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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Diabetes (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 | |
| US61/552592 | 2011-10-28 | ||
| US61/552,592 | 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 |
|---|---|---|---|---|
| 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 |
| 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 |
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 |
| CN103269592B (zh) | 2010-10-29 | 2016-05-11 | 默沙东公司 | 环胺取代的噁唑烷酮cetp抑制剂 |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (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 |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | 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 |
| WO2014099834A1 (en) | 2012-12-20 | 2014-06-26 | Merck Sharp & Dohme Corp. | Therapeutic thiazolidinone compounds |
| ES2642172T3 (es) * | 2013-01-31 | 2017-11-15 | Chong Kun Dang Pharmaceutical Corp. | Compuestos derivados de ciclohexeno sustituidos con biarilo o biarilo heterocíclico como inhibidores de CETP |
| 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 |
| WO2015054088A1 (en) | 2013-10-10 | 2015-04-16 | Merck Sharp & Dohme Corp. | 3,3'-disubstituted indolines as inhibitors of cholesterol ester transfer protein |
| CN105814064A (zh) * | 2013-12-17 | 2016-07-27 | 默沙东公司 | 作为胆固醇酯转运蛋白的抑制剂的稠合双环异噁唑啉类 |
| MX369471B (es) | 2014-02-05 | 2019-11-08 | Dezima Pharma B V | Inhibidor de proteina de transferencia del ester de colesterilo (cetp) y composiciones farmaceuticas que comprenden el inhibidor para uso en el tratamiento o prevencion de enfermedades cardiovasculares. |
| RU2715236C2 (ru) | 2014-03-26 | 2020-02-26 | Астекс Терапьютикс Лтд | Комбинации |
| HRP20210319T1 (hr) | 2014-03-26 | 2021-04-30 | Astex Therapeutics Ltd. | Kombinacije inhibitora fgfr i inhibitora igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| EP3174537B1 (en) | 2014-07-29 | 2021-06-23 | 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 |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| CN109996757A (zh) * | 2015-06-12 | 2019-07-09 | 罗地亚经营管理公司 | 含枝状体的混合纳米粒子、生产此类混合纳米粒子的方法以及它们的用途 |
| WO2017011279A1 (en) | 2015-07-13 | 2017-01-19 | Merck Sharp & Dohme Corp. | Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein |
| EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| US11155555B2 (en) | 2015-09-23 | 2021-10-26 | Janssen Pharmaceutica Nv | Compounds |
| 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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-
2012
- 2012-10-21 JO JOP/2012/0317A patent/JO3210B1/ar active
- 2012-10-25 KR KR1020147013895A patent/KR101686308B1/ko 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 US US13/660,010 patent/US8871738B2/en active Active
- 2012-10-25 SI SI201230757A patent/SI2771345T1/sl unknown
- 2012-10-25 IN IN3073CHN2014 patent/IN2014CN03073A/en unknown
- 2012-10-25 CN CN201280052931.5A patent/CN103958524B/zh not_active Expired - Fee Related
- 2012-10-25 LT LTEP12781551.2T patent/LT2771345T/lt unknown
- 2012-10-25 EP EP12781551.2A patent/EP2771345B1/en active Active
- 2012-10-25 ME MEP-2016-268A patent/ME02557B/me unknown
- 2012-10-25 SG SG11201401884PA patent/SG11201401884PA/en unknown
- 2012-10-25 PL PL12781551T patent/PL2771345T3/pl unknown
- 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 CA CA2852743A patent/CA2852743C/en not_active Expired - Fee Related
- 2012-10-25 EA EA201490889A patent/EA026123B1/ru not_active IP Right Cessation
- 2012-10-25 DK DK12781551.2T patent/DK2771345T3/en active
- 2012-10-25 RS RS20161003A patent/RS55420B1/sr unknown
- 2012-10-25 PT PT127815512T patent/PT2771345T/pt unknown
- 2012-10-25 HR HRP20161541TT patent/HRP20161541T1/hr unknown
- 2012-10-25 HU HUE12781551A patent/HUE030568T2/en unknown
- 2012-10-25 WO PCT/US2012/061842 patent/WO2013063217A1/en not_active Ceased
- 2012-10-25 ES ES12781551.2T patent/ES2604953T3/es active Active
- 2012-10-25 JP JP2014538988A patent/JP5658427B2/ja not_active Expired - Fee Related
- 2012-10-25 BR BR112014010204A patent/BR112014010204A2/pt not_active Application Discontinuation
- 2012-10-25 GE GEAP201213478A patent/GEP20166434B/en unknown
- 2012-10-25 UA UAA201405743A patent/UA114612C2/uk unknown
- 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
- 2014-04-22 CO CO14085787A patent/CO6940419A2/es active IP Right Grant
- 2014-04-25 ZA ZA2014/03091A patent/ZA201403091B/en unknown
- 2014-04-25 DO DO2014000086A patent/DOP2014000086A/es unknown
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
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