17 Beta-amino and hydroxylamino-11 beta-arylsteroids and their derivatives having agonist or antagonist hormonal properties

17 Beta-amino and hydroxylamino-11 beta-arylsteroids and their derivatives having agonist or antagonist hormonal properties

  • CN 1,303,391 A
  • Filed: 05/28/1999
  • Published: 07/11/2001
  • Est. Priority Date: 05/29/1998
  • Status: Abandoned Application
First Claim
Patent Images

1. , the hormone of structure I or hormone antagonist steroide, Wherein R 1Be (R 2R 3N (O) r)-, r wherein is 0 or 1, R 2And R 3Be H, C independently of one another 1-6Alkyl, C 3-8Cycloalkyl, C 2-6Thiazolinyl or C 2-6Alkynyl, they can be optional substituted arbitrarily;

  • Perhaps R1 is, Q wherein is 0 or 1, and Y is-(CH 2) m-, m wherein is 0 to 5 integer, perhaps Y is-(CH 2) n-Z-(CH 2) p-, n wherein is 0 to 2 integer, and p is 0 to 2 integer, and Z is heteroatoms (optional being substituted), CH wherein 2Group can be optional substituted;

    Perhaps R 1Be TMSIM N imidazole base, N-pyrryl, H, halo, HO-, CF 3SO 2O-, C 1-6Alkyl-O-, C 1-6Alkyl-S, C 1-6Alkyl-S (O)-, C 1-6Alkyl-S (O 2)-, C 1-6Alkyl-CO-, C 1-6Alkyl-CH (OH)-, NC-, HCC-, C 6H 5CC-, 2 '"'"'-furyl, 3 '"'"'-furyl, 2 '"'"'-thienyl, 3 '"'"'-thienyl, 2 '"'"'-pyridyl, 3 '"'"'-pyridyl, 4 '"'"'-pyridyl, 2 '"'"'-thiazolyl, 2 '"'"'-N-methylimidazolyl, 5 '"'"'-pyrimidyl, C 6H 5-, H 2C=CH-, C 1-6Alkyl or MeC (=CH 2)-;

    R 12Be H or halo;

    Perhaps R 1And R 12Unite and form a ring W wherein is CH 2, CH, NH, N, O or S, R 4Be H or C 1-6Alkyl;

    X is O or NOR 5, R wherein 5Be H or C 1-6Alkyl, C 3-8Cycloalkyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 6-12Aryl or heteroaryl, they can be optional substituted arbitrarily;

    Perhaps X be (H, H), (H, OH), (H, OSi (C 1-6Alkyl)

         3) or (H, OCOR 5), R wherein 5Be C 1-6Alkyl, C 3-8Cycloalkyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 6-12Aryl, aralkyl, arylalkenyl, sweet-smelling alkynyl, heteroaryl, heteroaralkyl, impure aromatic ene base or hetaryne base, they can be optional substituted arbitrarily;

    Perhaps X is, Y wherein is-(CH 2) m-, m wherein is 0 to 3 integer, perhaps Y is-(CH 2) n-Z-(CH 2) p-, n wherein is 0 to 2 integer, and p is 0 to 2 integer, and Z is heteroatoms (optional being substituted), and perhaps Z is by one or two C 1-6The carbon atom that alkyl replaces;

    R 6Be H, C 1-6Alkyl or halogen;

    R 7Be H, C 1-6Alkyl, C 2-6Thiazolinyl, C 2-6Alkynyl, C 3-8Cycloalkyl, C 6-12Aryl, aralkyl, arylalkenyl, sweet-smelling alkynyl, heteroaryl, heteroaralkyl, impure aromatic ene base or hetaryne base, they can be optional substituted arbitrarily, R 7Or CN, COOR 10Or CONHR 10, R wherein 10Be H, C 1-18Alkyl, C 2-18Thiazolinyl, C 2-18Alkynyl, C 3-8Cycloalkyl, C 6-12Aryl, aralkyl, arylalkenyl, sweet-smelling alkynyl, heteroaryl, heteroaralkyl, impure aromatic ene base or hetaryne base, they can be optional substituted arbitrarily;

    S is 0 or 1;

    R 8And R 9Be H, C independently of one another 1-6Alkyl, C 2-6Thiazolinyl or C 2-6Alkynyl, R 10CO, OR 11, they can be optional substituted arbitrarily, R wherein 10Be H, C 1-18Alkyl, C 2-18Thiazolinyl, C 2-18Alkynyl, C 3-8Cycloalkyl, C 6-12Aryl, aralkyl, arylalkenyl, sweet-smelling alkynyl, heteroaryl, heteroaralkyl, impure aromatic ene base or hetaryne base, they can be optional substituted arbitrarily, R wherein 11Be H, C 1-6Alkyl, Si (C 1-6Alkyl) 3,2 '"'"'-THP trtrahydropyranyl or R 10CO, R wherein 10Be as defined above, Wherein when s is 0, R 8Also can be O-, R 9Be=CH 2Or=C (H, C 1-6Alkyl) ,=C (H, aryl) or=C (C 1-6Alkyl) 2, be connected to the nitrogen positively charged on the 17-position;

    And pharmacy acceptable salt.

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