JP2008511592A5 - - Google Patents
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- JP2008511592A5 JP2008511592A5 JP2007528886A JP2007528886A JP2008511592A5 JP 2008511592 A5 JP2008511592 A5 JP 2008511592A5 JP 2007528886 A JP2007528886 A JP 2007528886A JP 2007528886 A JP2007528886 A JP 2007528886A JP 2008511592 A5 JP2008511592 A5 JP 2008511592A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- formula
- peg
- compound
- 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
- 239000008194 pharmaceutical composition Substances 0.000 claims 46
- 150000001875 compounds Chemical class 0.000 claims 22
- 239000002245 particle Substances 0.000 claims 13
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 12
- 239000002585 base Substances 0.000 claims 11
- 239000000203 mixture Substances 0.000 claims 11
- 238000004519 manufacturing process Methods 0.000 claims 9
- 239000004480 active ingredient Substances 0.000 claims 8
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 6
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 6
- 229920001213 Polysorbate 20 Polymers 0.000 claims 6
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 6
- 229960001681 croscarmellose sodium Drugs 0.000 claims 6
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 6
- 239000012458 free base Substances 0.000 claims 6
- 229960001021 lactose monohydrate Drugs 0.000 claims 6
- 235000019359 magnesium stearate Nutrition 0.000 claims 6
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 claims 6
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 claims 6
- 229940068977 polysorbate 20 Drugs 0.000 claims 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 5
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 claims 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 4
- 239000000843 powder Substances 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 229940035044 sorbitan monolaurate Drugs 0.000 claims 4
- 239000000080 wetting agent Substances 0.000 claims 4
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 3
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims 3
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 239000002202 Polyethylene glycol Substances 0.000 claims 3
- HVUMOYIDDBPOLL-XWVZOOPGSA-N Sorbitan monostearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O HVUMOYIDDBPOLL-XWVZOOPGSA-N 0.000 claims 3
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 3
- IIRDTKBZINWQAW-UHFFFAOYSA-N hexaethylene glycol Chemical compound OCCOCCOCCOCCOCCOCCO IIRDTKBZINWQAW-UHFFFAOYSA-N 0.000 claims 3
- 229920003125 hypromellose 2910 Polymers 0.000 claims 3
- 229940031672 hypromellose 2910 Drugs 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 3
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 3
- 239000001593 sorbitan monooleate Substances 0.000 claims 3
- 235000011069 sorbitan monooleate Nutrition 0.000 claims 3
- 229940035049 sorbitan monooleate Drugs 0.000 claims 3
- 239000001587 sorbitan monostearate Substances 0.000 claims 3
- 235000011076 sorbitan monostearate Nutrition 0.000 claims 3
- 229940035048 sorbitan monostearate Drugs 0.000 claims 3
- GUBGYTABKSRVRQ-UHFFFAOYSA-N 2-(hydroxymethyl)-6-[4,5,6-trihydroxy-2-(hydroxymethyl)oxan-3-yl]oxyoxane-3,4,5-triol Chemical compound OCC1OC(OC2C(O)C(O)C(O)OC2CO)C(O)C(O)C1O GUBGYTABKSRVRQ-UHFFFAOYSA-N 0.000 claims 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- 238000010521 absorption reaction Methods 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims 2
- VERWQPYQDXWOGT-LVJNJWHOSA-N 4-amino-5-fluoro-1-[(2r,5s)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one;[[(2r)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-(propan-2-yloxycarbonyloxymethoxy)phosphoryl]oxymethyl propan-2-yl carbonate;(e)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VERWQPYQDXWOGT-LVJNJWHOSA-N 0.000 claims 1
- IGUMRIFUXCYFFQ-AATRIKPKSA-N C(\C=C\C(=O)OOC(C)C)(=O)OOC(C)C Chemical compound C(\C=C\C(=O)OOC(C)C)(=O)OOC(C)C IGUMRIFUXCYFFQ-AATRIKPKSA-N 0.000 claims 1
- 238000001157 Fourier transform infrared spectrum Methods 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 229940122313 Nucleoside reverse transcriptase inhibitor Drugs 0.000 claims 1
- NWGKJDSIEKMTRX-AAZCQSIUSA-N Sorbitan monooleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NWGKJDSIEKMTRX-AAZCQSIUSA-N 0.000 claims 1
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 claims 1
- 239000004147 Sorbitan trioleate Substances 0.000 claims 1
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 claims 1
- NCHJGQKLPRTMAO-XWVZOOPGSA-N [(2R)-2-[(2R,3R,4S)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O NCHJGQKLPRTMAO-XWVZOOPGSA-N 0.000 claims 1
- IJCWFDPJFXGQBN-RYNSOKOISA-N [(2R)-2-[(2R,3R,4S)-4-hydroxy-3-octadecanoyloxyoxolan-2-yl]-2-octadecanoyloxyethyl] octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCCCCCCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCCCCCCCCCCCC IJCWFDPJFXGQBN-RYNSOKOISA-N 0.000 claims 1
- LWZFANDGMFTDAV-BURFUSLBSA-N [(2r)-2-[(2r,3r,4s)-3,4-dihydroxyoxolan-2-yl]-2-hydroxyethyl] dodecanoate Chemical compound CCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O LWZFANDGMFTDAV-BURFUSLBSA-N 0.000 claims 1
- RKZXQQPEDGMHBJ-LIGJGSPWSA-N [(2s,3r,4r,5r)-2,3,4,5,6-pentakis[[(z)-octadec-9-enoyl]oxy]hexyl] (z)-octadec-9-enoate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC RKZXQQPEDGMHBJ-LIGJGSPWSA-N 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000314 lubricant Substances 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 239000002773 nucleotide Substances 0.000 claims 1
- 125000003729 nucleotide group Chemical group 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000377 silicon dioxide Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 229950006451 sorbitan laurate Drugs 0.000 claims 1
- 235000011067 sorbitan monolaureate Nutrition 0.000 claims 1
- 235000011071 sorbitan monopalmitate Nutrition 0.000 claims 1
- 239000001570 sorbitan monopalmitate Substances 0.000 claims 1
- 229940031953 sorbitan monopalmitate Drugs 0.000 claims 1
- 229950004959 sorbitan oleate Drugs 0.000 claims 1
- 235000019337 sorbitan trioleate Nutrition 0.000 claims 1
- 229960000391 sorbitan trioleate Drugs 0.000 claims 1
- 239000001589 sorbitan tristearate Substances 0.000 claims 1
- 235000011078 sorbitan tristearate Nutrition 0.000 claims 1
- 229960004129 sorbitan tristearate Drugs 0.000 claims 1
- UWHCKJMYHZGTIT-UHFFFAOYSA-N tetraethylene glycol Chemical compound OCCOCCOCCOCCO UWHCKJMYHZGTIT-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| MYPI20043578A MY169670A (en) | 2003-09-03 | 2004-09-02 | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| MYPI20043578 | 2004-09-02 | ||
| EPPCT/EP2004/052028 | 2004-09-03 | ||
| PCT/EP2004/052028 WO2005021001A1 (en) | 2003-09-03 | 2004-09-03 | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| EP05101467 | 2005-02-25 | ||
| EP05101467.8 | 2005-02-25 | ||
| PCT/EP2005/054342 WO2006024668A1 (en) | 2004-09-02 | 2005-09-02 | Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl] amino]benzonitrile |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008511592A JP2008511592A (ja) | 2008-04-17 |
| JP2008511592A5 true JP2008511592A5 (https=) | 2011-08-04 |
| JP4912309B2 JP4912309B2 (ja) | 2012-04-11 |
Family
ID=38091637
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007528886A Expired - Lifetime JP4912309B2 (ja) | 2004-09-02 | 2005-09-02 | ４−［［４−［［４−（２−シアノエテニル）−２，６−ジメチルフェニル］アミノ］−２−ピリミジニル］アミノ］ベンゾニトリルの塩酸塩 |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1632232B3 (https=) |
| JP (1) | JP4912309B2 (https=) |
| CN (1) | CN104586850A (https=) |
| AT (1) | ATE508748T1 (https=) |
| BR (1) | BRPI0514871A (https=) |
| CY (3) | CY1112249T1 (https=) |
| DK (1) | DK1632232T6 (https=) |
| EA (1) | EA013686B1 (https=) |
| ES (1) | ES2371442T7 (https=) |
| FR (2) | FR16C1023I2 (https=) |
| HK (1) | HK1210029A1 (https=) |
| HU (2) | HUS1600060I1 (https=) |
| IL (1) | IL181650A (https=) |
| LT (2) | LTPA2016043I1 (https=) |
| ME (1) | ME01246B (https=) |
| MX (1) | MX2007002595A (https=) |
| NI (1) | NI200700068A (https=) |
| NO (3) | NO340654B1 (https=) |
| PT (1) | PT1632232E (https=) |
| RS (1) | RS51923B2 (https=) |
| SI (1) | SI1632232T1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY169670A (en) | 2003-09-03 | 2019-05-08 | Tibotec Pharm Ltd | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| BRPI0707179A2 (pt) * | 2006-01-20 | 2011-04-26 | Tibotec Pharm Ltd | tratamento de longo termo de infecção por hiv |
| CL2008000746A1 (es) | 2007-03-14 | 2008-09-22 | Tibotec Pharm Ltd | Composicion farmaceutica en solucion que comprende tmc278 y un polimero soluble en agua; proceso de preparacion de dicha composicion; y uso de un polvo que comprende tmc278 para tratar sida. |
| SG10201509521WA (en) * | 2010-11-19 | 2015-12-30 | Gilead Sciences Inc | Therapeutic compositions comprising rilpivirine hcl and tenofovir disoproxil fumarate |
| JP5870183B2 (ja) * | 2011-04-15 | 2016-02-24 | エムキュア ファーマシューティカルズ リミテッド | リルピビリン中間体の合成方法 |
| EP2628732A1 (en) * | 2012-02-20 | 2013-08-21 | Sandoz AG | Novel crystalline form of rilpivirine hydrochloride |
| EP2604593A1 (en) | 2011-12-14 | 2013-06-19 | Sandoz AG | Polymorph of Rilpivirine hydrochloride and its use as antiviral |
| WO2013087794A1 (en) | 2011-12-14 | 2013-06-20 | Sandoz Ag | Polymorph of rilpivirine hydrochloride and its use as antiviral |
| WO2013153161A2 (en) * | 2012-04-11 | 2013-10-17 | Sandoz Ag | Novel polymorph of rilpivirine hydrochloride |
| WO2013153162A1 (en) * | 2012-04-11 | 2013-10-17 | Sandoz Ag | Polymorph of rilpivirine hydrochloride |
| CN103570688B (zh) * | 2012-07-19 | 2016-06-08 | 中国科学院上海药物研究所 | 2，5-二氨甲基吡嗪类化合物、其药物组合物、制备方法和用途 |
| GR1008965B (el) * | 2015-12-02 | 2017-02-28 | Φαρματεν Ανωνυμος Βιομηχανικη Και Εμπορικη Εταιρεια Φαρμακευτικων Ιατρικων Και Καλλυντικων Προϊοντων | Φαρμακευτικο σκευασμα που περιλαμβανει δαρουναβιρη και μεθοδος παρασκευης αυτου |
| RU2616267C1 (ru) * | 2016-01-25 | 2017-04-13 | Закрытое Акционерное Общество "БИОКОМ" | Твердая лекарственная форма индинавира немедленного высвобождения и способ ее получения |
| WO2018077815A1 (en) * | 2016-10-24 | 2018-05-03 | Janssen Sciences Ireland Uc | Dispersible compositions |
| JP7287906B2 (ja) * | 2017-06-30 | 2023-06-06 | ヴィーブ ヘルスケア カンパニー | 組み合わせ並びにその使用及びそれによる治療 |
| CN114392241B (zh) * | 2022-01-10 | 2023-07-25 | 安徽贝克生物制药有限公司 | 一种利匹韦林片及其制备方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6307543B1 (en) * | 1998-09-10 | 2001-10-23 | Silicon Image, Inc. | Bi-directional data transfer using two pair of differential lines as a single additional differential pair |
| 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 |
| KR101140785B1 (ko) * | 2002-08-09 | 2012-05-03 | 얀센 파마슈티카 엔.브이. | 4-〔〔4-〔〔4-（2-시아노에테닐）-2,6-디메틸페닐〕아미노〕-2-피리미디닐〕아미노〕벤조니트릴의 제조방법 |
| AU2002350719A1 (en) * | 2002-11-29 | 2004-06-23 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
| BRPI0407329A (pt) * | 2003-02-07 | 2006-01-10 | Janssen Pharmaceutica Nv | Derivados de pirimidina para a prevenção de infecção de hiv |
-
2005
- 2005-09-02 AT AT05108086T patent/ATE508748T1/de active
- 2005-09-02 ES ES05108086T patent/ES2371442T7/es active Active
- 2005-09-02 JP JP2007528886A patent/JP4912309B2/ja not_active Expired - Lifetime
- 2005-09-02 ME MEP-2011-144A patent/ME01246B/me unknown
- 2005-09-02 DK DK05108086.9T patent/DK1632232T6/da active
- 2005-09-02 EA EA200700536A patent/EA013686B1/ru active Protection Beyond IP Right Term
- 2005-09-02 EP EP05108086.9A patent/EP1632232B3/en not_active Expired - Lifetime
- 2005-09-02 MX MX2007002595A patent/MX2007002595A/es active IP Right Grant
- 2005-09-02 PT PT05108086T patent/PT1632232E/pt unknown
- 2005-09-02 RS RS20110355A patent/RS51923B2/sr unknown
- 2005-09-02 BR BRPI0514871-5A patent/BRPI0514871A/pt not_active Application Discontinuation
- 2005-09-02 CN CN201510012919.7A patent/CN104586850A/zh active Pending
- 2005-09-02 SI SI200531339T patent/SI1632232T1/sl unknown
-
2007
- 2007-03-01 IL IL181650A patent/IL181650A/en active IP Right Grant
- 2007-03-01 NI NI200700068A patent/NI200700068A/es unknown
- 2007-04-02 NO NO20071745A patent/NO340654B1/no active Protection Beyond IP Right Term
-
2011
- 2011-08-10 CY CY20111100775T patent/CY1112249T1/el unknown
-
2015
- 2015-11-03 HK HK15110805.7A patent/HK1210029A1/xx unknown
-
2016
- 2016-12-20 FR FR16C1023C patent/FR16C1023I2/fr active Active
- 2016-12-20 CY CY2016050C patent/CY2016050I1/el unknown
- 2016-12-20 HU HUS1600060C patent/HUS1600060I1/hu unknown
- 2016-12-20 LT LTPA2016043C patent/LTPA2016043I1/lt unknown
- 2016-12-20 FR FR16C1025C patent/FR16C1025I2/fr active Active
- 2016-12-20 CY CY2016051C patent/CY2016051I1/el unknown
- 2016-12-20 LT LTPA2016042C patent/LTC1632232I2/lt unknown
- 2016-12-20 HU HUS1600061C patent/HUS1600061I1/hu unknown
-
2017
- 2017-11-21 NO NO2017063C patent/NO2017063I1/no unknown
- 2017-11-21 NO NO2017065C patent/NO2017065I1/no unknown
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