CY1117145T1 - Ετεροδιαρυλο-κυκλοεξυλο-τετρααζαβενζο[ε]αζουλενια - Google Patents
Ετεροδιαρυλο-κυκλοεξυλο-τετρααζαβενζο[ε]αζουλενιαInfo
- Publication number
- CY1117145T1 CY1117145T1 CY20161100048T CY161100048T CY1117145T1 CY 1117145 T1 CY1117145 T1 CY 1117145T1 CY 20161100048 T CY20161100048 T CY 20161100048T CY 161100048 T CY161100048 T CY 161100048T CY 1117145 T1 CY1117145 T1 CY 1117145T1
- Authority
- CY
- Cyprus
- Prior art keywords
- tetrazazabenzo
- present
- act
- azulenia
- cycloxyl
- Prior art date
Links
Classifications
-
- 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
Landscapes
- 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
Η παρούσα εφεύρεση σχετίζεται με ετεροδιαρυλο-κυκλοεξυλο-τετρααζαβενζο[e]αζουλένια του τύπου (I), όπου οι R1, R2 και R3 είναι όπως περιγράφονται στο παρόν. Οι ενώσεις σύμφωνα με την εφεύρεση δρουν ως διαμορφωτές του V1a υποδοχέα, και πιο συγκεκριμένα ως ανταγωνιστές του V1α υποδοχέα, η παραγωγή τους, φαρμακευτικές συνθέσεις που τις περιέχουν και η χρήση τους ως φάρμακα. Οι δραστικές ενώσεις της παρούσας εφεύρεσης είναι χρήσιμες ως θεραπευτικοί παράγοντες που δρουν περιφερικά και κεντρικά σε παθήσεις δυσμηνόρροιας, αρσενικής ή θηλυκής σεξουαλικής δυσλειτουργίας, υπέρτασης, χρόνιας καρδιακής ανεπάρκειας, ακατάλληλης έκκρισης βασοπρεσσίνης, κίρρωσης ήπατος, νεφρωσικού συνδρόμου, άγχους, διαταραχών κατάθλιψης, ιδεοψυχαναγκαστικής διαταραχής, διαταραχών αυτιστικού φάσματος, σχιζοφρένειας και επιθετικής συμπεριφοράς.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10161043 | 2010-04-26 | ||
| EP11715545.7A EP2571879B1 (en) | 2010-04-26 | 2011-04-21 | Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1117145T1 true CY1117145T1 (el) | 2017-04-05 |
Family
ID=43991411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20161100048T CY1117145T1 (el) | 2010-04-26 | 2016-01-19 | Ετεροδιαρυλο-κυκλοεξυλο-τετρααζαβενζο[ε]αζουλενια |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US8481528B2 (el) |
| EP (1) | EP2571879B1 (el) |
| JP (1) | JP5579925B2 (el) |
| KR (1) | KR101506778B1 (el) |
| CN (1) | CN102858778B (el) |
| AR (1) | AR081182A1 (el) |
| AU (1) | AU2011246553B2 (el) |
| BR (1) | BR112012027392A2 (el) |
| CA (1) | CA2794824A1 (el) |
| CL (1) | CL2012002954A1 (el) |
| CO (1) | CO6612268A2 (el) |
| CR (1) | CR20120515A (el) |
| CY (1) | CY1117145T1 (el) |
| DK (1) | DK2571879T3 (el) |
| EA (1) | EA021495B1 (el) |
| EC (1) | ECSP12012209A (el) |
| ES (1) | ES2553246T3 (el) |
| HK (1) | HK1176933A1 (el) |
| HR (1) | HRP20160051T1 (el) |
| HU (1) | HUE028018T2 (el) |
| IL (1) | IL222408A (el) |
| MA (1) | MA34173B1 (el) |
| MX (1) | MX2012012517A (el) |
| MY (1) | MY160977A (el) |
| NZ (1) | NZ602663A (el) |
| PE (1) | PE20130189A1 (el) |
| PL (1) | PL2571879T3 (el) |
| PT (1) | PT2571879E (el) |
| RS (1) | RS54418B1 (el) |
| SG (1) | SG184533A1 (el) |
| SI (1) | SI2571879T1 (el) |
| TW (1) | TWI419891B (el) |
| UA (1) | UA110031C2 (el) |
| WO (1) | WO2011134877A1 (el) |
| ZA (1) | ZA201207693B (el) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2356123T3 (da) * | 2008-11-13 | 2012-10-15 | Hoffmann La Roche | Spiro-5,6-dihydro-4h-2,3,5,10b-tetraaza-benzo[e]azulener |
| CN102216304B (zh) * | 2008-11-18 | 2014-07-09 | 弗·哈夫曼-拉罗切有限公司 | 二氢四氮杂苯并薁的烷基环己基醚 |
| RU2507205C2 (ru) | 2008-11-28 | 2014-02-20 | Ф. Хоффманн-Ля Рош Аг | Арилциклогексилэфиры дигидротетраазабензоазуленов для применения в качестве антагонистов рецептора вазопрессина v1a |
| 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 |
Family Cites Families (22)
| 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 |
| PT1000062E (pt) * | 1997-07-30 | 2004-12-31 | Wyeth Corp | Agonistas triciclicos de vasopressina |
| IL144270A0 (en) | 1999-01-19 | 2002-05-23 | 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 |
| US7109193B2 (en) * | 2001-04-12 | 2006-09-19 | Wyeth | Tricyclic diazepines tocolytic oxytocin receptor antagonists |
| SI1597260T1 (sl) * | 2003-02-19 | 2007-04-30 | Pfizer | Spojine triazola, uporabne pri terapiji |
| 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 |
| AP2006003768A0 (en) | 2004-05-25 | 2006-10-31 | Pfizer Prod Inc | TetraazabenzoÄeÜazulene derivatives and analogs tehereof |
| KR100840852B1 (ko) | 2004-05-25 | 2008-06-23 | 화이자 프로덕츠 인크. | 테트라아자벤조[ｅ]아줄렌 유도체 및 이의 유사체 |
| GB0412874D0 (en) * | 2004-06-09 | 2004-07-14 | Pfizer Ltd | Novel pharmaceuticals |
| 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 |
| WO2006114706A1 (en) | 2005-04-26 | 2006-11-02 | Pfizer Limited | Triazole derivatives as vasopressin antagonists |
| CA2608718A1 (en) | 2005-05-18 | 2006-11-23 | Pfizer Limited | 1, 2, 4-triazole derivatives as vasopressin antagonists |
| KR101129791B1 (ko) | 2007-01-12 | 2012-03-23 | 에프. 호프만-라 로슈 아게 | 스파이로피페리딘 글리신아마이드 유도체 |
| CN102216304B (zh) | 2008-11-18 | 2014-07-09 | 弗·哈夫曼-拉罗切有限公司 | 二氢四氮杂苯并薁的烷基环己基醚 |
| 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 |
-
2011
- 2011-04-19 US US13/089,354 patent/US8481528B2/en active Active
- 2011-04-21 ES ES11715545.7T patent/ES2553246T3/es active Active
- 2011-04-21 UA UAA201213289A patent/UA110031C2/uk unknown
- 2011-04-21 PL PL11715545T patent/PL2571879T3/pl unknown
- 2011-04-21 WO PCT/EP2011/056391 patent/WO2011134877A1/en active Application Filing
- 2011-04-21 EA EA201291109A patent/EA021495B1/ru not_active IP Right Cessation
- 2011-04-21 AU AU2011246553A patent/AU2011246553B2/en not_active Ceased
- 2011-04-21 EP EP11715545.7A patent/EP2571879B1/en not_active Not-in-force
- 2011-04-21 RS RS20150763A patent/RS54418B1/en unknown
- 2011-04-21 DK DK11715545.7T patent/DK2571879T3/en active
- 2011-04-21 SI SI201130662T patent/SI2571879T1/sl unknown
- 2011-04-21 PT PT117155457T patent/PT2571879E/pt unknown
- 2011-04-21 NZ NZ602663A patent/NZ602663A/xx not_active IP Right Cessation
- 2011-04-21 HU HUE11715545A patent/HUE028018T2/en unknown
- 2011-04-21 SG SG2012075149A patent/SG184533A1/en unknown
- 2011-04-21 MA MA35327A patent/MA34173B1/fr unknown
- 2011-04-21 BR BR112012027392A patent/BR112012027392A2/pt not_active IP Right Cessation
- 2011-04-21 CN CN201180021078.6A patent/CN102858778B/zh not_active Expired - Fee Related
- 2011-04-21 CA CA2794824A patent/CA2794824A1/en not_active Abandoned
- 2011-04-21 PE PE2012002067A patent/PE20130189A1/es not_active Application Discontinuation
- 2011-04-21 KR KR1020127030686A patent/KR101506778B1/ko not_active IP Right Cessation
- 2011-04-21 JP JP2013506597A patent/JP5579925B2/ja not_active Expired - Fee Related
- 2011-04-21 MY MYPI2012004626A patent/MY160977A/en unknown
- 2011-04-21 MX MX2012012517A patent/MX2012012517A/es active IP Right Grant
- 2011-04-25 AR ARP110101400A patent/AR081182A1/es unknown
- 2011-04-25 TW TW100114337A patent/TWI419891B/zh not_active IP Right Cessation
-
2012
- 2012-09-28 CO CO12170756A patent/CO6612268A2/es not_active Application Discontinuation
- 2012-10-02 EC ECSP12012209 patent/ECSP12012209A/es unknown
- 2012-10-11 CR CR20120515A patent/CR20120515A/es unknown
- 2012-10-11 IL IL222408A patent/IL222408A/en active IP Right Grant
- 2012-10-12 ZA ZA2012/07693A patent/ZA201207693B/en unknown
- 2012-10-23 CL CL2012002954A patent/CL2012002954A1/es unknown
-
2013
- 2013-04-12 HK HK13104455.5A patent/HK1176933A1/xx not_active IP Right Cessation
-
2016
- 2016-01-15 HR HRP20160051TT patent/HRP20160051T1/hr unknown
- 2016-01-19 CY CY20161100048T patent/CY1117145T1/el unknown
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