DK1529032T3 - Fremgangsmåder til fremstilling af 4-4-4-(2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)aminobenzonitrill - Google Patents
Fremgangsmåder til fremstilling af 4-4-4-(2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)aminobenzonitrillInfo
- Publication number
- DK1529032T3 DK1529032T3 DK03787813.9T DK03787813T DK1529032T3 DK 1529032 T3 DK1529032 T3 DK 1529032T3 DK 03787813 T DK03787813 T DK 03787813T DK 1529032 T3 DK1529032 T3 DK 1529032T3
- Authority
- DK
- Denmark
- Prior art keywords
- cyanoethenyl
- aminobenzonitrile
- dimethylphenyl
- pyrimidinyl
- amino
- Prior art date
Links
- HLCPWBZNUKCSBN-UHFFFAOYSA-N 2-aminobenzonitrile Chemical compound NC1=CC=CC=C1C#N HLCPWBZNUKCSBN-UHFFFAOYSA-N 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/20—Preparation of carboxylic acid nitriles by dehydration of carboxylic acid amides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02078306 | 2002-08-09 | ||
| PCT/EP2003/050366 WO2004016581A1 (en) | 2002-08-09 | 2003-08-07 | Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK1529032T3 true DK1529032T3 (da) | 2013-07-08 |
Family
ID=31725448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK03787813.9T DK1529032T3 (da) | 2002-08-09 | 2003-08-07 | Fremgangsmåder til fremstilling af 4-4-4-(2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)aminobenzonitrill |
Country Status (27)
| Country | Link |
|---|---|
| US (3) | US7399856B2 (da) |
| EP (1) | EP1529032B1 (da) |
| JP (1) | JP4822707B2 (da) |
| KR (2) | KR101140785B1 (da) |
| CN (4) | CN102225902B (da) |
| AR (1) | AR040964A1 (da) |
| AU (1) | AU2003266413B2 (da) |
| BR (1) | BR0313545B1 (da) |
| CA (2) | CA2686429C (da) |
| CL (1) | CL2010000284A1 (da) |
| CY (1) | CY1114428T1 (da) |
| DK (1) | DK1529032T3 (da) |
| EA (1) | EA007953B1 (da) |
| ES (1) | ES2422196T3 (da) |
| HK (4) | HK1129671A1 (da) |
| HR (1) | HRP20050104B1 (da) |
| IL (1) | IL166710A (da) |
| IS (1) | IS2980B (da) |
| MX (1) | MXPA05001541A (da) |
| MY (1) | MY144894A (da) |
| NO (1) | NO330013B1 (da) |
| NZ (1) | NZ538611A (da) |
| PL (1) | PL208533B1 (da) |
| PT (1) | PT1529032E (da) |
| SI (1) | SI1529032T1 (da) |
| TW (1) | TWI314146B (da) |
| WO (1) | WO2004016581A1 (da) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7638522B2 (en) | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
| US8101629B2 (en) * | 2001-08-13 | 2012-01-24 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
| MY169670A (en) | 2003-09-03 | 2019-05-08 | Tibotec Pharm Ltd | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| JO3429B1 (ar) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| BR0313545B1 (pt) | 2002-08-09 | 2021-07-27 | Janssen Pharmaceutica Nv | processos para a preparação de 4-[[4-[[4-(2-cianoetenil)-2,6-dimetilfenil]amino]-2-pirimidinil]amino]benzonitrila |
| JP2006508997A (ja) * | 2002-11-28 | 2006-03-16 | シエーリング アクチエンゲゼルシャフト | Ｃｈｋ−、Ｐｄｋ−およびＡｋｔ−阻害性ピリミジン、それらの製造および薬剤としての使用 |
| WO2005123662A1 (en) * | 2004-06-18 | 2005-12-29 | Janssen Pharmaceutica N.V. | Modified heck reaction |
| CN101056673A (zh) * | 2004-09-02 | 2007-10-17 | 詹森药业有限公司 | 4－[[4－[[4－(2－氰基乙烯基)－2,6－二甲基苯基]氨基]－2－嘧啶基]氨基]苄腈的盐酸盐 |
| PL1632232T6 (pl) * | 2004-09-02 | 2022-06-27 | Janssen Pharmaceutica Nv | Sól 4-[[4-[[4-(2-cyjanoetenylo)-2,6-dimetylofenylo]amino]-2-pirymidynylo]amino]benzonitrylu |
| SI1632232T1 (sl) * | 2004-09-02 | 2011-09-30 | Janssen Pharmaceutica Nv | Sol 4((4((4-(2-cianoetenil)-2,6-dimetilfenil)amino)-2-pirimidinil)amino) benzonitrila |
| MX2007002594A (es) * | 2004-09-02 | 2007-04-25 | Janssen Pharmaceutica Nv | Fumarato de 4-((4-((4- (2-cianoetenil)-2, 6-dimetilfenil) amino)-2-pirimidinil) amino) benzonitrilo. |
| AU2005279157B2 (en) * | 2004-09-02 | 2011-07-14 | Janssen Pharmaceutica N.V. | Fumarate of 4-[[4-[[4- (2-cyanoethenyl) -2,6-dimethylphenyl]amino)-2-pyrimidinyl)amino]benzonitrile |
| US7314962B2 (en) * | 2005-04-15 | 2008-01-01 | E. I. Du Pont De Nemours & Co. | Alkylation of aromatic compounds |
| DK1888537T3 (da) * | 2005-05-26 | 2013-12-09 | Janssen R & D Ireland | Fremgangsmåde til fremstilling af 4[(1,6-dihydro-6-oxo-2-pyrimidinyl)amino]benzonitril |
| AR065720A1 (es) | 2007-03-14 | 2009-06-24 | Tibotec Pharm Ltd | Polvos para reconstitucion que comprenden rilpivirina dispersos en ciertos polimeros. uso. proceso. |
| DK2175857T3 (da) * | 2007-07-12 | 2013-12-02 | Janssen R & D Ireland | Krystallinsk form af (e) 4-[[4-[[4-(2-cyanoethenyl)-2.6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitril |
| WO2012125993A1 (en) | 2011-03-17 | 2012-09-20 | Teva Pharmaceutical Industries Ltd. | Solid state forms of rilpivirine base, and rilipivirine salts |
| KR101879468B1 (ko) * | 2011-04-15 | 2018-07-17 | 엠큐어 파마슈티컬즈 리미티드 | 릴피비린 중간체의 제조를 위한 공정 |
| US9126949B2 (en) | 2011-04-25 | 2015-09-08 | Hetero Research Foundation | Process for rilpivirine |
| WO2013038425A1 (en) * | 2011-09-16 | 2013-03-21 | Hetero Research Foundation | Rilpivirine hydrochloride |
| WO2013170421A1 (zh) * | 2012-05-14 | 2013-11-21 | 上海迪赛诺药业有限公司 | 利匹韦林盐酸盐醇化物多晶型物及其制备方法 |
| WO2013179105A1 (en) * | 2012-06-01 | 2013-12-05 | Laurus Labs Private Limited | Improved process for preparation of rilpivirine and pharmaceutically acceptable salts thereof |
| US9139535B2 (en) | 2012-07-12 | 2015-09-22 | Hetero Research Foundation | Process for rilpivirine using novel intermediate |
| CZ201532A3 (cs) | 2015-01-21 | 2015-02-25 | Zentiva, K.S. | Způsob výroby vysoce čistého Rilpivirinu a jeho solí |
| CN106008366A (zh) * | 2016-05-25 | 2016-10-12 | 山东大学 | 一种利匹韦林的制备方法 |
| DK3528791T3 (da) | 2016-10-24 | 2024-01-29 | Janssen Sciences Ireland Unlimited Co | Dispergible sammensætninger |
| WO2020084142A1 (en) | 2018-10-25 | 2020-04-30 | Minakem | Process for the preparation of rilpivirine |
| CN110526873B (zh) * | 2019-08-15 | 2022-09-16 | 复旦大学 | 氰乙烯基取代的苯并二芳基嘧啶类化合物及其制备方法和用途 |
| WO2021104487A1 (en) | 2019-11-29 | 2021-06-03 | Aptorum Therapeutics Limited | Composition including rilpivirine and use thereof for treating tumors or cancer |
| CN112010810B (zh) * | 2020-09-09 | 2024-01-30 | 瑞阳制药股份有限公司 | 一锅法制备高纯度利匹韦林中间体的方法 |
| CN112778214A (zh) * | 2021-01-13 | 2021-05-11 | 安徽贝克联合制药有限公司 | 用于合成利匹韦林的中间体、其合成方法和利匹韦林的合成方法 |
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| US3459731A (en) | 1966-12-16 | 1969-08-05 | Corn Products Co | Cyclodextrin polyethers and their production |
| JPS5490121A (en) | 1977-11-28 | 1979-07-17 | Boettcher Barry | Neutral copper bonded body and antiinflaming agent |
| US5691364A (en) | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| SK67298A3 (en) | 1995-11-23 | 1998-11-04 | Janssen Pharmaceutica Nv | Solid mixtures of cyclodextrins prepared via melt-extrusion |
| GB9705361D0 (en) | 1997-03-14 | 1997-04-30 | Celltech Therapeutics Ltd | Chemical compounds |
| US6982091B2 (en) | 2001-08-29 | 2006-01-03 | Umd, Inc. | Vaginal delivery of chemotherapeutic agents and inhibitors of membrane efflux systems for cancer therapy |
| BRPI9909191B8 (pt) | 1998-03-27 | 2021-07-06 | Janssen Pharmaceutica Nv | derivados de pirimidina inibidores do hiv, seu uso e composição farmacêutica que os compreende |
| SI0945443T1 (en) | 1998-03-27 | 2003-08-31 | Janssen Pharmaceutica N.V. | HIV inhibiting pyrimidine derivatives |
| JP2000035628A (ja) | 1998-07-16 | 2000-02-02 | Konica Corp | ハロゲン化銀写真感光材料 |
| ES2274634T3 (es) | 1998-08-29 | 2007-05-16 | Astrazeneca Ab | Compuestos de pirimidina. |
| NZ511116A (en) * | 1998-11-10 | 2003-08-29 | Janssen Pharmaceutica Nv | HIV replication inhibiting pyrimidines |
| SK12582001A3 (sk) | 1999-03-09 | 2002-02-05 | Pharmacia & Upjohn Company | 4-Oxo-4,7-dihydro-tieno[2,3-b] pyridín-5-karboxamidy ako antivírusové prostriedky, spôsob ich prípravy, medziprodukty a farmaceutická kompozícia |
| MXPA01010292A (es) | 1999-04-15 | 2002-10-23 | Squibb Bristol Myers Co | Inhibidores ciclicos de la proteina tirosina cinasa. |
| GB9914258D0 (en) | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| DE19945982A1 (de) | 1999-09-24 | 2001-03-29 | Knoll Ag | Geschwindigkeitsbestimmte Partikel |
| IL148801A0 (en) | 1999-09-24 | 2002-09-12 | Janssen Pharmaceutica Nv | Antiviral compositions |
| CA2400447C (en) | 2000-02-17 | 2008-04-22 | Amgen Inc. | Kinase inhibitors |
| GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| GB0004888D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
| AU783981C (en) * | 2000-05-08 | 2007-05-03 | Janssen Pharmaceutica N.V. | HIV replication inhibitors |
| US6596729B2 (en) * | 2000-07-20 | 2003-07-22 | Bristol-Myers Squibb Company | Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors |
| PL364658A1 (en) | 2001-03-02 | 2004-12-13 | Smithkline Beecham Corporation | Benzophenones as inhibitors of reverse transcriptase |
| DE60223790D1 (de) | 2001-03-29 | 2008-01-10 | Vertex Pharma | Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase |
| JO3429B1 (ar) * | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | مشتقات برميدينات مثبطة فيروس الايدز |
| MY169670A (en) | 2003-09-03 | 2019-05-08 | Tibotec Pharm Ltd | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| DE60318035T2 (de) | 2002-05-03 | 2008-12-11 | Janssen Pharmaceutica N.V. | Polymermikroemulsionen |
| BR0313545B1 (pt) | 2002-08-09 | 2021-07-27 | Janssen Pharmaceutica Nv | processos para a preparação de 4-[[4-[[4-(2-cianoetenil)-2,6-dimetilfenil]amino]-2-pirimidinil]amino]benzonitrila |
| WO2004050068A1 (en) | 2002-11-29 | 2004-06-17 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
-
2003
- 2003-08-07 BR BRPI0313545A patent/BR0313545B1/pt active IP Right Grant
- 2003-08-07 SI SI200332275T patent/SI1529032T1/sl unknown
- 2003-08-07 CA CA2686429A patent/CA2686429C/en not_active Expired - Lifetime
- 2003-08-07 US US10/523,753 patent/US7399856B2/en not_active Expired - Lifetime
- 2003-08-07 KR KR1020057000881A patent/KR101140785B1/ko active IP Right Grant
- 2003-08-07 MX MXPA05001541A patent/MXPA05001541A/es active IP Right Grant
- 2003-08-07 NZ NZ538611A patent/NZ538611A/en not_active IP Right Cessation
- 2003-08-07 JP JP2004528518A patent/JP4822707B2/ja not_active Expired - Lifetime
- 2003-08-07 KR KR1020107026275A patent/KR101086678B1/ko active IP Right Grant
- 2003-08-07 CN CN2011101114129A patent/CN102225902B/zh not_active Expired - Lifetime
- 2003-08-07 CN CN201210159781.XA patent/CN102702111B/zh not_active Expired - Lifetime
- 2003-08-07 CN CN200910001327XA patent/CN101481356B/zh not_active Expired - Lifetime
- 2003-08-07 EA EA200500325A patent/EA007953B1/ru unknown
- 2003-08-07 CA CA2493794A patent/CA2493794C/en not_active Expired - Lifetime
- 2003-08-07 AU AU2003266413A patent/AU2003266413B2/en not_active Expired
- 2003-08-07 ES ES03787813T patent/ES2422196T3/es not_active Expired - Lifetime
- 2003-08-07 PL PL373679A patent/PL208533B1/pl unknown
- 2003-08-07 DK DK03787813.9T patent/DK1529032T3/da active
- 2003-08-07 CN CNB038192764A patent/CN100554245C/zh not_active Expired - Lifetime
- 2003-08-07 WO PCT/EP2003/050366 patent/WO2004016581A1/en active Application Filing
- 2003-08-07 MY MYPI20032999A patent/MY144894A/en unknown
- 2003-08-07 PT PT37878139T patent/PT1529032E/pt unknown
- 2003-08-07 EP EP03787813.9A patent/EP1529032B1/en not_active Expired - Lifetime
- 2003-08-08 AR ARP030102882A patent/AR040964A1/es active IP Right Grant
- 2003-08-08 TW TW092121743A patent/TWI314146B/zh not_active IP Right Cessation
-
2004
- 2004-12-29 IS IS7621A patent/IS2980B/is unknown
-
2005
- 2005-02-01 NO NO20050524A patent/NO330013B1/no not_active IP Right Cessation
- 2005-02-01 HR HRP20050104AA patent/HRP20050104B1/hr not_active IP Right Cessation
- 2005-02-07 IL IL166710A patent/IL166710A/en active Protection Beyond IP Right Term
-
2006
- 2006-02-09 HK HK09108307.2A patent/HK1129671A1/xx not_active IP Right Cessation
- 2006-02-09 HK HK06101734.3A patent/HK1081527A1/xx not_active IP Right Cessation
-
2007
- 2007-04-23 US US11/738,688 patent/US7563922B2/en active Active
-
2008
- 2008-02-14 US US12/031,011 patent/US7705148B2/en active Active
-
2010
- 2010-03-29 CL CL2010000284A patent/CL2010000284A1/es unknown
-
2012
- 2012-02-23 HK HK12101815.7A patent/HK1161869A1/xx not_active IP Right Cessation
-
2013
- 2013-02-25 HK HK13102335.5A patent/HK1174922A1/xx not_active IP Right Cessation
- 2013-07-24 CY CY20131100631T patent/CY1114428T1/el unknown
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