BR112012026890A2 - heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a - Google Patents

heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a

Info

Publication number
BR112012026890A2
BR112012026890A2 BR112012026890A BR112012026890A BR112012026890A2 BR 112012026890 A2 BR112012026890 A2 BR 112012026890A2 BR 112012026890 A BR112012026890 A BR 112012026890A BR 112012026890 A BR112012026890 A BR 112012026890A BR 112012026890 A2 BR112012026890 A2 BR 112012026890A2
Authority
BR
Brazil
Prior art keywords
heteroaryl
cyclohexyl
receptor antagonists
azulenes
tetra azabenzo
Prior art date
Application number
BR112012026890A
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 BR112012026890A2 publication Critical patent/BR112012026890A2/pt

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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

Abstract

heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a a presente invenção refere-se a heteroaril-cicloexil-tetra-azabenzo[e]azulejos de fórmula l em que r^ 1^, r^ 2^ e r^ 3^ são como descrito aqui. os compostos de acordo com a invenção agem como moduladores de receptor de v1a, e em particular com antagonistas de receptor de v1a, sua fabricação , composições farmacêuticas contendo-os e seu uso como medicamentos. os compostos ativos da presente invenção são úteis como terâpeuticos agindo perifericamente e centralmente nas condições de dismenorreia, disfunção sexual masculina ou feminina, hipertensão , insuficiência cardíaca crônica, secreção inapropriada de vasopressina, cirrose hepática, síndrome nefrótica, ansiedade, distírbios depressivos , distúrbio obsessivo compulsivo, distúrbios de espectro, esquizofrenia , e comportamento agressivo.
BR112012026890A 2010-04-21 2011-04-18 heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a BR112012026890A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10160643 2010-04-21
PCT/EP2011/056071 WO2011131596A1 (en) 2010-04-21 2011-04-18 Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes as vasopressin v1a receptor antagonists

Publications (1)

Publication Number Publication Date
BR112012026890A2 true BR112012026890A2 (pt) 2016-07-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012026890A BR112012026890A2 (pt) 2010-04-21 2011-04-18 heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a

Country Status (35)

Country Link
US (1) US8492376B2 (pt)
EP (1) EP2560975B1 (pt)
JP (1) JP5579923B2 (pt)
KR (1) KR101506776B1 (pt)
CN (1) CN102858776B (pt)
AR (1) AR080927A1 (pt)
AU (1) AU2011244407B2 (pt)
BR (1) BR112012026890A2 (pt)
CA (1) CA2795526A1 (pt)
CL (1) CL2012002905A1 (pt)
CO (1) CO6640209A2 (pt)
CR (1) CR20120513A (pt)
CY (1) CY1116661T1 (pt)
DK (1) DK2560975T3 (pt)
EA (1) EA021418B1 (pt)
EC (1) ECSP12012210A (pt)
ES (1) ES2542953T3 (pt)
HK (1) HK1176609A1 (pt)
HR (1) HRP20150929T1 (pt)
HU (1) HUE026538T2 (pt)
IL (1) IL222403A (pt)
MA (1) MA34174B1 (pt)
MX (1) MX2012012046A (pt)
MY (1) MY160457A (pt)
NZ (1) NZ602627A (pt)
PE (2) PE20160589A1 (pt)
PL (1) PL2560975T3 (pt)
PT (1) PT2560975E (pt)
RS (1) RS54121B1 (pt)
SG (1) SG184534A1 (pt)
SI (1) SI2560975T1 (pt)
TW (1) TWI419890B (pt)
UA (1) UA109543C2 (pt)
WO (1) WO2011131596A1 (pt)
ZA (1) ZA201207689B (pt)

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CA3079133A1 (en) * 2017-12-08 2019-06-13 F. Hoffmann-La Roche Ag Pharmaceutical formulation
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JP2023534721A (ja) * 2020-07-23 2023-08-10 エフ． ホフマン－ラ ロシュ アーゲー バソプレシン受容体ｖ１ａアンタゴニストとしてのヘテロアリール－メチル置換トリアゾール
JP2023534713A (ja) * 2020-07-23 2023-08-10 エフ． ホフマン－ラ ロシュ アーゲー バソプレシン受容体ｖ１ａアンタゴニストとしてのシクロヘキシル置換トリアゾール
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Publication number Publication date
CN102858776A (zh) 2013-01-02
RS54121B1 (en) 2015-12-31
IL222403A (en) 2014-08-31
TW201139444A (en) 2011-11-16
EA021418B1 (ru) 2015-06-30
CO6640209A2 (es) 2013-03-22
SI2560975T1 (sl) 2015-08-31
AU2011244407B2 (en) 2013-06-13
CA2795526A1 (en) 2011-10-27
JP5579923B2 (ja) 2014-08-27
PE20160589A1 (es) 2016-06-11
ZA201207689B (en) 2015-06-24
AR080927A1 (es) 2012-05-16
MX2012012046A (es) 2012-11-22
EP2560975B1 (en) 2015-06-17
CL2012002905A1 (es) 2013-03-22
CR20120513A (es) 2012-11-01
KR101506776B1 (ko) 2015-03-27
TWI419890B (zh) 2013-12-21
MA34174B1 (fr) 2013-04-03
WO2011131596A1 (en) 2011-10-27
CY1116661T1 (el) 2017-03-15
NZ602627A (en) 2013-07-26
HRP20150929T1 (hr) 2015-10-09
UA109543C2 (xx) 2015-09-10
EP2560975A1 (en) 2013-02-27
AU2011244407A1 (en) 2012-10-18
MY160457A (en) 2017-03-15
DK2560975T3 (en) 2015-06-29
ES2542953T3 (es) 2015-08-13
CN102858776B (zh) 2016-01-20
PT2560975E (pt) 2015-08-28
US20110263578A1 (en) 2011-10-27
US8492376B2 (en) 2013-07-23
KR20130008619A (ko) 2013-01-22
PL2560975T3 (pl) 2015-11-30
SG184534A1 (en) 2012-11-29
JP2013525319A (ja) 2013-06-20
ECSP12012210A (es) 2012-10-30
EA201291092A1 (ru) 2013-04-30
HK1176609A1 (zh) 2013-08-02
HUE026538T2 (en) 2016-06-28
PE20130190A1 (es) 2013-02-21

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