AR080955A1 - Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenos - Google Patents

Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenos

Info

Publication number
AR080955A1
AR080955A1 ARP110101211A ARP110101211A AR080955A1 AR 080955 A1 AR080955 A1 AR 080955A1 AR P110101211 A ARP110101211 A AR P110101211A AR P110101211 A ARP110101211 A AR P110101211A AR 080955 A1 AR080955 A1 AR 080955A1
Authority
AR
Argentina
Prior art keywords
alkyl
halogen
alkoxy
group
cyano
Prior art date
Application number
ARP110101211A
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 AR080955A1 publication Critical patent/AR080955A1/es

Links

Classifications

    • 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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61P25/14—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
    • A61P25/18—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
    • 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
    • A61P9/12—Antihypertensives

Abstract

Los compuestos segun la solicitud actuan como moduladores del receptor de la V1a y en particular como antagonistas del receptor de la V1a. Se refiere también a su obtencion, a composiciones farmacéuticas que los contienen y a su utilizacion como medicamentos. Los compuestos activos de la presente solicitud son utiles como sustancias terapéuticas que actuan a nivel periférico y central en estados patologicos tales como la dismenorrea, disfuncion sexual masculina o femenina, hipertension, fallo cardíaco cronico, secrecion inapropiada de vasopresina, cirrosis hepática, síndrome nefrotico, ansiedad, trastornos depresivos, trastorno obsesivo-compulsivo, trastornos del espectro autista, esquizofrenia y conducta agresiva. Reivindicacion 1: Un compuesto de la formula (1) en la que R1 se elige entre el grupo formado por i) H, ii) alquilo C1-6, sin sustituir o sustituido de 1 a 5 veces por sustituyentes elegidos individualmente entre el grupo formado por OH, halogeno, ciano y alcoxi C1-6, iii) -S(O)2-alquilo C1-6, dicho alquilo C1-6 está sin sustituir o sustituido de 1 a 5 veces por sustituyentes elegidos individualmente entre el grupo formado por OH, halogeno, ciano y alcoxi C1-6, iv) -C(O)-alquilo C1-6, dicho alquilo C1-6 está sin sustituir o sustituido de 1 a 5 veces por sustituyentes elegidos individualmente entre el grupo formado por OH, halogeno, ciano y alcoxi C1-6, y v) -C(O)O-alquilo C1-6, dicho alquilo C1-6 está sin sustituir o sustituido de 1 a 5 veces por sustituyentes elegidos individualmente entre el grupo formado por OH, halogeno, ciano y alcoxi C1-6; R2 es halogeno; R3 es arilo o heteroarilo, sin sustituir o sustituidos de 1 a 5 veces por sustituyentes elegidos individualmente entre el grupo formado por OH, halogeno, ciano, alquilo C1-6, alcoxi C1-6, halogeno-alquilo C1-6, halogeno-alcoxi C1-6 e hidroxi-alquilo C1-6; o una sal farmacéuticamente aceptable del mismo.
ARP110101211A 2010-04-13 2011-04-11 Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenos AR080955A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10159822 2010-04-13

Publications (1)

Publication Number Publication Date
AR080955A1 true AR080955A1 (es) 2012-05-23

Family

ID=43971443

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110101211A AR080955A1 (es) 2010-04-13 2011-04-11 Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenos

Country Status (13)

Country Link
US (1) US8461151B2 (es)
EP (1) EP2558467B1 (es)
JP (1) JP5579920B2 (es)
KR (1) KR101468285B1 (es)
CN (1) CN102834396B (es)
AR (1) AR080955A1 (es)
BR (1) BR112012025942A2 (es)
CA (1) CA2790687A1 (es)
HK (1) HK1175785A1 (es)
MX (1) MX2012011500A (es)
RU (1) RU2568642C2 (es)
TW (1) TWI417294B (es)
WO (1) WO2011128265A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2356123T1 (sl) * 2008-11-13 2013-01-31 F. Hoffmann-La Roche Ag Piro-5,6-dihidro-4h-2,3,5,10b-tetraaza-benzo(e)azuleni
SG171742A1 (en) * 2008-11-18 2011-07-28 Hoffmann La Roche Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
EP2370441B1 (en) 2008-11-28 2013-09-11 F. Hoffmann-La Roche AG Arylcyclohexylethers of dihydrotetraazabenzoazulenes for use as vasopressin v1a receptor antagonists
US8420633B2 (en) 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-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
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

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US5516774A (en) * 1993-07-29 1996-05-14 American Cyanamid Company Tricyclic diazepine vasopressin antagonists and oxytocin antagonists
US5521173A (en) 1995-01-17 1996-05-28 American Home Products Corporation Tricyclic benzazepine vasopressin antagonists
WO1999006409A1 (en) * 1997-07-30 1999-02-11 American Home Products Corporation Tricyclic vasopressin agonists
HU229074B1 (en) 1999-01-19 2013-07-29 Ortho Mcneil Pharm Inc Tricyclic benzodiazepines as vasopressin receptor antagonists
US7022699B2 (en) 2001-04-12 2006-04-04 Wyeth Cyclohexenyl phenyl diazepines vasopressin and oxytocin receptor modulators
PT1597260E (pt) * 2003-02-19 2007-01-31 Pfizer Composto de triazole úteis em terapia
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
GB0412874D0 (en) * 2004-06-09 2004-07-14 Pfizer Ltd Novel pharmaceuticals
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SG171742A1 (en) 2008-11-18 2011-07-28 Hoffmann La Roche Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
US8420633B2 (en) * 2010-03-31 2013-04-16 Hoffmann-La Roche Inc. Aryl-cyclohexyl-tetraazabenzo[e]azulenes
US8492376B2 (en) 2010-04-21 2013-07-23 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes
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US8513238B2 (en) 2010-05-10 2013-08-20 Hoffmann-La Roche Inc. Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes

Also Published As

Publication number Publication date
JP5579920B2 (ja) 2014-08-27
CA2790687A1 (en) 2011-10-20
TW201139442A (en) 2011-11-16
BR112012025942A2 (pt) 2016-06-28
US8461151B2 (en) 2013-06-11
CN102834396B (zh) 2016-06-01
EP2558467B1 (en) 2017-05-17
US20110251183A1 (en) 2011-10-13
MX2012011500A (es) 2012-11-06
JP2013523853A (ja) 2013-06-17
KR20130028721A (ko) 2013-03-19
TWI417294B (zh) 2013-12-01
CN102834396A (zh) 2012-12-19
WO2011128265A1 (en) 2011-10-20
RU2012145778A (ru) 2014-05-20
EP2558467A1 (en) 2013-02-20
HK1175785A1 (zh) 2013-07-12
KR101468285B1 (ko) 2014-12-03
RU2568642C2 (ru) 2015-11-20

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