JP2017505784A5 - - Google Patents
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- JP2017505784A5 JP2017505784A5 JP2016550815A JP2016550815A JP2017505784A5 JP 2017505784 A5 JP2017505784 A5 JP 2017505784A5 JP 2016550815 A JP2016550815 A JP 2016550815A JP 2016550815 A JP2016550815 A JP 2016550815A JP 2017505784 A5 JP2017505784 A5 JP 2017505784A5
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- 150000001875 compounds Chemical class 0.000 claims 19
- 239000000203 mixture Substances 0.000 claims 19
- 208000006673 Asthma Diseases 0.000 claims 9
- 206010046851 Uveitis Diseases 0.000 claims 8
- 206010064930 Age-related macular degeneration Diseases 0.000 claims 6
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 6
- 206010009839 Coeliac disease Diseases 0.000 claims 6
- 208000002780 Macular Degeneration Diseases 0.000 claims 6
- 208000004644 Retinal Vein Occlusion Diseases 0.000 claims 6
- 201000005667 central retinal vein occlusion Diseases 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 206010009900 Colitis ulcerative Diseases 0.000 claims 4
- 206010011401 Crohn's disease Diseases 0.000 claims 4
- 206010013774 Dry eye Diseases 0.000 claims 4
- 206010023332 Keratitis Diseases 0.000 claims 4
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000011780 sodium chloride Substances 0.000 claims 4
- 201000006704 ulcerative colitis Diseases 0.000 claims 4
- 208000002205 Allergic Conjunctivitis Diseases 0.000 claims 3
- 206010003694 Atrophy Diseases 0.000 claims 3
- 206010006451 Bronchitis Diseases 0.000 claims 3
- 206010006458 Bronchitis chronic Diseases 0.000 claims 3
- 208000007451 Chronic Bronchitis Diseases 0.000 claims 3
- 206010010741 Conjunctivitis Diseases 0.000 claims 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 3
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 3
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 3
- 206010014561 Emphysema Diseases 0.000 claims 3
- 206010064212 Eosinophilic oesophagitis Diseases 0.000 claims 3
- 208000010412 Glaucoma Diseases 0.000 claims 3
- 206010021972 Inflammatory bowel disease Diseases 0.000 claims 3
- 208000002551 Irritable Bowel Syndrome Diseases 0.000 claims 3
- 208000001344 Macular Edema Diseases 0.000 claims 3
- 206010025415 Macular oedema Diseases 0.000 claims 3
- 206010039073 Rheumatoid arthritis Diseases 0.000 claims 3
- 206010039083 Rhinitis Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 206010052779 Transplant rejections Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 201000003883 cystic fibrosis Diseases 0.000 claims 3
- 201000011190 diabetic macular edema Diseases 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 201000000708 eosinophilic esophagitis Diseases 0.000 claims 3
- 201000009794 idiopathic pulmonary fibrosis Diseases 0.000 claims 3
- 230000000968 intestinal Effects 0.000 claims 3
- 201000010230 macular retinal edema Diseases 0.000 claims 3
- 201000008482 osteoarthritis Diseases 0.000 claims 3
- 201000000306 sarcoidosis Diseases 0.000 claims 3
- 201000009890 sinusitis Diseases 0.000 claims 3
- 238000001356 surgical procedure Methods 0.000 claims 3
- 238000002054 transplantation Methods 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 2
- 206010036346 Posterior capsule opacification Diseases 0.000 claims 2
- LRFVTYWOQMYALW-UHFFFAOYSA-N Xanthine Natural products O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 239000000969 carrier Substances 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 230000005713 exacerbation Effects 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000011859 microparticle Substances 0.000 claims 2
- ARAIBEBZBOPLMB-UFGQHTETSA-N (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid Chemical compound CC(=O)N[C@@H]1[C@@H](N=C(N)N)C=C(C(O)=O)O[C@H]1[C@H](O)[C@H](O)CO ARAIBEBZBOPLMB-UFGQHTETSA-N 0.000 claims 1
- 229940005497 ANTICHOLINERGIC AGENTS Drugs 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000002177 Cataract Diseases 0.000 claims 1
- 206010012601 Diabetes mellitus Diseases 0.000 claims 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 1
- QNRRHYPPQFELSF-CNYIRLTGSA-N Laninamivir Chemical compound OC[C@@H](O)[C@@H](OC)[C@@H]1OC(C(O)=O)=C[C@H](N=C(N)N)[C@H]1NC(C)=O QNRRHYPPQFELSF-CNYIRLTGSA-N 0.000 claims 1
- 229950004244 Laninamivir Drugs 0.000 claims 1
- 229960003752 Oseltamivir Drugs 0.000 claims 1
- VSZGPKBBMSAYNT-RRFJBIMHSA-N Oseltamivir Chemical compound CCOC(=O)C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1 VSZGPKBBMSAYNT-RRFJBIMHSA-N 0.000 claims 1
- 229960002194 Oseltamivir phosphate Drugs 0.000 claims 1
- XRQDFNLINLXZLB-CKIKVBCHSA-N Peramivir Chemical compound CCC(CC)[C@H](NC(C)=O)[C@@H]1[C@H](O)[C@@H](C(O)=O)C[C@H]1NC(N)=N XRQDFNLINLXZLB-CKIKVBCHSA-N 0.000 claims 1
- 206010047461 Viral infection Diseases 0.000 claims 1
- 208000001756 Virus Disease Diseases 0.000 claims 1
- 229960001028 Zanamivir Drugs 0.000 claims 1
- 125000006242 amine protecting group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000000840 anti-viral Effects 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 230000001684 chronic Effects 0.000 claims 1
- 201000006233 congestive heart failure Diseases 0.000 claims 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N fumaric acid Chemical compound OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims 1
- 200000000018 inflammatory disease Diseases 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound 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 GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 239000011976 maleic acid Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000003149 muscarinic antagonist Substances 0.000 claims 1
- 210000000056 organs Anatomy 0.000 claims 1
- PGZUMBJQJWIWGJ-ONAKXNSWSA-N oseltamivir phosphate Chemical compound OP(O)(O)=O.CCOC(=O)C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1 PGZUMBJQJWIWGJ-ONAKXNSWSA-N 0.000 claims 1
- 229960001084 peramivir Drugs 0.000 claims 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 239000000021 stimulant Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229940065721 systemic for obstructive airway disease Xanthines Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000017613 viral reproduction Effects 0.000 claims 1
- 230000003612 virological Effects 0.000 claims 1
Claims (19)
- 式（Ｉ）の化合物：
- そのマレイン酸の形態にある、請求項１に記載の化合物。
- その形態２の結晶多形の形態にある、請求項２に記載の化合物。
- 場合によっては１種若しくはそれ以上の製薬学的に許容できる希釈剤若しくは担体との組合せの、請求項１若しくは請求項２に記載の式（Ｉ）の化合物を含んでなる製薬学的組成物。
- 微粒子のラクトースとの組合せの、微粒子の形態の請求項１若しくは請求項２に記載の式（Ｉ）の化合物を含んでなる製薬学的組成物。
- 微粒子のステアリン酸マグネシウムをさらに含んでなる、請求項５に記載の製薬学的組成物。
- （Ａ）請求項１若しくは２に記載の化合物；および
（Ｂ）１種若しくはそれ以上の他の治療薬
を含んでなる組合せ製品であって、
ここで成分（Ａ）および（Ｂ）のそれぞれが製薬学的に許容できる補助物質、希釈剤若しくは担体と混合状態で配合されている、上記製品。 - 医薬品としての使用のための、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の組成物、または請求項７に記載の組合せ製品。
- １種若しくはそれ以上の他の有効成分との組合せにおける医薬品としての使用のための請求項１若しくは請求項２に記載の化合物。
- ＣＯＰＤ（慢性気管支炎および肺気腫を包含する）、喘息、小児喘息、嚢胞性線維症、サルコイドーシス、特発性肺線維症、アレルギー性鼻炎、鼻炎、副鼻腔炎、アレルギー性結膜炎、結膜炎、乾性角結膜炎（ドライアイ）、緑内障、糖尿病性網膜症、黄斑浮腫（糖尿病性黄斑浮腫を包含する）、網膜中心静脈閉塞症（ＣＲＶＯ）、萎縮および／若しくは滲出型加齢黄斑変性症（ＡＭＤ）、白内障術後炎症、ブドウ膜炎（後方、前方および全ブドウ膜炎を包含する）、角膜移植および角膜縁細胞移植拒絶、グルテン過敏性腸症（セリアック病）、好酸球性食道炎、腸移植片対宿主病、クローン病、潰瘍性大腸炎、ＩＢＤ、関節リウマチまたは変形性関節症の処置での使用のための、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の組成物、または請求項７に記載の組合せ製品。
- ＣＯＰＤ、喘息、乾性角結膜炎（ドライアイ）、ブドウ膜炎（後方、前方および全ブドウ膜炎を包含する）、クローン病若しくは潰瘍性大腸炎、とりわけＣＯＰＤ若しくは喘息の処置での使用のための、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の組成物、または請求項７に記載の組合せ製品。
- ＣＯＰＤ（慢性気管支炎および肺気腫を包含する）、喘息、小児喘息、嚢胞性線維症、サルコイドーシス、特発性肺線維症、アレルギー性鼻炎、鼻炎、副鼻腔炎、アレルギー性結膜炎、結膜炎、乾性角結膜炎（ドライアイ）、緑内障、糖尿病性網膜症、黄斑浮腫（糖尿病性黄斑浮腫を包含する）、網膜中心静脈閉塞症（ＣＲＶＯ）、萎縮および／若しくは滲出型加齢黄斑変性症（ＡＭＤ）、白内障術後炎症、ブドウ膜炎（後方、前方および全ブドウ膜炎を包含する）、角膜移植および角膜縁細胞移植拒絶、グルテン過敏性腸症（セリアック病）、好酸球性食道炎、腸移植片対宿主病、クローン病、潰瘍性大腸炎、ＩＢＤ、関節リウマチまたは変形性関節症の処置のための医薬品の製造のための、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の組成物、または請求項７に記載の組合せ製品の使用。
- 有効量の請求項、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の製薬学的組成物、または請求項７に記載の組合せ製品を含んでなる、ＣＯＰＤ（慢性気管支炎および肺気腫を包含する）、喘息、小児喘息、嚢胞性線維症、サルコイドーシス、特発性肺線維症、アレルギー性鼻炎、鼻炎、副鼻腔炎、アレルギー性結膜炎、結膜炎、乾性角結膜炎（ドライアイ）、緑内障、糖尿病性網膜症、黄斑浮腫（糖尿病性黄斑浮腫を包含する）、網膜中心静脈閉塞症（ＣＲＶＯ）、萎縮および／若しくは滲出型加齢黄斑変性症（ＡＭＤ）、白内障術後炎症、ブドウ膜炎（後方、前方および全ブドウ膜炎を包含する）、角膜移植および角膜縁細胞移植拒絶、グルテン過敏性腸症（セリアック病）、好酸球性食道炎、腸移植片対宿主病、クローン病、潰瘍性大腸炎、ＩＢＤ、関節リウマチならびに変形性関節症から選択される状態を処置するための製薬学的組成物。
- うっ血性心不全、ＣＯＰＤ、喘息、糖尿病、癌のような１種若しくはそれ以上の慢性状態を伴う患者、および／または免疫抑制された患者例えば臓器移植後における、炎症性疾患の増悪とりわけウイルス性の増悪の処置における若しくはウイルス感染症の処置における使用のための、請求項１若しくは請求項２に記載の化合物、請求項３ないし６のいずれか１つに記載の組成物、または請求項７に記載の組合せ製品。
- ザナミビル、オセルタミビル（例えばオセルタミビルリン酸塩）ペラミビル若しくはラニナミビルのような抗ウイルス療法と組合せの使用のための、請求項１４に記載の化合物、組成物若しくは組合せ製品。
- 式（ＩＩＩ）の化合物
- 式（ＶＩＩ）の化合物
- 式（ＶＩＩＩ）の化合物
である、請求項１６に記載の式（ＩＩＩ）の化合物；
若しくはその塩。 - １種若しくはそれ以上の他の治療薬または有効成分が、ステロイド、β刺激薬、キサンチン、抗コリン薬、ムスカリン拮抗薬、ＰＩ３キナーゼ阻害剤および抗ウイルス薬から成る群から選択される、請求項７に記載の組合せ製品または請求項９に記載の化合物。
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461940282P | 2014-02-14 | 2014-02-14 | |
| US61/940,282 | 2014-02-14 | ||
| US201461941064P | 2014-02-18 | 2014-02-18 | |
| US61/941,064 | 2014-02-18 | ||
| PCT/EP2015/053151 WO2015121444A1 (en) | 2014-02-14 | 2015-02-13 | Aromatic heterocyclic compounds as antiinflammatory compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019220267A Division JP6841891B2 (ja) | 2014-02-14 | 2019-12-05 | 抗炎症化合物としての芳香族複素環化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017505784A JP2017505784A (ja) | 2017-02-23 |
| JP2017505784A5 true JP2017505784A5 (ja) | 2018-03-22 |
| JP6630280B2 JP6630280B2 (ja) | 2020-01-15 |
Family
ID=52573661
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016550815A Active JP6630280B2 (ja) | 2014-02-14 | 2015-02-13 | 抗炎症化合物としての芳香族複素環化合物 |
| JP2016551294A Active JP6586098B2 (ja) | 2014-02-14 | 2015-02-13 | キナーゼ阻害剤としてのピラゾリル尿素 |
| JP2019162164A Active JP6952085B2 (ja) | 2014-02-14 | 2019-09-05 | キナーゼ阻害剤としてのピラゾリル尿素 |
| JP2019220267A Active JP6841891B2 (ja) | 2014-02-14 | 2019-12-05 | 抗炎症化合物としての芳香族複素環化合物 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016551294A Active JP6586098B2 (ja) | 2014-02-14 | 2015-02-13 | キナーゼ阻害剤としてのピラゾリル尿素 |
| JP2019162164A Active JP6952085B2 (ja) | 2014-02-14 | 2019-09-05 | キナーゼ阻害剤としてのピラゾリル尿素 |
| JP2019220267A Active JP6841891B2 (ja) | 2014-02-14 | 2019-12-05 | 抗炎症化合物としての芳香族複素環化合物 |
Country Status (21)
| Country | Link |
|---|---|
| US (8) | US9447076B2 (ja) |
| EP (4) | EP3357919B1 (ja) |
| JP (4) | JP6630280B2 (ja) |
| KR (1) | KR102413704B1 (ja) |
| CN (4) | CN113264921A (ja) |
| AU (3) | AU2015216957B2 (ja) |
| BR (1) | BR112016015838B1 (ja) |
| CA (2) | CA2938924C (ja) |
| DK (2) | DK3357919T3 (ja) |
| EA (1) | EA034927B1 (ja) |
| ES (2) | ES2677595T3 (ja) |
| HK (1) | HK1259444A1 (ja) |
| JO (1) | JO3392B1 (ja) |
| MX (2) | MX371353B (ja) |
| PL (2) | PL3357919T3 (ja) |
| PT (2) | PT3357919T (ja) |
| SG (1) | SG11201607058PA (ja) |
| TR (1) | TR201809072T4 (ja) |
| TW (2) | TWI751099B (ja) |
| UY (1) | UY35998A (ja) |
| WO (2) | WO2015121660A1 (ja) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0821227A2 (pt) | 2007-12-19 | 2015-06-16 | Cancer Rec Tech Ltd | Composto, composição farmacêutica, método para preparar a mesma, uso de um composto, método para tratar uma doença ou distúrbio, para inibir função de raf e para inibir proliferação celular, inibir progressão do ciclo celular, promover apoptose, ou uma combinação de um ou mais dos mesmos |
| AU2011209586B2 (en) | 2010-02-01 | 2016-01-21 | Cancer Research Technology Limited | 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro- 4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo [4,5-b]pyridin-7-yloxy)-phenyl] -urea and related compounds and their use in therapy |
| EP2578582A1 (en) | 2011-10-03 | 2013-04-10 | Respivert Limited | 1-Pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl)ureas as p38 MAP kinase inhibitors |
| ES2583853T3 (es) | 2011-10-03 | 2016-09-22 | Respivert Limited | 1-Pirazolil-3-(4-((2-anilinopirimidin-4-il)oxi)naftalen-1-il)ureas como inhibidores de p38 MAP cinasa |
| GB201214750D0 (en) | 2012-08-17 | 2012-10-03 | Respivert Ltd | Compounds |
| WO2014033449A1 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| EP2890695A2 (en) | 2012-08-29 | 2015-07-08 | Respivert Limited | Kinase inhibitors |
| WO2014033446A1 (en) | 2012-08-29 | 2014-03-06 | Respivert Limited | Kinase inhibitors |
| EP2925742B1 (en) | 2012-11-16 | 2016-10-26 | Respivert Limited | Kinase inhibitors |
| US20160016934A1 (en) | 2013-03-14 | 2016-01-21 | Respivert Limited | Kinase inhibitors |
| US9771353B2 (en) | 2013-04-02 | 2017-09-26 | Topivert Pharma Limited | Kinase inhibitors based upon N-alkyl pyrazoles |
| CN105246884B (zh) | 2013-04-02 | 2018-05-22 | 瑞斯比维特有限公司 | 用作激酶抑制剂的脲衍生物 |
| GB201320732D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Methods of chemical synthesis |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| JP6514703B2 (ja) | 2013-12-20 | 2019-05-15 | トピバート ファーマ リミテッド | キナーゼインヒビターとして有用な尿素誘導体 |
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