HUP9901024A2 - Telített azolok oxoszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk - Google Patents

Telített azolok oxoszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

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Publication number
HUP9901024A2
HUP9901024A2 HU9901024A HUP9901024A HUP9901024A2 HU P9901024 A2 HUP9901024 A2 HU P9901024A2 HU 9901024 A HU9901024 A HU 9901024A HU P9901024 A HUP9901024 A HU P9901024A HU P9901024 A2 HUP9901024 A2 HU P9901024A2
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HU
Hungary
Prior art keywords
ring
alkenyl
alkyl
condensed
hydrogen atom
Prior art date
Application number
HU9901024A
Other languages
English (en)
Inventor
Clarence Webster Andrews III.
Christopher Todd Baker
Govinda Rao Bhisetti
David D. Deininger
Wieslaw M. Kazmierski
Francesco Gerald Salituro
Andrew Spaltenstein
Roger Dennis Tung
Original Assignee
Vertex Pharmaceuticals Incorporated
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
Priority claimed from US08/592,777 external-priority patent/US5883252A/en
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP9901024A2 publication Critical patent/HUP9901024A2/hu

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • 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
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/30—Oxygen or sulfur atoms
    • C07D233/32—One oxygen atom
    • C07D233/36—One oxygen atom with hydrocarbon radicals, substituted by nitrogen atoms, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (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)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

A találmány aszpartil prőteáz inhibitőr hatású (I) általánős képletűvegyületekre vőnatkőzik, amelyek képletében Z adőtt esetben R6 csőpőrttal kőndenzált (a) vagy (b) vagy (c)csőpőrt; X és X' karbőnil-, őxalil-, szűlfinil- vagy szűlfőnilcsőpőrt; Y és Y' -[C(R2)2]p-, -NR2-, -[C(R2)2]p-M-, >C=C(R2)2 vagy -N(R2)-CH2-csőpőrt; R1 hidrőgénatőm, R6, alkil-, alkenil-, alkinil-, adőtt esetben R6csőpőrttal kindenzált ciklőalkil- vagy ciklőalkenilcsőpőrt; és aszőmszédős atőmőkhőz kapcsőlódó R1 szűbsztitűensek karbőciklűsős vagyheterőciklűsős gyűrűrendszert képezhetnek; ahől bármely R1 adőttesetben szűbsztitűált; R4 -OR9, -X-R9, -N(R9)2, -C(O)N(R9)2, R6, alkil-, alkenil-, adőttesetben R6 csőpőrttal kőndenzált ciklőalkil- vagy ciklőalkenilcsőpőrt;ahől bármely R4 szűbsztitűens adőtt esetben egy vagy több csőpőrttalszűbsztitűált; R5 hidrőgénatőm, hidrőxi-, őxőcsőpőrt vagy R1; R6 adőtt esetben szűbsztitűált aril-, karbőciklűsős vagyheterőciklűsős csőpőrt; R7 hidrőgénatőm, hidrőxi- vagy őxőcsőpőrt; Q metincsőpőrt vagy nitrőgénatőm; M iminő-, -NR2-, őxigén-, tiő-, szűlfinil-, szűlfőnilcsőpőrt; n és p értéke 1 vagy 2; q mindegyikének értéke 1, 2 vagy 3; és G iminő-, -NR2-, őxigén-, tiő-, szűlfinil-, szűlfőnil-, karbőnil- vagy-C(R2)2- csőpőrt. ŕ
HU9901024A 1996-01-26 1997-01-22 Telített azolok oxoszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk HUP9901024A2 (hu)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/592,777 US5883252A (en) 1996-01-26 1996-01-26 Aspartyl protease inhibitors
US08/724,563 US5945413A (en) 1996-01-26 1996-09-30 Aspartyl protease inhibitors

Publications (1)

Publication Number Publication Date
HUP9901024A2 true HUP9901024A2 (hu) 1999-09-28

Family

ID=27081545

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9901024A HUP9901024A2 (hu) 1996-01-26 1997-01-22 Telített azolok oxoszármazékai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk

Country Status (12)

Country Link
EP (1) EP0882022A1 (hu)
JP (1) JP2000501111A (hu)
AP (1) AP844A (hu)
AU (1) AU709239B2 (hu)
BR (1) BR9707086A (hu)
CA (1) CA2243121A1 (hu)
CZ (1) CZ234498A3 (hu)
HU (1) HUP9901024A2 (hu)
IL (1) IL125479A0 (hu)
NO (1) NO983435L (hu)
PL (1) PL328223A1 (hu)
WO (1) WO1997027180A1 (hu)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1019056A1 (en) * 1997-05-17 2000-07-19 Glaxo Group Limited Antiviral combinations containing the carbocyclic nucleoside 1592u89
US6420401B1 (en) 1997-08-22 2002-07-16 Wichita State University 1,2,5, thiadiazolidin-3-one 1,1-dioxide derivatives
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors
US6337340B1 (en) * 1998-08-14 2002-01-08 Gpi Nil Holdings, Inc. Carboxylic acids and isosteres of heterocyclic ring compounds having multiple heteroatoms for vision and memory disorders
US6303609B1 (en) * 1998-11-18 2001-10-16 Dupont Pharmaceuticals Company Isoxazoline fibrinogen receptor antagonists
DE10047110A1 (de) * 2000-09-22 2002-04-18 Bayer Ag Optisch aktive 2,5-Bisaryl-DELTA·1·-Pyrroline
CA2527159A1 (en) 2003-05-30 2004-12-09 Neuromed Technologies, Inc. 3-aminomethyl-pyrrolidines as n-type calcium channel blockers
CN102627609B (zh) * 2003-12-15 2016-05-04 默沙东公司 杂环天冬氨酰蛋白酶抑制剂
JP2005232103A (ja) * 2004-02-20 2005-09-02 Nagase & Co Ltd 光学活性なビシナルジアミンおよびその製造方法
GB0412019D0 (en) * 2004-05-28 2004-06-30 Novartis Ag Organic compounds
US7388008B2 (en) 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
CA2606025A1 (en) * 2005-04-27 2006-11-02 Ambrilia Biopharma Inc. Method for improving pharmacokinetics of protease inhibitors and protease inhibitor precursors
JP2008543841A (ja) * 2005-06-14 2008-12-04 シェーリング コーポレイション 大環状複素環式アスパルチルプロテアーゼインヒビター
AU2006319716B2 (en) 2005-11-30 2012-02-02 Taimed Biologics, Inc. Lysine-based prodrugs of aspartyl protease inhibitors and processes for their preparation
PE20080942A1 (es) 2006-06-20 2008-09-03 Wyeth Corp Compuestos 1-n-amino-2-imidazolidinonas como inhibidores del canal de potasion kv1.5
JP5401652B2 (ja) 2006-09-21 2014-01-29 タイメッド バイオロジクス インコーポレイテッド プロテアーゼ阻害剤
EP2726108B1 (en) 2011-06-29 2018-01-10 The Trustees of Columbia University in the City of New York Inhibitor of neuronal connectivity linked to schizophrenia susceptibility and cognitive dysfunction
CN103626713B (zh) * 2012-08-29 2017-07-04 中国科学院上海药物研究所 氮(氧)杂环戊烷‑2‑酮(硫酮)类化合物、其药物组合物、制备方法和用途
CN105111198B (zh) * 2015-08-05 2018-08-07 贵州大学 硝基异噁唑拼接2-吡咯烷酮类化合物及其制备方法及应用

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5610294A (en) * 1991-10-11 1997-03-11 The Du Pont Merck Pharmaceutical Company Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
ATE184594T1 (de) * 1994-03-07 1999-10-15 Vertex Pharma Sulfonamidderivate als aspartylprotease- inhibitoren

Also Published As

Publication number Publication date
PL328223A1 (en) 1999-01-18
AP9700961A0 (en) 1997-04-30
AP844A (en) 2000-06-09
NO983435L (no) 1998-09-21
JP2000501111A (ja) 2000-02-02
IL125479A0 (en) 1999-03-12
BR9707086A (pt) 1999-04-13
AU709239B2 (en) 1999-08-26
AU1758097A (en) 1997-08-20
EP0882022A1 (en) 1998-12-09
CA2243121A1 (en) 1997-07-31
CZ234498A3 (cs) 1998-10-14
WO1997027180A1 (en) 1997-07-31
NO983435D0 (no) 1998-07-24

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