BRPI1014572B8 - Imidazopirazinas para uso como inibidores de cinase - Google Patents

Imidazopirazinas para uso como inibidores de cinase

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Publication number
BRPI1014572B8
BRPI1014572B8 BRPI1014572A BRPI1014572A BRPI1014572B8 BR PI1014572 B8 BRPI1014572 B8 BR PI1014572B8 BR PI1014572 A BRPI1014572 A BR PI1014572A BR PI1014572 A BRPI1014572 A BR PI1014572A BR PI1014572 B8 BRPI1014572 B8 BR PI1014572B8
Authority
BR
Brazil
Prior art keywords
imidazopyrazines
kinase inhibitors
compounds
treatment
kinase
Prior art date
Application number
BRPI1014572A
Other languages
English (en)
Inventor
Oyarzabal Santamarina Julen
Pastor Fernández Joaquín
Martínez González Sonia
Original Assignee
Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii
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 Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii filed Critical Fundacion Centro Nac De Investigaciones Oncologicas Carlos Iii
Publication of BRPI1014572A2 publication Critical patent/BRPI1014572A2/pt
Publication of BRPI1014572B1 publication Critical patent/BRPI1014572B1/pt
Publication of BRPI1014572B8 publication Critical patent/BRPI1014572B8/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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61P37/08—Antiallergic agents
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    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20—Nitrogen atoms
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond

Abstract

IMIDAZOPIRAZINAS PARA USO COMO INIBIDORES DE CINASE. São fornecidos compostos da fórmula I, I Em que R1, R2, R3, R4 e R5 têm significados dados na descrição, e ésteres farmaceuticamente aceitáveis, amidas, solvatos ou sais dos mesmo, cujos compostos são úteis no tratamento de doenças nas quais inibição de uma proteína ou lipídeo cinase (por exemplo, um pi3-k e/ou mTOR) é desejada e/ou exigida, e particularmente no tratamento de câncer ou uma doença proliferativa.
BRPI1014572A 2009-04-16 2010-04-16 Imidazopirazinas para uso como inibidores de cinase BRPI1014572B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09380079 2009-04-16
EP09380079.5 2009-04-16
PCT/GB2010/000773 WO2010119264A1 (en) 2009-04-16 2010-04-16 Imidazopyrazines for use as kinase inhibitors

Publications (3)

Publication Number Publication Date
BRPI1014572A2 BRPI1014572A2 (pt) 2016-04-26
BRPI1014572B1 BRPI1014572B1 (pt) 2021-07-13
BRPI1014572B8 true BRPI1014572B8 (pt) 2022-07-19

Family

ID=40940522

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1014572A BRPI1014572B8 (pt) 2009-04-16 2010-04-16 Imidazopirazinas para uso como inibidores de cinase

Country Status (18)

Country Link
US (1) US8778935B2 (pt)
EP (1) EP2419429B1 (pt)
JP (1) JP5805623B2 (pt)
KR (2) KR20120034613A (pt)
CN (1) CN102428087B (pt)
AU (1) AU2010238361B2 (pt)
BR (1) BRPI1014572B8 (pt)
CA (1) CA2756759C (pt)
DK (1) DK2419429T3 (pt)
EA (1) EA022629B1 (pt)
ES (1) ES2475091T3 (pt)
HK (1) HK1167142A1 (pt)
IL (1) IL215297A (pt)
MX (1) MX2011010915A (pt)
NZ (1) NZ596185A (pt)
SG (1) SG175195A1 (pt)
WO (1) WO2010119264A1 (pt)
ZA (1) ZA201107717B (pt)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
WO2010108074A2 (en) 2009-03-20 2010-09-23 Amgen Inc. Inhibitors of pi3 kinase
CN102596961B (zh) 2009-10-30 2015-12-02 詹森药业有限公司 咪唑并[1，2-b]哒嗪衍生物及其作为PDE10抑制剂的用途
WO2011089400A1 (en) 2010-01-22 2011-07-28 Centro Nacional De Investigaciones Oncológicas (Cnio) Inhibitors of pi3 kinase
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
TW201200518A (en) * 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
CA2797118C (en) 2010-04-22 2021-03-30 Vertex Pharmaceuticals Incorporated Process of producing cycloalkylcarboxamido-indole compounds
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 ２－芳基咪唑并［１，２－ｂ］嗒．２－苯基咪唑并［１，２－ａ］吡啶，和２－苯基咪唑并［１，２－ａ］吡衍生物
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
BR112013033375B1 (pt) 2011-06-27 2022-05-10 Janssen Pharmaceutica N.V Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário
DK2841075T3 (da) 2012-04-26 2020-06-22 Massachusetts Gen Hospital Midler og fremgangsmåder til behandling og forebyggelse af seboroisk keratose
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途
CN102675323B (zh) 2012-06-01 2014-04-09 南京药石药物研发有限公司 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途
AU2013283426B2 (en) 2012-06-26 2018-02-22 Janssen Pharmaceutica Nv Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological or metabolic disorders
ES2607184T3 (es) 2012-07-09 2017-03-29 Janssen Pharmaceutica, N.V. Inhibidores de la enzima fosfodiesterasa 10
WO2014022728A1 (en) 2012-08-02 2014-02-06 Endo Pharmaceuticals, Inc Substituted 5 - (quinazolin - 2 - yl) pyrimidin- 2 -amine derivatives useful as pi3k/mtor inhibitors for the treatment of cancer
US10508309B2 (en) * 2013-05-17 2019-12-17 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
HUE045725T2 (hu) 2014-02-13 2020-01-28 Incyte Corp Ciklopropilaminok mint LSD1 inhibitorok
AU2015217073B2 (en) 2014-02-13 2019-08-22 Incyte Holdings Corporation Cyclopropylamines as LSD1 inhibitors
KR102447581B1 (ko) 2014-04-15 2022-09-28 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막전도 조절자 매개 질환 치료용 약제학적 조성물
WO2016007736A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
TWI687419B (zh) 2014-07-10 2020-03-11 美商英塞特公司 作為ｌｓｄ１抑制劑之咪唑并吡啶及咪唑并吡嗪
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
TWI714567B (zh) 2015-04-03 2021-01-01 美商英塞特公司 作為lsd1抑制劑之雜環化合物
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
WO2017070089A1 (en) 2015-10-19 2017-04-27 Incyte Corporation Heterocyclic compounds as immunomodulators
EP4141002A1 (en) 2015-11-19 2023-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
PL3394033T3 (pl) 2015-12-22 2021-05-31 Incyte Corporation Związki heterocykliczne jako immunomodulatory
CN105622526A (zh) * 2016-02-24 2016-06-01 湖北工业大学 一种2-氨基吡嗪衍生物的制备方法
ES2957233T3 (es) * 2016-04-15 2024-01-15 Blueprint Medicines Corp Inhibidores de quinasa tipo receptor de activina
EP3445339B1 (en) 2016-04-22 2023-08-23 Incyte Corporation Formulations of an lsd1 inhibitor
TW201808950A (zh) 2016-05-06 2018-03-16 英塞特公司 作為免疫調節劑之雜環化合物
MA45116A (fr) 2016-05-26 2021-06-02 Incyte Corp Composés hétérocycliques comme immunomodulateurs
MX2018016273A (es) 2016-06-20 2019-07-04 Incyte Corp Compuestos heterociclicos como inmunomoduladores.
EP3484866B1 (en) 2016-07-14 2022-09-07 Incyte Corporation Heterocyclic compounds as immunomodulators
MA46045A (fr) 2016-08-29 2021-04-28 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
US11136323B2 (en) 2016-12-07 2021-10-05 Beigene, Ltd. Imidazo[1,5-a]pyrazine derivatives as PI3K δ inhibitors
US10858364B2 (en) * 2016-12-21 2020-12-08 Acerta Pharma B.V. Imidazopyrazine inhibitors of Bruton's tyrosine kinase
CN110582493B (zh) 2016-12-22 2024-03-08 因赛特公司 作为免疫调节剂的苯并噁唑衍生物
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
MD3558990T2 (ro) 2016-12-22 2023-02-28 Incyte Corp Derivați tetrahidro imidazo[4,5-c]piridină ca inductori de internalizare a PD-L1
EP3558989B1 (en) 2016-12-22 2021-04-14 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
WO2019048036A1 (en) 2017-09-06 2019-03-14 Biontech Ag SUBSTITUTED IMIDAZOQUINOLINES
JP7128264B2 (ja) * 2017-09-08 2022-08-30 ベイジーン リミテッド ＰＩ３Ｋδ阻害剤としてのイミダゾ［１，５－ａ］ピラジン誘導体
SG11202003428VA (en) * 2017-10-18 2020-05-28 Incyte Corp Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors
ES2910071T3 (es) 2018-03-08 2022-05-11 Incyte Corp Compuestos de aminopirazina diol como inhibidores de PI3K-Y
SG11202009440WA (en) 2018-03-30 2020-10-29 Incyte Corp Heterocyclic compounds as immunomodulators
DK3790877T3 (da) 2018-05-11 2023-04-24 Incyte Corp Tetrahydro-imidazo[4,5-c]pyridinderivater som pd-l1-immunmodulatorer
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CA3112819A1 (en) 2018-09-13 2020-03-19 Fundacion Del Sector Publico Estatal Centro Nacional De Investigaciones Oncologicas Carlos Iii (F.S.P. Cnio) Modulation of trf1 for brain cancer treatment
EP3623009A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Modulation of trf1 for brain cancer treatment
EP3623370A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Novel trf1 modulators and analogues thereof
WO2021030162A1 (en) 2019-08-09 2021-02-18 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
US11401279B2 (en) 2019-09-30 2022-08-02 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
TW202120504A (zh) 2019-11-11 2021-06-01 美商英塞特公司 Pd-1/pd-l1 抑制劑之鹽及結晶型
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
JP2023542724A (ja) 2020-09-28 2023-10-11 ファースト・バイオセラピューティクス・インコーポレイテッド 造血前駆細胞キナーゼ１（ｈｐｋ１）阻害剤としてのインダゾールおよびその使用方法
AU2021373044A1 (en) 2020-11-06 2023-06-08 Incyte Corporation Process for making a pd-1/pd-l1 inhibitor and salts and crystalline forms thereof
TW202233615A (zh) 2020-11-06 2022-09-01 美商英塞特公司 Ｐｄ—１／ｐｄ—ｌ１抑制劑之結晶形式
WO2022099018A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Process of preparing a pd-1/pd-l1 inhibitor
WO2022140647A1 (en) * 2020-12-23 2022-06-30 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
EP4049726A1 (en) 2021-02-25 2022-08-31 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Imidazo[1,2-a]pyrazines as inhibitors of haspin and therapeutic uses thereof

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
DE69921124T2 (de) 1998-06-12 2005-11-10 Société de Conseils de Recherches et d'Applications Scientifiques S.A.S. Imidazolderivate und ihre verwendung als somatostatin rezeptorliganden
ES2282275T3 (es) 2000-08-01 2007-10-16 Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) Derivados de imidazolilo.
EP1363702A4 (en) * 2001-01-30 2007-08-22 Cytopia Pty Ltd PROCESS FOR INHIBITING KINASES
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
BR0309398A (pt) * 2002-04-19 2005-02-01 Cellular Genomics Inc Composto ou um seu sal, hidrato, solvato, forma cristalina, diastereÈmero, prodroga farmaceuticamente aceitável, ou misturas deles, composição farmacêutica, e, métodos para tratar uma condição envolvida com a cinase em um mamìfero, para tratar câncer, e para identificar uma cinase
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
WO2004022562A1 (en) 2002-09-09 2004-03-18 Cellular Genomics, Inc. 6-ARYL-IMIDAZO[1,2-a]PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
EP1543008B1 (en) * 2002-09-23 2007-11-07 Schering Corporation Imidazopyrazines as cyclin dependent kinase inhibitors
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
EP1928237A4 (en) 2005-09-02 2011-03-09 Abbott Lab NEW HETEROCYCLES BASED ON IMIDAZO
CN101300233A (zh) * 2005-09-09 2008-11-05 先灵公司 氮杂稠合的细胞周期蛋白依赖性激酶抑制剂
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
KR101422301B1 (ko) 2006-04-26 2014-07-30 에프. 호프만-라 로슈 아게 약학적 화합물
TW200808802A (en) * 2006-06-06 2008-02-16 Schering Corp Imidazopyrazines as protein kinase inhibitors
WO2008059373A1 (en) 2006-11-17 2008-05-22 Raqualia Pharma Inc. Imidazo [1, 2-a] pyrazine derivatives and their use as acid pump antagonists
AR066958A1 (es) 2007-06-14 2009-09-23 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
DE102007032349A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
US9620456B2 (en) 2007-07-12 2017-04-11 Nxp B.V. Integrated circuits on a wafer and methods for manufacturing integrated circuits

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