JP2002508364A - セロトニン１ａ受容体に対して活性を有するアリールピペラジン - Google Patents

セロトニン１ａ受容体に対して活性を有するアリールピペラジン

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Publication number
JP2002508364A
JP2002508364A JP2000539004A JP2000539004A JP2002508364A JP 2002508364 A JP2002508364 A JP 2002508364A JP 2000539004 A JP2000539004 A JP 2000539004A JP 2000539004 A JP2000539004 A JP 2000539004A JP 2002508364 A JP2002508364 A JP 2002508364A
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JP
Japan
Prior art keywords
alkyl
hydrogen
alkoxy
cycloalkyl
phenyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
JP2000539004A
Other languages
English (en)
Japanese (ja)
Other versions
JP2002508364A5 (enExample
Inventor
アレキサンダー・グレン・ゴッドフリー
ダニエル・ティモシー・コールマン
ジョン・カニンガム・オトゥール
ヤオ−チャン・シュ
トニー・ヤンタオ・ジャン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of JP2002508364A publication Critical patent/JP2002508364A/ja
Publication of JP2002508364A5 publication Critical patent/JP2002508364A5/ja
Withdrawn legal-status Critical Current

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    • 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
    • C07D295/084—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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    • 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
    • C07D295/084—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—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 attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
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    • 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
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • 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
    • C07D295/10—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 doubly bound oxygen or sulphur atoms
    • C07D295/104—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 doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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    • 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
    • C07D295/10—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 doubly bound oxygen or sulphur atoms
    • C07D295/104—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 doubly bound oxygen or sulphur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurology (AREA)
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  • Psychiatry (AREA)
  • Epidemiology (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
JP2000539004A 1997-12-16 1998-12-08 セロトニン１ａ受容体に対して活性を有するアリールピペラジン Withdrawn JP2002508364A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US6979197P 1997-12-16 1997-12-16
US6972297P 1997-12-16 1997-12-16
US60/069,791 1997-12-16
US60/069,722 1997-12-16
US8958998P 1998-06-17 1998-06-17
US60/089,589 1998-06-17
PCT/US1998/026008 WO1999031077A1 (en) 1997-12-16 1998-12-08 Arylpiperazines having activity at the serotonin 1a receptor

Related Child Applications (1)

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JP2008120430A Division JP2008266337A (ja) 1997-12-16 2008-05-02 セロトニン１ａ受容体に対して活性を有するアリールピペラジン

Publications (2)

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JP2002508364A true JP2002508364A (ja) 2002-03-19
JP2002508364A5 JP2002508364A5 (enExample) 2005-09-15

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JP2000539004A Withdrawn JP2002508364A (ja) 1997-12-16 1998-12-08 セロトニン１ａ受容体に対して活性を有するアリールピペラジン
JP2008120430A Pending JP2008266337A (ja) 1997-12-16 2008-05-02 セロトニン１ａ受容体に対して活性を有するアリールピペラジン

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JP2008120430A Pending JP2008266337A (ja) 1997-12-16 2008-05-02 セロトニン１ａ受容体に対して活性を有するアリールピペラジン

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US (9) US6239135B1 (enExample)
EP (2) EP0924205B1 (enExample)
JP (2) JP2002508364A (enExample)
KR (1) KR100539651B1 (enExample)
CN (2) CN100355714C (enExample)
AR (1) AR017864A1 (enExample)
AT (1) ATE296296T1 (enExample)
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CA (2) CA2506802A1 (enExample)
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005538063A (ja) * 2002-06-14 2005-12-15 レコルダチ アイルランド リミティッド セロトニン作動性機能不全に起因するｃｎｓ障害の処置に有用なｎ，ｎ−二置換ジアゾシクロアルカン
JP2006502102A (ja) * 2002-06-14 2006-01-19 レコルダチ アイルランド リミティッド １−フェニルアルキル−ピペラジン

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA66370C2 (en) * 1997-12-16 2004-05-17 Lilly Co Eli Arylpiperazines having activity to setotonin 1 receptors
EP1671628B1 (en) * 1999-09-03 2012-10-03 APBI Holdings, LLC Methods of using rapid-onset selective serotonin reuptake inhibitors for treating sexual dysfunction
EP1286980A2 (en) * 2000-03-24 2003-03-05 Eli Lilly And Company Enantioselective process for preparing arylated lactones and derivatives
WO2002069973A1 (en) * 2001-03-02 2002-09-12 Sepracor, Inc. Piperidine-piperazine ligand for neurotransmitter receptors
DE10161644A1 (de) * 2001-12-14 2003-06-26 Gruenenthal Gmbh N,N'-disubstituierte Piperazin-Verbindungen
DE10161809A1 (de) * 2001-12-14 2003-06-26 Gruenenthal Gmbh Arzneimittel enthaltend N,N'-disubstituierte Piperazin-Verbindungen
DE10205721A1 (de) * 2002-02-12 2003-08-21 Biotronik Mess & Therapieg Führungsdraht und implantierbare Elektrodenleitung
US20030189215A1 (en) 2002-04-09 2003-10-09 Jong-Lam Lee Method of fabricating vertical structure leds
US7071197B2 (en) 2002-06-14 2006-07-04 Recordati S.A. N,N-disubstituted diazocycloalkanes
ITMI20021329A1 (it) * 2002-06-14 2003-12-15 Recordati Chem Pharm Nuove ossialchilammine sostituite
US20040072839A1 (en) * 2002-06-14 2004-04-15 Amedeo Leonardi 1-Phenylalkylpiperazines
WO2004019892A2 (en) * 2002-08-30 2004-03-11 Watson Pharmaceuticals, Inc. Drug delivery system for treating urinary incontinence
RU2339624C2 (ru) * 2002-12-12 2008-11-27 Авентис Фарма С.А. Производные аминоиндазолов и их применение в качестве ингибиторов киназ
GB0317370D0 (en) * 2003-07-24 2003-08-27 Synaptics Uk Ltd Magnetic calibration array
US20050165025A1 (en) * 2004-01-22 2005-07-28 Recordati Ireland Ltd. Combination therapy with 5HT 1A and 5HT 1B-receptor antagonists
EP2813225B1 (en) * 2004-09-24 2017-12-13 University of Maryland, Baltimore Method of treating organophosphorous poisoning
US9132135B2 (en) * 2004-09-24 2015-09-15 University Of Maryland, Baltimore Method of treating organophosphorous poisoning
WO2007075964A2 (en) * 2005-12-22 2007-07-05 Schering Corporation Thrombin receptor antagonists as prophylaxis to complications from cardiopulmonary surgery
US20080081067A1 (en) * 2006-10-03 2008-04-03 Gupta Manishkumar Sustained release pharmaceutical compositions of venlafaxine and process for preparation thereof
BRPI0922770A2 (pt) * 2008-12-01 2019-09-24 Procter & Gamble sistemas de perfume
CA2774039A1 (en) * 2009-11-06 2011-05-12 Aerpio Therapeutics Inc. Methods for increasing the stabilization of hypoxia inducible factor-1 alpha
US9765380B2 (en) 2010-12-08 2017-09-19 Expression Pathology, Inc. Truncated HER2 SRM/MRM assay
CN110713442A (zh) * 2018-07-11 2020-01-21 程先波 一种邻硝基苯甲醛的制备方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB230303A (enExample) * 1900-01-01
US1013907A (en) * 1910-08-22 1912-01-09 David M Neuberger Engine.
BE637389A (enExample) 1962-09-13
GB1013907A (en) * 1962-09-13 1965-12-22 Ici Ltd Alkene derivatives
GB8909209D0 (en) 1989-04-22 1989-06-07 Wyeth John & Brother Ltd Piperazine derivatives
US5382583A (en) 1989-04-22 1995-01-17 John Wyeth & Brother, Limited Piperazine derivatives
US5340812A (en) 1989-04-22 1994-08-23 John Wyeth & Brother, Limited Piperazine derivatives
GB9021535D0 (en) 1990-10-03 1990-11-14 Wyeth John & Brother Ltd Piperazine derivatives
GB2248499A (en) 1990-10-05 1992-04-08 Richard Branson Seismic data interpretation digitising scanner
MX9201991A (es) 1991-05-02 1992-11-01 Jonh Wyeth & Brother Limited Derivados de piperazina y procedimiento para su preparacion.
TW224974B (enExample) * 1991-07-02 1994-06-11 Hoffmann La Roche
CN1036395C (zh) 1992-03-19 1997-11-12 约翰韦恩兄弟有限公司 哌嗪衍生物的制备方法
GB9306103D0 (en) 1993-03-24 1993-05-12 Wyeth John & Brother Ltd Piperazine derivatives
JPH06293803A (ja) 1993-11-26 1994-10-21 Loctite Corp 光硬化性組成物
EP0661266A1 (en) 1993-12-27 1995-07-05 Toa Eiyo Ltd. Substituted cyclic amine compounds as 5HT2 antagonists
US5614523A (en) * 1995-01-17 1997-03-25 Eli Lilly And Company Compounds having effects on serotonin-related systems
GB9514384D0 (en) * 1995-07-13 1995-09-13 American Home Prod Medical treatment
UA66370C2 (en) * 1997-12-16 2004-05-17 Lilly Co Eli Arylpiperazines having activity to setotonin 1 receptors
EP1286980A2 (en) * 2000-03-24 2003-03-05 Eli Lilly And Company Enantioselective process for preparing arylated lactones and derivatives

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005538063A (ja) * 2002-06-14 2005-12-15 レコルダチ アイルランド リミティッド セロトニン作動性機能不全に起因するｃｎｓ障害の処置に有用なｎ，ｎ−二置換ジアゾシクロアルカン
JP2006502102A (ja) * 2002-06-14 2006-01-19 レコルダチ アイルランド リミティッド １−フェニルアルキル−ピペラジン

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