HUP0500455A2 - Parciális és teljes A1-agonisták N6-heterociklusos-5'-tiocsoporttal szubsztituált adenozinszármazékok - Google Patents

Parciális és teljes A1-agonisták N6-heterociklusos-5'-tiocsoporttal szubsztituált adenozinszármazékok

Info

Publication number
HUP0500455A2
HUP0500455A2 HU0500455A HUP0500455A HUP0500455A2 HU P0500455 A2 HUP0500455 A2 HU P0500455A2 HU 0500455 A HU0500455 A HU 0500455A HU P0500455 A HUP0500455 A HU P0500455A HU P0500455 A2 HUP0500455 A2 HU P0500455A2
Authority
HU
Hungary
Prior art keywords
group
partial
full
heterocyclic
agonists
Prior art date
Application number
HU0500455A
Other languages
English (en)
Inventor
Jeff A. Zablocki
Venkata P. Palle
Vaibhav Varkhedkar
Luiz Belardinelli
Prabha N. Ibrahim
Original Assignee
Cv Therapeutics, Inc.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Cv Therapeutics, Inc. filed Critical Cv Therapeutics, Inc.
Publication of HUP0500455A2 publication Critical patent/HUP0500455A2/hu

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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
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Genetics & Genomics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

A találmány tárgyát képezik az (Ia) általános képletű vegyületek, azokelőállítása és alkalmazásuk. Az (Ia) képletben X1 jelentése S, S(O)vagy S(O)2 képletű csoport; R1 jelentése heterociklusos csoport,amelynek legalább az egyik szénatomját nitrogén-, oxigén- vagyfoszforatom, vagy S(O)0-2 csoport helyettesíti; R2 jelentése hidrogén-vagy halogénatom, CF3 vagy cianocsoport; R3 és R4 jelentése egymástólfüggetlenül alkil-, alkenil-, alkinilcsoport, heterociklil-, aril-vagy heteroarilcsoport, amelyek önmagukban is 1-3 szubsztituensthordozhatnak; R5 jelentése alkil-, alkenil-, alkinil-, heterociklil-,aril vagy heteroarilcsoport, amelyek önmagukban is 1-3 szubsztituensthordozhatnak. A találmány szerinti vegyületek parciális vagy teljesadenozin A1-receptoragonisták; ennek alapján a koszorúerekaktivitásának növelésére, a szívizomsejtek funkciójának módosítására,központi idegrendszeri megbetegedések és cukorbetegség kezelésérealkalmazhatók.
HU0500455A 1999-12-03 2000-12-01 Parciális és teljes A1-agonisták N6-heterociklusos-5'-tiocsoporttal szubsztituált adenozinszármazékok HUP0500455A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/454,136 US6605597B1 (en) 1999-12-03 1999-12-03 Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives
PCT/US2000/032721 WO2001040246A1 (en) 1999-12-03 2000-12-01 Partial or full a1 agonists - n6 heterocyclic 5'-thio substituted adenosine derivatives

Publications (1)

Publication Number Publication Date
HUP0500455A2 true HUP0500455A2 (hu) 2005-08-29

Family

ID=23803455

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0500455A HUP0500455A2 (hu) 1999-12-03 2000-12-01 Parciális és teljes A1-agonisták N6-heterociklusos-5'-tiocsoporttal szubsztituált adenozinszármazékok

Country Status (25)

Country Link
US (2) US6605597B1 (hu)
EP (1) EP1233973B1 (hu)
JP (1) JP4021195B2 (hu)
KR (1) KR100484988B1 (hu)
CN (1) CN1152042C (hu)
AR (1) AR029199A1 (hu)
AT (1) ATE254133T1 (hu)
AU (3) AU4138701A (hu)
BR (1) BR0016126A (hu)
CA (1) CA2389264C (hu)
CZ (1) CZ20013705A3 (hu)
DE (1) DE60006576T2 (hu)
DK (1) DK1233973T3 (hu)
ES (1) ES2208437T3 (hu)
HK (1) HK1047941A1 (hu)
HU (1) HUP0500455A2 (hu)
IL (1) IL145903A (hu)
MX (1) MXPA01011113A (hu)
NO (1) NO20015373L (hu)
NZ (1) NZ514777A (hu)
PT (1) PT1233973E (hu)
TR (2) TR200103129T2 (hu)
TW (1) TWI249536B (hu)
WO (2) WO2001040243A2 (hu)
ZA (1) ZA200204380B (hu)

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USRE47351E1 (en) 1999-06-22 2019-04-16 Gilead Sciences, Inc. 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
US6605597B1 (en) * 1999-12-03 2003-08-12 Cv Therapeutics, Inc. Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives
AU2001238665A1 (en) * 2000-02-23 2001-09-03 Cv Therapeutics, Inc. Method of identifying partial agonists of the a2a receptor
GB2372742A (en) * 2001-03-03 2002-09-04 Univ Leiden C2,5'-Disubstituted and N6,C2,5'-trisubstituted adenosine derivatives and their different uses
GB2372741A (en) * 2001-03-03 2002-09-04 Univ Leiden C2,8-Disubstituted adenosine derivatives and their different uses
US7713946B2 (en) 2002-07-11 2010-05-11 Cv Therapeutics, Inc. Partial and full agonists A1 adenosine receptors
US6946449B2 (en) * 2001-07-13 2005-09-20 Cv Therapeutics, Inc. Partial and full agonists of A1 adenosine receptors
US7157440B2 (en) 2001-07-13 2007-01-02 Cv Therapeutics, Inc. Partial and full agonists of A1 adenosine receptors
IL163613A0 (en) * 2002-02-19 2005-12-18 Cv Therapeutics Inc Partial and full agonists of a1 adenosine receptors
ATE418991T1 (de) * 2002-04-18 2009-01-15 Cv Therapeutics Inc Methode zur behandlung von herzrhythmusstörungen mit einem a1 adenosin agonist zusammen mit einem beta blocker
CN1671399A (zh) * 2002-07-29 2005-09-21 Cv医药有限公司 利用a2a受体激动剂的心肌灌注显像
US20050020915A1 (en) * 2002-07-29 2005-01-27 Cv Therapeutics, Inc. Myocardial perfusion imaging methods and compositions
US8470801B2 (en) 2002-07-29 2013-06-25 Gilead Sciences, Inc. Myocardial perfusion imaging methods and compositions
CA2515068A1 (en) 2003-02-03 2004-08-19 Cv Therapeutics Inc. Partial and full agonists of a1 adenosine receptors
US7749981B2 (en) 2003-10-21 2010-07-06 Inspire Pharmaceuticals, Inc. Drug-eluting stents coated with non-nucleotide P2Y12 receptor antagonist compound
US7335648B2 (en) 2003-10-21 2008-02-26 Inspire Pharmaceuticals, Inc. Non-nucleotide composition and method for inhibiting platelet aggregation
WO2005039590A1 (en) 2003-10-21 2005-05-06 Inspire Pharmaceuticals, Inc. Non-nucleotide compositions and method for treating pain
WO2005040174A1 (en) 2003-10-21 2005-05-06 Inspire Pharmaceuticals, Inc. Tetrahydro-furo`3,4-d!dioxole compounds and compositions and method for inhibiting platelet aggregation
PL1682537T3 (pl) * 2003-11-05 2012-09-28 Sarcode Bioscience Inc Modulatory adhezji komórkowej
CA2583185A1 (en) 2004-10-20 2006-04-27 Cv Therapeutics, Inc. Use of a2a adenosine receptor agonists
US7932376B2 (en) 2005-05-05 2011-04-26 Inspire Pharmaceuticals, Inc. Pyrimidine-based non-nucleotide composition and method for inhibiting platelet aggregation
CA2609053C (en) * 2005-05-17 2017-04-25 Sarcode Corporation Compositions and methods for treatment of eye disorders
CA2627319A1 (en) * 2005-11-30 2007-06-07 Prakash Jagtap Purine derivatives and methods of use thereof
EP2581381A3 (en) * 2006-02-03 2013-10-30 Gilead Sciences, Inc. Process for preparing an A2A-adenosine receptor agonist and its polymorphs
WO2007107598A1 (en) 2006-03-21 2007-09-27 Heinrich-Heine-Universität Düsseldorf Phosphorylated a2a receptor agonists
JP2009541354A (ja) * 2006-06-22 2009-11-26 シーブイ・セラピューティクス・インコーポレイテッド 虚血の治療におけるａ２ａアデノシン受容体アゴニストの使用
US20090081120A1 (en) * 2006-09-01 2009-03-26 Cv Therapeutics, Inc. Methods and Compositions for Increasing Patient Tolerability During Myocardial Imaging Methods
WO2008028140A1 (en) * 2006-09-01 2008-03-06 Cv Therapeutics, Inc. Methods and compositions for increasing patient tolerability during myocardial imaging methods
CA2663361A1 (en) * 2006-09-29 2008-04-10 Cv Therapeutics, Inc. Methods for myocardial imaging in patients having a history of pulmonary disease
WO2008086096A2 (en) * 2007-01-03 2008-07-17 Cv Therapeutics, Inc. Myocardial perfusion imaging
EP3797775A1 (en) 2007-10-19 2021-03-31 Novartis AG Compositions and methods for treatment of diabetic retinopathy
WO2009114533A2 (en) 2008-03-10 2009-09-17 Cornell University Modulation of blood brain barrier permeability
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Also Published As

Publication number Publication date
IL145903A (en) 2006-04-10
DE60006576T2 (de) 2004-09-16
PT1233973E (pt) 2004-02-27
CA2389264C (en) 2007-03-06
NO20015373D0 (no) 2001-11-02
ATE254133T1 (de) 2003-11-15
KR100484988B1 (ko) 2005-04-22
CZ20013705A3 (cs) 2002-04-17
TR200103129T2 (tr) 2002-10-21
AU761029B2 (en) 2003-05-29
EP1233973B1 (en) 2003-11-12
US20050054605A1 (en) 2005-03-10
DE60006576D1 (de) 2003-12-18
WO2001040246A1 (en) 2001-06-07
NO20015373L (no) 2001-11-29
MXPA01011113A (es) 2002-06-04
DK1233973T3 (da) 2004-02-16
CN1152042C (zh) 2004-06-02
JP4021195B2 (ja) 2007-12-12
HK1047941A1 (zh) 2003-03-14
EP1233973A1 (en) 2002-08-28
AU1811701A (en) 2001-06-12
ZA200204380B (en) 2003-06-25
AU4138701A (en) 2001-06-12
CA2389264A1 (en) 2001-06-07
BR0016126A (pt) 2002-08-06
TR200301971T4 (tr) 2004-01-21
WO2001040243A3 (en) 2001-12-13
CN1378550A (zh) 2002-11-06
AU7938301A (en) 2002-03-21
JP2003516325A (ja) 2003-05-13
NZ514777A (en) 2004-01-30
KR20030032907A (ko) 2003-04-26
AR029199A1 (es) 2003-06-18
TWI249536B (en) 2006-02-21
US6605597B1 (en) 2003-08-12
WO2001040243A2 (en) 2001-06-07
ES2208437T3 (es) 2004-06-16

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