AR080955A1 - Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenos - Google Patents
Aril-/heteroaril-ciclohexenil-tetraazabenzo(e)azulenosInfo
- 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
Links
Classifications
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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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Reproductive Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- Gynecology & Obstetrics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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.
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20110537A1 (es) * | 2008-11-13 | 2011-08-04 | Hoffmann La Roche | ESPIRO-5,6-DIHIDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENOS COMO ANTAGONISTAS DE LA V1a |
| WO2010057795A1 (en) * | 2008-11-18 | 2010-05-27 | F. Hoffmann-La Roche Ag | Alkylcyclohexylethers of dihydrotetraazabenzoazulenes |
| PE20110582A1 (es) | 2008-11-28 | 2011-08-17 | Hoffmann La Roche | Arilciclohexileteres de dihidro-tetraazabenzoazuleno |
| 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 |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
| 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 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SI1000062T1 (en) * | 1997-07-30 | 2004-12-31 | Wyeth | Tricyclic vasopressin agonists |
| NZ512960A (en) | 1999-01-19 | 2004-01-30 | 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 |
| CA2516557C (en) * | 2003-02-19 | 2008-11-18 | Pfizer Inc. | Triazole compounds useful in therapy |
| 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 |
| CA2568056A1 (en) | 2004-05-25 | 2005-12-08 | Pfizer Products Inc. | Tetraazabenzo[e]azulene derivatives and analogs thereof |
| GB0412874D0 (en) * | 2004-06-09 | 2004-07-14 | Pfizer Ltd | Novel pharmaceuticals |
| US7572506B2 (en) | 2004-06-30 | 2009-08-11 | E. I. Du Pont De Nemours And Company | Aqueous primer surfacer compositions |
| 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 |
| CA2605899C (en) | 2005-04-26 | 2011-02-08 | Pfizer Limited | Triazole derivatives as vasopressin antagonists |
| BRPI0806538A2 (pt) | 2007-01-12 | 2014-04-22 | Hoffmann La Roche | Derivados de glicinamida de espiropiperidina |
| 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 |
| 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 |
-
2011
- 2011-04-04 US US13/079,031 patent/US8461151B2/en not_active Expired - Fee Related
- 2011-04-08 WO PCT/EP2011/055516 patent/WO2011128265A1/en active Application Filing
- 2011-04-08 CA CA2790687A patent/CA2790687A1/en not_active Abandoned
- 2011-04-08 CN CN201180018435.3A patent/CN102834396B/zh not_active Expired - Fee Related
- 2011-04-08 JP JP2013504209A patent/JP5579920B2/ja not_active Expired - Fee Related
- 2011-04-08 EP EP11715194.4A patent/EP2558467B1/en not_active Not-in-force
- 2011-04-08 BR BR112012025942A patent/BR112012025942A2/pt not_active IP Right Cessation
- 2011-04-08 MX MX2012011500A patent/MX2012011500A/es active IP Right Grant
- 2011-04-08 RU RU2012145778/04A patent/RU2568642C2/ru not_active IP Right Cessation
- 2011-04-08 KR KR1020127026573A patent/KR101468285B1/ko not_active IP Right Cessation
- 2011-04-11 TW TW100112498A patent/TWI417294B/zh not_active IP Right Cessation
- 2011-04-11 AR ARP110101211A patent/AR080955A1/es unknown
-
2013
- 2013-03-18 HK HK13103291.5A patent/HK1175785A1/zh not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| TWI417294B (zh) | 2013-12-01 |
| RU2568642C2 (ru) | 2015-11-20 |
| BR112012025942A2 (pt) | 2016-06-28 |
| HK1175785A1 (zh) | 2013-07-12 |
| CN102834396A (zh) | 2012-12-19 |
| JP5579920B2 (ja) | 2014-08-27 |
| EP2558467A1 (en) | 2013-02-20 |
| RU2012145778A (ru) | 2014-05-20 |
| KR20130028721A (ko) | 2013-03-19 |
| EP2558467B1 (en) | 2017-05-17 |
| JP2013523853A (ja) | 2013-06-17 |
| WO2011128265A1 (en) | 2011-10-20 |
| KR101468285B1 (ko) | 2014-12-03 |
| MX2012011500A (es) | 2012-11-06 |
| CN102834396B (zh) | 2016-06-01 |
| US20110251183A1 (en) | 2011-10-13 |
| TW201139442A (en) | 2011-11-16 |
| CA2790687A1 (en) | 2011-10-20 |
| US8461151B2 (en) | 2013-06-11 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |