CN1319958C - 作为血清素再摄取抑制剂的苯基哌嗪衍生物 - Google Patents

作为血清素再摄取抑制剂的苯基哌嗪衍生物 Download PDF

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Publication number
CN1319958C
CN1319958C CNB028190254A CN02819025A CN1319958C CN 1319958 C CN1319958 C CN 1319958C CN B028190254 A CNB028190254 A CN B028190254A CN 02819025 A CN02819025 A CN 02819025A CN 1319958 C CN1319958 C CN 1319958C
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China
Prior art keywords
phenyl
sulfenyl
piperazine
alkyl
compound
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Expired - Lifetime
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CNB028190254A
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English (en)
Chinese (zh)
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CN1561336A (zh
Inventor
T·鲁兰
G·P·史密斯
B·邦-安德森
A·皮施尔
E·K·莫尔岑
K·安德森
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H Lundbeck AS
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H Lundbeck AS
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Publication of CN1561336A publication Critical patent/CN1561336A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • 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
    • A61P25/22—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/033—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/096—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CNB028190254A 2001-10-04 2002-10-02 作为血清素再摄取抑制剂的苯基哌嗪衍生物 Expired - Lifetime CN1319958C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200101466 2001-10-04
DKPA200101466 2001-10-04

Publications (2)

Publication Number Publication Date
CN1561336A CN1561336A (zh) 2005-01-05
CN1319958C true CN1319958C (zh) 2007-06-06

Family

ID=8160750

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB028190254A Expired - Lifetime CN1319958C (zh) 2001-10-04 2002-10-02 作为血清素再摄取抑制剂的苯基哌嗪衍生物

Country Status (38)

Country Link
US (10) US7144884B2 (enExample)
EP (2) EP1436271B3 (enExample)
JP (3) JP3896116B2 (enExample)
KR (3) KR100770194B1 (enExample)
CN (1) CN1319958C (enExample)
AR (2) AR036659A1 (enExample)
AT (2) ATE441631T1 (enExample)
AU (2) AU2002333220C1 (enExample)
BE (1) BE2014C036I2 (enExample)
BR (3) BR122012023120B8 (enExample)
CA (1) CA2462110C (enExample)
CO (1) CO5580746A2 (enExample)
CY (3) CY1107924T1 (enExample)
DE (2) DE60233608D1 (enExample)
DK (2) DK1436271T6 (enExample)
EA (2) EA011096B1 (enExample)
EG (1) EG25095A (enExample)
ES (2) ES2298425T7 (enExample)
FR (1) FR14C0033I2 (enExample)
HR (1) HRP20040220A2 (enExample)
HU (3) HU228956B1 (enExample)
IL (1) IL160655A0 (enExample)
IS (2) IS2578B (enExample)
LT (1) LTC1436271I2 (enExample)
LU (1) LU92397I2 (enExample)
ME (1) ME00039B (enExample)
MX (1) MXPA04002959A (enExample)
MY (1) MY140950A (enExample)
NL (1) NL300652I1 (enExample)
NO (3) NO326443B1 (enExample)
NZ (1) NZ531556A (enExample)
PL (2) PL209253B1 (enExample)
PT (2) PT1749818E (enExample)
RS (2) RS52865B (enExample)
SI (1) SI1436271T1 (enExample)
UA (2) UA81749C2 (enExample)
WO (1) WO2003029232A1 (enExample)
ZA (1) ZA200401583B (enExample)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
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UA81749C2 (uk) 2001-10-04 2008-02-11 Х. Луннбек А/С Фенілпіперазинові похідні як інгібітори зворотного захоплення серотоніну
GB0305575D0 (en) * 2003-03-11 2003-04-16 Glaxo Group Ltd Novel compounds
HRP20080478T3 (hr) * 2003-04-04 2009-02-28 H. Lundbeck A/S Derivati 4-(2-fenilsulfanil-fenil)-piperidina kaoinhibitori ponovne pohrane serotonina
UA81300C2 (en) * 2003-04-04 2007-12-25 Lundbeck & Co As H Derivates of 4-(2-fenilsulfanilfenil)-1,2,3,6-tetrahydropiridin as retarding agents of serotonin recapture
EA010869B1 (ru) * 2003-04-04 2008-12-30 Х. Лундбекк А/С Производные 4-(2-фенилсульфанилфенил)пиперидина в качестве ингибиторов повторного поглощения серотонина
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ZA200505031B (en) * 2003-04-04 2006-09-27 Lundbeck & Co As H 4-(2-Phenyloxyphenyl)-piperidine or -1,2,3,6-tetrahy-dropyridine derivatives as serotonin reuptake inhibitors
RS50589B (sr) 2003-12-23 2010-05-07 H. Lundbeck A/S. 2-(1h-indolilsulfanil)-benzil amin derivati kao ssri
AR052308A1 (es) * 2004-07-16 2007-03-14 Lundbeck & Co As H Derivados de 2-(1h-indolilsulfanil)-arilamina y una composicion farmaceutica que contiene al compuesto
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AR054393A1 (es) 2005-06-17 2007-06-20 Lundbeck & Co As H Derivados de benzo(b)furano y benzo(b)tiofeno, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la reabsorcion de neurotransmisores de amina biogenicos.
US7629473B2 (en) 2005-06-17 2009-12-08 H. Lundbeck A/S 2-(1H-indolylsulfanyl)-aryl amine derivatives
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JP7179035B2 (ja) * 2006-06-16 2022-11-28 ハー・ルンドベック・アクチエゼルスカベット 認識機能障害（ｃｏｇｎｉｔｉｖｅ ｉｍｐａｉｒｍｅｎｔ）を治療するための、組み合わされたセロトニン再取り込み、５－ＨＴ３および５－ＨＴ１Ａ活性を有する化合物としての１－［２－（２，４－ジメチルフェニルスルファニル）－フェニル］ピペラジン
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TW200848411A (en) * 2007-03-20 2008-12-16 Lundbeck & Co As H Novel therapeutic uses of 1-[2-(2, 4-dimethylphenylsulfanyl)phenyl]-piperazine
TWI405588B (zh) * 2007-03-20 2013-08-21 Lundbeck & Co As H ４-〔２-（４-甲苯基硫基）-苯基〕哌啶之鹽類的液體調配物
TWI432194B (zh) * 2007-03-20 2014-04-01 Lundbeck & Co As H ４-〔２-（４-甲基苯硫基）苯基〕哌啶之新穎治療用途
HRP20140044T1 (hr) * 2007-06-15 2014-02-14 H. Lundbeck A/S 4-[2-(4-metilfenilsulfanil)fenil]piperidin za lijeäśenje iritabilnog sindroma crijeva (ibs)
TW200932233A (en) * 2007-11-13 2009-08-01 Lundbeck & Co As H Therapeutic uses of compounds having combined SERT, 5-HT3 and 5-HT1a activity
AU2014200364B2 (en) * 2007-11-13 2015-09-17 H. Lundbeck A/S Therapeutic uses of compounds having combined SERT, 5-HT3 and 5-HT1A activity
TW200932225A (en) * 2007-12-14 2009-08-01 Lundbeck & Co As H 4-[2,3-difluoro-6-(2-fluoro-4-methyl-phenylsulfanyl)-phenyl]-piperidine
TW200938194A (en) * 2007-12-14 2009-09-16 Lundbeck & Co As H Therapeutic uses of compounds having affinity to the serotonin transporter, serotonin receptors and noradrenalin transporter
WO2009081259A1 (en) * 2007-12-21 2009-07-02 Pfizer Inc. Phenoxy-pyridyl derivatives
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PT2358675E (pt) 2008-11-14 2012-12-12 Theravance Inc Compostos de 4-[2-(2-fluorofenoximetil)fenil]piperidina
TW201033181A (en) * 2009-02-17 2010-09-16 Lundbeck & Co As H Purification of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine
EP2421534B1 (en) 2009-04-24 2014-09-03 H. Lundbeck A/S Liquid formulations of salts of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine
JP2013502446A (ja) 2009-08-24 2013-01-24 ハー・ルンドベック・アクチエゼルスカベット １−［２−（２，４−ジメチル−フェニルスルファニル）−フェニル］ピペラジンの新規組成物
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RU2593771C2 (ru) 2010-04-30 2016-08-10 Такеда Фармасьютикал Компани Лимитед Энтеросолюбильная таблетка
BR112012027794A2 (pt) * 2010-04-30 2016-08-02 Takeda Pharmaceutical tablete entérico
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TW201212918A (en) 2010-08-23 2012-04-01 Lundbeck & Co As H Therapeutic uses of 1-[2-(2,4-dimethyl-phenylsulfanyl)phenyl]piperazine
SI3135656T1 (sl) 2011-06-20 2019-05-31 H. Lundbeck A/S Devterirani 1-piperazino-3-fenil indani za zdravljenje shizofrenije
EP2780467B1 (en) 2011-11-14 2018-10-17 Alfasigma S.p.A. Assays and methods for selecting a treatment regimen for a subject with depression and methods for treatment
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BR112015006075B1 (pt) 2012-09-19 2022-10-04 Sandoz Ag Composto cristalino, composição farmacêutica, uso do composto cristalino, hidrato cristalino do bromidrato de vortioxetina, método para a preparação do hidrato cristalino de bromidrato de vortioxetina, método para a preparação do composto cristalino e uso do hidrato cristalino de bromidrato de vortioxetina
CN104853755B (zh) 2012-12-13 2017-08-22 H.隆德贝克有限公司 包含沃替西汀和多奈哌齐的组合物
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CN104710345B (zh) * 2013-12-17 2017-09-05 江苏恩华药业股份有限公司 用于制备4‑（2‑（4‑甲基苯基硫基））苯基哌啶的化合物、其制备方法及应用
JP6448645B2 (ja) 2013-12-20 2019-01-09 ハー・ルンドベック・アクチエゼルスカベット メランコリアの特徴を伴う抑うつ障害を処置するための、カッパ−活性を伴うオピオイド受容体拮抗薬およびボルチオキセチンの使用
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