CN113260619B - 雷帕霉素衍生物 - Google Patents

雷帕霉素衍生物

Info

Publication number
CN113260619B
CN113260619B CN201980087363.4A CN201980087363A CN113260619B CN 113260619 B CN113260619 B CN 113260619B CN 201980087363 A CN201980087363 A CN 201980087363A CN 113260619 B CN113260619 B CN 113260619B
Authority
CN
China
Prior art keywords
formula
compound
pharmaceutically acceptable
disease
acceptable salt
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.)
Active
Application number
CN201980087363.4A
Other languages
English (en)
Chinese (zh)
Other versions
CN113260619A (zh
Inventor
S·波纳齐
M·康诺利
D·J·格拉斯
M·米哈里克
A·W·帕特森
S·罗格
T·沙夫拉卡泽
P·齐格
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.)
Novartis AG
Original Assignee
Novartis 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 Novartis AG filed Critical Novartis AG
Publication of CN113260619A publication Critical patent/CN113260619A/zh
Application granted granted Critical
Publication of CN113260619B publication Critical patent/CN113260619B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • C07D498/12—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

Landscapes

  • 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)
CN201980087363.4A 2018-12-18 2019-12-17 雷帕霉素衍生物 Active CN113260619B (zh)

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 (2)

Publication Number Publication Date
CN113260619A CN113260619A (zh) 2021-08-13
CN113260619B true CN113260619B (zh) 2026-02-03

Family

ID=69165426

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980087363.4A Active CN113260619B (zh) 2018-12-18 2019-12-17 雷帕霉素衍生物

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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996041865A1 (en) * 1995-06-07 1996-12-27 Ariad Gene Therapeutics, Inc. Rapamcycin-based regulation of biological events
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

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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
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
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996041865A1 (en) * 1995-06-07 1996-12-27 Ariad Gene Therapeutics, Inc. Rapamcycin-based regulation of biological events
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

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
KR20210105397A (ko) 2021-08-26
JP2022514254A (ja) 2022-02-10
MX2021007247A (es) 2021-07-15
LT3898637T (lt) 2025-03-10
CA3122922A1 (en) 2020-06-25
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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