CR20230103A - Análogos de rapamicina ligados a c40, c28 y c32 como inhibidores de mtor - Google Patents
Análogos de rapamicina ligados a c40, c28 y c32 como inhibidores de mtorInfo
- Publication number
- CR20230103A CR20230103A CR20230103A CR20230103A CR20230103A CR 20230103 A CR20230103 A CR 20230103A CR 20230103 A CR20230103 A CR 20230103A CR 20230103 A CR20230103 A CR 20230103A CR 20230103 A CR20230103 A CR 20230103A
- Authority
- CR
- Costa Rica
- Prior art keywords
- mtor inhibitors
- rapamycin analogs
- mtor
- linked rapamycin
- linked
- Prior art date
Links
- 229940124302 mTOR inhibitor Drugs 0.000 title abstract 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 title abstract 2
- 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
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 abstract 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000002194 synthesizing effect Effects 0.000 abstract 1
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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
Abstract
Inhibidores de mTOR, así como compuestos y composiciones para inhibir mTOR, métodos de tratamiento de enfermedades mediadas por mTOR y métodos para sintetizar estos compuestos.
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 |
---|---|
CR20230103A true CR20230103A (es) | 2023-04-11 |
Family
ID=66484166
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20230103A CR20230103A (es) | 2018-05-01 | 2019-04-29 | Análogos de rapamicina ligados a c40, c28 y c32 como inhibidores de mtor |
CR20200578A CR20200578A (es) | 2018-05-01 | 2019-04-29 | Análogos de rapamicina a c40, c28 y c32 como inhibidores de mtor |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CR20200578A CR20200578A (es) | 2018-05-01 | 2019-04-29 | Análogos de rapamicina a c40, c28 y c32 como inhibidores de mtor |
Country Status (29)
Country | Link |
---|---|
US (4) | US20190336609A1 (es) |
EP (2) | EP4234031A3 (es) |
JP (2) | JP7358387B2 (es) |
KR (1) | KR20210018244A (es) |
CN (1) | CN112771054B (es) |
AU (2) | AU2019262978B2 (es) |
BR (1) | BR112020022201A2 (es) |
CA (1) | CA3098692A1 (es) |
CL (1) | CL2020002827A1 (es) |
CO (1) | CO2020013865A2 (es) |
CR (2) | CR20230103A (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 (1) | 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) |
TW (1) | TW202014208A (es) |
WO (1) | WO2019212990A1 (es) |
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TWI806832B (zh) | 2016-07-12 | 2023-07-01 | 美商銳新醫藥公司 | 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪 |
CA3051054A1 (en) | 2017-01-23 | 2018-07-26 | Revolution Medicines, Inc. | Pyridine compounds as allosteric shp2 inhibitors |
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 |
RU2020115095A (ru) | 2017-10-12 | 2021-11-12 | Революшн Медсинз, Инк. | Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2 |
BR112020009757A2 (pt) | 2017-12-15 | 2020-11-03 | Revolution Medicines, Inc. | compostos policíclicos como inibidores alostéricos de shp2 |
BR112020022201A2 (pt) | 2018-05-01 | 2021-02-02 | Revolution Medicines, Inc. | análogos de rapamicina ligada a c40, c28, e c-32 como inibidores de mtor |
JP7381492B2 (ja) | 2018-05-01 | 2023-11-15 | 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 | Mtor阻害剤としてのc26-連結ラパマイシン類似体 |
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 |
KR20210146287A (ko) | 2019-03-01 | 2021-12-03 | 레볼루션 메디슨즈, 인크. | 이환식 헤테로아릴 화합물 및 이의 용도 |
CN115873020A (zh) | 2019-11-04 | 2023-03-31 | 锐新医药公司 | Ras抑制剂 |
AU2020379734A1 (en) | 2019-11-04 | 2022-05-05 | Revolution Medicines, Inc. | Ras inhibitors |
KR20220109407A (ko) | 2019-11-04 | 2022-08-04 | 레볼루션 메디슨즈, 인크. | Ras 억제제 |
MX2022005525A (es) | 2019-11-08 | 2022-06-08 | Revolution Medicines Inc | Compuestos de heteroarilo bicíclicos y usos de estos. |
EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
AU2021293228A1 (en) | 2020-06-18 | 2023-02-09 | Revolution Medicines, Inc. | Methods for delaying, preventing, and treating acquired resistance to RAS inhibitors |
US11857551B1 (en) | 2020-07-10 | 2024-01-02 | Ting Therapeutics Llc | Methods for the prevention and treatment of hearing loss |
CA3187757A1 (en) | 2020-09-03 | 2022-03-24 | Ethan AHLER | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
JP2023541916A (ja) | 2020-09-15 | 2023-10-04 | レボリューション メディシンズ インコーポレイテッド | がんの治療における、ras阻害剤としてのインドール誘導体 |
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CN117412954A (zh) * | 2021-04-09 | 2024-01-16 | 锐新医药公司 | 雷帕霉素类似物化合物的合成 |
JP2024517847A (ja) | 2021-05-05 | 2024-04-23 | レボリューション メディシンズ インコーポレイテッド | Ras阻害剤 |
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 |
CN117616031A (zh) | 2021-05-05 | 2024-02-27 | 锐新医药公司 | 用于治疗癌症的ras抑制剂 |
EP4337678A1 (en) * | 2021-05-12 | 2024-03-20 | Revolution Medicines, Inc. | Use of sos1 inhibitors with mtor inhibitors to treat cancers |
CN114044775B (zh) * | 2021-08-30 | 2023-04-07 | 杭州医学院 | 一种靶向泛素化诱导bcr-abl蛋白降解的化合物及其应用 |
AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
EP4448526A1 (en) | 2021-12-17 | 2024-10-23 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
TW202402277A (zh) | 2022-05-25 | 2024-01-16 | 美商銳新醫藥公司 | 以mtor抑制劑治療癌症之方法 |
WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
GB202212000D0 (en) * | 2022-08-17 | 2022-09-28 | Mironid Ltd | Compounds and their use as PDE4 activators |
WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
WO2024211712A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
US20240352038A1 (en) | 2023-04-14 | 2024-10-24 | Revolution Medicines, Inc. | Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof |
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