C07K5/02

TREATMENTS FOR GASTROINTESTINAL DISORDERS

The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein. using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

SALT FORMS OF S-(N, N-DIETHYLCARBAMOYL)GLUTATHIONE
20220153780 · 2022-05-19 ·

The invention relates in various aspects to a salt form S—(N, N-diethylcarbamoyl)glutathione, a method of producing the salt form, a pharmaceutical composition comprising said salt form. The invention also relates to a method of preventing or treating a glutamate-related disorder comprising administering to said subject a therapeutically effective amount of said salt form.

Cyclic peptide tyrosine tyrosine compounds as modulators of neuropeptide Y receptors

The present invention comprises compounds of Formula I. ##STR00001## wherein: Z.sub.4, Z.sub.7, Z.sub.9, Z.sub.11, Z.sub.22, Z.sub.23, Z.sub.26, Z.sub.30, Z.sub.34, Z.sub.35, p, m, n, q, and BRIDGE are defined in the specification. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel compounds are useful for preventing, treating or ameliorating diseases and disorders, such as obesity, type 2 diabetes, the metabolic syndrome, insulin resistance, and dyslipidemia, among others.

Peptidomimetic proteasome inhibitors

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′): ##STR00001##
where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and ##STR00002##
where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Peptidomimetic proteasome inhibitors

The compounds of the present invention are represented by the following compounds having Formula (I) and Formula (I′): ##STR00001##
where the substituents R, R.sup.1, R.sup.3, R.sup.4, R, W, X, Y, Z, k, and m are as defined herein and ##STR00002##
where the substituents R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, Y, Z, and m are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Derivatives of dolaproine-dolaisoleucine peptides

Provided are peptide analogs, pharmaceutical compositions comprising such compounds, and methods of treating cancer with such compounds.

Treatments for Gastrointestinal Disorders

The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein. using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

Treatments for Gastrointestinal Disorders

The present invention features peptides, compositions, and related methods for treating gastrointestinal disorders and conditions, including but not limited to, irritable bowel syndrome (IBS), gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia, visceral pain, gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudo-obstruction), disorders and conditions associated with constipation, and other conditions and disorders are described herein. using peptides and other agents that activate the guanylate cyclase C (GC-C) receptor.

METHOD FOR PREPARING DRUG-LINKER MC-MMAF FOR ANTIBODY DRUG CONJUGATE, AND INTERMEDIATES THEREIN
20220119441 · 2022-04-21 ·

The disclosure provides a method for preparing drug-linker MC-MMAF for antibody drug conjugates and intermediates therein. The preparation method of the present disclosure improves the reactivity of the N-terminal, thereby effectively controlling the occurrence of racemization; does not directly use the toxin MMAF, but uses fragmented peptides with lower toxicity, which minimizes the operational difficulty in scale-up production; no reverse phase is required and it is easy to prepare and operate.

Heteroaryl sulfone-based conjugation handles, methods for their preparation, and their use in synthesizing antibody drug conjugates

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: ##STR00001##
(wherein R.sup.1, R.sup.2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.