BR112017026535A2 - composto de fórmula estrutural i, enantiômero isolado, composição farmacêutica, método para inibir atividade do transportador de monocarboxilato mct4, método para inibir seletivamente atividade do transportador de monocarboxilato mct4, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 e uso de um composto - Google Patents

composto de fórmula estrutural i, enantiômero isolado, composição farmacêutica, método para inibir atividade do transportador de monocarboxilato mct4, método para inibir seletivamente atividade do transportador de monocarboxilato mct4, método para tratar um distúrbio mediado por transportador de monocarboxilato mct4 e uso de um composto

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Publication number
BR112017026535A2
BR112017026535A2 BR112017026535A BR112017026535A BR112017026535A2 BR 112017026535 A2 BR112017026535 A2 BR 112017026535A2 BR 112017026535 A BR112017026535 A BR 112017026535A BR 112017026535 A BR112017026535 A BR 112017026535A BR 112017026535 A2 BR112017026535 A2 BR 112017026535A2
Authority
BR
Brazil
Prior art keywords
mct4
monocarboxylate transporter
compound
transporter activity
inhibiting
Prior art date
Application number
BR112017026535A
Other languages
English (en)
Other versions
BR112017026535B1 (pt
Inventor
M Mccall John
Mark Parnell Kenneth
Original Assignee
Vettore Llc
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Publication date
Application filed by Vettore Llc filed Critical Vettore Llc
Publication of BR112017026535A2 publication Critical patent/BR112017026535A2/pt
Publication of BR112017026535B1 publication Critical patent/BR112017026535B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/4151,2-Diazoles
    • 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P35/00Antineoplastic agents
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

são revelados no presente documento os compostos e composições úteis no tratamento de doenças mediadas por mct4, como doenças proliferativas e inflamatórias, que têm a estrutura de fórmula i: (i) métodos de inibição atividade de mct4 em um indivíduo humano ou animal também são fornecidos.
BR112017026535-4A 2015-06-12 2016-06-13 Composto e composição farmacêutica BR112017026535B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562174685P 2015-06-12 2015-06-12
US62/174,685 2015-06-12
PCT/US2016/037213 WO2016201426A1 (en) 2015-06-12 2016-06-13 Mct4 inhibitors for treating disease

Publications (2)

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BR112017026535A2 true BR112017026535A2 (pt) 2018-08-14
BR112017026535B1 BR112017026535B1 (pt) 2023-12-19

Family

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BR112017026535-4A BR112017026535B1 (pt) 2015-06-12 2016-06-13 Composto e composição farmacêutica

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US (5) US10202350B2 (pt)
EP (2) EP3307068B1 (pt)
JP (2) JP6944442B2 (pt)
KR (1) KR102653599B1 (pt)
CN (1) CN107635404B (pt)
AU (2) AU2016277126A1 (pt)
BR (1) BR112017026535B1 (pt)
CA (1) CA2988983A1 (pt)
ES (1) ES2894919T3 (pt)
HK (1) HK1253239A1 (pt)
IL (2) IL256206A (pt)
WO (1) WO2016201426A1 (pt)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10202350B2 (en) 2015-06-12 2019-02-12 Vettore, LLC MCT4 inhibitors for treating disease
MX2019006893A (es) 2016-12-12 2019-10-09 Vettore Llc Inhibidores heterociclicos de mct4.
AU2019317518B2 (en) * 2018-04-25 2023-05-25 Charles R. Drew University Of Medicine And Science Novel MCT4 inhibitors and uses thereof
TWI823932B (zh) * 2018-05-11 2023-12-01 中國大陸商迪哲(江蘇)醫藥有限公司 三唑并嘧啶化合物及其在治療癌症中之用途
WO2020234454A1 (en) 2019-05-23 2020-11-26 Deutsches Krebsforschungszentrum Combination treatment of cancer targeting energy metabolism and intracellular ph
US20210214731A1 (en) * 2019-10-25 2021-07-15 President And Fellows Of Harvard College Methods for treating cancer
WO2022243574A1 (en) * 2021-05-21 2022-11-24 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh 3-(phthalazin-1-yl)benzenesulfonamide-based slc16a3 inhibitors and their therapeutic use
CN113929627A (zh) * 2021-10-19 2022-01-14 吕梁学院 一种宾达利的合成方法
WO2023077739A1 (zh) * 2021-11-08 2023-05-11 中国药科大学 一种喹诺酮衍生物及其制备方法和用途
WO2024031445A1 (en) * 2022-08-10 2024-02-15 Vettore, LLC Methods and processes for the preparation of mct4 inhibitors

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IT1293795B1 (it) 1997-07-28 1999-03-10 Angelini Ricerche Spa Farmaco attivo nel ridurre la produzione di proteina mcp-1
AU2003285503A1 (en) * 2003-11-21 2005-06-24 Astrazeneca Ab Screening method
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KR101581828B1 (ko) * 2008-03-07 2015-12-31 아지엔드 키미쉐 리유나이트 안젤리니 프란체스코 에이.씨.알.에이.에프. 에스.피.에이 신규한 1-벤질-3-하이드록시메틸인다졸 유도체들 및 mcp-1, cx3cr1 및 p40의 발현을 기초로 한 질환들의 치료에서 이의 용도
CN102093341B (zh) 2009-12-10 2013-07-24 天津药物研究院 吲哚环取代的吡唑羧酸类内皮素受体拮抗剂及其制备方法和用途
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Also Published As

Publication number Publication date
US20160362378A1 (en) 2016-12-15
BR112017026535B1 (pt) 2023-12-19
CN107635404B (zh) 2021-09-28
KR20180012852A (ko) 2018-02-06
CA2988983A1 (en) 2016-12-15
IL278247B (en) 2021-12-01
AU2021200919A1 (en) 2021-03-04
AU2021200919B2 (en) 2022-06-30
CN107635404A (zh) 2018-01-26
US20210009524A1 (en) 2021-01-14
AU2016277126A1 (en) 2017-12-14
US20220251045A1 (en) 2022-08-11
JP2018516994A (ja) 2018-06-28
US11724989B2 (en) 2023-08-15
JP6944442B2 (ja) 2021-10-06
NZ738078A (en) 2021-11-26
EP3942934A1 (en) 2022-01-26
US20240101518A1 (en) 2024-03-28
EP3307068A1 (en) 2018-04-18
US20190112274A1 (en) 2019-04-18
JP2021152056A (ja) 2021-09-30
US10202350B2 (en) 2019-02-12
US11155522B2 (en) 2021-10-26
KR102653599B1 (ko) 2024-04-01
EP3307068B1 (en) 2021-08-25
EP3307068A4 (en) 2018-12-26
ES2894919T3 (es) 2022-02-16
HK1253239A1 (zh) 2019-06-14
WO2016201426A1 (en) 2016-12-15
IL256206A (en) 2018-02-28

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