Cancer Research Technology Limited

Sharon Michele Gowan

Stephen Neidle

Lloyd Royston Kelland

Richard John Harrison

Martin Anthony Read

Anthony Reszka

Anthony Reskza

The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is &#x2550;O, L is &#x2014;H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: Jis a 2- or 3-substituent; Jis a 6- or 7-substituent; Jand Jare each independently a group of the formula &#x2014;NHCO(CH)NRR, wherein: n is an integer from 1 to 5; and, Rand Rare independently hydrogen, Calkyl, Cheterocyclyl, or Caryl, or Rand R, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula &#x2014;N(R)Q, wherein: Ris an amino substituent and is hydrogen, Calkyl, Cheterocyclyl, or Caryl; and, Q is Calkyl, Cheterocyclyl, or Caryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

Therapeutic acridone and acridine compounds

This invention pertains to certain acridone and acridine compounds of the formula which inhibit telomerase, regulate cell proliferation, etc., and/or treat cancer, proliferative conditions, etc.: wherein either: (a) K is &#x2550;O, L is &#x2014;H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: Jis a 2- or 3-substituent; Jis a 6- or 7-substituent; Jand Jare each a group of the formula &#x2014;N(R)&#x2014;W, wherein: Ris a nitrogen substituent and is hydrogen, Calkyl, Cheterocyclyl, or Caryl, and is optionally substituted; and, W is Calkyl, Cheterocyclyl, or Caryl, and is optionally substituted; and, wherein, when K is a 9-substituent, K is a group of the formula &#x2014;N(R)&#x2014;Q, wherein: Ris an amino substituent and is hydrogen, Calkyl, Cheterocyclyl, or Caryl; and, Q is Calkyl, Cheterocyclyl, or Caryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, etc., and/or in the treatment of cancer, proliferative conditions, etc.

The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is &#x2550;O, L is &#x2014;H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: Jis a 2- or 3-substituent; Jis a 6- or 7-substituent; Jand Jare each independently a group of the formula &#x2014;NHCO(CH)NRR, wherein: n is an integer from 1 to 5; and, Rand Rare independently hydrogen, Calkyl, Cheterocyclyl, or Caryl, or Rand R, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula &#x2014;N(R)Q, wherein: Ris an amino substituent and is hydrogen, Calkyl, Cheterocyclyl, or Caryl; and, Q is Calkyl, Cheterocyclyl, or Caryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

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Tolworth, United Kingdom

Sharon Michele Gowan