Pin1-modulating compounds and methods of use thereof
AssigneePintex Pharmaceuticals, Inc.
InventorsRobert K. Suto, Timothy D. McKee
Life of this patent
Estimating the term…
Abstract
The invention is directed to modulators, e.g, inhibitors, of Pin1 and Pin1-related proteins and the use of such modulators for treatment of Pin1 associated states, e.g., for the treatment of cancer.
Claims136
A method for treating a Pin1-associated state in a subject comprising administering to said subject an effective amount of a Pin1-modulating compound of formula (I):
- 200
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- such that said Pin1-associated state is treated.
A method for treating cyclin D1 overexpression in a subject comprising administering to said subject an effective amount of a Pin1-modulating compound of formula (I):
- 201
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- such that said cyclin D1 overexpression is treated.
A packaged Pin1-associated state treatment, comprising a Pin1-modulating compound of formula (I):
- 202
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- packaged with instructions for using an effective amount of the Pin1-modulating compound to treat a Pin1-associated state.
A packaged cyclin D1 overexpression treatment, comprising a Pin1-modulating compound of formula (I):
- 203
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- packaged with instructions for using an effective amount of the Pin1-modulating compound to treat cyclin D1 overexpression.
A packaged cancer treatment, comprising a Pin1-modulating compound of formula (I):
- 204
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- packaged with instructions for using an effective amount of the Pin1-modulating compound to treat cancer.
A method for treating a Pin1-associated state in a subject comprising administering to a subject an effective amount of a combination of a Pin1-modulating compound of formula (I):
- 205
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- a hyperplastic inhibitory agent such that the Pin1-associated state is treated.
A method for treating cancer in a subject comprising administering to a subject an effective amount of a combination of a Pin1-modulating compound of formula (I):
- 206
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- a hyperplastic inhibitory agent such that the cancer is treated.
A method for treating cyclin D1 overexpression in a subject comprising administering to a subject an effective amount of a combination of a Pin1-modulating compound of formula (I):
- 207
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof;
- a hyperplastic inhibitory agent such that the cyclin D1 overexpression is treated.
A Pin1-modulator comprising formula (I):
- 208
- wherein
- the dashed lines indicate a single or a double bond;
- n is 0, 1, or 2;
- G1 is CH2, CH, or N;
- G2 and G3 are independently selected from the group consisting of O, OR2, NR2, NR2R6, hydrogen, alkyl, aryl;
- and
- R1, R2, R3, R4, R5, R6 and R7 are each independently substituted or unsubstituted:
- alkyl, alkenyl, alkynyl, aryl, hydrogen, acyl, or any combination thereof.
Dependencies are inferred from the claim text.