Modulators of the relaxin receptor 1

Patent metadata

Field	Value
Publication number	US-10125112-B2
Application number	US-201615247438-A
Country	US
Kind code	B2
Filing date	Aug 25, 2016
Priority date	May 4, 2012
Publication date	Nov 13, 2018
Grant date	Nov 13, 2018

Abstract

Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R 1 , and R 2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

First claim

The invention claimed is:

1. A compound or pharmaceutically acceptable salt thereof having the formula

where:
R 10 and R 21 are each 0 to 3 substitutents independently chosen from hydroxyl, halogen, nitro, cyano, amino, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, mono- and di-(C 1 -C 2 alkyl)amino-, a C 1 -C 2 haloalkyl, and C 1 -C 2 haloalkoxy;
R 20 is NO 2 , CN, C 2 -C 10 haloalkyl, C 1 -C 10 haloalkoxy, —SR 7 , —SOR 7 , or —SO 2 R 7 , where R 7 is C 1 -C 10 carbhydryl or C 1 -C 10 haloalkyl; and
R 3 is cyclohexyl.

2. A method for therapeutic intervention in a facet of mammalian health that is mediated by a mammalian relaxin receptor 1, the method comprising administering to a mammal in need thereof an effective amount of a compound or salt of claim 1 , wherein the facet of mammalian health is heart failure.

3. A compound or salt of the formula

wherein R 2 is selected from:

Assignees

• The Us Secretary Department Of Health And Human Service
• The Florida International Univ Board Of Trustees
• Us Health

Inventors

• Marugan Juan Jose
• Xiao Jingbo
• Ferrer-Alegre Marc
• Chen Catherine
• Southall Noel
• Zheng Wei
• Agoulnik Alexander
• Agoulnik Irina

Classifications

• C07D333/40

  Thiophene-2-carboxylic acid · CPC title

• C07C2601/04

  with a four-membered ring · CPC title

• C07C235/64

  having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring · CPC title

• C07C2603/74

  Adamantanes · CPC title

• C07D403/10

  linked by a carbon chain containing aromatic rings · CPC title