JP2013536833A5 - - Google Patents
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- JP2013536833A5 JP2013536833A5 JP2013526566A JP2013526566A JP2013536833A5 JP 2013536833 A5 JP2013536833 A5 JP 2013536833A5 JP 2013526566 A JP2013526566 A JP 2013526566A JP 2013526566 A JP2013526566 A JP 2013526566A JP 2013536833 A5 JP2013536833 A5 JP 2013536833A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- disease
- compound according
- medicament
- pharmaceutically acceptable
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 77
- 239000003814 drug Substances 0.000 claims description 47
- 150000003839 salts Chemical class 0.000 claims description 34
- 229940002612 prodrug Drugs 0.000 claims description 32
- 239000000651 prodrug Substances 0.000 claims description 32
- 201000010099 disease Diseases 0.000 claims description 28
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
- 238000011282 treatment Methods 0.000 claims description 26
- 230000000694 effects Effects 0.000 claims description 21
- 239000004480 active ingredient Substances 0.000 claims description 18
- 238000004519 manufacturing process Methods 0.000 claims description 18
- 230000002265 prevention Effects 0.000 claims description 16
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- -1 2-oxo-pyrrolidin-1-ylmethyl Chemical group 0.000 claims description 12
- 208000024827 Alzheimer disease Diseases 0.000 claims description 12
- 208000010412 Glaucoma Diseases 0.000 claims description 12
- 208000018737 Parkinson disease Diseases 0.000 claims description 12
- 201000006417 multiple sclerosis Diseases 0.000 claims description 12
- 230000004936 stimulating effect Effects 0.000 claims description 12
- 210000002569 neuron Anatomy 0.000 claims description 11
- 208000000172 Medulloblastoma Diseases 0.000 claims description 10
- 208000012902 Nervous system disease Diseases 0.000 claims description 10
- 230000000638 stimulation Effects 0.000 claims description 10
- 102000015534 trkB Receptor Human genes 0.000 claims description 10
- 108010064880 trkB Receptor Proteins 0.000 claims description 10
- 102000007339 Nerve Growth Factor Receptors Human genes 0.000 claims description 9
- 108010032605 Nerve Growth Factor Receptors Proteins 0.000 claims description 9
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 9
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 8
- 230000004112 neuroprotection Effects 0.000 claims description 8
- 102000005962 receptors Human genes 0.000 claims description 8
- 108020003175 receptors Proteins 0.000 claims description 8
- 230000008929 regeneration Effects 0.000 claims description 8
- 238000011069 regeneration method Methods 0.000 claims description 8
- 208000025966 Neurological disease Diseases 0.000 claims description 7
- 229940079593 drug Drugs 0.000 claims description 7
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 6
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 6
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 6
- 206010006187 Breast cancer Diseases 0.000 claims description 6
- 208000026310 Breast neoplasm Diseases 0.000 claims description 6
- 208000017897 Carcinoma of esophagus Diseases 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims description 6
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 6
- 208000024412 Friedreich ataxia Diseases 0.000 claims description 6
- 206010065681 HIV peripheral neuropathy Diseases 0.000 claims description 6
- 208000023105 Huntington disease Diseases 0.000 claims description 6
- 201000002832 Lewy body dementia Diseases 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 6
- 206010029260 Neuroblastoma Diseases 0.000 claims description 6
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims description 6
- 206010033128 Ovarian cancer Diseases 0.000 claims description 6
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 6
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 208000032839 leukemia Diseases 0.000 claims description 6
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 6
- 208000024714 major depressive disease Diseases 0.000 claims description 6
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 6
- 206010027191 meningioma Diseases 0.000 claims description 6
- 208000007538 neurilemmoma Diseases 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- 230000003959 neuroinflammation Effects 0.000 claims description 6
- 230000000324 neuroprotective effect Effects 0.000 claims description 6
- 201000008968 osteosarcoma Diseases 0.000 claims description 6
- 201000002528 pancreatic cancer Diseases 0.000 claims description 6
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 6
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 6
- 201000000980 schizophrenia Diseases 0.000 claims description 6
- 208000002320 spinal muscular atrophy Diseases 0.000 claims description 6
- 102000015336 Nerve Growth Factor Human genes 0.000 claims description 5
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 5
- 201000005619 esophageal carcinoma Diseases 0.000 claims description 5
- 230000002519 immonomodulatory effect Effects 0.000 claims description 5
- 229940053128 nerve growth factor Drugs 0.000 claims description 5
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 4
- 102000004219 Brain-derived neurotrophic factor Human genes 0.000 claims description 4
- 108090000715 Brain-derived neurotrophic factor Proteins 0.000 claims description 4
- 102100033733 Tumor necrosis factor receptor superfamily member 1B Human genes 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 4
- 229940077737 brain-derived neurotrophic factor Drugs 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 208000005017 glioblastoma Diseases 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 239000002955 immunomodulating agent Substances 0.000 claims description 4
- 230000002584 immunomodulator Effects 0.000 claims description 4
- 229940121354 immunomodulator Drugs 0.000 claims description 4
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 4
- 210000005036 nerve Anatomy 0.000 claims description 4
- 230000000926 neurological effect Effects 0.000 claims description 4
- 208000020016 psychiatric disease Diseases 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 230000016273 neuron death Effects 0.000 claims description 3
- 230000003961 neuronal insult Effects 0.000 claims description 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 2
- 125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004493 2-methylbut-1-yl group Chemical group CC(C*)CC 0.000 claims description 2
- 125000005916 2-methylpentyl group Chemical group 0.000 claims description 2
- 125000005917 3-methylpentyl group Chemical group 0.000 claims description 2
- 206010003571 Astrocytoma Diseases 0.000 claims description 2
- 201000000053 blastoma Diseases 0.000 claims description 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 230000005779 cell damage Effects 0.000 claims description 2
- 230000030833 cell death Effects 0.000 claims description 2
- 208000037887 cell injury Diseases 0.000 claims description 2
- 201000008184 embryoma Diseases 0.000 claims description 2
- 125000001207 fluorophenyl group Chemical group 0.000 claims description 2
- 239000003292 glue Substances 0.000 claims description 2
- 150000002367 halogens Chemical class 0.000 claims description 2
- 210000003494 hepatocyte Anatomy 0.000 claims description 2
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 2
- 230000001172 regenerating effect Effects 0.000 claims description 2
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 2
- 102000015533 trkA Receptor Human genes 0.000 claims description 2
- 108010064884 trkA Receptor Proteins 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 38
- 210000004027 cell Anatomy 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 230000034994 death Effects 0.000 claims 1
- 230000007794 irritation Effects 0.000 claims 1
- 201000010901 lateral sclerosis Diseases 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 22
- 238000011321 prophylaxis Methods 0.000 description 2
- 210000004556 brain Anatomy 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37882310P | 2010-08-31 | 2010-08-31 | |
| US61/378,823 | 2010-08-31 | ||
| PCT/IB2011/002562 WO2012028959A1 (en) | 2010-08-31 | 2011-08-31 | Agonists of neurotrophin receptors and their use as medicaments |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013536833A JP2013536833A (ja) | 2013-09-26 |
| JP2013536833A5 true JP2013536833A5 (enExample) | 2014-10-09 |
| JP5946454B2 JP5946454B2 (ja) | 2016-07-06 |
Family
ID=45048148
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013526566A Active JP5946454B2 (ja) | 2010-08-31 | 2011-08-31 | ニューロトロフィン受容体のアゴニストおよび医薬としてのその使用 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8791076B2 (enExample) |
| EP (1) | EP2611775B8 (enExample) |
| JP (1) | JP5946454B2 (enExample) |
| KR (1) | KR101964954B1 (enExample) |
| CN (1) | CN103270022B (enExample) |
| AU (1) | AU2011298091B2 (enExample) |
| BR (1) | BR112013004662B8 (enExample) |
| CA (1) | CA2809774C (enExample) |
| DK (1) | DK2611775T3 (enExample) |
| ES (1) | ES2575684T3 (enExample) |
| HR (1) | HRP20160553T1 (enExample) |
| HU (1) | HUE029393T2 (enExample) |
| IL (1) | IL224972A (enExample) |
| MX (1) | MX340233B (enExample) |
| PL (1) | PL2611775T3 (enExample) |
| PT (1) | PT2611775E (enExample) |
| RU (1) | RU2606622C2 (enExample) |
| SI (1) | SI2611775T1 (enExample) |
| WO (1) | WO2012028959A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2289886A1 (en) * | 2009-08-31 | 2011-03-02 | Institut d'Investigacions Biomédiques August PI I Sunyer | Peptoid agonists of nerve growth factor and their use as medicaments |
| AU2011298091B2 (en) | 2010-08-31 | 2015-08-20 | Accure Therapeutics, S.L. | Agonists of neurotrophin receptors and their use as medicaments |
| WO2014100433A1 (en) * | 2012-12-19 | 2014-06-26 | Brown University | Methods for treatment of microcephaly associated autism disorders |
| EP2950095B1 (en) * | 2014-05-28 | 2018-08-29 | Technische Universität Dresden | Cell-based assay and screening methods for modulators of p75NTR signaling |
| WO2018039641A1 (en) * | 2016-08-25 | 2018-03-01 | Pharmatrophix, Inc. | Methods and compounds for treating alcohol use disorders and associated diseases |
| KR101821118B1 (ko) | 2016-09-06 | 2018-01-23 | 가톨릭대학교 산학협력단 | 감보그 산(gambogic acid)을 포함한 알러지성 질환 예방 또는 치료용 조성물 |
| CN107802823A (zh) * | 2017-10-27 | 2018-03-16 | 胡军 | Sh2b衔接蛋白1在治疗帕金森病中的功能应用 |
| JP2021530507A (ja) * | 2018-07-18 | 2021-11-11 | マンザニータ ファーマシューティカルズ，インク． | 神経細胞に抗がん剤を送達するためのコンジュゲート、その使用方法及び製造方法 |
| AU2019391942B2 (en) | 2018-12-05 | 2024-03-21 | Scohia Pharma, Inc. | Macrocyclic compound and use thereof |
| TW202116297A (zh) * | 2019-07-03 | 2021-05-01 | 西班牙商布爾奴爾法碼有限公司 | 組合療法之方法、組成物與套組 |
| JP2022548337A (ja) * | 2019-09-03 | 2022-11-17 | ピーター ジェイ． シークマイヤー， | グルタミン酸受容体アゴニストにより認知機能を増加させる方法 |
| TW202131914A (zh) * | 2019-10-30 | 2021-09-01 | 西班牙商布爾奴爾法碼有限公司 | 用於神經疾病或病狀的治療之新治療方案 |
| JPWO2023190675A1 (enExample) | 2022-03-30 | 2023-10-05 | ||
| IL321571A (en) * | 2022-12-22 | 2025-08-01 | Oculis Operations S?Rl | Synthesis of small molecules that are agonists for neurotrophins |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU189214B (en) | 1983-01-20 | 1986-06-30 | Alkaloida Vegyeszeti Gyar,Hu | Process for preparing pyrroline and pyrrolidine carboxamide derivatives |
| US6271205B1 (en) | 1994-09-21 | 2001-08-07 | University Of Massachusetts Medical Center | Cancer treatment by expression of differentiation factor receptor |
| US5747458A (en) | 1995-06-07 | 1998-05-05 | Chiron Corporation | Urokinase receptor ligands |
| US6391871B1 (en) | 1996-09-20 | 2002-05-21 | John W. Olney | Preventing neuronal degeneration in Alzheimer's disease |
| DE19751062A1 (de) | 1997-11-18 | 1999-07-08 | Univ Ludwigs Albert | An 4-Stellung substituierte 2-Pyrrolidinon-Derivate zur Verringerung des extrazellulären Glutamat-Spiegels |
| US6124361A (en) | 1997-12-31 | 2000-09-26 | Pfizer Inc | Bicyclo[3.1.0]hexanes and related compounds |
| CZ304308B6 (cs) | 2000-05-04 | 2014-02-26 | Basf Aktiengesellschaft | Fenylsulfamoylové karboxamidy, substituované uracilem, způsob jejich přípravy a herbicidní kompozice s jejich obsahem |
| ES2169690B1 (es) * | 2000-10-06 | 2004-03-16 | Diverdrugs Sl | Trimeros de n-alquilglicina capaces de proteger a neuronas contra agresiones excitotoxicas, y composiciones que los contienen. |
| ES2169691B1 (es) * | 2000-10-11 | 2004-03-16 | Diverdrugs Sl | Trimeros de n-alquilglicina capaces de bloquear la respuesta a sustancias quimicas, estimulos termicos o mediadores de la inflamacion de receptores neuronales, y composiciones que los contienen. |
| CA2506850C (en) | 2002-11-20 | 2014-05-13 | Neuronova Ab | Compounds and methods for increasing neurogenesis |
| DE10303229B4 (de) | 2003-01-28 | 2007-07-26 | Keyneurotek Ag | Ambroxol und Inhibitoren des Angiotensin Converting-Enzyms (ACE) umfassende Arzneimittel Arzneimittel-Zubereitung und ihre Verwendung zur Behandlung von neurodegenerativen Erkrankungen |
| US20110052603A1 (en) | 2006-10-06 | 2011-03-03 | The Walter And Eliza Hall Institute Of Medical Research | method of treatment and agents useful for same |
| EP1994944A1 (en) * | 2007-05-21 | 2008-11-26 | Laboratorios SALVAT, S.A. | Polymer conjugate compounds for the inhibition of apoptosis |
| JP5602020B2 (ja) | 2008-09-24 | 2014-10-08 | 株式会社リボミック | Ｎｇｆに対するアプタマー及びその使用 |
| RU2410392C2 (ru) * | 2009-02-16 | 2011-01-27 | Учреждение Российской академии медицинских наук Научно-исследовательский институт фармакологии имени В.В. Закусова РАМН | Дипептидные миметики нейротрофинов ngf и bdnf |
| EP2289882A1 (en) | 2009-08-31 | 2011-03-02 | Institut d'Investigacions Biomédiques August PI I Sunyer | 3-oxopiperazinium derivatives as agonists of nerve growth factor and their use as medicaments |
| EP2289886A1 (en) * | 2009-08-31 | 2011-03-02 | Institut d'Investigacions Biomédiques August PI I Sunyer | Peptoid agonists of nerve growth factor and their use as medicaments |
| AU2011298091B2 (en) | 2010-08-31 | 2015-08-20 | Accure Therapeutics, S.L. | Agonists of neurotrophin receptors and their use as medicaments |
-
2011
- 2011-08-31 AU AU2011298091A patent/AU2011298091B2/en active Active
- 2011-08-31 JP JP2013526566A patent/JP5946454B2/ja active Active
- 2011-08-31 MX MX2013002329A patent/MX340233B/es active IP Right Grant
- 2011-08-31 SI SI201130839A patent/SI2611775T1/sl unknown
- 2011-08-31 WO PCT/IB2011/002562 patent/WO2012028959A1/en not_active Ceased
- 2011-08-31 EP EP11788579.8A patent/EP2611775B8/en active Active
- 2011-08-31 US US13/223,166 patent/US8791076B2/en active Active
- 2011-08-31 RU RU2013113634A patent/RU2606622C2/ru active
- 2011-08-31 CA CA2809774A patent/CA2809774C/en active Active
- 2011-08-31 CN CN201180049622.8A patent/CN103270022B/zh active Active
- 2011-08-31 ES ES11788579.8T patent/ES2575684T3/es active Active
- 2011-08-31 HR HRP20160553TT patent/HRP20160553T1/hr unknown
- 2011-08-31 KR KR1020137008259A patent/KR101964954B1/ko active Active
- 2011-08-31 PT PT117885798T patent/PT2611775E/pt unknown
- 2011-08-31 DK DK11788579.8T patent/DK2611775T3/en active
- 2011-08-31 PL PL11788579.8T patent/PL2611775T3/pl unknown
- 2011-08-31 BR BR112013004662A patent/BR112013004662B8/pt active IP Right Grant
- 2011-08-31 HU HUE11788579A patent/HUE029393T2/en unknown
-
2013
- 2013-02-28 IL IL224972A patent/IL224972A/en active IP Right Grant
-
2014
- 2014-06-11 US US14/301,981 patent/US9453047B2/en active Active
-
2016
- 2016-09-09 US US15/261,410 patent/US10106577B2/en active Active
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