AR073568A1 - Inhibidores macrociclicos de serina proteasas de hepatitis c - Google Patents

Inhibidores macrociclicos de serina proteasas de hepatitis c

Info

Publication number
AR073568A1
AR073568A1 ARP090103469A ARP090103469A AR073568A1 AR 073568 A1 AR073568 A1 AR 073568A1 AR P090103469 A ARP090103469 A AR P090103469A AR P090103469 A ARP090103469 A AR P090103469A AR 073568 A1 AR073568 A1 AR 073568A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
heteroatoms selected
carbocycle
aryl
heterocycle
Prior art date
Application number
ARP090103469A
Other languages
English (en)
Inventor
Seble H Wagaw
Keith F Mcdaniel
Dale Kempf
Yi-Yin Ku
Dong Liu
Ying Sun
Yat Sun Or
Yonghua Gai
Hui-Ju Chen
Jason P Shanley
Ken Engstrom
Tim Grieme
David J Grampovnik
Ahmad Sheikh
Jianzhang Mei
Original Assignee
Enanta Pharm Inc
Abbott Lab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42005677&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR073568(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Enanta Pharm Inc, Abbott Lab filed Critical Enanta Pharm Inc
Publication of AR073568A1 publication Critical patent/AR073568A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/113—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides without change of the primary structure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Analytical Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Compuestos macrocíclicos y con el uso de los mismos para el tratamiento de las infecciones con VHC. Composiciones farmacéuticas que comprenden estos compuestos, o las sales, ésteres o prodrogas farmacéuticamente aceptables, en combinacion con un vehículo o excipiente farmacéuticamente aceptable. Se proveen, además métodos para su preparacion. Reivindicacion 1: Un compuesto caracterizado porque es de formula 1 o 2, o una sal, éster o prodroga farmacéuticamente aceptable del mismo, donde: J se encuentra ausente, o es alquileno opcionalmente sustituido, alquenileno opcionalmente sustituido, alquinileno opcionalmente sustituido, - C(O)-, -O-C(O)-, - N(R3)-C(O)-, -C(S)-, -C(=NR4)-. -S(O)-, -S(O2)-, o -N(R3)-; A es alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido o alquinilo opcionalmente sustituido, cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; arilo opcionalmente sustituido, arilalquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclo opcionalmente sustituido, o carbociclo opcionalmente sustituido; cada R1 se selecciona independientemente entre (i) halogeno, hidroxi, amino, -CN, -CF, N3, -NO2. -OR4, -SR4, -SOR4, -SO2R4, -N(R3)S(O)2-R4, -N(R3)(SO2)NR3R4, -NR3R4, -C(O)-OR4, -C(O)R4, -C(O)NR3R4, o -N(R3)C(O)R4; ii) arilo opcionalmente sustituido; (iii) heteroarilo opcionalmente sustituido; (iv) heterociclo opcionalmente sustituido; (v) carbociclo opcionalmente sustituido; o (vi) alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, o alquinilo opcionalmente sustituido, cada uno con 0, 1 2, o 3 heteroátomos seleccionados entre O, S, o N; G es -E-R5; donde E se encuentra ausente; o es alquileno opcionalmente sustituido, alquenileno opcionalmente sustituido, alquinileno opcionalmente sustituido, cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; o -O-, -S-, -N(R3)-, -N(R3)S(Op)-, -N(R3)C(O)-, -N(R3)C(O)S(Op)-, -OS(Op)-, -C(O)S(Op)-, o -C(O)N(R3)S(Op)-; p es 0, 1, o 2; R5 es H; alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido, o alquinilo opcionalmente sustituido, cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; carbociclo opcionalmente sustituido, heterociclo opcionalmente sustituido, arilo opcionalmente sustituido, o heteroarilo opcionalmente sustituido; R3 y R4 cada uno se selecciona independientemente en cada oportunidad entre los siguientes: alquilo opcionalmente sustituido, alquenilo opcionalmente sustituido o alquinilo opcionalmente sustituido, cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; arilo opcionalmente sustituido; heteroarilo opcionalmente sustituido; heterociclo opcionalmente sustituido; carbociclo opcionalmente sustituido; o hidrogeno; L se encuentra ausente o se selecciona entre alquileno opcionalmente sustituido, alquenileno opcionalmente sustituido o alquinileno opcionalmente sustituido, cada uno con 0, 1, 2, o 3 heteroátomos seleccionados entre O, S, o N; Y es N o -C(Rö)-; donde A, R1, R' y/o Rö se pueden tomar juntos para formar un anillo, j = 0, 1, 2, 3, o 4; K = 0, 1, 2, o 3; m = 0, 1, o2; n es 0, 1, 2, 3, o 4; y -------- denota una union carbono-carbono simple o doble, donde si Y es N, luego R' es heterociclo opcionalmente sustituido o carbociclo opcionalmente sustituido, y comprende dos o más anillos fusionados, y donde R' no es o como los anillos de formulas (3), donde si Y es -C(Rö)-, luego R' y Rö tomados junto con los átomos de carbono a los cuales se encuentran unidos forman un anillo arilo o heteroarilo, cada uno de dichos anillos se sustituye opcionalmente; siempre que dicho compuesto no sea (2R,6S,13aS,14aR,16aS,Z)-2-(3-(benzo[d]tiazol-2il)quinoxalin-2-iloxi)-14a-(ciclopropilsulfonilcarbamoil)-5, 16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahidrociclopropa[e]pirrol[1,2-a][1,4]diazaciclopentadecin-6-ilcarbamato de ter-butilo
ARP090103469A 2008-09-11 2009-09-10 Inhibidores macrociclicos de serina proteasas de hepatitis c AR073568A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19172508P 2008-09-11 2008-09-11
US20968909P 2009-03-10 2009-03-10

Publications (1)

Publication Number Publication Date
AR073568A1 true AR073568A1 (es) 2010-11-17

Family

ID=42005677

Family Applications (3)

Application Number Title Priority Date Filing Date
ARP090103469A AR073568A1 (es) 2008-09-11 2009-09-10 Inhibidores macrociclicos de serina proteasas de hepatitis c
ARP120101342A AR086181A2 (es) 2008-09-11 2012-04-19 Metodo para preparar inhibidores macrociclicos inhibidores de serina proteasas del virus de la hepatitis c
ARP130104634A AR093924A2 (es) 2008-09-11 2013-12-11 Inhibidores macrociclicos de serina proteasas de hepatitis c

Family Applications After (2)

Application Number Title Priority Date Filing Date
ARP120101342A AR086181A2 (es) 2008-09-11 2012-04-19 Metodo para preparar inhibidores macrociclicos inhibidores de serina proteasas del virus de la hepatitis c
ARP130104634A AR093924A2 (es) 2008-09-11 2013-12-11 Inhibidores macrociclicos de serina proteasas de hepatitis c

Country Status (41)

Country Link
US (3) US8420596B2 (es)
EP (5) EP2468285B1 (es)
JP (4) JP5259537B2 (es)
KR (3) KR101379365B1 (es)
CN (3) CN101775017B (es)
AR (3) AR073568A1 (es)
AU (1) AU2009292182B2 (es)
BR (2) BRPI0918724B8 (es)
CA (1) CA2736895C (es)
CL (2) CL2011000512A1 (es)
CO (1) CO6341565A2 (es)
CR (1) CR20140180A (es)
CY (6) CY1115137T1 (es)
DK (5) DK2468286T3 (es)
DO (1) DOP2011000077A (es)
EA (2) EA022891B1 (es)
EC (2) ECSP11010879A (es)
ES (5) ES2475163T3 (es)
GT (2) GT201100056AA (es)
HK (4) HK1170936A1 (es)
HR (5) HRP20140493T1 (es)
HU (2) HUE039478T2 (es)
IL (2) IL218441A (es)
LT (2) LT2805726T (es)
LU (1) LU92667I2 (es)
MX (1) MX2011002486A (es)
MY (1) MY159820A (es)
NL (1) NL300730I2 (es)
NO (1) NO2015014I1 (es)
NZ (2) NZ592170A (es)
PA (1) PA8842201A1 (es)
PE (3) PE20110704A1 (es)
PL (5) PL2468287T3 (es)
PT (5) PT2468285E (es)
SG (1) SG179414A1 (es)
SI (5) SI2805726T1 (es)
TR (1) TR201809771T4 (es)
TW (3) TWI429449B (es)
UY (3) UY32099A (es)
WO (1) WO2010030359A2 (es)
ZA (2) ZA201101558B (es)

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