MA27347A1 - Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese - Google Patents

Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese

Info

Publication number
MA27347A1
MA27347A1 MA27423A MA27423A MA27347A1 MA 27347 A1 MA27347 A1 MA 27347A1 MA 27423 A MA27423 A MA 27423A MA 27423 A MA27423 A MA 27423A MA 27347 A1 MA27347 A1 MA 27347A1
Authority
MA
Morocco
Prior art keywords
compositions containing
hiv protease
compounds
materials
protease inhibitors
Prior art date
Application number
MA27423A
Other languages
English (en)
Inventor
Koch Stacie S Canan
Therese N Alexander
Mark R Barvian
Gary L Bolton
Frederick E Boyer Jr
Benjamin J Burke
Tod P Holler
Tanya M Jewell
Vara Prasad Venkata Na Josyula
David J Kucera
Maria A Linton
Jeff J Machak
Lennert J Mitchell Jr
Sean T Murphy
Siegfried H Reich
Donald J Skalitzky
John H Tatlock
Michael D Varney
Scott C Virgil
Stephen E Webber
Stephen T Worland
Michael Melnick
Original Assignee
Stephen T Worland
Michael Melnick
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 Stephen T Worland, Michael Melnick filed Critical Stephen T Worland
Publication of MA27347A1 publication Critical patent/MA27347A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
    • 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
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/08—Heterocyclic 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
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/04—Heterocyclic 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
    • C07D207/10—Heterocyclic 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/24—Heterocyclic 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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic 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
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/04—Heterocyclic 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
    • C07D277/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/12—Heterocyclic 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
    • C07D295/125—Heterocyclic 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
    • C07D295/13—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic 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
    • C07D307/38—Heterocyclic 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
    • C07D307/52—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D417/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D471/08—Bridged systems

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  • 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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)

Abstract

Inhibiteurs de protéase du VIH, compositions les contenant, leurs utilisations pharmaceutiques et matières pour leur synthèse TEXTE de L'ABREGE Des composés de formule (I), dans laquelle les variables répondant aux définitions figurant dans le présent mémoire, qui inhibent ou bloquent avantageusement l'activité biologique de la protéase du VIH, sont décrits. Ces composés, ainsi que des compositions pharmaceutiques contenant ces composés, sont utiles pour le traitement de patients ou d'hôtes infectés par le virus VIH. Des intermédiaires et des procédés de synthèse pour la préparation de ces composés sont également décrits.
MA27423A 2001-06-11 2003-12-04 Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese MA27347A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29746001P 2001-06-11 2001-06-11
US29772901P 2001-06-12 2001-06-12

Publications (1)

Publication Number Publication Date
MA27347A1 true MA27347A1 (fr) 2005-06-01

Family

ID=26970163

Family Applications (2)

Application Number Title Priority Date Filing Date
MA27423A MA27347A1 (fr) 2001-06-11 2003-12-04 Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese
MA27424A MA27348A1 (fr) 2001-06-11 2003-12-04 Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese

Family Applications After (1)

Application Number Title Priority Date Filing Date
MA27424A MA27348A1 (fr) 2001-06-11 2003-12-04 Inhibiteurs de protease du vih, compositions les contenant, leurs utilisations pharmaceutiques et matieres pour leur synthese

Country Status (27)

Country Link
US (4) US7179918B2 (fr)
EP (3) EP1448539A1 (fr)
JP (2) JP2005508867A (fr)
KR (2) KR20040023616A (fr)
CN (2) CN1599729A (fr)
AP (2) AP2003002915A0 (fr)
AR (2) AR036046A1 (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) HRP20031014A2 (fr)
IL (2) IL159076A0 (fr)
IS (2) IS7049A (fr)
MA (2) MA27347A1 (fr)
MX (2) MXPA03011336A (fr)
NO (2) NO20035489D0 (fr)
NZ (2) NZ530024A (fr)
OA (2) OA12696A (fr)
PA (2) PA8547501A1 (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 (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7169932B2 (en) * 2001-06-11 2007-01-30 Pfizer Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material 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
AU2004295187A1 (en) * 2003-12-04 2005-06-16 Pfizer Inc. Methods for the preparation of stereoisomerically enriched amines
EP1692104A1 (fr) * 2003-12-04 2006-08-23 Pfizer Inc. Procedes pour preparer des composes utiles en tant qu'inhibiteurs de la protease
BRPI0417492A (pt) * 2003-12-09 2007-05-29 Pfizer composições compreendendo um inibidor de protease de hiv
RU2006128606A (ru) * 2004-01-30 2008-03-10 Пфайзер Инк. (US) Терапевтические комбинации
JP2007519706A (ja) * 2004-01-30 2007-07-19 ファイザー・インク Ｈｉｖプロテアーゼ阻害剤及びシトクロームｐ４５０酵素活性阻害剤を含んでなる組成物
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
KR102438072B1 (ko) * 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
JP6817962B2 (ja) 2015-01-20 2021-01-20 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． ターゲティングされたアンドロゲン受容体分解のための化合物および方法
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
AU2016232705C1 (en) 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
WO2016197114A1 (fr) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs et procédés d'utilisation associés
GB201511382D0 (en) 2015-06-29 2015-08-12 Imp Innovations Ltd Novel compounds and their use in therapy
EP3337476A4 (fr) 2015-08-19 2019-09-04 Arvinas, Inc. Composés et procédés pour la dégradation ciblée de protéines contenant un bromodomaine
BR112018008918A8 (pt) 2015-11-02 2019-02-26 Univ Yale compostos de quimera proteólise dirigida e métodos para preparação e uso dos mesmos
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
EP3512842B1 (fr) 2016-09-15 2024-01-17 Arvinas, Inc. Dérivés d'indole en tant qu'agents de dégradation des récepteurs de l'estrogène
SI3526202T1 (sl) 2016-10-11 2025-04-30 Arvinas Operations, Inc. Spojine in postopki za ciljno razgradnjo androgenskih receptorjev
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
IL266842B (en) 2016-12-01 2022-09-01 Arvinas Operations Inc History of tetrahydronaphthalene and tetrahydroisoquinoline as estrogen receptor antagonists
US10806737B2 (en) 2016-12-23 2020-10-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
CN110753693A (zh) 2016-12-23 2020-02-04 阿尔维纳斯运营股份有限公司 Egfr蛋白水解靶向嵌合分子和相关使用方法
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
IL325835A (en) 2016-12-23 2026-03-01 Univ Yale Compounds and methods for the targeted degradation of rapidly accelerated fibrosarcoma polypeptides
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
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzothiophene compounds, preparations containing them and their use in therapy
IL319363A (en) 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
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
US12539292B2 (en) 2018-04-01 2026-02-03 Arvinas Operations, Inc. BRM targeting compounds and associated methods of use
BR112020020307A2 (pt) 2018-04-04 2021-01-12 Arvinas Operations, Inc. Moduladores de proteólise e métodos de uso associados
US11707452B2 (en) 2018-08-20 2023-07-25 Arvinas Operations, Inc. Modulators of alpha-synuclein proteolysis and associated methods of use
EP3999182A1 (fr) 2019-07-17 2022-05-25 Arvinas Operations, Inc. Composés ciblant la protéine tau et procédés d'utilisation associés
WO2021041348A1 (fr) 2019-08-26 2021-03-04 Arvinas Operations, Inc. Procédés de traitement du cancer du sein avec des dérivés de tétrahydronaphtalène en tant qu'agents de dégradation du récepteur des œstrogènes
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
JP2021138694A (ja) 2020-03-06 2021-09-16 ファイザー・インク ＳＡＲＳ−ＣｏＶ−２複製を阻害し、コロナウイルス疾患２０１９を処置する方法
CN115996918A (zh) 2020-05-09 2023-04-21 阿尔维纳斯运营股份有限公司 制造双官能团化合物的方法、双官能团化合物的超纯形式以及包括所述双官能团化合物的剂型
WO2022047145A1 (fr) 2020-08-28 2022-03-03 Arvinas Operations, Inc. Composés de dégradation de protéine de fibrosarcome rapidement accéléré et leurs procédés d'utilisation
AU2021342287A1 (en) 2020-09-14 2023-04-13 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors
EP4584258A1 (fr) 2022-09-07 2025-07-16 Arvinas Operations, Inc. Composés de dégradation de fibrosarcome rapidement accéléré (raf) et procédés d'utilisation associés
CN119997982A (zh) 2022-09-09 2025-05-13 迈里克斯制药有限公司 包含nmt抑制剂的抗体药物偶联物及其用途
PE20260006A1 (es) 2023-01-26 2026-01-06 Arvinas Operations Inc Protacs degradadores de kras basados en cereblon y usos relacionados con los mismos
AU2024392985A1 (en) 2023-12-08 2026-06-04 Arvinas Operations, Inc. Use of androgen receptor degrader for the treatment of spinal and bulbar muscular atrophy

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
IE920414A1 (en) * 1991-02-08 1992-08-12 Sankyo Co New beta-amino-alpha-hydroxycarboxylic acids and their use
WO1993013066A1 (fr) 1991-12-20 1993-07-08 Syntex (U.S.A.) Inc. Amides cycliques d'acides 3-amino-2-hydroxy-carboxyliques utilises comme inhibiteurs de la protease du vih
DE69322127T2 (de) 1992-05-13 1999-06-24 Japan Energy Corp., Tokio/Tokyo 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
NZ248332A (en) * 1992-08-07 1995-01-27 Sankyo Co Hiv protease inhibitor and its 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
US5932550A (en) * 1995-06-30 1999-08-03 Japan Energy Corporation Dipeptide compound or pharmaceutically acceptable salt thereof and medical use thereof
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
CA2463975A1 (fr) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Inhibiteurs de l'integrase du vih a base de dihydroxypyrimidine carboxamide
AU2002349675A1 (en) 2001-12-05 2003-06-17 Shionogi And Co., Ltd. Derivative having hiv integrase inhibitory activity
CA2469592C (fr) 2001-12-12 2005-08-23 Bristol-Myers Squibb Company Inhibiteurs de l'integrase du vih
EP1467970B1 (fr) 2002-01-17 2007-08-22 Merck & Co., Inc. Carboxamides hydroxynaphthyridinone utiles comme inhibiteurs de l'integrase du 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
EP1692104A1 (fr) * 2003-12-04 2006-08-23 Pfizer Inc. Procedes pour preparer des composes utiles en tant qu'inhibiteurs de la protease

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