GB2600384A - Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia - Google Patents

Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia Download PDF

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Publication number
GB2600384A
GB2600384A GB2015536.2A GB202015536A GB2600384A GB 2600384 A GB2600384 A GB 2600384A GB 202015536 A GB202015536 A GB 202015536A GB 2600384 A GB2600384 A GB 2600384A
Authority
GB
United Kingdom
Prior art keywords
compound
hht
treatment
subject
telangiectasia
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.)
Withdrawn
Application number
GB2015536.2A
Other languages
English (en)
Other versions
GB202015536D0 (en
Inventor
Picard Damien
Saint-Mezard Pierre
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.)
Vaderis Therapeutics AG
Original Assignee
Vaderis Therapeutics AG
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 Vaderis Therapeutics AG filed Critical Vaderis Therapeutics AG
Priority to GB2015536.2A priority Critical patent/GB2600384A/en
Publication of GB202015536D0 publication Critical patent/GB202015536D0/en
Priority to PCT/EP2021/076811 priority patent/WO2022069552A1/en
Priority to KR1020237014688A priority patent/KR20230080448A/ko
Priority to BR112023004885A priority patent/BR112023004885A2/pt
Priority to US18/247,261 priority patent/US12466839B2/en
Priority to IL301466A priority patent/IL301466A/en
Priority to JP2023519016A priority patent/JP2023543993A/ja
Priority to MX2023002996A priority patent/MX2023002996A/es
Priority to AU2021352108A priority patent/AU2021352108B2/en
Priority to CN202180066598.2A priority patent/CN116419924A/zh
Priority to EP21789616.6A priority patent/EP4221713A1/en
Priority to CA3192433A priority patent/CA3192433A1/en
Publication of GB2600384A publication Critical patent/GB2600384A/en
Priority to CL2023000926A priority patent/CL2023000926A1/es
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/535—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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • A61K31/536—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 ortho- or peri-condensed with carbocyclic ring systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
GB2015536.2A 2020-09-30 2020-09-30 Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia Withdrawn GB2600384A (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
GB2015536.2A GB2600384A (en) 2020-09-30 2020-09-30 Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
CA3192433A CA3192433A1 (en) 2020-09-30 2021-09-29 Allosteric akt inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
JP2023519016A JP2023543993A (ja) 2020-09-30 2021-09-29 遺伝性出血性毛細血管拡張症の治療における使用のためのアロステリックａｋｔ阻害剤
AU2021352108A AU2021352108B2 (en) 2020-09-30 2021-09-29 Allosteric akt inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
BR112023004885A BR112023004885A2 (pt) 2020-09-30 2021-09-29 Composto de fórmula (i), ou um sal farmaceuticamente aceitável do mesmo, para uso no tratamento de telangiectasia hemorrágica hereditária (hht) em um indivíduo e composto para uso
US18/247,261 US12466839B2 (en) 2020-09-30 2021-09-29 Allosteric AKT inhibitors for use in the treatment of Hereditary Hemorrhagic Telangiectasia
IL301466A IL301466A (en) 2020-09-30 2021-09-29 Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic capillary dilatation
PCT/EP2021/076811 WO2022069552A1 (en) 2020-09-30 2021-09-29 Allosteric akt inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
MX2023002996A MX2023002996A (es) 2020-09-30 2021-09-29 Inhibidores alostéricos de akt para su uso en el tratamiento de la telangiectasia hemorrágica hereditaria.
KR1020237014688A KR20230080448A (ko) 2020-09-30 2021-09-29 유전성 출혈성 모세혈관확장증의 치료에 사용하기 위한 알로스테릭 akt 저해제
CN202180066598.2A CN116419924A (zh) 2020-09-30 2021-09-29 用于治疗遗传性出血性毛细血管扩张症的变构akt抑制剂
EP21789616.6A EP4221713A1 (en) 2020-09-30 2021-09-29 Allosteric akt inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
CL2023000926A CL2023000926A1 (es) 2020-09-30 2023-03-29 Inhibidores alostéricos de akt para su uso en el tratamiento de telangiectasia hemorrágica hereditaria

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB2015536.2A GB2600384A (en) 2020-09-30 2020-09-30 Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia

Publications (2)

Publication Number Publication Date
GB202015536D0 GB202015536D0 (en) 2020-11-11
GB2600384A true GB2600384A (en) 2022-05-04

Family

ID=73197201

Family Applications (1)

Application Number Title Priority Date Filing Date
GB2015536.2A Withdrawn GB2600384A (en) 2020-09-30 2020-09-30 Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia

Country Status (13)

Country Link
US (1) US12466839B2 (https=)
EP (1) EP4221713A1 (https=)
JP (1) JP2023543993A (https=)
KR (1) KR20230080448A (https=)
CN (1) CN116419924A (https=)
AU (1) AU2021352108B2 (https=)
BR (1) BR112023004885A2 (https=)
CA (1) CA3192433A1 (https=)
CL (1) CL2023000926A1 (https=)
GB (1) GB2600384A (https=)
IL (1) IL301466A (https=)
MX (1) MX2023002996A (https=)
WO (1) WO2022069552A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2600384A (en) 2020-09-30 2022-05-04 Vaderis Therapeutics Ag Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia
WO2026038045A1 (en) 2024-08-15 2026-02-19 Almac Discovery Limited Crystalline forms of 6-(4-((1s,3s)-1-amino-3-hydroxycyclobutyl)phenyl)-1-ethyl-7-phenyl-1h-pyrido[2,3-b][1,4]oxazin-2(3h)-one salts and free base

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011077098A1 (en) * 2009-12-23 2011-06-30 Almac Discovery Limited Inhibitors of akt activity

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI301760B (en) 2004-02-27 2008-10-11 Merz Pharma Gmbh & Co Kgaa Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors
US7910561B2 (en) 2004-12-15 2011-03-22 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
EP1898903B8 (en) 2005-06-10 2013-05-15 Merck Sharp & Dohme Corp. Inhibitors of akt activity
WO2008011032A1 (en) 2006-07-17 2008-01-24 Amgen Inc. Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors
AR064010A1 (es) 2006-12-06 2009-03-04 Merck & Co Inc Inhibidores de la actividad de la akt
JP2010512312A (ja) 2006-12-06 2010-04-22 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性の阻害剤
US7999107B2 (en) 2007-01-31 2011-08-16 Merck Sharp & Dohme Corp. Substituted pyrano[2,3-B]pyridine derivatives as cannabinoid-1 receptor modulators
JP2011522048A (ja) 2008-06-03 2011-07-28 メルク・シャープ・エンド・ドーム・コーポレイション Ａｋｔ活性の阻害剤
US8536193B2 (en) 2008-06-03 2013-09-17 Merck Sharp & Dohme Corp. Inhibitors of AKT activity
EP2116237A1 (en) 2008-08-05 2009-11-11 Polichem SA Compositions for treating rosacea comprising chitosan and a dicarboxylic acid
EA201101186A1 (ru) 2009-02-13 2012-04-30 Байер Фарма Акциенгезельшафт Конденсированные пиримидины
HUE026323T2 (en) 2011-04-07 2016-05-30 Bayer Ip Gmbh Imidazopyridazines as akt kinase inhibitors
EP3294314A4 (en) 2015-05-15 2019-01-16 Memorial Sloan Kettering Cancer Center USE OF PHOPHOINOSITIDE-3-KINASE INHIBITORS FOR THE TREATMENT OF VASCULAR DISEASES
MX2020002611A (es) 2017-09-07 2020-07-13 Univ Res Inst Inc Augusta Activador especifico de akt3 y usos del mismo.
GB2600384A (en) 2020-09-30 2022-05-04 Vaderis Therapeutics Ag Allosteric AKT inhibitors for use in the treatment of hereditary hemorrhagic telangiectasia

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011077098A1 (en) * 2009-12-23 2011-06-30 Almac Discovery Limited Inhibitors of akt activity

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
Circulation, vol. 138, 2018, Ola et al. "SAMD4 prevents flow induced arteriovenous malformations by inhibiting casein kinase 2", pages 2379-2394 [Available from: https://www.ahajournals.org/doi/10.1161/CIRCULATIONAHA.118.033842] *
Nature Cell Biology, vol. 19, No. 6, 2017, Jin et al. "Endoglin prevents vascular malformation by regulating flow-induced cell migration and specification through VEGFR2 signalling", pages 639-652, [Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5467724/] *
Nature Communications, vol. 7, No. 13650, 2016, Ola et al. "PI3 kinase inhibition improves vascular malformations in mouse models of hereditary haemorrhagic telangiectasia", pages 1-12, [Available from: https://www.nature.com/articles/ncomms13650] *
The Journal of Clinical Investigation, vol. 130, No. 2, 2020, Ruiz et al. "Correcting Smad1/5/8, mTOR, and VEGFR2 treats pathology in hereditary hemorrhagic telangiectasia models", pages 942-957, [Available from https://www.jci.org/articles/view/127425] *

Also Published As

Publication number Publication date
US20240092801A1 (en) 2024-03-21
AU2021352108A1 (en) 2023-05-11
CN116419924A (zh) 2023-07-11
WO2022069552A1 (en) 2022-04-07
CL2023000926A1 (es) 2023-11-03
EP4221713A1 (en) 2023-08-09
JP2023543993A (ja) 2023-10-19
MX2023002996A (es) 2023-05-03
KR20230080448A (ko) 2023-06-07
CA3192433A1 (en) 2022-04-07
GB202015536D0 (en) 2020-11-11
AU2021352108B2 (en) 2026-04-02
US12466839B2 (en) 2025-11-11
BR112023004885A2 (pt) 2023-04-18
IL301466A (en) 2023-05-01
AU2021352108A9 (en) 2024-05-23

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WAP Application withdrawn, taken to be withdrawn or refused ** after publication under section 16(1)