301847-02-9Relevant articles and documents
Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair
Antczak, Monika I.,Zhang, Yongyou,Wang, Changguang,Doran, Jennifer,Naidoo, Jacinth,Voruganti, Sukesh,Williams, Noelle S.,Markowitz, Sanford D.,Ready, Joseph M.
, p. 3979 - 4001 (2017/05/19)
The enzyme 15-prostaglandin dehydrogenase (15-PGDH) catalyzes the first step in the degradation of prostaglandins including PGE2. It is a negative regulator of tissue repair and regeneration in multiple organs. Accordingly, inhibitors of 15-PGDH are anticipated to elevate in vivo levels of PGE2 and to promote healing and tissue regeneration. The small molecule SW033291 (1) inhibits 15-PGDH with Ki = 0.1 nM in vitro, doubles PGE2 levels in vivo, and shows efficacy in mouse models of recovery from bone marrow transplantation, ulcerative colitis, and partial hepatectomy. Here we describe optimized variants of 1 with improved solubility, druglike properties, and in vivo activity.
COMPOSITIONS AND METHODS OF MODULATING 15-PGDH ACTIVITY
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, (2013/11/05)
Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.
Synthesis and reactions of some new heterocyclic compounds containing the thienylthieno[2,3-b]pyridine moiety
Bakhite, Etify A.,Abdel-Rahman, Abdu E.,Mohamed, Omima S.,Thabet, Eman A.
, p. 1983 - 2006 (2007/10/03)
(4-Aryl-3-cyano-6-(2-thienyl)pyridin-2-ylthio)acethydrazides (5a-c), 3-amino-4-aryl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carbohydrazides (6a-c) and 3-amino-4-phenyl-6-(2-thienyl)thieno[2,3-b]pyridine-2-carboxylic acid (30) were prepared and employed as key intermediates in the synthesis of the title compounds.
Bicyclic heteroamatic compounds useful as LH agonists
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, (2008/06/13)
The invention relates to a bicyclic heteroaromatic derivative compound according to general formula (I), or a pharmaceutically acceptable salt thereof, wherein R1is NR5R6, OR5, SR5or R7; R5and R6are independently selected from H, (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, alkyl(1-8C)carbonyl, (6-14C)arylcarbonyl, (6-14C)aryl or (4-13C)heteroaryl, or R5and R6together are joined in a (2-7C)heterocloalkyl ring; R7is (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl or (4-13C)heteroaryl, R2is (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, or (6-14C)aryl or (4-13C)heteroaryl, both optionally substituted with one or more substituents selected from (1-8C)alkyl, (1-8C)alkylthio, (1-8C)(di)alkylamino, (1-8C)alkoxy, (2-8C)alkenyl, or (2-8C)alkynyl; R3is (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, or (6-14C)aryl or (4-13C)heteroaryl, both optionally substituted with one or more substituents selected from (1-8C)alkyl, (1-8C)(di)alkylamino or (1-8C)alkoxy; X is S, O or N(R4); R4is H, (1-8C)alkyl, (1-8C)alkylcarbonyl, (6-14C)arylcarbonyl or (6-14C)aryl(1-8C)alkyl; Y is CH or N; Z is NH2or OH; A is S, N(H), N(R9), O or a bond; R9can be selected from the same groups as described for R2and B is N(H), O or a bond. The compounds of the invention have LH receptor activating activity and can be used in fertility regulating therapies.