Derivatives of 1,3,5 estra - (10) - 3 -, 16 - tetraen carboxamide, processes for their preparation, Pharmaceutical Preparations Containing them, and their use for preparing medicaments
ULRICH DR. BOTHE,NAOMI DRA. BARAK,MATTHIAS DR. BUSEMANN,OLIVER MARTIN DR. FISCHER,ANDREA DR. ROTGERI,ISABELLA DRA. GASHAW,INGO DR. HARTUNG,TOBIAS DR. MARQUARDT
申请号:
ARP120103610
公开号:
AR088180A1
申请日:
2012.09.28
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
It refers to akr1c3 inhibitors and their preparation procedures, procedures for the treatment and / or prevention of diseases, and procedures for the treatment and / or prevention of diseases, especially bleeding and intrauterine diseases. 1. Requirement 1: formula compound (1),There, R1 and R2 are independent,Hydrogen, fluorine, chlorine, nitro, trifluoromethyl, pentafluoroacetylene, metoxi, etoxi, trifluorometoxi, - oc8322%; cf832323;CH₃SO₂-,CH CH SO -- (C 3DO) CH1. Carbohydrate, c8321j-83318324;Hydroxy -, ch8322; - C (ch832323) 8322; - Oh, - conh832222;-(C = O) NH asphalt, - (C = O) n (ch832323) 8322;-SO₂NH₂,-SO NH (CH)-SO₂N (CH₃) ₂ or the replacement of a C-H group in the pyridine ring with a nitrogen atom; and R³ and R⁴ are hydrogen or R³ is hydroxyl, fluorine, methoxy or ethoxy and R⁴ is hydrogen or R³ is hydrogen and R⁴ is hydroxyl, fluorine, methoxy or ethoxy; and R⁵ and R⁶ are hydrogen or R⁵ is fluorine, hydroxyl, methoxy or ethoxy and R⁶ is hydrogen or R⁵ is hydrogen and R⁶ is fluorine; and R⁷ is hydrogen, C₁₋₄ alkyl,C₃₋₆ cycloalkyl,1. Cyclopropyl methyl, trifluoromethyl or 2,2,2-trifluoroethane; and r831222 es-cr7491; r74955-cooh, where r74919 and r7495son are independent;a. Hydrogen, methyl, ethyl or r74491y and r74955 together - (ch832225) - are combined with n = 2, 3, 4 or 5, where ch832291 and r7495son are added together - ch8322-o-ch8322 -, in which up to four ch83222 hydrogen atoms can be replaced by r74919 and r7495n;-CH₂-NH-CH₂-,-CH -N (CH) -CH --CH CH -O-CH CH --CH CH -NH-CH CH --Ch8322; - ch8322n (ch832323) - ch8322; - or r749191 together with r8311l - (ch832222) - 8345; - n = 1, 2, 3, 4, including at most four ch832291 hydrogen atoms, together with r8311ch2283o-228391;-Ch-832222-n (ch-8322); ch 832222 - and r-74959 hydrogen, methyl or ethyl o-cr75808; r74969-cr7497; r758480;R74966,R7497r75848 is hydrogen, r758080;R7496son, independent of each other,methyl, ethyl or are together - (CH₂) ₙ- with n = 2, 3, 4, 5 or -CH₂CH₂-O-CH₂CH₂- and Rᵉ,R758484