ECSP992915A - PYRAZOLOPIRIMIDINONAS INHIBITORS OF GMPc PDES FOR THE TREATMENT OF SEXUAL DYSFUNCTION - Google Patents
PYRAZOLOPIRIMIDINONAS INHIBITORS OF GMPc PDES FOR THE TREATMENT OF SEXUAL DYSFUNCTIONInfo
- Publication number
- ECSP992915A ECSP992915A ECSP992915A ECSP992915A EC SP992915 A ECSP992915 A EC SP992915A EC SP992915 A ECSP992915 A EC SP992915A EC SP992915 A ECSP992915 A EC SP992915A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkyl
- optionally substituted
- treatment
- sexual dysfunction
- inhibitors
- Prior art date
Links
- 101150085511 PEDS1 gene Proteins 0.000 title 1
- 102100037592 Plasmanylethanolamine desaturase Human genes 0.000 title 1
- 201000001880 Sexual dysfunction Diseases 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 229920003199 poly(diethylsiloxane) Polymers 0.000 title 1
- 231100000872 sexual dysfunction Toxicity 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 206010057671 Female sexual dysfunction Diseases 0.000 abstract 2
- NYHBQMYGNKIUIF-UUOKFMHZSA-N Guanosine Chemical compound C1=NC=2C(=O)NC(N)=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NYHBQMYGNKIUIF-UUOKFMHZSA-N 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 abstract 1
- MIKUYHXYGGJMLM-GIMIYPNGSA-N Crotonoside Natural products C1=NC2=C(N)NC(=O)N=C2N1[C@H]1O[C@@H](CO)[C@H](O)[C@@H]1O MIKUYHXYGGJMLM-GIMIYPNGSA-N 0.000 abstract 1
- 101710111837 Cyclic phosphodiesterase Proteins 0.000 abstract 1
- NYHBQMYGNKIUIF-UHFFFAOYSA-N D-guanosine Natural products C1=2NC(N)=NC(=O)C=2N=CN1C1OC(CO)C(O)C1O NYHBQMYGNKIUIF-UHFFFAOYSA-N 0.000 abstract 1
- 101100189582 Dictyostelium discoideum pdeD gene Proteins 0.000 abstract 1
- 208000010228 Erectile Dysfunction Diseases 0.000 abstract 1
- 101150098694 PDE5A gene Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 102100029175 cGMP-specific 3',5'-cyclic phosphodiesterase Human genes 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229940029575 guanosine Drugs 0.000 abstract 1
- 125000004438 haloalkoxy group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 201000001881 impotence Diseases 0.000 abstract 1
- 150000004712 monophosphates Chemical class 0.000 abstract 1
- 125000002757 morpholinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se refiere a los compuestos de las fórmulas (IA) o (IB) (gráfico), en las que R1 es alquilo C4 a C3 opcionalmente sustituido con fenilo, Het o un grupo heterociclico unido a N seleccionado entre piperidinilo y morfolinilo; donde dicho grupo fenilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre alcoxi C1 a C4; halo; CN; CF3, OCF3 o alquilo C1 a C4, donde dicho grupo alquilo C1 a C4 está opcionalmente sustituido con haloalquilo o haloalcoxi C1 a C4, estando cualquiera de ellos sustituido con uno o mas átomos de halo; R2 es alquilo C1 a C6 y R13 es OR3 o NR5R6, las sales farmacéutica o veterinariamente aceptables de los mismos, o los solvatos farmacéutica o veterinariamente aceptables de cualquier entidad, son inhibidores potentes selectivos de la guanosina 3¿,5¿monofosfato cíclica fosfodiesterasa de tipo 5 (GMPc PDE5) y tienen utilidad en el tratamiento de, entre otros, la disfunción eréctil en machos (MED) y la disfunción sexualde hembas (FSD).The present invention relates to compounds of formulas (IA) or (IB) (graph), wherein R1 is C4 to C3 alkyl optionally substituted with phenyl, Het or an N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted with one or more substituents selected from C1 to C4 alkoxy; halo; CN; CF3, OCF3 or C1 to C4 alkyl, wherein said C1 to C4 alkyl group is optionally substituted with haloalkyl or C1 to C4 haloalkoxy, any of them being substituted with one or more halo atoms; R2 is C1 to C6 alkyl and R13 is OR3 or NR5R6, the pharmaceutically or veterinarily acceptable salts thereof, or the pharmaceutically or veterinarily acceptable solvates of any entity, are potent selective inhibitors of guanosine 3¿, 5¿ cyclic phosphodiesterase monophosphate type 5 (cGMP PDE5) and are useful in the treatment of, among others, male erectile dysfunction (MED) and female sexual dysfunction (FSD).
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP992915 ECSP992915A (en) | 1999-04-09 | 1999-04-09 | PYRAZOLOPIRIMIDINONAS INHIBITORS OF GMPc PDES FOR THE TREATMENT OF SEXUAL DYSFUNCTION |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ECSP992915 ECSP992915A (en) | 1999-04-09 | 1999-04-09 | PYRAZOLOPIRIMIDINONAS INHIBITORS OF GMPc PDES FOR THE TREATMENT OF SEXUAL DYSFUNCTION |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP992915A true ECSP992915A (en) | 1999-06-11 |
Family
ID=42043905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP992915 ECSP992915A (en) | 1999-04-09 | 1999-04-09 | PYRAZOLOPIRIMIDINONAS INHIBITORS OF GMPc PDES FOR THE TREATMENT OF SEXUAL DYSFUNCTION |
Country Status (1)
| Country | Link |
|---|---|
| EC (1) | ECSP992915A (en) |
-
1999
- 1999-04-09 EC ECSP992915 patent/ECSP992915A/en unknown
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