JP2016537344A - N−(4−クロロ−2−ヒドロキシ−3−((3s)−3−ピペリジニルスルホニル)フェニル−n’−(3−フルオロ−2−メチルフェニル)尿素の臭化水素酸塩 - Google Patents
N−(4−クロロ−2−ヒドロキシ−3−((3s)−3−ピペリジニルスルホニル)フェニル−n’−(3−フルオロ−2−メチルフェニル)尿素の臭化水素酸塩 Download PDFInfo
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- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
- C07D211/54—Sulfur atoms
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
Description
N-{4-クロロ-2-ヒドロキシ-3-[(3S)-3-ピペリジニルスルホニル]フェニル}-N'-(3-フルオロ-2-メチルフェニル)尿素の臭化水素酸塩の合成
HBr塩の溶解度は、高pHの模擬腸液において遊離塩基よりも高い(以下の表を参照)。模擬腸液中の溶解度は経時的に低下するが、対応する遊離塩基の溶解度よりもはるかに高い。
カプセル中のHBr塩(遊離形態として50mg)の溶解プロフィールを、pH1.6の模擬胃液及びpH4のクエン酸緩衝液中で、遊離塩基と比較した。HBr塩がより良い。メシル酸はゲル状に見え、HBrがメシル酸塩及び遊離塩基の両方よりも優れていると考えられた。図1及び図2を参照されたい。
Claims (16)
- N-{4-クロロ-2-ヒドロキシ-3-[(3S)-3-ピペリジニルスルホニル]フェニル}-N'-(3-フルオロ-2-メチルフェニル)尿素の臭化水素酸塩である化合物。
- 治療に使用するための請求項1に記載の化合物。
- CXCR2拮抗薬が適応される疾患又は病態の治療に使用するための請求項1に記載の化合物。
- 疾患又は病態がCOPDである、請求項3に記載の使用のための化合物。
- 請求項1の化合物、並びに医薬として許容される担体、希釈剤及び賦形剤のうちの1種以上を含む医薬組成物。
- 治療有効量の請求項1に記載の化合物を投与することを含む、対象における、CXCR2拮抗薬が適応される疾患又は病態を治療する方法。
- 疾患又は病態がCOPDである、請求項6に記載の方法。
- CXCR2拮抗薬が適応される疾患又は病態の治療に使用するための薬物の製造における、請求項1に記載の化合物の使用。
- 請求項1に記載の化合物及び少なくとも1種のさらなる治療剤を含む組み合わせ。
- 治療に使用するための請求項6に記載の組み合わせ。
- CXCR2拮抗薬が適応される疾患又は病態の治療に使用するための請求項6に記載の組み合わせ。
- 疾患又は病態がCOPDである、請求項11に記載の使用のための組み合わせ。
- その必要のあるヒトに治療有効量の請求項6に記載の組み合わせを投与することを含む、CXCR2拮抗薬が適応される疾患又は病態を治療する方法。
- 疾患又は病態がCOPDである、請求項13に記載の方法。
- CXCR2拮抗薬が適応される疾患又は病態を治療するための薬物の製造における、請求項1に記載の組み合わせの使用。
- 請求項6に記載の組み合わせ、並びに医薬として許容される担体、希釈剤及び賦形剤のうちの1種以上を含む医薬組成物。
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Application Number | Priority Date | Filing Date | Title |
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GB1320021.7 | 2013-11-13 | ||
GBGB1320021.7A GB201320021D0 (en) | 2013-11-13 | 2013-11-13 | Novel Compounds |
PCT/EP2014/074222 WO2015071235A1 (en) | 2013-11-13 | 2014-11-11 | Hydrobromide salt ofn-(4-chloro-2-hydroxy-3-((3s)-3-piperidinylsulfonyl)phenyl-n'-(3-fluoro-2-methylphenyl)urea |
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JP2016537344A true JP2016537344A (ja) | 2016-12-01 |
JP2016537344A5 JP2016537344A5 (ja) | 2018-02-08 |
JP6401265B2 JP6401265B2 (ja) | 2018-10-10 |
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JP (1) | JP6401265B2 (ja) |
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PT (1) | PT3068763T (ja) |
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KR20170003673A (ko) * | 2014-05-12 | 2017-01-09 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 감염성 질환을 치료하기 위한 다니릭신을 포함하는 약제 조성물 |
AU2016364380B2 (en) * | 2015-11-30 | 2019-06-20 | Glaxosmithkline Intellectual Property (No.2) Limited | Formulations for intravenous injection of danirixin |
WO2018073248A1 (en) | 2016-10-17 | 2018-04-26 | Icm (Institut Du Cerveau Et De La Moelle Épinière) | Prognosis of demyelinating diseases patients and treatment thereof |
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US9809540B2 (en) | 2017-11-07 |
AU2014350334B2 (en) | 2017-08-10 |
CA2929907A1 (en) | 2015-05-21 |
CN105683162A (zh) | 2016-06-15 |
HUE041873T2 (hu) | 2019-05-28 |
ES2714721T3 (es) | 2019-05-29 |
RU2016116955A (ru) | 2017-12-19 |
SI3068763T1 (sl) | 2019-04-30 |
WO2015071235A1 (en) | 2015-05-21 |
CY1121581T1 (el) | 2020-05-29 |
US10604485B2 (en) | 2020-03-31 |
US20160264525A1 (en) | 2016-09-15 |
EP3068763A1 (en) | 2016-09-21 |
ME03328B (me) | 2019-10-20 |
PL3068763T3 (pl) | 2019-05-31 |
PT3068763T (pt) | 2019-03-20 |
GB201320021D0 (en) | 2013-12-25 |
JP6401265B2 (ja) | 2018-10-10 |
RU2685408C1 (ru) | 2019-04-18 |
TR201902981T4 (tr) | 2019-03-21 |
KR20160083950A (ko) | 2016-07-12 |
US20180079722A1 (en) | 2018-03-22 |
BR112016010409A8 (pt) | 2020-04-22 |
RS58382B1 (sr) | 2019-04-30 |
AU2014350334A1 (en) | 2016-06-02 |
DK3068763T3 (en) | 2019-03-18 |
LT3068763T (lt) | 2019-03-12 |
HRP20190449T1 (hr) | 2019-04-19 |
US20190112269A1 (en) | 2019-04-18 |
EP3068763B1 (en) | 2018-12-19 |
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