BR112021011643A2 - Compostos macrocíclicos e seu uso no tratamento de doença - Google Patents

Compostos macrocíclicos e seu uso no tratamento de doença Download PDF

Info

Publication number
BR112021011643A2
BR112021011643A2 BR112021011643-5A BR112021011643A BR112021011643A2 BR 112021011643 A2 BR112021011643 A2 BR 112021011643A2 BR 112021011643 A BR112021011643 A BR 112021011643A BR 112021011643 A2 BR112021011643 A2 BR 112021011643A2
Authority
BR
Brazil
Prior art keywords
thia
diaza
trifluoromethyl
dipyridine
dioxide
Prior art date
Application number
BR112021011643-5A
Other languages
English (en)
Portuguese (pt)
Inventor
Mihai Azimioara
Lewis Whitehead
Baogen Wu
Shanshan YAN
Xuefeng Zhu
Badry Bursulaya
Songchun Jiang
Casey Jacob Nelson MATHISON
Victor Ivanovich NIKULIN
Truc Ngoc Nguyen
Barun Okram
Sejal Patel
Dean Paul Phillips
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of BR112021011643A2 publication Critical patent/BR112021011643A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three or more hetero 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
    • A61K31/435Heterocyclic 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/12Heterocyclic 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
    • C07D513/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/22Heterocyclic 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 four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D515/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, 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
    • C07D515/18Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
BR112021011643-5A 2018-12-21 2019-12-18 Compostos macrocíclicos e seu uso no tratamento de doença BR112021011643A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862783270P 2018-12-21 2018-12-21
US62/783,270 2018-12-21
PCT/IB2019/061054 WO2020128925A1 (en) 2018-12-21 2019-12-18 Macrocyclic compounds and their use in the treatment of disease

Publications (1)

Publication Number Publication Date
BR112021011643A2 true BR112021011643A2 (pt) 2021-09-08

Family

ID=69165443

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021011643-5A BR112021011643A2 (pt) 2018-12-21 2019-12-18 Compostos macrocíclicos e seu uso no tratamento de doença

Country Status (10)

Country Link
US (1) US20220071971A1 (https=)
EP (1) EP3898621A1 (https=)
JP (1) JP2022513959A (https=)
KR (1) KR20210107046A (https=)
CN (1) CN113227087A (https=)
AU (1) AU2019404934B2 (https=)
BR (1) BR112021011643A2 (https=)
CA (1) CA3119656A1 (https=)
MX (1) MX2021007592A (https=)
WO (1) WO2020128925A1 (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019222758B2 (en) 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
CA3150162A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
WO2022194399A1 (en) 2020-07-13 2022-09-22 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
CR20230120A (es) * 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
IL300413A (en) 2020-08-13 2023-04-01 Vertex Pharma Crystal forms of CFTR modulators
EP4225762A1 (en) 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225765A2 (en) * 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
EP4225447A1 (en) * 2020-10-07 2023-08-16 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004074A (es) * 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
AU2021397294A1 (en) 2020-12-10 2023-07-06 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
EP4308575A1 (en) * 2021-03-16 2024-01-24 Idorsia Pharmaceuticals Ltd Macrocycles as cftr modulators
TWI904194B (zh) * 2021-07-12 2025-11-11 瑞士商愛杜西亞製藥有限公司 作為cftr調節劑之巨環
IL315715A (en) * 2022-04-06 2024-11-01 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulation
TW202421102A (zh) 2022-09-15 2024-06-01 瑞士商愛杜西亞製藥有限公司 巨環cftr調節劑與cftr校正子及/或cftr增效劑之組合
CA3267791A1 (en) 2022-09-15 2024-03-21 Idorsia Pharmaceuticals Ltd CRYSTALLINE FORM OF (3S,7S,10R,13R)-13-BENZYL-20-FLUORO-7-ISOBUTYL-N-(2-(3-METHOXY-1,2,4-OXADIAZOL-5-YL)ETHYL)-6,9-DIMETHYL-1,5,8,11-TETRAOXO-10-(2,2,2-TRIFLUOROETHYL)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-TETRADECAHYDRO-[1]OXA[4,7,10,14]TETRAAZACYCLOHEPTADECINO [16,17-F]QUINOLINE-3-CARBOXAMIDE
KR20250084132A (ko) 2022-09-15 2025-06-10 이도르시아 파마슈티컬스 리미티드 마크로시클릭 cftr 조절제
CN115498160B (zh) * 2022-09-29 2025-09-30 郑州大学 一种锂-有机硫电池正极材料及其制备方法和应用
WO2025186214A1 (en) 2024-03-05 2025-09-12 Idorsia Pharmaceuticals Ltd Macrocyclic cftr modulators

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9617282B2 (en) * 2013-03-15 2017-04-11 Biogen Ma Inc. Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases
WO2015138934A1 (en) * 2014-03-13 2015-09-17 Proteostasis Therapeutics, Inc. Compounds, compositions, and methods for increasing cftr activity
US9981945B2 (en) * 2015-10-07 2018-05-29 NuBridge BioSciences Pyrimidine derivatives as CFTR modulators
TW201811766A (zh) * 2016-08-29 2018-04-01 瑞士商諾華公司 N-(吡啶-2-基)吡啶-磺醯胺衍生物及其用於疾病治療之用途
EP3580224B1 (en) * 2017-02-07 2022-07-13 Biogen MA Inc. Ask1 inhibiting agents
AU2019222758B2 (en) * 2018-02-15 2022-07-07 Vertex Pharmaceuticals Incorporated Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them

Also Published As

Publication number Publication date
AU2019404934A1 (en) 2021-06-03
CN113227087A (zh) 2021-08-06
EP3898621A1 (en) 2021-10-27
WO2020128925A1 (en) 2020-06-25
JP2022513959A (ja) 2022-02-09
KR20210107046A (ko) 2021-08-31
US20220071971A1 (en) 2022-03-10
CA3119656A1 (en) 2020-06-25
AU2019404934B2 (en) 2022-04-21
MX2021007592A (es) 2021-08-11

Similar Documents

Publication Publication Date Title
BR112021011643A2 (pt) Compostos macrocíclicos e seu uso no tratamento de doença
JP2022513959A5 (https=)
ES2838977T3 (es) Inhibidores de la lisil oxidasa fluorada tipo 2 y usos de los mismos
ES2898069T3 (es) Derivados de N-(piridin-2-il)piridinosulfonamida y su uso en el tratamiento de la enfermedad
AU2020374957A1 (en) Small molecule degraders of Helios and methods of use
US20230119547A1 (en) Di-substituted pyrazole compounds for the treatment of diseases
CN104725359B (zh) 取代的哌嗪化合物及其使用方法和用途
WO2021078301A1 (zh) 蛋白降解剂及其在疾病治疗中的应用
ES2821400T3 (es) Compuestos de 6-heterociclil-4-morfolin-4-ilpiridin-2-ona útiles para el tratamiento del cáncer y la diabetes
JP2019501142A (ja) Usp30の阻害剤としての1−シアノピロリジン誘導体
US20220127247A1 (en) N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease
US9809568B2 (en) Compounds inhibiting leucine-rich repeat kinase enzyme activity
CN103917534B (zh) 作为h3受体抑制剂的包含哌啶和哌嗪环的氨基甲酸酯/脲衍生物
CN105085482B (zh) 取代的哌嗪化合物及其使用方法和用途
WO2023215471A1 (en) Tetrahydroisoquinoline heterobifunctional bcl-xl degraders
WO2020020377A1 (zh) 用作fgfr4抑制剂的稠环衍生物
RU2804139C2 (ru) Макроциклические соединения и их применение в лечении заболевания
JP2023509496A (ja) RORγt阻害剤、その製造方法及び使用
CN106065018A (zh) 取代的吲哚化合物及其使用方法和用途
WO2025042896A1 (en) DNA TOPOISOMERASE IIβ INHIBITORS
AU2015200638B2 (en) Pyrazolo [1, 5 -a] pyrimidines as antiviral agents
TW202430501A (zh) 醯基磺胺化合物作為多瘤病毒的抑制劑
HK40063935A (zh) 多环tlr7/8拮抗剂及其在治疗免疫失调中的用途
BR112020006456A2 (pt) compostos químicos
BR112020006456B1 (pt) Compostos químicos, composição farmacêutica e seus usos para tratar uma infecção por vírus da hepatite b e para inibir o nível do antígeno hbe ou hbs em um hbsag de mamífero in vitro

Legal Events

Date Code Title Description
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 6A 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 2859 DE 21-10-2025 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.