Patent classifications
A61K31/4418
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR
- Mark Thomas Miller ,
- Corey Anderson ,
- Vijayalaksmi Arumugam ,
- Brian Richard Bear ,
- Hayley Marie Binch ,
- Jeremy J. Clemens ,
- Thomas Cleveland ,
- Erica Conroy ,
- Timothy Richard Coon ,
- Bryan A. Frieman ,
- Peter Diederik Jan Grootenhuis ,
- Raymond Stanley Gross ,
- Sara Sabina Hadida-Ruah ,
- Haripada Khatuya ,
- Pramod Virupax Joshi ,
- Paul John Krenitsky ,
- Chun-Chieh Lin ,
- Gulin Erdogan Marelius ,
- Vito Melillo ,
- Jason McCartney ,
- Georgia McGaughey Nicholls ,
- Fabrice Jean Denis Pierre ,
- Alina Silina ,
- Andreas P. Termin ,
- Johnny Uy ,
- Jinglan Zhou
The present invention features a compound of formula I:
##STR00001##
or a pharmaceutically acceptable salt thereof, where R.sub.1, R.sub.2, R.sub.3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.
COMBINATION OF AN AZETIDINE LPA1 RECEPTOR ANTAGONIST WITH PIRFENIDONE AND/OR NINTEDANIB FOR USE IN THE TREATMENT OF FIBROTIC DISEASES
The present invention concerns the compounds of formula (I)
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, X, and Y are as described in the description, and their use as antagonists of the LPA.sub.1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and/or nintedanib, in the prevention and/or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.
COMBINATION OF AN AZETIDINE LPA1 RECEPTOR ANTAGONIST WITH PIRFENIDONE AND/OR NINTEDANIB FOR USE IN THE TREATMENT OF FIBROTIC DISEASES
The present invention concerns the compounds of formula (I)
##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, X, and Y are as described in the description, and their use as antagonists of the LPA.sub.1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and/or nintedanib, in the prevention and/or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.
CYSTEINE PROTEASE INHIBITORS AND METHODS OF USE THEREOF
Described herein are Mpro cysteine protease inhibitors and methods of utilizing such inhibitors in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
CYSTEINE PROTEASE INHIBITORS AND METHODS OF USE THEREOF
Described herein are Mpro cysteine protease inhibitors and methods of utilizing such inhibitors in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
OPIOID RECEPTOR AGONIST, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL USE THEREOF
The invention belongs to the field of pharmacy, and relates to a class of opioid receptor agonists, their preparation method and the pharmaceutical use thereof, in particular to 3-(dimethylaminomethyl) cyclohex-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivatives or salts thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, 3-(dimethylaminomethyl) piperidin-4-ol derivative or salt thereof and preparation method thereof, and relate to the use of said compounds in the treatment of opioid receptor-mediated diseases. The use of the compound or pharmaceutically acceptable salt, solvate or hydrate thereof in the preparation of a medicament for treating indications related to opioid receptors. The opioid receptor-related indications are pain, irritable bowel syndrome, pruritus, addiction and depression.
AMLODIPINE MESYLATE MONOHYDRATE PREPARATION METHOD THEREFOR AND USE THEREOF
Amlodipine mesylate monohydrate, a preparation method therefor and a use thereof. The described amlodipine mesylate monohydrate has high purity, has good fluidity and compressibility, and is suitable for direct tableting processing by a high-speed tablet press.
IMPROVEMENTS IN ULTRASOUND-MEDIATED THERAPY
The present invention relates to the field of ultrasound-mediated therapeutic treatments in combination with gas-filled microvesicles. It relates in particular to enhancing the efficacy of a combined therapeutic treatment of gas-filled microvesicles and ultrasound, by reducing the vasospasm effect caused by said therapeutic treatment.
IMPROVEMENTS IN ULTRASOUND-MEDIATED THERAPY
The present invention relates to the field of ultrasound-mediated therapeutic treatments in combination with gas-filled microvesicles. It relates in particular to enhancing the efficacy of a combined therapeutic treatment of gas-filled microvesicles and ultrasound, by reducing the vasospasm effect caused by said therapeutic treatment.
Treatment of immunosuppressed subjects
An EL-15 super agonist (IL-15N72D:IL-15RαSU/IgG1Fc; N-803) increases circulating NK cells, effector memory and effector memory RA cells in post-allogeneic hematopoietic stem cell transplant patients (HCT). Methods of treatment include administration of N-803 to subjects in need of such treatment.