AR088565A1 - Inhibidor de cetp de oxazolidinona biciclico fusionado - Google Patents
Inhibidor de cetp de oxazolidinona biciclico fusionadoInfo
- Publication number
- AR088565A1 AR088565A1 ARP120104037A ARP120104037A AR088565A1 AR 088565 A1 AR088565 A1 AR 088565A1 AR P120104037 A ARP120104037 A AR P120104037A AR P120104037 A ARP120104037 A AR P120104037A AR 088565 A1 AR088565 A1 AR 088565A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkynyl
- alkenyl
- optionally substituted
- halogens
- Prior art date
Links
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 title 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 title 1
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 25
- 150000002367 halogens Chemical class 0.000 abstract 25
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 abstract 24
- 125000003342 alkenyl group Chemical group 0.000 abstract 18
- 125000000304 alkynyl group Chemical group 0.000 abstract 18
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 9
- 125000002947 alkylene group Chemical group 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- -1 -OH Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Vascular Medicine (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 (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552592P | 2011-10-28 | 2011-10-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088565A1 true AR088565A1 (es) | 2014-06-18 |
Family
ID=47143312
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120104037A AR088565A1 (es) | 2011-10-28 | 2012-10-26 | Inhibidor de cetp de oxazolidinona biciclico fusionado |
Country Status (41)
Families Citing this family (34)
| 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 |
| 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 |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (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 |
| US9493430B2 (en) * | 2013-01-31 | 2016-11-15 | Chong Kun Dang Pharmaceutical Corp. | Biaryl- or heterocyclic biaryl-substituted cyclohexene derivative compounds as CETP inhibitors |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US9981970B2 (en) | 2013-07-30 | 2018-05-29 | 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 |
| 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 |
| 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 |
| KR102479693B1 (ko) | 2014-03-26 | 2022-12-22 | 아스텍스 테라퓨틱스 리미티드 | 조합물 |
| RU2715893C2 (ru) | 2014-03-26 | 2020-03-04 | Астекс Терапьютикс Лтд | Комбинации ингибитора fgfr и ингибитора igf1r |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| 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 |
| US20170252338A1 (en) * | 2014-11-28 | 2017-09-07 | Kowa Company, Ltd. | Medicine |
| 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 |
| US10207919B2 (en) * | 2015-06-12 | 2019-02-19 | Rhodia Operations | Hybrid nanoparticles containing dendrons, methods of producing such hybrid nanoparticles, and uses thereof |
| US20180230166A1 (en) * | 2015-07-13 | 2018-08-16 | Merck Sharp & Dohme Corp. | Bicyclic heterocycles as inhibitors of cholesterol ester transfer protein |
| CN108137546B (zh) | 2015-09-23 | 2021-07-27 | 詹森药业有限公司 | 双杂芳基取代的1,4-苯并二氮杂卓化合物及其用于治疗癌症的用途 |
| DK3353177T3 (da) | 2015-09-23 | 2020-08-24 | Janssen Pharmaceutica Nv | Tricykliske heterocykler til behandling af cancer |
| 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 |
| 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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| AU2005233160B2 (en) * | 2004-04-13 | 2011-06-02 | Merck Sharp & Dohme Corp. | CETP inhibitors |
| DOP2005000123A (es) | 2004-07-02 | 2011-07-15 | Merck Sharp & Dohme | Inhibidores de cetp |
| AR058400A1 (es) | 2005-12-22 | 2008-01-30 | Schering Corp | Derivados de oxazoloisoquinolina como antagonistas del receptor de trombina |
| US7910592B2 (en) | 2005-12-30 | 2011-03-22 | Merck Sharp & Dohme Corp. | CETP inhibitors |
| JP5040036B2 (ja) | 2005-12-30 | 2012-10-03 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｃｅｔｐ阻害剤として有用な１，３−オキサゾリジン−２−オン誘導体 |
| JP5199121B2 (ja) * | 2005-12-30 | 2013-05-15 | メルク・シャープ・エンド・ドーム・コーポレイション | Ｃｅｔｐ阻害剤 |
| EP2348859B1 (en) * | 2008-10-01 | 2013-12-04 | Merck Sharp & Dohme Corp. | Prodrugs of oxazolidinone cetp inhibitors |
| WO2011028395A1 (en) | 2009-08-24 | 2011-03-10 | Merck Sharp & Dohme Corp. | Pyridyl oxazolidinone cetp inhibitor |
| 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 |
| US9353101B2 (en) | 2012-05-02 | 2016-05-31 | Merck Sharp & Dohme Corp. | Cyclic amine substituted heterocyclic CETP inhibitors |
-
2012
- 2012-10-21 JO JOP/2012/0317A patent/JO3210B1/ar active
- 2012-10-25 GE GEAP201213478A patent/GEP20166434B/en unknown
- 2012-10-25 PL PL12781551T patent/PL2771345T3/pl unknown
- 2012-10-25 RS RS20161003A patent/RS55420B1/sr unknown
- 2012-10-25 ES ES12781551.2T patent/ES2604953T3/es active Active
- 2012-10-25 WO PCT/US2012/061842 patent/WO2013063217A1/en not_active Ceased
- 2012-10-25 DK DK12781551.2T patent/DK2771345T3/en active
- 2012-10-25 US US13/660,010 patent/US8871738B2/en active Active
- 2012-10-25 PH PH1/2014/500890A patent/PH12014500890A1/en unknown
- 2012-10-25 AU AU2012328759A patent/AU2012328759B2/en not_active Ceased
- 2012-10-25 MX MX2014005074A patent/MX345222B/es active IP Right Grant
- 2012-10-25 CN CN201280052931.5A patent/CN103958524B/zh not_active Expired - Fee Related
- 2012-10-25 HU HUE12781551A patent/HUE030568T2/en unknown
- 2012-10-25 KR KR1020147013895A patent/KR101686308B1/ko not_active Expired - Fee Related
- 2012-10-25 PE PE2014000616A patent/PE20141230A1/es not_active Application Discontinuation
- 2012-10-25 SG SG11201401884PA patent/SG11201401884PA/en unknown
- 2012-10-25 PT PT127815512T patent/PT2771345T/pt unknown
- 2012-10-25 SI SI201230757A patent/SI2771345T1/sl unknown
- 2012-10-25 LT LTEP12781551.2T patent/LT2771345T/lt unknown
- 2012-10-25 EA EA201490889A patent/EA026123B1/ru not_active IP Right Cessation
- 2012-10-25 UA UAA201405743A patent/UA114612C2/uk unknown
- 2012-10-25 CA CA2852743A patent/CA2852743C/en not_active Expired - Fee Related
- 2012-10-25 ME MEP-2016-268A patent/ME02557B/me unknown
- 2012-10-25 JP JP2014538988A patent/JP5658427B2/ja not_active Expired - Fee Related
- 2012-10-25 IN IN3073CHN2014 patent/IN2014CN03073A/en unknown
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2014
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2016
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