NO20054127L - HIV-hemmende 1,2,4-triaziner - Google Patents

HIV-hemmende 1,2,4-triaziner

Info

Publication number
NO20054127L
NO20054127L NO20054127A NO20054127A NO20054127L NO 20054127 L NO20054127 L NO 20054127L NO 20054127 A NO20054127 A NO 20054127A NO 20054127 A NO20054127 A NO 20054127A NO 20054127 L NO20054127 L NO 20054127L
Authority
NO
Norway
Prior art keywords
alkyl
amino
substituted
aminocarbonyl
optionally substituted
Prior art date
Application number
NO20054127A
Other languages
English (en)
Inventor
Jan Heeres
Lucien Maria Henricus Koymans
Hendrikk Maarten Vinkers
Frederik Frans Desire Daeyaert
Paulus Joannes Lewi
Marc Rene De Jonge
Donald William Ludovici
Ruben Gerardus George Leenders
Georges Joseph Corne Hoornaert
Amuri Kilonda
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of NO20054127L publication Critical patent/NO20054127L/no

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5

Abstract

Den foreliggende oppfinnelse vedrører HIV-replikasjonsinhibitorer med formel 2a et 7V-oksid, et farmasøytisk akseptabelt addisjonssalt, et kvaternært amih eller en stereokjemisk isomer form derav, hvori ringen inneholdende -a1=a2-a3=a4- og -b1=b2-b3=b4- representerer fenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n og m er 0 til 4; R1 er hydrogen; aryl; formyl; Ci-6alkylkarbonyl; Ci-6alkyl; Ci_6alkyloksykarbonyl; Ci-6alkyl substituert med formyl, Ci_6alkyl-karbonyl, Ci-6alkyloksykarbonyl, Ci-6alkylkarbonyloksy; Ci-6alkyloksy Ci-6alkylkarbonyl substituert med Ci-6alkyloksykarbonyl; hver R2 er uavhengig hydroksy; halo; eventuelt substituert C]-6alkyl eller C2-6alkenyl eller C2-6alkynyl; C3.7cykloalkyl; Ci-6alkyloksykarbonyl; karboksyl; cyano; nitro; amino; mono- eller di(Ci.6alkyl)amino; polyhalometyl; polyhalometyltio; -S(=O)PR6; -NH-S(=O)PR6; -C(=O)R6; -NHC(=O)H; -C(=O)NHNH2; NHC(=O)R6; C(=NH)R6; R eller R3 er cyano; aminokarbonyl; amino; C^alkyl; halo; eventuelt substituert C,.6alkyloksy; NHR13; NR13R14; -C(=O)-NHR13; -C(=O)-NR13R14; -C(=O)-R15; -CH=N-NH-C(=O)-R16; substituert Ci_6alkyl; Ci-6alkyl substituert med hydroksy og en andre substituent; eventuelt substituert Ci^alkyloksyC^alkyl; substituert C2-6alkenyl eller C2-6alkynyl; -C(=N-O-R8)-CMalkyl; R7 eller-X3-R7; X, er-NR1-, - NH-NH-, -N=N-, -O-, -C(=O)-, CMalkandiyl, -CHOH-, -S-, -S(=O)P-, -X2-Ci. 4alkandiyl- eller -Ci4alkandiyl-X2-; R4 er halo; hydroksy; eventuelt substituert Ci_ . 6alkyl eller C2-6alkenyl eller C2-6alkynyl; C3-7cykloalkyl; Ci-6alkyloksy; cyano; nitro; polyhaloCi_6alkyl; polyhaloCi-éalkyloksy; aminokarbonyl; mono- eller di(CMalkyl)aminokarbonyl; Ci-6alkyloksykarbonyl; Ci-6alkylkarbonyl; formyl; amino; mono- eller di(Ci4alkyl)amino eller R7; R5 er hydrogen; halo; aminokarbonyl; mono- eller di(Ci^alkyl)aminokarbonyl; amino; Ci.6alkyloksykarbonyl; Ci^alkyl oksykarbonylamino; polyhaloCi-6alkyl; eventuelt substituert Ci^alkyl eller C2-6alkenyl eller C2-6alkynyl; forutsatt at de følgende forbindelser 1,2,4-triazin-6-karboksylsyre, 3,5-bis[(4-metylfenyl)amino]-, etylester; l,2,4-triazin-6-karboksylsyre, 3,5-bis[(4-nitrofenyl)amino]-, etylester; A^v/V-bis(4-klorfenyl)-6-fluor-l,2,4-triazin-3,5-diamin ikke er inkludert; deres anvendelse som en medisin, deres fremgangsmåter for fremstilling og farmasøytiske sammensetninger omfattende dem.
NO20054127A 2003-02-07 2005-09-05 HIV-hemmende 1,2,4-triaziner NO20054127L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP0301289 2003-02-07
PCT/EP2004/050084 WO2004074266A1 (en) 2003-02-07 2004-02-05 Hiv inhibiting 1,2,4-triazines

Publications (1)

Publication Number Publication Date
NO20054127L true NO20054127L (no) 2005-09-05

Family

ID=32892827

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20054127A NO20054127L (no) 2003-02-07 2005-09-05 HIV-hemmende 1,2,4-triaziner

Country Status (20)

Country Link
US (1) US7585861B2 (no)
EP (1) EP1597242B1 (no)
JP (1) JP4783725B2 (no)
KR (1) KR20050105190A (no)
CN (2) CN1747941A (no)
AP (1) AP2005003365A0 (no)
AT (1) ATE402152T1 (no)
AU (1) AU2004213173B2 (no)
BR (1) BRPI0407306A (no)
CA (1) CA2513123C (no)
DE (1) DE602004015254D1 (no)
EA (1) EA010379B1 (no)
ES (1) ES2311146T3 (no)
HR (1) HRP20050690A2 (no)
IL (1) IL170120A (no)
MX (1) MXPA05008368A (no)
NO (1) NO20054127L (no)
PL (1) PL232814B1 (no)
WO (1) WO2004074266A1 (no)
ZA (1) ZA200506254B (no)

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US7923554B2 (en) * 2004-08-10 2011-04-12 Janssen Pharmaceutica N.V. HIV inhibiting 1,2,4-triazin-6-one derivatives
NZ553492A (en) 2004-08-25 2010-11-26 Targegen Inc Triazole derivatives and methods of use
CN101084212A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶介导剂的用途
US7592343B2 (en) 2004-09-20 2009-09-22 Xenon Pharmaceuticals Inc. Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors
EP2289510A1 (en) 2004-09-20 2011-03-02 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-coa desaturase enzymes
WO2006034440A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-coa desaturase inhibitors
EP2316458A1 (en) 2004-09-20 2011-05-04 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
MX2007003321A (es) 2004-09-20 2007-06-05 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como agentes terapeuticos.
CN101084207A (zh) 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
CN101208089A (zh) 2005-06-03 2008-06-25 泽农医药公司 氨基噻唑衍生物作为人硬酯酰-CoA去饱和酶抑制剂
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
PT1951684T (pt) 2005-11-01 2016-10-13 Targegen Inc Inibidores de cinases de tipo biaril-meta-pirimidina
JP2010518014A (ja) * 2007-01-31 2010-05-27 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害剤として有用な２−アミノピリジン誘導体
DK2300013T3 (en) 2008-05-21 2017-12-04 Ariad Pharma Inc PHOSPHORUS DERIVATIVES AS KINASE INHIBITORS
MX2011000837A (es) 2008-07-23 2011-04-05 Vertex Pharma Inhibidores de pirazolpiridina cinasa triciclica.
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WO2011094290A1 (en) 2010-01-27 2011-08-04 Vertex Pharmaceuticals Incorporated Pyrazolopyrimidine kinase inhibitors
EP2528917B1 (en) 2010-01-27 2016-10-19 Vertex Pharmaceuticals Incorporated Pyrazolopyridines useful for the treatment of autoimmune, inflammatory or (hyper)proliferative diseases
AU2010363329A1 (en) 2010-11-07 2013-05-09 Targegen, Inc. Compositions and methods for treating myelofibrosis
WO2016044445A2 (en) 2014-09-17 2016-03-24 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
EP4108659A1 (en) 2016-06-07 2022-12-28 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
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CN111333543B (zh) * 2020-04-17 2022-09-16 武汉工程大学 一种利匹韦林中间体的合成方法
CN115745848A (zh) * 2022-12-07 2023-03-07 上海优合生物科技有限公司 一种氨基胍的加工合成工艺

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Also Published As

Publication number Publication date
CN102503903A (zh) 2012-06-20
KR20050105190A (ko) 2005-11-03
JP2006516983A (ja) 2006-07-13
HRP20050690A2 (en) 2006-08-31
AP2005003365A0 (en) 2005-09-30
AU2004213173B2 (en) 2010-07-29
PL378107A1 (pl) 2006-03-06
EP1597242B1 (en) 2008-07-23
MXPA05008368A (es) 2005-11-04
JP4783725B2 (ja) 2011-09-28
PL232814B1 (pl) 2019-07-31
ZA200506254B (en) 2008-02-27
CA2513123A1 (en) 2004-09-02
CA2513123C (en) 2013-04-23
BRPI0407306A (pt) 2006-02-21
AU2004213173A1 (en) 2004-09-02
EA200501268A1 (ru) 2006-02-24
WO2004074266A1 (en) 2004-09-02
EA010379B1 (ru) 2008-08-29
EP1597242A1 (en) 2005-11-23
ES2311146T3 (es) 2009-02-01
ATE402152T1 (de) 2008-08-15
US20070037811A1 (en) 2007-02-15
IL170120A (en) 2013-04-30
DE602004015254D1 (de) 2008-09-04
US7585861B2 (en) 2009-09-08
CN1747941A (zh) 2006-03-15
WO2004074266A8 (en) 2004-11-11

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