CN103958524B - 稠合的二环噁唑烷酮cetp抑制剂 - Google Patents
稠合的二环噁唑烷酮cetp抑制剂 Download PDFInfo
- Publication number
- CN103958524B CN103958524B CN201280052931.5A CN201280052931A CN103958524B CN 103958524 B CN103958524 B CN 103958524B CN 201280052931 A CN201280052931 A CN 201280052931A CN 103958524 B CN103958524 B CN 103958524B
- Authority
- CN
- China
- Prior art keywords
- compound
- mmol
- pharmaceutically acceptable
- following structure
- phenyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- XJRJFJUQEUZJCN-NLCCLPPVSA-N CCCC[C@@H](CCC)[C@H]([C@@H](C)/C=C(/CC)\C(C)(C)CN)OC Chemical compound CCCC[C@@H](CCC)[C@H]([C@@H](C)/C=C(/CC)\C(C)(C)CN)OC XJRJFJUQEUZJCN-NLCCLPPVSA-N 0.000 description 1
- DKQNXCKLZCCAIW-QUFPSDLASA-O C[C@@H](CC1)C=CC1[C@@H](N)[OH2+] Chemical compound C[C@@H](CC1)C=CC1[C@@H](N)[OH2+] DKQNXCKLZCCAIW-QUFPSDLASA-O 0.000 description 1
Classifications
-
- 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
- C07D498/02—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 two hetero rings
- C07D498/04—Ortho-condensed 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
- A61K31/41—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
- A61K31/42—Oxazoles
- A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
-
- 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
- A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic 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)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552592P | 2011-10-28 | 2011-10-28 | |
| US61/552,592 | 2011-10-28 | ||
| US61/552592 | 2011-10-28 | ||
| PCT/US2012/061842 WO2013063217A1 (en) | 2011-10-28 | 2012-10-25 | Fused bicyclic oxazolidinone cetp inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103958524A CN103958524A (zh) | 2014-07-30 |
| CN103958524B true CN103958524B (zh) | 2016-04-06 |
Family
ID=47143312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280052931.5A Expired - Fee Related CN103958524B (zh) | 2011-10-28 | 2012-10-25 | 稠合的二环噁唑烷酮cetp抑制剂 |
Country Status (41)
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106432053A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种尼拉帕布中间体4‑(3s‑哌啶‑3‑基)溴苯的制备方法 |
| CN106432058A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种Niraparib中间体4‑（3S‑哌啶‑3‑基）苯胺的制备方法 |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| WO2012058187A1 (en) | 2010-10-29 | 2012-05-03 | Merck Sharp & Dohme Corp. | Cyclic amine substituted oxazolidinone cetp inhibitor |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| EP2934518B1 (en) | 2012-12-19 | 2020-02-19 | Merck Sharp & Dohme Corp. | Spirocyclic cetp inhibitors |
| US9376408B2 (en) | 2012-12-20 | 2016-06-28 | Merck Sharp & Dohme Corp. | Therapeutic thiazolidinone compounds |
| CN105143193B (zh) * | 2013-01-31 | 2017-12-15 | 株式会社钟根堂 | 作为cetp抑制剂的联芳基或杂环联芳基取代的环己烯衍生化合物 |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| WO2015017302A2 (en) | 2013-07-30 | 2015-02-05 | Merck Sharp & Dohme Corp. | Bicyclic ureas and thiadiazolidine-1,1-dioxides as cetp inhibitors |
| US9937153B2 (en) * | 2013-08-30 | 2018-04-10 | Merck Sharp & Dohme Ltd. | Oral pharmaceutical formulation of omarigliptin |
| EP3054945B1 (en) | 2013-10-10 | 2018-08-15 | Merck Sharp & Dohme Corp. | 3,3'-disubstituted indolines as inhibitors of cholesterol ester transfer protein |
| EP3083642B1 (en) * | 2013-12-17 | 2018-09-05 | Merck Sharp & Dohme Corp. | Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| CA2938718C (en) | 2014-02-05 | 2022-10-18 | Dezima Pharma B.V. | Cholesteryl ester transfer protein (cetp) inhibitor and pharmaceutical compositions comprising said inhibitor for use in the treatment or prevention of cardiovascular diseases |
| JP6980385B2 (ja) | 2014-03-26 | 2021-12-15 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | Ｆｇｆｒ阻害剤とｉｇｆ１ｒ阻害剤の組合せ |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| MA55696A (fr) | 2014-03-26 | 2022-02-23 | Astex Therapeutics Ltd | Combinaisons |
| WO2016018729A1 (en) | 2014-07-29 | 2016-02-04 | Merck Sharp & Dohme Corp. | Monocyclic isoxazolines as inhibitors of cholesterol ester transfer protein |
| WO2016067194A1 (en) * | 2014-10-27 | 2016-05-06 | Sun Pharmaceutical Industries Limited | Process for the preparation of anacetrapib and an intermediate thereof |
| JPWO2016084949A1 (ja) * | 2014-11-28 | 2017-09-07 | 興和株式会社 | 医薬 |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| EP3307672A4 (en) * | 2015-06-12 | 2019-04-10 | Rhodia Operations | HYBRIDNANOPARTICLES WITH DENDRONES, METHOD FOR PRODUCING SUCH HYBRIDNANOPARTICLES AND USES THEREOF |
| WO2017011279A1 (en) | 2015-07-13 | 2017-01-19 | Merck Sharp & Dohme Corp. | Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein |
| HRP20220012T1 (hr) | 2015-09-23 | 2022-04-01 | Janssen Pharmaceutica Nv | Bi-heteroaril supstituirani 1,4-benzodiazepini i njihova upotreba za liječenje raka |
| BR112018005637B1 (pt) | 2015-09-23 | 2023-11-28 | Janssen Pharmaceutica Nv | Compostos derivados de quinoxalina, quinolina e quinazolinona,composições farmacêuticas que os compreende, e uso dos referidos compostos |
| CN111285894B (zh) * | 2018-12-10 | 2021-03-05 | 北京天一绿甫医药科技有限公司 | 用于制备软海绵素类化合物的中间体及其制备方法 |
| CN110639018B (zh) * | 2019-11-14 | 2020-06-26 | 牡丹江医学院 | 一种防治老年性高血压的药物组合物及其用途 |
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| DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
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-
2012
- 2012-10-21 JO JOP/2012/0317A patent/JO3210B1/ar active
- 2012-10-25 HR HRP20161541TT patent/HRP20161541T1/hr unknown
- 2012-10-25 UA UAA201405743A patent/UA114612C2/uk unknown
- 2012-10-25 ME MEP-2016-268A patent/ME02557B/me unknown
- 2012-10-25 US US13/660,010 patent/US8871738B2/en active Active
- 2012-10-25 JP JP2014538988A patent/JP5658427B2/ja not_active Expired - Fee Related
- 2012-10-25 PT PT127815512T patent/PT2771345T/pt unknown
- 2012-10-25 WO PCT/US2012/061842 patent/WO2013063217A1/en not_active Ceased
- 2012-10-25 KR KR1020147013895A patent/KR101686308B1/ko not_active Expired - Fee Related
- 2012-10-25 EP EP12781551.2A patent/EP2771345B1/en active Active
- 2012-10-25 RS RS20161003A patent/RS55420B1/sr unknown
- 2012-10-25 BR BR112014010204A patent/BR112014010204A2/pt not_active Application Discontinuation
- 2012-10-25 GE GEAP201213478A patent/GEP20166434B/en unknown
- 2012-10-25 CA CA2852743A patent/CA2852743C/en not_active Expired - Fee Related
- 2012-10-25 MX MX2014005074A patent/MX345222B/es active IP Right Grant
- 2012-10-25 AU AU2012328759A patent/AU2012328759B2/en not_active Ceased
- 2012-10-25 DK DK12781551.2T patent/DK2771345T3/en active
- 2012-10-25 EA EA201490889A patent/EA026123B1/ru not_active IP Right Cessation
- 2012-10-25 PH PH1/2014/500890A patent/PH12014500890A1/en unknown
- 2012-10-25 PE PE2014000616A patent/PE20141230A1/es not_active Application Discontinuation
- 2012-10-25 ES ES12781551.2T patent/ES2604953T3/es active Active
- 2012-10-25 IN IN3073CHN2014 patent/IN2014CN03073A/en unknown
- 2012-10-25 SI SI201230757A patent/SI2771345T1/sl unknown
- 2012-10-25 PL PL12781551T patent/PL2771345T3/pl unknown
- 2012-10-25 LT LTEP12781551.2T patent/LT2771345T/lt unknown
- 2012-10-25 HU HUE12781551A patent/HUE030568T2/en unknown
- 2012-10-25 SG SG11201401884PA patent/SG11201401884PA/en unknown
- 2012-10-25 CN CN201280052931.5A patent/CN103958524B/zh not_active Expired - Fee Related
- 2012-10-26 TW TW101139812A patent/TWI601731B/zh not_active IP Right Cessation
- 2012-10-26 AR ARP120104037A patent/AR088565A1/es unknown
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2014
- 2014-04-13 IL IL232130A patent/IL232130A/en not_active IP Right Cessation
- 2014-04-15 TN TNP2014000158A patent/TN2014000158A1/en unknown
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106432053A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种尼拉帕布中间体4‑(3s‑哌啶‑3‑基)溴苯的制备方法 |
| CN106432058A (zh) * | 2016-09-17 | 2017-02-22 | 青岛云天生物技术有限公司 | 一种Niraparib中间体4‑（3S‑哌啶‑3‑基）苯胺的制备方法 |
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