KR20210105397A - 라파마이신 유도체 - Google Patents

라파마이신 유도체 Download PDF

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Publication number
KR20210105397A
KR20210105397A KR1020217022532A KR20217022532A KR20210105397A KR 20210105397 A KR20210105397 A KR 20210105397A KR 1020217022532 A KR1020217022532 A KR 1020217022532A KR 20217022532 A KR20217022532 A KR 20217022532A KR 20210105397 A KR20210105397 A KR 20210105397A
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KR
South Korea
Prior art keywords
cancer
compound
formula
disease
pharmaceutically acceptable
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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
KR1020217022532A
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English (en)
Korean (ko)
Inventor
사이먼 보나지
마이클 코널리
데이비드 제이. 글래스
마누엘 미할릭
앤드류 더블유. 패터슨
실비오 로고
테아 샤블라카제
파트리크 쥐거
Original Assignee
노파르티스 아게
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.)
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Application filed by 노파르티스 아게 filed Critical 노파르티스 아게
Publication of KR20210105397A publication Critical patent/KR20210105397A/ko
Pending legal-status Critical Current

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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
    • A61K31/4353—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
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (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)
KR1020217022532A 2018-12-18 2019-12-17 라파마이신 유도체 Pending KR20210105397A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862781242P 2018-12-18 2018-12-18
US62/781,242 2018-12-18
PCT/IB2019/060957 WO2020128861A1 (en) 2018-12-18 2019-12-17 Rapamycin derivatives

Publications (1)

Publication Number Publication Date
KR20210105397A true KR20210105397A (ko) 2021-08-26

Family

ID=69165426

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217022532A Pending KR20210105397A (ko) 2018-12-18 2019-12-17 라파마이신 유도체

Country Status (20)

Country Link
US (1) US12281125B2 (https=)
EP (1) EP3898637B1 (https=)
JP (1) JP7618553B2 (https=)
KR (1) KR20210105397A (https=)
CN (1) CN113260619B (https=)
AU (1) AU2019409366B2 (https=)
BR (1) BR112021011325A2 (https=)
CA (1) CA3122922A1 (https=)
DK (1) DK3898637T3 (https=)
ES (1) ES3014225T3 (https=)
FI (1) FI3898637T3 (https=)
HR (1) HRP20250197T1 (https=)
HU (1) HUE070859T2 (https=)
LT (1) LT3898637T (https=)
MX (1) MX2021007247A (https=)
PL (1) PL3898637T3 (https=)
PT (1) PT3898637T (https=)
RS (1) RS66527B1 (https=)
SI (1) SI3898637T1 (https=)
WO (1) WO2020128861A1 (https=)

Families Citing this family (7)

* 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
IL285067B2 (en) 2019-01-22 2025-02-01 Aeovian Pharmaceuticals Inc MTORC Modulators and Their Uses
AU2020397938A1 (en) 2019-12-05 2022-06-23 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
CN115776907B (zh) 2020-03-27 2025-02-25 艾奥维安制药公司 Mtorc1调节剂及其用途
EP4688148A1 (en) * 2023-04-07 2026-02-11 Regeneron Pharmaceuticals, Inc. Selective rapamycin analogs and uses thereof
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

Family Cites Families (33)

* 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
US4316885A (en) 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
WO1996041865A1 (en) * 1995-06-07 1996-12-27 Ariad Gene Therapeutics, Inc. Rapamcycin-based regulation of biological events
DE69637641D1 (de) 1995-06-07 2008-09-25 Ariad Gene Therapeutics Inc Auf rapamycin basierende regulation biologischer vorgänge
US5985890A (en) 1995-06-09 1999-11-16 Novartis Ag Rapamycin derivatives
GB9606452D0 (en) 1996-03-27 1996-06-05 Sandoz Ltd Organic compounds
CA2257803C (en) 1996-07-12 2008-12-02 Ariad Pharmaceuticals, Inc. Non immunosuppressive antifungal rapalogs
JP2002508971A (ja) 1998-01-15 2002-03-26 アリアド・ジーン・セラピューティクス・インコーポレーテッド 多量体キメラ蛋白質を使用する生物学的イベントの調節
ATE264863T1 (de) 1999-08-24 2004-05-15 Ariad Gene Therapeutics Inc 28-epirapaloge
MX368013B (es) 2001-02-19 2019-09-13 Novartis Ag Tratamiento de cáncer.
PT1478648E (pt) 2002-02-01 2014-07-15 Ariad Pharma Inc Compostos contendo fósforo e suas utilizações
GB0601406D0 (en) 2006-01-24 2006-03-08 Novartis Ag Organic Compounds
US20090023768A1 (en) 2006-02-24 2009-01-22 Novartis Ag Rapamycin derivatives for treating neuroblastoma
WO2008022256A2 (en) 2006-08-16 2008-02-21 Blagosklonny Mikhail V Methods and compositions for preventing or treating age-related diseases
WO2011133636A1 (en) 2010-04-20 2011-10-27 Cedars-Sinai Medical Center COMBINATION THERAPY WITH CD4 LYMPHOCYTE DEPLETION AND mTOR INHIBITORS
EP2670758B1 (en) 2011-02-04 2022-09-28 Synthon BV Process for making trisubstituted silyloxyethyl triflates
CN103391780B (zh) 2011-02-16 2015-08-19 诺瓦提斯公司 用于治疗神经变性疾病的治疗剂的组合物
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
PE20170255A1 (es) 2014-01-24 2017-03-22 Dana Farber Cancer Inst Inc Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas
EP3109250A1 (en) 2015-06-23 2016-12-28 Synbias Pharma AG Method for the synthesis of rapamycin derivatives
US10683308B2 (en) 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
WO2018204416A1 (en) 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
US20220202787A1 (en) 2019-03-26 2022-06-30 Novartis Ag Isothiazolidine 1,1-dioxide and 1,4-butan sultone containing rapamycin derivatives and uses thereof

Also Published As

Publication number Publication date
PL3898637T3 (pl) 2025-05-19
HUE070859T2 (hu) 2025-07-28
CN113260619A (zh) 2021-08-13
PT3898637T (pt) 2025-02-24
JP7618553B2 (ja) 2025-01-21
JP2022514254A (ja) 2022-02-10
MX2021007247A (es) 2021-07-15
LT3898637T (lt) 2025-03-10
CA3122922A1 (en) 2020-06-25
CN113260619B (zh) 2026-02-03
SI3898637T1 (sl) 2025-04-30
HRP20250197T1 (hr) 2025-04-11
AU2019409366A1 (en) 2021-06-10
ES3014225T3 (en) 2025-04-21
EP3898637A1 (en) 2021-10-27
US20220064185A1 (en) 2022-03-03
US12281125B2 (en) 2025-04-22
EP3898637B1 (en) 2024-11-20
FI3898637T3 (fi) 2025-02-24
AU2019409366B2 (en) 2022-10-27
WO2020128861A1 (en) 2020-06-25
DK3898637T3 (da) 2025-02-17
RS66527B1 (sr) 2025-03-31
BR112021011325A2 (pt) 2021-11-16

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