CN100389109C - 非核苷逆转录酶抑制剂 - Google Patents

非核苷逆转录酶抑制剂 Download PDF

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Publication number
CN100389109C
CN100389109C CNB2004800044061A CN200480004406A CN100389109C CN 100389109 C CN100389109 C CN 100389109C CN B2004800044061 A CNB2004800044061 A CN B2004800044061A CN 200480004406 A CN200480004406 A CN 200480004406A CN 100389109 C CN100389109 C CN 100389109C
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CN
China
Prior art keywords
alkyl
alkoxy
phenyl
substituted
optionally
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.)
Expired - Fee Related
Application number
CNB2004800044061A
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English (en)
Chinese (zh)
Other versions
CN1751028A (zh
Inventor
J·P·杜恩
J·H·霍格
T·米尔扎德甘
S·斯沃洛
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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.)
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Publication date
Application filed by F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CN1751028A publication Critical patent/CN1751028A/zh
Application granted granted Critical
Publication of CN100389109C publication Critical patent/CN100389109C/zh
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • C07D231/20—One oxygen atom attached in position 3 or 5
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CNB2004800044061A 2003-02-18 2004-02-17 非核苷逆转录酶抑制剂 Expired - Fee Related CN100389109C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US44797403P 2003-02-18 2003-02-18
US60/447,974 2003-02-18

Publications (2)

Publication Number Publication Date
CN1751028A CN1751028A (zh) 2006-03-22
CN100389109C true CN100389109C (zh) 2008-05-21

Family

ID=32908518

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2004800044061A Expired - Fee Related CN100389109C (zh) 2003-02-18 2004-02-17 非核苷逆转录酶抑制剂

Country Status (17)

Country Link
US (1) US7241794B2 (enExample)
EP (1) EP1597235B1 (enExample)
JP (1) JP4608480B2 (enExample)
KR (1) KR100776093B1 (enExample)
CN (1) CN100389109C (enExample)
AR (1) AR043195A1 (enExample)
AT (1) ATE370124T1 (enExample)
BR (1) BRPI0407591A (enExample)
CA (1) CA2515151C (enExample)
CL (1) CL2004000270A1 (enExample)
DE (1) DE602004008227T2 (enExample)
ES (1) ES2291854T3 (enExample)
MX (1) MXPA05008748A (enExample)
PL (1) PL378556A1 (enExample)
RU (1) RU2305680C2 (enExample)
TW (1) TW200423930A (enExample)
WO (1) WO2004074257A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004099157A1 (en) * 2003-05-07 2004-11-18 Pfizer Products Inc. Cannabinoid receptor ligands and uses thereof
WO2006013948A1 (ja) 2004-08-04 2006-02-09 Taisho Pharmaceutical Co., Ltd. トリアゾール誘導体
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
CN101415691B (zh) 2006-02-03 2011-12-14 大正制药株式会社 三唑衍生物
JP5218737B2 (ja) 2006-02-06 2013-06-26 大正製薬株式会社 スフィンゴシン−１−リン酸結合阻害物質
CN101384556B (zh) * 2006-02-14 2012-06-20 庵原化学工业株式会社 5-烷氧基-4-羟基甲基吡唑化合物的制备方法
CL2007002105A1 (es) * 2006-07-21 2008-02-22 Hoffmann La Roche Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u
CN101501002B (zh) * 2006-08-16 2012-06-27 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
KR20090127178A (ko) 2007-03-29 2009-12-09 에프. 호프만-라 로슈 아게 비뉴클레오시드 역전사 효소 억제제
RU2468009C2 (ru) 2007-08-01 2012-11-27 Тайсо Фармасьютикал Ко., Лтд. Ингибитор связывания s1p1
BRPI0821349A2 (pt) * 2007-12-21 2019-09-24 Hoffmann La Roche compostos antivirais heterocíclicos
DE102008015033A1 (de) * 2008-03-17 2009-09-24 Aicuris Gmbh & Co. Kg Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung
DK2924034T3 (en) * 2010-03-30 2017-02-06 Merck Canada Inc PHARMACEUTICAL COMPOSITION CONTAINING A NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR
AU2011277426B2 (en) 2010-07-15 2015-04-23 Sumitomo Pharma Co., Ltd. Pyrazole compound
EP2508511A1 (en) * 2011-04-07 2012-10-10 Laboratoire Biodim Inhibitors of viral replication, their process of preparation and their therapeutical uses
US9505728B2 (en) 2012-03-09 2016-11-29 Inception 2, Inc. Triazolone compounds and uses thereof
BR112014031899A8 (pt) 2012-06-20 2017-10-24 Univ Vanderbilt composto, composição farmacêutica, e, método para tratamento de um distúrbio
US8901125B2 (en) 2012-06-20 2014-12-02 Vanderbilt University Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
EP2935228B9 (en) 2012-12-20 2017-12-06 Inception 2, Inc. Triazolone compounds and uses thereof
PE20160880A1 (es) 2013-09-06 2016-09-22 Inception 2 Inc Compuestos de triazolona y usos de los mismos
CA2944187C (en) 2014-04-01 2018-06-19 Merck Sharp & Dohme Corp. Prodrugs of hiv reverse transcriptase inhibitors
US20170298055A1 (en) 2014-09-17 2017-10-19 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
WO2016044446A2 (en) 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. Sgc stimulators
WO2016149311A1 (en) * 2015-03-19 2016-09-22 E I Du Pont De Nemours And Company Fungicidal pyrazoles
EP3478665A1 (en) * 2016-06-29 2019-05-08 Esteve Pharmaceuticals, S.A. Pyrazole derivatives having activity against pain
CN110818636A (zh) * 2019-11-29 2020-02-21 河北科技大学 一种化合物或其盐及其应用和合成方法
CN115677585B (zh) * 2022-10-31 2024-03-19 上海群力化工有限公司 一种甲醛吡唑衍生物的合成工艺

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002004424A1 (en) * 2000-07-07 2002-01-17 Pfizer Limited Pyrazole derivatives
WO2002030907A1 (en) * 2000-10-10 2002-04-18 F. Hoffmann-La Roche Ag Pyrazole derivatives for the treatment of viral diseases
WO2002100853A1 (en) * 2001-06-04 2002-12-19 F. Hoffmann-La Roche Ag Pyrazole derivatives as hiv reverse transcriptase inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0786455B1 (en) 1994-09-26 2003-12-03 Shionogi & Co., Ltd. Imidazole derivative
DE19734664A1 (de) * 1997-08-11 1999-02-18 Bayer Ag (Hetero)Aryloxypyrazole
US20030008841A1 (en) * 2000-08-30 2003-01-09 Rene Devos Anti-HCV nucleoside derivatives
GB0028484D0 (en) * 2000-11-22 2001-01-10 Hoffmann La Roche Imidazolone derivatives for the treatment of viral diseases
BRPI0208811B8 (pt) * 2001-04-10 2021-05-25 Pfizer derivados de pirazol, seu uso e processo de preparação, bem como composição farmacêutica compreendendo os mesmos

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002004424A1 (en) * 2000-07-07 2002-01-17 Pfizer Limited Pyrazole derivatives
WO2002030907A1 (en) * 2000-10-10 2002-04-18 F. Hoffmann-La Roche Ag Pyrazole derivatives for the treatment of viral diseases
WO2002100853A1 (en) * 2001-06-04 2002-12-19 F. Hoffmann-La Roche Ag Pyrazole derivatives as hiv reverse transcriptase inhibitors

Also Published As

Publication number Publication date
RU2305680C2 (ru) 2007-09-10
CA2515151C (en) 2010-11-30
DE602004008227T2 (de) 2008-05-15
ES2291854T3 (es) 2008-03-01
JP4608480B2 (ja) 2011-01-12
JP2006515339A (ja) 2006-05-25
CL2004000270A1 (es) 2005-02-04
WO2004074257A1 (en) 2004-09-02
RU2005128832A (ru) 2006-04-27
EP1597235A1 (en) 2005-11-23
BRPI0407591A (pt) 2006-02-14
PL378556A1 (pl) 2006-05-02
US7241794B2 (en) 2007-07-10
DE602004008227D1 (de) 2007-09-27
EP1597235B1 (en) 2007-08-15
CN1751028A (zh) 2006-03-22
AU2004213134A1 (en) 2004-09-02
ATE370124T1 (de) 2007-09-15
CA2515151A1 (en) 2004-09-02
KR20050105471A (ko) 2005-11-04
TW200423930A (en) 2004-11-16
US20040192666A1 (en) 2004-09-30
KR100776093B1 (ko) 2007-11-15
MXPA05008748A (es) 2005-09-20
AR043195A1 (es) 2005-07-20

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C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
C17 Cessation of patent right
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20080521

Termination date: 20120217