ES2255190T3 - Compuestos indol 2,3-sustituidos como inhibidores de cox-2. - Google Patents

Compuestos indol 2,3-sustituidos como inhibidores de cox-2.

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Publication number
ES2255190T3
ES2255190T3 ES98959082T ES98959082T ES2255190T3 ES 2255190 T3 ES2255190 T3 ES 2255190T3 ES 98959082 T ES98959082 T ES 98959082T ES 98959082 T ES98959082 T ES 98959082T ES 2255190 T3 ES2255190 T3 ES 2255190T3
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ES
Spain
Prior art keywords
alkyl
halo
alkoxy
substituted
amino
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 - Lifetime
Application number
ES98959082T
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English (en)
Inventor
Kazunari Nakao
Rodney William Stevens
Kiyoshi Kawamura
Chikara Uchida
Hiroki Koike
Stephane Caron
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.)
Pfizer Corp Belgium
Pfizer Corp SRL
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Pfizer Corp Belgium
Pfizer Corp SRL
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Application filed by Pfizer Corp Belgium, Pfizer Corp SRL filed Critical Pfizer Corp Belgium
Application granted granted Critical
Publication of ES2255190T3 publication Critical patent/ES2255190T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • 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
    • 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
    • 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
    • C07D401/10Heterocyclic 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 aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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

Abstract

Un compuesto de la siguiente fórmula (I) o las sales farmacéuticamente aceptables del mismo en la que Z es OH, alcoxi C1-6, -NR2R3 o un grupo de fórmula (II) o (III): en la que r es 1, 2, 3 ó 4, Y es un enlace directo, O, S o NR4, y W es OH o -NR2R3; Q se selecciona entre los siguientes: (a) fenilo opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre (a-1) halo, alquilo C1-4, alquilo C1-4 halo-sustituido, OH, alcoxi C1-4, alcoxi C1-4 halo-sustituido, alquil C1-4-tio, NO2, NH2, di-(alquil C1, 4)amino, alquil C1-4-amino, CN, HO-alquilo (C1-4), alcoxi C1-4-alquilo C1-4, alquil C1-4-sulfonilo, aminosulfonilo, -NH2S(O)2NR2R3, acetilo, -COOH, -C(O)O-alquilo C1-4, alquil C1, 4-sulfonilamino y cicloalquilo C3-7, (a-2) arilo o -O-(CH2)n-arilo, y el arilo o resto arilo está opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre halo, alquilo C1-4, alquilo C1-4 halo-sustituido, OH, alcoxi C1-4, alcoxi C1-4 halo-sustituido, alquil C1-4-tio, NO2, NH2, di-(alquil C1-4)amino, alquil C1-4 amino y CN, (a-3) grupo aromático monocíclico de 5 miembros opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre halo, alquilo C1-4, alquilo C 1-4 halo-sustituido, OH, alcoxi C1-4, alcoxi C1-4 halo-sustituido, alquil C1-4-tio, NO2, NH2, di-(alquil C1, 4)amino, alquil C1-4-amino y CN, (a-4) grupo aromático monocíclico de 6 miembros opcionalmente sustituido con uno, dos o tres sustituyentes seleccionados independientemente entre halo, alquilo C1-4, alquilo C1-4 halo-sustituido, OH, alcoxi C1-4, alcoxi C1-4 halo-sustituido, alquil C1-4-tio, NO2, NH2, di-(alquil C1-4)amino, alquil C1-4-amino y CN.
ES98959082T 1998-01-05 1998-12-18 Compuestos indol 2,3-sustituidos como inhibidores de cox-2. Expired - Lifetime ES2255190T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IB9800003 1998-01-05
WOPCT/IB98/00003 1998-01-05

Publications (1)

Publication Number Publication Date
ES2255190T3 true ES2255190T3 (es) 2006-06-16

Family

ID=11004645

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98959082T Expired - Lifetime ES2255190T3 (es) 1998-01-05 1998-12-18 Compuestos indol 2,3-sustituidos como inhibidores de cox-2.

Country Status (39)

Country Link
US (1) US6608070B1 (es)
EP (1) EP1045833B1 (es)
JP (1) JP3347136B2 (es)
KR (1) KR100404054B1 (es)
CN (1) CN1284064A (es)
AP (1) AP869A (es)
AR (1) AR016977A1 (es)
AT (1) ATE308519T1 (es)
AU (1) AU748107B2 (es)
BG (1) BG104643A (es)
BR (1) BR9813124A (es)
CA (1) CA2316863A1 (es)
CO (1) CO4970807A1 (es)
DE (1) DE69832200T2 (es)
DZ (1) DZ2700A1 (es)
EA (1) EA200000614A1 (es)
ES (1) ES2255190T3 (es)
GT (1) GT199800205A (es)
HN (1) HN1997000098A (es)
HR (1) HRP20000454A2 (es)
HU (1) HUP0102922A3 (es)
ID (1) ID24876A (es)
IL (1) IL136885A0 (es)
IS (1) IS5532A (es)
MA (1) MA24736A1 (es)
NO (1) NO20003451L (es)
OA (1) OA11441A (es)
PA (1) PA8466201A1 (es)
PE (1) PE20000055A1 (es)
PL (1) PL341696A1 (es)
SA (1) SA99191299A (es)
SK (1) SK9912000A3 (es)
TN (1) TNSN99001A1 (es)
TR (1) TR200001906T2 (es)
TW (1) TW436482B (es)
UY (2) UY25332A1 (es)
WO (1) WO1999035130A1 (es)
YU (1) YU41600A (es)
ZA (1) ZA9911B (es)

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US6555540B1 (en) * 1999-06-30 2003-04-29 Pfizer Inc Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
MXPA00006605A (es) 1999-07-02 2004-12-09 Pfizer Compuestos de carbonil-indol biciclicos como agentes antiinflamatorios/analgesicos.
PT1065206E (pt) * 1999-07-02 2003-01-31 Pfizer Compostos de tetrazolilalquilindole e como agentes anti-inflamatorios e analgesicos
WO2001041760A2 (en) 1999-12-08 2001-06-14 Pharmacia Corporation Cyclooxygenase-2 inhibitor compositions having rapid onset of therapeutic effect
EP1572678A4 (en) * 2002-12-19 2008-05-07 Elan Pharm Inc SUBSTITUTED N-PHENYL SULPHONAMIDES ALSBRADYKININ ANTAGONISTS
US7098231B2 (en) 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
JP4354984B2 (ja) 2003-05-07 2009-10-28 オステオロジックス エイ/エス 水溶性ストロンチウム塩を用いる軟骨/骨症状の治療
KR100795462B1 (ko) 2006-09-27 2008-01-16 한국생명공학연구원 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물
EP2114895A4 (en) * 2006-10-17 2011-06-22 Stiefel Laboratories TALARAZOLMETABOLITEN
US20120022121A1 (en) * 2007-11-29 2012-01-26 Dalton James T Indoles, derivatives and analogs thereof and uses therefor
WO2011133442A1 (en) * 2010-04-19 2011-10-27 Metabolic Solutions Development Company Novel synthesis for thiazolidinedione compounds
EP2590656B1 (en) 2010-07-07 2017-11-15 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
JP5827326B2 (ja) 2010-07-07 2015-12-02 アーデリクス,インコーポレーテッド リン酸輸送を阻害する化合物及び方法
JP5827327B2 (ja) 2010-07-07 2015-12-02 アーデリクス,インコーポレーテッド リン酸輸送を阻害する化合物及び方法
WO2012006477A1 (en) * 2010-07-07 2012-01-12 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
MX349006B (es) 2010-08-10 2017-07-06 Cirius Therapeutics Inc Nueva sintesis para compuestos de tiazolidindiona.
PL2603507T3 (pl) 2010-08-10 2016-12-30 Synteza związków tiazolidynodionu
WO2013138600A1 (en) * 2012-03-16 2013-09-19 Rosen Eliot M Radioprotector compounds
US9808443B1 (en) 2016-11-28 2017-11-07 King Saud University Cyclooxygenase inhibitors
CN111004121A (zh) * 2019-12-09 2020-04-14 南京杰运医药科技有限公司 一种4-烷氧基乙酰乙酸酯类化合物的制备方法
CN112409281B (zh) * 2020-08-20 2022-11-18 上海大学 (e)-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的合成方法
US20240165148A1 (en) 2021-03-15 2024-05-23 Saul Yedgar Hyaluronic acid-conjugated dipalmitoyl phosphatidyl ethanolamine in combination with non-steroidal anti-inflammatory drugs (nsaids) for treating or alleviating inflammatory diseases
US20240287042A1 (en) * 2021-06-10 2024-08-29 Uif (University Industry Foundation), Yonsei University Novel compound having inhibitory activity against pendrin, and pharmaceutical uses thereof
CN116262721B (zh) * 2023-01-12 2026-03-13 浙江师范大学 一种二氢吲哚衍生物及吲哚衍生物的制备方法及产品

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US5510368A (en) * 1995-05-22 1996-04-23 Merck Frosst Canada, Inc. N-benzyl-3-indoleacetic acids as antiinflammatory drugs
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CN1284064A (zh) 2001-02-14
JP3347136B2 (ja) 2002-11-20
IL136885A0 (en) 2001-06-14
DE69832200D1 (de) 2005-12-08
KR20010033859A (ko) 2001-04-25
SK9912000A3 (en) 2001-11-06
CO4970807A1 (es) 2000-11-07
AP869A (en) 2000-09-04
AU748107B2 (en) 2002-05-30
HUP0102922A2 (hu) 2001-12-28
WO1999035130A1 (en) 1999-07-15
ID24876A (id) 2000-08-31
HN1997000098A (es) 1998-12-28
PA8466201A1 (es) 2000-09-29
UY25590A1 (es) 1999-09-27
JP2002500217A (ja) 2002-01-08
EP1045833B1 (en) 2005-11-02
AR016977A1 (es) 2001-08-01
EA200000614A1 (ru) 2001-02-26
AU1500599A (en) 1999-07-26
EP1045833A1 (en) 2000-10-25
SA99191299A (ar) 2005-12-03
YU41600A (sh) 2003-08-29
KR100404054B1 (ko) 2003-11-01
TR200001906T2 (tr) 2001-01-22
ATE308519T1 (de) 2005-11-15
UY25332A1 (es) 2001-01-31
ZA9911B (en) 2000-07-04
PL341696A1 (en) 2001-04-23
IS5532A (is) 2000-06-13
DZ2700A1 (fr) 2003-09-01
DE69832200T2 (de) 2006-04-20
US6608070B1 (en) 2003-08-19
TW436482B (en) 2001-05-28
AP9801423A0 (en) 1998-12-31
MA24736A1 (fr) 1999-10-01
BG104643A (bg) 2001-02-28
GT199800205A (es) 2000-06-21
NO20003451D0 (no) 2000-07-04
BR9813124A (pt) 2000-10-10
PE20000055A1 (es) 2000-02-08
NO20003451L (no) 2000-09-01
HRP20000454A2 (en) 2001-04-30
OA11441A (en) 2004-04-27
CA2316863A1 (en) 1999-07-15
TNSN99001A1 (fr) 2005-11-10
HUP0102922A3 (en) 2003-06-30

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