AU2016377658B2 - Tripartite modulators of endosomal G protein-coupled receptors - Google Patents

Tripartite modulators of endosomal G protein-coupled receptors Download PDF

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Publication number
AU2016377658B2
AU2016377658B2 AU2016377658A AU2016377658A AU2016377658B2 AU 2016377658 B2 AU2016377658 B2 AU 2016377658B2 AU 2016377658 A AU2016377658 A AU 2016377658A AU 2016377658 A AU2016377658 A AU 2016377658A AU 2016377658 B2 AU2016377658 B2 AU 2016377658B2
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AU
Australia
Prior art keywords
pain
group
endosomal
optionally
compound
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Ceased
Application number
AU2016377658A
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English (en)
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AU2016377658A1 (en
Inventor
Nigel W. Bunnett
Derek Cole
Gareth HICKS
Gavin Hirst
Christopher J.H. Porter
Junya Shirai
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Endosome Therapeutics Inc
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Endosome Therapeutics Inc
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Filing date
Publication date
Priority claimed from AU2015905333A external-priority patent/AU2015905333A0/en
Application filed by Endosome Therapeutics Inc filed Critical Endosome Therapeutics Inc
Publication of AU2016377658A1 publication Critical patent/AU2016377658A1/en
Application granted granted Critical
Publication of AU2016377658B2 publication Critical patent/AU2016377658B2/en
Priority to AU2022291659A priority Critical patent/AU2022291659A1/en
Assigned to ENDOSOME THERAPEUTICS, INC. reassignment ENDOSOME THERAPEUTICS, INC. Request for Assignment Assignors: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Priority to AU2025201136A priority patent/AU2025201136A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
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    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
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    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Botany (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Nutrition Science (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
AU2016377658A 2015-12-22 2016-12-21 Tripartite modulators of endosomal G protein-coupled receptors Ceased AU2016377658B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2022291659A AU2022291659A1 (en) 2015-12-22 2022-12-28 Tripartite modulators of endosomal G protein-coupled receptors
AU2025201136A AU2025201136A1 (en) 2015-12-22 2025-02-18 Tripartite modulators of endosomal G protein-coupled receptors

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
AU2015905333 2015-12-22
AU2015905333A AU2015905333A0 (en) 2015-12-22 Modulators of Endosomal G Protein-Coupled Receptors
US201662291161P 2016-02-04 2016-02-04
US62/291,161 2016-02-04
PCT/US2016/068075 WO2017112792A1 (en) 2015-12-22 2016-12-21 Tripartite modulators of endosomal g protein-coupled receptors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2022291659A Division AU2022291659A1 (en) 2015-12-22 2022-12-28 Tripartite modulators of endosomal G protein-coupled receptors

Publications (2)

Publication Number Publication Date
AU2016377658A1 AU2016377658A1 (en) 2018-06-21
AU2016377658B2 true AU2016377658B2 (en) 2022-09-29

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Application Number Title Priority Date Filing Date
AU2016377658A Ceased AU2016377658B2 (en) 2015-12-22 2016-12-21 Tripartite modulators of endosomal G protein-coupled receptors
AU2022291659A Abandoned AU2022291659A1 (en) 2015-12-22 2022-12-28 Tripartite modulators of endosomal G protein-coupled receptors
AU2025201136A Abandoned AU2025201136A1 (en) 2015-12-22 2025-02-18 Tripartite modulators of endosomal G protein-coupled receptors

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2022291659A Abandoned AU2022291659A1 (en) 2015-12-22 2022-12-28 Tripartite modulators of endosomal G protein-coupled receptors
AU2025201136A Abandoned AU2025201136A1 (en) 2015-12-22 2025-02-18 Tripartite modulators of endosomal G protein-coupled receptors

Country Status (8)

Country Link
US (3) US11324832B2 (enExample)
EP (1) EP3393519A1 (enExample)
JP (3) JP7074673B2 (enExample)
CN (2) CN115531553A (enExample)
AU (3) AU2016377658B2 (enExample)
CA (1) CA3009325A1 (enExample)
EA (1) EA201891472A1 (enExample)
WO (1) WO2017112792A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2770050C2 (ru) 2015-03-04 2022-04-14 Ванда Фармасьютиклз Инк. Способ лечения с применением традипитанта
EA201891472A1 (ru) * 2015-12-22 2018-12-28 Такеда Фармасьютикал Компани Лимитед Тройные модуляторы эндосомальных рецепторов, сопряженных с g-белком
WO2017197463A1 (en) * 2016-05-20 2017-11-23 Monash University Treatment of pain
DK3710000T3 (da) * 2017-11-17 2025-06-16 Vanda Pharmaceuticals Inc Tradipitant til anvendelse til behandling af gastroparese
IT202200018768A1 (it) * 2022-09-14 2024-03-14 Alberto Chiarugi Trattamento della nausea e vomito da chemioterapia
IT202200018780A1 (it) * 2022-09-14 2024-03-14 Alberto Chiarugi Modulatori degli effetti della chemioterapia

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US20030148449A1 (en) * 2000-04-21 2003-08-07 Athan Kuliopulos G protein coupled receptor agonists and antagonists and methods of activating and inhibiting G protein coupled receptors using the same
WO2005097199A1 (en) * 2004-04-08 2005-10-20 Jadolabs Gmbh Tripartite conjugates containing a structure interacting with cell membrane rafts and their use
WO2006004195A1 (en) * 2004-07-02 2006-01-12 Tanabe Seiyaku Co., Ltd. Piperidine compound and process for preparing the same
WO2014168721A2 (en) * 2013-04-12 2014-10-16 Tufts Medical Center Methods and systems for designing and/or characterizing soluble lipidated ligand agents

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EP1035115B1 (en) * 1999-02-24 2004-09-29 F. Hoffmann-La Roche Ag 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
IL144851A0 (en) * 1999-02-24 2002-06-30 Hoffmann La Roche 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
TWI287003B (en) * 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
TWI259180B (en) * 2000-08-08 2006-08-01 Hoffmann La Roche 4-Phenyl-pyridine derivatives
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BR112013007566A2 (pt) * 2010-09-28 2016-08-02 Panacea Biotec Ltd novos compostos bicíclicos
EP3018126A4 (en) 2013-07-03 2016-12-07 Takeda Pharmaceuticals Co HETEROCYCLIC CONNECTION
EA201891472A1 (ru) * 2015-12-22 2018-12-28 Такеда Фармасьютикал Компани Лимитед Тройные модуляторы эндосомальных рецепторов, сопряженных с g-белком

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
US20030148449A1 (en) * 2000-04-21 2003-08-07 Athan Kuliopulos G protein coupled receptor agonists and antagonists and methods of activating and inhibiting G protein coupled receptors using the same
WO2005097199A1 (en) * 2004-04-08 2005-10-20 Jadolabs Gmbh Tripartite conjugates containing a structure interacting with cell membrane rafts and their use
WO2006004195A1 (en) * 2004-07-02 2006-01-12 Tanabe Seiyaku Co., Ltd. Piperidine compound and process for preparing the same
WO2014168721A2 (en) * 2013-04-12 2014-10-16 Tufts Medical Center Methods and systems for designing and/or characterizing soluble lipidated ligand agents

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Title
DOYLE J R. et al., "A Two-Step Strategy to Enhance Activity of Low Potency Peptides", PLOS ONE, (2014-11-12), vol. 9, no. 11, doi:10.1371/journal.pone.0110502, page e110502 *

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JP2019503356A (ja) 2019-02-07
JP7074673B2 (ja) 2022-05-24
JP2024073581A (ja) 2024-05-29
EA201891472A1 (ru) 2018-12-28
JP7458681B2 (ja) 2024-04-01
US20230119819A1 (en) 2023-04-20
US11324832B2 (en) 2022-05-10
AU2022291659A1 (en) 2023-02-02
JP2022113164A (ja) 2022-08-03
AU2016377658A1 (en) 2018-06-21
WO2017112792A1 (en) 2017-06-29
EP3393519A1 (en) 2018-10-31
CA3009325A1 (en) 2017-06-29
CN115531553A (zh) 2022-12-30
AU2025201136A1 (en) 2025-03-06
CN108712913A (zh) 2018-10-26
CN108712913B (zh) 2022-06-24
BR112018012425A2 (pt) 2018-12-18
US20250235544A1 (en) 2025-07-24
US20190000981A1 (en) 2019-01-03

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