PE20181002A1 - Derivados del acido 5-(n- bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana - Google Patents

Derivados del acido 5-(n- bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana

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Publication number
PE20181002A1
PE20181002A1 PE2018000174A PE2018000174A PE20181002A1 PE 20181002 A1 PE20181002 A1 PE 20181002A1 PE 2018000174 A PE2018000174 A PE 2018000174A PE 2018000174 A PE2018000174 A PE 2018000174A PE 20181002 A1 PE20181002 A1 PE 20181002A1
Authority
PE
Peru
Prior art keywords
acid
alkyl
benzyl
tetrahidroisoquinolin
acetico
Prior art date
Application number
PE2018000174A
Other languages
English (en)
Inventor
Kyle J Eastman
John F Kadow
Kyle E Parcella
B Narasimhulu Naidu
Tao Wang
Zhiwei Yin
Zhongxing Zhang
Original Assignee
Viiv Healthcare Uk No 5 Ltd
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.)
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=56851651&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20181002(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Viiv Healthcare Uk No 5 Ltd filed Critical Viiv Healthcare Uk No 5 Ltd
Publication of PE20181002A1 publication Critical patent/PE20181002A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion refiere un compuesto de formula I : En donde: R1 esta seleccionado de H, alquilo o cicloalquilo; R2 esta seleccionado de tetrahidroisoquibolinilo y esta sustituido con 1 sustituyente R6; R3 esta seleccionado de azetidinilo, pirrolidinilo, piperazinilo, entre otros; R4 es alquilo o haloalquilo; R5 es alquilo; R6 esta seleccionado de Ar1, (Ar1)alquilo, entre otros. Ar1 es fenilo sustituido con 0-5 sustituyentes seleccionados de ciano, halo, alquilo, entre otros. Son compuestos preferidos: acido (S)-2-(terc-butoxi)-2-(4-(4,4-dimetilpiperidin-1-il)-5-(2-(4-fluorobencil)-1,2,3,4-tetrahidroisoquinolin-6-il)-2,6-dimetilpiridin-3-il)acetico; : acido (S)-2-(terc-butoxi)-2-(4-(4,4-dimetilpiperidin-1-il)-2,6-dimetil-5-(2-(3-(trifluorometil)bencil)-1,2,3,4-tetrahidroisoquinolin-6-il)-2,6-dimetilpiridin-3-il)acetico, entre otros. La presente invencion es util para la inhibicion del VIH y tratamiento de los infectados con VIH y SIDA.
PE2018000174A 2015-08-11 2016-08-10 Derivados del acido 5-(n- bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana PE20181002A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562203791P 2015-08-11 2015-08-11

Publications (1)

Publication Number Publication Date
PE20181002A1 true PE20181002A1 (es) 2018-06-26

Family

ID=56851651

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2018000174A PE20181002A1 (es) 2015-08-11 2016-08-10 Derivados del acido 5-(n- bencil-tetrahidroisoquinolin-6-il)-piridin-3-il acetico como inhibidores de la replicacion del virus de la inmunodeficiencia humana

Country Status (23)

Country Link
US (2) US10189816B2 (es)
EP (1) EP3334716A1 (es)
JP (1) JP6782766B2 (es)
KR (1) KR20180032649A (es)
CN (1) CN108137534A (es)
AR (1) AR105653A1 (es)
AU (1) AU2016306089B2 (es)
CA (1) CA2994791A1 (es)
CL (1) CL2018000363A1 (es)
CO (1) CO2018001359A2 (es)
CR (1) CR20180091A (es)
DO (1) DOP2018000035A (es)
EA (1) EA033057B1 (es)
HK (1) HK1249503A1 (es)
IL (1) IL257240B (es)
MA (1) MA42614A (es)
MX (1) MX2018001722A (es)
PE (1) PE20181002A1 (es)
PH (1) PH12018500294A1 (es)
TW (1) TWI657086B (es)
UA (1) UA120464C2 (es)
WO (1) WO2017025917A1 (es)
ZA (1) ZA201800689B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018522913A (ja) * 2015-08-12 2018-08-16 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5−(n−[6,5]−縮合二環式アリールテトラヒドロイソキノリン−6−イル)ピリジン−3−イル酢酸誘導体
TW201718537A (zh) * 2015-08-12 2017-06-01 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吡啶-3-基乙酸衍生物
JP2019515003A (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
US20200325127A1 (en) * 2016-05-11 2020-10-15 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
EP3455214A1 (en) * 2016-05-11 2019-03-20 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
UY37555A (es) * 2017-01-03 2018-08-31 Viiv Healthcare Uk No 5 Ltd Derivados de ácido piridin-3-il-acético como inhibidores de la replicación del virus de la inmunodeficiencia humana
JP2020503352A (ja) * 2017-01-03 2020-01-30 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

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CA2705318C (en) * 2007-11-15 2013-12-31 Boehringer Ingelheim International Gmbh Inhibitors of human immunodeficiency virus replication
WO2009062288A1 (en) 2007-11-15 2009-05-22 Boehringer Ingelheim International Gmbh Inhibitors of human immunodeficiency virus replication
EP2220046B1 (en) 2007-11-16 2014-06-18 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
ES2463720T3 (es) 2007-11-16 2014-05-29 Gilead Sciences, Inc. Inhibidores de la replicación del virus de inmunodeficiencia humana
US8338441B2 (en) * 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
GB0908394D0 (en) 2009-05-15 2009-06-24 Univ Leuven Kath Novel viral replication inhibitors
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US8633200B2 (en) 2010-09-08 2014-01-21 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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WO2014164467A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
US9527842B2 (en) 2013-03-14 2016-12-27 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
EP3116880B1 (en) * 2014-02-20 2018-03-21 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid macrocycles as inhibitors of human immunodeficiency virus replication
US9193720B2 (en) 2014-02-20 2015-11-24 Bristol-Myers Squibb Company Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201718537A (zh) * 2015-08-12 2017-06-01 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吡啶-3-基乙酸衍生物
US10214516B2 (en) * 2015-08-12 2019-02-26 VIIV Healthcare UK (No.5) Limited 5-(N-fused tricyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
JP2018522913A (ja) * 2015-08-12 2018-08-16 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5−(n−[6,5]−縮合二環式アリールテトラヒドロイソキノリン−6−イル)ピリジン−3−イル酢酸誘導体

Also Published As

Publication number Publication date
CN108137534A (zh) 2018-06-08
JP6782766B2 (ja) 2020-11-11
CL2018000363A1 (es) 2018-07-06
WO2017025917A1 (en) 2017-02-16
CR20180091A (es) 2018-06-13
DOP2018000035A (es) 2018-03-30
CO2018001359A2 (es) 2018-05-10
AU2016306089A1 (en) 2018-03-01
US10189816B2 (en) 2019-01-29
MX2018001722A (es) 2018-05-16
HK1249503A1 (zh) 2018-11-02
US20180230129A1 (en) 2018-08-16
EP3334716A1 (en) 2018-06-20
UA120464C2 (uk) 2019-12-10
US20190092754A1 (en) 2019-03-28
TW201718549A (zh) 2017-06-01
IL257240B (en) 2020-02-27
IL257240A (en) 2018-03-29
MA42614A (fr) 2021-05-26
AU2016306089B2 (en) 2018-08-09
EA033057B1 (ru) 2019-08-30
PH12018500294A1 (en) 2018-08-13
AR105653A1 (es) 2017-10-25
TWI657086B (zh) 2019-04-21
ZA201800689B (en) 2021-08-25
JP2018522927A (ja) 2018-08-16
CA2994791A1 (en) 2017-02-16
EA201890361A1 (ru) 2018-11-30
KR20180032649A (ko) 2018-03-30

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