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 (https=) | 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 (https=) |
| EP (1) | EP2331542B1 (https=) |
| JP (1) | JP5431476B2 (https=) |
| AU (1) | AU2009276411B2 (https=) |
| CA (1) | CA2732320C (https=) |
| WO (1) | WO2010014921A2 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2009231978C1 (en) * | 2008-03-31 | 2014-01-30 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Purine derivatives as A3 adenosine receptor- selective agonists |
| EP2331542B1 (en) | 2008-08-01 | 2016-07-27 | The United States of America, as Represented by The Secretary, Department of Health and Human Services | A3 adenosine receptor antagonists and partial agonists |
| 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 |
| WO2010043721A1 (en) | 2008-10-17 | 2010-04-22 | Oryzon Genomics, S.A. | Oxidase inhibitors and their use |
| US8993808B2 (en) | 2009-01-21 | 2015-03-31 | Oryzon Genomics, S.A. | Phenylcyclopropylamine derivatives and their medical use |
| US8859555B2 (en) | 2009-09-25 | 2014-10-14 | Oryzon Genomics S.A. | Lysine Specific Demethylase-1 inhibitors and their use |
| EP2486002B1 (en) | 2009-10-09 | 2019-03-27 | Oryzon Genomics, S.A. | Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use |
| WO2011106574A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Inhibitors for antiviral use |
| WO2011106106A2 (en) | 2010-02-24 | 2011-09-01 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae |
| WO2011123518A1 (en) | 2010-03-31 | 2011-10-06 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Adenosine receptor agonists for the treatment and prevention of vascular or joint capsule calcification disorders |
| CA2796726C (en) | 2010-04-19 | 2021-02-16 | Oryzon Genomics S.A. | Lysine specific demethylase-1 inhibitors and their use |
| US9006449B2 (en) | 2010-07-29 | 2015-04-14 | Oryzon Genomics, S.A. | Cyclopropylamine derivatives useful as LSD1 inhibitors |
| BR112013002164B1 (pt) | 2010-07-29 | 2021-11-09 | Oryzon Genomics S.A. | Inibidores de desmetilase à base de arilciclopropilamina de lsd1, seus usos, e composição farmacêutica |
| 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 |
| EP2712315B1 (en) | 2011-02-08 | 2021-11-24 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
| US20140329833A1 (en) * | 2011-05-19 | 2014-11-06 | Oryzon Genomics, S.A | Lysine demethylase inhibitors for inflammatory diseases or conditions |
| US20140296255A1 (en) * | 2011-05-19 | 2014-10-02 | Oryzong Genomics, S.A. | Lysine demethylase inhibitors for thrombosis and cardiovascular diseases |
| EP2768805B1 (en) | 2011-10-20 | 2020-03-25 | Oryzon Genomics, S.A. | (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors |
| JP6046154B2 (ja) | 2011-10-20 | 2016-12-14 | オリソン ヘノミクス エセ． アー． | Ｌｓｄ１阻害剤としての（ヘテロ）アリールシクロプロピルアミン化合物 |
| 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 |
| US9963450B2 (en) | 2013-11-27 | 2018-05-08 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | A3 adenosine receptor agonists |
| ES2578363B1 (es) | 2015-01-22 | 2017-01-31 | Palobiofarma, S.L. | Moduladores de los receptores A3 de adenosina |
| EP3445368B1 (en) | 2016-04-21 | 2024-07-17 | Astrocyte Pharmaceuticals, Inc. | Compounds and methods for treating neurological and cardiovascular conditions |
| ES2676535B1 (es) | 2017-01-20 | 2019-04-29 | Palobiofarma Sl | Moduladores de los receptores a3 de adenosina |
| CN112218638A (zh) | 2018-02-09 | 2021-01-12 | 阿斯特罗赛特制药公司 | 用于治疗成瘾和相关病症的化合物和方法 |
| EP3856741A4 (en) | 2018-09-26 | 2022-06-22 | Astrocyte Pharmaceuticals, Inc. | POLYMORPHOUS COMPOUNDS AND USES THEREOF |
| US12397010B2 (en) | 2019-02-15 | 2025-08-26 | Saint Louis University | Treatment of chronic headaches |
Family Cites Families (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO1995002604A1 (en) | 1993-07-13 | 1995-01-26 | The United States Of America, Represented By The Secretary, 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 |
| CA2244774C (en) | 1996-01-29 | 2006-10-17 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Dihydropyridine derivatives, their preparation and their use as adenosine receptor antagonists |
| 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 |
| KR20010020443A (ko) | 1997-04-30 | 2001-03-15 | 캐서린 구 | 생체내 세포 치사를 이미지화시키는 방법 |
| US6211165B1 (en) | 1997-05-09 | 2001-04-03 | The Trustees Of The University Of Pennsylvania | Methods and compositions for reducing ischemic injury of the heart by administering adenosine receptor agonists and antagonists |
| US6187284B1 (en) | 1997-09-03 | 2001-02-13 | Immunomedics, Inc. | Fluorination of proteins and peptides for F-18 positron emission tomography |
| ATE290910T1 (de) | 1998-07-16 | 2005-04-15 | 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 |
| US7087589B2 (en) | 2000-01-14 | 2006-08-08 | The United States Of America As Represented By The Department Of Health And Human Services | Methanocarba cycloakyl 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 |
| JP2008512457A (ja) * | 2004-09-09 | 2008-04-24 | アメリカ合衆国 | Ａ３及びａ１アデノシン受容体作用薬としてのプリン誘導体 |
| 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 |
| JP5042996B2 (ja) | 2005-05-19 | 2012-10-03 | ギリアード・パロ・アルト・インコーポレイテッド | Ａ１アデノシンレセプターアゴニスト |
| US20090221523A1 (en) | 2005-05-25 | 2009-09-03 | Tseng Christopher K | North-2'-deoxy-methanocarbathymidines as antiviral agents against poxviruses |
| US20090220516A1 (en) | 2005-06-22 | 2009-09-03 | Alan Laties | 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 |
| EP1959939B1 (en) | 2005-11-30 | 2012-01-11 | Can-Fite Biopharma Ltd. | Use of a3 adenosine receptor agonist in osteoarthritis treatment |
| EP1798233A1 (en) | 2005-12-19 | 2007-06-20 | Faust Pharmaceuticals | Pyrrolo[1,2-a]quinoxaline derivatives as Adenosine A3 receptor modulators and uses thereof |
| BRPI0621052A2 (pt) | 2006-01-27 | 2012-07-17 | Can Fite Biopharma Ltd | uso de um agonista de receptor de adenosina a3 (a3ar) |
| US20070219223A1 (en) | 2006-03-07 | 2007-09-20 | Endacea, Inc. | Compositions and methods for treating respiratory disorders |
| GB0607944D0 (en) | 2006-04-21 | 2006-05-31 | Novartis Ag | Organic compounds |
| EP2049127B1 (en) * | 2006-05-23 | 2014-11-26 | University of Connecticut | N-methanocarba derivatives to treat cardiac diseases |
| US20090029949A1 (en) | 2006-05-25 | 2009-01-29 | Parrill-Baker Abby L | GPCR Ligands Identified by Computational Modeling |
| EP2054415A1 (en) | 2006-07-14 | 2009-05-06 | 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 |
| WO2008056361A1 (en) | 2006-11-09 | 2008-05-15 | Can-Fite Biopharma Ltd. | A biological marker for psoriasis |
| RU2009121815A (ru) | 2006-11-09 | 2010-12-20 | Сантр Де Решерш Пюблик Де Ля Сантэ (Lu) | Применение антагониста аденозина |
| GB0625100D0 (en) | 2006-12-15 | 2007-01-24 | Univ Murcia | Epigallocatechin-3-gallate compositions for cancer therapy and chemoprotection |
| AU2009231978C1 (en) * | 2008-03-31 | 2014-01-30 | The United States Of America, As Represented By The Secretary, 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 |
| EP2331542B1 (en) | 2008-08-01 | 2016-07-27 | The United States of America, as Represented by The Secretary, Department of Health and Human Services | A3 adenosine receptor antagonists and partial agonists |
| 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 |
| US8518957B2 (en) * | 2009-12-02 | 2013-08-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methanocarba adenosine derivatives, pharmaceutical compositions, and method of reducing intraocular pressure |
| US9132131B2 (en) * | 2011-04-21 | 2015-09-15 | Saint Louis University | Use of adenosine A3 receptor agonists for treatment of neuropathic pain |
-
2009
- 2009-07-31 EP EP09791060.8A patent/EP2331542B1/en not_active Not-in-force
- 2009-07-31 CA CA2732320A patent/CA2732320C/en not_active Expired - Fee Related
- 2009-07-31 WO PCT/US2009/052439 patent/WO2010014921A2/en not_active Ceased
- 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 JP JP2011521360A patent/JP5431476B2/ja not_active Expired - Fee Related
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