CA3098698A1 - C26-linked rapamycin analogs as mtor inhibitors - Google Patents
C26-linked rapamycin analogs as mtor inhibitors Download PDFInfo
- Publication number
- CA3098698A1 CA3098698A1 CA3098698A CA3098698A CA3098698A1 CA 3098698 A1 CA3098698 A1 CA 3098698A1 CA 3098698 A CA3098698 A CA 3098698A CA 3098698 A CA3098698 A CA 3098698A CA 3098698 A1 CA3098698 A1 CA 3098698A1
- Authority
- CA
- Canada
- Prior art keywords
- ome
- compound
- pharmaceutically acceptable
- cancer
- acceptable salt
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3098698A1 true CA3098698A1 (en) | 2019-11-07 |
Family
ID=66625253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3098698A Pending CA3098698A1 (en) | 2018-05-01 | 2019-04-29 | C26-linked rapamycin analogs as mtor inhibitors |
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)
| 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)
| 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 |
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| JP7381492B2 (ja) | 2023-11-15 |
| IL278335A (en) | 2020-12-31 |
| US20240166667A1 (en) | 2024-05-23 |
| SG11202010560QA (en) | 2020-11-27 |
| KR102859103B1 (ko) | 2025-09-12 |
| CN112368289A (zh) | 2021-02-12 |
| MX2023007581A (es) | 2023-07-10 |
| WO2019212991A1 (en) | 2019-11-07 |
| US11685749B2 (en) | 2023-06-27 |
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