JP2011529917A5 - - Google Patents
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- Publication number
- JP2011529917A5 JP2011529917A5 JP2011521360A JP2011521360A JP2011529917A5 JP 2011529917 A5 JP2011529917 A5 JP 2011529917A5 JP 2011521360 A JP2011521360 A JP 2011521360A JP 2011521360 A JP2011521360 A JP 2011521360A JP 2011529917 A5 JP2011529917 A5 JP 2011529917A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- group
- alkynyl
- cycloalkyl
- 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
- 125000003118 aryl group Chemical group 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000000304 alkynyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- -1 amino, hydroxyl Chemical group 0.000 claims 7
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 7
- 150000001602 bicycloalkyls Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 5
- 125000005914 C6-C14 aryloxy group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000003358 C2-C20 alkenyl group Chemical group 0.000 claims 4
- YCWSUKQGVSGXJO-NTUHNPAUSA-N nifuroxazide Chemical group C1=CC(O)=CC=C1C(=O)N\N=C\C1=CC=C([N+]([O-])=O)O1 YCWSUKQGVSGXJO-NTUHNPAUSA-N 0.000 claims 4
- 125000003396 thiol group Chemical class [H]S* 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 3
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 3
- 125000005096 aminoalkylaminocarbonyl group Chemical group 0.000 claims 3
- 125000004663 dialkyl amino group Chemical group 0.000 claims 3
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 125000004665 trialkylsilyl group Chemical group 0.000 claims 3
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 2
- 125000006279 3-bromobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Br)=C1[H])C([H])([H])* 0.000 claims 2
- 125000006482 3-iodobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(I)=C1[H])C([H])([H])* 0.000 claims 2
- 125000003860 C1-C20 alkoxy group Chemical group 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000001769 aryl amino group Chemical group 0.000 claims 2
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 2
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 2
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims 2
- 230000000302 ischemic effect Effects 0.000 claims 2
- 210000000056 organ Anatomy 0.000 claims 2
- 125000005030 pyridylthio group Chemical group N1=C(C=CC=C1)S* 0.000 claims 2
- 125000005309 thioalkoxy group Chemical group 0.000 claims 2
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 2
- 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004916 (C1-C6) alkylcarbonyl group Chemical group 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 125000003852 3-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(Cl)=C1[H])C([H])([H])* 0.000 claims 1
- 102000009346 Adenosine receptors Human genes 0.000 claims 1
- 108050000203 Adenosine receptors Proteins 0.000 claims 1
- 206010006482 Bronchospasm Diseases 0.000 claims 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 241000159243 Toxicodendron radicans Species 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- 208000030961 allergic reaction Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000007885 bronchoconstriction Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000008602 contraction Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000003384 imaging method Methods 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000031225 myocardial ischemia Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000002285 radioactive effect Effects 0.000 claims 1
- 206010039083 rhinitis Diseases 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 0 CC(*)*(C)C1=C(*)*(C)C(C*)*C1C Chemical compound CC(*)*(C)C1=C(*)*(C)C(C*)*C1C 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8558808P | 2008-08-01 | 2008-08-01 | |
| US61/085,588 | 2008-08-01 | ||
| PCT/US2009/052439 WO2010014921A2 (en) | 2008-08-01 | 2009-07-31 | A3 adenosine receptor antagonists and partial agonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011529917A JP2011529917A (ja) | 2011-12-15 |
| JP2011529917A5 true JP2011529917A5 (enExample) | 2012-07-12 |
| JP5431476B2 JP5431476B2 (ja) | 2014-03-05 |
Family
ID=41111356
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011521360A Expired - Fee Related JP5431476B2 (ja) | 2008-08-01 | 2009-07-31 | Ａ３アデノシン受容体アンタゴニストおよびａ３アデノシン受容体部分アゴニスト |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8796291B2 (enExample) |
| EP (1) | EP2331542B1 (enExample) |
| JP (1) | JP5431476B2 (enExample) |
| AU (1) | AU2009276411B2 (enExample) |
| CA (1) | CA2732320C (enExample) |
| WO (1) | WO2010014921A2 (enExample) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010014921A2 (en) | 2008-08-01 | 2010-02-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
| US8735407B2 (en) * | 2008-03-31 | 2014-05-27 | The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services | Purine derivatives as A3 adenosine receptor-selective agonists |
| US8916570B2 (en) * | 2008-03-31 | 2014-12-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor agonists and antagonists |
| US9181253B2 (en) | 2008-08-01 | 2015-11-10 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Adenosine receptor agonists, partial agonists, and antagonists |
| EP2361242B1 (en) | 2008-10-17 | 2018-08-01 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| WO2010084160A1 (en) | 2009-01-21 | 2010-07-29 | Oryzon Genomics S.A. | Phenylcyclopropylamine derivatives and their medical use |
| CA2812683C (en) | 2009-09-25 | 2017-10-10 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| US8946296B2 (en) | 2009-10-09 | 2015-02-03 | Oryzon Genomics S.A. | Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use |
| WO2011106573A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011106105A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| US20130109645A1 (en) | 2010-03-31 | 2013-05-02 | The united States of America,as represented by Secretary,Dept.,of Health and Human Services | Adenosine receptor agonists for the treatment and prevention of vascular or joint capsule calcification disorders |
| HUE030938T2 (en) | 2010-04-19 | 2017-06-28 | Oryzon Genomics Sa | Lysine-specific demethylase-1 inhibitors and their use |
| MX341732B (es) | 2010-07-29 | 2016-08-30 | Oryzon Genomics S A * | Inhibidores de la demetilasa lsd1 basados en arilciclopropilamina y sus usos médicos. |
| WO2012013727A1 (en) | 2010-07-29 | 2012-02-02 | Oryzon Genomics S.A. | Cyclopropylamine derivatives useful as lsd1 inhibitors |
| US9061966B2 (en) | 2010-10-08 | 2015-06-23 | Oryzon Genomics S.A. | Cyclopropylamine inhibitors of oxidases |
| WO2012072713A2 (en) | 2010-11-30 | 2012-06-07 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae |
| EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| EP2750671A2 (en) * | 2011-05-19 | 2014-07-09 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| EP2741741A2 (en) * | 2011-05-19 | 2014-06-18 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| BR112014009306B1 (pt) | 2011-10-20 | 2021-07-20 | Oryzon Genomics S.A. | Compostos de (hetero)aril ciclopropilamina como inibidores de lsd1 |
| WO2013057322A1 (en) | 2011-10-20 | 2013-04-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| JP2013256491A (ja) * | 2012-05-14 | 2013-12-26 | Kyoto Univ | 不安定プラークへの選択的集積性に優れる化合物 |
| CN110003212B (zh) | 2013-11-27 | 2022-12-06 | 美国卫生和人力服务部 | A3腺苷受体激动剂 |
| ES2578363B1 (es) | 2015-01-22 | 2017-01-31 | Palobiofarma, S.L. | Moduladores de los receptores A3 de adenosina |
| ES2989621T3 (es) | 2016-04-21 | 2024-11-27 | Astrocyte Pharmaceuticals Inc | Compuestos y métodos para el tratamiento de afecciones neurológicas y cardiovasculares |
| ES2676535B1 (es) | 2017-01-20 | 2019-04-29 | Palobiofarma Sl | Moduladores de los receptores a3 de adenosina |
| JP7311855B2 (ja) | 2018-02-09 | 2023-07-20 | アストロサイト ファーマシューティカルズ， インコーポレイテッド | 嗜癖および関連する障害を処置するための化合物および方法 |
| AU2019346585B2 (en) | 2018-09-26 | 2025-02-27 | Astrocyte Pharmaceuticals, Inc. | Polymorphic compounds and uses thereof |
| WO2020168274A1 (en) | 2019-02-15 | 2020-08-20 | Saint Louis University | Treatment of chronic headaches |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU7331094A (en) | 1993-07-13 | 1995-02-13 | United States Of America, As Represented By The Secretary, Department Of Health And Human Services, The | A3 adenosine receptor agonists |
| US5688774A (en) | 1993-07-13 | 1997-11-18 | The United States Of America As Represented By The Department Of Health And Human Services | A3 adenosine receptor agonists |
| US5646156A (en) | 1994-04-25 | 1997-07-08 | Merck & Co., Inc. | Inhibition of eosinophil activation through A3 adenosine receptor antagonism |
| ATE548351T1 (de) | 1996-01-29 | 2012-03-15 | Us Of America Represented By The Secretary Dept Of Health And Human Services | Dihydropyridin-pyridin-, benzopyranon- und triazolochinazolin-derivate, deren herstellung und verwendung als adenosinrezeptor-antagonisten |
| US5840728A (en) | 1996-08-07 | 1998-11-24 | United States Of America As Represented By The Department Of Health And Human Services | Conformationally locked nucleoside analogs as antiherpetic agents |
| WO1998048699A1 (en) | 1997-04-30 | 1998-11-05 | The Board Of Trustees Of The Leland Stanford Junior University | Method of imaging cell death in vivo |
| AU750322B2 (en) | 1997-05-09 | 2002-07-18 | Trustees Of The University Of Pennsylvania, The | Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists |
| CA2302360C (en) | 1997-09-03 | 2005-11-15 | Immunomedics, Inc. | Fluorination of proteins and peptides for f-18 positron emission tomography |
| DE69924254D1 (de) | 1998-07-16 | 2005-04-21 | Univ Pennsylvania | Verwendung von a3-adenosine antagonisten zur herstellung eines arzneimittels zur senkung des augeninnendrucks |
| US6921825B2 (en) | 1998-09-16 | 2005-07-26 | King Pharmaceuticuals Research & Development, Inc. | Adenosine A3 receptor modulators |
| US6586413B2 (en) | 1999-11-05 | 2003-07-01 | The United States Of America As Represented By The Department Of Health And Human Services | Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists |
| EP1252160B1 (en) | 2000-01-14 | 2006-08-16 | The Government of the United States of America, as represented by the Secretary of the Department of Health and Human Services | Methanocarba cycloalkyl nucleoside analogues |
| GB2372742A (en) | 2001-03-03 | 2002-09-04 | Univ Leiden | C2,5'-Disubstituted and N6,C2,5'-trisubstituted adenosine derivatives and their different uses |
| US20030143282A1 (en) | 2002-01-28 | 2003-07-31 | Pnina Fishman | Adenosine A3 receptor agonist |
| WO2004030621A2 (en) | 2002-09-30 | 2004-04-15 | The Trustees Of Boston University | Method of treating cancer using adenosine and its analogs |
| CN101056879B (zh) | 2004-09-09 | 2011-10-05 | 美国政府卫生与公共服务部 | 作为a3和a1腺苷受体激动剂的嘌呤衍生物 |
| WO2006091905A1 (en) | 2005-02-25 | 2006-08-31 | Gilead Sciences, Inc. | Bicyclo (3.1.0) hexane derivatives as antiviral compounds |
| WO2006113204A2 (en) | 2005-04-15 | 2006-10-26 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Thymidine derivatives for treatmemt of kaposi's sarcoma |
| US7381714B2 (en) | 2005-05-19 | 2008-06-03 | Cv Therapeutics, Inc. | A1 adenosine receptor agonists |
| US20090221523A1 (en) | 2005-05-25 | 2009-09-03 | Tseng Christopher K | North-2'-deoxy-methanocarbathymidines as antiviral agents against poxviruses |
| WO2007002139A2 (en) | 2005-06-22 | 2007-01-04 | The Trustees Of The University Of Pennsylvania | Neuroprotection of retinal ganglion cells |
| GB0514809D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| WO2007043054A1 (en) | 2005-10-12 | 2007-04-19 | Can-Fite Biopharma Ltd. | Treatment and monitoring disease state of liver cancer |
| ATE540673T1 (de) | 2005-11-30 | 2012-01-15 | Can Fite Biopharma Ltd | Verwendung von a3-adenosin-rezeptor-agonisten bei der behandlung von osteoarthritis |
| EP1798233A1 (en) | 2005-12-19 | 2007-06-20 | Faust Pharmaceuticals | Pyrrolo[1,2-a]quinoxaline derivatives as Adenosine A3 receptor modulators and uses thereof |
| EP1976494A1 (en) | 2006-01-27 | 2008-10-08 | Can-Fite Biopharma Ltd. | Adenosine a3 receptor agonists for the treatment of dry eye disorders |
| CA2644613A1 (en) | 2006-03-07 | 2007-09-13 | Endacea, Inc. | Compositions and methods for treating respiratory disorders |
| GB0607944D0 (en) | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| DK2049127T3 (en) | 2006-05-23 | 2015-01-05 | Univ Connecticut | N-METHANOCARBA DERIVATIVES FOR TREATMENT OF HEART DISEASES |
| US20090029949A1 (en) | 2006-05-25 | 2009-01-29 | Parrill-Baker Abby L | GPCR Ligands Identified by Computational Modeling |
| WO2008006369A1 (en) | 2006-07-14 | 2008-01-17 | Santaris Pharma A/S | Adenosine receptor antagonists |
| WO2008023362A2 (en) | 2006-08-21 | 2008-02-28 | Can-Fite Biopharma Ltd. | Use of a combination of methotrexate and an a3ar agonist for the treatment of cancer |
| US20100047798A1 (en) | 2006-11-08 | 2010-02-25 | Thomas Jefferson University | Adenosine a1 and a3 receptor gene sequence variations for predicting disease outcome and treatment outcome |
| CA2669166A1 (en) | 2006-11-09 | 2008-05-15 | Centre De Recherche Public De La Sante | Use of an adenosine antagonist |
| WO2008056361A1 (en) | 2006-11-09 | 2008-05-15 | Can-Fite Biopharma Ltd. | A biological marker for psoriasis |
| GB0625100D0 (en) | 2006-12-15 | 2007-01-24 | Univ Murcia | Epigallocatechin-3-gallate compositions for cancer therapy and chemoprotection |
| US8735407B2 (en) * | 2008-03-31 | 2014-05-27 | The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services | Purine derivatives as A3 adenosine receptor-selective agonists |
| WO2010014921A2 (en) | 2008-08-01 | 2010-02-04 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor antagonists and partial agonists |
| US8916570B2 (en) * | 2008-03-31 | 2014-12-23 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor agonists and antagonists |
| US9181253B2 (en) * | 2008-08-01 | 2015-11-10 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Adenosine receptor agonists, partial agonists, and antagonists |
| EP2507241A1 (en) * | 2009-12-02 | 2012-10-10 | The U.S.A. As Represented By The Secretary, Department Of Health And Human Services | Methanocarba adenosine derivatives and dendrimer conjugates thereof |
| WO2012145098A1 (en) * | 2011-04-21 | 2012-10-26 | Saint Louis University | Use of adenosine a3 receptor agonists for treatment of neuropathic pain |
-
2009
- 2009-07-31 WO PCT/US2009/052439 patent/WO2010014921A2/en not_active Ceased
- 2009-07-31 EP EP09791060.8A patent/EP2331542B1/en not_active Not-in-force
- 2009-07-31 US US13/056,997 patent/US8796291B2/en not_active Expired - Fee Related
- 2009-07-31 AU AU2009276411A patent/AU2009276411B2/en not_active Ceased
- 2009-07-31 CA CA2732320A patent/CA2732320C/en not_active Expired - Fee Related
- 2009-07-31 JP JP2011521360A patent/JP5431476B2/ja not_active Expired - Fee Related
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