BR112018013251A2 - compostos heterocílicos tricíclicos fundidos como inibidores da hiv integrase - Google Patents

compostos heterocílicos tricíclicos fundidos como inibidores da hiv integrase

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Publication number
BR112018013251A2
BR112018013251A2 BR112018013251A BR112018013251A BR112018013251A2 BR 112018013251 A2 BR112018013251 A2 BR 112018013251A2 BR 112018013251 A BR112018013251 A BR 112018013251A BR 112018013251 A BR112018013251 A BR 112018013251A BR 112018013251 A2 BR112018013251 A2 BR 112018013251A2
Authority
BR
Brazil
Prior art keywords
tricyclic heterocyclic
fused tricyclic
heterocyclic compounds
hiv integrase
integrase inhibitors
Prior art date
Application number
BR112018013251A
Other languages
English (en)
Inventor
W Stamford Andrew
Cai Jiaqiang
A Mccauley John
T Waddell Sherman
Yu Tao
H Graham Thomas
Zhang Yonglian
Qi Zhiqi
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 BR112018013251A2 publication Critical patent/BR112018013251A2/pt

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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
    • C07D471/12—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 three hetero rings
    • C07D471/16—Peri-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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/5365—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 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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

Abstract

a presente invenção refere-se a compostos heterocíclicos tricíclicos fundidos de fórmula (i), e sais farmaceuticamente aceitáveis dos mesmos, em que r1, r2 e r3 são como aqui definidos. a presente invenção refere-se também a composições compreendendo pelo menos um composto heterocíclico tricíclico fundido, e métodos de utilização dos compostos heterocíclicos tricíclicos fundidos para tratar ou prevenir infecção por hiv em um indivíduo.
BR112018013251A 2015-12-31 2016-12-22 compostos heterocílicos tricíclicos fundidos como inibidores da hiv integrase BR112018013251A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/CN2015/100106 WO2017113288A1 (en) 2015-12-31 2015-12-31 Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
PCT/US2016/068173 WO2017116928A1 (en) 2015-12-31 2016-12-22 Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
BR112018013251A2 true BR112018013251A2 (pt) 2018-12-04

Family

ID=57799839

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018013251A BR112018013251A2 (pt) 2015-12-31 2016-12-22 compostos heterocílicos tricíclicos fundidos como inibidores da hiv integrase

Country Status (15)

Country Link
US (4) US20170190701A1 (pt)
EP (1) EP3397639B1 (pt)
JP (1) JP2019500387A (pt)
KR (1) KR20180095833A (pt)
CN (1) CN108473494A (pt)
AR (1) AR107170A1 (pt)
AU (1) AU2016381072B2 (pt)
BR (1) BR112018013251A2 (pt)
CA (1) CA3008018A1 (pt)
JO (1) JO3811B1 (pt)
MA (1) MA43528A (pt)
MX (1) MX2018008095A (pt)
RU (1) RU2740187C2 (pt)
TW (1) TW201726683A (pt)
WO (2) WO2017113288A1 (pt)

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CN110062627A (zh) 2016-12-02 2019-07-26 默沙东公司 可用作hiv整合酶抑制剂的三环杂环化合物
BR112020021768A2 (pt) * 2018-04-27 2021-01-26 Merck Sharp & Dohme Corp. compostos heterocíclicos tricíclicos úteis como inibidores de hiv-integrase
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MA52802A (fr) 2018-05-31 2021-04-14 Shionogi & Co Dérivé de pyridone polycyclique
WO2019236396A1 (en) 2018-06-05 2019-12-12 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
MX2021011394A (es) 2019-03-22 2021-10-13 Gilead Sciences Inc Compuestos de carbamoilpiridona triciclica puenteada y su uso farmaceutico.
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
US20230059640A1 (en) 2019-11-28 2023-02-23 Shionogi & Co., Ltd. Prophylactic and therapeutic pharmaceutical agent for hiv infectious diseases characterized by comprising combination of integrase inhibitor and anti-hiv agent
EP4110783A1 (en) 2020-02-24 2023-01-04 Gilead Sciences, Inc. Tetracyclic compounds for treating hiv infection
EP4196479B1 (en) 2021-01-19 2023-11-01 Gilead Sciences, Inc. Substituted pyridotriazine compounds and uses thereof

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Also Published As

Publication number Publication date
US20190322666A1 (en) 2019-10-24
EP3397639B1 (en) 2022-02-23
KR20180095833A (ko) 2018-08-28
WO2017113288A1 (en) 2017-07-06
CA3008018A1 (en) 2017-07-06
MX2018008095A (es) 2018-08-23
AR107170A1 (es) 2018-03-28
JP2019500387A (ja) 2019-01-10
AU2016381072B2 (en) 2020-11-26
EP3397639A1 (en) 2018-11-07
MA43528A (fr) 2018-11-07
US20210040096A1 (en) 2021-02-11
RU2740187C2 (ru) 2021-01-12
US20180099967A1 (en) 2018-04-12
WO2017116928A1 (en) 2017-07-06
JO3811B1 (ar) 2021-01-31
RU2018127728A (ru) 2020-02-03
RU2018127728A3 (pt) 2020-02-14
AU2016381072A1 (en) 2018-05-31
TW201726683A (zh) 2017-08-01
CN108473494A (zh) 2018-08-31
US20170190701A1 (en) 2017-07-06

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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]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B12B Appeal against refusal [chapter 12.2 patent gazette]