BR112019018894A2 - combinação farmacêutica compreendendo ponesimod - Google Patents
combinação farmacêutica compreendendo ponesimod Download PDFInfo
- Publication number
- BR112019018894A2 BR112019018894A2 BR112019018894A BR112019018894A BR112019018894A2 BR 112019018894 A2 BR112019018894 A2 BR 112019018894A2 BR 112019018894 A BR112019018894 A BR 112019018894A BR 112019018894 A BR112019018894 A BR 112019018894A BR 112019018894 A2 BR112019018894 A2 BR 112019018894A2
- Authority
- BR
- Brazil
- Prior art keywords
- ponesimod
- pharmaceutical composition
- pharmaceutical
- teriflunomide
- combination
- Prior art date
Links
- 229950009275 ponesimod Drugs 0.000 title claims abstract description 58
- LPAUOXUZGSBGDU-STDDISTJSA-N chembl1096146 Chemical compound O=C1N(C=2C(=CC=CC=2)C)C(=N/CCC)/S\C1=C/C1=CC=C(OC[C@H](O)CO)C(Cl)=C1 LPAUOXUZGSBGDU-STDDISTJSA-N 0.000 title claims abstract description 57
- 239000004480 active ingredient Substances 0.000 claims abstract description 77
- UTNUDOFZCWSZMS-YFHOEESVSA-N teriflunomide Chemical compound C\C(O)=C(/C#N)C(=O)NC1=CC=C(C(F)(F)F)C=C1 UTNUDOFZCWSZMS-YFHOEESVSA-N 0.000 claims abstract description 53
- 229960000331 teriflunomide Drugs 0.000 claims abstract description 51
- VHOGYURTWQBHIL-UHFFFAOYSA-N leflunomide Chemical compound O1N=CC(C(=O)NC=2C=CC(=CC=2)C(F)(F)F)=C1C VHOGYURTWQBHIL-UHFFFAOYSA-N 0.000 claims abstract description 37
- 229960000681 leflunomide Drugs 0.000 claims abstract description 36
- 239000008194 pharmaceutical composition Substances 0.000 claims description 77
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 44
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 29
- 201000010099 disease Diseases 0.000 claims description 26
- 239000003814 drug Substances 0.000 claims description 22
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- 229940126601 medicinal product Drugs 0.000 claims 1
- 150000003839 salts Chemical group 0.000 description 16
- 238000002474 experimental method Methods 0.000 description 10
- 150000001875 compounds Chemical class 0.000 description 9
- 241000700159 Rattus Species 0.000 description 8
- 230000000306 recurrent effect Effects 0.000 description 8
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- 230000001154 acute effect Effects 0.000 description 6
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- 206010039073 rheumatoid arthritis Diseases 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 3
- 208000009329 Graft vs Host Disease Diseases 0.000 description 3
- 201000004681 Psoriasis Diseases 0.000 description 3
- 230000001363 autoimmune Effects 0.000 description 3
- 229910052805 deuterium Inorganic materials 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 208000024908 graft versus host disease Diseases 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 238000012423 maintenance Methods 0.000 description 3
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- 238000012360 testing method Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- -1 2,3-dihydroxy-propoxy Chemical group 0.000 description 2
- KISWVXRQTGLFGD-UHFFFAOYSA-N 2-[[2-[[6-amino-2-[[2-[[2-[[5-amino-2-[[2-[[1-[2-[[6-amino-2-[(2,5-diamino-5-oxopentanoyl)amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-(diaminomethylideneamino)p Chemical compound C1CCN(C(=O)C(CCCN=C(N)N)NC(=O)C(CCCCN)NC(=O)C(N)CCC(N)=O)C1C(=O)NC(CO)C(=O)NC(CCC(N)=O)C(=O)NC(CCCN=C(N)N)C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(C(=O)NC(CC(C)C)C(O)=O)CC1=CC=C(O)C=C1 KISWVXRQTGLFGD-UHFFFAOYSA-N 0.000 description 2
- 208000023275 Autoimmune disease Diseases 0.000 description 2
- 208000011231 Crohn disease Diseases 0.000 description 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 description 2
- 238000012313 Kruskal-Wallis test Methods 0.000 description 2
- 241000699670 Mus sp. Species 0.000 description 2
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- 210000003734 kidney Anatomy 0.000 description 2
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- 239000002207 metabolite Substances 0.000 description 2
- 229920000609 methyl cellulose Polymers 0.000 description 2
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- 239000007787 solid Substances 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- LPAUOXUZGSBGDU-ULCCENQXSA-N (5z)-5-[[3-chloro-4-[(2r)-2,3-dihydroxypropoxy]phenyl]methylidene]-3-(2-methylphenyl)-2-propylimino-1,3-thiazolidin-4-one Chemical compound O=C1N(C=2C(=CC=CC=2)C)C(=NCCC)S\C1=C/C1=CC=C(OC[C@H](O)CO)C(Cl)=C1 LPAUOXUZGSBGDU-ULCCENQXSA-N 0.000 description 1
- UTNUDOFZCWSZMS-UHFFFAOYSA-N 2-cyano-3-hydroxy-n-[4-(trifluoromethyl)phenyl]but-2-enamide Chemical compound CC(O)=C(C#N)C(=O)NC1=CC=C(C(F)(F)F)C=C1 UTNUDOFZCWSZMS-UHFFFAOYSA-N 0.000 description 1
- 208000012657 Atopic disease Diseases 0.000 description 1
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 description 1
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- 239000002253 acid Substances 0.000 description 1
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- 229940059756 arava Drugs 0.000 description 1
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- 229940057415 aubagio Drugs 0.000 description 1
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- 239000012876 carrier material Substances 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 208000007118 chronic progressive multiple sclerosis Diseases 0.000 description 1
- 210000004087 cornea Anatomy 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 239000007933 dermal patch Substances 0.000 description 1
- 230000006806 disease prevention Effects 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000003221 ear drop Substances 0.000 description 1
- 229940047652 ear drops Drugs 0.000 description 1
- 201000002491 encephalomyelitis Diseases 0.000 description 1
- 208000012997 experimental autoimmune encephalomyelitis Diseases 0.000 description 1
- 239000003889 eye drop Substances 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 150000002431 hydrogen Chemical class 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 230000002519 immonomodulatory effect Effects 0.000 description 1
- 230000006698 induction Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
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- 238000011694 lewis rat Methods 0.000 description 1
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- 230000002503 metabolic effect Effects 0.000 description 1
- 230000009401 metastasis Effects 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- BLIPZPLXBCHKDW-UHFFFAOYSA-N n-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide Chemical compound C1=CC(C(F)(F)F)=CC=C1NC(=O)C1=CON=C1 BLIPZPLXBCHKDW-UHFFFAOYSA-N 0.000 description 1
- 239000007922 nasal spray Substances 0.000 description 1
- 229940097496 nasal spray Drugs 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 238000003305 oral gavage Methods 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 210000000496 pancreas Anatomy 0.000 description 1
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- 239000000843 powder Substances 0.000 description 1
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- 102000004169 proteins and genes Human genes 0.000 description 1
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- 239000000018 receptor agonist Substances 0.000 description 1
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- 230000002459 sustained effect Effects 0.000 description 1
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Classifications
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
-
- 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
- A61K31/275—Nitriles; Isonitriles
- A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
-
- 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
-
- 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
- A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
-
- 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyrane Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017055994 | 2017-03-14 | ||
| PCT/EP2018/056185 WO2018167030A1 (en) | 2017-03-14 | 2018-03-13 | Pharmaceutical combination comprising ponesimod |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112019018894A2 true BR112019018894A2 (pt) | 2020-04-14 |
Family
ID=61655772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112019018894A BR112019018894A2 (pt) | 2017-03-14 | 2018-03-13 | combinação farmacêutica compreendendo ponesimod |
Country Status (24)
| Country | Link |
|---|---|
| US (2) | US11723896B2 (enExample) |
| EP (1) | EP3595657A1 (enExample) |
| JP (3) | JP7281406B2 (enExample) |
| KR (1) | KR102574562B1 (enExample) |
| CN (1) | CN110381942B (enExample) |
| AU (2) | AU2018233109B2 (enExample) |
| BR (1) | BR112019018894A2 (enExample) |
| CA (1) | CA3056301C (enExample) |
| CL (1) | CL2019002525A1 (enExample) |
| CO (1) | CO2019008510A2 (enExample) |
| CR (1) | CR20190464A (enExample) |
| DO (1) | DOP2019000257A (enExample) |
| EA (1) | EA201992117A1 (enExample) |
| EC (1) | ECSP19073317A (enExample) |
| IL (1) | IL269239B2 (enExample) |
| JO (1) | JOP20190207A1 (enExample) |
| MA (1) | MA49822A (enExample) |
| MX (1) | MX390941B (enExample) |
| NI (1) | NI201900092A (enExample) |
| PE (1) | PE20191489A1 (enExample) |
| PH (1) | PH12019502110A1 (enExample) |
| SG (1) | SG11201907308UA (enExample) |
| UA (1) | UA125756C2 (enExample) |
| WO (1) | WO2018167030A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190207A1 (ar) * | 2017-03-14 | 2019-09-10 | Actelion Pharmaceuticals Ltd | تركيبة صيدلانية تشتمل على بونيسيمود |
| US11013723B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms of a thiazolidinone compound, compositions and methods of use thereof |
| US11014897B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Solid forms comprising a thiazolidinone compound, compositions and methods of use thereof |
| US11186556B1 (en) | 2018-10-16 | 2021-11-30 | Celgene Corporation | Salts of a thiazolidinone compound, solid forms, compositions and methods of use thereof |
| US11014940B1 (en) | 2018-10-16 | 2021-05-25 | Celgene Corporation | Thiazolidinone and oxazolidinone compounds and formulations |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES448386A1 (es) | 1975-06-05 | 1978-04-16 | Hoechst Ag | Procedimiento para la preparacion de anilidas de acido 5-me-til-isoxazol-4-carboxilico. |
| DE2854439A1 (de) | 1978-12-16 | 1980-07-03 | Hoechst Ag | Ein isoxazolderivat, verfahren zu seiner herstellung, diese verbindung enthaltende mittel und verwendung |
| DE3534440A1 (de) | 1985-09-27 | 1987-04-02 | Hoechst Ag | Arzneimittel gegen chronische graft-versus-host-krankheiten sowie gegen autoimmunerkrankungen, insbesondere systemischen lupus erythematodes |
| US5268382A (en) | 1985-09-27 | 1993-12-07 | Hoechst Aktiengesellschaft | Medicaments to combat autoimmune diseases, in particular systemic lupus erythematosus |
| HUP0301865A3 (en) * | 2000-02-15 | 2005-12-28 | Teva Pharma | A method for synthesizing leflunomide |
| GB0123571D0 (en) | 2001-04-05 | 2001-11-21 | Aventis Pharm Prod Inc | Use of (Z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide for treating multiple sclerosis |
| ES2305287T3 (es) | 2001-04-05 | 2008-11-01 | Aventis Pharmaceuticals Inc. | Uso de (4'-trifluorometifenil)-amida del acido (z)-ciano-3-hidroxi-but-2-enoico para tratar la esclerosis multiple. |
| US6894184B2 (en) | 2003-03-18 | 2005-05-17 | Aventis Pharma Deutschland Gmbh | Process for preparing 2-cyano-3-hydroxy-N-(phenyl)but-2-enamides |
| EP2295418A1 (en) * | 2003-11-21 | 2011-03-16 | Actelion Pharmaceuticals Ltd. | 5-(benz-(z)-ylidene)-thiazolidin-4-one derivatives as immunosuppressant agents |
| USRE43833E1 (en) | 2003-11-21 | 2012-11-27 | Actelion Pharmaceuticals Ltd. | Thiazolidin-4-one derivatives |
| CA2584655A1 (en) * | 2004-10-19 | 2006-04-27 | Aventis Pharmaceuticals Inc. | Use of (z)-2-cyano-3-hydroxy-but-2-enoic acid-(4'-trifluoromethylphenyl)-amide for treating inflammatory bowel disease |
| DE102006017896A1 (de) | 2006-04-13 | 2007-10-25 | Tiefenbacher Pharmachemikalien Alfred E. Tiefenbacher Gmbh & Co. Kg | Leflunomid enthaltende pharmazeutische Zusammensetzungen |
| DK2094676T3 (da) | 2006-11-23 | 2013-06-10 | Actelion Pharmaceuticals Ltd | Ny fremgangsmåde til fremstillingen af 2-iminothiazolidin-4-on-derivater |
| US8912340B2 (en) | 2006-11-23 | 2014-12-16 | Actelion Pharmaceuticals Ltd. | Process for the preparation of 2-imino-thiazolidin-4-one derivatives |
| KR101718639B1 (ko) | 2008-03-17 | 2017-03-21 | 액테리온 파마슈티칼 리미티드 | 선별적 ｓ1ｐ₁ 수용체 작동약에 대한 투약 섭생 |
| GB0819182D0 (en) | 2008-10-20 | 2008-11-26 | Actelion Pharmaceuticals Ltd | Crystalline forms |
| PL2477611T3 (pl) | 2009-09-18 | 2017-09-29 | Sanofi | Formulacje tabletki 4'-trifluorometylofenyloamidu kwasu (Z)-2-cyjano-3-hydroksy-but-2-enowego o zwiększonej stabilności |
| WO2012015758A2 (en) | 2010-07-30 | 2012-02-02 | Saint Louis University | Methods of treating pain |
| AR082436A1 (es) | 2010-08-02 | 2012-12-05 | Sanofi Aventis Us Llc | Uso de teriflunomida para tratar la esclerosis multiple |
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