BR112012028763A2 - heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos - Google Patents

heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos

Info

Publication number
BR112012028763A2
BR112012028763A2 BR112012028763A BR112012028763A BR112012028763A2 BR 112012028763 A2 BR112012028763 A2 BR 112012028763A2 BR 112012028763 A BR112012028763 A BR 112012028763A BR 112012028763 A BR112012028763 A BR 112012028763A BR 112012028763 A2 BR112012028763 A2 BR 112012028763A2
Authority
BR
Brazil
Prior art keywords
azulenes
heteroaryl
cyclohexyl
tetraazatetra
azabenzene
Prior art date
Application number
BR112012028763A
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 BR112012028763A2 publication Critical patent/BR112012028763A2/pt

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
    • A61K31/551—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
    • 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
    • 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
    • A61P25/22—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
    • 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

heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos. a presente invenção refere-se a heteroaril-cicloexil-tetra-azabenzo[e]azulenos de fórmula i em que r1,r2 e r3 são como aqui descrito. os compostos de acordo com a invenção agem como moduladores do receptor de via, e em particular como antagonistas do receptor de via, sua fabricação, composições farmacêuticas contendo-os, e seu uso como medicamentos. os compostos ativos da presente invenção são úteis como terapêuticos que agem perifericamente e centralmente nas condições de dismenorreia, disfunção sexual masculina ou feminina, hipertensão, insuficiência cardíada crônica,s ecreção imprópria de vasopressina, cirrose hepática, síndrome nefrótica, ansiedade, transtornos depressivos, trasntorno obssessivo-compulsivo, transtornos do espectro autista, esquizofrenia e comportamento agressivo.
BR112012028763A 2010-05-10 2011-05-09 heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos BR112012028763A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10162451 2010-05-10
PCT/EP2011/057368 WO2011141396A1 (en) 2010-05-10 2011-05-09 Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes

Publications (1)

Publication Number Publication Date
BR112012028763A2 true BR112012028763A2 (pt) 2016-07-19

Family

ID=44080459

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012028763A BR112012028763A2 (pt) 2010-05-10 2011-05-09 heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos

Country Status (34)

Country Link
US (1) US8513238B2 (pt)
EP (1) EP2569319B1 (pt)
JP (1) JP5868959B2 (pt)
KR (1) KR20130109958A (pt)
CN (1) CN102884065B (pt)
AR (1) AR081374A1 (pt)
AU (1) AU2011252116B2 (pt)
BR (1) BR112012028763A2 (pt)
CA (1) CA2797920A1 (pt)
CL (1) CL2012003132A1 (pt)
CO (1) CO6620058A2 (pt)
CR (1) CR20120542A (pt)
CY (1) CY1115820T1 (pt)
DK (1) DK2569319T3 (pt)
EA (1) EA021441B1 (pt)
EC (1) ECSP12012291A (pt)
ES (1) ES2523881T3 (pt)
HK (1) HK1176934A1 (pt)
HR (1) HRP20141250T1 (pt)
IL (1) IL222815A (pt)
MA (1) MA34252B1 (pt)
MX (1) MX2012012857A (pt)
MY (1) MY160517A (pt)
NZ (1) NZ603223A (pt)
PE (1) PE20130401A1 (pt)
PL (1) PL2569319T3 (pt)
PT (1) PT2569319E (pt)
RS (1) RS53669B1 (pt)
SG (1) SG185484A1 (pt)
SI (1) SI2569319T1 (pt)
TW (1) TWI419892B (pt)
UA (1) UA110616C2 (pt)
WO (1) WO2011141396A1 (pt)
ZA (1) ZA201208317B (pt)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0921110A2 (pt) 2008-11-13 2016-02-16 Hoffmann La Roche espiro-5,6-di-hidro-4h-2,3,5,10b-tetraaza-benzo[e]azulenos
WO2010057795A1 (en) 2008-11-18 2010-05-27 F. Hoffmann-La Roche Ag Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
ES2431279T3 (es) 2008-11-28 2013-11-25 F. Hoffmann-La Roche Ag Arilciclohexiléteres de dihidro-tetraazabenzoazulenos para uso como antagonistas del receptor V1A de la vasopresina
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
CN110382485B (zh) 2017-01-10 2022-05-10 拜耳公司 作为害虫防治剂的杂环烯衍生物
KR102628073B1 (ko) 2017-01-10 2024-01-22 바이엘 악티엔게젤샤프트 해충 방제제로서의 헤테로사이클 유도체
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
US20220167618A1 (en) 2019-03-08 2022-06-02 Syngenta Crop Protection Ag Pesticidally active azole-amide compounds
WO2020188014A1 (en) 2019-03-20 2020-09-24 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.
NZ502449A (en) * 1997-07-30 2002-08-28 Wyeth Corp Tricyclic vasopressin agonists and their pharmaceutical use
EP1147115B3 (en) 1999-01-19 2008-12-24 Ortho-McNeil Pharmaceutical, Inc. Tricyclic benzodiazepines as vasopressin receptor antagonists
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
US6852730B2 (en) 2002-02-07 2005-02-08 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
CA2568056A1 (en) 2004-05-25 2005-12-08 Pfizer Products Inc. Tetraazabenzo[e]azulene derivatives and analogs thereof
KR100840852B1 (ko) 2004-05-25 2008-06-23 화이자 프로덕츠 인크. 테트라아자벤조[ｅ]아줄렌 유도체 및 이의 유사체
EP1632494A1 (en) 2004-08-24 2006-03-08 Ferring B.V. Vasopressin v1a antagonists
JP2008510789A (ja) 2004-08-25 2008-04-10 ファイザー・インク トリアゾロベンゾジアゼピン及びバゾプレシンアンタゴニストとしてのそれらの使用
AU2005276132B2 (en) * 2004-08-26 2011-09-29 Pfizer Inc. Pyrazole-substituted aminoheteroaryl compounds as protein kinase inhibitors
US20080188478A1 (en) 2005-04-26 2008-08-07 Pfizer Inc. Compounds Useful In Therapy
US20080234252A1 (en) 2005-05-18 2008-09-25 Pfizer Inc Compounds Useful in Therapy
ES2376378T3 (es) 2007-01-12 2012-03-13 F. Hoffmann-La Roche Ag Derivados de espiropiperidina-glicinamida.
WO2010057795A1 (en) 2008-11-18 2010-05-27 F. Hoffmann-La Roche Ag Alkylcyclohexylethers of dihydrotetraazabenzoazulenes
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
AR081374A1 (es) 2012-08-29
ES2523881T3 (es) 2014-12-02
TW201200520A (en) 2012-01-01
SG185484A1 (en) 2012-12-28
AU2011252116B2 (en) 2014-03-13
RS53669B1 (en) 2015-04-30
MA34252B1 (fr) 2013-05-02
JP2013526500A (ja) 2013-06-24
MX2012012857A (es) 2012-11-29
ZA201208317B (en) 2014-04-30
HRP20141250T1 (en) 2015-03-13
PL2569319T3 (pl) 2015-03-31
SI2569319T1 (sl) 2014-12-31
EP2569319A1 (en) 2013-03-20
WO2011141396A1 (en) 2011-11-17
UA110616C2 (uk) 2016-01-25
US20110275801A1 (en) 2011-11-10
CN102884065A (zh) 2013-01-16
MY160517A (en) 2017-03-15
TWI419892B (zh) 2013-12-21
DK2569319T3 (da) 2014-10-20
JP5868959B2 (ja) 2016-02-24
US8513238B2 (en) 2013-08-20
CN102884065B (zh) 2015-11-25
IL222815A (en) 2014-08-31
CL2012003132A1 (es) 2013-06-28
KR20130109958A (ko) 2013-10-08
PE20130401A1 (es) 2013-04-10
HK1176934A1 (zh) 2013-08-09
EP2569319B1 (en) 2014-09-24
PT2569319E (pt) 2014-11-24
NZ603223A (en) 2014-09-26
CR20120542A (es) 2013-01-11
EA201291187A1 (ru) 2013-04-30
AU2011252116A1 (en) 2012-11-22
CA2797920A1 (en) 2011-11-17
CO6620058A2 (es) 2013-02-15
EA021441B1 (ru) 2015-06-30
CY1115820T1 (el) 2017-01-25
ECSP12012291A (es) 2012-12-28

Similar Documents

Publication Publication Date Title
BR112012028763A2 (pt) heteroaril-cicloexil-tetra-azatetra-azabenzeno[e]azulenos
BR112012024306A2 (pt) aril-cicloexil-tetraazabenzo[e] azulenos
BR112012026890A2 (pt) heteroarial-cicloexil-tetra-azabenzo[e] azulenos como antagonistas do receptor vasopressina v1a
JOP20180103B1 (ar) التركيب الصيدلاني للكاربيتوسين
BR112015012555A2 (pt) derivados de benzimidazol como antagonistas de ep4
BR112012027392A2 (pt) heterobiaril-ciclo-hexil-tetra-azabenzo{e} azulenos
BR112012025942A2 (pt) aril-/heteroaril-ciclo-hexenil-tetra-azabenzo[e]azulenos como antagonistas de vasopressina
PH12014502540A1 (en) Benzimidazole-proline derivatives
CO6341478A2 (es) Arilciclohexileteres de dihidro-tetraazabenzoazulenos para su uso como antagonistas del receptor v1a de vasopresina
PH12014501514A1 (en) New azetidine derivatives, pharmaceutical compositions and uses thereof
BR112015010221A2 (pt) inibidores de cinase alk
BR112012007322A2 (pt) composto de 2-piridona usados como inibidores de neutrófilo elastase
BR112013021798A2 (pt) 1,4 tiazepinaas/sulfonas como inibidores de bace1 e/ou bace2
CR10577A (es) 2-fenilindoles como antagonistas del receptor de la prostaglandina d2
BR112014007851A2 (pt) ciclo-hexil-4h,6h-oxa-2,3,10b-triaza-benzo[e]azulenos como antagonistas de v1a
BR112013029730A2 (pt) composição farmacêutica de rosuvastatina cálcica
BR112014012459A2 (pt) 2h-indazóis como antagonistas do receptor de ep2
IN2012DN00239A (pt)
BR112014006945A2 (pt) óxi-ciclo-hexil-4h,6h-5-oxa-2,3,10b-triaza-benzo[e]azulenos como antagonistas de v1a
BR112017007363A2 (pt) espiro-tiazolonas

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2513 DE 06-03-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.