CZ20024052A3 - Pyrido [2,3-d]pyrimidinové a pyrimido[4,5-d]pyrimidinové nukleosidy - Google Patents
Pyrido [2,3-d]pyrimidinové a pyrimido[4,5-d]pyrimidinové nukleosidy Download PDFInfo
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- CZ20024052A3 CZ20024052A3 CZ20024052A CZ20024052A CZ20024052A3 CZ 20024052 A3 CZ20024052 A3 CZ 20024052A3 CZ 20024052 A CZ20024052 A CZ 20024052A CZ 20024052 A CZ20024052 A CZ 20024052A CZ 20024052 A3 CZ20024052 A3 CZ 20024052A3
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- pyrimidine
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- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 title abstract description 30
- QGDYVSSVBYMOJN-UHFFFAOYSA-N pyrimido[4,5-d]pyrimidine Chemical compound C1=NC=NC2=NC=NC=C21 QGDYVSSVBYMOJN-UHFFFAOYSA-N 0.000 title abstract description 4
- 239000002718 pyrimidine nucleoside Substances 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 140
- 229940002612 prodrug Drugs 0.000 claims abstract description 16
- 239000000651 prodrug Substances 0.000 claims abstract description 16
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- 230000012010 growth Effects 0.000 claims abstract description 5
- 210000004027 cell Anatomy 0.000 claims description 60
- 238000000034 method Methods 0.000 claims description 28
- 239000002777 nucleoside Substances 0.000 claims description 27
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 claims description 10
- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- 229940127073 nucleoside analogue Drugs 0.000 claims description 10
- 229910052731 fluorine Inorganic materials 0.000 claims description 9
- 229910052760 oxygen Inorganic materials 0.000 claims description 9
- 230000026731 phosphorylation Effects 0.000 claims description 9
- 238000006366 phosphorylation reaction Methods 0.000 claims description 9
- 230000006907 apoptotic process Effects 0.000 claims description 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 6
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 6
- 125000000524 functional group Chemical group 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
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- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 4
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 2
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- 150000003834 purine nucleoside derivatives Chemical class 0.000 abstract 3
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- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 description 38
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- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 19
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- 235000011152 sodium sulphate Nutrition 0.000 description 17
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 16
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Classifications
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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- Medicinal Chemistry (AREA)
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- Engineering & Computer Science (AREA)
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- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| UA (1) | UA72612C2 (enExample) |
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| MY164523A (en) | 2000-05-23 | 2017-12-29 | Univ Degli Studi Cagliari | Methods and compositions for treating hepatitis c virus |
| CZ301182B6 (cs) | 2000-05-26 | 2009-12-02 | Idenix (Cayman) Limited | Použití nukleosidových derivátu pro výrobu farmaceutických prostredku pro lécení infekcí vyvolaných flaviviry a pestiviry |
| JP4942915B2 (ja) | 2002-04-26 | 2012-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖプロテアーゼ阻害剤化合物のホスホネートアナログの細胞蓄積 |
| MXPA04012802A (es) | 2002-06-28 | 2005-04-19 | Idenix Cayman Ltd | Ester 2'-c-metil-3'-o-l-valina de ribofuranosil-citidina para el tratamiento de infecciones por flaviviridae. |
| NZ537662A (en) | 2002-06-28 | 2007-10-26 | Idenix Cayman Ltd | 2'-C-methyl-3'-O-L-valine ester ribofuranosyl cytidine for treatment of flaviviridae infections |
| CA2494340C (en) | 2002-08-01 | 2012-01-24 | Pharmasset Inc. | Compounds with the bicyclo[4.2.1]nonane system for the treatment of flaviviridae infections |
| WO2004046331A2 (en) | 2002-11-15 | 2004-06-03 | Idenix (Cayman) Limited | 2’-branched nucleosides and flaviviridae mutation |
| US7598373B2 (en) | 2002-12-12 | 2009-10-06 | Idenix Pharmaceuticals, Inc. | Process for the production of 2-C-methyl-D-ribonolactone |
| US7300924B2 (en) | 2003-04-25 | 2007-11-27 | Gilead Sciences, Inc. | Anti-infective phosphonate analogs |
| MXPA05011296A (es) | 2003-04-25 | 2006-01-24 | Gilead Sciences Inc | Conjugados de fosfonato inhibidores de la cinasa. |
| US7470724B2 (en) | 2003-04-25 | 2008-12-30 | Gilead Sciences, Inc. | Phosphonate compounds having immuno-modulatory activity |
| US7432261B2 (en) | 2003-04-25 | 2008-10-07 | Gilead Sciences, Inc. | Anti-inflammatory phosphonate compounds |
| US7427636B2 (en) | 2003-04-25 | 2008-09-23 | Gilead Sciences, Inc. | Inosine monophosphate dehydrogenase inhibitory phosphonate compounds |
| EP1628685B1 (en) | 2003-04-25 | 2010-12-08 | Gilead Sciences, Inc. | Antiviral phosphonate analogs |
| US7452901B2 (en) | 2003-04-25 | 2008-11-18 | Gilead Sciences, Inc. | Anti-cancer phosphonate analogs |
| WO2005002626A2 (en) | 2003-04-25 | 2005-01-13 | Gilead Sciences, Inc. | Therapeutic phosphonate compounds |
| US7407965B2 (en) | 2003-04-25 | 2008-08-05 | Gilead Sciences, Inc. | Phosphonate analogs for treating metabolic diseases |
| WO2004113357A2 (en) * | 2003-05-20 | 2004-12-29 | The Board Of Trustees Of The University Of Illinois | Nucleoside analog inhibitors of reverse transcriptase |
| EP2345659A1 (en) | 2003-05-30 | 2011-07-20 | Pharmasset, Inc. | Modified fluorinated nucleoside analogues |
| DE602004028841D1 (de) | 2003-07-25 | 2010-10-07 | Centre Nat Rech Scient | Purin nucleoside für die behandlung von durch flavividrae verursachten krankheiten, einschliesslich hepatitis c |
| US7432273B2 (en) | 2003-10-24 | 2008-10-07 | Gilead Sciences, Inc. | Phosphonate analogs of antimetabolites |
| EP1678321A1 (en) | 2003-10-24 | 2006-07-12 | Gilead Sciences, Inc. | Methods and compositions for identifying therapeutic compounds |
| WO2005044279A1 (en) | 2003-10-24 | 2005-05-19 | Gilead Sciences, Inc. | Purine nucleoside phosphonate conjugates |
| JP2007515495A (ja) | 2003-12-22 | 2007-06-14 | ギリアード サイエンシーズ， インコーポレイテッド | ４’−置換カルボビル誘導体およびアバカビル誘導体ならびにｈｉｖおよびｈｃｖ抗ウイルス活性を有する関連化合物 |
| US20050182252A1 (en) | 2004-02-13 | 2005-08-18 | Reddy K. R. | Novel 2'-C-methyl nucleoside derivatives |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| RU2364596C2 (ru) * | 2004-06-11 | 2009-08-20 | Джапан Тобакко Инк. | ПРОИЗВОДНЫЕ 5-АМИНО-2,4,7-ТРИОКСО-3,4,7,8-ТЕТРАГИДРО-2Н-ПИРИДО[2,3-d] ПИРИМИДИНА, ОБЛАДАЮЩИЕ ПРОТИВООПУХОЛЕВОЙ АКТИВНОСТЬЮ |
| CN101023094B (zh) * | 2004-07-21 | 2011-05-18 | 法莫赛特股份有限公司 | 烷基取代的2-脱氧-2-氟代-d-呋喃核糖基嘧啶和嘌呤及其衍生物的制备 |
| WO2006110157A2 (en) | 2004-07-27 | 2006-10-19 | Gilead Sciences, Inc. | Nucleoside phosphonate conjugates as anti hiv agents |
| ES2769377T3 (es) * | 2004-09-14 | 2020-06-25 | Gilead Pharmasset Llc | Intermedios de D-ribonolactona con sustitución de 2-fluoro-2-alquilo |
| AU2006222563A1 (en) * | 2005-03-08 | 2006-09-14 | Biota Scientific Management Pty Ltd. | Bicyclic nucleosides and nucleotides as therapeutic agents |
| US7951789B2 (en) * | 2006-12-28 | 2011-05-31 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| BRPI0815563A2 (pt) * | 2007-07-12 | 2015-02-18 | Univ South Florida | Inibidores de akt/pkb com atividade antitumoral |
| US8173621B2 (en) | 2008-06-11 | 2012-05-08 | Gilead Pharmasset Llc | Nucleoside cyclicphosphates |
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| US3423398A (en) * | 1965-05-10 | 1969-01-21 | Pfizer & Co C | Sangivamycin and derivatives thereof |
| JPH0725788B2 (ja) * | 1985-09-09 | 1995-03-22 | 帝人株式会社 | オリゴまたはポリヌクレオチド |
| US5034393A (en) * | 1989-07-27 | 1991-07-23 | Dowelanco | Fungicidal use of pyridopyrimidine, pteridine, pyrimidopyrimidine, pyrimidopyridazine, and pyrimido-1,2,4-triazine derivatives |
-
2001
- 2001-03-07 UA UA2002119182A patent/UA72612C2/uk unknown
- 2001-07-03 CZ CZ20024052A patent/CZ20024052A3/cs unknown
- 2001-07-03 NZ NZ521457A patent/NZ521457A/en unknown
- 2001-07-03 KR KR1020027014601A patent/KR20030032944A/ko not_active Abandoned
- 2001-07-03 WO PCT/US2001/041242 patent/WO2002003997A1/en not_active Ceased
- 2001-07-03 IL IL15184901A patent/IL151849A0/xx unknown
- 2001-07-03 MX MXPA02012156A patent/MXPA02012156A/es unknown
- 2001-07-03 AU AU7367001A patent/AU7367001A/xx active Pending
- 2001-07-03 CN CN01812327A patent/CN1440292A/zh active Pending
- 2001-07-03 HU HU0301614A patent/HUP0301614A3/hu unknown
- 2001-07-03 JP JP2002508451A patent/JP2004522694A/ja not_active Withdrawn
- 2001-07-03 US US10/221,397 patent/US7081449B2/en not_active Expired - Fee Related
- 2001-07-03 SK SK11-2003A patent/SK112003A3/sk unknown
- 2001-07-03 BR BR0111531-6A patent/BR0111531A/pt not_active IP Right Cessation
- 2001-07-03 EP EP01952967A patent/EP1303282A4/en not_active Withdrawn
- 2001-07-03 CA CA002405798A patent/CA2405798A1/en not_active Abandoned
- 2001-07-03 PL PL01359559A patent/PL359559A1/xx not_active Application Discontinuation
- 2001-07-03 AU AU2001273670A patent/AU2001273670B2/en not_active Expired - Fee Related
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2002
- 2002-10-04 ZA ZA200208010A patent/ZA200208010B/en unknown
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| IL151849A0 (en) | 2003-04-10 |
| CN1440292A (zh) | 2003-09-03 |
| JP2004522694A (ja) | 2004-07-29 |
| SK112003A3 (en) | 2003-04-01 |
| MXPA02012156A (es) | 2004-08-19 |
| EP1303282A4 (en) | 2004-04-07 |
| KR20030032944A (ko) | 2003-04-26 |
| CA2405798A1 (en) | 2002-01-17 |
| ZA200208010B (en) | 2004-04-28 |
| AU2001273670B2 (en) | 2005-07-14 |
| US20030144502A1 (en) | 2003-07-31 |
| NZ521457A (en) | 2005-03-24 |
| UA72612C2 (en) | 2005-03-15 |
| NO20030033D0 (no) | 2003-01-03 |
| NO20030033L (no) | 2003-01-03 |
| HUP0301614A3 (en) | 2005-02-28 |
| WO2002003997A1 (en) | 2002-01-17 |
| EP1303282A1 (en) | 2003-04-23 |
| PL359559A1 (en) | 2004-08-23 |
| HUP0301614A2 (hu) | 2003-09-29 |
| BR0111531A (pt) | 2004-07-06 |
| AU7367001A (en) | 2002-01-21 |
| US7081449B2 (en) | 2006-07-25 |
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