C07D277/18

IL-17A ACTIVITY INHIBITOR AND USE THEREOF

A low-molecular-weight compound (IL-17 activity inhibitor) having an IL-17 activity-inhibiting ability. The IL-17RA inhibitor is a compound which can bind to interleukin 17 receptor A (IL-17RA) through a non-covalent interaction including at least one intermolecular interaction selected from the group that includes a van der Waals force acting among at least 13 amino acid residues selected from amino acid residues Phe60, Gln87, Asp121, Pro122, Asp123, Gln124, Asp153, Cys154, Glu155, Lys160, Pro164, Cys16 5, Ser167, Ser168, Gly169, Ser170, Leu171, Trp172, Asp173, Pro174, Pro254, Phe256, Ser258, Cys 259, Asp262, Cys263, Leu264 and His266 contained in, for example, an extracellular domain of human IL-17RA and preferably consists of an ionic bond, a hydrogen bond, a CH- interaction and a hydrophobic interaction each acting among specified amino acid residues among the above-mentioned amino acid residues in a space surrounded by the above-mentioned amino acid residues, and which has an activity to inhibit the binding of interleukin-17A (IL-17A) to IL-17RA originated from human or the like, or a pharmaceutically acceptable salt, solvate or prodrug of the compound.

MANUFACTURING METHODS AND POLYMORPHS OF A THIAZOLINE ANTI-HYPERALGESIC AGENT
20200354328 · 2020-11-12 ·

Provided herein are methods of making a thiazoline anti-hyperalgesic, Compound 1, and polymorphs thereof. The methods described herein use inexpensive reagents and are capable of providing Compound 1 in commercial-scale quantities. Also provided are pharmaceutical compositions of Compound 1 suitable for human administration.

MANUFACTURING METHODS AND POLYMORPHS OF A THIAZOLINE ANTI-HYPERALGESIC AGENT
20200354328 · 2020-11-12 ·

Provided herein are methods of making a thiazoline anti-hyperalgesic, Compound 1, and polymorphs thereof. The methods described herein use inexpensive reagents and are capable of providing Compound 1 in commercial-scale quantities. Also provided are pharmaceutical compositions of Compound 1 suitable for human administration.

PROCEDURE FOR THE PREPARATION OF 2-CYANOIMINO-1,3-THIAZOLIDINE
20200347024 · 2020-11-05 ·

The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.

PROCEDURE FOR THE PREPARATION OF 2-CYANOIMINO-1,3-THIAZOLIDINE
20200347024 · 2020-11-05 ·

The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.

Procedure for the preparation of 2-cyanoimino-1,3-thiazolidine

The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.

Procedure for the preparation of 2-cyanoimino-1,3-thiazolidine

The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

N-acyl amino acid compounds and methods of use

The invention relates to compounds of formula (I): ##STR00001##
or a salt thereof, wherein R.sup.1, A, L, and R.sup.2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are v1 integrin inhibitors that are useful for treating tissue specific fibrosis.

Procedure for the Preparation of 2-Cyanoimino-1,3-Thiazolidine
20190152933 · 2019-05-23 ·

The disclosure provides for methods for preparing 2-cyanoimino-1,3-thiazolidine, which is an important building block for the preparation of crop protection active ingredients and pharmaceuticals. To this end, the disclosure provides for more efficient and improved methods of preparing 2-cyanoimino-1,3-thiazolidine.