EA200501730A1 - Производные n-пирролидин-3-ил-амида в качестве ингибиторов обратного захвата серотонина и норадреналина - Google Patents
Производные n-пирролидин-3-ил-амида в качестве ингибиторов обратного захвата серотонина и норадреналинаInfo
- Publication number
- EA200501730A1 EA200501730A1 EA200501730A EA200501730A EA200501730A1 EA 200501730 A1 EA200501730 A1 EA 200501730A1 EA 200501730 A EA200501730 A EA 200501730A EA 200501730 A EA200501730 A EA 200501730A EA 200501730 A1 EA200501730 A1 EA 200501730A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- aryl
- het
- cycloalkyl
- alkoxy
- Prior art date
Links
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 title abstract 4
- 229940076279 serotonin Drugs 0.000 title abstract 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 229960002748 norepinephrine Drugs 0.000 title 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 4
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010046543 Urinary incontinence Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 abstract 1
- 239000003772 serotonin uptake inhibitor Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- -1 —C (X) Y Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/14—Nitrogen atoms not forming part of a nitro radical
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
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- 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
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Psychology (AREA)
- Gynecology & Obstetrics (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Rheumatology (AREA)
- Anesthesiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Соединение формулы (I) и его фармацевтически и/или ветеринарно приемлемые производные, где Rпредставляет собой Н, Cалкил, -C(X)Y, Сциклоалкил, арил, het, арил-Салкил или het-Салкил, где группы циклоалкил, арил или het возможно замещены по меньшей мере одним заместителем, независимо выбранным из Салкила, Салкокси, ОН, галогено, CF, OCF, SCF, гидрокси-Салкила, Салкокси-Салкила и Салкил-S-Cалкила; Rпредставляет собой арил или гетероарил, каждый из которых возможно замещен по меньшей мере одним заместителем, независимо выбранным из Салкила, Салкокси, ОН, галогено, CF, OCF, SCF, гидрокси-Салкила, Салкокси-Cалкила и Салкил-S-Салкила; Rпредставляет собой Cалкил, Сциклоалкил, Сциклоалкил-Салкил, арил, het, арил-Салкил или het-Cалкил, где группы циклоалкил, арил или het возможно замещены по меньшей мере одним заместителем, независимо выбранным из Cалкила, Cалкокси, ОН, галогено, CF, OCF, SCF, гидрокси-Салкила, Салкокси-Салкила и Салкил-S-Салкила; Х представляет собой S или О; Y представляет собой Н, Cалкил, арил, het, арил-Салкил или het-Салкил; и n равно 1 или 2, при условии что, когда n равно 1, тогда m равно 0 или 1, и когда n равно 2, тогда m равно 0, причем если m равно 0, то * представляет собой хиральный центр. Соединения по изобретению проявляют активность ингибиторов обратного захвата как серотонина, так и норадреналина и, следовательно, применимы в различных терапевтических областях, например при недержании мочи.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0314048.0A GB0314048D0 (en) | 2003-06-17 | 2003-06-17 | Novel compounds |
| US49312603P | 2003-08-06 | 2003-08-06 | |
| PCT/IB2004/001943 WO2004110995A1 (en) | 2003-06-17 | 2004-06-07 | N-pyrrolidin-3-yl-amide derivatives as serotonin and noradrenaline re-uptake inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200501730A1 true EA200501730A1 (ru) | 2006-08-25 |
| EA009881B1 EA009881B1 (ru) | 2008-04-28 |
Family
ID=33554153
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA200501730A EA009881B1 (ru) | 2003-06-17 | 2004-06-07 | Производные n-пирролидин-3-ил-амида в качестве ингибиторов обратного захвата серотонина и норадреналина |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US7378436B2 (ru) |
| EP (1) | EP1638933B1 (ru) |
| JP (1) | JP4137159B2 (ru) |
| KR (1) | KR100803796B1 (ru) |
| AP (1) | AP2005003467A0 (ru) |
| AR (1) | AR044715A1 (ru) |
| AT (1) | ATE398107T1 (ru) |
| AU (1) | AU2004247487B2 (ru) |
| BR (1) | BRPI0411594A (ru) |
| CA (1) | CA2530159C (ru) |
| CY (1) | CY1110434T1 (ru) |
| DE (1) | DE602004014372D1 (ru) |
| DK (1) | DK1638933T3 (ru) |
| EA (1) | EA009881B1 (ru) |
| EC (1) | ECSP056232A (ru) |
| ES (1) | ES2305776T3 (ru) |
| HR (2) | HRP20050993A2 (ru) |
| IL (1) | IL172063A0 (ru) |
| IS (1) | IS8136A (ru) |
| MA (1) | MA27885A1 (ru) |
| MX (1) | MXPA05013960A (ru) |
| NL (1) | NL1026438C2 (ru) |
| NZ (1) | NZ544046A (ru) |
| PA (1) | PA8605301A1 (ru) |
| PE (1) | PE20050631A1 (ru) |
| PL (1) | PL1638933T3 (ru) |
| PT (1) | PT1638933E (ru) |
| SI (1) | SI1638933T1 (ru) |
| TW (1) | TW200505852A (ru) |
| UY (1) | UY28360A1 (ru) |
| WO (1) | WO2004110995A1 (ru) |
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| US7868014B2 (en) | 2004-10-18 | 2011-01-11 | Eli Lilly And Company | 1-(hetero)aryl-3-amino-pyrrolidine derivatives for use as mGluR3 antagonists |
| GB0425766D0 (en) * | 2004-11-23 | 2004-12-22 | Pfizer Ltd | Novel compounds |
| US7122683B2 (en) | 2004-11-23 | 2006-10-17 | Pfizer Inc. | Amides useful as monoamine re-uptake inhibitors |
| EP1828119A1 (en) * | 2004-12-14 | 2007-09-05 | Pfizer Limited | N-pyrrolidin-3-yl-amide derivatives as serotonin and noradrenalin re-uptake inhibitors |
| CA2590229A1 (en) * | 2004-12-14 | 2006-06-22 | Pfizer Limited | N-pyrrolidin-3-yl-amide derivatives as serotonin and noradrenalin re-uptake inhibitors |
| TWI449692B (zh) | 2005-05-13 | 2014-08-21 | Otsuka Pharma Co Ltd | 吡咯烷化合物（三） |
| EP1893603B1 (en) * | 2005-06-02 | 2009-10-14 | F. Hoffmann-La Roche AG | Piperidin-4-yl-amide derivatives and their use as sst receptor subtype 5 antagonists |
| WO2007135530A2 (en) * | 2006-05-22 | 2007-11-29 | Pfizer Limited | Pharmaceutically & veterinarily suitable salt |
| US20080014152A1 (en) * | 2006-07-13 | 2008-01-17 | Di Mauro Thomas M | Intranasal delivery of clenbuterol across the cribriform plate and into the brain |
| JP5219465B2 (ja) * | 2006-11-10 | 2013-06-26 | 大塚製薬株式会社 | 医薬 |
| EP2119702A4 (en) * | 2007-01-31 | 2010-12-08 | Dainippon Sumitomo Pharma Co | amide derivative |
| JP2010189275A (ja) * | 2007-06-14 | 2010-09-02 | Dainippon Sumitomo Pharma Co Ltd | ナフタレン誘導体 |
| US8263652B2 (en) | 2007-10-31 | 2012-09-11 | Sk Biopharmaceuticals Co., Ltd. | Stabilized pediatric suspension of carisbamate |
| TWI434690B (zh) | 2007-12-19 | 2014-04-21 | Dainippon Sumitomo Pharma Co | 雜雙環衍生物 |
| JP5405571B2 (ja) | 2008-07-24 | 2014-02-05 | セラヴァンス， インコーポレーテッド | ３−（フェノキシフェニルメチル）ピロリジン化合物 |
| RU2515612C2 (ru) | 2008-11-14 | 2014-05-20 | Тереванс, Инк. | 4-[2-(2-фторфеноксиметил)фенил]пиперидиновые соединения |
| WO2010120910A1 (en) * | 2009-04-15 | 2010-10-21 | Theravance, Inc. | 3-(phenoxypyrrolidin-3-yl-methyl)heteroaryl, 3-(phenylpyrrolidin-3-ylmethoxy)heteroaryl, and 3-(heteroarylpyrrolidin-3-ylmethoxy)heteroaryl compounds |
| JP5331883B2 (ja) | 2009-06-24 | 2013-10-30 | 大日本住友製薬株式会社 | Ｎ−置換−環状アミノ誘導体 |
| AU2010273645B2 (en) | 2009-07-13 | 2014-12-04 | Theravance Biopharma R&D Ip, Llc | 3-phenoxymethylpyrrolidine compounds |
| JP5714580B2 (ja) | 2009-07-21 | 2015-05-07 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | ３−フェノキシメチルピロリジン化合物 |
| JP5705239B2 (ja) | 2010-01-11 | 2015-04-22 | セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー | セロトニンおよびノルエピネフリン再取込みインヒビターとしての１−（２−フェノキシメチルフェニル）ピペラジン化合物 |
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| WO2004022536A1 (en) | 2002-09-04 | 2004-03-18 | Glenmark Pharmaceuticals Limited | New heterocyclic amide compounds useful for the treatment of inflammatory and allergic disorders: process for their preparation and pharmaceutical compositions containing them |
| WO2004058705A2 (en) | 2002-12-20 | 2004-07-15 | Chemocentryx | Inhibitors of the binding of chemokines i-tac or sdf-1 to the ccxckr2 receptor |
| DK1638933T3 (da) * | 2003-06-17 | 2008-07-28 | Pfizer | N-pyrrolidin-3-yl-amid-derivater som serotonin- og noradrenalin-genoptagelses inhibitorer |
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2004
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- 2004-06-07 EA EA200501730A patent/EA009881B1/ru not_active IP Right Cessation
- 2004-06-07 EP EP04736241A patent/EP1638933B1/en not_active Expired - Lifetime
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- 2004-06-07 KR KR1020057024147A patent/KR100803796B1/ko not_active Expired - Fee Related
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- 2004-06-17 US US10/872,160 patent/US7378436B2/en not_active Expired - Fee Related
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2005
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| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
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