EA200101067A1 - SUBSTITUTED BICYCLIC HETEROARYLIC COMPOUNDS AS ANTAGONISTS INTEGRINE - Google Patents

SUBSTITUTED BICYCLIC HETEROARYLIC COMPOUNDS AS ANTAGONISTS INTEGRINE

Info

Publication number
EA200101067A1
EA200101067A1 EA200101067A EA200101067A EA200101067A1 EA 200101067 A1 EA200101067 A1 EA 200101067A1 EA 200101067 A EA200101067 A EA 200101067A EA 200101067 A EA200101067 A EA 200101067A EA 200101067 A1 EA200101067 A1 EA 200101067A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bond
compounds
optionally substituted
heteroaryl
alkylene
Prior art date
Application number
EA200101067A
Other languages
Russian (ru)
Inventor
Дэвид Эдвард Кларк
Пол Роберт Иствуд
Нил Виктор Харрис
Клайв Маккарти
Эндрю Дэвид Морли
Стефен Деннис Пикетт
Original Assignee
Авентис Фарма Лимитед
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 Авентис Фарма Лимитед filed Critical Авентис Фарма Лимитед
Priority claimed from PCT/GB2000/001393 external-priority patent/WO2000061580A1/en
Publication of EA200101067A1 publication Critical patent/EA200101067A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Данное изобретение относится к физиологически активным соединениям общей формулы (I) RZet-Het-L-Ar-L-Y, в которой Het представляет необязательно замещенное, насыщенное, частично насыщенное или полностью ненасыщенное 8-10-членное бициклическое кольцо, содержащее, по меньшей мере, один гетероатом, выбранный из О, S или N; Rпредставляет необязательно замещенный арил, гетероарил, алкил, алкенил, алкинил, циклоалкил или гетероциклоалкил; Zпредставляет простую связь, алкиленовую цепь, NR, О или S(O); Lпредставляет -R-R-связку, где Rозначает алкилен, алкенилен или алкинилен, a Rозначает простую связь, циклоалкилен, гетероциклоалкилен, арилен, гетероарилдиил, -С(=Z)-NR-, -NR-C(=Z)-, -Z-, -C(=O)-, -C(=NOR)-, -NR-, NR-C(=Z)-NR-, -SO-NR-, -NR-SO-, -O-C(=O)-, -C(=O)-O-, -NR-C(=O)-О- или -O-C(=O)-NR-; Lозначает простую связь; необязательно замещенную алкиленовую, алкениленовую, алкиниленовую, циклоалкениленовую, циклоалкиленовую, гетероарилдииловую, гетероциклоалкиленовую или ариленовую связку; -[(=O)-N(R)-С(R)(R)]-связку; -Z-R-связку; -С(=O)-CH-C(=O)-связку; -R-Z-R-связку; или -L-L-L-связку; a Y представляет карбоксил или кислотный биоизостер; а также к соответствующим N-оксидам и их пролекарствам; и фармацевтически приемлемым солям и сольватам (например, гидратам) таких соединений и их N-оксидам и пролекарствам. Такие соединения обладают ценными фармацевтическими свойствами, в частности способностью регулировать взаимодействие VCAM-1 и фибронектина с интегрином VLA-4 (α4β1).Международная заявка была опубликована вместе с отчетом о международном поиске.This invention relates to physiologically active compounds of the general formula (I) RZet-Het-L-Ar-LY, in which Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8-10 membered bicyclic ring, containing at least one heteroatom selected from O, S, or N; R3 is an optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, or heterocycloalkyl; Z represents a simple bond, alkylene chain, NR, O or S (O); L represents -RR-bond, where R means alkylene, alkenylene or alkynylene, a R means simple bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryl diyl, -C (= Z) -NR-, -NR-C (= Z) -, -Z- , -C (= O) -, -C (= NOR) -, -NR-, NR-C (= Z) -NR-, -SO-NR-, -NR-SO-, -OC (= O) -, -C (= O) -O-, -NR-C (= O) -O- or -OC (= O) -NR-; Lose a simple connection; an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryl diyl, heterocycloalkylene, or arylene bond; - [(= O) -N (R) -C (R) (R)] is a bundle; -Z-R-bunch; -C (= O) -CH-C (= O) -bond; -R-Z-R-bond; or -L-L-L-bunch; a Y is carboxyl or acid bioisostere; as well as to the corresponding N-oxides and their prodrugs; and pharmaceutically acceptable salts and solvates (for example, hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular, the ability to regulate the interaction of VCAM-1 and fibronectin with VLA-4 integrin (α4β1). The international application was published along with an international search report.

EA200101067A 1999-04-12 2000-04-12 SUBSTITUTED BICYCLIC HETEROARYLIC COMPOUNDS AS ANTAGONISTS INTEGRINE EA200101067A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB9908355.2A GB9908355D0 (en) 1999-04-12 1999-04-12 Chemical compounds
US14147099P 1999-06-29 1999-06-29
PCT/GB2000/001393 WO2000061580A1 (en) 1999-04-12 2000-04-12 Substituted bicyclic heteroaryl compounds as integrin antagonists

Publications (1)

Publication Number Publication Date
EA200101067A1 true EA200101067A1 (en) 2002-04-25

Family

ID=10851398

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200101067A EA200101067A1 (en) 1999-04-12 2000-04-12 SUBSTITUTED BICYCLIC HETEROARYLIC COMPOUNDS AS ANTAGONISTS INTEGRINE

Country Status (6)

Country Link
JP (1) JP4864206B2 (en)
CR (1) CR6559A (en)
EA (1) EA200101067A1 (en)
GB (1) GB9908355D0 (en)
YU (1) YU71501A (en)
ZA (1) ZA200108302B (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006056830A (en) * 2004-08-20 2006-03-02 Dai Ichi Seiyaku Co Ltd 2-arylaminobenzoxazole derivative

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU674553B2 (en) * 1992-10-14 1997-01-02 Merck & Co., Inc. Fibrinogen receptor antagonists
CA2150550A1 (en) * 1992-12-01 1994-06-09 Melissa S. Egbertson Fibrinogen receptor antagonists
ES2161373T3 (en) * 1995-08-30 2001-12-01 Searle & Co DERIVATIVES OF META-GUANIDINA, UREA, THIOUREA OR AZACICLICO-AMINOBENZOIC ACID AS INTEGRINE ANTAGONISTS.
WO1997024119A1 (en) * 1995-12-29 1997-07-10 Smithkline Beecham Corporation Vitronectin receptor antagonists
WO1997048697A1 (en) * 1996-06-19 1997-12-24 Rhone-Poulenc Rorer Limited Substituted azabicylic compounds and their use as inhibitors of the production of tnf and cyclic amp phosphodiesterase
WO1998031359A1 (en) * 1997-01-17 1998-07-23 Merck & Co., Inc. Integrin antagonists
JP2002511462A (en) * 1998-04-10 2002-04-16 ジー・ディー・サール・アンド・カンパニー Heterocyclic glycyl β-alanine derivatives as vitronectin antagonists
DE60027700T2 (en) * 1999-02-16 2007-05-03 Aventis Pharma Ltd., West Malling BICYCLIC COMPOUNDS AND THEIR USE AS INTEGRIN RECEPTOR LIGANDS
GB9910394D0 (en) * 1999-05-05 1999-07-07 Rhone Poulenc Rorer Ltd Chemical compounds

Also Published As

Publication number Publication date
JP2002541257A (en) 2002-12-03
JP4864206B2 (en) 2012-02-01
YU71501A (en) 2005-07-19
CR6559A (en) 2008-11-25
ZA200108302B (en) 2003-03-26
GB9908355D0 (en) 1999-06-09

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