WO2019142053A2 - Composés inhibiteurs thérapeutiques - Google Patents

Composés inhibiteurs thérapeutiques Download PDF

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Publication number
WO2019142053A2
WO2019142053A2 PCT/IB2019/000079 IB2019000079W WO2019142053A2 WO 2019142053 A2 WO2019142053 A2 WO 2019142053A2 IB 2019000079 W IB2019000079 W IB 2019000079W WO 2019142053 A2 WO2019142053 A2 WO 2019142053A2
Authority
WO
WIPO (PCT)
Prior art keywords
methyl
chloro
carboxamide
fluoroquinolin
mmol
Prior art date
Application number
PCT/IB2019/000079
Other languages
English (en)
Other versions
WO2019142053A3 (fr
Inventor
Andrew Mcdonald
Shawn QIAN
Original Assignee
Lifesci Pharmaceuticals, Inc.
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 Lifesci Pharmaceuticals, Inc. filed Critical Lifesci Pharmaceuticals, Inc.
Publication of WO2019142053A2 publication Critical patent/WO2019142053A2/fr
Publication of WO2019142053A3 publication Critical patent/WO2019142053A3/fr

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Classifications

    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • 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
    • 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

Definitions

  • each R b is independently a direct bond or a straight or branched alkylene or alkenylene chain
  • R c is a straight or branched alkylene or alkenylene chain
  • prodrugs are also meant to include any covalently bonded carriers, which release the active compound in vivo when such prodrug is administered to a mammalian subject.
  • Prodrugs of an active compound, as described herein are prepared by modifying functional groups present in the active compound in such a way that the modifications are cleaved, either in routine manipulation or in vivo , to the parent active compound.
  • X is hydrogen, -NH 2 , -N0 2 , -CN, -NHCOCH 3 , -C0 2 H, optionally substituted alkoxycarbonyl, optionally substituted aminocarbonyl, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 alkoxy, -CH 2 F, -CHF 2 , or -CF 3.
  • Ring A is 3-chloro-lH-pyrrolo[2,3-b]pyridin- 5-yl.
  • One embodiment provides a compound of any one of Formula (I), (la), (II),

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La présente invention concerne des composés de dérivés hétérocycliques et des compositions pharmaceutiques comprenant ces composés qui sont utiles pour inhiber la kallicréine plasmatique. En outre, les composés et les compositions de l'invention sont utiles pour le traitement de maladies dans lesquelles l'inhibition de l'inhibition de la kallicréine plasmatique a été impliquée, telles que l'œdème de Quincke et analogue.
PCT/IB2019/000079 2018-01-17 2019-01-17 Composés inhibiteurs thérapeutiques WO2019142053A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862618578P 2018-01-17 2018-01-17
US62/618,578 2018-01-17

Publications (2)

Publication Number Publication Date
WO2019142053A2 true WO2019142053A2 (fr) 2019-07-25
WO2019142053A3 WO2019142053A3 (fr) 2019-11-14

Family

ID=67302024

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2019/000079 WO2019142053A2 (fr) 2018-01-17 2019-01-17 Composés inhibiteurs thérapeutiques

Country Status (1)

Country Link
WO (1) WO2019142053A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111303035A (zh) * 2020-03-18 2020-06-19 徐州圣元化工有限公司 一种3-(二氟甲基)-1-甲基-1h-吡唑-4-羧酸的制备方法
WO2024059186A1 (fr) * 2022-09-15 2024-03-21 Takeda Pharmaceutical Company Limited Dérivés de n-((isoquinolin-6-yl)méthyl)-1 h-pyrazole-4-carboxamide en tant qu' inhibiteurs de la kallicréine plasmatique pour le traitement de l'angioœdème héréditaire

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9611252B2 (en) * 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
EP3481391A4 (fr) * 2016-07-11 2020-03-11 Lifesci Pharmaceuticals, Inc. Composés inhibiteurs thérapeutiques

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111303035A (zh) * 2020-03-18 2020-06-19 徐州圣元化工有限公司 一种3-(二氟甲基)-1-甲基-1h-吡唑-4-羧酸的制备方法
WO2024059186A1 (fr) * 2022-09-15 2024-03-21 Takeda Pharmaceutical Company Limited Dérivés de n-((isoquinolin-6-yl)méthyl)-1 h-pyrazole-4-carboxamide en tant qu' inhibiteurs de la kallicréine plasmatique pour le traitement de l'angioœdème héréditaire

Also Published As

Publication number Publication date
WO2019142053A3 (fr) 2019-11-14

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