BRPI0720588B8 - derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase - Google Patents

derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase

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Publication number
BRPI0720588B8
BRPI0720588B8 BRPI0720588A BRPI0720588A BRPI0720588B8 BR PI0720588 B8 BRPI0720588 B8 BR PI0720588B8 BR PI0720588 A BRPI0720588 A BR PI0720588A BR PI0720588 A BRPI0720588 A BR PI0720588A BR PI0720588 B8 BRPI0720588 B8 BR PI0720588B8
Authority
BR
Brazil
Prior art keywords
preparation
quinazoline derivatives
kinase inhibitors
substituted pyrazol
pyrazol
Prior art date
Application number
BRPI0720588A
Other languages
English (en)
Inventor
Valsasina Barbara
Posteri Helena
Beria Italo
Gabriella Brasca Maria
Caruso Michele
Ferguson Ronald
Original Assignee
Nerviano Medical Sciences Srl
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Publication date
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Application filed by Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of BRPI0720588A2 publication Critical patent/BRPI0720588A2/pt
Publication of BRPI0720588B1 publication Critical patent/BRPI0720588B1/pt
Publication of BRPI0720588B8 publication Critical patent/BRPI0720588B8/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/135—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C40B50/14—Solid phase synthesis, i.e. wherein one or more library building blocks are bound to a solid support during library creation; Particular methods of cleavage from the solid support

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Abstract

derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase a presente invenção se refere aos derivados de pirazol-quinazolina de fórmula (i), como definido no relatório descritivo e sais farmaceuticamente aceitáveis destes, processos para a sua preparação e composições farmacêuticas compreendendo-os conforme, além do processo para a sua preparação e as composições farmacêuticas que os compre-endem. os compostos da invenção podem ser úteis nas terapias para tratamento de doenças associadas à atividade desordenada da proteína quinase, tal como o câncer.
BRPI0720588A 2006-12-21 2007-12-17 derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase BRPI0720588B8 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP06126902 2006-12-21
EP06126902.3 2006-12-21
IT06126902.3 2006-12-21
IT07118039.2 2007-10-08
EP07118039 2007-10-08
EP07118039.2 2007-10-08
PCT/EP2007/064096 WO2008074788A1 (en) 2006-12-21 2007-12-17 Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors

Publications (3)

Publication Number Publication Date
BRPI0720588A2 BRPI0720588A2 (pt) 2014-02-25
BRPI0720588B1 BRPI0720588B1 (pt) 2020-03-10
BRPI0720588B8 true BRPI0720588B8 (pt) 2021-05-25

Family

ID=39304592

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Application Number Title Priority Date Filing Date
BRPI0720588A BRPI0720588B8 (pt) 2006-12-21 2007-12-17 derivados de pirazol-quinazolina substituídos, processo para sua preparação e seu uso como inibidores da quinase

Country Status (24)

Country Link
US (1) US8614220B2 (pt)
EP (1) EP2125822B1 (pt)
JP (1) JP5498796B2 (pt)
KR (1) KR101512284B1 (pt)
AR (1) AR064608A1 (pt)
AU (1) AU2007336281B2 (pt)
BR (1) BRPI0720588B8 (pt)
CA (1) CA2673451C (pt)
CL (1) CL2007003756A1 (pt)
DK (1) DK2125822T3 (pt)
EA (1) EA017769B1 (pt)
ES (1) ES2527696T3 (pt)
HK (1) HK1136292A1 (pt)
HU (1) HUE024105T2 (pt)
IL (1) IL199323A (pt)
MX (1) MX2009006613A (pt)
NO (1) NO342675B1 (pt)
NZ (1) NZ578417A (pt)
PL (1) PL2125822T3 (pt)
PT (1) PT2125822E (pt)
SG (1) SG177911A1 (pt)
SI (1) SI2125822T1 (pt)
TW (1) TWI418560B (pt)
WO (1) WO2008074788A1 (pt)

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JP5400791B2 (ja) * 2007-12-04 2014-01-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ 置換ジヒドロプテリジン−６−オン誘導体、その製造方法及びキナーゼ阻害剤としてのその使用
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IT1395724B1 (it) * 2009-02-25 2012-10-19 Neuroscienze Pharmaness S C A R L Composti farmaceutici
AR076784A1 (es) * 2009-05-26 2011-07-06 Nerviano Medical Sciences Srl Combinacion terapeutica que comprende un inhibidor de plk1 y un agente antineoplasico
CN103626777B (zh) * 2009-07-29 2015-10-21 内尔维阿诺医学科学有限公司 Plk抑制剂的盐类
WO2012013557A1 (en) * 2010-07-30 2012-02-02 Nerviano Medical Sciences S.R.L. Isoxazolo-quinazolines as modulators of protein kinase activity
EP3567042B1 (en) * 2010-10-25 2021-07-07 G1 Therapeutics, Inc. Cdk inhibitors
JP5980225B2 (ja) 2010-12-17 2016-08-31 ナーヴィアノ メディカル サイエンシズ エス．アール．エル． キナーゼ阻害剤としての置換ピラゾロ−キナゾリン誘導体
WO2012101029A1 (en) * 2011-01-26 2012-08-02 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
ES2602791T3 (es) * 2011-01-26 2017-02-22 Nerviano Medical Sciences S.R.L. Derivados de pirrolo tricíclicos, proceso para su preparación y su uso como inhibidores de cinasa
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JP2022511282A (ja) 2018-08-26 2022-01-31 カーディフ・オンコロジー・インコーポレイテッド Ｐｌｋ１標的のリン酸化状態及びｐｌｋ１阻害剤を用いた癌の治療
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
CN113631224A (zh) * 2019-02-25 2021-11-09 凯帝夫肿瘤科技有限公司 用于抑制平滑肌的非肾上腺素能收缩和前列腺细胞增殖的onvansertib
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
WO2020223558A1 (en) 2019-05-01 2020-11-05 Incyte Corporation Tricyclic amine compounds as cdk2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
KR20220064369A (ko) 2019-08-14 2022-05-18 인사이트 코포레이션 Cdk2 저해제로서의 이미다졸릴 피리디미딘일아민 화합물
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KR102313753B1 (ko) * 2020-03-27 2021-10-19 (주) 업테라 Plk1의 선택적 분해를 유도하는 바닐린 유도체 화합물
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
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