JP2007516205A5 - - Google Patents
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- Publication number
- JP2007516205A5 JP2007516205A5 JP2006518663A JP2006518663A JP2007516205A5 JP 2007516205 A5 JP2007516205 A5 JP 2007516205A5 JP 2006518663 A JP2006518663 A JP 2006518663A JP 2006518663 A JP2006518663 A JP 2006518663A JP 2007516205 A5 JP2007516205 A5 JP 2007516205A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- heteroaryl
- formula
- hydrogen
- halogen
- 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.)
- Granted
Links
- 125000001072 heteroaryl group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000004076 pyridyl group Chemical group 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 208000030507 AIDS Diseases 0.000 claims 5
- -1 azabenzofuryl Chemical group 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 208000031886 HIV Infections Diseases 0.000 claims 2
- 208000037357 HIV infectious disease Diseases 0.000 claims 2
- 229960005475 antiinfective agent Drugs 0.000 claims 2
- 239000003443 antiviral agent Substances 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 2
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 229940126154 HIV entry inhibitor Drugs 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 230000002924 anti-infective effect Effects 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002519 immonomodulatory effect Effects 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- XSDLDLIXLLMXDY-UHFFFAOYSA-N n-methoxyhydroxylamine Chemical compound CONO XSDLDLIXLLMXDY-UHFFFAOYSA-N 0.000 claims 1
- 125000004593 naphthyridinyl group Chemical group N1=C(C=CC2=CC=CN=C12)* 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48422403P | 2003-07-01 | 2003-07-01 | |
| US49328303P | 2003-08-07 | 2003-08-07 | |
| US54197004P | 2004-02-05 | 2004-02-05 | |
| PCT/US2004/019890 WO2005004801A2 (en) | 2003-07-01 | 2004-06-22 | Indole, azaindole and related heterocyclic n-substituted piperazine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007516205A JP2007516205A (ja) | 2007-06-21 |
| JP2007516205A5 true JP2007516205A5 (enExample) | 2007-10-18 |
| JP4584923B2 JP4584923B2 (ja) | 2010-11-24 |
Family
ID=34069101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006518663A Expired - Fee Related JP4584923B2 (ja) | 2003-07-01 | 2004-06-22 | インドール、アザインドール、および関連するヘテロ環状ｎ−置換ピペラジン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US20050075364A1 (enExample) |
| EP (1) | EP1638568B1 (enExample) |
| JP (1) | JP4584923B2 (enExample) |
| AT (1) | ATE517625T1 (enExample) |
| IS (1) | IS2881B (enExample) |
| NO (1) | NO332402B1 (enExample) |
| WO (1) | WO2005004801A2 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050075364A1 (en) * | 2003-07-01 | 2005-04-07 | Kap-Sun Yeung | Indole, azaindole and related heterocyclic N-substituted piperazine derivatives |
| MXPA06005686A (es) | 2003-11-20 | 2006-08-17 | Janssen Pharmaceutica Nv | 2-quinolinonas y 2-quinoxalinonas 7-fenilaquilo sustituidas como inhibidores de la poli(adp-ribosa)polimerasa. |
| KR101118582B1 (ko) | 2003-11-20 | 2012-02-27 | 얀센 파마슈티카 엔.브이. | 폴리(ａｄｐ-리보스)폴리머라제 저해제로서의 6-알케닐 및6-페닐알킬 치환된 2-퀴놀리논 및 2-퀴녹살리논 |
| US20050124623A1 (en) * | 2003-11-26 | 2005-06-09 | Bender John A. | Diazaindole-dicarbonyl-piperazinyl antiviral agents |
| EA012837B1 (ru) | 2004-06-30 | 2009-12-30 | Янссен Фармацевтика Н.В. | Производные хиназолинона в качестве ингибиторов parp |
| ES2415771T3 (es) | 2004-06-30 | 2013-07-26 | Janssen Pharmaceutica N.V. | Derivados de quinazolina como inhibidores de PARP |
| CN1980674B (zh) * | 2004-06-30 | 2011-05-25 | 詹森药业有限公司 | 作为parp抑制剂的2,3-二氮杂萘衍生物 |
| US20060100209A1 (en) * | 2004-11-09 | 2006-05-11 | Chong-Hui Gu | Formulations of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione |
| US20060100432A1 (en) * | 2004-11-09 | 2006-05-11 | Matiskella John D | Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione |
| DE102005027567A1 (de) | 2005-06-14 | 2006-12-21 | Basf Ag | Verfahren zum Passivieren von metallischen Oberflächen mit Säuregruppen aufweisenden Polymeren |
| US7396830B2 (en) * | 2005-10-04 | 2008-07-08 | Bristol-Myers Squibb Company | Piperazine amidines as antiviral agents |
| US7851476B2 (en) * | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
| US20070259879A1 (en) * | 2006-03-06 | 2007-11-08 | Trimeris, Inc. | Piperazine and piperidine biaryl derivatives |
| US7807671B2 (en) * | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
| CN101432278B (zh) * | 2006-04-25 | 2012-11-28 | 布里斯托尔-迈尔斯斯奎布公司 | 作为抗病毒剂的二酮基哌嗪和哌啶衍生物 |
| US7504399B2 (en) * | 2006-06-08 | 2009-03-17 | Bristol-Meyers Squibb Company | Piperazine enamines as antiviral agents |
| ATE542799T1 (de) | 2007-03-08 | 2012-02-15 | Janssen Pharmaceutica Nv | Chinolinonderivate als parp und tank-inhibitoren |
| EP2215075B1 (en) | 2007-10-26 | 2013-12-11 | Janssen Pharmaceutica, N.V. | Quinolinone derivatives as parp inhibitors |
| EP2271626B1 (en) | 2008-03-27 | 2014-11-26 | Janssen Pharmaceutica, N.V. | Tetrahydrophenanthridinones and tetrahydrocyclopentaquinolinones as parp and tubulin polymerization inhibitors |
| EP2260026B1 (en) | 2008-03-27 | 2011-06-22 | Janssen Pharmaceutica, N.V. | Quinazolinone derivatives as tubulin polymerization inhibitors |
| CN102076686B (zh) * | 2008-06-25 | 2013-03-06 | 百时美施贵宝公司 | 作为hiv附着抑制剂的二酮哌啶衍生物 |
| WO2009158394A1 (en) * | 2008-06-25 | 2009-12-30 | Bristol-Myers Squibb Company | Diketo azolopiperidines and azolopiperazines as anti-hiv agents |
| EP2895475B1 (en) * | 2012-08-09 | 2016-11-09 | VIIV Healthcare UK (No.5) Limited | Tricyclic amidine derivatives as hiv attachment inhibitors |
| EP2978762A1 (en) * | 2013-03-27 | 2016-02-03 | Bristol-Myers Squibb Company | Piperazine and homopiperazine derivatives as hiv attachment inhibitors |
| BG111544A (bg) | 2013-07-29 | 2015-01-30 | Николай Цветков | Субституирани бензамидни производни като in vitro mao-b инхибитори |
| CN107400130A (zh) * | 2017-08-22 | 2017-11-28 | 长沙深橙生物科技有限公司 | 一种咪唑并吡啶衍生物的制备方法 |
| US10111873B1 (en) | 2018-01-17 | 2018-10-30 | King Saud University | Dihydropyrimidinone derivatives |
| CN114478367B (zh) * | 2021-12-28 | 2025-01-17 | 乐威医药（江苏）股份有限公司 | 一种2,5-二氧代吡啶衍生物的制备方法 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB944443A (enExample) * | 1959-09-25 | 1900-01-01 | ||
| ES2093090T3 (es) * | 1989-12-28 | 1996-12-16 | Upjohn Co | Compuestos sustituidos diaromaticos anti-sida. |
| US5023265A (en) * | 1990-06-01 | 1991-06-11 | Schering Corporation | Substituted 1-H-pyrrolopyridine-3-carboxamides |
| DK0594702T3 (da) | 1991-07-03 | 1997-07-21 | Upjohn Co | Substituerede indoler som midler mod AIDS |
| WO1993005020A1 (en) | 1991-09-06 | 1993-03-18 | Merck & Co., Inc. | Indoles as inhibitors of hiv reverse transcriptase |
| US5124327A (en) * | 1991-09-06 | 1992-06-23 | Merck & Co., Inc. | HIV reverse transcriptase |
| RU2124511C1 (ru) * | 1993-05-14 | 1999-01-10 | Фармасьютикал Ко., Лтд | Производные пиперазина |
| IT1265057B1 (it) | 1993-08-05 | 1996-10-28 | Dompe Spa | Tropil 7-azaindolil-3-carbossiamidi |
| US5424329A (en) * | 1993-08-18 | 1995-06-13 | Warner-Lambert Company | Indole-2-carboxamides as inhibitors of cell adhesion |
| GB9420521D0 (en) | 1994-10-12 | 1994-11-30 | Smithkline Beecham Plc | Novel compounds |
| TW406075B (en) * | 1994-12-13 | 2000-09-21 | Upjohn Co | Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds |
| DE19636150A1 (de) * | 1996-09-06 | 1998-03-12 | Asta Medica Ag | N-substituierte Indol-3-glyoxylamide mit antiasthmatischer, antiallergischer und immunsuppressiver/immunmodulierender Wirkung |
| DE19814838C2 (de) | 1998-04-02 | 2001-01-18 | Asta Medica Ag | Indolyl-3-glyoxylsäure-Derivate mit Antitumorwirkung |
| US6469006B1 (en) * | 1999-06-15 | 2002-10-22 | Bristol-Myers Squibb Company | Antiviral indoleoxoacetyl piperazine derivatives |
| US6476034B2 (en) * | 2000-02-22 | 2002-11-05 | Bristol-Myers Squibb Company | Antiviral azaindole derivatives |
| US20020061892A1 (en) * | 2000-02-22 | 2002-05-23 | Tao Wang | Antiviral azaindole derivatives |
| DE60113543T2 (de) * | 2000-07-10 | 2006-07-13 | Bristol-Myers Squibb Co. | Zusammensetzung und antivirale wirkung von substituierten indol-oxo-aceto-piperidin-derivaten |
| US6573262B2 (en) * | 2000-07-10 | 2003-06-03 | Bristol-Myers Sqibb Company | Composition and antiviral activity of substituted indoleoxoacetic piperazine derivatives |
| US20030207910A1 (en) | 2001-02-02 | 2003-11-06 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| KR20030079979A (ko) * | 2001-02-02 | 2003-10-10 | 브리스톨-마이어스스퀴브컴파니 | 치환된 아자인돌옥소아세틱 피페라진 유도체의 조성물 및항바이러스 활성 |
| US6825201B2 (en) * | 2001-04-25 | 2004-11-30 | Bristol-Myers Squibb Company | Indole, azaindole and related heterocyclic amidopiperazine derivatives |
| US7037913B2 (en) | 2002-05-01 | 2006-05-02 | Bristol-Myers Squibb Company | Bicyclo 4.4.0 antiviral derivatives |
| US20040063744A1 (en) * | 2002-05-28 | 2004-04-01 | Tao Wang | Indole, azaindole and related heterocyclic 4-alkenyl piperidine amides |
| US6900206B2 (en) | 2002-06-20 | 2005-05-31 | Bristol-Myers Squibb Company | Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives |
| US20040063746A1 (en) | 2002-07-25 | 2004-04-01 | Alicia Regueiro-Ren | Indole, azaindole and related heterocyclic ureido and thioureido piperazine derivatives |
| US20050075364A1 (en) * | 2003-07-01 | 2005-04-07 | Kap-Sun Yeung | Indole, azaindole and related heterocyclic N-substituted piperazine derivatives |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| US7807671B2 (en) * | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
-
2004
- 2004-06-18 US US10/871,931 patent/US20050075364A1/en not_active Abandoned
- 2004-06-22 AT AT04785827T patent/ATE517625T1/de not_active IP Right Cessation
- 2004-06-22 WO PCT/US2004/019890 patent/WO2005004801A2/en not_active Ceased
- 2004-06-22 EP EP04785827A patent/EP1638568B1/en not_active Expired - Lifetime
- 2004-06-22 JP JP2006518663A patent/JP4584923B2/ja not_active Expired - Fee Related
-
2005
- 2005-01-05 US US11/029,673 patent/US20050261296A1/en not_active Abandoned
- 2005-12-30 IS IS8215A patent/IS2881B/is unknown
-
2006
- 2006-01-05 NO NO20060082A patent/NO332402B1/no not_active IP Right Cessation
-
2008
- 2008-02-08 US US12/028,189 patent/US8039486B2/en not_active Expired - Fee Related