Patent classifications
C07D207/12
AMINO DITHIOPERACID THIOESTER COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF
An amino dithioperacid thioester compound, a preparation method therefor, and use thereof. The structural formula of compound is as shown in formula I: wherein m=1-11, X is a nitrogen-containing aliphatic heterocyclic ring, and a nitrogen atom in the aliphatic heterocyclic ring is connected to a carbon atom of a thiocarbonyl group. The compounds disclosed by the invention are found to be capable of relieving muscular atrophy and lipolysis caused by cancer cachexia through in-vivo and in-vitro experiments. The compounds are also capable of obviously relieving weight and food intake reduction caused by cancer cachexia in animal experiments, so that the carbamo(dithioperoxo)thioates compounds have the effect on resisting cancer cachexia, can be applied to the treatment of cancer cachexia and related diseases, and become one kind of ideal cancer cachexia treatment medicament.
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CARBOHYDRATE CONJUGATE RNA AGENTS AND PROCESS FOR THEIR PREPARATION
This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.
CARBOHYDRATE CONJUGATE RNA AGENTS AND PROCESS FOR THEIR PREPARATION
This disclosure relates to an improved process for the preparation of carbohydrate conjugates. The disclosure also relates to carbohydrate conjugated iRNA agents comprising these carbohydrate conjugates, which have improved purity and are advantageous for the in vivo delivery of the iRNA agents.
PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS
The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.
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PROSTAGLANDIN E2 (PGE2) EP4 RECEPTOR ANTAGONISTS
The present invention relates to novel compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as prostaglandin E2 (PGE2) EP4 receptor antagonists, which renders them highly advantageous for use in therapy, particularly in the treatment or prevention of cancer, a neovascular eye disease, inflammatory pain, or an inflammatory disease, such as, e.g., multiple sclerosis, rheumatoid arthritis or endometriosis.
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CHOLINE METABOLISM INHIBITORS
The present disclosure relates to compounds, compositions and methods for inhibiting choline metabolism, e.g., conversion of choline to trimethylamine. Disclosed herein are compounds, compositions, and methods for inhibiting choline metabolism, e.g., conversion of choline to TMA. Also disclosed herein are compounds, methods and compositions for inhibiting choline metabolism by gut microbiota resulting in reduction in the formation of trimethylamine (TMA) and trimethylamine N-oxide (TMAO).
Synthetic Lubricity Additives for Hydrocarbon Fuels
Lubricity additives for hydrocarbon fuels are presented according to formula I:
R.sup.1[(—O—R.sup.2).sub.n-Q].sub.p (I)
wherein p is 3 or greater; each n is independently selected from integers equal to 2 or greater; R.sup.1 is a C3-C20 aliphatic hydrocarbon group of valence p which is branched or linear and which is substituted or unsubstituted; each R.sup.2 is independently selected from C2-C20 divalent aliphatic or aromatic hydrocarbon groups which are branched or linear and which are substituted or unsubstituted; and each Q is independently selected from —NH.sub.2 or a moiety according to formula II:
##STR00001##
wherein each R.sup.3 is independently selected from C8-C60 alkenyl groups which are substituted or unsubstituted, providing that at least one Q is the moiety according to formula II.
Synthetic Lubricity Additives for Hydrocarbon Fuels
Lubricity additives for hydrocarbon fuels are presented according to formula I:
R.sup.1[(—O—R.sup.2).sub.n-Q].sub.p (I)
wherein p is 3 or greater; each n is independently selected from integers equal to 2 or greater; R.sup.1 is a C3-C20 aliphatic hydrocarbon group of valence p which is branched or linear and which is substituted or unsubstituted; each R.sup.2 is independently selected from C2-C20 divalent aliphatic or aromatic hydrocarbon groups which are branched or linear and which are substituted or unsubstituted; and each Q is independently selected from —NH.sub.2 or a moiety according to formula II:
##STR00001##
wherein each R.sup.3 is independently selected from C8-C60 alkenyl groups which are substituted or unsubstituted, providing that at least one Q is the moiety according to formula II.
Crystalline form of sofpironium bromide and preparation method thereof
A cocrystal containing the 1′R-diastereomer and the 1′S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1′R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.
Crystalline form of sofpironium bromide and preparation method thereof
A cocrystal containing the 1′R-diastereomer and the 1′S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1′R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.