CO2020004301A2 - Derivados de 1-benzil-2-imino-4-fenil-5-oxoimidazolidina como inhibidores de la proteasa del vih - Google Patents

Derivados de 1-benzil-2-imino-4-fenil-5-oxoimidazolidina como inhibidores de la proteasa del vih

Info

Publication number
CO2020004301A2
CO2020004301A2 CONC2020/0004301A CO2020004301A CO2020004301A2 CO 2020004301 A2 CO2020004301 A2 CO 2020004301A2 CO 2020004301 A CO2020004301 A CO 2020004301A CO 2020004301 A2 CO2020004301 A2 CO 2020004301A2
Authority
CO
Colombia
Prior art keywords
imino
benzyl
phenyl
formula
protease inhibitors
Prior art date
Application number
CONC2020/0004301A
Other languages
English (en)
Inventor
Aesop Cho
Salman Y Jabri
Jie Xu
Zhenhong R Cai
Ryan Mcfadden
Yingmei Qi
Johannes Voigt
Lianhong Xu
Hong Yang
Buenrostro Ana Zurisadai Gonzalez
Xiaochun Han
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of CO2020004301A2 publication Critical patent/CO2020004301A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D247/00—Heterocyclic compounds containing rings having two nitrogen atoms as the only ring hetero atoms, according to more than one of groups C07D229/00 - C07D245/00
    • 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/41—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/88—Nitrogen atoms, e.g. allantoin
    • 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
    • C07D401/10—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 linked by a carbon chain containing aromatic rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (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)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La invención proporciona un compuesto de Fórmula I: o una sal farmacéuticamente aceptable del mismo como se describe a continuación. La invención también proporciona composiciones farmacéuticas que comprenden un Compuesto de Fórmula I, procesos para preparar Compuestos de Fórmula I, métodos terapéuticos para tratar la proliferación del virus VIH, tratar el SIDA o retrasar la aparición de síntomas de SIDA en un mamífero usando Compuestos de Fórmula I.
CONC2020/0004301A 2017-10-13 2020-04-08 Derivados de 1-benzil-2-imino-4-fenil-5-oxoimidazolidina como inhibidores de la proteasa del vih CO2020004301A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762572243P 2017-10-13 2017-10-13
PCT/US2018/055554 WO2019075291A1 (en) 2017-10-13 2018-10-12 1-BENZYL-2-IMINO-4-PHENYL-5-OXOIMIDAZOLIDINE DERIVATIVES AS INHIBITORS OF HIV PROTEASE

Publications (1)

Publication Number Publication Date
CO2020004301A2 true CO2020004301A2 (es) 2020-05-15

Family

ID=64051787

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2020/0004301A CO2020004301A2 (es) 2017-10-13 2020-04-08 Derivados de 1-benzil-2-imino-4-fenil-5-oxoimidazolidina como inhibidores de la proteasa del vih

Country Status (23)

Country Link
US (2) US10774053B2 (es)
EP (1) EP3694846B1 (es)
JP (2) JP7136892B2 (es)
KR (1) KR102515284B1 (es)
CN (1) CN111212832B (es)
AR (1) AR113765A1 (es)
AU (1) AU2018347541C1 (es)
BR (1) BR102018071016A2 (es)
CA (1) CA3076761C (es)
CL (1) CL2020000886A1 (es)
CO (1) CO2020004301A2 (es)
CR (1) CR20200149A (es)
EA (1) EA202090530A1 (es)
ES (1) ES2979368T3 (es)
IL (1) IL273842A (es)
JO (1) JOP20180092A1 (es)
MX (1) MX2020003430A (es)
PE (1) PE20201497A1 (es)
PH (1) PH12020550256A1 (es)
PL (1) PL3694846T3 (es)
SG (1) SG11202002235XA (es)
TW (2) TWI697491B (es)
WO (1) WO2019075291A1 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102498819B1 (ko) 2017-04-11 2023-02-10 미쓰이가가쿠 아그로 가부시키가이샤 피리돈 화합물 및 그것을 유효성분으로 하는 농원예용 살균제
KR20240151256A (ko) 2019-03-22 2024-10-17 길리애드 사이언시즈, 인코포레이티드 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도
WO2020214647A1 (en) * 2019-04-17 2020-10-22 Gilead Sciences, Inc. Solid forms of an hiv protease inhibitor
TW202104210A (zh) * 2019-04-17 2021-02-01 美商基利科學股份有限公司 Hiv蛋白酶抑制劑
KR102987126B1 (ko) 2020-03-20 2026-07-07 길리애드 사이언시즈, 인코포레이티드 4'-c-치환된-2-할로-2'-데옥시아데노신 뉴클레오시드의 프로드러그 및 이의 제조 및 사용 방법
WO2021226208A2 (en) 2020-05-05 2021-11-11 Nuvalent, Inc. Heteroaromatic macrocyclic ether chemotherapeutic agents
KR102698413B1 (ko) 2020-05-05 2024-08-26 뉴베일런트, 아이엔씨. 헤테로방향족 거대환식 에터 화학치료제
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
CN116437958A (zh) 2020-11-11 2023-07-14 吉利德科学公司 鉴定对采用gp120 CD4结合位点导向的抗体的疗法敏感的HIV患者的方法
TW202320768A (zh) 2021-10-01 2023-06-01 美商努法倫特公司 雜芳族大環醚化合物之固體形式、醫藥組成物及製備
WO2023074936A1 (ko) * 2021-10-27 2023-05-04 주식회사 오토텍바이오 Ubr 박스 도메인 결합 리간드를 이용한 이중기능성 화합물
AU2022399845B2 (en) 2021-12-03 2026-03-26 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
AU2022403012B2 (en) 2021-12-03 2026-02-12 Gilead Sciences, Inc. Therapeutic compounds for hiv virus infection
FI4440702T3 (fi) 2021-12-03 2025-08-08 Gilead Sciences Inc Terapeuttisia yhdisteitä hiv-virusinfektiota varten
TWI856796B (zh) 2022-04-06 2024-09-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
CN115260167B (zh) * 2022-08-01 2025-01-21 陕西盘龙药业集团股份有限公司 一种3-四唑基甲基-1,3,5-三嗪-2,4-二酮类化合物及其制备方法和应用
CN119768183A (zh) 2022-08-26 2025-04-04 吉利德科学公司 用于广泛中和抗体的给药和安排方案
WO2024076915A1 (en) 2022-10-04 2024-04-11 Gilead Sciences, Inc. 4'-thionucleoside analogues and their pharmaceutical use
CN116270698A (zh) * 2023-03-01 2023-06-23 上海复星医药产业发展有限公司 一种复方固体制剂及制备方法和应用
CN116270699A (zh) * 2023-03-07 2023-06-23 上海复星医药产业发展有限公司 一种三方制剂及制备方法和应用
EP4698174A1 (en) 2023-04-19 2026-02-25 Gilead Sciences, Inc. Dosing regimen of capsid inhibitor
WO2024249573A1 (en) 2023-05-31 2024-12-05 Gilead Sciences, Inc. Solid forms of compounds useful in the treatment of hiv
CN122295099A (zh) 2023-07-28 2026-06-26 吉利德科学公司 用于治疗和预防hiv的来那卡帕韦的每周方案
AU2023462614A1 (en) 2023-08-23 2026-03-19 Gilead Sciences, Inc. Dosing regimen of hiv capsid inhibitor
IL327206A (en) 2023-10-11 2026-05-01 Gilead Sciences Inc Bridged tricyclic carbamoylpyridone compounds and their uses
AU2024360779A1 (en) 2023-10-11 2026-04-16 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
KR20260093341A (ko) 2023-10-11 2026-06-19 길리애드 사이언시즈, 인코포레이티드 가교 트리시클릭 카르바모일피리돈 화합물 및 이의 용도
WO2025137245A1 (en) 2023-12-22 2025-06-26 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025184447A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2025184452A1 (en) 2024-03-01 2025-09-04 Gilead Sciences, Inc. Solid forms of hiv integrase inhibitors
WO2025260028A1 (en) 2024-06-14 2025-12-18 Gilead Sciences, Inc. Pharmaceutical compositions comprising hiv integrase inhibitors
WO2026076265A1 (en) 2024-10-03 2026-04-09 Gilead Sciences, Inc. Combination therapy comprising bridged tricyclic carbamoylpyridone compounds and p-glycoprotein inhibitors

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4326525A (en) 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US5364620A (en) 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4902514A (en) 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
IL102183A (en) 1991-06-27 1999-11-30 Takeda Chemical Industries Ltd Biphenyl substituted heterocyclic compounds their production and pharmaceutical compositions comprising them
GB0016787D0 (en) * 2000-07-07 2000-08-30 Pfizer Ltd Compounds useful in therapy
SI1762567T1 (sl) * 2001-04-10 2012-08-31 Pfizer Derivati pirazola za zdravljenje HIV-a
SG182849A1 (en) 2003-04-25 2012-08-30 Gilead Sciences Inc Antiviral phosphonate analogs
CA2548388A1 (en) * 2003-12-15 2005-06-30 Schering Corporation Heterocyclic aspartyl protease inhibitors
US7763609B2 (en) * 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
DOP2005000123A (es) 2004-07-02 2011-07-15 Merck Sharp & Dohme Inhibidores de cetp
PT2258376T (pt) 2004-07-27 2019-05-31 Gilead Sciences Inc Análogos fosfonatados de compostos inibidores do vih
WO2007059195A1 (en) 2005-11-14 2007-05-24 University Of Southern California Integrin-binding small molecules
ATE516016T1 (de) 2005-12-05 2011-07-15 Merck Sharp & Dohme Selbstemulgierende formulierungen von cetp- hemmern
WO2007081569A2 (en) 2005-12-30 2007-07-19 Merck & Co., Inc. Cetp inhibitors
JP5040036B2 (ja) 2005-12-30 2012-10-03 メルク・シャープ・エンド・ドーム・コーポレイション Ｃｅｔｐ阻害剤として有用な１，３−オキサゾリジン−２−オン誘導体
US7781426B2 (en) 2005-12-30 2010-08-24 Merck Sharp & Dohme Corp. CETP inhibitors
CN101378731B (zh) 2006-02-09 2014-03-05 默沙东公司 Cetp抑制剂的聚合物制剂
US8354429B2 (en) 2007-11-16 2013-01-15 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
WO2009070305A1 (en) 2007-11-26 2009-06-04 Eisai E & D Management Co., Ltd. Method of making imidazoazepinone compounds
UY32306A (es) 2008-12-09 2010-07-30 Gilead Sciences Inc Derivados de pteridinona y pirimidinodiazepinona y composiciones farmacéuticas que modulan en forma selectiva los receptores tipo toll, métodos y usos
US8338441B2 (en) 2009-05-15 2012-12-25 Gilead Sciences, Inc. Inhibitors of human immunodeficiency virus replication
WO2011133719A2 (en) 2010-04-23 2011-10-27 Kineta, Inc. Anti-viral compounds
WO2011139637A1 (en) 2010-05-03 2011-11-10 Philadelphia Health & Education Corporation Small-molecule modulators of hiv-1 capsid stability and methods thereof
CN103140474A (zh) 2010-07-02 2013-06-05 吉里德科学公司 治疗aids的萘-2-基乙酸衍生物
EP2588455B1 (en) 2010-07-02 2018-04-04 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
MX2013012266A (es) 2011-04-21 2013-11-22 Gilead Sciences Inc Compuestos de benzotiazol y su uso farmaceutico.
CA2840095A1 (en) 2011-07-06 2013-01-10 Gilead Sciences, Inc. Compounds for the treatment of hiv
CN102863512B (zh) 2011-07-07 2016-04-20 上海泓博智源医药技术有限公司 抗病毒化合物
JP6144698B2 (ja) 2011-12-20 2017-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｈｉｖ複製の阻害剤としての縮合三環式化合物
ES2571479T3 (es) 2012-04-20 2016-05-25 Gilead Sciences Inc Derivados del ácido benzotiazol-6-il acético y su uso para tratar una infección por VIH
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
US9169214B2 (en) 2012-12-21 2015-10-27 The Board Of Trustees Of The Leland Stanford Junior University Compounds and compositions that bind and stabilize transthyretin and their use for inhibiting transthyretin amyloidosis and protein-protein interactions
HK1214817A1 (en) 2012-12-27 2016-08-05 Japan Tobacco Inc. Substituted spiropyrido[1,2-a]pyrazine derivative and medicinal use thereof as hiv integrase inhibitor
WO2014130582A2 (en) 2013-02-19 2014-08-28 Senomyx, Inc. Compounds useful as modulators of trpm8
US20160024071A1 (en) 2013-03-15 2016-01-28 Elan Pharmaceuticals, Llc Inhibitors of lrrk2 kinase activity
ES2834430T3 (es) 2013-03-15 2021-06-17 Univ Southern California Procedimientos, compuestos y composiciones para el tratamiento de enfermedades relacionadas con la angiotensina
US20190046507A1 (en) * 2016-02-18 2019-02-14 Merck Sharp & Dohme Corp. Compounds for the treatment of malaria
EP3551192A4 (en) * 2016-12-06 2020-07-08 Merck Sharp & Dohme Corp. HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS
EP3558285A4 (en) * 2016-12-22 2020-09-09 Merck Sharp & Dohme Corp. USEFUL HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS
WO2018118829A1 (en) * 2016-12-22 2018-06-28 Merck Sharp & Dohme Corp. Heterocyclic compounds as hiv protease inhibitors

Also Published As

Publication number Publication date
US10774053B2 (en) 2020-09-15
AR113765A1 (es) 2020-06-10
AU2018347541A1 (en) 2020-04-16
JP7136892B2 (ja) 2022-09-13
JOP20180092A1 (ar) 2019-04-13
CA3076761C (en) 2024-03-26
IL273842A (en) 2020-05-31
WO2019075291A1 (en) 2019-04-18
US20190210978A1 (en) 2019-07-11
KR102515284B1 (ko) 2023-03-31
US11352329B2 (en) 2022-06-07
MX2020003430A (es) 2020-07-29
JP2021178852A (ja) 2021-11-18
PE20201497A1 (es) 2020-12-29
TWI697491B (zh) 2020-07-01
PL3694846T3 (pl) 2024-08-26
ES2979368T3 (es) 2024-09-25
EP3694846B1 (en) 2024-05-08
SG11202002235XA (en) 2020-04-29
BR102018071016A2 (pt) 2019-05-07
EP3694846C0 (en) 2024-05-08
EP3694846A1 (en) 2020-08-19
TW202045490A (zh) 2020-12-16
AU2018347541B2 (en) 2021-06-17
JP2020536911A (ja) 2020-12-17
US20210078959A1 (en) 2021-03-18
PH12020550256A1 (en) 2021-03-01
CL2020000886A1 (es) 2020-10-09
CN111212832A (zh) 2020-05-29
TW201927766A (zh) 2019-07-16
KR20200071098A (ko) 2020-06-18
EA202090530A1 (ru) 2020-10-06
AU2018347541C1 (en) 2022-01-13
CA3076761A1 (en) 2019-04-18
CR20200149A (es) 2020-05-22
CN111212832B (zh) 2023-09-15

Similar Documents

Publication Publication Date Title
DOP2019000201A (es) Compuestos inhibidores del vih
CL2020000886A1 (es) Derivados de 1-benzil-2-imino-4-fenil-5-oxoimidazolidina como inhibidores de la proteasa del vih.
AR118707A1 (es) Inhibidores de la proteasa del vih
DOP2020000102A (es) Compuestos útiles para inhibir a cdk7
ECSP22023220A (es) Derivados de indol mono o disustituidos como inhibidores de la replicación viral del dengue
UY37710A (es) Inhibidores de la replicación del virus de la inmunodeficiencia humana
CO6660497A2 (es) Derivados del ácido nft-2-ilacético para tratar el sida
CO2021005532A2 (es) Derivados de quinolina como inhibidores de la integrina alfa4beta7
UY37182A (es) Derivados de indolina sustituidos como inhibidores de la replicación viral del dengue
SG10201811384TA (en) Mnk inhibitors and methods related thereto
PH12018502026A1 (en) Substituted indole compound derivatives as dengue viral replication inhibitors
EA201692487A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
CO2018008421A2 (es) Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
CR20190446A (es) Derivados de indolina sustituidos como inhibidores de la replicación viral de dengue
UY37742A (es) Derivados de indolina sustituidos como inhibidores de la replicación vírica de dengue
CL2017001822A1 (es) Derivados de indol mono o disustituido como inhibidores de la replicación del virus del dengue
UY36339A (es) Indoles mono o disustituidos como inhibidores de la replicación del virus del dengue
CO2018009559A2 (es) Derivados de indol sustituidos como inhibidores de la replicación vírica del dengue
EA201692249A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
EA201692268A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
EA201692265A1 (ru) Ингибиторы фосфатидилинозитол-3-киназы
MX2020003732A (es) Derivado de anillo fusionado como inhibidor del receptor a2a.
MX2017013103A (es) Metodos para el tratamiento de trastornos cardiovasculares.
EA202091169A1 (ru) Применяемые в качестве ингибиторов iap миметики smac и их применение