ES2665461T3 - Moduladores del receptor esfingosina 1-fosfato y métodos de síntesis quiral - Google Patents
Moduladores del receptor esfingosina 1-fosfato y métodos de síntesis quiral Download PDFInfo
- Publication number
- ES2665461T3 ES2665461T3 ES10830877.6T ES10830877T ES2665461T3 ES 2665461 T3 ES2665461 T3 ES 2665461T3 ES 10830877 T ES10830877 T ES 10830877T ES 2665461 T3 ES2665461 T3 ES 2665461T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- independently
- cooh
- coor1
- optionally substituted
- 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.)
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- 229940127530 Sphingosine 1-Phosphate Receptor Modulators Drugs 0.000 title 1
- 238000001308 synthesis method Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract description 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 abstract 4
- 125000001963 4 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000002883 imidazolyl group Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002393 azetidinyl group Chemical group 0.000 abstract 1
- -1 benzoimidazolyl Chemical group 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
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 description 13
- OHCQJHSOBUTRHG-KGGHGJDLSA-N FORSKOLIN Chemical compound O=C([C@@]12O)C[C@](C)(C=C)O[C@]1(C)[C@@H](OC(=O)C)[C@@H](O)[C@@H]1[C@]2(C)[C@@H](O)CCC1(C)C OHCQJHSOBUTRHG-KGGHGJDLSA-N 0.000 description 10
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 description 10
- 230000000694 effects Effects 0.000 description 9
- 210000004027 cell Anatomy 0.000 description 8
- SUZLHDUTVMZSEV-UHFFFAOYSA-N Deoxycoleonol Natural products C12C(=O)CC(C)(C=C)OC2(C)C(OC(=O)C)C(O)C2C1(C)C(O)CCC2(C)C SUZLHDUTVMZSEV-UHFFFAOYSA-N 0.000 description 5
- OHCQJHSOBUTRHG-UHFFFAOYSA-N colforsin Natural products OC12C(=O)CC(C)(C=C)OC1(C)C(OC(=O)C)C(O)C1C2(C)C(O)CCC1(C)C OHCQJHSOBUTRHG-UHFFFAOYSA-N 0.000 description 5
- 101000693265 Homo sapiens Sphingosine 1-phosphate receptor 1 Proteins 0.000 description 4
- 239000000556 agonist Substances 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- ZZMYWYZPNZRYPX-SANMLTNESA-N (2r)-2-amino-2-[5-[4-[2-(4-phenylphenyl)ethoxy]-3-(trifluoromethyl)phenyl]-1h-imidazol-2-yl]propan-1-ol Chemical compound N1C([C@@](N)(CO)C)=NC=C1C(C=C1C(F)(F)F)=CC=C1OCCC1=CC=C(C=2C=CC=CC=2)C=C1 ZZMYWYZPNZRYPX-SANMLTNESA-N 0.000 description 2
- JKMHFZQWWAIEOD-UHFFFAOYSA-N 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid Chemical compound OCC[NH+]1CCN(CCS([O-])(=O)=O)CC1 JKMHFZQWWAIEOD-UHFFFAOYSA-N 0.000 description 2
- 102100029802 Sphingosine 1-phosphate receptor 5 Human genes 0.000 description 2
- 101710155451 Sphingosine 1-phosphate receptor 5 Proteins 0.000 description 2
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 description 2
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 description 2
- 238000003556 assay Methods 0.000 description 2
- 238000002866 fluorescence resonance energy transfer Methods 0.000 description 2
- 230000014509 gene expression Effects 0.000 description 2
- 230000001404 mediated effect Effects 0.000 description 2
- 238000005400 testing for adjacent nuclei with gyration operator Methods 0.000 description 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- 229920002307 Dextran Polymers 0.000 description 1
- 108090000204 Dipeptidase 1 Proteins 0.000 description 1
- 239000007995 HEPES buffer Substances 0.000 description 1
- 101001021281 Homo sapiens Protein HEXIM1 Proteins 0.000 description 1
- 102100025749 Sphingosine 1-phosphate receptor 2 Human genes 0.000 description 1
- 101710155462 Sphingosine 1-phosphate receptor 2 Proteins 0.000 description 1
- 102100029803 Sphingosine 1-phosphate receptor 4 Human genes 0.000 description 1
- 101710155458 Sphingosine 1-phosphate receptor 4 Proteins 0.000 description 1
- 125000003275 alpha amino acid group Chemical group 0.000 description 1
- 102000006635 beta-lactamase Human genes 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 239000002299 complementary DNA Substances 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000013613 expression plasmid Substances 0.000 description 1
- 238000001943 fluorescence-activated cell sorting Methods 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 239000002773 nucleotide Substances 0.000 description 1
- 125000003729 nucleotide group Chemical group 0.000 description 1
- 229920001992 poloxamer 407 Polymers 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 238000011282 treatment Methods 0.000 description 1
Classifications
-
- 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
- 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
- A61K31/445—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
-
- 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
- A61K31/535—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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Immunology (AREA)
- Virology (AREA)
- Pulmonology (AREA)
- Transplantation (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (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)
- Hydrogenated Pyridines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US26128209P | 2009-11-13 | 2009-11-13 | |
| US261282P | 2009-11-13 | ||
| US26247409P | 2009-11-18 | 2009-11-18 | |
| US262474P | 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2665461T3 true ES2665461T3 (es) | 2018-04-25 |
Family
ID=43992104
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10830877.6T Active ES2665461T3 (es) | 2009-11-13 | 2010-11-15 | Moduladores del receptor esfingosina 1-fosfato y métodos de síntesis quiral |
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 (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112012011430A8 (pt) | 2009-11-13 | 2017-12-26 | Celgene Int Ii Sarl | Compostos moduladores de receptor de esfingosina 1 fosfato e composições farmacêuticas |
| HUE037535T2 (hu) * | 2009-11-13 | 2018-09-28 | Celgene Int Ii Sarl | Szelektív szfingozin-1-foszfát receptor modulátorok és királis szintézis eljárások |
| ES2758841T3 (es) | 2011-05-13 | 2020-05-06 | Celgene Int Ii Sarl | Moduladores heterocíclicos selectivos del receptor de la esfingosina-1-fosfato |
| 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 |
| AU2013346882B2 (en) | 2012-11-16 | 2017-05-04 | F. Hoffmann-La Roche Ag | Process for the preparation of 2-trifluoromethyl isonicotinic acid and esters |
| EP2958913B1 (en) | 2013-02-20 | 2018-10-03 | LG Chem, Ltd. | Sphingosine-1-phosphate receptor agonists, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent |
| WO2015066515A1 (en) * | 2013-11-01 | 2015-05-07 | Receptos, Inc. | Selective sphingosine 1 phosphate receptor modulators and combination therapy therewith |
| WO2017083756A1 (en) | 2015-11-13 | 2017-05-18 | Oppilan Pharma Ltd. | Heterocyclic compounds for the treatment of disease |
| CA3009428A1 (en) * | 2015-12-22 | 2017-06-29 | AbbVie Deutschland GmbH & Co. KG | Fused (hetero)cyclic compounds as s1p modulators |
| WO2017190107A1 (en) * | 2016-04-29 | 2017-11-02 | Board Of Regents, The University Of Texas System | Sigma receptor binders |
| WO2018014862A1 (zh) * | 2016-07-22 | 2018-01-25 | 南京明德新药研发股份有限公司 | S1p1激动剂及其应用 |
| 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 |
| CN110256288A (zh) * | 2019-05-13 | 2019-09-20 | 苏州山青竹生物医药有限公司 | 一种制备(s)-1-氨基-2,3-二氢-1h-茚-4-甲腈的方法 |
| CN112062785B (zh) * | 2019-06-11 | 2023-06-27 | 广东东阳光药业有限公司 | 奥扎莫德及其中间体的制备方法 |
| KR20220124209A (ko) * | 2020-01-06 | 2022-09-13 | 아레나 파마슈티칼스, 인크. | S1p1 수용체와 관련된 이상의 치료 방법 |
| EP4101445B1 (en) | 2020-02-06 | 2025-04-30 | Mitsubishi Tanabe Pharma Corporation | Amiselimod for use in the treatment of myalgic encephalomyelitis/chronic fatigue syndrome |
| WO2021175225A1 (zh) * | 2020-03-04 | 2021-09-10 | 南京明德新药研发有限公司 | 三环类化合物及其应用 |
| WO2024246174A1 (en) | 2023-05-31 | 2024-12-05 | Química Sintética, S.A. | Amorphous and crystalline form of ozanimod hydrochloride |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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| FR2628103B1 (fr) | 1988-03-03 | 1991-06-14 | Roussel Uclaf | Nouveaux esters pyrethrinoides portant un noyau indanyle, leur procede de preparation et leur application comme pesticides |
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| JPH0825973B2 (ja) * | 1991-04-12 | 1996-03-13 | シェリング・コーポレーション | アシル補酵素ａ：コレステロールアシルトランスフェラーゼの阻害剤としての二環式アミド |
| GB2290790A (en) * | 1994-06-30 | 1996-01-10 | Merck & Co Inc | Asymmetric synthesis of 6-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes |
| TR200002072T2 (tr) | 1998-01-23 | 2000-12-21 | Sankyo Company Limited | Spiropiperidin türevleri |
| US20040058894A1 (en) | 2002-01-18 | 2004-03-25 | Doherty George A. | Selective S1P1/Edg1 receptor agonists |
| CA2509218C (en) * | 2002-12-20 | 2010-09-07 | Merck & Co., Inc. | 1-(amino)indanes and (1,2-dihydro-3-amino)-benzofurans, benzothiophenes and indoles as edg receptor agonists |
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| AU2004277947A1 (en) | 2003-10-01 | 2005-04-14 | Merck & Co., Inc. | 3,5-aryl, heteroaryl or cycloalkyl substituted-1,2,4-oxadiazoles as S1P receptor agonists |
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| EP1851188A1 (en) * | 2005-02-22 | 2007-11-07 | Teva Pharmaceutical Industries Limited | Improved process for the synthesis of enantiomeric indanylamine derivatives |
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| BR112012011430A8 (pt) | 2009-11-13 | 2017-12-26 | Celgene Int Ii Sarl | Compostos moduladores de receptor de esfingosina 1 fosfato e composições farmacêuticas |
| HUE037535T2 (hu) | 2009-11-13 | 2018-09-28 | Celgene Int Ii Sarl | Szelektív szfingozin-1-foszfát receptor modulátorok és királis szintézis eljárások |
| CN105130922A (zh) | 2009-11-13 | 2015-12-09 | 瑞塞普托斯公司 | 选择性的杂环1-磷酸鞘氨醇受体调节剂 |
| SG11201401330YA (en) | 2011-10-12 | 2014-05-29 | Teva Pharma | Treatment of multiple sclerosis with combination of laquinimod and fingolimod |
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2010
- 2010-11-15 BR BR112012011430A patent/BR112012011430A8/pt not_active Application Discontinuation
- 2010-11-15 CN CN201080061143.3A patent/CN102724880B/zh active Active
- 2010-11-15 EP EP10830877.6A patent/EP2498611B1/en active Active
- 2010-11-15 US US12/946,800 patent/US8357706B2/en active Active
- 2010-11-15 MY MYPI2012002085A patent/MY160907A/en unknown
- 2010-11-15 ES ES10830877.6T patent/ES2665461T3/es active Active
- 2010-11-15 JP JP2012539063A patent/JP5988379B2/ja active Active
- 2010-11-15 LT LTEP10830877.6T patent/LT2498611T/lt unknown
- 2010-11-15 DK DK10830877.6T patent/DK2498611T3/en active
- 2010-11-15 WO PCT/US2010/056757 patent/WO2011060389A1/en not_active Ceased
- 2010-11-15 PT PT108308776T patent/PT2498611T/pt unknown
- 2010-11-15 PL PL10830877T patent/PL2498611T3/pl unknown
- 2010-11-15 RS RS20180389A patent/RS57070B1/sr unknown
- 2010-11-15 NZ NZ599913A patent/NZ599913A/en unknown
- 2010-11-15 KR KR1020127015219A patent/KR101781233B1/ko active Active
- 2010-11-15 MX MX2012005562A patent/MX2012005562A/es active IP Right Grant
- 2010-11-15 HU HUE10830877A patent/HUE036391T2/hu unknown
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- 2010-11-15 CA CA2780433A patent/CA2780433C/en active Active
- 2010-11-15 AU AU2010320041A patent/AU2010320041B2/en active Active
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- 2012-05-09 IL IL219690A patent/IL219690B/en active IP Right Grant
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