C07H13/12

TARGETED DELIVERY OF 1,2,4,5 TETRAOXANE COMPOUNDS AND THEIR USES
20240101584 · 2024-03-28 · ·

1, 2, 4, 5-tetraoxane compounds and derivatives thereof that have anticancer properties are disclosed. Pharmaceutical compositions and pharmaceutical formulations in unit dosage form suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical compositions or formulations may include one or more active agents in addition to the compounds, such as one or more additional anticancer agents. Methods for treating a cancer, reducing a cancer, or treating or ameliorating one or more symptoms associated with a cancer in a subject are also disclosed. The methods include (i) administering to a subject in need thereof an effective amount of the compound (s). The compound (s) can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. The compound can selectively kill cancer cells and/or cancer stem cells over non-cancerous cells by triggering ferroptosis in the cancer cells and/or cancer stem cells.

TARGETED DELIVERY OF 1,2,4,5 TETRAOXANE COMPOUNDS AND THEIR USES
20240101584 · 2024-03-28 · ·

1, 2, 4, 5-tetraoxane compounds and derivatives thereof that have anticancer properties are disclosed. Pharmaceutical compositions and pharmaceutical formulations in unit dosage form suitable for the delivery of the compounds to a subject in need thereof are disclosed. The pharmaceutical compositions or formulations may include one or more active agents in addition to the compounds, such as one or more additional anticancer agents. Methods for treating a cancer, reducing a cancer, or treating or ameliorating one or more symptoms associated with a cancer in a subject are also disclosed. The methods include (i) administering to a subject in need thereof an effective amount of the compound (s). The compound (s) can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. The compound can selectively kill cancer cells and/or cancer stem cells over non-cancerous cells by triggering ferroptosis in the cancer cells and/or cancer stem cells.

Use of CO2 for the synthesis of cyclic glycocarbonates and linear polyglycocarbonates by polycondensation from glycans

Provided herein are methods for synthesizing cyclic carbonates, glycocarbonates, and polyglycocarbonates by reacting polyol glycans with carbon dioxide. Synthesis can include selective polycondensation of polyol glycan hydroxyl moieties.

Use of CO2 for the synthesis of cyclic glycocarbonates and linear polyglycocarbonates by polycondensation from glycans

Provided herein are methods for synthesizing cyclic carbonates, glycocarbonates, and polyglycocarbonates by reacting polyol glycans with carbon dioxide. Synthesis can include selective polycondensation of polyol glycan hydroxyl moieties.

Glucuronide prodrugs of tofacitinib

The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: ##STR00001##
where A.sup.1 and R.sup.1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Glucuronide prodrugs of tofacitinib

The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: ##STR00001##
where A.sup.1 and R.sup.1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.

Ribose cationic lipids

Disclosed are cationic lipids which are compounds of Formula (I). Cationic lipids provided herein can be useful for delivery and expression of mRNA and encoded protein, e.g., as a component of liposomal delivery vehicle, and accordingly can be useful for treating various diseases, disorders and conditions, such as those associated with deficiency of one or more proteins. ##STR00001##

KRAS INHIBITOR AND PHARMACEUTICAL USES THEREOF

The disclosure relates to KRAS.sup.G12D inhibitor compounds having the structure of Formula (A) or Formula (B), pharmaceutical compositions thereof, and methods of use thereof for inhibiting, treating, and/or preventing KRAS.sup.G12D mutation-associated diseases, disorders and conditions.

##STR00001##

Alpha-selective sialyl donor and its uses for preparation of sialosides
10435425 · 2019-10-08 · ·

Disclosed herein a sialyl donor and its use for the synthesis of gangliosides. The sialyl donor has the structure of, ##STR00001##
wherein, R.sub.1 and R.sub.2 are independently benzoyl, toluenesulfonyl, pivaloyl or acetyl optionally substituted with a halogen; and R.sub.3 is acetyl or (O)CCH.sub.2OH. In one preferred embodiment, in the sialyl donor of formula (I), R is acetyl. Also disclosed herein is a method of synthesizing a sialoside. The method comprises steps of: coupling the sialyl donor of formula (I) with a glycosyl acceptor having a primary hydroxyl group in the presence of N-iodosuccinimide (NIS) and trifluoromethanesulfonic acid (TfOH) under suitable conditions; and isolating the sialoside, which has an -glycosidic linkage. According to preferred embodiments, the coupling is conducted in a solvent selected from the group consisting of, CH.sub.3CN, CH.sub.3Cl, and CH.sub.2Cl.sub.2 at a temperature between 20 C. to 60 C. Additionally or optionally, the coupling is conducted in CH.sub.2Cl.sub.2 with the presence of a powdered molecular sieve at 40 C.

Alpha-selective sialyl donor and its uses for preparation of sialosides
10435425 · 2019-10-08 · ·

Disclosed herein a sialyl donor and its use for the synthesis of gangliosides. The sialyl donor has the structure of, ##STR00001##
wherein, R.sub.1 and R.sub.2 are independently benzoyl, toluenesulfonyl, pivaloyl or acetyl optionally substituted with a halogen; and R.sub.3 is acetyl or (O)CCH.sub.2OH. In one preferred embodiment, in the sialyl donor of formula (I), R is acetyl. Also disclosed herein is a method of synthesizing a sialoside. The method comprises steps of: coupling the sialyl donor of formula (I) with a glycosyl acceptor having a primary hydroxyl group in the presence of N-iodosuccinimide (NIS) and trifluoromethanesulfonic acid (TfOH) under suitable conditions; and isolating the sialoside, which has an -glycosidic linkage. According to preferred embodiments, the coupling is conducted in a solvent selected from the group consisting of, CH.sub.3CN, CH.sub.3Cl, and CH.sub.2Cl.sub.2 at a temperature between 20 C. to 60 C. Additionally or optionally, the coupling is conducted in CH.sub.2Cl.sub.2 with the presence of a powdered molecular sieve at 40 C.