AR105665A1 - Derivados del ácido piridin-3-il acético como inhibidores de la replicación del virus de la inmunodeficiencia humana - Google Patents

Derivados del ácido piridin-3-il acético como inhibidores de la replicación del virus de la inmunodeficiencia humana

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Publication number
AR105665A1
AR105665A1 ARP160102454A ARP160102454A AR105665A1 AR 105665 A1 AR105665 A1 AR 105665A1 AR P160102454 A ARP160102454 A AR P160102454A AR P160102454 A ARP160102454 A AR P160102454A AR 105665 A1 AR105665 A1 AR 105665A1
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AR
Argentina
Prior art keywords
alkyl
alkoxy
alkoxyalkyl
halo
substituents
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ARP160102454A
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English (en)
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VIIV HEALTHCARE UK (Nº 5) LTD
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Application filed by VIIV HEALTHCARE UK (Nº 5) LTD filed Critical VIIV HEALTHCARE UK (Nº 5) LTD
Publication of AR105665A1 publication Critical patent/AR105665A1/es

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    • 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
    • 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
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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

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

Abstract

Reivindicación 1: Un compuesto de fórmula (1) en la que: R¹ está seleccionado de hidrógeno, halo, alquilo, haloalquilo, hidroxialquilo, alcoxialquilo, (alcoxi)alcoxialquilo, ((cicloalquil)alcoxi)alquilo, (cicloalcoxi)alquilo, haloalcoxialquilo, (haloalcoxi)alcoxialquilo, ((halocicloalquil)alcoxi)alquilo, (halocicloalcoxi)alquilo, (halofenoxi)alquilo, (Ar¹)alquilo, (Ar²)alquilo, ((R¹⁰)(R¹¹)N)alquilo, (trialquilamonio)alquilo, (R⁶)alquilo, alquenilo, (alcoxi)alquenilo, hidroxi, alcoxi, (Ar¹)alcoxi, (R¹⁰)(R¹¹)N, CO₂R¹⁰, CON(R¹⁰)(R¹¹), ((Ar¹)alquil)imidazolilo, o halobenzimidazolilo; con la condición de que cuando R¹ es hidrógeno R⁵ no sea alquilo; R² está seleccionado de halo, fenilo o tetrahidroisoquinolinilo y está sustituido con 1 sustituyente R⁷ y con 0 - 3 sustituyentes seleccionados de halo, alquilo, haloalquilo, alcoxi y haloalcoxi; con la condición de que cuando R² es halo, R¹ y R⁵ no sean simultáneamente alquilo; R³ está seleccionado de azetidinilo, pirrolidinilo, piperidinilo, piperazinilo u homopiperidinilo sustituido con 0 - 3 sustituyentes halo o alquilo; R⁴ está seleccionado de alquilo o haloalquilo; R⁵ está seleccionado de hidrógeno, alquilo, haloalquilo, hidroxi, hidroxialquilo, alcoxi, alcoxialquilo, (alcoxi)alcoxialquilo, (((alcoxi)alcoxi)alcoxi)alquilo, ((benciloxi)alcoxi)alquilo, ((R¹⁰)(R¹¹)N)alquilo o (R⁶)alquilo; con la condición de que R¹ y R⁵ no sean simultáneamente alquilo; R⁶ está seleccionado de (oxetanil)alquilo, ((oxetanil)alcoxi)alquilo, (tetrahidropiraniloxi)alquilo, (tetrahidropiranil)alcoxi) alquilo, ((pirrolidinonil)alcoxi)alquilo, (Ar¹O)alquilo, ((Ar¹)alcoxi)alquilo, ((Ar²)alcoxi)alquilo, (oxetanil)oxi, ((R⁸)(R⁹)N)alcoxi, alquiltio, alquilsulfonilo o (R⁸)(R⁹)N; R⁷ está seleccionado de (Ar¹)alquilo, (Ar¹)alcoxi, N-alcoxicarbonilo o ((Ar¹)alquil)HNCO; o R⁷ está seleccionado de pirimidinilo, benzofuropirimidinilo o pirazolopirimidinilo sustituido con 0 - 1 sustituyentes alquilo; R⁸ está seleccionado de hidrógeno, alquilo, (cicloalquil)alquilo, alcoxialquilo, (tetrahidropiranil)alquilo, tetrahidropiranilo o alcoxifenilo; R⁹ está seleccionado de hidrógeno o alquilo; o (R⁸)(R⁹)N tomado conjuntamente está seleccionado de azetidinilo, pirrolidinilo, piperidinilo, (espirociclobutil)piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo o dioxidotiomorfolinilo, y está sustituido con 0 - 3 sustituyentes alquilo o alcoxicarbonilo; R¹⁰ está seleccionado de hidrógeno, alquilo o alcoxialquilo; R¹¹ está seleccionado de hidrógeno, alquilo, (cicloalquil)alquilo, hidroxialquilo, alcoxialquilo, (oxetanil)alquilo, (tetrahidropiranil)alquilo, (Ar¹)alquilo, (Ar²)alquilo, (((Ar¹)alquil)carbonil) alquilo, oxetanilo, Ar¹, formilo, alquilcarbonilo, (Ar²)carbonilo, (dialquilamino)oxoacetilo o alquilsulfonilo; o (R¹⁰)(R¹¹)N tomado conjuntamente está seleccionado de azetidinilo, biciclo[1,1,1]pentanilo, pirrolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo, dioxidotiomorfolinilo, [3,1,1]diazabicicloheptanilo, [3,2,1]diazabiciclooctanilo o tetrahidroquinolinilo y está sustituido con 0 - 3 sustituyentes halo, alquilo, haloalquilo, bencilo, hidroxi, alcoxi o haloalcoxi y con 0 - 1 sustituyentes espiroalquilenilo C₃₋₇; Ar¹ es fenilo sustituido con 0 - 3 sustituyentes seleccionados de halo, alquilo, haloalquilo, alcoxi y haloalcoxi; y Ar² está seleccionado de pirazolilo, oxazolilo, tiazolilo, triazolilo, oxadiazolilo o piridinilo y está sustituido con 0 - 3 sustituyentes halo o alquilo; o una sal farmacéuticamente aceptable del mismo.
ARP160102454A 2015-08-12 2016-08-10 Derivados del ácido piridin-3-il acético como inhibidores de la replicación del virus de la inmunodeficiencia humana AR105665A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562204239P 2015-08-12 2015-08-12

Publications (1)

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AR105665A1 true AR105665A1 (es) 2017-10-25

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ID=56883826

Family Applications (1)

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ARP160102454A AR105665A1 (es) 2015-08-12 2016-08-10 Derivados del ácido piridin-3-il acético como inhibidores de la replicación del virus de la inmunodeficiencia humana

Country Status (13)

Country Link
US (1) US10351546B2 (es)
EP (1) EP3334724A1 (es)
JP (1) JP2018522926A (es)
KR (1) KR20180035914A (es)
CN (1) CN108349939A (es)
AR (1) AR105665A1 (es)
AU (1) AU2016306087A1 (es)
BR (1) BR112018002689A2 (es)
CA (1) CA2995099A1 (es)
IL (1) IL257247A (es)
RU (1) RU2018106504A (es)
TW (1) TW201718537A (es)
WO (1) WO2017025915A1 (es)

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TWI657086B (zh) * 2015-08-11 2019-04-21 英商Viiv醫療保健英國(No.5)有限公司 做為人類免疫缺陷病毒複製抑制劑之５－（ｎ－苯甲基四氫異喹啉－６－基）吡啶－３－基乙酸衍生物
US10577353B2 (en) * 2015-08-12 2020-03-03 VIIV Healthcare UK (No.5) Limited 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2017195111A1 (en) * 2016-05-11 2017-11-16 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
JP2019515000A (ja) * 2016-05-11 2019-06-06 ヴィーブ ヘルスケア ユーケー（ナンバー５）リミテッド ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−３−イル酢酸誘導体
EP3565810A1 (en) * 2017-01-03 2019-11-13 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2018127800A1 (en) 2017-01-03 2018-07-12 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2019244066A2 (en) 2018-06-19 2019-12-26 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2020003093A1 (en) 2018-06-25 2020-01-02 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

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KR20180025914A (ko) * 2015-07-09 2018-03-09 비브 헬스케어 유케이 (넘버5) 리미티드 인간 면역결핍 바이러스 복제의 억제제로서의 피리딘-3-일 아세트산 유도체
AU2016290205A1 (en) * 2015-07-09 2018-01-18 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TWI657086B (zh) * 2015-08-11 2019-04-21 英商Viiv醫療保健英國(No.5)有限公司 做為人類免疫缺陷病毒複製抑制劑之５－（ｎ－苯甲基四氫異喹啉－６－基）吡啶－３－基乙酸衍生物
CA2995087A1 (en) * 2015-08-12 2017-02-16 John F. Kadow 5-(n-fused tricyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US10577353B2 (en) * 2015-08-12 2020-03-03 VIIV Healthcare UK (No.5) Limited 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

Also Published As

Publication number Publication date
CA2995099A1 (en) 2017-02-16
US10351546B2 (en) 2019-07-16
TW201718537A (zh) 2017-06-01
IL257247A (en) 2018-03-29
KR20180035914A (ko) 2018-04-06
BR112018002689A2 (pt) 2018-11-27
EP3334724A1 (en) 2018-06-20
US20180230124A1 (en) 2018-08-16
CN108349939A (zh) 2018-07-31
JP2018522926A (ja) 2018-08-16
AU2016306087A1 (en) 2018-03-08
RU2018106504A (ru) 2019-09-13
WO2017025915A1 (en) 2017-02-16

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