Nothing Special   »   [go: up one dir, main page]

BR112012021595A2 - "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial" - Google Patents

"composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial"

Info

Publication number
BR112012021595A2
BR112012021595A2 BR112012021595A BR112012021595A BR112012021595A2 BR 112012021595 A2 BR112012021595 A2 BR 112012021595A2 BR 112012021595 A BR112012021595 A BR 112012021595A BR 112012021595 A BR112012021595 A BR 112012021595A BR 112012021595 A2 BR112012021595 A2 BR 112012021595A2
Authority
BR
Brazil
Prior art keywords
hiv
pyrido
tetrahydro
pyrazine derivative
compositions
Prior art date
Application number
BR112012021595A
Other languages
English (en)
Inventor
Isoshima Hirotaka
Adachi Kaoru
Oshita Kengo
Kawashita Seiji
Fukuda Shunichi
Miyazaki Susumu
Bessho Yuki
Original Assignee
Japan Tobacco 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44506987&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012021595(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Japan Tobacco Inc filed Critical Japan Tobacco Inc
Publication of BR112012021595A2 publication Critical patent/BR112012021595A2/pt

Links

Classifications

    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina e uso do mesmo como inibidor de integrase de hiv. a presente invenção refere-se a um novo derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina ou um sal farmaceuticamente aceitável do mesmo ou um solvato do mesmo que é útil como um agente anti-hiv. a presente invenção refere-se a um composto representado pela fórmula [i] que segue em que cada símbolo é conforme definido do relatório ou um sal farmaceuticamente aceitável do mesmo ou um solvato do mesmo.
BR112012021595A 2010-02-26 2011-02-25 "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial" BR112012021595A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2010043567 2010-02-26
US33972910P 2010-03-09 2010-03-09
PCT/JP2011/054404 WO2011105590A1 (ja) 2010-02-26 2011-02-25 １，３，４，８－テトラヒドロ－２Ｈ－ピリド［１，２－ａ］ピラジン誘導体及びそのＨＩＶインテグラーゼ阻害剤としての利用

Publications (1)

Publication Number Publication Date
BR112012021595A2 true BR112012021595A2 (pt) 2017-02-21

Family

ID=44506987

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012021595A BR112012021595A2 (pt) 2010-02-26 2011-02-25 "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial"

Country Status (18)

Country Link
US (2) US10065950B2 (pt)
EP (1) EP2540720B1 (pt)
JP (1) JP5765965B2 (pt)
KR (1) KR20120130185A (pt)
CN (1) CN102858771A (pt)
AR (1) AR080314A1 (pt)
AU (1) AU2011221037A1 (pt)
BR (1) BR112012021595A2 (pt)
CA (1) CA2789457A1 (pt)
CL (1) CL2012002355A1 (pt)
CO (1) CO6571861A2 (pt)
MX (1) MX2012009869A (pt)
NZ (1) NZ601847A (pt)
PE (1) PE20130010A1 (pt)
RU (1) RU2012140961A (pt)
SG (1) SG183484A1 (pt)
TW (1) TW201139437A (pt)
WO (1) WO2011105590A1 (pt)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112012021595A2 (pt) * 2010-02-26 2017-02-21 Japan Tobacco Inc "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial"
WO2013054862A1 (ja) 2011-10-12 2013-04-18 塩野義製薬株式会社 インテグラーゼ阻害活性を有する多環性ピリドン誘導体
WO2014099586A1 (en) * 2012-12-17 2014-06-26 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
EA037633B1 (ru) 2012-12-21 2021-04-23 Джилид Сайэнс, Инк. Полициклические карбамоилпиридоновые соединения, их фармацевтические композиции и применение
TW201431859A (zh) * 2012-12-27 2014-08-16 Japan Tobacco Inc 經取代之螺吡啶並［１，２－ａ］吡□衍生物及該衍生物作爲ＨＩＶ整合酶抑制劑之醫藥用途
AU2014267951A1 (en) * 2013-05-17 2015-11-19 Merck Sharp & Dohme Corp. Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors
WO2014200880A1 (en) 2013-06-13 2014-12-18 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
NO2865735T3 (pt) 2013-07-12 2018-07-21
CA2916993C (en) 2013-07-12 2019-01-15 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
AU2014318832B2 (en) 2013-09-12 2018-11-29 Janssen Biopharma, Inc. Aza-pyridone compounds and uses thereof
CN103736081A (zh) * 2013-12-18 2014-04-23 首都医科大学附属北京佑安医院 Ontak在制备清除潜伏hiv病毒药物中的应用
WO2015089847A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
NO2717902T3 (pt) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
EP3196201B1 (en) 2014-08-22 2021-04-28 Shionogi & Co., Ltd. Polycyclic pyridone derivative having integrase-inhibiting activity
WO2016090545A1 (en) 2014-12-09 2016-06-16 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrate inhibitors
US10150780B2 (en) 2014-12-09 2018-12-11 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as HIV integrase inhibitors
TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
JP6772141B2 (ja) * 2014-12-24 2020-10-21 ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ，ベイジン ネクローシス阻害薬
BR112017020837A2 (pt) 2015-04-02 2018-07-03 Gilead Sciences, Inc. compostos de carbamoilpiridona policíclicos e seu uso farmacêutico
WO2016187788A1 (en) * 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10624912B2 (en) 2015-11-17 2020-04-21 Merck Sharp & Dohme Corp. Spirocyclic Pyridotriazine Derivatives useful as HIV integrase inhibitors
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
KR102714478B1 (ko) 2017-10-06 2024-10-10 시오노기세야쿠 가부시키가이샤 치환된 다환성 피리돈 유도체의 입체 선택적인 제조 방법
AU2019277547B2 (en) 2018-05-31 2024-10-10 Shionogi & Co., Ltd. Polycyclic pyridone derivative
AR115455A1 (es) 2018-05-31 2021-01-20 Shionogi & Co Derivado de piridotriazina policíclica
LT3938047T (lt) 2019-03-22 2022-10-10 Gilead Sciences, Inc. Tilteliniai tricikliniai karbamoilpiridono junginiai ir jų naudojimas farmacijoje
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
WO2021107066A1 (ja) 2019-11-28 2021-06-03 塩野義製薬株式会社 インテグラーゼ阻害剤及び抗ｈｉｖ薬を組み合わせることを特徴とするｈｉｖ感染症の予防及び治療用医薬
CA3166480A1 (en) 2020-02-24 2021-09-02 Lan Jiang Tetracyclic compounds for treating hiv infection
CN112574155A (zh) * 2020-11-25 2021-03-30 南京杰运医药科技有限公司 一种3-(苄氧基)-4-氧代-4h-吡喃-2-羧酸的合成方法
HRP20231654T1 (hr) 2021-01-19 2024-03-15 Gilead Sciences, Inc. Supstituirani spojevi piridotriazina i njihove uporabe
TWI843506B (zh) 2022-04-06 2024-05-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7399763B2 (en) 2002-09-11 2008-07-15 Merck & Co., Inc. 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors
EP1549315A4 (en) 2002-09-11 2007-05-23 Merck & Co Inc DIHYDROXYPYRIDOPYRAZINE-1,6-DION COMPOUNDS AS HIV INTEGRASE INHIBITORS
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
CA2542047A1 (en) 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as hiv integrase inhibitors
JP2007528379A (ja) * 2004-03-09 2007-10-11 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・ピー・アー Ｈｉｖインテグラーゼ阻害薬
US7820680B2 (en) 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
EP1756114B1 (en) 2004-05-07 2014-11-19 Merck Sharp & Dohme Corp. Hiv integrase inhibitors
EP1973906A1 (en) 2004-12-23 2008-10-01 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
WO2006088173A1 (ja) 2005-02-21 2006-08-24 Shionogi & Co., Ltd. Ｈｉｖインテグラーゼ阻害活性を有する２環性カルバモイルピリドン誘導体
EP3284520B1 (en) 2005-04-28 2019-06-05 VIIV Healthcare Company Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
WO2007050510A2 (en) 2005-10-27 2007-05-03 Merck & Co., Inc. Hiv integrase inhibitors
CN101346376A (zh) * 2005-10-27 2009-01-14 盐野义制药株式会社 具有hiv整合酶抑制活性的多环性氨基甲酰基吡啶酮衍生物
CA2626956A1 (en) 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
CN102143962B (zh) * 2008-07-02 2015-03-11 爱维艾珂瑟有限公司 具有抗病毒特性的化合物
US8431581B2 (en) 2008-07-02 2013-04-30 Avexa Limited Imidazopyrimidines and uses thereof
US8426405B2 (en) 2008-07-02 2013-04-23 Avexa Limited Thiazopyrimidinones and uses thereof
BR112012021595A2 (pt) * 2010-02-26 2017-02-21 Japan Tobacco Inc "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial"
UY33241A (es) 2010-02-26 2011-09-30 Boehringer Ingelheim Int ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?.
EA201201192A1 (ru) 2010-02-26 2013-04-30 Бёрингер Ингельхайм Интернациональ Гмбх Тиенопиримидины, содержащие замещенную алкильную группу, предназначенные для фармацевтических композиций
CN102946859B (zh) 2010-02-26 2016-03-02 泽农医药公司 用于局部给药的螺-羟吲哚化合物的药物组合物及其作为治疗剂的用途
US8754079B2 (en) 2010-02-26 2014-06-17 Boehringer Ingelheim International Gmbh Cycloalkyl containing thienopyrimidines for pharmaceutical compositions
JP5766690B2 (ja) 2010-04-12 2015-08-19 塩野義製薬株式会社 インテグラーゼ阻害活性を有するピリドン誘導体

Also Published As

Publication number Publication date
CN102858771A (zh) 2013-01-02
EP2540720B1 (en) 2015-04-15
RU2012140961A (ru) 2014-04-10
US20180319798A1 (en) 2018-11-08
CA2789457A1 (en) 2011-09-01
WO2011105590A1 (ja) 2011-09-01
KR20120130185A (ko) 2012-11-29
PE20130010A1 (es) 2013-02-05
AR080314A1 (es) 2012-03-28
AU2011221037A1 (en) 2012-09-06
TW201139437A (en) 2011-11-16
CL2012002355A1 (es) 2013-01-25
JP5765965B2 (ja) 2015-08-19
CO6571861A2 (es) 2012-11-30
US20120108564A1 (en) 2012-05-03
EP2540720A4 (en) 2013-07-31
MX2012009869A (es) 2012-09-12
US10065950B2 (en) 2018-09-04
JP2011195585A (ja) 2011-10-06
NZ601847A (en) 2014-03-28
SG183484A1 (en) 2012-09-27
EP2540720A1 (en) 2013-01-02

Similar Documents

Publication Publication Date Title
BR112012021595A2 (pt) "composto derivado de 1,3,4,8-tetra-hidro-2h-pirido[1,2-a]pirazina, suas composições, seus usos, agente anti-hiv, inibidor da integrase de hiv e embalagem comercial"
PH12015501412A1 (en) SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND MEDICINAL USE THEREOF AS HIV INTEGRASE INHIBITOR
BR112015019590A2 (pt) derivados de ácido betulínico modificado com c-3 alquila e alquenila úteis no tratamento de hiv
BR112015018738A8 (pt) compostos de tetra-hidropirrolotiazina, seus usos, e composição farmacêutica
BR112013018601A2 (pt) composto, uso de composto, composição farmacêutica, e, produto farmacêutico
NZ711982A (en) Cytotoxic and anti-mitotic compounds, and methods of using the same
CO6741203A2 (es) Derivados de biciclo[3,2,1]octilamida y sus usos
ECSP099750A (es) Imidazoquinolinas con propiedades inmunomoduladoras
BR112012030810A2 (pt) "c-28 amidas de derivados de ácido c-3 betulínico modificados como inibidores de maturação de hiv"
BR112016010080A8 (pt) compostos de pirazolopirimidina, composição farmacêutica e seu uso
BR112014001018A2 (pt) derivado de azabenzimidazol tendo atividade de ativação de ampk
MX2012000414A (es) Derivados piridin-4-ilo.
NZ739760A (en) Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
NI201200191A (es) Derivados de indolizina, su procedimiento de preparación y su aplicación en terapéutica
BR112012018345A2 (pt) "compostos de heteroarila, bem como composições e usos dos mesmos"
MX2016002185A (es) Formulacion combinada de dos compuestos antivirales.
PH12014501967B1 (en) Benzodioxanes in combination with other actives for inhibiting leukotriene production
MX361618B (es) Formulaciones farmacéuticas que comprenden derivados de nitrocatecol y métodos para hacer las mismas.
BR112016007427A2 (pt) compostos de pirazol-amida e usos dos mesmos
BR112014004651A2 (pt) composto de pirazol e uso farmacêutico do mesmo
MY165918A (en) Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof
BR112015012825A2 (pt) piridopirazinas substituídas como inibidores de syk
MX340574B (es) Imidazo pirazinas.
BR112015026967A8 (pt) fenoxietil di-hidro-1h-isoquinolina, seus usos, e composição farmacêutica
WO2014101295A3 (zh) 一种詹纳斯激酶（jaks）抑制活性的异恶唑衍生物

Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]