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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    • 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
    • C07D401/02Heterocyclic 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
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    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
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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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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)
  • Veterinary Medicine (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)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Anesthesiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Mechanical Treatment Of Semiconductor (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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

Family

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Family Applications (1)

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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 (https=)
EP (1) EP1377580B1 (https=)
JP (1) JP2004526699A (https=)
CN (1) CN1275967C (https=)
AT (1) ATE340795T1 (https=)
AU (1) AU2002236730B2 (https=)
BR (1) BR0206595A (https=)
CA (1) CA2433351A1 (https=)
DE (1) DE60214990T2 (https=)
ES (1) ES2272667T3 (https=)
MX (1) MXPA03006605A (https=)
WO (1) WO2002060871A2 (https=)

Families Citing this family (26)

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Publication number Priority date Publication date Assignee Title
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.
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.
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.
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.
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.
HRP20090419T1 (hr) * 2004-01-02 2009-09-30 Suven Life Sciences Limited Novi indeno[2,1a]indeni i izoindol[2,1-a]indoli
EP1910321A4 (en) * 2005-07-05 2010-09-01 Astrazeneca Ab NEW COMPOUNDS, METHOD FOR THE PRODUCTION THEREOF, INTERMEDIATE PRODUCTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE IN THE TREATMENT OF 5-HT6-MEDIATED ILLNESSES SUCH AS ALZHEIMER'S DISEASE, COGNITIVE ILLUSTRATIONS, SCHOISOPHRENIC ASSOCIATED COGNITIVE DISORDERS, OBESITAS AND PARKINSON DISEASE
AU2006306497A1 (en) * 2005-10-24 2007-05-03 Janssen Pharmaceutica, N.V. 3-piperidin-4-yl-indole ORL-1 receptor modulators
CA2637531A1 (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
EP2079731B1 (en) * 2006-10-27 2011-09-14 Boehringer Ingelheim International GmbH Novel substituted piperidyl-propane-thiols
WO2008049874A1 (en) * 2006-10-27 2008-05-02 Boehringer Ingelheim International Gmbh Piperidyl-propane-thiol ccr3 modulators
AU2007343063B2 (en) 2007-01-08 2011-02-17 Suven Life Sciences Limited 5-(Heterocyclyl)alkyl-N-(arylsulfonyl)indole compounds and their use as 5-HT6 ligands
BRPI0809873A2 (pt) 2007-05-03 2018-11-13 Suven Life Sciences Ltd "composto, processo para a preparação do composto, método para o tratamento de uma desordem do sistema nervoso central, composição farmacêutica, uso do composto, método para testar antagonistas e antagonistas com seletividade para o receptor 5-th6 e método de tratamento"
CN101835748B (zh) 2007-10-26 2012-11-14 苏文生命科学有限公司 氨基芳基磺胺化合物及其作为5-ht6配体的用途
WO2010032257A1 (en) 2008-09-17 2010-03-25 Suven Life Sciences Limited Aryl indolyl sulfonamide compounds and their use as 5-ht6 ligands
EP2346847B1 (en) 2008-09-17 2013-05-15 Suven Life Sciences Limited Aryl sulfonamide amine compounds and their use as 5-ht6 ligands
WO2011082266A2 (en) 2009-12-30 2011-07-07 Arqule, Inc. Substituted heterocyclic compounds
CA2786072C (en) 2010-01-05 2014-10-28 Suven Life Sciences Limited Sulfone compounds as 5-ht6 receptor ligands
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
US10385036B2 (en) * 2015-01-30 2019-08-20 Pfizer Inc. Sulfonamide-substituted indole modulators of RORC2 and methods of use thereof
WO2017023894A1 (en) * 2015-08-03 2017-02-09 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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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
NZ305166A (en) 1995-03-20 1998-12-23 Lilly Co Eli 5-substituted-3-(1,2,3,6-tetrahydropyridin-4-yl)- and 3-(piperidin-4-yl)-1h-indoles; preparation and medicaments
US5942536A (en) 1995-10-10 1999-08-24 Eli Lilly And Company N- 2-substituted-3-(2-aminoethyl)-1H-indol-5-YL!-Amides: new 5-HT1F agonists
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US6133287A (en) 1998-03-24 2000-10-17 Allelix Biopharmaceuticals Inc. Piperidine-indole compounds having 5-HT6 affinity
ATE375990T1 (de) * 1999-04-21 2007-11-15 Nps Allelix Corp Piperidin-indol derivate mit 5-ht6 affinität
ATE321751T1 (de) 1999-07-28 2006-04-15 Kirin Brewery Harnstoffderivate als ccr-3 rezeptor-inhibitoren

Also Published As

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

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