EA034357B1 - Способ получения синтетических промежуточных соединений для получения производных тетрагидрохинолина - Google Patents
Способ получения синтетических промежуточных соединений для получения производных тетрагидрохинолина Download PDFInfo
- Publication number
- EA034357B1 EA034357B1 EA201790364A EA201790364A EA034357B1 EA 034357 B1 EA034357 B1 EA 034357B1 EA 201790364 A EA201790364 A EA 201790364A EA 201790364 A EA201790364 A EA 201790364A EA 034357 B1 EA034357 B1 EA 034357B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- formula
- compound
- acid
- mixture
- reaction mixture
- Prior art date
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Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/38—Nitrogen atoms
- C07D215/42—Nitrogen atoms attached in position 4
-
- 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
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| NL2014050556 | 2014-08-12 | ||
| PCT/NL2015/050555 WO2016024858A1 (en) | 2014-08-12 | 2015-07-29 | Process for preparing synthetic intermediates for preparing tetrahydroquinoline derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201790364A1 EA201790364A1 (ru) | 2017-07-31 |
| EA034357B1 true EA034357B1 (ru) | 2020-01-30 |
Family
ID=51429345
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201790364A EA034357B1 (ru) | 2014-08-12 | 2015-07-29 | Способ получения синтетических промежуточных соединений для получения производных тетрагидрохинолина |
Country Status (28)
| Country | Link |
|---|---|
| US (1) | US10112904B2 (enExample) |
| EP (2) | EP4083022A1 (enExample) |
| JP (1) | JP6670310B2 (enExample) |
| KR (1) | KR102572626B1 (enExample) |
| CN (1) | CN107108558B (enExample) |
| AR (1) | AR101509A1 (enExample) |
| AU (1) | AU2015302407B2 (enExample) |
| BR (1) | BR112017002873B1 (enExample) |
| CA (1) | CA2958040C (enExample) |
| CL (1) | CL2017000367A1 (enExample) |
| CY (1) | CY1125574T1 (enExample) |
| DK (1) | DK3180314T3 (enExample) |
| EA (1) | EA034357B1 (enExample) |
| ES (1) | ES2926775T3 (enExample) |
| HR (1) | HRP20221061T1 (enExample) |
| HU (1) | HUE059947T2 (enExample) |
| IL (1) | IL250525B (enExample) |
| LT (1) | LT3180314T (enExample) |
| MA (1) | MA40378B1 (enExample) |
| MX (1) | MX367908B (enExample) |
| PL (1) | PL3180314T3 (enExample) |
| PT (1) | PT3180314T (enExample) |
| RS (1) | RS63575B1 (enExample) |
| SG (1) | SG11201701077XA (enExample) |
| SI (1) | SI3180314T1 (enExample) |
| SM (1) | SMT202200385T1 (enExample) |
| TW (1) | TWI691490B (enExample) |
| WO (1) | WO2016024858A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2988112T3 (es) | 2021-03-05 | 2024-11-19 | Newamsterdam Pharma B V | Obicetrapib para el tratamiento de demencias |
| IL310115A (en) | 2021-07-26 | 2024-03-01 | Newamsterdam Pharma B V | Treatment of his hyporesponders |
| CA3242880A1 (en) | 2021-12-30 | 2023-07-06 | Newamsterdam Pharma B.V. | COMBINATION OF OBITECRAPIB AND SGLT2 INHIBITOR |
| US12006305B2 (en) | 2022-07-05 | 2024-06-11 | Newamsterdam Pharma B.V. | Salts of obicetrapib and processes for their manufacture and intermediates thereof |
| WO2024042061A1 (en) | 2022-08-22 | 2024-02-29 | Newamsterdam Pharma B.V. | Obicetrapib and ezetimibe combination treatment and fixed dose pharmaceutical compositions |
| EP4661865A1 (en) | 2023-02-07 | 2025-12-17 | NewAmsterdam Pharma B.V. | Obicetrapib and ezetimibe combination treatment and fixed dose pharmaceutical compositions |
| WO2025059594A1 (en) | 2023-09-15 | 2025-03-20 | Newamsterdam Pharma B.V. | METHODS FOR TREATING HETEROZYGOUS FAMILIAL HYPERCHOLESTEROLEMIA (HeFH) |
| WO2025093129A1 (en) | 2023-11-01 | 2025-05-08 | Newamsterdam Pharma B.V. | Treatment and prevention of age-related macular degeneration using a cetp inhibitor |
| WO2025093436A1 (en) | 2023-11-01 | 2025-05-08 | Newamsterdam Pharma B.V. | Treatment and prevention of age-related macular degeneration using a cetp inhibitor |
| WO2025146262A1 (en) | 2024-01-03 | 2025-07-10 | Newamsterdam Pharma B.V. | Obicetrapib for use in the treatment of hemoglobinopathies |
| WO2025146415A1 (en) | 2024-01-03 | 2025-07-10 | Newamsterdam Pharma B.V. | Improvement in atherosclerotic plaque characteristics with obicetrapib |
| EP4746866A1 (en) | 2024-09-17 | 2026-05-27 | NewAmsterdam Pharma B.V. | Obicetrapib for use in methods for treating a subject having heterozygous familial hypercholesterolemia (hefh) and/or atherosclerotic cardiovascular disease (ascvd) |
| WO2026062049A1 (en) | 2024-09-21 | 2026-03-26 | Newamsterdam Pharma B.V., | Obicetrapib for the treatment of dementias |
| WO2026063944A1 (en) | 2024-09-21 | 2026-03-26 | Newamsterdam Pharma B.V. | Obicetrapib for the treatment of dementias |
| WO2026087915A1 (en) | 2024-10-25 | 2026-04-30 | Newamsterdam Pharma B.V. | Treatment and prevention of sepsis or other dysregulated inflammatory responses using cetp inhibitor obicetrapib |
| WO2026115019A1 (en) | 2024-11-27 | 2026-06-04 | Newamsterdam Pharma B.V. | Enantioselective process for preparing tetrahydroquinoline derivatives |
| WO2026146129A1 (en) | 2025-01-02 | 2026-07-09 | Newamsterdam Pharma B.V. | Magnesium salts of obicetrapib |
| WO2026146132A1 (en) | 2025-01-02 | 2026-07-09 | Newamsterdam Pharma B.V. | Salts of obicetrapib |
| WO2026146133A1 (en) | 2025-01-02 | 2026-07-09 | Newamsterdam Pharma B.V. | Deuterated derivatives of obicetrapib |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000017164A1 (en) * | 1998-09-17 | 2000-03-30 | Pfizer Products Inc. | 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines as cetp inhibitors |
| WO2007116922A1 (en) * | 2006-03-30 | 2007-10-18 | Mitsubishi Tanabe Pharma Corporation | A process for preparing tetrahydroquinoline derivatives |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2445623A1 (en) * | 2001-04-30 | 2002-11-07 | Pfizer Products Inc. | Methods for preparing cetp inhibitors |
| UA90269C2 (ru) * | 2004-04-02 | 2010-04-26 | Мицубиси Танабе Фарма Корпорейшн | Тетрагидрохинолиновые производные и способ их получения |
| CN101466679A (zh) * | 2006-03-30 | 2009-06-24 | 田边三菱制药株式会社 | 制备四氢喹啉衍生物的方法 |
-
2015
- 2015-07-29 CN CN201580046606.1A patent/CN107108558B/zh active Active
- 2015-07-29 ES ES15767345T patent/ES2926775T3/es active Active
- 2015-07-29 HR HRP20221061TT patent/HRP20221061T1/hr unknown
- 2015-07-29 SI SI201531874T patent/SI3180314T1/sl unknown
- 2015-07-29 HU HUE15767345A patent/HUE059947T2/hu unknown
- 2015-07-29 AU AU2015302407A patent/AU2015302407B2/en active Active
- 2015-07-29 EP EP22179712.9A patent/EP4083022A1/en active Pending
- 2015-07-29 SG SG11201701077XA patent/SG11201701077XA/en unknown
- 2015-07-29 CA CA2958040A patent/CA2958040C/en active Active
- 2015-07-29 BR BR112017002873-5A patent/BR112017002873B1/pt active IP Right Grant
- 2015-07-29 EP EP15767345.0A patent/EP3180314B1/en active Active
- 2015-07-29 JP JP2017528754A patent/JP6670310B2/ja active Active
- 2015-07-29 US US15/503,686 patent/US10112904B2/en active Active
- 2015-07-29 PL PL15767345.0T patent/PL3180314T3/pl unknown
- 2015-07-29 PT PT157673450T patent/PT3180314T/pt unknown
- 2015-07-29 WO PCT/NL2015/050555 patent/WO2016024858A1/en not_active Ceased
- 2015-07-29 DK DK15767345.0T patent/DK3180314T3/da active
- 2015-07-29 SM SM20220385T patent/SMT202200385T1/it unknown
- 2015-07-29 MA MA40378A patent/MA40378B1/fr unknown
- 2015-07-29 KR KR1020177006422A patent/KR102572626B1/ko active Active
- 2015-07-29 LT LTEPPCT/NL2015/050555T patent/LT3180314T/lt unknown
- 2015-07-29 RS RS20220810A patent/RS63575B1/sr unknown
- 2015-07-29 EA EA201790364A patent/EA034357B1/ru active IP Right Revival
- 2015-07-29 MX MX2017001930A patent/MX367908B/es active IP Right Grant
- 2015-08-10 TW TW104125888A patent/TWI691490B/zh active
- 2015-08-11 AR ARP150102597A patent/AR101509A1/es active IP Right Grant
-
2017
- 2017-02-09 IL IL250525A patent/IL250525B/en active IP Right Grant
- 2017-02-10 CL CL2017000367A patent/CL2017000367A1/es unknown
-
2022
- 2022-09-22 CY CY20221100631T patent/CY1125574T1/el unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2000017164A1 (en) * | 1998-09-17 | 2000-03-30 | Pfizer Products Inc. | 4-carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines as cetp inhibitors |
| WO2007116922A1 (en) * | 2006-03-30 | 2007-10-18 | Mitsubishi Tanabe Pharma Corporation | A process for preparing tetrahydroquinoline derivatives |
Non-Patent Citations (2)
| Title |
|---|
| ANA ESCRIBANO; ANA I. MATEO; EVA M. MARTIN DE LA NAVA; DANIEL R. MAYHUGH; SANDRA L. COCKERHAM; THOMAS P. BEYER; ROBERT J. SCHMIDT;: "Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, AMSTERDAM, NL, vol. 22, no. 11, 7 April 2012 (2012-04-07), AMSTERDAM, NL, pages 3671 - 3675, XP028423341, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2012.04.042 * |
| KOUZNETSOV, V.V.: "Recent synthetic developments in a powerful imino Diels-Alder reaction (Povarov reaction): application to the synthesis of N-polyheterocycles and related alkaloids", TETRAHEDRON, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 65, no. 14, 4 April 2009 (2009-04-04), AMSTERDAM, NL, pages 2721 - 2750, XP026001418, ISSN: 0040-4020, DOI: 10.1016/j.tet.2008.12.059 * |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ BY KZ KG TJ TM |
|
| NF4A | Restoration of lapsed right to a eurasian patent |
Designated state(s): AM AZ BY KZ KG TJ TM |