PE20211733A1 - Amidas de pirrolidina sustituidas - Google Patents

Amidas de pirrolidina sustituidas

Info

Publication number
PE20211733A1
PE20211733A1 PE2021001146A PE2021001146A PE20211733A1 PE 20211733 A1 PE20211733 A1 PE 20211733A1 PE 2021001146 A PE2021001146 A PE 2021001146A PE 2021001146 A PE2021001146 A PE 2021001146A PE 20211733 A1 PE20211733 A1 PE 20211733A1
Authority
PE
Peru
Prior art keywords
phenyl
compounds
cycloalkyl
alkyl
substitute
Prior art date
Application number
PE2021001146A
Other languages
English (en)
Inventor
Florian Jakob
Jo Alen
Sebastian Kruger
Daniela Friebe
Stephanie Hennen
Philipp Barbie
Original Assignee
Gruenenthal Chemie
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 Gruenenthal Chemie filed Critical Gruenenthal Chemie
Publication of PE20211733A1 publication Critical patent/PE20211733A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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 carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • 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
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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 linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • 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
    • C07D409/14Heterocyclic 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
    • 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
    • C07D413/14Heterocyclic 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
    • 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
    • C07D471/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Esta referido a compuestos de Formula I, en donde: R1 es fenilo, alquileno-fenilo, entre otros; R1' es H, alquilo o cicloalquilo; R2 es alquilo C(=O), cicloalquilo C(=O), entre otros; R3 y R3' son H, F, Cl, alquilo, cicloalquilo, entre otros; R4 es fenilo, alquileno-fenilo, heteroarilo, entre otros; A, X, Y, Z son N, CH. Entre los compuestos preferidos tenemos los siguientes: N-[(2R,3S)-1-[1-(4-Fluorofenil)-1H-indazol-5-il]-4,4-dimetil-5-oxo-2-fenilpirrolidin-3-il]-amida acida ciclopropanecarboxilica; 2,2-Difluoro-N-[(2S,3R)-1-[1-(4-fluorofenil)-1H-indazol-5-il]-4,4-dimetil-5-oxo-2- fenil-pirrolidin-3-il]-propionamida; entre otros. Estos compuestos son moduladores del receptor de glucocorticoides y que se pueden utilizar en el tratamiento y/o la profilaxis de trastornos que son mediados, al menos parcialmente, por el receptor de glucocorticoides. Estos compuestos se emplean en el tratamiento y/o la profilaxis del dolor y/o la inflamacion
PE2021001146A 2019-01-11 2020-01-13 Amidas de pirrolidina sustituidas PE20211733A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP19151406 2019-01-11
EP19152282 2019-01-17
EP19181203 2019-06-19
PCT/EP2020/050626 WO2020144375A1 (en) 2019-01-11 2020-01-13 Substituted pyrrolidine amides iii

Publications (1)

Publication Number Publication Date
PE20211733A1 true PE20211733A1 (es) 2021-09-06

Family

ID=69165383

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021001146A PE20211733A1 (es) 2019-01-11 2020-01-13 Amidas de pirrolidina sustituidas

Country Status (16)

Country Link
US (2) US20200223840A1 (es)
EP (1) EP3908581A1 (es)
JP (1) JP7446316B2 (es)
KR (1) KR20210114972A (es)
CN (1) CN113382990A (es)
AU (1) AU2020207591A1 (es)
BR (1) BR112021013557A2 (es)
CA (1) CA3125929A1 (es)
CL (1) CL2021001823A1 (es)
CO (1) CO2021008998A2 (es)
EC (1) ECSP21051067A (es)
IL (1) IL284642A (es)
MX (1) MX2021008364A (es)
PE (1) PE20211733A1 (es)
TW (1) TWI827785B (es)
WO (1) WO2020144375A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL275333B2 (en) 2017-12-15 2023-09-01 Praxis Biotech LLC Inhibitors of fibroblast activation protein
US20230382910A1 (en) 2022-04-22 2023-11-30 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
US20230373925A1 (en) 2022-04-22 2023-11-23 Vertex Pharma Heteroaryl compounds for the treatment of pain
WO2023205465A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain
WO2023205468A1 (en) 2022-04-22 2023-10-26 Vertex Pharmaceuticals Incorporated Heteroaryl compounds for the treatment of pain

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200815361A (en) 2005-10-20 2008-04-01 Astrazeneca Ab Chemical compounds
WO2007114763A1 (en) * 2006-03-31 2007-10-11 Astrazeneca Ab Sulphonamide derivates as modulators of the glucocorticoid receptor
US8178573B2 (en) * 2006-04-20 2012-05-15 Glaxo Group Limited Compounds
GB0620385D0 (en) 2006-10-13 2006-11-22 Glaxo Group Ltd Novel compounds
JO2754B1 (en) 2006-12-21 2014-03-15 استرازينكا ايه بي Amylendazoleil derivatives for the treatment of glucocorticoid-mediated disorders
JP2009084273A (ja) 2007-09-13 2009-04-23 Santen Pharmaceut Co Ltd 1,3,3−トリメチル−7−フェニル−3,4−ジヒドロ−1h−キノキサリン−2−オン誘導体からなるグルココルチコイド受容体アゴニスト
TWI445705B (zh) * 2008-05-20 2014-07-21 Astrazeneca Ab 經苯基及苯并二基取代之吲唑衍生物
TW201416348A (zh) * 2012-08-29 2014-05-01 Gruenenthal Chemie 以氟甲基取代之吡咯甲醯胺
TN2017000096A1 (en) 2014-09-26 2018-07-04 Astrazeneca Ab 1-alkyl-6-oxo-1,6-dihydropyridin-3-yl compounds and use as sgrm modulators.
KR20180043329A (ko) 2015-08-25 2018-04-27 산텐 세이야꾸 가부시키가이샤 [4-(1,3,3-트리메틸-2-옥소-3,4-디히드로-1h-퀴녹살린-7-일)페녹시]에틸옥시 화합물 또는 그의 염
TW201927769A (zh) 2017-12-18 2019-07-16 德商歌林達有限公司 經取代之吡咯啶醯胺ii
MX2020006348A (es) * 2017-12-18 2020-09-03 Gruenenthal Gmbh Pirrolidinamidas i sustituidas.

Also Published As

Publication number Publication date
ECSP21051067A (es) 2021-12-30
EP3908581A1 (en) 2021-11-17
AU2020207591A1 (en) 2021-09-02
KR20210114972A (ko) 2021-09-24
TWI827785B (zh) 2024-01-01
US20200223840A1 (en) 2020-07-16
CA3125929A1 (en) 2020-07-16
CO2021008998A2 (es) 2021-07-30
CL2021001823A1 (es) 2022-02-04
JP2022516785A (ja) 2022-03-02
WO2020144375A1 (en) 2020-07-16
JP7446316B2 (ja) 2024-03-08
IL284642A (en) 2021-08-31
US20220089573A1 (en) 2022-03-24
CN113382990A (zh) 2021-09-10
WO2020144375A9 (en) 2020-10-29
TW202043211A (zh) 2020-12-01
MX2021008364A (es) 2021-08-05
BR112021013557A2 (pt) 2021-09-21

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