PE20212112A1 - Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor - Google Patents
Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtorInfo
- Publication number
- PE20212112A1 PE20212112A1 PE2020001763A PE2020001763A PE20212112A1 PE 20212112 A1 PE20212112 A1 PE 20212112A1 PE 2020001763 A PE2020001763 A PE 2020001763A PE 2020001763 A PE2020001763 A PE 2020001763A PE 20212112 A1 PE20212112 A1 PE 20212112A1
- Authority
- PE
- Peru
- Prior art keywords
- rapamycin analogs
- mtor inhibitors
- mtor
- analogs linked
- compounds
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
- A61K47/545—Heterocyclic compounds
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- 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
- A61K31/495—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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
- A61K31/495—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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Immunology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Referido a un compuesto de formula Ic; en donde R32 es -H, =O, -OR3, -N3, entre otros; R28 es -H, (C1-C6)alquilo, entre otros; R40 es -H o -C(=Z1)-R40a; donde si R28 y R40 son H, luego R32 no es =O; cada Z1 es en forma independiente O o S; o una sal farmaceuticamente aceptable o tautomero del mismo. Estos compuestos analogos de rapamicina ligados a C40, C28 Y C-32 son inhibidores de mTOR. Tambien se refiere a metodos para sintetizar estos compuestos; preparaciones farmaceuticas que comprenden dichos compuestos, y su uso en el tratamiento de enfermedades mediados por mTOR, tales como el cancer, entre tumores de cerebro y neurovasculares, cancer mama, cancer pulmonar, entre otros.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862665435P | 2018-05-01 | 2018-05-01 | |
| US201862752874P | 2018-10-30 | 2018-10-30 | |
| US201962836036P | 2019-04-18 | 2019-04-18 | |
| PCT/US2019/029737 WO2019212990A1 (en) | 2018-05-01 | 2019-04-29 | C40-, c28-, and c-32-linked rapamycin analogs as mtor inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20212112A1 true PE20212112A1 (es) | 2021-11-04 |
Family
ID=66484166
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020001763A PE20212112A1 (es) | 2018-05-01 | 2019-04-29 | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor |
| PE2025001721A PE20252397A1 (es) | 2018-05-01 | 2019-04-29 | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2025001721A PE20252397A1 (es) | 2018-05-01 | 2019-04-29 | Analogos de rapamicina ligados a c40, c28 y c-32 como inhibidores de mtor |
Country Status (28)
| Country | Link |
|---|---|
| US (5) | US20190336609A1 (es) |
| EP (2) | EP3788049B1 (es) |
| JP (2) | JP7358387B2 (es) |
| KR (2) | KR20210018244A (es) |
| CN (3) | CN118894869A (es) |
| AU (3) | AU2019262978B2 (es) |
| BR (1) | BR112020022201A2 (es) |
| CA (1) | CA3098692A1 (es) |
| CL (2) | CL2020002827A1 (es) |
| CO (1) | CO2020013865A2 (es) |
| CR (3) | CR20240382A (es) |
| DK (1) | DK3788049T3 (es) |
| ES (1) | ES2945560T3 (es) |
| FI (1) | FI3788049T3 (es) |
| HR (1) | HRP20230488T1 (es) |
| HU (1) | HUE062352T2 (es) |
| IL (2) | IL300091A (es) |
| LT (1) | LT3788049T (es) |
| MX (3) | MX2020011565A (es) |
| PE (2) | PE20212112A1 (es) |
| PH (1) | PH12020551795A1 (es) |
| PL (1) | PL3788049T3 (es) |
| PT (1) | PT3788049T (es) |
| RS (1) | RS64272B1 (es) |
| SA (1) | SA520420458B1 (es) |
| SG (1) | SG11202010559UA (es) |
| SI (1) | SI3788049T1 (es) |
| WO (1) | WO2019212990A1 (es) |
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| CN110446709B (zh) | 2017-01-23 | 2023-09-12 | 锐新医药公司 | 作为变构shp2抑制剂的二环化合物 |
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| AU2018385713A1 (en) | 2017-12-15 | 2020-06-18 | Revolution Medicines, Inc. | Polycyclic compounds as allosteric SHP2 inhibitors |
| CR20240382A (es) | 2018-05-01 | 2025-08-29 | Revolution Medicines Inc | ANÁLOGOS DE RAPAMICINA A C40, C28 Y C32 COMO INHIBIDORES DE MTOR (Divisional 2020-578) |
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| WO2020180768A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
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| WO2022020114A2 (en) | 2020-07-10 | 2022-01-27 | Ting Therapeutics Llc | Methods for the prevention and treatment of hearing loss |
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