CA3009325A1 - 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
CA3009325A1
CA3009325A1 CA3009325A CA3009325A CA3009325A1 CA 3009325 A1 CA3009325 A1 CA 3009325A1 CA 3009325 A CA3009325 A CA 3009325A CA 3009325 A CA3009325 A CA 3009325A CA 3009325 A1 CA3009325 A1 CA 3009325A1
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CA
Canada
Prior art keywords
group
endosomal
compound
modulator
optionally
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3009325A
Other languages
English (en)
French (fr)
Inventor
Nigel W. Bunnett
Christopher J.H. Porter
Derek Cole
Gareth HICKS
Junya Shirai
Gavin Hirst
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
Original Assignee
Takeda Pharmaceutical Co Ltd
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
Priority claimed from AU2015905333A external-priority patent/AU2015905333A0/en
Application filed by Takeda Pharmaceutical Co Ltd filed Critical Takeda Pharmaceutical Co Ltd
Publication of CA3009325A1 publication Critical patent/CA3009325A1/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/554Medicinal 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • AHUMAN NECESSITIES
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/59Medicinal 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
    • A61K47/60Medicinal 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 the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
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    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P25/24Antidepressants
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    • AHUMAN NECESSITIES
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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Chemical & Material Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
  • Botany (AREA)
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  • 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)
CA3009325A 2015-12-22 2016-12-21 Tripartite modulators of endosomal g protein-coupled receptors Pending CA3009325A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
AU2015905333A AU2015905333A0 (en) 2015-12-22 Modulators of Endosomal G Protein-Coupled Receptors
AU2015905333 2015-12-22
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

Publications (1)

Publication Number Publication Date
CA3009325A1 true CA3009325A1 (en) 2017-06-29

Family

ID=59091175

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3009325A Pending CA3009325A1 (en) 2015-12-22 2016-12-21 Tripartite modulators of endosomal g protein-coupled receptors

Country Status (8)

Country Link
US (3) US11324832B2 (https=)
EP (1) EP3393519A1 (https=)
JP (3) JP7074673B2 (https=)
CN (2) CN108712913B (https=)
AU (3) AU2016377658B2 (https=)
CA (1) CA3009325A1 (https=)
EA (1) EA201891472A1 (https=)
WO (1) WO2017112792A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2978736C (en) 2015-03-04 2023-11-07 Vanda Pharmaceuticals Inc. Dosing regimen of tradipitant
WO2017112792A1 (en) * 2015-12-22 2017-06-29 Takeda Pharmaceutical Company Limited Tripartite modulators of endosomal g protein-coupled receptors
CN109152777A (zh) * 2016-05-20 2019-01-04 武田药品工业株式会社 疼痛的治疗
KR20250140655A (ko) * 2017-11-17 2025-09-25 반다 파마슈티칼즈, 인코퍼레이티드. 트라디피탄트를 이용한 위장 질환의 치료 방법
IT202200018780A1 (it) * 2022-09-14 2024-03-14 Alberto Chiarugi Modulatori degli effetti della chemioterapia
IT202200018768A1 (it) * 2022-09-14 2024-03-14 Alberto Chiarugi Trattamento della nausea e vomito da chemioterapia

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1394150B1 (en) 1999-02-24 2011-01-19 F. Hoffmann-La Roche AG 4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
SI1157005T1 (en) 1999-02-24 2005-02-28 F. Hoffmann-La Roche Ag 3-phenylpyridine derivatives and their use as nk-1 receptor antagonists
US7696168B2 (en) * 2000-04-21 2010-04-13 Tufts Medical Center, Inc. G protein coupled receptor agonists and antagonists and methods of activating and inhibiting G protein coupled receptors using the same
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
EP2119455A1 (en) * 2004-04-08 2009-11-18 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Tripartite raftophilic structures and their use
NZ551563A (en) 2004-06-30 2009-06-26 Janssen Pharmaceutica Nv Alpha,beta-unsaturated esters and acids by stereoselective dehydration
TW200606152A (en) 2004-07-02 2006-02-16 Tanabe Seiyaku Co Piperidine compound and process for preparing the same
JP2013542929A (ja) * 2010-09-28 2013-11-28 パナセア バイオテック リミテッド 新規ビシクロ環化合物
WO2014168721A2 (en) * 2013-04-12 2014-10-16 Tufts Medical Center Methods and systems for designing and/or characterizing soluble lipidated ligand agents
JP6427491B2 (ja) 2013-07-03 2018-11-21 武田薬品工業株式会社 複素環化合物
WO2017112792A1 (en) * 2015-12-22 2017-06-29 Takeda Pharmaceutical Company Limited Tripartite modulators of endosomal g protein-coupled receptors

Also Published As

Publication number Publication date
US11324832B2 (en) 2022-05-10
JP2019503356A (ja) 2019-02-07
AU2016377658A1 (en) 2018-06-21
US20190000981A1 (en) 2019-01-03
US20230119819A1 (en) 2023-04-20
AU2025201136A1 (en) 2025-03-06
JP2024073581A (ja) 2024-05-29
AU2022291659A1 (en) 2023-02-02
CN108712913B (zh) 2022-06-24
EP3393519A1 (en) 2018-10-31
BR112018012425A2 (pt) 2018-12-18
EA201891472A1 (ru) 2018-12-28
CN115531553A (zh) 2022-12-30
JP7458681B2 (ja) 2024-04-01
JP7074673B2 (ja) 2022-05-24
WO2017112792A1 (en) 2017-06-29
US20250235544A1 (en) 2025-07-24
AU2016377658B2 (en) 2022-09-29
CN108712913A (zh) 2018-10-26
JP2022113164A (ja) 2022-08-03

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