KR100317755B1 - 1H-인돌-3-아세트아미드sPLA2저해제 - Google Patents

1H-인돌-3-아세트아미드sPLA2저해제 Download PDF

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Publication number
KR100317755B1
KR100317755B1 KR1019940007935A KR19940007935A KR100317755B1 KR 100317755 B1 KR100317755 B1 KR 100317755B1 KR 1019940007935 A KR1019940007935 A KR 1019940007935A KR 19940007935 A KR19940007935 A KR 19940007935A KR 100317755 B1 KR100317755 B1 KR 100317755B1
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South Korea
Prior art keywords
indole
methyl
phenylmethyl
mmol
methoxy
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.)
Expired - Fee Related
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KR1019940007935A
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English (en)
Korean (ko)
Inventor
니콜라스제임스바크
로버트딜란딜라드
수잔엘리자베쓰드라하임
로버트벨허만
리차드월터쉐비츠
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일라이 릴리 앤드 캄파니
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Publication of KR100317755B1 publication Critical patent/KR100317755B1/ko
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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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
    • C07D401/06Heterocyclic 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 linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/16Central respiratory analeptics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/22Radicals 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 an aralkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/24Radicals 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 an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • C07F9/5728Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Nutrition Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1019940007935A 1993-04-16 1994-04-15 1H-인돌-3-아세트아미드sPLA2저해제 Expired - Fee Related KR100317755B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US4862993A 1993-04-16 1993-04-16
US048,629 1993-04-16
US20872194A 1994-03-15 1994-03-15
US208,721 1994-03-15

Publications (1)

Publication Number Publication Date
KR100317755B1 true KR100317755B1 (ko) 2002-08-09

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019940007935A Expired - Fee Related KR100317755B1 (ko) 1993-04-16 1994-04-15 1H-인돌-3-아세트아미드sPLA2저해제

Country Status (25)

Country Link
US (1) US5684034A (enExample)
EP (1) EP0620215B1 (enExample)
JP (1) JPH0725850A (enExample)
KR (1) KR100317755B1 (enExample)
CN (1) CN1068588C (enExample)
AT (1) ATE183503T1 (enExample)
AU (1) AU676884B2 (enExample)
BR (1) BR9401482A (enExample)
CA (1) CA2121323A1 (enExample)
CO (1) CO4230092A1 (enExample)
CZ (1) CZ289750B6 (enExample)
DE (1) DE69420068T2 (enExample)
DK (1) DK0620215T3 (enExample)
ES (1) ES2138648T3 (enExample)
FI (1) FI941767A7 (enExample)
GR (1) GR3031783T3 (enExample)
HU (1) HUT70836A (enExample)
IL (1) IL109311A0 (enExample)
NO (1) NO300732B1 (enExample)
NZ (1) NZ260298A (enExample)
PL (1) PL181319B1 (enExample)
RU (1) RU2162463C2 (enExample)
TW (1) TW268942B (enExample)
UA (1) UA44218C2 (enExample)
YU (1) YU20194A (enExample)

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IL109311A0 (en) * 1993-04-16 1994-07-31 Lilly Co Eli 1H-indole-3-acetamide sPla2 inhibitors
IL109309A (en) * 1993-04-16 2000-06-29 Lilly Co Eli 1-H-indole-3-acetic acid hydrazide SPLA2 inhibitors and pharmaceutical compositions containing them
US6252084B1 (en) 1994-03-15 2001-06-26 Eli Lilly And Company 1H-indole-3-acetamide sPLA2 inhibitors
RU2128169C1 (ru) * 1994-04-01 1999-03-27 Эли Лилли Энд Компани Iн-индол-3-глиоксиламиды, ингибирующие spla2-медиируемое выделение жирных кислот, фармацевтическая композиция
US5641800A (en) * 1994-07-21 1997-06-24 Eli Lilly And Company 1H-indole-1-functional sPLA2 inhibitors
US6214876B1 (en) 1994-07-21 2001-04-10 Eli Lilly And Company Indene-1-acetamide sPLA2 inhibitors
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US6630496B1 (en) 1996-08-26 2003-10-07 Genetics Institute Llc Inhibitors of phospholipase enzymes
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US6713645B1 (en) * 1996-10-30 2004-03-30 Eli Lilly And Company Substituted tricyclics
JP2001503055A (ja) * 1996-10-30 2001-03-06 イーライ・リリー・アンド・カンパニー 置換三環化合物群
US5919774A (en) * 1996-12-10 1999-07-06 Eli Lilly And Company Pyrroles as sPLA2 inhibitors
WO1998037069A1 (en) * 1997-02-20 1998-08-27 Shionogi & Co., Ltd. Indole dicarboxylic acid derivatives
IL137718A0 (en) * 1998-02-25 2001-10-31 Genetics Inst Inhibitors of phospholipase enzymes
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CA2322162A1 (en) * 1998-02-25 1999-09-02 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6916841B2 (en) 1998-02-25 2005-07-12 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6828344B1 (en) 1998-02-25 2004-12-07 Genetics Institute, Llc Inhibitors of phospholipase enzymes
US6500853B1 (en) 1998-02-28 2002-12-31 Genetics Institute, Llc Inhibitors of phospholipase enzymes
AU3054399A (en) 1998-03-31 1999-10-25 Shionogi & Co., Ltd. Pyrrolo(1,2-a)pyrazine sPLA2 inhibitor
IL129484A0 (en) * 1998-04-17 2000-02-29 Lilly Co Eli Substituted tricyclics
DZ2769A1 (fr) * 1998-04-17 2003-12-01 Lilly Co Eli Composés tricycliques substitués.
WO1999059999A1 (en) 1998-05-21 1999-11-25 Shionogi & Co., Ltd. PYRROLO[1,2-b]PYRIDAZINE DERIVATIVES HAVING sPLA2 INHIBITORY EFFECT
JP2002522386A (ja) 1998-08-03 2002-07-23 イーライ・リリー・アンド・カンパニー インドールsPLA2インヒビター
CA2338855A1 (en) 1998-08-03 2000-02-17 Eli Lilly And Company Indole spla2 inhibitors
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AU6004799A (en) 1998-10-14 2000-05-01 Shionogi & Co., Ltd. Remedies or preventives for ischemic reflow failure
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US6706752B1 (en) 1999-07-19 2004-03-16 Eli Lilly And Company sPLA2 inhibitors
AU6015600A (en) 1999-07-19 2001-02-05 Shionogi & Co., Ltd. Tricyclic compounds having spla2-inhibitory activities
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US6787545B1 (en) 1999-08-23 2004-09-07 Shiongi & Co., Ltd. Pyrrolotriazine derivatives having spla2-inhibitory activities
ATE347545T1 (de) * 1999-09-20 2006-12-15 Lilly Co Eli Hydroxyfunktionelle amid-1h-indolderivate aktiv als spla2 inhibitoren
US6831095B1 (en) 1999-09-20 2004-12-14 Eli Lilly And Company Hydroxyfunctional amide 1h-indole derivatives active as sPLA2 inhibitors
AU7559600A (en) * 1999-10-15 2001-04-23 Shionogi & Co., Ltd. V type and/or x type spla2 inhibitors
US6756376B1 (en) 1999-11-15 2004-06-29 Shionogi & Co., Ltd. Tricyclic azaindolizine derivatives having an sPLA2-inhibitory activities
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Also Published As

Publication number Publication date
JPH0725850A (ja) 1995-01-27
AU676884B2 (en) 1997-03-27
ES2138648T3 (es) 2000-01-16
BR9401482A (pt) 1994-10-18
HUT70836A (en) 1995-11-28
CN1068588C (zh) 2001-07-18
FI941767L (fi) 1994-10-17
RU2162463C2 (ru) 2001-01-27
YU20194A (sh) 1997-09-30
NZ260298A (en) 1996-05-28
FI941767A0 (fi) 1994-04-15
CZ289750B6 (cs) 2002-03-13
CA2121323A1 (en) 1994-10-17
GR3031783T3 (en) 2000-02-29
EP0620215B1 (en) 1999-08-18
HU9401060D0 (en) 1994-07-28
DE69420068D1 (de) 1999-09-23
EP0620215A1 (en) 1994-10-19
FI941767A7 (fi) 1994-10-17
CZ89394A3 (en) 1994-12-15
DE69420068T2 (de) 1999-12-23
TW268942B (enExample) 1996-01-21
PL181319B1 (pl) 2001-07-31
UA44218C2 (uk) 2002-02-15
IL109311A0 (en) 1994-07-31
DK0620215T3 (da) 1999-12-06
NO941361D0 (no) 1994-04-15
NO300732B1 (no) 1997-07-14
CN1098715A (zh) 1995-02-15
CO4230092A1 (es) 1995-10-19
NO941361L (no) 1994-10-17
AU5949294A (en) 1994-10-20
US5684034A (en) 1997-11-04
ATE183503T1 (de) 1999-09-15

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