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AR091279A1 - Inhibidores macrociclicos de virus flaviviridae - Google Patents

Inhibidores macrociclicos de virus flaviviridae

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Publication number
AR091279A1
AR091279A1 ARP130101987A AR091279A1 AR 091279 A1 AR091279 A1 AR 091279A1 AR P130101987 A ARP130101987 A AR P130101987A AR 091279 A1 AR091279 A1 AR 091279A1
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AR
Argentina
Prior art keywords
alkyl
heterocycloalkyl
cycloalkyl
alkylene
aryl
Prior art date
Application number
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English (en)
Inventor
Alexandra Steadman Victoria
G Poullennec Karine
Lazarides Linos
Aciro Caroline
Kenneth Dean David
John Keats Andrew
Scott Siegel Dustin
James Schrier Adam
Mackman Richard
Jansa Petr
Original Assignee
Gilead Sciences Inc
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Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR091279A1 publication Critical patent/AR091279A1/es

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    • 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15—Depsipeptides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/02—Bacterial antigens
    • A61K39/05—Actinobacteria, e.g. Actinomyces, Streptomyces, Nocardia, Bifidobacterium, Gardnerella, Corynebacterium; Propionibacterium
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/12—Viral antigens
    • A61K39/29—Hepatitis virus
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P31/12—Antivirals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18—Bridged systems
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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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Abstract

Los compuestos, composiciones, y métodos son útiles para el tratamiento de infecciones virales, en particular infecciones por el virus de hepatitis C. Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1) o una sal farmacéuticamente aceptable del mismo, donde: A es una unión, -O-, -S(O)ₙ-, -NH-, -N(alquilo C₁₋₄)- o alquileno C₁₋₂; A¹ es alquileno C₁₋₅, alquenileno C₂₋₅, alquinileno C₂₋₅, arileno, heteroarileno, cicloalquileno, heterociclo-alquileno, aril-alquileno C₁₋₂, heteroaril-alquileno C₁₋₂, cicloalquil-alquileno C₁₋₂ o heterocicloalquil-alquileno C₁₋₂, donde un átomo de carbono sp³ de A¹ opcionalmente se reemplaza por -O-, -S(O)ₙ-, -NH- o -N(alquilo C₁₋₄)-, y donde un átomo de carbono sp³ o sp² de A¹ está sustituido opcionalmente con uno o más grupos seleccionados entre el grupo que consiste en halo, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, arilo, heterocicloalquilo, cicloalquilo, arilalquilo C₁₋₄, cicloalquilalquilo C₁₋₄, heterocicloalquil-alquilo C₁₋₄, arilheterocicloalquil-alquilo C₁₋₄, -OR⁹, -SR⁹, -S(O)R⁹, -S(O)₂R⁹ y -N(R⁹)₂; A² es -CH(R⁸)-arileno, -CH(R⁸)-heteroarileno, -CH(R⁸)-heterocicloalquileno, -CH(R⁸)-cicloalquileno, arileno, cicloalquileno, alquileno C₁₋₃, alquenileno C₂₋₃ o alquinileno C₂₋₃, donde A² está sustituido opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en -OR⁹, -SR⁹, -S(O)R⁹, -S(O)₂R⁹, -N(R⁹)₂, halo, haloalquilo C₁₋₄, haloalcoxi C₁₋₄, ciano y alquilo C₁₋₈; L¹ es -O-C(O)-, -O-CH₂-, -NR¹⁰-C(O)-, -NR¹¹-CH₂-, -NH-C(R¹⁰)₂- o -NH-S(O)₂-, donde cada R¹⁰ es en forma independiente H, alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₁₋₄ o cicloalquilo; y R¹¹ es alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₁₋₄ o cicloalquilo; X¹ es una unión, -O-, -NH-, -N(alquilo C₁₋₄)- o heterociclo-alquileno; R¹ y R² son en forma independiente H, alquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, halo, ciano o -C(O)-alquilo C₁₋₄; o R¹ y R², cuando se toman junto con el carbono al cual ambos están unidos, forman -C(=O)-, -C(=S)- o -C(=N-alquilo C₁₋₄)-; R³ es H o alquilo C₁₋₄ el cual está sustituido opcionalmente con halo, ciano, hidroxilo o alcoxi C₁₋₄; R⁴ᵃ y R⁴ᵇ son en forma independiente H, alquilo C₁₋₈, arilo, arilalquilo C₁₋₄, heterocicloalquilo, heterocicloalquil-alquilo C₁₋₄, cicloalquilo o cicloalquilalquilo C₁₋₄, donde cada R⁴ᵃ y R⁴ᵇ está sustituido opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en ciano, -COOH, halo, hidroxilo, amino, alcoxi C₁₋₈, monoalquil C₁₋₈amino, dialquil C₁₋₈amino, arilo y heteroarilo; R⁵ᵃ y R⁵ᵇ son en forma independiente H, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈, arilo, heterocicloalquilo, cicloalquilo, arilalquilo C₁₋₄, cicloalquilalquilo C₁₋₄ o heterocicloalquil-alquilo C₁₋₄, donde cada R⁵ᵃ y R⁵ᵇ está sustituido opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en -N₃, ciano, -COOH, halo, hidroxilo, amino, monoalquil C₁₋₈amino, dialquil C₁₋₈amino, alcoxi C₁₋₈, arilo y heteroarilo, o R⁵ᵃ y R⁵ᵇ juntos forman un espirociclo de fórmula (2), donde uno o más átomos de carbono del anillo de fórmula (2) opcionalmente se reemplaza por un átomo de nitrógeno, oxígeno o azufre, y donde un átomo del anillo de fórmula (2) opcionalmente tiene uno o más sustituyentes seleccionados entre el grupo que consiste en oxo, halo, hidroxilo, -NH₂, alquilo C₁₋₄, alcoxi C₁₋₄, -OC(O)R⁹, -C(O)₂R⁹, y -S(O)₂R⁹; R⁶ᵃ y R⁶ᵇ son en forma independiente H, hidroxilo, alquilo C₁₋₈, alquenilo C₂₋₈, alquinilo C₂₋₈, alcoxi C₁₋₈, -CH₂CH₂CR⁹(=N-alcoxi C₁₋₄), arilo, heterocicloalquilo, cicloalquilo, -SR⁹, -S(O)R⁹, -S(O)₂R⁹ y -N(R⁹)₂, donde cada de R⁶ᵃ y R⁶ᵇ está sustituido opcionalmente con uno o más sustituyentes seleccionados entre el grupo que consiste en halo, hidroxilo, ciano, alquilo C₁₋₄, alcoxi C₁₋₄, haloalcoxi C₁₋₄, arilo, cicloalquilo, heterocicloalquilo, monoalquil C₁₋₈amino, dialquil C₁₋₈amino, -NHS(O)R⁹, -NHC(O)R⁹ y alcanoilo C₁₋₈; o R⁶ᵃ y R⁶ᵇ juntos forman un espirociclo de fórmula (2); cada R⁸ es en forma independiente H, alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₂₋₄, alquinilo C₂₋₄, arilo, heteroarilo, heterocicloalquilo o cicloalquilo, donde R⁸ está sustituido opcionalmente con -O, -N(R⁹)₂, -CON(R⁹)₂, o ciano; cada R⁹ es en forma independiente H, alquilo C₁₋₄, haloalquilo C₁₋₄, alquenilo C₂₋₄ o alquinilo C₂₋₄; cada n es en forma independiente 0, 1 ó 2; y m es 1, 2, 3, 4 ó 5.
ARP130101987 2012-06-08 2013-06-05 Inhibidores macrociclicos de virus flaviviridae AR091279A1 (es)

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Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9428845B1 (en) 2010-12-28 2016-08-30 Warp Drive Bio, Inc. Identifying new therapeutic agents
SG11201408045UA (en) 2012-06-08 2015-01-29 Gilead Sciences Inc MACROCYCLIC INHIBITORS OF <i>FLAVIVIRIDAE</i> VIRUSES
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
EP2861604B1 (en) * 2012-06-08 2017-03-01 Gilead Sciences, Inc. Macrocyclic inhibitors of flaviviridae viruses
US9233974B2 (en) 2012-12-21 2016-01-12 Gilead Sciences, Inc. Antiviral compounds
UA118256C2 (uk) 2013-01-31 2018-12-26 Гіліад Фармассет Елелсі Комбінований склад двох противірусних сполук
PL3650014T3 (pl) 2013-08-27 2022-01-31 Gilead Pharmasset Llc Preparat złożony dwóch związków przeciwwirusowych
US20150150897A1 (en) 2013-12-02 2015-06-04 Gilead Pharmasset Llc Methods of treating hepatitis c virus infection in subjects with cirrhosis
TW201609785A (zh) 2013-12-23 2016-03-16 吉李德製藥公司 固體型之抗病毒化合物
WO2015103509A1 (en) 2014-01-06 2015-07-09 Bristol-Myers Squibb Company Pyrrolidinyl sulfone derivatives and their use as ror gamma modulators
SG11201705069YA (en) 2014-12-26 2017-07-28 Univ Emory N4-hydroxycytidine and derivatives and anti-viral uses related thereto
EP3247378B8 (en) 2015-01-09 2023-08-23 Revolution Medicines, Inc. Macrocyclic compounds that participate in cooperative binding and medical uses thereof
MD20170081A2 (ro) 2015-03-04 2018-03-31 Gilead Sciences, Inc. Compuşi 4,6-diamino-pirido[3,2-D]pirimidină modulatori ai receptorilor de tip Toll
JP2018525412A (ja) 2015-08-26 2018-09-06 ギリアード サイエンシーズ， インコーポレイテッド 重水素化トール様受容体調節因子
US9989535B2 (en) 2015-10-01 2018-06-05 Warp Drive Bio, Inc. Methods and reagents for analyzing protein-protein interfaces
WO2017184670A2 (en) 2016-04-22 2017-10-26 Gilead Sciences, Inc. Methods for treating zika virus infections
WO2017197051A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Amine-linked c3-glutarimide degronimers for target protein degradation
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4483875A2 (en) 2016-05-10 2025-01-01 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
BR102017010009A2 (pt) 2016-05-27 2017-12-12 Gilead Sciences, Inc. Compounds for the treatment of hepatitis b virus infection
WO2017205078A1 (en) 2016-05-27 2017-11-30 Gilead Sciences, Inc. Methods for treating hepatitis b virus infections using ns5a, ns5b or ns3 inhibitors
BR102017011025A2 (pt) 2016-06-02 2017-12-19 Gilead Pharmasset Llc Formulation of combination of three antiviral compounds
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
EP3507288B1 (en) 2016-09-02 2020-08-26 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
ES2906581T3 (es) 2016-09-02 2022-04-19 Gilead Sciences Inc Compuestos moduladores de los receptores tipo Toll
CA3040143A1 (en) 2016-10-14 2018-04-19 Precision Biosciences, Inc. Engineered meganucleases specific for recognition sequences in the hepatitis b virus genome
WO2018136559A1 (en) * 2017-01-17 2018-07-26 The Regents Of The University Of California Methods for treating flaviviruses and zika infections
TWI714820B (zh) 2017-01-31 2021-01-01 美商基利科學股份有限公司 替諾福韋艾拉酚胺(tenofovir alafenamide)之晶型
JOP20180008A1 (ar) 2017-02-02 2019-01-30 Gilead Sciences Inc مركبات لعلاج إصابة بعدوى فيروس الالتهاب الكبدي b
US20220235013A1 (en) 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
JOP20180040A1 (ar) 2017-04-20 2019-01-30 Gilead Sciences Inc مثبطات pd-1/pd-l1
WO2018232174A2 (en) * 2017-06-16 2018-12-20 Avalon Flaviviral Therapeutics (Hk) Limited Compositions and methods for treating flavivirus infections
AU2018319538B9 (en) 2017-08-22 2021-05-27 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
AU2018378832B9 (en) 2017-12-07 2021-05-27 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
US10966999B2 (en) 2017-12-20 2021-04-06 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
JP7098748B2 (ja) 2017-12-20 2022-07-11 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． Ｓｔｉｎｇアダプタータンパク質を活性化するホスホン酸結合を有する２’３’環状ジヌクレオチド
CN118084940A (zh) 2018-02-13 2024-05-28 吉利德科学公司 Pd-1/pd-l1抑制剂
WO2019165374A1 (en) 2018-02-26 2019-08-29 Gilead Sciences, Inc. Substituted pyrrolizine compounds as hbv replication inhibitors
EP3774883A1 (en) 2018-04-05 2021-02-17 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TW201945388A (zh) 2018-04-12 2019-12-01 美商精密生物科學公司 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶
CA3097231A1 (en) 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
US10899735B2 (en) 2018-04-19 2021-01-26 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
WO2019211799A1 (en) 2018-05-03 2019-11-07 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide
EP3818052A1 (en) 2018-07-06 2021-05-12 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
CA3104398A1 (en) 2018-07-06 2020-01-09 Gilead Sciences, Inc. Therapeutic heterocyclic compounds
KR102625712B1 (ko) 2018-07-13 2024-01-19 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
AU2019366355B2 (en) 2018-10-24 2022-10-13 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
CN112969505B (zh) 2018-10-31 2023-11-14 吉利德科学公司 具有hpk1抑制活性的取代的6-氮杂苯并咪唑化合物
HRP20240541T1 (hr) 2018-10-31 2024-07-05 Gilead Sciences, Inc. Supstituirani spojevi 6-azabenzimidazola kao inhibitori hpk1
SG11202106605VA (en) * 2018-12-21 2021-07-29 Revolution Medicines Inc Compounds that participate in cooperative binding and uses thereof
WO2020178768A1 (en) 2019-03-07 2020-09-10 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
CN113543851A (zh) 2019-03-07 2021-10-22 捷克共和国有机化学与生物化学研究所 2’3’-环二核苷酸及其前药
US20220143061A1 (en) 2019-03-07 2022-05-12 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3'-cyclic dinucleotides and prodrugs thereof
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
CA3140708A1 (en) 2019-06-18 2020-12-24 Helen Horton Combination of hepatitis b virus (hbv) vaccines and pyridopyrimidine derivatives
BR112021026376A2 (pt) 2019-06-25 2022-05-10 Gilead Sciences Inc Proteínas de fusão flt3l-fc e métodos de uso
US20220257619A1 (en) 2019-07-18 2022-08-18 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
US20220296619A1 (en) 2019-08-19 2022-09-22 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
FI4037708T3 (fi) 2019-09-30 2024-10-31 Gilead Sciences Inc Hbv-rokotteita ja menetelmiä, hbv:n hoitamiseksi
WO2021091982A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
TW202132315A (zh) 2019-11-04 2021-09-01 美商銳新醫藥公司 Ras 抑制劑
BR112022008535A2 (pt) 2019-11-04 2022-08-09 Revolution Medicines Inc Composto, composição farmacêutica, métodos para tratar câncer e um distúrbio relativo à proteína ras
EP4069729B1 (en) 2019-12-06 2025-01-22 Precision BioSciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome
TW202421168A (zh) 2020-03-20 2024-06-01 美商基利科學股份有限公司 4’-c-經取代-2-鹵基-2’-去氧腺苷核苷之前藥及其製造與使用方法
JPWO2021221043A1 (es) * 2020-04-30 2021-11-04
BR112023002164A2 (pt) 2020-08-07 2023-03-14 Gilead Sciences Inc Profármacos de análogos de nucleotídeos de fosfonamida e seu uso farmacêutico
WO2022060836A1 (en) 2020-09-15 2022-03-24 Revolution Medicines, Inc. Indole derivatives as ras inhibitors in the treatment of cancer
TWI815194B (zh) 2020-10-22 2023-09-11 美商基利科學股份有限公司 介白素2-Fc融合蛋白及使用方法
TW202310852A (zh) 2021-05-13 2023-03-16 美商基利科學股份有限公司 ＴＬＲ８調節化合物及抗ＨＢＶ ｓｉＲＮＡ療法之組合
CR20230585A (es) 2021-06-23 2024-02-19 Gilead Sciences Inc Compuestos Moduladores de Diacilglicerol Quinasa.
CN117396478A (zh) 2021-06-23 2024-01-12 吉利德科学公司 二酰基甘油激酶调节化合物
AU2022299051A1 (en) 2021-06-23 2023-12-07 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
JP2024524210A (ja) 2021-06-23 2024-07-05 ギリアード サイエンシーズ， インコーポレイテッド ジアシルグリセロールキナーゼ調節化合物
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
GB202207348D0 (en) 2022-05-19 2022-07-06 Cypralis Ltd Macrocyclic compounds and uses thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS62193147A (ja) 1986-02-19 1987-08-25 Toshiba Corp 半導体装置の製造方法
US6124453A (en) 1995-07-04 2000-09-26 Novartis Ag Macrolides
AR006514A1 (es) * 1995-07-04 1999-09-08 Sandoz Ag Un macrolido, sus usos, un proceso para producirlo, un aislado biologicamente puro capaz de producirlo, y una composicion farmaceutica quelo comprende
JP2003510360A (ja) 1999-10-04 2003-03-18 メルク エンド カムパニー インコーポレーテッド インテグリン受容体拮抗薬
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
US20050159345A1 (en) 2002-10-29 2005-07-21 Boehringer Ingelheim International Gmbh Composition for the treatment of infection by Flaviviridae viruses
JP2008505100A (ja) 2004-06-30 2008-02-21 シェーリング　コーポレイション ガンマ−セクレターゼ阻害剤としての置換ｎ−アリールスルホニル複素環アミン
AU2006259411B2 (en) 2005-06-16 2012-03-22 Gilead Sciences, Inc. Prodrugs of A2B adenosine receptor antagonists
EP1893211B1 (en) 2005-06-17 2011-09-14 Novartis AG Use of sanglifehrin in hcv
CL2008003384A1 (es) * 2007-11-14 2009-12-11 Enanta Pharm Inc Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c.
KR101164602B1 (ko) 2008-01-09 2012-07-10 주식회사 케이알바이오텍 배큘로바이러스?기반 백신
US20100080770A1 (en) 2008-09-29 2010-04-01 Bristol-Myers Squibb Company Hepatitis C Virus Inhibitors
MX2011006764A (es) * 2008-12-23 2011-08-03 Ortho Mcneil Janssen Pharm Procedimiento y compuestos intermedios para preparar un inhibidor de proteasa macrociclico del vhc.
UY33183A (es) 2010-01-15 2011-08-31 Gilead Sciences Inc Compuestos inhibidores de virus flaviviridae, composición farmaceutica que los contiene y su uso en la manufactura de un medicamento
WO2011098808A1 (en) 2010-02-09 2011-08-18 Biotica Technology Limited Sanglifehrin based compounds
GB201008123D0 (en) 2010-05-17 2010-06-30 Biotica Tech Ltd Novel compounds
WO2012040040A1 (en) 2010-09-21 2012-03-29 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
UY33775A (es) 2010-12-10 2012-07-31 Gilead Sciences Inc Inhibidores macrocíclicos de virus flaviviridae, composiciones farmacéuticas que los comprenden y sus usos
EP2861604B1 (en) * 2012-06-08 2017-03-01 Gilead Sciences, Inc. Macrocyclic inhibitors of flaviviridae viruses
AR091279A1 (es) 2012-06-08 2015-01-21 Gilead Sciences Inc Inhibidores macrociclicos de virus flaviviridae
IN2014MN02467A (es) 2012-06-08 2015-07-10 Glenmark Pharmaceuticals Sa
SG11201408045UA (en) 2012-06-08 2015-01-29 Gilead Sciences Inc MACROCYCLIC INHIBITORS OF <i>FLAVIVIRIDAE</i> VIRUSES

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