AU699914B2 - Novel enzyme inhibitors, their synthesis, and methods for use - Google Patents

Novel enzyme inhibitors, their synthesis, and methods for use Download PDF

Info

Publication number
AU699914B2
AU699914B2 AU78476/94A AU7847694A AU699914B2 AU 699914 B2 AU699914 B2 AU 699914B2 AU 78476/94 A AU78476/94 A AU 78476/94A AU 7847694 A AU7847694 A AU 7847694A AU 699914 B2 AU699914 B2 AU 699914B2
Authority
AU
Australia
Prior art keywords
pyrimidine
compound
phenylthio
uracil
phenylselenenyl
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.)
Ceased
Application number
AU78476/94A
Other languages
English (en)
Other versions
AU7847694A (en
Inventor
Mahmoud H El Kouni
Fardos N. M. Naguib
Raymond F. Schinazi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
FARDOS N M NAGUIB
Original Assignee
FARDOS N M NAGUIB
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 FARDOS N M NAGUIB filed Critical FARDOS N M NAGUIB
Publication of AU7847694A publication Critical patent/AU7847694A/en
Application granted granted Critical
Publication of AU699914B2 publication Critical patent/AU699914B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU78476/94A 1993-11-02 1994-09-30 Novel enzyme inhibitors, their synthesis, and methods for use Ceased AU699914B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US08/146,838 US5476855A (en) 1993-11-02 1993-11-02 Enzyme inhibitors, their synthesis and methods for use
US08/146838 1993-11-02
PCT/US1994/011173 WO1995012400A1 (en) 1993-11-02 1994-09-30 Novel enzyme inhibitors, their synthesis, and methods for use

Publications (2)

Publication Number Publication Date
AU7847694A AU7847694A (en) 1995-05-23
AU699914B2 true AU699914B2 (en) 1998-12-17

Family

ID=22519188

Family Applications (1)

Application Number Title Priority Date Filing Date
AU78476/94A Ceased AU699914B2 (en) 1993-11-02 1994-09-30 Novel enzyme inhibitors, their synthesis, and methods for use

Country Status (9)

Country Link
US (3) US5476855A (enExample)
EP (1) EP0725641B1 (enExample)
JP (1) JP3621102B2 (enExample)
AT (1) ATE198046T1 (enExample)
AU (1) AU699914B2 (enExample)
DE (1) DE69426423T2 (enExample)
ES (1) ES2155093T3 (enExample)
PT (1) PT725641E (enExample)
WO (1) WO1995012400A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5476855A (en) * 1993-11-02 1995-12-19 Mahmoud H. el Kouni Enzyme inhibitors, their synthesis and methods for use
DE69430587T2 (de) * 1994-02-28 2003-01-09 Sunkyong Industries Co. Ltd., Suwon Pyrimidin-acyclonukleosid-derivate
US5811073A (en) * 1995-06-19 1998-09-22 President And Fellows Of Harvard College Method for radioisotopic detection and localization of inflammation in a host
US5719132A (en) * 1996-06-27 1998-02-17 Bristol-Myers Squibb Company Compositions and methods of treating HIV with d4T, 5-fluorouracil/tegafur, and uracil
US6306909B1 (en) 1997-03-12 2001-10-23 Queen's University At Kingston Anti-epileptogenic agents
US6177437B1 (en) * 1998-09-04 2001-01-23 University Of Massachusetts Medical Center Inhibitors of Herpes Simplex virus uracil-DNA glycosylase
DK1255738T3 (da) * 2000-01-25 2012-06-25 Neurocrine Biosciences Inc Gonadotropin-frigivende hormonreceptor-antagonister og fremgangsmåder relateret dertil
US7501429B2 (en) * 2001-04-11 2009-03-10 Queen's University At Kingston Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents
JP2004536071A (ja) * 2001-05-25 2004-12-02 クイーンズ　ユニバーシティ　アット　キングストン 複素環ベータアミノ酸およびそれらの抗癲癇誘発剤としての使用
WO2005012309A1 (fr) * 2003-08-04 2005-02-10 Valery Khazhmuratovich Zhilov Bioisosteres cycliques issus d'un systeme purine et composition pharmaceutique a base desdits bioisosteres
EP1827443A1 (en) * 2004-12-03 2007-09-05 Adherex Technologies, Inc. Methods for administering dpd inhibitors in combination with 5-fu and 5-fu prodrugs
US20100158967A1 (en) * 2005-05-24 2010-06-24 Ted Reid Selenium-based biocidal formulations and methods of use thereof
AU2006269657B2 (en) * 2005-05-24 2012-04-19 Selenbio, Inc. Selenium-based biocidal formulations and methods of use thereof
US9370187B2 (en) 2005-05-24 2016-06-21 Selenium, Ltd. Selenium-based biocidal formulations and methods of use thereof
US20100158966A1 (en) * 2005-05-24 2010-06-24 Ted Reid Selenium-based biocidal formulations and methods of use thereof
NZ565955A (en) 2005-08-22 2011-08-26 Melior Pharmaceuticals I Inc Methods and formulations for modulating lyn kinase activity and treating related disorders
CN101686686A (zh) * 2007-02-20 2010-03-31 梅里奥尔医药I公司 鉴别Lyn激酶激活剂的方法
CA2693809A1 (en) * 2007-07-23 2009-01-29 Melior Discovery, Inc. Methods of activating irs-1 and akt
AU2009223453B2 (en) 2008-03-03 2014-05-01 Tosk, Inc. Methotrexate adjuvants to reduce toxicity and methods for using the same
US8552184B2 (en) * 2008-07-03 2013-10-08 Melior Pharmaceuticals I, Inc. Compounds and methods for treating disorders related to glucose metabolism
WO2010080086A1 (en) * 2009-01-12 2010-07-15 Selenium, Ltd. Anti-microbial orthodontic compositions and appliances and methods of production and use thereof
US8658618B2 (en) * 2009-10-14 2014-02-25 Adherex Technologies, Inc. Methods for preventing or reducing neurotoxicity associated with administering DPD inhibitors in combination with 5-FU and 5-FU prodrugs
US20130158055A1 (en) 2010-05-28 2013-06-20 Andrew G. Reaume Prevention Of Pancreatic Beta Cell Degeneration
KR102634575B1 (ko) 2017-04-10 2024-02-06 멜리어 파마슈티칼스 아이, 인코포레이티드 지방세포의 처리
US11446303B2 (en) 2019-06-21 2022-09-20 Tosk, Inc. Uridine phosphorylase (UPase) inhibitors for treatment of liver conditions

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4613604A (en) * 1985-07-31 1986-09-23 Brown University Research Foundation Hydroxymethyl derivatives of 5-benzylacyclouridine and 5-benzoyloxybenzylacyclouridine and their use as potentiators for 5-fluoro-2'-deoxyuridine
US5077280A (en) * 1988-04-12 1991-12-31 Brown University Research Foundation Treatment of viral infections

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3755295A (en) * 1969-10-24 1973-08-28 Syntex Corp 1-(2-amino-2-deoxy-{62 -d-ribofuranosyl) pyrimidines and derivatives thereof
US3687931A (en) * 1970-03-19 1972-08-29 Syntex Corp Halogenated purine and pyrimidine nucleosides and process therefor
JPS5738774A (en) * 1980-08-19 1982-03-03 Chugai Pharmaceut Co Ltd Uracil derivative and its preparation
US4868187A (en) * 1980-09-16 1989-09-19 Syntex (U.S.A.) Inc. Anti-viral N-substituted pyrimidines
DD283613A5 (de) * 1988-03-31 1990-10-17 ��@���������@�������k�� Verfahren zur herstellung von in 6-stellung substituierte acyclopyrimidin-nucleosid-derivaten
EP0449726B1 (en) * 1990-03-29 1997-06-11 Mitsubishi Chemical Corporation Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient
US5141943A (en) * 1990-04-12 1992-08-25 Brown University Research Foundation 5-benzyl barbiturate derivatives
US5476855A (en) * 1993-11-02 1995-12-19 Mahmoud H. el Kouni Enzyme inhibitors, their synthesis and methods for use
KR0151811B1 (ko) * 1993-12-21 1998-10-15 강박광 신규한 항바이러스성 2,4-피리미딘디온 유도체 및 그의 제조방법

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4613604A (en) * 1985-07-31 1986-09-23 Brown University Research Foundation Hydroxymethyl derivatives of 5-benzylacyclouridine and 5-benzoyloxybenzylacyclouridine and their use as potentiators for 5-fluoro-2'-deoxyuridine
US5077280A (en) * 1988-04-12 1991-12-31 Brown University Research Foundation Treatment of viral infections

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PHARMAC. THERAP. V8 1981 P629-651 *

Also Published As

Publication number Publication date
DE69426423T2 (de) 2001-07-12
ES2155093T3 (es) 2001-05-01
AU7847694A (en) 1995-05-23
JPH09507054A (ja) 1997-07-15
DE69426423D1 (de) 2001-01-18
US5721241A (en) 1998-02-24
PT725641E (pt) 2001-05-31
EP0725641A4 (enExample) 1996-09-04
ATE198046T1 (de) 2000-12-15
WO1995012400A1 (en) 1995-05-11
EP0725641B1 (en) 2000-12-13
US5476855A (en) 1995-12-19
JP3621102B2 (ja) 2005-02-16
EP0725641A1 (en) 1996-08-14
USRE37623E1 (en) 2002-04-02

Similar Documents

Publication Publication Date Title
AU699914B2 (en) Novel enzyme inhibitors, their synthesis, and methods for use
US5141943A (en) 5-benzyl barbiturate derivatives
Tanaka et al. Synthesis and antiviral activity of deoxy analogs of 1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine (HEPT) as potent and selective anti-HIV-1 agents
KR100279953B1 (ko) 항-b형 간염 바이러스제 및 항-사람 면역결핍 바이러스제로서의 l-2',3'-디데옥시 누클레오시드 유사체
Niedzwicki et al. 5-Benzylacyclouridine and 5-benzyloxybenzylacyclouridine, potent inhibitors of uridine phosphorylase
JP4737934B2 (ja) ヌクレオシドホスホリラーゼ及びヌクレオシダーゼのインヒビター
US6436945B2 (en) Substituted O6-benzyl-8-aza-guanines
Rosowsky et al. Synthesis and antitumor activity of an acyclonucleoside derivative of 5-fluorouracil
Goudgaon et al. Phenylselenenyl-and phenylthio-substituted pyrimidines as inhibitors of dihydrouracil dehydrogenase and uridine phosphorylase
CN112110938B (zh) 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途
JPS63297381A (ja) ９−〔２−（ヒドロキシメチル）シクロアルキルメチル〕グアニン類
CZ16196A3 (en) 5-substituted or 5,6-dihydro-5-substituted uracil derivative or a pharmaceutical preparation or a combination thereof containing said derivative
Siddiqui et al. Chemistry and anti-HIV properties of 2'-fluoro-2', 3'-dideoxyarabinofuranosylpyrimidines
EP0711555A2 (en) Enzyme inactivators
CA2176720C (en) Novel enzyme inhibitors, their synthesis, and methods for use
JPS63287770A (ja) １−〔２−（ヒドロキシメチル）シクロアルキルメチル〕−５−置換ウラシル類
JP2000516578A (ja) アデノシンデアミナーゼ阻害剤
Schinazi et al. Synthesis, antiviral activity, cytotoxicity, and cellular pharmacology of 5-carboranyl-pyrimidine nucleosides
US6677345B1 (en) Cyclin dependent kinase inhibitors
JPH06172365A (ja) １０−チアイソアロキサジン誘導体およびその用途
JPS6223723B2 (enExample)
KR20010006730A (ko) 신규한 항바이러스성 2,4-피리미딘디온 유도체
Saheb The Synthesis of Fluorinated Thymine Analogues as Potential Anticancer Agents
HK1013257B (en) L-2',3'-dideoxy nucleoside analogs as anti-hepatitis b (hbv) and anti-hiv agents