C07C229/38

TRNA SYNTHETASE INHIBITORS
20210053997 · 2021-02-25 ·

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

Compositions and methods of use for opioid hexadienoates and optionally substituted hexadienoates

The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation. A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

Compositions and methods of use for opioid hexadienoates and optionally substituted hexadienoates

The present invention relates to opiate derived compositions and their antagonists useful in therapeutic areas associated with opioid receptor modulation. A 3-hexadienoate modification of the opioids is formulated to improve opiates' engagement of the opioid receptors when given orally. A 3-hexadienoate modification of nalbuphine or a pharmaceutically acceptable salt of thereof to improve quality of pain management when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation. A 3-hexadienoate modification of the opioids antagonists is formulated to improve inhibition of the opioid receptors when given orally. A 3-hexadienoate modification of naloxone or a pharmaceutically acceptable salt of thereof to improve quality of Sobering when given intravenously, intranasally, transdermally, sublingually, rectally, topically, intramuscularly, subcutaneously or via inhalation.

Lipids and lipid compositions for the delivery of active agents

This invention provides for a compound of formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.4, L.sub.1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Lipids and lipid compositions for the delivery of active agents

This invention provides for a compound of formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein R.sup.1-R.sup.4, L.sub.1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

Benzathine analogs

A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001## wherein X is a divalent linking moiety; and R.sup.1-R.sup.10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R.sup.3 or R.sup.8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.

Benzathine analogs

A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001## wherein X is a divalent linking moiety; and R.sup.1-R.sup.10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R.sup.3 or R.sup.8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.

Self-oriented material, self-oriented liquid crystal material and manufacturing method of liquid crystal panel

The invention provides a self-oriented material, a self-oriented liquid crystal material and a manufacturing method of the liquid crystal panel. The self-oriented material provided by the invention can be used for carrying out alignment on liquid crystal molecules, and a polyimide alignment layer is not required to be arranged in the liquid crystal panel when the self-oriented material is added into the liquid crystal material. The self-oriented liquid crystal material disclosed by the invention contains the self-oriented material, the self-oriented material can be used for carrying out alignment on liquid crystal molecules, therefore a polyimide alignment layer is not required to be arranged in the liquid crystal panel. According to the manufacturing method of the liquid crystal panel, the orientation of the liquid crystal molecules is realized by utilizing the self-oriented material in the self-oriented liquid crystal material, and the polyimide alignment layer does not need to be manufactured, so that the process for manufacturing the polyimide alignment layer is saved, and the production cost is reduced.

Self-oriented material, self-oriented liquid crystal material and manufacturing method of liquid crystal panel

The invention provides a self-oriented material, a self-oriented liquid crystal material and a manufacturing method of the liquid crystal panel. The self-oriented material provided by the invention can be used for carrying out alignment on liquid crystal molecules, and a polyimide alignment layer is not required to be arranged in the liquid crystal panel when the self-oriented material is added into the liquid crystal material. The self-oriented liquid crystal material disclosed by the invention contains the self-oriented material, the self-oriented material can be used for carrying out alignment on liquid crystal molecules, therefore a polyimide alignment layer is not required to be arranged in the liquid crystal panel. According to the manufacturing method of the liquid crystal panel, the orientation of the liquid crystal molecules is realized by utilizing the self-oriented material in the self-oriented liquid crystal material, and the polyimide alignment layer does not need to be manufactured, so that the process for manufacturing the polyimide alignment layer is saved, and the production cost is reduced.

ORGANIC AMINE ESTER DERIVATIVE DRUG OF 2-(alpha-HYDROXYPENTYL)BENZOIC ACID
20210002224 · 2021-01-07 · ·

An organic amine ester derivative drug of 2-(-hydroxypentyl)benzoic acid and a preparation method thereof and an use thereof are disclosed. The present disclosure particularly relates to a compound having the general formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable formulation prepared from the compound or the pharmaceutically acceptable salt thereof. The compound having the general formula I or the pharmaceutically acceptable salt thereof has in vitro a good solubility and a low hygroscopicity, and has in vivo a bioavailability and a brain aggregation concentration that are significantly greater than those of the original medicine butyphthalide and/or an improving drug efficacy. The use of the compound in the preparation of a drug for preventing and/or treating heart and cerebral ischemic diseases, a drug for preventing and/or treating heart and cerebral artery occlusion diseases, an anti-parkinsonian drug and an anti-senile-dementia drug is also disclosed.

##STR00001##