JP2013533286A5 - - Google Patents
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- JP2013533286A5 JP2013533286A5 JP2013521879A JP2013521879A JP2013533286A5 JP 2013533286 A5 JP2013533286 A5 JP 2013533286A5 JP 2013521879 A JP2013521879 A JP 2013521879A JP 2013521879 A JP2013521879 A JP 2013521879A JP 2013533286 A5 JP2013533286 A5 JP 2013533286A5
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- JP
- Japan
- Prior art keywords
- group
- individual
- receptor agonist
- combinations
- antagonist
- 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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- 238000000034 method Methods 0.000 claims description 41
- 102000011011 Sphingosine 1-phosphate receptors Human genes 0.000 claims description 21
- 108050001083 Sphingosine 1-phosphate receptors Proteins 0.000 claims description 21
- 239000000018 receptor agonist Substances 0.000 claims description 15
- 229940044601 receptor agonist Drugs 0.000 claims description 15
- 229940079593 drug Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- YXEQXPNSBUIRDZ-OAQYLSRUSA-N 1-[5-[(3r)-3-amino-4-hydroxy-3-methylbutyl]-1-methylpyrrol-2-yl]-4-(4-methylphenyl)butan-1-one Chemical compound C1=CC(C)=CC=C1CCCC(=O)C1=CC=C(CC[C@@](C)(N)CO)N1C YXEQXPNSBUIRDZ-OAQYLSRUSA-N 0.000 claims description 6
- KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 claims description 6
- QDDQIPUKAXBMBX-UHFFFAOYSA-N 1-[[6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-3,4-dihydronaphthalen-2-yl]methyl]azetidine-3-carboxylic acid Chemical compound COC1=CC(CCC)=CC=C1COC1=CC=C(C(C)=C(CN2CC(C2)C(O)=O)CC2)C2=C1 QDDQIPUKAXBMBX-UHFFFAOYSA-N 0.000 claims description 6
- MYIFLDFUXIHOCJ-UHFFFAOYSA-N 2-amino-2-[2-[2-chloro-4-(3-phenylmethoxyphenyl)sulfanylphenyl]ethyl]propane-1,3-diol;hydrochloride Chemical compound Cl.C1=C(Cl)C(CCC(CO)(CO)N)=CC=C1SC1=CC=CC(OCC=2C=CC=CC=2)=C1 MYIFLDFUXIHOCJ-UHFFFAOYSA-N 0.000 claims description 6
- JRZJZOSWCNBQFS-NYYVNYEXSA-N 3-[[(1r)-1-[4-[5-[4-(2-methylpropyl)phenyl]-1,2,4-oxadiazol-3-yl]phenyl]ethyl]amino]cyclobutane-1-carboxylic acid Chemical compound C1=CC(CC(C)C)=CC=C1C1=NC(C=2C=CC(=CC=2)[C@@H](C)NC2CC(C2)C(O)=O)=NO1 JRZJZOSWCNBQFS-NYYVNYEXSA-N 0.000 claims description 6
- 229960000556 fingolimod Drugs 0.000 claims description 6
- KKGQTZUTZRNORY-UHFFFAOYSA-N fingolimod Chemical compound CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 KKGQTZUTZRNORY-UHFFFAOYSA-N 0.000 claims description 6
- BQJCRHHNABKAKU-KBQPJGBKSA-N morphine Chemical compound O([C@H]1[C@H](C=C[C@H]23)O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O BQJCRHHNABKAKU-KBQPJGBKSA-N 0.000 claims description 6
- 239000002464 receptor antagonist Substances 0.000 claims description 6
- 229940044551 receptor antagonist Drugs 0.000 claims description 6
- 206010020751 Hypersensitivity Diseases 0.000 claims description 5
- 208000026935 allergic disease Diseases 0.000 claims description 5
- 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 claims description 5
- 238000002512 chemotherapy Methods 0.000 claims description 5
- 230000009610 hypersensitivity Effects 0.000 claims description 5
- 208000002193 Pain Diseases 0.000 claims description 4
- 229940127240 opiate Drugs 0.000 claims description 4
- 229950009275 ponesimod Drugs 0.000 claims description 4
- 229960005181 morphine Drugs 0.000 claims description 3
- 208000004296 neuralgia Diseases 0.000 claims description 3
- 208000021722 neuropathic pain Diseases 0.000 claims description 3
- 229930012538 Paclitaxel Natural products 0.000 claims description 2
- 229940079156 Proteasome inhibitor Drugs 0.000 claims description 2
- 229940123237 Taxane Drugs 0.000 claims description 2
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 2
- 229940045985 antineoplastic platinum compound Drugs 0.000 claims description 2
- 229960001467 bortezomib Drugs 0.000 claims description 2
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims description 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 2
- 229960001756 oxaliplatin Drugs 0.000 claims description 2
- 229960001592 paclitaxel Drugs 0.000 claims description 2
- 150000003058 platinum compounds Chemical class 0.000 claims description 2
- 239000003207 proteasome inhibitor Substances 0.000 claims description 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 2
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 2
- 229960004528 vincristine Drugs 0.000 claims description 2
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims description 2
- -1 ponecimod Chemical compound 0.000 claims 1
- 239000005557 antagonist Substances 0.000 description 13
- ZDRVLAOYDGQLFI-UHFFFAOYSA-N 4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol;hydrochloride Chemical compound Cl.C1=CC(O)=CC=C1NC1=NC(C=2C=CC(Cl)=CC=2)=CS1 ZDRVLAOYDGQLFI-UHFFFAOYSA-N 0.000 description 5
- 239000000556 agonist Substances 0.000 description 5
- 108010035597 sphingosine kinase Proteins 0.000 description 5
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 description 4
- 102100025750 Sphingosine 1-phosphate receptor 1 Human genes 0.000 description 4
- 101710155454 Sphingosine 1-phosphate receptor 1 Proteins 0.000 description 4
- 230000003502 anti-nociceptive effect Effects 0.000 description 3
- 206010065390 Inflammatory pain Diseases 0.000 description 2
- 208000027866 inflammatory disease Diseases 0.000 description 2
- WGSHXYXZHQJPQL-DMBFJYOSSA-N (E,16R,17S)-17-amino-16,18-dihydroxyoctadec-14-ene-1,1,1-tricarbaldehyde Chemical compound C(=O)C(CCCCCCCCCCCC/C=C/[C@H]([C@H](CO)N)O)(C=O)C=O WGSHXYXZHQJPQL-DMBFJYOSSA-N 0.000 description 1
- ZKVKFPZCVMFTCI-CWFJQSRLSA-N (E,3R,4R)-3-amino-2,4-dihydroxynonadec-5-enal Chemical compound C(=O)C(O)[C@H](N)[C@H](O)\C=C\CCCCCCCCCCCCC ZKVKFPZCVMFTCI-CWFJQSRLSA-N 0.000 description 1
- 208000004454 Hyperalgesia Diseases 0.000 description 1
- 208000035154 Hyperesthesia Diseases 0.000 description 1
- 229940127450 Opioid Agonists Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- OTKJDMGTUTTYMP-UHFFFAOYSA-N dihydrosphingosine Natural products CCCCCCCCCCCCCCCC(O)C(N)CO OTKJDMGTUTTYMP-UHFFFAOYSA-N 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- YRXOQXUDKDCXME-QWKHPXNBSA-N n,n-dimethylsphingosine Chemical compound CCCCCCCCCCCCC\C=C\[C@H](O)[C@@H](CO)N(C)C YRXOQXUDKDCXME-QWKHPXNBSA-N 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US36950410P | 2010-07-30 | 2010-07-30 | |
| US61/369,504 | 2010-07-30 | ||
| PCT/US2011/045236 WO2012015758A2 (en) | 2010-07-30 | 2011-07-25 | Methods of treating pain |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013533286A JP2013533286A (ja) | 2013-08-22 |
| JP2013533286A5 true JP2013533286A5 (cg-RX-API-DMAC7.html) | 2014-09-11 |
Family
ID=44543779
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013521879A Pending JP2013533286A (ja) | 2010-07-30 | 2011-07-25 | 疼痛を治療する方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US8747844B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2598126A2 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2013533286A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2012015758A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20161133T1 (hr) | 2008-07-23 | 2016-12-02 | Arena Pharmaceuticals, Inc. | DERIVATI SUSPSTITUIRANE 1,2,3,4-TETRAHIDROCIKLOPENTA[b]INDOL-3-IL-OCTENE KISELINE KORISNI U LIJEČENJU AUTOIMUNIH I UPALNIH POREMEĆAJA |
| CN105816453B (zh) | 2008-08-27 | 2021-03-05 | 艾尼纳制药公司 | 用于治疗自身免疫性病症和炎性病症的作为s1p1受体激动剂的经取代的三环酸衍生物 |
| EP2528894A1 (en) | 2010-01-27 | 2012-12-05 | Arena Pharmaceuticals, Inc. | Processes for the preparation of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid and salts thereof |
| CA2789480A1 (en) | 2010-03-03 | 2011-09-09 | Arena Pharmaceuticals, Inc. | Processes for the preparation of s1p1 receptor modulators and crystalline forms thereof |
| CA2875069C (en) * | 2012-05-31 | 2018-01-02 | Kinki University | Agent for prophylactic and/or therapeutic treatment of peripheral neuropathic pain caused by anticancer agent |
| US20150087613A1 (en) * | 2013-09-26 | 2015-03-26 | Saint Louis University | Inhibition of Opioid Antinociceptive Tolerance and Withdrawal in Nociceptive Pain Therapy |
| WO2016112075A1 (en) | 2015-01-06 | 2016-07-14 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the s1p1 receptor |
| KR102603199B1 (ko) | 2015-06-22 | 2023-11-16 | 아레나 파마슈티칼스, 인크. | Ｓ1ｐ1 수용체-관련 장애에서의 사용을 위한 (ｒ)-2-(7-(4-시클로펜틸-3-(트리플루오로메틸)벤질옥시)-1,2,3,4-테트라히드로시클로-펜타[ｂ]인돌-3-일)아세트산 (화합물 1)의 결정성 ｌ-아르기닌 염 |
| EP3118621A1 (en) * | 2015-07-14 | 2017-01-18 | Fundació Institut d'Investigació Biomèdica de Bellvitge (IDIBELL) | Methods and compositions for the diagnosis and for the treatment of adrenoleukodystrophy |
| US10877045B2 (en) * | 2015-07-21 | 2020-12-29 | Saint Louis University | Compositions and methods for diagnosing and treating endometriosis-related infertility |
| MA42625A (fr) * | 2015-08-11 | 2018-06-20 | Akaal Pharma Pty Ltd | Compositions comprenant des modulateurs de récepteurs de s1p |
| CA2996281C (en) | 2015-08-31 | 2022-03-08 | Regents Of The University Of Minnesota | Opioid receptor modulators and use thereof |
| MA47504A (fr) | 2017-02-16 | 2019-12-25 | Arena Pharm Inc | Composés et méthodes de traitement de l'angiocholite biliaire primitive |
| MA47503A (fr) | 2017-02-16 | 2021-04-21 | Arena Pharm Inc | Composés et méthodes pour le traitement de maladies inflammatoires chroniques de l'intestin avec manifestations extra-intestinales |
| JOP20190207A1 (ar) | 2017-03-14 | 2019-09-10 | Actelion Pharmaceuticals Ltd | تركيبة صيدلانية تشتمل على بونيسيمود |
| CN112601516A (zh) | 2018-06-06 | 2021-04-02 | 艾尼纳制药公司 | 治疗与s1p1受体相关的病况的方法 |
| US11555015B2 (en) | 2018-09-06 | 2023-01-17 | Arena Pharmaceuticals, Inc. | Compounds useful in the treatment of autoimmune and inflammatory disorders |
| US11497795B2 (en) | 2018-09-28 | 2022-11-15 | Asahi Kasei Pharma Corporation | Medicament for mitigating conditions and/or suppressing onset of peripheral neuropathy induced by anti-malignant tumor agent |
| CN110511240B (zh) * | 2019-08-27 | 2022-03-08 | 南京医科大学 | 一种髓细胞触发受体2的内源性配体及其应用 |
| US11594117B2 (en) | 2020-12-18 | 2023-02-28 | Itron, Inc. | Network edge detection and notification of gas pressure situation |
| CN117042738A (zh) * | 2021-03-17 | 2023-11-10 | 埃科特莱茵药品有限公司 | 药物剂量系统 |
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| JP5795833B2 (ja) * | 2006-10-27 | 2015-10-14 | エルパス・インコーポレイテッドＬｐａｔｈ， Ｉｎｃ． | スフィンゴシン−１−リン酸と結合させるための組成物および方法 |
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-
2011
- 2011-07-25 EP EP11745855.4A patent/EP2598126A2/en not_active Withdrawn
- 2011-07-25 JP JP2013521879A patent/JP2013533286A/ja active Pending
- 2011-07-25 WO PCT/US2011/045236 patent/WO2012015758A2/en not_active Ceased
- 2011-07-25 US US13/189,954 patent/US8747844B2/en active Active
-
2014
- 2014-04-07 US US14/246,847 patent/US8945549B2/en active Active
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