[go: up one dir, main page]

AR107974A1 - Análogos de nucleósidos alquinil como inhibidores de rinovirus humanos - Google Patents

Análogos de nucleósidos alquinil como inhibidores de rinovirus humanos

Info

Publication number
AR107974A1
AR107974A1 ARP170100737A ARP170100737A AR107974A1 AR 107974 A1 AR107974 A1 AR 107974A1 AR P170100737 A ARP170100737 A AR P170100737A AR P170100737 A ARP170100737 A AR P170100737A AR 107974 A1 AR107974 A1 AR 107974A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
groups selected
halo
hydroxy
amino
Prior art date
Application number
ARP170100737A
Other languages
English (en)
Inventor
Weidong Zhong
Fumiaki Yokokawa
Oliver Saunders
Martijn Fenaux
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR107974A1 publication Critical patent/AR107974A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/14Pyrrolo-pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • 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
    • 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
    • A61P31/16Antivirals for RNA viruses for influenza or rhinoviruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Proporciona además composiciones farmacéuticas que comprenden estos compuestos, y composiciones que comprenden estos compuestos con un co-agente terapéutico, y métodos para usar los compuestos y composiciones para el tratamiento de infecciones virales, especialmente HRV. Reivindicación 1: Un compuesto de fórmula (1), donde: R¹ es H, Me, Et, iPr, o ciclopropilo; R² es H, fosfato, difosfato, trifosfato, -P(=X)(OR⁴)₂, -P(=X)(OR⁴)(NR⁵R⁶), o -P(=X)(NR⁵R⁶)₂, y R³ es H o -C(O)R; o R³ y R² tomados juntos forman -P(=X)(OR⁴)- o -P(=X)(NR⁵R⁶)-; X en cada aparición es independientemente O ó S; R⁴ se selecciona de H, fenilo opcionalmente sustituido con uno o dos grupos seleccionados de la lista A, y alquilo C₁₋₄ opcionalmente sustituido con uno o dos grupos seleccionados de halo, -OR, -OC(O)R, -OC(O)-OR, -NR₂, C(O)R, COOR y -C(O)NR₂; cada R⁵ es independientemente H, -C(O)R, COOR, o alquilo C₁₋₄ opcionalmente sustituido con OH, amino, o COOR; cada R⁶ se selecciona independientemente de H, fenilo opcionalmente sustituido con uno o dos grupos seleccionados de la lista A, y alquilo C₁₋₄ opcionalmente sustituido con uno o dos grupos seleccionados de la lista B; cada R es independientemente H o un grupo alquilo C₁₋₄ opcionalmente sustituido con uno a tres grupos seleccionados de halo, hidroxi, CN, amino, alcoxi C₁₋₃, -C(O)R⁷, -OC(O)R⁷, -C(O)-OR⁷, o -OC(O)-OR⁷; R⁷ se selecciona de H, alquilo C₁₋₄ opcionalmente sustituido con uno a tres grupos seleccionados de halo, hidroxi, CN, amino, y alcoxi C₁₋₃, o fenilo opcionalmente sustituido con uno o dos grupos seleccionados de la lista A; la lista A es halo, hidroxi, -NO₂, CN, -OR⁸, -OC(O)R⁸, -OC(O)-OR⁸, -N(R⁸)₂, -C(O)R⁸, COOR⁸, -C(O)N(R⁸)₂, y alquilo C₁₋₃ opcionalmente sustituido con uno a tres grupos seleccionados de halo, hidroxi, CN, amino, y alcoxi C₁₋₃; la lista B es halo, hidroxi, oxo, CN, -OR⁸, -OC(O)R⁸, -OC(O)-OR⁸, -N(R⁸)₂, -C(O)R⁸, COOR⁸ y -C(O)N(R⁸)₂; y R⁸ es independientemente en cada caso seleccionado de H y alquilo C₁₋₄ opcionalmente sustituido con uno a tres grupos seleccionados de halo, hidroxi, CN, amino y alcoxi C₁₋₃, y dos R⁸ unidos al mismo átomo de nitrógeno puede opcionalmente ciclarse para formar un heterociclo de 3 - 7 miembros, que contiene opcionalmente un N, O ó S adicional como miembro del anillo, y puede estar sustituido por uno o dos grupos seleccionados de oxo, halo, -OH, amino, alquilo C₁₋₃, alcoxi C₁₋₃, y haloalquilo C₁₋₃; o una sal farmacéuticamente aceptable del mismo.
ARP170100737A 2016-03-24 2017-03-23 Análogos de nucleósidos alquinil como inhibidores de rinovirus humanos AR107974A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SG10201602360R 2016-03-24

Publications (1)

Publication Number Publication Date
AR107974A1 true AR107974A1 (es) 2018-07-04

Family

ID=58448587

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170100737A AR107974A1 (es) 2016-03-24 2017-03-23 Análogos de nucleósidos alquinil como inhibidores de rinovirus humanos

Country Status (13)

Country Link
US (2) US9988416B2 (es)
EP (2) EP4292658A3 (es)
JP (1) JP7005508B2 (es)
CN (1) CN109311885A (es)
AR (1) AR107974A1 (es)
DK (1) DK3433257T3 (es)
ES (1) ES2962269T3 (es)
FI (1) FI3433257T3 (es)
PL (1) PL3433257T3 (es)
PT (1) PT3433257T (es)
TW (1) TWI746532B (es)
UY (1) UY37166A (es)
WO (1) WO2017163186A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017163186A1 (en) * 2016-03-24 2017-09-28 Novartis Ag Alkynyl nucleoside analogs as inhibitors of human rhinovirus
WO2018048882A1 (en) 2016-09-06 2018-03-15 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for bacterial infection

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0090505B1 (en) 1982-03-03 1990-08-08 Genentech, Inc. Human antithrombin iii, dna sequences therefor, expression vehicles and cloning vectors containing such sequences and cell cultures transformed thereby, a process for expressing human antithrombin iii, and pharmaceutical compositions comprising it
US6111090A (en) 1996-08-16 2000-08-29 Schering Corporation Mammalian cell surface antigens; related reagents
DK0920505T3 (da) 1996-08-16 2008-09-08 Schering Corp Pattedyrcelleoverfladeantigener og tilhörende reagenser
CZ126799A3 (cs) 1996-10-16 1999-07-14 Icn Pharmaceuticals Purinové L-nukleosidy a jejich analogy a farmaceutické prostředky, které je obsahují
AU1102399A (en) 1997-10-21 1999-05-10 Human Genome Sciences, Inc. Human tumor necrosis factor receptor-like proteins tr11, tr11sv1, and tr11sv2
JP2002502607A (ja) 1998-02-09 2002-01-29 ジェネンテク・インコーポレイテッド 新規な腫瘍壊死因子レセプター相同体及びそれをコードする核酸
ATE376837T1 (de) 1999-07-12 2007-11-15 Genentech Inc Stimulierung oder hemmung von angiogenese und herzvaskularisierung mit tumor nekrose faktor ligand/rezeptor homologen
NZ526703A (en) 2001-01-22 2004-12-24 Merck & Co Inc Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
AU2003288675B2 (en) 2002-12-23 2010-07-22 Medimmune Limited Antibodies against PD-1 and uses therefor
US20040229839A1 (en) 2003-05-14 2004-11-18 Biocryst Pharmaceuticals, Inc. Substituted nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
KR20060052681A (ko) 2003-05-23 2006-05-19 와이어쓰 Gitr 리간드, gitr 리간드-연관 분자, 항체 및그의 용도
US20050048054A1 (en) 2003-07-11 2005-03-03 Shino Hanabuchi Lymphocytes; methods
EP1692318A4 (en) 2003-12-02 2008-04-02 Genzyme Corp COMPOSITIONS AND METHODS FOR DIAGNOSIS AND TREATMENT OF LUNG CANCER
GB0409799D0 (en) 2004-04-30 2004-06-09 Isis Innovation Method of generating improved immune response
US20060002932A1 (en) 2004-06-04 2006-01-05 Duke University Methods and compositions for enhancement of immunity by in vivo depletion of immunosuppressive cell activity
EP1866339B8 (en) 2005-03-25 2021-12-01 GITR, Inc. Gitr binding molecules and uses therefor
AU2006244885B2 (en) 2005-05-09 2011-03-31 E. R. Squibb & Sons, L.L.C. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
KR101888321B1 (ko) 2005-07-01 2018-08-13 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체
WO2007133822A1 (en) 2006-01-19 2007-11-22 Genzyme Corporation Gitr antibodies for the treatment of cancer
WO2008156712A1 (en) 2007-06-18 2008-12-24 N. V. Organon Antibodies to human programmed death receptor pd-1
EP2175884B8 (en) 2007-07-12 2017-02-22 GITR, Inc. Combination therapies employing gitr binding molecules
AU2009213738B2 (en) 2008-02-11 2015-01-22 Curetech Ltd. Monoclonal antibodies for tumor treatment
EP2262837A4 (en) 2008-03-12 2011-04-06 Merck Sharp & Dohme PD-1 BINDING PROTEINS
EA201170031A1 (ru) 2008-07-02 2011-08-30 Эмерджент Продакт Дивелопмент Сиэтл, Ллс СВЯЗЫВАЮЩИЕ НЕСКОЛЬКО МИШЕНЕЙ БЕЛКИ, ОБЛАДАЮЩИЕ АНТАГОНИСТИЧЕСКИМ ДЕЙСТВИЕМ ПО ОТНОШЕНИЮ К TGF-β
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
KR20110074850A (ko) 2008-08-25 2011-07-04 앰플리뮨, 인크. Pd-1 길항제 및 그의 사용 방법
EA023148B1 (ru) 2008-08-25 2016-04-29 Эмплиммьюн, Инк. Композиции на основе антагонистов pd-1 и их применение
JPWO2010030002A1 (ja) 2008-09-12 2012-02-02 国立大学法人三重大学 外来性gitrリガンド発現細胞
EP4331604B1 (en) 2008-12-09 2025-03-05 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
TW201031675A (en) * 2008-12-23 2010-09-01 Pharmasset Inc Synthesis of purine nucleosides
ES2629337T3 (es) 2009-02-09 2017-08-08 Inserm - Institut National De La Santé Et De La Recherche Médicale Anticuerpos contra PD-1 y anticuerpos contra PD-L1 y usos de los mismos
SG174364A1 (en) 2009-03-20 2011-10-28 Alios Biopharma Inc Substituted nucleoside and nucleotide analogs
RU2646139C1 (ru) 2009-09-03 2018-03-01 Мерк Шарп И Доум Корп. Анти-gitr-антитела
GB0919054D0 (en) 2009-10-30 2009-12-16 Isis Innovation Treatment of obesity
JP2013512251A (ja) 2009-11-24 2013-04-11 アンプリミューン、インコーポレーテッド Pd−l1/pd−l2の同時阻害
US20130089554A1 (en) 2009-12-29 2013-04-11 Emergent Product Development Seattle, Llc RON Binding Constructs and Methods of Use Thereof
US9198972B2 (en) 2010-01-28 2015-12-01 Alnylam Pharmaceuticals, Inc. Monomers and oligonucleotides comprising cycloaddition adduct(s)
CA2804375C (en) 2010-07-19 2018-08-21 Gilead Sciences, Inc. Methods for the preparation of diasteromerically pure phosphoramidate prodrugs
WO2012040124A1 (en) 2010-09-22 2012-03-29 Alios Biopharma, Inc. Azido nucleosides and nucleotide analogs
US20130108641A1 (en) 2011-09-14 2013-05-02 Sanofi Anti-gitr antibodies
ES2808152T3 (es) 2011-11-28 2021-02-25 Merck Patent Gmbh Anticuerpos anti-PD-L1 y usos de los mismos
AR091649A1 (es) 2012-07-02 2015-02-18 Bristol Myers Squibb Co Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos
JP6284547B2 (ja) 2012-12-21 2018-02-28 アリオス バイオファーマ インク. 置換ヌクレオシド、置換ヌクレオチドおよびそれらの類似体
TW201542578A (zh) * 2013-06-26 2015-11-16 Alios Biopharma Inc 經取代之核苷、核苷酸及其類似物
EA201690526A1 (ru) * 2013-10-11 2017-02-28 Алиос Биофарма, Инк. Замещенные нуклеозиды, нуклеотиды и их аналоги
LT3160476T (lt) * 2014-06-24 2021-04-12 Janssen Biopharma, Inc. Pakeistieji nukleozidai, nukleotidai ir jų analogai, skirti naudoti virusinių infekcijų gydyme
WO2017163186A1 (en) * 2016-03-24 2017-09-28 Novartis Ag Alkynyl nucleoside analogs as inhibitors of human rhinovirus

Also Published As

Publication number Publication date
JP2019509316A (ja) 2019-04-04
TW201736391A (zh) 2017-10-16
EP4292658A3 (en) 2024-03-06
PT3433257T (pt) 2023-11-29
EP3433257B1 (en) 2023-10-11
US20180258129A1 (en) 2018-09-13
ES2962269T3 (es) 2024-03-18
CN109311885A (zh) 2019-02-05
EP4292658A2 (en) 2023-12-20
DK3433257T3 (da) 2024-01-02
WO2017163186A1 (en) 2017-09-28
UY37166A (es) 2017-10-31
EP3433257A1 (en) 2019-01-30
US9988416B2 (en) 2018-06-05
FI3433257T3 (fi) 2024-01-08
JP7005508B2 (ja) 2022-01-21
TWI746532B (zh) 2021-11-21
PL3433257T3 (pl) 2024-02-12
US20170275329A1 (en) 2017-09-28
US10428105B2 (en) 2019-10-01

Similar Documents

Publication Publication Date Title
ECSP23095674A (es) Análogos de triazolo pirimidina para el tratamiento de enfermedades relacionadas con la inhibición de la helicasa recq del síndrome de werner (wrn)
AR117616A1 (es) Compuestos anti-vih
AR111407A1 (es) Compuestos inhibidores de ask1 y usos de los mismos
UY37133A (es) Derivados de pirazolo[1,5-a]pirazin-4-ilo
AR100809A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
NI201700020A (es) Compuestos de aminopirimidinilo como inhibidores de jak
AR101600A1 (es) COMPUESTOS DE SPIRO[3H-INDOL-3,2-PIRROLIDIN]-2(1H)-ONA Y DERIVADOS COMO INHIBIDORES DE MDM2-p53
AR102177A1 (es) Compuestos de heteroarilo como inhibidores de btk y usos de los mismos
AR110298A1 (es) Compuestos de heterociclo tetracíclicos útiles como inhibidores de la integrasa del vih
AR089143A1 (es) Triazolopiridinas sustituidas con actividad inhibidora de ttk
AR101106A1 (es) Inhibidores de tirosina quinasa de bruton
AR100808A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR109437A1 (es) Derivados de n-(piridin-2-il)piridina-sulfonamida y su uso en el tratamiento de enfermedades
AR106070A1 (es) Benzamidas sustituidas con isoxazolina como insecticidas
AR097199A1 (es) Inhibidores de rorc2 y sus métodos de uso
CO2019004978A2 (es) Compuestos terapéuticos y métodos para utilizarlos
JOP20190115B1 (ar) مثبّطات إنزيم بولي (adp-ريبوز) بوليمراز (parp)
AR094496A1 (es) Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas
AR096846A1 (es) Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas como inhibidores de la proteína bet
AR097948A1 (es) Inhibidores de la proteasa de cisteína catepsina
AR101638A1 (es) Combinaciones de inhibidores de la recaptación de serotonina-norepinefrina (irsn) y ligandos del receptores sigma
AR094497A1 (es) Compuestos tetracíclicos sustituidos con tiofeno y métodos de uso de los mismos para el tratamiento de enfermedades víricas
AR117472A1 (es) Inhibidores de tienopiridina de ripk2
AR107974A1 (es) Análogos de nucleósidos alquinil como inhibidores de rinovirus humanos
AR114082A1 (es) INHIBIDORES DE LA PI4KIIIb