公开(公告)号：US09914719B2

公开(公告)日：2018-03-13

申请号：US14467946

申请日：2014-08-25

Applicant: Astex Therapeutics Ltd.

Inventor： Gianni Chessari ,  Miles Stuart Congreve ,  Martyn Frederickson ,  Christopher William Murray ,  Eva Figueroa Navarro ,  Alison Jo-Anne Woolford ,  Maria Grazia Carr ,  Robert Downham ,  Michael Alistair O'Brien ,  Theresa Rachel Phillips ,  Andrew James Woodhead

IPC: A61K31/454 ,  A61K31/496 ,  A61K31/445 ,  A61K31/4035 ,  C07D401/12 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10 ,  C07C65/21

CPC classification number: C07D401/12 ,  C07C65/21 ,  C07D209/08 ,  C07D209/44 ,  C07D215/08 ,  C07D217/06 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D471/04 ,  C07D471/10 ,  C07D491/08 ,  C07D491/10

Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

公开(公告)号：US09428439B2

公开(公告)日：2016-08-30

申请号：US14149450

申请日：2014-01-07

Applicant: Astex Therapeutics Ltd.

Inventor： Martyn Frederickson ,  John Francis Lyons ,  Neil Thomas Thompson ,  Mladen Vinkovic ,  Brian John Williams ,  Andrew James Woodhead ,  Alison Jo-Anne Woolford

IPC: C07D209/44 ,  C07C67/317 ,  C07C67/313 ,  C07C59/08 ,  C07C69/92 ,  C07C235/60

CPC classification number: C07C67/317 ,  C07C59/08 ,  C07C67/313 ,  C07C69/92 ,  C07C235/60 ,  C07D209/44

Abstract: The invention provides an acid addition salt of a compound of the formula (1). Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogs thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analog.

Abstract translation: 本发明提供式（1）化合物的酸加成盐。 本发明还提供制备式（1）化合物及其烷基类似物的方法，用于该方法的新中间体和制备中间体的方法。 本发明还提供式（1）化合物及其乙基类似物的新的医学用途。