MX338024B - Derivado de dibencilamina opticamente activa y metodo para prepararla. - Google Patents
Derivado de dibencilamina opticamente activa y metodo para prepararla.Info
- Publication number
- MX338024B MX338024B MX2012014149A MX2012014149A MX338024B MX 338024 B MX338024 B MX 338024B MX 2012014149 A MX2012014149 A MX 2012014149A MX 2012014149 A MX2012014149 A MX 2012014149A MX 338024 B MX338024 B MX 338024B
- Authority
- MX
- Mexico
- Prior art keywords
- manufacturing
- same
- optically active
- derivative
- dibenzylamine derivative
- Prior art date
Links
- BWLUMTFWVZZZND-UHFFFAOYSA-N Dibenzylamine Chemical class C=1C=CC=CC=1CNCC1=CC=CC=C1 BWLUMTFWVZZZND-UHFFFAOYSA-N 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 101001098868 Homo sapiens Proprotein convertase subtilisin/kexin type 9 Proteins 0.000 abstract 1
- 102000000853 LDL receptors Human genes 0.000 abstract 1
- 108010001831 LDL receptors Proteins 0.000 abstract 1
- 102100038955 Proprotein convertase subtilisin/kexin type 9 Human genes 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- -1 {2-[({1-[3,5-bis(trifluoromethyl) phenyl] ethyl}{5-[2-(methylsulfonyl) ethoxy] pyrimidine-2-yl} amino) methyl]-4-(trifluoromethyl) phenyl} (ethyl) amino Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Virology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
El ácido (S)-trans-{4-[({2-[({1-[3,5-bis (trifluorometil) fenil] etil}{5-[2-(metilsulfonil)etoxi]pirimidin-2-il}amino)metil]-4-(tr ifluorometil)fenil} (etil)amino)metil]ciclohexil}acético sustancialmente ópticamente puro, o una sal de él o un solvato de él, que tiene acciones de reducción de la cantidad de proteína PCSK9 y aumento de la cantidad del receptor de LDL.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010128585 | 2010-06-04 | ||
| JP2010218299 | 2010-09-29 | ||
| PCT/JP2011/062751 WO2011152508A1 (ja) | 2010-06-04 | 2011-06-03 | 光学活性ジベンジルアミン誘導体及びその製造方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2012014149A MX2012014149A (es) | 2013-02-27 |
| MX338024B true MX338024B (es) | 2016-03-31 |
Family
ID=45066863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012014149A MX338024B (es) | 2010-06-04 | 2011-06-03 | Derivado de dibencilamina opticamente activa y metodo para prepararla. |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8906895B2 (es) |
| EP (1) | EP2578574B1 (es) |
| JP (1) | JP5555320B2 (es) |
| KR (2) | KR20130111512A (es) |
| CN (2) | CN102933559B (es) |
| AU (1) | AU2011259929B2 (es) |
| BR (1) | BR112012030787A2 (es) |
| CA (1) | CA2801417C (es) |
| EA (1) | EA024241B1 (es) |
| ES (1) | ES2581557T3 (es) |
| IL (1) | IL223377A (es) |
| IN (1) | IN2012CN10925A (es) |
| MX (1) | MX338024B (es) |
| PT (1) | PT2578574E (es) |
| TW (1) | TWI492749B (es) |
| WO (1) | WO2011152508A1 (es) |
| ZA (1) | ZA201209372B (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5793143B2 (ja) * | 2010-07-22 | 2015-10-14 | 興和株式会社 | 光学活性1−ブロモ−1−[3,5−ビス(トリフルオロメチル)フェニル]エタンの製造方法 |
| EP2626351A4 (en) * | 2010-10-04 | 2014-03-12 | Kowa Co | MEANS FOR INHIBITING THE EXPRESSION OF MRNA INVOLVED IN THE FAT REPLACEMENT |
| US20140303198A1 (en) * | 2011-11-29 | 2014-10-09 | Kowa Company, Ltd. | Agent for inhibiting expression of npc1l1 and/or lipg mrna and agent for preventing and/or treating obesity |
| TW201335109A (zh) * | 2011-12-02 | 2013-09-01 | Kowa Co | 光學活性化合物之製造方法 |
| WO2013137371A1 (ja) * | 2012-03-15 | 2013-09-19 | 興和株式会社 | 新規ピリミジン化合物及びそれらを含有する医薬 |
| US9255154B2 (en) | 2012-05-08 | 2016-02-09 | Alderbio Holdings, Llc | Anti-PCSK9 antibodies and use thereof |
| JP2016516804A (ja) | 2013-04-17 | 2016-06-09 | ファイザー・インク | 心血管疾患を治療するためのn−ピペリジン−3−イルベンズアミド誘導体 |
| KR20160014620A (ko) | 2013-05-31 | 2016-02-11 | 코와 가부시키가이샤 | 디벤질아민 구조를 갖는 피리미딘 화합물의 신규 형태 |
| US10034892B2 (en) * | 2014-08-21 | 2018-07-31 | Srx Cardio, Llc | Composition and methods of use of small molecules as binding ligands for the modulation of proprotein convertase subtilisin/kexin type 9(PCSK9) protein activity |
| TWI691331B (zh) * | 2014-09-26 | 2020-04-21 | 日商興和股份有限公司 | 脂質異常症治療劑 |
| WO2016084950A1 (ja) * | 2014-11-28 | 2016-06-02 | 興和株式会社 | 医薬組成物 |
| JPWO2016084949A1 (ja) * | 2014-11-28 | 2017-09-07 | 興和株式会社 | 医薬 |
| JP2019131472A (ja) * | 2016-05-31 | 2019-08-08 | 興和株式会社 | 医薬組成物 |
| HRP20241674T1 (hr) | 2019-01-18 | 2025-02-14 | Astrazeneca Ab | 6'-[[(1s,3s)-3-[[5-(difluormetoksi)-2-pirimidinil]amino]ciklopentil]amino][1(2h),3'-bipiridin]-2-on kao inhibitor pcsk9 i postupci njegove upotrebe |
| MX2021008661A (es) | 2019-01-18 | 2021-08-19 | Astrazeneca Ab | Inhibidores de la pcsk9 y metodos de uso de los mismos. |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5189208A (en) | 1991-07-01 | 1993-02-23 | Ethyl Corporation | Ibuprofen resolution |
| EA017321B1 (ru) | 2007-04-13 | 2012-11-30 | Кова Компани, Лтд. | Производные n,n-дибензил-2-аминопиримидина и лекарственные средства, их содержащие |
| US8673850B2 (en) * | 2008-05-30 | 2014-03-18 | Institut De Recherches Cliniques De Montreal | PCSK9 inhibitors and methods of use thereof |
| EP2626351A4 (en) | 2010-10-04 | 2014-03-12 | Kowa Co | MEANS FOR INHIBITING THE EXPRESSION OF MRNA INVOLVED IN THE FAT REPLACEMENT |
-
2011
- 2011-06-03 ES ES11789909.6T patent/ES2581557T3/es active Active
- 2011-06-03 TW TW100119614A patent/TWI492749B/zh not_active IP Right Cessation
- 2011-06-03 PT PT117899096T patent/PT2578574E/pt unknown
- 2011-06-03 BR BR112012030787-8A patent/BR112012030787A2/pt not_active IP Right Cessation
- 2011-06-03 JP JP2012518458A patent/JP5555320B2/ja not_active Expired - Fee Related
- 2011-06-03 AU AU2011259929A patent/AU2011259929B2/en not_active Ceased
- 2011-06-03 IN IN10925CHN2012 patent/IN2012CN10925A/en unknown
- 2011-06-03 MX MX2012014149A patent/MX338024B/es active IP Right Grant
- 2011-06-03 US US13/700,849 patent/US8906895B2/en not_active Expired - Fee Related
- 2011-06-03 KR KR1020137000104A patent/KR20130111512A/ko not_active Ceased
- 2011-06-03 CN CN201180027596.9A patent/CN102933559B/zh not_active Expired - Fee Related
- 2011-06-03 WO PCT/JP2011/062751 patent/WO2011152508A1/ja not_active Ceased
- 2011-06-03 KR KR1020177017703A patent/KR20170078865A/ko not_active Ceased
- 2011-06-03 EA EA201291447A patent/EA024241B1/ru not_active IP Right Cessation
- 2011-06-03 CA CA2801417A patent/CA2801417C/en not_active Expired - Fee Related
- 2011-06-03 CN CN201510015412.7A patent/CN104529910B/zh not_active Expired - Fee Related
- 2011-06-03 EP EP11789909.6A patent/EP2578574B1/en not_active Not-in-force
-
2012
- 2012-12-02 IL IL223377A patent/IL223377A/en active IP Right Grant
- 2012-12-11 ZA ZA2012/09372A patent/ZA201209372B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL223377A (en) | 2016-12-29 |
| BR112012030787A2 (pt) | 2020-09-01 |
| WO2011152508A1 (ja) | 2011-12-08 |
| KR20170078865A (ko) | 2017-07-07 |
| US20130225814A1 (en) | 2013-08-29 |
| TWI492749B (zh) | 2015-07-21 |
| EP2578574A1 (en) | 2013-04-10 |
| CN104529910A (zh) | 2015-04-22 |
| PT2578574E (pt) | 2016-06-17 |
| ES2581557T3 (es) | 2016-09-06 |
| IN2012CN10925A (es) | 2015-04-24 |
| HK1179959A1 (en) | 2013-10-11 |
| CN102933559B (zh) | 2016-01-27 |
| IL223377A0 (en) | 2013-03-05 |
| ZA201209372B (en) | 2014-02-26 |
| KR20130111512A (ko) | 2013-10-10 |
| TW201208688A (en) | 2012-03-01 |
| JP5555320B2 (ja) | 2014-07-23 |
| US8906895B2 (en) | 2014-12-09 |
| CN104529910B (zh) | 2017-05-10 |
| EA201291447A1 (ru) | 2013-05-30 |
| JPWO2011152508A1 (ja) | 2013-08-01 |
| EP2578574B1 (en) | 2016-04-27 |
| CA2801417A1 (en) | 2011-12-08 |
| EA024241B1 (ru) | 2016-08-31 |
| CN102933559A (zh) | 2013-02-13 |
| AU2011259929A1 (en) | 2013-01-17 |
| MX2012014149A (es) | 2013-02-27 |
| EP2578574A4 (en) | 2013-12-04 |
| AU2011259929B2 (en) | 2014-07-31 |
| CA2801417C (en) | 2017-07-11 |
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