TWI691490B - 四氫喹啉衍生物的合成中間體、製備方法及用途 - Google Patents
四氫喹啉衍生物的合成中間體、製備方法及用途 Download PDFInfo
- Publication number
- TWI691490B TWI691490B TW104125888A TW104125888A TWI691490B TW I691490 B TWI691490 B TW I691490B TW 104125888 A TW104125888 A TW 104125888A TW 104125888 A TW104125888 A TW 104125888A TW I691490 B TWI691490 B TW I691490B
- Authority
- TW
- Taiwan
- Prior art keywords
- formula
- compound
- item
- salt
- preparing
- Prior art date
Links
- 0 *C(*1=NC1)=O Chemical compound *C(*1=NC1)=O 0.000 description 2
- OEGXWYMCPLEGDA-UHFFFAOYSA-N CC(C1)Nc2ccc(C(F)(F)F)cc2C1NC(C)=O Chemical compound CC(C1)Nc2ccc(C(F)(F)F)cc2C1NC(C)=O OEGXWYMCPLEGDA-UHFFFAOYSA-N 0.000 description 1
- ATMIPLRWLMNMCB-ACGXKRRESA-N CCC(C[C@@H]1NC=O)Nc2c1cc(C(F)(F)F)cc2 Chemical compound CCC(C[C@@H]1NC=O)Nc2c1cc(C(F)(F)F)cc2 ATMIPLRWLMNMCB-ACGXKRRESA-N 0.000 description 1
- NRWORBQAOQVYBJ-GJZUVCINSA-N CC[C@H](C1)N(C(OCC)=O)c2ccc(C(F)(F)F)cc2[C@H]1N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c(nc1)ncc1OCCCC(O)=O Chemical compound CC[C@H](C1)N(C(OCC)=O)c2ccc(C(F)(F)F)cc2[C@H]1N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c(nc1)ncc1OCCCC(O)=O NRWORBQAOQVYBJ-GJZUVCINSA-N 0.000 description 1
- RRIWMEAWOLZGND-UHFFFAOYSA-O [NH3+]C(C1)c2cc(C(F)(F)F)ccc2NC1O Chemical compound [NH3+]C(C1)c2cc(C(F)(F)F)ccc2NC1O RRIWMEAWOLZGND-UHFFFAOYSA-O 0.000 description 1
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
-
- 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
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Quinoline Compounds (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 |
|---|---|---|---|
| WOPCT/NL2014/050556 | 2014-08-12 | ||
| NL2014050556 | 2014-08-12 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW201613868A TW201613868A (en) | 2016-04-16 |
| TWI691490B true TWI691490B (zh) | 2020-04-21 |
Family
ID=51429345
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW104125888A TWI691490B (zh) | 2014-08-12 | 2015-08-10 | 四氫喹啉衍生物的合成中間體、製備方法及用途 |
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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2023010211A (es) | 2021-03-05 | 2023-11-22 | Newamsterdam Pharma B V | Obicetrapib para tratamiento de demencias. |
| MX2024001170A (es) | 2021-07-26 | 2024-05-14 | Newamsterdam Pharma B V | Tratamiento de personas hiporreactivas a his. |
| US20250170128A1 (en) | 2021-12-30 | 2025-05-29 | NEWAMSTERDAM PHARMA B.V. (Dutch Chamber of Commerce No. 5597 1946) | Obicetrapib and SGLT2 Inhibitor Combination |
| US12006305B2 (en) | 2022-07-05 | 2024-06-11 | Newamsterdam Pharma B.V. | Salts of obicetrapib and processes for their manufacture and intermediates thereof |
| TW202416994A (zh) | 2022-08-22 | 2024-05-01 | 荷蘭商新阿姆斯特丹製藥公司 | 固定劑量醫藥組合物及其用途 |
| WO2024165395A1 (en) | 2023-02-07 | 2024-08-15 | 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) |
| WO2025093436A1 (en) | 2023-11-01 | 2025-05-08 | Newamsterdam Pharma B.V. | Treatment and prevention of age-related macular degeneration using a cetp inhibitor |
| WO2025093129A1 (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 |
| WO2026062050A1 (en) | 2024-09-17 | 2026-03-26 | Newamsterdam Pharma B.V. | Obicetrapib for use in methods for treating a subject having heterozygous familial hypercholesterolemia (hefh) and/or atherosclerotic cardiovascular disease (ascvd) |
| WO2026063944A1 (en) | 2024-09-21 | 2026-03-26 | Newamsterdam Pharma B.V. | Obicetrapib for the treatment of dementias |
| WO2026062049A1 (en) | 2024-09-21 | 2026-03-26 | Newamsterdam Pharma B.V., | Obicetrapib for the treatment of dementias |
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 |
|---|---|---|---|---|
| MXPA03009935A (es) * | 2001-04-30 | 2004-01-29 | Pfizer Prod Inc | Metodos e intermedios para preparar inhibidores 4-aminoquinolina de cetp. |
| 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 ES ES15767345T patent/ES2926775T3/es active Active
- 2015-07-29 LT LTEPPCT/NL2015/050555T patent/LT3180314T/lt unknown
- 2015-07-29 SI SI201531874T patent/SI3180314T1/sl unknown
- 2015-07-29 DK DK15767345.0T patent/DK3180314T3/da active
- 2015-07-29 AU AU2015302407A patent/AU2015302407B2/en active Active
- 2015-07-29 HR HRP20221061TT patent/HRP20221061T1/hr unknown
- 2015-07-29 PL PL15767345.0T patent/PL3180314T3/pl unknown
- 2015-07-29 EP EP22179712.9A patent/EP4083022A1/en active Pending
- 2015-07-29 RS RS20220810A patent/RS63575B1/sr unknown
- 2015-07-29 KR KR1020177006422A patent/KR102572626B1/ko active Active
- 2015-07-29 EP EP15767345.0A patent/EP3180314B1/en active Active
- 2015-07-29 MX MX2017001930A patent/MX367908B/es active IP Right Grant
- 2015-07-29 BR BR112017002873-5A patent/BR112017002873B1/pt active IP Right Grant
- 2015-07-29 SG SG11201701077XA patent/SG11201701077XA/en unknown
- 2015-07-29 US US15/503,686 patent/US10112904B2/en active Active
- 2015-07-29 SM SM20220385T patent/SMT202200385T1/it unknown
- 2015-07-29 EA EA201790364A patent/EA034357B1/ru active IP Right Revival
- 2015-07-29 CA CA2958040A patent/CA2958040C/en active Active
- 2015-07-29 WO PCT/NL2015/050555 patent/WO2016024858A1/en not_active Ceased
- 2015-07-29 CN CN201580046606.1A patent/CN107108558B/zh active Active
- 2015-07-29 HU HUE15767345A patent/HUE059947T2/hu unknown
- 2015-07-29 JP JP2017528754A patent/JP6670310B2/ja active Active
- 2015-07-29 PT PT157673450T patent/PT3180314T/pt unknown
- 2015-07-29 MA MA40378A patent/MA40378B1/fr unknown
- 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 |
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