SG11202010560QA - C26-linked rapamycin analogs as mtor inhibitors - Google Patents

C26-linked rapamycin analogs as mtor inhibitors

Info

Publication number
SG11202010560QA
SG11202010560QA SG11202010560QA SG11202010560QA SG11202010560QA SG 11202010560Q A SG11202010560Q A SG 11202010560QA SG 11202010560Q A SG11202010560Q A SG 11202010560QA SG 11202010560Q A SG11202010560Q A SG 11202010560QA SG 11202010560Q A SG11202010560Q A SG 11202010560QA
Authority
SG
Singapore
Prior art keywords
mtor inhibitors
rapamycin analogs
linked rapamycin
linked
analogs
Prior art date
Application number
SG11202010560QA
Inventor
Christopher Michael Semko
Gang Wang
G Leslie Burnett
James Bradley Aggen
Gert Kiss
James Joseph Cregg
Micah James Evans Gliedt
Jennifer Pitzen
Julie Chu-Li Lee
Walter Won
Arun P Thottumkara
Adrian Liam Gill
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 SG11202010560QA publication Critical patent/SG11202010560QA/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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
SG11202010560QA 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors SG11202010560QA (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 (1)

Publication Number Publication Date
SG11202010560QA true SG11202010560QA (en) 2020-11-27

Family

ID=66625253

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11202010560QA SG11202010560QA (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors

Country Status (11)

Country Link
US (2) US11685749B2 (en)
EP (1) EP3788050A1 (en)
JP (1) JP7381492B2 (en)
KR (1) KR20210018243A (en)
CN (1) CN112368289B (en)
AU (2) AU2019262979B2 (en)
CA (1) CA3098698A1 (en)
IL (2) IL278335B1 (en)
MX (2) MX2020011564A (en)
SG (1) SG11202010560QA (en)
WO (1) WO2019212991A1 (en)

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3484856B1 (en) 2016-07-12 2023-11-15 Revolution Medicines, Inc. 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
EP3571199A1 (en) 2017-01-23 2019-11-27 Revolution Medicines, Inc. Bicyclic compounds as allosteric shp2 inhibitors
BR112019014527A2 (en) 2017-01-23 2020-02-27 Revolution Medicines, Inc. PYRIDINE COMPOUNDS AS ALLOSTIC SHP2 INHIBITORS
AU2018347516A1 (en) 2017-10-12 2020-05-07 Revolution Medicines, Inc. Pyridine, pyrazine, and triazine compounds as allosteric SHP2 inhibitors
MX2020006273A (en) 2017-12-15 2020-09-14 Revolution Medicines Inc Polycyclic compounds as allosteric shp2 inhibitors.
EP3788050A1 (en) 2018-05-01 2021-03-10 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
IL300091A (en) 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
EP3931195A1 (en) 2019-03-01 2022-01-05 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
AU2020232616A1 (en) 2019-03-01 2021-09-09 Revolution Medicines, Inc. Bicyclic heterocyclyl compounds and uses thereof
CN115873020A (en) 2019-11-04 2023-03-31 锐新医药公司 RAS inhibitors
CN114867735A (en) 2019-11-04 2022-08-05 锐新医药公司 RAS inhibitors
EP4054719A1 (en) 2019-11-04 2022-09-14 Revolution Medicines, Inc. Ras inhibitors
KR20220100903A (en) 2019-11-08 2022-07-18 레볼루션 메디슨즈, 인크. Bicyclic heteroaryl compounds and uses thereof
EP4065231A1 (en) 2019-11-27 2022-10-05 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing, and treating acquired resistance to ras inhibitors
MX2023002248A (en) 2020-09-03 2023-05-16 Revolution Medicines Inc Use of sos1 inhibitors to treat malignancies with shp2 mutations.
PE20231207A1 (en) 2020-09-15 2023-08-17 Revolution Medicines Inc INDOLIC DERIVATIVES AS RAS INHIBITORS IN CANCER TREATMENT
CN117396472A (en) 2020-12-22 2024-01-12 上海齐鲁锐格医药研发有限公司 SOS1 inhibitors and uses thereof
CN113101290A (en) * 2021-03-23 2021-07-13 徐州医科大学 Application of mTOR inhibitor Torin1 in preparation of cholestatic bile duct injury drug
IL307600A (en) * 2021-04-09 2023-12-01 Revolution Medicines Inc Synthesis of rapamycin analog compounds
EP4334324A1 (en) 2021-05-05 2024-03-13 Revolution Medicines, Inc. Covalent ras inhibitors and uses thereof
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
AR125782A1 (en) 2021-05-05 2023-08-16 Revolution Medicines Inc RAS INHIBITORS
AR127308A1 (en) 2021-10-08 2024-01-10 Revolution Medicines Inc RAS INHIBITORS
WO2023114954A1 (en) 2021-12-17 2023-06-22 Genzyme Corporation Pyrazolopyrazine compounds as shp2 inhibitors
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
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
US20240124450A1 (en) 2022-09-21 2024-04-18 Pfizer Inc. Novel SIK Inhibitors

Family Cites Families (147)

* 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 (en) 1985-10-03 1988-12-02 Merck Sharp & Dohme LIQUID-GEL PHASE TRANSITION PHARMACEUTICAL COMPOSITION
US4650803A (en) 1985-12-06 1987-03-17 University Of Kansas Prodrugs of rapamycin
JPH0249775A (en) 1988-05-19 1990-02-20 Nippon Soda Co Ltd Heterocyclic compound having 6-membered or 7-membered ring and production thereof
JPH04230389A (en) 1990-07-16 1992-08-19 American Home Prod Corp Rapamycin derivative
US5023264A (en) 1990-07-16 1991-06-11 American Home Products Corporation Rapamycin oximes
US5120726A (en) 1991-03-08 1992-06-09 American Home Products Corporation Rapamycin hydrazones
US5023263A (en) 1990-08-09 1991-06-11 American Home Products Corporation 42-oxorapamycin
JPH04112877A (en) 1990-09-04 1992-04-14 Nippon Soda Co Ltd New cyanopyrazine derivative and production thereof
PT98990A (en) 1990-09-19 1992-08-31 American Home Prod PROCESS FOR THE PREPARATION OF CARBOXYLIC ACID ESTERS OF RAPAMICIN
US5221670A (en) 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
US5130307A (en) 1990-09-28 1992-07-14 American Home Products Corporation Aminoesters of rapamycin
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
JP2594486B2 (en) 1991-01-15 1997-03-26 アルコン ラボラトリーズ インコーポレイテッド Topical ophthalmic composition
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
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
ZA935112B (en) 1992-07-17 1994-02-08 Smithkline Beecham Corp Rapamycin derivatives
ZA935111B (en) 1992-07-17 1994-02-04 Smithkline Beecham Corp Rapamycin derivatives
US5256790A (en) 1992-08-13 1993-10-26 American Home Products Corporation 27-hydroxyrapamycin and derivatives thereof
MX9304868A (en) 1992-08-13 1994-05-31 American Home Prod 27-HYDROXYRAPAMICINE, DERIVED FROM THE SAME AND PHARMACEUTICAL COMPOSITION THAT CONTAINS IT.
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5489680A (en) 1992-10-13 1996-02-06 American Home Products Corporation Carbamates of rapamycin
US5480988A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5480989A (en) 1992-10-13 1996-01-02 American Home Products Corporation Carbamates of rapamycin
US5302584A (en) 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
US5411967A (en) 1992-10-13 1995-05-02 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
AU6711994A (en) 1993-04-23 1994-11-21 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
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
US5391730A (en) 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
EP0729471A1 (en) 1993-11-19 1996-09-04 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being immunomodulators
US5385908A (en) 1993-11-22 1995-01-31 American Home Products Corporation Hindered esters of rapamycin
US5385909A (en) 1993-11-22 1995-01-31 American Home Products Corporation Heterocyclic esters of rapamycin
US5385910A (en) 1993-11-22 1995-01-31 American Home Products Corporation Gem-distributed esters of rapamycin
ATE191218T1 (en) 1993-12-17 2000-04-15 Novartis Ag RAPAMYCIN DERIVATIVES AS IMMUNOSUPPRESSORS
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
CA2219659C (en) 1995-06-09 2008-03-18 Novartis Ag Rapamycin derivatives
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
KR20000022040A (en) 1996-06-20 2000-04-25 보오드 오브 리젠츠, 더 유니버시티 오브 텍사스 시스템 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
CA2318402A1 (en) 1998-01-15 1999-07-22 Ariad Gene Therapeutics, Inc. Regulation of biological events using multimeric chimeric proteins
AU783158B2 (en) 1999-08-24 2005-09-29 Ariad Pharmaceuticals, Inc. 28-epirapalogs
US6277983B1 (en) 2000-09-27 2001-08-21 American Home Products Corporation Regioselective synthesis of rapamycin derivatives
CZ307637B6 (en) 2001-02-19 2019-01-23 Novartis Ag 40-O- (2-Hydroxyethyl) rapamycin as the only active ingredient in the treatment
MXPA05002418A (en) 2002-09-12 2005-05-27 Pharmacia & Upjohn Co Llc Substituted 1,4-pyrazine derivatives.
JP2004161716A (en) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Jnk inhibitor
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
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
ZA200609259B (en) 2004-04-30 2008-07-30 Takeda Pharmaceutical Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
CN100516195C (en) 2004-07-19 2009-07-22 汕头市双骏生物科技有限公司 New strain and method of producing pacilitaxel using said strain
EP1831225A2 (en) 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
BRPI0608885A2 (en) 2005-03-07 2017-02-21 Wyeth Corp sdz-rad isomer c compound, pharmaceutical composition, and pharmaceutical packaging
US7189582B2 (en) * 2005-04-27 2007-03-13 Dade Behring Inc. Compositions and methods for detection of sirolimus
TWI320036B (en) 2005-05-20 2010-02-01 Process for preparing a chlorohydrin starting from a polyhydroxylated aliphatic hydrocarbon
WO2007049228A1 (en) 2005-10-27 2007-05-03 Koninklijke Philips Electronics, N.V. Using tissue acceleration to create better dit waveforms (doppler tissue imaging) for crt (cardiac resynchronization therapy)
EP2385053B1 (en) 2005-11-17 2013-10-02 OSI Pharmaceuticals, Inc. Intermediates for the preparation of fused bicyclic mTOR inhibitors
AU2006314444C1 (en) 2005-11-21 2018-01-04 Novartis Ag Neuroendocrine tumor treatment using mTOR inhibitors
GB0525546D0 (en) 2005-12-15 2006-01-25 Novartis Ag Organic compounds
EA200870409A1 (en) 2006-04-04 2009-04-28 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния ANTAGONISTS OF KINASE PI3
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 (en) 2006-06-29 2009-04-17 Facom Sa SUPPORT FOR A SERIES OF TOOLS.
SI2057156T1 (en) 2006-08-23 2017-06-30 Kudos Pharmaceuticals Limited 2-methylmorpholine pyrido-,pyrazo- and pyrimido-pyrimidine derivatives as mtor inhibitors
US8492405B2 (en) 2006-10-18 2013-07-23 Takeda Pharmaceutical Company Limited Glucokinase-activating fused heterocyclic compounds and methods of treating diabetes and obesity
EP1916006A1 (en) 2006-10-19 2008-04-30 Albert Schömig Implant coated with a wax or a resin
JP5456321B2 (en) 2006-11-27 2014-03-26 テルモ株式会社 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
CA2678415A1 (en) 2007-04-05 2008-10-16 Wyeth Wortmannin-rapamycin conjugate and uses thereof
US20100190980A1 (en) 2007-06-21 2010-07-29 Taisho Pharmaceutical Co., Ltd Pyrazinamide compound
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
MX2010007418A (en) 2008-01-04 2010-11-12 Intellikine Inc Certain chemical entities, compositions and methods.
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
US7842475B2 (en) * 2008-01-08 2010-11-30 Siemens Healthcare Diagnostics Inc. Stabilization of solid support assay reagents
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
US20110098241A1 (en) 2008-04-14 2011-04-28 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
BRPI0915231A2 (en) 2008-07-08 2018-06-12 Intellikine Inc kinase inhibitor compounds and methods of use
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
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
DK2358720T3 (en) 2008-10-16 2016-06-06 Univ California Heteroarylkinaseinhibitorer fused-ring
EP2350053B1 (en) 2008-10-17 2013-12-11 Whitehead Institute For Biomedical Research Modulators of MTOR Complexes
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
US8476282B2 (en) 2008-11-03 2013-07-02 Intellikine Llc Benzoxazole kinase inhibitors and methods of use
WO2010059593A1 (en) 2008-11-18 2010-05-27 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
CA2763008A1 (en) 2009-05-26 2010-12-02 Exelixis, Inc. Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
MX353747B (en) 2009-08-17 2018-01-26 Memorial Sloan Kettering Cancer Center Star Heat shock protein binding compounds, compositions, and methods for making and using same.
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
US9321782B2 (en) 2010-08-04 2016-04-26 Meril Life Sciences Pvt. Ltd. Process for preparation of novel 42-O-(heteroalkoxyalkyl) rapamicin compounds with anti-proliferative properties
JP5847386B2 (en) 2010-09-15 2016-01-20 関東化學株式会社 Method for producing amine compound
ES2753529T3 (en) 2010-11-19 2020-04-13 Biocon Ltd Processes for the preparation of everolimus and intermediate products thereof
EP4230631A3 (en) 2011-02-04 2024-03-27 Synthon B.V. Process for making trisubstituted silyloxyethyl triflates
AR085397A1 (en) 2011-02-23 2013-09-25 Intellikine Inc COMBINATION OF QUINASA INHIBITORS AND THEIR USES
CN103703174B (en) 2011-05-04 2017-05-10 因特利凯有限责任公司 Combination pharmaceutical compositions and uses thereof
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
AU2012341028C1 (en) 2011-09-02 2017-10-19 Mount Sinai School Of Medicine Substituted pyrazolo[3,4-D]pyrimidines and uses thereof
CN104854112A (en) 2012-11-30 2015-08-19 杭州归创生物医药有限公司 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
IL290330B2 (en) 2013-12-19 2023-09-01 Seagen Inc Methylene carbamate linkers for use with targeted-drug conjugates
CN105461738B (en) 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 A kind of rapamycin derivative, preparation method, its pharmaceutical composition and purposes
KR101668590B1 (en) 2014-06-19 2016-10-25 전남대학교병원 Bioactive Peptide-coated Stent Promotes Endothelial Cell Proliferation and Prevents Stent Thrombosis
JP6692798B2 (en) 2014-09-11 2020-05-13 ザ・リージエンツ・オブ・ザ・ユニバーシテイ・オブ・カリフオルニア mTORC1 inhibitor
US20170362305A1 (en) * 2014-12-17 2017-12-21 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
US20160279108A1 (en) 2015-02-24 2016-09-29 University Of Kansas Targeted mtor inhibitors
US10683308B2 (en) * 2015-09-11 2020-06-16 Navitor Pharmaceuticals, Inc. Rapamycin analogs and uses thereof
CA3010890C (en) 2016-01-11 2023-09-26 Merck Patent Gmbh Quinolin-2-one derivatives
CN109641858B (en) 2016-07-21 2021-06-25 正大天晴药业集团股份有限公司 Crystals and salts of resorcin derivatives and process for producing the same
AU2018263886C1 (en) 2017-05-02 2022-12-22 Revolution Medicines, Inc. Rapamycin analogs as mTOR inhibitors
UY37900A (en) 2017-09-26 2019-04-30 Novartis Ag NEW DERIVATIVES OF RAPAMYCIN
IL300091A (en) 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
EP3788050A1 (en) 2018-05-01 2021-03-10 Revolution Medicines, Inc. C26-linked rapamycin analogs as mtor inhibitors
AU2020218383A1 (en) 2019-02-07 2021-09-02 Beigene, Ltd. Imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivatives as TLR7 agonist

Also Published As

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

Similar Documents

Publication Publication Date Title
IL278335A (en) C26-linked rapamycin analogs as mtor inhibitors
SG11202010559UA (en) C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
IL268030B (en) Bicyclic compounds as allosteric shp2 inhibitors
IL275365A (en) 6-azaindole compounds
IL289474A (en) Substituted thiazolo-pyridine compounds as malt1 inhibitors
IL275344B1 (en) 4-azaindole compounds
EP3341381A4 (en) RAPAMYCIN ANALOGS SHOWING IMPROVED mTORC1 SPECIFICITY
SI3687999T1 (en) Rapamycin derivatives
IL275532A (en) Mtor inhibitor compounds
IL279329A (en) Rapamycin analogs and uses thereof
IL287717A (en) Substituted pyrrolopyridines as jak inhibitors
IL289252A (en) Ep2 antagonist
HK1253576A1 (en) Pyrropyrimidine compounds as mnks inhibitors
EP3730935A4 (en) Method for detecting trifluridine- and/or tipiracil-derived analogs
IL275531A (en) Mtor inhibitor compounds
LT3589637T (en) Compounds useful for inhibiting ror-gamma-t
HUE054483T2 (en) Compounds useful for inhibiting ror-gamma-t
IL264465B (en) Substituted thiazolo-pyridine compounds as malt1 inhibitors
IL269414A (en) Rapar for safetyin taneis
GB201812604D0 (en) Antagonist compounds