WO1996002553B1 - DERIVES AMINO PURINE-β-D-RIBOFURANURONAMIDE - Google Patents
DERIVES AMINO PURINE-β-D-RIBOFURANURONAMIDEInfo
- Publication number
- WO1996002553B1 WO1996002553B1 PCT/EP1995/002837 EP9502837W WO9602553B1 WO 1996002553 B1 WO1996002553 B1 WO 1996002553B1 EP 9502837 W EP9502837 W EP 9502837W WO 9602553 B1 WO9602553 B1 WO 9602553B1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- alkylamino
- alk
- alkyl
- group
- guanidino
- Prior art date
Links
- MLSLQUCVGRPRBC-RDPLPRSHSA-N NC1=NC=C2NC=NC2=N1.NC(=O)[C@H]1O[C@@H](O)[C@H](O)[C@@H]1O Chemical class NC1=NC=C2NC=NC2=N1.NC(=O)[C@H]1O[C@@H](O)[C@H](O)[C@@H]1O MLSLQUCVGRPRBC-RDPLPRSHSA-N 0.000 title abstract 2
- -1 2-oxopyrrolidin-4-yl Chemical group 0.000 claims abstract 6
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 5
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 4
- 150000001875 compounds Chemical class 0.000 claims abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 4
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims abstract 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 2
- 239000001257 hydrogen Substances 0.000 claims abstract 2
- 239000001301 oxygen Substances 0.000 claims abstract 2
- 125000004755 (C2-C7) acylamino group Chemical group 0.000 claims 4
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 3
- MDFFNEOEWAXZRQ-UHFFFAOYSA-N aminyl Chemical compound [NH2] MDFFNEOEWAXZRQ-UHFFFAOYSA-N 0.000 claims 3
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 125000006260 ethylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 125000001183 hydrocarbyl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 101100490437 Mus musculus Acvrl1 gene Proteins 0.000 abstract 1
- 239000005864 Sulphur Chemical group 0.000 abstract 1
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 229940121363 anti-inflammatory agent Drugs 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 210000000265 leukocyte Anatomy 0.000 abstract 1
- 125000004483 piperidin-3-yl group Chemical group N1CC(CCC1)* 0.000 abstract 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- 229930195734 saturated hydrocarbon Natural products 0.000 abstract 1
- 230000000451 tissue damage Effects 0.000 abstract 1
- 231100000827 tissue damage Toxicity 0.000 abstract 1
- 229930195735 unsaturated hydrocarbon Chemical group 0.000 abstract 1
Abstract
L'invention concerne des dérivés amino purine-β-D-ribofuranuronamide de formule générale (I) ainsi que leurs sels et solvates. Dans cette formule, R1 est hydrogène, cycloalkyleC¿3-8? ou alkyleC1-6; A représente O, S, SO, SO2, un fragment hydrocarbure saturé possédant de 1 à 4 atomes de carbone ou bien un fragment hydrocarbure insaturé possédant de 2 à 4 atomes de carbone; R?2¿ est cycloalkyleC¿3-8?, cycloalkyleC3-8 alkyleC1-6, Alk1Y, -(CHR?5)¿m (Alk2)nZ ou bien cycloalkyleC3-8, cycloalkyleC3-8 alkyleC1-16 à substitution appropriée, pyrrolidin-3-yl, 2-oxopyrrolidin-4-yl, 2-oxopyrrolidin-5-yl, piperidin-3-yl ou piperidin-4-yl, et Q est oxygène ou soufre à condition que lorsque A représente O, S, SO ou bien SO2, Alk1 représente un groupe alkylèneC2-6. Ces composés de formule (I) ainsi que leurs sels et solvates s'utilisent en médecine comme agents anti-inflammatoires, notamment dans le traitement de patients atteints de manifestations inflammatoires, qui sont sujets à des lésions tissulaires à induction leucocytaire.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU36982/95A AU3698295A (en) | 1994-07-14 | 1995-07-14 | Amino purine-beta -d-ribofuranuronamide derivatives |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB9414193A GB9414193D0 (en) | 1994-07-14 | 1994-07-14 | Compounds |
| GB9414193.4 | 1994-07-14 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| WO1996002553A2 WO1996002553A2 (fr) | 1996-02-01 |
| WO1996002553A3 WO1996002553A3 (fr) | 1996-03-07 |
| WO1996002553B1 true WO1996002553B1 (fr) | 1996-03-28 |
Family
ID=10758311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/EP1995/002837 WO1996002553A2 (fr) | 1994-07-14 | 1995-07-14 | DERIVES AMINO PURINE-β-D-RIBOFURANURONAMIDE |
Country Status (5)
| Country | Link |
|---|---|
| AU (1) | AU3698295A (fr) |
| GB (1) | GB9414193D0 (fr) |
| IL (1) | IL114578A0 (fr) |
| WO (1) | WO1996002553A2 (fr) |
| ZA (1) | ZA955784B (fr) |
Families Citing this family (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW528755B (en) * | 1996-12-24 | 2003-04-21 | Glaxo Group Ltd | 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives |
| YU44900A (sh) | 1998-01-31 | 2003-01-31 | Glaxo Group Limited | Derivati 2-(purin-9-il)tetrahidrofuran-3,4-diola |
| PE20000270A1 (es) | 1998-02-14 | 2000-05-20 | Glaxo Group Ltd | Derivados de 2-(purin-9-il)-tetrahidrofuran-3,4-diol |
| GB9813540D0 (en) * | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| GB9813535D0 (en) | 1998-06-23 | 1998-08-19 | Glaxo Group Ltd | Chemical compounds |
| HRP20000894A2 (en) | 1998-06-23 | 2001-12-31 | Glaxo Group Ltd | 2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives |
| CA2336967C (fr) | 1998-07-10 | 2010-06-29 | The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Antagonistes du recepteur de l'adenosine a3 |
| US6232297B1 (en) | 1999-02-01 | 2001-05-15 | University Of Virginia Patent Foundation | Methods and compositions for treating inflammatory response |
| US7378400B2 (en) | 1999-02-01 | 2008-05-27 | University Of Virginia Patent Foundation | Method to reduce an inflammatory response from arthritis |
| US7427606B2 (en) * | 1999-02-01 | 2008-09-23 | University Of Virginia Patent Foundation | Method to reduce inflammatory response in transplanted tissue |
| GB9924361D0 (en) | 1999-10-14 | 1999-12-15 | Pfizer Ltd | Purine derivatives |
| AU2001230913B2 (en) | 2000-01-14 | 2005-06-30 | The Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Methanocarba cycloalkyl nucleoside analogues |
| US20010051612A1 (en) * | 2000-02-23 | 2001-12-13 | Gloria Cristalli | 2-Thioether A2A receptor agonists |
| US6921753B2 (en) | 2000-06-27 | 2005-07-26 | Pfizer Inc | Purine derivatives |
| JP4514452B2 (ja) * | 2001-10-01 | 2010-07-28 | ユニバーシティ オブ バージニア パテント ファウンデーション | Ａ２ａアゴニスト活性を有する２−プロピルアデノシン・アナログおよびその組成物 |
| AR044519A1 (es) | 2003-05-02 | 2005-09-14 | Novartis Ag | Derivados de piridin-tiazol amina y de pirimidin-tiazol amina |
| GB0401334D0 (en) | 2004-01-21 | 2004-02-25 | Novartis Ag | Organic compounds |
| GB0411056D0 (en) | 2004-05-18 | 2004-06-23 | Novartis Ag | Organic compounds |
| AR049384A1 (es) | 2004-05-24 | 2006-07-26 | Glaxo Group Ltd | Derivados de purina |
| MXPA06013560A (es) | 2004-05-26 | 2007-03-15 | Inotek Pharmaceuticals Corp | Derivados de purina como agonistas del receptor de adenosina a1 y metodos de uso de los mismos. |
| WO2006023272A1 (fr) | 2004-08-02 | 2006-03-02 | University Of Virginia Patent Foundation | Analogues de 2-polycyclique propynyle adenosine presentant une activite agoniste de a2a |
| WO2006015357A2 (fr) | 2004-08-02 | 2006-02-09 | University Of Virginia Patent Foundation | Analogues de 2-propynyle adenosine comprenant des groupes 5'-ribose modifies presentant une activite agoniste a2a |
| US7576069B2 (en) | 2004-08-02 | 2009-08-18 | University Of Virginia Patent Foundation | 2-polycyclic propynyl adenosine analogs having A2A agonist activity |
| NZ554506A (en) | 2004-09-20 | 2011-01-28 | Inotek Pharmaceuticals Corp | Purine derivatives and methods of use thereof |
| GB0424284D0 (en) | 2004-11-02 | 2004-12-01 | Novartis Ag | Organic compounds |
| GB0426164D0 (en) | 2004-11-29 | 2004-12-29 | Novartis Ag | Organic compounds |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| GB0514809D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| KR20080049113A (ko) | 2005-10-21 | 2008-06-03 | 노파르티스 아게 | Ｉｌ-13에 대항한 인간 항체 및 치료적 용도 |
| WO2007064795A2 (fr) | 2005-11-30 | 2007-06-07 | Inotek Pharmaceuticals Corporation | Derives de purine et leurs procedes d'utilisation |
| GB0601951D0 (en) | 2006-01-31 | 2006-03-15 | Novartis Ag | Organic compounds |
| MX2008013431A (es) | 2006-04-21 | 2008-11-04 | Novartis Ag | Derivados de purina para utilizarse como agonistas del receptor de adenosina a2a. |
| JP2010504933A (ja) | 2006-09-29 | 2010-02-18 | ノバルティス アーゲー | Ｐｉ３ｋ脂質キナーゼ阻害剤としてのピラゾロピリミジン |
| WO2008052734A1 (fr) | 2006-10-30 | 2008-05-08 | Novartis Ag | Composés hétérocycliques en tant qu'agents anti-inflammatoires |
| WO2009006089A2 (fr) * | 2007-06-29 | 2009-01-08 | Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services | Agonistes des récepteurs d'adénosine a2 |
| CA2711637A1 (fr) | 2008-01-11 | 2009-07-16 | Novartis Ag | Pyrimidines utilises en tant qu'inhibiteurs de kinase |
| PT2391366E (pt) | 2009-01-29 | 2013-02-05 | Novartis Ag | Benzimidazoles substituídos para o tratamento de astrocitomas |
| US8389526B2 (en) | 2009-08-07 | 2013-03-05 | Novartis Ag | 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives |
| MX2012001838A (es) | 2009-08-12 | 2012-02-29 | Novartis Ag | Compuestos de hidrazona heterociclico y sus usos para tratar cancer e inflamacion. |
| SG10201404886PA (en) | 2009-08-17 | 2014-10-30 | Intellikine Llc | Heterocyclic compounds and uses thereof |
| JP5775871B2 (ja) | 2009-08-20 | 2015-09-09 | ノバルティス アーゲー | ヘテロ環式オキシム化合物 |
| WO2011068978A1 (fr) | 2009-12-02 | 2011-06-09 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Dérivés de méthanocarba-adénosine et conjugués de dendrimère de ceux-ci |
| SG10201502588UA (en) | 2010-01-11 | 2015-05-28 | Inotek Pharmaceuticals Corp | Combination, kit and method of reducing intraocular pressure |
| KR20130029050A (ko) | 2010-03-26 | 2013-03-21 | 이노텍 파마슈티컬스 코포레이션 | Ｎ6-시클로펜틸아데노신(ｃｐａ), ｃｐａ 유도체 또는 이의 전구 약물을 사용하여 사람의 안압을 감소시키는 방법 |
| US8637516B2 (en) | 2010-09-09 | 2014-01-28 | Irm Llc | Compounds and compositions as TRK inhibitors |
| WO2012034095A1 (fr) | 2010-09-09 | 2012-03-15 | Irm Llc | Composés et compositions comme inhibiteurs de trk |
| JP2014505088A (ja) | 2011-02-10 | 2014-02-27 | ノバルティス アーゲー | Ｃ−ＭＥＴチロシンキナーゼ阻害剤としての［１，２，４］トリアゾロ［４，３−ｂ］ピリダジン化合物 |
| US9127000B2 (en) | 2011-02-23 | 2015-09-08 | Intellikine, LLC. | Heterocyclic compounds and uses thereof |
| ES2551592T3 (es) | 2011-02-25 | 2015-11-20 | Novartis Ag | Pirazolo[1,5-a]piridinas como inhibidores de TRK |
| MX339302B (es) | 2011-09-15 | 2016-05-19 | Novartis Ag | 3-(quinolin-6-il-tio)-[1,2,4]-triazolo-[4,3-a]-piridinas 6-sustituidas como cinasas de tirosina. |
| CA2856803A1 (fr) | 2011-11-23 | 2013-05-30 | Intellikine, Llc | Regimes de traitement ameliores utilisant des inhibiteurs de mtor |
| HRP20171204T1 (hr) | 2012-01-26 | 2017-10-06 | Inotek Pharmaceuticals Corporation | Anhidridni polimorfi od [(2r,3s,4r,5r)-5-(6-(ciklopentilamino)-9h-purin- 9-il)-3,4-dihidroksitetrahidrofuran-2-il)]metil-nitrata i postupci njihove proizvodnje |
| EP3964513A1 (fr) | 2012-04-03 | 2022-03-09 | Novartis AG | Produits combinés comprenant des inhibiteurs de tyrosine kinase et leur utilisation |
| AU2014239222A1 (en) | 2013-03-15 | 2015-10-01 | Inotek Pharmaceuticals Corporation | Ophthalmic formulations |
| HK1219421A1 (zh) | 2013-03-15 | 2017-04-07 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| WO2015084804A1 (fr) | 2013-12-03 | 2015-06-11 | Novartis Ag | Combinaison d'un inhibiteur de mdm2 et d'un inhibiteur de braf, et leur utilisation |
| WO2016011658A1 (fr) | 2014-07-25 | 2016-01-28 | Novartis Ag | Polythérapie |
| JP6526789B2 (ja) | 2014-07-31 | 2019-06-05 | ノバルティス アーゲー | 組み合わせ療法 |
| CN109879787A (zh) * | 2019-01-10 | 2019-06-14 | 安徽昊帆生物有限公司 | 碘代硫代乙酰胆碱、其制备方法、及其应用 |
| TW202140550A (zh) | 2020-01-29 | 2021-11-01 | 瑞士商諾華公司 | 使用抗ｔｓｌｐ抗體治療炎性或阻塞性氣道疾病之方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4738954A (en) * | 1985-11-06 | 1988-04-19 | Warner-Lambert Company | Novel N6 -substituted-5'-oxidized adenosine analogs |
| WO1988003147A1 (fr) * | 1986-10-31 | 1988-05-05 | Warner-Lambert Company | Adenosines a substitution n6 selectionees ayant une activite de liaison a2 selective |
| FI880405A7 (fi) * | 1987-02-04 | 1988-08-05 | Ciba Geigy Ag | Adenosin-5'-karboxamidderivat. |
-
1994
- 1994-07-14 GB GB9414193A patent/GB9414193D0/en active Pending
-
1995
- 1995-07-12 ZA ZA955784A patent/ZA955784B/xx unknown
- 1995-07-13 IL IL11457895A patent/IL114578A0/xx unknown
- 1995-07-14 WO PCT/EP1995/002837 patent/WO1996002553A2/fr active Application Filing
- 1995-07-14 AU AU36982/95A patent/AU3698295A/en not_active Abandoned
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