ECSP066647A - TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS - Google Patents

TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS

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Publication number
ECSP066647A
ECSP066647A EC2006006647A ECSP066647A ECSP066647A EC SP066647 A ECSP066647 A EC SP066647A EC 2006006647 A EC2006006647 A EC 2006006647A EC SP066647 A ECSP066647 A EC SP066647A EC SP066647 A ECSP066647 A EC SP066647A
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EC
Ecuador
Prior art keywords
saturated
optionally substituted
heterocyclic ring
ring
number chosen
Prior art date
Application number
EC2006006647A
Other languages
Spanish (es)
Inventor
Patrick Stephen Johnson
Thomas Ryckmans
Lee Richard Roberts
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0329693A external-priority patent/GB0329693D0/en
Priority claimed from GB0408789A external-priority patent/GB0408789D0/en
Application filed by Pfizer filed Critical Pfizer
Publication of ECSP066647A publication Critical patent/ECSP066647A/en

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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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  • Veterinary Medicine (AREA)
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  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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Abstract

Un compuesto de la fórmula (I) consta gráfico o derivados del mismo aceptables farmacéuticamente, en el que:X representa -[CH2]a-R ó -[CH2]a-O-[CH2]b-R; a representa un número elegido entre 0 y 6; b representa un número elegido entre 0 y 6; R representa H, CF3 o Het; Het representa un anillo heterocíclico de 5 ó 6 miembros, saturado, parcialmente saturado o aromático;Y representa uno o más sustituyentes elegidos independientemente entre -[O]c-[CH2]d-R1, que pueden ser iguales o diferentes en cada aparición; c en cada aparición representa independientemente un número elegido entre 0 ó 1; d en cada aparición representa independientemente un número elegido entre 0 y 6; R1 en cada aparición representa independientemente H, halo, CF3, CN o Het1; Het1 en cada aparición representa independientemente un anillo heterocíclico insaturado de 5 ó 6 miembros;V representa un enlace directo ó -O-;el anillo A representa un anillo heterocíclico saturado de 5 a 7 miembros, o un grupo fenileno;Q representa un enlace directo ó -N(R2)-; R2 representa hidrógeno o alquilo C1-C6;Z representa -[O]e-[CH2]f-R3, un anillo de fenilo (opcionalmente fusionado con un anillo de benceno o Het2, y además siendo el grupo en su conjunto opcionalmente sustituido), o Het3 (opcionalmente fusionado con un anillo de benceno o Het4, y además siendo el grupo en su conjunto un grupo opcionalmente sustituido); R3 representa alquilo C1-C6 (opcionalmente sustituido), cicloalquilo C3-C6, cicloalquenilo C3-C6, fenilo (opcionalmente sustituido), Het5 ó NR4R5; e representa un número elegido entre 0 ó 1; f representa un número elegido entre 0 y 6; Het2 y Het5 representan independientemente anillos heterocíclicos saturados, parcialmente saturados o aromáticos, de 5 ó 6 miembros; Het3 representa un anillo heterocíclico saturado, parcialmente saturado o aromático, de 4 a 6 miembros; Het4 representa un anillo heterocíclico aromático de 6 miembros, opcionalmente sustituido; R4 y R5 representan independientemente alquilo C1-C6, alquiloxi C1-C6, cicloalquilo C3-C8 (opcionalmente fusionado con cicloalquilo C3-C8), Het6 ó hidrógeno; Het6 representa un anillo heterocíclico saturado, parcialmente saturado o aromático de 5 ó 6 miembros opcionalmente sustituido;son útiles para tratar un trastorno para el cual está indicado un antagonista de V1a, en particular la dismenorrea.A compound of the formula (I) consists of a graph or pharmaceutically acceptable derivatives thereof, in which: X represents - [CH2] a-R or - [CH2] a-O- [CH2] b-R; a represents a number chosen between 0 and 6; b represents a number chosen between 0 and 6; R represents H, CF3 or Het; Het represents a 5 or 6 membered heterocyclic ring, saturated, partially saturated or aromatic, and represents one or more substituents independently selected from - [O] c- [CH2] d-R1, which may be the same or different at each occurrence; c at each occurrence independently represents a number chosen from 0 or 1; d at each occurrence independently represents a number chosen between 0 and 6; R1 at each occurrence independently represents H, halo, CF3, CN or Het1; Het1 at each occurrence independently represents a 5 or 6-membered unsaturated heterocyclic ring; V represents a direct bond or -O-; ring A represents a 5- to 7-membered saturated heterocyclic ring, or a phenylene group; Q represents a direct bond or -N (R2) -; R2 represents hydrogen or C1-C6 alkyl; Z represents - [O] e- [CH2] f-R3, a phenyl ring (optionally fused with a benzene or Het2 ring, and also being the group as a whole optionally substituted) , or Het3 (optionally fused with a benzene ring or Het4, and the group as a whole being an optionally substituted group); R3 represents C1-C6 alkyl (optionally substituted), C3-C6 cycloalkyl, C3-C6 cycloalkenyl, phenyl (optionally substituted), Het5 or NR4R5; e represents a number chosen from 0 or 1; f represents a number chosen between 0 and 6; Het2 and Het5 independently represent saturated, partially saturated or aromatic, heterocyclic rings of 5 or 6 members; Het3 represents a saturated, partially saturated or aromatic heterocyclic ring of 4 to 6 members; Het4 represents an optionally substituted 6-membered aromatic heterocyclic ring; R4 and R5 independently represent C1-C6 alkyl, C1-C6 alkyloxy, C3-C8 cycloalkyl (optionally fused with C3-C8 cycloalkyl), Het6 or hydrogen; Het6 represents an optionally substituted 5 or 6-membered saturated, partially saturated or aromatic heterocyclic ring; they are useful for treating a disorder for which a V1a antagonist is indicated, in particular dysmenorrhea.

EC2006006647A 2003-12-22 2006-06-15 TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS ECSP066647A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0329693A GB0329693D0 (en) 2003-12-22 2003-12-22 Compounds useful in therapy
GB0408789A GB0408789D0 (en) 2004-04-20 2004-04-20 Triazole derivatives

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ECSP066647A true ECSP066647A (en) 2006-10-25

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EC2006006647A ECSP066647A (en) 2003-12-22 2006-06-15 TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS

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JP (1) JP4698604B2 (en)
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CA (1) CA2551038C (en)
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DO (1) DOP2004001062A (en)
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EC (1) ECSP066647A (en)
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