JP2021523113A5 - - Google Patents

Info

Publication number
JP2021523113A5
JP2021523113A5 JP2020561075A JP2020561075A JP2021523113A5 JP 2021523113 A5 JP2021523113 A5 JP 2021523113A5 JP 2020561075 A JP2020561075 A JP 2020561075A JP 2020561075 A JP2020561075 A JP 2020561075A JP 2021523113 A5 JP2021523113 A5 JP 2021523113A5
Authority
JP
Japan
Prior art keywords
cancers
cancer
independently
alkyl
pharmaceutically acceptable
Prior art date
Application number
JP2020561075A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2019212991A5 (https=
JP2021523113A (ja
JP7381492B2 (ja
Filing date
Publication date
Application filed filed Critical
Priority claimed from PCT/US2019/029738 external-priority patent/WO2019212991A1/en
Publication of JP2021523113A publication Critical patent/JP2021523113A/ja
Publication of JPWO2019212991A5 publication Critical patent/JPWO2019212991A5/ja
Publication of JP2021523113A5 publication Critical patent/JP2021523113A5/ja
Application granted granted Critical
Publication of JP7381492B2 publication Critical patent/JP7381492B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

JP2020561075A 2018-05-01 2019-04-29 Mtor阻害剤としてのc26-連結ラパマイシン類似体 Active JP7381492B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201862665426P 2018-05-01 2018-05-01
US62/665,426 2018-05-01
US201862752881P 2018-10-30 2018-10-30
US62/752,881 2018-10-30
US201962836040P 2019-04-18 2019-04-18
US62/836,040 2019-04-18
PCT/US2019/029738 WO2019212991A1 (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors

Publications (4)

Publication Number Publication Date
JP2021523113A JP2021523113A (ja) 2021-09-02
JPWO2019212991A5 JPWO2019212991A5 (https=) 2022-05-02
JP2021523113A5 true JP2021523113A5 (https=) 2022-05-02
JP7381492B2 JP7381492B2 (ja) 2023-11-15

Family

ID=66625253

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2020561075A Active JP7381492B2 (ja) 2018-05-01 2019-04-29 Mtor阻害剤としてのc26-連結ラパマイシン類似体

Country Status (11)

Country Link
US (2) US11685749B2 (https=)
EP (1) EP3788050B1 (https=)
JP (1) JP7381492B2 (https=)
KR (1) KR102859103B1 (https=)
CN (1) CN112368289B (https=)
AU (2) AU2019262979B2 (https=)
CA (1) CA3098698A1 (https=)
IL (2) IL312291A (https=)
MX (2) MX2020011564A (https=)
SG (1) SG11202010560QA (https=)
WO (1) WO2019212991A1 (https=)

Families Citing this family (53)

* 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
KR102598895B1 (ko) 2016-07-12 2023-11-07 레볼루션 메디슨즈, 인크. 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
MX2019008696A (es) 2017-01-23 2019-09-13 Revolution Medicines Inc Compuestos de piridina como inhibidores de shp2 alostericos.
MX2019008695A (es) 2017-01-23 2019-09-11 Revolution Medicines Inc Compuestos biciclicos como inhibidores alostericos de shp2.
MX2020003579A (es) 2017-10-12 2020-07-22 Revolution Medicines Inc Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos.
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
IL300091A (en) 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
WO2020180768A1 (en) 2019-03-01 2020-09-10 Revolution Medicines, Inc. Bicyclic heteroaryl compounds and uses thereof
CN113727758A (zh) 2019-03-01 2021-11-30 锐新医药公司 双环杂环基化合物及其用途
CN120699039A (zh) 2019-11-04 2025-09-26 锐新医药公司 Ras抑制剂
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
TW202128688A (zh) 2019-11-08 2021-08-01 美商銳新醫藥公司 雙環雜芳基化合物及其用途
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 (es) 2020-09-03 2023-05-16 Revolution Medicines Inc Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2.
MX2023003060A (es) 2020-09-15 2023-04-05 Revolution Medicines Inc Derivados indolicos como inhibidores de ras en el tratamiento del cancer.
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US20240051956A1 (en) 2020-12-22 2024-02-15 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
IL307600A (en) * 2021-04-09 2023-12-01 Revolution Medicines Inc Synthesis of rapamycin analog compounds
AU2022268962A1 (en) 2021-05-05 2023-12-14 Revolution Medicines, Inc. Ras inhibitors for the treatment of cancer
CA3217393A1 (en) 2021-05-05 2022-11-10 Elena S. Koltun Ras inhibitors
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
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
AU2023275778A1 (en) 2022-05-25 2024-12-12 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor
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
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
AU2024265078A1 (en) 2023-05-04 2025-12-11 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
IL326136A (en) 2023-08-07 2026-03-01 Revolution Medicines Inc RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
TW202542151A (zh) 2023-12-22 2025-11-01 美商銳格醫藥有限公司 Sos1抑制劑及其用途
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
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
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
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

Family Cites Families (156)

* 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
US5023264A (en) 1990-07-16 1991-06-11 American Home Products Corporation Rapamycin oximes
JPH04230389A (ja) 1990-07-16 1992-08-19 American Home Prod Corp ラパマイシン誘導体
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 (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
US5221670A (en) 1990-09-19 1993-06-22 American Home Products Corporation Rapamycin esters
PT98990A (pt) 1990-09-19 1992-08-31 American Home Prod Processo para a preparacao de esteres de acidos carboxilicos de rapamicina
US5233036A (en) 1990-10-16 1993-08-03 American Home Products Corporation Rapamycin alkoxyesters
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
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
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 (es) 1992-08-13 1994-05-31 American Home Prod 27-hidroxirapamicina, derivados de la misma y composicion farmaceutica que la contiene.
GB9221220D0 (en) 1992-10-09 1992-11-25 Sandoz Ag Organic componds
EP1266900A1 (en) 1992-10-13 2002-12-18 Wyeth Carbamates of rapamycin
US5411967A (en) 1992-10-13 1995-05-02 American Home Products Corporation Carbamates of rapamycin
US5434260A (en) 1992-10-13 1995-07-18 American Home Products Corporation Carbamates of rapamycin
US5489680A (en) 1992-10-13 1996-02-06 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
US5480988A (en) 1992-10-13 1996-01-02 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
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
US5378836A (en) 1993-10-08 1995-01-03 American Home Products Corporation Rapamycin oximes and hydrazones
US5391730A (en) 1993-10-08 1995-02-21 American Home Products Corporation Phosphorylcarbamates of rapamycin and oxime derivatives thereof
US5373014A (en) 1993-10-08 1994-12-13 American Home Products Corporation Rapamycin oximes
US5527907A (en) 1993-11-19 1996-06-18 Abbott Laboratories Macrolide immunomodulators
WO1995014023A1 (en) 1993-11-19 1995-05-26 Abbott Laboratories Semisynthetic analogs of rapamycin (macrolides) being 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
US5912253A (en) 1993-12-17 1999-06-15 Novartis Ag Rapamycin derivatives
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
EP0833828B1 (en) 1995-06-09 2002-11-20 Novartis AG Rapamycin derivatives
US5780462A (en) 1995-12-27 1998-07-14 American Home Products Corporation Water soluble rapamycin esters
HUP9904567A3 (en) 1996-06-20 2001-10-29 Univ Texas Use of azo, thioalkyl, thiocarbonyl derivatives substituted by fused heterocycles and/or phenyl group for the preparation of pharmaceutical compositions stimulating bone growth
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
PL409579A1 (pl) 2001-02-19 2015-03-02 Novartis Ag Leczenie raka
US20040116444A1 (en) 2002-09-12 2004-06-17 Corbett Jeffrey W. 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
WO2005010010A1 (en) 2003-07-16 2005-02-03 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
BRPI0510305A (pt) 2004-04-30 2007-10-02 Takeda Pharmaceutical composto ou um sal do mesmo, pródroga ou um sal da mesma, agente farmacêutico, método de produção do composto ou um sal do mesmo, inibidor de metaloproteinase de matriz ou um sal do mesmo ou uma pródroga do mesmo, método de inibir uma metaloproteinase de matriz, e, uso de um composto ou de um sal do mesmo ou de uma pródroga do mesmo
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
US7241771B2 (en) 2005-03-07 2007-07-10 Wyeth Oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin
US7189582B2 (en) * 2005-04-27 2007-03-13 Dade Behring Inc. Compositions and methods for detection of sirolimus
CA2608722A1 (en) 2005-05-20 2006-09-28 Solvay (Societe Anonyme) Method for making an epoxide starting with a polyhydroxylated aliphatic hydrocarbon and a chlorinating agent
US20080288218A1 (en) 2005-10-27 2008-11-20 Koninklijke Philips Electronics, N.V. Using Tissue Acceleration to Create Better Dti 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
RU2487711C2 (ru) 2005-11-21 2013-07-20 Новартис Аг Лечение нейроэндокринных опухолей
GB0525546D0 (en) 2005-12-15 2006-01-25 Novartis Ag Organic compounds
WO2007114926A2 (en) 2006-04-04 2007-10-11 The Regents Of The University Of California Kinase antagonists
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.
KR101438245B1 (ko) 2006-08-23 2014-09-04 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서의 2-메틸모르폴린 피리도-, 피라조- 및 피리미도-피리미딘 유도체
EP2077267A4 (en) 2006-10-18 2010-04-07 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
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
JP2010523566A (ja) 2007-04-05 2010-07-15 ワイス エルエルシー ワートマニン−ラパマイシンコンジュゲートおよびその使用
EP2157090A4 (en) 2007-06-21 2011-09-07 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
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
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
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン, エルエルシー キナーゼインヒビターおよび使用方法
US20100055145A1 (en) 2008-08-29 2010-03-04 Biosensors International Group Stent coatings for reducing late stent thrombosis
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
WO2010045542A2 (en) 2008-10-16 2010-04-22 The Regents Of The University Of California Fused ring heteroaryl kinase inhibitors
CN102256966B (zh) 2008-10-17 2016-02-10 白头生物医学研究所 可溶性mTOR复合物和其调节剂
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
WO2010059593A1 (en) 2008-11-18 2010-05-27 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
CN102459248A (zh) 2009-05-26 2012-05-16 埃克塞里艾克西斯公司 作为PI3K/mTOR抑制剂的苯并氧杂环庚三烯以及它们使用与制造方法
PE20121148A1 (es) 2009-08-17 2012-09-07 Intellikine Llc Compuestos heterociclicos y usos de los mismos
KR101906146B1 (ko) 2009-08-17 2018-10-10 메모리얼 슬로안-케터링 캔서 센터 열 충격 단백질 결합 화합물, 조성물, 및 이의 제조 방법 및 사용 방법
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
EP2601201B1 (en) 2010-08-04 2014-09-24 Meril Life Sciences Pvt. Ltd. Process for preparation of novel 42-0-(heteroalkoxyalkyl) rapamycin compounds with anti-proliferative properties"
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
WO2012066502A1 (en) 2010-11-19 2012-05-24 Biocon Limited Processes for preparation of everolimus and intermediates thereof
EP2670756B1 (en) 2011-02-04 2017-06-21 Synthon BV Process for making everolimus
US9295673B2 (en) 2011-02-23 2016-03-29 Intellikine Llc Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof
WO2012151562A1 (en) 2011-05-04 2012-11-08 Intellikine, Llc Combination pharmaceutical compositions and uses thereof
JP6122420B2 (ja) 2011-05-06 2017-04-26 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 多発性嚢胞疾患の治療
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
MX370814B (es) 2011-09-02 2020-01-08 Univ California Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas.
CA2863243A1 (en) 2012-11-30 2014-06-05 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
JP6701077B2 (ja) 2013-12-19 2020-05-27 シアトル ジェネティックス, インコーポレイテッド 標的化薬物結合体と使用するためのメチレンカルバメートリンカー
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
WO2016040806A1 (en) * 2014-09-11 2016-03-17 The Regents Of The University Of California mTORC1 INHIBITORS
WO2016100116A1 (en) * 2014-12-17 2016-06-23 Siemens Healthcare Diagnostics Inc. Sandwich assay design for small molecules
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
SG11201805869XA (en) 2016-01-11 2018-08-30 Merck Patent Gmbh Quinolin-2-one derivatives
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
CA3061907A1 (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
IL300091A (en) 2018-05-01 2023-03-01 Revolution Medicines Inc C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors
CN112368289B (zh) 2018-05-01 2024-02-20 锐新医药公司 作为mtor抑制剂的c26-连接的雷帕霉素类似物
JP7637328B2 (ja) 2019-02-07 2025-02-28 ベイジーン リミテッド Tlr7アゴニストとしてのイミダゾ[2,1-f][1,2,4]トリアジン-4-アミン誘導体
IL299131A (en) 2020-06-18 2023-02-01 Revolution Medicines Inc Methods for delaying, preventing and treating acquired resistance to RAS inhibitors
IL307600A (en) 2021-04-09 2023-12-01 Revolution Medicines Inc Synthesis of rapamycin analog compounds
AU2023275778A1 (en) 2022-05-25 2024-12-12 Revolution Medicines, Inc. Methods of treating cancer with an mtor inhibitor

Similar Documents

Publication Publication Date Title
JP2021523113A5 (https=)
JPWO2019212991A5 (https=)
IL278334B2 (en) c40-, c28-, and c-32-linked rapamycin analogs as mTOR inhibitors
JP2021523112A5 (https=)
JPWO2019212990A5 (https=)
JP2021508686A5 (https=)
JP2018510850A5 (https=)
JP2009513703A5 (https=)
JP2019094345A5 (https=)
RU2004130440A (ru) Производные 4-(имидазол-5-ил)-2-(4-сульфоанилино)пиримидина, обладающие ингибирующим действием по отношению к cdk
JP2020517616A5 (https=)
JP6837479B2 (ja) 医薬化合物
JPWO2019232419A5 (https=)
JP2008526888A5 (https=)
JP2010510237A5 (https=)
WO2007049532A1 (ja) アミノジヒドロチアジン誘導体
JP2020506884A5 (https=)
JP2017500295A5 (https=)
JP2011520954A (ja) フェニルまたはピリジニル置換インダゾール誘導体
JP2018515623A5 (https=)
JP2020502047A5 (https=)
JP2015508092A5 (https=)
RU2004139099A (ru) 1-(аминоалкил)-3-сульфонилиндольные и -индазольные производные в качестве лигандов 5-гидрокситриптамина-6
CN111511736B (zh) 含氮6元环化合物
JP2017531680A (ja) 三環式アトロプ異性体の化合物