HRP20031015A2 - Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis - Google Patents

Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis

Info

Publication number
HRP20031015A2
HRP20031015A2 HR20031015A HRP20031015A HRP20031015A2 HR P20031015 A2 HRP20031015 A2 HR P20031015A2 HR 20031015 A HR20031015 A HR 20031015A HR P20031015 A HRP20031015 A HR P20031015A HR P20031015 A2 HRP20031015 A2 HR P20031015A2
Authority
HR
Croatia
Prior art keywords
group
carbocyclic
aliphatic
image
heterocyclic
Prior art date
Application number
HR20031015A
Other languages
English (en)
Croatian (hr)
Inventor
S. Canon-Koch Stacie
N. Alexander Therese
Barvian Mark
Bolton Gary
E. Boyer Fredrick
J. Burke Benjamin
Holler Tod
M. Jewell Tanya
Prasad Josyula Vara
David
Maria
Machak Jeff
J. Mitchell Lennert
T. Murphy Sean
H. Reich Siegfried
J. Skalitzky Donald
H. Tatlock John
D. Varney Michael
C. Virgil Scott
E. Webber Stephen
T. Worland Stephen
Melnick Michael
Original Assignee
Agouron Pharmaceuticals 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 Agouron Pharmaceuticals Inc. filed Critical Agouron Pharmaceuticals Inc.
Publication of HRP20031015A2 publication Critical patent/HRP20031015A2/hr

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D277/06Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/52Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
HR20031015A 2001-06-11 2003-12-08 Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis HRP20031015A2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29746001P 2001-06-11 2001-06-11
US29772901P 2001-06-12 2001-06-12
PCT/US2002/018717 WO2002100844A2 (fr) 2001-06-11 2002-06-11 Inhibiteurs de la protease vih, compositions les contenant, leurs utilisations pharmaceutiques et materiaux utilises pour leur synthese

Publications (1)

Publication Number Publication Date
HRP20031015A2 true HRP20031015A2 (en) 2005-10-31

Family

ID=26970163

Family Applications (2)

Application Number Title Priority Date Filing Date
HR20031015A HRP20031015A2 (en) 2001-06-11 2003-12-08 Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
HR20031014A HRP20031014A2 (en) 2001-06-11 2003-12-08 Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis

Family Applications After (1)

Application Number Title Priority Date Filing Date
HR20031014A HRP20031014A2 (en) 2001-06-11 2003-12-08 Hiv protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis

Country Status (27)

Country Link
US (4) US6953858B2 (fr)
EP (3) EP1739082A1 (fr)
JP (2) JP2005508867A (fr)
KR (2) KR20040035601A (fr)
CN (2) CN1599729A (fr)
AP (2) AP1770A (fr)
AR (2) AR036093A1 (fr)
AU (2) AU2002316235A2 (fr)
BR (2) BR0210344A (fr)
CA (2) CA2450269A1 (fr)
EA (2) EA200400023A1 (fr)
GE (1) GEP20063890B (fr)
HN (1) HN2002000136A (fr)
HR (2) HRP20031015A2 (fr)
IL (2) IL159022A0 (fr)
IS (2) IS7049A (fr)
MA (2) MA27347A1 (fr)
MX (2) MXPA03011397A (fr)
NO (2) NO20035489D0 (fr)
NZ (2) NZ530024A (fr)
OA (2) OA12696A (fr)
PA (2) PA8547601A1 (fr)
PE (2) PE20040241A1 (fr)
PL (1) PL366622A1 (fr)
TN (1) TNSN03130A1 (fr)
TW (1) TW200538447A (fr)
WO (2) WO2002100844A2 (fr)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7169932B2 (en) 2001-06-11 2007-01-30 Pfizer Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis
US7094909B2 (en) 2001-06-11 2006-08-22 Agouron Pharmaceuticals, Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
JP2006076882A (ja) * 2002-09-13 2006-03-23 Sumitomo Pharmaceut Co Ltd 新規なジペプチド化合物及びその医薬用途
WO2005026114A1 (fr) * 2003-09-17 2005-03-24 Pfizer Inc. Inhibiteurs de la protease du vih, compositions les contenant et leurs utilisations pharmaceutiques
BRPI0417223A (pt) * 2003-12-04 2007-03-06 Pfizer métodos de preparar compostos úteis como inibidores de protease
EP1737818A2 (fr) * 2003-12-04 2007-01-03 Pfizer, Inc. Procedes pour la preparation d'amines stereoisomeriquement enrichies
BRPI0417248A (pt) * 2003-12-04 2007-03-06 Pfizer métodos de preparação de compostos utilizáveis como inibidores de protease
BRPI0417492A (pt) * 2003-12-09 2007-05-29 Pfizer composições compreendendo um inibidor de protease de hiv
MXPA06008632A (es) * 2004-01-30 2006-09-04 Pfizer Combinaciones terapeuticas.
KR20060127939A (ko) * 2004-01-30 2006-12-13 화이자 인코포레이티드 Hiv 프로테아제 억제제 및 사이토크롬 p450 효소 활성억제제를 포함하는 조성물
WO2005121094A1 (fr) * 2004-06-09 2005-12-22 Pfizer Limited Derives de piperazine et de piperidine utilises comme agents anti-vih
EP2707346A1 (fr) * 2011-05-13 2014-03-19 Vertex Pharmaceuticals Inc. Procédé de préparation d'inhibiteurs de la protéase
RU2666530C2 (ru) 2012-01-12 2018-09-11 Йейл Юниверсити Соединения и способы усиления деградации белков-мишеней и других полипептидов с помощью е3 убиквитин лигазы
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
AU2016209349B2 (en) 2015-01-20 2020-05-07 Arvinas, Inc. Compounds and methods for the targeted degradation of the Androgen Receptor
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
WO2016149668A1 (fr) 2015-03-18 2016-09-22 Arvinas, Inc. Composés et procédés de dégradation accrue de protéines ciblées
US20180147202A1 (en) 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
EP3370715A4 (fr) 2015-11-02 2019-05-15 Yale University Composés chimères de ciblage de protéolyse et procédés de préparation et d'utilisation de ceux-ci
WO2018053354A1 (fr) 2016-09-15 2018-03-22 Arvinas, Inc. Dérivés d'indole en tant qu'agents de dégradation des récepteurs des œstrogènes
PL3660004T3 (pl) 2016-10-11 2023-10-02 Arvinas Operations, Inc. Związki i sposoby do ukierunkowanej degradacji receptora androgenowego
KR20230127371A (ko) 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 타우(Tau)-단백질 표적화 프로탁(PROTAC) 및 관련 사용 방법
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
IL294423B2 (en) 2016-12-23 2024-01-01 Univ Yale Compounds and methods for targeted reduction of rapidly accelerated polypeptide fibrosarcoma
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018118598A1 (fr) 2016-12-23 2018-06-28 Arvinas, Inc. Composés et procédés pour la dégradation ciblée de polypeptides de kinase du foie fœtal
JP2020505327A (ja) 2016-12-23 2020-02-20 アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. Egfrタンパク質分解標的化キメラ分子およびその関連する使用方法
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
BR112019015312A2 (pt) 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
CA3095494C (fr) 2018-04-04 2023-11-07 Arvinas Operations, Inc. Modulateurs de proteolyse et procedes d'utilisation associes
CN112912376A (zh) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物
EP3999182A1 (fr) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Composés ciblant la protéine tau et procédés d'utilisation associés
CN112574201B (zh) * 2019-09-29 2024-04-19 四川科伦博泰生物医药股份有限公司 芳基胺类化合物、包含其的药物组合物及其制备方法和用途
CN110803996B (zh) * 2019-11-13 2022-01-11 台州市创源工业技术有限公司 一种羟基苄胺的合成方法
WO2021127443A1 (fr) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Composés et méthodes pour la dégradation ciblée du récepteur des androgènes
US20230157998A1 (en) 2020-03-06 2023-05-25 Pfizer Inc. Methods of Inhibiting SARS-CoV-2 Replication and Treating Corona Virus Disease 2019
WO2024054591A1 (fr) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Composés de dégradation de fibrosarcome rapidement accéléré (raf) et procédés d'utilisation associés

Family Cites Families (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6418260A (en) * 1987-07-14 1989-01-23 Sanyo Electric Co Transistor
US6313094B1 (en) * 1990-12-11 2001-11-06 Japan Energy Corporation β-amino-α-hydroxycarboxylic acid derivatives and HIV protease inhibitors
CA2056911C (fr) * 1990-12-11 1998-09-22 Yuuichi Nagano Inhibiteurs de la protease de vih
IL100899A (en) 1991-02-08 1997-06-10 Sankyo Co Beta-amino-alpha- hydroxycarboxylic acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same
ZA929869B (en) * 1991-12-20 1994-06-20 Syntex Inc Hiv protease inhibitors
DE69322127T2 (de) 1992-05-13 1999-06-24 Japan Energy Corp Verfahren zur Herstellung von Peptidderivaten und ihrer Salze
US5644028A (en) * 1992-05-13 1997-07-01 Japan Energy Corporation Process for producing peptide derivatives and salts therefor
ZA935697B (en) * 1992-08-07 1994-03-10 Sankyo Co Peptides capable of inhibiting the activity of hiv protease their preparation and their therapeutic use
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
EP0706794B1 (fr) 1994-10-14 2001-12-12 Japan Energy Corporation Composition pharmaceutique anti-SIDA et procédé de préparation
JPH08259532A (ja) 1995-03-24 1996-10-08 Japan Energy Corp ペプチド様化合物又はその薬理的に許容される塩
US6222043B1 (en) * 1995-06-30 2001-04-24 Japan Energy Corporation Methods of preparing novel dipeptide compounds or pharmaceutically acceptable salts thereof
CA2179935C (fr) * 1995-06-30 2010-09-07 Ryohei Kato Compose dipeptidique ou sel de ce dernier acceptable en pharmacie; utilisation en medecine
JPH1087489A (ja) 1996-09-13 1998-04-07 Sankyo Co Ltd Ahpba構造含有ジペプチド化合物を有効成分とする医薬
JPH10101654A (ja) 1996-10-02 1998-04-21 Japan Energy Corp 新規なジペプチド化合物又はその薬理的に許容される塩及びその医薬用途
JPH10182601A (ja) 1996-12-27 1998-07-07 Japan Energy Corp 新規なジペプチド化合物又はその薬理的に許容される塩及びその医薬用途
AR012374A1 (es) 1997-04-15 2000-10-18 Smithkline Beecham Corp Inhibidores de proteasas, composiones farmaceuticas y usos para la preparacion de medicamentos.
US6673772B2 (en) 1999-01-14 2004-01-06 Sumitomo Pharmaceuticals Company Limited Dipeptide compounds and their use as antiviral agents
EP1155009A2 (fr) 1999-02-19 2001-11-21 Oklahoma Medical Research Foundation Inhibiteurs de protease surmontant la resistance medicamenteuse
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
WO2003035650A1 (fr) 2001-09-25 2003-05-01 Takeda Chemical Industries, Ltd. Inhibiteur d'entree
JP2003119137A (ja) 2001-10-10 2003-04-23 Japan Tobacco Inc Hiv阻害剤
DE60218511T2 (de) 2001-10-26 2007-10-25 Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.P.A. Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
WO2003047564A1 (fr) 2001-12-05 2003-06-12 Shionogi & Co., Ltd. Dérivé ayant une activité d'inhibition de l'intégrase du vih
KR20040065251A (ko) 2001-12-12 2004-07-21 브리스톨-마이어스 스큅 컴퍼니 Hiv 인티그레이즈 억제제
ES2291642T3 (es) 2002-01-17 2008-03-01 MERCK & CO., INC. Hidroxinaftiridinoncarboxamidas utiles como inhibidores de la integrasa de vih.
TW200306192A (en) 2002-01-18 2003-11-16 Bristol Myers Squibb Co Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors
WO2005026114A1 (fr) * 2003-09-17 2005-03-24 Pfizer Inc. Inhibiteurs de la protease du vih, compositions les contenant et leurs utilisations pharmaceutiques
BRPI0417248A (pt) * 2003-12-04 2007-03-06 Pfizer métodos de preparação de compostos utilizáveis como inibidores de protease

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US6953858B2 (en) 2005-10-11
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