JP7381492B2 - Mtor阻害剤としてのc26-連結ラパマイシン類似体 - Google Patents
Mtor阻害剤としてのc26-連結ラパマイシン類似体 Download PDFInfo
- Publication number
- JP7381492B2 JP7381492B2 JP2020561075A JP2020561075A JP7381492B2 JP 7381492 B2 JP7381492 B2 JP 7381492B2 JP 2020561075 A JP2020561075 A JP 2020561075A JP 2020561075 A JP2020561075 A JP 2020561075A JP 7381492 B2 JP7381492 B2 JP 7381492B2
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- disease
- independently
- alkyl
- pharmaceutically acceptable
- 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.)
- Active
Links
Classifications
-
- 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
-
- 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
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)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2021523113A JP2021523113A (ja) | 2021-09-02 |
| JP2021523113A5 JP2021523113A5 (enExample) | 2022-05-02 |
| JP7381492B2 true 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 (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) | IL312291A (enExample) |
| MX (2) | MX2020011564A (enExample) |
| SG (1) | SG11202010560QA (enExample) |
| WO (1) | WO2019212991A1 (enExample) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA44075A (fr) | 2015-12-17 | 2021-05-19 | Incyte Corp | Dérivés de n-phényl-pyridine-2-carboxamide et leur utilisation en tant que modulateurs des interactions protéine/protéine pd-1/pd-l1 |
| EP4302834A3 (en) | 2016-07-12 | 2024-07-17 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| US20180179202A1 (en) | 2016-12-22 | 2018-06-28 | Incyte Corporation | Heterocyclic compounds as immunomodulators |
| KR20190110588A (ko) | 2017-01-23 | 2019-09-30 | 레볼루션 메디슨즈, 인크. | 알로스테릭 shp2 억제제로서의 피리딘 화합물 |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ,インコーポレイテッド | アロステリックshp2阻害剤としての二環式化合物 |
| TW201930292A (zh) | 2017-10-12 | 2019-08-01 | 美商銳新醫藥公司 | 作為變構shp2抑制劑的吡啶、吡嗪和三嗪化合物 |
| JP7361693B2 (ja) | 2017-12-15 | 2023-10-16 | レヴォリューション・メディスンズ,インコーポレイテッド | アロステリックshp2阻害剤としての多環式化合物 |
| MX2020011565A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor. |
| IL312291A (en) | 2018-05-01 | 2024-06-01 | Revolution Medicines Inc | C-26-linked rapamycin analogs as MTOR inhibitors |
| MX2021010323A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos bicíclicos de heterociclilo y usos de este. |
| MX2021010319A (es) | 2019-03-01 | 2021-12-10 | Revolution Medicines Inc | Compuestos biciclicos de heteroarilo y usos de estos. |
| AU2020377925A1 (en) | 2019-11-04 | 2022-05-05 | Revolution Medicines, Inc. | Ras inhibitors |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
| TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| CA3156359A1 (en) | 2019-11-08 | 2021-05-14 | Adrian Liam Gill | 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 |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| CR20230230A (es) | 2020-11-06 | 2023-07-27 | Incyte Corp | Proceso para hacer un inhibidor de pd-1/pdl1 y sales y formas cristalinas del mismo |
| JP7849366B2 (ja) | 2020-12-22 | 2026-04-21 | キル・レガー・セラピューティクス・インコーポレーテッド | Sos1阻害剤およびその使用 |
| 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 |
| CA3214664A1 (en) * | 2021-04-09 | 2022-10-13 | Steven G. Ballmer | Synthesis of rapamycin analog compounds |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| JP2024516450A (ja) | 2021-05-05 | 2024-04-15 | レボリューション メディシンズ インコーポレイテッド | 共有結合性ras阻害剤及びその使用 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| CN119212994A (zh) | 2021-12-17 | 2024-12-27 | 建新公司 | 作为shp2抑制剂的吡唑并吡嗪化合物 |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| CA3256390A1 (en) | 2022-05-25 | 2023-11-30 | Revolution Medicines, Inc. | CANCER TREATMENT METHODS USING 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 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| CN121464140A (zh) | 2023-04-14 | 2026-02-03 | 锐新医药公司 | Ras抑制剂的结晶形式、含有其的组合物及其使用方法 |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ras相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic 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 |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ras抑制劑 |
| WO2025255438A1 (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 |
| WO2026015790A1 (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 |
| WO2026015796A1 (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 |
Citations (5)
| 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 |
| WO2017044720A1 (en) | 2015-09-11 | 2017-03-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| JP2017531624A (ja) | 2014-09-11 | 2017-10-26 | 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阻害剤 |
Family Cites Families (151)
| 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 |
| 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 |
| 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 (ja) | 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 | 局所的眼薬組成物 |
| 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 |
| 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 |
| US5302584A (en) | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| 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 |
| SG47580A1 (en) | 1992-10-13 | 1998-04-17 | American Home Prod | Carbamates of rapamycin |
| US5480989A (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 |
| 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 |
| CA2175215C (en) | 1993-11-19 | 2008-06-03 | Yat Sun Or | 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 |
| SK78196A3 (en) | 1993-12-17 | 1997-02-05 | Sandoz Ag | Rapamycin demethoxy-derivatives, preparation method thereof and pharmaceutical agent containing them |
| 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 |
| US5985890A (en) | 1995-06-09 | 1999-11-16 | Novartis Ag | Rapamycin derivatives |
| US5780462A (en) | 1995-12-27 | 1998-07-14 | American Home Products Corporation | Water soluble rapamycin esters |
| WO1997048694A1 (en) | 1996-06-20 | 1997-12-24 | Board Of Regents, The University Of Texas System | 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 |
| JP2002508971A (ja) | 1998-01-15 | 2002-03-26 | アリアド・ジーン・セラピューティクス・インコーポレーテッド | 多量体キメラ蛋白質を使用する生物学的イベントの調節 |
| ATE264863T1 (de) | 1999-08-24 | 2004-05-15 | Ariad Gene Therapeutics Inc | 28-epirapaloge |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| MX368013B (es) | 2001-02-19 | 2019-09-13 | Novartis Ag | Tratamiento de cáncer. |
| 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 |
| 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 |
| ATE418559T1 (de) | 2004-03-01 | 2009-01-15 | Terumo Corp | Verfahren zur herstellung von o-alkylierten rapamycinderivaten |
| ZA200609259B (en) | 2004-04-30 | 2008-07-30 | Takeda Pharmaceutical | Heterocyclic amide compound and use thereof as an mmp-13 inhibitor |
| 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 |
| EP1831225A2 (en) | 2004-11-19 | 2007-09-12 | The Regents of the University of California | Anti-inflammatory pyrazolopyrimidines |
| EP1838288A4 (en) | 2004-12-20 | 2010-08-04 | Ariad Pharma Inc | THERAPEUTIC MATERIALS AND METHODS |
| CA2602010A1 (en) | 2005-03-07 | 2006-09-14 | Wyeth | Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin |
| EA013681B1 (ru) | 2005-05-20 | 2010-06-30 | Солвей (Сосьете Аноним) | Способ получения дихлорпропанола, способ получения эпихлоргидрина и способ получения эпоксидных смол |
| 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) |
| ES2365869T3 (es) | 2005-11-17 | 2011-10-11 | OSI Pharmaceuticals, LLC | COMPUESTOS BICÍCLICOS FUSIONADOS INHIBIDORES DE LA mTOR. |
| NO20220050A1 (no) | 2005-11-21 | 2008-08-12 | Novartis Ag | Neuroendokrin tumorbehandling |
| 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. |
| CA2659851C (en) | 2006-08-23 | 2014-02-25 | 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 |
| EP2090580B1 (en) | 2006-11-27 | 2014-06-04 | 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 |
| MX2009010683A (es) | 2007-04-05 | 2010-01-20 | Wyeth Corp | Conjugado de wortmanina-rapamicina y usos del mismo. |
| 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 |
| MX2010007419A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| 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 (pt) | 2008-07-08 | 2018-06-12 | Intellikine Inc | compostos inibidores de quinase e métodos de uso |
| 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 |
| CA2738429C (en) | 2008-09-26 | 2016-10-25 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| EP2358720B1 (en) | 2008-10-16 | 2016-03-02 | The Regents of The University of California | Fused ring heteroaryl kinase inhibitors |
| 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 |
| 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 |
| 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 |
| 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 |
| NZ598220A (en) | 2009-08-17 | 2014-02-28 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| NZ713361A (en) | 2009-08-17 | 2017-06-30 | Memorial Sloan Kettering Cancer Center | Heat shock protein binding compounds, compositions, and methods for making and using same |
| WO2011047384A2 (en) | 2009-10-16 | 2011-04-21 | 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 |
| WO2012017449A1 (en) | 2010-08-04 | 2012-02-09 | 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 |
| 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 |
| US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
| 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 |
| 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 |
| CA2846496C (en) | 2011-09-02 | 2020-07-14 | 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 |
| KR102442906B1 (ko) | 2013-12-19 | 2022-09-14 | 씨젠 인크. | 표적화된-약물 컨쥬게이트와 함께 사용되는 메틸렌 카바메이트 링커 |
| 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 |
| 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 |
| MX382436B (es) | 2016-01-11 | 2025-03-13 | Merck Patent Gmbh | Derivados de quinolin-2-ona. |
| US10851071B2 (en) | 2016-07-21 | 2020-12-01 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | M-dihydroxybenzene derivative crystal and salt, and manufacturing method thereof |
| WO2018204416A1 (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 |
| IL312291A (en) | 2018-05-01 | 2024-06-01 | Revolution Medicines Inc | C-26-linked rapamycin analogs as MTOR inhibitors |
| MX2020011565A (es) | 2018-05-01 | 2021-01-29 | Revolution Medicines Inc | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor. |
| MX2021009439A (es) | 2019-02-07 | 2021-11-12 | Beigene Ltd | Derivados de imidazo [2,1-f] [1,2,4] triazin-4-amina como agonista de tlr7. |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| CA3214664A1 (en) | 2021-04-09 | 2022-10-13 | Steven G. Ballmer | Synthesis of rapamycin analog compounds |
| CA3256390A1 (en) | 2022-05-25 | 2023-11-30 | Revolution Medicines, Inc. | CANCER TREATMENT METHODS USING AN MTOR INHIBITOR |
-
2019
- 2019-04-29 IL IL312291A patent/IL312291A/en unknown
- 2019-04-29 MX MX2020011564A patent/MX2020011564A/es unknown
- 2019-04-29 WO PCT/US2019/029738 patent/WO2019212991A1/en not_active Ceased
- 2019-04-29 EP EP19725444.4A patent/EP3788050B1/en active Active
- 2019-04-29 AU AU2019262979A patent/AU2019262979B2/en active Active
- 2019-04-29 SG SG11202010560QA patent/SG11202010560QA/en unknown
- 2019-04-29 IL IL278335A patent/IL278335B2/en unknown
- 2019-04-29 KR KR1020207034116A patent/KR102859103B1/ko active Active
- 2019-04-29 CN CN201980042858.5A patent/CN112368289B/zh active Active
- 2019-04-29 CA CA3098698A patent/CA3098698A1/en active Pending
- 2019-04-29 JP JP2020561075A patent/JP7381492B2/ja active Active
-
2020
- 2020-10-30 US US17/086,169 patent/US11685749B2/en active Active
- 2020-10-30 MX MX2023007581A patent/MX2023007581A/es unknown
-
2023
- 2023-04-10 US US18/298,313 patent/US12187746B2/en active Active
- 2023-10-03 AU AU2023241273A patent/AU2023241273A1/en not_active Abandoned
Patent Citations (5)
| 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 |
| JP2017531624A (ja) | 2014-09-11 | 2017-10-26 | 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阻害剤 |
| WO2016100116A1 (en) | 2014-12-17 | 2016-06-23 | Siemens Healthcare Diagnostics Inc. | Sandwich assay design for small molecules |
| WO2017044720A1 (en) | 2015-09-11 | 2017-03-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019262979B2 (en) | 2023-07-06 |
| MX2023007581A (es) | 2023-07-10 |
| AU2023241273A1 (en) | 2023-10-26 |
| WO2019212991A1 (en) | 2019-11-07 |
| EP3788050A1 (en) | 2021-03-10 |
| IL278335B2 (en) | 2024-09-01 |
| US20220340596A1 (en) | 2022-10-27 |
| JP2021523113A (ja) | 2021-09-02 |
| US12187746B2 (en) | 2025-01-07 |
| SG11202010560QA (en) | 2020-11-27 |
| US20240166667A1 (en) | 2024-05-23 |
| IL312291A (en) | 2024-06-01 |
| CN112368289B (zh) | 2024-02-20 |
| MX2020011564A (es) | 2021-01-29 |
| CA3098698A1 (en) | 2019-11-07 |
| IL278335B1 (en) | 2024-05-01 |
| KR20210018243A (ko) | 2021-02-17 |
| US11685749B2 (en) | 2023-06-27 |
| AU2019262979A1 (en) | 2020-12-10 |
| IL278335A (en) | 2020-12-31 |
| CN112368289A (zh) | 2021-02-12 |
| KR102859103B1 (ko) | 2025-09-12 |
| EP3788050B1 (en) | 2024-08-28 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7381492B2 (ja) | Mtor阻害剤としてのc26-連結ラパマイシン類似体 | |
| JP7358387B2 (ja) | Mtor阻害剤としてのc40-、c28-およびc-32-連結ラパマイシン類似体 | |
| RU2826559C2 (ru) | C26-СВЯЗАННЫЕ АНАЛОГИ РАПАМИЦИНА В КАЧЕСТВЕ ИНГИБИТОРОВ mTOR | |
| TWI913217B (zh) | 作為mTOR抑制劑之C40-、C28-及C-32連接之雷帕黴素類似物 | |
| RU2805211C2 (ru) | С40-, с28- и с-32-связанные аналоги рапамицина в качестве ингибиторов mtor | |
| HK40052499A (en) | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors | |
| HK40052499B (zh) | 作为mtor抑制剂的c40-、c28-及c-32连接的雷帕霉素类似物 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20220421 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20220421 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20230314 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20230309 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20230425 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20230912 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20231024 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20231102 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 7381492 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |