CN107108558B - 制备用于制备四氢喹啉衍生物的合成中间体的方法 - Google Patents

制备用于制备四氢喹啉衍生物的合成中间体的方法 Download PDF

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Publication number
CN107108558B
CN107108558B CN201580046606.1A CN201580046606A CN107108558B CN 107108558 B CN107108558 B CN 107108558B CN 201580046606 A CN201580046606 A CN 201580046606A CN 107108558 B CN107108558 B CN 107108558B
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formula
compound
acid
preparation
mixture
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Chinese (zh)
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CN107108558A (zh
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J.福德
J.P.G.西尔登
A.勒鲁
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New Amsterdam Pharmaceutical Pte Ltd
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Dezima Pharma BV
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    • 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

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  • 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)
CN201580046606.1A 2014-08-12 2015-07-29 制备用于制备四氢喹啉衍生物的合成中间体的方法 Active CN107108558B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
NL2014050556 2014-08-12
NLPCT/NL2014/050556 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
CN107108558A CN107108558A (zh) 2017-08-29
CN107108558B true CN107108558B (zh) 2019-11-19

Family

ID=51429345

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Application Number Title Priority Date Filing Date
CN201580046606.1A Active CN107108558B (zh) 2014-08-12 2015-07-29 制备用于制备四氢喹啉衍生物的合成中间体的方法

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)

* Cited by examiner, † Cited by third party
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1318058A (zh) * 1998-09-17 2001-10-17 辉瑞产品公司 用作cetp抑制剂的4－羧基氨基－2－取代的－1,2,3,4－四氢喹啉
CN100357265C (zh) * 2001-04-30 2007-12-26 辉瑞产品公司 用作4－氨基喹啉衍生物中间体的化合物
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

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA90269C2 (ru) * 2004-04-02 2010-04-26 Мицубиси Танабе Фарма Корпорейшн Тетрагидрохинолиновые производные и способ их получения
UY30244A1 (es) 2006-03-30 2007-11-30 Tanabe Seiyaku Co Un proceso para preparar derivados de tetrahidroquinolina

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1318058A (zh) * 1998-09-17 2001-10-17 辉瑞产品公司 用作cetp抑制剂的4－羧基氨基－2－取代的－1,2,3,4－四氢喹啉
CN100357265C (zh) * 2001-04-30 2007-12-26 辉瑞产品公司 用作4－氨基喹啉衍生物中间体的化合物
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Ana Escribano等.Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.《Bioorganic & Medicinal Chemistry Letters》.2012,第22卷第3671-3675页. *
Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors;Ana Escribano等;《Bioorganic & Medicinal Chemistry Letters》;20120413;第22卷;第3671-3675页 *

Also Published As

Publication number Publication date
ES2926775T3 (es) 2022-10-28
TWI691490B (zh) 2020-04-21
PT3180314T (pt) 2022-09-02
MX2017001930A (es) 2018-03-01
AU2015302407B2 (en) 2019-09-19
US10112904B2 (en) 2018-10-30
MX367908B (es) 2019-09-11
EA201790364A1 (ru) 2017-07-31
KR102572626B1 (ko) 2023-08-30
PL3180314T3 (pl) 2022-11-21
MA40378A (fr) 2017-06-21
BR112017002873A2 (pt) 2018-07-17
CY1125574T1 (el) 2026-02-25
EP3180314B1 (en) 2022-06-22
CL2017000367A1 (es) 2018-02-09
HUE059947T2 (hu) 2023-01-28
IL250525A0 (en) 2017-03-30
AR101509A1 (es) 2016-12-21
JP6670310B2 (ja) 2020-03-18
CA2958040A1 (en) 2016-02-18
BR112017002873B1 (pt) 2023-03-28
SI3180314T1 (sl) 2022-11-30
TW201613868A (en) 2016-04-16
WO2016024858A1 (en) 2016-02-18
IL250525B (en) 2019-08-29
MA40378B1 (fr) 2022-10-31
KR20170102204A (ko) 2017-09-08
SG11201701077XA (en) 2017-03-30
US20170267640A1 (en) 2017-09-21
HRP20221061T1 (hr) 2022-11-25
CA2958040C (en) 2022-09-13
EP4083022A1 (en) 2022-11-02
LT3180314T (lt) 2022-11-10
EP3180314A1 (en) 2017-06-21
CN107108558A (zh) 2017-08-29
EA034357B1 (ru) 2020-01-30
DK3180314T3 (da) 2022-08-29
BR112017002873A8 (pt) 2022-11-08
AU2015302407A1 (en) 2017-03-02
JP2017524742A (ja) 2017-08-31
RS63575B1 (sr) 2022-10-31
SMT202200385T1 (it) 2022-11-18

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