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

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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
CA3061907A1 (en) * 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors
EP3638649A4 (en) 2017-06-16 2021-03-17 The Research Foundation for The State University of New York Anti-fungals compounds targeting the synthesis of fungal sphingolipids
JP6944584B2 (ja) * 2017-07-20 2021-10-06 キュリジン カンパニー，リミテッド ＡＲ遺伝子及びｍＴＯＲ遺伝子の発現を同時に抑制する核酸
WO2019178536A1 (en) * 2018-03-16 2019-09-19 The Regents Of The University Of California Mtor inhibitors and uses thereof
AU2019262978B2 (en) 2018-05-01 2023-07-13 Revolution Medicines, Inc. C40-, C28-, and C-32-linked rapamycin analogs as mTOR inhibitors
MX2020011564A (es) * 2018-05-01 2021-01-29 Revolution Medicines Inc Analogos de rapamicina unidos a c26 como inhibidores de mtor.
CN108676882B (zh) * 2018-05-30 2022-02-22 中山大学肿瘤防治中心（中山大学附属肿瘤医院、中山大学肿瘤研究所） NOP14基因及其蛋白作为肿瘤对mTOR抑制剂敏感性的标志物的应用
PL3813946T3 (pl) 2018-06-15 2024-09-02 Janssen Pharmaceutica Nv Analogi rapamycyny i ich zastosowania
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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
KR20220128345A (ko) 2019-12-05 2022-09-20 아나쿠리아 테라퓨틱스, 인코포레이티드 라파마이신 유사체 및 이의 용도
JP7606591B2 (ja) 2020-03-27 2024-12-25 エオビアン ファーマシューティカルズ， インコーポレイテッド Ｍｔｏｒｃ１モジュレーターおよびその使用
BR112022025550A2 (pt) 2020-06-18 2023-03-07 Revolution Medicines Inc Métodos para retardar, prevenir e tratar resistência adquirida aos inibidores de ras
WO2022020522A2 (en) * 2020-07-21 2022-01-27 Aeovian Pharmaceuticals, Inc. Mtorc1 modulators and uses thereof
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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US12097262B2 (en) 2024-09-24
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