BR112021015996A2 - Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes - Google Patents

Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes

Info

Publication number
BR112021015996A2
BR112021015996A2 BR112021015996A BR112021015996A BR112021015996A2 BR 112021015996 A2 BR112021015996 A2 BR 112021015996A2 BR 112021015996 A BR112021015996 A BR 112021015996A BR 112021015996 A BR112021015996 A BR 112021015996A BR 112021015996 A2 BR112021015996 A2 BR 112021015996A2
Authority
BR
Brazil
Prior art keywords
derivatives
pkm2
thieno
pyrrol
obesity
Prior art date
Application number
BR112021015996A
Other languages
English (en)
Inventor
Jingjing Ji
Tao Liu
Zhihua Sui
Original Assignee
Agios Pharmaceuticals 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 Agios Pharmaceuticals Inc filed Critical Agios Pharmaceuticals Inc
Publication of BR112021015996A2 publication Critical patent/BR112021015996A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

derivados de tieno[3,2-b] pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes. são descritos, neste documento, compostos que regulam a atividade da piruvato quinase, composições farmacêuticas e métodos de uso dos mesmos. esses compostos são representados pela fórmula (i), em que r2, l1-l2, u1-u7, m, anel a e q são conforme definidos neste documento.
BR112021015996A 2019-02-13 2020-02-12 Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes BR112021015996A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962805040P 2019-02-13 2019-02-13
PCT/US2020/017965 WO2020167976A1 (en) 2019-02-13 2020-02-12 Thieno[3,2-b] pyrrole[3,2-d]pyridazinone derivatives and their use as pkm2 derivatives for the treatment of cancer, obesity and diabetes related disorders

Publications (1)

Publication Number Publication Date
BR112021015996A2 true BR112021015996A2 (pt) 2021-11-09

Family

ID=69941460

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021015996A BR112021015996A2 (pt) 2019-02-13 2020-02-12 Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes

Country Status (14)

Country Link
US (1) US20220127267A1 (pt)
EP (1) EP3924056A1 (pt)
JP (1) JP2022520090A (pt)
KR (1) KR20210128435A (pt)
CN (1) CN113646050A (pt)
AU (1) AU2020221837A1 (pt)
BR (1) BR112021015996A2 (pt)
CA (1) CA3129829A1 (pt)
CO (1) CO2021011919A2 (pt)
IL (1) IL285445A (pt)
MA (1) MA54948A (pt)
MX (1) MX2021009743A (pt)
SG (1) SG11202108744WA (pt)
WO (1) WO2020167976A1 (pt)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11364240B2 (en) 2017-08-15 2022-06-21 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in treating blood disorders
CA3183980A1 (en) * 2020-07-21 2022-01-27 The Regents Of The University Of Michigan Compositions and methods for activating pyruvate kinase
WO2022170200A1 (en) 2021-02-08 2022-08-11 Global Blood Therapeutics, Inc. 1-(2-sulfonyl-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4h)-yl]-ethanone derivatives as pyruvate kinase (pkr) and pkm2 activators for the treatment of sickle cell disease
CA3231728A1 (en) 2021-09-30 2023-04-06 Sitryx Therapeutics Limited Novel compounds
WO2023079294A1 (en) 2021-11-05 2023-05-11 Sitryx Therapeutics Limited Phthalazine derivatives as pyruvate kinase modulators
CN118434720A (zh) 2021-12-22 2024-08-02 西特瑞治疗有限公司 作为丙酮酸激酶调节剂的酞嗪衍生物
MX2024007744A (es) 2021-12-22 2024-07-01 Sitryx Therapeutics Ltd Derivados de ftalazina como moduladores de piruvato quinasa.
CN115487190A (zh) * 2022-11-01 2022-12-20 复旦大学附属中山医院 丙酮酸激酶m2激活剂在制备治疗系统性红斑狼疮的药物中的应用
CN116808223A (zh) * 2023-08-04 2023-09-29 复旦大学附属中山医院 丙酮酸激酶m2激活剂在制备治疗银屑病的药物中的应用

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3173415B1 (en) * 2008-10-09 2019-06-05 The U.S.A. as represented by the Secretary, Department of Health and Human Services Activators of human pyruvate kinase
US8785450B2 (en) 2009-06-29 2014-07-22 Agios Pharmaceuticals, Inc. Therapeutic compounds and compositions
EP2704719B1 (en) * 2011-05-03 2018-02-21 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use for increasing lifetime of the red blood cells and treating anemia
CA2834692A1 (en) * 2011-05-03 2012-11-08 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in therapy
PL3406251T3 (pl) 2011-05-03 2024-04-29 Agios Pharmaceuticals, Inc. Aktywatory kinazy pirogronianowej do stosowania w terapii
US9921221B2 (en) 2012-07-26 2018-03-20 Joslin Diabetes Center, Inc. Predicting and treating diabetic complications
US11364240B2 (en) * 2017-08-15 2022-06-21 Agios Pharmaceuticals, Inc. Pyruvate kinase activators for use in treating blood disorders

Also Published As

Publication number Publication date
MX2021009743A (es) 2021-11-12
EP3924056A1 (en) 2021-12-22
MA54948A (fr) 2021-12-22
CO2021011919A2 (es) 2021-12-10
KR20210128435A (ko) 2021-10-26
CA3129829A1 (en) 2020-08-20
SG11202108744WA (en) 2021-09-29
JP2022520090A (ja) 2022-03-28
WO2020167976A1 (en) 2020-08-20
CN113646050A (zh) 2021-11-12
AU2020221837A1 (en) 2021-09-02
US20220127267A1 (en) 2022-04-28
IL285445A (en) 2021-09-30

Similar Documents

Publication Publication Date Title
BR112021015996A2 (pt) Derivados de tieno[3,2-b]pirrol[3,2-d]piridazinona e seu uso como derivados de pkm2 para o tratamento de câncer, obesidade e distúrbios relacionados a diabetes
BR112022012641A2 (pt) Compostos tricíclicos substituídos
PH12020551870A1 (en) Tetracyclic heteroaryl compounds
PH12019501350A1 (en) Amino-triazolopyridine compounds and their use in treating cancer
CR20200520A (es) Compuestos heterocíclicos como inmunomoduladores
BR112021024674A2 (pt) Derivado heterocíclico de nitrogênio com cinco membros de pirimidina, método de preparação do mesmo e uso farmacêutico do mesmo
WO2018049152A8 (en) Pyrazolopyrimidine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
BRPI0709680B8 (pt) derivados de pirrol, tiofeno e furano substituídos por piridil e piridimil como inibidores de quinase
WO2019035863A8 (en) PYRUVATE KINASE ACTIVATORS FOR USE IN THE TREATMENT OF HEMATOLOGICAL DISORDERS
MX2019010354A (es) Derivado de heteroaril[4,3-c]pirimidina-5-amina, metodo de preparacion del mismo y usos medicos del mismo.
EP4321513A3 (en) Pyrrolotriazine compounds as tam inhibitors
BR112014022106A2 (pt) derivados macrocíclicos para o tratamento de doenças
EP4104837A3 (en) Heterocyclic compounds as ret kinase inhibitors
NZ725600A (en) Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of asgpr
CR20200553A (es) Moduladores de enzimas modificadoras de metilo, composiciones y usos de estos
EA200701808A1 (ru) Производные тетрагидроиндолона и тетрагидроиндазолона
CR20140203A (es) Derivados de octahidro-pirrolo (3,4-b) pirrol
UY29414A1 (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
BR112021025102A2 (pt) Derivados de quinazolin-4-ona úteis para o tratamento de doenças e distúrbios associados a braf
BR112021017831A2 (pt) Derivados heteroaromáticos e aromáticos heterobicíclicos para o tratamento de distúrbios relacionados com ferroptose
WO2021011713A8 (en) Imidazopyrimidines as eed inhibitors and the use thereof
BR112017007708A2 (pt) composto macrocíclicos, uso de um composto macrocíclicos, método para tratamento, unidade de dose, composição farmacêutica e método para tratar câncer em um paciente
MX2010002900A (es) Derivados heterociclicos triciclicos.
MX2022006229A (es) Composiciones y metodos para el tratamiento de resistencia a la insulina.
CR20210544A (es) DERIVADOS DE 1,1-DIÓXIDO DE 3-AMINO-4H-BENZO[E][1,2,4] tiadiazina COMO INHIBIDORES DE MRGX2

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 4A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2761 DE 05-12-2023 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.