DE60124577T2 - Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer - Google Patents

Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer Download PDF

Info

Publication number
DE60124577T2
DE60124577T2 DE60124577T DE60124577T DE60124577T2 DE 60124577 T2 DE60124577 T2 DE 60124577T2 DE 60124577 T DE60124577 T DE 60124577T DE 60124577 T DE60124577 T DE 60124577T DE 60124577 T2 DE60124577 T2 DE 60124577T2
Authority
DE
Germany
Prior art keywords
alkyl
substituted
fluoroalkyl
halogen
independently selected
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
DE60124577T
Other languages
German (de)
English (en)
Other versions
DE60124577D1 (en
Inventor
Neville J. Rahway ANTHONY
Robert P. Rahway GOMEZ
Jennifer J. Rahway BENNETT
Steven D. Rahway YOUNG
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.)
Merck and Co Inc
Original Assignee
Merck and Co 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 Merck and Co Inc filed Critical Merck and Co Inc
Application granted granted Critical
Publication of DE60124577D1 publication Critical patent/DE60124577D1/de
Publication of DE60124577T2 publication Critical patent/DE60124577T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Compression Or Coding Systems Of Tv Signals (AREA)
  • Pyrrole Compounds (AREA)
  • Decoration By Transfer Pictures (AREA)
  • Indole Compounds (AREA)
DE60124577T 2000-10-12 2001-10-09 Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer Expired - Fee Related DE60124577T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23967900P 2000-10-12 2000-10-12
US239679P 2000-10-12
PCT/US2001/042565 WO2002055079A2 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
DE60124577D1 DE60124577D1 (en) 2006-12-28
DE60124577T2 true DE60124577T2 (de) 2007-09-27

Family

ID=22903252

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60124577T Expired - Fee Related DE60124577T2 (de) 2000-10-12 2001-10-09 Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer

Country Status (9)

Country Link
US (1) US6841558B2 (https=)
EP (1) EP1326610B1 (https=)
JP (1) JP2004517860A (https=)
AT (1) ATE345129T1 (https=)
AU (1) AU2002246499B2 (https=)
CA (1) CA2425625A1 (https=)
DE (1) DE60124577T2 (https=)
ES (1) ES2274913T3 (https=)
WO (1) WO2002055079A2 (https=)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3616628B2 (ja) 2001-03-01 2005-02-02 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
ATE355064T1 (de) * 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
ATE409187T1 (de) * 2002-03-15 2008-10-15 Merck & Co Inc N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer
ATE404537T1 (de) 2002-08-13 2008-08-15 Shionogi & Co Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung
ATE404563T1 (de) * 2002-09-11 2008-08-15 Merck & Co Inc 8-hydroxy-1- oxotetrahydropyrrolopyrazinverbindungen, die sich als inhibitoren von hiv-integrase eignen
CA2498111A1 (en) * 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
WO2004035577A2 (en) 2002-10-16 2004-04-29 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
SK2662004A3 (sk) 2002-11-20 2005-06-02 Japan Tobacco, Inc. Zlúčenina s obsahom 4-oxochinolínu a jej použitie ako inhibítora integráz
NZ540729A (en) 2002-12-27 2008-03-28 Angeletti P Ist Richerche Bio Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds useful as HIV integrase inhibitors
AU2004234087A1 (en) * 2003-04-28 2004-11-11 Tibotec Pharmaceuticals Ltd. HIV integrase inhibitors
EP1622615A4 (en) 2003-05-13 2009-02-18 Smithkline Beecham Corp INHIBITORS OF THE INTEGRASE OF NAPHTHYRIDINE
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
CA2537325A1 (en) * 2003-09-19 2005-03-31 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
AU2004285449A1 (en) 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
JP4789144B2 (ja) * 2004-02-04 2011-10-12 塩野義製薬株式会社 Ｈｉｖインテグラーゼ阻害活性を有するナフチリジン誘導体
CN1976915A (zh) 2004-02-11 2007-06-06 史密丝克莱恩比彻姆公司 Hiv整合酶抑制剂
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
US20070161639A1 (en) 2004-03-09 2007-07-12 Philip Jones Hiv integrase inhibitors
CN101014574A (zh) * 2004-03-09 2007-08-08 默克公司 Hiv整合酶抑制剂
JP4625838B2 (ja) * 2004-03-09 2011-02-02 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラーゼ阻害薬
US7538112B2 (en) * 2004-05-07 2009-05-26 Merck & Co., Inc. HIV integrase inhibitors
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
EP1758581A1 (en) 2004-05-21 2007-03-07 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-hiv agents
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
CA2600832C (en) * 2005-03-31 2011-12-13 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
WO2006121831A2 (en) * 2005-05-10 2006-11-16 Merck & Co., Inc. Hiv integrase inhibitors
US7939537B2 (en) * 2005-10-04 2011-05-10 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HIV integrase inhibitors
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
US7902182B2 (en) * 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
ES2531190T3 (es) 2006-03-06 2015-03-11 Japan Tobacco Inc Método para producir un compuesto de 4-oxoquinolina
AU2007254190A1 (en) 2006-05-16 2007-11-29 Gilead Sciences, Inc. Integrase inhibitors
US20100056516A1 (en) * 2006-07-17 2010-03-04 Williams Peter D 1-hydroxy naphthyridine compounds as anti-hiv agents
JP2010504978A (ja) 2006-09-29 2010-02-18 アイデニクス ファーマシューティカルズ，インコーポレーテッド Ｈｉｖ阻害剤としての鏡像異性的に純粋なホスホインドール
WO2008048538A1 (en) * 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
EP1972627A1 (en) * 2007-03-19 2008-09-24 Technische Universität Carolo-Wilhelmina zu Braunschweig Amino-napthyridine derivatives
US8513420B2 (en) * 2007-03-19 2013-08-20 Monika Mazik Amino-naphthyridine derivatives
ES2572631T3 (es) 2008-01-25 2016-06-01 Chimerix, Inc. Métodos de tratamiento de infecciones virales
DE102009038123A1 (de) 2009-08-17 2011-02-24 Aicuris Gmbh & Co. Kg Substituierte (Thiazolyl-carbonyl)imidazolidinone und ihre Verwendung
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US9006218B2 (en) 2010-02-12 2015-04-14 Chimerix Inc. Nucleoside phosphonate salts
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
WO2012102985A1 (en) * 2011-01-24 2012-08-02 Glaxosmithkline Llc Isoquinoline compounds and methods for treating hiv
CN105611927A (zh) 2013-05-16 2016-05-25 美国政府(由卫生和人类服务部的部长所代表) 用于抑制耐药性hiv-1整合酶耐药株的化合物

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5751837B2 (https=) * 1973-04-05 1982-11-04
US4416884A (en) 1978-04-12 1983-11-22 Otsuka Pharmaceutical Co., Ltd. Piperazinylbenzoheterocyclic compounds
FR2632639B1 (fr) 1988-06-09 1990-10-05 Sanofi Sa Derives d'amino-4 carboxy-3 naphtyridines, leur preparation et compositions pharmaceutiques qui les contiennent
IL101860A0 (en) 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
US5681832A (en) 1995-02-17 1997-10-28 The United States Of America As Represented By The Department Of Health And Human Services Aroylaniline compounds, pharmaceutical compositions, and methods of using same to inhibit viral activity
WO1997004775A1 (en) 1995-08-02 1997-02-13 Chiroscience Limited Quinolones and their therapeutic use
US5945431A (en) 1996-03-15 1999-08-31 Biochem Therapeutics Incorporated Cytomegalovirus inhibiting compounds
US6310211B1 (en) * 1996-09-10 2001-10-30 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
WO1998013350A1 (en) 1996-09-25 1998-04-02 Zeneca Limited Qinoline derivatives inhibiting the effect of growth factors such as vegf
DE69828284T2 (de) 1997-06-30 2005-12-08 Nippon Kayaku K.K. Naphthyridinderivate oder salze davon
KR20010023313A (ko) 1997-08-25 2001-03-26 해피 페너 ; 해리 에이치. 페너 2세 Ｇａｂａ 뇌 수용체 리간드로서의 치환된4-옥소-나프티리딘-3-카르복스아미드
US6143760A (en) 1997-08-25 2000-11-07 Neurogen Corporation Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands
GB9720052D0 (en) * 1997-09-19 1997-11-19 Smithkline Beecham Plc Novel compounds
KR20010015639A (ko) 1997-09-30 2001-02-26 스즈키 다다시 술포닐 유도체
PL341364A1 (en) 1997-12-22 2001-04-09 Upjohn Co 4-hydroxyqinoline-3-carboxamides and hydrazides as antiviral agents
US6262055B1 (en) 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6306891B1 (en) 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
US6730682B2 (en) 2000-07-12 2004-05-04 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
GB0017676D0 (en) 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
IL161337A0 (en) 2001-10-26 2004-09-27 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase

Also Published As

Publication number Publication date
WO2002055079A2 (en) 2002-07-18
CA2425625A1 (en) 2002-07-18
DE60124577D1 (en) 2006-12-28
ATE345129T1 (de) 2006-12-15
EP1326610B1 (en) 2006-11-15
US6841558B2 (en) 2005-01-11
WO2002055079A3 (en) 2002-09-06
ES2274913T3 (es) 2007-06-01
AU2002246499B2 (en) 2005-12-22
US20040044207A1 (en) 2004-03-04
JP2004517860A (ja) 2004-06-17
EP1326610A2 (en) 2003-07-16
EP1326610A4 (en) 2004-06-09

Similar Documents

Publication Publication Date Title
DE60124577T2 (de) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
DE60128936T2 (de) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
DE69426422T2 (de) Pyridazino-chinolin verbindungen
DE60021630T2 (de) Tricyclische kondensierte heterocyclische Verbindungen als CRF Antagonisten
EP0944631B1 (de) Neue substituierte pyrazolderivate zur behandlung von herzkreislauferkrankungen
DE69719193T2 (de) Substituierte pyrido- oder pyrimidogruppen enthaltende 6,6- oder 6,7-bicyclische derivate
DE60110749T2 (de) Pyridinderivative als angiogenese- und/oder vegf-rezeptor-tyrosinkinase-inhibitoren
DE60317353T2 (de) Imidazopyrazine als cdk-inhibitoren
DE69736711T2 (de) Substituierte 6,5-heterobicyclische-derivate
EP1339714B1 (de) Neue sulfonamid-substituierte pyrazolopyridinderivate
EP0533058A1 (de) Imidazo-annellierte Iso- und Heterocyclen, Antagonisten als Angiotensin II
DE10232572A1 (de) Neue 2,5-disubstituierte Pyrimidinderivate
EP0528922B1 (de) Neue sulfonylverbindungen
DE60209721T2 (de) Oxazolo- und furopyrimidine und deren verwendung als medikamente gegen tumore
WO2003086407A1 (de) Verwendung von stimulatoren der löslichen guanylatcyclase zur behandlung von glaukom
EP1628976A1 (de) Neue pyridopyrazine und deren verwendung als kinase-inhibitoren
DE60310767T2 (de) PYRAZOL-3,4-d-PYRIMIDINDERIVATE UND IHRE VERWENDUNG BEI DER BEHANDLUNG VON H.PYLORI-INFEKTIONEN
DE60317684T4 (de) SUBSTITUIERTE 2,4-DIHYDROPYRROLOc3,4BÜCHINOLIN-9-ONDERIVATE, DIE SICH ALS PHOSPHODIESTERASEINHIBITOREN EIGNEN
DE10226943A1 (de) Phenylaminopyrimidine und ihre Verwendung
DD216019A5 (de) Verfahren zur herstellung heterocyclisch ankondensierter pyrazolo (3,4-d) pyridin-3-one
DE68913365T2 (de) 4-Amino-3-carboxynaphthyridin-Derivate, ihre Herstellung und pharmazeutische Zusammensetzungen.
DE60026883T2 (de) Methoden und zusammensetzungen zur behandlung von schmerzen
EP1833830B1 (de) Chinolinderivat, dessen verwendung, herstellung und dieses enthaltendes arzneimittel
DE602004010931T2 (de) Für die behandlung von krankheiten wie krebs und atherosclerose geeignete substituierte isochinoline
DE60013326T2 (de) Verbindungen und verfahren zur behandlung von schmerz

Legal Events

Date Code Title Description
8381 Inventor (new situation)

Inventor name: ANTHONY, NEVILLE, J., RAHWAY, NJ 07065-0907, US

Inventor name: GOMEZ, ROBERT, P., RAHWAY, NJ 07065-0907, US

Inventor name: BENNETT, JENNIFER, J., RAHWAY, NJ 07065-0907, US

Inventor name: YOUNG, STEVEN, D., RAHWAY, NJ 07065-0907, US

8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: MERCK & CO., INC., RAHWAY, N.J., US

8339 Ceased/non-payment of the annual fee