BR0315405A - Compostos inibidores da integrase tricìclica pré-organizados - Google Patents

Compostos inibidores da integrase tricìclica pré-organizados

Info

Publication number
BR0315405A
BR0315405A BR0315405-0A BR0315405A BR0315405A BR 0315405 A BR0315405 A BR 0315405A BR 0315405 A BR0315405 A BR 0315405A BR 0315405 A BR0315405 A BR 0315405A
Authority
BR
Brazil
Prior art keywords
organized
tricyclically
inhibitor compounds
integrase inhibitor
aryl
Prior art date
Application number
BR0315405-0A
Other languages
English (en)
Inventor
James M Chen
Xiaowu Chen
Maria Fardis
Haolun Jin
Choung U Kim
Laura N Schacherer
Original Assignee
Gilead Sciences 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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of BR0315405A publication Critical patent/BR0315405A/pt

Links

Classifications

    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—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 two 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/404—2,5-Pyrrolidine-diones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. succinimide
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems

Abstract

"COMPOSTOS INIBIDORES DA INTEGRASE TRICìCLICA PRé-ORGANIZADOS". São apresentados compostos tricíclicos de acordo com a estrutura abaixo, seus Intermediários protegidos, e métodos para a inibição da HIV integrase. Fórmula (I). A^ 1^ e A^ 2^ são porções que formam um anel de cinco, seis ou sete membros. L é uma ligação ou um ligante que se conecta a um átomo do anel de Ar a N. X é O, S ou nitrogênio substituído. Ar é arila ou heteroarila. Q é N, ^ +^NR ou CR^ 4^. Os carbonos de arila podem ser independentemente substituídos com substituintes diferentes de hidrogênio. Os compostos podem incluir porções de pró-droga covalentemente fixados em qualquer sítio.
BR0315405-0A 2002-10-16 2003-10-16 Compostos inibidores da integrase tricìclica pré-organizados BR0315405A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41896302P 2002-10-16 2002-10-16
US47878303P 2003-06-16 2003-06-16
PCT/US2003/032666 WO2004035576A2 (en) 2002-10-16 2003-10-16 Pre-organized tricyclic integrase inhibitor compounds

Publications (1)

Publication Number Publication Date
BR0315405A true BR0315405A (pt) 2005-08-09

Family

ID=32110203

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0315405-0A BR0315405A (pt) 2002-10-16 2003-10-16 Compostos inibidores da integrase tricìclica pré-organizados

Country Status (19)

Country Link
US (3) US20040157804A1 (pt)
EP (1) EP1558613A2 (pt)
JP (1) JP2006514099A (pt)
KR (1) KR20050087787A (pt)
CN (1) CN100374438C (pt)
AP (1) AP1858A (pt)
AU (2) AU2003301439A1 (pt)
BR (1) BR0315405A (pt)
CA (1) CA2501881A1 (pt)
EA (1) EA011399B1 (pt)
HR (1) HRP20050431A2 (pt)
IS (1) IS7845A (pt)
MX (1) MXPA05003950A (pt)
NO (1) NO20052378L (pt)
NZ (1) NZ539264A (pt)
OA (1) OA13079A (pt)
PL (1) PL377966A1 (pt)
UA (1) UA79830C2 (pt)
WO (2) WO2004035577A2 (pt)

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2369746A1 (en) * 1999-05-19 2000-11-30 Neurosearch A/S Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders
KR20060006047A (ko) * 2003-04-28 2006-01-18 티보텍 파마슈티칼즈 리미티드 Ｈｉｖ 인테그레이즈 저해제
EP1664046B1 (en) * 2003-09-19 2009-06-17 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
JP4804361B2 (ja) * 2003-12-08 2011-11-02 ザ リサーチ ファウンデイション オブ ステイト ユニバーシティー オブ ニューヨーク センサー利用のための、部位選択的にタグ付および鋳造された分子インプリントポリマー
EP1694686A1 (en) 2003-12-19 2006-08-30 Takeda San Diego, Inc. Kinase inhibitors
AU2005205341B2 (en) * 2004-01-07 2009-11-19 The Research Foundation Of State University Of New York Protein imprinted polymers with integrated emission sites
ES2315922T3 (es) * 2004-04-14 2009-04-01 Gilead Sciences, Inc. Analogos de fosfonato de compuestos inhibidores de la integrasa del vih.
US7538112B2 (en) * 2004-05-07 2009-05-26 Merck & Co., Inc. HIV integrase inhibitors
WO2005120516A2 (en) * 2004-06-09 2005-12-22 Merck & Co., Inc. Hiv integrase inhibitors
US7745459B2 (en) 2004-09-21 2010-06-29 Japan Tobacco Inc. Quinolizinone compound and use thereof as HIV integrase inhibitor
DE602005023333D1 (de) 2004-10-15 2010-10-14 Takeda Pharmaceutical Kinaseinhibitoren
TW200716632A (en) * 2005-05-16 2007-05-01 Gilead Sciences Inc Integrase inhibitor compounds
EP1885722B1 (en) 2005-05-19 2011-11-16 Merck Canada Inc. Quinoline derivatives as ep4 antagonists
AU2006272521A1 (en) * 2005-07-27 2007-02-01 Gilead Sciences, Inc. Antiviral phosphonate conjugates for inhibition of HIV
WO2007019130A2 (en) * 2005-08-04 2007-02-15 Smithkline Beecham Corporation Hiv integrase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP1973908A2 (en) * 2005-12-21 2008-10-01 Gilead Sciences, Inc. Processes and intermediates useful for preparing integrase inhibitor compounds
SG170795A1 (en) * 2005-12-30 2011-05-30 Gilead Sciences Inc Methods for improving the pharmacokinetics of hiv integrase inhibitors
US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
JP2009537546A (ja) * 2006-05-16 2009-10-29 ギリアード サイエンシーズ， インコーポレイテッド インテグラーゼ阻害剤
US20100120717A1 (en) 2006-10-09 2010-05-13 Brown Jason W Kinase inhibitors
US20090291921A1 (en) * 2007-11-20 2009-11-26 Gilead Sciences, Inc. Integrase inhibitors
WO2009094190A2 (en) 2008-01-25 2009-07-30 Chimerix, Inc. Methods of treating viral infections
KR101700267B1 (ko) 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
CA2732572A1 (en) * 2008-07-28 2010-02-04 Polymedix, Inc. Anti-malarial compounds
ES2641765T3 (es) 2008-12-11 2017-11-13 Shionogi & Co., Ltd. Síntesis de inhibidores de integrasa de VIH carbamoilpiridona y productos intermedios
KR101682058B1 (ko) 2008-12-11 2016-12-02 비이브 헬쓰케어 컴퍼니 카르바모일피리돈 ｈｉｖ 인테그라제 억제제를 위한 제조방법 및 중간체
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
EP2270021A1 (en) * 2009-06-18 2011-01-05 Centre National de la Recherche Scientifique Phosphonates synthons for the synthesis of phosphonates derivatives showing better bioavailability
WO2011011483A1 (en) * 2009-07-22 2011-01-27 Glaxosmithkline Llc Chemical compounds
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
JP5745869B2 (ja) * 2010-01-22 2015-07-08 富山化学工業株式会社 アルアルキル基を有する複素環化合物
HUE032860T2 (en) 2010-02-12 2017-11-28 Chimerix Inc A method for treating a virus infection
TWI582097B (zh) 2010-03-23 2017-05-11 Ｖｉｉｖ醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
TWI503323B (zh) 2010-03-29 2015-10-11 Oncotherapy Science Inc 三環化合物以及含此化合物之ｐｂｋ抑制劑
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
CN104185420B (zh) 2011-11-30 2017-06-09 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
KR101365849B1 (ko) * 2012-03-28 2014-02-24 경동제약 주식회사 솔리페나신 또는 그의 염의 제조방법 및 이에 사용되는 신규 중간체
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
US10260089B2 (en) 2012-10-29 2019-04-16 The Research Foundation Of The State University Of New York Compositions and methods for recognition of RNA using triple helical peptide nucleic acids
EP3939985A1 (en) 2014-12-26 2022-01-19 Emory University Pharmaceutical compositions comprising n4-hydroxycytidine derivatives for the treatment or prevention of influenza or coronavirus infections
JP6628805B2 (ja) 2015-02-03 2020-01-15 ファイザー・インク 新規シクロプロパベンゾフラニルピリドピラジンジオン
CN104803905B (zh) * 2015-04-17 2017-10-10 复旦大学 一种合成异吲哚啉‑1‑酮衍生物的方法
WO2017133517A1 (zh) * 2016-02-03 2017-08-10 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN109305989B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酰胺衍生物及制备方法和用途
CN109305990B (zh) * 2017-07-28 2021-02-26 四川海思科制药有限公司 一种磷酸衍生物及制备方法和用途
RU2020116571A (ru) 2017-12-07 2021-11-22 Эмори Юниверсити N4-гидроксицитидин и производные и связанные с этим противовирусные применения

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH385846A (de) 1960-03-31 1964-12-31 Geigy Ag J R Verfahren zur Herstellung von neuen 7-Acyl-8-hydroxy-chinolinen und ihre Verwendung als Fungizide und Bakterizide im Pflanzen- und Materialschutz
US4816570A (en) 1982-11-30 1989-03-28 The Board Of Regents Of The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
US4968788A (en) 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
WO1991019721A1 (en) 1990-06-13 1991-12-26 Arnold Glazier Phosphorous produgs
DE10399025I2 (de) 1990-09-14 2007-11-08 Acad Of Science Czech Republic Wirkstoffvorläufer von Phosphonaten
DK0498722T3 (da) 1991-02-07 1998-03-09 Roussel Uclaf Nye bicycliske nitrogenforbindelser substitueret med en benzylgruppe, fremgangsmåde til deres fremstilling, de opnåede nye intermediærer, deres anvendelse som lægemidler og de pharmaceutiske præparater som de indgår i
EP0520573A1 (en) 1991-06-27 1992-12-30 Glaxo Inc. Cyclic imide derivatives
US5639881A (en) * 1991-11-08 1997-06-17 Arizona Board Of Regents Acting On Behalf Of Arizona State University Synthesis and elucidation of pyrimido (4,5-Q) quinazoline derivatives
TW304945B (pt) 1992-06-27 1997-05-11 Hoechst Ag
US5798340A (en) 1993-09-17 1998-08-25 Gilead Sciences, Inc. Nucleotide analogs
US5538988A (en) 1994-04-26 1996-07-23 Martinez; Gregory R. Benzocycloalkylazolethione derivatives
US5854275A (en) 1996-05-16 1998-12-29 Pfizer Inc. Cyclic imide derivatives
WO1998011073A1 (en) 1996-09-10 1998-03-19 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
US6329375B1 (en) * 1997-08-05 2001-12-11 Sugen, Inc. Tricyclic quinoxaline derivatives as protein tyrosine kinase inhibitors
US6312662B1 (en) 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
WO1999062520A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
JP2002516858A (ja) 1998-06-03 2002-06-11 メルク エンド カムパニー インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬
KR20010072598A (ko) * 1998-06-10 2001-07-31 리처드 피. 버군 쥬니어 아세틸콜린 증강제
US6187907B1 (en) 1998-08-31 2001-02-13 James Chen Triple helix coil template having a biologically active ligand
WO2000036132A1 (en) 1998-12-14 2000-06-22 Merck & Co., Inc. Hiv integrase inhibitors
NZ512184A (en) 1998-12-25 2003-08-29 Shionogi & Co Aromatic heterocycle compounds having HIV integrase inhibiting activities
WO2000075122A1 (fr) 1999-06-02 2000-12-14 Shionogi & Co., Ltd. Nouveau procede de preparation de derives de propenone a substitution
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
US6245806B1 (en) 1999-08-03 2001-06-12 Merck & Co., Inc. HIV integrase inhibitors
WO2001027309A1 (en) 1999-10-13 2001-04-19 Merck & Co., Inc. Hiv integrase inhibitors
CA2425067A1 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
DE60128936T2 (de) * 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
SK4322003A3 (en) * 2000-10-12 2003-09-11 Merck & Co Inc Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
JP2004517860A (ja) 2000-10-12 2004-06-17 メルク　エンド　カムパニー　インコーポレーテッド Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
WO2002030970A2 (en) * 2000-10-13 2002-04-18 Bayer Aktiengesellschaft Human histone deacetylase gene
US6518767B1 (en) * 2000-10-19 2003-02-11 Schweitzer Engineering Laboratories, Inc. Line differential protection system for a power transmission line
ES2315922T3 (es) * 2004-04-14 2009-04-01 Gilead Sciences, Inc. Analogos de fosfonato de compuestos inhibidores de la integrasa del vih.

Also Published As

Publication number Publication date
NZ539264A (en) 2007-08-31
HRP20050431A2 (en) 2005-10-31
US20040157804A1 (en) 2004-08-12
US20040167124A1 (en) 2004-08-26
EA200500660A1 (ru) 2005-10-27
EA011399B1 (ru) 2009-02-27
AP1858A (en) 2008-06-30
PL377966A1 (pl) 2006-02-20
AU2003301439A1 (en) 2004-05-04
WO2004035576A3 (en) 2004-06-24
MXPA05003950A (es) 2005-06-17
JP2006514099A (ja) 2006-04-27
EP1558613A2 (en) 2005-08-03
WO2004035577A2 (en) 2004-04-29
NO20052378D0 (no) 2005-05-13
KR20050087787A (ko) 2005-08-31
IS7845A (is) 2005-05-13
CN1726212A (zh) 2006-01-25
AU2003301306A1 (en) 2004-05-04
WO2004035577A3 (en) 2004-07-29
OA13079A (en) 2006-11-10
AU2003301439A8 (en) 2004-05-04
UA79830C2 (en) 2007-07-25
CA2501881A1 (en) 2004-04-29
NO20052378L (no) 2005-07-18
US20090029939A1 (en) 2009-01-29
CN100374438C (zh) 2008-03-12
US7253180B2 (en) 2007-08-07
WO2004035576A2 (en) 2004-04-29
AP2005003279A0 (en) 2005-06-30

Similar Documents

Publication Publication Date Title
BR0315405A (pt) Compostos inibidores da integrase tricìclica pré-organizados
IL161559A0 (en) Dibenzylamine derivatives and pharmaceutical compositions containing the same
UA83243C2 (ru) Соединения, которые ингибируют натриезависимый переносчик глюкозы
TW200407309A (en) 1,2-Azole derivatives
MX2007005694A (es) Nuevos derivados de betulina, preparacion y uso de los mismos.
TW200602319A (en) Indole derivative and use thereof
DE602004008098D1 (de) Substituierte 2h-ä1,2,4ütriazoloä4,3-aüpyrazine als gsk-3-inhibitoren
ATE253545T1 (de) Biarylessigsäure-derivate und ihre verwendung als cox-2 inhibitoren
TW200612920A (en) Novel imidazolidine derivatives
HUP0402376A2 (hu) Imidazol-4-karboxamid-származékok, előállításuk és az ezeket tartalmazó, elhízás kezelésére alkalmas gyógyszerkészítmények
EA200870117A1 (ru) Азаиндоловые ингибиторы аурора-киназ
MY149180A (en) Uracil compound having inhibitor activity on human deoxyuridine triphosphatase or salt thereof
TW200612958A (en) Substituted imidazole derivatives
TW200621759A (en) Novel aminopyridine derivatives having aurora A selective inhibitory action
TW200720249A (en) Pyrrolidine compound
UA88329C2 (en) Dna-pk inhibitors
EP1500648A4 (en) NEW PIPERIDINE DERIVATIVES
ATE194982T1 (de) Benzoxazepin-derivate als cholinesterase- inhibitoren
MX2022003656A (es) Compuestos farmaceuticos.
NO20053302D0 (no) Imidazolderivater med affinitet for alfa 2-reseptoraktivitet.
EP1496059A4 (en) CONDENSED BICYCLIC PYRIMIDINE DERIVATIVES
MX2008002753A (es) Derivados de piridazinona utilizados para el tratamiento de dolor.

Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2160 DE 29/05/2012.