BR112018008506A2 - inibidores do fator xia - Google Patents

inibidores do fator xia

Info

Publication number
BR112018008506A2
BR112018008506A2 BR112018008506A BR112018008506A BR112018008506A2 BR 112018008506 A2 BR112018008506 A2 BR 112018008506A2 BR 112018008506 A BR112018008506 A BR 112018008506A BR 112018008506 A BR112018008506 A BR 112018008506A BR 112018008506 A2 BR112018008506 A2 BR 112018008506A2
Authority
BR
Brazil
Prior art keywords
compounds
factor inhibitors
xia factor
factor xia
xia inhibitors
Prior art date
Application number
BR112018008506A
Other languages
English (en)
Other versions
BR112018008506B1 (pt
BR112018008506B8 (pt
Inventor
Ali Amjad
Harper Bart
Zhu Cheng
Shen Dong-Ming
Mertz Eric
Xu Jiayi
Yang Meng
F Neelamkavil Santhosh
D Edmondson Scott
Bara Thomas
Sun Wanying
Zhou Wei
Liu Weiguo
Lim Yeon-Hee
Gao Ying-Duo
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of BR112018008506A2 publication Critical patent/BR112018008506A2/pt
Publication of BR112018008506B1 publication Critical patent/BR112018008506B1/pt
Publication of BR112018008506B8 publication Critical patent/BR112018008506B8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D471/08—Bridged 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
    • C07D487/02—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
    • C07D487/08—Bridged 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
    • C07D513/02—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 two hetero rings
    • C07D513/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

a presente invenção proporciona um composto de fórmula (i) e composições farmacêuticas compreendendo um ou mais dos referidos compostos, e métodos para usar os referidos compostos para tratar ou prevenir tromboses, embolias, hipercoagulabilidade ou alterações fibróticas. os compostos são inibidores seletivos do fator xia ou inibidores duais do fator xia e calicreína plasmática.
BR112018008506A 2015-10-29 2016-10-24 Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos BR112018008506B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562248075P 2015-10-29 2015-10-29
US62/248,075 2015-10-29
PCT/US2016/058362 WO2017074832A1 (en) 2015-10-29 2016-10-24 FACTOR XIa INHIBITORS

Publications (3)

Publication Number Publication Date
BR112018008506A2 true BR112018008506A2 (pt) 2018-10-23
BR112018008506B1 BR112018008506B1 (pt) 2023-11-14
BR112018008506B8 BR112018008506B8 (pt) 2023-12-05

Family

ID=58631804

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018008506A BR112018008506B8 (pt) 2015-10-29 2016-10-24 Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos

Country Status (12)

Country Link
US (1) US10214512B2 (pt)
EP (1) EP3368036B1 (pt)
JP (1) JP6892858B2 (pt)
KR (1) KR20180073602A (pt)
CN (1) CN108430471B (pt)
AU (1) AU2016344476B2 (pt)
BR (1) BR112018008506B8 (pt)
CA (1) CA2998902C (pt)
MA (1) MA43128A (pt)
MX (1) MX2018005045A (pt)
RU (1) RU2728783C2 (pt)
WO (1) WO2017074832A1 (pt)

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* Cited by examiner, † Cited by third party
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EP3870171A4 (en) * 2018-10-25 2022-07-06 Merck Sharp & Dohme Corp. FACTOR XIA INHIBITORS
JP7270770B2 (ja) 2019-04-16 2023-05-10 チャイナ・リソースズ・バイオファーマシューティカル・カンパニー・リミテッド ＸＩａ因子阻害剤としての大環状誘導体
US20220281868A1 (en) * 2019-07-23 2022-09-08 Medshine Discovery Inc. Macrocyclic derivatives as factor xia inhibitors
CN116887831A (zh) * 2021-01-28 2023-10-13 默沙东有限责任公司 因子XIa抑制剂
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors

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JP2004518688A (ja) 2001-01-30 2004-06-24 ブリストル−マイヤーズ　スクイブ　カンパニー ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法
AU2002331707A1 (en) 2001-08-20 2003-03-03 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives as antithrombotic agents
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Also Published As

Publication number Publication date
JP6892858B2 (ja) 2021-06-23
JP2018531954A (ja) 2018-11-01
EP3368036B1 (en) 2022-07-20
MA43128A (fr) 2018-09-05
BR112018008506B1 (pt) 2023-11-14
MX2018005045A (es) 2018-08-01
KR20180073602A (ko) 2018-07-02
CA2998902A1 (en) 2017-05-04
WO2017074832A1 (en) 2017-05-04
CN108430471A (zh) 2018-08-21
CA2998902C (en) 2024-03-26
CN108430471B (zh) 2021-07-09
BR112018008506B8 (pt) 2023-12-05
US10214512B2 (en) 2019-02-26
RU2018119015A (ru) 2019-11-29
EP3368036A1 (en) 2018-09-05
US20180339977A1 (en) 2018-11-29
EP3368036A4 (en) 2019-04-17
AU2016344476B2 (en) 2020-08-13
RU2728783C2 (ru) 2020-07-31
AU2016344476A1 (en) 2018-03-08
RU2018119015A3 (pt) 2020-02-18

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B25A Requested transfer of rights approved

Owner name: MERCK SHARP AND DOHME LLC (US)

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 24/10/2016, OBSERVADAS AS CONDICOES LEGAIS

B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: REFERENTE A RPI 2758 DE 14/11/2023, QUANTO AO ITEM (73) ENDERECO DO TITULAR.