AR113968A1 - Pirrolidinamidas ii sustituidas - Google Patents

Pirrolidinamidas ii sustituidas

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Publication number
AR113968A1
AR113968A1 ARP180103706A ARP180103706A AR113968A1 AR 113968 A1 AR113968 A1 AR 113968A1 AR P180103706 A ARP180103706 A AR P180103706A AR P180103706 A ARP180103706 A AR P180103706A AR 113968 A1 AR113968 A1 AR 113968A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
alkylene
aryl
membered heterocycloalkyl
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ARP180103706A
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English (en)
Inventor
Hennen Stephanie Dr
Friebe Daniela Dr
Schade Markus Dr
Krger Sebastian Dr
Alen Jo Dr
Jakob Florian Dr
Original Assignee
Gruenenthal Gmbh
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Application filed by Gruenenthal Gmbh filed Critical Gruenenthal Gmbh
Publication of AR113968A1 publication Critical patent/AR113968A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicación 1: Un compuesto de acuerdo con la fórmula general (1), donde R¹ representa alquilo-C₁₋₁₀-; cicloalquilo-C₃₋₁₀-; alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; heterocicloalquilo de 3 a 7 miembros; alquileno-C₁₋₆-(heterocicloalquilo de 3 a 7 miembros); arilo; alquileno-C₁₋₆-arilo; heteroarilo de 5 ó 6 miembros; o alquileno-C₁₋₆-(heteroarilo de 5 ó 6 miembros); R² representa -C(=O)-alquilo-C₁₋₁₀-; -C(=O)-cicloalquilo-C₃₋₁₀-; -C(=O)-alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; -C(=O)-(heterocicloalquilo de 3 a 7 miembros); -C(=O)-alquileno-C₁₋₆-(heterocicloalquilo de 3 a 7 miembros); -C(=O)-arilo; -C(=O)-alquileno-C₁₋₆-arilo; -C(=O)-(heteroarilo de 5 ó 6 miembros); -C(=O)-alquileno-C₁₋₆-(heteroarilo de 5 ó 6 miembros); -S(=O)₁₋₂-alquilo-C₁₋₁₀-; -S(=O)₁₋₂-cicloalquilo-C₃₋₁₀-; -S(=O)₁₋₂-alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; -S(=O)₁₋₂-(heterocicloalquilo de 3 a 7 miembros); -S(=O)₁₋₂-alquileno-C₁₋₆-(heterocicloalquilo de 3 a 7 miembros); -S(=O)₁₋₂-arilo; -S(=O)₁₋₂-alquileno-C₁₋₆-arilo; -S(=O)₁₋₂-(heteroarilo de 5 ó 6 miembros); o -S(=O)₁₋₂-alquileno-C₁₋₆-(heteroarilo de 5 ó 6 miembros); R³ representa -alquilo-C₁₋₁₀-; -cicloalquilo-C₃₋₁₀-; -alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; arilo; -alquileno-C₁₋₆-arilo; -C(=O)-alquilo-C₁₋₁₀-; -C(=O)-cicloalquilo-C₃₋₁₀-; -C(=O)-alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; -C(=O)-arilo; -C(=O)-alquileno-C₁₋₆-arilo; -S(=O)₁₋₂-alquilo-C₁₋₁₀-; -S(=O)₁₋₂-cicloalquilo-C₃₋₁₀-; -S(=O)₁₋₂-alquileno-C₁₋₆-cicloalquilo-C₃₋₁₀-; -S(=O)₁₋₂-arilo; o -S(=O)₁₋₂-alquileno-C₁₋₆-arilo; R⁴ representa -H; -F; -Cl; -Br; -I; -CN; -CH₃; -CF₃; -CF₂H; -CFH₂ o ciclopropilo; X representa N o CR⁵; donde R⁵ representa -H; -F; -Cl; -Br; -I; -CN; alquilo-C₁₋₁₀- o cicloalquilo-C₃₋₁₀-; Y representa N o CR⁶; donde R⁶ representa -H; -F; -Cl; -Br; -I; -CN; alquilo-C₁₋₁₀- o cicloalquilo-C₃₋₁₀-; Z representa N o CR⁷; donde R⁷ representa -H; -F; -Cl; -Br; -I; -CN; alquilo-C₁₋₁₀- o cicloalquilo-C₃₋₁₀-; donde alquilo-C₁₋₁₀-, alquilo-C₁₋₄- y alquileno-C₁₋₆- en cada caso independientemente uno de otro es lineal o ramificado, saturado o insaturado; donde alquilo-C₁₋₁₀-, alquilo-C₁₋₄-, alquileno-C₁₋₆-, cicloalquilo-C₃₋₁₀- y heterocicloalquilo de 3 a 7 miembros en cada caso independientemente uno de otro están no sustituidos o mono o polisustituidos con uno o más sustituyentes que se seleccionan de -F; -Cl; -Br; -I; -CN; alquilo-C₁₋₆-; -CF₃; -CF₂H; -CFH₂; -CF₂Cl; -CFCl₂; -C(=O)-alquilo-C₁₋₆-; -C(=O)-OH; -C(=O)-O-alquilo-C₁₋₆-; -C(=O)-NH₂; -C(=O)-NH(alquilo-C₁₋₆-); -C(=O)-N(alquilo-C₁₋₆-)₂; -OH; =O; -OCF₃; -OCF₂H; -OCFH₂; -OCF₂Cl; -OCFCl₂; -O-alquilo-C₁₋₆-; -O-C(=O)-alquilo-C₁₋₆-; -O-C(=O)-O-alquilo-C₁₋₆-; -O-(CO)-NH(alquilo-C₁₋₆-); -O-C(=O)-N(alquilo-C₁₋₆-)₂; -O-S(=O)₂-NH₂; -O-S(=O)₂-NH(alquilo-C₁₋₆-); -O-S(=O)₂-N(alquilo-C₁₋₆-)₂; -NH₂; -NH(alquilo-C₁₋₆-); -N(alquilo-C₁₋₆-)₂; -NH-C(=O)-alquilo-C₁₋₆-; -NH-C(=O)-O-alquilo-C₁₋₆-; -NH-C(=O)-NH₂; -NH-C(=O)-NH (alquilo-C₁₋₆-); -NH-C(=O)-N(alquilo-C₁₋₆-)₂; -N(alquilo-C₁₋₆-)-C(=O)-alquilo-C₁₋₆-; -N(alquilo-C₁₋₆-)-C(=O)-O-alquilo-C₁₋₆-; -N(alquilo-C₁₋₆-)-C(=O)-NH₂; -N(alquilo-C₁₋₆-)-C(=O)-NH(alquilo-C₁₋₆-); -N(alquilo-C₁₋₆-)-C(=O)-N(alquilo-C₁₋₆-)₂; -NH-S(=O)₂OH; NH-S(=O)₂-alquilo-C₁₋₆-; -NH-S(=O)₂-O-alquilo-C₁₋₆-; -NH-S(=O)₂-NH₂; -NH-S(=O)₂-NH(alquilo-C₁₋₆-); -NH-S(=O)₂-N(alquilo-C₁₋₆-)₂; -N(alquilo-C₁₋₆-)-S(=O)₂-OH; -N(alquilo-C₁₋₆-)-S(=O)₂-alquilo-C₁₋₆-; -N(alquilo-C₁₋₆-) -S(=O)₂-O-alquilo-C₁₋₆-; -N(alquilo-C₁₋₆-)-S(=O)₂-NH₂; -N(alquilo-C₁₋₆-)-S(=O)₂-NH(alquilo-C₁₋₆-); -N(alquilo-C₁₋₆-) -S(=O)₂-N(alquilo-C₁₋₆-)₂; -SCF₃; -SCF₂H; -SCFH₂; -S-alquilo-C₁₋₆-; -S(=O)-alquilo-C₁₋₆-; -S(=O)₂-alquilo-C₁₋₆-; -S(=O)₂-OH; -S(=O)₂-O-alquilo-C₁₋₆-; -S(=O)₂-NH₂; -S(=O)₂-NH(alquilo-C₁₋₆-); -S(=O)₂-N(alquilo-C₁₋₆-)₂; cicloalquilo-C₃₋₆-; heterocicloalquilo de 3 a 6 miembros; fenilo; heteroarilo de 5 ó 6 miembros; -O-cicloalquilo-C₃₋₆-; -O-(heterocicloalquilo de 3 a 6 miembros) ; -O-fenilo; -O-(heteroarilo de 5 ó 6 miembros) ; -C(=O)-cicloalquilo-C₃₋₆-; -C(=O)-(heterocicloalquilo de 3 a 6 miembros); -C(=O)-fenilo; -C(=O)-(heteroarilo de 5 ó 6 miembros); -S(=O)₂-(cicloalquilo-C₃₋₆-); -S(=O)₂-(heterocicloalquilo de 3 a 6 miembros); -S(=O)₂-fenilo o -S(=O)₂-(heteroarilo de 5 ó 6 miembros); donde arilo y heteroarilo de 5 ó 6 miembros en cada caso independientemente uno de otro están no sustituidos o mono o polisustituidos con uno o más sustituyentes que se seleccionan de -F; -Cl; -Br; -I; -CN; alquilo-C₁₋₆-; -CF₃; -CF₂H; -CFH₂; -CF₂Cl; -CFCl₂; alquileno-C₁₋₄-CF₃; alquileno-C₁₋₄-CF₂H; alquileno-C₁₋₄-CFH₂; -C(=O)-alquilo-C₁₋₆-; -C(=O)-OH; -C(=O)-O-alquilo-C₁₋₆-; -C(=O)-NH(OH); -C(=O)-NH₂; -C(=O)-NH(alquilo-C₁₋₆-); -C(=O)-N(alquilo-C₁₋₆-)₂; -OH; =O; -OCF₃; -OCF₂H; -OCFH₂; -OCF₂Cl; -OCFCl₂; -O-alquilo-C₁₋₆-; -O-cicloalquilo-C₃₋₆-; -O-(heterocicloalquilo de 3 a 6 miembros); -NH₂; -NH(alquilo-C₁₋₆-); -N(alquilo-C₁₋₆-)₂; -NH-C(=O)-alquilo-C₁₋₆-; -N(alquilo-C₁₋₆-) -C(=O)-alquilo-C₁₋₆-; -NH-C(=O)-NH₂; -NH-C(=O)-NH(alquilo-C₁₋₆-); -NH-C(=O)-N(alquilo-C₁₋₆-)₂; -N(alquilo-C₁₋₆-)-C(=O)-NH(alquilo-C₁₋₆-); -N(alquilo-C₁₋₆-)-C(=O)-N(alquilo-C₁₋₆-)₂; -NH-S(=O)₂-alquilo-C₁₋₆-; -SCF₃; -S-alquilo-C₁₋₆-; -S(=O)-alquilo-C₁₋₆-; -S(=O)₂-alquilo-C₁₋₆-; -S(=O)₂-NH₂; -S(=O)₂-NH(alquilo-C₁₋₆-); -S(=O)₂-N(alquilo-C₁₋₆-)₂; cicloalquilo-C₁₋₆-; alquileno-C₁₋₄-cicloalquilo-C₃₋₆-; heterocicloalquilo de 3 a 6 miembros; alquileno-C₁₋₄-(heterocicloalquilo de 3 a 6 miembros); fenilo o heteroarilo de 5 ó 6 miembros; en forma del compuesto libre o una sal fisiológicamente aceptable de este.
ARP180103706A 2017-12-18 2018-12-18 Pirrolidinamidas ii sustituidas AR113968A1 (es)

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US (2) US20190185470A1 (es)
EP (1) EP3728233B1 (es)
JP (1) JP2021506965A (es)
CN (1) CN111491931A (es)
AR (1) AR113968A1 (es)
AU (1) AU2018387747A1 (es)
BR (1) BR112020012221A2 (es)
CA (1) CA3085879A1 (es)
EA (1) EA202091428A1 (es)
ES (1) ES2920359T3 (es)
IL (1) IL275375A (es)
MX (1) MX2020006355A (es)
TW (1) TW201927769A (es)
WO (1) WO2019121611A1 (es)

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CN111556867A (zh) 2017-12-18 2020-08-18 格吕伦塔尔有限公司 经取代的吡咯烷酰胺i
CN113382990A (zh) 2019-01-11 2021-09-10 格吕伦塔尔有限公司 取代的吡咯烷酰胺iii
JP2023535279A (ja) 2020-06-22 2023-08-17 コーセプト セラピューティクス， インコーポレイテッド ４級インダゾールグルココルチコイド受容体アンタゴニスト
WO2022008705A1 (en) 2020-07-09 2022-01-13 Grünenthal GmbH Substituted pyrrolidine amines and amides as mediator of the glucocortoid receptor
WO2023122600A1 (en) * 2021-12-21 2023-06-29 Corcept Therapeutics Incorporated Piperazine indazole glucocorticoid receptor antagonists
US20230242514A1 (en) * 2021-12-21 2023-08-03 Corcept Therapeutics Incorporated Bicyclic indazole glucocorticoid receptor antagonists

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US20220127264A1 (en) 2022-04-28
EA202091428A1 (ru) 2020-10-27
CN111491931A (zh) 2020-08-04
EP3728233B1 (en) 2022-04-20
EP3728233A1 (en) 2020-10-28
WO2019121611A1 (en) 2019-06-27
AU2018387747A1 (en) 2020-08-06
JP2021506965A (ja) 2021-02-22
IL275375A (en) 2020-07-30
ES2920359T3 (es) 2022-08-03
BR112020012221A2 (pt) 2020-11-24
CA3085879A1 (en) 2019-06-27
MX2020006355A (es) 2020-08-17
US20190185470A1 (en) 2019-06-20

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