CU24001B1 - Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteína tirosina - Google Patents

Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteína tirosina

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Publication number
CU24001B1
CU24001B1 CU2010000219A CU20100219A CU24001B1 CU 24001 B1 CU24001 B1 CU 24001B1 CU 2010000219 A CU2010000219 A CU 2010000219A CU 20100219 A CU20100219 A CU 20100219A CU 24001 B1 CU24001 B1 CU 24001B1
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Cuba
Prior art keywords
methyl
quinoxalin
dimethoxy
amide
phenyl
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CU2010000219A
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English (en)
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CU20100219A7 (es
Inventor
Pascal Furet
Porta Diana Graus
Vito Guagnano
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of CU20100219A7 publication Critical patent/CU20100219A7/es
Publication of CU24001B1 publication Critical patent/CU24001B1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C07D215/06Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms having only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/42Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

La invención se refiere a los derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteína tirosina de fórmulas: [5-(4-etil-piperazin-1-il-metil)-piridin-2-il]-amida del ácido 8-(2,6-difluoro-2,5-dimetoxi-fenil)-quinoxalin-5-carboxílico; (4-dimetil-amino-metil-1H-imidazol-2-il)-amida del ácido 8-(2,6-difluoro-2,5-dimetoxi-fenil)-quinoxalin-5-carboxílico; 5-(4-metil-piperazin-1-il-metil)-piridin-2-il]-amida del ácido 8-(2-cloro-6-fluoro-3,5-dimetoxi-fenil)-quinoxalin-5-carboxílico y (5-piperazin-1-metil-piridin-2-il)-amida del ácido 8--(2-cloro-6-fluoro-3,5-dimetoxi-fenil)-quinoxalin-5-carboxílico. En particular para el tratamiento de enfermedades mediadas por proteína tirosina quinasa, tales como el cáncer.
CU2010000219A 2008-05-23 2010-11-12 Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteína tirosina CU24001B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08156846 2008-05-23
PCT/EP2009/056154 WO2009141386A1 (en) 2008-05-23 2009-05-20 Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
CU20100219A7 CU20100219A7 (es) 2011-11-15
CU24001B1 true CU24001B1 (es) 2014-06-27

Family

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Family Applications (1)

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CU2010000219A CU24001B1 (es) 2008-05-23 2010-11-12 Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteína tirosina

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US (4) US8273882B2 (es)
EP (1) EP2282995B1 (es)
JP (1) JP5351254B2 (es)
KR (1) KR101257158B1 (es)
CN (1) CN102036963B (es)
AR (1) AR071867A1 (es)
AU (1) AU2009248774B2 (es)
BR (1) BRPI0913031A2 (es)
CA (1) CA2725185C (es)
CO (1) CO6321283A2 (es)
CR (1) CR11727A (es)
CU (1) CU24001B1 (es)
DO (1) DOP2010000343A (es)
EA (1) EA021421B1 (es)
EC (1) ECSP10010627A (es)
ES (1) ES2554513T3 (es)
GE (1) GEP20125502B (es)
HN (1) HN2010002491A (es)
IL (1) IL209124A (es)
MA (1) MA32306B1 (es)
MX (1) MX2010012699A (es)
MY (1) MY155535A (es)
NI (1) NI201000190A (es)
NZ (1) NZ588511A (es)
PA (1) PA8827901A1 (es)
PE (1) PE20091955A1 (es)
SM (1) SMP201000124B (es)
SV (1) SV2010003741A (es)
TW (1) TWI448460B (es)
UA (1) UA103478C2 (es)
UY (1) UY31838A (es)
WO (1) WO2009141386A1 (es)
ZA (1) ZA201007086B (es)

Families Citing this family (108)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2010012699A (es) 2008-05-23 2010-12-07 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteina tirosina.
JP5503655B2 (ja) 2008-09-22 2014-05-28 アレイ バイオファーマ、インコーポレイテッド Trkキナーゼ阻害剤としての置換イミダゾ[1,2b]ピリダジン化合物
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
GB201007286D0 (en) 2010-04-30 2010-06-16 Astex Therapeutics Ltd New compounds
GB201020179D0 (en) 2010-11-29 2011-01-12 Astex Therapeutics Ltd New compounds
JP6076913B2 (ja) 2010-12-07 2017-02-08 ドレクセル ユニバーシティ 癌からの転移を阻害する方法
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
US9340500B2 (en) 2011-04-20 2016-05-17 Shionogi & Co., Ltd. Aromatic heterocyclic derivative having TRPV4-inhibiting activity
GB201118675D0 (en) 2011-10-28 2011-12-14 Astex Therapeutics Ltd New compounds
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
GB201118656D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118654D0 (en) 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
GB201118652D0 (en) * 2011-10-28 2011-12-07 Astex Therapeutics Ltd New compounds
US20140288073A1 (en) 2011-10-28 2014-09-25 Novartis Ag Method of Treating Gastrointestinal Stromal Tumors
SG11201402765TA (en) 2011-12-30 2014-06-27 Hanmi Pharm Ind Co Ltd THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASES
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
GB201209609D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
LT3176170T (lt) 2012-06-13 2019-04-25 Incyte Holdings Corporation Pakeisti tricikliniai junginiai, kaip fgfr inhibitoriai
BR112015000349A2 (pt) 2012-07-11 2017-06-27 Novartis Ag método de tratamento de tumores estromais gastrointestinais
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
US9663524B2 (en) 2013-03-15 2017-05-30 Celgene Car Llc Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
UA120248C2 (uk) 2013-03-15 2019-11-11 Селджен Кар Ллс Гетероарильні сполуки та їх застосування
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
GB201307577D0 (en) 2013-04-26 2013-06-12 Astex Therapeutics Ltd New compounds
EP3049442A4 (en) 2013-09-26 2017-06-28 Costim Pharmaceuticals Inc. Methods for treating hematologic cancers
AU2014360743C1 (en) 2013-12-02 2021-01-28 Chemocentryx, Inc. CCR6 compounds
MX2016008362A (es) 2013-12-23 2016-09-08 Novartis Ag Combinaciones farmaceuticas.
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
MX2016011993A (es) 2014-03-14 2016-12-09 Novartis Ag Moleculas de anticuerpo que se unen a lag-3 y usos de las mismas.
JO3512B1 (ar) 2014-03-26 2020-07-05 Astex Therapeutics Ltd مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز
HUE053653T2 (hu) 2014-03-26 2021-07-28 Astex Therapeutics Ltd FGFR inhibitor és IGF1R inhibitor kombinációi
LT3122358T (lt) 2014-03-26 2021-04-12 Astex Therapeutics Ltd. Egfr ir cmet inhibitorių deriniai, skirti vėžio gydymui
RU2658821C1 (ru) 2014-08-18 2018-06-25 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Соль моноциклического производного пиридина и ее кристалл
EP3925622A1 (en) 2014-09-13 2021-12-22 Novartis AG Combination therapies
CN107106687A (zh) 2014-10-03 2017-08-29 诺华股份有限公司 组合治疗
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
EP4245376A3 (en) 2014-10-14 2023-12-13 Novartis AG Antibody molecules to pd-l1 and uses thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JOP20200201A1 (ar) 2015-02-10 2017-06-16 Astex Therapeutics Ltd تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين
CN107438607B (zh) 2015-02-20 2021-02-05 因赛特公司 作为fgfr抑制剂的双环杂环
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
BR112017018908A2 (pt) 2015-03-10 2018-04-17 Aduro Biotech, Inc. composições e métodos para ativar a sinalização dependente do "estimulador do gene de interferon
US10478494B2 (en) 2015-04-03 2019-11-19 Astex Therapeutics Ltd FGFR/PD-1 combination therapy for the treatment of cancer
WO2017003723A1 (en) * 2015-07-01 2017-01-05 Crinetics Pharmaceuticals, Inc. Somatostatin modulators and uses thereof
SI3322706T1 (sl) 2015-07-16 2021-04-30 Array Biopharma, Inc. Substituirane pirazolo(1,5-A)piridinske spojine kot zaviralci ret-kinaze
WO2017019897A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to tim-3
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
CN108137514A (zh) * 2015-07-30 2018-06-08 百时美施贵宝公司 芳基取代的二环杂芳基化合物
HRP20220012T1 (hr) 2015-09-23 2022-04-01 Janssen Pharmaceutica Nv Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka
CN108026095B (zh) 2015-09-23 2021-07-27 詹森药业有限公司 新化合物
US10724102B2 (en) 2015-10-26 2020-07-28 Loxo Oncology, Inc. Point mutations in TRK inhibitor-resistant cancer and methods relating to the same
MX2018007423A (es) 2015-12-17 2018-11-09 Novartis Ag Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas.
BR112018070017A2 (pt) 2016-04-04 2019-02-05 Loxo Oncology Inc métodos de tratamento de cânceres pediátricos
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
CU20180125A7 (es) 2016-04-04 2019-05-03 Loxo Oncology Inc Formulaciones líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil) -pirrolidin-1-il)-pirazolo[1,5-alpirimidin-3-il)-3 hidroxipirrolidina-1-carboxamida
AU2017268371B2 (en) 2016-05-18 2020-11-19 Array Biopharma Inc. Preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-A)pyrimidin-3-y l)-3-hydroxypyrrolidine-1-carboxamide
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
EP3484881B1 (en) 2016-07-14 2020-04-29 Bristol-Myers Squibb Company Bicyclic heteroaryl substituted compounds
WO2018013776A1 (en) 2016-07-14 2018-01-18 Bristol-Myers Squibb Company Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as par4 inhibitors
CA3034875A1 (en) * 2016-08-23 2018-03-01 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of hepatocellular carcinoma
RU2019113764A (ru) * 2016-10-10 2020-11-13 Девелопмент Сентер Фор Байотекнолоджи Соединения хиноксалина в качестве ингибиторов рецепторной тирозинкиназы iii типа
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
US11168090B2 (en) 2017-01-18 2021-11-09 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyrazines as RET kinase inhibitors
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
US11267817B2 (en) 2017-05-02 2022-03-08 Drexel University Substituted pyrrolo[1,2-a]quinoxalin-4(5H)-ones as CX3CR1 antagonists
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EP3642240A1 (en) 2017-06-22 2020-04-29 Novartis AG Antibody molecules to cd73 and uses thereof
EP3658560A4 (en) 2017-07-25 2021-01-06 Crinetics Pharmaceuticals, Inc. SOMATOSTAT IN MODULATORS AND USES THEREOF
TWI812649B (zh) 2017-10-10 2023-08-21 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
CA3087578C (en) 2018-01-18 2023-08-08 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
CN111971286B (zh) 2018-01-18 2023-04-14 阿雷生物药品公司 作为RET激酶抑制剂的取代的吡咯并[2,3-d]嘧啶化合物
MX2020008610A (es) 2018-03-28 2020-09-21 Eisai R&D Man Co Ltd Agente terapeutico para carcinoma hepatocelular.
WO2019213506A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
PE20210920A1 (es) 2018-05-04 2021-05-19 Incyte Corp Formas solidas de un inhibidor de fgfr y procesos para prepararlas
UY38247A (es) 2018-05-30 2019-12-31 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
CA3224945A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
JP2022500383A (ja) 2018-09-10 2022-01-04 アレイ バイオファーマ インコーポレイテッド Retキナーゼ阻害剤としての縮合複素環式化合物
WO2020131674A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
EP3898626A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Entpd2抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
KR20220100879A (ko) 2019-10-14 2022-07-18 인사이트 코포레이션 Fgfr 저해제로서의 이환식 헤테로사이클
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN110840876A (zh) * 2019-11-18 2020-02-28 青海民族大学 圆孢蘑菇中的没食子酸在cdc25磷酸蛋白酶上应用
PE20221504A1 (es) 2019-12-04 2022-09-30 Incyte Corp Derivados de un inhibidor de fgfr
JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Fgfr阻害剤としての三環式複素環
IL294214A (en) 2019-12-27 2022-08-01 Schr?Dinger Inc Cyclic compounds and methods of using them
WO2021164742A1 (zh) * 2020-02-20 2021-08-26 广州白云山医药集团股份有限公司白云山制药总厂 喹啉类化合物
JP2023515620A (ja) * 2020-02-28 2023-04-13 リミックス セラピューティクス インコーポレイテッド スプライシングを調節するための化合物及び方法
CN111646945A (zh) * 2020-05-29 2020-09-11 凯美克(上海)医药科技有限公司 一种4-溴-2-硝基-1h-咪唑的合成方法
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー, インコーポレイテッド がんの治療のための複素環式ペリ縮環cdc7キナーゼ阻害剤
JP2024505890A (ja) 2021-01-26 2024-02-08 シュレーディンガー, インコーポレイテッド がん、自己免疫及び炎症性障害の治療に有用な三環式化合物
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
WO2023034811A1 (en) * 2021-08-30 2023-03-09 Remix Therapeutics Inc. Compounds and methods for modulating splicing
CN114605391B (zh) * 2022-02-21 2024-01-26 广州六顺生物科技股份有限公司 喹喔啉类衍生物及其制备方法和应用

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9823871D0 (en) * 1998-10-30 1998-12-23 Pharmacia & Upjohn Spa 2-Amino-thiazole derivatives, process for their preparation, and their use as antitumour agents
CN1368970A (zh) * 1999-04-06 2002-09-11 克诺尔股份有限公司 作为酪氨酸激酶抑制剂的取代的1,4-二氢茚并[1,2-c]吡唑
GB0104422D0 (en) 2001-02-22 2001-04-11 Glaxo Group Ltd Quinoline derivative
EP1408986B1 (en) 2001-05-08 2008-09-24 Yale University Proteomimetic compounds and methods
AU2002317377A1 (en) 2001-07-20 2003-03-03 Cancer Research Technology Limited Biphenyl apurinic/apyrimidinic site endonuclease inhibitors to treat cancer
JPWO2003024446A1 (ja) 2001-09-11 2004-12-24 三菱ウェルファーマ株式会社 酸化ストレス抑制剤および酸化ストレスの測定方法
WO2003024448A2 (en) 2001-09-14 2003-03-27 Methylgene, Inc. Inhibitors of histone deacetylase
ATE511840T1 (de) 2001-10-09 2011-06-15 Amgen Inc Imidazolderivate als entzündungshemmende mittel
EP1620413A2 (en) 2003-04-30 2006-02-01 Cytokinetics, Inc. Compounds, compositions, and methods
AR046845A1 (es) 2003-11-21 2005-12-28 Novartis Ag Derivados de 1h-imidazo[4,5-c]quinolina para tratamiento de enfermedades dependientes de las proteino-quinasas
AU2004297235A1 (en) * 2003-12-04 2005-06-23 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
US7501416B2 (en) 2004-02-06 2009-03-10 Bristol-Myers Squibb Company Quinoxaline compounds and methods of using them
WO2005087742A1 (en) 2004-03-08 2005-09-22 Exelixis, Inc. Metabolic kinase modulators and methods of use as pesticides
SE0401345D0 (sv) 2004-05-25 2004-05-25 Astrazeneca Ab Therapeutic compounds: Pyridine as scaffold
US20070066646A1 (en) * 2005-08-02 2007-03-22 Genmedica Therapeutics Sl Compounds for Inhibiting Copper-Containing Amine Oxidases and Uses Thereof
AR058051A1 (es) 2005-09-21 2008-01-23 Astrazeneca Ab Quinolinas de alquilnitrilo.proceso de obtencion y composiciones farmaceuticas.
TW200808739A (en) 2006-04-06 2008-02-16 Novartis Vaccines & Diagnostic Quinazolines for PDK1 inhibition
AR066879A1 (es) * 2007-06-08 2009-09-16 Novartis Ag Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus
JP4718650B2 (ja) 2007-11-26 2011-07-06 ファイザー・インク 5−lo阻害剤としてのピラゾール誘導体
US8236792B2 (en) 2008-05-23 2012-08-07 Janssen Pharmaceutica Nv Substituted pyrrolidine amides as modulators of the histamine H3 receptor
MX2010012699A (es) * 2008-05-23 2010-12-07 Novartis Ag Derivados de quinolinas y quinoxalinas como inhibidores de cinasa de proteina tirosina.
MX2010012814A (es) 2008-05-23 2010-12-20 Amira Pharmaceuticals Inc Inhibidor de proteina activadora de 5-lipoxigenasa.
AP2775A (en) 2008-05-23 2013-09-30 Wyeth Llc Triazine compounds as P13 kinase and MTOR inhibitors
NZ589062A (en) 2008-05-23 2012-06-29 Glaxo Group Ltd Tricyclic nitrogen containing compounds and their use as antibacterials

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