PE20040479A1 - Inhibidores de proteasa del vih y composiciones que los contienen - Google Patents

Inhibidores de proteasa del vih y composiciones que los contienen

Info

Publication number
PE20040479A1
PE20040479A1 PE2002000512A PE2002000512A PE20040479A1 PE 20040479 A1 PE20040479 A1 PE 20040479A1 PE 2002000512 A PE2002000512 A PE 2002000512A PE 2002000512 A PE2002000512 A PE 2002000512A PE 20040479 A1 PE20040479 A1 PE 20040479A1
Authority
PE
Peru
Prior art keywords
aliphatic
group
halo
carbocyclic
alkyl
Prior art date
Application number
PE2002000512A
Other languages
English (en)
Inventor
Therese N Alexander
Stephen E Webber
Gary Bolton
Fredrick E Boyer
Benjamin J Burke
Stacie S Canon-Koch
Tod Holler
Tanya M Jewell
Vara Prasad Josyula
David J Kucera
Maria A Linton
Jeff Machak
Michael Melnick
Lennert J Mitchell
Sean T Murphy
Siegfried H Reich
Donald J Skalitzky
John H Tatlock
Michael D Varney
Scott C Virgil
Mark Barvian
Original Assignee
Agouron Pharma
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 Pharma filed Critical Agouron Pharma
Publication of PE20040479A1 publication Critical patent/PE20040479A1/es

Links

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIERE A COMPUESTOS DE FORMULA I ENTRE OTROS DONDE R1 ES UN GRUPO ALIFATICO, CARBOCICLICO, HETEROCICLICO, GRUPO DE FORMULA OR1´, SR1´, NHR1´, C(O)R1 DONDE R1´ ES UN GRUPO ALIFATICO, CARBOCICLICO, HETEROCICLICO, ENTRE OTROS; V ES C=O, C=S, SO2; R2 ES UN GRUPO ALIFATICO, GRUPO CARBOCICLICO, CARBOCICLICO-ALIFATICO, HETEROCICLICO, HETEROCICLICO-ALIFATICO, N(R2a)R2b DONDE R2a ES GRUPO ALIFATICO, CARBOCICLICO, HETEROCICLICO Y R2b ES H, ALIFATICO C1-C6; W ES N, O, C, CH CUANDO W ES N, C o CH, R2' ES H o UN GRUPO ALIFATICO C1-C6 o R2 Y R2' TOMADOS JUNTO CON EL ATOMO W AL CUAL ESTAN UNIDOS FORMAN UN ANILLO HETEROCICLICO O CARBOCICLICO SUSTITUIDO O NO SUSTITUIDO; CUANDO W ES O, R2' ESTA AUSENTE; X ES EL GRUPO a, b DONDE Y', Y'' SON H, HALO, ALIFATICO C1-C6; n ES 1-2; Rx ES H, ALQUILO C1-C6, NITRO, AMINO, CIANO, HALO, HALOALQUILO, ENTRE OTROS; R8 Y R8' SON H, HALO, GRUPO ALIFATICO; R3 ES H, ALQUILO C1-C6; R4 Y R5 SON H, HALO, ALQUILO C1-C6; R6 Y R7 SON H, HALO, ALQUILO C1-C6. SE REFIERE TAMBIEN A PRODUCTOS INTERMEDIOS, PROCEDIMIENTO PARA LA PREPARACION Y UNA COMPOSICION FARMACEUTICA QUE COMPRENDE INHIBIDORES DE PROTEASA UTILES PARA EL TRATAMIENTO DE INFECTADOS POR VIH
PE2002000512A 2001-06-11 2002-06-14 Inhibidores de proteasa del vih y composiciones que los contienen PE20040479A1 (es)

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
PE20040479A1 true PE20040479A1 (es) 2004-09-20

Family

ID=26970163

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2002000513A PE20040241A1 (es) 2001-06-11 2002-06-14 Inhibidores proteasa hiv, composiciones que los contienen y materiales para sus sintesis
PE2002000512A PE20040479A1 (es) 2001-06-11 2002-06-14 Inhibidores de proteasa del vih y composiciones que los contienen

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2002000513A PE20040241A1 (es) 2001-06-11 2002-06-14 Inhibidores proteasa hiv, composiciones que los contienen y materiales para sus sintesis

Country Status (27)

Country Link
US (4) US7179918B2 (es)
EP (3) EP1409466A2 (es)
JP (2) JP2005508867A (es)
KR (2) KR20040023616A (es)
CN (2) CN1599729A (es)
AP (2) AP1770A (es)
AR (2) AR036093A1 (es)
AU (2) AU2002316235A2 (es)
BR (2) BR0210344A (es)
CA (2) CA2450265A1 (es)
EA (2) EA008169B1 (es)
GE (1) GEP20063890B (es)
HN (1) HN2002000136A (es)
HR (2) HRP20031014A2 (es)
IL (2) IL159076A0 (es)
IS (2) IS7050A (es)
MA (2) MA27348A1 (es)
MX (2) MXPA03011336A (es)
NO (2) NO20035489D0 (es)
NZ (2) NZ530023A (es)
OA (2) OA12696A (es)
PA (2) PA8547601A1 (es)
PE (2) PE20040241A1 (es)
PL (1) PL366622A1 (es)
TN (1) TNSN03130A1 (es)
TW (1) TW200538447A (es)
WO (2) WO2002100845A1 (es)

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
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
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
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 (en) * 2003-09-17 2005-03-24 Pfizer Inc. Hiv protease inhibitors, compositions containing the same and their pharmaceutical uses
KR20060097047A (ko) * 2003-12-04 2006-09-13 화이자 인코포레이티드 프로테아제 억제제로서 유용한 화합물의 제조 방법
BRPI0417046A (pt) * 2003-12-04 2007-02-06 Pfizer métodos para o preparo de aminas estereoisomericamente enriquecidas
JP2007513142A (ja) * 2003-12-04 2007-05-24 ファイザー インコーポレイテッド プロテアーゼ阻害剤として有用な化合物の製造法
JP2007513937A (ja) * 2003-12-09 2007-05-31 ファイザー インコーポレイテッド Hivプロテアーゼ阻害剤を含む組成物
KR20060127939A (ko) * 2004-01-30 2006-12-13 화이자 인코포레이티드 Hiv 프로테아제 억제제 및 사이토크롬 p450 효소 활성억제제를 포함하는 조성물
CA2555171A1 (en) * 2004-01-30 2005-09-09 Pfizer Inc. Therapeutic combinations
WO2005121094A1 (en) * 2004-06-09 2005-12-22 Pfizer Limited Piperazine and piperidine derivatives as anti-hiv-agents
WO2012158515A1 (en) * 2011-05-13 2012-11-22 Vertex Phamaceuticals Incorporated Process for the preparation of protease inhibitors
MX358660B (es) * 2012-01-12 2018-08-30 Univ Yale Compuestos y metodos para degradacion mejorada de proteinas y otros polipeptidos elegidos como blanco mediante una ubiquitina ligasa e3.
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
US10071164B2 (en) 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
KR20230119040A (ko) 2015-01-20 2023-08-14 아비나스 오퍼레이션스, 인코포레이티드 안드로겐 수용체의 표적화된 분해를 위한 화합물 및방법
US20170327469A1 (en) 2015-01-20 2017-11-16 Arvinas, Inc. Compounds and methods for the targeted degradation of androgen receptor
US10730870B2 (en) 2015-03-18 2020-08-04 Arvinas Operations, Inc. Compounds and methods for the enhanced degradation of targeted proteins
EP3302482A4 (en) 2015-06-05 2018-12-19 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
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF PROTEINS CONTAINING BROMODOMAIN
KR20180097530A (ko) 2015-11-02 2018-08-31 예일 유니버시티 단백질분해 표적화 키메라 화합물(Proteolysis Targeting Chimera compound) 및 그의 제조 및 사용 방법
US20180072711A1 (en) 2016-09-15 2018-03-15 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
HRP20230414T1 (hr) 2016-10-11 2023-07-07 Arvinas Operations, Inc. Spojevi i postupci za ciljanu razgradnju androgenog receptora
IL290809B2 (en) 2016-11-01 2024-01-01 Arvinas Operations Inc PROTACS Targeted Tau-Protein and Related Methods of Use
KR102173464B1 (ko) 2016-12-01 2020-11-04 아비나스 오퍼레이션스, 인코포레이티드 에스트로겐 수용체 분해제로서의 테트라히드로나프탈렌 및 테트라히드로이소퀴놀린 유도체
EP3559006A4 (en) 2016-12-23 2021-03-03 Arvinas Operations, Inc. COMPOUNDS AND METHODS FOR TARGETED DEGRADATION OF FETAL LIVER KINASE POLYPEPTIDES
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
EP3559002A4 (en) 2016-12-23 2021-02-17 Arvinas Operations, Inc. CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED METHODS OF USE
MX2019007649A (es) 2016-12-23 2019-09-10 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de polipeptidos de fibrosarcoma acelerado rapidamente.
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
CA3049912A1 (en) 2017-01-26 2018-08-02 Arvinas Operations, Inc. Modulators of estrogen receptor proteolysis and associated methods of use
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
MX2020010420A (es) 2018-04-04 2020-12-11 Arvinas Operations Inc Moduladores de la proteólisis y métodos asociados de uso.
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
JP2022540935A (ja) 2019-07-17 2022-09-20 アルビナス・オペレーションズ・インコーポレイテッド タウタンパク質標的化化合物および関連する使用方法
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
PE20221582A1 (es) 2019-12-19 2022-10-06 Arvinas Operations Inc Compuestos y metodos para la degradacion dirigida de receptor de androgenos
WO2021176369A1 (en) 2020-03-06 2021-09-10 Pfizer Inc. Methods of inhibiting sars-cov-2 replication and treating coronavirus disease 2019
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use

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 (en) 1990-12-11 1998-09-22 Yuuichi Nagano Hiv protease inhibitors
AU647239B2 (en) * 1991-02-08 1994-03-17 Sankyo Company Limited New beta-amino- alpha-hydroxycarboxylic acids and their use
ZA929869B (en) 1991-12-20 1994-06-20 Syntex Inc Hiv protease inhibitors
US5644028A (en) * 1992-05-13 1997-07-01 Japan Energy Corporation Process for producing peptide derivatives and salts therefor
DE69322127T2 (de) 1992-05-13 1999-06-24 Japan Energy Corp Verfahren zur Herstellung von Peptidderivaten und ihrer Salze
FI933472A (fi) 1992-08-07 1994-02-08 Sankyo Co Peptider med foermaoga att inhibera effekten av HIV-proteas, deras framstaellning och terapeutiska anvaendning
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
EP0706794B1 (en) * 1994-10-14 2001-12-12 Japan Energy Corporation Anti-aids pharmaceutical preparations and processes for the production thereof
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 (en) 1999-02-19 2001-11-21 Oklahoma Medical Research Foundation Protease inhibitors that overcome drug resistance
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
EP1441734B1 (en) 2001-10-26 2007-02-28 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
WO2003047564A1 (fr) 2001-12-05 2003-06-12 Shionogi & Co., Ltd. Dérivé ayant une activité d'inhibition de l'intégrase du vih
MXPA04005623A (es) 2001-12-12 2004-12-06 Squibb Bristol Myers Co Inhibidores de integrasa del virus de inmunodeficiencia humana (vih).
AU2003216049B2 (en) 2002-01-17 2008-07-17 Merck Sharp & Dohme Corp. Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
TW200306192A (en) 2002-01-18 2003-11-16 Bristol Myers Squibb Co Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors
WO2005026114A1 (en) * 2003-09-17 2005-03-24 Pfizer Inc. Hiv protease inhibitors, compositions containing the same and their pharmaceutical uses
KR20060097047A (ko) * 2003-12-04 2006-09-13 화이자 인코포레이티드 프로테아제 억제제로서 유용한 화합물의 제조 방법

Also Published As

Publication number Publication date
JP2005508867A (ja) 2005-04-07
EA200400023A1 (ru) 2004-06-24
IL159076A0 (en) 2004-05-12
PL366622A1 (en) 2005-02-07
EA008169B1 (ru) 2007-04-27
TW200538447A (en) 2005-12-01
EP1448539A1 (en) 2004-08-25
EP1739082A1 (en) 2007-01-03
PE20040241A1 (es) 2004-04-26
HRP20031014A2 (en) 2005-10-31
US7179918B2 (en) 2007-02-20
US20050250707A1 (en) 2005-11-10
NO20035488D0 (no) 2003-12-10
OA12697A (en) 2006-06-21
US20030225071A1 (en) 2003-12-04
KR20040023616A (ko) 2004-03-18
MXPA03011397A (es) 2005-03-07
AU2002345644A2 (en) 2002-12-23
WO2002100844A2 (en) 2002-12-19
AP1770A (en) 2007-08-22
AR036046A1 (es) 2004-08-04
PA8547501A1 (es) 2003-02-14
NO20035489D0 (no) 2003-12-10
AP2003002916A0 (en) 2003-12-31
AU2002345644B2 (en) 2006-08-10
US6953858B2 (en) 2005-10-11
AU2002345644C1 (en) 2002-12-23
IL159022A0 (en) 2004-05-12
MA27348A1 (fr) 2005-06-01
GEP20063890B (en) 2006-08-10
HN2002000136A (es) 2003-07-31
NZ530024A (en) 2005-10-28
AU2002316235A2 (en) 2002-12-23
CA2450265A1 (en) 2002-12-19
WO2002100845A1 (en) 2002-12-19
AP2003002915A0 (en) 2003-12-31
CN100338044C (zh) 2007-09-19
BR0210358A (pt) 2004-06-22
EA200400026A1 (ru) 2004-04-29
US20070021354A1 (en) 2007-01-25
WO2002100845A8 (en) 2003-03-20
MXPA03011336A (es) 2004-12-06
JP2004534061A (ja) 2004-11-11
WO2002100844A3 (en) 2003-03-06
KR20040035601A (ko) 2004-04-29
US20030153507A1 (en) 2003-08-14
NZ530023A (en) 2005-10-28
BR0210344A (pt) 2004-07-13
AR036093A1 (es) 2004-08-11
TNSN03130A1 (en) 2005-12-23
EP1409466A2 (en) 2004-04-21
HRP20031015A2 (en) 2005-10-31
CN1599729A (zh) 2005-03-23
PA8547601A1 (es) 2003-12-30
IS7050A (is) 2003-11-21
MA27347A1 (fr) 2005-06-01
CN1622942A (zh) 2005-06-01
OA12696A (en) 2006-06-22
CA2450269A1 (en) 2002-12-19
IS7049A (is) 2003-11-21

Similar Documents

Publication Publication Date Title
PE20040479A1 (es) Inhibidores de proteasa del vih y composiciones que los contienen
ES2064310T3 (es) Procedimiento para preparar compuestos de imidazopiridina.
PE20040840A1 (es) Derivados de 4-oxoquinolina como inhibidores de la integrasa del vih
AR034268A1 (es) Compuestos derivados de piperidina, su uso en preparacion de medicamentos, composicion farmaceutica, metodo de tratamiento y proceso para su preparacion
PA8556801A1 (es) Compuestos de imidazopiridin como moduladores de receptor 5-ht 4
AR004219A1 (es) Nuevos derivados de quinazolina, procedimientos para su preparacion, composiciones que los contienen y su uso en la preparacion de medicamentos,particularmente en el tratamiento de trastornos inflamatorios
PE20060381A1 (es) Analogos de dipeptidos inhibidores de la hepatitis c
AR004655A1 (es) Un compuesto derivado de aminoacido, una composicion farmaceutica que lo contiene, un proceso para su sintesis y su uso para la fabricacion de un medicamento
PE20040164A1 (es) Mimeticos de glucocorticoides, procedimientos para su preparacion y composiciones farmaceuticas
PE108898A1 (es) Derivados 6,5-heterobiciclicos sustituidos
HUP0301187A2 (hu) Új benzil-piperidin-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
ES2059327T3 (es) Derivados de tetrahidronaftaleno y de indano, obtencion de los mismos y utilizacion en preparados farmaceuticos.
PE108698A1 (es) Derivados 6,6-heterobiciclicos sustituidos
ES2182535T3 (es) Derivados de benzo(b)tiepina-1,-dioxido, procedimiento para su preparacion, medicamentos que contienen estos compuestos y su utilizacion.
UY29312A1 (es) Piperazin-1-carboxamidas n,4,sustituidas y sus derivados, composiciones que los contienen, procedimientos de preparación y aplicaciones
MX9307654A (es) Derivados de amina, proceso para su preparacion y composicion farmaceutica que los contiene.
AR006720A1 (es) Un compuesto derivado de azahexano heterociclico, su uso para la preparacion de una composicion farmaceutica, procedimiento para prepararlo y una composicion farmaceutica que lo comprende
PE107999A1 (es) Derivados 3-amidinoanilina, inhibidores del factor x de coagulacion de la sangre activado e intermediarios de los mismos
ES2038678T3 (es) Procedimiento para la preparacion de n-(2-alquil-3-mercapto-glutaril)-alfamino-acidos.
ECSP045420A (es) Derivados de benzoxazina como moduladores 5-ht6 y usos de los mismos
ES2026669T3 (es) Procedimiento para la preparacion y el uso terapeutico de los beta-d-fenil tioxilosidos.
DK71780A (da) Fremgangsmaade til fremstilling af difenylhydantoinderivater
PA8475401A1 (es) Compuestos de sulfonilbenceno como agentes antiinflamatorios/analgesicos
PE20021018A1 (es) DERIVADOS DE ß - CARBOLINA
PT83726B (pt) Processo para preparacao de derivados da beta-carbolina substituidas por grupos fenoxi e de composicoes farmaceuticas que os contem

Legal Events

Date Code Title Description
FA Abandonment or withdrawal