BR112012027392A2 - heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos - Google Patents

heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos

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Publication number
BR112012027392A2
BR112012027392A2 BR112012027392A BR112012027392A BR112012027392A2 BR 112012027392 A2 BR112012027392 A2 BR 112012027392A2 BR 112012027392 A BR112012027392 A BR 112012027392A BR 112012027392 A BR112012027392 A BR 112012027392A BR 112012027392 A2 BR112012027392 A2 BR 112012027392A2
Authority
BR
Brazil
Prior art keywords
tetraazabenzo
azulenes
heterobiaryl
cyclohexyl
present
Prior art date
Application number
BR112012027392A
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 BR112012027392A2 publication Critical patent/BR112012027392A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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
    • 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

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

Abstract

"heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos" a presente invenção refere-se a heterobiaril-ciclo-hexil-tetraazabenzo{e}azulenos de fórmula i em que r1,r2 e r3 são como descritos aqui.os compostos de acordo com a invenção agem como moduladores do receptor v1a ,e em particular como antagonistas do receptor v1 a sua fabricação ,composições farmacêuticas contendo -os e seu uso como medicamentos.os compostos ativos da presente invenção são úteis como produtos terapêuticos que agem perifericamente e centralmente nas condições de dismenorreia,disfusão sexual masculina ou feminina ,hipertensão ,insuficiência cardiaca crônica,secreção inapropiada de vasopressina,cirrose hepática,síndrome nef´rtica,ansiedade ,distúbios depressivos ,disturbio obsessivo compulsivo,distúrbios de espectro autístico ,esquizofrenia ,e comportamento agressivo.
BR112012027392A 2010-04-26 2011-04-21 heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos BR112012027392A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10161043 2010-04-26
PCT/EP2011/056391 WO2011134877A1 (en) 2010-04-26 2011-04-21 Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes

Publications (1)

Publication Number Publication Date
BR112012027392A2 true BR112012027392A2 (pt) 2016-08-09

Family

ID=43991411

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012027392A BR112012027392A2 (pt) 2010-04-26 2011-04-21 heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos

Country Status (35)

Country Link
US (1) US8481528B2 (pt)
EP (1) EP2571879B1 (pt)
JP (1) JP5579925B2 (pt)
KR (1) KR101506778B1 (pt)
CN (1) CN102858778B (pt)
AR (1) AR081182A1 (pt)
AU (1) AU2011246553B2 (pt)
BR (1) BR112012027392A2 (pt)
CA (1) CA2794824A1 (pt)
CL (1) CL2012002954A1 (pt)
CO (1) CO6612268A2 (pt)
CR (1) CR20120515A (pt)
CY (1) CY1117145T1 (pt)
DK (1) DK2571879T3 (pt)
EA (1) EA021495B1 (pt)
EC (1) ECSP12012209A (pt)
ES (1) ES2553246T3 (pt)
HK (1) HK1176933A1 (pt)
HR (1) HRP20160051T1 (pt)
HU (1) HUE028018T2 (pt)
IL (1) IL222408A (pt)
MA (1) MA34173B1 (pt)
MX (1) MX2012012517A (pt)
MY (1) MY160977A (pt)
NZ (1) NZ602663A (pt)
PE (1) PE20130189A1 (pt)
PL (1) PL2571879T3 (pt)
PT (1) PT2571879E (pt)
RS (1) RS54418B1 (pt)
SG (1) SG184533A1 (pt)
SI (1) SI2571879T1 (pt)
TW (1) TWI419891B (pt)
UA (1) UA110031C2 (pt)
WO (1) WO2011134877A1 (pt)
ZA (1) ZA201207693B (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009315754B2 (en) * 2008-11-13 2013-08-15 F. Hoffmann-La Roche Ag Spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes
DK2358714T3 (da) * 2008-11-18 2012-08-20 Hoffmann La Roche Alkylcyclohexylethere af dihydrotetraazabenzoazulener
MX2011005596A (es) * 2008-11-28 2011-06-16 Hoffmann La Roche Arilciclohexileteres de dihidro-tetraazabenzoazulenos para uso como antagonistas del receptor de vasopresina via.
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
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
CN115246781B (zh) * 2021-04-28 2024-03-29 南京正大天晴制药有限公司 一种沙芬酰胺的制备方法

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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
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
CA2794824A1 (en) 2011-11-03
CY1117145T1 (el) 2017-04-05
JP5579925B2 (ja) 2014-08-27
EA201291109A1 (ru) 2013-04-30
SG184533A1 (en) 2012-11-29
MY160977A (en) 2017-03-31
ECSP12012209A (es) 2012-10-30
AU2011246553B2 (en) 2014-02-13
HRP20160051T1 (hr) 2016-02-12
DK2571879T3 (en) 2015-11-09
AR081182A1 (es) 2012-07-04
PE20130189A1 (es) 2013-02-21
MA34173B1 (fr) 2013-04-03
PT2571879E (pt) 2015-11-30
TWI419891B (zh) 2013-12-21
CR20120515A (es) 2012-11-01
TW201141870A (en) 2011-12-01
HUE028018T2 (en) 2016-11-28
US20110263573A1 (en) 2011-10-27
WO2011134877A1 (en) 2011-11-03
CN102858778A (zh) 2013-01-02
KR101506778B1 (ko) 2015-03-27
NZ602663A (en) 2013-09-27
ZA201207693B (en) 2016-08-31
RS54418B1 (en) 2016-04-28
EP2571879B1 (en) 2015-10-21
MX2012012517A (es) 2012-11-23
CL2012002954A1 (es) 2013-04-12
KR20130031267A (ko) 2013-03-28
HK1176933A1 (en) 2013-08-09
SI2571879T1 (sl) 2015-12-31
AU2011246553A1 (en) 2012-10-18
PL2571879T3 (pl) 2016-04-29
EA021495B1 (ru) 2015-06-30
CO6612268A2 (es) 2013-02-01
EP2571879A1 (en) 2013-03-27
CN102858778B (zh) 2015-08-26
US8481528B2 (en) 2013-07-09
UA110031C2 (xx) 2015-11-10
IL222408A (en) 2014-08-31
ES2553246T3 (es) 2015-12-07
JP2013525396A (ja) 2013-06-20

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