JP2016533323A5 - - Google Patents
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- Publication number
- JP2016533323A5 JP2016533323A5 JP2016516547A JP2016516547A JP2016533323A5 JP 2016533323 A5 JP2016533323 A5 JP 2016533323A5 JP 2016516547 A JP2016516547 A JP 2016516547A JP 2016516547 A JP2016516547 A JP 2016516547A JP 2016533323 A5 JP2016533323 A5 JP 2016533323A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- laquinimod
- subject
- medicament
- 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.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims 27
- 239000003814 drug Substances 0.000 claims 26
- GKWPCEFFIHSJOE-UHFFFAOYSA-N laquinimod Chemical compound OC=1C2=C(Cl)C=CC=C2N(C)C(=O)C=1C(=O)N(CC)C1=CC=CC=C1 GKWPCEFFIHSJOE-UHFFFAOYSA-N 0.000 claims 25
- 229960004577 laquinimod Drugs 0.000 claims 25
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 10
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 10
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 239000007787 solid Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 230000003113 alkalizing effect Effects 0.000 claims 6
- 239000000945 filler Substances 0.000 claims 6
- 239000003826 tablet Substances 0.000 claims 6
- 239000000314 lubricant Substances 0.000 claims 5
- 239000002245 particle Substances 0.000 claims 5
- 239000002265 redox agent Substances 0.000 claims 5
- 238000002560 therapeutic procedure Methods 0.000 claims 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 4
- 206010061818 Disease progression Diseases 0.000 claims 4
- 229930195725 Mannitol Natural products 0.000 claims 4
- 210000004556 brain Anatomy 0.000 claims 4
- 239000011248 coating agent Substances 0.000 claims 4
- 238000000576 coating method Methods 0.000 claims 4
- 230000005750 disease progression Effects 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 4
- 239000000594 mannitol Substances 0.000 claims 4
- 235000010355 mannitol Nutrition 0.000 claims 4
- 208000024891 symptom Diseases 0.000 claims 4
- 239000000443 aerosol Substances 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 239000002775 capsule Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 230000000977 initiatory effect Effects 0.000 claims 3
- 239000007788 liquid Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 2
- GUBGYTABKSRVRQ-DCSYEGIMSA-N Beta-Lactose Chemical compound OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)[C@H](O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-DCSYEGIMSA-N 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 2
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical group CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- 238000009825 accumulation Methods 0.000 claims 2
- 229960004977 anhydrous lactose Drugs 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 239000002274 desiccant Substances 0.000 claims 2
- 239000007884 disintegrant Substances 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 239000003623 enhancer Substances 0.000 claims 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical group CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 2
- 230000036541 health Effects 0.000 claims 2
- 230000003862 health status Effects 0.000 claims 2
- 239000000905 isomalt Substances 0.000 claims 2
- 235000010439 isomalt Nutrition 0.000 claims 2
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims 2
- 229960001375 lactose Drugs 0.000 claims 2
- 239000008101 lactose Substances 0.000 claims 2
- 229960001021 lactose monohydrate Drugs 0.000 claims 2
- 235000019359 magnesium stearate Nutrition 0.000 claims 2
- 229960003194 meglumine Drugs 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 230000035699 permeability Effects 0.000 claims 2
- 239000000049 pigment Substances 0.000 claims 2
- 229920000642 polymer Polymers 0.000 claims 2
- 239000008109 sodium starch glycolate Substances 0.000 claims 2
- 229940079832 sodium starch glycolate Drugs 0.000 claims 2
- 229920003109 sodium starch glycolate Polymers 0.000 claims 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 2
- 239000000600 sorbitol Substances 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 229940032147 starch Drugs 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- OBRNDARFFFHCGE-PERKLWIXSA-N (S,S)-formoterol fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 OBRNDARFFFHCGE-PERKLWIXSA-N 0.000 claims 1
- 208000024806 Brain atrophy Diseases 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- UETNIIAIRMUTSM-UHFFFAOYSA-N Jacareubin Natural products CC1(C)OC2=CC3Oc4c(O)c(O)ccc4C(=O)C3C(=C2C=C1)O UETNIIAIRMUTSM-UHFFFAOYSA-N 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 208000028389 Nerve injury Diseases 0.000 claims 1
- 101100202644 Parasynechococcus marenigrum (strain WH8102) bsmB gene Proteins 0.000 claims 1
- 208000007400 Relapsing-Remitting Multiple Sclerosis Diseases 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 230000005856 abnormality Effects 0.000 claims 1
- 239000006096 absorbing agent Substances 0.000 claims 1
- 238000011374 additional therapy Methods 0.000 claims 1
- 230000003110 anti-inflammatory effect Effects 0.000 claims 1
- 239000002981 blocking agent Substances 0.000 claims 1
- 239000001913 cellulose Substances 0.000 claims 1
- 229920002678 cellulose Polymers 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 230000003247 decreasing effect Effects 0.000 claims 1
- 230000006866 deterioration Effects 0.000 claims 1
- 230000009266 disease activity Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000005713 exacerbation Effects 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 206010016256 fatigue Diseases 0.000 claims 1
- 229960000193 formoterol fumarate Drugs 0.000 claims 1
- 150000002344 gold compounds Chemical class 0.000 claims 1
- 229920001903 high density polyethylene Polymers 0.000 claims 1
- 239000004700 high-density polyethylene Substances 0.000 claims 1
- XXSMGPRMXLTPCZ-UHFFFAOYSA-N hydroxychloroquine Chemical compound ClC1=CC=C2C(NC(C)CCCN(CCO)CC)=CC=NC2=C1 XXSMGPRMXLTPCZ-UHFFFAOYSA-N 0.000 claims 1
- 229960004171 hydroxychloroquine Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 229940124589 immunosuppressive drug Drugs 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 210000003141 lower extremity Anatomy 0.000 claims 1
- 230000003340 mental effect Effects 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 230000008764 nerve damage Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 230000009251 neurologic dysfunction Effects 0.000 claims 1
- 208000015015 neurological dysfunction Diseases 0.000 claims 1
- 230000009223 neuronal apoptosis Effects 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims 1
- 150000003873 salicylate salts Chemical class 0.000 claims 1
- 239000000741 silica gel Substances 0.000 claims 1
- 229910002027 silica gel Inorganic materials 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 239000007921 spray Substances 0.000 claims 1
- 230000003637 steroidlike Effects 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 claims 1
- 229960001940 sulfasalazine Drugs 0.000 claims 1
- NCEXYHBECQHGNR-UHFFFAOYSA-N sulfasalazine Natural products C1=C(O)C(C(=O)O)=CC(N=NC=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-UHFFFAOYSA-N 0.000 claims 1
- 230000004382 visual function Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361883698P | 2013-09-27 | 2013-09-27 | |
| US61/883,698 | 2013-09-27 | ||
| PCT/US2014/057705 WO2015065628A2 (en) | 2013-09-27 | 2014-09-26 | Laquinimod combination therapy for treatment of multiple sclerosis |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016533323A JP2016533323A (ja) | 2016-10-27 |
| JP2016533323A5 true JP2016533323A5 (https=) | 2017-11-09 |
Family
ID=52740749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016516547A Withdrawn JP2016533323A (ja) | 2013-09-27 | 2014-09-26 | 多発性硬化症の治療のためのラキニモド併用療法 |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US20150094332A1 (https=) |
| EP (1) | EP3049075A4 (https=) |
| JP (1) | JP2016533323A (https=) |
| KR (1) | KR20160085757A (https=) |
| CN (1) | CN105848653A (https=) |
| AR (1) | AR097792A1 (https=) |
| AU (1) | AU2014342917A1 (https=) |
| BR (1) | BR112016006582A2 (https=) |
| CA (1) | CA2925493A1 (https=) |
| EA (1) | EA201690673A1 (https=) |
| IL (1) | IL244620A0 (https=) |
| MX (1) | MX2016003763A (https=) |
| SG (1) | SG11201602175VA (https=) |
| TW (1) | TW201601722A (https=) |
| UY (1) | UY35748A (https=) |
| WO (1) | WO2015065628A2 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201692180A1 (ru) | 2014-04-29 | 2017-08-31 | Тева Фармасьютикал Индастриз Лтд. | Лахинимод для лечения пациентов с рецидивирующе-ремиттирующим рассеянным склерозом (рррс) с высоким статусом инвалидизации |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19853487A1 (de) * | 1998-11-19 | 2000-05-25 | Fumapharm Ag Muri | Verwendung von Dialkylfumaraten |
| EP1915334A2 (en) * | 2005-07-07 | 2008-04-30 | Aditech Pharma AB | Novel salts of fumaric acid monoalkylesters and their pharmaceutical use |
| RS52169B (sr) * | 2006-06-12 | 2012-08-31 | Teva Pharmaceutical Industries Limited | Stabilni preparati lakvinimoda |
| RS54328B1 (sr) * | 2009-06-19 | 2016-02-29 | Teva Pharmaceutical Industries Ltd. | Tretman multiple skleroze lakvinimodom |
| EA201490377A1 (ru) * | 2011-07-28 | 2014-11-28 | Тева Фармасьютикал Индастриз Лтд. | Лечение рассеянного склероза комбинацией лаквинимода и глатирамера ацетата |
-
2014
- 2014-09-26 CA CA2925493A patent/CA2925493A1/en active Pending
- 2014-09-26 TW TW103133660A patent/TW201601722A/zh unknown
- 2014-09-26 SG SG11201602175VA patent/SG11201602175VA/en unknown
- 2014-09-26 EA EA201690673A patent/EA201690673A1/ru unknown
- 2014-09-26 EP EP14857795.0A patent/EP3049075A4/en not_active Withdrawn
- 2014-09-26 AR ARP140103582A patent/AR097792A1/es unknown
- 2014-09-26 US US14/498,024 patent/US20150094332A1/en not_active Abandoned
- 2014-09-26 CN CN201480053575.8A patent/CN105848653A/zh active Pending
- 2014-09-26 MX MX2016003763A patent/MX2016003763A/es unknown
- 2014-09-26 KR KR1020167011039A patent/KR20160085757A/ko not_active Withdrawn
- 2014-09-26 AU AU2014342917A patent/AU2014342917A1/en not_active Abandoned
- 2014-09-26 JP JP2016516547A patent/JP2016533323A/ja not_active Withdrawn
- 2014-09-26 BR BR112016006582A patent/BR112016006582A2/pt not_active IP Right Cessation
- 2014-09-26 WO PCT/US2014/057705 patent/WO2015065628A2/en not_active Ceased
- 2014-09-26 UY UY0001035748A patent/UY35748A/es not_active Application Discontinuation
-
2016
- 2016-03-15 IL IL244620A patent/IL244620A0/en unknown
- 2016-05-31 US US15/169,139 patent/US20160271094A1/en not_active Abandoned
-
2017
- 2017-07-06 US US15/643,214 patent/US20170304253A1/en not_active Abandoned
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