BR112019003504A2 - compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos - Google Patents

compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos

Info

Publication number
BR112019003504A2
BR112019003504A2 BR112019003504-4A BR112019003504A BR112019003504A2 BR 112019003504 A2 BR112019003504 A2 BR 112019003504A2 BR 112019003504 A BR112019003504 A BR 112019003504A BR 112019003504 A2 BR112019003504 A2 BR 112019003504A2
Authority
BR
Brazil
Prior art keywords
pyrrolopyrimidinone
amino
compounds
methods
compound
Prior art date
Application number
BR112019003504-4A
Other languages
English (en)
Inventor
Bates Craig
Eathiraj Sudharshan
Inagaki Hiroaki
Lapierre Jean-Marc
Momose Takayuki
Nakayama Kiyoshi
Odagiri Takashi
Ota Masahiro
Ota Yusuke
Shibata Yoshihiro
Tandon Manish
Tsunemi Tomoyuki
Original Assignee
Arqule, Inc.
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 Arqule, Inc. filed Critical Arqule, Inc.
Publication of BR112019003504A2 publication Critical patent/BR112019003504A2/pt

Links

Classifications

    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10Transferases (2.)
    • C12N9/12Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine

Abstract

o pedido refere-se a um composto de fórmula (i): (i), ou um sal, hidrato, solvato, pró-fármaco, estereoisômero, ou tautômero farmaceuticamente aceitável do mesmo, que modula a atividade de btk, uma composição farmacêutica compreendendo um composto de fórmula (i), e um método de tratar ou prevenir uma doença em que btk desempenha um papel.
BR112019003504-4A 2016-08-24 2017-08-23 compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos BR112019003504A2 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201662378871P 2016-08-24 2016-08-24
US201662378868P 2016-08-24 2016-08-24
US201662378872P 2016-08-24 2016-08-24
US62/378,871 2016-08-24
US62/378,868 2016-08-24
US62/378,872 2016-08-24
PCT/US2017/048152 WO2018039310A1 (en) 2016-08-24 2017-08-23 Amino-pyrrolopyrimidinone compounds and methods of use thereof

Publications (1)

Publication Number Publication Date
BR112019003504A2 true BR112019003504A2 (pt) 2019-05-21

Family

ID=61241149

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112019003504-4A BR112019003504A2 (pt) 2016-08-24 2017-08-23 compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos

Country Status (14)

Country Link
US (2) US11020398B2 (pt)
EP (1) EP3504213A4 (pt)
JP (1) JP2019530650A (pt)
KR (1) KR20190035925A (pt)
CN (1) CN109890821A (pt)
AU (1) AU2017315343A1 (pt)
BR (1) BR112019003504A2 (pt)
CA (1) CA3034010A1 (pt)
MX (1) MX2019002212A (pt)
PH (1) PH12019500395A1 (pt)
RU (1) RU2019108280A (pt)
SG (1) SG11201901197PA (pt)
TW (1) TW201811795A (pt)
WO (1) WO2018039310A1 (pt)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2019108280A (ru) 2016-08-24 2020-09-25 Аркьюл, Инк. Аминопирролопиримидиноновые соединения и способы их применения
CA3081751A1 (en) 2017-11-03 2019-05-09 Aclaris Therapeutics, Inc. Substituted pyrrolopyrimidine jak inhibitors and methods of making and using the same
CN109956870A (zh) * 2017-12-14 2019-07-02 南京卡文迪许生物工程技术有限公司 一种罗沙司他的合成方法及其中间体化合物
EP3774767A1 (en) * 2018-04-05 2021-02-17 Beth Israel Deaconess Medical Center, Inc. Aryl hydrocarbon receptor modulators and uses thereof
KR102545594B1 (ko) 2018-07-31 2023-06-21 록쏘 온콜로지, 인코포레이티드 (s)-5-아미노-3-(4-((5-플루오로-2-메톡시벤즈아미도)메틸)페닐)-1-(1,1,1-트리플루오로프로판-2-일)-1h-피라졸-4-카르복스아미드의 분무-건조된 분산물 및 제제
SG11202100525SA (en) 2018-08-10 2021-02-25 Aclaris Therapeutics Inc Pyrrolopyrimidine itk inhibitors
TWI820182B (zh) * 2018-08-13 2023-11-01 美商亞闊股份有限公司 四氫哌喃基胺基-吡咯并嘧啶酮化合物的固體形式
KR20220004726A (ko) 2019-05-02 2022-01-11 어클라리스 쎄라퓨틱스, 인코포레이티드 Jak 억제제로서의 치환된 피롤로피리딘
CA3137985A1 (en) * 2019-05-31 2020-12-03 Fochon Pharmaceuticals, Ltd. Substituted pyrrolo [2, 3-b] pyridine and pyrazolo [3, 4-b] pyridine derivatives as protein kinase inhibitors
US20230357248A1 (en) * 2019-11-13 2023-11-09 Medshine Discovery Inc. Pyrrolopyrimidine compound as btk inhibitor and use thereof
CN112812100B (zh) * 2019-11-18 2022-04-05 四川海思科制药有限公司 一种具有降解btk激酶的化合物及其制备方法和药学上的应用
CN112608318B (zh) * 2019-12-16 2023-09-08 成都海博为药业有限公司 一种作为蛋白质激酶抑制剂的化合物及其用途
CN111320634A (zh) * 2020-04-14 2020-06-23 浙江工业大学 一种乙酰氧取代的吡咯并[2,3-d]嘧啶衍生物的制备方法
US20230405009A1 (en) * 2020-11-05 2023-12-21 Merck Sharp & Dohme Llc Methods for treating hematologic malignancies with amino-pyrrolopyrimidinone compounds
US20240100172A1 (en) 2020-12-21 2024-03-28 Hangzhou Jijing Pharmaceutical Technology Limited Methods and compounds for targeted autophagy
US11530222B2 (en) * 2021-02-03 2022-12-20 Accutar Biotechnology Inc. Substituted pyrrolopyrimidine and pyrazolopyrimidine as Bruton's tyrosine kinase (BTK) degraders
CN112574200B (zh) * 2021-02-26 2021-06-11 安润医药科技(苏州)有限公司 Btk和/或btk的突变体c481s的小分子抑制剂
CN115028633B (zh) * 2021-03-08 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物的制备及其应用
CN114761410B (zh) * 2021-04-06 2023-08-25 广州必贝特医药股份有限公司 吡咯并嘧啶酮类化合物及其应用
WO2022213932A1 (zh) * 2021-04-06 2022-10-13 广州必贝特医药股份有限公司 吡咯并嘧啶酮类化合物及其应用
CN117794934A (zh) * 2021-05-12 2024-03-29 浙江龙传生物医药科技有限公司 吡咯并嘧啶类化合物的晶型及其制备方法
AU2022280865A1 (en) * 2021-05-28 2023-11-09 Merck Sharp & Dohme Llc Synthesis of btk inhibitor and intermediates thereof
CN114409654A (zh) * 2021-12-30 2022-04-29 安徽普利药业有限公司 一种btk抑制剂的中间体合成方法
WO2023192183A1 (en) * 2022-03-29 2023-10-05 Merck Sharp & Dohme Llc Pharmaceutical combinations and methods of use of amino-pyrrolopyrimidinone compound
CN115894500A (zh) * 2022-11-02 2023-04-04 中国药科大学 一种作为btk激酶抑制剂的化合物及其制备方法与用途

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
PL175347B1 (pl) 1992-04-03 1998-12-31 Upjohn Co Trójpierścieniowe heterocykliczne aminy aktywne farmaceutycznie
DK0938486T3 (da) 1996-08-23 2008-07-07 Novartis Ag Substituerede pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
GB0031080D0 (en) 2000-12-20 2001-01-31 Novartis Ag Organic compounds
JPWO2002051849A1 (ja) 2000-12-26 2004-04-22 第一製薬株式会社 Cdk4活性阻害剤
JP2003321472A (ja) 2002-02-26 2003-11-11 Takeda Chem Ind Ltd Grk阻害剤
FR2842525B1 (fr) 2002-07-16 2005-05-13 Aventis Pharma Sa Derives de 3-guanidinocarbonyl-1-heteroaryl-indole, procede de preparation a titre de medicaments et compositions pharmaceutiques les renfermant
EP1689407A1 (en) 2003-11-25 2006-08-16 Pfizer Products Inc. Method of treatment of atherosclerosis
US20070066641A1 (en) 2003-12-19 2007-03-22 Prabha Ibrahim Compounds and methods for development of RET modulators
JP5138938B2 (ja) 2003-12-19 2013-02-06 プレキシコン インコーポレーテッド Ret調節剤の開発のための化合物および方法
JPWO2005080377A1 (ja) 2004-02-20 2007-10-25 キリンホールディングス株式会社 TGFβ阻害活性を有する化合物およびそれを含んでなる医薬組成物
AU2005249380C1 (en) 2004-04-23 2012-09-20 Exelixis, Inc. Kinase modulators and methods of use
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
UA91027C2 (ru) 2004-09-22 2010-06-25 Янссен Фармацевтика Н.В. ИНГИБИТОРЫ ВЗАИМОДЕЙСТВИЯ МЕЖДУ MDM2 И р53
WO2006042102A2 (en) 2004-10-05 2006-04-20 Neurogen Corporation Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
JP2008545652A (ja) 2005-05-17 2008-12-18 プレキシコン,インコーポレーテッド c−kitおよびc−fms活性を調節する化合物およびその用途
US8093264B2 (en) 2005-05-20 2012-01-10 Methylgene Inc. Fused heterocycles as inhibitors of VEGF receptor and HGF receptor signaling
EP2348023B9 (en) 2005-12-13 2017-03-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
AU2007228784B2 (en) 2006-03-22 2012-03-08 Janssen Pharmaceutica N.V. Cyclic-alkylaminederivatives as inhibitors of the interaction between MDM2 and p53
US20100273776A1 (en) 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
WO2007125405A2 (en) 2006-05-01 2007-11-08 Pfizer Products Inc. Substituted 2-amino-fused heterocyclic compounds
EP1889847A1 (en) 2006-07-10 2008-02-20 DeveloGen Aktiengesellschaft Pyrrolopyrimidines for pharmaceutical compositions
AU2007332143B2 (en) 2006-12-11 2012-11-08 Bionomics Limited Chemical compounds and processes
WO2008075007A1 (en) 2006-12-21 2008-06-26 Cancer Research Technology Limited Morpholino-substituted bicycloheteroaryl compounds and their use as anti cancer agents
US20080161254A1 (en) 2007-01-03 2008-07-03 Virobay, Inc. Hcv inhibitors
US20100129933A1 (en) 2007-04-26 2010-05-27 Forschungszentrum Karlsruhe Gmbh Method for detecting the binding between mdm2 and the proteasome
WO2008135232A1 (en) 2007-05-02 2008-11-13 Riccardo Cortese Use and compositions of purine derivatives for the treatment of proliferative disorders
BRPI0820342A2 (pt) 2007-11-07 2015-05-26 Foldrx Pharmaceuticals Inc Modulação de tráfego de proteína
ES2616255T3 (es) 2008-04-30 2017-06-12 National Health Research Institutes Compuestos de pirimidina bicíclicos condensados como inhibidores de las aurora cinasas
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
WO2009143018A2 (en) 2008-05-19 2009-11-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2010002954A1 (en) 2008-07-02 2010-01-07 Wyeth (2-aryl-7h-pyrrolo[2,3-d]pyrimidin-4-yl)morpholine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
WO2010030757A2 (en) 2008-09-10 2010-03-18 Kalypsys Inc. Aminopyrimidine inhibitors of histamine receptors for the treatment of disease
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
EA024252B1 (ru) 2009-01-08 2016-08-31 Кьюрис, Инк. Ингибиторы фосфоинозитид-3-киназ с цинксвязывающей группой
CN102665718B (zh) 2009-10-06 2016-03-09 米伦纽姆医药公司 可用作pdk1抑制剂的杂环化合物
WO2011063159A1 (en) * 2009-11-18 2011-05-26 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
WO2011082268A2 (en) 2009-12-30 2011-07-07 Arqule Inc. Substituted naphthalenyl-pyrimidine compounds
AU2010339444A1 (en) * 2009-12-30 2012-07-19 Arqule, Inc. Substituted pyrrolo-aminopyrimidine compounds
CN102970868A (zh) 2010-04-16 2013-03-13 柯瑞斯公司 具有k-ras突变的癌症的治疗
TWI619713B (zh) * 2010-04-21 2018-04-01 普雷辛肯公司 用於激酶調節的化合物和方法及其適應症
CN103002738A (zh) 2010-05-21 2013-03-27 英特利凯恩有限责任公司 用于激酶调节的化学化合物、组合物和方法
WO2011149827A1 (en) 2010-05-24 2011-12-01 Glaxosmithkline Llc Compounds and methods
WO2011153553A2 (en) 2010-06-04 2011-12-08 The Regents Of The University Of California Methods and compositions for kinase inhibition
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
JP5844376B2 (ja) 2010-10-06 2016-01-13 ジェイファーマ株式会社 強力な尿酸トランスポーター阻害剤の開発:それらの尿酸***効果のために設計された化合物
PE20141360A1 (es) 2011-02-07 2014-10-13 Plexxikon Inc Compuestos y metodos para la modulacion de quinasas e indicaciones para los mismos.
US20130096136A1 (en) 2011-09-30 2013-04-18 Methylgene Inc. Inhibitors of Protein Tyrosine Kinase Activity
CN104185420B (zh) 2011-11-30 2017-06-09 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
WO2013082275A1 (en) 2011-11-30 2013-06-06 Trustees Of Boston College Inhibitors of phosphodiesterases 11 (pde11) and methods of use to elevate cortisol production
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
WO2013182612A1 (en) 2012-06-07 2013-12-12 Bayer Pharma Aktiengesellschaft Glucose transport inhibitors
WO2014011911A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
BR112015002152B1 (pt) 2012-08-02 2021-04-27 Nerviano Medical Sciences S.R.L. Compostos de pirróis substituídos ativos como inibidores de quinases, processo para a preparação de tais compostos, composição farmacêutica, método in vitro para a inibição da atividade de proteínas quinases da família jak e produto compreendendo os referidos compostos
CN103664996B (zh) 2012-08-31 2017-10-03 中国医学科学院医药生物技术研究所 吲哚衍生物及其制备方法
CA2883894C (en) 2012-09-06 2020-08-18 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
CN104812389B (zh) 2012-09-24 2020-07-17 润新生物公司 某些化学实体、组合物及方法
WO2014048869A1 (en) 2012-09-26 2014-04-03 Bayer Pharma Aktiengesellschaft Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperproliferative diseases
CA2885787A1 (en) 2012-09-26 2014-04-03 Lars Wortmann Substituted indazol-pyrrolopyrimidines useful in the treatment of hyperfoliferative disorders
JP2015533181A (ja) 2012-10-16 2015-11-19 アルミラル・ソシエダッド・アノニマAlmirall, S.A. Pi3k阻害剤としてのピロロトリアジノン誘導体
JP6495886B2 (ja) 2013-03-15 2019-04-03 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Btk阻害剤としての複素環式芳香族化合物
EP2970266B1 (en) 2013-03-15 2018-01-31 Epizyme, Inc. 1-phenoxy-3-(alkylamino)-propan-2-ol derivatives as carm1 inhibitors and uses thereof
GB201309085D0 (en) 2013-05-20 2013-07-03 Redx Pharma Ltd Compounds
MX2015015966A (es) 2013-05-30 2016-04-13 Plexxikon Inc Compuestos para la modulacion de cinasas e indicaciones para los mismos.
AU2014289415A1 (en) 2013-07-08 2016-01-21 Bayer Pharma Aktiengesellschaft Substituted pyrazolo-pyridinamines
ES2654051T3 (es) 2013-12-05 2018-02-12 Pfizer Inc. Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinil acrilamidas
GB201410430D0 (en) 2014-06-11 2014-07-23 Redx Pharma Ltd Compounds
WO2016004272A1 (en) * 2014-07-02 2016-01-07 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016044650A1 (en) 2014-09-17 2016-03-24 Epizyme, Inc. Carm1 inhibitors and uses thereof
GB201419015D0 (en) 2014-10-24 2014-12-10 Orca Pharmaceuticals Ltd Compounds
US9630968B1 (en) * 2015-12-23 2017-04-25 Arqule, Inc. Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
FI3882250T3 (fi) 2015-12-23 2023-04-27 Arqule Inc TETRAHYDROPYRANYYLIAMINO-PYRROLOPYRIMIDINONI KÄYTETTÄVÄKSI HOIDETTAESSA BTK-VÄLITTEISiÄ HÄIRIÖITÄ
RU2019108280A (ru) 2016-08-24 2020-09-25 Аркьюл, Инк. Аминопирролопиримидиноновые соединения и способы их применения

Also Published As

Publication number Publication date
US20190358233A1 (en) 2019-11-28
JP2019530650A (ja) 2019-10-24
SG11201901197PA (en) 2019-03-28
US20180055846A1 (en) 2018-03-01
KR20190035925A (ko) 2019-04-03
MX2019002212A (es) 2019-07-08
RU2019108280A (ru) 2020-09-25
CN109890821A (zh) 2019-06-14
PH12019500395A1 (en) 2019-05-20
WO2018039310A1 (en) 2018-03-01
CA3034010A1 (en) 2018-03-01
EP3504213A4 (en) 2020-01-15
AU2017315343A1 (en) 2019-02-28
TW201811795A (zh) 2018-04-01
EP3504213A1 (en) 2019-07-03
US11020398B2 (en) 2021-06-01

Similar Documents

Publication Publication Date Title
BR112019003504A2 (pt) compostos de amino-pirrolopirimidinona e métodos de uso dos mesmos
BR112018070602A2 (pt) composto, composição farmacêutica, uso do composto, e, método para tratar uma doença ou distúrbio
EA201891191A1 (ru) 2-замещенные соединения хиназолина, содержащие замещенную гетероциклическую группу, и способы их применения
BR112019006712A2 (pt) composto, composição farmacêutica, composição para uso no tratamento de uma doença, elemento implantável, e, dispositivo.
BR112019024525A2 (pt) composto, sal farmaceuticamente aceitável e formulação farmacêutica de inibidores de kras c12c
CL2018002009A1 (es) Compuestos derivados de ciclopentanoperhidofenantreno, moduladores de fxr; composicion farmaceutica que comprende dichos compuestos; y su uso para el tratamiento de enfermedades colestásicas, fibróticas, hipercolesterolemia, entre otras.
BR112019002275A2 (pt) inibidores aminopirimidina de ssaos
BR112018008966A2 (pt) compostos inibidores de jak quinase para o tratamento de doença respiratória
EA201991884A3 (ru) Ингибиторы g12c kras
EA201690752A1 (ru) Ингибиторы g12c kras
PH12018501390A1 (en) Tetrahydropyranyl amino-pyrrolopyrimidinone and methods of use thereof
BR112016000489A8 (pt) composto, composição farmacêutica que o compreende, uso da composição e métodos para fabricar compostos
BR112015022785A2 (pt) composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
BR112016008468A2 (pt) Composto de fórmula, composição farmacêutica, composto, uso de um composto e método para o tratamento ou melhora de câncer
BR112016028876A2 (pt) composto, composição farmacêutica, método para tratar uma doença ou condição em um ser humano, kit, e, uso de um composto, um sal, isômero ou uma mistura farmaceuticamente aceitável dos mesmos.
EA201891063A1 (ru) Производные дигидроимидазопиразинона, применимые в лечении рака
BR112016028642A2 (pt) composto, composição farmacêutica, método de tratamento de uma doença ou condição, método de inibição da atividade de um polipeptídeo de fosfatidilinositol 3-quinase, método de inibição de reações imunes ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, e, uso de um composto, de um sal, de um isômero ou de uma mistura farmaceuticamente aceitável do mesmo.
BR112016028814A2 (pt) ?composição farmacêutica, métodos de tratamento de uma doença ou condição, de inibição de reações imunitárias ou crescimento excessivo ou destrutivo ou de proliferação de células cancerosas, kit, composto, um sal, um isômero, ou uma mistura farmaceuticamente aceitável do mesmo, e, uso de um composto, de um sal, de um isômero, ou de uma mistura farmaceuticamente aceitável do mesmo?
BR112015020139A2 (pt) compostos terapêuticos e usos dos mesmos
EA201692481A1 (ru) Комбинация, содержащая глюкокортикоид и edo-s101
PH12016502353A1 (en) Pharmaceutical composition
BR112015030399B8 (pt) Derivados heterocíclicos, uso dos referidos derivados e composição farmacêutica para a prevenção ou tratamento de doenças associadas com a ativação da proteína stat3
BR112018070536A2 (pt) composto, composição farmacêutica, combinação, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, método de tratamento de uma doença ou condição
BR112017016817A2 (pt) derivados heterocíclicos formilados como inibidores de fgfr4
BR112014029439A2 (pt) derivados de ácido salicílico, sal farmaceuticamente aceitável dos mesmos, composição dos mesmos e método de uso dos mesmos

Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]