ECSP12012291A - Heteroaril-ciclohexil-tetraazabenzo[e]azulenos - Google Patents

Heteroaril-ciclohexil-tetraazabenzo[e]azulenos

Info

Publication number
ECSP12012291A
ECSP12012291A ECSP12012291A ECSP12012291A EC SP12012291 A ECSP12012291 A EC SP12012291A EC SP12012291 A ECSP12012291 A EC SP12012291A EC SP12012291 A ECSP12012291 A EC SP12012291A
Authority
EC
Ecuador
Prior art keywords
tetraazabenzo
receptor
relates
present
act
Prior art date
Application number
Other languages
English (en)
Inventor
Patrick Schnider
Cosimo Dolente
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 ECSP12012291A publication Critical patent/ECSP12012291A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic 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
    • A61K31/55131,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/55171,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

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

Abstract

La presente invención se refiere a heteroaril-ciclo-hexil-tetraazabenzo[e]azulenos de la fórmula I en la que R1, R2 y R3 tienen 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 también a su obtención, a composiciones farmacéuticas que los contienen y a su utilización 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.
ECSP12012291 2010-05-10 2012-11-09 Heteroaril-ciclohexil-tetraazabenzo[e]azulenos ECSP12012291A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10162451 2010-05-10

Publications (1)

Publication Number Publication Date
ECSP12012291A true ECSP12012291A (es) 2012-12-28

Family

ID=44080459

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP12012291 ECSP12012291A (es) 2010-05-10 2012-11-09 Heteroaril-ciclohexil-tetraazabenzo[e]azulenos

Country Status (34)

Country Link
US (1) US8513238B2 (es)
EP (1) EP2569319B1 (es)
JP (1) JP5868959B2 (es)
KR (1) KR20130109958A (es)
CN (1) CN102884065B (es)
AR (1) AR081374A1 (es)
AU (1) AU2011252116B2 (es)
BR (1) BR112012028763A2 (es)
CA (1) CA2797920A1 (es)
CL (1) CL2012003132A1 (es)
CO (1) CO6620058A2 (es)
CR (1) CR20120542A (es)
CY (1) CY1115820T1 (es)
DK (1) DK2569319T3 (es)
EA (1) EA021441B1 (es)
EC (1) ECSP12012291A (es)
ES (1) ES2523881T3 (es)
HR (1) HRP20141250T1 (es)
IL (1) IL222815A (es)
MA (1) MA34252B1 (es)
MX (1) MX2012012857A (es)
MY (1) MY160517A (es)
NZ (1) NZ603223A (es)
PE (1) PE20130401A1 (es)
PH (1) PH12012502174A1 (es)
PL (1) PL2569319T3 (es)
PT (1) PT2569319E (es)
RS (1) RS53669B1 (es)
SG (1) SG185484A1 (es)
SI (1) SI2569319T1 (es)
TW (1) TWI419892B (es)
UA (1) UA110616C2 (es)
WO (1) WO2011141396A1 (es)
ZA (1) ZA201208317B (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2356123E (pt) 2008-11-13 2012-10-31 Hoffmann La Roche Espiro-5,6-di-hidro-4h-2,3,5,10b-tetra-azabenzo[ e]azulenos
RU2510397C2 (ru) 2008-11-18 2014-03-27 Ф. Хоффманн-Ля Рош Аг Алкилциклогексиловые эфиры дигидротетраазабензоазуленов
BRPI0922303B1 (pt) 2008-11-28 2019-11-12 Hoffmann La Roche arilciclo-hexiléteres de di-hidrotetra-azabenzoazulenos, seu processo de preparação, composição farmacêutica que os compreende e uso
US8420633B2 (en) 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-tetraazabenzo[e]azulenes
US8461151B2 (en) 2010-04-13 2013-06-11 Hoffmann-La Roche Inc. Aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8481528B2 (en) 2010-04-26 2013-07-09 Hoffmann-La Roche Inc. Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8513238B2 (en) 2010-05-10 2013-08-20 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes
WO2017191117A1 (en) 2016-05-03 2017-11-09 Bayer Pharma Aktiengesellschaft V1a receptor antagonists for use in the treatment of renal diseases
AR113206A1 (es) 2017-01-10 2020-02-19 Bayer Cropscience Ag Derivados heterocíclicos como pesticidas
UY37556A (es) 2017-01-10 2018-07-31 Bayer Ag Derivados heterocíclicos como pesticidas
TW201938171A (zh) 2017-12-15 2019-10-01 匈牙利商羅特格登公司 作為血管升壓素V1a受體拮抗劑之三環化合物
HU231206B1 (hu) 2017-12-15 2021-10-28 Richter Gedeon Nyrt. Triazolobenzazepinek
ES2953140T3 (es) 2019-03-08 2023-11-08 Syngenta Crop Protection Ag Compuestos de azol-amida activos de manera plaguicida
US12552766B2 (en) 2019-03-20 2026-02-17 Syngenta Crop Protection Ag Pesticidally active azole amide compounds
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

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5428157A (en) 1993-11-22 1995-06-27 Merck & Co., Inc. 3-acylaminobenzodiazepines
NL9401174A (nl) 1994-07-15 1996-02-01 A P I S Medical Bv Inspuitsamenstel met opzuignaald en terugtrekbare inspuitnaald.
BR9811585A (pt) * 1997-07-30 2000-09-26 American Home Prod Agonistas de vasopressinas tricìclicas
ME00129B (me) 1999-01-19 2010-10-10 Ortho Mcneil Janssen Pharmaceuticals Inc Triciklicnj benzodiazepini kao antagonisti receptora vazopresina
US7109193B2 (en) 2001-04-12 2006-09-19 Wyeth Tricyclic diazepines tocolytic oxytocin receptor antagonists
US7022699B2 (en) 2001-04-12 2006-04-04 Wyeth Cyclohexenyl phenyl diazepines vasopressin and oxytocin receptor modulators
EP1472252A1 (en) 2002-02-07 2004-11-03 Neurogen Corporation Substituted fused pyrazolecarboxylic acid arylamides and related compounds
GB0303852D0 (en) 2003-02-19 2003-03-26 Pfizer Ltd Triazole compounds useful in therapy
GB0400700D0 (en) 2004-01-13 2004-02-18 Pfizer Ltd Compounds useful in therapy
KR100840852B1 (ko) 2004-05-25 2008-06-23 화이자 프로덕츠 인크. 테트라아자벤조[e]아줄렌 유도체 및 이의 유사체
AP2006003768A0 (en) 2004-05-25 2006-10-31 Pfizer Prod Inc TetraazabenzoÄeÜazulene derivatives and analogs tehereof
EP1632494A1 (en) 2004-08-24 2006-03-08 Ferring B.V. Vasopressin v1a antagonists
CA2578370A1 (en) 2004-08-25 2006-03-02 Pfizer Inc. Triazolobenzodiazepines and their use as vasopressin antagonists
ES2355923T3 (es) * 2004-08-26 2011-04-01 Pfizer, Inc. Compuestos de aminoheteroarilo sustituidos con pirazol como inhibidores de proteina quinasa.
WO2006114706A1 (en) 2005-04-26 2006-11-02 Pfizer Limited Triazole derivatives as vasopressin antagonists
CA2608718A1 (en) 2005-05-18 2006-11-23 Pfizer Limited 1, 2, 4-triazole derivatives as vasopressin antagonists
CN101583615B (zh) 2007-01-12 2012-07-04 弗·哈夫曼-拉罗切有限公司 螺哌啶甘氨酰胺衍生物
RU2510397C2 (ru) 2008-11-18 2014-03-27 Ф. Хоффманн-Ля Рош Аг Алкилциклогексиловые эфиры дигидротетраазабензоазуленов
US8420633B2 (en) 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-tetraazabenzo[e]azulenes
US8461151B2 (en) 2010-04-13 2013-06-11 Hoffmann-La Roche Inc. Aryl-/heteroaryl-cyclohexenyl-tetraazabenzo[e]azulenes
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8481528B2 (en) 2010-04-26 2013-07-09 Hoffmann-La Roche Inc. Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes
US8513238B2 (en) 2010-05-10 2013-08-20 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes

Also Published As

Publication number Publication date
CY1115820T1 (el) 2017-01-25
AR081374A1 (es) 2012-08-29
RS53669B1 (sr) 2015-04-30
HK1176934A1 (zh) 2013-08-09
CR20120542A (es) 2013-01-11
PT2569319E (pt) 2014-11-24
PH12012502174A1 (en) 2013-02-04
EA021441B1 (ru) 2015-06-30
KR20130109958A (ko) 2013-10-08
US20110275801A1 (en) 2011-11-10
AU2011252116B2 (en) 2014-03-13
DK2569319T3 (da) 2014-10-20
MA34252B1 (fr) 2013-05-02
MX2012012857A (es) 2012-11-29
ZA201208317B (en) 2014-04-30
TWI419892B (zh) 2013-12-21
WO2011141396A1 (en) 2011-11-17
TW201200520A (en) 2012-01-01
EP2569319B1 (en) 2014-09-24
NZ603223A (en) 2014-09-26
CA2797920A1 (en) 2011-11-17
CN102884065B (zh) 2015-11-25
ES2523881T3 (es) 2014-12-02
BR112012028763A2 (pt) 2016-07-19
JP2013526500A (ja) 2013-06-24
SG185484A1 (en) 2012-12-28
EP2569319A1 (en) 2013-03-20
EA201291187A1 (ru) 2013-04-30
SI2569319T1 (sl) 2014-12-31
PE20130401A1 (es) 2013-04-10
UA110616C2 (uk) 2016-01-25
MY160517A (en) 2017-03-15
CL2012003132A1 (es) 2013-06-28
CO6620058A2 (es) 2013-02-15
CN102884065A (zh) 2013-01-16
HRP20141250T1 (en) 2015-03-13
IL222815A (en) 2014-08-31
PL2569319T3 (pl) 2015-03-31
AU2011252116A1 (en) 2012-11-22
US8513238B2 (en) 2013-08-20
JP5868959B2 (ja) 2016-02-24

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