WO2002050030A3 - Cycloalkylfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases - Google Patents

Cycloalkylfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases Download PDF

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Publication number
WO2002050030A3
WO2002050030A3 PCT/US2001/043187 US0143187W WO0250030A3 WO 2002050030 A3 WO2002050030 A3 WO 2002050030A3 US 0143187 W US0143187 W US 0143187W WO 0250030 A3 WO0250030 A3 WO 0250030A3
Authority
WO
WIPO (PCT)
Prior art keywords
cycloalkylfused
treatment
inflammatory diseases
spla2
inhibitors
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.)
Ceased
Application number
PCT/US2001/043187
Other languages
French (fr)
Other versions
WO2002050030A8 (en
WO2002050030A2 (en
Inventor
Douglas Wade Beight
Michael Dean Kinnick
Ho-Shen Lin
John Michael Junior Morin
Michael Enrico Richett
Daniel Jon Sall
Jason Scott Sawyer
Edward C R Smith
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
Priority to JP2002551527A priority Critical patent/JP2004518658A/en
Priority to CA002430808A priority patent/CA2430808A1/en
Priority to AU2002233928A priority patent/AU2002233928A1/en
Priority to EP01984924A priority patent/EP1349834A2/en
Priority to US10/450,741 priority patent/US6974831B2/en
Publication of WO2002050030A2 publication Critical patent/WO2002050030A2/en
Publication of WO2002050030A3 publication Critical patent/WO2002050030A3/en
Anticipated expiration legal-status Critical
Publication of WO2002050030A8 publication Critical patent/WO2002050030A8/en
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/70—[b]- or [c]-condensed containing carbocyclic rings other than six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/58—[b]- or [c]-condensed
    • C07D209/60—Naphtho [b] pyrroles; Hydrogenated naphtho [b] pyrroles
    • 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
    • C07D409/10—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 aromatic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Otolaryngology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A class of cycloalkylfused (g) indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
PCT/US2001/043187 2000-12-18 2001-12-06 Cycloalkylfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases Ceased WO2002050030A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
JP2002551527A JP2004518658A (en) 2000-12-18 2001-12-06 Novel sPLA2 inhibitors
CA002430808A CA2430808A1 (en) 2000-12-18 2001-12-06 Cycloalkylfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases
AU2002233928A AU2002233928A1 (en) 2000-12-18 2001-12-06 Cycloalkylfused (g)-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases
EP01984924A EP1349834A2 (en) 2000-12-18 2001-12-06 Cycloalkyfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases
US10/450,741 US6974831B2 (en) 2000-12-18 2001-12-06 sPLA2 inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25639700P 2000-12-18 2000-12-18
US60/256,397 2000-12-18

Publications (3)

Publication Number Publication Date
WO2002050030A2 WO2002050030A2 (en) 2002-06-27
WO2002050030A3 true WO2002050030A3 (en) 2002-09-12
WO2002050030A8 WO2002050030A8 (en) 2003-11-13

Family

ID=22972097

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/043187 Ceased WO2002050030A2 (en) 2000-12-18 2001-12-06 Cycloalkylfused [g]-indole compounds as spla2-inhibitors in the treatment of inflammatory diseases

Country Status (6)

Country Link
US (1) US6974831B2 (en)
EP (1) EP1349834A2 (en)
JP (1) JP2004518658A (en)
AU (1) AU2002233928A1 (en)
CA (1) CA2430808A1 (en)
WO (1) WO2002050030A2 (en)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2565387A1 (en) * 2004-05-03 2005-11-17 Ilypsa, Inc. Modulation of lysophosphatidylcholine and treatment of diet-induced conditions
US20110104109A1 (en) * 2005-07-13 2011-05-05 Frank Bennett Tetracyclic indole derivatives and their use for treating or preventing viral infections
JP2009514883A (en) * 2005-11-03 2009-04-09 イリプサ， インコーポレイテッド Azaindole compounds and their use as phospholipase A2 inhibitors
EP1960356A2 (en) * 2005-11-03 2008-08-27 Ilypsa, Inc. Multivalent indole compounds and use thereof as phospholipase-a2 inhibitors
EP1948604A1 (en) * 2005-11-03 2008-07-30 Ilypsa, Inc. Indole compounds having c4-acidic substituents and use thereof as phospholipase-a2 inhibitors
MX2008005661A (en) * 2005-11-03 2008-12-15 Ilypsa Inc PHOSPHOLIPASE INHIBITORS, WHICH INCLUDE MULTIVALLY PHOSPHOLIPASE INHIBITORS, AND USE OF THE SAME, WHICH INCLUDE AS PHOSPHOLIPASE INHIBITORS LOCATED IN THE LUMEN.
EP1948602A2 (en) * 2005-11-03 2008-07-30 Ilypsa, Inc. Indole compounds having c4-amide substituents and use thereof as phospholipase-a2 inhibitors
JP5055377B2 (en) 2006-12-22 2012-10-24 シェーリング コーポレイション [5,6-Ring] Ring-forming indole derivatives and methods of use thereof
JP5079818B2 (en) 2006-12-22 2012-11-21 メルク・シャープ・アンド・ドーム・コーポレーション 4,5-cyclic indole derivatives for the treatment or prevention of HCV and related viral diseases
KR20090106539A (en) * 2006-12-22 2009-10-09 쉐링 코포레이션 4,5-cyclic cyclic indole derivatives for the treatment or prevention of HCV and related viral infections
EP2195317B1 (en) * 2007-08-29 2012-01-18 Schering Corporation 2,3-substituted azaindole derivatives for treating viral infections
WO2009032124A1 (en) * 2007-08-29 2009-03-12 Schering Corporation Substituted indole derivatives and methods of use thereof
RU2010111550A (en) * 2007-08-29 2011-10-10 Шеринг Корпорейшн (US) 2,3-SUBSTITUTED INDOLIC DERIVATIVES FOR TREATING VIRAL INFECTIONS
US8765757B2 (en) * 2007-11-16 2014-07-01 Merck Sharp & Dohme Corp. 3-heterocyclic substituted indole derivatives and methods of use thereof
CN102317285A (en) * 2007-11-16 2012-01-11 先灵公司 Substituted indole derivatives of 3-amino-sulfonyl and method of use thereof
JP5580814B2 (en) * 2008-06-13 2014-08-27 メルク・シャープ・アンド・ドーム・コーポレーション Tricyclic indole derivatives and methods of use thereof
CN107233337A (en) 2009-04-29 2017-10-10 阿马里纳药物爱尔兰有限公司 Pharmaceutical composition containing EPA and cardiovascular agents and use its method
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
CN117120442A (en) * 2021-01-26 2023-11-24 薛定谔公司 Tricyclic compounds used to treat cancer, autoimmune conditions and inflammatory conditions
JP2025524002A (en) * 2022-07-22 2025-07-25 シュレーディンガー， インコーポレイテッド Cyclic compounds and methods of using same

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994021608A1 (en) * 1993-03-25 1994-09-29 The Upjohn Company Indoletetralins having dopaminergic activity
EP0620214A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetic acid hydrazide sPLA2 inhibitors
US5684034A (en) * 1993-04-16 1997-11-04 Eli Lilly And Company 1H-indole-3-acetamide sPLA2 inhibitors
WO2000010568A1 (en) * 1998-08-24 2000-03-02 Draheim Susan E Methods and compositions for treating periodontal disease with an inhibitor of secretory phospholipase a¿2?
WO2000069818A1 (en) * 1999-05-12 2000-11-23 Eli Lilly And Company MORPHOLINO-N-ETHYL ESTER DERIVATIVE OF AN INDOLE sPLA2 INHIBITOR

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6831095B1 (en) * 1999-09-20 2004-12-14 Eli Lilly And Company Hydroxyfunctional amide 1h-indole derivatives active as sPLA2 inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994021608A1 (en) * 1993-03-25 1994-09-29 The Upjohn Company Indoletetralins having dopaminergic activity
EP0620214A1 (en) * 1993-04-16 1994-10-19 Eli Lilly And Company 1H-indole-3-acetic acid hydrazide sPLA2 inhibitors
US5684034A (en) * 1993-04-16 1997-11-04 Eli Lilly And Company 1H-indole-3-acetamide sPLA2 inhibitors
WO2000010568A1 (en) * 1998-08-24 2000-03-02 Draheim Susan E Methods and compositions for treating periodontal disease with an inhibitor of secretory phospholipase a¿2?
WO2000069818A1 (en) * 1999-05-12 2000-11-23 Eli Lilly And Company MORPHOLINO-N-ETHYL ESTER DERIVATIVE OF AN INDOLE sPLA2 INHIBITOR

Also Published As

Publication number Publication date
CA2430808A1 (en) 2002-06-27
EP1349834A2 (en) 2003-10-08
US6974831B2 (en) 2005-12-13
AU2002233928A1 (en) 2002-07-01
US20040077704A1 (en) 2004-04-22
WO2002050030A8 (en) 2003-11-13
WO2002050030A2 (en) 2002-06-27
JP2004518658A (en) 2004-06-24

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