17alfa - alkyl 17beta Oxy estratrienos and Intermediates for their preparation, use of 17alfa - alkyl 17beta Oxy estratrienos to obtain Medicines and Pharmaceutical preparations.

摘要

The disadvantage of known estrogen reactive compounds in stratified groups is that they do not have species effectiveness, so,Reduced tolerance In order to solve this problem, it is proposed to change the general formula (1) of 17 tar-17b-oxi-estra-1, 3, 5 (10) - three-year period to. In addition, 17-oxo-estra-1, 3, 5 (10) - 3 years, and 17b-hidroxi-estra-1, 3, 5 (10) - 3 years are mentioned in this document as intermediate products to help inventors prepare. The method involves the use of 17 tar-17b-oxygen-stratosphere to obtain drugs and pharmaceutical preparations containing at least 17 tar-17b-oxygen-stratosphere and at least one drug resistant scaffold. 1. Requirement 1: 17a-ojil-17b-oxi-prsp-general (1),Among them, Hal is f or Cl, which is in 11b position and connected with basic stratospheric structure; R3 is hydrogen, C1-4 tar, C1-4 alkane or c3-7 cyclic ether containing O atom; R17 is hydrogen, C1-4 tar and C1-4 alkane; R17 '' is C1-4 tar, C1-4 tar, and at least part of fluorinated C1-4 radical tar, Among them, R17 '- or connected with 17b and R17 position' 'is the 17th position connected with the basic trench structure, while SK is the u-v-w-x-y-z-e cluster. Through the u-v-w-x-y-z-e cluster, it is connected with the trench structure at 7a position. U represents the radical cypress reservoir of C1-13,C1-13 alquenileno C1-13 or C1-13 linear or separable chain or group A-B, in which a is connected to the stratospheric basic structure connected by - CH2 and a chlorobenzene matrix to the stratospheric basic structure, The basic stratospheric structure is connected by a concrete layer and a group B of phenyl radicals or c1-3 type radical tenants. It is a C1-13, C1-13 alquenileno C1-13 or C1-13 linear or separable chain asphalt, where a and B can also be connected by O atoms, Where V represents a CH2 or C (o) group,Where W is an n (R6) or N + (o -) (R6) group or a Azolla ring or an N-oxidation Azolla ring, wherein the Azolla or N-oxidation Azolla ring contains at least one C atom of group x, in addition, R6 is h, or ch2-r7 or C (o) - R7, R7 may mean (a) hydrogen or (b) a c1-14, c1-14 alquinio c1-14 or c1-14 linear or separable chain tar, nonfluorinated or at least partially fluorinated, monomeric or polyhydroxy, interrupted by one to three heteroatoms (o-y-s) and / or composition (nr9),where R9 is hydrogen or a C1-3 alkyl radical, or c) an unsubstituted or substituted aryl or heteroaryl radical or d) an unsubstituted or substituted C3-10 cycloalkyl radical or e) an unsubstituted or substituted C4-15 cycloalkylalkyl radical of) a C7 aralkyl radical -20 unsubstituted or substituted or g) an unsubstituted or substituted heteroaryl-C1-6 alkyl radical or oh) an unsubstituted or substituted aminoalkyl radical or a biphenyl radical; where X is, in addition, a radical of straight or branched chain C1-12 alkylene, C1-12 alkenylene or C1-12 alkynylene, where y is a direct bond between X and Z or may mean the following: a) a SOn- group R10, where n = 0, 1 or 2,Only when w is n + (o -) (R6) or n-nitrous oxide ring instead of n (R6) or subland ring, R10 represents the direct connection between Z or C1-6 tar, C1-6 alquenileno C1-6 or C1-6 tar, or (b) R11 u-o-r11 group, wherein R11 is (I) C1-5 radical tar,straight or branched chain C1-5 alkenylene or C1-5 alkynylene or ii) an unsubstituted or substituted C3-10 cycloalkyl radical or iv) an unsubstituted or substituted cycloalkylalkyl radical or iv ) an unsubstituted or substituted C7-20 aralkyl radical or vi) an unsubstituted or substituted heteroaryl-C1-6 alkyl, or c) the CH = CF group or d) the HN-C (O) -NH-R12 group, where R12 is a unsubstituted or substituted arylene radical and where R12 is attached to Z, and where in addition Z represents a direct bond between Y and E or a C1-9 alkylene radical,C1-9 alquenileno c1-9 or c1-9 linear or branched diene may be partially or completely fluorinated. In addition, e is a CF3 or at least partially fluorinated arilo group, and the addition of salts and esters of pharmacologically resistant acid is also included.