CN116137811B - 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途 - Google Patents

用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途

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Publication number
CN116137811B
CN116137811B CN202180057821.7A CN202180057821A CN116137811B CN 116137811 B CN116137811 B CN 116137811B CN 202180057821 A CN202180057821 A CN 202180057821A CN 116137811 B CN116137811 B CN 116137811B
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formula
compound
pharmaceutically acceptable
acceptable salt
administering
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CN116137811A (zh
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G·加里波帝
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Noema Pharma AG
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Noema Pharma AG
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Psychology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Zoology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
CN202180057821.7A 2020-06-05 2021-06-04 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途 Active CN116137811B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202511962745.0A CN121891333A (zh) 2020-06-05 2021-06-04 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202063035310P 2020-06-05 2020-06-05
US63/035310 2020-06-05
US202163160302P 2021-03-12 2021-03-12
US63/160302 2021-03-12
PCT/EP2021/065074 WO2021245280A1 (en) 2020-06-05 2021-06-04 Use of a phosphodiesterase 10 inhibitor for the treatment of tourette syndrome

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202511962745.0A Division CN121891333A (zh) 2020-06-05 2021-06-04 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途

Publications (2)

Publication Number Publication Date
CN116137811A CN116137811A (zh) 2023-05-19
CN116137811B true CN116137811B (zh) 2026-01-09

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CN202180057821.7A Active CN116137811B (zh) 2020-06-05 2021-06-04 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途
CN202511962745.0A Pending CN121891333A (zh) 2020-06-05 2021-06-04 用于治疗杜尔雷斯综合征的磷酸二酯酶10抑制剂的用途

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Country Status (13)

Country Link
US (2) US11883385B2 (https=)
EP (1) EP4161526A1 (https=)
JP (2) JP7748974B2 (https=)
KR (2) KR20250171459A (https=)
CN (2) CN116137811B (https=)
AU (1) AU2021285225A1 (https=)
BR (1) BR112022024751A2 (https=)
CA (1) CA3180793A1 (https=)
CL (2) CL2022003400A1 (https=)
IL (1) IL298713A (https=)
MX (1) MX2022015400A (https=)
PH (1) PH12023550007A1 (https=)
WO (1) WO2021245280A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12544364B2 (en) * 2020-06-05 2026-02-10 Noema Pharma Ag Use of a phosphodiesterase 10 inhibitor for the treatment of tourette syndrome
WO2022162193A1 (en) * 2021-01-28 2022-08-04 Noema Pharma Ag Methods for the treatment of childhood-onset fluency disorder
WO2026068583A1 (en) * 2024-09-25 2026-04-02 Noema Pharma Ag Use of phosphodiesterase 10 inhibitor gemlapodect for weight loss

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103237803A (zh) * 2010-12-07 2013-08-07 霍夫曼-拉罗奇有限公司 三唑并吡啶化合物
CN107011343A (zh) * 2013-02-27 2017-08-04 持田制药株式会社 新型吡唑衍生物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5605897A (en) * 1991-04-23 1997-02-25 Eli Lilly And Company 2-methyl-thieno-benzodiazepine
US20030032579A1 (en) * 2001-04-20 2003-02-13 Pfizer Inc. Therapeutic use of selective PDE10 inhibitors
EP1723134A2 (en) * 2004-02-18 2006-11-22 Pfizer Products Incorporated Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
US7786139B2 (en) * 2006-11-21 2010-08-31 Omeros Corporation PDE10 inhibitors and related compositions and methods
BR112014004310B8 (pt) * 2011-08-25 2023-04-18 Merck Sharp & Dohme Composto de pirimidina inibidor da enzima fosfodiesterase 10, composição farmacêutica, uso de um composto
PL3919060T3 (pl) * 2012-07-12 2025-10-20 Emalex Biosciences, Inc. Ekopipam do leczenia zespołu tourette'a
MY169128A (en) * 2013-04-30 2019-02-18 Hoffmann La Roche Pd-catalyzed coupling of pyrazole amides

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103237803A (zh) * 2010-12-07 2013-08-07 霍夫曼-拉罗奇有限公司 三唑并吡啶化合物
CN107011343A (zh) * 2013-02-27 2017-08-04 持田制药株式会社 新型吡唑衍生物

Also Published As

Publication number Publication date
CN116137811A (zh) 2023-05-19
KR102892626B1 (ko) 2025-11-28
CA3180793A1 (en) 2021-12-09
BR112022024751A2 (pt) 2023-03-07
CN121891333A (zh) 2026-04-21
IL298713A (en) 2023-02-01
CL2022003400A1 (es) 2023-07-28
US20260076950A1 (en) 2026-03-19
JP2025183391A (ja) 2025-12-16
US11883385B2 (en) 2024-01-30
AU2021285225A1 (en) 2023-01-19
WO2021245280A1 (en) 2021-12-09
JP7748974B2 (ja) 2025-10-03
EP4161526A1 (en) 2023-04-12
MX2022015400A (es) 2023-03-16
WO2021245280A9 (en) 2022-01-27
CL2025002636A1 (es) 2025-11-28
US20230149372A1 (en) 2023-05-18
PH12023550007A1 (en) 2024-03-11
JP2023528896A (ja) 2023-07-06
KR20230040978A (ko) 2023-03-23
KR20250171459A (ko) 2025-12-08

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