WO2020249791A1 - SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS - Google Patents

SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS Download PDF

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Publication number
WO2020249791A1
WO2020249791A1 PCT/EP2020/066391 EP2020066391W WO2020249791A1 WO 2020249791 A1 WO2020249791 A1 WO 2020249791A1 EP 2020066391 W EP2020066391 W EP 2020066391W WO 2020249791 A1 WO2020249791 A1 WO 2020249791A1
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WIPO (PCT)
Prior art keywords
pyrazolo
phenyl
pyridin
fluoro
methyl
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Ceased
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PCT/EP2020/066391
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English (en)
French (fr)
Inventor
Afton HISCOX
Brice Stenne
Christine GELIN
Andrew SAMANT
Jessica WALL
Michael A. Letavic
Curt Dvorak
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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.)
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Publication date
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Priority to BR112021025136A priority Critical patent/BR112021025136A2/pt
Priority to CA3143102A priority patent/CA3143102A1/en
Priority to JP2021573717A priority patent/JP2022536174A/ja
Priority to CN202080043665.4A priority patent/CN113993583A/zh
Priority to KR1020227001094A priority patent/KR20220020917A/ko
Priority to US17/618,066 priority patent/US20220324860A1/en
Priority to EP20734122.3A priority patent/EP3983073A1/en
Priority to AU2020293642A priority patent/AU2020293642A1/en
Priority to MX2021015510A priority patent/MX2021015510A/es
Publication of WO2020249791A1 publication Critical patent/WO2020249791A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants

Definitions

  • R 2 is selected from the group consisting of:
  • An additional embodiment of the invention is a compound of Formula (I) wherein Ar 1 is phenyl.
  • An additional embodiment of the invention is a compound of Formula (I) wherein Ar 1 is phenyl substituted with one member selected from the group consisting of: F, CFb, CF2H, CF2CH3, CF3, and OCF3.
  • R 1 is H, halo, or Cfb
  • enantiomers and diastereomers of the compounds of Formula (I) are enantiomers and diastereomers of the compounds of Formula (I) (as well as Formulas (IA), and (IB)).
  • pharmaceutically acceptable salts, N-oxides or solvates of the compounds of Formula (I) are also within the scope of the invention.
  • pharmaceutically acceptable prodrugs of compounds of Formula (I) are also within the scope of the invention, and pharmaceutically active metabolites of the compounds of Formula (I) (as well as Formulas (IA), and (IB)).
  • An additional embodiment of the invention is a method of treating a subject suffering from or diagnosed with a disease, disorder, or medical condition mediated by GluN2B receptor activity, comprising administering to a subject in need of such treatment an effective amount of at least one compound selected from compounds of Formula (I):
  • the disease, disorder, or medical condition is selected from: neurologic and psychiatric disorders including, but not limited to: (1) mood disorders and mood affective disorders; (2) neurotic, stress-related and somatoform disorders including anxiety disorders; (3) disorders of psychological development; (4) behavioral syndromes associated with physiological disturbances and physical factors; (5) extrapy rami dal and movement disorders; (6) episodic and paroxysmal disorders, epilepsy; (7) pain; (8) forms of neurodegeneration; (9) cerebrovascular diseases, acute and chronic; and any sequelae of cerebrovascular diseases.
  • neurologic and psychiatric disorders including, but not limited to: (1) mood disorders and mood affective disorders; (2) neurotic, stress-related and somatoform disorders including anxiety disorders; (3) disorders of psychological development; (4) behavioral syndromes associated with physiological disturbances and physical factors; (5) extrapy rami dal and movement disorders; (6) episodic and paroxysmal disorders, epilepsy; (7) pain; (8) forms of neurodegeneration; (9) cerebrovascular diseases, acute and chronic
  • disorders belonging to the neurotic, stress-related and somatoform disorders include, but are not limited to, anxiety disorders, general anxiety disorder, panic disorder with or without agoraphobia, specific phobia, social anxiety disorder, chronic anxiety disorders; obsessive compulsive disorder; reaction to sever stress and adjustment disorders, such as post-traumatic stress disorder (PTSD); other neurotic disorders such as depersonalisation-derealisation syndrome.
  • anxiety disorders general anxiety disorder, panic disorder with or without agoraphobia, specific phobia, social anxiety disorder, chronic anxiety disorders; obsessive compulsive disorder; reaction to sever stress and adjustment disorders, such as post-traumatic stress disorder (PTSD); other neurotic disorders such as depersonalisation-derealisation syndrome.
  • PTSD post-traumatic stress disorder
  • CHFCF 3 monofluoroethyl
  • CH2CH2F trifluoroethyl
  • -CF(CF 3 )2 tetrafluorotrifluoromethylethyl
  • a chiral compound can exist as either an individual enantiomer or as a mixture thereof.
  • a mixture containing equal proportions of the enantiomers is called a“racemic mixture.”
  • Example 83 (RS)-6-(3-(Difluoromethyl )-4-fluorophenyl )- l -((ethyl sulfinyl jmethyl )- l H- pyrazolor4.3-blpyridine.
  • Example 17 ((RS)-l-(oxetan-2- ylmethyl)-6-[3-(trifluoromethyl)phenyl]pyrazolo[4,3-b]pyridine) with Agilent Bond Elut SCX cartridge.
  • Example 101 The title compound was prepared by the separation of Example 101 using chiral SFC (Stationary phase: CHIRALPAK IC 5pm 250x20mm, Mobile phase: 70% C0 2 , 30% iPrOH). MS (ESI): mass calcd. for C18H18FN3O, 311.1; m/z found, 312.1 [M+H] + .
  • Example 108 l-(2-Cvclopropyl-2.2-difluoro-ethvO-6-r3-(difluoromethvO-4-fluoro-
  • Example 120 The title compound was prepared by the separation of Example 120 using chiral SFC (Stationary phase: CHIRALPAK AD-H 5pm 250*30mm, Mobile phase: 75% C0 2 , 25% MeOH). MS (ESI): mass calcd. for C19H17F3N4O, 374.1; m/z found, 375.0 [M+H] + . f1uoro ethyl )-4-fluoro-phenyllpyrazolor4.3-blpyridin- l -
  • R 2 is selected from the group consisting of:

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
PCT/EP2020/066391 2019-06-14 2020-06-12 SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS Ceased WO2020249791A1 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
BR112021025136A BR112021025136A2 (pt) 2019-06-14 2020-06-12 Pirazolo[4,3-b]piridinas substituídas e seu uso como moduladoras do receptor de glun2b
CA3143102A CA3143102A1 (en) 2019-06-14 2020-06-12 Substituted pyrazolo[4,3-b]pyridines and their use as glun2b receptor modulators
JP2021573717A JP2022536174A (ja) 2019-06-14 2020-06-12 置換ピラゾロ［４，３－ｂ］ピリジニル及びＧＬＵＮ２Ｂ受容体調節因子としてのそれらの使用
CN202080043665.4A CN113993583A (zh) 2019-06-14 2020-06-12 取代的吡唑并[4,3-b]吡啶及其作为GLUN2B受体调节剂的用途
KR1020227001094A KR20220020917A (ko) 2019-06-14 2020-06-12 치환된 피라졸로[4,3-b]피리딘 및 GLUN2B 수용체 조절제로서의 이들의 용도
US17/618,066 US20220324860A1 (en) 2019-06-14 2020-06-12 SUBSTITUTED PYRAZOLO[4,3-b]PYRIDINES AND THEIR USE AS GLUN2B RECEPTOR MODULATORS
EP20734122.3A EP3983073A1 (en) 2019-06-14 2020-06-12 Substituted pyrazolo[4,3-b]pyridines and their use as glun2b receptor modulators
AU2020293642A AU2020293642A1 (en) 2019-06-14 2020-06-12 Substituted pyrazolo[4,3-b]pyridines and their use as GluN2B receptor modulators
MX2021015510A MX2021015510A (es) 2019-06-14 2020-06-12 Pirazolo[4,3-b]piridinas sustituidas y su uso como moduladores del receptor glun2b.

Applications Claiming Priority (2)

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US201962861674P 2019-06-14 2019-06-14
US62/861,674 2019-06-14

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US (2) US11161846B2 (https=)
EP (1) EP3983073A1 (https=)
JP (1) JP2022536174A (https=)
KR (1) KR20220020917A (https=)
CN (1) CN113993583A (https=)
AU (1) AU2020293642A1 (https=)
BR (1) BR112021025136A2 (https=)
CA (1) CA3143102A1 (https=)
MX (1) MX2021015510A (https=)
WO (1) WO2020249791A1 (https=)

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US11207298B2 (en) 2016-10-06 2021-12-28 Janssen Pharmaceutica Nv Substituted 1H-imidazo[4,5-b]pyridin-2(3H)-ones and their use as GLUN2B receptor modulators
US11214563B2 (en) 2019-06-14 2022-01-04 Janssen Pharmaceutica Nv Substituted pyrazolo-pyrazines and their use as GluN2B receptor modulators
US11447503B2 (en) 2019-06-14 2022-09-20 Janssen Pharmaceutica Nv Pyridine carbamates and their use as GLUN2B receptor modulators
US11459336B2 (en) 2019-06-14 2022-10-04 Janssen Pharmaceutica Nv Pyrazine carbamates and their use as GluN2B receptor modulators
US11530210B2 (en) 2019-06-14 2022-12-20 Janssen Pharmaceutica Nv Substituted heteroaromatic pyrazolo-pyridines and their use as GLUN2B receptor modulators
US11618750B2 (en) 2019-06-14 2023-04-04 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as GluN2B receptor modulators
US12172997B2 (en) 2019-06-14 2024-12-24 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as GluN2B receptor modulators

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