JP5988379B2 - スフィンゴシン−１−リン酸受容体変調因子および不斉合成方法 - Google Patents
スフィンゴシン−１−リン酸受容体変調因子および不斉合成方法 Download PDFInfo
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- JP5988379B2 JP5988379B2 JP2012539063A JP2012539063A JP5988379B2 JP 5988379 B2 JP5988379 B2 JP 5988379B2 JP 2012539063 A JP2012539063 A JP 2012539063A JP 2012539063 A JP2012539063 A JP 2012539063A JP 5988379 B2 JP5988379 B2 JP 5988379B2
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- 0 *c(c(O)ccc1)c1O Chemical compound *c(c(O)ccc1)c1O 0.000 description 6
- ULFIAFQQKNGMNA-UHFFFAOYSA-N CC(C)OC(C(C#N)=C1)=CCC1c1nc(-c(c2c3CCCC2)ccc3[O]=S(CCOC)(N)O)n[o]1 Chemical compound CC(C)OC(C(C#N)=C1)=CCC1c1nc(-c(c2c3CCCC2)ccc3[O]=S(CCOC)(N)O)n[o]1 ULFIAFQQKNGMNA-UHFFFAOYSA-N 0.000 description 1
- RZHAJSSBJMNRQF-MEFGMAGPSA-N CC(C)OC(C(C1)C#N)=CC=C1c1nc(-c2c(CCC/C3=N/C(COC)=O)c3ccc2)n[o]1 Chemical compound CC(C)OC(C(C1)C#N)=CC=C1c1nc(-c2c(CCC/C3=N/C(COC)=O)c3ccc2)n[o]1 RZHAJSSBJMNRQF-MEFGMAGPSA-N 0.000 description 1
- URNODGRGHQLPCI-UHFFFAOYSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c(c(CCC2)c3C2N2)ccc3[O]=S2(CCN(C)C)=O)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c(c(CCC2)c3C2N2)ccc3[O]=S2(CCN(C)C)=O)n[o]1 URNODGRGHQLPCI-UHFFFAOYSA-N 0.000 description 1
- WBZRGEDTTLHOBQ-QLYXXIJNSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2c(CCC/C3=N/CCO)c3ccc2)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2c(CCC/C3=N/CCO)c3ccc2)n[o]1 WBZRGEDTTLHOBQ-QLYXXIJNSA-N 0.000 description 1
- GFSDOTNHWQHHFQ-NRFANRHFSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2c(CCC[C@@H]3NC(C)=O)c3ccc2)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2c(CCC[C@@H]3NC(C)=O)c3ccc2)n[o]1 GFSDOTNHWQHHFQ-NRFANRHFSA-N 0.000 description 1
- BDBWZMJLGMRPJF-UHFFFAOYSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCCC3NCC(O)=O)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCCC3NCC(O)=O)n[o]1 BDBWZMJLGMRPJF-UHFFFAOYSA-N 0.000 description 1
- MVTYQLFUYSBUQE-DEOSSOPVSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCC[C@@H]3N(CC(OC)=O)C(OC(C)(C)C)=O)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCC[C@@H]3N(CC(OC)=O)C(OC(C)(C)C)=O)n[o]1 MVTYQLFUYSBUQE-DEOSSOPVSA-N 0.000 description 1
- WKQXDSRICDOGLX-NRFANRHFSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCC[C@@H]3NCCS=O)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(-c2cccc3c2CCC[C@@H]3NCCS=O)n[o]1 WKQXDSRICDOGLX-NRFANRHFSA-N 0.000 description 1
- WHQTZBYFEJNIKT-GLCUGAKSSA-N CC(C)Oc(c(C#N)c1)ccc1-c1nc(C(C2CCC3)C=CCC2[C@@H]3N)n[o]1 Chemical compound CC(C)Oc(c(C#N)c1)ccc1-c1nc(C(C2CCC3)C=CCC2[C@@H]3N)n[o]1 WHQTZBYFEJNIKT-GLCUGAKSSA-N 0.000 description 1
- CHEWDTSTFRLQEW-AQTVZULBSA-N CC(C)Oc(ccc(-c1nc(-c2cccc3c2CCCC3NS(CCC(CCC2)[C@H](C)C[C@@H]2O)(=O)=O)n[o]1)c1)c1C#N Chemical compound CC(C)Oc(ccc(-c1nc(-c2cccc3c2CCCC3NS(CCC(CCC2)[C@H](C)C[C@@H]2O)(=O)=O)n[o]1)c1)c1C#N CHEWDTSTFRLQEW-AQTVZULBSA-N 0.000 description 1
- VQKVMHGHSKLHJK-UHFFFAOYSA-N CC(C)Oc(ccc(-c1nc(-c2ccnc(CO)c2)n[o]1)c1)c1C#N Chemical compound CC(C)Oc(ccc(-c1nc(-c2ccnc(CO)c2)n[o]1)c1)c1C#N VQKVMHGHSKLHJK-UHFFFAOYSA-N 0.000 description 1
- LICQOMGJILFGPK-UHFFFAOYSA-N CC(C)Oc(ccc(-c1ncc(-c2c(CCC3NCCO)c3ccc2)[o]1)c1)c1C#N Chemical compound CC(C)Oc(ccc(-c1ncc(-c2c(CCC3NCCO)c3ccc2)[o]1)c1)c1C#N LICQOMGJILFGPK-UHFFFAOYSA-N 0.000 description 1
- BJSVUUUXVSJMIW-UHFFFAOYSA-N CC(C)Oc(ccc(-c1ncc(-c2c(CCC3O)c3ccc2)[o]1)c1)c1C#N Chemical compound CC(C)Oc(ccc(-c1ncc(-c2c(CCC3O)c3ccc2)[o]1)c1)c1C#N BJSVUUUXVSJMIW-UHFFFAOYSA-N 0.000 description 1
- SCTBWJINDJVNDM-UHFFFAOYSA-N N#Cc1c(CCC2=O)c2ccc1 Chemical compound N#Cc1c(CCC2=O)c2ccc1 SCTBWJINDJVNDM-UHFFFAOYSA-N 0.000 description 1
- VIHLGHRPFVEQBU-UHFFFAOYSA-N N#Cc1c(CCCC2=O)c2ccc1 Chemical compound N#Cc1c(CCCC2=O)c2ccc1 VIHLGHRPFVEQBU-UHFFFAOYSA-N 0.000 description 1
- MEFZMTYUOQFQHF-UHFFFAOYSA-N N#Cc1cccc2c1CCC2O Chemical compound N#Cc1cccc2c1CCC2O MEFZMTYUOQFQHF-UHFFFAOYSA-N 0.000 description 1
- DZCSWIQGBIAWSF-UHFFFAOYSA-O N=C(c1c(CCC2O)c2ccc1)N[OH2+] Chemical compound N=C(c1c(CCC2O)c2ccc1)N[OH2+] DZCSWIQGBIAWSF-UHFFFAOYSA-O 0.000 description 1
- RPHKINMPYFJSCF-UHFFFAOYSA-N Nc1cc(N)cc(N)c1 Chemical compound Nc1cc(N)cc(N)c1 RPHKINMPYFJSCF-UHFFFAOYSA-N 0.000 description 1
- UVVYFYLSZIMKMC-UHFFFAOYSA-N O=C(CC1)c2c1c(Br)ccc2 Chemical compound O=C(CC1)c2c1c(Br)ccc2 UVVYFYLSZIMKMC-UHFFFAOYSA-N 0.000 description 1
- YNYDFXYUVDPNAU-LRTDYKAYSA-N OCCN[C@H](CC1)C(CC=C2)C1=C2c1n[o]c(-c2cc(-c3ccccc3)c(C(F)(F)F)[s]2)n1 Chemical compound OCCN[C@H](CC1)C(CC=C2)C1=C2c1n[o]c(-c2cc(-c3ccccc3)c(C(F)(F)F)[s]2)n1 YNYDFXYUVDPNAU-LRTDYKAYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
- C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
-
- 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
- A61K31/4245—Oxadiazoles
-
- A—HUMAN NECESSITIES
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- 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
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Virology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26128209P | 2009-11-13 | 2009-11-13 | |
| US61/261,282 | 2009-11-13 | ||
| US26247409P | 2009-11-18 | 2009-11-18 | |
| US61/262,474 | 2009-11-18 | ||
| PCT/US2010/056757 WO2011060389A1 (en) | 2009-11-13 | 2010-11-15 | Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510883A JP2013510883A (ja) | 2013-03-28 |
| JP2013510883A5 JP2013510883A5 (enExample) | 2014-01-09 |
| JP5988379B2 true JP5988379B2 (ja) | 2016-09-07 |
Family
ID=43992104
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012539063A Active JP5988379B2 (ja) | 2009-11-13 | 2010-11-15 | スフィンゴシン−１−リン酸受容体変調因子および不斉合成方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US8357706B2 (enExample) |
| EP (1) | EP2498611B1 (enExample) |
| JP (1) | JP5988379B2 (enExample) |
| KR (1) | KR101781233B1 (enExample) |
| CN (1) | CN102724880B (enExample) |
| AU (1) | AU2010320041B2 (enExample) |
| BR (1) | BR112012011430A8 (enExample) |
| CA (1) | CA2780433C (enExample) |
| CY (1) | CY1120427T1 (enExample) |
| DK (1) | DK2498611T3 (enExample) |
| EA (1) | EA023183B1 (enExample) |
| ES (1) | ES2665461T3 (enExample) |
| HR (1) | HRP20180527T1 (enExample) |
| HU (1) | HUE036391T2 (enExample) |
| IL (1) | IL219690B (enExample) |
| LT (1) | LT2498611T (enExample) |
| MX (1) | MX2012005562A (enExample) |
| MY (1) | MY160907A (enExample) |
| NZ (1) | NZ599913A (enExample) |
| PH (1) | PH12012500938A1 (enExample) |
| PL (1) | PL2498611T3 (enExample) |
| PT (1) | PT2498611T (enExample) |
| RS (1) | RS57070B1 (enExample) |
| SI (1) | SI2498611T1 (enExample) |
| WO (1) | WO2011060389A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2498610T5 (pl) * | 2009-11-13 | 2024-11-04 | Receptos Llc | Selektywne modulatory receptora sfingozyno-1-fosforanu i sposoby syntezy chiralnej |
| HUE036391T2 (hu) | 2009-11-13 | 2018-07-30 | Celgene Int Ii Sarl | Szfingozin 1 foszfát receptor modulátorok és királis szintézis eljárások |
| US9481659B2 (en) | 2011-05-13 | 2016-11-01 | Celgene International Ii Sàrl | Selective heterocyclic sphingosine 1 phosphate receptor modulators |
| CN103251950B (zh) * | 2012-02-16 | 2018-10-02 | 中国人民解放军军事科学院军事医学研究院辐射医学研究所 | S1p受体调节剂防治肠型放射病及放射性肠炎的用途 |
| CN104781236B (zh) | 2012-11-16 | 2018-04-24 | 霍夫曼-拉罗奇有限公司 | 制备2-三氟甲基异烟酸和酯的方法 |
| HUE039931T2 (hu) | 2013-02-20 | 2019-02-28 | Lg Chemical Ltd | Szfingozin-1-foszfát receptor agonisták, azok elkészítési eljárásai, és azokat aktív ágensként tartalmazó gyógyszerészeti készítmények |
| WO2015066515A1 (en) * | 2013-11-01 | 2015-05-07 | Receptos, Inc. | Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith |
| HRP20221417T1 (hr) | 2015-11-13 | 2023-02-03 | Oppilan Pharma Ltd. | Heterociklički spojevi za liječenje bolesti |
| US10280159B2 (en) * | 2015-12-22 | 2019-05-07 | AbbVie Deutschland GmbH & Co. KG | Fused (hetero)cyclic compounds as S1P modulators |
| CA3022432A1 (en) * | 2016-04-29 | 2017-11-02 | Board Of Regents, The University Of Texas System | Sigma receptor binders |
| RU2754845C2 (ru) * | 2016-07-22 | 2021-09-08 | Медшайн Дискавери Инк. | Агонист s1p1 и его применение |
| CN106749213B (zh) * | 2016-11-25 | 2019-07-02 | 济南大学 | 一种具有1,2,4-恶二唑结构的吲哚衍生物及制备方法和在制备抗菌药物中的应用 |
| CN108727292A (zh) * | 2017-04-21 | 2018-11-02 | 宁波爱诺医药科技有限公司 | 一种奥扎莫德及其中间体的制备方法 |
| CN108727291A (zh) * | 2017-04-21 | 2018-11-02 | 宁波爱诺医药科技有限公司 | 奥扎莫德及其中间体的制备方法 |
| AR116479A1 (es) | 2018-09-25 | 2021-05-12 | Quim Sintetica S A | Intermediarios para la síntesis de ozanimod y procedimiento para la preparación del mencionado agonista del receptor de esfingosina-1-fosfato y de dichos intermediarios |
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