CN112533917B - 作为vps34的抑制剂的吗啉衍生物 - Google Patents
作为vps34的抑制剂的吗啉衍生物 Download PDFInfo
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- CN112533917B CN112533917B CN201980032053.2A CN201980032053A CN112533917B CN 112533917 B CN112533917 B CN 112533917B CN 201980032053 A CN201980032053 A CN 201980032053A CN 112533917 B CN112533917 B CN 112533917B
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- substituted
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/08—1,2,4-Thiadiazoles; Hydrogenated 1,2,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
- C07D285/12—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles
- C07D285/125—1,3,4-Thiadiazoles; Hydrogenated 1,3,4-thiadiazoles with oxygen, sulfur or nitrogen atoms, directly attached to ring carbon atoms, the nitrogen atoms not forming part of a nitro radical
- C07D285/135—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862655723P | 2018-04-10 | 2018-04-10 | |
| US62/655,723 | 2018-04-10 | ||
| PCT/US2019/026646 WO2019199874A1 (en) | 2018-04-10 | 2019-04-09 | Morpholine derivates as inhibitors of vps34 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112533917A CN112533917A (zh) | 2021-03-19 |
| CN112533917B true CN112533917B (zh) | 2024-06-21 |
Family
ID=66248835
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980032053.2A Active CN112533917B (zh) | 2018-04-10 | 2019-04-09 | 作为vps34的抑制剂的吗啉衍生物 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US11236079B2 (https=) |
| EP (1) | EP3774792B1 (https=) |
| JP (1) | JP7369140B2 (https=) |
| KR (1) | KR102803763B1 (https=) |
| CN (1) | CN112533917B (https=) |
| AU (1) | AU2019251363B2 (https=) |
| CA (1) | CA3095512A1 (https=) |
| EA (1) | EA202092446A1 (https=) |
| ES (1) | ES2929292T3 (https=) |
| MX (1) | MX2020010577A (https=) |
| SG (1) | SG11202008851UA (https=) |
| WO (1) | WO2019199874A1 (https=) |
| ZA (1) | ZA202005899B (https=) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112533917B (zh) | 2018-04-10 | 2024-06-21 | 神经孔疗法股份有限公司 | 作为vps34的抑制剂的吗啉衍生物 |
| ES3032793T3 (en) | 2018-04-10 | 2025-07-24 | Neuropore Therapies Inc | Tri-substituted aryl and heteroaryl derivatives as modulators of pi3-kinase and autophagy pathways |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101389622A (zh) * | 2006-01-20 | 2009-03-18 | 诺瓦提斯公司 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008070740A1 (en) * | 2006-12-07 | 2008-06-12 | F.Hoffmann-La Roche Ag | Phosphoinositide 3-kinase inhibitor compounds and methods of use |
| WO2009066084A1 (en) | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| EP2475375A4 (en) * | 2009-09-09 | 2013-02-20 | Avila Therapeutics Inc | PI3 KINASE INHIBITORS AND USES THEREOF |
| ES2608967T3 (es) * | 2011-03-28 | 2017-04-17 | Mei Pharma, Inc. | (Aralquilamino sustituido en alfa y heteroarilalquilamino)pirimidinil y 1,3,5-triazinil benzimidazoles, composiciones farmacéuticas que los contienen, y estos compuestos para usar en el tratamiento de enfermedades proliferativas |
| DK3416957T3 (da) * | 2016-02-19 | 2020-09-21 | Sprint Bioscience Ab | 6-heterocyclyl-4-morpholin-4-ylpyridin-2-on-forbindelser anvendelige ved behandlingen af cancer og diabetes |
| AU2017275657B2 (en) | 2016-06-02 | 2021-08-19 | Novartis Ag | Potassium channel modulators |
| CN112533917B (zh) | 2018-04-10 | 2024-06-21 | 神经孔疗法股份有限公司 | 作为vps34的抑制剂的吗啉衍生物 |
-
2019
- 2019-04-09 CN CN201980032053.2A patent/CN112533917B/zh active Active
- 2019-04-09 AU AU2019251363A patent/AU2019251363B2/en active Active
- 2019-04-09 US US17/046,750 patent/US11236079B2/en active Active
- 2019-04-09 KR KR1020207032483A patent/KR102803763B1/ko active Active
- 2019-04-09 JP JP2020555504A patent/JP7369140B2/ja active Active
- 2019-04-09 ES ES19719103T patent/ES2929292T3/es active Active
- 2019-04-09 EA EA202092446A patent/EA202092446A1/ru unknown
- 2019-04-09 CA CA3095512A patent/CA3095512A1/en active Pending
- 2019-04-09 EP EP19719103.4A patent/EP3774792B1/en active Active
- 2019-04-09 WO PCT/US2019/026646 patent/WO2019199874A1/en not_active Ceased
- 2019-04-09 SG SG11202008851UA patent/SG11202008851UA/en unknown
- 2019-04-09 MX MX2020010577A patent/MX2020010577A/es unknown
-
2020
- 2020-09-23 ZA ZA2020/05899A patent/ZA202005899B/en unknown
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101389622A (zh) * | 2006-01-20 | 2009-03-18 | 诺瓦提斯公司 | 用作pi-3激酶抑制剂的嘧啶衍生物 |
Non-Patent Citations (1)
| Title |
|---|
| A highly potent and selective Vps34 inhibitor alters vesicle trafficking and autophagy;Baptiste ronan，等;《Nature Chemical Biology》;第10卷(第12期);1013-1019 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US11236079B2 (en) | 2022-02-01 |
| AU2019251363A1 (en) | 2020-10-08 |
| MX2020010577A (es) | 2021-03-02 |
| EA202092446A1 (ru) | 2021-01-26 |
| ZA202005899B (en) | 2025-05-28 |
| CN112533917A (zh) | 2021-03-19 |
| US20210163467A1 (en) | 2021-06-03 |
| CA3095512A1 (en) | 2019-10-17 |
| EP3774792B1 (en) | 2022-09-14 |
| ES2929292T3 (es) | 2022-11-28 |
| SG11202008851UA (en) | 2020-10-29 |
| JP7369140B2 (ja) | 2023-10-25 |
| WO2019199874A1 (en) | 2019-10-17 |
| KR20200142549A (ko) | 2020-12-22 |
| KR102803763B1 (ko) | 2025-05-09 |
| EP3774792A1 (en) | 2021-02-17 |
| JP2021521179A (ja) | 2021-08-26 |
| AU2019251363B2 (en) | 2024-03-07 |
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| GR01 | Patent grant | ||
| GR01 | Patent grant |