JP7461369B2 - イソチアゾリジン１，１－ジオキシド及び１，４－ブタンスルトン含有ラパマイシン誘導体並びにその使用 - Google Patents

イソチアゾリジン１，１－ジオキシド及び１，４－ブタンスルトン含有ラパマイシン誘導体並びにその使用 Download PDF

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JP7461369B2
JP7461369B2 JP2021557231A JP2021557231A JP7461369B2 JP 7461369 B2 JP7461369 B2 JP 7461369B2 JP 2021557231 A JP2021557231 A JP 2021557231A JP 2021557231 A JP2021557231 A JP 2021557231A JP 7461369 B2 JP7461369 B2 JP 7461369B2
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disease
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JP2022527270A (ja
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ボナッツィ，サイモン
コノリー，マイケル
ジェイ． グラス，デービッド
ダブリュ． パターソン，アンドリュ
シャフラカージェ，ティー
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ノバルティス アーゲー
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    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/18—Bridged 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/436—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 six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021557231A 2019-03-26 2020-03-25 イソチアゾリジン１，１－ジオキシド及び１，４－ブタンスルトン含有ラパマイシン誘導体並びにその使用 Active JP7461369B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962824190P 2019-03-26 2019-03-26
US62/824,190 2019-03-26
PCT/IB2020/052825 WO2020194209A1 (en) 2019-03-26 2020-03-25 Isothiazolidine 1,1-dioxide and 1,4-butan sultone containing rapamycin derivatives and uses thereof

Publications (3)

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JP2022527270A JP2022527270A (ja) 2022-06-01
JP2022527270A5 JP2022527270A5 (https=) 2023-04-03
JP7461369B2 true JP7461369B2 (ja) 2024-04-03

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JP2021557231A Active JP7461369B2 (ja) 2019-03-26 2020-03-25 イソチアゾリジン１，１－ジオキシド及び１，４－ブタンスルトン含有ラパマイシン誘導体並びにその使用

Country Status (20)

Country Link
US (1) US20220202787A1 (https=)
EP (1) EP3947392B1 (https=)
JP (1) JP7461369B2 (https=)
KR (1) KR20210142689A (https=)
CN (1) CN113614090B (https=)
AU (1) AU2020250026B2 (https=)
BR (1) BR112021018692A2 (https=)
CA (1) CA3134653A1 (https=)
DK (1) DK3947392T3 (https=)
ES (1) ES2987625T3 (https=)
FI (1) FI3947392T3 (https=)
HR (1) HRP20240633T1 (https=)
HU (1) HUE067396T2 (https=)
LT (1) LT3947392T (https=)
MX (1) MX2021011376A (https=)
PL (1) PL3947392T3 (https=)
PT (1) PT3947392T (https=)
RS (1) RS65531B1 (https=)
SI (1) SI3947392T1 (https=)
WO (1) WO2020194209A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
WO2019241789A1 (en) 2018-06-15 2019-12-19 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
HRP20250197T1 (hr) 2018-12-18 2025-04-11 Novartis Ag Derivati rapamicina
AU2020397938A1 (en) 2019-12-05 2022-06-23 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
JP2023028473A (ja) * 2021-08-19 2023-03-03 日本マイクロバイオファーマ株式会社 エベロリムスの製造方法
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001014387A1 (en) 1999-08-24 2001-03-01 Ariad Gene Therapeutics, Inc. 28-epirapalogs
JP2002514165A (ja) 1996-07-12 2002-05-14 アリアド・ファーマシューティカルズ・インコーポレイテッド 病原性真菌感染の治療または予防材料および方法
JP2009527520A (ja) 2006-02-24 2009-07-30 ノバルティス アクチエンゲゼルシャフト 神経芽腫を処置するためのラパマイシン誘導体
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA737247B (en) 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
ZA935112B (en) * 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
JP6130391B2 (ja) 2011-11-23 2017-05-17 インテリカイン， エルエルシー Ｍｔｏｒ阻害剤を使用する強化された治療レジメン
AR112834A1 (es) * 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002514165A (ja) 1996-07-12 2002-05-14 アリアド・ファーマシューティカルズ・インコーポレイテッド 病原性真菌感染の治療または予防材料および方法
WO2001014387A1 (en) 1999-08-24 2001-03-01 Ariad Gene Therapeutics, Inc. 28-epirapalogs
JP2009527520A (ja) 2006-02-24 2009-07-30 ノバルティス アクチエンゲゼルシャフト 神経芽腫を処置するためのラパマイシン誘導体
WO2017044720A1 (en) 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Luengo, Juan I. et al.，Manipulation of the Rapamycin Effector Domain. Selective Nucleophilic Substitution of the C7 Methoxy Group，Journal of Organic Chemistry，1994年，(1994), 59(22), 6512-13

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Publication number Publication date
MX2021011376A (es) 2021-10-13
KR20210142689A (ko) 2021-11-25
EP3947392B1 (en) 2024-02-28
CN113614090A (zh) 2021-11-05
RS65531B1 (sr) 2024-06-28
SI3947392T1 (sl) 2024-07-31
EP3947392A1 (en) 2022-02-09
HUE067396T2 (hu) 2024-10-28
PT3947392T (pt) 2024-05-14
AU2020250026B2 (en) 2023-08-10
AU2020250026A1 (en) 2021-09-23
LT3947392T (lt) 2024-05-27
BR112021018692A2 (pt) 2021-11-23
WO2020194209A1 (en) 2020-10-01
JP2022527270A (ja) 2022-06-01
US20220202787A1 (en) 2022-06-30
HRP20240633T1 (hr) 2024-08-02
FI3947392T3 (fi) 2024-05-08
CA3134653A1 (en) 2020-10-01
PL3947392T3 (pl) 2024-07-15
CN113614090B (zh) 2026-04-28
ES2987625T3 (es) 2024-11-15
DK3947392T3 (da) 2024-04-29

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