EA200000614A1 - 2,3-замещенные соединения индола в качестве ингибиторов сох-2 - Google Patents

2,3-замещенные соединения индола в качестве ингибиторов сох-2

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Publication number
EA200000614A1
EA200000614A1 EA200000614A EA200000614A EA200000614A1 EA 200000614 A1 EA200000614 A1 EA 200000614A1 EA 200000614 A EA200000614 A EA 200000614A EA 200000614 A EA200000614 A EA 200000614A EA 200000614 A1 EA200000614 A1 EA 200000614A1
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Eurasian Patent Office
Prior art keywords
alkyl
halogen
optionally substituted
substituted
alkoxy
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EA200000614A
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English (en)
Inventor
Казунари Накао
Родни Уильям Стивенз
Кийоси Кавамура
Тикара Утида
Хироки Коике
Стефан Карон
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Пфайзер Инк.
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Application filed by Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of EA200000614A1 publication Critical patent/EA200000614A1/ru

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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
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    • 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

Данное изобретение относится к соединению формулы (I) или его фармацевтически приемлемым солям, где Z представляет OH, Cалкокси, -NRRили гетероцикл; Q выбран из следующего: (a) необязательно замещенного фенила, (b) необязательно замещенной 6-членной моноциклической ароматической группы, содержащей один, два, три или четыре атома азота; (c) необязательно замещенной 5-членной моноциклической ароматической группы, содержащей один гетероатом, выбранный из O, S и N, и необязательно содержащей один, два или три атома азота в дополнение к указанному гетероатому, (d) необязательно замещенного Cциклоалкила и (e) необязательно замещенного бензоконденсированного гетероцикла; Rпредставляет водород, Cалкил или галоген; Rи Rнезависимо представляют H, OH, Cалкокси, Cалкил или Cалкил, замещенный галогеном, OH, Cалкокси или CN; X независимо выбран из H, галогена, Cалкила, галогензамещенного Cалкила, OH, Cалкокси, галогензамещенного Cалкокси, Cалкилтио, NO, NH, ди-(Cалкил)амино, Cалкиламино и CN; и n равно 0, 1, 2, 3 или 4. Изобретение также относится к фармацевтической композиции, которая может использоваться при лечении болезненного состояния, которое включает простагландины в качестве патогенов.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000614A 1998-01-05 1998-12-18 2,3-замещенные соединения индола в качестве ингибиторов сох-2 EA200000614A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IB9800003 1998-01-05
PCT/IB1998/002065 WO1999035130A1 (en) 1998-01-05 1998-12-18 2,3-substituted indole compounds as cox-2 inhibitors

Publications (1)

Publication Number Publication Date
EA200000614A1 true EA200000614A1 (ru) 2001-02-26

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ID=11004645

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000614A EA200000614A1 (ru) 1998-01-05 1998-12-18 2,3-замещенные соединения индола в качестве ингибиторов сох-2

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

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US6555540B1 (en) * 1999-06-30 2003-04-29 Pfizer Inc Combinations of aldose reductase inhibitors and selective cyclooxygenase-2 inhibitors
ATE225785T1 (de) * 1999-07-02 2002-10-15 Pfizer Tetrazolylalkyl-indolderivate als entzündungshemmende und analgetische mittel
MXPA00006605A (es) 1999-07-02 2004-12-09 Pfizer Compuestos de carbonil-indol biciclicos como agentes antiinflamatorios/analgesicos.
AU2003299757A1 (en) * 2002-12-19 2004-07-14 Elan Pharmaceuticals Inc. Substituted n-phenyl sulfonamide bradykinin 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
EP2266585B1 (en) 2003-05-07 2013-06-26 Osteologix A/S Water-soluble strontium salts for use in treatment of cartilage and/or bone conditions
KR100795462B1 (ko) * 2006-09-27 2008-01-16 한국생명공학연구원 인돌 유도체, 이의 제조방법 및 이를 유효성분으로함유하는 대사성 질환 예방 및 치료용 약학적 조성물
CN101611016B (zh) * 2006-10-17 2012-01-25 斯蒂菲尔实验室公司 他拉罗唑代谢物
US20120022121A1 (en) * 2007-11-29 2012-01-26 Dalton James T Indoles, derivatives and analogs thereof and uses therefor
KR101781665B1 (ko) * 2010-04-19 2017-09-25 씨리우스 테라퓨틱스, 엘엘씨 티아졸리딘디온 화합물을 위한 신규한 합성법
EP2590510B1 (en) 2010-07-07 2016-09-28 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
WO2012054110A2 (en) 2010-07-07 2012-04-26 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590655B1 (en) 2010-07-07 2015-06-24 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
EP2590965B1 (en) 2010-07-07 2016-04-20 Ardelyx, Inc. Compounds and methods for inhibiting phosphate transport
PL2603507T3 (pl) 2010-08-10 2016-12-30 Synteza związków tiazolidynodionu
KR20130099034A (ko) 2010-08-10 2013-09-05 메타볼릭 솔루션스 디벨롭먼트 컴퍼니, 엘엘씨 티아졸리딘디온 화합물의 신규한 합성법
US10266490B2 (en) * 2012-03-16 2019-04-23 Georgetown University 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
IL305573A (en) 2021-03-15 2023-10-01 Saul Yedgar Hyaluronic acid conjugated with dipalmitoyl phosphatidyl ethanolamine in combination with non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment or suppression of inflammatory diseases

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US5510368A (en) * 1995-05-22 1996-04-23 Merck Frosst Canada, Inc. N-benzyl-3-indoleacetic acids as antiinflammatory drugs
US5604253A (en) * 1995-05-22 1997-02-18 Merck Frosst Canada, Inc. N-benzylindol-3-yl propanoic acid derivatives as cyclooxygenase inhibitors
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Also Published As

Publication number Publication date
AR016977A1 (es) 2001-08-01
TR200001906T2 (tr) 2001-01-22
AU1500599A (en) 1999-07-26
UY25590A1 (es) 1999-09-27
TW436482B (en) 2001-05-28
CA2316863A1 (en) 1999-07-15
HN1997000098A (es) 1998-12-28
AP9801423A0 (en) 1998-12-31
MA24736A1 (fr) 1999-10-01
PE20000055A1 (es) 2000-02-08
ZA9911B (en) 2000-07-04
US6608070B1 (en) 2003-08-19
ATE308519T1 (de) 2005-11-15
AU748107B2 (en) 2002-05-30
HUP0102922A2 (hu) 2001-12-28
PL341696A1 (en) 2001-04-23
GT199800205A (es) 2000-06-21
BR9813124A (pt) 2000-10-10
NO20003451L (no) 2000-09-01
BG104643A (bg) 2001-02-28
JP3347136B2 (ja) 2002-11-20
DE69832200D1 (de) 2005-12-08
NO20003451D0 (no) 2000-07-04
HUP0102922A3 (en) 2003-06-30
UY25332A1 (es) 2001-01-31
IS5532A (is) 2000-06-13
EP1045833B1 (en) 2005-11-02
SK9912000A3 (en) 2001-11-06
IL136885A0 (en) 2001-06-14
ID24876A (id) 2000-08-31
TNSN99001A1 (fr) 2005-11-10
HRP20000454A2 (en) 2001-04-30
WO1999035130A1 (en) 1999-07-15
CO4970807A1 (es) 2000-11-07
ES2255190T3 (es) 2006-06-16
SA99191299A (ar) 2005-12-03
DZ2700A1 (fr) 2003-09-01
KR100404054B1 (ko) 2003-11-01
AP869A (en) 2000-09-04
JP2002500217A (ja) 2002-01-08
PA8466201A1 (es) 2000-09-29
DE69832200T2 (de) 2006-04-20
EP1045833A1 (en) 2000-10-25
CN1284064A (zh) 2001-02-14
KR20010033859A (ko) 2001-04-25
YU41600A (sh) 2003-08-29
OA11441A (en) 2004-04-27

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