Back to results
US 2004/0063643 A1Published application
Bombesin antagonists
AssigneePfizer Inc.
InventorsMichael Higginbottom, Suzanne Ross Kesten, Russell Andrew Lewthwaite, Martyn Clive Pritchard, David James Rawson, Robert Michael Schelkun, Po-Wai Yuen
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I): 1 and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are bombesin antagonists, which have utility in a variety of therapeutic areas including male and female sexual dysfunction, particularly female sexual dysfunction (FSD) especially wherein the FSD is female sexual arousal disorder (FSAD) and male erectile dysfunction (MED)
Claims26
A compound of formula (I):
- 395
- wherein
- R1 is selected from
- a) aryl
- b) aromatic heterocycle
- c) CO2R5
- d) CONR5R6
- e) NR5R7
- f) OR5
- g) C1-6 alkyl
- h) C1-6 cycloalkyl and
- i) —C(O)—N-morpholine
- Wherein group (a) may be optionally substituted by 1-3 groups each independently selected from NR5R5, N(R5)C(O)R5, NO2, halo, OR5, R5 and R4NR5R5;
- and group (b) may be optionally substituted by 1-3 groups each independently selected from halo, R5 and OR5;
- m is 0-2;
- n is 0-2;
- p is 0-2;
- q is 0-2;
- r is 0-4
- Y is NR3 or CHR3;
- R2 is selected from
- a) C3-7 cycloalkyl,
- b) aromatic heterocycle, optionally fused with a phenyl group,
- c) aryl, wherein said aryl group may optionally be fused with a heterocycle or a C3-7 cycloalkyl group, wherein said fused cycloalkyl moiety may also incorporate a C═O group,
- d) Oaryl,
- e) C1-6 alkyl,
- f) Adamantyl, and
- g) C1-6 alkenyl, optionally substituted by 1 or 2 phenyl,
- wherein groups (a), (b), (c), (d) and (e) may be optionally substituted by 1-3 substituents selected from:
- R5, C1-6 alkenyl, aryl, OR4, OR5, OH, CF3, halo, SO2R5, NO2, SR5, CN, OCF3, CO2R5, C(O)R5, Oaryl, OR aryl, R4OR5, C(NH)NR5R5, OC(O)C1-6alkyl and NR5R7;
- R3 is selected from
- a) C1-6 alkyl,
- b) C1-6 alkenyl,
- c) C1-6 alkynyl,
- d) Aromatic heterocycle, optionally fused with phenyl,
- e) Phenyl, optionally fused with phenyl, heterocycle or aromatic heterocycle,
- said groups (a), (b), (c), (d) and (e) optionally substituted by 1-3 groups each independently selected from halo, CN, SR5, heterocycle, aromatic heterocycle, R5, OR7, C(O)NR5R7, SO2NR5R7, NHSO2R5, OH, CF3, OR5, OR5OR5, NR5R7, CO2H, CO2R5, OC(O)R5, C3-7 cycloalkyl group (wherein said cycloalkyl group may optionally be substituted by C1-6 alkyl), CH2OC(O)CH3 and phenyl, wherein said phenyl may optionally be fused with a heterocycle, aromatic heterocycle, phenyl or C3-7 cycloalkyl, said phenyl, fused phenyl, or aromatic heterocycle optionally substituted by 1-3 groups each independently selected from:
- phenyl, R4, CN, OH, OR4Ph, OR4CO2R5, C1-6 alkynyl, R4OC(O)R5, R4SR5, OC(O)R5, CF3, OR7, OR4OR5, CO2R5, OR4, CO2R5, HNC(O)R5, C1-6 alkenyl, OCF3, NO2, halo, HNSO2R5, SO2NR5R5, C(O)NR5R5, C(NH)NR5R5, OR5, OC(O)R4-heterocycle, NR5R7, SR5 and tetrazole;
- R4 is C1-6 alkyl;
- R5 is independently selected from H and C1-6 alkyl, said alkyl groups optionally substituted by 1-3 groups each independently selected from halo or OH;
- R6 is independently selected from H, heterocycle, OC1-6 alkyl, C1-6 alkyl, said alkyl groups optionally substituted by 1-3 groups each independently selected from halo or OH;
- or R5 and R6 can be taken together with the N atom to which they are attached to form a 5, 6 or 7-membered ring optionally containing a further hetero moiety selected from O, NH, or S;
- R7 is selected from H and C1-6 alkyl said alkyl groups optionally substituted by an aryl group;
- and
- R8 and R9 are both independently selected from H or C1-6 alkyl;
- or R8 and R9 may combine to form a 3-7 membered cycloalkyl group. Optionally said cycloalkyl group may incorporate an atom or group selected from NR4, NH, O or S;
- With the proviso that when R is an aryl or aromatic heterocycle group, R2 is a phenyl, pyridyl or pyrimidinyl group, said groups optionally substituted, R8 and R9 combine to form a 3-7 membered cycloalkyl group, Y is NR3 and m, p, q and r are 0;
- then R3 cannot be C4-6 alkyl or C1 alkyl substituted by phenyl, said phenyl group optionally substituted by 1-3 groups each independently selected from halo, OC1-6 alkyl and NR5R7;
- and the pharmaceutically acceptable salts, prodrugs, solvates thereof.
46 more elements
Dependencies are inferred from the claim text.