CO6640209A2 - Heteroaril-ciclohexil-tetraazabenzo[e]azulenos como antagonistas del receptor v1a de la vasopresina - Google Patents

Heteroaril-ciclohexil-tetraazabenzo[e]azulenos como antagonistas del receptor v1a de la vasopresina

Info

Publication number
CO6640209A2
CO6640209A2 CO12165814A CO12165814A CO6640209A2 CO 6640209 A2 CO6640209 A2 CO 6640209A2 CO 12165814 A CO12165814 A CO 12165814A CO 12165814 A CO12165814 A CO 12165814A CO 6640209 A2 CO6640209 A2 CO 6640209A2
Authority
CO
Colombia
Prior art keywords
heteroaryl
receptor antagonists
tetraazabenzo
azulenes
vasopressin
Prior art date
Application number
CO12165814A
Other languages
English (en)
Inventor
Cosimo Dolente
Patrick Schnider
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CO6640209A2 publication Critical patent/CO6640209A2/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • 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
    • A61P15/10—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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
    • A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

La presente invención se refiere a heteroaril-ciclo-hexiltetraazabenzo[e]azulenos de la fórmula Ien la que R, Ry Rtienen los significados aquí descritos.Los compuestos de la invención actúan como moduladores del receptor de la V1a y en particular como antagonistas del receptor de la V1a; la invención se refiere además a su obtención, a las composiciones farmacéuticas que los contienen y al uso de los mismos como medicamentos. Los compuestos activos de la presente invención son útiles como agentes terapéuticos que actúan a nivel periférico y central en los estados patológicos tales como la dismenorrea, disfunción sexual masculina o femenina, hipertensión, fallo cardíaco crónico, secreción inapropiada de vasopresina, cirrosis hepática, síndrome nefrótico, ansiedad, trastornos depresivos, trastorno obsesivo-compulsivo, trastornos del espectro autista, esquizofrenia y conducta agresiva.
CO12165814A 2010-04-21 2012-09-24 Heteroaril-ciclohexil-tetraazabenzo[e]azulenos como antagonistas del receptor v1a de la vasopresina CO6640209A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10160643 2010-04-21

Publications (1)

Publication Number Publication Date
CO6640209A2 true CO6640209A2 (es) 2013-03-22

Family

ID=43919925

Family Applications (1)

Application Number Title Priority Date Filing Date
CO12165814A CO6640209A2 (es) 2010-04-21 2012-09-24 Heteroaril-ciclohexil-tetraazabenzo[e]azulenos como antagonistas del receptor v1a de la vasopresina

Country Status (35)

Country Link
US (1) US8492376B2 (es)
EP (1) EP2560975B1 (es)
JP (1) JP5579923B2 (es)
KR (1) KR101506776B1 (es)
CN (1) CN102858776B (es)
AR (1) AR080927A1 (es)
AU (1) AU2011244407B2 (es)
BR (1) BR112012026890A2 (es)
CA (1) CA2795526A1 (es)
CL (1) CL2012002905A1 (es)
CO (1) CO6640209A2 (es)
CR (1) CR20120513A (es)
CY (1) CY1116661T1 (es)
DK (1) DK2560975T3 (es)
EA (1) EA021418B1 (es)
EC (1) ECSP12012210A (es)
ES (1) ES2542953T3 (es)
HK (1) HK1176609A1 (es)
HR (1) HRP20150929T1 (es)
HU (1) HUE026538T2 (es)
IL (1) IL222403A (es)
MA (1) MA34174B1 (es)
MX (1) MX2012012046A (es)
MY (1) MY160457A (es)
NZ (1) NZ602627A (es)
PE (2) PE20130190A1 (es)
PL (1) PL2560975T3 (es)
PT (1) PT2560975E (es)
RS (1) RS54121B1 (es)
SG (1) SG184534A1 (es)
SI (1) SI2560975T1 (es)
TW (1) TWI419890B (es)
UA (1) UA109543C2 (es)
WO (1) WO2011131596A1 (es)
ZA (1) ZA201207689B (es)

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CN116194441A (zh) * 2020-07-23 2023-05-30 豪夫迈·罗氏有限公司 作为加压素受体v1 a拮抗剂的环己基取代的三唑
CN116234801A (zh) * 2020-07-23 2023-06-06 豪夫迈·罗氏有限公司 作为加压素受体v1 a拮抗剂的杂芳基-甲基取代的三唑
TWI804119B (zh) * 2020-12-21 2023-06-01 大陸商上海濟煜醫藥科技有限公司 三氮唑類三并環衍生物及其製備方法和應用
CN116836111A (zh) * 2023-09-01 2023-10-03 峰成医药科技(天津)有限公司 一种氟代吡啶的连续化合成方法

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Publication number Publication date
AR080927A1 (es) 2012-05-16
HRP20150929T1 (hr) 2015-10-09
EA201291092A1 (ru) 2013-04-30
ZA201207689B (en) 2015-06-24
AU2011244407A1 (en) 2012-10-18
HUE026538T2 (en) 2016-06-28
KR101506776B1 (ko) 2015-03-27
SG184534A1 (en) 2012-11-29
US20110263578A1 (en) 2011-10-27
HK1176609A1 (zh) 2013-08-02
ES2542953T3 (es) 2015-08-13
EP2560975B1 (en) 2015-06-17
UA109543C2 (xx) 2015-09-10
IL222403A (en) 2014-08-31
BR112012026890A2 (pt) 2016-07-19
TWI419890B (zh) 2013-12-21
CY1116661T1 (el) 2017-03-15
WO2011131596A1 (en) 2011-10-27
CA2795526A1 (en) 2011-10-27
MY160457A (en) 2017-03-15
DK2560975T3 (en) 2015-06-29
MA34174B1 (fr) 2013-04-03
EA021418B1 (ru) 2015-06-30
US8492376B2 (en) 2013-07-23
JP5579923B2 (ja) 2014-08-27
PT2560975E (pt) 2015-08-28
EP2560975A1 (en) 2013-02-27
PE20130190A1 (es) 2013-02-21
CN102858776B (zh) 2016-01-20
PL2560975T3 (pl) 2015-11-30
MX2012012046A (es) 2012-11-22
CL2012002905A1 (es) 2013-03-22
SI2560975T1 (sl) 2015-08-31
PE20160589A1 (es) 2016-06-11
NZ602627A (en) 2013-07-26
CR20120513A (es) 2012-11-01
RS54121B1 (en) 2015-12-31
KR20130008619A (ko) 2013-01-22
JP2013525319A (ja) 2013-06-20
ECSP12012210A (es) 2012-10-30
TW201139444A (en) 2011-11-16
CN102858776A (zh) 2013-01-02
AU2011244407B2 (en) 2013-06-13

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