Cancer Research Technology Limited

Lloyd Royston Kelland

Stephen Neidle

Richard John Harrison

Sharon Michele Gowan

Martin Anthony Read

Anthony Reszka

Malcolm F G Stevens

Robert A Heald

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.

The present invention pertains to certain N,N-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each Ris &#x2014;H or a ring substituent; each Ris &#x2014;H or a ring substituent; each Ris &#x2014;H or a ring substituent; Ris a nitrogen substituent; Ris a nitrogen substituent; and, Q is an anion. 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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Reigate, United Kingdom

Lloyd Royston Kelland