CA3078191A1 - Rapamycin derivatives - Google Patents

Rapamycin derivatives Download PDF

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Publication number
CA3078191A1
CA3078191A1 CA3078191A CA3078191A CA3078191A1 CA 3078191 A1 CA3078191 A1 CA 3078191A1 CA 3078191 A CA3078191 A CA 3078191A CA 3078191 A CA3078191 A CA 3078191A CA 3078191 A1 CA3078191 A1 CA 3078191A1
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Canada
Prior art keywords
cancer
disease
pharmaceutically acceptable
disorder
acceptable salt
Prior art date
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Pending
Application number
CA3078191A
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English (en)
French (fr)
Inventor
Simone BONAZZI
Michael Connolly
David Jonathan Glass
Manuel Mihalic
Andrew William PATTERSON
Silvio Roggo
Tea Shavlakadze
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Novartis AG
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Novartis AG
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Publication of CA3078191A1 publication Critical patent/CA3078191A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • 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
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    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Communicable Diseases (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
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CA3078191A 2017-09-26 2018-09-25 Rapamycin derivatives Pending CA3078191A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762563312P 2017-09-26 2017-09-26
US62/563,312 2017-09-26
PCT/IB2018/057422 WO2019064182A1 (en) 2017-09-26 2018-09-25 RAPAMYCIN DERIVATIVES

Publications (1)

Publication Number Publication Date
CA3078191A1 true CA3078191A1 (en) 2019-04-04

Family

ID=63857991

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3078191A Pending CA3078191A1 (en) 2017-09-26 2018-09-25 Rapamycin derivatives

Country Status (23)

Country Link
US (4) US10800793B2 (https=)
EP (2) EP4365179A3 (https=)
JP (2) JP7387590B2 (https=)
KR (2) KR20250054121A (https=)
CN (2) CN117417351A (https=)
AR (1) AR112834A1 (https=)
AU (1) AU2018342784B2 (https=)
BR (1) BR112020005898A2 (https=)
CA (1) CA3078191A1 (https=)
DK (1) DK3687999T3 (https=)
ES (1) ES2973975T3 (https=)
FI (1) FI3687999T3 (https=)
HR (1) HRP20240199T8 (https=)
HU (1) HUE065692T2 (https=)
LT (1) LT3687999T (https=)
MX (2) MX2020007265A (https=)
PL (1) PL3687999T3 (https=)
PT (1) PT3687999T (https=)
RS (1) RS65270B1 (https=)
SI (1) SI3687999T1 (https=)
TW (1) TW201920189A (https=)
UY (1) UY37900A (https=)
WO (1) WO2019064182A1 (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11066416B2 (en) 2016-02-04 2021-07-20 The Johns Hopkins University Rapafucin derivative compounds and methods of use thereof
MX380313B (es) 2016-02-04 2025-03-12 Univ Johns Hopkins Rapadocinas, inhibidores de transportador 1 de nucleósido equilibrador y usos de los mismos.
US11708391B2 (en) 2016-02-04 2023-07-25 The Johns Hopkins University Rapaglutins, novel inhibitors of GLUT and use thereof
AR112834A1 (es) 2017-09-26 2019-12-18 Novartis Ag Derivados de rapamicina
IL312291A (en) 2018-05-01 2024-06-01 Revolution Medicines Inc C-26-linked rapamycin analogs as MTOR inhibitors
MX2020011565A (es) 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor.
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
IL285067B2 (en) 2019-01-22 2025-02-01 Aeovian Pharmaceuticals Inc MTORC Modulators and Their Uses
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
KR102486721B1 (ko) * 2019-08-23 2023-01-10 이화여자대학교 산학협력단 신규 mTOR 억제제 화합물 및 이의 용도
KR102497821B1 (ko) * 2019-08-23 2023-02-08 이화여자대학교 산학협력단 신규 mTOR 억제제 화합물 및 이의 용도
TW202126323A (zh) * 2019-10-01 2021-07-16 約翰斯赫普金斯大學 雷帕弗辛（Ｒａｐａｆｕｃｉｎ）衍生化合物及其使用方法
AU2020397938A1 (en) 2019-12-05 2022-06-23 Janssen Pharmaceutica Nv Rapamycin analogs and uses thereof
EP4118431B1 (de) 2020-03-12 2026-05-06 Heinrich-Heine-Universität Düsseldorf Inhibition von fkbp1a zur therapie des triple-negativen mammakarzinoms
DE102020203224A1 (de) 2020-03-12 2021-09-16 Heinrich-Heine-Universität Düsseldorf Inhibition von FKBP1A zur Therapie des Triple-negativen Mammakarzinoms
CN115776907B (zh) * 2020-03-27 2025-02-25 艾奥维安制药公司 Mtorc1调节剂及其用途
CN121426814A (zh) * 2020-07-21 2026-01-30 艾奥维安制药公司 Mtorc1调节剂及其用途
TW202206093A (zh) * 2020-08-12 2022-02-16 中國醫藥大學 Ｓｅｍａ３ｄ拮抗劑用於預防或治療神經退化性疾病以及延長壽命之用途
CA3256390A1 (en) 2022-05-25 2023-11-30 Revolution Medicines, Inc. CANCER TREATMENT METHODS USING AN MTOR INHIBITOR
EP4688148A1 (en) * 2023-04-07 2026-02-11 Regeneron Pharmaceuticals, Inc. Selective rapamycin analogs and uses thereof
WO2024243449A1 (en) * 2023-05-23 2024-11-28 Tornado Therapeutics, Inc. Rapamycin derivatives and uses thereof
GB202415232D0 (en) 2024-10-16 2024-11-27 Nacamed As Composition

Family Cites Families (38)

* 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
DE69637641D1 (de) 1995-06-07 2008-09-25 Ariad Gene Therapeutics Inc Auf rapamycin basierende regulation biologischer vorgänge
WO1996041865A1 (en) 1995-06-07 1996-12-27 Ariad Gene Therapeutics, Inc. Rapamcycin-based regulation of biological events
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
GB0504994D0 (en) * 2005-03-11 2005-04-20 Biotica Tech Ltd Novel compounds
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
GB0911888D0 (en) * 2009-07-08 2009-08-19 Oxford Biodynamics Ltd Method of treating age related disorders
US20150361120A1 (en) * 2010-03-31 2015-12-17 Chengzhi Zhang MACROLIDE INHIBITORS OF mTOR
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
PH12017500997A1 (en) * 2012-04-04 2018-02-19 Samumed Llc Indazole inhibitors of the wnt signal pathway and therapeutic uses thereof
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
HRP20250197T1 (hr) 2018-12-18 2025-04-11 Novartis Ag Derivati 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

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