EA200000488A1 - Замена катехина на биоизостеру индазола в терапевтически активных соединениях - Google Patents

Замена катехина на биоизостеру индазола в терапевтически активных соединениях

Info

Publication number
EA200000488A1
EA200000488A1 EA200000488A EA200000488A EA200000488A1 EA 200000488 A1 EA200000488 A1 EA 200000488A1 EA 200000488 A EA200000488 A EA 200000488A EA 200000488 A EA200000488 A EA 200000488A EA 200000488 A1 EA200000488 A1 EA 200000488A1
Authority
EA
Eurasian Patent Office
Prior art keywords
activity
catechin
compounds
replacement
indicated
Prior art date
Application number
EA200000488A
Other languages
English (en)
Inventor
Энтони Марфат
Original Assignee
Пфайзер Продактс Инк.
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 Пфайзер Продактс Инк. filed Critical Пфайзер Продактс Инк.
Publication of EA200000488A1 publication Critical patent/EA200000488A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Описаны терапевтически активные соединения и типы их производных, включающие индазолсодержащие соединения, причем указанные соединения и их терапевтическая активность являются результатом непосредственной замены биоизостеры катехина на индазол у катехинсодержащего соединения, имеющего такую же терапевтическую активность, где некатехиновые заместители такие же или гомологичны до и после указанной замены и где указанные соединения включают соединение формулы (I) или (I)или его фармацевтически приемлемую соль, где в предпочтительном варианте Rпредставляет водород; Rпредставляет циклогексил и Rпредставляет этил, Rи R, каждый по отдельности и независимо, представляет водород или некатехиновые заместители указанных соединений, являющихся результатом непосредственной замены биоизостеры катехина на индазол у указанного катехинсодержащего соединения, имеющего указанную терапевтическую активность, где указанные некатехиновые заместители такие же или гомологичны до и после указанной замены, при условии, что оба из Rи Rне могут быть одновременно водородом. Указанная терапевтическая активность может включать ингибирующую холинэстеразу активность, адренергическую α-антагонистическую и β-агонистическую активность, ингибирующую кальциевые каналы активность, противоопухолевую активность и ингибирующую фосфодиэстеразу типа IV активность.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000488A 1997-11-04 1998-10-26 Замена катехина на биоизостеру индазола в терапевтически активных соединениях EA200000488A1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US6422897P 1997-11-04 1997-11-04
US6402497P 1997-11-04 1997-11-04
US6418797P 1997-11-04 1997-11-04
US6419897P 1997-11-04 1997-11-04
US6422997P 1997-11-04 1997-11-04
PCT/IB1998/001710 WO1999023077A1 (en) 1997-11-04 1998-10-26 Indazole bioisostere replacement of catechol in therapeutically active compounds

Publications (1)

Publication Number Publication Date
EA200000488A1 true EA200000488A1 (ru) 2000-10-30

Family

ID=27535645

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000488A EA200000488A1 (ru) 1997-11-04 1998-10-26 Замена катехина на биоизостеру индазола в терапевтически активных соединениях

Country Status (29)

Country Link
US (1) US6391872B1 (ru)
EP (1) EP1028946A1 (ru)
JP (1) JP2001521926A (ru)
CN (1) CN1284948A (ru)
AP (1) AP910A (ru)
AR (1) AR013746A1 (ru)
AU (1) AU754734B2 (ru)
BG (1) BG104450A (ru)
BR (1) BR9813926A (ru)
CA (1) CA2309150A1 (ru)
CZ (1) CZ20001621A3 (ru)
DZ (1) DZ2640A1 (ru)
EA (1) EA200000488A1 (ru)
HR (1) HRP20000253A2 (ru)
HU (1) HUP0004150A3 (ru)
ID (1) ID23921A (ru)
IL (1) IL135900A0 (ru)
IS (1) IS5465A (ru)
MA (1) MA26563A1 (ru)
NO (1) NO20002129L (ru)
NZ (1) NZ503918A (ru)
OA (1) OA11354A (ru)
PE (1) PE129199A1 (ru)
PL (1) PL340753A1 (ru)
SK (1) SK6252000A3 (ru)
TN (1) TNSN98200A1 (ru)
TR (1) TR200001234T2 (ru)
WO (1) WO1999023077A1 (ru)
YU (1) YU25000A (ru)

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US8017641B2 (en) 2003-03-03 2011-09-13 Array Biopharma Inc. P38 inhibitors and methods of use thereof
US8039639B2 (en) 2006-01-31 2011-10-18 Array Biopharma Inc. Kinase inhibitors and methods of use thereof

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HN2001000008A (es) 2000-01-21 2003-12-11 Inc Agouron Pharmaceuticals Compuesto de amida y composiciones farmaceuticas para inhibir proteinquinasas, y su modo de empleo
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CN100439341C (zh) 2002-12-02 2008-12-03 弗·哈夫曼-拉罗切有限公司 作为促肾上腺皮质激素释放因子拮抗剂的吲唑衍生物
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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8017641B2 (en) 2003-03-03 2011-09-13 Array Biopharma Inc. P38 inhibitors and methods of use thereof
US8518983B2 (en) 2003-03-03 2013-08-27 Array Biopharma Inc. P38 inhibitors and methods of use thereof
US8039639B2 (en) 2006-01-31 2011-10-18 Array Biopharma Inc. Kinase inhibitors and methods of use thereof
US8044083B2 (en) 2006-01-31 2011-10-25 Array Biopharma Inc. Kinase inhibitors and methods of use thereof

Also Published As

Publication number Publication date
JP2001521926A (ja) 2001-11-13
PE129199A1 (es) 1999-12-16
TR200001234T2 (tr) 2000-08-21
WO1999023077A1 (en) 1999-05-14
EP1028946A1 (en) 2000-08-23
AU9455298A (en) 1999-05-24
HRP20000253A2 (en) 2001-06-30
IL135900A0 (en) 2001-05-20
NO20002129D0 (no) 2000-04-26
OA11354A (en) 2003-12-23
CZ20001621A3 (cs) 2001-08-15
TNSN98200A1 (fr) 2005-03-15
US6391872B1 (en) 2002-05-21
HUP0004150A3 (en) 2001-08-28
AP910A (en) 2000-12-05
NO20002129L (no) 2000-07-03
DZ2640A1 (fr) 2003-03-08
MA26563A1 (fr) 2004-12-20
AP9801375A0 (en) 1998-12-31
BR9813926A (pt) 2000-09-19
BG104450A (en) 2000-12-29
AR013746A1 (es) 2001-01-10
CA2309150A1 (en) 1999-05-14
PL340753A1 (en) 2001-02-26
SK6252000A3 (en) 2001-11-06
IS5465A (is) 2000-04-19
ID23921A (id) 2000-05-25
YU25000A (sh) 2003-12-31
HUP0004150A2 (hu) 2001-05-28
NZ503918A (en) 2002-03-28
CN1284948A (zh) 2001-02-21
AU754734B2 (en) 2002-11-21

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