IL278335B2 - C26-linked rapamycin analogs as mtor inhibitors - Google Patents

C26-linked rapamycin analogs as mtor inhibitors

Info

Publication number
IL278335B2
IL278335B2 IL278335A IL27833520A IL278335B2 IL 278335 B2 IL278335 B2 IL 278335B2 IL 278335 A IL278335 A IL 278335A IL 27833520 A IL27833520 A IL 27833520A IL 278335 B2 IL278335 B2 IL 278335B2
Authority
IL
Israel
Prior art keywords
cancer
disease
example example
independently
compound
Prior art date
Application number
IL278335A
Other languages
English (en)
Hebrew (he)
Other versions
IL278335B1 (en
IL278335A (en
Original Assignee
Revolution Medicines Inc
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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of IL278335A publication Critical patent/IL278335A/en
Publication of IL278335B1 publication Critical patent/IL278335B1/en
Publication of IL278335B2 publication Critical patent/IL278335B2/en

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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
IL278335A 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors IL278335B2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862665426P 2018-05-01 2018-05-01
US201862752881P 2018-10-30 2018-10-30
US201962836040P 2019-04-18 2019-04-18
PCT/US2019/029738 WO2019212991A1 (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors

Publications (3)

Publication Number Publication Date
IL278335A IL278335A (en) 2020-12-31
IL278335B1 IL278335B1 (en) 2024-05-01
IL278335B2 true IL278335B2 (en) 2024-09-01

Family

ID=66625253

Family Applications (2)

Application Number Title Priority Date Filing Date
IL278335A IL278335B2 (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors
IL312291A IL312291A (en) 2018-05-01 2019-04-29 C-26-linked rapamycin analogs as MTOR inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL312291A IL312291A (en) 2018-05-01 2019-04-29 C-26-linked rapamycin analogs as MTOR inhibitors

Country Status (11)

Country Link
US (2) US11685749B2 (enExample)
EP (1) EP3788050B1 (enExample)
JP (1) JP7381492B2 (enExample)
KR (1) KR102859103B1 (enExample)
CN (1) CN112368289B (enExample)
AU (2) AU2019262979B2 (enExample)
CA (1) CA3098698A1 (enExample)
IL (2) IL278335B2 (enExample)
MX (2) MX2020011564A (enExample)
SG (1) SG11202010560QA (enExample)
WO (1) WO2019212991A1 (enExample)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
IL311645B2 (en) 2016-07-12 2025-11-01 Revolution Medicines Inc 2,5- disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines asallosteric shp2 inhibitors
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
BR112020007058A2 (pt) 2017-10-12 2020-10-06 Revolution Medicines, Inc. compostos de piridina, pirazina, e triazina como inibidores de shp2 alostéricos
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
PL3788049T3 (pl) 2018-05-01 2023-06-19 Revolution Medicines, Inc. Połączone z C40, C28 i C32 analogi rapamycyny jako inhibitory mTOR
EP3788050B1 (en) 2018-05-01 2024-08-28 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
US20230096028A1 (en) 2019-03-01 2023-03-30 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
MX2022005359A (es) 2019-11-04 2022-06-02 Revolution Medicines Inc Inhibidores de ras.
WO2021091956A1 (en) 2019-11-04 2021-05-14 Revolution Medicines, Inc. Ras inhibitors
CN121471132A (zh) 2019-11-04 2026-02-06 锐新医药公司 Ras抑制剂
PH12022551102A1 (en) 2019-11-08 2023-11-20 Revolution Medicines Inc Bicyclic heteroaryl compounds and uses thereof
CN114980976A (zh) 2019-11-27 2022-08-30 锐新医药公司 共价ras抑制剂及其用途
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
EP4208261A1 (en) 2020-09-03 2023-07-12 Revolution Medicines, Inc. Use of sos1 inhibitors to treat malignancies with shp2 mutations
IL301298A (en) 2020-09-15 2023-05-01 Revolution Medicines Inc Indole derivatives as RAS inhibitors in cancer therapy
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
AU2021409816A1 (en) 2020-12-22 2023-07-06 Qilu Regor Therapeutics Inc. Sos1 inhibitors and uses thereof
CN113101290B (zh) * 2021-03-23 2025-08-26 徐州医科大学 mTOR抑制剂Torin1在制备胆汁淤积性胆管损伤药物中的应用
AU2022253019A1 (en) * 2021-04-09 2023-11-16 Revolution Medicines, Inc. Synthesis of rapamycin analog compounds
IL308195A (en) 2021-05-05 2024-01-01 Revolution Medicines Inc RAS inhibitors for cancer treatment
PE20240088A1 (es) 2021-05-05 2024-01-16 Revolution Medicines Inc Inhibidores de ras
WO2022235866A1 (en) 2021-05-05 2022-11-10 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
AR127308A1 (es) 2021-10-08 2024-01-10 Revolution Medicines Inc Inhibidores ras
TW202340214A (zh) 2021-12-17 2023-10-16 美商健臻公司 做為shp2抑制劑之吡唑并吡𠯤化合物
EP4227307A1 (en) 2022-02-11 2023-08-16 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
WO2023172940A1 (en) 2022-03-08 2023-09-14 Revolution Medicines, Inc. Methods for treating immune refractory lung cancer
EP4531859A4 (en) 2022-05-25 2026-05-27 Revolution Medicines Inc CANCER TREATMENT METHODS USING AN MTOR INHIBITOR
EP4536364A1 (en) 2022-06-10 2025-04-16 Revolution Medicines, Inc. Macrocyclic ras inhibitors
US20240124450A1 (en) 2022-09-21 2024-04-18 Pfizer Inc. Novel SIK Inhibitors
CN121487738A (zh) 2023-03-30 2026-02-06 锐新医药公司 诱导ras gtp水解的组合物和其用途
CN121487951A (zh) 2023-04-07 2026-02-06 锐新医药公司 大环ras抑制剂
WO2024211712A1 (en) 2023-04-07 2024-10-10 Revolution Medicines, Inc. Condensed macrocyclic compounds as ras inhibitors
EP4695261A1 (en) 2023-04-14 2026-02-18 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
AU2024251341A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of a ras inhibitor
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
AU2024404879A1 (en) 2023-12-22 2026-06-25 Regor Pharmaceuticals, Inc. Sos1 inhibitors and uses thereof
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006116727A2 (en) * 2005-04-27 2006-11-02 Dade Rehring Inc. Compositions and methods for detection of sirolimus
WO2009089262A1 (en) * 2008-01-08 2009-07-16 Siemens Healthcare Diagnostics Inc. Stabilization of solid support assay reagents
WO2016100116A1 (en) * 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
WO2018204416A1 (en) * 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors

Family Cites Families (152)

* 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
GB1459571A (en) 1974-09-12 1976-12-22 Pfizer Ltd Thiophene-2-sulphonamide derivatives and their use as therapeutic agents sheet orienting apparatus
US4316885A (en) 1980-08-25 1982-02-23 Ayerst, Mckenna And Harrison, Inc. Acyl derivatives of rapamycin
US4513135A (en) 1982-03-05 1985-04-23 Eli Lilly And Company Diaryl-pyrazine derivatives affecting GABA binding
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
JPH0249775A (ja) 1988-05-19 1990-02-20 Nippon Soda Co Ltd ６員環又は７員環を有する複素環化合物及びその製造方法
US5120726A (en) 1991-03-08 1992-06-09 American Home Products Corporation Rapamycin hydrazones
JPH04230389A (ja) 1990-07-16 1992-08-19 American Home Prod Corp ラパマイシン誘導体
US5023264A (en) 1990-07-16 1991-06-11 American Home Products Corporation Rapamycin oximes
US5023263A (en) 1990-08-09 1991-06-11 American Home Products Corporation 42-oxorapamycin
JPH04112877A (ja) 1990-09-04 1992-04-14 Nippon Soda Co Ltd 新規シアノピラジン誘導体及びその製造方法
US5130307A (en) 1990-09-28 1992-07-14 American Home Products Corporation Aminoesters of rapamycin
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5221670A (en) 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
GB9103430D0 (en) 1991-02-19 1991-04-03 Smithkline Beecham Plc Novel compound
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US5120842A (en) 1991-04-01 1992-06-09 American Home Products Corporation Silyl ethers of rapamycin
US5100883A (en) 1991-04-08 1992-03-31 American Home Products Corporation Fluorinated esters of rapamycin
US5118678A (en) 1991-04-17 1992-06-02 American Home Products Corporation Carbamates of rapamycin
US5102876A (en) 1991-05-07 1992-04-07 American Home Products Corporation Reduction products of rapamycin
US5118677A (en) 1991-05-20 1992-06-02 American Home Products Corporation Amide esters of rapamycin
US5162333A (en) 1991-09-11 1992-11-10 American Home Products Corporation Aminodiesters of rapamycin
US5151413A (en) 1991-11-06 1992-09-29 American Home Products Corporation Rapamycin acetals as immunosuppressant and antifungal agents
GB9125660D0 (en) 1991-12-03 1992-01-29 Smithkline Beecham Plc Novel compound
US5221740A (en) 1992-01-16 1993-06-22 American Home Products Corporation Oxepane isomers of rapamycin useful as immunosuppressive agents
US5177203A (en) 1992-03-05 1993-01-05 American Home Products Corporation Rapamycin 42-sulfonates and 42-(N-carboalkoxy) sulfamates useful as immunosuppressive agents
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
MX9304868A (es) 1992-08-13 1994-05-31 American Home Prod 27-hidroxirapamicina, derivados de la misma y composicion farmaceutica que la contiene.
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5411967A (en) 1992-10-13 1995-05-02 American Home Products Corporation Carbamates of rapamycin
US5489680A (en) 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
DE69333995T2 (de) 1992-10-13 2006-10-19 Wyeth Carbamate von Rapamycin
US5480989A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5480988A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5434260A (en) 1992-10-13 1995-07-18 American Home Products Corporation Carbamates of rapamycin
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5262423A (en) 1992-10-29 1993-11-16 American Home Products Corporation Rapamycin arylcarbonyl and alkoxycarbonyl carbamates as immunosuppressive and antifungal agents
US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
US5258389A (en) 1992-11-09 1993-11-02 Merck & Co., Inc. O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives
US5260300A (en) 1992-11-19 1993-11-09 American Home Products Corporation Rapamycin carbonate esters as immuno-suppressant agents
US5252579A (en) 1993-02-16 1993-10-12 American Home Products Corporation Macrocyclic immunomodulators
US5504091A (en) 1993-04-23 1996-04-02 American Home Products Corporation Biotin esters of rapamycin
WO1994025072A1 (en) 1993-04-23 1994-11-10 American Home Products Corporation Rapamycin conjugates and antibodies
US5387680A (en) 1993-08-10 1995-02-07 American Home Products Corporation C-22 ring stabilized rapamycin derivatives
US5391730A (en) 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5378836A (en) 1993-10-08 1995-01-03 American Home Products Corporation Rapamycin oximes and hydrazones
US5373014A (en) 1993-10-08 1994-12-13 American Home Products Corporation Rapamycin oximes
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
US5385909A (en) 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
US5385908A (en) 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
US5385910A (en) 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
BR9408323A (pt) 1993-12-17 1997-08-19 Sandoz Ag Derivados de rapamicina
US5389639A (en) 1993-12-29 1995-02-14 American Home Products Company Amino alkanoic esters of rapamycin
US5362718A (en) 1994-04-18 1994-11-08 American Home Products Corporation Rapamycin hydroxyesters
US5463048A (en) 1994-06-14 1995-10-31 American Home Products Corporation Rapamycin amidino carbamates
US5491231A (en) 1994-11-28 1996-02-13 American Home Products Corporation Hindered N-oxide esters of rapamycin
US5563145A (en) 1994-12-07 1996-10-08 American Home Products Corporation Rapamycin 42-oximes and hydroxylamines
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US5741677A (en) 1995-06-07 1998-04-21 Geron Corporation Methods for measuring telomere length
DE69624921T2 (de) 1995-06-09 2003-09-11 Novartis Ag, Basel Rapamycinderivate
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
IL127559A0 (en) 1996-06-20 1999-10-28 Univ Texas Compounds and methods for providing pharmacologically active preparations and uses thereof
US6342507B1 (en) 1997-09-05 2002-01-29 Isotechnika, Inc. Deuterated rapamycin compounds, method and uses thereof
WO1999036553A2 (en) 1998-01-15 1999-07-22 Ariad Gene Therapeutics, Inc. Regulation of biological events using multimeric chimeric proteins
IL147803A0 (en) 1999-08-24 2002-08-14 Ariad Gene Therapeutics Inc 28-epirapalogs
US6277983B1 (en) 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
CN1551767A (zh) 2001-02-19 2004-12-01 ��˹��ŵ�� 癌症的治疗
EP1539736A1 (en) 2002-09-12 2005-06-15 Pharmacia & Upjohn Company LLC Substituted 1,4-pyrazine derivatives
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
US7160867B2 (en) 2003-05-16 2007-01-09 Isotechnika, Inc. Rapamycin carbohydrate derivatives
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
EP1646635A1 (en) 2003-07-16 2006-04-19 Wyeth Cci-779 isomer c
US7220755B2 (en) 2003-11-12 2007-05-22 Biosensors International Group, Ltd. 42-O-alkoxyalkyl rapamycin derivatives and compositions comprising same
EP1571151B1 (en) 2004-03-01 2008-12-24 Terumo Kabushiki Kaisha Process for production of O-alkylated rapamycin derivatives
MXPA06012333A (es) 2004-04-30 2007-01-17 Takeda Pharmaceutical Compuesto de amida heterociclico y uso del mismo como un inhibidor mmp-13.
CN100516195C (zh) 2004-07-19 2009-07-22 汕头市双骏生物科技有限公司 一种新的菌株及应用该菌株生产紫杉醇的方法
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
US20060194829A1 (en) 2004-12-20 2006-08-31 Clackson Timothy P Therapeutic materials and methods
AU2006221024A1 (en) 2005-03-07 2006-09-14 Wyeth Oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin
US8344185B2 (en) 2005-05-20 2013-01-01 SOLVAY (Société Anonyme Method for making a chlorhydrine by reaction between a polyhydroxylated aliphatic hydrocarbon and a chlorinating agent
CN101296659A (zh) 2005-10-27 2008-10-29 皇家飞利浦电子股份有限公司 使用组织加速度来创建crt(心脏再同步治疗)的更好的dit波形(多普勒组织成像)
CA2630271C (en) 2005-11-17 2014-04-08 Osi Pharmaceuticals, Inc. Fused bicyclic mtor inhibitors
PT2275103E (pt) 2005-11-21 2014-07-24 Novartis Ag Inibidores de mtor para o tratamento de tumores endócrinos
GB0525546D0 (en) 2005-12-15 2006-01-25 Novartis Ag Organic compounds
KR20150038395A (ko) 2006-04-04 2015-04-08 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 키나제 길항물질
US20090274739A1 (en) 2006-04-13 2009-11-05 The Trustees Of Columbia University In The City Of New York Methods and compositions for treating neointimal hyperplasia
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
FR2903038B1 (fr) 2006-06-29 2009-04-17 Facom Sa Support pour une serie d'outils.
JP5227321B2 (ja) 2006-08-23 2013-07-03 クドス ファーマシューティカルズ リミテッド Ｍｔｏｒ阻害剤としての２−メチルモルホリンピリド−、ピラゾ−及びピリミド−ピリミジン誘導体
EP2298772A1 (en) 2006-10-18 2011-03-23 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
EP1916006A1 (en) 2006-10-19 2008-04-30 Albert Schömig Implant coated with a wax or a resin
WO2008065887A1 (en) 2006-11-27 2008-06-05 Terumo Kabushiki Kaisha Process for producing o-alkylated rapamycin derivative, and o-alkylated rapamycin derivative
US20080234262A1 (en) 2007-03-21 2008-09-25 Wyeth Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors
WO2008124026A1 (en) 2007-04-05 2008-10-16 Wyeth Wortmannin-rapamycin conjugate and uses thereof
WO2008156174A1 (ja) 2007-06-21 2008-12-24 Taisho Pharmaceutical Co., Ltd. ピラジンアミド化合物
US20090074831A1 (en) 2007-09-18 2009-03-19 Robert Falotico LOCAL VASCULAR DELIVERY OF mTOR INHIBITORS IN COMBINATION WITH PEROXISOME PROLIFERATORS-ACTIVATED RECEPTOR STIMULATORS
WO2009046436A1 (en) 2007-10-04 2009-04-09 Memorial Sloan-Kettering Cancer Center Methods for inhibiting senescence of epithelial cells
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
BRPI0906473A8 (pt) 2008-01-04 2016-02-10 Intellikine Inc Certas entidades químicas, composições e métodos
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
US20090253733A1 (en) 2008-04-02 2009-10-08 Biointeractions, Ltd. Rapamycin carbonate esters
WO2009131631A1 (en) 2008-04-14 2009-10-29 Poniard Pharmaceuticals, Inc. Rapamycin analogs as anti-cancer agents
TW200948361A (en) 2008-05-26 2009-12-01 Chunghwa Chemical Synthesis & Biotech Co Ltd Method for synthesizing Biolimus A9 and the like and method for improving stability of the same
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
US20100055145A1 (en) 2008-08-29 2010-03-04 Biosensors International Group Stent coatings for reducing late stent thrombosis
WO2010036380A1 (en) 2008-09-26 2010-04-01 Intellikine, Inc. Heterocyclic kinase inhibitors
AU2009305669A1 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
WO2010044885A2 (en) 2008-10-17 2010-04-22 Whitehead Institute For Biomedical Research Soluble mtor complexes and modulators thereof
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
US20110269779A1 (en) 2008-11-18 2011-11-03 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
JP5789252B2 (ja) 2009-05-07 2015-10-07 インテリカイン， エルエルシー 複素環式化合物およびその使用
MX2011012584A (es) 2009-05-26 2012-02-21 Exelixis Inc Benzoxazepinas como inhibidores de pi3k/m tor, metodos para su uso y fabricación.
NZ623069A (en) 2009-08-17 2015-11-27 Sloan Kettering Inst Cancer Heat shock protein binding compounds, compositions, and methods for making and using same
UA111579C2 (uk) 2009-08-17 2016-05-25 Інтеллікіне Ллк ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
JP5951600B2 (ja) 2010-05-21 2016-07-13 インフィニティー ファーマシューティカルズ， インコーポレイテッド キナーゼ調節のための、化合物、組成物および方法
JP5985474B2 (ja) 2010-08-04 2016-09-06 メリル ライフ サイエンシズ ピーブィティ．エルティディ 抗増殖特性を有する新規４２−ｏ−（ヘテロアルコキシアルキル）ラパマイシン化合物の調製プロセス
JP5847386B2 (ja) 2010-09-15 2016-01-20 関東化學株式会社 アミン化合物の製造方法
ES2753529T3 (es) 2010-11-19 2020-04-13 Biocon Ltd Procesos para la preparación de everolimús y productos intermedios del mismo
EP2670758B1 (en) 2011-02-04 2022-09-28 Synthon BV Process for making trisubstituted silyloxyethyl triflates
TWI592411B (zh) 2011-02-23 2017-07-21 英特爾立秦有限責任公司 激酶抑制劑之組合及其用途
JP6047149B2 (ja) 2011-05-04 2016-12-21 インテリカイン， エルエルシー 併用の医薬組成物およびその使用
CA2835197A1 (en) 2011-05-06 2012-11-15 Intellikine Llc Treatment of polycystic disease
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
SG11201404432QA (en) 2012-11-30 2014-10-30 Hangzhou Zylox Pharma Co Ltd Rafamycin analogs and methods for making same
WO2015066371A1 (en) 2013-10-31 2015-05-07 Forum Pharmaceuticals, Inc. SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS
CN105813653B (zh) 2013-12-19 2020-06-26 西雅图基因公司 与目标-药物偶联物并用的亚甲基氨基甲酸酯连接物
CN105461738B (zh) 2014-06-03 2019-03-08 中国人民解放军军事医学科学院毒物药物研究所 一种雷帕霉素衍生物、其制备方法、其药物组合物及用途
KR101668590B1 (ko) 2014-06-19 2016-10-25 전남대학교병원 재협착 억제 및 재내피화 촉진을 위한 신규한 펩타이드 화합물 및 이의 제조방법
EP3193902A4 (en) 2014-09-11 2018-03-28 The Regents of The University of California mTORC1 INHIBITORS
US20160279108A1 (en) 2015-02-24 2016-09-29 University Of Kansas Targeted mtor inhibitors
CN106188093B (zh) 2015-05-08 2018-06-12 上海医药工业研究院 一种雷帕霉素结构类似物及其制备方法
US10683308B2 (en) * 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
MX382436B (es) 2016-01-11 2025-03-13 Merck Patent Gmbh Derivados de quinolin-2-ona.
CN109641858B (zh) 2016-07-21 2021-06-25 正大天晴药业集团股份有限公司 间苯二酚类衍生物的结晶、盐及其制备方法
UY37900A (es) 2017-09-26 2019-04-30 Novartis Ag Nuevos derivados de rapamicina
EP3788050B1 (en) 2018-05-01 2024-08-28 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
PL3788049T3 (pl) 2018-05-01 2023-06-19 Revolution Medicines, Inc. Połączone z C40, C28 i C32 analogi rapamycyny jako inhibitory mTOR
KR102853071B1 (ko) 2019-02-07 2025-09-02 베이진 엘티디 Tlr7 작용제로서의 이미다조[2,1-f][1,2,4]트리아진-4-아민 유도체
CN115916194A (zh) 2020-06-18 2023-04-04 锐新医药公司 用于延迟、预防和治疗针对ras抑制剂的获得性抗性的方法
AU2022253019A1 (en) 2021-04-09 2023-11-16 Revolution Medicines, Inc. Synthesis of rapamycin analog compounds
EP4531859A4 (en) 2022-05-25 2026-05-27 Revolution Medicines Inc CANCER TREATMENT METHODS USING AN MTOR INHIBITOR

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006116727A2 (en) * 2005-04-27 2006-11-02 Dade Rehring Inc. Compositions and methods for detection of sirolimus
WO2009089262A1 (en) * 2008-01-08 2009-07-16 Siemens Healthcare Diagnostics Inc. Stabilization of solid support assay reagents
WO2016100116A1 (en) * 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
WO2018204416A1 (en) * 2017-05-02 2018-11-08 Revolution Medicines, Inc. Rapamycin analogs as mtor inhibitors

Also Published As

Publication number Publication date
WO2019212991A1 (en) 2019-11-07
US20220340596A1 (en) 2022-10-27
EP3788050A1 (en) 2021-03-10
AU2019262979B2 (en) 2023-07-06
CN112368289A (zh) 2021-02-12
JP7381492B2 (ja) 2023-11-15
KR20210018243A (ko) 2021-02-17
MX2023007581A (es) 2023-07-10
US11685749B2 (en) 2023-06-27
EP3788050B1 (en) 2024-08-28
JP2021523113A (ja) 2021-09-02
AU2023241273A1 (en) 2023-10-26
US20240166667A1 (en) 2024-05-23
SG11202010560QA (en) 2020-11-27
CA3098698A1 (en) 2019-11-07
KR102859103B1 (ko) 2025-09-12
MX2020011564A (es) 2021-01-29
US12187746B2 (en) 2025-01-07
AU2019262979A1 (en) 2020-12-10
CN112368289B (zh) 2024-02-20
IL278335B1 (en) 2024-05-01
IL312291A (en) 2024-06-01
IL278335A (en) 2020-12-31

Similar Documents

Publication Publication Date Title
US12187746B2 (en) C26-linked rapamycin analogs as mTOR inhibitors
US12048749B2 (en) C40-, C28-, and C-32-linked rapamycin analogs as mTOR inhibitors
RU2826559C2 (ru) C26-СВЯЗАННЫЕ АНАЛОГИ РАПАМИЦИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR
RU2805211C2 (ru) С40-, с28- и с-32-связанные аналоги рапамицина в качестве ингибиторов mtor
HK40095848A (en) C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors