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US 8,569,348 B2Granted
Compounds, compositions, and methods for preventing metastasis of cancer cells
AssigneeAerpio Therapeutics Inc.
InventorsRobert Shalwitz, Kevin G. Peters
Life of this patent
Estimating the term…
Abstract
Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.
Claims15
A method for rebducing and/or delaying metastasis in a subject, comprising contacting the subject with an effective amount of a compound having the formula:
- wherein R is a substituted or unsubstituted thiazolyl unit having the formula:
- R2, R3, and R4 are each independently:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- iii) substituted or unsubstituted C2-C6 linear, branched, or cyclic alkenyl;
- iv) substituted or unsubstituted C2-C6 linear or branched alkynyl;
- v) substituted or unsubstituted C6 or C10 aryl;
- vi) substituted or unsubstituted C1-C9 heteroaryl;
- vii) substituted or unsubstituted C1-C9 heterocyclic;
- or
- viii) R2 and R3 can be taken together to form a saturated or unsaturated ring having from 5 to 7 atoms;
- wherein from 1 to 3 atoms can optionally be heteroatoms chosen from oxygen, nitrogen, and sulfur;
- Z is a unit having the formula:
- -(L)n-R1
- R1 is chosen from:
- i) hydrogen;
- ii) hydroxyl;
- iii) amino;
- iv) substituted or unsubstituted C1-C6 linear, branched or cyclic alkyl;
- v) substituted or unsubstituted C1-C6 linear, branched or cyclic alkoxy;
- vi) substituted or unsubstituted C6 or C10 aryl;
- vii) substituted or unsubstituted C1-C9 heterocyclic rings;
- or
- viii) substituted or unsubstituted C1-C9 heteroaryl rings;
- L is a linking unit having the formula:
- -[Q]y[C(R5aR5b)]x[Q1]z[C(R6aR6b)]w—
- Q and Q1 are each independently:
- i) —C(O)—;
- ii) —NH—;
- iii) —C(O)NH—;
- iv) —NHC(O)—;
- v) —NHC(O)NH—;
- vi) —NHC(O)O—;
- vii) —C(O)O—;
- viii) —C(O)NHC(O)—;
- ix) —O—;
- x) —S—;
- xi) —SO2—;
- xii) —C(═NH)—;
- xiii) —C(═NH)NH—;
- xiv) —NHC(═NH)—;
- or
- xv) —NHC(═NH)NH—;
- R5a and R5b are each independently:
- i) hydrogen;
- ii) hydroxy;
- iii) halogen;
- iv) C1-C6 substituted or unsubstituted linear or branched alkyl;
- or
- v) a unit having the formula:
- —[C(R7aR7b)]tR8
- R7a and R7b are each independently:
- i) hydrogen;
- or
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- R8 is:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- iii) substituted or unsubstituted C6 or C10 aryl;
- iv) substituted or unsubstituted C1-C9 heteroaryl;
- or
- v) substituted or unsubstituted C1-C9 heterocyclic;
- R6a and R6b are each independently:
- i) hydrogen;
- or
- ii) C1-C4 linear or branched alkyl;
- the index n is 0 or 1;
- the indices t, w and x are each independently from 0 to 4;
- the indices y and z are each independently 0 or 1;
- or
- a pharmaceutically acceptable salt thereof;
- wherein the cancer is malignant melanoma or lung cancer.
69 more elements
A method for reducing and/or delaying metastasis in a subject, comprising contacting the subject with a composition comprising:
- A) an effective amount of one or more compounds having the formula:
- wherein R is a substituted or unsubstituted thiazolyl unit having the formula:
- R2, R3, and R4 are each independently:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- iii) substituted or unsubstituted C2-C6 linear, branched, or cyclic alkenyl;
- iv) substituted or unsubstituted C2-C6 linear or branched alkynyl;
- v) substituted or unsubstituted C6 or C10 aryl;
- vi) substituted or unsubstituted C1-C9 heteroaryl;
- vii) substituted or unsubstituted C1-C9 heterocyclic;
- or
- viii) R2 and R3 can be taken together to form a saturated or unsaturated ring having from 5 to 7 atoms;
- wherein from 1 to 3 atoms can optionally be heteroatoms chosen from oxygen, nitrogen, and sulfur;
- Z is a unit having the formula:
- -(L)n-R1
- R1 is chosen from:
- i) hydrogen;
- ii) hydroxyl;
- iii) amino;
- iv) substituted or unsubstituted C1-C6 linear, branched or cyclic alkyl;
- v) substituted or unsubstituted C1-C6 linear, branched or cyclic alkoxy;
- vi) substituted or unsubstituted C6 or C10 aryl;
- vii) substituted or unsubstituted C1-C9 heterocyclic rings;
- or
- viii) substituted or unsubstituted C1-C9 heteroaryl rings;
- L is a linking unit having the formula:
- -[Q]y[C(R5aR5b)]x[Q1]z[C(R6aR6b)]w—
- Q and Q1 are each independently:
- i) —C(O)—;
- ii) —NH—;
- iii) —C(O)NH—;
- iv) —NHC(O)—;
- v) —NHC(O)NH—;
- vi) —NHC(O)O—;
- vii) —C(O)O—;
- viii) —C(O)NHC(O)—;
- ix) —O—;
- x) —S—;
- xi) —SO2—;
- xii) —C(═NH)—;
- xiii) —C(═NH)NH—;
- xiv) —NHC(═NH)—;
- or
- xv) —NHC(═NH)NH—;
- R5a and R5b are each independently:
- i) hydrogen;
- ii) hydroxy;
- iii) halogen;
- iv) C1-C6 substituted or unsubstituted linear or branched alkyl;
- or
- v) a unit having the formula:
- —[C(R7aR7b)]tR8
- R7a and R7b are each independently:
- i) hydrogen;
- or
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- R8 is:
- i) hydrogen;
- ii) substituted or unsubstituted C1-C6 linear, branched, or cyclic alkyl;
- iii) substituted or unsubstituted C6 or C10 aryl;
- iv) substituted or unsubstituted C1-C9 heteroaryl;
- or
- v) substituted or unsubstituted C1-C9 heterocyclic;
- R6a and R6b are each independently:
- i) hydrogen;
- or
- ii) C1-C4 linear or branched alkyl;
- the index n is 0 or 1;
- the indices t, w and x are each independently from 0 to 4;
- the indices y and z are each independently 0 or 1;
- or
- a pharmaceutically acceptable salt thereof;
- and
- B) an effective amount of one or more chemotherapeutic agents;
- wherein the cancer is malignant melanoma or lung cancer.
72 more elements
Dependencies are inferred from the claim text.