EA201170100A1 - Алканолпиперазиновые производные бензотиофена и их применение в качестве антидепрессанта - Google Patents
Алканолпиперазиновые производные бензотиофена и их применение в качестве антидепрессантаInfo
- Publication number
- EA201170100A1 EA201170100A1 EA201170100A EA201170100A EA201170100A1 EA 201170100 A1 EA201170100 A1 EA 201170100A1 EA 201170100 A EA201170100 A EA 201170100A EA 201170100 A EA201170100 A EA 201170100A EA 201170100 A1 EA201170100 A1 EA 201170100A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- benzothiophene
- derivatives
- antidepressants
- present
- alkanolpiperazine
- Prior art date
Links
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical class C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 title abstract 6
- 239000000935 antidepressant agent Substances 0.000 title abstract 4
- 229940005513 antidepressants Drugs 0.000 title abstract 4
- 230000001430 anti-depressive effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 abstract 1
- ZEUITGRIYCTCEM-KRWDZBQOSA-N (S)-duloxetine Chemical compound C1([C@@H](OC=2C3=CC=CC=C3C=CC=2)CCNC)=CC=CS1 ZEUITGRIYCTCEM-KRWDZBQOSA-N 0.000 abstract 1
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 abstract 1
- 229960003914 desipramine Drugs 0.000 abstract 1
- 229960002866 duloxetine Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229960002464 fluoxetine Drugs 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 231100001231 less toxic Toxicity 0.000 abstract 1
- 210000000653 nervous system Anatomy 0.000 abstract 1
- 150000004885 piperazines Chemical class 0.000 abstract 1
- 230000009103 reabsorption Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229940066771 systemic antihistamines piperazine derivative Drugs 0.000 abstract 1
- 229960004688 venlafaxine Drugs 0.000 abstract 1
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
Abstract
Настоящее изобретение относится к алканолпиперазиновым производным бензотиофена и к их применению в качестве антидепрессантов. В настоящем изобретении описано указанное алканолпиперазиновое производное бензотиофена, оказывающее тройной ингибирующий эффект на повторное поглощение 5-ГТ, НА и ДА. В сравнении с применяемыми в настоящее время в медицине антидепрессантами, которые имеют всего одну мишень, такими как дезипрамин и флуоксетин, и с применяемыми в медицине антидепрессантами с двумя мишенями воздействия, например с венлафаксином и дулоксетином, указанные алконолпиперазиновые производные бензотиофена по настоящему изобретению характеризуются более широким диапазоном показаний для их применения, меньшими токсическими и побочными эффектами в отношении нервной системы. Указанные алконолпиперазиновые производные бензотиофена представляют собой соединения указанной ниже формулы или фармацевтически приемлемые соли таких соединений, где Ar, R-R, X, Y, m и n определены в п.1 формулы изобретения.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2008100401054A CN101619056B (zh) | 2008-07-02 | 2008-07-02 | 苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁症药物的应用 |
| PCT/CN2009/072534 WO2010000198A1 (zh) | 2008-07-02 | 2009-06-30 | 苯并噻吩烷醇哌嗪衍生物及其作为抗抑郁症药物的应用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201170100A1 true EA201170100A1 (ru) | 2011-08-30 |
| EA019360B1 EA019360B1 (ru) | 2014-03-31 |
Family
ID=41465502
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201170100A EA019360B1 (ru) | 2008-07-02 | 2009-06-30 | Алканолпиперазиновые производные бензотиофена и их применение в качестве антидепрессанта |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8680097B2 (ru) |
| EP (1) | EP2311828B9 (ru) |
| JP (1) | JP5528439B2 (ru) |
| KR (1) | KR20110042291A (ru) |
| CN (1) | CN101619056B (ru) |
| AP (1) | AP2011005554A0 (ru) |
| AU (1) | AU2009266196A1 (ru) |
| BR (1) | BRPI0914747A2 (ru) |
| CA (1) | CA2729720A1 (ru) |
| CO (1) | CO6341629A2 (ru) |
| EA (1) | EA019360B1 (ru) |
| IL (1) | IL210306A0 (ru) |
| MX (1) | MX2011000163A (ru) |
| WO (1) | WO2010000198A1 (ru) |
| ZA (1) | ZA201100713B (ru) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101380181B1 (ko) | 2012-02-01 | 2014-03-31 | 한국과학기술연구원 | 단가아민 재흡수 억제 활성을 보이는 (1Ｓ,3ａＲ,9ｂＳ)-1-페닐-2,3,3ａ,4,5,9ｂ-헥사하이드로-1Ｈ-벤조［ｅ］인돌 유도체와 3,4-다이아릴피롤리딘-2-온 유도체 |
| WO2015014256A1 (en) | 2013-07-29 | 2015-02-05 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use thereof |
| US9714232B2 (en) | 2013-12-20 | 2017-07-25 | Sunshine Lake Pharma Co., Ltd. | Substituted piperazine compounds and methods of use thereof |
| WO2016192657A1 (en) | 2015-06-03 | 2016-12-08 | Sunshine Lake Pharma Co., Ltd. | Substituted piperazine compounds and methods of use and use thereof |
| LT3762368T (lt) | 2018-03-08 | 2022-06-10 | Incyte Corporation | Aminopirazindiolio junginiai, kaip pi3k-γ inhibitoriai |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| AU2021305165A1 (en) * | 2020-07-06 | 2023-02-02 | Tactogen Inc | Advantageous benzothiophene compositions for mental disorders or enhancement |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2128266B1 (es) | 1997-07-08 | 2000-01-16 | Vita Invest Sa | Compuestos derivados de tiofeno y benzotiofeno y utilizacion y composicion correspondientes. |
| ES2188344B1 (es) | 2000-11-29 | 2004-09-16 | Laboratorios Vita, S.A. | Compuestos derivados de benzotiofeno, su procedimiento de obtencion y utilizacion de los mismos. |
| CN1172919C (zh) * | 2002-06-03 | 2004-10-27 | 上海医药工业研究院 | 芳烷醇哌嗪衍生物及其在制备抗抑郁症药物中的应用 |
| US7276603B2 (en) | 2003-05-02 | 2007-10-02 | Wyeth | Benzofuranyl-and benzothienyl-piperazinyl quinolines and methods of their use |
| CN1812984A (zh) * | 2003-05-02 | 2006-08-02 | 惠氏公司 | 作为5－羟色胺重摄取抑制剂的苯并呋喃基－哌嗪基喹啉和苯并噻吩基－哌嗪基喹啉 |
| CN100415728C (zh) * | 2005-10-10 | 2008-09-03 | 上海医药工业研究院 | 烷醇哌嗪衍生物光学异构体或其盐及其制备药物的应用 |
| CN1844120A (zh) | 2006-04-27 | 2006-10-11 | 天津大学 | 芳基哌嗪修饰的苯并[b]噻酚化合物及制备方法和应用 |
| CN100554266C (zh) * | 2006-04-27 | 2009-10-28 | 天津大学 | 芳基哌嗪修饰的苯并[b]噻酚化合物及制备方法和应用 |
-
2008
- 2008-07-02 CN CN2008100401054A patent/CN101619056B/zh not_active Expired - Fee Related
-
2009
- 2009-06-30 CA CA2729720A patent/CA2729720A1/en not_active Abandoned
- 2009-06-30 EP EP09771968.6A patent/EP2311828B9/en not_active Not-in-force
- 2009-06-30 EA EA201170100A patent/EA019360B1/ru not_active IP Right Cessation
- 2009-06-30 MX MX2011000163A patent/MX2011000163A/es not_active Application Discontinuation
- 2009-06-30 BR BRPI0914747A patent/BRPI0914747A2/pt not_active IP Right Cessation
- 2009-06-30 US US13/001,998 patent/US8680097B2/en not_active Expired - Fee Related
- 2009-06-30 AU AU2009266196A patent/AU2009266196A1/en not_active Abandoned
- 2009-06-30 WO PCT/CN2009/072534 patent/WO2010000198A1/zh active Application Filing
- 2009-06-30 JP JP2011515075A patent/JP5528439B2/ja not_active Expired - Fee Related
- 2009-06-30 KR KR1020117001760A patent/KR20110042291A/ko not_active Application Discontinuation
- 2009-06-30 AP AP2011005554A patent/AP2011005554A0/xx unknown
-
2010
- 2010-12-28 IL IL210306A patent/IL210306A0/en unknown
-
2011
- 2011-01-27 ZA ZA2011/00713A patent/ZA201100713B/en unknown
- 2011-01-28 CO CO11009671A patent/CO6341629A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| ZA201100713B (en) | 2012-07-25 |
| AP2011005554A0 (en) | 2011-02-28 |
| EP2311828A1 (en) | 2011-04-20 |
| CN101619056B (zh) | 2013-07-17 |
| EP2311828B1 (en) | 2015-03-25 |
| IL210306A0 (en) | 2011-03-31 |
| WO2010000198A1 (zh) | 2010-01-07 |
| JP5528439B2 (ja) | 2014-06-25 |
| AU2009266196A1 (en) | 2010-01-07 |
| US20110118263A1 (en) | 2011-05-19 |
| US8680097B2 (en) | 2014-03-25 |
| MX2011000163A (es) | 2011-03-15 |
| BRPI0914747A2 (pt) | 2017-05-23 |
| CO6341629A2 (es) | 2011-11-21 |
| EA019360B1 (ru) | 2014-03-31 |
| JP2011526254A (ja) | 2011-10-06 |
| CA2729720A1 (en) | 2010-01-07 |
| KR20110042291A (ko) | 2011-04-26 |
| EP2311828A4 (en) | 2011-11-23 |
| CN101619056A (zh) | 2010-01-06 |
| EP2311828B9 (en) | 2016-03-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG MD TJ TM |
|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): RU |