BRPI0407403A - compostos de isoxanol - Google Patents

compostos de isoxanol

Info

Publication number
BRPI0407403A
BRPI0407403A BRPI0407403-3A BRPI0407403A BRPI0407403A BR PI0407403 A BRPI0407403 A BR PI0407403A BR PI0407403 A BRPI0407403 A BR PI0407403A BR PI0407403 A BRPI0407403 A BR PI0407403A
Authority
BR
Brazil
Prior art keywords
alk
optionally substituted
group
formula
hydrogen
Prior art date
Application number
BRPI0407403-3A
Other languages
English (en)
Inventor
Martin James Drysdale
Brian William Dymock
Harry Finch
Paul Webb
Edward Mcdonald
Karen Elizabeth James
Kwai Ming Cheung
Thomas Peter Mathews
Original Assignee
Vernalis Cambridge Ltd
Cancer Rec Tech Ltd
Cancer Res Inst
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
Priority claimed from GB0303105A external-priority patent/GB0303105D0/en
Priority claimed from GBGB0306560.4A external-priority patent/GB0306560D0/en
Priority claimed from GB0313751A external-priority patent/GB0313751D0/en
Application filed by Vernalis Cambridge Ltd, Cancer Rec Tech Ltd, Cancer Res Inst filed Critical Vernalis Cambridge Ltd
Publication of BRPI0407403A publication Critical patent/BRPI0407403A/pt
Publication of BRPI0407403B1 publication Critical patent/BRPI0407403B1/pt

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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D495/04—Ortho-condensed systems

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Abstract

"COMPOSTOS DE ISOXAZOL". Isoxazóis da fórmula (A) ou (B) são inibidores da atividade de HSP90, e úteis para o tratamento, por exemplo, de cânceres: (A), (B) em que R~ 1~ é um grupo da fórmula (IA): -Ar¬ 1¬-(Alk¬ 1¬)~ p~-(Z)~ r~-(ALk¬ 2¬)~ s~ -Q, em que em qualquer combinação compatível Ar¬ 1¬ é um radical de arila ou heteroarila opcionalmente substituído, Alk¬ 1¬ e Alk¬ 2¬ são radicais de C~ 1~-C~ 6~ alquileno ou C~ 2~-C~ 6~ alquenileno divalentes opcionalmente substituídos, p, r e s são independentemente 0 ou 1, Z é -O-, -S-, -(C=O)-, (C=S)-, -SO~ 2~-, -C(=O)O-, -C(=O)NR¬ A¬ -C(=S)NR¬ A¬-, -SO~ 2~NR¬ A¬-, -NR¬ A¬C(=O)-,- NR¬ A¬SO~ 2~- ou -NR¬ A¬- em que R¬ A¬ é hidrogênio OU C~ 1~-C~ 6~ alquila, e Q é hidrogênio ou um radical carbocíclico ou heterocíclico opcionalmente substituido; R~ 2~ é (i) um grupo da fórmula (IA) acima ou (ii) um radical de carboxamida; ou (iii) um anel carbocíclico ou heterocíclico não-aromático em que um carbono do anel é opcionalmente substituído, e/ou um nitrogênio do anel é opcionalmente substituído por um grupo da fórmula -(Alk¬ 1¬)~ p~-(Z)~ r~-(Alk¬ 2¬)~ s~Q em que Q, Alk¬ 1¬, Alk¬ 2¬, Z, p, r e s são como definidos acima em relação ao grupo (IA); e R~ 3~ é hidrogênio, cicloalquila opcionalmente substituída, cicloalquenila, C~ 1~-C~ 6~ alquila, C~ 1~-C~ 6~ alquenila ou C~ 1~-C~ 6~ alquinila; ou um grupo carboxila, carboxamida ou éster de carboxila.
BRPI0407403-3A 2003-02-11 2004-02-09 Compostos de isoxazol e composição farmacêutica BRPI0407403B1 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB0303105.1 2003-02-11
GB0303105A GB0303105D0 (en) 2003-02-11 2003-02-11 Isoxazole compounds
GBGB0306560.4A GB0306560D0 (en) 2003-03-21 2003-03-21 Isoxazole compounds
GB0306560.4 2003-03-21
GB0313751.0 2003-06-13
GB0313751A GB0313751D0 (en) 2003-06-13 2003-06-13 Isoxazole compounds
PCT/GB2004/000506 WO2004072051A1 (en) 2003-02-11 2004-02-09 Isoxazole compounds as inhibitors of heat shock proteins

Publications (2)

Publication Number Publication Date
BRPI0407403A true BRPI0407403A (pt) 2006-10-03
BRPI0407403B1 BRPI0407403B1 (pt) 2022-07-19

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BRPI0407403-3A BRPI0407403B1 (pt) 2003-02-11 2004-02-09 Compostos de isoxazol e composição farmacêutica

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US (6) US7705027B2 (pt)
EP (1) EP1611112B1 (pt)
JP (1) JP4921162B2 (pt)
KR (1) KR101166749B1 (pt)
CN (1) CN1771235B (pt)
AU (1) AU2004210779B2 (pt)
BR (1) BRPI0407403B1 (pt)
CA (1) CA2515726C (pt)
CY (1) CY1113761T1 (pt)
DK (1) DK1611112T3 (pt)
EA (1) EA009919B1 (pt)
ES (1) ES2393483T3 (pt)
HK (1) HK1091831A1 (pt)
MX (1) MXPA05008335A (pt)
NO (1) NO335001B1 (pt)
NZ (1) NZ541479A (pt)
PT (1) PT1611112E (pt)
SI (1) SI1611112T1 (pt)
WO (1) WO2004072051A1 (pt)

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TWI252847B (en) 2001-07-10 2006-04-11 Synta Pharmaceuticals Corp Synthesis of taxol enhancers
TWI330079B (en) 2003-01-15 2010-09-11 Synta Pharmaceuticals Corp Treatment for cancers
SI1611112T1 (sl) 2003-02-11 2012-12-31 Vernalis (R&D) Limited Izoksazolne spojine kot inhibitorji vroäśinskih ĺ ok proteinov
GB0315111D0 (en) * 2003-06-27 2003-07-30 Cancer Rec Tech Ltd Substituted 5-membered ring compounds and their use
JPWO2005063222A1 (ja) 2003-12-26 2007-07-19 協和醗酵工業株式会社 Ｈｓｐ９０ファミリー蛋白質阻害剤
KR20120117948A (ko) 2004-05-28 2012-10-24 유니젠, 인크. 이핵성 효소의 강력한 저해제로서의 디아릴알칸
GB0412769D0 (en) 2004-06-08 2004-07-07 Novartis Ag Organic compounds
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