Back to results
US 7,410,951 B2Granted
Biologically active peptides and compositions, their use
AssigneeThe University of British Columbia
InventorsRaymond Andersen, John Coleman, Dilip De Silva, Fangming Kong, Edward Piers, Debra Wallace, Michel Roberge, Theresa Allen
Life of this patent
Estimating the term…
Abstract
Derivatives of hemiasterlin or Geodiamolide G having anti-mitotic activities and useful in treating cancer. These derivatives are represented by formula I wherein Y, n, R1, R2, R3, R7, R70, R71, R72, R74, and R75 are as defined in the specification.
Claims11
A compound of general formula I
- wherein:
- R1, R2, and R70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group, wherein the alkyl or acyl group has up to 8 carbon atoms, and wherein the optional substituents are selected from the group consisting of halogen atoms and nitro, cyano, alkoxy, hydroxy, amino, alkylamino, sulfinyl, alkylsulfinyl, sulfonyl, alkylsulfonyl, amido, alkylamido, alkylcarbonyl, haloalkoxycarbonyl, and haloalkyl groups;
- Y represents an optional substituent;
- n represents 0, 1, 2, 3, or 4;
- R3 represents a hydrogen atom, or an optionally substituted alkyl group;
- R74 represents a hydrogen atom, a hydroxy group or an optionally substituted alkyl or acyl group;
- R7 represents a hydrogen atom or an alkyl group;
- R75 represents an optionally substituted alkyl group up to 6 carbon atoms;
- and
- i) R71 represents a hydrogen atom or an optionally substituted alkyl or acyl group;
- and R72 represents a hydrogen atom;
- or
- ii) R71 and R72 each represent radicals so that a double bond is formed between the carbon atoms to which they are attached.
10 more elements
A compound of general formula I
- wherein:
- R1, R2, and R70 independently represent a hydrogen atom or an optionally substituted alkyl or acyl group, wherein the alkyl or acyl group has up to 8 carbon atoms, and wherein the optional substituents are selected from the group consisting of halogen atoms and nitro, cyano, alkoxy, hydroxy, amino, alkylamino, sulfinyl, alkylsulfinyl, sulfonyl, alkylsulfonyl, amido, alkylamido, alkylcarbonyl, haloalkoxycarbonyl, and haloalkyl groups;
- Y represents an optional substituent;
- n represents 0, 1, 2, 3, or 4;
- R3 represents a hydrogen atom, or an optionally substituted alkyl group;
- R74 represents a hydrogen atom, a hydroxy group or an optionally substituted alkyl or acyl group;
- R7 represents a hydrogen atom or an alkyl group;
- R75 represents a group of general formula II:
- wherein Q represents an optionally substituted —CH2—, CH2CH2—, —CH2CH2CH2—, —CH2CHCH—, —CH2C≡C—, or phenylene moiety;
- and
- X represents a group —OR8, —SR8, or —NR9R10, wherein R8 independently represents a hydrogen atom or an optionally substituted alkyl group, and R9 and R10 independently represent a hydrogen atom or an optionally substituted alkyl group having up to 8 carbon atoms;
- and
- i) R71 represents a hydrogen atom or an optionally substituted alkyl or acyl group;
- and R72 represents a hydrogen atom;
- or
- ii) R71 and R72 each represent radicals so that a double bond is formed between the carbon atoms to which they are attached.
13 more elements
A compound of general formula I
- wherein
- R1 represents a hydrogen atom;
- R2 represents a hydrogen atom, or an alkyl group, or an acyl group;
- R3 represents a hydrogen atom, or an optionally substituted alkyl group;
- Y represents an optional substituent;
- n represents 0;
- R70 and R71 independently represent a hydrogen atom or an optionally substituted alkyl group;
- R72 and R74 represent hydrogen atoms;
- R74 represents an optionally substituted alkyl or acyl group;
- R7 represents a hydrogen atom or an alkyl group;
- R75 represents a group of general formula III,
- wherein
- R4 represents a hydrogen atom, or an optionally substituted alkyl group;
- R5 represents a hydrogen atom or an alkyl group;
- R76 and R77 each represent a hydrogen atom or a radical so that a double bond is formed between the carbon atoms to which they are attached;
- and
- X represents a group —OR8 or a group —NR9R10,
- wherein
- R8, R9 and R10 independently represent a hydrogen atom or an optionally substituted alkyl group.
16 more elements
A compound of general formula I
- wherein
- R1 represents a hydrogen atom or an alkyl group;
- R2 represents an acyl group;
- R3 represents a hydrogen atom, or an optionally substituted alkyl group;
- Y represents an optional substituent;
- n represents 0;
- R70 and R71 independently represent a hydrogen atom or an optionally substituted alkyl group;
- R72 and R74 represent hydrogen atoms;
- R74 represents an optionally substituted alkyl or acyl group;
- R7 represents a hydrogen atom or an alkyl group;
- R75 represents a group of general formula III,
- wherein
- R4 represents a hydrogen atom, or an optionally substituted alkyl group;
- R5 represents a hydrogen atom or an alkyl group;
- R76 and R77 each represent a hydrogen atom or a radical so that a double bond is formed between the carbon atoms to which they are attached;
- and
- X represents a group —OR8 or a group —NR9R10, wherein
- R8, R9 and R10 independently represent a hydrogen atom or an optionally substituted alkyl group.
15 more elements
Dependencies are inferred from the claim text.