JP2010515747A5 - - Google Patents
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- Publication number
- JP2010515747A5 JP2010515747A5 JP2009545660A JP2009545660A JP2010515747A5 JP 2010515747 A5 JP2010515747 A5 JP 2010515747A5 JP 2009545660 A JP2009545660 A JP 2009545660A JP 2009545660 A JP2009545660 A JP 2009545660A JP 2010515747 A5 JP2010515747 A5 JP 2010515747A5
- Authority
- JP
- Japan
- Prior art keywords
- alkenylene
- heterocycloalkyl
- alkylene
- cycloalkyl
- heteroaryl
- 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.)
- Pending
Links
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 54
- 125000004450 alkenylene group Chemical group 0.000 claims 52
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 36
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 35
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 25
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000002947 alkylene group Chemical group 0.000 claims 20
- 125000003342 alkenyl group Chemical group 0.000 claims 18
- 125000005275 alkylenearyl group Chemical group 0.000 claims 18
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 18
- 125000003118 aryl group Chemical group 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 18
- 125000000547 substituted alkyl group Chemical group 0.000 claims 18
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 9
- LHQIJBMDNUYRAM-AWFVSMACSA-N D-erythro-biopterin Chemical compound N1=C(N)NC(=O)C2=NC([C@H](O)[C@H](O)C)=CN=C21 LHQIJBMDNUYRAM-AWFVSMACSA-N 0.000 claims 7
- 206010020772 Hypertension Diseases 0.000 claims 6
- LHQIJBMDNUYRAM-UHFFFAOYSA-N L-erythro-Biopterin Natural products N1=C(N)NC(=O)C2=NC(C(O)C(O)C)=CN=C21 LHQIJBMDNUYRAM-UHFFFAOYSA-N 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 150000003862 amino acid derivatives Chemical class 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000019553 vascular disease Diseases 0.000 claims 5
- 201000011252 Phenylketonuria Diseases 0.000 claims 4
- 239000002202 Polyethylene glycol Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 229920001223 polyethylene glycol Polymers 0.000 claims 4
- FEMXZDUTFRTWPE-DZSWIPIPSA-N L-erythro-7,8-dihydrobiopterin Chemical group N1C(N)=NC(=O)C2=C1NCC([C@@H](O)[C@@H](O)C)=N2 FEMXZDUTFRTWPE-DZSWIPIPSA-N 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010048554 Endothelial dysfunction Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 206010022562 Intermittent claudication Diseases 0.000 claims 2
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 2
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 2
- 206010063837 Reperfusion injury Diseases 0.000 claims 2
- 208000007536 Thrombosis Diseases 0.000 claims 2
- 102000005506 Tryptophan Hydroxylase Human genes 0.000 claims 2
- 108010031944 Tryptophan Hydroxylase Proteins 0.000 claims 2
- 108091000117 Tyrosine 3-Monooxygenase Proteins 0.000 claims 2
- 102000048218 Tyrosine 3-monooxygenases Human genes 0.000 claims 2
- 206010047163 Vasospasm Diseases 0.000 claims 2
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 2
- 230000003247 decreasing effect Effects 0.000 claims 2
- 230000008694 endothelial dysfunction Effects 0.000 claims 2
- 208000021156 intermittent vascular claudication Diseases 0.000 claims 2
- 208000012947 ischemia reperfusion injury Diseases 0.000 claims 2
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 230000024883 vasodilation Effects 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000014249 Classic phenylketonuria Diseases 0.000 claims 1
- 206010053567 Coagulopathies Diseases 0.000 claims 1
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000014094 Dystonic disease Diseases 0.000 claims 1
- 208000004248 Familial Primary Pulmonary Hypertension Diseases 0.000 claims 1
- 206010018910 Haemolysis Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 1
- 208000014252 Mild phenylketonuria Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000024248 Vascular System injury Diseases 0.000 claims 1
- 208000012339 Vascular injury Diseases 0.000 claims 1
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- -1 aminoglucosyl Chemical group 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 230000035602 clotting Effects 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000010118 dystonia Diseases 0.000 claims 1
- 238000000835 electrochemical detection Methods 0.000 claims 1
- 238000001917 fluorescence detection Methods 0.000 claims 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 claims 1
- 230000008588 hemolysis Effects 0.000 claims 1
- 208000007475 hemolytic anemia Diseases 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 229950003188 isovaleryl diethylamide Drugs 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 201000004792 malaria Diseases 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 239000002858 neurotransmitter agent Substances 0.000 claims 1
- 230000003647 oxidation Effects 0.000 claims 1
- 238000007254 oxidation reaction Methods 0.000 claims 1
- 210000001147 pulmonary artery Anatomy 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 238000006722 reduction reaction Methods 0.000 claims 1
- 238000004007 reversed phase HPLC Methods 0.000 claims 1
- 229940076279 serotonin Drugs 0.000 claims 1
- 210000002966 serum Anatomy 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
- 230000000391 smoking effect Effects 0.000 claims 1
- 210000002700 urine Anatomy 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US88472707P | 2007-01-12 | 2007-01-12 | |
| PCT/US2008/050637 WO2008089008A2 (en) | 2007-01-12 | 2008-01-09 | Tetrahydrobiopterin prodrugs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010515747A JP2010515747A (ja) | 2010-05-13 |
| JP2010515747A5 true JP2010515747A5 (enExample) | 2011-03-03 |
Family
ID=39535519
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009545660A Pending JP2010515747A (ja) | 2007-01-12 | 2008-01-09 | テトラヒドロビオプテリンプロドラッグ |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20100016328A1 (enExample) |
| EP (1) | EP2114944A2 (enExample) |
| JP (1) | JP2010515747A (enExample) |
| AR (1) | AR064874A1 (enExample) |
| AU (1) | AU2008206486C1 (enExample) |
| CA (1) | CA2675134A1 (enExample) |
| CL (1) | CL2008000094A1 (enExample) |
| PE (1) | PE20081612A1 (enExample) |
| TW (1) | TW200843778A (enExample) |
| WO (1) | WO2008089008A2 (enExample) |
Families Citing this family (61)
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|---|---|---|---|---|
| ES2524026T3 (es) | 2008-01-03 | 2014-12-03 | Biomarin Pharmaceutical Inc. | Análogo de pterina para tratar una afección que responde a BH4 |
| CA2711444C (en) | 2008-01-07 | 2017-12-12 | Biomarin Pharmaceutical Inc. | Method of synthesizing tetrahydrobiopterin |
| EP2562176B1 (en) | 2010-04-22 | 2018-08-15 | Nihon University | Medicinal agent and beverage/food for preventing cerebral dysfunction and improving same |
| US9260462B2 (en) | 2011-02-18 | 2016-02-16 | Alexion Pharmaceuticals, Inc. | Methods for synthesizing molybdopterin precursor Z derivatives |
| ES2773376T3 (es) * | 2011-08-31 | 2020-07-10 | Catabasis Pharmaceuticals Inc | Amidas de ácidos grasos, composiciones y procedimientos de uso |
| WO2014037832A2 (en) | 2012-09-06 | 2014-03-13 | Mahesh Kandula | Compositions and methods for the treatment of epilepsy and neurological diseases |
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| WO2013167990A1 (en) | 2012-05-07 | 2013-11-14 | Mahesh Kandula | Compositions and methods for the treatment of depression |
| JP2015519333A (ja) | 2012-05-07 | 2015-07-09 | セリックスビオ プライヴェート リミテッド | 神経疾患の治療のための組成物および方法 |
| CN104603096A (zh) | 2012-05-07 | 2015-05-06 | 塞利克斯比奥私人有限公司 | 用于治疗神经肌肉障碍和神经退行性疾病的组合物和方法 |
| US9434704B2 (en) | 2012-05-08 | 2016-09-06 | Cellix Bio Private Limited | Compositions and methods for the treatment of neurological degenerative disorders |
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| WO2014037833A2 (en) | 2012-09-06 | 2014-03-13 | Mahesh Kandula | Compositions and methods for the treatment inflammation and lipid disorders |
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| WO2014041446A2 (en) * | 2012-09-17 | 2014-03-20 | Mahesh Kandula | Compositions and methods for the treatment of metabolic diseases |
| EP2968792B1 (en) | 2013-03-11 | 2019-05-15 | Antares Pharma, Inc. | Dosage injector with pinion system |
| US9333187B1 (en) | 2013-05-15 | 2016-05-10 | Cellix Bio Private Limited | Compositions and methods for the treatment of inflammatory bowel disease |
| SG11201509782TA (en) | 2013-06-04 | 2015-12-30 | Cellix Bio Private Ltd | Compositions and methods for the treatment of diabetes and pre-diabetes |
| US9096537B1 (en) | 2014-12-31 | 2015-08-04 | Mahesh Kandula | Compositions and methods for the treatment of mucositis |
| NZ736131A (en) | 2014-09-26 | 2019-04-26 | Cellix Bio Private Ltd | Compositions and methods for the treatment of epilepsy and neurological disorders |
| JP6698643B2 (ja) | 2014-09-29 | 2020-05-27 | セリックス バイオ プライヴェート リミテッドＣｅｌｌｉｘ Ｂｉｏ Ｐｒｉｖａｔｅ Ｌｉｍｉｔｅｄ | 多発性硬化症の治療のための組成物及び方法 |
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| US9173877B1 (en) | 2014-11-05 | 2015-11-03 | Cellix Bio Private Limited | Compositions and methods for the treatment of local pain |
| US9150557B1 (en) | 2014-11-05 | 2015-10-06 | Cellix Bio Private Limited | Compositions and methods for the treatment of hyperglycemia |
| US9290486B1 (en) | 2014-11-05 | 2016-03-22 | Cellix Bio Private Limited | Compositions and methods for the treatment of epilepsy |
| US9932294B2 (en) | 2014-12-01 | 2018-04-03 | Cellix Bio Private Limited | Compositions and methods for the treatment of multiple sclerosis |
| US9206111B1 (en) | 2014-12-17 | 2015-12-08 | Cellix Bio Private Limited | Compositions and methods for the treatment of neurological diseases |
| EP3242869B1 (en) | 2015-01-06 | 2021-10-27 | Cellixbio Private Limited | Compositions and methods for the treatment of inflammation and pain |
| US20190076434A1 (en) * | 2016-04-01 | 2019-03-14 | University Of Utah Research Foundation | Methods of treating peripheral vascular diseases, including systemic sclerosis vasculopathy |
| GB2566516A (en) | 2017-09-15 | 2019-03-20 | Univ Oxford Innovation Ltd | Electrochemical recognition and quantification of cytochrome c oxidase expression in bacteria |
| WO2019175332A1 (en) | 2018-03-14 | 2019-09-19 | Imba - Institut Für Molekulare Biotechnologie Gmbh | Bh4 pathway inhibition and use thereof for treating t-cell mediated autoimmune diseases or hypersensitivity |
| WO2019175328A1 (en) | 2018-03-14 | 2019-09-19 | Imba - Institut Für Molekulare Biotechnologie Gmbh | Bh4pathwayactivationandusethereoffortreatingcancer |
| US11471963B2 (en) | 2019-01-25 | 2022-10-18 | Black & Decker Inc. | Reciprocating saw blade |
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| DE19944767A1 (de) * | 1999-09-17 | 2001-03-29 | Vasopharm Biotech Gmbh & Co Kg | N-substituierte 4-Aminopteridine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel |
| US20030078231A1 (en) * | 2001-06-22 | 2003-04-24 | Wilburn Michael D. | Orthomolecular sulpho-adenosylmethionine derivatives with antioxidant properties |
| DE10260263A1 (de) * | 2002-12-20 | 2004-07-15 | Biocrates Life Sciences Gmbh | Verwendung von Tetrahydrobiopterinderivaten zur Behandlung und Ernährung von Patienten mit Aminosäurestoffwechselstörungen |
| US20050137141A1 (en) * | 2003-10-24 | 2005-06-23 | John Hilfinger | Prodrug composition |
| US20070167353A1 (en) * | 2003-10-24 | 2007-07-19 | John Hilfinger | Prodrug composition |
| JP5184783B2 (ja) * | 2003-11-17 | 2013-04-17 | バイオマリン ファーマシューティカル インコーポレイテッド | テトラヒドロビオプテリン、及びテトラヒドロビオプテリン類似体の製造方法 |
| PL1708690T3 (pl) * | 2003-11-17 | 2017-01-31 | Biomarin Pharmaceutical Inc. | Leczenie fenyloketonurii za pomocą BH4 |
| US7067659B2 (en) * | 2004-04-23 | 2006-06-27 | Duke University | Reactive oxygen generating enzyme inhibitor with nitric oxide bioactivity and uses thereof |
| WO2006055511A2 (en) * | 2004-11-17 | 2006-05-26 | Biomarin Pharmaceutical Inc. | Stable tablet formulation of tetrahydrobiopterin |
| US20060194800A1 (en) * | 2005-01-07 | 2006-08-31 | University Of Strathclyde | Pteridine derivatives as nitric oxide synthase activators |
| US20060194808A1 (en) * | 2005-01-14 | 2006-08-31 | Chronorx Llc, An Alaska Limited Liability Company | Clinical applications of tetrahydrobiopterin, lipoic acid and their salts and methods of preparing tetrahydrobiopterin bis-lipoate |
| ES2524026T3 (es) * | 2008-01-03 | 2014-12-03 | Biomarin Pharmaceutical Inc. | Análogo de pterina para tratar una afección que responde a BH4 |
-
2008
- 2008-01-09 JP JP2009545660A patent/JP2010515747A/ja active Pending
- 2008-01-09 EP EP08705803A patent/EP2114944A2/en not_active Withdrawn
- 2008-01-09 CA CA002675134A patent/CA2675134A1/en not_active Abandoned
- 2008-01-09 WO PCT/US2008/050637 patent/WO2008089008A2/en not_active Ceased
- 2008-01-09 AU AU2008206486A patent/AU2008206486C1/en not_active Ceased
- 2008-01-11 TW TW097101226A patent/TW200843778A/zh unknown
- 2008-01-11 AR ARP080100139A patent/AR064874A1/es unknown
- 2008-01-11 PE PE2008000117A patent/PE20081612A1/es not_active Application Discontinuation
- 2008-01-11 CL CL200800094A patent/CL2008000094A1/es unknown
-
2009
- 2009-07-09 US US12/500,537 patent/US20100016328A1/en not_active Abandoned
-
2011
- 2011-09-16 US US13/235,115 patent/US20120022072A1/en not_active Abandoned
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