A61K38/31

Arylfluorosulfate compounds and methods

A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO.sub.2F.sub.2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilanol to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.

Arylfluorosulfate compounds and methods

A high-throughput screening methods for identifying candidate anticancer medicinal agents is described herein. The candidate anticancer medicinal agents are arylfluorosulfate compounds derived from phenolic compounds. The method involves in situ generation of the arylfluorosulfate compounds in multi-well plates by reaction of phenolic compounds in DMSO with a saturated solution of SO.sub.2F.sub.2 dissolved in a solvent such as acetonitrile, in the presence of an organic base, followed by reaction of generated fluoride ion with trimethylsilanol to form volatile trimethylsilyl fluoride. Solvents, organic base, and silyl compounds are then removed, in vacuo, to afford the arylfluorosulfate compounds suitable for biological screening in cancer cell lines without further purification.

STORAGE STABLE SOMATOSTATIN-DOPAMINE CHIMERIC COMPOUNDS AND SALT FORMS THEREOF

The disclosure provides storage-stable somatostatin-dopamine chimeric analog compounds and storage-stable pharmaceutical compositions thereof for use in treating endocrine diseases and endocrine tumors.

STORAGE STABLE SOMATOSTATIN-DOPAMINE CHIMERIC COMPOUNDS AND SALT FORMS THEREOF

The disclosure provides storage-stable somatostatin-dopamine chimeric analog compounds and storage-stable pharmaceutical compositions thereof for use in treating endocrine diseases and endocrine tumors.

METHODS OF TREATING HEPATIC ENCEPHALOPATHY
20230330071 · 2023-10-19 ·

The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin.

METHODS OF TREATING HEPATIC ENCEPHALOPATHY
20230330071 · 2023-10-19 ·

The application describes treatment of hepatic encephalopathy using gastrointestinal specific antibiotics. One example of a gastrointestinal specific antibiotic is rifaximin.

METHODS OF REDUCING THE LIKELIHOOD OF CARCINOID HEART DISEASE IN PATIENTS WITH NEUROENDOCRINE TUMORS
20230310434 · 2023-10-05 ·

Described herein are methods of treating a human patient with a newly diagnosed neuroendocrine tumor, methods of treating patients with neuroendocrine tumors with early signs of carcinoid heart disease who have not had a heart valve replacement, and methods of treating a human patient with the neuroendocrine tumor who has had a recent heart valve replacement. Administering telotristat ethyl to these patients can reduce the development of carcinoid heart disease and improve clinical outcomes.

METHODS OF REDUCING THE LIKELIHOOD OF CARCINOID HEART DISEASE IN PATIENTS WITH NEUROENDOCRINE TUMORS
20230310434 · 2023-10-05 ·

Described herein are methods of treating a human patient with a newly diagnosed neuroendocrine tumor, methods of treating patients with neuroendocrine tumors with early signs of carcinoid heart disease who have not had a heart valve replacement, and methods of treating a human patient with the neuroendocrine tumor who has had a recent heart valve replacement. Administering telotristat ethyl to these patients can reduce the development of carcinoid heart disease and improve clinical outcomes.

MIXTURES AND FORMULATIONS
20230285502 · 2023-09-14 · ·

The present invention relates to mixtures comprising: i) at least one lipid and/or at least one oil; and ii) an alkyl ammonium EDTA salt;
wherein the mixture has a water content in the range of 0 to 1.0 wt %.

The invention further relates to mixtures which are pre-formulations, methods of treatment comprising administration of such pre-formulations, to pre-filled administration devices and kits containing the formulations, to the use of an alkylammonium EDTA salt to reduce the decomposition of the lipid components and/or any active agent contained within the pre-formulation, and to alkyl ammonium EDTA salts as described herein.

Method of delivering a somatostatin compound into a lumen of the intestinal tract using a swallowable drug delivery device
11813314 · 2023-11-14 · ·

Embodiments of the invention provide swallowable devices, preparations and methods for delivering drugs and other therapeutic agents within the GI tract. Many embodiments provide a swallowable device for delivering the agents. Particular embodiments provide a swallowable device such as a capsule for delivering drugs into the intestinal wall or other GI lumen. Embodiments also provide various drug preparations that are configured to be contained within the capsule, advanced from the capsule into the intestinal wall and degrade to release the drug into the bloodstream to produce a therapeutic effect. The preparation can be operably coupled to delivery means having a first configuration where the preparation is contained in the capsule and a second configuration where the preparation is advanced out of the capsule into the intestinal wall. Embodiments of the invention are particularly useful for the delivery of drugs which are poorly absorbed, tolerated and/or degraded within the GI tract.