BR112017013677A2 - compostos macrocíclicos como inibidores de irak1/4 e usos dos mesmos - Google Patents

compostos macrocíclicos como inibidores de irak1/4 e usos dos mesmos

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Publication number
BR112017013677A2
BR112017013677A2 BR112017013677-5A BR112017013677A BR112017013677A2 BR 112017013677 A2 BR112017013677 A2 BR 112017013677A2 BR 112017013677 A BR112017013677 A BR 112017013677A BR 112017013677 A2 BR112017013677 A2 BR 112017013677A2
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Brazil
Prior art keywords
ring
sulfur
nitrogen
oxygen
independently selected
Prior art date
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BR112017013677-5A
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English (en)
Other versions
BR112017013677B1 (pt
Inventor
Chen Xiaoling
Yu Henry
Lan Ruoxi
Jorand-Lebrun Catherine
L. Johnson Theresa
Goutopoulos Andreas
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Merck Patent Gmbh
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Publication of BR112017013677A2 publication Critical patent/BR112017013677A2/pt
Publication of BR112017013677B1 publication Critical patent/BR112017013677B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • 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
    • C07D471/22—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 systems contains four or more hetero rings
    • 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/439—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P19/00—Drugs for skeletal disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • 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
    • C07D487/18—Bridged 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
    • C07D498/18—Bridged 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
    • C07D498/22—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 four or more hetero rings
    • 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
    • C07D513/22—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 four or more hetero rings

Abstract

a presente invenção refere-se aos compostos de fórmula i e composições farmaceuticamente aceitáveis dos mesmos, úteis como inibidores de irak. em que anel a é um anel heterocíclico de 5 mem-bros tendo 1 a 4 heteroátomos independentemente selecionados de nitrogênio, oxigênio, ou enxofre, cada um dos quais é opcionalmente substituído; o anel b é uma arila de 6 membros, ou uma heteroarila monocíclica de 6 membros tendo 1 a 4 heteroátomos independentemente selecionados de nitrogênio, oxigênio, ou enxofre; cada um dos quais é opcionalmente substituído; o anel c é um anel heterocíclico de 5 membros tendo de 1 a 4 heteroátomos independentemente selecionados de nitrogênio, oxigênio, ou enxofre, ou um anel heteroarila monocíclico de 5 membros tendo de 1 a 4 heteroátomos independentemente selecionados de nitrogênio, oxigênio, ou enxofre; cada um dos quais é opcionalmente substituído;
BR112017013677-5A 2015-02-05 2016-02-05 Compostos macrocíclicos como inibidores de irak1/4, seu processo de fabricação e seus usos, e composições farmacêuticas BR112017013677B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562112374P 2015-02-05 2015-02-05
US62/112,374 2015-02-05
PCT/US2016/016709 WO2016127025A1 (en) 2015-02-05 2016-02-05 Macrocyclic compounds as irak1/4 inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
BR112017013677A2 true BR112017013677A2 (pt) 2018-01-09
BR112017013677B1 BR112017013677B1 (pt) 2023-11-21

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BR112017013677-5A BR112017013677B1 (pt) 2015-02-05 2016-02-05 Compostos macrocíclicos como inibidores de irak1/4, seu processo de fabricação e seus usos, e composições farmacêuticas

Country Status (15)

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US (2) US9708324B2 (pt)
EP (1) EP3253764B1 (pt)
JP (1) JP6835727B2 (pt)
KR (1) KR20170109546A (pt)
CN (1) CN107849055B (pt)
AU (1) AU2016215185B2 (pt)
BR (1) BR112017013677B1 (pt)
CA (1) CA2970534C (pt)
ES (1) ES2886577T3 (pt)
IL (1) IL253520B (pt)
MX (1) MX2017009625A (pt)
NZ (1) NZ732538A (pt)
RU (1) RU2730016C2 (pt)
SG (1) SG11201704628VA (pt)
WO (1) WO2016127025A1 (pt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
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TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
US11254667B2 (en) 2016-08-17 2022-02-22 Children's Hospital Medical Center Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
JP2021528470A (ja) * 2018-06-25 2021-10-21 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Ｔａｉｒｅファミリーキナーゼインヒビターおよびそれらの使用
TW202136268A (zh) 2018-07-13 2021-10-01 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
CA3108065A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
PE20220169A1 (es) * 2019-03-28 2022-01-28 Lupin Ltd Compuestos macrociclicos como agonistas de sting
CN111603471B (zh) * 2020-06-24 2021-07-09 山东省科学院生物研究所 一种邻二氮杂环化合物在制备抑制tlr4受体的药物中的用途
WO2024030908A1 (en) * 2022-08-01 2024-02-08 Children's Hospital Medical Center Multi-cyclic irak1 and irak4 inhibiting compounds and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7678783B2 (en) * 2004-11-17 2010-03-16 Merck Sharp & Dohme Corp. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
MY169441A (en) * 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US8933066B2 (en) * 2011-04-14 2015-01-13 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
US9586948B2 (en) * 2012-10-08 2017-03-07 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
CA2900442C (en) * 2013-02-07 2021-09-21 Merck Patent Gmbh Macrocyclic pyridazinone derivatives
US9617282B2 (en) * 2013-03-15 2017-04-11 Biogen Ma Inc. Macrocyclic compounds as IRAK4 inhibitors for the treatment of inflammatory diseases

Also Published As

Publication number Publication date
CN107849055A (zh) 2018-03-27
RU2730016C2 (ru) 2020-08-14
US9815836B2 (en) 2017-11-14
WO2016127025A1 (en) 2016-08-11
US20160229856A1 (en) 2016-08-11
EP3253764A1 (en) 2017-12-13
SG11201704628VA (en) 2017-07-28
US20170275284A1 (en) 2017-09-28
IL253520B (en) 2020-07-30
AU2016215185B2 (en) 2020-06-25
RU2017130762A3 (pt) 2019-04-30
NZ732538A (en) 2022-04-29
CA2970534C (en) 2023-08-29
RU2017130762A (ru) 2019-03-05
ES2886577T3 (es) 2021-12-20
KR20170109546A (ko) 2017-09-29
IL253520A0 (en) 2017-09-28
EP3253764B1 (en) 2021-06-09
US9708324B2 (en) 2017-07-18
CN107849055B (zh) 2020-08-07
BR112017013677B1 (pt) 2023-11-21
JP2018506531A (ja) 2018-03-08
JP6835727B2 (ja) 2021-02-24
CA2970534A1 (en) 2016-08-11
AU2016215185A1 (en) 2017-06-29
MX2017009625A (es) 2017-11-20

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