AU2002236730B2 - Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-HT6 receptor - Google Patents

Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-HT6 receptor Download PDF

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Publication number
AU2002236730B2
AU2002236730B2 AU2002236730A AU2002236730A AU2002236730B2 AU 2002236730 B2 AU2002236730 B2 AU 2002236730B2 AU 2002236730 A AU2002236730 A AU 2002236730A AU 2002236730 A AU2002236730 A AU 2002236730A AU 2002236730 B2 AU2002236730 B2 AU 2002236730B2
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Prior art keywords
ester
methylpiperidin
acid
indol
methyl
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Ceased
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AU2002236730A
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AU2002236730A1 (en
Inventor
Sandra Ann Filla
Michael Edward Flaugh
James Ronald Gillig
Lawrence Joseph Heinz
Joseph Herman Krushinski Jr
Bin Liu
Marta Maria Pineiro-Nunez
John Mehnert Schaus
John Stanley Ward
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Eli Lilly and Co
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Eli Lilly and Co
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/08Antiepileptics; Anticonvulsants
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34Tobacco-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Mechanical Treatment Of Semiconductor (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
AU2002236730A 2001-01-30 2002-01-17 Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-HT6 receptor Ceased AU2002236730B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26499601P 2001-01-30 2001-01-30
US60/264,996 2001-01-30
PCT/US2002/000502 WO2002060871A2 (en) 2001-01-30 2002-01-17 Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-ht6 receptor

Publications (2)

Publication Number Publication Date
AU2002236730A1 AU2002236730A1 (en) 2003-02-20
AU2002236730B2 true AU2002236730B2 (en) 2006-06-15

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AU2002236730A Ceased AU2002236730B2 (en) 2001-01-30 2002-01-17 Benzenesulfonic acid indol-5-yl esters as antagonists of the 5-HT6 receptor

Country Status (12)

Country Link
US (2) US7230011B2 (enExample)
EP (1) EP1377580B1 (enExample)
JP (1) JP2004526699A (enExample)
CN (1) CN1275967C (enExample)
AT (1) ATE340795T1 (enExample)
AU (1) AU2002236730B2 (enExample)
BR (1) BR0206595A (enExample)
CA (1) CA2433351A1 (enExample)
DE (1) DE60214990T2 (enExample)
ES (1) ES2272667T3 (enExample)
MX (1) MXPA03006605A (enExample)
WO (1) WO2002060871A2 (enExample)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2222828B1 (es) * 2003-07-30 2006-04-16 Laboratorios Del Dr. Esteve, S.A. Derivados de 1-sulfonilindoles, su preparacion y su aplicacion como medicamentos.
ES2222829B1 (es) * 2003-07-30 2006-03-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 4-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
ES2222832B1 (es) * 2003-07-30 2006-02-16 Laboratorios Del Dr. Esteve, S.A. Derivados de 6-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
ES2222830B1 (es) 2003-07-30 2006-02-16 Laboratorios Del Dr. Esteve, S.A. Derivados de 7-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
ES2222827B1 (es) * 2003-07-30 2006-03-01 Laboratorios Del Dr. Esteve, S.A. Derivados de 5-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos.
MXPA06007415A (es) * 2004-01-02 2007-01-26 Suven Life Sciences Ltd Inden [2, 1a] indenos e isoindol [2,1-a] indoles novedosos.
JP2009501705A (ja) * 2005-07-05 2009-01-22 アストラゼネカ・アクチエボラーグ 新規化合物、その製造方法、中間体、医薬組成物、並びにアルツハイマー病、認知障害、統合失調症に伴う認識機能障害、肥満及びパーキンソン病のような5−ht6介在疾患の治療におけるそれらの使用
JP2009515833A (ja) * 2005-10-24 2009-04-16 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 3−ピペリジン−4−イル−インドールorl−1受容体モジュレーター
AU2007217040A1 (en) 2006-02-17 2007-08-30 Memory Pharmaceuticals Corporation Compounds having 5-HT6 receptor affinity
AR061637A1 (es) * 2006-06-26 2008-09-10 Epix Delaware Inc Composiciones y metodos de tratamiento de trastornos del snc
ATE537166T1 (de) * 2006-10-27 2011-12-15 Boehringer Ingelheim Int Piperidylpropanthiole als ccr3-modulatoren
WO2008049875A1 (en) * 2006-10-27 2008-05-02 Boehringer Ingelheim International Gmbh Novel substituted piperidyl-propane-thiols
JP2010515674A (ja) 2007-01-08 2010-05-13 スベン ライフ サイエンシズ リミティド 5−(ヘテロシクリル)アルキル−n−(アリールスルホニル)インドール化合物および5−ht6リガンドとしてのそれらの使用
CA2683124C (en) 2007-05-03 2012-09-25 Suven Life Sciences Limited Aminoalkoxy aryl sulfonamide compounds and their use as 5-ht6 ligands
AU2008315309B2 (en) 2007-10-26 2011-06-09 Suven Life Sciences Limited Amino arylsulfonamide compounds and their use as 5-HT6 ligands
US8318725B2 (en) 2008-09-17 2012-11-27 Suven Life Sciences Limited Aryl indolyl sulfonamide compounds and their use as 5-HT6 ligands
ES2424036T3 (es) 2008-09-17 2013-09-26 Suven Life Sciences Limited Compuestos de amina de arilsulfonamida y su uso como ligandos de 5-HT6
US8563567B2 (en) 2009-12-30 2013-10-22 Arqule, Inc. Substituted heterocyclic compounds
MX2012007783A (es) 2010-01-05 2012-10-03 Suven Life Sciences Ltd Compuestos sulfona que actuan como ligandos del receptor 5-ht6.
KR101250606B1 (ko) * 2011-01-24 2013-04-03 이화여자대학교 산학협력단 5-ht6 수용체 억제 작용을 갖는 신규한 벤조티아졸 및 벤즈이소티아졸유도체, 이의 제조 방법 및 이를 포함하는 약학적 조성물
AU2012321345B2 (en) * 2011-10-03 2016-03-17 The University Of Utah Research Foundation Application of 5-HT6 receptor antagonists for the alleviation of cognitive deficits of down syndrome
WO2015082499A2 (en) * 2013-12-03 2015-06-11 Iomet Pharma Ltd Pharmaceutical compound
EP3166924B1 (en) 2014-07-08 2019-02-20 Sunshine Lake Pharma Co., Ltd. Aromatic heterocyclic derivatives and pharmaceutical applications thereof
EP3250561A1 (en) * 2015-01-30 2017-12-06 Pfizer Inc Sulfonamide-subsituted indole modulators of rorc2 and methods of use thereof
EP3331530A4 (en) * 2015-08-03 2018-12-19 Raze Therapeutics Inc. Mthfd2 inhibitors and uses thereof
CN115521307B (zh) * 2022-09-30 2023-09-22 甘肃皓天医药科技有限责任公司 一种5-卤代-7-氮杂吲哚的制备方法

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RU2126399C1 (ru) * 1991-11-25 1999-02-20 Пфайзер Инк. Производные индола, замещенные индолы и способ ингибирования 5ht1 рецептора серотонина
US5521196A (en) 1994-10-05 1996-05-28 Eli Lilly And Company 5-HT1F agonists for the treatment of migraine
US5521197A (en) 1994-12-01 1996-05-28 Eli Lilly And Company 3-<1-alkylenearyl>-4-<1,2,3,6-tetrahydropyridinyl>-and 3-<1-alkylenearyl>-4-piperidinyl-1h-indoles: new 5-HT1F agonists
DE4444864A1 (de) * 1994-12-16 1996-06-20 Bayer Ag Verwendung von 5-Acyl-1,4-dihydropyridinen
PL322843A1 (en) 1995-03-20 1998-02-16 Lilly Co Eli 5-substituted 3-91,2,3,6-tetrahydropyridin-4-yl)- and 3-9piperydin-4-4-yl0-1h-indoles nevel 5-htif natagonists
AU7261196A (en) 1995-10-10 1997-04-30 Eli Lilly And Company N-{2-substituted-3-(2-aminoethyl)-1h-indol-5-yl}-amides: new 5-ht1f agonists
CA2268164A1 (en) 1996-10-08 1998-04-16 Yao-Chang Xu New serotonin 5-ht1f agonists
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ATE321751T1 (de) 1999-07-28 2006-04-15 Kirin Brewery Harnstoffderivate als ccr-3 rezeptor-inhibitoren

Also Published As

Publication number Publication date
BR0206595A (pt) 2004-07-13
MXPA03006605A (es) 2003-09-22
US7230011B2 (en) 2007-06-12
CA2433351A1 (en) 2002-08-08
WO2002060871A8 (en) 2003-12-18
US20040102481A1 (en) 2004-05-27
WO2002060871A3 (en) 2003-09-12
CN1489591A (zh) 2004-04-14
ES2272667T3 (es) 2007-05-01
EP1377580A2 (en) 2004-01-07
ATE340795T1 (de) 2006-10-15
WO2002060871A2 (en) 2002-08-08
DE60214990T2 (de) 2007-04-05
EP1377580B1 (en) 2006-09-27
JP2004526699A (ja) 2004-09-02
US20070135484A1 (en) 2007-06-14
CN1275967C (zh) 2006-09-20
DE60214990D1 (de) 2006-11-09

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