CO5560557A2 - Derivados de indol como inhibidores de cox-ii - Google Patents

Derivados de indol como inhibidores de cox-ii

Info

Publication number
CO5560557A2
CO5560557A2 CO04027740A CO04027740A CO5560557A2 CO 5560557 A2 CO5560557 A2 CO 5560557A2 CO 04027740 A CO04027740 A CO 04027740A CO 04027740 A CO04027740 A CO 04027740A CO 5560557 A2 CO5560557 A2 CO 5560557A2
Authority
CO
Colombia
Prior art keywords
alkyl
nr5r6
alkoxy
hydroxy
hydrogen
Prior art date
Application number
CO04027740A
Other languages
English (en)
Inventor
Chris Allen Broka
Jeffrey Allen Campbell
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CO5560557A2 publication Critical patent/CO5560557A2/es

Links

Classifications

    • 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
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/06Antiabortive agents; Labour repressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • 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
    • 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
    • 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
    • C07D209/32Oxygen atoms
    • C07D209/36Oxygen atoms in position 3, e.g. adrenochrome

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

1.- Un compuesto seleccionado entre el grupo de compuestos representados por la Fórmula I: donde: - A es un -CH2, -O-, -S- o -S(O) -; - Ar es un fenilo opcionalmente sustituido o un naftalenilo opcionalmente sustituido; - R1 es hidrógeno, alquilo C1-6, alcoxi C1-6, hidroxi, hidroxi-alquilo C1-6, alquiltio C1-6, halo, ciano, C(O)R5, -C(O)NR5R6, -NR5R6, -(CRAND#39R")0-3OC(O)R5, -(CRAND#39R")0-3SO2R5 y -(CRAND#39R")0-3NSO2R5, donde R5, R6, RAND#39, y R" son cada uno, independientemente, cada vez que aparecen, hidrógeno o alquilo C1-6, con la condición de que si A es -CH2-, entonces R1 no es -C(O)NR5R6; - R2 es hidrógeno, alquilo C1-6, alcoxi C1-6, hidroxi, halo, halo-alquilo C1-6, nitro, ciano, o -NR5R6; donde R5 y R6 son los definidos con anterioridad; - R3 es -SOR7, -SO2R7, o -SO2NR5R6, donde R7 es alquilo C1-6, hidroxi-alquilo C1-6, alcoxi C1-6-alquilo C1-6, o carbonil-alcoxi C1-6-alquilo C1-6; y R5 y R6 son los definidos con anterioridad; - R4 es hidrógeno o alquilo C1-6;o isómeros individuales, mezclas de isómeros o sales farmacéuticamente aceptables de los mismos.
CO04027740A 2001-09-27 2004-03-24 Derivados de indol como inhibidores de cox-ii CO5560557A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US32538901P 2001-09-27 2001-09-27

Publications (1)

Publication Number Publication Date
CO5560557A2 true CO5560557A2 (es) 2005-09-30

Family

ID=23267681

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04027740A CO5560557A2 (es) 2001-09-27 2004-03-24 Derivados de indol como inhibidores de cox-ii

Country Status (25)

Country Link
US (3) US6872744B2 (es)
EP (1) EP1438289B1 (es)
JP (1) JP4141954B2 (es)
KR (1) KR20040047862A (es)
CN (1) CN1261412C (es)
AR (1) AR036624A1 (es)
AT (1) ATE292115T1 (es)
BR (1) BR0212925A (es)
CA (1) CA2461670A1 (es)
CO (1) CO5560557A2 (es)
DE (1) DE60203529T2 (es)
DK (1) DK1438289T3 (es)
ES (1) ES2238616T3 (es)
HR (1) HRPK20040271B3 (es)
HU (1) HUP0401499A3 (es)
IL (1) IL160752A0 (es)
MX (1) MXPA04002824A (es)
NO (1) NO20041237L (es)
NZ (1) NZ531577A (es)
PL (1) PL370342A1 (es)
PT (1) PT1438289E (es)
RU (1) RU2004113111A (es)
SI (1) SI1438289T1 (es)
WO (1) WO2003029212A1 (es)
ZA (1) ZA200402360B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL370342A1 (en) * 2001-09-27 2005-05-16 F.Hoffmann-La Roche Ag Indole derivatives as cox ii inhibitors
SE0202241D0 (sv) * 2002-07-17 2002-07-17 Astrazeneca Ab Novel Compounds
US7365090B2 (en) * 2002-08-07 2008-04-29 Idenix Pharmaceuticals, Inc. Substituted phenylindoles for the treatment of HIV
CA2550091A1 (en) * 2003-12-19 2005-07-07 Elixir Pharmaceuticals, Inc. Methods of treating a disorder
EP1589016A1 (en) * 2004-04-13 2005-10-26 Cephalon France Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
US7119214B2 (en) 2004-04-13 2006-10-10 Cephalon France Thio-substituted tricyclic and bicyclic aromatic methanesulfinyl derivatives
US7423176B2 (en) 2004-04-13 2008-09-09 Cephalon, Inc. Bicyclic aromatic sulfinyl derivatives
CA2570363A1 (en) 2004-06-18 2005-12-29 Biolipox Ab Indoles useful in the treatment of inflammation
WO2006041961A1 (en) * 2004-10-05 2006-04-20 GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTHAND HUMAN SERVICES Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same
US8097623B2 (en) 2005-01-19 2012-01-17 Biolipox Ab Indoles useful in the treatment of inflammation
US7622495B2 (en) * 2006-10-03 2009-11-24 Neurim Pharmaceuticals (1991) Ltd. Substituted aryl-indole compounds and their kynurenine/kynuramine-like metabolites as therapeutic agents
JP2010509259A (ja) 2006-11-09 2010-03-25 エフ.ホフマン−ラ ロシュ アーゲー インドール及びベンゾフラン2−カルボキサミド誘導体
CN103201262B (zh) * 2010-08-20 2016-06-01 艾米拉医药股份有限公司 自分泌运动因子抑制剂及其用途
US9260416B2 (en) 2011-05-27 2016-02-16 Amira Pharmaceuticals, Inc. Heterocyclic autotaxin inhibitors and uses thereof
JP2016530209A (ja) 2013-09-17 2016-09-29 ファーマケア,インク. ビニルオートタキシン阻害剤化合物
EP3046909A4 (en) 2013-09-17 2017-03-29 Pharmakea, Inc. Heterocyclic vinyl autotaxin inhibitor compounds
JP2016531874A (ja) 2013-09-26 2016-10-13 ファーマケア,インク. オートタキシン阻害剤化合物
PT3071561T (pt) 2013-11-22 2021-06-25 Sabre Therapeutics Llc Compostos inibidores de autotaxina
EP4026549A1 (en) 2015-05-27 2022-07-13 Sabre Therapeutics LLC Autotaxin inhibitors and uses thereof
KR102241064B1 (ko) 2019-07-30 2021-04-16 부산대학교 산학협력단 신규한 인돌 유도체 및 이를 포함하는 염증성 질환 예방 또는 치료용 조성물
CN113004187B (zh) * 2021-03-16 2022-09-20 沈阳药科大学 一种具有抑制有机阴离子转运体1活性的化合物及制备方法和应用

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4654360A (en) 1984-06-01 1987-03-31 Syntex (U.S.A.) Inc. 1,2,3-trisubstituted indoles for treatment of inflammation
JPH0347123A (ja) 1989-05-05 1991-02-28 G D Searle & Co インドール―2―カルボキシレート化合物類を含有するcns疾患治療用組成物
DE4338770A1 (de) 1993-11-12 1995-05-18 Matthias Dr Lehr Indol-2-alkansäuren und ihre Derivate als Hemmstoffe der Phospholipase A¶2¶
JP2000516958A (ja) 1996-08-26 2000-12-19 ジェネティックス・インスチチュート・インコーポレーテッド ホスホリパーゼ酵素の阻害剤
WO1998051667A1 (fr) * 1997-05-16 1998-11-19 Chugai Seiyaku Kabushiki Kaisha Derives d'indole et derives de mono- et diazaindole
CA2322163A1 (en) 1998-02-25 1999-09-02 John Mckew Inhibitors of phospholipase a2
MXPA00006605A (es) * 1999-07-02 2004-12-09 Pfizer Compuestos de carbonil-indol biciclicos como agentes antiinflamatorios/analgesicos.
US6306890B1 (en) * 1999-08-30 2001-10-23 Vanderbilt University Esters derived from indolealkanols and novel amides derived from indolealkylamides that are selective COX-2 inhibitors
US6376708B1 (en) * 2000-04-11 2002-04-23 Monsanto Technology Llc Process and catalyst for dehydrogenating primary alcohols to make carboxylic acid salts
PL370342A1 (en) * 2001-09-27 2005-05-16 F.Hoffmann-La Roche Ag Indole derivatives as cox ii inhibitors
TW200400177A (en) * 2002-06-04 2004-01-01 Wyeth Corp 1-(Aminoalkyl)-3-sulfonylindole and-indazole derivatives as 5-hydroxytryptamine-6 ligands

Also Published As

Publication number Publication date
CN1261412C (zh) 2006-06-28
DK1438289T3 (da) 2005-08-08
RU2004113111A (ru) 2005-06-27
US7074939B2 (en) 2006-07-11
CN1561334A (zh) 2005-01-05
DE60203529T2 (de) 2006-03-16
IL160752A0 (en) 2004-08-31
SI1438289T1 (es) 2005-08-31
US6872744B2 (en) 2005-03-29
CA2461670A1 (en) 2003-04-10
KR20040047862A (ko) 2004-06-05
ES2238616T3 (es) 2005-09-01
PL370342A1 (en) 2005-05-16
EP1438289B1 (en) 2005-03-30
NO20041237L (no) 2004-03-24
MXPA04002824A (es) 2004-07-05
PT1438289E (pt) 2005-06-30
US7410994B2 (en) 2008-08-12
NZ531577A (en) 2005-09-30
EP1438289A1 (en) 2004-07-21
HRP20040271A2 (en) 2004-08-31
US20030130337A1 (en) 2003-07-10
WO2003029212A1 (en) 2003-04-10
DE60203529D1 (de) 2005-05-04
HUP0401499A3 (en) 2007-05-02
ATE292115T1 (de) 2005-04-15
AR036624A1 (es) 2004-09-22
US20050176803A1 (en) 2005-08-11
US20060178420A1 (en) 2006-08-10
JP4141954B2 (ja) 2008-08-27
BR0212925A (pt) 2004-10-13
HUP0401499A2 (hu) 2004-12-28
JP2005510474A (ja) 2005-04-21
HRPK20040271B3 (en) 2006-02-28
ZA200402360B (en) 2005-04-26

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