Antagonists of gonadotropin releasing hormone
AssigneeMerck & Co., Inc.
InventorsMark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
Life of this patent
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Abstract
There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.
Claims10
The compound of the structural formula ##STR297## wherein R is as indicated in the table below:
- ______________________________________ Ex. # R ______________________________________ 8A #STR298## - 8B #STR299## - 8C #STR300## - 8D #STR301## - 8E #STR302## - 8F #STR303## - 8G #STR304## - 8H #STR305## - 8I ##STR306## ______________________________________
The compound of of the structural formula ##STR307## wherein R.sub.6 is as indicated in the table below:
- ______________________________________ Ex. # R.sub.6 ______________________________________ 9A #STR308## - 9B #STR309## - 9C #STR310## - 9D #STR311## - 9E #STR312## - 9F #STR313## - 9G #STR314## - 9H #STR315## - 9I ##STR316## ______________________________________
The compound of the structural formula ##STR317## wherein R and R.sub.6 are as indicated in the table below:
- ______________________________________ Ex. # R R.sub.6 ______________________________________ 10A #STR318## #STR319## - 10B #STR320## #STR321## - 10C #STR322## #STR323## - 10D #STR324## #STR325## - 10E #STR326## #STR327## - 10F #STR328## #STR329## - 10G #STR330## #STR331## - 10H #STR332## #STR333## - 10I #STR334## #STR335## - 10J #STR336## #STR337## - 10J #STR338## #STR339## - 10K #STR340## #STR341## - 10L #STR342## #STR343## - 10M #STR344## #STR345## - 10N #STR346## #STR347## - 10O #STR348## #STR349## - 10P #STR350## #STR351## - 10Q #STR352## #STR353## - 10R #STR354## #STR355## - 10S #STR356## #STR357## - 10T #STR358## #STR359## - 10U #STR360## #STR361## - 10V #STR362## #STR363## - 10W #STR364## #STR365## - 10X #STR366## #STR367## - 10Y #STR368## ##STR369## ______________________________________
The compound of the structural formula ##STR370## wherein R and R.sub.6 are as indicated in the table below:
- ______________________________________ Ex. # R R.sub.6 ______________________________________ 11A #STR371## #STR372## - 11B #STR373## #STR374## - 11C #STR375## #STR376## - 11D #STR377## #STR378## - 11E #STR379## #STR380## - 11F #STR381## #STR382## - 11G #STR383## #STR384## - 11H #STR385## #STR386## - 11I #STR387## #STR388## - 11J #STR389## #STR390## - 11K #STR391## #STR392## - 11L #STR393## #STR394## - 11N #STR395## #STR396## - 11O #STR397## #STR398## - 11P #STR399## #STR400## - 11Q #STR401## #STR402## - 11R #STR403## #STR404## - 11S #STR405## ##STR406## ______________________________________
The compound of the structural formula ##STR407## wherein R.sub.6, R.sub.7 and R.sub.8 is as indicated in the table below:
- ______________________________________ Ex. # R.sub.6 R.sub.7 R.sub.8 ______________________________________ 12A H H TR408## - 12B H H TR409## - 12C H H TR410## - 12D H Cl R411## - 12E H Cl R412## - 12F H H TR413## - 12F H Cl R414## - 12G CF.sub.3 H - 12H CF.sub.3 H ______________________________________
The compound of the structural formula ##STR417## wherein R.sub.6 is as indicated in the table below:
- ______________________________________ Ex. # R.sub.6 ______________________________________ 13A #STR418## - 13B ##STR419## ______________________________________
The compound of the structural formula ##STR420## wherein R, R.sub.2, R.sub.3, R.sub.4 and R.sub.6 are as indicated in the table below:
- __________________________________________________________________________ Ex. # R R.sub.6 ##STR421## __________________________________________________________________________ 14A #STR422## #STR423## #STR424## 14B ## TR425## ##STR426## ##STR427## - 14C #STR428## #STR429## #STR430## - 14D #STR431## #STR432## ##STR433## __________________________________________________________________________
A compound of the formula ##STR434## or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof, wherein R is as indicated in the table below:
- ______________________________________ Ex. # R ______________________________________ 3A #STR435## - 3B #STR436## - 3C #STR437## - 3D #STR438## - 3P #STR439## - 4I #STR440## - 4EE #STR441## - 4LL #STR442## - 5 #STR443## - 6V #STR444## - 6W #STR445## - 12I #STR446## - 12J #STR447## - 12K ##STR448## ______________________________________
A compound of the formula ##STR449## or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof, wherein R is as indicated in the table below:
- ______________________________________ Ex. # R ______________________________________ 9G ##STR450## ______________________________________
The compound the structural formula ##STR451## wherein R.sub.6 is as indicated in the table below:
- ______________________________________ Ex. # R.sub.6 ______________________________________ 1A #STR452## - 1B #STR453## - 1C #STR454## - 1D #STR455## - 1E #STR456## - 1F #STR457## - 1G #STR458## - 1H #STR459## - 1I #STR460## - 1J #STR461## - 1K #STR462## - 1L #STR463## - 1M #STR464## - 1N #STR465## - 1O #STR466## - 1P #STR467## - 1Q #STR468## - 1R #STR469## - 1S #STR470## - 1T #STR471## - 1U #STR472## - 1V #STR473## - 2A #STR474## - 2B #STR475## - 2C #STR476## - 2D #STR477## - 2E #STR478## - 2F #STR479## - 2G #STR480## - 2H #STR481## - 2I #STR482## - 2J #STR483## - 2K #STR484## - 2L #STR485## - 3E #STR486## - 3F #STR487## - 3G #STR488## - 3H #STR489## - 3I #STR490## - 3J #STR491## - 3K #STR492## - 3L #STR493## - 3M #STR494## - 3N #STR495## - 3O #STR496## - 4A #STR497## - 4B #STR498## - 4C #STR499## - 4D #STR500## - 4E #STR501## - 4F #STR502## - 4G #STR503## - 4H #STR504## - 4J #STR505## - 4K #STR506## - 4L #STR507## - 4M #STR508## - 4N #STR509## - 4O #STR510## - 4P #STR511## - 4Q #STR512## - 4R #STR513## - 4S #STR514## - 4T #STR515## - 4U #STR516## - 4V #STR517## - 4W #STR518## - 4X #STR519## - 4Y #STR520## - 4Z #STR521## - 4AA #STR522## - 4BB #STR523## - 4CC #STR524## - 4DD #STR525## - 4FF #STR526## - 4GG #STR527## - 4HH #STR528## - 4II #STR529## - 4JJ #STR530## - 4KK #STR531## - 4MM #STR532## - 4NN #STR533## - 4OO #STR534## - 4PP #STR535## - 6A #STR536## - 6B #STR537## - 6C #STR538## - 6D #STR539## - 6E #STR540## - 6F #STR541## - 6G #STR542## - 6H #STR543## - 6I #STR544## - 6J #STR545## - 6K #STR546## - 6L #STR547## - 6M #STR548## - 6N #STR549## - 6O #STR550## - 6P #STR551## - 6Q #STR552## - 6R #STR553## - 6S #STR554## - 6T #STR555## - 6U #STR556## - 6X #STR557## - 6Y #STR558## - 6Z #STR559## - 7A #STR560## - 7B #STR561## - 7C #STR562## - 7D #STR563## - 7E #STR564## - 7F #STR565## - 7G #STR566## - 7H ##STR567## ______________________________________
Dependencies are inferred from the claim text.