JP2008511592A5 - - Google Patents
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- Publication number
- 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 |
|---|---|---|---|
| MYPI20043578 | 2004-09-02 | ||
| MYPI20043578A MY169670A (en) | 2003-09-03 | 2004-09-02 | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| PCT/EP2004/052028 WO2005021001A1 (en) | 2003-09-03 | 2004-09-03 | Combinations of a pyrimidine containing nnrti with rt inhibitors |
| EPPCT/EP2004/052028 | 2004-09-03 | ||
| EP05101467.8 | 2005-02-25 | ||
| EP05101467 | 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 (23)
| Country | Link |
|---|---|
| EP (1) | EP1632232B3 (https=) |
| JP (1) | JP4912309B2 (https=) |
| KR (1) | KR101284361B1 (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) | HUS1600061I1 (https=) |
| IL (1) | IL181650A (https=) |
| LT (2) | LTC1632232I2 (https=) |
| ME (1) | ME01246B (https=) |
| MX (1) | MX2007002595A (https=) |
| NI (1) | NI200700068A (https=) |
| NO (3) | NO340654B1 (https=) |
| PL (1) | PL1632232T6 (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 |
| PT1981506E (pt) * | 2006-01-20 | 2013-06-25 | Janssen R & D Ireland | Tratamento a longo prazo da infeção pelo vih com tmc278 |
| AR065720A1 (es) | 2007-03-14 | 2009-06-24 | Tibotec Pharm Ltd | Polvos para reconstitucion que comprenden rilpivirina dispersos en ciertos polimeros. uso. proceso. |
| JP2014500261A (ja) * | 2010-11-19 | 2014-01-09 | ギリアード サイエンシーズ， インコーポレイテッド | リルピビリンＨＣｌおよびフマル酸テノホビルジソプロキシルを含有する治療用組成物 |
| KR101879468B1 (ko) * | 2011-04-15 | 2018-07-17 | 엠큐어 파마슈티컬즈 리미티드 | 릴피비린 중간체의 제조를 위한 공정 |
| 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 |
| EP2628732A1 (en) | 2012-02-20 | 2013-08-21 | Sandoz AG | Novel crystalline form of rilpivirine hydrochloride |
| WO2013153162A1 (en) | 2012-04-11 | 2013-10-17 | Sandoz Ag | Polymorph of rilpivirine hydrochloride |
| WO2013153161A2 (en) | 2012-04-11 | 2013-10-17 | Sandoz Ag | Novel 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 |
| US11065198B2 (en) * | 2016-10-24 | 2021-07-20 | Janssen Sciences Ireland Unlimited Company | Dispersible compositions |
| CN110958883A (zh) * | 2017-06-30 | 2020-04-03 | Viiv保健公司 | 组合及其用途和疗法 |
| 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 |
| DK1529032T3 (da) * | 2002-08-09 | 2013-07-08 | Janssen Pharmaceutica Nv | Fremgangsmåder til fremstilling af 4-4-4-(2-cyanoethenyl)-2,6-dimethylphenyl)amino)-2-pyrimidinyl)aminobenzonitrill |
| 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 |
| 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 BR BRPI0514871-5A patent/BRPI0514871A/pt not_active Application Discontinuation
- 2005-09-02 RS RS20110355A patent/RS51923B2/sr unknown
- 2005-09-02 EP EP05108086.9A patent/EP1632232B3/en not_active Expired - Lifetime
- 2005-09-02 JP JP2007528886A patent/JP4912309B2/ja not_active Expired - Lifetime
- 2005-09-02 SI SI200531339T patent/SI1632232T1/sl unknown
- 2005-09-02 ES ES05108086T patent/ES2371442T7/es active Active
- 2005-09-02 DK DK05108086.9T patent/DK1632232T6/da active
- 2005-09-02 PT PT05108086T patent/PT1632232E/pt unknown
- 2005-09-02 AT AT05108086T patent/ATE508748T1/de active
- 2005-09-02 CN CN201510012919.7A patent/CN104586850A/zh active Pending
- 2005-09-02 EA EA200700536A patent/EA013686B1/ru active Protection Beyond IP Right Term
- 2005-09-02 MX MX2007002595A patent/MX2007002595A/es active IP Right Grant
- 2005-09-02 ME MEP-2011-144A patent/ME01246B/me unknown
- 2005-09-02 PL PL05108086T patent/PL1632232T6/pl unknown
- 2005-09-02 KR KR1020077006837A patent/KR101284361B1/ko not_active Expired - Lifetime
-
2007
- 2007-03-01 NI NI200700068A patent/NI200700068A/es unknown
- 2007-03-01 IL IL181650A patent/IL181650A/en active IP Right Grant
- 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 HU HUS1600061C patent/HUS1600061I1/hu unknown
- 2016-12-20 HU HUS1600060C patent/HUS1600060I1/hu unknown
- 2016-12-20 FR FR16C1023C patent/FR16C1023I2/fr active Active
- 2016-12-20 LT LTPA2016042C patent/LTC1632232I2/lt 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 CY CY2016050C patent/CY2016050I1/el unknown
-
2017
- 2017-11-21 NO NO2017065C patent/NO2017065I1/no unknown
- 2017-11-21 NO NO2017063C patent/NO2017063I1/no unknown
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