C07C307/02

COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATMENT OF ANDROGEN-MEDIATED DISEASE

Provided herein are steroid sulfatase inhibitor compounds and androgen receptor inhibitor compounds that can be useful in, for example, the treatment of cancers such as prostate cancer and breast cancer. Pharmaceutical compositions and kits including the compounds are described, as well as methods for the treatment of cancer such as prostate cancer and breast cancer.

ACID ADDITION SALTS OF APOMORPHINE, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND METHODS OF USING THE SAME
20210179561 · 2021-06-17 ·

Acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, and acid addition salt of apomorphine isobutyrate salts are disclosed. Also disclosed are pharmaceutical compositions (e.g., unit dosage forms, e.g., films) containing acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, or acid addition salt of apomorphine isobutyrate. Further disclosed are methods of use of acid addition salt of apomorphine glycolate, acid addition salt of apomorphine sulfamate, or acid addition salt of apomorphine isobutyrate.

Compounds for inhibiting the activity of SARS-COV-2 spike glycoprotein
11034655 · 2021-06-15 ·

The present invention relates to compounds of formula (I) and its analogues (II) and (III): in which R.sub.1-R.sub.14, X, Y, Z.sub.1-Z.sub.4 are in the Summary of the Invention; capable of inhibiting the activity of RBD of SARS-COV-2 in its “closed” conformation before it binds with the human ACE2 receptor. The invention further provides a process for the preparation of compounds of the invention. ##STR00001##

Compounds for inhibiting the activity of SARS-COV-2 spike glycoprotein
11034655 · 2021-06-15 ·

The present invention relates to compounds of formula (I) and its analogues (II) and (III): in which R.sub.1-R.sub.14, X, Y, Z.sub.1-Z.sub.4 are in the Summary of the Invention; capable of inhibiting the activity of RBD of SARS-COV-2 in its “closed” conformation before it binds with the human ACE2 receptor. The invention further provides a process for the preparation of compounds of the invention. ##STR00001##

AFFINITY ILLUDOFULVENE CONJUGATES
20210155583 · 2021-05-27 · ·

In an embodiment of the invention, a composition for treating a cell population comprises a medicant. The medicant moiety can be an illudofulvene analog. In an embodiment of the invention, a composition for treating a cell population comprises an Affinity Medicant Conjugate (AMC). The affinity moiety can be an antibody, an antibody fragment, a receptor protein, a peptidic growth factor, an anti-angiogenic protein, a specific binding peptide, protease cleavable peptide, a glycopeptide, a peptide, a peptidic toxin, a protein toxin and an oligonucleotide. The affinity moiety can be covalently bound to the medicant via a linker.

SOLID FORMS COMPRISING 4-AMINO-2-(2,6-DIOXOPIPERIDINE-3-YL)ISOINDOLINE-1,3-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.

SOLID FORMS COMPRISING 4-AMINO-2-(2,6-DIOXOPIPERIDINE-3-YL)ISOINDOLINE-1,3-DIONE AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF

Provided herein are solid forms comprising (a) 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.

CARBAMOYL PHENYLALANINOL ANALOGS AND USES THEREOF
20210093603 · 2021-04-01 ·

The present invention relates to carbamoyl phenylalaninol analogs and methods of using the same to treat disorders.

CARBAMOYL PHENYLALANINOL ANALOGS AND USES THEREOF
20210093603 · 2021-04-01 ·

The present invention relates to carbamoyl phenylalaninol analogs and methods of using the same to treat disorders.

Process for producing acesulfame potassium

In one embodiment, the invention relates to processes for producing acesulfame potassium. In one embodiment, the process comprises the step of reacting a first reaction mixture to form an amidosulfamic acid salt such as a trialkyl ammonium amidosulfamic acid salt. The first reaction mixture comprises sulfamic acid, an amine, and smaller amounts, if any, acetic acid, e.g., less than 1 wt % (10000 wppm). In terms of ranges, the first reaction mixture may comprise from 1 wppm to 1 wt % acetic acid. The process further comprises the step of reacting the amidosulfamic acid salt with diketene to form an acetoacetamide salt. In preferred embodiments, the amidosulfamic acid salt formation reaction is conducted at pH levels from 5.5 to 7.0. The process further comprises the step of deriving the acesulfame-K from the acetoacetamide salt.