WO2001007431A3 - Benzothiophene derivatives - Google Patents

Benzothiophene derivatives Download PDF

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Publication number
WO2001007431A3
WO2001007431A3 PCT/US2000/016334 US0016334W WO0107431A3 WO 2001007431 A3 WO2001007431 A3 WO 2001007431A3 US 0016334 W US0016334 W US 0016334W WO 0107431 A3 WO0107431 A3 WO 0107431A3
Authority
WO
WIPO (PCT)
Prior art keywords
benzothiophene derivatives
benzothiophene
derivatives
glur6
disorders
Prior art date
Application number
PCT/US2000/016334
Other languages
French (fr)
Other versions
WO2001007431A2 (en
Inventor
Stephen Richard Baker
David Bleakman
Fernandez Carmen Dominguez
Esteban Almudena Rubio
Manzanares Esteban Dominguez
Original Assignee
Lilly Co Eli
Stephen Richard Baker
David Bleakman
Fernandez Carmen Dominguez
Esteban Almudena Rubio
Manzanares Esteban Dominguez
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 Lilly Co Eli, Stephen Richard Baker, David Bleakman, Fernandez Carmen Dominguez, Esteban Almudena Rubio, Manzanares Esteban Dominguez filed Critical Lilly Co Eli
Priority to AU60505/00A priority Critical patent/AU6050500A/en
Publication of WO2001007431A2 publication Critical patent/WO2001007431A2/en
Publication of WO2001007431A3 publication Critical patent/WO2001007431A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/58—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compounds of formula (I) in which R1, R2, Y, L and Z have the meanings given in the specification are GluR6 antagonists useful for the treatment of disorders of the central nervous system.
PCT/US2000/016334 1999-07-21 2000-07-18 Benzothiophene derivatives WO2001007431A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU60505/00A AU6050500A (en) 1999-07-21 2000-07-18 Benzothiophene derivatives

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99500123.7 1999-07-21
EP99500123 1999-07-21

Publications (2)

Publication Number Publication Date
WO2001007431A2 WO2001007431A2 (en) 2001-02-01
WO2001007431A3 true WO2001007431A3 (en) 2001-08-16

Family

ID=8242511

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/016334 WO2001007431A2 (en) 1999-07-21 2000-07-18 Benzothiophene derivatives

Country Status (2)

Country Link
AU (1) AU6050500A (en)
WO (1) WO2001007431A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1150176C (en) * 2002-05-22 2004-05-19 上海医药工业研究院 Aralkylone pipeazine derivative and its application
DE102008042061A1 (en) 2008-09-12 2010-03-18 Basf Se Process for the preparation of geometric shaped catalyst bodies
DE102008042064A1 (en) 2008-09-12 2010-03-18 Basf Se Process for the preparation of geometric shaped catalyst bodies
JP5246715B2 (en) * 2009-01-27 2013-07-24 独立行政法人科学技術振興機構 Protein crosslinking inhibitors and uses thereof
AU2011202542A1 (en) * 2010-07-14 2012-02-02 Indian Institute Of Science Benzothiophene carboxamide compounds, composition and applications thereof
CA2839438C (en) * 2011-06-15 2020-08-04 Nono Inc. Agents and methods for treating ischemic and other diseases
KR20230038125A (en) * 2021-09-10 2023-03-17 주식회사 프롬바이오 Heteroaryl derivatives as STAT3 inhibitor, and uses thereof

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3646047A (en) * 1970-02-02 1972-02-29 American Cyanamid Co Certain benzo(b)thiophene-2-carboxamide derivatives
US3734915A (en) * 1970-02-02 1973-05-22 American Cyanamid Co N-(-(4-phenyl-1-piperazinyl)alkyl)benzo(b)thiophene or benzofuran-2-carboxamides
US4018893A (en) * 1974-05-28 1977-04-19 Schering Corporation Methods for treating microbial infections
WO1996015792A1 (en) * 1994-11-17 1996-05-30 Molecular Geriatrics Corporation Methods for treating or preventing alzheimer's disease using substituted 1-aryl-3-piperazin-1'-yl propanones
WO1996016052A2 (en) * 1994-11-17 1996-05-30 Molecular Geriatrics Corporation Certain substituted 1-aryl-3-piperazin-1'-yl propanones
WO1999002516A1 (en) * 1997-07-08 1999-01-21 Vita-Invest, S.A. Compounds derived from thophene and benzothiophene, and related utilisation and composition

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3646047A (en) * 1970-02-02 1972-02-29 American Cyanamid Co Certain benzo(b)thiophene-2-carboxamide derivatives
US3734915A (en) * 1970-02-02 1973-05-22 American Cyanamid Co N-(-(4-phenyl-1-piperazinyl)alkyl)benzo(b)thiophene or benzofuran-2-carboxamides
US4018893A (en) * 1974-05-28 1977-04-19 Schering Corporation Methods for treating microbial infections
WO1996015792A1 (en) * 1994-11-17 1996-05-30 Molecular Geriatrics Corporation Methods for treating or preventing alzheimer's disease using substituted 1-aryl-3-piperazin-1'-yl propanones
WO1996016052A2 (en) * 1994-11-17 1996-05-30 Molecular Geriatrics Corporation Certain substituted 1-aryl-3-piperazin-1'-yl propanones
WO1999002516A1 (en) * 1997-07-08 1999-01-21 Vita-Invest, S.A. Compounds derived from thophene and benzothiophene, and related utilisation and composition

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
ARTAMANOVA, O.S. ET AL: "Synthesis and pharmacological activity of the amides and dialkylaminoalkyl esters of 3-chlorobenzothiophene-2-carboxylic acid", FIZIOL. AKT. VESHCHESTVA, vol. 8, 1976, pages 49 - 51, XP000913616 *
DATABASE CHEMABS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002139651 *
DATABASE WPI Week 200023, Derwent World Patents Index; AN 1999-131723, XP002139652 *
RIED, W. ET AL: "Umsetzung von Säurechloriden und Chlorformamidinen mit Stickstoff-Heterocyclen", CHEMIKER ZEITUNG, vol. 105, no. 4, 1981, pages 120 - 123, XP000907078 *

Also Published As

Publication number Publication date
WO2001007431A2 (en) 2001-02-01
AU6050500A (en) 2001-02-13

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