BR112021010715A2 - Pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1) - Google Patents

Pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1)

Info

Publication number
BR112021010715A2
BR112021010715A2 BR112021010715A BR112021010715A BR112021010715A2 BR 112021010715 A2 BR112021010715 A2 BR 112021010715A2 BR 112021010715 A BR112021010715 A BR 112021010715A BR 112021010715 A BR112021010715 A BR 112021010715A BR 112021010715 A2 BR112021010715 A2 BR 112021010715A2
Authority
BR
Brazil
Prior art keywords
usp1
substituted
ubiquitin
inhibitors
specific processing
Prior art date
Application number
BR112021010715A
Other languages
English (en)
Inventor
Alistair WYLIE Andrew
Beyer KRALL Elsa
Burnett Brenneman Jehrod
Michael Schlabach
Original Assignee
Ksq Therapeutics 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 Ksq Therapeutics Inc filed Critical Ksq Therapeutics Inc
Publication of BR112021010715A2 publication Critical patent/BR112021010715A2/pt

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C12Q1/6886—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers

Abstract

pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1). a presente invenção refere-se a compostos apresentando a fórmula i: e os sais e solvatos farmaceuticamente aceitáveis dos mesmos, em que x1, x2, x11, x12, r1, r3, r5, r5', r6 e r7 são definidos conforme apresentado no relatório descritivo. a presente invenção também é direcionada ao uso de compostos da fórmula i para inibir uma proteína usp1 e/ou para tratar um distúrbio responsivo à inibição de proteínas usp1 e atividade de usp1. os compostos da presente invenção são especialmente úteis para tratamento de câncer.
BR112021010715A 2018-12-20 2019-12-19 Pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1) BR112021010715A2 (pt)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201862783014P 2018-12-20 2018-12-20
US201962799423P 2019-01-31 2019-01-31
US201962857986P 2019-06-06 2019-06-06
US201962868616P 2019-06-28 2019-06-28
US201962946263P 2019-12-10 2019-12-10
PCT/US2019/067521 WO2020132269A1 (en) 2018-12-20 2019-12-19 Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (usp1) inhibitors

Publications (1)

Publication Number Publication Date
BR112021010715A2 true BR112021010715A2 (pt) 2021-11-16

Family

ID=71100912

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021010715A BR112021010715A2 (pt) 2018-12-20 2019-12-19 Pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1)

Country Status (14)

Country Link
US (2) US11485736B2 (pt)
EP (1) EP3897652A4 (pt)
JP (1) JP2022511515A (pt)
KR (1) KR20210105887A (pt)
CN (1) CN113164485A (pt)
AU (1) AU2019405925A1 (pt)
BR (1) BR112021010715A2 (pt)
CA (1) CA3122108A1 (pt)
CL (1) CL2021001575A1 (pt)
CO (1) CO2021009078A2 (pt)
IL (1) IL284050A (pt)
MX (1) MX2021007179A (pt)
SG (1) SG11202106232TA (pt)
WO (1) WO2020132269A1 (pt)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113164485A (zh) 2018-12-20 2021-07-23 Ksq治疗公司 被取代的吡唑并嘧啶和被取代的嘌呤以及其作为泛素特异性加工蛋白酶1(usp1)抑制剂的用途
WO2021146378A1 (en) * 2020-01-15 2021-07-22 KSQ Therapeutics, Inc. Compositions of substituted pyrazolopyrimidines and uses thereof
MX2022009818A (es) * 2020-02-14 2022-09-05 Ksq Therapeutics Inc Combinaciones terapeuticas que comprenden inhibidores de proteasa 1 de procesamiento especifico de ubiquitina (usp1) e inhibidores de poli (adp-ribosa) polimerasa (parp).
US20230219965A1 (en) * 2020-06-02 2023-07-13 KSQ Therapeutics, Inc. Nitrogen-containing fused bicyclic compounds and their use as ubiquitin-specific-processing protease 1 (usp1) inhibitors
TW202233621A (zh) 2020-10-30 2022-09-01 美商Ｋｓｑ治療公司 經取代吡唑并嘧啶之固態形式及其用途
WO2022174184A1 (en) * 2021-02-15 2022-08-18 Tango Therapeutics, Inc. Pyrrolo[3,2-d]pyrimidine compounds and methods of use in the treatment of cancer
KR20240006509A (ko) * 2021-03-17 2024-01-15 탱고 테라퓨틱스, 인크. 항암제로서의 퓨린 유도체
CN117241801A (zh) * 2021-04-07 2023-12-15 福马治疗有限公司 抑制泛素特异性蛋白酶1（usp1）
CN117337290A (zh) * 2021-05-03 2024-01-02 山东轩竹医药科技有限公司 三并环类泛素特异性蛋白酶1抑制剂及其用途
WO2022253188A1 (en) * 2021-05-31 2022-12-08 Impact Therapeutics (Shanghai) , Inc Nitrogen-containing fused heteroaromatic bicyclic compounds as usp1 inhibitors and the use thereof
GB202114863D0 (en) 2021-10-18 2021-12-01 Syngenta Crop Protection Ag Improvements in or relating to organic compounds
WO2023066299A1 (en) * 2021-10-19 2023-04-27 Impact Therapeutics (Shanghai) , Inc Substituted triazoloheteroaryl compounds as usp1 inhibitors and the use thereof
CN114031556B (zh) * 2021-11-08 2023-03-31 温州大学 一种绿色的一锅法制备5-氨基-n-芳基-3-芳基吡唑类化合物的合成方法
WO2023083285A1 (en) * 2021-11-12 2023-05-19 Insilico Medicine Ip Limited Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof
AR127646A1 (es) 2021-11-12 2024-02-14 Insilico Medicine Ip Ltd Inhibidores de molécula pequeña de proteasa 1 específica de ubiquitina (usp1) y usos de los mismos
CN114181237B (zh) * 2021-12-01 2024-02-23 上海凌凯医药科技有限公司 一种1-异丙基吡唑-5-硼酸频那醇酯的合成方法
WO2023108048A2 (en) * 2021-12-09 2023-06-15 KSQ Therapeutics, Inc. Methods of preparing substituted pyrazolopyrimidines
WO2023143424A1 (zh) * 2022-01-27 2023-08-03 四川海思科制药有限公司 一种氮杂并环衍生物及其在医药上的应用
WO2023148643A1 (en) * 2022-02-03 2023-08-10 Aurigene Oncology Limited Fused bicyclic heterocyclyl compounds as usp1 inhibitors
WO2023155866A1 (zh) * 2022-02-18 2023-08-24 四川海思科制药有限公司 一种吡唑并吡啶衍生物及其在医药上的应用
WO2023196955A1 (en) * 2022-04-08 2023-10-12 KSQ Therapeutics, Inc. Therapeutic combinations comprising ubiquitin- specific-processing protease 1 (usp1) inhibitors and chemotherapy agents
CN116496252A (zh) * 2022-04-29 2023-07-28 江苏亚虹医药科技股份有限公司 嘧啶类化合物、其制备方法及其医药用途
WO2023250084A1 (en) * 2022-06-23 2023-12-28 Forma Therapeutics, Inc. Usp1 inhibitors and uses thereof
US20240092779A1 (en) * 2022-06-29 2024-03-21 Zentaur Therapeutics Usa Inc. Usp1 inhibitors and uses thereof
WO2024022266A1 (en) * 2022-07-25 2024-02-01 Guangdong Newopp Biopharmaceuticals Co., Ltd. Heteroaryl compounds as inhibitors of usp1
WO2024022519A1 (zh) * 2022-07-28 2024-02-01 先声再明医药有限公司 杂环并嘧啶类化合物及其应用
WO2024032647A1 (zh) * 2022-08-09 2024-02-15 上海济煜医药科技有限公司 含氮杂环化合物作为泛素-特异性蛋白酶1抑制剂的制备方法、应用及其用途
WO2024041634A1 (zh) * 2022-08-26 2024-02-29 先声再明医药有限公司 三环类化合物及其应用
WO2024046471A1 (zh) * 2022-09-02 2024-03-07 上海齐鲁制药研究中心有限公司 Usp1抑制剂
WO2024051795A1 (zh) * 2022-09-09 2024-03-14 正大天晴药业集团股份有限公司 用作泛素-特异性蛋白酶抑制剂的取代嘌呤酮衍生物
WO2024061213A1 (zh) * 2022-09-20 2024-03-28 正大天晴药业集团股份有限公司 用作泛素-特异性蛋白酶抑制剂的羰基稠合杂环衍生物
WO2024078436A1 (zh) * 2022-10-09 2024-04-18 海南先声再明医药股份有限公司 杂环并嘧啶类化合物、药物组合物及其应用
WO2024086790A1 (en) 2022-10-21 2024-04-25 Exelixis, Inc. 4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[4,3-c]PYRIDINE COMPOUNDS AND DERIVATIVES AS USP1 INHIBITORS
CN116768906B (zh) * 2023-05-29 2024-04-09 遵义医科大学珠海校区 一种三并环化合物及其制备方法和应用

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5010175A (en) 1988-05-02 1991-04-23 The Regents Of The University Of California General method for producing and selecting peptides with specific properties
ES2259800T3 (es) 1990-06-11 2006-10-16 Gilead Sciences, Inc. Procedimientos de uso de ligandos de acido nucleico.
AU672790B2 (en) 1992-07-15 1996-10-17 Novartis Ag Variants of parathyroid hormone and its fragments
WO1996023899A1 (en) 1995-02-01 1996-08-08 University Of Massachusetts Medical Center Methods of selecting a random peptide that binds to a target protein
AU4474497A (en) 1996-10-08 1998-05-05 U-Bisys B.V. Methods and means for selecting peptides and proteins having specific affinity for a target
US6453242B1 (en) 1999-01-12 2002-09-17 Sangamo Biosciences, Inc. Selection of sites for targeting by zinc finger proteins and methods of designing zinc finger proteins to bind to preselected sites
JP2008520744A (ja) * 2004-11-19 2008-06-19 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 抗炎症性ピラゾロピリミジン
WO2007149484A2 (en) 2006-06-20 2007-12-27 Dana-Farber Cancer Institute Inhibitors of usp1 deubiquitinating enzyme complex
AU2007325900A1 (en) 2006-10-20 2008-06-05 Dnar, Inc. DNA damage repair inhibitors and methods for treating cancer
US7964356B2 (en) 2007-01-16 2011-06-21 Somalogic, Inc. Method for generating aptamers with improved off-rates
EP2209786B1 (en) * 2007-10-05 2013-02-27 Verastem, Inc. Pyrimidine substituted purine derivatives
CN102014631A (zh) * 2008-03-03 2011-04-13 泰格尔医药科技公司 酪氨酸激酶抑制剂
US20110130384A1 (en) * 2008-06-25 2011-06-02 Takeda Pharmaceutical Company Limited Amide compound
GB0917934D0 (en) * 2009-10-13 2009-11-25 Syngenta Ltd Herbicidal compounds
CA2797719C (en) * 2010-04-30 2019-11-26 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of usp1 deubiquitinating enzyme activity
CA2896731A1 (en) 2012-12-28 2014-07-03 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof
EP3071695A2 (en) 2013-11-18 2016-09-28 Crispr Therapeutics AG Crispr-cas system materials and methods
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
MX2021001186A (es) 2015-11-20 2022-10-11 Forma Therapeutics Inc Purinonas como inhibidores de proteasa especifica de ubiquitina 1.
CN113164485A (zh) 2018-12-20 2021-07-23 Ksq治疗公司 被取代的吡唑并嘧啶和被取代的嘌呤以及其作为泛素特异性加工蛋白酶1(usp1)抑制剂的用途
WO2022174184A1 (en) 2021-02-15 2022-08-18 Tango Therapeutics, Inc. Pyrrolo[3,2-d]pyrimidine compounds and methods of use in the treatment of cancer

Also Published As

Publication number Publication date
KR20210105887A (ko) 2021-08-27
US11787813B2 (en) 2023-10-17
CL2021001575A1 (es) 2022-06-03
IL284050A (en) 2021-08-31
SG11202106232TA (en) 2021-07-29
EP3897652A4 (en) 2022-09-14
US20230203046A1 (en) 2023-06-29
US11485736B2 (en) 2022-11-01
CO2021009078A2 (es) 2021-10-29
TW202039501A (zh) 2020-11-01
JP2022511515A (ja) 2022-01-31
MX2021007179A (es) 2021-09-28
WO2020132269A1 (en) 2020-06-25
AU2019405925A1 (en) 2021-07-29
CN113164485A (zh) 2021-07-23
US20210115049A1 (en) 2021-04-22
EP3897652A1 (en) 2021-10-27
CA3122108A1 (en) 2020-06-25

Similar Documents

Publication Publication Date Title
BR112021010715A2 (pt) Pirazolopirimidinas substituídas e purinas substituídas e seu uso como inibidores de protease de processamento ubiquitina-específica 1 (usp1)
BR112022020841A2 (pt) Inibidores de kras tricíclicos fundidos
BR112022008858A2 (pt) Composto, composição farmacêutica e métodos para inibir sos1 em um sujeito, para inibir a interação de sos1 e uma proteína, para tratar ou prevenir uma doença e para tratar ou prevenir câncer
BR112019001666A2 (pt) n-(fenilsulfonil)benzamidas e compostos relacionados como inibidores de bcl-2
BR112021023359A2 (pt) Inibidores de g12c de kras e usos dos mesmos
BR112022003184A2 (pt) Inibidores de pirazolo[3,4-b]pirazina shp2 fosfatase
BR112021026395A2 (pt) Compostos de 2,3-di-hidroquinazolina como inibidores de nav1.8
CL2020002146A1 (es) Derivados de n-(fenil)-2-(fenil)pirimidina-4-carboxamida y compuestos relacionados como inhibidores hpki para tratar el cáncer.
BR112018076534A2 (pt) compostos heterocíclicos como imunomoduladores
BR112022002532A2 (pt) Compostos heterocíclicos como inibidores de quinase
BR112022009514A2 (pt) Compostos úteis como inibidores de proteína helios
BR112018012756A2 (pt) compostos heterocíclicos como imunomoduladores
BR112016015983A2 (pt) Compostos de indazol como inibidores de irak4, seus usos, e composição farmacêutica
BR112022009571A2 (pt) Uso de inibidor de fak na preparação de um fármaco para tratar tumores que têm mutação nras
BR112022016382A2 (pt) Triptaminas específicas para o uso no tratamento de doenças do humor
BR112015016793A2 (pt) compostos de tiazolacarboxamidas e piridinacarbo-xamida úteis como inibidores de quinase pim
BR112015028879A8 (pt) compostos derivados heterocíclicos, composição farmacêutica compreendendo os referidos compostos e usos dos mesmos
BR112022000019A2 (pt) Composto da fórmula, composição farmacêutica e método de tratamento de câncer
BR112016028819A2 (pt) composição farmacêutica, métodos para tratar uma doença ou condição em um ser humano e para inibir a atividade de um polipeptídeo de fosfatidilinositol 3-quinase e reações imunológicas excessivas ou destrutivas ou o crescimento ou a proliferação de células cancerosas, kit, composto, sal farmaceuticamente aceitável, isômero ou mistura dos mesmos, e, uso de um composto, sal farmaceuticamente aceitável ou mistura dos mesmos.
BR112023009531A2 (pt) Gcn2 e inibidores de perk quinase e métodos de uso dos mesmos
BR112019024830A2 (pt) inibidores de bcl6 derivados de benzimidazolona
BR112017004589A2 (pt) composto, composição farmacêutica, método para tratar um paciente, uso de um composto, kit, e método para tratar um distúrbio mediado por proteína smyd
BR112022010319A2 (pt) Uso de bi853520 no tratamento de câncer
BR112018072740A2 (pt) realçador de inibidores de homólogo 2 de zeste
BR112021006319A2 (pt) compostos de indolinona para uso como inibidores de map4k1