C07C229/38

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.

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COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I)

##STR00001##

including stereoisomers and pharmaceutically acceptable salts thereof, wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.3, R.sup.3a, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and the subscript n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

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.

Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds

Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds

Methods of synthesizing compounds using CO.sub.2 as a directing group for CH functionalization, and compounds made thereby, are described.

LSD1 INHIBITOR AND PREPARATION METHOD AND APPLICATION THEREOF

A cyclopropylamine compound as a lysine-specific demethylase 1 (LSD1) inhibitor. Particularly, the present invention relates to a compound represented by formula (I) and a pharmaceutically acceptable salt thereof. The present invention also provides an application of the same in preparing a drug for treating an LSD1-related disease.

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Substituted phenyl aziridine precursor analogs for inhibiting androgen-independent prostate cancer cell growth

Disclosed are methods and pharmaceutical compositions for modulating one or more steroidal receptor activities. The methods typically utilize and the pharmaceutical compositions typically include one or more substituted phenyl aziridine precursors, their respective aziridines, analogs thereof, derivatives thereof, or pharmaceutically acceptable salts thereof such as CpdA. The methods and compositions may be used for treating diseases, disorders, and conditions associated with glucocorticoid receptor activity, androgen receptor activity, or both, such as cancers, acne vulgaris, and alopecia.

Substituted phenyl aziridine precursor analogs for inhibiting androgen-independent prostate cancer cell growth

Disclosed are methods and pharmaceutical compositions for modulating one or more steroidal receptor activities. The methods typically utilize and the pharmaceutical compositions typically include one or more substituted phenyl aziridine precursors, their respective aziridines, analogs thereof, derivatives thereof, or pharmaceutically acceptable salts thereof such as CpdA. The methods and compositions may be used for treating diseases, disorders, and conditions associated with glucocorticoid receptor activity, androgen receptor activity, or both, such as cancers, acne vulgaris, and alopecia.

Compounds and compositions for delivery of nutrients and micronutrients to plants

Compounds, including chelated compounds, which may be used for the delivery of nutrients and micronutrients to plants are provided. In addition, processes for preparing such compounds, compositions comprising such compounds, and methods for delivering nutrients and micronutrients to plants with such compounds are provided.