JP2014528418A5 - - Google Patents
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- JP2014528418A5 JP2014528418A5 JP2014533430A JP2014533430A JP2014528418A5 JP 2014528418 A5 JP2014528418 A5 JP 2014528418A5 JP 2014533430 A JP2014533430 A JP 2014533430A JP 2014533430 A JP2014533430 A JP 2014533430A JP 2014528418 A5 JP2014528418 A5 JP 2014528418A5
- Authority
- JP
- Japan
- Prior art keywords
- pain
- independently
- aliphatic
- compound according
- item
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 86
- 208000002193 Pain Diseases 0.000 claims description 37
- 230000013629 beta-amyloid clearance Effects 0.000 claims description 17
- -1 1,2- methylenedioxy Chemical group 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 15
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 208000010877 cognitive disease Diseases 0.000 claims description 12
- 208000024827 Alzheimer disease Diseases 0.000 claims description 11
- 125000001931 aliphatic group Chemical group 0.000 claims description 10
- 125000005842 heteroatom Chemical group 0.000 claims description 10
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 10
- 201000010374 Down Syndrome Diseases 0.000 claims description 9
- 230000003920 cognitive function Effects 0.000 claims description 9
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 8
- 206010044688 Trisomy 21 Diseases 0.000 claims description 8
- 230000000971 hippocampal effect Effects 0.000 claims description 8
- 230000027928 long-term synaptic potentiation Effects 0.000 claims description 8
- 208000028698 Cognitive impairment Diseases 0.000 claims description 7
- 230000002708 enhancing effect Effects 0.000 claims description 7
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 7
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 6
- 125000004043 oxo group Chemical group O=* 0.000 claims description 6
- 125000000464 thioxo group Chemical group S=* 0.000 claims description 6
- 230000009529 traumatic brain injury Effects 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 5
- 208000004296 neuralgia Diseases 0.000 claims description 5
- 208000021722 neuropathic pain Diseases 0.000 claims description 5
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 claims description 4
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 4
- 201000006417 multiple sclerosis Diseases 0.000 claims description 4
- 230000000699 topical effect Effects 0.000 claims description 4
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 3
- 206010061218 Inflammation Diseases 0.000 claims description 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 3
- 229910052794 bromium Inorganic materials 0.000 claims description 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 3
- 230000004054 inflammatory process Effects 0.000 claims description 3
- 238000001356 surgical procedure Methods 0.000 claims description 3
- 208000030507 AIDS Diseases 0.000 claims description 2
- 208000007848 Alcoholism Diseases 0.000 claims description 2
- 208000000412 Avitaminosis Diseases 0.000 claims description 2
- 208000037157 Azotemia Diseases 0.000 claims description 2
- 208000001640 Fibromyalgia Diseases 0.000 claims description 2
- 201000005569 Gout Diseases 0.000 claims description 2
- 206010019233 Headaches Diseases 0.000 claims description 2
- 208000007514 Herpes zoster Diseases 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010021135 Hypovitaminosis Diseases 0.000 claims description 2
- 208000019695 Migraine disease Diseases 0.000 claims description 2
- 206010028391 Musculoskeletal Pain Diseases 0.000 claims description 2
- 208000028389 Nerve injury Diseases 0.000 claims description 2
- 208000001738 Nervous System Trauma Diseases 0.000 claims description 2
- 206010029240 Neuritis Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000004983 Phantom Limb Diseases 0.000 claims description 2
- 206010056238 Phantom pain Diseases 0.000 claims description 2
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 2
- 208000004550 Postoperative Pain Diseases 0.000 claims description 2
- 208000028911 Temporomandibular Joint disease Diseases 0.000 claims description 2
- 206010045171 Tumour pain Diseases 0.000 claims description 2
- 208000027418 Wounds and injury Diseases 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 208000005298 acute pain Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 201000007930 alcohol dependence Diseases 0.000 claims description 2
- 238000002266 amputation Methods 0.000 claims description 2
- 238000002512 chemotherapy Methods 0.000 claims description 2
- 230000006378 damage Effects 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 2
- 231100000869 headache Toxicity 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims description 2
- 238000007913 intrathecal administration Methods 0.000 claims description 2
- 238000007914 intraventricular administration Methods 0.000 claims description 2
- 230000003821 menstrual periods Effects 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 206010027599 migraine Diseases 0.000 claims description 2
- 230000008764 nerve damage Effects 0.000 claims description 2
- 208000028412 nervous system injury Diseases 0.000 claims description 2
- 201000008482 osteoarthritis Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000002685 pulmonary effect Effects 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 230000006016 thyroid dysfunction Effects 0.000 claims description 2
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 2
- 208000009852 uremia Diseases 0.000 claims description 2
- 208000030401 vitamin deficiency disease Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 12
- 239000002552 dosage form Substances 0.000 claims 9
- 208000009525 Myocarditis Diseases 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 238000010276 construction Methods 0.000 claims 1
- 239000006202 intradermal dosage form Substances 0.000 claims 1
- 239000006207 intravenous dosage form Substances 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000006203 subcutaneous dosage form Substances 0.000 claims 1
- 239000006208 topical dosage form Substances 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 30
- 239000000556 agonist Substances 0.000 description 6
- 208000037259 Amyloid Plaque Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 230000006999 cognitive decline Effects 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 210000001508 eye Anatomy 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 210000000214 mouth Anatomy 0.000 description 1
- 210000004165 myocardium Anatomy 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 230000003956 synaptic plasticity Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161541919P | 2011-09-30 | 2011-09-30 | |
| US61/541,919 | 2011-09-30 | ||
| PCT/US2012/058080 WO2013049686A1 (en) | 2011-09-30 | 2012-09-28 | Uridine diphosphate derivatives, compositions and methods for treating neurodegenerative disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014528418A JP2014528418A (ja) | 2014-10-27 |
| JP2014528418A5 true JP2014528418A5 (enExample) | 2015-11-19 |
| JP6162125B2 JP6162125B2 (ja) | 2017-07-12 |
Family
ID=47996472
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014533430A Expired - Fee Related JP6162125B2 (ja) | 2011-09-30 | 2012-09-28 | 神経変性障害を処置するためのウリジン二リン酸誘導体、組成物および方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (6) | US8598141B2 (enExample) |
| EP (1) | EP2760858B1 (enExample) |
| JP (1) | JP6162125B2 (enExample) |
| CN (2) | CN103906745B (enExample) |
| AU (1) | AU2012315671B2 (enExample) |
| CA (1) | CA2850367C (enExample) |
| IL (1) | IL231787A (enExample) |
| IN (1) | IN2014CN03043A (enExample) |
| WO (1) | WO2013049686A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103906745B (zh) | 2011-09-30 | 2017-08-25 | 塔夫斯大学 | 用于治疗神经变性疾病的尿苷二磷酸衍生物、组合物和方法 |
| JP6523958B2 (ja) | 2012-09-28 | 2019-06-05 | タフツ・ユニバーシティ | ウリジン二リン酸誘導体、プロドラッグ、組成物およびそれらの使用 |
| WO2014160502A1 (en) * | 2013-03-13 | 2014-10-02 | Tufts University | Uridine nucleoside derivatives, compositions and methods of use |
| US10138265B2 (en) | 2013-03-13 | 2018-11-27 | Tufts University | Uridine nucleoside derivatives, compositions and methods of use |
| US10526287B2 (en) | 2015-04-23 | 2020-01-07 | Constellation Pharmaceuticals, Inc. | LSD1 inhibitors and uses thereof |
| CR20170544A (es) | 2015-05-29 | 2018-03-20 | Univ Nat Yang Ming | Agentes nucleosidos para la reducción de la actividad perjudicial de los genes que contienen repeticiones de nucleótidos extendidas. |
| EP3515447A4 (en) * | 2016-09-26 | 2020-05-27 | Tufts University | Uridine nucleoside derivatives, compositions and methods of use |
| MD3532459T2 (ro) | 2016-10-26 | 2024-06-30 | Constellation Pharmaceuticals Inc | Inhibitori ai LSD1 și utilizările medicale ale acestora |
| US20220241311A1 (en) * | 2018-06-14 | 2022-08-04 | Mayo Foundation For Medical Education And Research | Methods and materials for treating glycosylation disorders |
| WO2021194959A1 (en) * | 2020-03-24 | 2021-09-30 | Gliaguard, Inc. | Treatment of eye disorders with uridine phosphate derivatives |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH0621073B2 (ja) | 1986-03-06 | 1994-03-23 | 日水製薬株式会社 | 中枢抑制剤 |
| JP3032053B2 (ja) | 1991-09-06 | 2000-04-10 | 日水製薬株式会社 | ウリジン誘導体及びこれを含有する医薬 |
| US5962459A (en) | 1996-05-28 | 1999-10-05 | Polifarma S.P.A. | Therapeutic active agent for treatment of neuron degenerative diseases |
| CA2300146A1 (en) | 1997-08-29 | 1999-03-04 | Richard C. Boucher, Jr. | Use of uridine 5'-diphosphate and analogs thereof for the treatment of lung diseases |
| US8314064B2 (en) * | 1998-07-31 | 2012-11-20 | Massachusetts Institute Of Technology | Uridine administration stimulates membrane production |
| US8518882B2 (en) | 1998-07-31 | 2013-08-27 | Massachusetts Institute Of Technology | Methods and compositions for ameliorating or inhibiting decline in memory or intelligence or improving same |
| ATE374029T1 (de) | 1998-07-31 | 2007-10-15 | Massachusetts Inst Technology | Behandlung der alzheimer-krankheit durch erhöhung des cytidin-spiegels in vivo |
| US20050203053A1 (en) | 1999-07-30 | 2005-09-15 | Wurtman Richard J. | Uridine administration improves phosphatide synthesis, synaptic transmission and cogntive function |
| US20060069061A1 (en) | 1998-07-31 | 2006-03-30 | Dick Wurtman | Compositions containing uridine and choline, and methods utilizing same |
| US20070004670A1 (en) | 1998-07-31 | 2007-01-04 | Richard Wurtman | Compositions containing citicoline, and methods of use thereof |
| US8143234B2 (en) | 1998-07-31 | 2012-03-27 | Massachusetts Institute Of Technology | Uridine administration improves phosphatide synthesis, synaptic transmission and cognitive function |
| GB0004297D0 (en) | 2000-02-23 | 2000-04-12 | Ucb Sa | 2-oxo-1 pyrrolidine derivatives process for preparing them and their uses |
| US6875751B2 (en) | 2000-06-15 | 2005-04-05 | Idenix Pharmaceuticals, Inc. | 3′-prodrugs of 2′-deoxy-β-L-nucleosides |
| CA2444161A1 (en) * | 2003-10-01 | 2005-04-01 | Japan Health Sciences Foundation | A screening method of drug for treatment of neuropathic pain |
| US7737128B2 (en) | 2004-06-10 | 2010-06-15 | The Mclean Hospital Corporation | Pyrimidines, such as uridine, in treatments for patients with bipolar disorder |
| US7851456B2 (en) | 2005-06-29 | 2010-12-14 | Inspire Pharmaceuticals, Inc. | P2Y6 receptor agonists for treating lung diseases |
| CN101765369A (zh) | 2007-03-19 | 2010-06-30 | 俄勒冈州由俄勒冈州立大学代表州高等教育委员会行使 | 曼尼希碱n-氧化物药物 |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| EP2342616A2 (en) | 2008-09-23 | 2011-07-13 | Alnylam Pharmaceuticals Inc. | Chemical modifications of monomers and oligonucleotides with cycloaddition |
| US9221868B2 (en) | 2010-12-01 | 2015-12-29 | Bar-Ilan University | Uridine di- or tri-phosphate derivatives and uses thereof |
| CN103906745B (zh) * | 2011-09-30 | 2017-08-25 | 塔夫斯大学 | 用于治疗神经变性疾病的尿苷二磷酸衍生物、组合物和方法 |
| JP6523958B2 (ja) | 2012-09-28 | 2019-06-05 | タフツ・ユニバーシティ | ウリジン二リン酸誘導体、プロドラッグ、組成物およびそれらの使用 |
| WO2014160502A1 (en) | 2013-03-13 | 2014-10-02 | Tufts University | Uridine nucleoside derivatives, compositions and methods of use |
| US10138265B2 (en) | 2013-03-13 | 2018-11-27 | Tufts University | Uridine nucleoside derivatives, compositions and methods of use |
-
2012
- 2012-09-28 CN CN201280053228.6A patent/CN103906745B/zh not_active Expired - Fee Related
- 2012-09-28 CN CN201710598982.2A patent/CN107353316B/zh not_active Expired - Fee Related
- 2012-09-28 IN IN3043CHN2014 patent/IN2014CN03043A/en unknown
- 2012-09-28 WO PCT/US2012/058080 patent/WO2013049686A1/en not_active Ceased
- 2012-09-28 AU AU2012315671A patent/AU2012315671B2/en not_active Ceased
- 2012-09-28 JP JP2014533430A patent/JP6162125B2/ja not_active Expired - Fee Related
- 2012-09-28 EP EP12837369.3A patent/EP2760858B1/en active Active
- 2012-09-28 CA CA2850367A patent/CA2850367C/en not_active Expired - Fee Related
-
2013
- 2013-03-08 US US13/791,447 patent/US8598141B2/en not_active Expired - Fee Related
- 2013-11-06 US US14/073,476 patent/US8785620B2/en active Active
-
2014
- 2014-03-27 IL IL231787A patent/IL231787A/en active IP Right Grant
- 2014-07-03 US US14/323,690 patent/US9227993B2/en not_active Expired - Fee Related
-
2016
- 2016-01-04 US US14/987,554 patent/US20160318968A1/en not_active Abandoned
-
2018
- 2018-12-03 US US16/208,481 patent/US11072627B2/en not_active Expired - Fee Related
-
2021
- 2021-07-26 US US17/385,894 patent/US20210347807A1/en not_active Abandoned
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