JP2008545793A5 - - Google Patents
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- JP2008545793A5 JP2008545793A5 JP2008515915A JP2008515915A JP2008545793A5 JP 2008545793 A5 JP2008545793 A5 JP 2008545793A5 JP 2008515915 A JP2008515915 A JP 2008515915A JP 2008515915 A JP2008515915 A JP 2008515915A JP 2008545793 A5 JP2008545793 A5 JP 2008545793A5
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- JP
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- Prior art keywords
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- hydrogen atom
- aralkyl
- alkyl
- aryl
- Prior art date
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- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 124
- 125000000217 alkyl group Chemical group 0.000 claims 123
- 125000003710 aryl alkyl group Chemical group 0.000 claims 112
- 125000003118 aryl group Chemical group 0.000 claims 109
- 150000001875 compounds Chemical class 0.000 claims 43
- 125000005843 halogen group Chemical group 0.000 claims 40
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims 36
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 34
- 125000005117 dialkylcarbamoyl group Chemical group 0.000 claims 34
- 239000000126 substance Substances 0.000 claims 34
- 125000003545 alkoxy group Chemical group 0.000 claims 33
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 33
- 125000004104 aryloxy group Chemical group 0.000 claims 33
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 33
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 claims 31
- 125000004442 acylamino group Chemical group 0.000 claims 27
- 125000004423 acyloxy group Chemical group 0.000 claims 27
- -1 aralkylene group Chemical group 0.000 claims 27
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 27
- 125000005358 mercaptoalkyl group Chemical group 0.000 claims 27
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 27
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate dianion Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 24
- 150000001408 amides Chemical class 0.000 claims 24
- 150000002148 esters Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 24
- 239000011780 sodium chloride Substances 0.000 claims 24
- 125000002947 alkylene group Chemical group 0.000 claims 18
- 125000006833 (C1-C5) alkylene group Chemical group 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 10
- 125000002252 acyl group Chemical group 0.000 claims 9
- 229940079593 drugs Drugs 0.000 claims 9
- 102000015534 trkB Receptor Human genes 0.000 claims 8
- 108010064880 trkB Receptor Proteins 0.000 claims 8
- 125000000732 arylene group Chemical group 0.000 claims 6
- 210000004027 cells Anatomy 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000005649 substituted arylene group Chemical group 0.000 claims 6
- 229940077737 Brain-Derived Neurotrophic Factor Drugs 0.000 claims 5
- 102000004219 Brain-Derived Neurotrophic Factor Human genes 0.000 claims 5
- 108090000715 Brain-Derived Neurotrophic Factor Proteins 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000004480 active ingredient Substances 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 230000001105 regulatory Effects 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 3
- 208000001293 Peripheral Nervous System Disease Diseases 0.000 claims 2
- 206010034606 Peripheral neuropathy Diseases 0.000 claims 2
- 230000003213 activating Effects 0.000 claims 2
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 claims 2
- 125000004429 atoms Chemical group 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000001809 detectable Effects 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 210000002569 neurons Anatomy 0.000 claims 2
- 230000001737 promoting Effects 0.000 claims 2
- 230000004083 survival Effects 0.000 claims 2
- 206010065040 AIDS dementia complex Diseases 0.000 claims 1
- 102100012672 ARTN Human genes 0.000 claims 1
- 101700061329 ARTN Proteins 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 206010002026 Amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 210000004556 Brain Anatomy 0.000 claims 1
- 208000001183 Brain Injury Diseases 0.000 claims 1
- 206010008118 Cerebral infarction Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 208000001636 Diabetic Neuropathy Diseases 0.000 claims 1
- 206010012680 Diabetic neuropathy Diseases 0.000 claims 1
- 206010015037 Epilepsy Diseases 0.000 claims 1
- 208000004559 Hearing Loss Diseases 0.000 claims 1
- 206010011879 Hearing loss Diseases 0.000 claims 1
- 201000001971 Huntington's disease Diseases 0.000 claims 1
- 206010021143 Hypoxia Diseases 0.000 claims 1
- 206010061255 Ischaemia Diseases 0.000 claims 1
- 102100014726 MECP2 Human genes 0.000 claims 1
- 101700029603 MECP2 Proteins 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000005264 Motor Neuron Disease Diseases 0.000 claims 1
- 206010028003 Motor neurone disease Diseases 0.000 claims 1
- 101700009327 NTF3 Proteins 0.000 claims 1
- 108060005033 NTRK2 Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061536 Parkinson's disease Diseases 0.000 claims 1
- 208000006289 Rett Syndrome Diseases 0.000 claims 1
- 208000008513 Spinal Cord Injury Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000011248 coating agent Substances 0.000 claims 1
- 238000000576 coating method Methods 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 231100000888 hearing loss Toxicity 0.000 claims 1
- 230000001146 hypoxic Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000003900 neurotrophic factor Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 0 *C(C1*)C(*C(*=C(C*I*)C=*)=O)*C1I* Chemical compound *C(C1*)C(*C(*=C(C*I*)C=*)=O)*C1I* 0.000 description 12
- CXIGIXHNCUFRDV-UHFFFAOYSA-N CCCN(CCO)c1ccc(C(c(cc2)ccc2N(CCO)CCO)c(cc2)ccc2Cl)cc1 Chemical compound CCCN(CCO)c1ccc(C(c(cc2)ccc2N(CCO)CCO)c(cc2)ccc2Cl)cc1 CXIGIXHNCUFRDV-UHFFFAOYSA-N 0.000 description 1
Claims (32)
- TrkB受容体に接触し、それを活性化し又はそれを抑止することにより治療できる疾患の治療を必要とする患者の疾患を治療するため又は神経細胞若しくはその他の細胞の生存を促進するための薬剤であって、有効量の、TrkB受容体分子に結合特異性及び/又は調節特異性を持つ化合物から成り、該化合物が脳由来神経栄養因子(BDNF)のβ−ターンループの類似体である薬剤。
- 前記疾患が、アルツハイマー病、ハンチントン病、筋萎縮性側索硬化症、レット症候群、てんかん、パーキンソン病、脊髄損傷、脳梗塞、低酸素症、虚血症、脳損傷、糖尿病性神経障害、末梢性神経障害、神経移植合併症、運動ニューロン病、多発性硬化症、HIV痴呆症、末梢神経障害、聴力損失、鬱病、肥満症、メタボリックシンドローム、痛み、癌、及びその他のTrkBを発現する細胞の変性又は機能不全を含む病気からなる群から選択される請求項1に記載の薬剤。
- 前記化合物が下記化学式(I)
- 前記化合物が下記化学式(II)
- 前記化合物が下記化学式(III)
- 前記化合物が下記化学式(IV)
- 前記化合物が下記化学式(V)
- 前記化合物が下記化学式(VI)
- 前記化合物が下記化学式(VII)
- 前記化合物が下記化学式(VIII)
- 前記化合物が下記化学式(IX)
- 前記化合物が下記化学式(X)
- 前記化合物が下記化学式(XI)
- TrkB受容体に結合特異性及び/又は調節特異性を持つ親化合物であって、該化合物が化学式(I)〜(XI)のいずれか1つの構造を有し、該化学式(I)が下記
該化学式(II)が下記
化学式(III)が下記
化学式(IV)が下記
化学式(V)が下記
化学式(VI)が下記
化学式(VII)が下記
化学式(VIII)が下記
化学式(IX)が下記
化学式(X)が下記
化学式(XI)が下記
又はこれらの医薬的に許容されうる塩、エステル、アミド若しくはカーボネートであり、
ただし、化学式(I)〜(XI)で表される化合物が下記
- TrkB受容体が存在する環境で用いるための医療機器の製法であって、該医療機器を、TrkB受容体分子に結合特異性及び/又は調節特異性を持つ化合物から成る組成物で被覆することからなり、該化合物が脳由来神経栄養因子(BDNF)のβ−ターンループの類似体である製法。
- 下記(a)及び(b)から成るTrkB受容体を有する細胞を描写する方法。
(a)該細胞に、TrkB受容体分子に結合特異性及び/又は調節特異性を持つ化合物を接触させる段階であって、該化合物が脳由来神経栄養因子(BDNF)のβ−ターンループの類似体であり、該化合物が更に検出可能なラベルを含む段階、及び
(b)該検出可能なラベルを検出し、それにより該細胞を描写する段階 - 活性成分と医薬グレードの担体との単位投与量から成る医薬組成物であって、該活性成分が化学式(I)〜(XI)のいずれか1つの構造を有する化合物から選択される化合物、又はこれらの医薬的に許容されうる塩、エステル、アミド若しくはカーボネートであり、該化学式(I)が下記
該化学式(II)が下記
化学式(III)が下記
化学式(IV)が下記
化学式(V)が下記
化学式(VI)が下記
化学式(VII)が下記
化学式(VIII)が下記
化学式(IX)が下記
化学式(X)が下記
化学式(XI)が下記
- 前記組成物が経口又は非経口投与のための組成物である請求項28又は29に記載の医薬組成物。
- 前記組成物が更に第2の活性成分を含む請求項28〜30のいずれか一項に記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US68876705P | 2005-06-08 | 2005-06-08 | |
US60/688,767 | 2005-06-08 | ||
PCT/US2006/022268 WO2006133353A2 (en) | 2005-06-08 | 2006-06-08 | Methods of facilitating neural cell survival using non-peptide and peptide bdnf neurotrophin mimetics |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2008545793A JP2008545793A (ja) | 2008-12-18 |
JP2008545793A5 true JP2008545793A5 (ja) | 2009-07-30 |
JP5461009B2 JP5461009B2 (ja) | 2014-04-02 |
Family
ID=37499118
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008515915A Active JP5461009B2 (ja) | 2005-06-08 | 2006-06-08 | 非ペプチド及びペプチドbdnfニューロトロフィン類似体を用いた神経細胞生存促進法 |
Country Status (5)
Country | Link |
---|---|
US (2) | US8686045B2 (ja) |
EP (3) | EP2581440B1 (ja) |
JP (1) | JP5461009B2 (ja) |
ES (1) | ES2569881T3 (ja) |
WO (1) | WO2006133353A2 (ja) |
Families Citing this family (33)
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ATE479754T1 (de) | 2003-03-19 | 2010-09-15 | Biogen Idec Inc | Nogo rezeptor bindendes protein |
RS52593B (en) | 2004-06-24 | 2013-04-30 | Biogen Idec Ma Inc. | TREATMENT OF THE CONDITIONS CONCERNING DEMYELINIZATION |
US20110230479A1 (en) * | 2005-04-15 | 2011-09-22 | Longo Frank M | Neurotrophin mimetics and uses thereof |
EP2586445A1 (en) * | 2005-04-15 | 2013-05-01 | University Of North Carolina At Chapel Hill | Methods of facilitating cell survival using neurotrophin mimetics |
ES2569881T3 (es) | 2005-06-08 | 2016-05-12 | The University Of North Carolina At Chapel Hill | Procedimientos para facilitar la supervivencia de células neuronales usando miméticos de neurotrofina BDNF peptídicos y no peptídicos |
EP2394661A1 (en) | 2005-07-08 | 2011-12-14 | Biogen Idec MA Inc. | Sp35 antibodies and uses thereof |
EP2114436A1 (en) * | 2006-12-20 | 2009-11-11 | Rinat Neuroscience Corp. | Trkb agonists for treating autoimmune disorders |
CA2701189C (en) * | 2007-10-11 | 2017-05-16 | Biogen Idec Ma Inc. | Methods for treating pressure induced optic neuropathy, preventing neuronal degeneration and promoting neuronal cell survival via administration of lingo-1 antagonists and trkb agonists |
CN101918540B (zh) * | 2007-11-08 | 2016-05-11 | 比奥根Ma公司 | Lingo-4拮抗剂在治疗涉及脱髓鞘的疾患中的应用 |
US20110217280A1 (en) * | 2007-12-19 | 2011-09-08 | Vollrath Benedikt | Methods for treating neuropsychiatric conditions |
US20100317715A1 (en) * | 2007-12-21 | 2010-12-16 | Vollrath Benedikt | Methods for treating neuropsychiatric conditions |
CA2997870A1 (en) | 2008-07-09 | 2010-01-14 | Biogen Ma Inc. | Compositions comprising antibodies to lingo or fragments thereof |
TW201100411A (en) | 2009-05-21 | 2011-01-01 | Chlorion Pharma Inc | Pyrimidines as novel therapeutic agents |
KR101138048B1 (ko) | 2009-11-06 | 2012-04-23 | 성균관대학교산학협력단 | Bdnf의 발현을 증가시키는 신규 펩타이드 및 이를 포함하는 알츠하이머병 또는 파킨슨병의 예방 및 치료용 약학 조성물 |
US10273219B2 (en) | 2009-11-12 | 2019-04-30 | Pharmatrophix, Inc. | Crystalline forms of neurotrophin mimetic compounds and their salts |
AU2010319349B2 (en) | 2009-11-12 | 2015-07-16 | Pharmatrophix, Inc. | Crystalline forms of neurotrophin mimetic compounds and their salts |
AU2010329847A1 (en) | 2009-12-11 | 2012-07-26 | Genecode As | Methods of facilitating neural cell survival using GDNF family ligand (GFL) mimetics or RET signaling pathway activators |
WO2011150347A2 (en) * | 2010-05-28 | 2011-12-01 | Pharmatrophix | Non-peptide bdnf neurotrophin mimetics |
NZ702178A (en) | 2012-05-14 | 2017-01-27 | Biogen Ma Inc | Lingo-2 antagonists for treatment of conditions involving motor neurons |
JP6120311B2 (ja) * | 2013-02-12 | 2017-04-26 | 学校法人銀杏学園 | ポリフェノール化合物 |
WO2014143985A1 (en) * | 2013-03-15 | 2014-09-18 | Pharmatrophix, Inc. | Non-peptide bdnf neurotrophin mimetics |
AU2014227623B2 (en) * | 2013-03-15 | 2018-08-16 | Pharmatrophix, Inc. | Non-peptide BDNF Neurotrophin mimetics |
WO2014169280A2 (en) | 2013-04-12 | 2014-10-16 | Achillion Pharmaceuticals, Inc. | Deuterated nucleoside prodrugs useful for treating hcv |
RS62434B1 (sr) | 2014-12-26 | 2021-11-30 | Univ Emory | Antivirusni n4-hidroksicitidin derivati |
JP2018504400A (ja) | 2015-01-08 | 2018-02-15 | バイオジェン・エムエイ・インコーポレイテッドBiogen MA Inc. | Lingo‐1拮抗薬及び脱髄障害の治療のための使用 |
WO2016196012A1 (en) * | 2015-05-29 | 2016-12-08 | The Board Of Trustees Of The Leland Stanford Junior University | Nucleoside agents for the reduction of the deleterious activity of extended nucleotide repeat containing genes |
EP3328440A4 (en) * | 2015-07-28 | 2019-01-16 | Otonomy, Inc. | TREATMENT USING TRK B TRK B TRK ANTAGONISTS |
CA3010615C (en) | 2016-01-14 | 2024-02-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
KR102626210B1 (ko) | 2017-12-07 | 2024-01-18 | 에모리 유니버시티 | N4-하이드록시사이티딘 및 유도체 및 이와 관련된 항-바이러스 용도 |
EP3886854A4 (en) | 2018-11-30 | 2022-07-06 | Nuvation Bio Inc. | PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE |
AU2021280287A1 (en) | 2020-05-27 | 2023-01-05 | Axial Therapeutics, Inc. | TLR2 modulator compounds, pharmaceutical compositions and uses thereof |
EP4074317A1 (en) | 2021-04-14 | 2022-10-19 | Bayer AG | Phosphorus derivatives as novel sos1 inhibitors |
WO2023078252A1 (en) | 2021-11-02 | 2023-05-11 | Flare Therapeutics Inc. | Pparg inverse agonists and uses thereof |
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EP2586445A1 (en) | 2005-04-15 | 2013-05-01 | University Of North Carolina At Chapel Hill | Methods of facilitating cell survival using neurotrophin mimetics |
ES2569881T3 (es) | 2005-06-08 | 2016-05-12 | The University Of North Carolina At Chapel Hill | Procedimientos para facilitar la supervivencia de células neuronales usando miméticos de neurotrofina BDNF peptídicos y no peptídicos |
-
2006
- 2006-06-08 ES ES12169982.1T patent/ES2569881T3/es active Active
- 2006-06-08 WO PCT/US2006/022268 patent/WO2006133353A2/en active Application Filing
- 2006-06-08 US US11/449,381 patent/US8686045B2/en active Active
- 2006-06-08 EP EP12169982.1A patent/EP2581440B1/en active Active
- 2006-06-08 JP JP2008515915A patent/JP5461009B2/ja active Active
- 2006-06-08 EP EP06784665A patent/EP1893192A4/en not_active Withdrawn
- 2006-06-08 EP EP12169984.7A patent/EP2526942B1/en active Active
-
2014
- 2014-01-27 US US14/165,090 patent/US9604907B2/en active Active
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