fluoroalkyl; n is 0, 1, 2, 3, 4, 5, or 6; W is Wor W; Wis NRR, NRR.A, Rand Rare each independently H, alkyl, cycloalkyl, or a protecting group for amino; m is 0, 1, 2, or 3; A is an acid; Wis COOR, OPO(OR), or PO(OR); Ris H, or a protecting group for carboxyl or hydroxyl in phosphoric acid. 

Carboxylic acid derivatives and use thereof in the preparation of prodrugs

The present invention relates to a new benzodiazepine derivative, pharmaceutically acceptable salt thereof, preparation method therefor, and use thereof. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have obvious anesthetic effect and low toxicity in body, thereby enhancing the medication safety. The benzodiazepine derivative and the pharmaceutically acceptable salt thereof of the present invention have sedative, hypnotic, and anesthetic effect, and can be used as sedative, hypnotic, and anesthetic drugs.

Benzodiazepine derivative and use thereof

The present invention discloses a class of water soluble taxane derivatives, a method for treating tumor using the same, use thereof as anti-tumor drugs and use thereof in the preparation of anti-tumor drugs. The water soluble taxane derivatives have the general formula (I-1), (I-2) or (I-3): wherein, Ris H or methyl; Ris H, methyl or acetyl; Ris phenyl or OC(CH); X is H, Calkyl or F; Y is F or Calkyl substituted with one or more F; n is 1, 2, 3, 4, 5 or 6; W is NRR.A or Rand Rare each independently H, Calkyl optionally substituted with phenyl, or Ccycloalkyl; m is 0, 1, 2 or 3; and A is a pharmaceutically acceptable acid. 

Water-soluble taxane derivatives and uses thereof

The present invention discloses a class of water-soluble propofol derivatives, preparation method thereof, anesthetization method using the same, use thereof as prodrugs and use thereof in the preparation of intravenous anesthetics. The water-soluble propofol derivatives have the general formula (I); wherein X is H or F, Y is F or alkyl substituted by one or more F, n is 1, 2, 3, 4, 5 or 6, W is Wor W; Wis NRR.A or Rand Rare each independently H, alkyl optionally substituted with phenyl, or cycloalkyl, m is 0, 1, 2 or 3, A is a pharmaceutically acceptable acid, Wis COOMor OPO(M)or PO(M); M is a metal ion, an ammonium ion or a basic amino acid cation which can form a salt with an acid radical; t is the charge number of M. 

Water-soluble propofol derivatives and uses thereof

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Chongqing, China

Qingeng Li