CO5021135A1 - Compuestos quimicos - Google Patents
Compuestos quimicosInfo
- Publication number
- CO5021135A1 CO5021135A1 CO98065179A CO98065179A CO5021135A1 CO 5021135 A1 CO5021135 A1 CO 5021135A1 CO 98065179 A CO98065179 A CO 98065179A CO 98065179 A CO98065179 A CO 98065179A CO 5021135 A1 CO5021135 A1 CO 5021135A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- alq
- group
- optionally substituted
- ring
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H1/00—Processes for the preparation of sugar derivatives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Genetics & Genomics (AREA)
- Pharmacology & Pharmacy (AREA)
- Biochemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un compuesto de la fórmula (I) el cual es un agonista en elreceptor de la adenosina A1en donde R2 representa alquilo con 1 a 3 átomos de carbono, halógeno o hidrógeno;R3 representa un grupo alquilo recto o ramificado, fluorado, de 1-6 átomos de carbono;R1 representa un grupo seleccionado de(1) -(alq)n -(C3-7 ) cicloalquilo, que incluyen el cicloalquilo con puentes, el grupo cicloalquilo que está substituido opcionalmente por uno o más de los substituyentes seleccionados de OH, halógeno, -(C1-3 ) alcoxi, en donde (alq) representa alquileno con C1-3 y n representa 0 ó 1.(2) un grupo heterocíclico alifático de anillos de 4 a 6 elementos que contienen al menos un heteroátomo seleccionado de O, N, o S, substituido opcionalmente por uno o más substituyentes seleccionados del grupo que consiste de -(C1-3 )alquilo, -CO2 - (C1-4 )alquilo, -CO(C1-3 alquilo), -S(=O)n - (C1-3 alquilo), -CONRa Rb (en donde Ra y Rb representan independientemente H o C1-3 alquilo) o =O; en donde existe un átomo de azufre en el anillo heterocíclico, y el azufre está substituido opcionalmente por (=O)n , en donde n es 1 o 2.(3) alquilo con C1-12 recto o ramificado que incluye opcionalmente uno o más O,S(=O)n (en donde n es 0, 1 ó 2) o grupos N substituidos dentro de la cadena de alquilo, el alquilo substituido opcionalmente por uno o más de los siguientes grupos, fenilo, halógeno, hidroxi o NRa Rb en donde Ra y Rb ambos representan C1-3 alquilo o hidrógeno.(4) un anillo aromático bicíclico fusionado - 2 -en donde B representa un grupo aromático heterocíclico de 5 o 6 elementos que contiene 1 o más átomos de O, N o S, en donde el anillo bicíclico está unido al átomo de nitrógeno de la fórmula (I) por medio de un átomo del anillo, del anillo A, y el anillo B está substituido opcionalmente por -CO2 -(C1-3 alquilo).(5) un grupo fenilo substituido opcionalmente por uno o más substituyentes seleccionados de:-halógeno -SO3 H, (alq)n OH, -(alq)n ciano, -(O)n -(C1-6 )alquilo (substituido opcionalmente por uno o más halógenos), -(alq)n - nitro, -(O)m -(alq)n -CO2 Rc , -(alq)n -CONRc Rd -(alq)n -CORc , -(alq)n -SORe , -(alq)n SO2 Re , -(alq)n SO2 NRc Rd , -(alq)n ORc , -(alq)n -(CO)m -NHSO2 Re , -(alq)n -NHCORc , -(alq)n -NRc Rd en donde m y n son 0 ó 1 y alq representa un grupo C1-6 alquileno o un grupo C2-6 alquenilo.(6) un grupo fenilo substituido por un grupo aromático haterocíclico de 5 o 6 elementos, el grupo aromático heterocíclico está substituido opcionalmente por C1-3 alquilo o NRc Rd Rc y Rd pueden representar cada uno independientemente hidrógeno, o C1-3 alquilo y cuando forma parte de un grupo NRc Rd , Rc y Rd junto con el átomo de nitrógeno pueden formar un anillo heterocíclico de 5 o 6 elementos que contiene opcionalmente otros heteroátomos, tal anillo heterocíclico puede estar substituido opcionalmente de manera adicional por uno o más grupos C1-3 alquilo.Re representa C1-3 alquiloy la sales y los solvatos de los mimos, en particular, las sales y solvatos de los mismos aceptables fisiologicamente.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9723589.9A GB9723589D0 (en) | 1997-11-08 | 1997-11-08 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5021135A1 true CO5021135A1 (es) | 2001-03-27 |
Family
ID=10821760
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO98065179A CO5021135A1 (es) | 1997-11-08 | 1998-11-05 | Compuestos quimicos |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US6455510B1 (es) |
| EP (2) | EP1457495A1 (es) |
| JP (1) | JP2001522857A (es) |
| KR (1) | KR20010031875A (es) |
| CN (1) | CN1285843A (es) |
| AP (1) | AP2000001801A0 (es) |
| AR (1) | AR011229A1 (es) |
| AT (1) | ATE273990T1 (es) |
| AU (1) | AU2048399A (es) |
| BR (1) | BR9813976A (es) |
| CA (1) | CA2309200A1 (es) |
| CO (1) | CO5021135A1 (es) |
| DE (1) | DE69825780T2 (es) |
| EA (1) | EA200000392A1 (es) |
| EE (1) | EE200000285A (es) |
| ES (1) | ES2222621T3 (es) |
| GB (1) | GB9723589D0 (es) |
| HR (1) | HRP20000275A2 (es) |
| HU (1) | HUP0004082A2 (es) |
| IL (1) | IL135964A0 (es) |
| IS (1) | IS5477A (es) |
| MA (1) | MA26565A1 (es) |
| NO (1) | NO20002361L (es) |
| PE (1) | PE20000013A1 (es) |
| PL (1) | PL340921A1 (es) |
| SK (1) | SK6722000A3 (es) |
| TR (1) | TR200002131T2 (es) |
| WO (1) | WO1999024449A2 (es) |
| ZA (1) | ZA9810125B (es) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9723589D0 (en) * | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
| GB0106867D0 (en) | 2001-03-20 | 2001-05-09 | Glaxo Group Ltd | Process |
| US20040162422A1 (en) * | 2001-03-20 | 2004-08-19 | Adrian Hall | Chemical compounds |
| US7157440B2 (en) | 2001-07-13 | 2007-01-02 | Cv Therapeutics, Inc. | Partial and full agonists of A1 adenosine receptors |
| US6946449B2 (en) | 2001-07-13 | 2005-09-20 | Cv Therapeutics, Inc. | Partial and full agonists of A1 adenosine receptors |
| US7713946B2 (en) | 2002-07-11 | 2010-05-11 | Cv Therapeutics, Inc. | Partial and full agonists A1 adenosine receptors |
| AU2002362443B2 (en) | 2001-10-01 | 2008-05-15 | University Of Virginia Patent Foundation | 2-propynyl adenosine analogs having A2A agonist activity and compositions thereof |
| EP1375508A1 (en) * | 2002-06-27 | 2004-01-02 | Aventis Pharma Deutschland GmbH | N6-substituted adenosine analogues and their use as pharmaceutical agents |
| US7265111B2 (en) | 2002-06-27 | 2007-09-04 | Sanofi-Aventis Deutschland Gmbh | Adenosine analogues and their use as pharmaceutical agents |
| FR2842810B1 (fr) * | 2002-07-25 | 2006-01-27 | Inst Nat Sciences Appliq | Nouveaux composes gem difluores, leur procedes de preparation et leurs applications. |
| DE60315164T2 (de) * | 2002-08-15 | 2008-04-30 | CV Therapeutics, Inc., Palo Alto | Partielle und volle agonisten von a1-adenosinrezeptoren |
| US7163928B2 (en) | 2003-02-03 | 2007-01-16 | Cv Therapeutics, Inc. | Partial and full agonists of A1 adenosine receptors |
| 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 |
| EP1794162A1 (en) * | 2004-09-09 | 2007-06-13 | The Government of the United States of America, as repres. by the Secretary of Health and Human Services, Nat. Inst. of Health | Purine derivatives as a3 and a1 adenosine receptor agonists |
| 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 |
| EP2532677A1 (en) | 2005-10-21 | 2012-12-12 | Novartis AG | Human antibodies against il13 and therapeutic uses |
| GB0601951D0 (en) | 2006-01-31 | 2006-03-15 | Novartis Ag | Organic compounds |
| WO2007120972A2 (en) * | 2006-02-10 | 2007-10-25 | University Of Virginia Patent Foundation | Method to treat sickle cell disease |
| US8188063B2 (en) * | 2006-06-19 | 2012-05-29 | University Of Virginia Patent Foundation | Use of adenosine A2A modulators to treat spinal cord injury |
| BRPI0717564A2 (pt) | 2006-09-29 | 2013-10-22 | Novartis Ag | Pirazolopirimidinas como inibidores de pi3k lipídeo cinase |
| CA2667962A1 (en) | 2006-10-30 | 2008-05-08 | Novartis Ag | Heterocyclic compounds as antiinflammatory agents |
| US8058259B2 (en) * | 2007-12-20 | 2011-11-15 | University Of Virginia Patent Foundation | Substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists |
| EP2240020A4 (en) * | 2008-01-09 | 2011-05-11 | Trovis Pharmaceuticals Llc | INTRATHEAL TREATMENT OF NEUROPATHIC PAIN WITH A2AR AGONISTS |
| KR20100113557A (ko) | 2008-01-11 | 2010-10-21 | 노파르티스 아게 | 키나제 억제제로서의 피리미딘 |
| ES2396023T3 (es) | 2009-01-29 | 2013-02-18 | Novartis Ag | Bencimidazoles sustituidos para el tratamiento de astrocitomas |
| US8389526B2 (en) | 2009-08-07 | 2013-03-05 | Novartis Ag | 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives |
| JP5781510B2 (ja) | 2009-08-12 | 2015-09-24 | ノバルティス アーゲー | ヘテロ環式ヒドラゾン化合物および癌および炎症の処置のためのそれらの使用 |
| JP5819831B2 (ja) | 2009-08-17 | 2015-11-24 | インテリカイン， エルエルシー | 複素環式化合物およびそれらの使用 |
| WO2011020861A1 (en) | 2009-08-20 | 2011-02-24 | Novartis Ag | Heterocyclic oxime compounds |
| WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
| US8637516B2 (en) | 2010-09-09 | 2014-01-28 | Irm Llc | Compounds and compositions as TRK inhibitors |
| 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 |
| WO2012116237A2 (en) | 2011-02-23 | 2012-08-30 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| US9102671B2 (en) | 2011-02-25 | 2015-08-11 | Novartis Ag | Compounds and compositions as TRK inhibitors |
| DE102011005232A1 (de) | 2011-03-08 | 2012-09-13 | AristoCon GmbH & Co. KG | Adenosin und seine Derivate zur Verwendung in der Schmerztherapie |
| JP5957526B2 (ja) | 2011-09-15 | 2016-07-27 | ノバルティス アーゲー | チロシンキナーゼとしての６−置換３−（キノリン−６−イルチオ）−［１，２，４］トリアゾロ［４，３−ａ］ピラジン |
| EP2793893A4 (en) | 2011-11-23 | 2015-07-08 | Intellikine Llc | IMPROVED TREATMENT REGIMES USING MTOR INHIBITORS |
| EP3964513A1 (en) | 2012-04-03 | 2022-03-09 | Novartis AG | Combination products with tyrosine kinase inhibitors and their use |
| CN105246482A (zh) | 2013-03-15 | 2016-01-13 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| TW201605450A (zh) | 2013-12-03 | 2016-02-16 | 諾華公司 | Ｍｄｍ２抑制劑與ＢＲＡＦ抑制劑之組合及其用途 |
| WO2016011658A1 (en) | 2014-07-25 | 2016-01-28 | Novartis Ag | Combination therapy |
| US10195208B2 (en) | 2014-07-31 | 2019-02-05 | Novartis Ag | Combination therapy |
| 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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3575959A (en) * | 1969-05-13 | 1971-04-20 | Merck & Co Inc | 5'-substituted ribofuranosyl nucleosides |
| US5589467A (en) | 1993-09-17 | 1996-12-31 | Novo Nordisk A/S | 2,5',N6-trisubstituted adenosine derivatives |
| AU2022597A (en) * | 1996-03-13 | 1997-10-01 | Novo Nordisk A/S | A method of treating disorders related to cytokines in mammals |
| GB9610031D0 (en) * | 1996-05-14 | 1996-07-17 | Glaxo Group Ltd | Chemical compounds |
| GB9723589D0 (en) * | 1997-11-08 | 1998-01-07 | Glaxo Group Ltd | Chemical compounds |
-
1997
- 1997-11-08 GB GBGB9723589.9A patent/GB9723589D0/en not_active Ceased
-
1998
- 1998-11-05 AR ARP980105590A patent/AR011229A1/es unknown
- 1998-11-05 PE PE1998001065A patent/PE20000013A1/es not_active Application Discontinuation
- 1998-11-05 MA MA25336A patent/MA26565A1/fr unknown
- 1998-11-05 CO CO98065179A patent/CO5021135A1/es unknown
- 1998-11-05 ZA ZA9810125A patent/ZA9810125B/xx unknown
- 1998-11-06 PL PL98340921A patent/PL340921A1/xx unknown
- 1998-11-06 TR TR2000/02131T patent/TR200002131T2/xx unknown
- 1998-11-06 CA CA002309200A patent/CA2309200A1/en not_active Abandoned
- 1998-11-06 EP EP04076482A patent/EP1457495A1/en not_active Withdrawn
- 1998-11-06 WO PCT/EP1998/007021 patent/WO1999024449A2/en active IP Right Grant
- 1998-11-06 AP APAP/P/2000/001801A patent/AP2000001801A0/en unknown
- 1998-11-06 HU HU0004082A patent/HUP0004082A2/hu unknown
- 1998-11-06 ES ES98965151T patent/ES2222621T3/es not_active Expired - Lifetime
- 1998-11-06 SK SK672-2000A patent/SK6722000A3/sk unknown
- 1998-11-06 DE DE1998625780 patent/DE69825780T2/de not_active Expired - Fee Related
- 1998-11-06 BR BR9813976-2A patent/BR9813976A/pt not_active Application Discontinuation
- 1998-11-06 JP JP2000520457A patent/JP2001522857A/ja active Pending
- 1998-11-06 IL IL13596498A patent/IL135964A0/xx unknown
- 1998-11-06 AT AT98965151T patent/ATE273990T1/de not_active IP Right Cessation
- 1998-11-06 CN CN98812979A patent/CN1285843A/zh active Pending
- 1998-11-06 AU AU20483/99A patent/AU2048399A/en not_active Abandoned
- 1998-11-06 KR KR1020007004959A patent/KR20010031875A/ko not_active Application Discontinuation
- 1998-11-06 US US09/530,573 patent/US6455510B1/en not_active Expired - Fee Related
- 1998-11-06 EA EA200000392A patent/EA200000392A1/ru unknown
- 1998-11-06 EE EEP200000285A patent/EE200000285A/xx unknown
- 1998-11-06 EP EP98965151A patent/EP1030857B1/en not_active Expired - Lifetime
-
2000
- 2000-05-03 IS IS5477A patent/IS5477A/is unknown
- 2000-05-05 NO NO20002361A patent/NO20002361L/no not_active Application Discontinuation
- 2000-05-08 HR HR20000275A patent/HRP20000275A2/hr not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AP2000001801A0 (en) | 2000-06-30 |
| NO20002361D0 (no) | 2000-05-05 |
| HUP0004082A2 (hu) | 2001-04-28 |
| WO1999024449A3 (en) | 1999-08-19 |
| PL340921A1 (en) | 2001-03-12 |
| CA2309200A1 (en) | 1999-05-20 |
| TR200002131T2 (tr) | 2001-01-22 |
| EE200000285A (et) | 2001-08-15 |
| ES2222621T3 (es) | 2005-02-01 |
| NO20002361L (no) | 2000-07-05 |
| AR011229A1 (es) | 2000-08-02 |
| ZA9810125B (en) | 2000-05-05 |
| IS5477A (is) | 2000-05-03 |
| HRP20000275A2 (en) | 2000-12-31 |
| SK6722000A3 (en) | 2001-01-18 |
| AU2048399A (en) | 1999-05-31 |
| KR20010031875A (ko) | 2001-04-16 |
| BR9813976A (pt) | 2000-09-26 |
| IL135964A0 (en) | 2001-05-20 |
| EP1030857B1 (en) | 2004-08-18 |
| ATE273990T1 (de) | 2004-09-15 |
| DE69825780D1 (de) | 2004-09-23 |
| CN1285843A (zh) | 2001-02-28 |
| WO1999024449A2 (en) | 1999-05-20 |
| US6455510B1 (en) | 2002-09-24 |
| EP1457495A1 (en) | 2004-09-15 |
| EA200000392A1 (ru) | 2000-12-25 |
| PE20000013A1 (es) | 2000-01-21 |
| JP2001522857A (ja) | 2001-11-20 |
| MA26565A1 (fr) | 2004-12-20 |
| DE69825780T2 (de) | 2005-01-13 |
| EP1030857A2 (en) | 2000-08-30 |
| GB9723589D0 (en) | 1998-01-07 |
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