ECSP066647A - TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS - Google Patents

TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS

Info

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
Authority
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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06—Antiabortive agents; Labour repressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)

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

Publications (1)

Publication Number Publication Date
ECSP066647A true ECSP066647A (en) 2006-10-25

Family

ID=34740750

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2006006647A ECSP066647A (en) 2003-12-22 2006-06-15 TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS

Country Status (24)

Country Link
EP (1) EP1701959A1 (en)
JP (1) JP4698604B2 (en)
KR (1) KR100854872B1 (en)
AP (1) AP2331A (en)
AR (1) AR047340A1 (en)
AU (1) AU2004309164B2 (en)
BR (1) BRPI0417267A (en)
CA (1) CA2551038C (en)
CR (1) CR8481A (en)
DO (1) DOP2004001062A (en)
EA (1) EA010132B1 (en)
EC (1) ECSP066647A (en)
GE (1) GEP20084571B (en)
IL (1) IL176349A (en)
IS (1) IS8472A (en)
MA (1) MA28393B1 (en)
NL (1) NL1027833C2 (en)
NO (1) NO20063380L (en)
OA (1) OA13347A (en)
PA (1) PA8620501A1 (en)
PE (1) PE20051051A1 (en)
TW (1) TWI287541B (en)
UY (1) UY28693A1 (en)
WO (1) WO2005063754A1 (en)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2566094A1 (en) 2004-05-26 2005-12-08 Eisai R & D Management Co., Ltd. Cinnamide compound
MX2007003327A (en) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase.
TW200626138A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
AR051026A1 (en) 2004-09-20 2006-12-13 Xenon Pharmaceuticals Inc HETEROCICLIC DERIVATIVES AND THEIR USE AS INHIBITORS OF ESTEAROIL-COA DESATURASA
WO2006034341A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
US8071603B2 (en) 2004-09-20 2011-12-06 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
BRPI0515482A (en) 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc heterocyclic derivatives and their uses as therapeutic agents
CA2580855A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
AU2005297966B2 (en) 2004-10-26 2010-12-23 Eisai R & D Management Co., Ltd. Amorphous object of cinnamide compound
AP2007004047A0 (en) 2005-01-20 2007-06-30 Pfizer Ltd Substituted triazole derivatives as oxtocin antagonists
US8541457B2 (en) 2005-06-03 2013-09-24 Xenon Pharmaceuticals Inc. Aminothiazole derivatives as human stearoyl-CoA desaturase inhibitors
CN102295636A (en) * 2005-07-29 2011-12-28 弗·哈夫曼-拉罗切有限公司 Indol-3-y-carbonyl-piperidin and piperazin-derivatives
TWI370130B (en) 2005-11-24 2012-08-11 Eisai R&D Man Co Ltd Two cyclic cinnamide compound
TWI378091B (en) 2006-03-09 2012-12-01 Eisai R&D Man Co Ltd Multi-cyclic cinnamide derivatives
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
US9090604B2 (en) 2006-07-27 2015-07-28 E I Du Pont De Nemours And Company Fungicidal azocyclic amides
US7737141B2 (en) 2006-07-28 2010-06-15 Eisai R&D Management Co., Ltd. Prodrug of cinnamide compound
ATE469899T1 (en) * 2006-12-07 2010-06-15 Hoffmann La Roche SPIROPIPERIDINE DERIVATIVES
KR101050568B1 (en) 2006-12-07 2011-07-19 에프. 호프만-라 로슈 아게 Spiro-piperidine Derivatives as VII1 Receptor Antagonists
US7495008B2 (en) * 2006-12-22 2009-02-24 Hoffmann-La Roche Inc. Spiro-piperidine derivatives
DK2125827T3 (en) * 2006-12-29 2010-12-20 Hoffmann La Roche Azaspiro derivatives
CL2008000582A1 (en) 2007-02-28 2008-06-27 Eisai R&D Man Co Ltd CYCLE COMPOUNDS DERIVED FROM CONDENSED OXIMORPHOLINE; PHARMACES THAT INCLUDE SUCH COMPOUNDS; AND ITS USE TO TREAT ALZHEIMER'S DISEASE, SENILE DEMENTIA, DOWN SYNDROME OR AMYLOIDOSIS.
CA2694401C (en) 2007-08-31 2012-12-04 Eisai R&D Management Co., Ltd. Polycyclic compound
US7935815B2 (en) 2007-08-31 2011-05-03 Eisai R&D Management Co., Ltd. Imidazoyl pyridine compounds and salts thereof
WO2010051245A1 (en) 2008-11-03 2010-05-06 Merck Sharp & Dohme Corp. Benzimidazole and aza-benzimidazole carboxamides
EP2623499B1 (en) * 2010-10-01 2015-04-22 Taisho Pharmaceutical Co., Ltd 1,2,4-triazolone derivative
KR102243637B1 (en) 2013-03-14 2021-04-26 리커리엄 아이피 홀딩스, 엘엘씨 Bicyclic analgesic compounds
EP3080072A4 (en) 2013-12-12 2017-07-19 Kalyra Pharmaceuticals, inc. Bicyclic alkyl compounds and synthesis
WO2015134710A1 (en) 2014-03-07 2015-09-11 Kalyra Pharmaceuticals, Inc. Propellane derivates and synthesis
WO2016044331A1 (en) 2014-09-17 2016-03-24 Kalyra Pharmaceuticals, Inc. Bicyclic compounds
ES2712886T3 (en) 2014-09-24 2019-05-16 Bayer Pharma AG Derivatives of pyridobenzazepine and pyridobenzazocine that inhibit factor XIa
EA032137B1 (en) * 2014-11-03 2019-04-30 Байер Фарма Акциенгезельшафт Hydroxyalkyl-substituted phenyltriazole derivatives and uses thereof
RU2637101C2 (en) * 2016-01-11 2017-11-29 Федеральное государственное бюджетное научное учреждение "Федеральный исследовательский центр вирусологии и микробиологии" (ФГБНУ ФИЦВиМ) Device for determination of aspired dose of aerosols
US20190308956A1 (en) * 2016-02-23 2019-10-10 Servicio Andaluz De Salud Piperazine derivatives as antiviral agents with increased therapeutic activity
WO2017191105A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft Amide-substituted aryltriazole derivatives and uses thereof
EP3452472A1 (en) 2016-05-03 2019-03-13 Bayer Aktiengesellschaft Hydroxyalkyl-substituted heteroaryltriazole derivatives and uses thereof
US10815205B2 (en) 2016-05-03 2020-10-27 Bayer Pharma Aktiengesellschaft Amide-substituted phenyltriazole derivatives and uses thereof
CN109071464A (en) 2016-05-03 2018-12-21 拜耳制药股份公司 The Phenyltriazole derivatives and application thereof that oxoalkyl group replaces
US9988367B2 (en) 2016-05-03 2018-06-05 Bayer Pharma Aktiengesellschaft Amide-substituted pyridinyltriazole derivatives and uses thereof
WO2017191112A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft Fluoroalkyl-substituted aryltriazole derivatives and uses thereof
EP3456716A4 (en) * 2016-05-09 2019-11-06 Nippon Soda Co., Ltd. CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT
US10927098B2 (en) 2016-10-20 2021-02-23 Bayer Pharma Aktiengesellschaft Hydroxyalkyl-substituted triazole derivatives and uses thereof
MX389668B (en) 2017-05-15 2025-03-20 Recurium Ip Holdings Llc Analgesic compounds
WO2019081306A1 (en) 2017-10-24 2019-05-02 Bayer Pharma Aktiengesellschaft Substituted triazole derivatives and uses thereof
EP3700896A1 (en) 2017-10-24 2020-09-02 Bayer Pharma Aktiengesellschaft Amine substituted triazole derivatives and uses thereof
WO2019081303A1 (en) 2017-10-24 2019-05-02 Bayer Pharma Aktiengesellschaft Substituted triazole derivatives and uses thereof
WO2019081291A1 (en) 2017-10-24 2019-05-02 Bayer Aktiengesellschaft Prodrugs of substituted triazole derivatives and uses thereof
EP3700897A1 (en) 2017-10-24 2020-09-02 Bayer Pharma Aktiengesellschaft Substituted triazole derivatives and uses thereof
CA3084308A1 (en) 2017-10-24 2019-05-02 Bayer Aktiengesellschaft Substituted triazole derivatives and uses thereof
KR20200069361A (en) 2017-10-24 2020-06-16 바이엘 악티엔게젤샤프트 Prodrugs of substituted triazole derivatives and uses thereof
TW201938171A (en) 2017-12-15 2019-10-01 匈牙利商羅特格登公司 Tricyclic compounds as vasopressin V1a receptor antagonists
HU231206B1 (en) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepines
NZ790364A (en) * 2020-01-29 2025-12-19 Kamari Pharma Ltd Compounds and compositions for use in treating skin disorders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4481360A (en) * 1983-08-26 1984-11-06 The Upjohn Company 4H-1,2,4-Triazol-3-yl compounds
AU2000223275A1 (en) * 2000-02-08 2001-08-20 Yamanouchi Pharmaceutical Co..Ltd. Novel triazole derivatives
JP3873746B2 (en) * 2000-05-19 2007-01-24 アステラス製薬株式会社 Triazole derivative

Also Published As

Publication number Publication date
EA200600925A1 (en) 2006-12-29
KR100854872B1 (en) 2008-08-28
JP2007515468A (en) 2007-06-14
PE20051051A1 (en) 2005-12-17
BRPI0417267A (en) 2007-04-17
DOP2004001062A (en) 2005-06-30
TW200528099A (en) 2005-09-01
IL176349A0 (en) 2006-10-05
KR20060101546A (en) 2006-09-25
AR047340A1 (en) 2006-01-18
NO20063380L (en) 2006-09-22
WO2005063754A1 (en) 2005-07-14
UY28693A1 (en) 2005-07-29
EP1701959A1 (en) 2006-09-20
CR8481A (en) 2007-12-04
AP2006003631A0 (en) 2006-06-30
AU2004309164B2 (en) 2007-11-15
OA13347A (en) 2007-04-13
CA2551038A1 (en) 2005-07-14
JP4698604B2 (en) 2011-06-08
NL1027833C2 (en) 2006-03-06
AP2331A (en) 2011-12-05
GEP20084571B (en) 2008-12-25
EA010132B1 (en) 2008-06-30
IS8472A (en) 2006-05-18
CA2551038C (en) 2010-04-27
IL176349A (en) 2011-11-30
PA8620501A1 (en) 2005-08-04
MA28393B1 (en) 2007-01-02
HK1095822A1 (en) 2007-07-06
NL1027833A1 (en) 2005-06-23
TWI287541B (en) 2007-10-01
AU2004309164A1 (en) 2005-07-14

Similar Documents

Publication Publication Date Title
ECSP066647A (en) TRIAZOL DERIVATIVES AS VASOPRESINE ANTAGONISTS
AR030762A1 (en) PYRIDINILAMIDS AND IMIDES TO USE AS FUNGICIDES
CO5031253A1 (en) RECEIVING ANTAGONISTS Y5 OF NEUROPEPTIDES PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
CO6321130A2 (en) PIRIDINES CARBOXAMIDS AS INHIBITORS OF THE 11 BETA-HSD1
CO5590957A2 (en) AMINO-1,3,5-TRIAZINES REPLACED IN N WITH CHIRAL BICYCLE RADICALS, PROCEDURE FOR PREPARATION, COMPOSITIONS OF THE SAME AND ITS USE AS HERBICIDES AND REGULATORS OF GROWTH OF PLANTS
NO20052469L (en) Inhibitors of II-beta-hydroxysteroid dehydrogenase type 1 and type 2.
AR046297A1 (en) DPP INHIBITORS - IV METHODS TO PREPARE THEM AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AS ACTIVE AGENTS
CO4950557A1 (en) COMPOUNDS AND METHODS
AR046711A1 (en) 5-7-DIAMINOPIRAZOLO [4,3D] PYRIMIDINS AS INHIBITORS OF THE PDE-5, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES IN THE TREATMENT OF HYPERTENSIONS
AR074435A1 (en) DERIVATIVES OF 1,3-BENZOTIAZOL, DRUGS THAT CONTAIN THEM AND USE OF THE SAME IN THE TREATMENT OF CANCER.
PE20080524A1 (en) DERIVATIVES OF 1H-IMIDAZO [4,5-b] PIRAZIN AND THE PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM
AR053120A1 (en) AMINOPIRIDINS AS INHIBITORS OF BETA SECRETASA
AR040870A1 (en) INHIBITING COMPOUNDS OF PROTEINQUINASES AND PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS THEM
ES2116583T3 (en) AZACICLIC COMPOUNDS, COMPOSITIONS CONTAINING THEM AND THEIR USE AS TACHYCIN ANTAGONISTS.
PA8607001A1 (en) DERIVATIVES OF TRIAZOLOPIRIMIDINS AS INHIBITORS OF GLUCOGENO SINTASA QUINASA 3
ES2196772T3 (en) AMINO CYCLES COMPOUNDS.
NO20062633L (en) Pyrazole derivatives as protein kinase modulators
CR9980A (en) IMIDAZOLINS 4,4,5,5 TETRASUSTITUIDAS
EA200970493A1 (en) MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
PE20110405A1 (en) PYRIDINE-PYRIDINONE DERIVATIVES AS INHIBITORS OF THE ACTIVITY OF PDGF-R AND / OR FLT-3 TYROSINE KINASE AND THEIR PREPARATION
PE54294A1 (en) DERIVATIVE OF 5-AMINOALKYL-1,4-BENZODIAZEPINE
CY1116183T1 (en) Piperazinoidions as antagonists of oxytocin receptors
PE20071177A1 (en) 3,5-PYRIDINE DERIVATIVES AS RENIN INHIBITORS
AR065583A1 (en) MACROCICLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITION
PA8573501A1 (en) BENZOXAZINE DERIVATIVES AND THEIR EMPLOYMENT