CA2960992C - Mtorc1 inhibitors - Google Patents

Mtorc1 inhibitors Download PDF

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Publication number
CA2960992C
CA2960992C CA2960992A CA2960992A CA2960992C CA 2960992 C CA2960992 C CA 2960992C CA 2960992 A CA2960992 A CA 2960992A CA 2960992 A CA2960992 A CA 2960992A CA 2960992 C CA2960992 C CA 2960992C
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Prior art keywords
substituted
unsubstituted
independently
nhc
disease
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Active
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CA2960992A
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English (en)
French (fr)
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CA2960992A1 (en
Inventor
Kevan Shokat
Masanori Okaniwa
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University of California San Diego UCSD
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University of California San Diego UCSD
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Publication of CA2960992A1 publication Critical patent/CA2960992A1/en
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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
CA2960992A 2014-09-11 2015-09-11 Mtorc1 inhibitors Active CA2960992C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462049186P 2014-09-11 2014-09-11
US62/049,186 2014-09-11
PCT/US2015/049693 WO2016040806A1 (en) 2014-09-11 2015-09-11 mTORC1 INHIBITORS

Publications (2)

Publication Number Publication Date
CA2960992A1 CA2960992A1 (en) 2016-03-17
CA2960992C true CA2960992C (en) 2024-04-09

Family

ID=55459613

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2960992A Active CA2960992C (en) 2014-09-11 2015-09-11 Mtorc1 inhibitors

Country Status (7)

Country Link
US (5) US10117945B2 (enExample)
EP (1) EP3193902A4 (enExample)
JP (3) JP6692798B2 (enExample)
CN (2) CN113620978A (enExample)
CA (1) CA2960992C (enExample)
MX (2) MX2017001981A (enExample)
WO (1) WO2016040806A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
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EP3193902A4 (en) * 2014-09-11 2018-03-28 The Regents of The University of California mTORC1 INHIBITORS
WO2016094307A1 (en) 2014-12-08 2016-06-16 The Research Foundation For The State University Of New York Anti-fungals targeting the synthesis of fungal shingolipids
WO2017044720A1 (en) * 2015-09-11 2017-03-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
EP3619216A1 (en) * 2017-05-02 2020-03-11 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
WO2018232298A1 (en) 2017-06-16 2018-12-20 The Research Foundation For The State University Of New York Anti-fungals compounds targeting the synthesis of fungal sphingolipids
CN110945129B (zh) * 2017-07-20 2024-02-02 株式会社库利金 同时抑制雄激素受体基因及哺乳动物雷帕霉素靶蛋白基因的表达的核酸
WO2019178536A1 (en) * 2018-03-16 2019-09-19 The Regents Of The University Of California Mtor inhibitors and uses thereof
IL278335B2 (en) * 2018-05-01 2024-09-01 Revolution Medicines Inc C26-linked rapamycin analogs as mtor inhibitors
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WO2020163594A1 (en) * 2019-02-07 2020-08-13 The Regents Of The University Of California Immunophilin binding agents and uses thereof
WO2020163598A1 (en) * 2019-02-07 2020-08-13 The Regents Of The University Of California Immunophilin-dependent inhibitors and uses thereof
CN110152004B (zh) * 2019-07-08 2021-09-03 天津医科大学 甘氨酸在制备药物递送增强剂及细胞移植试剂方面的用途
CA3163680A1 (en) 2019-12-05 2021-06-10 David John O'neill Rapamycin analogs and uses thereof
CN119954829A (zh) 2020-03-27 2025-05-09 艾奥维安制药公司 Mtorc1调节剂及其用途
TW202214253A (zh) 2020-06-18 2022-04-16 美商銳新醫藥公司 延遲、預防及治療對ｒａｓ抑制劑之後天抗性之方法
CN116322677B (zh) * 2020-07-21 2025-09-23 艾奥维安制药公司 Mtorc1调节剂及其用途
CN114507236A (zh) * 2022-02-28 2022-05-17 山东中医药大学 mTOR蛋白降解靶向嵌合体及其制备方法和应用
CA3256390A1 (en) 2022-05-25 2023-11-30 Revolution Medicines Inc CANCER TREATMENT METHODS USING AN MTOR INHIBITOR
CN119462690A (zh) * 2024-11-08 2025-02-18 西安交通大学 一类基于自噬-溶酶体途径的选择性mTORC1降解剂及其制备方法和应用

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US20210052735A1 (en) 2021-02-25
EP3193902A4 (en) 2018-03-28
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US10646577B2 (en) 2020-05-12
US11452780B2 (en) 2022-09-27
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US20250099597A1 (en) 2025-03-27
EP3193902A1 (en) 2017-07-26
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US10117945B2 (en) 2018-11-06
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US20240066134A1 (en) 2024-02-29
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US20190091340A1 (en) 2019-03-28
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