BR112021011325A2 - Derivados de rapamicina - Google Patents
Derivados de rapamicinaInfo
- Publication number
- BR112021011325A2 BR112021011325A2 BR112021011325A BR112021011325A BR112021011325A2 BR 112021011325 A2 BR112021011325 A2 BR 112021011325A2 BR 112021011325 A BR112021011325 A BR 112021011325A BR 112021011325 A BR112021011325 A BR 112021011325A BR 112021011325 A2 BR112021011325 A2 BR 112021011325A2
- Authority
- BR
- Brazil
- Prior art keywords
- formula
- rapamycin derivatives
- compound
- methods
- pharmaceutically acceptable
- Prior art date
Links
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical class C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 208000037765 diseases and disorders Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- QFMKPDZCOKCBAQ-NFCVMBANSA-N sar943-nxa Chemical class C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)CC1 QFMKPDZCOKCBAQ-NFCVMBANSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
-
- 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
- A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862781242P | 2018-12-18 | 2018-12-18 | |
| PCT/IB2019/060957 WO2020128861A1 (en) | 2018-12-18 | 2019-12-17 | Rapamycin derivatives |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021011325A2 true BR112021011325A2 (pt) | 2021-11-16 |
Family
ID=69165426
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021011325A BR112021011325A2 (pt) | 2018-12-18 | 2019-12-17 | Derivados de rapamicina |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US12281125B2 (https=) |
| EP (1) | EP3898637B1 (https=) |
| JP (1) | JP7618553B2 (https=) |
| KR (1) | KR20210105397A (https=) |
| CN (1) | CN113260619B (https=) |
| AU (1) | AU2019409366B2 (https=) |
| BR (1) | BR112021011325A2 (https=) |
| CA (1) | CA3122922A1 (https=) |
| DK (1) | DK3898637T3 (https=) |
| ES (1) | ES3014225T3 (https=) |
| FI (1) | FI3898637T3 (https=) |
| HR (1) | HRP20250197T1 (https=) |
| HU (1) | HUE070859T2 (https=) |
| LT (1) | LT3898637T (https=) |
| MX (1) | MX2021007247A (https=) |
| PL (1) | PL3898637T3 (https=) |
| PT (1) | PT3898637T (https=) |
| RS (1) | RS66527B1 (https=) |
| SI (1) | SI3898637T1 (https=) |
| WO (1) | WO2020128861A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR112834A1 (es) | 2017-09-26 | 2019-12-18 | Novartis Ag | Derivados de rapamicina |
| WO2019241789A1 (en) | 2018-06-15 | 2019-12-19 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses thereof |
| IL285067B2 (en) | 2019-01-22 | 2025-02-01 | Aeovian Pharmaceuticals Inc | MTORC Modulators and Their Uses |
| AU2020397938A1 (en) | 2019-12-05 | 2022-06-23 | Janssen Pharmaceutica Nv | Rapamycin analogs and uses thereof |
| CN115776907B (zh) | 2020-03-27 | 2025-02-25 | 艾奥维安制药公司 | Mtorc1调节剂及其用途 |
| EP4688148A1 (en) * | 2023-04-07 | 2026-02-11 | Regeneron Pharmaceuticals, Inc. | Selective rapamycin analogs and uses thereof |
| GB202415232D0 (en) | 2024-10-16 | 2024-11-27 | Nacamed As | Composition |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US4316885A (en) | 1980-08-25 | 1982-02-23 | Ayerst, Mckenna And Harrison, Inc. | Acyl derivatives of rapamycin |
| US4650803A (en) | 1985-12-06 | 1987-03-17 | University Of Kansas | Prodrugs of rapamycin |
| US5120842A (en) | 1991-04-01 | 1992-06-09 | American Home Products Corporation | Silyl ethers of rapamycin |
| US5151413A (en) | 1991-11-06 | 1992-09-29 | American Home Products Corporation | Rapamycin acetals as immunosuppressant and antifungal agents |
| ZA935112B (en) | 1992-07-17 | 1994-02-08 | Smithkline Beecham Corp | Rapamycin derivatives |
| GB9221220D0 (en) | 1992-10-09 | 1992-11-25 | Sandoz Ag | Organic componds |
| US5302584A (en) | 1992-10-13 | 1994-04-12 | American Home Products Corporation | Carbamates of rapamycin |
| US5258389A (en) | 1992-11-09 | 1993-11-02 | Merck & Co., Inc. | O-aryl, O-alkyl, O-alkenyl and O-alkynylrapamycin derivatives |
| US5527907A (en) | 1993-11-19 | 1996-06-18 | Abbott Laboratories | Macrolide immunomodulators |
| US5362718A (en) | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| WO1996041865A1 (en) * | 1995-06-07 | 1996-12-27 | Ariad Gene Therapeutics, Inc. | Rapamcycin-based regulation of biological events |
| DE69637641D1 (de) | 1995-06-07 | 2008-09-25 | Ariad Gene Therapeutics Inc | Auf rapamycin basierende regulation biologischer vorgänge |
| US5985890A (en) | 1995-06-09 | 1999-11-16 | Novartis Ag | Rapamycin derivatives |
| GB9606452D0 (en) | 1996-03-27 | 1996-06-05 | Sandoz Ltd | Organic compounds |
| CA2257803C (en) | 1996-07-12 | 2008-12-02 | Ariad Pharmaceuticals, Inc. | Non immunosuppressive antifungal rapalogs |
| 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 |
| MX368013B (es) | 2001-02-19 | 2019-09-13 | Novartis Ag | Tratamiento de cáncer. |
| PT1478648E (pt) | 2002-02-01 | 2014-07-15 | Ariad Pharma Inc | Compostos contendo fósforo e suas utilizações |
| GB0601406D0 (en) | 2006-01-24 | 2006-03-08 | Novartis Ag | Organic Compounds |
| US20090023768A1 (en) | 2006-02-24 | 2009-01-22 | Novartis Ag | Rapamycin derivatives for treating neuroblastoma |
| WO2008022256A2 (en) | 2006-08-16 | 2008-02-21 | Blagosklonny Mikhail V | Methods and compositions for preventing or treating age-related diseases |
| WO2011133636A1 (en) | 2010-04-20 | 2011-10-27 | Cedars-Sinai Medical Center | COMBINATION THERAPY WITH CD4 LYMPHOCYTE DEPLETION AND mTOR INHIBITORS |
| EP2670758B1 (en) | 2011-02-04 | 2022-09-28 | Synthon BV | Process for making trisubstituted silyloxyethyl triflates |
| CN103391780B (zh) | 2011-02-16 | 2015-08-19 | 诺瓦提斯公司 | 用于治疗神经变性疾病的治疗剂的组合物 |
| JP6130391B2 (ja) | 2011-11-23 | 2017-05-17 | インテリカイン， エルエルシー | Ｍｔｏｒ阻害剤を使用する強化された治療レジメン |
| PE20170255A1 (es) | 2014-01-24 | 2017-03-22 | Dana Farber Cancer Inst Inc | Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas |
| EP3109250A1 (en) | 2015-06-23 | 2016-12-28 | Synbias Pharma AG | Method for the synthesis of rapamycin derivatives |
| US10683308B2 (en) | 2015-09-11 | 2020-06-16 | Navitor Pharmaceuticals, Inc. | Rapamycin analogs and uses 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 |
| US20220202787A1 (en) | 2019-03-26 | 2022-06-30 | Novartis Ag | Isothiazolidine 1,1-dioxide and 1,4-butan sultone containing rapamycin derivatives and uses thereof |
-
2019
- 2019-12-17 HR HRP20250197TT patent/HRP20250197T1/hr unknown
- 2019-12-17 LT LTEPPCT/IB2019/060957T patent/LT3898637T/lt unknown
- 2019-12-17 MX MX2021007247A patent/MX2021007247A/es unknown
- 2019-12-17 HU HUE19836546A patent/HUE070859T2/hu unknown
- 2019-12-17 BR BR112021011325A patent/BR112021011325A2/pt unknown
- 2019-12-17 JP JP2021534201A patent/JP7618553B2/ja active Active
- 2019-12-17 CN CN201980087363.4A patent/CN113260619B/zh active Active
- 2019-12-17 KR KR1020217022532A patent/KR20210105397A/ko active Pending
- 2019-12-17 CA CA3122922A patent/CA3122922A1/en active Pending
- 2019-12-17 PL PL19836546.2T patent/PL3898637T3/pl unknown
- 2019-12-17 WO PCT/IB2019/060957 patent/WO2020128861A1/en not_active Ceased
- 2019-12-17 AU AU2019409366A patent/AU2019409366B2/en active Active
- 2019-12-17 US US17/414,696 patent/US12281125B2/en active Active
- 2019-12-17 SI SI201930897T patent/SI3898637T1/sl unknown
- 2019-12-17 FI FIEP19836546.2T patent/FI3898637T3/fi active
- 2019-12-17 ES ES19836546T patent/ES3014225T3/es active Active
- 2019-12-17 DK DK19836546.2T patent/DK3898637T3/da active
- 2019-12-17 EP EP19836546.2A patent/EP3898637B1/en active Active
- 2019-12-17 PT PT198365462T patent/PT3898637T/pt unknown
- 2019-12-17 RS RS20250163A patent/RS66527B1/sr unknown
Also Published As
| Publication number | Publication date |
|---|---|
| PL3898637T3 (pl) | 2025-05-19 |
| HUE070859T2 (hu) | 2025-07-28 |
| CN113260619A (zh) | 2021-08-13 |
| PT3898637T (pt) | 2025-02-24 |
| JP7618553B2 (ja) | 2025-01-21 |
| KR20210105397A (ko) | 2021-08-26 |
| JP2022514254A (ja) | 2022-02-10 |
| MX2021007247A (es) | 2021-07-15 |
| LT3898637T (lt) | 2025-03-10 |
| CA3122922A1 (en) | 2020-06-25 |
| CN113260619B (zh) | 2026-02-03 |
| SI3898637T1 (sl) | 2025-04-30 |
| HRP20250197T1 (hr) | 2025-04-11 |
| AU2019409366A1 (en) | 2021-06-10 |
| ES3014225T3 (en) | 2025-04-21 |
| EP3898637A1 (en) | 2021-10-27 |
| US20220064185A1 (en) | 2022-03-03 |
| US12281125B2 (en) | 2025-04-22 |
| EP3898637B1 (en) | 2024-11-20 |
| FI3898637T3 (fi) | 2025-02-24 |
| AU2019409366B2 (en) | 2022-10-27 |
| WO2020128861A1 (en) | 2020-06-25 |
| DK3898637T3 (da) | 2025-02-17 |
| RS66527B1 (sr) | 2025-03-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |